TREA

Tyrosine Derivatives As Ppar-Gamma-Modulators

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Information

  • Patent Application
  • 20070276043
  • Publication Number
    20070276043
  • Date Filed
    July 29, 2005
    19 years ago
  • Date Published
    November 29, 2007
    17 years ago
Information
Abstract
Compounds of general formula I, and the salts and solvates thereof, wherein R1 represents the radical 2-benzoylphenylamino; R2 represents —(CH2)s—N(COR3)-A-J-T or —(CH2)S—N(R4)—B-J-T; and s, R3, R4, A, B, J and T have the meanings disclosed in the description. These compounds are PPARγ modulators and, therefore, are useful for the treatment or prevention of a condition or a disease mediated by these receptors.
Description

The present invention relates to new tyrosine derivatives acting as PPARγ modulators, as well as to processes and intermediates useful for their preparation, to pharmaceutical compositions containing them and their application in medicine.


BACKGROUND ART

Peroxisome proliferator activated receptors (PPARs) belong to the superfamily of transcription factors known as nuclear receptors. This family includes steroid, retinoid and thyroid hormone receptors. Three sub-types of PPARs have been identified in humans, rodents and Xenopus laevis. They are PPARα, PPARβ/δ and PPARγ, each encoded by a different gene and showing different tissue distribution.


The gene encoding for PPARγ is transcribed in humans in three different mRNA isoforms (PPARγ1, PPARγ2 and PPARγ3) through different splicing and promoter usage (Fajas et al., J. Biol. Chem. 1997, vol. 272, p. 18779-18789). The PPARγ1 isoform shows a wide tissular distribution, while PPARγ2 and PPARγ3 are confined to certain tissues: PPARγ2 is expressed only in adipose tissue and PPARγ3 in adipose tissue as well as in macrophages (Fajas et al., FEBS Lett. 1998, vol. 438, p. 55-60).


Differences detected in tissue distribution as well as in the activation profile of the PPARγ isoforms suggest they are involved in a variety of physiological functions playing a central role in glucose homeostasis and lipid metabolism (Vamecq et al., Lancet 1999, vol. 354, p, 141-148). These functions include, for example, lipidic transport in plasma and catabolism of fatty acids, regulation of insulin sensitivity and blood glucose levels, differentiation of macrophages that form atherosclerotic plaques, inflammatory response, carcinogenesis, hyperplasia, and adipocyte differentiation, the latter being the most verified function of the PPARγ (Grimaldi, Prog. Lipid Res. 2001, vol. 40, p. 269-281; Schiller et al., J. Biol. Chem. 2001, vol. 276, p. 14133-14137). Thus, the discovery of these transcription factors has provided new pharmacological targets for the development of useful therapeutic agents for the prevention and treatment of metabolic diseases such as diabetes, obesity and dyslipidaemia.


Non-insulin dependent diabetes mellitus (NIDDM) or type 2 diabetes is characterized by an insulin resistance in peripheral tissues, including muscle, liver, and adipose tissue. Glitazones, selective PPARγ agonist compounds, are drugs that reduce insulin resistance and lower blood glucose levels. Currently two products belonging to this family, rosiglitazone and pioglitazone, have been approved for the treatment of type 2 diabetes in humans.


A great effort has been made in recent years to design new drugs that improve the side effect profile of the first glitazones, show a greater affinity as a PPARγ ligands, and increase their potency in type 2 diabetes. This rational design has yielded structurally diverse compounds that show great potency and selectivity (e.g. farglitazar).


PPARγ agonists have had shortcomings which have so far detracted from their attractiveness, such as liver toxicity (especially troglitazone), weigh gain, edema, heart weight gain (in rodents) and adiposity, as well as modest efficacy in monotherapy for type 2 diabetes. These facts have provided an incentive to develop improved insulin sensitizers.


Compounds totally or partially blocking PPARγ activity have demonstrated to inhibit adipocyte differentiation. Thus, full antagonists constitute an effective treatment for obesity. Moreover, compounds that are partial agonists in addition of being antagonists may be particularly desirable because they are effective in treating not only obesity but also in controlling hyperglycemia. The PPARγ antagonists/partial agonists are therefore effective in treating obesity and other symptoms that generally occur in non-insulin dependent diabetes, such as elevated plasma levels of glucose, tryglicerides, and insulin.


Recently, there have been reports of compounds that are PPARγ antagonists or partial agonists (WO01/30343, WO02/08188, WO2004/020408), which are useful for the treatment of obesity and type 2 diabetes, with reduced side effects (Berger et al., Trends Pharmacol. Sci. 2005, vol. 26, p. 244-51).


Examples of partial agonists in clinical development for diabetes are (−)-halofenate (metaglidasen), FK 614 (Minoura et al., Eur. J. Pharmacol. 2004, vol. 494, p. 273-8), T131 (Li et al., 64th Annu. Meet Sci. Sess. Am. Diabetes Assoc. (June 4-June 8, Orlando) 2004, Abst 659-P), LY818 (Reifel-Miller et al., Diabetes 2003, 52 (Suppl. 1): Abst 614-P) and telmisartan, an angiotensin II blocker approved for the treatment of hypertension, with PPAR partial agonistic activity at concentrations achievable at plasmatic levels during treatment (Kurtz et al., Acta Diabetol. 2005; vol. 42 Suppl 1: S 9-16) which are currently in phase II of clinical development.


In Henkel et al., J. Med. Chem. 1998, vol. 41, p. 5020-5036; Collins et al., J. Med. Chem. 1998, vol. 41, p. 5037-5054; Cobb et al., J. Med. Chem. 1998, vol. 41, p. 5055-5069, WO 94/29285 and in WO 97/31907 de N-(2-benzoylphenyl)-L-tyrosine derivatives are described as being potent and selective PPARγ agonists. Documents WO 03/011814 and WO 03/011834 disclose N-(2-benzoylphenyl)-L-tyrosine derivatives as partial PPARγ agonists. Document U.S. Pat. No. 6,274,608 describes N-(2-benzoylphenyl)-L-tyrosine derivatives as being useful in the treatment and/or prevention of conditions mediated by Retinoid X Receptor (RXR) and the PPAR families.


Obviously, it is of great interest to provide new therapeutic agents that modulate PPARγ.


SUMMARY OF THE INVENTION

One aspect of the present invention relates to the provision of new compounds of general formula I,


their stereoisomers and mixtures thereof, their polymorphs and mixtures thereof, and the pharmaceutically acceptable solvates and addition salts of all of them, wherein

  • R1 represents the radical 2-benzoylphenylamino;
  • R2 represents —(CH2)s—N(COR3)-A-J-T or —(CH2)s—N(R4)-B-J-T;
  • R3 represents —(C1-C10)alkyl optionally substituted by one or more substituents selected from —F, —Cl, —Br and —O(C1-C4)alkyl; —(C2-C6)alkenyl; —(C2-C6)alkynyl; —(C1-C3)alkylene-Y; —(C2-C3)alkenylene-Y; —(C2-C3)alkynylene-Y or —Y;
  • R4 represents —(C4-C10)alkyl optionally substituted by one or more substituents selected from —F, —Cl, —Br and —O(C1-C4)alkyl; —(C2-C6)alkenyl; —(C2-C6)alkynyl; —(C1-C4)alkylene-Y; —(C2-C4)alkenylene-Y; —(C2-C4)alkynylene-Y or —Y;
  • s represents 2 or 3;
  • A represents —(C1-C4)alkylene-; —(C2-C4)alkenylene-; —(C2-C4)alkynylene-; —(C1-C4)alkylene-Z-, wherein the alkylene part is attached to the N atom and Z is attached to J; or -Z-;
  • B represents —(C4)alkylene-; —(C2-C4)alkenylene-; —(C2-C4)alkynylene-; —(C1-C4)alkylene-Z-, wherein the alkylene part is attached to the N atom and Z is attached to J; or -Z-;
  • J represents a single bond or a biradical selected from the following groups:
    • a) —(CH2)14—, —O—, —S—, —SO—, —SO2—, —CO—, —OCO—, —COO—, —OCONR5-, —NR5COO—, —CONR5-, —NR5CO—, —NR5-, —NR5SO2, —SO2NR5-; and
    • b) —O(C1-C4)alkyl-, —(C1-C4)alkyl-O—, —S(C1-C4)alkyl-, —(C1-C4)alkyl-S—, —SO(C1-C4)alkyl-, —(C1-C4)alkyl-SO—, —SO2(C1-C4)alkyl-, —(C1-C4)alkyl-SO2—, —OCO—C1-C4)alkyl-, —COO—(C1-C4)alkyl-, —(C1-C4)alkyl-OCO—, —(C1-C4)alkyl-COO—, —OCONR5-(C1-C4)alkyl-, —NR5COO—(C1-C4)alkyl-, —(C1-C4)alkyl-OCONR5-, —(C1-C4)alkyl-NR5COO—, —CONR5-(C1-C4)alkyl-, —NR5CO—(C1-C4)alkyl-, —(C1-C4)alkyl-CONR5-, —(C1-C4)alkyl-NR5CO—, —NR5-(C1-C4)alkyl-, —(C1-C4)alkyl-NR5-, —SO2NR5-(C1-C4)alkyl-, —NR5SO2—(C1-C4)alkyl-, —(C1-C4)alkyl-SO2NR5-, —(C1-C4)alkyl-NR5SO2—;
  • T represents —H, —C1-C4)alkyl, —(C2-C4)alkenyl, —(C2-C4)alkynyl or —Y;
  • Y represents a monoradical coming from a cycle selected from a (C3-C6)cycloalkane, cyclohexene, a heterocycle, benzene and a bicycle, wherein all these cycles can be optionally substituted with one or more substituents selected from the group —OH, —CHO, —SH, —NO2, —CN, —F, —Cl, —Br, —CO(C1-C4)alkyl, —COO(C1-C4)alkyl, —OCO(C1-C4)alkyl, —S(C1-C4)alkyl, —SO(C1-C4)alkyl, —SO2(C1-C4)alkyl, —SO2—O(C1-C4)alkyl, —O—SO2(C1-C4)alkyl, —NR5R6, —CONR5R6, —(C1-C4)alkyl optionally substituted by one or more —OH or —F and —O(C1-C4)alkyl optionally substituted by one or more —OH or —F, and wherein the cycles (C3-C6)cycloalkane, cyclohexene and bicycle can also be optionally substituted with one or more substituents oxo (═O);
  • Z represents a biradical coming from a cycle selected from a (C3-C6)cycloalkane, cyclohexene, a heterocycle, benzene and a bicycle, wherein all these cycles can be optionally substituted with one or more substituents selected from the group —OH, —CHO, —SH, —NO2, —CN, —F, —Cl, —Br, —CO(C1-C4)alkyl, —COO(C1-C4)alkyl, —OCO(C1-C4)alkyl, —S(C1-C4)alkyl, —SO(C1-C4)alkyl, —SO2(C1-C4)alkyl, —SO2—O(C1-C4)alkyl, —O—SO2(C1-C4)alkyl, —NR5R6, —CONR5R6, —(C1-C4)alkyl optionally substituted by one or more —OH or —F and —O(C1-C4)alkyl optionally substituted by one or more —OH or —F, and wherein the cycles (C3-C6)cycloalkane, cyclohexene and bicycle can also be optionally substituted with one or more substituents oxo (═O); —


    R5 and R6 independently represent —H or —(C1-C4)alkyl;


    a heterocycle in the above definitions represents a five- or six-membered aromatic ring containing from one to three heteroatoms independently selected from O, S and N, wherein said ring can be attached to the rest of the molecule through a carbon or a nitrogen atom; and


    a bicycle in the above definitions represents a partially unsaturated, saturated or aromatic seven- to ten-membered ring optionally containing from one to three heteroatoms independently selected from O, S and N, wherein said ring or rings can be attached to the rest of the molecule through a carbon or a nitrogen atom.


The compounds of formula I are PPARγ modulators and, therefore, useful as active pharmaceutical substances.


Thus, another aspect of this invention relates to the pharmaceutical compositions which comprise an effective amount of a compound of formula I or a pharmaceutically acceptable salt or solvate thereof and one or more pharmaceutical acceptable excipients.


Another aspect of the present invention relates to the use of a compound of formula I for the manufacture of a medicament for the treatment or prevention of diseases mediated by PPARγ. Another aspect of the present invention relates to the use of a compound of formula I for the manufacture of a medicament for the treatment or prevention of metabolic diseases in a subject in need thereof, including a human. Another aspect of the present invention relates to the use of a compound of formula I or a pharmaceutically acceptable salt or solvate thereof for the manufacture of a medicament for the treatment or prevention of metabolic diseases selected from non-insulin-dependent diabetes mellitus and obesity in a subject in need thereof, including a human. Another aspect of the present invention relates to the use of a compound of formula I or a pharmaceutically acceptable salt or solvate thereof for the manufacture of a medicament for the treatment or prevention of cardiovascular diseases associated with metabolic syndrome, inflammatory diseases, cancer, bone diseases, skin wound healing, cutaneous disorders associated with an anomalous differentiation of epidermic cells, and other disorders where insulin resistance is a component in a subject in need thereof, including a human.


Another aspect of the present invention relates to the method for the treatment or prevention of diseases mediated by PPARγ comprising the administration to a mammal, including a human, an effective amount of a compound of formula I or a pharmaceutically acceptable salt or solvate thereof. Another aspect of the present invention relates to the method for the treatment or prevention of metabolic diseases comprising the administration to a mammal, including a human, an effective amount of a compound of formula I or a pharmaceutically acceptable salt or solvate thereof. Another aspect of the present invention relates to the method for the treatment or prevention of metabolic diseases selected from non-insulin-dependent diabetes mellitus and obesity comprising the administration to a mammal, including a human, an effective amount of a compound of formula I or a pharmaceutically acceptable salt or solvate thereof. Another aspect of the present invention relates to the method for the treatment or prevention of cardiovascular diseases associated with metabolic syndrome, inflammatory diseases, cancer, bone diseases, skin wound healing, cutaneous disorders associated with an anomalous differentiation of epidermic cells and other disorders where insulin resistance is a component, comprising the administration to a mammal, including a human, an effective amount of a compound of formula I or a pharmaceutically acceptable salt or solvate thereof.







In the previous definitions, the terms “alkyl” and “alkylene” mean respectively a monoradical or biradical straight or branched saturated hydrocarbon chain having the indicated number of carbon atoms. Examples of alkyl include, but are not limited to, methyl, ethyl, propyl, isopropyl, butyl, isobutyl, sec-butyl, tert-butyl, pentyl, isopentyl, neopentyl, hexyl, heptyl, octyl, nonyl, decyl and the like.


The terms “alkenyl” and “alkenylene”, as used herein, mean respectively a monoradical or biradical straight or branched unsaturated hydrocarbon chain, having the indicated number of carbon atoms and also containing one or more double bonds. Examples of alkenyl include, but are not limited to, ethenyl, 1-propenyl, 2-propenyl, 1-butenyl, 2-butenyl, 3-butenyl, 1,3-butadienyl, 1-pentenyl, 2-pentenyl, 3-pentenyl, 4-pentenyl, 1-hexenyl, 2-hexenyl, 3-hexenyl, 4-hexenyl, 5-hexenyl and the like.


The terms “alkynyl” and “alkynylene”, as used herein, mean respectively a monoradical or biradical straight or branched unsaturated hydrocarbon chain, having the indicated number of carbon atoms and also containing one or more triple bonds. Examples of alkynyl include, but are not limited to, ethynyl, 1-propynyl, 2-propynyl, 1-butynyl, 2-butynyl, 3-butynyl, 1,3-butadiynyl, 1-pentynyl, 2-pentynyl, 3-pentynyl, 4-pentynyl, 1-hexynyl, 2-hexynyl, 3-hexynyl, 4-hexynyl, 5-hexynyl and the like.


The term heterocycle as used herein refers to a five- or six-membered monocyclic aromatic ring containing from one to three heteroatoms independently selected from O, S and N. As mentioned previously, these heterocycles can be optionally substituted with one or more substituents, which can be placed on any available position of the cycle, and can be attached to the rest of the molecule via any available carbon or nitrogen atoms. Examples include, but are not limited to, 1, 2, 4-oxadiazole, 1, 2, 4-thiadiazole, 1,3,4-oxadiazole, 1,3,4-thiadiazole, furan, imidazole, isoxazole, isothiazole, oxazole, pyrazol, pyrrole, thiazole, thiophene, 1,2,3-triazole, 1,2,4-triazole, pyrazine, pyridazine, pyridine, pyrimidine and the like.


The term (C3-C6)cycloalkane as used herein refers to saturated monocyclic carbocyclic ring having the indicated number of carbon atoms. As mentioned previously, it can be optionally substituted with one or more substituents, which can be placed on any available position of the cycle. Examples of (C3-C6)cycloalkanes include, but are not limited to, cyclopropane, cyclobutane, cyclopentane and cyclohexane.


The term bicycle, as used herein refers to a partially unsaturated, saturated or aromatic seven- to ten-membered ring optionally containing from one to three heteroatoms independently selected from O, S and N, wherein said ring or rings can be attached to the rest of the molecule through a carbon or a nitrogen atom. As mentioned previously, it can be optionally substituted with one or more substituents, which can be placed on any available position of the cycle. Examples of bicyclic groups include, among others, naphthalene, 1,2,3,4-tetrahydronaphthalene, quinoline, 1,2,3,4-tetrahydroquinoline, isoquinoline, benzofuran, 2,3-dihydrobenzofuran, benzothiophene, indole, benzimidazole, benzotriazol, bicyclo[2.2.1]heptane, bicyclo[3.2.1]octane and bicyclo[3.2.2]nonane.


The expression “optionally substituted with one or more” means that a group can be unsubstituted or substituted with one or more, preferably with 1, 2, 3 or 4 substituents, provided that this group has 1, 2, 3 or 4 positions susceptible of being substituted.


Throughout the description and claims the word “comprise” and variations of the word, such as “comprising”, are not intended to exclude other additives, components, elements or steps. The disclosures in the abstract accompanying this application and in the application from which priority is claimed, are incorporated herein as reference.


As used therein the term “treatment” includes treatment, prevention and management of such condition. The term “pharmaceutically acceptable” as used herein refers to those compounds, compositions, and/or dosage forms which are, within the scope of medical judgement, suitable for use in contact with the tissues of humans and animals without excessive toxicity, irritation, allergic response, or other problem or complication, commensurate with a reasonable benefit/risk ratio.


Compounds of formula I of the present invention comprise at least one chiral center. The present invention includes both the racemic compounds and the enantiomeric compounds, i.e. compounds of formula Ia (wherein the configuration of the chiral carbon attached to R1 is (S)) and compounds of formula Ib (wherein the configuration of the chiral carbon attached to R1 is (R)) as shown below.


In a particular embodiment of the invention the configuration of the chiral carbon attached to R1 is (S).


In another embodiment in a compound of formula I or Ia, R2 represents —(CH2)s—N(COR3)-A-J-T. In another embodiment in a compound of formula I or Ia, R2 represents —(CH2)s—N(R4)-B-J-T. In another embodiment in a compound of formula I or Ia, J represents a single bond and T represents —H. In another embodiment in a compound of formula I or Ia, J represents —(CH2)1-4—, —O—, —S—, —SO—, —SO2—, —O(C1-C4)alkyl- or —S(C1-C4)alkyl-. In another embodiment in a compound of formula I or Ia, T represents —H or —(C1-C4)alkyl.


In another embodiment in a compound of formula I or Ia, R2 represents —(CH2)s—N(COR3)-A-J-T; R3 represents —(C1-C10)alkyl optionally substituted by one or more substituents selected from —F, —Cl, —Br and —O(C1-C4)alkyl; —(C2-C6)alkenyl; —(C1-C3)alkylene-Y; —(C2-C3)alkenylene-Y; —(C2-C3)alkynylene-Y or —Y; and Y in R3 represents a monoradical coming from a cycle selected from a (C3-C6)cycloalkane, a heterocycle, benzene and a bicycle, wherein all these cycles can be optionally substituted as defined above.


In another embodiment in a compound of formula I or Ia, R2 represents —(CH2)s—N(COR3)-A-J-T; A represents —(C1-C4)alkylene-; —(C1-C4)alkylene-Z- or -Z-; Z in A represents a biradical coming from a cycle selected from a (C3-C6)cycloalkane, a heterocycle, benzene and a bicycle, wherein all these cycles can be optionally substituted with one or more substituents selected from the group —F, —Cl, —Br, —S(C1-C4)alkyl, —(C1-C4)alkyl optionally substituted by one or more —OH or —F and —O(C1-C4)alkyl optionally substituted by one or more —OH or —F; J represents a single bond; and T represents —H.


In another embodiment in a compound of formula I or Ia, R2 represents —(CH2)s—N(COR3)-A-J-T; A represents —(C1-C4)alkylene-; —(C1-C4)alkylene-Z- or -Z-; Z in A represents an unsubstituted biradical coming from a cycle selected from a (C3-C6)cycloalkane and benzene; J represents a single bond; and T represents —H.


In another embodiment in a compound of formula I or Ia, R2 represents —(CH2)s—N(R4)-B-J-T; R4 represents —(C4-C10)alkyl optionally substituted by one or more substituents selected from —F, —Cl, —Br and —O(C1-C4)alkyl; —(C1-C4)alkylene-Y; or —Y; and Y in R4 represents a monoradical coming from a cycle selected from a (C3-C6)cycloalkane, a heterocycle, benzene and a bicycle, wherein all these cycles can be optionally substituted as defined above.


In another embodiment in a compound of formula I or Ia, R2 represents —(CH2)s—N(R4)-B-J-T, B represents —(C1-C4)alkylene-Z- or -Z-; Z in B represents a biradical coming from a cycle selected from a (C3-C6)cycloalkane, a heterocycle, benzene and a bicycle, wherein all these cycles can be optionally substituted as defined above; J represents a single bond; and T represents —H.


Furthermore, all possible combinations of the above-mentioned embodiments form also part of this invention.


The compounds of the present invention may contain one or more basic nitrogen atoms and, therefore, they may form salts with acids, that also form part of this invention. Examples of pharmaceutically acceptable salts include, among others, addition salts with inorganic acids such as hydrochloric, hydrobromic, hydroiodic, nitric, perchloric, sulphuric and phosphoric acid, as well as addition salts of organic acids such as acetic, methanesulfonic, trifluoromethanesulfonic, ethanesulfonic, benzenesulfonic, p-toluenesulfonic, benzoic, camphorsulfonic, mandelic, oxalic, succinic, fumaric, tartaric, and maleic acid. Likewise, compounds of the present invention may contain one or more acid protons and, therefore, they may form salts with bases, that also form part of this invention. Examples of these salts include salts with metal cations, such as for example an alkaline metal ion, an alkaline-earth metal ion or an aluminium ion; or it may be coordinated with an organic with an organic or inorganic base. An acceptable organic base includes among others diethylamine and triethylamine. An acceptable inorganic base includes aluminium hydroxide, calcium hydroxide, potassium hydroxide, sodium carbonate, and sodium hydroxide. There may be more than one cation or anion depending on the number of functions with charge and on the valency of cations and anions.


Salts derived from pharmaceutically acceptable organic nontoxic bases include salts of primary, secondary, and tertiary amines, substituted amines including naturally occurring substituted amines, cyclic amines, and basic ion exchange resins, such as arginine, betaine, caffeine, choline, N,N dibenzylethylenediamine, diethylamine, 2-diethylaminoethanol, 2-dimethylaminoethanol, ethanolamine, ethylenediamine, N-ethylmorpholine, ethylpiperidine, glucamine, glucosamine, histidine, hydrabamine, isopropylamine, lysine, methylglucamine, morpholine, piperazine, piperidine, polyamine resins, procaine, purines, theobromine, triethylamine, trimethylamine, tripropylamine, tromethamine, and the like.


There is no limitation on the type of salt that can be used provided that these are pharmaceutically acceptable when they are used for therapeutic purposes. Salts can be synthesized from the parent compound which contains a basic or acidic moiety by conventional chemical methods. Generally, such salts can be prepared by reacting the free acid or base forms of these compounds with a stoichiometric amount of the appropriate base or acid in water or in an organic solvent, such as ether, ethyl acetate, ethanol, isopropanol, or acetonitrile or in a mixture of the two. The compounds of formula I and their salts differ in some physical properties but they are equivalent for the purposes of the present invention.


Some of the compounds of formula I of the present invention may exist in unsolvated as well as solvated forms such as, for example, hydrates. The present invention encompasses all such above-mentioned forms which are pharmaceutically active.


Some of the compounds of general formula I may exhibit polymorphism, encompassing the present invention all the possible polymorphic forms, and mixtures thereof. Various polymorphs may be prepared by crystallization under different conditions or by heating or melting the compound followed by gradual or fast cooling. The presence of polymorphs may be determined by solid NMR spectroscopy, IR spectroscopy, differential scanning calorimetry, powder X-ray diffraction or such other techniques.


Compounds of formula I of the present invention comprise at least one chiral center. Additionally, compounds of formula I of the present invention may have further chiral centres. The present invention includes each one of the possible stereoisomers and mixtures thereof, particularly racemic mixtures thereof. A single enantiomer may be prepared by any of the commonly used processes, for example, by chromatographic separation of the racemic mixture on a stationary chiral phase, by resolution of the racemic mixture by fractional crystallisation techniques of the diastereomeric salts thereof, by chiral synthesis, by enzymatic resolution or by biotransformation. This resolution can be carried out on any chiral synthetic intermediate or on products of general Formula I. Alternatively, any enantiomer of a compound of the general Formula I may be obtained by enantiospecific synthesis using optically pure starting materials or reagents of known configuration.


Some of the compounds of the present invention may exist as several diastereoisomers, which may be separated by conventional techniques such as chromatography or fractional crystallization. Some compounds of the present invention may exhibit cis/trans isomers. The present invention includes each of the geometric isomers and its mixtures. The present invention covers all isomers and mixtures thereof (for example racemic mixtures) whether obtained by synthesis and also by physically mixing them.


The present invention relates to a process for the preparation of the above said novel compounds, their derivatives, their analogues, their tautomeric forms, their stereoisomers, their polymorphs or their pharmaceutical acceptable salts and solvates.


The compounds of the present invention may be synthesized using the methods described below, as well as other processes known in the field of organic synthesis. Preferred methods include, but are not limited to, the general processes shown in the attached schemes. Unless otherwise stated the groups R1, R2, R3, R4, R5, R6, s, A, B, J, and T have the meaning described in general formula I.


A compound of formula I may be obtained in general by hydrolysis of a compound of formula II, wherein R7 represents (C1-C4)alkyl. This reaction can be carried out in the presence of a base such as an alkaline hydroxide in a solvent such as tetrahydrofuran, aqueous methanol or a mixture thereof, at a temperature comprised between room temperature and the temperature of the boiling point of the solvent, preferably at room temperature.


A compound of formula II may be obtained as shown in the above scheme by Williamson ether synthesis (see for instance Bal-Tembe et al., Bioorg. Med. Chem. 1997, 5, 1381-1388; Cantello et al., J. Med. Chem. 1994, vol. 37, p. 3977-3985 or EP 875510) or by Mitsunobu conditions (Mitsunobu, Synthesis 1981, 1; Hughes, Org. React. 1992, 42, 335).


In the first case, phenol ester III may be reacted with R2-LG (IVa), wherein LG represents a leaving group, such as for instance a halogen including —Cl, —Br, —I or an alkylsulfonate or arylsulfonate, including mesylate, tosylate or nosylate. This reaction is carried out in the presence of a base, such as NaH, K2CO3 or Cs2CO3, in a solvent such as N,N-dimethylformamide, acetone or ethyl acetate, at a temperature comprised between room temperature and the temperature of the boiling point of the solvent, preferably heating.


In the second case, a compound of formula III may be reacted with an alcohol of formula R2-OH (IVb) using for example, diethyl azodicarboxylate (DEAD) and triphenylphosphine in tetrahydrofuran as a solvent, at a temperature comprised between room temperature and the temperature of the boiling point of the solvent, preferably at room temperature.


Isolated enantiomeric forms of formula Ia and Ib can be obtained either by chiral resolution of a compound of formula I or starting from the corresponding chiral compounds IIIa and IIIb respectively.


A compound of formula II wherein R2 represents —(CH2)s—N(COR3)-A-J-T (i.e. compound of formula IIa) may also be obtained by acylation of a compound of formula Va with a compound of formula R3-COX (VIa), wherein X represents halogen, preferably Cl.


This reaction is carried out in the presence of a base such as triethylamine, in a solvent such as dichloromethane or ethyl acetate, at a temperature comprised between room temperature and the temperature of the boiling point of the solvent.


Some compounds of formula IIa can also be obtained by reacting a compound Va with the corresponding acid of formula VIb (see for instance Elmore, Amino Acids Pep. Proteins 2001, 32, 107-162). This reaction is carried out in the presence of a coupling agent, such as the combination of 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide (EDC) and 1-hydroxybenzotriazol (HOBT) in the presence of a base such as triethylamine, in a solvent such as ethyl acetate or tetrahydrofuran, at a temperature comprised between room temperature and the temperature of the boiling point of the solvent.


Some compounds of formula II wherein R2 represents —(CH2)s—N(R4)-B-J-T (i.e. compounds of formula IIb) may also be obtained by reacting a compound of formula Vb with an alkylating agent of formula R4-LG (VII), wherein LG has the meaning previously described.


This reaction is carried out in the presence of a base, such as K2CO3, in a suitable solvent, such as N,N-dimethylformamide or acetonitrile, at a temperature and the temperature of the boiling point of the solvent, preferably room temperature.


Alternatively compounds of formula II can be obtained by solid synthesis using different types of polimeric solid resins, such as Wang or 2-chlorotrityl resins (Collins et al. J. Med. Chem. 1998, 41, 5037-5054). Compounds of formula III can be prepared following similar procedures to those described in Cobb et al., J. Med. Chem. 1998, 41, 5055-69.


Compounds IVa and IVb wherein R2 represents —(CH2)s—N(R4)-B-J-T (i.e. compounds of formula IVaa and IVba respectively) may be obtained as shown in the following scheme:


Compound VIII is acylated with a compound of formula IX to yield a compound of formula X, wherein R9 represents —CO2(C1-C4)alkyl or —OCO(C1-C4)alkyl, under the same conditions as the reaction of compound Va with VIa to give compound. IIa. Reduction of compound X with a reducing agent such as lithium aluminium hydride in diethyl ether affords compound IVba.


Alternatively, compound VIII can be reacted with an alkylating agent of formula XI to afford compound IVba (Daoud et al., J. Indian Chem. Soc. 1989, 66, 316-318). Compound of formula IVaa is obtained by converting the hydroxyl group of compound IVba into a leaving group. This reaction may be carried out using a sulfonyl halide such as methanesulfonyl chloride in the presence of a base, such as pyridine or triethylamine in a solvent such as dichloromethane or chloroform. Alternatively, compound IVba can be reacted with a halogenating agent such as SOCl2 in a a solvent such as tetrahydrofuran.


Compound VIII can be also converted directly into a compound of formula IVaa by reaction with a compound of formula XII, wherein each LG independently represents a leaving group as defined above, in the same conditions as described for the conversion of VIII into IVba.


A compound of formula V (including compounds of formula Va and Vb) may be obtained using two different synthetic sequences as shown in the following scheme:


Phenol III can be reacted with a protected amine of formula XIVa or XIVb, to yield a compound of formula XIII, wherein R8 represents -A-J-T or —B-J-T, LG represents a leaving group as previously described and PG represents a protecting group, such as for example, trifluoroacetyl or 2-nitrobenzenesulfonyl. The reaction is carried out under the same conditions described for the conversion of a compound of formula III into a compound of formula II. Compound V is subsequently obtained by deprotection of compound XIII. This reaction is carried out under different conditions depending upon the nature of the protecting group (see for instance Harland et al. Synthesis 1984, 941-43, Hirschmann et al. J. Amer. Chem. Soc. 1993, 12550-12568 for the group trifluororacetamide and Lin et al. Tetrahedron Letters 2000, 3309-3313 for the 2-nitrobenzenesulfonylamide group).


Alternatively a compound of formula V can be obtained by reacting phenol III with a secondary amine of formula XVa by Williamson ether synthesis. Compounds of formula VIII are commercially available or can be prepared by methods similar to those described for instance in WO 03/53966 or EP 875510. Compounds XIVa and XIVb can be obtained by reaction of the corresponding unprotected amine of formula XV and a protecting group (see Protective Groups in Organic Synthesis, John Wiley & Sons, 3rd Edition, 1999).


A compound of formula XV can be obtained using the following synthetic scheme:


Compound XVI is acylated to afford compound XVII under the same conditions for the reaction of compound Va and VIa to give compound IIa. Reduction of compound XVII gives compound XVb under the conditions described for the reduction of compound X. Compounds XVb wherein the amino group is less reactive than the hydroxyl group can be converted into compounds XVa under the conditions described for the conversion of IVba into IVaa.


Moreover, a compound of formula XVc can be obtained starting from a compound of formula XVIII.


This conversion can be carried out by reaction with an aldehyde of formula R10-CHO (XIX), wherein R10 represents R8 wherein the group attached to the N is —CH2, in the presence of a reducing agent, such as triacetoxyborohydride or cyanoborohydride in a solvent such as 1,2-dichloroethane. Alternatively, compound XVIII can be reacted with compound XX or a derivative thereof to afford the corresponding amide as previously described. The reduction of the resulting product gives rise a compound of formula XVc. Compounds VIa, VIb, VII, IX, XI, XII, XVI, XVIII, XIX and XX are commercially available or can be easily obtained by conventional methods.


As it will be obvious to a person skilled in the art some of the reactions described above can also be carried out on compounds of formula I.


The compounds of the present invention are ligands of the PPARγ receptor. Therefore, they are expectedly useful for the treatment or prevention of a condition mediated by PPARγ in a subject in need thereof, including a human.


Thus, the present invention relates to the use of these compounds for the preparation of a medicament for the treatment or prevention of metabolic diseases, cardiovascular diseases associated with metabolic syndrome (including vascular restenosis), inflammatory diseases, cancer, bone diseases (particularly osteoporosis), skin wound healing, cutaneous disorders associated with an anomalous differentiation of epidermic cells, particularly the formation of keloids, and other disorders where insulin resistance is a component, including Syndrome X.


As an example, metabolic diseases that can be treated or prevented include non-insulin-dependent diabetes mellitus, obesity, hypercholesterolaemia (including raising HDL levels), dyslipidemia (including hyperlipidemia and hypertriglyceridemia), and other lipid-mediated pathologies.


As an example, inflammatory diseases that can be treated or prevented include rheumatoid arthritis, atherosclerosis, psoriasis, inflammatory bowel disease and pancreatitis.


The compounds described herein may be used to treat these diseases or conditions separately, or may be used to treat them concurrently with the treatment of obesity.


The present invention further provides for pharmaceutical compositions comprising a compound of formula I or a pharmaceutical salt or solvate thereof together with one or more pharmaceutically acceptable excipients, in either single or multiple doses. The examples of the excipients mentioned below are given by way of illustration only and are not to be construed as limiting the scope of the invention.


The compounds of the present invention can be administered in the form of any pharmaceutical formulation. The pharmaceutical formulation will depend upon the nature of the active compound and its route of administration. Any route of administration may be used, for example such as oral, buccal, pulmonary, topical, parenteral (including subcutaneous, intramuscular, and intravenous), transdermal, ocular (ophthalmic), inhalation, intranasal, otic, transmucosal, implant or rectal administration. However oral, topical or parenteral administration are preferred.


Solid compositions for oral administration include among others tablets, granulates and hard gelatin capsules, formulated both as immediate release or modified release formulations.


