Claims
- 1. A compound represented by formula (I) whereR1 and R2 independently represent a group or R1 and R2 together form a C3-7 heterocycloalkyl or heterocycloalkenyl group which may be optionally substituted by C1-6 alkyl, C1-4 alkoxy, halogen, carboxylic acid or a C1-4 carboxylic acid ester group; R3 represents hydrogen, C1-3 alkyl, halogen, or C1-2 alkoxy; R4, R5 and R6 independently represent hydrogen, or halogen; R7 represents hydrogen or C1-6alkyl; R8 represents hydrogen, C3-7 cycloalkyl, C3-7 cycloalkenyl, C3-7 heterocycloalkyl, C3-7 heterocycloalkenyl, aryl, or heteroaryl, which groups are optionally substituted by one or more groups selected from halogen, hydroxy, CN, C1-6 alkyl, C1-6 alkoxy, C1-6 acyloxy, NR9R10, NHCOR11, NHSO2R12, COR3, CO2R14, CONR15R16, and SO2NHR17; X represents a bond, a C1-6alkyl chain, or a C3-6alkenyl chain, where one or two nitrogen, oxygen, or sulfur atoms may be optionally contained within each chain, and the chains are optionally substituted by one or more groups selected from halogen, hydroxy, CN, C1-6alkyl, C1-6alkoxy, C1-6acyloxy, NR9R10, NHCOR11, NHSO2R12, COR13, CO2R14, CONR15R16, and SO2NHR17; R9-R17 represent hydrogen, C1-6alkyl, or R9 and R10 or R15 and R16 form a C3-7 heterocycloalkyl ring, or R12 additionally may represent trifluoromethyl; or pharmaceutically acceptable salt or solvate thereof.
- 2. A compound according to claim 1 where R1 represents a group where X represents a bond or C1-6 alkyl group and R8 represents hydrogen, C3-7 cycloalkyl, aryl, or heteroaryl.
- 3. A compound according to claim 2 where X represents a bond and R8 represents phenyl optionally substituted by one or more halogen groups, or C3-7 cycloalkyl.
- 4. A compound according to claim 2 or claim 3 where X represents a C1-6 alkyl group and R8 represents hydrogen, cycloalkyl, or heteroaryl.
- 5. A compound according to claim 1 where R2 represents a group and X represents C3-6 alkenyl, or a C1-6 alkyl which optionally contains an oxygen group within the chain and is optionally substituted by a group selected from hydroxy, C1-6 alkoxy, NHSO2R12 CO2R14, CONR15R16, C1-6 acyloxy or SO2NHR17, and R8 represents hydrogen