The manufacturing method may be based on a simple mixture, dry granulation, wet granulation or lyophilization of the active compound with excipients. These excipients may be binding agents, such as syrup, acacia, gelatin, sorbitol, gum tragacanth, corn starch or polyvinylpyrrolidone; fillers such as lactose, sugar, microcrystalline cellulose, maize-starch, calcium phosphate or sorbitol; lubricants such as magnesium stearate, stearic acid, talc, polyethylene glycol or silica; disintegrants such as potato starch, alginic acid or sodium starch glycollate; wetting agents, such as sodium lauryl sulfate, sweetening agents such as sucrose, lactose, dextrose, mannitol, sorbitol or saccharin; bioadhesive agents such as hydroxypropyl cellulose, poly(vinyl alcohol), poly(isobutylene), sodium carboxymethyl cellulose; glidants such as magnesium trisilicate, powdered cellulose, starch, talc or tribasic calcium phosphate; flow enhancers such as colloidal silicon dioxide; release modifiers such as xanthan gum, ethylcellulose, carbomer, hydroxypropyl methyl cellulose or wax or osmotic agents such as potassium bicarbonate or sodium chloride.


The tablets may be coated according to methods well-known in the art such as aqueous dispersion coating, solvent-based coating or drying coating. The active compound can also be incorporated by coating onto inert pellets using film-coating agents, by extrusion and spheronization process, by hot melting pelletization or it can be in the form of a troche or lozenge. When a dosage unit form is a capsule, it may contain, in addition to materials of the above type, a liquid carrier such as a fatty oil or wax.


Powders and granulates for the preparation of oral suspensions by the addition of water can be obtained by mixing the active compound with dispersing or wetting agents; suspending agents, anticaking agents, buffering agents and preservatives. Other excipients may also be added, for example sweetening, flavouring and colouring agents.


Alternatively, the compounds of the present invention may be incorporated into oral liquid preparations such as emulsions, solutions, dispersions, suspensions, syrups, elixirs or in the form of soft gelatin capsules. They may contain commonly-used inert diluents, such as purified water, ethanol, sorbitol, glycerol, polyethylene glycols (macrogols) and propylene glycol. Aid compositions can also contain coadjuvants such as wetting, suspending, sweetening, flavouring agents, preservatives, buffers, chelating agents and antioxidants.


Solutions or suspensions may be prepared in water suitably mixed with a surfactant such as sodium lauryl sulfate. Dispersions may also be prepared in glycerol, liquid polyethylene glycols and mixtures thereof in oils. Under ordinary conditions of storage and use, these preparations contain a preservative to prevent the growth of microorganisms. Moreover, formulations containing these compounds may be presented as a dry product constitution with water or other suitable vehicle before use.


Injectable preparations for parenteral administration comprise sterile solutions, suspensions or emulsions in oily or aqueous vehicles, and may contain coadjuvants, such as suspending, stabilizing, tonicity agents or dispersing agents.


For nasal administration, the preparation may contain a compound of formula I dissolved or suspended in a liquid carrier, in particular an aqueous carrier, for aerosol application. The carrier may contain additives such as solubilizing agents, e.g. propylene glycol, surfactants, absorption enhancers such as lecithin (phosphatidylcholine) or cyclodextrin, or preservatives such as parabenes.


The compound can also be formulated for its topical application. Formulations include creams, lotions, gels, powders, solutions, shampoo preparations, oral paste, mouth wash preparations and patches wherein the compound is dispersed or dissolved in suitable excipients. These excipients may be antimicrobial preservatives such as imidurea, propylparaben, propylene glycol or methylparaben; emulsifying agents such as cetyl alcohol, methylcellulose, poloxamer or medium-chain triglycerids; emulsion stabilizers such as glyceril monostearate, magnesium aluminium silicate, cyclodextrins or wax; humectants such as triacetin, glycerin, propylene glycol or sorbitol; penetrants enhancing agents such as isopropyl miristate; buffering agents such as malic acid, potassium citrate or sodium phosphate dibasic; surfactants such as docusate sodium, sodium lauryl sulfate, polysorbates or sorbitan esters; thickening agents such as hydroxyethyl cellulose, hydroxypropyl cellulose or polyethylene oxide.


The effective dosage of active ingredient may vary depending on the particular compound administered, the route of administration, the nature and severity of the disease to be treated, as well as the age, the general condition and body weight of the patient, among other factors. A representative example of a suitable dosage range is from about 0.001 to about 100 mg/Kg body weight per day, which can be administered as a single or divided doses. However, the dosage administered will be generally left to the discretion of the physician.


PPARγ2 Binding Assay


The cDNA encoding for the open reading frame of the hPPARγ2 was amplified by PCR (polymerase chain reaction) and inserted in the plasmid pGEX-4T-2. This construction (pGEX-hPPARγ) was introduced into E. coli where it was overexpressed and semipurified as a fusion protein with glutathione S-transferase (GST) (Elbrecht et al., J. Biol. Chem. 1999, 274, 7913-7922). The binding of the compounds to the GST-hPPARγ2 s was determined by modifications in the method described by Lehmann et al. (J. Biol. Chem. 1995, 270, 12953-12957). The receptors (2.5 μg) were incubated in 96-well plates in the presence or in the absence of the products with [3H]BRL-49853 (100 nM) for 3 h at 4° C., in a final volume of 200 μL of buffer Tris-HCl 10 mM pH:8.0, containing KCl 50 mM and DTT 10 mM. Non-specific binding was determined in the presence of BRL49853 100 μM. The reaction mixture was transferred to a Multiscreen Durapore (Millipore) microplate containing glutathione-Sepharose 4B in every well. The reaction mixture was left to incubate with the resin during 10 min, and then centrifuged at 735 g during 2 min. To dissociate the receptor bound to the resin, reduced glutathione 10 mM is added and incubated during 10 min. The receptor was eluted by centrifugation. Then, scintillation liquid was added to the elution and the contained radioactivity was quantified by liquid scintillation spectroscopy (Microbeta Wallac, Perkin Elmer).


LBD-hPPARs Transactivation Assay


COS-7 cells were cultivated in 24-well plates and transfected with the pFACMV plasmids that encode the chimeric proteins containing the GAL4 DNA binding domain fused to the PPARγ LBD. The reporter plasmid for the foregoing constructions was pFR-Luc, which contains five repetitions of the GAL4-response element in front of a promoter that controls the transcription of the luciferase gene. Lipofectamine was used as a transfection agent. The plasmids of the chimeric receptors and the reporter gene were inserted in the cells by transitory transfection in COS-7 cells in culture. When the products were added to the culture for 48 h, the luciferase activity showed the effect of the PPAR activity modulation on the transcription of the reporter construction (Wright et al., J. Biol. Chem. 2000, 275, 1873).


Cloning of Human PPARγ2


The human PPAR cDNA was amplified through RT-PCR. For hPPARγ2, RNA was obtained from human white adipose tissue. Each amplified fragment was cloned into pBluescript (Stratagene®) and sequenced. One clone for each construction was selected and used as template for further subcloning and PCR amplifications.


GST-Fused Protein Construction


To generate this chimeric protein, the complete cDNA of the human PPAR was cloned into pGEX4T2 (Amersham Biosciences). The fragment was obtained from the pBluescript-cDNAs clones digested with endonucleases. To assess the plasmid identity and to ensure the in-phase cloning of the proteins, pGEX construction was sequenced. GST-hPPARγ2 fusion protein was generated in Escherichia coli (BL21 strain DE3). Cells were cultured in LB medium to a density of A600=1.6 odu, and induced for overexpression by addition of isopropyl-1-thio-β-D-galactopyranoside (IPTG)-induced cultures to a final concentration of 0.5 mM. The IPTG-induced cultures were grown at room temperature o/n, before cells were harvested by centrifugation at 5000 g for 15 min. After sonication, the GST-fusion protein was purified from the cell pellet using glutathione-Sepharose beads, following the procedure recommended by the manufacturer (Amersham Pharmacia Biotech). Excess of gluthatione was removed o/n by dyalisis at 4° C. Receptor purity was visualized by SDS-PAGE and protein content was determined by Bradford method. Receptor aliquots were stored at −80° C. until use.


In Table 1, affinity and functional activity data of some of the compounds of the present invention are shown.

TABLE 1ExampleAffinityFunctional activityNumberPPARγ(1)PPARγI_121++ANTAGONISTI_128++—I_149+—I_178+++—I_198++PARTIAL AGONISTI_262+++AGONISTI_265+++AGONISTI_280+++—I_303+++—I_375+++PARTIAL AGONISTI_379++—I_391++—I_410+++ANTAGONISTI_412+++—I_418++PARTIAL AGONISTI_438++—I_440++—I_467+++—I_469++—
(1)+++: Ki <500 nM, ++: 500 nM < Ki < 1500 nM, +: Ki >1500 nM


Additional objects, advantages and novel features of the invention will be set forth in part in the description, and in part will become apparent to those skilled in the art upon examination of the description or may be learned by practice of the invention. The present invention will be further illustrated by the following examples. The examples are given by way of illustration only and are not to be construed as limiting the scope of the invention.


The nomenclature of the different compounds used in the present document is based on the software AUTONOM (Automatic Nomenclature) from the Beilstein Institute, which uses the IUPAC systematic nomenclature.


LC-MS spectra have been performed using the following chromatographic equipment: Hewlett-Packard model 1100, equipped with a selective mass detector model 1100 VL, autosampler, ChemStation software and a laser printer (mass spectrometry ionization mode: Atmospheric pressure ionisation with positive ion detection) and using the following chromatographic methods:


Method A: Column Kromasil 100 C18, 40×4.0 mm, 3.5 μm, flow: 0.7 mL/min, eluent: A=0.1% formic acid in water, B=0.1% formic acid in acetonitrile, gradient: 0 min 5% B−8 min 90% B.


Method B: Column: Gemini 5u C18 110, 40×4.0 mm, flow: 0.7 mL/min, eluent: A=0.1% formic acid in water, B=0.1% formic acid in acetonitrile, gradient: 0 min 5% B−8 min 90% B.



1H-NMR spectra of the compounds have been recorded using a VARIAN GEMINI-200 MHz and a VARIAN UNITY-300 MHz equipment and chemical shifts are expressed as ppm (δ) from the internal reference TMS. Mass spectra have been obtained with an Agilent 1100 VL mass spectrometer.


The following abbreviations have been used in the examples:


DEAD: diethyl azodicarboxylate


DMF: N,N-dimethylformamide


EDC: 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide


eq: molar equivalent


EtOAc: ethyl acetate


HOBT: 1-hydroxybenzotriazol


LC-MS: liquid chromatography-mass spectrometry


rt: retention time


THF: tetrahydrofuran


TMS: trimethylsylane


Intermediates IIIa and IIIb:


Compounds of formula IIIa and IIIb can be prepared following similar procedures to those described in Cobb et al., J. Med. Chem. 1998, 41, 5055-69.


IIIa—1: (S)-2-(2-Benzoylphenylamino)-3-(4-hydroxyphenyl)propionic acid methyl ester; rt: 7.357, MS [M+1]+: 376.


IIIb—1: (R)-2-(2-Benzoylphenylamino)-3-(4-hydroxyphenyl)propionic acid methyl ester; rt: 7.357, MS [M+1]+: 376.


Intermediates XIII:


Compounds of formula XIII shown in Table 2 were obtained starting from a phenol III and an amine derivative of formula XIVa or XIVb following one of the procedures A-D described below.


PROCEDURE A: A 0.5 M suspension-of phenol III (1 eq) in EtOAc containing anhydrous potassium carbonate (3 eq) and compound XIVa (1.3 eq) was refluxed for 18 h. Then, the suspension was allowed to cool down and the white solid was filtered. The solvent was distilled off under reduced pressure, and the obtained residue was purified by column chromatography.


PROCEDURE B: A 0.5 M suspension of phenol III (1 eq) in anhydrous DMF containing cesium carbonate (3 eq), compound XIVa (1.3 eq) and potassium iodide (catalythic amount) was heated at 80° C. for 18 h. Then, the suspension was allowed to cool down at room temperature, and treated with water and EtOAc. The organic layer was washed three times with brine, dried over anhydrous sodium sulfate and filtered. The solvent was distilled off under reduced pressure, and the obtained residue was purified by column chromatography.


PROCEDURE C: To a 0.1 M solution of phenol III (1 eq) in anhydrous DMF, containing a catalythic amount of potassium iodide, sodium hydride (60%, 1.1 eq) was added. The resulting suspension was stirred at room temperature for 1 hour and then compound XIVa (1.1 eq) was added. The reaction mixture was stirred at 80° C. for 18 h, and then allowed to cool down to room temperature. After treating with water and EtOAc, the organic layer was washed three times with brine, dried over anhydrous sodium sulfate and filtered. The solvent was distilled off under reduced pressure, and the obtained residue was purified by column chromatography.


PROCEDURE D: To a 0.2 M solution of phenol III (1 eq) in THF, containing compound XIVb (2.2 eq) and triphenylphosphine (2.2 eq), DEAD (2.2 eq) was added under inert atmosphere. The solution was stirred at room temperature for 18 h. Then, the solvent was distilled off under reduced pressure, and the obtained residue was purified by column chromatography.

TABLE 2ExampleStartingHPLCNumberproductCompound name1H-NMR/LC-MSMethodXIII_1IIIa_1(S)-2-(2-Benzoylphenylamino)-3-(4-{2-8.86(d, 1H),A[benzyl-(2,2,2-trifluoroacetyl)amino]-7.62-7.56(ca, 2H),ethoxy}phenyl)propionic acid methyl7.56-7.16(ca,ester12H), 6.79(d, 2H),6.68-6.55(ca,2H), 4.80(s, 2H),4.40(q, 1H),4.10(t, 2H),3.75-3.60(ca, 5H), 3.19(dd,1H), 3.09(dd, 1H)XIII_2IIIa_1(S)-2-(2-Benzoylphenylamino)-3-(4-{3-rt: 9.383A[benzyl-(2,2,2-trifluoroacetyl)amino]-MS[M+1]+: 619propoxy}phenyl)propionic acid methylesterXIII_3IIIa_1(S)-2-(2-Benzoylphenylamino)-3-(4-{2-rt: 9.706A[cyclohexyl-(2,2,2-trifluoroacetyl)-MS[M+1]+: 597amino]ethoxy}phenyl)propionic acidmethyl esterXIII_4IIIa_1(S)-2-(2-Benzoylphenylamino)-3-(4-{2-rt: 9.287A[tert-butyl-(2,2,2-trifluoroacetyl)amino]-MS[M+1]+: 571ethoxy}phenyl)propionic acid methylesterXIII_5IIIa_1(S)-2-(2-Benzoylphenylamino)-3-(4-{2-rt: 8.969A[cyclopropylmethyl(2-MS[M+1]+: 658nitrobenzenesulfonyl)amino]ethoxy}-phenyl)propionic acid methyl esterXIII_6IIIa_1(S)-2-(2-Benzoylphenylamino)-3-(4-{3-rt: 9.103A[cyclopropylmethyl(2-MS[M+1]+: 672nitrobenzenesulfonyl)amino]propoxy}-phenyl)propionic acid methyl esterXIII_7IIIa_1(S)-2-(2-Benzoylphenylamino)-3-(4-{2-rt: 9.323A[(3-methylbenzyl)(2-MS[M+1]+: —nitrobenzenesulfonyl)amino]ethoxy}-phenyl)propionic acid methyl esterXIII_8IIIa_1(S)-2-(2-Benzoylphenylamino)-3-(4-{3-rt: 9.449A[(3-methylbenzyl)(2-MS[M+1]+: —nitrobenzenesulfonyl)amino]propoxy}-phenyl)propionic acid methyl esterXIII_9IIIa_1(S)-2-(2-Benzoylphenylamino)-3-(4-{2-rt: 8.948A[(2-nitrobenzenesulfonyl)propylamino]-MS[M+1]+: 646ethoxy}phenyl)propionic acid methylesterXIII_10IIIa_1(S)-2-(2-Benzoylphenylamino)-3-(4-{2-rt: 8.726A[ethyl-(2-nitrobenzenesulfonyl)amino]-MS[M+1]+: 632ethoxy}phenyl)propionic acid methylester


Intermediates V:


Compounds of formula V shown in Table 3 were obtained starting from phenol III and an amine derivative of formula XVa following one of the procedures A-C described above or alternatively starting from compound XIII using procedures E-F described below.


PROCEDURE E: To a 0.1 M solution of compound XIII (1 eq) (PG=trifluoroacetyl) in a mixture of THF:methanol (3:1), a 1 M aqueous solution of lithium hydroxide (5 eq) was added. The solution was stirred for 18 h at room temperature, then diluted with a mixture of water/EtOAc, and then acidified to pH=5 with HCl 1 N. The organic layer was dried over anhydrous sodium sulfate and filtered. The solvent was distilled off under reduced pressure, and the obtained residue was redissolved in methanol to afford a 0.1 M solution, which was treated with thionyl chloride (3.2 eq). The solution was refluxed for 18 h, and then allowed to cool down to room temperature. The solvent was distilled off under reduced pressure. The obtained residue was purified by column chromatography.


PROCEDURE F: To a 0.1 M solution of compound XIII (PG=2-nitrobenzenesulfonyl, 1 eq) in DMF containing thiophenol (1 eq), KOtBu (2 eq) was added. The solution was stirred at room temperature for 6 h and then diluted with a mixture of water/EtOAc. The organic layer was washed three times with brine, dried over anhydrous sodium sulfate and filtered. The solvent was distilled off under reduced pressure, and the obtained residue was purified by column chromatography.

TABLE 3ExampleStartingHPLCNumberproductCompound name1H-NMR/LC-MSMethodV_1XIII_1(S)-2-(2-Benzoylphenylamino)-3-[4-8.86(d, 1H),A(2-benzylaminoethoxy)phenyl]-7.62-7.56(ca, 2H),propionic acid methyl ester7.56-7.40(ca, 6H),7.40-7.27(ca, 4H), 7.14(d, 2H),6.83(d, 2H),6.65-6.53(ca, 2H), 4.63(q, 1H),4.13(t, 2H), 3.99(s,2H), 3.68(s, 3H),3.19(dd, 1H), 3.09(dd,1H), 3.03(t, 2H)V_2XIII_2(S)-2-(2-Benzoylphenylamino)-3-[4-rt: 6.385A(3-benzylaminopropoxy)phenyl]-MS[M+1]+: 523propionic acid methyl esterV_3XIII_3(S)-2-(2-Benzoylphenylamino)-3-[4-rt: 6.495A(2-cyclohexylaminoethoxy)phenyl]-MS[M+1]+: 501propionic acid methyl esterV_4XIII_4(S)-2-(2-Benzoylphenylamino)-3-[4-rt: 6.209A(2-tert-butylaminoethoxy)phenyl]-MS[M+1]+: 475propionic acid methyl esterV_5XIII_5(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 5.882A[2-cyclopropylmethylamino)ethoxy]-MS[M+1]+: 473phenyl}propionic acid methyl esterV_6XIII_6(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 6.354A[3-(cyclopropylmethylamino)-MS[M+1]+: 487propoxy]phenyl}propionic acidmethyl esterV_7XIII_7(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 6.591A[2-(3-methylbenzylamino)ethoxy]-MS[M+1]+: 523phenyl}propionic acid methyl esterV_8XIII_8(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 6.758A[3-(3-methylbenzylamino)propoxy]-MS[M+1]+: 537phenyl}propionic acid methyl esterV_9IIIa_1(S)-2-(2-Benzoylphenylamino)-3-[4-rt: 8.96A(2-phenylaminoethoxy)phenyl]-MS[M+1]+: 495propionic acid methyl esterV_10IIIa_1(S)-2-(2-Benzoylphenylamino)-3-[4-rt: 8.993A(3-phenylaminopropoxy)phenyl]-MS[M+1]+: 509propionic acid methyl esterV_11IIIa_1(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.131A[2-(2-fluorophenylamino)ethoxy]-MS[M+1]+: 513phenyl}propionic acid methyl esterV_12IIIa_1(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.013A[2-(3-fluorophenylamino)ethoxy]-MS[M+1]+: 513phenyl}propionic acid methyl esterV_13IIIa_1(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 8.876A[2-(4-fluorophenylamino)ethoxy]-MS[M+1]+: 513phenyl}propionic acid methyl esterV_14IIIa_1(S)-2-(2-Benzoylphenylamino)-3-[4-rt: 9.247A(2-o-tolylaminoethoxy)phenyl]-MS[M+1]+: 509propionic acid methyl esterV_15IIIa_1(S)-2-(2-Benzoylphenylamino)-3-[4-rt: 9.127A(2-m-tolylaminoethoxy)phenyl]-MS[M+1]+: 509propionic acid methyl esterV_16IIIa_1(S)-2-(2-Benzoylphenylamino)-3-[4-rt: 9.014A(2-p-tolylaminoethoxy)phenyl]-MS[M+1]+: 509propionic acid methyl esterV_17IIIa_1(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.431A[2-(2-chlorophenylamino)ethoxy]-MS[M, M+2]+: 530,phenyl}propionic acid methyl ester532V_18IIIa_1(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.293A[2-(3-chlorophenylamino)ethoxy]-MS[M, M+2]+: 530,phenyl}propionic acid methyl ester532V_19IIIa_1(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.265A[2-(4-chlorophenylamino)ethoxy]-MS[M, M+2]+: 530,phenyl}propionic acid methyl ester532V_20IIIa_1(S)-2-(2-Benzoylphenylamino)-3-[4-rt: 9.377A(3-o-tolylaminopropoxy)phenyl]-MS[M+1]+: 523propionic acid methyl esterV_21IIIa_1(S)-2-(2-Benzoylphenylamino)-3-[4-rt: 9.11A(3-m-tolylaminopropoxy)phenyl]-MS[M+1]+: 523propionic acid methyl esterV_22IIIa_1(S)-2-(2-Benzoylphenylamino)-3-[4-rt: 8.714A(3-p-tolylaminopropoxy)phenyl]-MS[M+1]+: 523propionic acid methyl esterV_23IIIa_1(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.632A[3-(2-chlorophenylamino)propoxy]-MS[M, M+2]+: 543,phenyl}propionic acid methyl ester545V_24IIIa_1(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.474A[3-(3-chlorophenylamino)propoxy]-MS[M, M+2]+: 543,phenyl}propionic acid methyl ester545V_25IIIa_1(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.435A[3-(4-chlorophenylamino)propoxy]-MS[M, M+2]+: 543,phenyl}propionic acid methyl ester545V_26IIIa_1(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 10.202A[2-(naphthalen-1-ylamino)ethoxy]-MS[M+1]+: 545phenyl}propionic acid methyl esterV_27IIIa_1(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.189A[2-(3-methylsulfanylphenylamino)-MS[M+1]+: 541ethoxy]phenyl}propionic acid methylesterV_28IIIa_1(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.178A[2-(4-methylsulfanylphenylamino)-MS[M+1]+: 541ethoxy]phenyl}propionic acid methylesterV_29IIIb_1(R)-2-(2-Benzoylphenylamino)-3-[4-rt: 8.968A(2-phenylaminoethoxy)phenyl]-MS[M+1]+: 495propionic acid methyl esterV_30IIIa_1(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.417A[2-(naphthalen-2-ylamino)ethoxy]-MS[M+1]+: 545phenyl}propionic acid methyl esterV_31IIIa_1(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.369A[3-(2-fluorophenylamino)propoxy]-MS[M+1]+: 527phenyl}propionic acid methyl esterV_32IIIa_1(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.233A[3-(3-fluorophenylamino)propoxy]-MS[M+1]+: 527phenyl}propionic acid methyl esterV_33IIIa_1(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 8.992A[3-(4-fluorophenylamino)propoxy]-MS[M+1]+: 527phenyl}propionic acid methyl esterV_34IIIa_1(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.085A[2-(2-methoxyphenylamino)ethoxy]-MS[M+1]+: 525phenyl}propionic acid methyl esterV_35IIIa_1(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 8.850A[2-(3-methoxyphenylamino)ethoxy]-MS[M+1]+: 525phenyl}propionic acid methyl esterV_36XIII_10(S)-2-(2-Benzoylphenylamino)-3-[4-rt: 5.889A(2-ethylaminoethoxy)phenyl]-MS[M+1]+: 447propionic acid methyl esterV_37IIIa_1(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.097A[3-(2-methoxyphenylamino)propoxy]-MS[M+1]+: 539phenyl}propionic acid methyl esterV_38IIIa_1(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 8.923A[3-(3-methoxyphenylamino)propoxy]-MS[M+1]+: 539phenyl}propionic acid methyl esterV_39XIII_9(S)-2-(2-Benzoylphenylamino)-3-[4-rt: 6.063A(2-propylaminoethoxy)phenyl]-MS[M+1]+: 461propionic acid methyl ester


Intermediates II:


Compounds of formula II shown in Table 4 were obtained starting from phenol III and a compound of formula IVa or IVb following one of the procedures A-D described above.

TABLE 4ExampleStartingHPLCNumberproductCompound name1H-NMR/LC-MSMethodII_1IIIa_1(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 10.561A[2-(benzylindan-5-ylamino)ethoxy]-MS[M+1]+: 625phenyl}propionic acid methyl esterII_2IIIa_1(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 10.023A{2-[benzyl(2,6-difluorophenyl)amino]-MS[M+1]+: 621ethoxy}phenyl)propionic acid methylesterII_3IIIa_1(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 10.22A{2-[(2-chlorophenyl)-(2-fluorobenzyl)-MS[M+1]+: 638amino]ethoxy}phenyl)propionic acidmethyl esterII_4IIIa_1(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.977A{2-[benzyl-(2-fluorophenyl)amino]-MS[M+1]+: 603ethoxy}phenyl)propionic acid methylesterII_5IIIa_1(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 10.123A{2-[(2-methylbenzyl)phenylamino]-MS[M+1]+: 599ethoxy}phenyl)propionic acid methylesterII_6IIIa_1(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 10.204A{2-[(3-chlorophenyl)-(2-MS[M+1]+: 650methoxybenzyl)amino]ethoxy}-phenyl)propionic acid methyl esterII_7IIIa_1(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 10.134A{2-[(2-methoxybenzyl)-m-tolylamino]-MS[M+1]+: 629ethoxy}phenyl)propionic acid methylesterII_8IIIa_1(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 10.014A{3-[(2-methoxybenzyl)phenylamino]-MS[M+1]+: 629propoxy}phenyl)propionic acidmethyl esterII_9IIIa_1(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 10.25A[2-(benzyl-o-tolylamino)ethoxy]-MS[M+1]+: 599phenyl}propionic acid methyl esterII_10IIIa_1(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 10.356A{2-[benzyl-(3-ethylphenyl)amino]-MS[M+1]+: 613ethoxy}phenyl)propionic acid methylesterII_11IIIa_1(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.864A{2-[benzyl-(3-fluorophenyl)amino]-MS[M+1]+: 603ethoxy}phenyl)propionic acid methylesterII_12IIIa_1(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 10.119A{2-[(2-chlorophenyl)-(3-MS[M+1]+: 650methoxybenzyl)amino]ethoxy}-phenyl)propionic acid methyl esterII_13IIIa_1(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 10.012A{2-[(3-chlorophenyl)-(3-MS[M+1]+: 650methoxybenzyl)amino]ethoxy}-phenyl)propionic acid methyl esterII_14IIIa_1(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 10.004A{2-[(3-methoxybenzyl)-m-tolylamino]-MS[M+1]+: 629ethoxy}phenyl)propionic acid methylesterII_15IIIa_1(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.931A{3-[(3-methoxybenzyl)phenylamino]-MS[M+1]+: 629propoxy}phenyl)propionic acidmethyl esterII_16IIIa_1(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 10.127A[2-(benzyl-m-tolylamino)ethoxy]-MS[M+1]+: 599phenyl}propionic acid methyl esterII_17IIIa_1(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 10.164A{2-[benzyl-(4-chlorophenyl)amino]-MS[M+1]+: 619ethoxy}phenyl)propionic acid methylesterII_18IIIa_1(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.863A{2-[benzyl-(4-fluorophenyl)amino]-MS[M+1]+: 603ethoxy}phenyl)propionic acid methylesterII_19IIIa_1(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 10.172A{2-[(4-methylbenzyl)phenylamino]-MS[M+1]+: 599ethoxy}phenyl)propionic acid methylesterII_20IIIa_1(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.879A{3-[(4-methoxybenzyl)phenylamino]-MS[M+1]+: 629propoxy}phenyl)propionic acidmethyl esterII_21IIIa_1(S)-2-(Benzoylphenylamino)-3-{4-[2-rt: 10.592A(di-p-tolylamino)ethoxy]phenyl}-MS[M+1]+: 599propionic acid methyl esterII_22IIIa_1(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 10.174A[2-(benzyl-p-tolylamino)ethoxy]-MS[M+1]+: 599phenyl}propionic acid methyl esterII_23IIIa_1(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 10.601A[3-(benzylindan-5-ylamino)propoxy]-MS[M+1]+: 639phenyl}propionic acid methyl esterII_24IIIa_1(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 10.507A{3-[benzyl-(3-ethylphenyl)amino]-MS[M+1]+: 627propoxy}phenyl)propionic acidmethyl esterII_25IIIa_1(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 10.261A[3-(benzyl-m-tolylamino)propoxy]-MS[M+1]+: 613phenyl}propionic acid methyl esterII_26IIIa_1(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 10.27A[3-(benzyl-p-tolylamino)propoxy]-MS[M+1]+: 613phenyl}propionic acid methyl esterII_27IIIa_1(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 7.251A[3-(benzylcyclohexylamino)propoxy]-MS[M+1]+: 605phenyl}propionic acid methyl esterII_28IIIa_1(S)-2-(2-Benzoylphenylamino)-3-{4-8.92(d, 1H), 7.60(d,A[3-(benzylphenylamino)propoxy]-2H), 7.60-7.15(ca,phenyl}propionic acid methyl ester17H), 6.85-6.55(ca,4H), 4.55(s, 2H),4.39(q, 1H), 3.97(t, 2H),3.69(s, 3H), 3.62(t,2H), 3.22(dd, 1H),3.13(dd, 1H),2.20-2.00(ca, 2H)II_29IIIa_1(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 10.281A{2-[(2-fluorophenyl)isobutylamino]-MS[M+1]+: 569ethoxy}phenyl)propionic acid methylesterII_30IIIa_1(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 10.614A[2-(isobutyl-o-tolylamino)ethoxy]-MS[M+1]+: 565phenyl}propionic acid methyl esterII_31IIIa_1(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 10.455A[3-(isobutyl-o-tolylamino)propoxy]-MS[M+1]+: 579phenyl}propionic acid methyl esterII_32IIIa_1(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 10.109A{2-[(3-fluorophenyl)isobutylamino]-MS[M+1]+: 569ethoxy}phenyl)propionic acid methylesterII_33IIIa_1(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 10.397A{2-[isobutyl-m-tolylamino]ethoxy}-MS[M+1]+: 565phenyl)propionic acid methyl esterII_34IIIa_1(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 10.412A[3-(isobutyl-m-tolylamino)propoxy]-MS[M+1]+: 579phenyl}propionic acid methyl esterII_35IIIa_1(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 7.539A[2-(benzylphenethylamino)ethoxy]-MS[M+1]+: 613phenyl}propionic acid methyl esterII_36IIIa_1(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 10.223A[2-(cyclobutylmethyl-o-tolylamino)-MS[M+1]+: 577ethoxy]phenyl}propionic acid methylesterII_37IIIa_1(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 7.03A[2-(benzylcyclopentylamino)ethoxy]-MS[M+1]+: 577phenyl}propionic acid methyl esterII_38IIIa_1(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 7.811A[3-(cyclopentylphenylamino)-MS[M+1]+: 577propoxy]phenyl}propionic acidmethyl esterII_39IIIa_1(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 10.786A{2-[cyclopentylmethyl-(2-MS[M+1]+: 595fluorophenyl)amino]ethoxy}phenyl)-propionic acid methyl esterII_40IIIa_1(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 10.602A[2-(cyclopentymethylphenylamino)-MS[M+1]+: 577ethoxy]phenyl}propionic acid methylesterII_41IIIa_1(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 6.954A[2-(benzylcyclopropylmethylamino)-MS[M+1]+: 563ethoxyl]phenyl}propionic acid methylesterII_42IIIa_1(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 7.052A[3-(benzylcyclopropylmethylamino)-MS[M+1]+: 577propoxy]phenyl}propionic acidmethyl esterII_43IIIa_1(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.936A{2-[(2-methoxybenzyl)phenylamino]-MS[M+1]+: 615ethoxy}phenyl)propionic acid methylesterII_44IIIa_1(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.8A{2-[(3-methoxybenzyl)phenylamino]-MS[M+1]+: 615ethoxy}phenyl)propionic acid methylesterII_45IIIa_1(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.831A{2-[(3-methoxyphenyl)phenylamino]-MS[M+1]+: 601ethoxy}phenyl)propionic acid methylesterII_46IIIa_1(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.788A{2-[(4-methoxybenzyl)phenylamino]-MS[M+1]+: 615ethoxy}phenyl)propionic acid methylesterII_47IIIa_1(S)-2-(2-Benzoylphenylamino)-3-(4-rt: —A{2-[(4-tert-butylbenzyl)phenylamino]-MS[M+1]+: 641ethoxy}phenyl)propionic acid methylesterII_48IIIa_1(S)-2-(2-Benzoylphenylamino)-3-{4-8.89(d, 1H), 7.59(d,A[2-(benzylphenylamino)ethoxy]-2H), 7.55-7.40(ca,phenyl}propionic acid methyl ester4H), 7.40-7.15(ca,11H), 6.85-6.55(ca,8H), 4.67(s, 2H),4.42(m, 1H), 4.18(t, 2H),3.85(t, 2H), 3.71(s,3H), 3.30-3.10(ca,2H)II_49IIIa_1(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 10.206A[2-(cyclobutylmethylphenylamino)-MS[M+1]+: 563ethoxy]phenyl}propionic acid methylesterII_50IIIa_1(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 10.01A[2-(cyclohexylphenylamino)ethoxy]-MS[M+1]+: 577phenyl}propionic acid methyl esterII_51IIIa_1(S)-2-(2-Benzoylphenylamino)-3-{4-rt: —A[2-(cyclohexylmethylphenylamino)-MS[M+1]+: 589ethoxy]phenyl}propionic acid methylesterII_52IIIa_1(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 8.769A[2-(cyclopentylphenylamino)ethoxy]-MS[M+1]+: 563phenyl}propionic acid methyl esterII_53IIIa_1(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.696A[2-(cyclopropylmethylphenylamino)-MS[M+1]+: 549ethoxy]phenyl}propionic acid methylesterII_54IIIa_1(S)-2-(2-Benzoylphenylamino)-3-{4-8.98(d, 1H),A[2-(diphenylamino)ethoxy]phenyl}-7.70-7.60(ca, 2H),propionic acid methyl ester7.60-7.45(ca, 3H),7.45-7.15(ca, 8H),7.15-6.95(ca, 6H), 6.85(d,2H), 6.75-6.60(ca,2H), 4.44(q, 1H),4.17(s, 4H), 3.72(s, 3H),3.30-3.10(ca, 2H).II_55IIIa_1(S)-2-(2-Benzoylphenylamino)-3-(4-rt: —A{2-[cyclohexylmethyl-(2-MS[M+1]+: —fluorophenyl)amino]ethoxy}phenyl)-propionic acid methyl esterII_56IIIa_1(S)-2-(2-Benzoylphenylamino)-3-(4-rt: —A{2-[(3-chlorophenyl)-MS[M+1]+: —cyclopentylmethylamino]ethoxy}-phenyl)propionic acid methyl esterII_57IIIa_1(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 10.527A{3-[cyclobutylmethyl-(3-MS[M+1]+: 595fluorophenyl)amino]propoxy}phenyl)-propionic acid methyl esterII_58IIIa_1(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.994A[3-(cyclobutylmethyl-m-tolylamino)-MS[M+1]+: 591propoxy]phenyl}propionic acidmethyl esterII_59IIIb_1(R)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.945A[2-(benzylphenylamino)ethoxy]-MS[M+1]+: 585phenyl}propionic acid methyl esterII_60IIIa_1(S)-2-(2-Benzoylphenylamino)-3-(4-rt: —A{2-[(2-chlorophenyl)-MS[M+1]+: —cyclopentylmethylamino]ethoxy}-phenyl)propionic acid methyl esterII_61IIIa_1(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.831A{2-[(2-fluorophenyl)thiophen-2-MS[M+1]+: 609ylmethylamino]ethoxy}phenyl)-propionic acid methyl esterII_62IIIa_1(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 10.561A{3-[(2-fluorophenyl)isobutylamino]-MS[M+1]+: 583propoxy}phenyl)propionic acidmethyl esterII_63IIIa_1(S)-2-(2-Benzoylphenylamino)-3-(4-rt: —A{3-[cyclopentylmethyl-(2-MS[M+1]+: —fluorophenyl)amino]propoxy}phenyl)-propionic acid methyl esterII_64IIIa_1(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.655A[3-(cyclobutylmethyl-o-tolylamino)-MS[M+1]+: 591propoxy]phenyl}propionic acidmethyl esterII_65IIIa_1(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.752A{2-[(3-fluorophenyl)thiophen-2-MS[M+1]+: 609ylmethylamino]ethoxy}phenyl)-propionic acid methyl esterII_66IIIa_1(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.996A[2-(thiophen-2-ylmethyl-m-MS[M+1]+: 605tolylamino)ethoxy]phenyl}propionicacid methyl esterII_67IIIa_1(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 10.131A[3-(thiophen-3-ylmethyl-m-MS[M+1]+: 316tolylamino)propoxy]phenyl}propionicacid methyl esterII_68IIIa_1(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.929A[3-(furan-2-ylmethyl-m-tolylamino)-MS[M+1]+: 603propoxy]phenyl}propionic acidmethyl esterII_69IIIa_I(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.744A{2-[(4-fluorophenyl)thiophen-2-MS[M+1]+: 609ylmethylamino]ethoxy}phenyl)-propionic acid methyl esterII_70IIIa_1(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.795A[2-(phenylthiophen-2-MS[M+1]+: 591ylmethylamino)ethoxy]phenyl}-propionic acid methyl esterII_71IIIa_1(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.933A[3-(phenylthiophen-2-MS[M+1]+: 605ylmethylamino)propoxy]phenyl}-propionic acid methyl ester


Intermediates IIa:


Compounds of formula IIa shown in Table 5 were obtained starting from a compound Va and a compund of formula VIa or VIb, following one of the procedures G-H described below.


PROCEDURE G: To a 0.2 M solution of compound Va (1 eq) in dichloromethane or EtOAc, triethylamine (3 eq) and a solution of an acyl chloride VIa (1.2 eq) were added. After stirring for 18 h, the crude was treated with 5% NaHCO3. The organic layer was washed twice with 5% NaHCO3 and once with brine. The organic layer was dried over anhydrous sodium sulfate and filtered. The solvent was distilled off under reduced pressure. The obtained residue was purified by column chromatography.


PROCEDURE H: To a 0.3 M suspension of compound Va (1 eq) in EtOAc containing HOBT (1.5 eq) and EDC (1.5 eq), triethylamine (3 eq) was added. Then, carboxylic acid VIb (1 eq) was added and stirred for 18 h. The reaction mixture was treated with water, the organic layer was separated and the aqueous layer was extracted once with EtOAc. The combined organic layers were washed once with 5% NaHCO3 and once with brine, dried over anhydrous sodium sulfate, and filtered. The solvent was distilled off under reduced pressure, and the obtained residue was purified by column chromatography.

TABLE 5ExampleStartingHPLCNumberproductCompound name1H-NMR/LC-MSMethodIIa_1V_17(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.069A{2-[(2-(2-chlorophenyl)-(2-MS[M+1]+: 597methylacryloyl)amino]ethoxy}-phenyl)propionic acid methyl esterIIa_2V_23(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.926B{3-[(2-chlorophenyl-(2-MS[M, M+2]+: 611,methylacryloyl)amino]propoxy}-613phenyl)propionic acid methyl esterIIa_3V_17(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.034A{2-[but-2-(E)-enoyl-(2-chlorophenyl)-MS[M, M+2]+: 597,amino]ethoxy}phenyl)propionic acid599methyl esterIIa_4V_17(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.532A{2-[(2-chlorophenyl)-(3-MS[M, M+2]+: 613,methylbutyryl)amino]ethoxy}phenyl)-615propionic acid methyl esterIIa_5V_17(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.427A{2-[(2-chlorophenyl)-MS[M, M+2]+: 611,cyclobutanecarbonylamino]ethoxy}-613phenyl)propionic acid methyl esterIIa_6V_17(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.657A{2-[(2-chlorophenyl)-MS[M, M+2]+: 625,cyclopentanecarbonylamino]ethoxy}-627phenyl)propionic acid methyl esterIIa_7V_17(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.094A{2-[(2-chlorophenyl)-MS[M, M+2]+: 597,cyclopropanecarbonylamino]ethoxy}-599phenyl)propionic acid methyl esterIIa_8V_23(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.28A{3-[(2-chlorophenyl)-MS[M, M+2]+: 611,cyclopropanecarbonylamino]-613propoxy}phenyl)propionic acidmethyl esterIIa_9V_17(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.049A{2-[(2-chlorophenyl)propionylamino]-MS[M, M+2]+: 585,ethoxy}phenyl)propionic acid methyl587esterIIa_10V_23(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.247A{3-[(2-chlorophenyl)propionylamino]-MS[M, M+2]+: 599,propoxy}phenyl)propionic acid601methyl esterIIa_11V_17(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.28A{2-[(2-chlorophenyl)isobutyrylamino]-MS[M, M+2]+: 599,ethoxy}phenyl)propionic acid methyl601esterIIa_12V_23(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 10.126B{3-[(2-chlorophenyl)isobutyrylamino]-MS[M, M+2]+: 613,propoxy}phenyl)propionic acid615methyl esterIIa_13V_17(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.069A{2-[butyryl-(2-chlorophenyl)amino]-MS[M, M+2]+: 597,ethoxy}phenyl)propionic acid methyl599esterIIa_14V_23(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 10.148B{3-[butyryl-(2-chlorophenyl)amino]-MS[M, M+2]+: 613,propoxy}phenyl)propionic acid615methyl esterIIa_15V_23(S)-3-(4-{3-[Acryloyl-(2-rt: 9.102Achlorophenyl)amino]propoxy}-MS[M, M+2]+: 597,phenyl)-2-(2-benzoylphenylamino)-599propionic acid methyl esterIIa_16V_11(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.961A{2-[(2-fluorophenyl)-(thiophene-2-MS[M+1]+: 623carbonyl)amino]ethoxy}phenyl)-propionic acid methyl esterIIa_17V_11(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.857A{2-[(2-fluorophenyl)-(2-MS[M+1]+: 581methylacryloyl)amino]ethoxy}-phenyl)propionic acid methyl esterIIa_18V_11(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.282A{2-[(2-fluorophenyl)-(3-MS[M+1]+: 597methylbutyryl)amino]ethoxy}phenyl)-propionic acid methyl esterIIa_19V_11(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.185A{2-[cyclobutanecarbonyl-(2-MS[M+1]+: 595fluorophenyl)amino]ethoxy}phenyl)-propionic acid methyl esterIIa_20V_11(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.412A{2-[cyclopentanecarbonyl-(2-MS[M+1]+: 609fluorophenyl)amino]ethoxy}phenyl)-propionic acid methyl esterIIa_21V_11(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.865A{2-[cyclopropanecarbonyl-(2-MS[M+1]+: 581fluorophenyl)amino]ethoxy}phenyl)-propionic acid methyl esterIIa_22V_11(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.796A{2-[(2-fluorophenyl)propionylamino]-MS[M+1]+: 569ethoxy}phenyl)propionic acid methylesterIIa_23V_11(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.04A{2-[(2-fluorophenyl)isobutyrylamino]-MS[M+1]+: 583ethoxy}phenyl)propionic acid methylesterIIa_24V_11(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.05A{2-[butyryl-(2-fluorophenyl)amino]-MS[M+1]+: 583ethoxy}phenyl)propionic acid methylesterIIa_25V_17(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.408A{2-[(2,2-dimethylpropionyl)-(2-MS[M+1]+: 597fluorophenyl)amino]ethoxy}phenyl)-propionic acid methyl esterIIa_26V_20(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.828B{3-[(2-methylacryloyl)-o-tolylamino]-MS[M+1]+: 591propoxy}phenyl)propionic acidmethyl esterIIa_27V_14(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.684A{2-[(2-ethylbutyryl)-o-tolylamino]-MS[M+1]+: 607ethoxy}phenyl)propionic acid methylesterIIa_28V_20(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 10.165B{3-[(3-methylbut-2-(E)-enoyl)-o-MS[M+1]+: 605tolylamino]propoxy}phenyl)propionicacid methyl esterIIa_29V_20(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.911B[3-(but-2-(E)-enoyl-o-tolylamino)-MS[M+1]+: 591propoxy]phenyl}propionic acidmethyl esterIIa_30V_14(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.788A{2-[(3,3-dimethylbutyryl)-o-MS[M+1]+: 607tolylamino]ethoxy}phenyl)propionicacid methyl esterIIa_31V_14(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.465A{2-[(3-methylbutyryl)-o-tolylamino]-MS[M+1]+: 593ethoxy}phenyl)propionic acid methylesterIIa_32V_20(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 10.331B{3-[(3-methylbutyryl)-o-tolylamino]-MS[M+1]+: 607propoxy}phenyl)propionic acidmethyl esterIIa_33V_20(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 10.129B[3-(o-tolylpent-4-enoylamino)-MS[M+1]+: 605propoxy]phenyl}propionic acidmethyl esterIIa_34V_14(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.378A[2-(cyclobutanecarbonyl-o-MS[M+1]+: 591tolylamino)ethoxy]phenyl}propionicacid methyl esterIIa_35V_14(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.607A[2-(cyclopentanecarbonyl-o-MS[M+1]+: 605tolylamino)ethoxy]phenyl}propionicacid methyl esterIIa_36V_20(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.849B[3-(propionyl-o-tolylamino)propoxy]-MS[M+1]+: 579phenyl}propionic acid methyl esterIIa_37V_14(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.22A[2-(isobutyryl-o-tolylamino)ethoxy]-MS[M+1]+: 579phenyl}propionic acid methyl esterIIa_38V_20(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 10.08B[3-(isobutyryl-o-tolylamino)propoxy]-MS[M+1]+: 593phenyl}propionic acid methyl esterIIa_39V_20(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 10.348B[3-(pentanoyl-o-tolylamino)propoxy]-MS[M+1]+: 607phenyl}propionic acid methyl esterIIa_40V_14(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.233A[2-(butyryl-o-tolylamino)ethoxy]-MS[M+1]+: 579phenyl}propionic acid methyl esterIIa_41V_20(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 10.094B[3-(butyryl-o-tolylamino)propoxy]-MS[M+1]+: 593phenyl}propionic acid methyl esterIIa_42V_14(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.077A[2-(benzoyl-o-tolylamino)ethoxy]-MS[M+1]+: 613phenyl}propionic acid methyl esterIIa_43V_14(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.597A{2-[(2,2-dimethylpropionyl)-o-MS[M+1]+: 593tolylamino]ethoxy}phenyl)propionicacid methyl esterIIa_44V_20(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 10.435B{3-[(2,2-dimethylpropionyl)-o-MS[M+1]+: 607tolylamino]propoxy}phenyl)propionicacid methyl esterIIa_45V_20(S)-3-{4-[3-(Acryloyl-o-tolylamino)-rt: 9.781Bpropoxy]phenyl}-2-(2-MS[M+1]+: 577benzoylphenylamino)propionic acidmethyl esterIIa_46V_18(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.126A{2-[(3-chlorophenyl)-(2-MS[M, M+2]+: 597,methylacryloyl)amino]ethoxy}-599phenyl)propionic acid methyl esterIIa_47V_18(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.184A{2-[but-2-(E)-enoyl-(3-chlorophenyl)-MS[M, M+2]+: 597,amino]ethoxy]phenyl}propionic acid599methyl esterIIa_48V_24(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.348A{3-[but-2-(E)-enoyl-(3-chlorophenyl)-MS[M, M+2]+: 611,amino]propoxy}phenyl)propionic acid613methyl esterIIa_49V_18(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.557A{2-[(3-chlorophenyl)-(3-MS[M, M+2]+: 613,methylbutyryl)amino]ethoxy}phenyl)-615propionic acid methyl esterIIa_50V_18(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.375A{2-[(3-chlorophenyl)-pent-4-MS[M, M+2]+: 611,enoylamino]ethoxy}phenyl)propionic613acid methyl esterIIa_51V_18(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.488A{2-[(3-chlorophenyl)-MS[M, M+2]+: 611,cyclobutanecarbonylamino]ethoxy}-613phenyl)propionic acid methyl esterIIa_52V_18(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.708A{2-[(3-chlorophenyl)-MS[M, M+2]+: 625,cyclopentanecarbonylamino]ethoxy}-627phenyl)propionic acid methyl esterIIa_53V_18(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.217A{2-[(3-chlorophenyl)-MS[M, M+2]+: 597,cyclopropanecarbonylamino]ethoxy}-599phenyl)propionic acid methyl esterIIa_54V_24(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.401A{3-[(3-chlorophenyl)-MS[M, M+2]+: 611,cyclopropanecarbonylamino]-613propoxy}phenyl)propionic acidmethyl esterIIa_55V_18(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.097A{2-[(3-chlorophenyl)propionylamino]-MS[M, M+2]+: 585,ethoxy}phenyl)propionic acid methyl587esterIIa_56V_24(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.279A{3-[(3-chlorophenyl)propionylamino]-MS[M, M+2]+: 599,propoxy}phenyl)propionic acid601methyl esterIIa_57V_18(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.332A{2-[(3-chlorophenyl)isobutyrylamino]-MS[M, M+2]+: 599,ethoxy}phenyl)propionic acid methyl601esterIIa_58V_24(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.502A{3-[(3-chlorophenyl)isobutyrylamino]-MS[M, M+2]+: 613,propoxy}phenyl)propionic acid615methyl esterIIa_59V_18(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.339A{2-[butyryl-(3-chlorophenyl)amino]-MS[M, M+2]+: 599,ethoxy}phenyl)propionic acid methyl601esterIIa_60V_24(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.508A{3-[butyryl-(3-chlorophenyl)amino]-MS[M, M+2]+: 613,propoxy}phenyl)propionic acid615methyl esterIIa_61V_18(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.669A{2-[(3-chlorophenyl)-(2,2-MS[M, M+2]+: 613,dimethylpropionyl)amino]ethoxy)-615phenyl)propionic acid methyl esterIIa_62V_24(S)-3-(4-{3-[Acryloyl-(3-rt: 9.202Achlorophenyl)amino]propoxy}-MS[M, M+2]+: 597,phenyl)-2-(2-benzoylphenylamino)-599propionic acid methyl esterIIa_63V_12(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.016A{2-[(3-fluorophenyl)-(thiophene-2-MS[M+1]+: 623carbonyl)amino]ethoxy}phenyl)-propionic acid methyl esterIIa_64V_12(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.86A{2-[(3-fluorophenyl)-(2-MS[M+1]+: 581methylacryloyl)amino]ethoxy}-phenyl)propionic acid methyl esterIIa_65V_12(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.284A{2-[(3-fluorophenyl)-(3-MS[M+1]+: 597methylbutyryl)amino]ethoxy}phenyl)-propionic acid methyl esterIIa_66V_12(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.198A{2-[cyclobutanecarbonyl-(3-MS[M+1]+: 595fluorophenyl)amino]ethoxy}phenyl)-propionic acid methyl esterIIa_67V_12(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.424A{2-[cyclopentanecarbonyl-(3-MS[M+1]+: 609fluorophenyl)amino]ethoxy}phenyl)-propionic acid methyl esterIIa_68V_12(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.93A{2-[cyclopropanecarbonyl-(3-MS[M+1]+: 581fluorophenyl)amino]ethoxy}phenyl)-propionic acid methyl esterIIa_69V_12(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.805A{2-[(3-fluorophenyl)propionylamino]-MS[M+1]+: 569ethoxy}phenyl)propionic acid methylesterIIa_70V_12(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.047A{2-[(3-fluorophenyl)isobutyrylamino]-MS[M+1]+: 583ethoxy}phenyl)propionic acid methylesterIIa_71V_12(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.057A{2-[butyryl-(3-fluorophenyl)amino]-MS[M+1]+: 583ethoxy}phenyl)propionic acid methylesterIIa_72V_12(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.393A{2-[(2,2-dimethylpropionyl)-(3-MS[M+1]+: 597fluorophenyl)amino]ethoxy}phenyl)-propionic acid methyl esterIIa_73V_8(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.199A{3-[(2-methylacryloyl)-(3-MS[M+1]+: 605methylbenzyl)amino]propoxy}-phenyl)propionic acid methyl esterIIa_74V_7(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.678A{2-[(2-ethylbutyryl)-(3-methylbenzyl)-MS[M+1]+: 621amino]ethoxy}phenyl)propionic acidmethyl esterIIa_75V_8(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.382A{3-[(3-methylbenzyl)-(3-methylbut-2-MS[M+1]+: 619(E)-enoyl)amino]propoxy}phenyl)-propionic acid methyl esterIIa_76V_8(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.153A{3-[but-2-(E)-enoyl-(3-methylbenzyl)-MS[M+1]+: 605amino]propoxy}phenyl)propionic acidmethyl esterIIa_77V_7(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.728A{2-[(3,3-dimethylbutyryl)-(3-MS[M+1]+: 621methylbenzyl)amino]ethoxy}phenyl)-propionic acid methyl esterIIa_78V_7(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.471A{2-[(3-methylbenzyl)-(3-MS[M+1]+: 607methylbutyryl)amino]ethoxy}phenyl)-propionic acid methyl esterIIa_79V_8(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.549A{3-[(3-methylbenzyl)-(3-MS[M+1]+: 621methylbutyryl)amino]propoxy}-phenyl)propionic acid methyl esterIIa_80V_7(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.389A{2-[cyclobutanecarbonyl-(3-MS[M+1]+: 605methylbenzyl)amino]ethoxy}phenyl)-propionic acid methyl esterIIa_81V_8(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.464A{3-[cyclobutanecarbonyl-(3-MS[M+1]+: 619methylbenzyl)amino]propoxy}-phenyl)propionic acid methyl esterIIa_82V_7(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.588A{2-[cyclopentanecarbonyl-(3-MS[M+1]+: 619methylbenzyl)amino]ethoxy}phenyl)-propionic acid methyl esterIIa_83V_8(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.194A{3-[cyclopropanecarbonyl-(3-MS[M+1]+: 605methylbenzyl)amino]propoxy}-phenyl)propionic acid methyl esterIIa_84V_8(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.095A{3-[(3-methylbenzyl)propionylamino]-MS[M+1]+: 593propoxy}phenyl)propionic acidmethyl esterIIa_85V_7(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.23A{2-[isobutyryl-(3-methylbenzyl)-MS[M+1]+: 593amino]ethoxy}phenyl)propionic acidmethyl esterIIa_86V_8(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.319A{3-[isobutyryl-(3-methylbenzyl)-MS[M+1]+: 607amino]propoxy}phenyl)propionic acidmethyl esterIIa_87V_7(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.247A{2-[butyryl-(3-methylbenzyl)amino]-MS[M+1]+: 593ethoxy}phenyl)propionic acid methylesterIIa_88V_8(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.328A{3-[butyryl-(3-methylbenzyl)amino]-MS[M+1]+: 607propoxy}phenyl)propionic acidmethyl esterIIa_89V_7(S)-3-(4-{2-[Benzoyl-(3-rt: 9.28Amethylbenzyl)amino]ethoxy}phenyl)-MS[M+1]+: 6272-(2-benzoylphenylamino)propionicacid methyl esterIIa_90V_7(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.602A{2-[(2,2-dimethylpropionyl)-(3-MS[M+1]+: 607methylbenzyl)amino]ethoxy}phenyl)-propionic acid methyl esterIIa_91V_8(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.635A{3-[(2,2-dimethylpropionyl)-(3-MS[M+1]+: 621methylbenzyl)amino]propoxy}-phenyl)propionic acid methyl esterIIa_92V_21(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.906B{3-[(2-methylacryloyl)-m-tolylamino]-MS[M+1]+: 591propoxy}phenyl)propionic acidmethyl esterIIa_93V_15(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.75A{2-[(2-ethylbutyryl)-m-tolylamino]-MS[M+1]+: 607ethoxy}phenyl)propionic acid methylesterIIa_94V_21(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 10.231B{3-[(3-methylbut-2-(E)-enoyl)-m-MS[M+1]+: 605tolylamino]propoxy}phenyl)propionicacid methyl esterIIa_95V_21(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.985B[3-(but-2-(E)-enoyl-m-tolylamino)-MS[M+1]+: 591propoxy]phenyl}propionic acidmethyl esterIIa_96V_15(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.826A{2-[(3,3-dimethylbutyryl)-m-MS[M+1]+: 607tolylamino]ethoxy}phenyl)propionicacid methyl esterIIa_97V_15(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.518A{2-[(3-methylbutyryl)-m-tolylamino]-MS[M+1]+: 593ethoxy}phenyl)propionic acid methylesterIIa_98V_15(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.46A[2-(cyclobutanecarbonyl-m-MS[M+1]+: 591tolylamino)ethoxy]phenyl}propionicacid methyl esterIIa_99V_15(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.671A[2-(cyclopentanecarbonyl-m-MS[M+1]+: 605tolylamino)ethoxy]phenyl}propionicacid methyl esterIIa_100V_21(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 10.041B[3-(cyclopropanecarbonyl-m-MS[M+1]+: 591tolylamino)propoxy]phenyl}propionicacid methyl esterIIa_101V_21(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.915B[3-(propionyl-m-tolylamino)propoxy]-MS[M+1]+: 579phenyl}propionic acid methyl esterIIa_102V_15(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.287A[2-(isobutyryl-m-tolylamino)ethoxy]-MS[M+1]+: 579phenyl}propionic acid methyl esterIIa_103V_21(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 10.134B[3-(isobutyryl-m-tolylamino)propoxy]-MS[M+1]+: 593phenyl}propionic acid methyl esterIIa_104V_21(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 10.398B[3-(pentanoyl-m-tolylamino)propoxy]-MS[M+1]+: 607phenyl}propionic acid methyl esterIIa_105V_15(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.296A[2-(butyryl-m-tolylamino)ethoxy]-MS[M+1]+: 579phenyl}propionic acid methyl esterIIa_106V_21(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 10.146B[3-(butyryl-m-tolylamino)propoxy]-MS[M+1]+: 593phenyl}propionic acid methyl esterIIa_107V_15(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.176A[2-(benzoyl-m-tolylamino)ethoxy]-MS[M+1]+: 613phenyl}propionic acid methyl esterIIa_108V_15(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.659A{2-[(2,2-dimethylpropionyl)-m-MS[M+1]+: 593tolylamino]ethoxy}phenyl)propionicacid methyl esterIIa_109V_21(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 10.508B{3-[(2,2-dimethylpropionyl)-m-MS[M+1]+: 607tolylamino]propoxy}phenyl)propionicacid methyl esterIIa_110V_21(S)-3-{4-[3-(Acryloyl-m-tolylamino)-rt: 9.85Bpropoxy]phenyl}-2-(2-MS[M+1]+: 577benzoylphenylamino)propionic acidmethyl esterIIa_111V_19(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.173A{2-[(4-chlorophenyl)-(2-MS[M, M+2]+: 597,methylacryloyl)amino]ethoxy}-599phenyl)propionic acid methyl esterIIa_112V_19(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.242A{2-[but-2-(E)-enoyl-(4-chlorophenyl)-MS[M, M+2]+: 597,amino]ethoxy}phenyl)propionic acid599methyl esterIIa_113V_19(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.615A{2-[(4-chlorophenyl)-(3-MS[M, M+2]+: 613,methylbutyryl)amino]ethoxy}phenyl)-615propionic acid methyl esterIIa_114V_19(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.428A{2-[(4-chlorophenyl)-pent-4-MS[M, M+2]+: 611,enoylamino]ethoxy}phenyl)propionic613acid methyl esterIIa_115V_19(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.532A{2-[(4-chlorophenyl)-MS[M, M+2]+: 611,cyclobutanecarbonylamino]ethoxy}-613phenyl)propionic acid methyl esterIIa_116V_19(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.763A{2-[(4-chlorophenyl)-MS[M, M+2]+: 625,cyclopentanecarbonylamino]ethoxy}-627phenyl)propionic acid methyl esterIIa_117V_19(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.263A{2-[(4-chlorophenyl)-MS[M, M+2]+: 597,cyclopropanecarbonylamino]ethoxy}-599phenyl)propionic acid methyl esterIIa_118V_25(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.442A{3-[(4-chlorophenyl)-MS[M, M+2]+: 611,cyclopropanecarbonylamino]-613propoxy}phenyl)propionic acidmethyl esterIIa_119V_19(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.146A{2-[(4-chlorophenyl)propionylamino]-MS[M, M+2]+: 585,ethoxy}phenyl)propionic acid methyl587esterIIa_120V_25(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.323A{3-[(4-chlorophenyl)propionylamino]-MS[M, M+2]+: 599,propoxy}phenyl)propionic acid601methyl esterIIa_121V_19(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.393A{2-[(4-chlorophenyl)isobutyrylamino]-MS[M, M+2]+: 599,ethoxy}phenyl)propionic acid methyl601esterIIa_122V_25(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.558A{3-[(4-chlorophenyl)isobutyrylamino]-MS[M, M+2]+: 613,propoxy}phenyl)propionic acid615methyl esterIIa_123V_19(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.393A{2-[butyryl-(4-chlorophenyl)amino]-MS[M, M+2]+: 599,ethoxy}phenyl)propionic acid methyl601esterIIa_124V_25(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.558A{3-[butyryl-(4-chlorophenyl)amino]-MS[M, M+2]+: 613,propoxy}phenyl)propionic acid615methyl esterIIa_125V_19(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.71A{2-[(4-chlorophenyl)-(2,2-MS[M, M+2]+: 613,dimethylpropionyl)amino]ethoxy}-615phenyl)propionic acid methyl esterIIa_126V_25(S)-3-(4-{3-[Acryloyl-(4-rt: 9.246Achlorophenyl)amino]propoxy}-MS[M, M+2]+: 597,phenyl)-2-(2-benzoylphenylamino)-599propionic acid methyl esterIIa_127V_13(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.015A{2-[(4-fluorophenyl)-(thiophene-2-MS[M+1]+: 623carbonyl)amino]ethoxy}phenyl)-propionic acid methyl esterIIa_128V_13(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.828A{2-[(4-fluorophenyl)-(2-MS[M+1]+: 581methylacryloyl)amino]ethoxy}-phenyl)propionic acid methyl esterIIa_129V_13(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.141A{2-[(4-fluorophenyl)-(3-methylbut-2-MS[M+1]+: 595(E)-enoyl)amino]ethoxy}phenyl)-propionic acid methyl esterIIa_130V_13(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.278A{2-[(4-fluorophenyl)-(3-MS[M+1]+: 597methylbutyryl)amino]ethoxy}phenyl)-propionic acid methyl esterIIa_131V_13(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.184A{2-[cyclobutanecarbonyl-(4-MS[M+1]+: 595fluorophenyl)amino]ethoxy}phenyl)-propionic acid methyl esterIIa_132V_13(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.413A{2-[cyclopentanecarbonyl-(4-MS[M+1]+: 609fluorophenyl)amino]ethoxy}phenyl)-propionic acid methyl esterIIa_133V_13(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.913A{2-[cyclopropanecarbonyl-(4-MS[M+1]+: 581fluorophenyl)amino]ethoxy}phenyl)-propionic acid methyl esterIIa_134V_13(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.794A{2-[(4-fluorophenyl)propionylamino]-MS[M+1]+: 569ethoxy}phenyl)propionic acid methylesterIIa_135V_13(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.038A{2-[(4-fluorophenyl)isobutyrylamino]-MS[M+1]+: 583ethoxy}phenyl)propionic acid methylesterIIa_136V_13(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.046A{2-[butyryl-(4-fluorophenyl)amino]-MS[M+1]+: 583ethoxy}phenyl)propionic acid methylesterIIa_137V_13(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.384A{2-[(2,2-dimethylpropionyl)-(4-MS[M+1]+: 597fluorophenyl)amino]ethoxy}phenyl)-propionic acid methyl esterIIa_138V_22(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.202A{3-[(2-methylacryloyl)-p-tolylamino]-MS[M+1]+: 591propoxy}phenyl)propionic acidmethyl esterIIa_139V_16(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.775A{2-[(2-ethylbutyryl)-p-tolylamino]-MS[M+1]+: 607ethoxy}phenyl)propionic acid methylesterIIa_140V_16(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.851A{2-[(3,3-dimethylbutyryl)-p-MS[M+1]+: 607tolylamino]ethoxy}phenyl)propionicacid methyl esterIIa_141V_16(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.541A{2-[(3-methylbutyryl)-p-tolylamino]-MS[M+1]+: 593ethoxy}phenyl)propionic acid methylesterIIa_142V_22(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.674A{3-[(3-methylbutyryl)-p-tolylamino]-MS[M+1]+: 607propoxy}phenyl)propionic acidmethyl esterIIa_143V_16(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.472A[2-(cyclobutanecarbonyl-p-MS[M+1]+: 591tolylamino)ethoxy]phenyl}propionicacid methyl esterIIa_144V_22(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.605A[3-(cyclobutanecarbonyl-p-MS[M+1]+: 605tolylamino)propoxy]phenyl}propionicacid methyl esterIIa_145V_16(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.693A[2-(cyclopentanecarbonyl-p-MS[M+1]+: 605tolylamino)ethoxy]phenyl}propionicacid methyl esterIIa_146V_22(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.208A[3-(propionyl-p-tolylamino)propoxy]-MS[M+1]+: 579phenyl}propionic acid methyl esterIIa_147V_16(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.307A[2-(isobutyryl-p-tolylamino)ethoxy]-MS[M+1]+: 579phenyl}propionic acid methyl esterIIa_148V_22(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.443A[3-(isobutyryl-p-tolylamino)propoxy]-MS[M+1]+: 593phenyl}propionic acid methyl esterIIa_149V_16(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.313A[2-(butyryl-p-tolylamino)ethoxy]-MS[M+1]+: 579phenyl}propionic acid methyl esterIIa_150V_16(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.169A[2-(benzoyl-p-tolylamino)ethoxy]-MS[M+1]+: 613phenyl}propionic acid methyl esterIIa_151V_16(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.671A{2-[(2,2-dimethylpropionyl)-p-MS[M+1]+: 593tolylamino]ethoxy}phenyl)propionicacid methyl esterIIa_152V_22(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.772A{3-[(2,2-dimethylpropionyl)-p-MS[M+1]+: 607tolylamino]propoxy}phenyl)propionicacid methyl esterIIa_153V_1(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.4A{2-[benzyl(naphthalene-1-carbonyl)-MS[M+1]+: 663amino]ethoxy}phenyl)propionic acidmethyl esterIIa_154V_1(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.42A{2-[benzyl(naphthalene-2-carbonyl)-MS[M+1]+: 663amino]ethoxy}phenyl)propionic acidmethyl esterIIa_155V_1(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.532A{2-[benzyl(pyrazine-2-carbonyl)-MS[M+1]+: 615amino]ethoxy}phenyl)propionic acidmethyl esterIIa_156V_2(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.642A{3-[benzyl(pyrazine-2-carbonyl)-MS[M+1]+: 629amino]propoxy}phenyl)propionic acidmethyl esterIIa_157V_1(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.693A{2-[benzyl(pyridine-2-carbonyl)-MS[M+1]+: 614amino]ethoxy}phenyl)propionic acidmethyl esterIIa_158V_2(S)-2-(2-Benzoylphenylamino)-3-(4-8.90(d, 1H), 8.55,A{3-[benzyl(pyridine-2-carbonyl)-8.45(2×d, 1H,amino]propoxy}phenyl)propionic acidrotamers mixture),methyl ester7.77-7.12(ca, 17H),6.81-6.55(ca, 4H),4.80, 4.69(2×s, 2H,rotamers mixture),4.39(q, 1H), 3.39,3.76(2×t, 2H,rotamers mixture),3.70, 3.69(2×s, 3H,rotamers mixture),3.62, 3.58(2×t, 2H,rotamers mixture),3.20(dd, 1H), 3.10(m,1H), 2.15-1.97(ca,2H)IIa_159V_1(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.294A{2-[benzyl(quinoline-2-carbonyl)-MS[M+1]+: 664amino]ethoxy}phenyl)propionic acidmethyl esterIIa_160V_2(S)-2-(2-Benzoylphenylamino)-3-(4-8.90(t, 1H), 8.21,A{3-[benzyl(quinoline-2-carbonyl)-8.13(2×d, 1H, rotamersamino]propoxy}phenyl)propionic acidmixture), 8.04,methyl ester7.80(2×t, 2H, rotamersmixture),7.73-7.25(ca, 14H), 7.18,7.06(2×d, 2H, rotamersmixture), 6.82,6.47(2×d, 2H, rotamersmixture),6.70-6.55(ca, 2H), 4.86,4.79(2×s, 2H, rotamersmixture), 4.37(q, 1H),4.02, 3.77(2×t, 2H,rotamers mixture),3.69-3.64(ca, 5H),3.25-3.05(ca, 2H),2.20-2.04(ca, 2H)IIa_161V_1(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.119A{2-[benzyl(quinoxaline-2-carbonyl)-MS[M+1]+: 665amino]ethoxy}phenyl)propionic acidmethyl esterIIa_162V_2(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.211A{3-[benzyl(quinoxaline-2-carbonyl)-MS[M+1]+: 679amino]propoxy}phenyl)propionic acidmethyl esterIIa_163V_1(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.07A{2-[benzyl(thiophene-2-carbonyl)-MS[M+1]+: 619amino]ethoxy}phenyl)propionic acidmethyl esterIIa_164V_2(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.193A{3-[benzyl(thiophene-2-carbonyl)-MS[M+1]+: 633amino]propoxy}phenyl)propionic acidmethyl esterIIa_165V_1(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.815A{2-[benzyl(furan-3-carbonyl)amino]-MS[M+1]+: 603ethoxy}phenyl)propionic acid methylesterIIa_166V_2(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.907A{3-[benzyl(furan-3-carbonyl)amino]-MS[M+1]+: 617propoxy}phenyl)propionic acidmethyl esterIIa_167V_1(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.1A{2-[benzyl(isoquinoline-3-carbonyl)-MS[M+1]+: 664amino]ethoxy}phenyl)propionic acidmethyl esterIIa_168V_2(S)-2-(2-Benzoylphenylamino)-3-(4-9.19, 9.10(2×s, 1H,A{3-[benzyl(isoquinoline-3-carbonyl)-rotamers mixture),amino]propoxy}phenyl)propionic acid8.90(t, 1H), 8.07,methyl ester7.99(2×s, 1H, rotamersmixture),7.64-7.25(ca, 16H), 7.18,7.05(2×d, 2H, rotamersmixture), 6.82,6.50(2×d, 2H, rotamersmixture),6.65-6.55(ca, 2H), 4.86,4.76(2×s, 2H, rotamersmixture), 4.37(m, 1H),4.02, 3.77(2×t, 2H,rotamers mixture),3.69-3.60(ca, 5H),3.25-3.05(ca, 2H),2.20-2.04(ca, 2H)IIa_169V_1(S)-2-(2-Benzoylphenylamino)-3-(4-8.90(d, 1H),A{2-benzyl(pyridine-3-carbonyl)-8.78-8.62(ca, 2H), 7.83-7.73(mamino]ethoxy}phenyl)propionic acid1H), 7.59(d, 2H),methyl ester7.51-7.41(ca, 4H),7.37-7.20(m, 9H),6.85-6.72(ca, 2H),6.65-6.56(ca, 2H),4.87, 4.69(2×s, 2H,rotamers mixture),4.40(q, 1H),4.25-3.58(ca, 7H), 3.25(dd,1H), 3.10(dd, 1H)IIa_170V_2(S)-2-(2-Benzoylphenylamino)-3-(4-8.90(d, 1H),A{3-[benzyl(pyridine-3-carbonyl)-8.67-8.59(ca, 2H), 7.67-7.10(mamino]propoxy}phenyl)propionic acid16H), 6.81-6.55(ca,methyl ester4H), 4.80, 4.51(2×s,2H, rotamers mixture),4.39(q, 1H),4.02-3.39(ca, 7H), 3.25(dd,1H), 3.10(dd, 1H),1.92-1.71(ca, 2H)IIa_171V_1(S)-2-(2-Benzoylphenylamino)-3-{4-8.91(d, 1H), 7.59(d,A[2-(benzylphenylacetylamino)-2H), 7.51-7.41(ca,ethoxy]phenyl}propionic acid methyl4H), 7.33-7.09(ca,ester13H), 6.78-6.70(ca,2H), 6.65-6.55(ca,2H), 4.71, 4.67(2×s,2H, rotamers mixture),4.39(q, 1H), 4.14,3.88(2×t, 2H,rotamers mixture),3.92-3.60(ca, 7H),3.26-3.08(ca, 2H)IIa_172V_2(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.26A[3-(benzylphenylacetylamino)-MS[M+1]+: 641propoxy]phenyl}propionic acidmethyl esterIIa_173V_1(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.865A{2-[benzyl-(2-methylacryloyl)amino]-MS[M+1]+: 577ethoxy}phenyl)propionic acid methylesterIIa_174V_2(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.948A{3-[benzyl-(2-methylacryloyl)amino]-MS[M+1]+: 591propoxy}phenyl)propionic acidmethyl esterIIa_175V_1(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.367A{2-[benzyl-(3-phenylpropynoyl)-MS[M+1]+: 637amino]ethoxy}phenyl)propionic acidmethyl esterIIa_176V_2(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.454A{3-[benzyl-(3-phenylpropynoyl)-MS[M+1]+: 651amino]propoxy}phenyl)propionic acidmethyl esterIIa_177V_1(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.45A{2-[benzyl-(2-ethylbutyryl)amino]-MS[M+1]+: 607ethoxy}phenyl)propionic acid methylesterIIa_178V_2(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.511A{3-[benzyl-(2-ethylbutyryl)amino]-MS[M+1]+: 621propoxy}phenyl)propionic acidmethyl esterIIa_179V_1(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.087A{2-[benzyl-(3-methylbut-2-(E)-enoyl)-MS[M+1]+: 591amino]ethoxy}phenyl)propionic acidmethyl esterIIa_180V_2(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.187A{3-[benzyl-(3-methylbut-2-(E)-enoyl)-MS[M+1]+: 605amino]propoxy}phenyl)propionic acidmethyl esterIIa_181V_1(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.027A{2-[benzyl-(3-furan-2-ylacryloyl)-MS[M+1]+: 629amino]ethoxy}phenyl)propionic acidmethyl esterIIa_182V_2(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.12A{3-[benzyl-(3-furan-2-ylacryloyl)-MS[M+1]+: 643amino]propoxy}phenyl)propionic acidmethyl esterIIa_183V_1(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.19A{2-[benzyl-(3-thiophen-2-ylacryloyl)-MS[M+1]+: 645amino]ethoxy}phenyl)propionic acidmethyl esterIIa_184V_2(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.304A{3-[benzyl-(3-thiophen-2-ylacryloyl)-MS[M+1]+: 659amino]propoxy}phenyl)propionic acidmethyl esterIIa_185V_1(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.889A{2-[benzyl-(3-furan-3-yl-(E)-acryloyl)-MS[M+1]+: 629amino]ethoxy}phenyl)propionic acidmethyl esterIIa_186V_2(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.005A{3-[benzyl-(3-furan-3-yl-(E)-acryloyl)-MS[M+1]+: 643amino]propoxy}phenyl)propionic acidmethyl esterIIa_187V_1(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.097A{2-[benzyl-(3-pyridin-3-yl-(E)-MS[M+1]+: 640acryloyl)amino]ethoxy}phenyl)-propionic acid methyl esterIIa_188V_2(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.245A{3-[benzyl-(3-pyridin-3-yl-(E)-MS[M+1]+: 654acryloyl)amino]propoxy}phenyl)-propionic acid methyl esterIIa_189V_1(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.105A{2-[benzyl-(3-thiophen-3-yl-(E)-MS[M+1]+: 645acryloyl)amino]ethoxy}phenyl)-propionic acid methyl esterIIa_190V_2(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.214A{3-[benzyl-(3-thiophen-3-yl-(E)-MS[M+1]+: 659acryloyl)amino]propoxy}phenyl)-propionic acid methyl esterIIa_191V_1(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 8.808A[2-(benzylbut-2-(E)-enoylamino)-MS[M+1]+: 577ethoxy]phenyl}propionic acid methylesterIIa_192V_2(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.336A[3-(benzylbut-2-(E)-enoylamino)-MS[M+1]+: 607propoxy]phenyl}propionic acidmethyl esterIIa_193V_1(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.093A{2-[benzyl-(2-thiophen-2-ylacetyl)-MS[M+1]+: 633amino]ethoxy}phenyl)propionic acidmethyl esterIIa_194V_2(S)-2-(2-Benzoylphenylamino)-3-(4-8.90(d, 1H), 7.59(d,A{3-[benzyl-(2-thiophen-2-ylacetyl)-2H), 7.50-7.43(m 4H),amino]propoxy}phenyl)propionic acid7.36-7.10(m, 9H),methyl ester6.91-6.74(ca, 4H),6.64-6.58(ca, 2H),4.63, 4.56(2×s, 2H,rotamers mixture),4.38(q, 1H), 3.98,3.86(2×s, 2H,rotamers mixture),3.92-3.85(ca, 2H),3.69(s, 3H), 3.56,3.47(2×t, 2H,rotamers mixture),3.25-3.06(ca, 2H),2.06-1.90(ca, 2H)IIa_195V_1(S)-2-(2-Benzoylphenylamino)-3-(4-8.90(d, 1H),A{2-[benzyl-(2-pyridin-3-ylacetyl)-8.52-8.34(ca, 2H), 7.61-7.14(mamino]ethoxy}phenyl)propionic acid16H), 6.83-6.74(ca,methyl ester2H), 6.65-6.56(ca,2H), 4.74, 4.70(2×s,2H, rotamers mixture),4.40(q, 1H), 4.15,3.98(2×t, 2H,rotamers mixture),3.93-3.66(ca, 7H),3.26-3.00(ca, 2H)IIa_196V_2(S)-2-(2-Benzoylphenylamino)-3-(4-8.90(d, 1H),A{3-[benzyl-(2-pyridin-3-ylacetyl)-8.48-8.37(ca, 2H),amino]propoxy}phenyl)propionic acid7.61-7.13(m 16H),methyl ester6.81-6.74(ca, 2H),6.64-6.55(ca, 2H), 4.63,4.57(2×s, 2H,rotamers mixture),4.38(q, 1H),3.92-3.88(ca, 2H),3.78-3.65(ca, 5H), 3.58,3.48(2×t, 2H, rotamersmixture),3.25-3.06(ca, 2H),2.06-1.94(ca, 2H)IIa_197V_1(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.076A{2-[benzyl-(2-thiophen-3-ylacetyl)-MS[M+1]+: 633amino]ethoxy}phenyl)propionic acidmethyl esterIIa_198V_2(S)-2-(2-Benzoylphenylamino)-3-(4-8.90(d, 1H), 7.59(d,A{3-[benzyl-(2-thiophen-3-ylacetyl)-2H), 7.51-7.43(m 4H),amino]propoxy}phenyl)propionic acid7.36-6.97(ca, 11H),methyl ester6.79-6.73(ca, 2H),6.64-6.55(ca, 2H),4.62, 4.52(2×s, 2H,rotamers mixture),4.38(q, 1H),3.91-3.85(ca, 2H),3.80-3.69(ca, 5H), 3.54,3.45(2×t, 2H, rotamersmixture),3.25-3.12(ca, 2H),2.05-1.89(ca, 2H)IIa_199V_1(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.502A{2-[benzyl-(3,3-dimethylbutyryl)-MS[M+1]+: 607amino]ethoxy}phenyl)propionic acidmethyl esterIIa_200V_2(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.594A{3-[benzyl-(3,3-dimethylbutyryl)-MS[M+1]+: 621amino]propoxy}phenyl)propionic acidmethyl esterIIa_201V_1(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.243A{2-[benzyl-(3-methylbutyryl)-amino]-MS[M+1]+: 593ethoxy}phenyl)propionic acid methylesterIIa_202V_2(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.324A{3-[benzyl-(3-methylbutyryl)amino]-MS[M+1]+: 607propoxy}phenyl)propionic acidmethyl esterIIa_203V_1(S)-2-(2-Benzoylphenylamino)-3-(4-8.90(d, 1H),A{2-[benzyl-(3-pyridin-3-ylpropionyl)-8.58-8.39(ca, 2H), 7.59(d, 2H),amino]ethoxy}phenyl)propionic acid7.49-7.05(ca, 14H),methyl ester6.79-6.56(ca, 4H),4.68, 4.63(2×s, 2H,rotamers mixture),4.39(q, 1H), 4.11,3.90(2×t, 2H,rotamers mixture),3.75-3.57(ca, 5H),3.21(dd, 1H), 3.10(m,1H), 3.96, 2.95(2×t,2H, rotamers mixture),2.84, 2.62(2×t, 2H,rotamers mixture)IIa_204V_2(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 7.131A{3-[benzyl-(3-pyridin-3-ylpropionyl)-MS[M+1]+: 656amino]propoxy}phenyl)propionic acidmethyl esterIIa_205V_1(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.064A[2-(benzylpent-4-enoylamino)-MS[M+1]+: 591ethoxy]phenyl}propionic acid methylesterIIa_206V_2(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.159A[3-(benzylpent-4-enoylamino)-MS[M+1]+: 605propoxy]phenyl}propionic acidmethyl esterIIa_207V_1(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.368A{2-[benzyl-(3-phenylpropionyl)-MS[M+1]+: 641amino]ethoxy}phenyl)propionic acidmethyl esterIIa_208V_2(S)-2-(2-Benzoylphenylamino)-3-(4-8.90(d, 1H), 7.59(d,A{3-[benzyl-(3-phenylpropionyl)-2H), 7.50-7.04(ca,amino]propoxy}phenyl)propionic acid14H), 6.78-6.71(ca,methyl ester2H), 6.64-6.55(ca,2H), 4.61, 4.43(2×s,2H, rotamers mixture),4.38(q, 1H), 3.88,3.82(2×t, 2H,rotamers mixture),3.69(s, 3H), 3.52,3.36(2×t, 2H,rotamers mixture),3.21(dd, 1H),3.10(dd, 1H),3.02-2.90(ca, 2H), 2.72,2.61(2×t, 2H, rotamersmixture), 2.03,1.88(2×t, 2H, rotamersmixture)IIa_209V_1(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.19A[2-MS[M+1]+: 591(benzylcyclobutanecarbonylamino)-ethoxy]phenyl}propionic acid methylesterIIa_210V_2(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.596A[3-MS[M+1]+: 621(benzylcyclobutanecarbonylamino)-propoxy]phenyl}propionic acidmethyl esterIIa_211V_1(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.536A[2-MS[M+1]+: 619(benzylcyclohexanecarbonylamino)-ethoxy]phenyl}propionic acid methylesterIIa_212V_2(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.624A[3-MS[M+1]+: 633(benzylcyclohexanecarbonylamino)-propoxy]phenyl}propionic acidmethyl esterIIa_213V_1(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 10.056A{2-[benzyl-(3-cyclohexylpropionyl)-MS[M+1]+: 647amino]ethoxy}phenyl)propionic acidmethyl esterIIa_214V_2(S)-2-(2-Benzoylphenylamino)-3-(4-8.90(d, 1H), 7.59(d,A{3-[benzyl-(3-cyclohexylpropionyl)-2H), 7.51-7.41(ca,amino]propoxy}phenyl)propionic acid4H), 7.31-7.13(ca,methyl ester8H), 6.78(d, 2H),6.64-6.55(ca, 2H),4.60, 4.52(2×s, 2H,rotamers mixture),4.38(q, 1H),3.93-3.86(ca, 2H), 3.69(s, 3H),3.52, 3.42(2×t, 2H,rotamers mixture),3.25-3.08(ca, 2H),2.43-2.29(ca, 2H),2.04-1.92(ca, 2H),1.69-1.48(ca, 13H)IIa_215V_1(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.828A{2-[benzyl-(2-cyclohexylacetyl)-MS[M+1]+: 633amino]ethoxy}phenyl)propionic acidmethyl esterIIa_216V_2(S)-2-(2-Benzoylphenylamino)-3-(4-8.90(d, 1H), 7.59(d,A{3-[benzyl-(2-cyclohexylacetyl)-2H), 7.51-7.41(ca,amino]propoxy}phenyl)propionic acid4H), 7.33-7.12(ca,methyl ester8H), 6.77(d, 2H),6.64-6.55(ca, 2H),4.61, 4.53(2×s, 2H,rotamers mixture),4.38(q, 1H),3.93-3.85(ca, 2H), 3.69(s, 3H),3.51, 3.44(2×t, 2H,rotamers mixture),3.25-3.08(ca, 2H),2.26, 2.18(2×d, 2H,rotamers mixture),2.04-1.92(ca, 3H),1.80-1.64(ca, 10H)IIa_217V_1(S)-2-(2-Benzoylphenylamino)-3-{4-8.90(d, 1H), 7.59(d,A[2-2H), 7.51-7.44(ca,(benzylcyclopentanecarbonylamino)-4H), 7.36-7.14(ca,ethoxy]phenyl}propionic acid methyl8H), 6.79-6.73(ca,ester2H), 6.64-6.55(ca,2H), 4.75, 4.69(2×s,2H, rotamers mixture),4.38(q, 1H), 4.11,3.96(2×t, 2H,rotamers mixture),3.75-3.65(ca, 5H),3.24-3.08(ca, 2H),2.75(m, 1H),1.87-1.74(ca, 8H)IIa_218V_2(S)-2-(2-Benzoylphenylamino)-3-{4-8.90(d, 1H), 7.59(d,A[3-2H), 7.51-7.41(ca,(benzylcyclopentanecarbonylamino)-4H), 7.33-7.13(ca,propoxy]phenyl}propionic acid8H), 6.77(d, 2H),methyl ester6.64-6.55(ca, 2H),4.61, 4.59(2×s, 2H,rotamers mixture),4.38(q, 1H),3.93-3.87(ca, 2H), 3.69(s,3H), 3.53-3.44(ca,2H), 3.25-3.10(ca,2H), 2.75(m, 1H),1.99-1.74(ca, 10H)IIa_219V_1(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.814A{2-[benzyl-(3-cyclopentylpropionyl)-MS[M+1]+: 633amino]ethoxy}phenyl)propionic acidmethyl esterIIa_220V_2(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.246A{3-[benzyl-(3-cyclopentylpropionyl)-MS[M+1]+: 605amino]propoxy}phenyl)propionic acidmethyl esterIIa_221V_1(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 8.885A[2-MS[M+1]+: 577(benzylcyclopropanecarbonylamino)-ethoxy]phenyl}propionic acid methylesterIIa_222V_2(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 8.969A[3-MS[M+1]+: 591(benzylcyclopropanecarbonylamino)-propoxy]phenyl}propionic acidmethyl esterIIa_223V_1(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 8.784A[2-(benzylpropionylamino)ethoxy]-MS[M+1]+: 565phenyl}propionic acid methyl esterIIa_224V_2(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 8.858A[3-(benzylpropionylamino)propoxy]-MS[M+1]+: 579phenyl}propionic acid methyl esterIIa_225V_1(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.02A[2-(benzylisobutyrylamino)ethoxy]-MS[M+1]+: 579phenyl}propionic acid methyl esterIIa_226V_2(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.091A[3-(benzylisobutyrylamino)propoxy]-MS[M+1]+: 593phenyl}propionic acid methyl esterIIa_227V_1(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.511A[2-(benzylhexanoylamino)ethoxy]-MS[M+1]+: 607phenyl}propionic acid methyl esterIIa_228V_2(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.108A[3-(benzylhexanoylamino)propoxy]-MS[M+]+: 593phenyl}propionic acid methyl esterIIa_229V_1(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.261A[2-(benzylpentanoylamino)ethoxy]-MS[M+1]+: 593phenyl}propionic acid methyl esterIIa_230V_2(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.337A[3-(benzylpentanoylamino)propoxy]-MS[M+1]+: 607phenyl}propionic acid methyl esterIIa_231V_1(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 10.027A[2-(benzyloctanoylamino)ethoxy]-MS[M+1]+: 635phenyl}propionic acid methyl esterIIa_232V_2(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 10.092A[3-(benzyloctanoylamino)propoxy]-MS[M+1]+: 649phenyl}propionic acid methyl esterIIa_233V_1(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.763A[2-(benzylheptanoylamino)ethoxy]-MS[M+1]+: 621phenyl}propionic acid methyl esterIIa_234V_2(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.829A[3-(benzylheptanoylamino)propoxy]-MS[M+1]+: 635phenyl}propionic acid methyl esterIIa_235V_1(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 10.341A[2-(benzylnonanoylamino)ethoxy]-MS[M+1]+: 649phenyl}propionic acid methyl esterIIa_236V_2(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 10.403A[3-(benzylnonanoylamino)propoxy]-MS[M+1]+: 663phenyl}propionic acid methyl esterIIa_237V_1(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.045A[2-(benzylbutyrylamino)ethoxy]-MS[M+1]+: 579phenyl}propionic acid methyl esterIIa_238V_2(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.873A[3-(benzylbutyrylamino)propoxy]-MS[M+1]+: 647phenyl}propionic acid methyl esterIIa_239V_1(S)-3-{4-[2-(Benzoylbenzylamino)-8.90(d, 1H), 7.59(d,Aethoxy]phenyl}-2-(2-2H), 7.51-7.15(ca,benzoylphenylamino)propionic acid17H), 6.85-6.56(ca,methyl ester4H), 4.87, 4.67(2×s,2H, rotamers mixture),4.39(q, 1H),4.24-3.56(ca, 7H),3.25-3.08(ca, 2H)IIa_240V_2(S)-3-{4-[3-(Benzoylbenzylamino)-8.90(bs, 1H), 7.59(d,Apropoxy]phenyl}-2-(2-2H), 7.51-7.14(ca,benzoylphenylamino)propionic acid17H), 6.83-6.55(ca,methyl ester4H), 4.80, 4.51(2×s,2H, rotamers mixture),4.38(m, 1H),4.00-3.38(ca, 7H),3.23(dd, 1H), 3.11(dd, 1H)IIa_241V_1(S)-2-(2-Benzoylphenylamino)-3-(4-8.90(d, 1H), 7.77(m,A{2-[benzyl-(3-phenylacryloyl)amino]-1H), 7.59(d, 2H),ethoxy}phenyl)propionic acid methyl7.50-7.05(ca, 18H),ester6.85-6.73(ca, 2H),6.64-6.55(ca, 2H),4.86, 4.81(2×s, 2H,rotamers mixture),4.38(q, 1H), 4.20,4.03(2×t, 2H,rotamers mixture),3.85-3.68(ca, 5H),3.23-3.08(ca, 2H)IIa_242V_2(S)-2-(2-Benzoylphenylamino)-3-(4-8.91(d, 1H), 7.75(m,A{3-[benzyl-(3-phenylactyloyl)amino]-1H), 7.59-7.16(ca,propoxy}phenyl)propionic acid19H), 7.03-6.79(ca,methyl ester2H), 6.64-6.55(ca,2H), 4.73, 4.69(2×s,2H, rotamers mixture),4.38(q, 1H),3.98-3.91(ca, 2H),3.69-3.59(ca, 5H),3.23-3.08(ca, 2H),2.12-2.01(ca, 2H)IIa_243V_1(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.363A{2-[benzyl-(2,2-dimethylpropionyl)-MS[M+1]+: 593amino]ethoxy}phenyl)propionic acidmethyl esterIIa_244V_2(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.411A{3-[benzyl-(2,2-dimethylpropionyl)-MS[M+1]+: 607amino]propoxy}phenyl)propionic acidmethyl esterIIa_245V_3(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.408A{2-[cyclohexyl-(3-furan-2-ylacryloyl)-MS[M+1]+: 621amino]ethoxy}phenyl)propionic acidmethyl esterIIa_246V_3(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.655A[2-MS[M+1]+: 583(cyclobutanecarbonylcyclohexylamino)ethoxy]phenyl}propionic acidmethyl esterIIa_247V_3(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 10.336A{2-[cyclohexyl-(3-MS[M+1]+: 625cyclopentylpropionyl)amino]ethoxy}-phenyl)propionic acid methyl esterIIa_248V_3(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.459A[2-(butyrylcyclohexylamino)ethoxy]-MS[M+1]+: 571phenyl}propionic acid methyl esterIIa_249V_5(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.272A{2-[cyclopropylmethyl(naphthalene-MS[M+1]+: 6272-carbonyl)amino]ethoxy}phenyl)-propionic acid methyl esterIIa_250V_6(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.351A{3-[cyclopropylmethyl(naphthalene-MS[M+1]+: 6412-carbonyl)amino]propoxy}phenyl)-propionic acid methyl esterIIa_251V_5(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.005A{2-[cyclopropylmethyl(quinoline-2-MS[M+1]+: 628carbonyl)amino]ethoxy}phenyl)-propionic acid methyl esterIIa_252V_6(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.065A{3-[cyclopropylmethyl(quinoline-2-MS[M+1]+: 642carbonyl)amino]propoxy}phenyl)-propionic acid methyl esterIIa_253V_5(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.896A{2-[cyclopropylmethyl(quinoxaline-2-MS[M+1]+: 629carbonyl)amino]ethoxy}phenyl)-propionic acid methyl esterIIa_254V_6(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.003A{3-[cyclopropylmethyl(quinoxaline-2-MS[M+1]+: 643carbonyl)amino]propoxy}phenyl)-propionic acid methyl esterIIa_255V_5(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.871A{2-[cyclopropylmethyl(thiophene-2-MS[M+1]+: 583carbonyl)amino]ethoxy}phenyl)-propionic acid methyl esterIIa_256V_6(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.976A{3-[cyclopropylmethyl(thiophene-2-MS[M+1]+: 597carbonyl)amino]propoxy}phenyl)-propionic acid methyl esterIIa_257V_5(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 7.92A{2-[cyclopropylmethyl(pyridine-3-MS[M+1]+: 578carbonyl)amino]ethoxy}phenyl)-propionic acid methyl esterIIa_258V_6(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.062A{3-[cyclopropylmethyl(pyridine-3-MS[M+1]+: 592carbonyl)amino]propoxy}phenyl)-propionic acid methyl esterIIa_259V_5(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 8.958A[2-MS[M+1]+: 591(cyclopropylmethylphenylacetylamino)ethoxy]phenyl}propionic acidmethyl esterIIa_260V_6(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.053A[3-MS[M+1]+: 605(cyclopropylmethylphenylacetylamino)propoxy]phenyl}propionic acidmethyl esterIIa_261V_5(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.833A{2-[cyclopropylmethyl-(3-furan-2-MS[M+1]+: 593ylacryloyl)amino]ethoxy}phenyl)-propionic acid methyl esterIIa_262V_6(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.934A{3-[cyclopropylmethyl-(3-furan-2-MS[M+1]+: 607ylacryloyl)amino]propoxy}phenyl)-propionic acid methyl esterIIa_263V_5(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.003A{2-[cyclopropylmethyl-(3-thiophen-2-MS[M+1]+: 609ylacryloyl)amino]ethoxy}phenyl)-propionic acid methyl esterIIa_264V_6(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.11A{3-[cyclopropylmethyl-(3-thiophen-2-MS[M+1]+: 623ylacryloyl)amino]propoxy}phenyl)-propionic acid methyl esterIIa_265V_5(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.864A{2-[cyclopropylmethyl-(2-thiophen-2-MS[M+1]+: 597ylacetyl)amino]ethoxy}phenyl)-propionic acid methyl esterIIa_266V_6(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.96A{3-[cyclopropylmethyl-(2-thiophen-2-MS[M+1]+: 611ylacetyl)amino]propoxy}phenyl)-propionic acid methyl esterIIa_267V_5(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.836A{2-[cyclopropylmethyl-(2-thiophen-3-MS[M+1]+: 597ylacetyl)amino]ethoxy}phenyl)-propionic acid methyl esterIIa_268V_6(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.929A{3-[cyclopropylmethyl-(2-thiophen-3-MS[M+1]+: 611ylacetyl)amino]propoxy}phenyl)-propionic acid methyl esterIIa_269V_5(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 6.894A{2-[cyclopropylmethyl-(3-pyridin-3-MS[M+1]+: 606ylpropionyl)amino]ethoxy}phenyl)-propionic acid methyl esterIIa_270V_6(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 6.961A{3-[cyclopropylmethyl-(3-pyridin-3-MS[M+1]+: 620ylpropionyl)amino]propoxy}phenyl)-propionic acid methyl esterIIa_271V_5(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.169A{2-[cyclopropylmethyl-(3-MS[M+1]+: 605phenylpropionyl)amino]ethoxy}-phenyl)propionic acid methyl esterIIa_272V_6(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.244A{3-[cyclopropylmethyl-(3-MS[M+1]+: 619phenylpropionyl)amino]propoxy}-phenyl)propionic acid methyl esterIIa_273V_5(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 8.977A[2-MS[M+1]+: 555(cyclobutanecarbonylcyclopropylmethylamino)ethoxy]phenyl}propionicacid methyl esterIIa_274V_6(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.059A[3-MS[M+1]+: 569(cyclobutanecarbonylcyclopropylmethylamino)propoxy]phenyl}propionicacid methyl esterIIa_275V_5(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.641A{2-[(2-cyclohexylacetyl)-MS[M+1]+: 597cyclopropylmethylamino]ethoxy}-phenyl)propionic acid methyl esterIIa_276V_6(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.707A{3-[(2-cyclohexylacetyl)-MS[M+1]+: 611cyclopropylmethylamino]propoxy}-phenyl)propionic acid methyl esterIIa_277V_5(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.201A[2-MS[M+1]+: 569(cyclopentanecarbonylcyclopropylmethylamino)ethoxy]phenyl}propionicacid methyl esterIIa_278V_6(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.285A[3-MS[M+1]+: 583(cyclopentanecarbonylcyclopropylmethylamino)propoxy]phenyl}propionicacid methyl esterIIa_279V_5(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 8.641A[2-MS[M+1]+: 541(cyclopropanecarbonylcyclopropylmethylamino)ethoxy]phenyl}propaonicacid methyl esterIIa_280V_6(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 8.747A[3-MS[M+1]+: 555(cyclopropanecarbonylcyclopropylmethylamino)propoxy]phenyl}propaonicacid methyl esterIIa_281V_5(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 8.525A[2-MS[M+1]+: 529(cyclopropylmethylpropionylamino)-ethoxy]phenyl}propionic acid methylesterIIa_282V_6(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 8.626A[3-MS[M+1]+: 543(cyclopropylmethylpropionylamino)-propoxy]phenyl}propionic acidmethyl esterIIa_283V_5(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 8.791A[2-MS[M+1]+: 543(cyclopropylmethylisobutyrylamino)-ethoxy]phenyh}propionic acid methylesterIIa_284V_6(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 8.895A[3MS[M+1]+: 557(cyclopropylmethylisobutyrylamino)-propoxy]phenyl}propionic acidmethyl esterIIa_285V_5(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 8.813A[2-(butyrylcyclopropylmethylamino)-MS[M+1]+: 543ethoxy]phenyl}propionic acid methylesterIIa_286V_6(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 8.903A[3-(butyrylcyclopropylmethylamino)-MS[M+1]+: 557propoxy]phenyl}propionic acidmethyl esterIIa_287V_5(S)-3-{4-[2-rt: 8.858A(Benzoylcyclopropylmethylamino)-MS[M+1]+: 577ethoxy]phenyl}-2-(2-benzoylphenylamino)propionic acidmethyl esterIIa_288V_6(S)-3-{4-[3-rt: 8.958A(Benzoylcyclopropylmethylamino)-MS[M+1]+: 591propoxy]phenyl}-2-(2-benzoylphenylamino)propionic acidmethyl esterIIa_289V_5(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.085A{2-[cyclopropylmethyl-(3-MS[M+1]+: 602phenylacryloyl)amino]ethoxy}-phenyl)propionic acid methyl esterIIa_290V_6(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.182A{3-[cyclopropylmethyl-(3-MS[M+1]+: 617phenylacryloyl)amino]propoxy}-phenyl)propionic acid methyl esterIIa_291V_9(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.13A{2-[(naphthalene-1-carbonyl)-MS[M+1]+: 649phenylamino]ethoxy}phenyl)-propionic acid methyl esterIIa_292V_10(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.283A{3-[(naphthalene-1-carbonyl)-MS[M+1]+: 663phenylamino]propoxy}phenyl)-propionic acid methyl esterIIa_293V_9(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.315A{2-[(naphthalene-2-carbonyl)-MS[M+1]+: 649phenylamino]ethoxy}phenyl)-propionic acid methyl esterIIa_294V_10(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.429A{3-[(naphthalene-2-carbonyl)-MS[M+1]+: 663phenylamino]propoxy}phenyl)-propionic acid methyl esterIIa_295V_9(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.904A{2-[phenyl(quinoline-2-carbonyl)-MS[M+1]+: 650amino]ethoxy}phenyl)propionic acidmethyl esterIIa_296V_10(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.023A{3-[phenyl(quinoline-2-carbonyl)-MS[M+1]+: 664amino]propoxy}phenyl)propionic acidmethyl esterIIa_297V_9(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.817A{2-[phenyl(quinoxaline-2-carbonyl)-MS[M+1]+: 651amino]ethoxy}phenyl)propionic acidmethyl esterIIa_298V_10(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.976A{3-[phenyl(quinoxaline-2-carbonyl)-MS[M+1]+: 665amino]propoxy}phenyl)propionic acidmethyl esterIIa_299V_9(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.049A{2-[phenyl(thiophene-2-carbonyl)-MS[M+1]+: 605amino]ethoxy}phenyl)propionic acidmethyl esterIIa_300V_10(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.155A{3-[phenyl(thiophene-2-carbonyl)-MS[M+1]+: 619amino]propoxy}phenyl)propionic acidmethyl esterIIa_301V_9(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.746A{2-[(isoquinoline-3-carbonyl)-MS[M+1]+: 650phenylamino]ethoxy}phenyl)-propionic acid methyl esterIIa_302V_9(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.086A{2-[phenyl(pyridine-3-carbonyl)-MS[M+1]+: 600amino]ethoxy}phenyl)propionic acidmethyl esterIIa_303V_10(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.264A{3-[phenyl(pyridine-3-carbonyl)-MS[M+1]+: 614amino]propoxy}phenyl)propionic acidmethyl esterIIa_304V_9(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 7.934A{2-[phenyl(pyridine-4-carbonyl)-MS[M+1]+: 600amino]ethoxy}phenyl)propionic acidmethyl esterIIa_305V_10(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.124A{3-[phenyl(pyridine-4-carbonyl)-MS[M+1]+: 614amino]propoxy}phenyl)propionic acidmethyl esterIIa_306V_9(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.22A[2-(phenylphenylacetylamino)-MS[M+1]+: 613ethoxy]phenyl}propionic acid methylesterIIa_307V_10(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.363A[3-(phenylphenylacetylamino)-MS[M+1]+: 627propoxy]phenyl}propionic acidmethyl esterIIa_308V_9(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.799A{2-[(2-methylacryloyl)phenylamino]-MS[M+1]+: 563ethoxy}phenyl)propionic acid methylesterIIa_309V_10(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.943A{3-[(2-methylacryloyl)phenylamino]-MS[M+1]+: 577propoxy}phenyl)propionic acidmethyl esterIIa_310V_9(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.245A{2-[phenyl-(3-phenylpropynoyl)-MS[M+1]+: 615amino]ethoxy}phenyl)propionic acidmethyl esterIIa_311V_9(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.5A{2-[(2-ethylbutyryl)phenylamino]-MS[M+1]+: 593ethoxy}phenyl)propionic acid methylesterIIa_312V_10(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.628A{3-[(2-ethylbutyryl)phenylamino]-MS[M+1]+: 607propoxy}phenyl)propionic acidmethyl esterIIa_313V_9(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.025A{2-[(3-furan-2-ylacryloyl)-MS[M+1]+: 615phenylamino]ethoxy}phenyl)-propionic acid methyl esterIIa_314V_10(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.164A{3-[(3-furan-2-ylacryloyl)-MS[M+1]+: 629phenylamino]propoxy}phenyl)-propionic acid methyl esterIIa_315V_9(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.267A{2-[phenyl-(3-thiophen-2-ylacryloyl)-MS[M+1]+: 631amino]ethoxy}phenyl)propionic acidmethyl esterIIa_316V_10(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.394A{3-[phenyl-(3-thiophen-2-ylacryloyl)-MS[M+1]+: 645amino]propoxy}phenyl)propionic acidmethyl esterIIa_317V_9(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.954A{2-[(3-furan-3-yl-(E)-acryloyl)-MS[M+1]+: 615phenylamino]ethoxy}phenyl)-propionic acid methyl esterIIa_318V_10(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.091A{3-[(3-furan-3-yl-(E)-acryloyl)-MS[M+1]+: 629phenylamino]propoxy}-phenyl)-propionic acid methyl esterIIa_319V_9(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.103A{2-[phenyl-(3-pyridin-3-yl-(E)-MS[M+1]+: 626acryloyl)amino]ethoxy}phenyl)-propionic acid methyl esterIIa_320V_10(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.293A{3-[phenyl-(3-pyridin-3-yl-(E)-MS[M+1]+: 640acryloyl)amino]propoxy}phenyl)-propionic acid methyl esterIIa_321V_9(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.213A{2-[phenyl-(3-thiophen-3-yl-(E)-MS[M+1]+: 631acryloyl)amino]ethoxy}phenyl)-propionic acid methyl esterIIa_322V_10(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.334A{3-[phenyl-(3-thiophen-3-yl-(E)-MS[M+1]+: 645acryloyl)amino]propoxy}phenyl)-propionic acid methyl esterIIa_323V_10(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 9A[3-(but-2-(E)-enoylphenylamino)-MS[M+1]+: 577propoxy]phenyl}propionic acidmethyl esterIIa_324V_9(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.132{2-[phenyl-(2-thiophen-2-ylacetyl)-MS[M+1]+: 619amino]ethoxy}phenyl)propionic acidmethyl esterIIa_325V_10(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.295A{3-[phenyl-(2-thiophen-2-ylacetyl)-MS[M+1]+: 633amino]propoxy}phenyl)propionic acidmethyl esterIIa_326V_10(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.23A{3-[phenyl-(2-thiophen-3-ylacetyl)-MS[M+1]+: 633amino]propoxy}phenyl)propionic acidmethyl esterIIa_327V_9(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.587A{2-[(3,3-dimethylbutyryl)-MS[M+1]+: 593phenylamino]ethoxy}phenyl)-propionic acid methyl esterIIa_328V_10(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.706A{3[(3,3-dimethylbutryl)-MS[M+1]+: 607phenylamino]propoxy}phenyl)-propionic acid methyl esterIIa_329V_9(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.271A{2-[(3-methylbutyryl)phenylamino]-MS[M+1]+: 579ethoxy}phenyl)propionic acid methylesterIIa_330V_10(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.401A{3-[(3-methylbutyryl)phenylamino]-MS[M+1]+: 593propoxy}phenyl)propionic acidmethyl esterIIa_331V_9(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 7.038A{2-[phenyl-(3-pyridin-3-ylpropionyl)-MS[M+1]+: 627amino]ethoxy}phenyl)propionic acidmethyl esterIIa_332V_10(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 7.229A{3-[phenyl-(3-pyridin-3-ylpropionyl)-MS[M+1]+: 641amino]propoxy}phenyl)propionic acidmethyl esterIIa_333V_9(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.078A[2-(pent-4-enoylphenylamino)-MS[M+1]+: 577ethoxy]phenyl}propionic acid methylesterIIa_334V_10(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.212A[3-(pent-4-enoylphenylamino)-MS[M+1]+: 591propoxy]phenyl}propionic acidmethyl esterIIa_335V_9(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.369A{2-[phenyl-(3-phenylpropionyl)-MS[M+1]+: 627amino]ethoxy}phenyl)propionic acidmethyl esterIIa_336V_10(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.494A{3-[phenyl-(3-phenylpropionyl)-MS[M+1]+: 641amino]propoxy}phenyl)propionic acidmethyl esterIIa_337V_9(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.203A[2-MS[M+1]+: 577(cyclobutanecarbonylphenylamino)-ethoxy]phenyl}propionic acid methylesterIIa_338V_10(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.333A[3-MS[M+1]+: 591(cyclobutanecarbonylphenylamino)-propoxy]phenyl}propionic acidmethyl esterIIa_339V_9(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.602A[2-MS[M+1]+: 605(cyclohexanecarbonylphenylamino)-ethoxy]phenyl}propionic acid methylesterIIa_340V_10(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.708A[3-MS[M+1]+: 619(cyclohexanecarbonylphenylamino)-propoxy]phenyl}propionic acidmethyl esterIIa_341V_9(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 10.166A{2-[(3-cyclohexylpropionyl)-MS[M+1]+: 633phenylamino]ethoxy}phenyl)-propionic acid methyl esterIIa_342V_10(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 10.282A{3-[(3-cyclohexylpropionyl)-MS[M+1]+: 647phenylamino]propoxy}phenyl)-propionic acid methyl esterIIa_343V_9(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.883A{2-[(2-cyclohexylacetyl)-MS[M+1]+: 619phenylamino]ethoxy}phenyl)-propionic acid methyl esterIIa_344V_10(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 10A{3-[(2-cyclohexylacetyl)-MS[M+1]+: 633phenylamino]propoxy}phenyl)-propionic acid methyl esterIIa_345V_9(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.463A[2-MS[M+1]+: 591(cyclopentanecarbonylphenylamino)-ethoxy]phenyl}propionic acid methylesterIIa_346V_10(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.582A[3-MS[M+1]+: 605(cyclopentanecarbonylphenylamino)-propoxy]phenyl}propionic acidmethyl esterIIa_347V_9(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.87A{2-[(3-cyclopentylpropionyl)-MS[M+1]+: 619phenylamino]ethoxy}phenyl)-propionic acid methyl esterIIa_348V_10(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.98A{3-[(3-cyclopentylpropionyl)-MS[M+1]+: 633phenylamino]propoxy}phenyl)-propionic acid methyl esterIIa_349V_9(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 8.91A[2-MS[M+1]+: 563(cyclopropanecarbonylphenylamino)-ethoxy]phenyl}propionic acid methylesterIIa_350V_10(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.06A[3-MS[M+1]+: 577(cyclopropanecarbonylphenylamino)-propoxy]phenyl}propionic acidmethyl esterIIa_351V_9(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 8.78A[2-(phenylpropionylamino)ethoxy]-MS[M+1]+: 551phenyl}propionic acid methyl esterIIa_352V_10(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 8.925A[3-(phenylpropionylamino)propoxy]-MS[M+1]+: 565phenyl}propionic acid methyl esterIIa_353V_9(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.033A[2-(isobutyrylphenylamino)ethoxy]-MS[M+1]+: 565phenyl}propionic acid methyl esterIIa_354V_10(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.168A[3-(isobutyrylphenylamino)propoxy]-MS[M+1]+: 579phenyl}propionic acid methyl esterIIa_355V_9(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.56A[2-(hexanoylphenylamino)ethoxy]-MS[M+1]+: 593phenyl}propionic acid methyl esterIIa_356V_10(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.671A[3-(hexanoylphenylamino)propoxy]-MS[M+1]+: 607phenyl}propionic acid methyl esterIIa_357V_9(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.298A[2-(pentanoylphenylamino)ethoxy]-MS[M+1]+: 579phenyl}propionic acid methyl esterIIa_358V_10(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.421A[3-(pentanoylphenylamino)propoxy]-MS[M+1]+: 593phenyl}propionic acid methyl esterIIa_359V_9(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 10.11A[2-(octanoylphenylamino)ethoxy]-MS[M+1]+: 621phenyl}propionic acid methyl esterIIa_360V_10(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 10.224A[3-(octanoylphenylamino)propoxy]-MS[M+1]+: 635phenyl}propionic acid methyl esterIIa_361V_9(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.825A[2-(heptanoylphenylamino)ethoxy]-MS[M+1]+: 607phenyl}propionic acid methyl esterIIa_362V_10(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.933A[3-(heptanoylphenylamino)propoxy]-MS[M+1]+: 621phenyl}propionic acid methyl esterIIa_363V_9(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 10.455A[2-(nonanoylphenylamino)ethoxy]-MS[M+1]+: 635phenyl}propionic acid methyl esterIIa_364V_10(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 10.588A[3-(nonanoylphenylamino)propoxy]-MS[M+1]+: 649phenyl}propionic acid methyl esterIIa_365V_9(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.043A[2-(butyrylphenylamino)ethoxy]-MS[M+1]+: 565phenyl}propionic acid methyl esterIIa_366V_10(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.18A[3-(butyrylphenylamino)propoxy]-MS[M+1]+: 579phenyl}propionic acid methyl esterIIa_367V_9(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 8.97A[2-(benzoylphenylamino)ethoxy]-MS[M+1]+: 599phenyl}propionic acid methyl esterIIa_368V_10(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.121A[3-(benzoylphenylamino)propoxy]-MS[M+1]+: 613phenyl}propionic acid methyl esterIIa_369V_9(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.383A{2-[phenyl-(3-phenylacryloyl)amino]-MS[M+1]+: 625ethoxy}phenyl)propionic acid methylesterIIa_370V_10(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.51A{3-[phenyl-(3-phenylacryloyl)amino]-MS[M+1]+: 639propoxy}phenyl)propionic acidmethyl esterIIa_371V_9(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.402A{2-[(2,2-dimethylpropionyl)-MS[M+1]+: 579phenylamino]ethoxy}phenyl)-propionic acid methyl esterIIa_372V_10(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.5A{3-[(2,2-dimethylpropionyl)-MS[M+1]+: 593phenylamino]propoxy}phenyl)-propionic acid methyl esterIIa_373V_4(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.256A[2-(tert-MS[M+1]+: 557butylcyclobutanecarbonylamino)-ethoxy]phenyl}propionic acid methylesterIIa_374V_4(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.917A{2-[tert-butyl-(3-MS[M+1]+: 599cyclopentylpropionyl)amino]ethoxy}-phenyl)propionic acid methyl esterIIa_375V_26(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.214A{2-[(2-methylacryloyl)naphthalen-1-MS[M+1]+: 613ylamino]ethoxy}phenyl)propionicacid methyl esterIIa_376V_26(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.276A[2-(but-2-(E)-enoylnaphthalen-1-MS[M+1]+: 613ylamino)ethoxy]phenyl}propionicacid methyl esterIIa_377V_26(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.336A[2-MS[M+1]+: 613(cyclopropanecarbonylnaphthalen-1-ylamino)ethoxy]phenyl}propionicacid methyl esterIIa_378V_26(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.273A[2-(naphthalen-1-ylpropionylamino)-MS[M+1]+: 601ethoxy]phenyl}propionic acid methylesterIIa_379V_30(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.261A{2-[(2-methylacryloyl)naphthalen-2-MS[M+1]+: 613ylamino]ethoxy}phenyl)propionicacid methyl esterIIa_380V_30(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.355A[2-(but-2-(E)-enoylnaphthalen-2-MS[M+1]+: 613ylamino)ethoxy]phenyl}propionicacid methyl esterIIa_381V_30(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.269A[2-(naphthalen-2-ylpropionylamino)-MS[M+1]+: 601ethoxy]phenyl}propionic acid methylesterIIa_382V_30(S)-3-{4-[2-(Acetylnaphthalen-2-rt: 8.914Aylamino)ethoxy]phenyl}-2-(2-MS[M+1]+: 587benzoylphenylamino)propionic acidmethyl esterIIa_383V_27(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.054A{2-[(2-methylacryloyl)-(3-MS[M+1]+: 609methylsulfanylphenyl)amino]ethoxy}-phenyl)propionic acid methyl esterIIa_384V_27(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.126A{2-[but-2-(E)-enoyl-(3-MS[M+1]+: 609methylsulfanylphenyl)amino]ethoxy}-phenyl)propionic acid methyl esterIIa_385V_27(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.28A{2-[butyryl-(3-methylsulfanylphenyl)-MS[M+1]+: 611amino]ethoxy}phenyl)propionic acidmethyl esterIIa_386V_28(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.051A{2-[(2-methylacryloyl)-(4-MS[M+1]+: 609methylsulfanylphenyl)amino]ethoxy}-phenyl)propionic acid methyl esterIIa_387V_28(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.134A{2-[but-2-(E)-enoyl-(4-MS[M+1]+: 609methylsulfanylphenyl)amino]ethoxy}-phenyl)propionic acid methyl esterIIa_388V_28(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.284A{2-[isobutyryl-(4-MS[M+1]+: 611methylsulfanylphenyl)amino]ethoxy}-phenyl)propionic acid methyl esterIIa_389V_28(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.284A{2-[butyryl-(4-methylsulfanylphenyl)-MS[M+1]+: 611amino]ethoxy}phenyl)propionic acidmethyl esterIIa_390V_26(S)-3-{4-[2-(Acetylnaphthalen-1-rt: 8.903Aylamino)ethoxy]phenyl}-2-(2-MS[M+1]+: 587benzoylphenylamino)propionic acidmethyl esterIIa_391V_30(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.387A[2-MS[M+1]+: 613(cyclopropanecarbonylnaphthalen-2-ylamino)ethoxy]phenyl}propionicacid methyl esterIIa_392V_31(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.23A{3-[butyryl-(2-fluorophenyl)amino]-MS[M+1]+: 597propoxy}phenyl)propionic acidmethyl esterIIa_393V_31(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.355A{3-[cyclobutanecarbonyl-(2-MS[M+1]+: 609fluorophenyl)amino]propoxy}phenyl)-propionic acid methyl esterIIa_394V_31(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.056A{3-[cyclopropanecarbonyl-(2-MS[M+1]+: 595fluorophenyl)amino]propoxy}phenyl)-propionic acid methyl esterIIa_395V_31(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.219A{3-[(2-fluorophenyl)isobutyrylamino]-MS[M+1]+: 597propoxy}phenyl)propionic acidmethyl esterIIa_396V_1(S)-3-{4-[2-(Acryloylbenzylamino)-rt: 8.639Aethoxy]phenyl}-2-(2-MS[M+1]+: 563benzoylphenylamino)propionic acidmethyl esterIIa_397V_2(S)-3-{4-[3-(Acryloylbenzylamino)-rt: 8.747Apropoxy]phenyl}-2-(2-MS[M+1]+: 577benzoylphenylamino)propionic acidmethyl esterIIa_398V_9(S)-3-{4-[2-(Acryloylphenylamino)-rt: 8.693Aethoxy]phenyl}-2-(2-MS[M+1]+: 549benzoylphenylamino)propionic acidmethyl esterIIa_399V_10(S)-3-{4-[2-(Acryloylphenylamino)-rt: 8.842Apropoxy]phenyl}-2-(2-MS[M+1]+: 563benzoylphenylamino)propionic acidmethyl esterIIa_400V_31(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.986A{3-[(2-fluorophenyl)propionylamino]-MS[M+1]+: 583propoxy}phenyl)propionic acidmethyl esterIIa_401V_31(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.279A{3-[(2-fluorophenyl)pent-4-MS[M+1]+: 609enoylamino]propoxy}phenyl)-propionic acid methyl esterIIa_402V_31(S)-3-(4-{3-[Acryloyl-(2-rt: 8.87Afluorophenyl)amino]propoxy}phenyl)-MS[M+1]+: 5812-(2-benzoylphenylamino)propionicacid methyl esterIIa_403V_31(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.009A{3-[but-2-(E)-enoyl-(2-fluorophenyl)-MS[M+1]+: 595amino]propoxy}phenyl)propionic acidmethyl esterIIa_404V_31(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.45A{3-[(2-fluorophenyl)-(3-MS[M+1]+: 611methylbutyryl)amino]propoxy}-phenyl)propionic acid methyl esterIIa_405V_29(R)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.023A{2-[phenyl(thiophene-2-carbonyl)-MS[M+1]+: 605amino]ethoxy}phenyl)propionic acidmethyl esterIIa_406V_31(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.048A{3-[(2-fluorophenyl)-(2-MS[M+1]+: 595methylacryloyl)amino]propoxy}-phenyl)propionic acid methyl esterIIa_407V_32(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.025A{3-[(3-fluorophenyl)-(2-MS[M+1]+: 595methylacryloyl)amino]propoxy}-phenyl)propionic acid methyl esterIIa_408V_34(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.84A{2-[but-2-(E)-enoyl-(2-MS[M+1]+: 593methoxyphenyl)amino]ethoxy}-phenyl)propionic acid methyl esterIIa_409V_35(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.852A{2-[but-2-(E)-enoyl-(3-MS[M+1]+: 593methoxyphenyl)amino]ethoxy}-phenyl)propionic acid methyl esterIIa_410V_34(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.303A{2-[(2-methoxyphenyl)-(3-MS[M+1]+: 609methylbutyryl)amino]ethoxy}phenyl)-propionic acid methyl esterIIa_411V_32(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.436A{3-[(3-fluorophenyl)-(3-MS[M+1]+: 611methylbutyryl)amino]propoxy}-phenyl)propionic acid methyl esterIIa_412V_35(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.243A{2-[(3-methoxyphenyl)-(3-MS[M+1]+: 609methylbutyryl)amino]ethoxy}phenyl)-propionic acid methyl esterIIa_413V_32(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.262A{3-[(3-fluorophenyl)pent-4-MS[M+1]+: 609enoylamino]propoxy}phenyl)-propionic acid methyl esterIIa_414V_32(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.353A{3-[cyclobutanecarbonyl-(3-MS[M+1]+: 609fluorophenyl)amino]propoxy}phenyl)-propionic acid methyl esterIIa_415V_33(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.338A{3-[cyclobutanecarbonyl-(4-MS[M+1]+: 609fluorophenyl)amino]propoxy}phenyl)-propionic acid methyl esterIIa_416V_29(R)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.207A[2-MS[M+1]+: 577(cyclobutanecarbonylphenylamino)-ethoxy]phenyl}propionic acid methylesterIIa_417V_34(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.891A{2-[cyclopropanecarbonyl-(2-MS[M+1]+: 593methoxyphenyl)amino]ethoxy}-phenyl)propionic acid methyl esterIIa_418V_32(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.103A{3-[cyclopropanecarbonyl-(3-MS[M+1]+: 595fluorophenyl)amino]propoxy}phenyl)-propionic acid methyl esterIIa_419V_33(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.082A{3-[cyclopropanecarbonyl-(4-MS[M+1]+: 595fluorophenyl)amino]propoxy}phenyl)-propionic acid methyl esterIIa_420V_34(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.817A{2-[(2-methoxyphenyl)-MS[M+1]+: 581propionylamino]ethoxy}phenyl)-propionic acid methyl esterIIa_421V_32(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.976A{3-[(3-fluorophenyl)propionylamino]-MS[M+1]+: 583propoxy}phenyl)propionic acidmethyl esterIIa_422V_35(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.766A{2-[(3-methoxyphenyl)-MS[M+1]+: 581propionylamino]ethoxy}phenyl)-propionic acid methyl esterIIa_423V_33(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.958A{3-[(4-fluorophenyl)propionylamino]-MS[M+1]+: 583propoxy}phenyl)propionic acidmethyl esterIIa_424V_29(R)-2-(2-Benzoylphenylamino)-3-{4-rt: 8.783A[2-(phenylpropionylamino)ethoxy]-MS[M+1]+: 551phenyl}propionic acid methyl esterIIa_425V_32(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.206A{3-[(3-fluorophenyl)isobutyrylamino]-MS[M+1]+: 597propoxy}phenyl)propionic acidmethyl esterIIa_426V_35(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.011A{2-[isobutyryl-(3-methoxyphenyl)-MS[M+1]+: 595amino]ethoxy}phenyl)propionic acidmethyl esterIIa_427V_33(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.187A{3-[(4-fluorophenyl)isobutyrylamino]-MS[M+1]+: 597propoxy}phenyl)propionic acidmethyl esterIIa_428V_31(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.473A{3-[(2-fluorophenyl)pentanoylamino]-MS[M+1]+: 611propoxy}phenyl)propionic acidmethyl esterIIa_429V_32(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.455A{3-[(3-fluorophenyl)pentanoylamino]-MS[M+1]+: 611propoxy}phenyl)propionic acidmethyl esterIIa_430V_34(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.069A{2-[butyryl-(2-methoxyphenyl)amino]-MS[M+1]+: 595ethoxy}phenyl)propionic acid methylesterIIa_431V_32(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.227A{3-[butyryl-(3-fluorophenyl)amino]-MS[M+1]+: 597propoxy}phenyl)propionic acidmethyl esterIIa_432V_35(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.014A{2-[butyryl-(3-methoxyphenyl)amino]-MS[M+1]+: 595ethoxy}phenyl)propionic acid methylesterIIa_433V_33(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.202A{3-[butyryl-(4-fluorophenyl)amino]-MS[M+1]+: 597propoxy}phenyl)propionic acidmethyl esterIIa_434V_31(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.539A{3-[(2,2-dimethylpropionyl)-(2-MS[M+1]+: 611fluorophenyl)amino]propoxy}phenyl)-propionic acid methyl esterIIa_435V_34(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.411A{2-[(2,2-dimethylpropionyl)-(2-MS[M+1]+: 609methoxyphenyl)amino]ethoxy}-phenyl)propionic acid methyl esterIIa_436V_32(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.518A{3-[(2,2-dimethylpropionyl)-(3-MS[M+1]+: 611fluorophenyl)amino]propoxy}phenyl)-propionic acid methyl esterIIa_437V_35(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.367A{2-[(2,2-dimethylpropionyl)-(3-MS[M+1]+: 609methoxyphenyl)amino]ethoxy}-phenyl)propionic acid methyl esterIIa_438V_27(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.277A{2-[isobutyryl-(3-MS[M+1]+: 611methylsulfanylphenyl)amino]ethoxy}-phenyl)propionic acid methyl esterIIa_439V_37(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.92A{3-[(2-methoxyphenyl)-MS[M+1]+: 595propionylamino]propoxy}phenyl)-propionic acid methyl esterIIa_440V_37(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.154A{3-[cyclopropanecarbonyl-(2-MS[M+1]+: 609methoxyphenyl)amino]propoxy}-phenyl)propionic acid methyl esterIIa_441V_37(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.999A{3-[isobutyryl-(2-methoxyphenyl)-MS[M+1]+: 607amino]propoxy}phenyl)propionic acidmethyl esterIIa_442V_37(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.942A{3-[but-2-(E)-(enoyl-(2-MS[M+1]+: 607methoxyphenyl)amino]propoxy)-phenyl)propionic acid methyl esterIIa_443V_37(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.954A{3-[(2-methoxyphenyl)-(2-MS[M+1]+: 607methylacryloyl)amino]propoxy)-phenyl)propionic acid methyl esterIIa_444V_37(S)-3-(4-{3-[Acryloyl-(2-rt: 8.82Amethoxyphenyl)amino]propoxy}-MS[M+1]+: 593phenyl)-2-(2-benzoylphenylamino)-propionic acid methyl esterIIa_445V_37(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.161A{3-[butyryl-(2-methoxyphenyl)amino]-MS[M+1]+: 609propoxy}phenyl)propionic acidmethyl esterIIa_446V_38(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.904A{3-[(3-methoxyphenyl)-MS[M+1]+: 595propionylamino]propoxy}phenyl)-propionic acid methyl esterIIa_447V_38(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.029A{3-[cyclopropanecarbonyl-(3-MS[M+1]+: 607methoxyphenyl)amino]propoxy}-phenyl)propionic acid methyl esterIIa_448V_38(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.137A{3-[isobutyryl-(3-methoxyphenyl)-MS[M+1]+: 609amino]propoxy}phenyl)propionic acidmethyl esterIIa_449V_38(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.98A{3-[but-2-(E)-enoyl-(3-MS[M+1]+: 607methoxyphenyl)amino]propoxy}-phenyl)propionic acid methyl esterIIa_450V_38(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.923A{3-[(3-methoxyphenyl)-(2-MS[M+1]+: 607methylacryloyl)amino]propoxy}-phenyl)propionic acid methyl esterIIa_451V_38(S)-3-(4-{3-[Acryloyl-(3-rt: 8.845Amethoxyphenyl)amino]propoxy}-MS[M+1]+: 593phenyl)-2-(2-benzoylphenylamino)-propionic acid methyl esterIIa_452V_38(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.143A{3-[butyryl-(3-methoxyphenyl)amino]-MS[M+1]+: 609propoxy}phenyl)propionic acidmethyl esterIIa_453V_34(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.202A{2-[cyclobutanecarbonyl-(2-MS[M+1]+: 607methoxyphenyl)amino]ethoxy}-phenyl)propionic acid methyl esterIIa_454V_34(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.066A{2-[isobutyryl-(2-methoxyphenyl)-MS[M+1]+: 595amino]ethoxy}phenyl)propionic acidmethyl esterIIa_455V_26(S)-3-{4-[2-(Acryloylnaphthalen-1-rt: 9.145Aylamino)ethoxy]phenyl}-2-(2-MS[M+1]+: 599benzoylphenylamino)propionic acidmethyl esterIIa_456V_30(S)-3-{4-[2-(Acryloylnaphthalen-2-rt: 9.201Aylamino)ethoxy]phenyl}-2-(2-MS[M+1]+: 599benzoylphenylamino)propionic acidmethyl esterIIa_457V_27(S)-3-(4-{2-[Acryloyl-(3-rt: 8.979Amethylsulfanylphenyl)amino]ethoxy}-MS[M+1]+: 595phenyl)-2-(2-benzoylphenylamino)-propionic acid methyl esterIIa_458V_28(S)-3-(4-{2-[Acryloyl-(4-rt: 8.982Amethylsulfanylphenyl)amino]ethoxy}-MS[M+1]+: 595phenyl)-2-(2-benzoylphenylamino)-propionic acid methyl esterIIa_459V_32(S)-3-(4-{3-[Acryloyl-(3-rt: 8.908Afluorophenyl)amino]propoxy}phenyl)-MS[M+1]+: 5812-(2-benzoylphenylamino)propionicacid methyl esterIIa_460V_32(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.06A{3-[but-2-(E)-enoyl-(3-fluorophenyl)-MS[M+1]+: 595amino]propoxy}phenyl)propionic acidmethyl esterIIa_461V_34(S)-3-(4-{2-[Acryloyl-(2-rt: 8.709Amethoxyphenyl)amino]ethoxy}-MS[M+1]+: 579phenyl)-2-(2-benzoylphenylamino)-propionic acid methyl esterIIa_462V_34(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.85A{2-[(2-methoxyphenyl)-(2-MS[M+1]+: 593methylacryloyl)amino]ethoxy}-phenyl)propionic acid methyl esterIIa_463V_35(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.887A{2-[cyclopropanecarbonyl-(3-MS[M+1]+: 593methoxyphenyl)amino]ethoxy}-phenyl)propionic acid methyl esterIIa_464V_35(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.164A{2-[cyclobutanecarbonyl-(3-MS[M+1]+: 607methoxyphenyl)amino]ethoxy}-phenyl)propionic acid methyl esterIIa_465V_35(S)-3-(4-{2-[Acryloyl-(3-rt: 8.703Amethoxyphenyl)amino]ethoxy}-MS[M+1]+: 579phenyl)-2-(2-benzoylphenylamino)-propionic acid methyl esterIIa_466V_35(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.786A{2-[(3-methoxyphenyl)-(2-MS[M+1]+: 593methylacryloyl)amino]ethoxy}-phenyl)propionic acid methyl esterIIa_467V_36(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.001A{2-[ethyl(naphthalene-2-carbonyl)-MS[M+1]+: 601amino]ethoxy}phenyl)propionic acidmethyl esterIIa_468V_39(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.244A{2-[(naphthalene-2-carbonyl)-MS[M+1]+: 615propylamino]ethoxy}phenyl)propionicacid methyl esterIIa_469V_36(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.712A{2-[ethyl(quinoline-2-carbonyl)-MS[M+1]+: 602amino]ethoxy}phenyl)propionic acidmethyl esterIIa_470V_39(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.999A{2-[propyl(quinoline-2-carbonyl)-MS[M+1]+: 616amino]ethoxy}phenyl)propionic acidmethyl esterIIa_471V_36(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.595A{2-[ethyl(quinoxaline-2-carbonyl)-MS[M+1]+: 603amino]ethoxy}phenyl)propionic acidmethyl esterIIa_472V_39(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.888A{2-[propyl(quinoxaline-2-carbonyl)-MS[M+1]+: 617amino]ethoxy}phenyl)propionic acidmethyl esterIIa_473V_36(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.558A{2-[ethyl(thiophene-2-carbonyl)-MS[M+1]+: 557amino]ethoxy}phenyl)propionic acidmethyl esterIIa_474V_39(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.841A{2-[propyl(thiophene-2-carbonyl)-MS[M+1]+: 571amino]ethoxy}phenyl)propionic acidmethyl esterIIa_475V_36(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 7.545A{2-[ethyl(pyridine-3-carbonyl)amino]-MS[M+1]+: 552ethoxy}phenyl)propionic acid methylesterIIa_476V_39(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 7.863A{2-[propyl(pyridine-3-carbonyl)-MS[M+1]+: 566amino]ethoxy}phenyl)propionic acidmethyl esterIIa_477V_36(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.711A{2-[ethyl-(3-thiophen-2-ylacryloyl)-MS[M+1]+: 583amino]ethoxy}phenyl)propionic acidmethyl esterIIa_478V_39(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.993A{2-[propyl-(3-thiophen-2-ylacryloyl)-MS[M+1]+: 597amino]ethoxy}phenyl)propionic acidmethyl esterIIa_479V_39(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.34A{2-[(3,3-dimethylbutyryl)-MS[M+1]+: 559propylamino]ethoxy}phenyl)propionicacid methyl esterIIa_480V_36(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 6.512A{2-[ethyl-(3-pyridin-3-ylpropionyl)-MS[M+1]+: 580amino]ethoxy}phenyl)propionic acidmethyl esterIIa_481V_39(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 6.767A{2-[propyl-(3-pyridin-3-ylpropionyl)-MS[M+1]+: 594amino]ethoxy}phenyl)propionic acidmethyl esterIIa_482V_39(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 8.955A[2-MS[M+1]+: 543(cyclobutanecarbonylpropylamino)-ethoxy]phenyl}propionic acid methylesterIIa_483V_39(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 8.789A[2-(isobutyrylpropylamino)ethoxy]-MS[M+1]+: 531phenyl}propionic acid methyl esterIIa_484V_39(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 8.775A[2-(butyrylpropylamino)ethoxy]-MS[M+1]+: 531phenyl}propionic acid methyl esterIIa_485V_36(S)-3-{4-[2-(Benzoylethylamino)-rt: 8.547Aethoxy]phenyl}-2-(2-MS[M+1]+: 551benzoylphenylamino)propionic acidmethyl esterIIa_486V_39(S)-2-(2-Benzoylphenylamino)-3-{4-rt: 8.829A[2-(benzoylpropylamino)ethoxy]-MS[M+1]+: 565phenyl}propionic acid methyl esterIIa_487V_36(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.806A{2-[ethyl-(3-phenylacryloyl)amino]-MS[M+1]+: 577ethoxy}phenyl)propionic acid methylesterIIa_488V_36(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.931A{2-[(2,2-dimethylpropionyl)-MS[M+1]+: 531ethylamino]ethoxy}phenyl)propionicacid methyl esterIIa_489V_39(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.233A{2-[(2,2-dimethylpropionyl)-MS[M+1]+: 545propylamino]ethoxy}phenyl)propionicacid methyl esterIIa_490V_24(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.298A{3-[(3-chlorophenyl)-(2-MS[M, M+2]+: 611,methylacryloyl)amino]propoxy}-613phenyl)propionic acid methyl esterIIa_491V_25(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.347A{3-[(3-chlorophenyl)-(2-MS[M, M+2]+: 611,methylacryloyl)amino]propoxy}-613phenyl)propionic acid methyl ester


Compounds I:


Compounds I described shown in Table 6 were obtained starting from the corresponding ester derivative of formula II following any of the procedures J or K described below.


PROCEDURE J: To a 0.02 M solution of compound II (1 eq) in a mixture of THF:methanol (3:1) or THF, a 1 M aqueous solution of lithium hydroxide (1.5 eq) was added. The resulting mixture was stirred at room temperature for 18 h, then treated with HCl 1 N until pH=56, and extracted twice with EtOAc. The organic layers were dried over anhydrous sodium sulfate and filtered. The solvent was distilled off under reduced pressure.


PROCEDURE K: To a solution 0.03 M of compound II (1 eq) in methanol, potassium hydroxide (10 eq) was added. The resulting solution was stirred at room temperature for 18 h, then treated with HCl 1 N until acid pH=4-5. To the resulting suspension, water and EtOAc were added. The organic layer was separated and the aqueous layer was extracted once with EtOAc. The combined organic layers were dried over anhydrous sodium sulfate and filtered. The solvent was distilled off under reduced pressure.

TABLE 6ExampleStartingHPLCNumberproductCompound name1H-NMR/LC-MSMethodI_1IIa_1(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.327A{2-[(2-chlorophenyl)-(2-MS[M, M+2]+: 583, 585methylacryloyl)amino]ethoxy}phenyl)-propionic acidI_2IIa_2(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.476A{3-[(2-chlorophenyl)-(2-MS[M, M+2]+: 597, 599methylacryloyl)amino]propoxy)-phenyl)propionic acidI_3IIa_3(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.295A{2-[but-2-(E)-enoyl-(2-chlorophenyl)-MS[M, M+2]+: 583, 585amino]ethoxy}phenyl)propionic acidI_4IIa_4(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.855A{2-[(2-chlorophenyl)-(3-methylbutyryl)-MS[M, M+2]+: 599, 601amino]ethoxy}phenyl)propionic acidI_5IIa_5(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.728A{2-[(2-chlorophenyl)-MS[M, M+2]+: 597, 599cyclobutanecarbonylamino]ethoxy}-phenyl)propionic acidI_6IIa_6(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.989A{2-[(2-chlorophenyl)-MS[M, M+2]+: 611, 613cyclopentanecarbonylamino]ethoxy}-phenyl)propionic acidI_7IIa_7(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.353; MS[M, M+2]+:A{2-[(2-chlorophenyl)-583, 585cyclopropanecarbonylamino]ethoxy}-phenyl)propionic acidI_8IIa_8(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.508A{3-[(2-chlorophenyl)-MS[M, M+2]+: 597, 599cyclopropanecarbonylamino]propoxy}-phenyl)propionic acidI_9IIa_9(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.298A{2-[(2-chlorophenyl)propionylamino]-MS[M, M+2]+: 571, 573ethoxy}phenyl)propionic acidI_10IIa_10(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.446A{3-[(2-chlorophenyl)propionylamino]-MS[M, M+2]+: 585, 587propoxy}phenyl)propionic acidI_11IIa_11(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.561A{2-[(2-chlorophenyl)isobutyrylamino]-MS[M, M+2]+: 585, 587ethoxy}phenyl)propionic acidI_12IIa_12(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.701A{3-[(2-chlorophenyl)isobutyrylamino]-MS[M, M+2]+: 599, 601propoxy}phenyl)propionic acidI_13IIa_13(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.588A{2-[butyryl-(2-chlorophenyl)amino]-MS[M, M+2]+: 585, 587ethoxy}phenyl)propionic acidI_14IIa_14(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.726A{3-[butyryl-(2-chlorophenyl)amino]-MS[M, M+2]+: 599, 601propoxy}phenyl)propionic acidI_15IIa_15(S)-3-(4-{3-[Acryloyl-(2-chlorophenyl)-rt: 8.293Aamino]propoxy}phenyl)-2-(2-MS[M, M+2]+: 583, 585benzoylphenylamino)propionic acidI_16IIa_16(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.19A{2-[(2-fluorophenyl)-(thiophene-2-MS[M+1]+: 609carbonyl)amino]ethoxy}phenyl)-propionic acidI_17IIa_17(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.054A{2-[(2-fluorophenyl)-(2-MS[M+1]+: 567methylacryloyl)amino]ethoxy}phenyl)-propionic acidI_18IIa_18(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.534A{2-[(2-fluorophenyl)-(3-methylbutyryl)-MS[M+1]+: 583amino]ethoxy}phenyl)propionic acidI_19IIa_19(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.414A{2-[cyclobutanecarbonyl-(2-MS[M+1]+: 581fluorophenyl)amino]ethoxy}phenyl)-propionic acidI_20IIa_20(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.674A{2-[cyclopentanecarbonyl-(2-MS[M+1]+: 595fluorophenyl)amino]ethoxyl}phenyl)-propionic acidI_21IIa_21(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.061A{2-[cyclopropanecarbonyl-(2-MS[M+1]+: 567fluorophenyl)amino]ethoxy}phenyl)-propionic acidI_22IIa_22(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 7.981A{2-[(2-fluorophenyl)propionylamino]-MS[M+1]+: 555ethoxy}phenyl)propionic acidI_23IIa_23(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.256A{2-[(2-fluorophenyl)isobutyrylamino]-MS[M+1]+: 569ethoxy}phenyl)propionic acidI_24IIa_24(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.269A{2-[butyryl-(2-fluorophenyl)amino]-MS[M+1]+: 569ethoxy}phenyl)propionic acidI_25IIa_25(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.665A{2-[(2,2-dimethylpropionyl)-(2-MS[M+1]+: 583fluorophenyl)amino]ethoxy}phenyl)-propionic acidI_26IIa_26(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.369A{3-[(2-methylacryloyl)-o-tolylamino]-MS[M+1]+: 577propoxy}phenyl)propionic acidI_27IIa_27(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.99A{2-[(2-ethylbutyryl)-o-tolylamino]-MS[M+1]+: 593ethoxy}phenyl)propionic acidI_28IIa_28(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.758A{3-[(3-methylbut-2-(E)-enoyl)-o-MS[M+1]+: 591tolylamino]propoxy}phenyl)propionicacidI_29IIa_29(S)-2-(2-Benzoylphenylamino)-3-{4-[3-rt: 8.471A(but-2-(E)-enoyl-o-tolylamino)-MS[M+1]+: 577propoxy]phenyl}propionic acidI_30IIa_30(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.101A{2-[(3,3-dimethylbutyryl)-o-tolylamino]-MS[M+1]+: 593ethoxy}phenyl)propionic acidI_31IIa_31(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.75A{2-[(3-methylbutyryl)-o-tolylamino]-MS[M+1]+: 579ethoxy}phenyl)propionic acidI_32IIa_32(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.945A{3-[(3-methylbutyryl)-o-tolylamino]-MS[M+1]+: 593propoxy}phenyl)propionic acidI_33IIa_33(S)-2-(2-Benzoylphenylamino)-3-{4-[3-rt: 8.742A(o-tolylpent-4-enoylamino)propoxy]-MS[M+1]+: 591phenyl}propionic acidI_34IIa_34(S)-2-(2-Benzoylphenylamino)-3-{4-[2-rt: 8.634A(cyclobutanecarbonyl-o-tolylamino)-MS[M+1]+: 577ethoxy]phenyl}propionic acidI_35IIa_35(S)-2-(2-Benzoylphenylamino)-3-{4-[2-rt: 8.898A(cyclopentanecarbonyl-o-tolylamino)-MS[M+1]+: 591ethoxy]phenyl}propionic acidI_36IIa_36(S)-2-(2-Benzoylphenylamino)-3-{4-[3-rt: 8.387A(propionyl-o-tolylamino)propoxy]-MS[M+1]+: 565phenyl}propionic acidI_37IIa_37(S)-2-(2-Benzoylphenylamino)-3-{4-[2-rt: 8.458A(isobutyryl-o-tolylamino)ethoxy]-MS[M+1]+: 565phenyl}propionic acidI_38IIa_38(S)-2-(2-Benzoylphenylamino)-3-{4-[3-rt: 8.66A(isobutyryl-o-tolylamino)propoxy]-MS[M+1]+: 579phenyl}propionic acidI_39IIa_39(S)-2-(2-Benzoylphenylamino)-3-{4-[3-rt: 8.968A(pentanoyl-o-tolylamino)propoxy]-MS[M+1]+: 593phenyl}propionic acidI_40IIa_40(S)-2-(2-Benzoylphenylamino)-3-{4-[2-rt: 8.474A(butyryl-o-tolylamino)ethoxy]phenyl}-MS[M+1]+: 565propionic acidI_41IIa_41(S)-2-(2-Benzoylphenylamino)-3-{4-[3-rt: 8.677A(butyryl-o-tolylamino)propoxy]phenyl)-MS[M+1]+: 579propionic acidI_42IIa_42(S)-2-(2-Benzoylphenylamino)-3-{4-[2-rt: 8.324A(benzoyl-o-tolylamino)ethoxy]phenyl}-MS[M+1]+: 599propionic acidI_43IIa_43(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.884A{2-[(2,2-dimethylpropionyl)-o-MS[M+1]+: 579tolylamino]ethoxy}phenyl)propionicacidI_44IIa_44(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.028A{3-[(2,2-dimethylpropionyl)-o-MS[M+1]+: 593tolylamino]propoxy}phenyl)propionicacidI_45IIa_45(S)-3-{4-[3-(Acryloyl-o-tolylamino)-rt: 8.31Apropoxy]phenyl}-2-(2-MS[M+1]+: 563benzoylphenylamino)propionic acidI_46IIa_46(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.385A{2-[(3-chlorophenyl)-(2-MS[M, M+2]+: 583, 586methylacryloyl)amino]ethoxy}phenyl)-propionic acidI_47IIa_490(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.54A{3-[(3-chlorophenyl)-(2-MS[M, M+2]+: 597, 599methylacryloyl)amino]propoxy}-phenyl)propionic acidI_48IIa_47(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.45A{2-[but-2-(E)-enoyl-(3-chlorophenyl)-MS[M, M+2]+: 583, 585amino]ethoxy}phenyl)propionic acidI_49IIa_48(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.596A{3-[but-2-(E)-enoyl-(3-chlorophenyl)-MS[M, M+2]+: 597, 599amino]propoxy}phenyl)propionic acidI_50IIa_49(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.877A{2-[(3-chlorophenyl)-(3-methylbutyryl)-MS[M, M+2]+: 599, 601amino]ethoxy}phenyl)propionic acidI_51IIa_50(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.68A{2-[(3-chlorophenyl)-pent-4-MS[M, M+2]+: 597, 599enoylamino]ethoxy}phenyl)propionicacidI_52IIa_51(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.787A{2-[(3-chlorophenyl)-MS[M, M+2]+: 597, 599cyclobutanecarbonylamino]ethoxy}-phenyl)propionic acidI_53IIa_52(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.040A{2-[(3-chlorophenyl)-MS[M, M+2]+: 611, 613cyclopentanecarbonylamino]ethoxy}-phenyl)propionic acidI_54IIa_53(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.481A{2-[(3-chlorophenyl)-MS[M, M+2]+: 583, 585cyclopropanecarbonylamino]ethoxy}-phenyl)propionic acidI_55IIa_54(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.645; MS[M, M+2]+:A{3-[(3-chlorophenyl)-597, 599cyclopropanecarbonylamino]propoxy}-phenyl)propionic acidI_56IIa_55(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.345A{2-[(3-chlorophenyl)propioylamino]-MS[M, M+2]+: 571, 573ethoxy}phenyl)propionic acidI_57IIa_56(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.509A{3-[(3-chlorophenyl)propionylamino]-MS[M, M+2]+: 585, 587propoxy}phenyl)propionic acidI_58IIa_57(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.613A{2-[(3-chlorophenyl)isobutyrylamino]-MS[M, M+2]+: 585, 587ethoxy}phenyl)propionic acidI_59IIa_58(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.768A{3-[(3-chlorophenyl)isobutyrylamino]-MS[M, M+2]+: 599, 601propoxy}phenyl)propionic acidI_60IIa_59(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.623A{2-[butyryl-(3-chlorophenyl)amino]-MS[M, M+2]+: 585, 587ethoxy}phenyl)propionic acidI_61IIa_60(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.779; MS[M, M+2]+:A{3-[butyryl-(3-chlorophenyl)amino]-599, 601propoxy}phenyl)propionic acidI_62IIa_61(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.995A{2-[(3-chlorophenyl)-(2,2-MS[M, M+2]+: 599, 601dimethylpropionyl)amino]ethoxy}-phenyl)propionic acidI_63IIa_62(S)-3-(4-{3-[Acryloyl-(3-chlorophenyl)-rt: 8.419Aamino]propoxy}phenyl)-2-(2-MS[M, M+2]+: 583, 585benzoylphenylamino)propionic acidI_64IIa_63(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.250A{2-[(3-fluorophenyl)-(thiophene-2-MS[M+1]+: 609carbonyl)amino]ethoxy}phenyl)-propionic acidI_65IIa_64(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.062A{2-[(3-fluorophenyl)-(2-MS[M+1]+: 567methylacryloyl)amino]ethoxy}phenyl)-propionic acidI_66IIa_65(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.538A{2-[(3-fluorophenyl)-(3-methylbutyryl)-MS[M+1]+: 583amino]ethoxy}phenyl)propionic acidI_67IIa_66(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.431A{2-[cyclobutanecarbonyl-(3-MS[M+1]+: 581fluorophenyl)amino]ethoxy}phenyl)-propionic acidI_68IIa_67(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.688A{2-[cyclopentanecarbonyl-(3-MS[M+1]+: 595fluorophenyl)amino]ethoxy}phenyl)-propionic acidI_69IIa_68(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.134A{2-[cyclopropanecarbonyl-(3-MS[M+1]+: 567fluorophenyl)amino]ethoxy}phenyl)-propionic acidI_70IIa_69(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 7.998A{2-[(3-fluorophenyl)propionylamino]-MS[M+1]+: 555ethoxy}phenyl)propionic acidI_71IIa_70(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.267A{2-[(3-fluorophenyl)isobutyrylamino]-MS[M+1]+: 569ethoxy}phenyl)propionic acidI_72IIa_71(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.278A{2-[butyryl-(3-fluorophenyl)amino]-MS[M+1]+: 569ethoxy}phenyl)propionic acidI_73IIa_72(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.65A{2-[(2,2-dimethylpropionyl)-(3-MS[M+1]+: 583fluorophenyl)amino]ethoxy}phenyl)-propionic acidI_74IIa_73(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.439A{3-[(2-methylacryloyl)-(3-MS[M+1]+: 591methylbenzyl)amino]propoxy}phenyl)-propionic acidI_75IIa_74(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.973A{2-[(2-ethylbutyryl)-(3-methylbenzyl)-MS[M+1]+: 607amino]ethoxy}phenyl)propionic acidI_76IIa_75(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.634A{3-[(3-methylbenzyl)-(3-methylbut-2-MS[M+1]+: 605(E)-enoyl)amino]propoxy}phenyl)-propionic acidI_77IIa_76(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.381A{3-[but-2-(E)-enoyl-(3-methylbenzyl)-MS[M+1]+: 591amino]propoxy}phenyl)propionic acidI_78IIa_77(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.041A{2-[(3,3-dimethylbutyryl)-(3-MS[M+1]+: 607methylbenzyl)amino]ethoxy}phenyl)-propionic acidI_79IIa_78(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.745A{2-[(3-methylbenzyl)-(3-MS[M+1]+: 593methylbutyryl)amino]ethoxy}phenyl)-propionic acidI_80IIa_79(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.828A{3-[(3-methylbenzyl)-(3-MS[M+1]+: 607methylbutyryl)amino]propoxy}phenyl)-propionic acidI_81IIa_80(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.645A{2-[cyclobutanecarbonyl-(3-MS[M+1]+: 591methylbenzyl)amino]ethoxy}phenyl)-propionic acidI_82IIa_81(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.722A{3-[cyclobutanecarbonyl-(3-MS[M+1]+: 605methylbenzyl)amino]propoxy}phenyl)-propionic acidI_83IIa_82(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.874A{2-[cyclopentanecarbonyl-(3-MS[M+1]+: 605methylbenzyl)amino]ethoxy}phenyl)-propionic acidI_84IIa_83(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.422A{3[cyclopropanecarbonyl-(3-MS[M+1]+: 591methylbenzyl)amino]propoxy}phenyl)-propionic acidI_85IIa_84(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.31A{3-[(3-methylbenzyl)propionylamino]-MS[M+1]+: 579propoxy}phenyl)propionic acidI_86IIa_85(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.468A{2-[isobutyryl-(3-methylbenzyl)amino]-MS[M+1]+: 579ethoxy}phenyl)propionic acidI_87IIa_86(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.56A{3-[isobutyryl-(3-methylbenzyl)amino]-MS[M+1]+: 593propoxy}phenyl)propionic acidI_88IIa_87(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.489A{2-[butyryl-(3-methylbenzyl)amino]-MS[M+1]+: 579ethoxy}phenyl)propionic acidI_89IIa_88(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.574A{3-[butyryl-(3-methylbenzl)amino]-MS[M+1]+: 593propoxy}phenyl)propionic acidI_90IIa_89(S)-3-(4-{2-[Benzoyl-(3-methylbenzyl)-rt: 8.545Aamino]ethoxy}phenyl)-2-(2-MS[M+1]+: 613benzoylphenylamino)propionic acidI_91IIa_90(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.886A{2-[(2,2-dimethylpropionyl)-(3-MS[M+1]+: 593methylbenzyl)amino]ethoxy}phenyl)-propionic acidI_92IIa_91(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.909A{3-[(2,2-dimethylpropionyl)-(3-MS[M+1]+: 607methylbenzyl)amino]propoxy}phenyl)-propionic acidI_93IIa_92(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.472A{3-[(2-methylacryloyl)-m-tolylamino]-MS[M+1]+: 577propoxy}phenyl)propionic acidI_94IIa_93(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.062A{2-[(2-ethylbutyryl)-m-tolylamino]-MS[M+1]+: 593ethoxy}phenyl)propionic acidI_95IIa_94(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.826A{3-[(3-methylbut-2-(E)-enoyl)-m-MS[M+1]+: 591tolylamino]propoxy}phenyl)propionicacidI_96IIa_95(S)-2-(2-Benzoylphenylamino)-3-{4-[3-rt: 8.554A(but-2-(E)-enoyl-m-tolylamino)-MS[M+1]+: 577propoxy]phenyl}propionic acidI_97IIa_96(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.152A{2-[(3,3-dimethylbutyryl)-m-MS[M+1]+: 593tolylamino]ethoxy}phenyl)propionicacidI_98IIa_97(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.802A{2-[(3-methylbutyryl)-m-tolylamino]-MS[M+1]+: 579ethoxy}phenyl)propionic acidI_99IIa_98(S)-2-(2-Benzoylphenylamino)-3-{4-[2-rt: 8.724A(cyclobutanecarbonyl-m-tolyamino)-MS[M+1]+: 577ethoxy]phenyl}propionic acidI_100IIa_99(S)-2-(2-Benzoylphenylamino)-3-{4-[2-rt: 8.958A(cyclopentanecabonyl-m-tolylamino)-MS[M+1]+: 591ethoxy]phenyl}propionic acidI_101IIa_100(S)-2-(2-Benzoylphenylamino)-3-{4-[3-rt: 8.607A(cyclopropanecarbonyl-m-tolylamino)-MS[M+1]+: 577propoxy]phenyl}propionic acidI_102IIa_101(S)-2-(2-Benzoylphenylamino)-3-{4-[3-rt: 8.468A(propionyl-m-tolylamino)propoxy]-MS[M+1]+: 565phenyl}propionic acidI_103IIa_102(S)-2-(2-Benzoylphenylamino)-3-{4-[2-rt: 8.532A(isobutyryl-m-tolyamino)ethoxy]-MS[M+1]+: 565phenyl}propionic acidI_104IIa_103(S)-2-(2-Benzoylphenylamino)-3-{4-[3-rt: 8.731A(isobutyryl-m-tolylamino)propoxy]-MS[M+1]+: 579phenyl}propionic acidI_105IIa_104(S)-2-(2-Benzoylphenylamino)-3-{4-[3-rt: 9.025A(pentanoyl-m-tolylamino)propoxy]-MS[M+1]+: 593phenyl}propionic acidI_106IIa_105(S)-2-(2-Benzoylphenylamino)-3-{4-[2-rt: 8.543A(butyryl-m-tolylamino)ethoxy]phenyl}-MS[M+1]+: 565propionic acidI_107IIa_106(S)-2-(2-Benzoylphenylamino)-3-{4-[3-rt: 8.741A(butyryl-m-tolylamino)propoxy]-MS[M+1]+: 579phenyl}propionic acidI_108IIa_107(S)-2-(2-Benzoylphenylamino)-3-{4-[2-rt: 8.436A(benzoyl-m-tolylamino)ethoxy]phenyl}-MS[M+1]+: 599propionic acidI_109IIa_108(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.953A{2-[(2,2-dimethylpropionyl)-m-MS[M+1]+: 579tolylamino]ethoxy}phenyl)propionicacidI_110IIa_109(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.109A{3-[(2,2-dimethylpropionyl)-m-MS[M+1]+: 593tolylamino]propoxy}phenyl)propionicacidI_111IIa_110(S)-3-{4-[3-(Acryloyl-m-tolylamino)-rt: 8.388Apropoxy]phenyl}-2-(2-MS[M+1]+: 563benzoylphenylamino)propionic acidI_112IIa_111(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.437A{2-[(4-chlorophenyl)-(2-MS[M, M+2]+: 583, 586methylacryloyl)amino]ethoxy}phenyl)-propionic acidI_113IIa_491(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.595A{3-[(4-chlorophenyl)-(2-MS[M, M+2]+: 597, 599methylacryloyl)amino]propoxy}-phenyl)propionic acidI_114IIa_112(S)-2-(2-Benzoylphenyamino)-3-(4-rt: 8.517A{2-[but-2-(E)-enoyl-(4-chlorophenyl)-MS[M, M+2]+: 583, 585amino]ethoxy}phenyl)propionic acidI_115IIa_113(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.942A{2-[(4-chlorophenyl)-(3-methylbutyryl)-MS[M, M+2]+: 599, 601amino]ethoxy}phenyl)propionic acidI_116IIa_114(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.739A{2-[(4-chlorophenyl)-pent-4-MS[M, M+2]+: 597, 599enoylamino]ethoxy}phenyl)propionicacidI_117IIa_115(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.839A{2-[(4-chlorophenyl)-MS[M, M+2]+: 597, 599cyclobutanecarbonylamino]ethoxy}-phenyl)propionic acidI_118IIa_116(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.103A{2-[(4-chlorophenyl)-MS[M, M+2]+: 611, 613cyclopentanecarbonylamino]ethoxy}-phenyl)propionic acidI_119IIa_117(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.533A{2-[(4-chlorophenyl)-MS[M, M+2]+: 583, 585cyclopropanecarbonylamino]ethoxy}-phenyl)propionic acidI_120IIa_118(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.696A{3-[(4-chlorophenyl)-MS[M, M+2]+: 597, 599cyclopropanecarbonylamino]propoxy}-phenyl)propionic acidI_121IIa_119(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.399A{2-[(4-chlorophenyl)propionylamino]-MS[M, M+2]+: 571, 573ethoxy}phenyl)propionic acidI_122IIa_120(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.562A{3-[(4-chlorophenyl)propionylamino]-MS[M, M+2]+: 585, 587propoxy}phenyl)propionic acidI_123IIa_121(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.682A{2-[(4-chlorophenyl)isobutyrylamino]-MS[M, M+2]+: 585, 587ethoxy}phenyl)propionic acidI_124IIa_122(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.835A{3-[(4-chlorophenyl)isobutyrylamino]-MS[M, M+2]+: 599, 601propoxy}phenyl)propionic acidI_125IIa_123(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.684A{2-[butyryl-(4-chlorophenyl)amino]-MS[M, M+2]+: 585, 587ethoxy}phenyl)propionic acidI_126IIa_124(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.836A{3-[butyryl-(4-chlorophenyl)amino]-MS[M, M+2]+: 599, 601propoxy}phenyl)propionic acidI_127IIa_125(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.043A{2-[(4-chlorophenyl)-(2,2-MS[M, M+2]+: 599, 601dimethylpropionyl)amino]ethoxy}-phenyl)propionic acidI_128IIa_126(S)-3-(4-{3-[Acryloyl-(4-chlorophenyl)-rt: 8.475Aamino]propoxy}phenyl)-2-(2-MS[M, M+2]+: 583, 585benzoylphenylamino)propionic acidI_129IIa_127(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.247A{2-[(4-fluorophenyl)-(thiophene-2-MS[M+1]+: 609carbonyl)amino]ethoxy}phenyl)-propionic acidI_130IIa_128(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.026A{2-[(4-fluorophenyl)-(2-MS[M+1]+: 567methylacryloyl)amino]ethoxy}phenyl)-propionic acidI_131IIa_129(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.365A{2-[(4-fluorophenyl)-(3-methylbut-2-MS[M+1]+: 581(E)-enoyl)amino]ethoxy}phenyl)-propionic acidI_132IIa_130(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.528A{2-[(4-fluorophenyl)-(3-methylbutyryl)-MS[M+1]+: 583amino]ethoxy}phenyl)propionic acidI_133IIa_131(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.421A{2-[cyclobutanecarbonyl-(4-MS[M+1]+: 581fluorophenyl)amino]ethoxy}phenyl)-propionic acidI_134IIa_132(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.675A{2-[cyclopentanecarbonyl-(4-MS[M+1]+: 595fluorophenyl)amino]ethoxy}phenyl)-propionic acidI_135IIa_133(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.117A{2-[cyclopropanecarbonyl-(4-MS[M+1]+: 567fluorophenyl)amino]ethoxy}phenyl)-propionic acidI_136IIa_134(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 7.987A{2-[(4-fluorophenyl)propionylamino]-MS[M+1]+: 555ethoxy}phenyl)propionic acidI_137IIa_135(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.253A{2-[(4-fluorophenyl)isobutyrylamino]-MS[M+1]+: 569ethoxy}phenyl)propionic acidI_138IIa_136(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.266A{2-[butyryl-(4-fluorophenyl)amino]-MS[M+1]+: 569ethoxy}phenyl)propionic acidI_139IIa_137(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.64A{2-[(2,2-dimethylpropionyl)-(4-MS[M+1]+: 583fluorophenyl)amino]ethoxy}phenyl)-propionic acidI_140IIa_138(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.483A{3-[(2-methylacryloyl)-p-tolylamino]-MS[M+1]+: 577propoxy}phenyl)propionic acidI_141IIa_139(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.088A{2-[(2-ethylbutyryl)-p-tolylamino]-MS[M+1]+: 593ethoxy}phenyl)propionic acidI_142IIa_140(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.178A{2-[(3,3-dimethylbutyryl)-p-tolylamino]-MS[M+1]+: 593ethoxy}phenyl)propionic acidI_143IIa_141(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.827A{2-[(3-methylbutyryl)-p-tolylamino]-MS[M+1]+: 579ethoxy}phenyl)propionic acidI_144IIa_142(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.025A{3-[(3-methylbutyryl)-p-tolylamino]-MS[M+1]+: 593propoxy}phenyl)propionic acidI_145IIa_143(S)-2-(2-Benzoylphenylamino)-3-{4-[2-rt: 8.737A(cyclobutanecarbonyl-p-tolylamino)-MS[M+1]+: 577ethoxy]phenyl}propionic acidI_146IIa_144(S)-2-(2-Benzoylphenylamino)-3-{4-[3-rt: 8.936A(cyclobutanecarbonyl-p-tolylamino)-MS[M+1]+: 591propoxy]phenyl}propionic acidI_147IIa_145(S)-2-(2-Benzoylphenylamino)-3-{4-[2-rt: 8.992A(cyclopentanecarbonyl-p-tolylamino)-MS[M+1]+: 591ethoxy]phenyl}propionic acidI_148IIa_146(S)-2-(2-Benzoylphenylamino)-3-{4-[3-rt: 8.486A(propionyl-p-tolylamino)propoxy]-MS[M+1]+: 565phenyl}propionic acidI_149IIa_147(S)-2-(2-Benzoylphenylamino)-3-{4-[2-rt: 8.554A(isobutyryl-p-tolylamino)ethoxy]-MS[M+1]+: 565phenyl}propionic acidI_150IIa_148(S)-2-(2-Benzoylphenylamino)-3-{4-[3-rt: 8.758A(isobutyryl-p-tolylamino)propoxy]-MS[M+1]+: 579phenyl}propionic acidI_151IIa_149(S)-2-(2-Benzoylphenylamino)-3-{4-[2-rt: 8.561A(butyryl-p-tolylamino)ethoxy]phenyl}-MS[M+1]+: 565propionic acidI_152IIa_150(S)-2-(2-Benzoylphenylamino)-3-{4-[2-rt: 8.431A(benzoyl-p-tolylamino)ethoxy]phenyl}-MS[M+1]+: 599propionic acidI_153IIa_151(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.967A{2-[(2,2-dimethylpropionyl)-p-MS[M+1]+: 579tolylamino]ethoxy}phenyl)propionicacidI_154IIa_152(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.126A{3-[(2,2-dimethylpropionyl)-p-MS[M+1]+: 593tolylamino]propoxy}phenyl)propionicacidI_155IIa_153(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.702A{2-[benzyl(naphthalene-1-carbonyl)-MS[M+1]+: 649amino]ethoxy}phenyl)propionic acidI_156IIa_154(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.744A{2-[benzyl(naphthalene-2-carbonyl)-MS[M+1]+: 649amino]ethoxy}phenyl)propionic acidI_157IIa_155(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 7.713A{2-[benzyl(pyrazine-2-carbonyl)-MS[M+1]+: 601amino]ethoxy}phenyl)propionic acidI_158IIa_156(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 7.813A{3-[benzyl(pyrazine-2-carbonyl)-MS[M+1]+: 615amino]propoxy}phenyl)propionic acidI_159IIa_157(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 7.866A{2-[benzyl(pyridine-2-carbonyl)amino]-MS[M+1]+: 600ethoxy}phenyl)propionic acidI_160IIa_158(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 7.978A{3-[benzyl(pyridine-2-carbonyl)amino]-MS[M+1]+: 614propoxy}phenyl)propionic acidI_161IIa_159(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.538A{2-[benzyl(quinoline-2-carbonyl)-MS[M+1]+: 650amino]ethoxy}phenyl)propionic acidI_162IIa_160(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.602A{3-[benzyl(quinoline-2-carbonyl)-MS[M+1]+: 664amino]propoxy}phenyl)propionic acidI_163IIa_161(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.374A{2-[benzyl(quinoxaline-2-carbonyl)-MS[M+1]+: 651amino]ethoxy}phenyl)propionic acidI_164IIa_162(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.455A{3-[benzyl(quinoxaline-2-carbonyl)-MS[M+1]+: 665amino]propoxy}phenyl)propionic acidI_165IIa_163(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.331A{2-[benzyl(thiophene-2-carbonyl)-MS[M+1]+: 605amino]ethoxy}phenyl)propionic acidI_166IIa_164(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.415A{3-[benzyl(thiophene-2-carbonyl)-MS[M+1]+: 619amino]propoxy}phenyl)propionic acidI_167IIa_165(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.026A{2-[benzyl(furan-3-carbonyl)amino]-MS[M+1]+: 589ethoxy}phenyl)propionic acidI_168IIa_166(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.105A{3-[benzyl(furan-3-carbonyl)amino]-MS[M+1]+: 603propoxy}phenyl)propionic acidI_169IIa_167(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.318A{2-[benzyl(isoquinoline-3-carbonyl)-MS[M+1]+: 650amino]ethoxy}phenyl)propionic acidI_170IIa_168(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.383A{3-[benzyl(isoquinoline-3-carbonyl)-MS[M+1]+: 664amino]propoxy}phenyl)propionic acidI_171IIa_169(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 7.448A{2-[benzyl(pyridine-3-carbonyl)amino]-MS[M+1]+: 600ethoxy}phenyl)propionic acidI_172IIa_170(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 7.584A{3-[benzyl(pyridine-3-carbonyl)amino]-MS[M+1]+: 614propoxy}phenyl)propionic acidI_173IIa_171(S)-2-(2-Benzoylphenylamino)-3-{4-[2-rt: 8.461A(benzylphenylacetylamino)ethoxy]-MS[M+1]+: 613phenyl}propionic acidI_174IIa_172(S)-2-(2-Benzoylphenylamino)-3-{4-[3-rt: 8.489A(benzylphenylacetylamino)propoxy]-MS[M+1]+: 627phenyl}propionic acidI_175IIa_173(S)-2.(2-Benzoylphenylamino)-3-(4-rt: 8.057A{2-[benzyl-(2-methylacryloyl)amino]-MS[M+1]+: 563ethoxy}phenyl)propionic acidI_176IIa_174(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.14A{3-[benzyl-(2-methylacryloyl)amino]-MS[M+1]+: 577propoxy}phenyl)propionic acidI_177IIa_175(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.675A{2-[benzyl-(3-phenylpropynoyl)amino]-MS[M+1]+: 623ethoxy}phenyl)propionic acidI_178IIa_176(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.762A{3-[benzyl-(3-phenylpropynoyl)amino]-MS[M+1]+: 637propoxy}phenyl)propionic acidI_179IIa_177(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.711A{2-[benzyl-(2-ethylbutyryl)amino]-MS[M+1]+: 593ethoxy}phenyl)propionic acidI_180IIa_178(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.766A{3-[benzyl-(2-ethylbutyryl)amino]-MS[M+1]+: 607propoxy}phenyl)propionic acidI_181IIa_179(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.278A{2-[benzyl-(3-methylbut-2-(E)-enoyl)-MS[M+1]+: 577amino]ethoxy}phenyl)propionic acidI_182IIa_180(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.381A{3-[benzyl-(3-methylbut-2-(E)-enoyl)-MS[M+1]+: 591amino]propoxy}phenyl)propionic acidI_183IIa_181(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.279A{2-[benzyl-(3-furan-2-ylacryloyl)-MS[M+1]+: 615amino]ethoxy}phenyl)propionic acidI_184IIa_182(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.386A{3-[benzyl-(3-furan-2-ylacryloyl)-MS[M+1]+: 629amino]propoxy}phenyl)propionic acidI_185IIa_183(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.436A{2-[benzyl-(3-thiophen-2-ylacryloyl)-MS[M+1]+: 631amino]ethoxy}phenyl)propionic acidI_186IIa_184(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.551A{3-[benzyl-(3-thiophen-2-ylacryloyl)-MS[M+1]+: 645amino]propoxy}phenyl)propionic acidI_187IIa_185(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.158A{2-[benzyl-(3-furan-3-yl-(E)-acryloyl)-MS[M+1]+: 615amino]ethoxy}phenyl)propionic acidI_188IIa_186(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.266A{3-[beznyl-(3-furan-3-yl-(E)-acryloyl)-MS[M+1]+: 629amino]propoxy}phenyl)propionic acidI_189IIa_187(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 7.303A{2-[benzyl-(3-pyridin-3-yl-(E)-acryloyl)-MS[M+1]+: 626amino]ethoxy}phenyl)propionic acidI_190IIa_188(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 7.428A{3-[benzyl-(3-pyridin-3-yl-(E)-acryloyl)-MS[M+1]+: 640amino]propoxy}phenyl)propionic acidI_191IIa_189(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.388A{2-[benzyl-(3-thiophen-3-yl-(E)-MS[M+1]+: 631acryloyl)amino]ethoxy}phenyl)-propionic acidI_192IIa_190(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.489A{3-[benzyl-(3-thiophen-3-yl-(E)-MS[M+1]+: 645acryloyl)amino]propoxy}phenyl)-propionic acidI_193IIa_191(S)-2-(2-Benzoylphenylamino)-3-{4-[2-rt: 8.008A(benzylbut-2-(E)-enoylamino)ethoxy]-MS[M+1]+: 563phenyl}propionic acidI_194IIa_192(S)-2-(2-Benzoylphenylamino)-3-{4-[3-rt: 8.114A(benzylbut-2-(E)-enoylamino)-MS[M+1]+: 577propoxy]phenyl}propionic acidI_195IIa_193(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.325A{2-[benzyl-(2-thiophen-2-ylacetyl)-MS[M+1]+: 619amino]ethoxy}phenyl)propionic acidI_196IIa_194(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.441A{3-[benzyl-(2-thiophe-2-ylacetyl)-MS[M+1]+: 633amino]propoxy}phenyl)propionic acidI_197IIa_195(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 6.546A{2-[benzyl-(2-pyridin-3-ylacetyl)-MS[M+1]+: 614amino]ethoxy}phenyl)propionic acidI_198IIa_196(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 6.683A{3-[benzyl-(2-pyridin-3-ylacetyl)-MS[M+1]+: 628amino]propoxy}phenyl)propionic acidI_199IIa_197(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.32A{2-[benzyl-(2-thiophen-3-ylacetyl)-MS[M+1]+: 619amino]ethoxy}phenyl)propionic acidI_200IIa_198(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.417A{3-[benzyl-(2-thiophen-3-ylacetyl)-MS[M+1]+: 633amino]propoxy}phenyl)propionic acidI_201IIa_199(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.803A{2-[benzyl(3,3-dimethylbutyryl)amino]-MS[M+1]+: 593ethoxy}phenyl)propionic acidI_202IIa_200(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.88A{3-[benzyl(3,3-dimethylbutyryl)amino]-MS[M+1]+: 607propoxy}phenyl)propionic acidI_203IIa_201(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.483A{2-[benzyl-(3-methylbutyryl)amino]-MS[M+1]+: 579ethoxy}phenyl)propionic acidI_204IIa_202(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.562A{3-[benzyl-(3-methylbutyryl)amino]-MS[M+1]+: 593propoxy}phenyl)propionic acidI_205IIa_203(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 6.329A{2-[benzyl-(3-pyridin-3-ylpropionyl)-MS[M+1]+: 628amino]ethoxy}phenyl)propionic acidI_206IIa_204(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 6.584A{3-[benzyl-(3-pyridin-3-ylpropionyl)-MS[M+1]+: 642amino]propoxy}phenyl)propionic acidI_207IIa_205(S)-2-(2-Benzoylphenylamino)-3-{4-[2-rt: 8.32A(benzylpent-4-enoylamino)ethoxy]-MS[M+1]+: 577phenyl}propionic acidI_208IIa_206(S)-2-(2-Benzoylphenylamino)-3-{4-[3-rt: 8.401A(benzylpent-4-enoylamino)propoxy]-MS[M+1]+: 591phenyl}propionic acidI_209IIa_207(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.628A{2-[benzyl-(3-phenylpropionyl)amino]-MS[M+1]+: 627ethoxy}phenyl)propionic acidI_210IIa_208(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.732A{3-[benzyl-(3-phenylpropionyl)amino]-MS[M+1]+: 641propoxy}phenyl)propionic acidI_211IIa_209(S)-2-(2-Benzoylphenylamino)-3-{4-[2-rt: 8.41A(benzylcyclobutanecarbonylamino)-MS[M+1]+: 577ethoxy]phenyl}propionic acidI_212IIa_210(S)-2-(2-Benzoylphenylamino)-3-{4-[3-rt: 8.481A(benzylcyclobutanecarbonylamino)-MS[M+1]+: 591propoxy]phenyl}propionic acidI_213IIa_211(S)-2-(2-Benzoylphenylamino)-3-{4-[2-rt: 8.786A(benzylcyclohexanecarbonylamino)-MS[M+1]+: 605ethoxy]phenyl}propionic acidI_214IIa_212(S)-2-(2-Benzoylphenylamino)-3-{4-[3-rt: 8.865A(benzylcyclohexanecarbonylamino)-MS[M+1]+: 619propoxy]phenyl}propionic acidI_215IIa_213(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.382A{2-[benzyl-(3-cyclohexylpropionyl)-MS[M+1]+: 633amino]ethoxy}phenyl)propionic acidI_216IIa_214(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.479A{3-[benzyl-(3-cyclohexylpropionyl)-MS[M+1]+: 647amino]propoxy}phenyl)propionic acidI_217IIa_215(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.109A{2-[benzyl-(2-cyclohexylacetyl)amino]-MS[M+1]+: 619ethoxy}phenyl)propionic acidI_218IIa_216(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.207A{3-[benzyl-(2-cyclohexylacetyl)amino]-MS[M+1]+: 633propoxy}phenyl)propionic acidI_219IIa_217(S)-2-(2-Benzoylphenylamino)-3-{4-[2-rt: 8.663A(benzylcyclopentanecarbonylamino)-MS[M+1]+: 591ethoxy]phenyl}propionic acidI_220IIa_218(S)-2-(2-Benzoylphenylamino)-3-{4-[3-rt: 8.84Abenzylcyclopentanecarbonylamino)-MS[M+1]+: 605propoxy]phenyl}propionic acidI_221IIa_219(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.16A{2-[benzyl-(3-cyclopentylpropionyl)-MS[M+1]+: 619amino]ethoxy}phenyl)propionic acidI_222IIa_220(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.208A{3-[benzyl-(3-cyclopentylpropionyl)-MS[M+1]+: 633amino]propoxy}phenyl)propionic acidI_223IIa_221(S)-2-(2-Benzoylphenylamino)-3-{4-[2-rt: 8.08A(benzylcyclopropanecarbonylamino)-MS[M+1]+: 563ethoxy]phenyl}propionic acidI_224IIa_222(S)-2-(2-Benzoylphenylamino)-3-{4-[3-rt: 8.181A(benzylcyclopropanecarbonylamino)-MS[M+1]+: 577propoxy]phenyl}propionic acidI_225IIa_223(S)-2-(2-Benzoylphenylamino)-3-{4-[2-rt: 7.968A(benzylpropionylamino)ethoxyl-MS[M+1]+: 551phenyl}propionic acidI_226IIa_224(S)-2-(2-Benzoylphenylamino)-3-{4-[3-rt: 8.054A(benzylpropionylamino)propoxy]-MS[M+1]+: 565phenyl}propionic acidI_227IIa_225(S)-2-(2-Benzoylphenylamino)-3-{4-[2-rt: 8.225A(benzylisobutyrylamino)ethoxy]-MS[M+1]+: 565phenyl}propionic acidI_228IIa_226(S)-2-(2-Benzoylphenylamino)-3-{4-[3-rt: 8.311A(benzylisobutyrylamino)propoxy]-MS[M+1]+: 579phenyl}propionic acidI_229IIa_227(S)-2-(2-Benzoylphenylamino)-3-{4-[2-rt: 8.843A(benzylhexanoylamino)ethoxy]-MS[M+1]+: 593phenyl}propionic acidI_230IIa_228(S)-2-(2-Benzoylphenylamino)-3-{4-[3-rt: 8.898A(benzylhexanoylamino)propoxy]-MS[M+1]+: 607phenyl}propionic acidI_231IIa_229(S)-2-(2-Benzoylphenylamino)-3-{4-[2-rt: 8.507A(benzylpentanoylamino)ethoxy]-MS[M+1]+: 579phenyl}propionic acidI_232IIa_230(S)-2-(2-Benzoylphenylamino)-3-{4-[3-rt: 8.581A(benzylpentanoylamino)propoxy]-MS[M+1]+: 593phenyl}propionic acidI_233IIa_231(S)-2-(2-Benzoylphenylamino)-3-{4-[2-rt: 9.396A(benzyloctanoylamino)ethoxy]phenyl}-MS[M+1]+: 621propionic acidI_234IIa_232(S)-2-(2-Benzoylphenylamino)-3-{4-[3-rt: 9.432A(benzyloctanoylamino)propoxy]-MS[M+1]+: 635phenyl}propionic acidI_235IIa_233(S)-2-(2-Benzoylphenylamino)-3-{4-[2-rt: 9.112A(benzylheptanoylamino)ethoxy]-MS[M+1]+: 607phenyl}propionic acidI_236IIa_234(S)-2-(2-Benzoylphenylamino)-3-{4-[3-rt: 9.158A(benzylheptanoylamino)propoxy]-MS[M+1]+: 621phenyl}propionic acidI_237IIa_235(S)-2-(2-Benzoylphenylamino)-3-{4-[2-rt: 9.653A(benzylnonanoylamino)ethoxy]-MS[M+1]+: 635phenyl}propionic acidI_238IIa_236(S)-2-(2-Benzoylphenylamino)-3-{4-[3-rt: 9.69A(benzylnonanoylamino)propoxy]-MS[M+1]+: 649phenyl}propionic acidI_239IIa_237(S)-2-(2-Benzoylphenylamino)-3-{4-[2-rt: 8.256A(benzylbutyrylamino)ethoxy]phenyl}-MS[M+1]+: 565propionic acidI_240IIa_238(S)-2-(2-Benzoylphenylamino)-3-{4-[3-rt: 8.332A(benzylbutyrylamino)propoxy]phenyl}-MS[M+1]+: 579propionic acidI_241IIa_239(S)-3-{4-12-(Benzoylbenzylamino)-rt: 8.333Aethoxy]phenyl}-2-(2-MS[M+1]+: 599(benzoylphenylamino)propionic acidI_242IIa_240(S)-3-{4-13-(Benzoylbenzylamino)-rt: 8.378Apropoxy]phenyl}-2-(2-MS[M+1]+: 613benzoylphenylamino)propionic acidI_243IIa_241(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.579A{2-[benzyl-(3-phenylacryloyl)amino]-MS[M+1]+: 625ethoxy}phenyl)propionic acidI_244IIa_242(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.68A{3-[benzyl-(3-phenylacryloyl)amino]-MS[M+1]+: 639propoxy}phenyl)propionic acidI_245IIa_243(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.628A{2-[benzyl-(2,2-dimethylpropionyl)-MS[M+1]+: 579amino]ethoxy}phenyl)propionic acidI_246IIa_244(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.656A{3-[benzyl-(2,2-dimethylpropionyl)-MS[M+1]+: 593amino]propoxy}phenyl)propionic acidI_247IIa_245(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.676A{2-[cyclohexyl-(3-furan-2-ylacryloyl)-MS[M+1]+: 607amino]ethoxy}phenyl)propionic acidI_248IIa_246(S)-2-(2-Benzoylphenylamino)-3-{4-[2-rt: 8.913A(cyclobutanecarbonylcyclohexylamino)MS[M+1]+: 569ethoxy]phenyl}propionic acidI_249IIa_247(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.607A{2-[cyclohexyl-(3-MS[M+1]+: 611cyclopentylpropionyl)amino]ethoxy}-phenyl)propionic acidI_250IIa_248(S)-2-(2-Benzoylphenylamino)-3-{4-[2-rt: 8.691A(butyrylcyclohexylamino)ethoxy]-MS[M+1]+: 557phenyl}propionic acidI_251IIa_249(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.536A{2-[cyclopropylmethyl(naphthalene-2-MS[M+1]+: 613carbonyl)amino]ethoxy}phenyl)-propionic acidI_252IIa_250(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.609A{3-[cyclopropylmethyl(naphthalene-2-MS[M+1]+: 627carbonyl)amino]propoxy}phenyl)-propionic acidI_253IIa_251(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.206A{2-[cyclopropylmethyl(quinoline-2-MS[M+1]+: 614carbonyl)amino]ethoxy}phenyl)-propionic acidI_254IIa_252(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.267A{3-[cyclopropylmethyl(quinoline-2-MS[M+1]+: 628carbonyl)amino]propoxy}phenyl)-propionic acidI_255IIa_253(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.084A{2-[cyclopropylmethyl(quinoxaline-2-MS[M+1]+: 615carbonyl)amino]ethoxy}phenyl)-propionic acidI_256IIa_254(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.192A{3-[cyclopropylmethy(quinoxaline-2-MS[M+1]+: 629carbonyl)amino]propoxy}phenyl)-propionic acidI_257IIa_255(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.068A{2-[cyclopropylmethyl(thiophene-2-MS[M+1]+: 569carbonyl)amino]ethoxy}phenyl)-propionic acidI_258IIa_256(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.17A{3-[cyclopropylmethyl(thiophene-2-MS[M+1]+: 583carbonyl)amino]propoxy}phenyl)-propionic acidI_259IIa_257(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 7.1A{2-[cyclopropylmethyl(pyridine-3-MS[M+1]+: 564carbonyl)amino]ethoxy}phenyl)-propionic acidI_260IIa_258(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 7.299A{3-[cyclopropylmethyl(pyridine-3-MS[M+1]+: 578carbonyl)amino]propoxy}phenyl)-propionic acidI_261IIa_259(S)-2-(2-Benzoylphenylamino)-3-{4-[2-rt: 8.179A(cyclopropylmethylphenylacetylamino)MS[M+1]+: 577ethoxy]phenyl}propionic acidI_262IIa_260(S)-2-(2-Benzoylphenylamino)-3-{4-[3-rt: 8.268A(cyclopropylmethylphenylacetylamino)MS[M+1]+: 591propoxy]phenyl}propionic acidI_263IIa_261(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.056A{2-[cyclopropylmethyl-(3-furan-2-MS[M+1]+: 579ylacryloyl)amino]ethoxy}phenyl)-propionic acidI_264IIa_262(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.149A{3-[cyclopropylmethyl-(3-furan-2-MS[M+1]+: 593ylacryloyl)amino]propoxy}phenyl)-propionic acidI_265IIa_263(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.239A{2-[cyclopropylmethyl-(3-thiophen-2-MS[M+1]+: 595ylacryloyl)amino]ethoxy}phenyl)-propionic acidI_266IIa_264(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.342A{3-[cyclopropylmethyl-(3-thiophen-2-MS[M+1]+: 609ylacryloyl)amino]propoxy}phenyl)-propionic acidI_267IIa_265(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.085A{2-[cyclopropylmethyl-(2-thiophen-2-MS[M+1]+: 583ylacetyl)amino]ethoxy}phenyl)-propionic acidI_268IIa_266(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.175A{3-[cyclopropylmethyl-(2-thiophen-2-MS[M+1]+: 597ylacetyl)amino]propoxy}phenyl)-propionic acidI_269IIa_267(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.056A{2-[cyclopropylmethyl-(2-thiophen-3-MS[M+1]+: 583ylacetyl)amino]ethoxy}phenyl)-propionic acidI_270IIa_268(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.142A{3-[cyclopropylmethyl-(2-thiophen-3-MS[M+1]+: 597ylacetyl)amino]propoxy}phenyl)-propionic acidI_271IIa_269(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 6.234A{2-[cyclopropylmethyl-(3-pyridin-3-MS[M+1]+: 592ylpropionyl)amino]ethoxy}phenyl)-propionic acidI_272IIa_270(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 6.385A{3-[cyclopropylmethyl-(3-pyridin-3-MS[M+1]+: 606ylpropionyl)amino]propoxy}phenyl)-popionic acidI_273IIa_271(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.413A{2-[cyclopropylmethyl-(3-MS[M+1]+: 591phenylpropionyl)amino]ethoxy}-phenyl)propionic acidI_274IIa_272(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.488A{3-[cyclopropylmethyl-(3-MS[M+1]+: 605phenylpropionyl)amino]propoxy}-phenyl)propionic acidI_275IIa_273(S)-2-(2-Benzoylphenylamino)-3-{4-[2-rt: 8.16A(cyclobutanecarbonylcyclopropylmethylamino)MS[M+1]+: 541ethoxy]phenyl}propionic acidI_276IIa_274(S)-2-(2-Benzoylphenylamino)-3-{4-[3-rt: 8.24A(cyclobutanecarbonylcyclopropylmethylamino)MS[M+1]+: 555propoxy]phenyl}propionicacidI_277IIa_275(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.907A{2-[(2-cyclohexylacetyl)-MS[M+1]+: 583cyclopropylmethylamino]ethoxy}-phenyl)propionic acidI_278IIa_276(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.975A{3-[(2-cyclohexylacetyl)-MS[M+1]+: 597cyclopropylmethylamino]propoxy}-phenyl)propionic acidI_279IIa_277(S)-2-(2-Benzoylphenylamino)-3-{4-[2-rt: 8.405A(cyclopentanecarbonylcyclopropylmethylamino)MS[M+1]+: 555ethoxy]phenyl}propionicacidI_280IIa_278(S)-2-(2-Benzoylphenylamino)-3-{4-[3-rt: 8.486A(cyclopentanecarbonylcyclopropylmethylamino)MS[M+1]+: 569propoxy]phenyl}propionicacidI_281IIa_279(S)-2-(2-Benzoylphenylamino)-3-{4-[2-rt: 7.808A(cyclopropanecarbonylcyclopropylmethylamino)MS[M+1]+: 527ethoxy]phenyl}propionicacidI_282IIa_280(S)-2-(2-Benzoylphenylamino)-3-{4-[3-rt: 7.905A(cyclopropanecarbonylcyclopropylmethylamino)MS[M+1]+: 541propoxy]phenyl}propionicacidI_283IIa_281(S)-2-(2-Benzoylphenylamino)-3-{4-[2-rt: 7.682A(cyclopropylmethylpropionylamino)-MS[M+1]+: 515ethoxy]phenyl}propionic acidI_284IIa_282(S)-2-(2-Benzoylphenylamino)-3-{4-[3-rt: 7.776A(cyclopropylmethylpropionylamino)-MS[M+1]+: 529propoxy]phenyl}propionic acidI_285IIa_283(S)-2-(2-Benzoylphenylamino)-3-{4-[2-rt: 7.966A(cyclopropylmethylisobutyrylamino)-MS[M+1]+: 529ethoxy]phenyl}propionic acidI_286IIa_284(S)-2-(2-Benzoylphenylamino)-3-{4-[3-rt: 8.056A(cyclopropylmethylisobutyrylamino)-MS[M+1]+: 543propoxy]phenyl}propionic acidI_287IIa_285(S)-2-(2-Benzoylphenylamino)-3-{4-[2-rt: 7.99A(butyrylcyclopropylmethylamino)-MS[M+1]+: 529ethoxy]phenyl}propionic acidI_288IIa_286(S)-2-(2-Benzoylphenylamino)-3-{4-[3-rt: 8.071A(butyrylcyclopropylmethylamino)-MS[M+1]+: 543propoxy]phenyl}propionic acidI_289IIa_287(S)-3-{4-[2-rt: 8.06A(Benzoylcyclopropylmethylamino)-MS[M+1]+: 563ethoxy]phenyl}-2-(2-benzoylphenylamino)propionic acidI_290IIa_288(S)-3-{4-[3-rt: 8.161A(Benzoylcyclopropylmethylamino)-MS[M+1]+: 577propoxy]phenyl}-2-(2-benzoylphenylamino)propionic acidI_291IIa_289(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.338A{2-[cyclopropylmethyl-(3-MS[M+1]+: 589phenylacryloyl)amino]ethoxy}phenyl)-propionic acidI_292IIa_290(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.424A{3-[cyclopropylmethyl-(3-MS[M+1]+: 603phenylacryloyl)amino]propoxy}-phenyl)propionic acidI_293IIa_291(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.404A{2-[(naphthalene-1-carbonyl)-MS[M+1]+: 635phenylamino]ethoxy}phenyl)propionicacidI_294IIa_292(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.588A{3-[(naphthalene-1-carbonyl)-MS[M+1]+: 649phenylamino]propoxy}phenyl)-propionic acidI_295IIa_293(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.618A{2-[(naphthalene-2-carbonyl)-MS[M+1]+: 635phenylamino]ethoxy}phenyl)propionicacidI_296IIa_294(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.762A{3-[(naphthalene-2-carbonyl)-MS[M+1]+: 649phenylamino]propoxy}phenyl)-propionic acidI_297IIa_295(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.095A{2-[(quinoline-2-carbonyl)-MS[M+1]+: 636phenylamino]ethoxy}phenyl)propionicacidI_298IIa_296(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.241A{3-[phenyl(quinoline-2-carbonyl)-MS[M+1]+: 650amino]propoxy}phenyl)propionic acidI_299IIa_297(S)-2-(2-Benzoylphenylamino)-3-(4-rt: —A{2-[phenyl(quinoxaline-2-carbonyl)-MS[M+1]+: 637amino]ethoxy}phenyl)propionic acidI_300IIa_298(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.214A{3-[phenyl(quinoxaline-2-carbonyl)-MS[M+1]+: 651amino]propoxy}phenyl)propionic acidI_301IIa_299(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.259A{2-[phenyl(thiophene-2-carbonyl)-MS[M+1]+: 591amino]ethoxy}phenyl)propionic acidI_302IIa_300(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.416A{3-[phenyl(thiophene-2-carbonyl)-MS[M+1]+: 605amino]propoxy}phenyl)propionic acidI_303IIa_301(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 7.925A{2-[(isoquinoline-3-carbonyl)-MS[M+1]+: 636phenylamino]ethoxy}phenyl)propionicacidI_304IIa_302(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 7.253A{2-[phenyl(pyridine-3-carbonyl)amino]-MS[M+1]+: 586ethoxy}phenyl)propionic acidI_305IIa_303(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 7.434A{3-[phenyl(pyridine-3-carbonyl)amino]-MS[M+1]+: 600propoxy}phenyl)propionic acidI_306IIa_304(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 7.061A{2-[phenyl(pyridine-4-carbonyl)amino]-MS[M+1]+: 586ethoxy}phenyl)propionic acidI_307IIa_305(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 7.261A{3-[phenyl(pyridine-4-carbonyl)amino]-MS[M+1]+: 600propoxy}phenyl)propionic acidI_308IIa_306(S)-2-(2-Benzoylphenylamino)-3-{4-[2-rt: 8.439A(phenylphenylacetylamino)ethoxy]-MS[M+1]+: 599phenyl}propionic acidI_309IIa_307(S)-2-(2-Benzoylphenylamino)-3-{4-[3-rt: 8.619A(phenylphenylacetylamino)propoxy]-MS[M+1]+: 613phenyl}propionic acidI_310IIa_308(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 7.98A{2-[(2-methylacryloyl)phenylamino]-MS[M+1]+: 549ethoxy}phenyl)propionic acidI_311IIa_309(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.146A{2-[(2-methylacryloyl)phenylamino]-MS[M+1]+: 563propoxy}phenyl)propionic acidI_312IIa_310(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.511A{2-[phenyl-(3-phenylpropynoyl)amino]-MS[M+1]+: 609ethoxy}phenyl)propionic acidI_313IIa_311(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.759A{2-[(2-ethylbutyryl)phenylamino]-MS[M+1]+: 579ethoxy}phenyl)propionic acidI_314IIa_312(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.917A{3-[(2-ethylbutyryl)phenylamino]-MS[M+1]+: 593propoxy}phenyl)propionic acidI_315IIa_313(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.259A{2-[(3-furan-2-ylacryloyl)phenylamino]-MS[M+1]+: 601ethoxy}phenyl)propionic acidI_316IIa_314(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.422A{3-[(3-furan-2-ylacryloyl)phenylamino]-MS[M+1]+: 615propoxy}phenyl)propionic acidI_317IIa_315(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.521A{2-[phenyl-(3-thiophen-2-ylacryloyl)-MS[M+1]+: 617amino]ethoxy}phenyl)propionic acidI_318IIa_316(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.677A{3-[phenyl-(3-thiophen-2-ylacryloyl)-MS[M+1]+: 631amino]propoxy}phenyl)propionic acidI_319IIa_317(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.191A{2-[(3-furan-3-yl-(E)-acryloyl)-MS[M+1]+: 601phenylamino]ethoxy}phenyl)propionicacidI_320IIa_318(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.348A{3-[(3-furan-3-yl-(E)-acryloyl)-MS[M+1]+: 615phenylamino]propoxy}phenyl)-propionic acidI_321IIa_319(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 7.217A{2-[phenyl-(3-pyridin-3-yl-(E)-acryloyl)-MS[M+1]+: 612amino]ethoxy}phenyl)propionic acidI_322IIa_320(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 7.417A{3-[phenyl-(3-pyridin-3-yl-(E)-acryloyl)-MS[M+1]+: 626amino]propoxy}phenyl)propionic acidI_323IIa_321(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.471A{2-[phenyl-(3-thiophen-3-yl-(E)-MS[M+1]+: 617acryloyl)amino]ethoxy}phenyl)-propionic acidI_324IIa_322(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.616A{3-[phenyl-(3-thiophen-3-yl-(E)-MS[M+1]+: 631acryloyl)amino]propoxy}phenyl)-propionic acidI_325IIa_323(S)-2-(2-Benzoylphenylamino)-3-{4-[3-rt: 8.213A(but-2-(E)-enoylphenylamino)-MS[M+1]+: 563propoxy]phenyl}propionic acidI_326IIa_324(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.348A{2-[phenyl-(2-thiophen-2-ylacetyl)-MS[M+1]+: —amino]ethoxy}phenyl)propionic acidI_327IIa_325(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.506A{3-[phenyl-(2-thiophen-2-ylacetyl)-MS[M+1]+: 619amino]propoxy}phenyl)propionic acidI_328IIa_326(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.478A{3-[phenyl-(2-thiophen-3-ylacetyl)-MS[M+1]+: 619amino]propoxy}phenyl)propionic acidI_329IIa_327(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.882A{2-[(3,3-dimethylbutyryl)phenylamino]-MS[M+1]+: 579ethoxy}phenyl)propionic acidI_330IIa_328(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.037A{3-[(3,3-dimethylbutyryl)phenylamino]-MS[M+1]+: 593propoxy}phenyl)propionic acidI_331IIa_329(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.503A{2-[(3-methylbutyryl)phenylamino]-MS[M+1]+: 565ethoxy}phenyl)propionic acidI_332IIa_330(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.663A{3-[(3-methylbutyryl)phenylamino]-MS[M+1]+: 579propoxy}phenyl)propionic acidI_333IIa_331(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 6.373A{2-[phenyl-(3-pyridin-3-ylpropionyl)-MS[M+1]+: 614amino]ethoxy}phenyl)propionic acidI_334IIa_332(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 6.561A{3-[phenyl-(3-pyridin-3-ylpropionyl)-MS[M+1]+: 628amino]propoxy}phenyl)propionic acidI_335IIa_333(S)-2-(2-Benzoylphenylamino)-3-{4-[2-rt: 8.317A(pent-4-enoylphenylamino)ethoxy]-MS[M+1]+: 563phenyl}propionic acidI_336IIa_334(S)-2-(2-Benzoylphenylamino)-3-{4-[3-rt: 8.482A(pent-4-enoylphenylamino)propoxy]-MS[M+1]+: 577phenyl}propionic acidI_337IIa_335(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.631A{2-[phenyl-(3-phenylpropionyl)amino]-MS[M+1]+: 613ethoxy}phenyl)propionic acidI_338IIa_336(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.791A{3-[phenyl-(3-phenylpropionyl)amino]-MS[M+1]+: 627propoxy}phenyl)propionic acidI_339IIa_337(S)-2-(2-Benzoylphenylamino)-3-{4-[2-rt: 8.432A(cyclobutanecarbonylphenylamino)-MS[M+1]+: 563ethoxy]phenyl}propionic acidI_340IIa_338(S)-2-(2-Benzoylphenylamino)-3-{4-[3-rt: 8.594A(cyclobutanecarbonylphenylamino)-MS[M+1]+: 577propoxy]phenyl}propionic acidI_341IIa_339(S)-2-(2-Benzoylphenylamino)-3-{4-[2-rt: —A(cyclohexanecarbonylphenylamino)-MS[M+1]+: —ethoxy]phenyl}propionic acidI_342IIa_340(S)-2-(2-Benzoylphenylamino)-3-{4-[3-rt: 8.986A(cyclohexanecarbonylphenylamino)-MS[M+1]+: 605propoxy]phenyl}propionic acidI_343IIa_341(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.466A{2-[(3-cyclohexylpropionyl)-MS[M+1]+: 619phenylamino]ethoxy}phenyl)propionicacidI_344IIa_342(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.587A{3-[(3-cyclohexylpropionyl)-MS[M+1]+: 633phenylamino]propoxy}phenyl)-propionic acidI_345IIa_343(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.175A{2-[(2-cyclohexylacetyl)phenylamino]-MS[M+1]+: 605ethoxy}phenyl)propionicI_346IIa_344(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.316A{3-[(2-cyclohexylacetyl)phenylamino]-MS[M+1]+: 619propoxy}phenyl)propionic acidI_347IIa_345(S)-2-(2-Benzoylphenylamino)-3-{4-[2-rt: 8.68A(cyclopentanecarbonylphenylamino)-MS[M+1]+: 577ethoxy]phenyl}propionic acidI_348IIa_346(S)-2-(2-Benzoylphenylamino)-3-{4-[3-rt: 8.839A(cyclopentanecarbonylphenylamino)-MS[M+1]+: 591propoxy]phenyl}propionic acidI_349IIa_347(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.207A{2-[(3-cyclopentylpropionyl)-MS[M+1]+: 605phenylamino]ethoxy}phenyl)propionicacidI_350IIa_348(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.339A{3-[(3-cyclopentylpropionyl)-MS[M+1]+: 619phenylamino]propoxy}phenyl)-propionic acidI_351IIa_349(S)-2-(2-Benzoylphenylamino)-3-{4-[2-rt: 8.11A(cyclopropanecarbonylphenylamino)-MS[M+1]+: 549ethoxy]phenyl}propionic acidI_352IIa_350(S)-2-(2-Benzoylphenylamino)-3-{4-[3-rt: 8.284A(cyclopropanecarbonylphenylamino)-MS[M+1]+: 563propoxy]phenyl}propionic acidI_353IIa_351(S)-2-(2-Benzoylphenylamino)-3-{4-[2-rt: 7.965A(phenylpropionylamino)ethoxy]-MS[M+1]+: 537phenyl}propionic acidI_354IIa_352(S)-2-(2-Benzoylphenylamino)-3-{4-[3-rt: 8.138A(phenylpropionylamino)propoxy]-MS[M+1]+: 551phenyl}propionic acidI_355IIa_353(S)-2-(2-Benzoylphenylamino)-3-{4-[2-rt: 8.246A(isobutyrylphenylamino)ethoxy]-MS[M+1]+: 551phenyl}propionic acidI_356IIa_354(S)-2-(2-Benzoylphenylamino)-3-{4-[3-rt: 8.411A(isobutyrylphenylamino)propoxy]-MS[M+1]+: 656phenyl}propionic acidI_357IIa_355(S)-2-(2-Benzoylphenylamino)-3-{4-[2-rt: 8.850A(hexanoylphenylamino)ethoxy]-MS[M+1]+: 579phenyl}propionic acidI_358IIa_356(S)-2-(2-Benzoylphenylamino)-3-{4-[3-rt: 8.996A(hexanoylphenylamino)propoxy]-MS[M+1]+: 593phenyl}propionic acidI_359IIa_357(S)-2-(2-Benzoylphenylamino)-3-{4-[2-rt: 8.535A(pentanoylphenylamino)ethoxy]-MS[M+1]+: 565phenyl}propionic acidI_360IIa_358(S)-2-(2-Benzoylphenylamino)-3-{4-[3-rt: 8.691A(pentanoylphenylamino)propoxy]-MS[M+1]+: 579phenyl}propionic acidI_361IIa_359(S)-2-(2-Benzoylphenylamino)-3-{4-[2-rt: 9.465A(octanoylphenylamino)ethoxy]phenyl}-MS[M+1]+: 607propionic acidI_362IIa_360(S)-2-(2-Benzoylphenylamino)-3-{4-[3-rt: 9.587A(octanoylphenylamino)propoxy]-MS[M+1]+: 621phenyl}propionic acidI_363IIa_361(S)-2-(2-Benzoylphenylamino)-3-{4-[2-rt: 9.168A(heptanoylphenylamino)ethoxy]-MS[M+1]+: 593phenyl}propionic acidI_364IIa_362(S)-2-(2-Benzoylphenylamino)-3-{4-[3-rt: 9.302A(heptanoylphenylamino)propoxy]-MS[M+1]+: 607phenyl}propionic acidI_365IIa_363(S)-2-(2-Benzoylphenylamino)-3-{4-[2-rt: 9.736A(nonanoylphenylamino)ethoxy]-MS[M+1]+: 621phenyl}propionic acidI_366IIa_364(S)-2-(2-Benzoylphenylamino)-3-{4-[3-rt: 9.85A(nonanoylphenylamino)propoxy]-MS[M+1]+: 635phenyl}propionic acidI_367IIa_365(S)-2-(2-Benzoylphenylamino)-3-{4-[2-rt: 8.259A(butyrylphenylamino)ethoxy]phenyl}-MS[M+1]+: 551propionic acidI_368IIa_366(S)-2-(2-Benzoylphenylamino)-3-{4-[3-rt: 8.426A(butylylphenylamino)propoxy]phenyl}-MS[M+1]+: 565propionic acidI_369IIa_367(S)-2-(2-Benzoylphenylamino)-3-{4-[2-rt: 8.172A(benzoylphenylamino)ethoxy]phenyl}-MS[M+1]+: 585propionic acidI_370IIa_368(S)-2-(2-Benzoylphenylamino)-3-{4-[3-rt: 8.348A(benzoylphenylamino)propoxy]-MS[M+1]+: 599phenyl}propionic acidI_371IIa_369(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.647A{2-[phenyl-(3-phenylacryloyl)amino]-MS[M+1]+: 611ethoxy}phenyl)propionic acidI_372IIa_370(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.81A{3-[phenyl-(3-phenylacryloyl)amino]-MS[M+1]+: 625propoxy}phenyl)propionic acidI_373IIa_371(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.661A{2-[(2,2-dimethylpropionyl)-MS[M+1]+: 565phenylamino]ethoxy}phenyl)propionicacidI_374IIa_372(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.79A{3-[(2,2-dimethylpropionyl)-MS[M+1]+: 579phenylamino]propoxy}phenyl)-propionic acidI_375IIa_373(S)-2-(2-Benzoylphenylamino)-3-{4-[2-rt: 8.443A(tert-butylcyclobutanecarbonylamino)-MS[M+1]+: 543ethoxy]phenyl}propionic acidI_376IIa_374(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.194A{2-[tert-butyl-(3-cyclopentylpropionyl)-MS[M+1]+: 585amino]ethoxy}phenyl)propionic acidI_377II_1(S)-2-(2-Benzoylphenylamino)-3-{4-[2-8.98(bs, 1H), 7.56(d,A(benzylindan-5-ylamino)ethoxy]-2H), 7.45-7.37(ca, 5H),phenyl}propionic acid7.27-7.19(ca, 8H),7.01(t, 1H), 6.71-6.65(ca,3H), 6.54-6.41(ca, 2H),4.60(s, 2H), 4.27(m,1H), 4.07(t, 2H),3.76(t, 2H), 3.27(dd, 1H),3.08(m, 1H), 2.80(ca,4H), 2.01(ca, 2H)I_378II_2(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.342A{2-[benzyl(2,6-difluorophenyl)amino]-MS[M+1]+: 607ethoxy}phenyl)propionic acidI_379II_3(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.516A{2-[(2-chlorophenyl)-(2-fluorobenzyl)-MS[M+1]+: 624amino]ethoxy}phenyl)propionic acidI_380II_4(S)-2-(2-Benzoylphenylamino)-3-(4-8.98(bs, 1H), 7.56(d,A{2-[benzyl-(2-fluorophenyl)amino]-2H), 7.46-7.37(ca, 5H),ethoxy}phenyl)propionic acid7.32-7.18(m, 9H),6.98-6.91(ca, 2H),6.70-6.65(ca, 3H), 6.44(t, 1H),4.46(s, 2H), 4.27(m,1H), 3.99(t, 2H),3.56(t, 2H), 3.27(m, 1H),3.08(m, 1H)I_381II_5(S)-2-(2-Benzoylphenylamino)-3-(4-8.88(bs, 1H), 7.57(d,A{2-[(2-methylbenzyl)phenylamino]-2H), 7.55-7.32(ca, 6H),ethoxy}phenyl)propionic acid7.24-7.09(ca, 8H),6.75-6.64(ca, 5H),6.58(t, 1H), 4.55(s, 2H),4.33(m, 1H), 4.11(t,2H), 3.80(t, 2H),3.25(m, 1H), 3.09(m, 1H),2.34(s, 3H)I_382II_6(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.546A{2-[(3-chlorophenyl)-(2-MS[M+1]+: 636methoxybenzyl)amino]ethoxy}phenyl)-propionic acidI_383II_7(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.461A{2-[(2-methoxybenzyl)-m-tolylamino]-MS[M+1]+: 615ethoxy}phenyl)propionic acidI_384II_8(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.292A{3-[(2-methoxybenzyl)phenylamino]-MS[M+1]+: 615propoxy}phenyl)propionic acidI_385II_9(S)-2-(2-Benzoylphenylamino)-3-{4-[2-rt: 9.523A(benzyl-o-tolylamino)ethoxy]phenyl}-MS[M+1]+: 585propionic acidI_386II_10(S)-2-(2-Benzoylphenylamino)-3-(4-8.98(bs, 1H), 7.56(d,A{2-[benzyl-(3-ethylphenyl)amino]-2H), 7.45-7.37(ca, 5H),ethoxy}phenyl)propionic acid7.28-7.20(m, 9H),7.08(t, 1H), 6.70(d, 2H),6.58-6.52(ca, 2H),6.43(t, 1H), 4.62(s, 2H),4.27(m, 1H), 4.09(t,2H), 3.78(t, 2H),3.27(m, 1H), 3.08(m, 1H),2.53(q, 2H), 1.14(t,3H)I_387II_11(S)-2-(2-Benzoylphenylamino)-3-(4-8.98(bs, 1H), 7.56(d,A{2-[benzyl-(3-fluorophenyl)amino]-2H), 7.46-7.37(ca, 5H),ethoxy}phenyl)propionic acid7.31-7.17(ca, 8H),7.08(m, 1H), 6.70(ca, 3H),6.48-6.32(ca, 3H),4.62(s, 2H), 4.27(m, 1H),4.08(t, 2H), 3.78(t,2H), 3.27(dd, 1H),3.08(m, 1H)I_388II_12(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.428A{2-[(2-chlorophenyl)-(3-MS[M+1]+: 636methoxybenzyl)amino]ethoxy}phenyl)-propionic acidI_389II_13(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.375A{2-[(3-chlorophenyl)-(3-MS[M+1]+: 636methoxybenzyl)amino]ethoxy}phenyl)-propionic acidI_390II_14(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.354A{2-[(3-methoxybenzyl)-m-tolylamino]-MS[M+1]+: 615ethoxy}phenyl)propionic acidI_391II_15(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.259A{3-[(3-methoxybenzyl)phenylamino]-MS[M+1]+: 615propoxy}phenyl)propionic acidI_392II_16(S)-2-(2-Benzoylphenylamino)-3-{4-[2-8.98(bs, 1H), 7.56(d,A(benzyl-m-tolylamino)ethoxy]phenyl}-2H), 7.45-7.37(ca, 5H),propionic acid7.27-7.19(ca, 7H),7.05(t, 1H), 6.71-6.68(ca,3H), 6.56-6.42(ca, 4H),4.61(s, 2H), 4.28(m,1H), 4.07(t, 2H),3.77(t, 2H), 3.26(dd, 1H),3.06(m, 1H), 2.25(s,3H)I_393II_17(S)-2-(2-Benzoylphenylamino)-3-(4-8.98(bs, 1H), 7.56(d,A{2-[benzyl-(4-chlorophenyl)amino]-2H), 7.47-7.39(ca, 5H),ethoxy}phenyl)propionic acid7.30-7.16(ca, 8H),7.08(d, 2H), 6.72-6.61(ca,4H), 6.44(t, 1H),4.60(s, 2H), 4.27(m, 1H),4.07(t, 2H), 3.77(t,2H), 3.26(dd, 1H),3.08(m, 1H)I_394II_18(S)-2-(2-Benzoylphenylamino)-3-(4-8.98(bs, 1H), 7.56(d,A{2-[benzyl-(4-fluorophenyl)amino]-2H), 7.46-7.37(ca, 5H),ethoxy}phenyl)propionic acid7.32-7.19(ca, 8H),6.89-6.84(ca, 2H),6.72-6.61(ca, 4H),6.44(t, 1H), 4.57(s, 2H),4.28(m, 1H), 4.06(t,2H), 3.75(t, 2H),3.27(dd, 1H), 3.08(m, 1H)I_395II_19(S)-2-(2-Benzoylphenylamino)-3-(4-8.96(bs, 1H), 7.55(d,A{2-[(4-methylbenzyl)phenylamino]-2H), 7.46-7.37(ca, 5H),ethoxy}phenyl)propionic acid7.24-7.09(m, 9H),6.72-6.64(ca, 5H), 6.45(t,1H), 4.58(s, 2H),4.27(m, 1H), 4.06(t, 2H),3.77(t, 2H), 3.27(dd,1H), 3.08(m, 1H),2.30(s, 3H)I_396II_20(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.178A{3-[(4-methoxybenzyl)phenylamino]-MS[M+1]+: 615propoxy}phenyl)propionic acidI_397II_21(S)-2-(Benzoylphenylamino)-3-{4-[2-8.96(bs, 1H), 7.53(d,A(di-p-tolylamino)ethoxy]phenyl}-2H), 7.48-7.35(ca, 5H),propionic acid7.22-7.15(m, 9H),7.03(d, 1H), 6.89(d, 1H),6.69-6.65(ca, 3H),6.43(t, 1H), 4.23(m, 1H),4.02(bs, 4H), 3.25(m,1H), 3.05(m, 1H),2.27(s, 6H)..I_398II_22(S)-2-(2-Benzoylphenylamino)-3-{4-[2-8.83(bs, 1H),A(benzyl-p-tolylamino)ethoxy]phenyl}-7.50-6.93(ca, 17H),propionic acid6.60-6.55(ca, 4H), 6.34(t, 1H),4.53(s, 2H), 4.21(m,1H), 3.93(t, 2H),3.62(t, 2H), 3.17(dd, 1H),2.98(m, 1H), 2.19(s,3H)I_399II_23(S)-2-(2-Benzoylphenylamino)-3-{4-[3-rt: 9.736A(benzylindan-5-ylamino)propoxy]-MS[M+1]+: 625phenyl}propionic acidI_400II_24(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.747A{3-[benzyl-(3-ethylphenyl)amino]-MS[M+1]+: 613propoxy}phenyl)propionic acidI_401II_25(S)-2-(2-Benzoylphenylamino)-3-{4-[3-rt: 9.549A(benzyl-m-tolylamino)propoxy]-MS[M+1]+: 599phenyl}propionic acidI_402II_26(S)-2-(2-Benzoylphenylamino)-3-{4-[3-rt: 9.526A(benzyl-p-tolylamino)propoxy]phenyl}-MS[M+1]+: 599propionic acidI_403II_27(S)-2-(2-Benzoylphenylamino)-3-{4-[3-rt: 6.67A(benzylcyclohexylamino)propoxy]-MS[M+1]+: 591phenyl}propionic acid methyl esterI_404II_28(S)-2-(2-Benzoylphenylamino)-3-{4-[3-8.92(bs, 1H), 7.56(d,A(benzyphenylamino)propoxy]phenyl}-2H), 7.46-7.37(ca, 5H),propionic acid7.30-7.10(ca, 10H),6.76-6.61(ca, 5H),6.44(t, 1H), 4.53(s, 2H),4.28(m, 1H), 3.92(t,2H), 3.62(t, 2H),3.22(dd, 1H), 3.10(m, 1H),2.09-1.98(ca, 2H)I_405II_29(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.565A{2-[(2-fluorophenyl)isobutylamino]-MS[M+1]+: 555ethoxy}phenyl)propionic acidI_406II_30(S)-2-(2-Benzoylphenylamino)-3-{4-[2-rt: 9.729A(isobutyl-o-tolylamino)ethoxy]phenyl}-MS[M+1]+: 551propionic acidI_407II_31(S)-2-(2-Benzoylphenylamino)-3-{4-[3-rt: 9.443A(isobutyl-o-tolylamino)propoxy]-MS[M+1]+: 565phenyl}propionic acidI_408II_32(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.445A{2-[(3-fluorophenyl)isobutylamino]-MS[M+1]+: 555ethoxy}phenyl)propionic acidI_409II_33(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.65A{2-[isobutyl-m-tolylamino]ethoxy}-MS[M+1]+: 551phenyl)propionic acidI_410II_34(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.573A{3-[isobutyl-m-tolylamino]propoxy}-MS[M+1]+: 565phenyl)propionic acidI_411II_35(S)-2-(2-Benzoylphenylamino)-3-{4-[2-8.99(bs, 1H), 7.57(d,A(benzylphenethylamino)ethoxy]-2H), 7.46-7.36(ca, 4H),phenyl}propionic acid7.32-7.21(ca, 11H),7.13(d, 2H),6.73-6.69(ca, 3H), 6.44(t, 1H),4.23(m, 1H), 3.94(t,2H), 3.76(s, 2H),3.27(m, 1H), 3.07(m, 1H),2.93(t, 2H), 2.81(bs,4H)I_412II_36(S)-2-(2-Benzoylphenylamino)-3-{4-[2-rt: 9.089A(cyclobutylmethyl-o-tolylamino)-MS[M+1]+: 563ethoxy]phenyl}propionic acidI_413II_37(S)-2-(2-Benzoylphenylamino)-3-{4-[2-rt: 6.418A(benzylcyclopentylamino)ethoxy]-MS[M+1]+: 563phenyl}propionic acidI_414II_38(S)-2-(2-Benzoylphenylamino)-3-{4-[3-rt: 6.97A(cyclopentylphenylamino)propoxy]-MS[M+1]+: 563phenyl}propionic acidI_415II_39(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.937A{2-[cyclopentylmethyl-(2-MS[M+1]+: 581fluorophenyl)amino]ethoxy}phenyl)-propionic acidI_416II_40(S)-2-(2-Benzoylphenylamino)-3-{4-[2-8.84(bs, 1H),A(cyclopentylmethylphenylamino)-7.57-7.41(ca, 7H), 7.22-7.16(ca,ethoxy]phenyl}propionic acid4H), 6.75-6.55(ca, 7H),4.31(ca, 3H), 3.98(t,1H), 3.71(t, 2H),3.30-3.20(ca, 3H), 3.09(m,1H), 2.29(m, 1H),1.75-1.54(ca, 8H)I_417II_41(S)-2-(2-Benzoylphenylamino)-3-{4-[2-rt: 6.432A(benzylcyclopropylmethylamino)-MS[M+1]+: 549ethoxy]phenyl}propionic acidI_418II_42(S)-2-(2-Benzoylphenylamino)-3-{4-[3-rt: 6.47A(benzylcyclopropylmethylamino)-MS[M+1]+: 563propoxy]phenyl}propionic acidI_419II_43(S)-2-(2-Benzoylphenylamino)-3-(4-8.98(bs, 1H), 7.57(d,A{2-[(2-methoxybenzyl)phenylamino]-2H), 7.48-7.39(ca, 5H),ethoxy}phenyl)propionic acid7.27-7.13(ca, 6H),7.05(d, 1H), 6.88-6.80(ca,2H), 6.73-6.60(ca, 5H),6.44(t, 1H), 4.59(s,2H), 4.27(m, 1H),4.10(t, 2H), 3.85(s, 3H),3.79(t, 2H), 3.27(dd,1H), 3.08(m, 1H)I_420II_44(S)-2-(2-Benzoylphenylamino)-3-(4-8.98(bs, 1H), 7.57(d,A{2-[(3-methoxybenzyl)phenylamino]-2H), 7.48-7.39(ca, 5H),ethoxy}phenyl)propionic acid7.27-7.13(ca, 6H),6.85-6.62(ca, 8H),6.44(t, 1H), 4.60(s, 2H),4.27(m, 1H), 4.10(t,2H), 3.85(s, 3H),3.79(t, 2H), 3.27(m, 1H),3.08(m, 1H)I_421II_45(S)-2-(2-Benzoylphenylamino)-3-(4-8.97(bs, 1H),A{2-[(3-methoxyphenyl)phenylamino]-7.55-7.3(ca, 6H), 7.28-6.95(ca,ethoxy}phenyl)propionic acid11H), 6.68-6.40(ca,5H), 4.23(m, 1H),4.05(bs, 4H), 3.71(s, 3H),3.25(m, 1H), 3.05(m,1H)I_422II_46(S)-2-(2-Benzoylphenylamino)-3-(4-8.98(bs, 1H), 7.57(d,A{2-[(4-methoxybenzoyl)phenylamino]-2H), 7.48-7.39(ca, 5H),ethoxy}phenyl)propionic acid7.27-7.13(ca, 7H),6.85(d, 2H), 6.75-6.60(ca,5H), 6.42(t, 1H),4.59(s, 2H), 4.27(m, 1H),4.10(t, 2H), 3.79(ca,2H), 3.76(s, 3H),3.27(m, 1H), 3.08(m, 1H)I_423II_47(S)-2-(2-Benzoylphenylamino)-3-(4-t: 9.939A{2-[(4-tert-butylbenzyl)phenylamino]-MS[M+1]+: 627ethoxy}phenyl)propionic acidI_424II_48(S)-2-(2-Benzoylphenylamino)-3-{4-[2-8.70(d, 1H),A(benzylphenylamino)ethoxy]phenyl}-7.60-7.40(ca, 4H), 7.40-7.10(m,propionic acid9H), 7.10-7.00(ca, 4H),6.80-6.60(ca, 4H),7.60-7.45(ca, 2H),4.60(s, 2H), 4.31(bs, 1H)4.07(t, 2H), 3.77(t,2H), 3.13(dd, 1H),2.96(dd, 1H).I_425II_49(S)-2-(2-Benzoylphenylamino)-3-{4-[2-8.98(d, 1H), 7.56(d,A(cyclobutylmethylphenylamino)-2H), 7.46-7.38(ca, 4H),ethoxy]phenyl}propionic acid7.21-7.15(ca, 5H),6.73-6.63(ca, 6H),6.45(t, 1H), 4.27(m, 1H),3.97(t, 2H), 3.68(t,2H), 3.37(d, 2H),3.26(dd, 1H), 2.68(m, 1H),2.03-1.70(ca, 6H)I_426II_50(S)-2-(2-Benzoylphenylamino)-3-{4-[2-rt: 9.029A(cyclohexylphenylamino)ethoxy]-MS[M+1]+: 563phenyl}propionic acidI_427II_51(S)-2-(2-Benzoylphenylamino)-3-{4-[2-8.98(d, 1H), 7.57(d,A(cyclohexylmethylphenylamino)-2H), 7.46-7.38(ca, 4H),ethoxy]phenyl}propionic acid7.21-7.15(ca, 6H),6.67-6.63(ca, 5H),6.44(t, 1H), 4.27(m, 1H),3.98(t, 2H), 3.70(t,2H), 3.26(dd, 1H),3.17(d, 2H), 3.06(m, 1H),1.80-1.50(ca, 11H)I_428II_52(S)-2-(2-Benzoylphenylamino)-3-{4-[2-rt: 7.669A(cyclopentylphenylamino)ethoxy]-MS[M+1]+: 549phenyl}propionic acidI_429II_53(S)-2-(2-Benzoylphenylamino)-3-{4-[2-8.98(bs, 1H), 7.56(d,A(cyclopropylmethylphenylamino)-2H), 7.44-7.40(ca, 4H),ethoxy]phenyl}propionic acid7.23-7.18(ca, 6H),6.78-6.66(ca, 5H),6.44(t, 1H), 4.27(m, 1H),4.04(t, 2H), 3.76(t,2H), 3.29-3.24(ca, 3H),3.06(m, 1H),1.00-0.80(m, 1H), 0.54-0.40(ca,2H), 0.26-0.21(ca, 2H)I_430II_54(S)-2-(2-Benzoylphenylamino)-3-{4-[2-8.62(d, 1H),A(diphenylamino)ethoxy]phenyl}-7.60-7.44(ca, 4H), 7.38(t, 1H),propionic acid7.32(dd, 2H), 7.24(td,4H), 7.07(d, 2H),6.99(d, 4H), 6.91(t, 2H),6.82(d, 1H), 6.73(d,2H), 6.57(t, 1H),4.50(m, 1H), 4.05(s, 4H),3.25-2.95(ca, 2H).I_431IIa_375(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.502A{2-[(2-methylacryloyl)naphthalen-1-MS[M+1]+: 599ylamino]ethoxy}phenyl)propionic acidI_432IIa_376(S)-2-(2-Benzoylphenylamino)-3-{4-[2-rt: 8.432A(but-2-(E)-enoylnaphthalen-1-MS[M+1]+: 599ylamino)ethoxy]phenyl}propionic acidI_433IIa_377(S)-2-(2-Benzoylphenylamino)-3-{4-[2-rt: 8.485A(cyclopropanecarbonylnaphthalen-1-MS[M+1]+: 587ylamino)ethoxy]phenyl}propionic acidI_434IIa_378(S)-2-(2-Benzoylphenylamino)-3-{4-[2-rt: 8.563A(naphthalen-1-ylpropionylamino)-MS[M+1]+: 599ethoxy]phenyl}propionic acidI_435IIa_379(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.599A{2-[(2-methylacryloyl)naphthalen-2-MS[M+1]+: 599ylamino]ethoxy}phenyl)propionic acidI_436IIa_380(S)-2-(2-Benzoylphenylamino)-3-{4-[2-rt: 8.491A(but-2-(E)-enoylnaphthalen-2-MS[M+1]+: 599ylamino)ethoxy]phenyl}propionic acidI_437IIa_381(S)-2-(2-Benzoylphenylamino)-3-{4-[2-rt: 8.494A(naphthalen-2-ylpropionylamino)-MS[M+1]+: 587ethoxy]phenyl}propionic acidI_438IIa_382(S)-3-{4-[2-(Acetylnaphthalen-2-rt: 8.099Aylamino)ethoxy]phenyl}-2-(2-MS[M+1]+: 573benzoylphenylamino)propionic acidI_439IIa_383(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.343A{2-[(2-methylacryloyl)-(3-MS[M+1]+: 595methylsulfanylphenyl)amino]ethoxy}-phenyl)propionic acidI_440IIa_334(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.261A{2-[but-2-(E)-enoyl-(3-MS[M+1]+: 595methylsulfanylphenyl)amino]ethoxy}-phenyl)propionic acidI_441IIa_385(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.51A{2-[butyryl-(3-methylsulfanylphenyl)-MS[M+1]+: 597amino]ethoxy}phenyl)propionic acidI_442IIa_386(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.36A{2-[(2-methylacryloyl)-(4-MS[M+1]+: 595methylsulfanylphenyl)amino]ethoxy}-phenyl)propionic acidI_443IIa_387(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.262A{2-[but-2-(E)-enoyl-(4-MS[M+1]+: 595methylsulfanylphenyl)amino]ethoxy}-phenyl)propionic acidI_444IIa_388(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.519A{2-[isobutyryl-(4-MS[M+1]+: 597methylsulfanylphenyl)amino]ethoxy}-phenyl)propionic acidI_445IIa_389(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.522A{2-[butyryl-(4-methylsulfanylphenyl)-MS[M+1]+: 597amino]ethoxy}phenyl)propionic acidI_446IIa_390(S)-3-{4-[2-Acetylnaphthalen-1-rt: 8.599Aylamino)ethoxy]phenyl}-2-(2-MS[M+1]+: —benzoylphenylamino)propionic acidI_447IIa_391(S)-2-(2-Benzoylphenylamino)-3-{4-[2-rt: 8.627A(cyclopropanecarbonylnaphthalen-2-MS[M+1]+: —ylamino)ethoxy]phenyl}propionic acidI_448IIa_392(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.464A{3-[butyryl-(2-fluorophenyl)amino]-MS[M+1]+: 583propoxy}phenyl)propionic acidI_449IIa_393(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.603A{3-[cyclobutanecarbonyl-(2-MS[M+1]+: 595fluorophenyl)amino]propoxy}phenyl)-propionic acidI_450IIa_394(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.269A{3-[cyclopropanecarbonyl-(2-MS[M+1]+: 581fluorophenyl)amino]propoxy}phenyl)-propionic acidI_451IIa_395(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.451A{3-[(2-fluorophenyl)isobutyrylamino]-MS[M+1]+: 583propoxy}phenyl)propionic acidI_452II_55(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 10.216A{2-[cyclohexylmethyl-(2-fluorophenyl)-MS[M+1]+: 595amino]ethoxy}phenyl)propionic acidI_453II_56(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 10.146A{2-[(3-chlorophenyl)-MS[M+1]+: 597, 599cyclopentylmethylamino]ethoxy}-phenyl)propionic acidI_454II_57(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.757A{3-[cyclobutylmethyl-(3-fluorophenyl)-MS[M+1]+: 581amino]propoxy}phenyl)propionic acidI_455II_58(S)-2-(2-Benzoylphenylamino)-3-{4-[3-rt: 8.973A(cyclobutylmethyl-m-tolylamino)-MS[M+1]+: 577propoxy]phenyl}propionic acidI_456II_59(R)-2-(2-Benzoylphenylamino)-3-{4-rt: 9.268A[2-(benzylphenylamino)ethoxy]-MS[M+1]+: 571phenyl}propionic acidI_457II_60(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 10.276A{2-[(2-chlorophenyl)-MS[M+1]+: 597, 599cyclopentylmethylamino]ethoxy}-phenyl)propionic acidI_458II_61(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.166A{2-[(2-fluorophenyl)thiophen-2-MS[M+1]+: 595ylmethylamino]ethoxy}phenyl)-propionic acidI_459II_62(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.755A{3-[(2-fluorophenyl)isobutylamino]-MS[M+1]+: 569propoxy}phenyl)propionic acidI_460II_63(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 10.09A{3-[cyclopentylmethyl-(2-MS[M+1]+: 595fluorophenyl)amino]propoxy}phenyl)-propionic acidI_461II_64(S)-2-(2-Benzoylphenylamino)-3-{4-[3-rt: 8.508A(cyclobutylmethyl-o-tolylamino)-MS[M+1]+: 577propoxy]phenyl}propionic acidI_462II_65(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.089A{2-[(3-fluorophenyl)thiophen-2-MS[M+1]+: 595ylmethylamino]ethoxy}phenyl)-propionic acidI_463II_66(S)-2-(2-Benzoylphenylamino)-3-{4-[2-rt: 9.325A(thiophen-2-ylmethyl-m-tolylamino)-MS[M+1]+: 591ethoxy]phenyl}propionic acidI_464II_67(S)-2-(2-Benzoylphenylamino)-3-{4-[3-rt: 9.412A(thiophen-3-ylmethyl-m-tolylamino)-MS[M+1]+: 605propoxy]phenyl}propionic acid methylesterI_465II_68(S)-2-(2-Benzoylphenylamino)-3-{4-[3-rt: 9.242A(furan-2-ylmethyl-m-tolylamino)-MS[M+1]+: 589propoxy]pheny}propionic acidI_466II_69(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 9.077A{2-[(4-fluorophenyl)thiophen-2-MS[M+1]+: 595ylmethylamino]ethoxy}phenyl)-propionic acidI_467II_70(S)-2-(2-Benzoylphenylamino)-3-{4-[2-rt: 9.11A(phenylthiophen-2-ylmethylamino)-MS[M+1]+: 577ethoxy]phenyl}propionic acidI_468II_71(S)-2-(2-Benzoylphenylamino)-3-{4-[3-rt: 9.251A(phenylthiophen-2-ylmethylamino)-MS[M+1]+: 591propoxy]phenyl}propionic acidI_469IIa_396(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 7.751A{2-[benzyl-(3-methoxypropionyl)-MS[M+1]+: 581amino]ethoxy}phenyl)propionic acidI_470IIa_397(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 7.849A{3-[benzyl-(3-methoxypropionyl)-MS[M+1]+: 595amino]propoxy}phenyl)propionic acidI_471IIa_398(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 7.665A{2-[(3-methoxypropionyl)-MS[M+1]+: 567phenylamino]ethoxy}phenyl)propionicacidI_472IIa_399(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 7.85A{3-[(3-methoxypropionyl)-MS[M+1]+: 581phenylamino]propoxy}phenyl)-propionic acidI_473IIa_400(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.169A{3-[(2-fluorophenyl)propionylamino]-MS[M+1]+: 569propoxy}phenyl)propionic acidI_474IIa_401(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.514A{3-[(2-fluorophenyl)pent-4-MS[M+1]+: 595enoylamino]propoxy}phenyl)propionicacidI_475IIa_402(S)-3-(4-{3-[Acryloyl-(2-fluorophenyl)-rt: 8.046Aamino]propoxy}phenyl)-2-(2-MS[M+1]+: 567benzoylphenylamino)propionic acidI_476IIa_403(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.208A{3-[but-2-(E)-enoyl-(2-fluorophenyl)-MS[M+1]+: 581amino]propoxy}phenyl)propionic acidI_477IIa_404(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.701A{3-[(2-fluorophenyl)-(3-methylbutyryl)-MS[M+1]+: 597amino]propoxy}phenyl)propionic acidI_478IIa_405(R)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.24A{2-[phenyl(thiophene-2-carbonyl)-MS[M+1]+: 579amino]ethoxy}phenyl)propionic acidI_479IIa_406(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.243A{3-[(2-fluorophenyl)-(2-MS[M+1]+: 581methylacryloyl)amino]propoxy}-phenyl)propionic acidI_480IIa_407(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.232A{3-[(3-fluorophenyl)-(2-MS[M+1]+: 581methylacryloyl)amino]propoxy}-phenyl)propionic acidI_481IIa_408(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.038A{2-[but-2-(E)-enoyl-(2-MS[M+1]+: 579methoxyphenyl)amino]ethoxy}phenyl)-propionic acidI_482IIa_409(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.053A{2-[but-2-(E)-enoyl-(3-MS[M+1]+: 579methoxyphenyl)amino]ethoxy}phenyl)-propionic acidI_483IIa_410(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.541A{2-[(2-methoxyphenyl)-(3-MS[M+1]+: 595methylbutyryl)amino]ethoxy}phenyl)-propionic acidI_484IIa_411(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.701A{3-[(3-fluorophenyl)-(3-methylbutyryl)-MS[M+1]+: 597amino]propoxy}phenyl)propionic acidI_485IIa_412(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.479A{2-[(3-methoxyphenyl)-(3-MS[M+1]+: 595methylbutyryl)amino]ethoxy}phenyl)-propionic acidI_486IIa_413(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.513A{3-[(3-fluorophenyl)pent-4-MS[M+1]+: 595enoylamino]propoxy}phenyl)propionicacidI_487IIa_414(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.596A{3-[cyclobutanecarbonyl-(3-MS[M+1]+: 595fluorophenyl)amino]propoxy}phenyl)-propionic acidI_488IIa_415(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.583A{3-[cyclobutanecarbonyl-(4-MS[M+1]+: 595fluorophenyl)amino]propoxy}phenyl)-propionic acidI_489IIa_416(R)-2-(2-Benzoylphenylamino)-3-{4-rt: 8.416A[2-(cyclobutanecarbonylphenylamino)-MS[M+1]+: 563ethoxy]phenyl}propionic acidI_490IIa_417(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.082A{2-[cyclopropanecarbonyl-(2-MS[M+1]+: 579methoxyphenyl)amino]ethoxy}phenyl)-propionic acidI_491IIa_418(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.313A{3-[cyclopropanecarbonyl-(3-MS[M+1]+: 581fluorophenyl)amino]propoxy}phenyl)-propionic acidI_492IIa_419(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.293A{3-[cyclopropanecarbonyl-(4-MS[M+1]+: 581fluorophenyl)amino]propoxy}phenyl)-propionic acidI_493IIa_420(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 7.996A{2-[(2-methoxyphenyl)-MS[M+1]+: 567propionylamino]ethoxy}phenyl)-propionic acidI_494IIa_421(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.175A{3-[(3-fluorophenyl)propionylamino]-MS[M+1]+: 569propoxy}phenyl)propionic acidI_495IIa_422(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 7.947A{2-[(3-methoxyphenyl)-MS[M+1]+: 567propionylamino]ethoxy}phenyl)-propionic acidI_496IIa_423(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.16A{3-[(4-fluorophenyl)propionylamino]-MS[M+1]+: 569propoxy}phenyl)propionic acidI_497IIa_424(R)-2-(2-Benzoylphenylamino)-3-{4-rt: 7.952A[2-(phenylpropionylamino)ethoxy]-MS[M+1]+: 593phenyl}propionic acidI_498IIa_425(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.434A{3-[(3-fluorophenyl)isobutyrylamino]-MS[M+1]+: 583propoxy}phenyl)propionic acidI_499IIa_426(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.218A{2-[isobutyryl-(3-methoxyphenyl)-MS[M+1]+: 581amino]ethoxy}phenyl)propionic acidI_500IIa_427(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.424A{3-[(4-fluorophenyl)isobutyrylamino]-MS[M+1]+: 583propoxy}phenyl)propionic acidI_501IIa_428(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.73A{3-[(2-fluorophenyl)pentanoylamino]-MS[M+1]+: 597propoxy}phenyl)propionic acidI_502IIa_429(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.726A{3-[(3-fluorophenyl)pentanoylamino]-MS[M+1]+: 597propoxy}phenyl)propionic acidI_503IIa_430(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.274A{2-[butyryl-(2-methoxyphenyl)amino]-MS[M+1]+: 581ethoxy}phenyl)propionic acidI_504IIa_431(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.447A{3-[butyryl-(3-fluorophenyl)amino]-MS[M+1]+: 583propoxy}phenyl)propionic acidI_505IIa_432(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.222A{2-[butyryl-(3-methoxyphenyl)amino]-MS[M+1]+: 581ethoxy}phenyl)propionic acidI_506IIa_433(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.436A{3-[butyryl-(4-fluorophenyl)amino]-MS[M+1]+: 583propoxy}phenyl)propionic acidI_507IIa_434(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.792A{3-[(2,2-dimethylpropionyl)-(2-MS[M+1]+: 597fluorophenyl)amino]propoxy}phenyl)-propionic acidI_508IIa_435(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.656A{2-[(2,2-dimethylpropionyl)-(2-MS[M+1]+: 595methoxyphenyl)amino]ethoxy}phenyl)-propionic acidI_509IIa_436(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.784A{3-[(2,2-dimethylpropionyl)-(3-MS[M+1]+: 597fluorophenyl)amino]propoxy}phenyl)-propionic acidI_510IIa_437(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.61A{2-[(2,2-dimethylpropionyl)-(3-MS[M+1]+: 595methoxyphenyl)amino]ethoxy}phenyl)-propionic acidI_511IIa_438(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.483A{2-[isobutyryl-(3-MS[M+1]+: 597methylsulfanylphenyl)amino]ethoxy}-phenyl)propionic acidI_512IIa_439(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.122A{3-[(2-methoxyphenyl)-MS[M+1]+: 581propionylamino]propoxy}phenyl)-propionic acidI_513IIa_440(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.213A{3-[cyclopropanecarbonyl-(2-MS[M+1]+: 593methoxyphenyl)amino]propoxy}-phenyl)propionic acidI_514IIa_441(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.385A{3-[isobutyryl-(2-methoxyphenyl)-MS[M+1]+: 595amino]propoxy}phenyl)propionic acidI_515IIa_442(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.159A{3-[but-2-(E)-enoyl-(2-MS[M+1]+: 593methoxyphenyl)amino]propoxy}-phenyl)propionic acidI_516IIa_443(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.163A{3-[(2-methoxyphenyl)-(2-MS[M+1]+: 593methylacryloyl)amino]propoxy}-phenyl)propionic acidI_517IIa_444(S)-3-(4-{3-[Acryloyl-(2-rt: 8.015Amethoxyphenyl)amino]propoxy}-MS[M+1]+: 579phenyl)-2-(2-benzoylphenylamino)-propionic acidI_518IIa_445(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.395A{3-[butyryl-(2-methoxyphenyl)amino]-MS[M+1]+: 595propoxy}phenyl)propionic acidI_519IIa_446(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.111A{3-[(3-methoxyphenyl)-MS[M+1]+: 581propionylamino]propoxy}phenyl)-propionic acidI_520IIa_447(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.246A{3-[cyclopropanecarbonyl-(3-MS[M+1]+: 593methoxyphenyl)amino]propoxy}-phenyl)propionic acidI_521IIa_448(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.374A{3-[isobutyryl-(3-methoxyphenyl)-MS[M+1]+: 595amino]propoxy}phenyl)propionic acidI_522IIa_449(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.204A{3-[but-2-(E)-enoyl-(3-MS[M+1]+: 593methoxyphenyl)amino]propoxy}-phenyl)propionic acidI_523IIa_450(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.134A{3-[(3-methoxyphenyl)-(2-MS[M+1]+: 593methylacryloyl)amino]propoxy}-phenyl)propionic acidI_524IIa_451(S)-3-(4-{3-[Acryloyl-(3-rt: 8.045Amethoxyphenyl)amino]propoxy}-MS[M+1]+: 579phenyl)-2-(2-benzoylphenylamino)-propionic acidI_525IIa_452(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.381A{3-[butyryl-(3-methoxyphenyl)amino]-MS[M+1]+: 595propoxy}phenyl)propionic acidI_526IIa_453(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.42A{2-[cyclobutanecarbonyl-(2-MS[M+1]+: 593methoxyphenyl)amino]ethoxy}phenyl)-propionic acidI_527IIa_454(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.27A{2-[isobutyryl-(2-methoxyphenyl)-MS[M+1]+: 581amino]ethoxy}phenyl)propionic acidI_528IIa_455(S)-3-{4-[2-(Acryloylnaphthalen-1-rt: 8.35Aylamino)ethoxy]phenyl}-2-(2-MS[M+1]+: 585benzoylphenylamino)propionic acidI_529IIa_456(S)-3-{4-[2-(Acryloylnaphthalen-2-rt: 8.418Aylamino)ethoxy]phenyl}-2-(2-MS[M+1]+: 585benzoylphenylamino)propionic acidI_530IIa_457(S)-3-(4-{2-[Acryloyl-(3-rt: 8.172Amethylsulfanylphenyl)amino]ethoxy}-MS[M+1]+: 581phenyl)-2-(2-benzoylphenylamino)-propionic acidrI_531IIa_458(S)-3-(4-{2-[Acryloyl-(4-rt: 8.182Amethylsulfanylphenyl)amino]ethoxy}-MS[M+1]+: 581phenyl)-2-(2-benzoylphenylamino)-propionic acidI_532IIa_459(S)-3-(4-{3-[Acryloyl-(3-fluorophenyl)-rt: 8.098Aamino]propoxy}phenyl)-2-(2-MS[M+1]+: 567benzoylphenylamino)propionic acidI_533IIa_460(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.274A{3-[but-2-(E)-enoyl-(3-fluorophenyl)-MS[M+1]+: 581amino]propoxy}phenyl)propionic acidI_534IIa_461(S)-3-(4-{2-[Acryloyl-(2-rt: 7.886Amethoxyphenyl)amino]ethoxy}phenyl)-MS[M+1]+: 5652-(2-benzoylphenylamino)propionicacidI_535IIa_462(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.037A{2-[(2-methoxyphenyl)-(2-MS[M+1]+: 579methylacryloyl)amino]ethoxy}phenyl)-propionic acidI_536IIa_463(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.081A{2-[cyclopropanecarbonyl-(3-MS[M+1]+: 579methoxyphenyl)amino]ethoxy}phenyl)-poropionic acidI_537IIa_464(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.384A{2-[cyclobutanecarbonyl-(3-MS[M+1]+: 593methoxyphenyl)amino]ethoxy}phenyl)-propionic acidI_538IIa_465(S)-3-(4-{2-[Acryloyl-(3-rt: 7.884Amethoxyphenyl)amino]ethoxy}phenyl)-MS[M+1]+: 5652-(2-benzoylphenylamino)propionicacidI_539IIa_466(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 7.975A{2-[(3-methoxyphenyl)-(2-MS[M+1]+: 579methylacryloyl)amino]ethoxy}phenyl)-propionic acidI_540IIa_467(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.236A{2-[ethyl(naphthalene-2-carbonyl)-MS[M+1]+: 587amino]ethoxy}phenyl)propionic acidI_541IIa_468(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.511A{2-[(naphthalene-2-carbonyl)-MS[M+1]+: 601propylamino]ethoxy}phenyl)propionicacidI_542IIa_469(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 7.881A{2-[ethyl(quinoline-2-carbonyl)amino]-MS[M+1]+: 588ethoxy}phenyl)propionic acidI_543IIa_470(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.2A{2-[propyl(quinoline-2-carbonyl)-MS[M+1]+: 602amino]ethoxy}phenyl)propionic acidI_544IIa_471(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 7.756A{2-[ethyl(quinoxaline-2-carbonyl)-MS[M+1]+: 589amino]ethoxy}phenyl)propionic acidI_545IIa_472(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.077A{2-[propyl(quinoxaline-2-carbonyl)-MS[M+1]+: 603amino]ethoxy}phenyl)propionic acidI_546IIa_473(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 7.732A{2-[ethyl(thiophene-2-carbonyl)-MS[M+1]+: 543amino]ethoxy}phenyl)propionic acidI_547IIa_474(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.04A{2-[propyl(thiophene-2-carbonyl)-MS[M+1]+: 557amino]ethoxy}phenyl)propionic acidI_548IIa_475(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 6.713A{2-[ethyl(pyridine-3-carbonyl)amino]-MS[M+1]+: 538ethoxy}phenyl)propionic acidI_549IIa_476(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 7.037A{2-[propyl(pyridine-3-carbonyl)amino]-MS[M+1]+: 552ethoxy}phenyl)propionic acidI_550IIa_477(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 7.924A{2-[ethyl-(3-thiophen-2-ylacryloyl)-MS[M+1]+: 569amino]ethoxy}phenyl)propionic acidI_551IIa_478(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.236A{2-[propyl-(3-thiophen-2-ylacryloyl)-MS[M+1]+: 583amino]ethoxy}phenyl)propionic acidI_552IIa_479(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.572A{2-[(3,3-dimethylbutyryl)propylamino]-MS[M+1]+: 545ethoxy}phenyl)propionic acidI_553IIa_480(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 5.866A{2-[ethyl-(3-pyridin-3-ylpropionyl)-MS[M+1]+: 566amino]ethoxy}phenyl)propionic acidI_554IIa_481(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 6.125A{2-[propyl-(3-pyridin-3-ylpropionyl)-MS[M+1]+: 580amino]ethoxy}phenyl)propionic acidI_555IIa_482(S)-2-(2-Benzoylphenylamino)-3-{4-[2-rt: 8.138A(cyclobutanecarbonylpropylamino)-MS[M+1]+: 529ethoxy]phenyl}propionic acidI_556IIa_483(S)-2-(2-Benzoylphenylamino)-3-{4-[2-rt: 7.963A(isobutyrylpropylamino)ethoxy]MS[M+1]+: 517phenyl}propionic acidI_557IIa_484(S)-2-(2-Benzoylphenylamino)-3-{4-[2-rt: 7.945Abutyrylpropylamino)ethoxy]phenyl}-MS[M+1]+: 517propionic acidI_558IIa_485(S)-3-{4-[2-(Benzoylethylamino)-rt: 7.725Aethoxy]phenyl}-2-(2-MS[M+1]+: 537benzoylphenylamino)propionic acidI_559IIa_486(S)-2-(2-Benzoylphenylamino)-3-{4-[2-rt: 8.03A(benzoylpropylamino)ethoxy]phenyl}-MS[M+1]+: 551propionic acidI_560IIa_487(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.034A{2-[ethyl-(3-phenylacryloyl)amino]MS[M+1]+: 563ethoxy}phenyl)propionic acidI_561IIa_488(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.102A{2-[(2,2-dimethylpropionyl)-MS[M+1]+: 517ethylamino]ethoxy}phenyl)propionicacidI_562IIa_489(S)-2-(2-Benzoylphenylamino)-3-(4-rt: 8.44A{2-[(2,2-dimethylpropionyl)-MS[M+1]+: 531propylamino]ethoxy}phenyl)propionicacid

Claims
  • 1: A compound of formula I
  • 2: A compound according to claim 1 wherein the configuration of the chiral carbon attached to R1 is (S), thus having the formula Ia.
  • 3: A compound according to claim 1, wherein R2 represents —(CH2), —N(COR3)-A-J-T.
  • 4: A compound according to claim 3, wherein R3 represents —(C1-C10)-alkyl optionally substituted by one or more substituents selected from —F, —Cl, —Br and —O(C1-C4)-alkyl; —(C2-C6)alkenyl; —(C1-C3)alkylene-Y; —(C2-C3)alkenylene-Y; —(C2-C3)alkynylene-Y or —Y; and Y in R3 represents a monoradical coming from a cycle selected from a (C3-C6)cycloalkane, a heterocycle, benzene and a bicycle, wherein all these cycles can be optionally substituted as defined in claim 1.
  • 5: A compound according to claim 3, wherein A represents —(C1-C4)-alkylene-; —(C1-C4)alkylene-Z- or -Z-; Z in A represents a biradical coming from a cycle selected from a (C3-C6)cycloalkane, a heterocycle, benzene and a bicycle, wherein all these cycles can be optionally substituted with one or more substituents selected from the group —F, —Cl, —Br, —S(C1-C4)alkyl, —(C1-C4)alkyl optionally substituted by one or more —OH or —F and —O(C1-C4)alkyl optionally substituted by one or more —OH or —F; J represents a single bond; and T represents —H.
  • 6: A compound according to claim 5 wherein Z in A represents an unsubstituted biradical coming from a cycle selected from a (C3-C6)cycloalkane and benzene.
  • 7: A compound according to claim 1, wherein R2 represents —(CH2)s—N(R4)-B-J-T.
  • 8: A compound according to claim 7, wherein R4 represents —(C4-C10)-alkyl optionally substituted by one or more substituents selected from —F, —Cl, —Br and —O(C1-C4)-alkyl; —(C1-C4)alkylene-Y; or —Y; and Y in R4 represents a monoradical coming from a cycle selected from a (C3-C6)cycloalkane, a heterocycle, benzene and a bicycle, wherein all these cycles can be optionally substituted as defined in claim 1.
  • 9: A compound according to claim 7, wherein B represents —(C1-C4)-alkylene-Z- or -Z-; Z in B represents a biradical coming from a cycle selected from a (C3-C6)cycloalkane, heterocycle, benzene and bicycle, wherein all these groups can be optionally substituted as defined in claim 1; J represents a single bond; and T represents —H.
  • 10: A pharmaceutical composition which comprises a therapeutically effective amount of the compound of formula I as defined in claim 1, together with appropriate amounts of pharmaceutically acceptable excipients.
  • 11-14. (canceled)
  • 15: A method for the treatment or prevention of diseases mediated by PPARγ comprising the administration to a mammal, including a human, of an effective amount of a compound of formula I as defined in claim 1.
  • 16: A method for the treatment or prevention of metabolic diseases comprising the administration to a mammal, including a human, of an effective amount of a compound of formula I as defined in claim 1.
  • 17: A method according to claim 1 wherein the metabolic disease is selected from non-insulin-dependent diabetes mellitus and obesity.
  • 18: A method for the treatment or prevention of cardiovascular diseases associated with metabolic syndrome, inflammatory diseases, cancer, bone diseases, skin wound healing, cutaneous disorders associated with an anomalous differentiation of epidermic cells and other disorders where insulin resistance is a component, comprising the administration to a mammal, including a human, of an effective amount of a compound of formula I as defined in claim 1.
  • 19: A method for the treatment or prevention of diseases mediated by PPARγ comprising the administration to a mammal, including a human, of an effective amount of a compound of formula I as defined in claim 1.
  • 20: A method for the treatment or prevention of metabolic diseases comprising the administration to a mammal, including a human, of an effective amount of a compound of formula I as defined in claim 1.
  • 21: A method according to claim 16 wherein the metabolic disease is selected from non-insulin-dependent diabetes mellitus and obesity.
  • 22: A method for the treatment or prevention of cardiovascular diseases associated with metabolic syndrome, inflammatory diseases, cancer, bone diseases, skin wound healing, cutaneous disorders associated with an anomalous differentiation of epidermic cells and other disorders where insulin resistance is a component, comprising the administration to a mammal, including a human, of an effective amount of a compound of formula I as defined in claim 1.
Priority Claims (1)
Number Date Country Kind
200401966 Jul 2004 ES national
PCT Information
Filing Document Filing Date Country Kind 371c Date
PCT/EP05/53728 7/29/2005 WO 3/22/2007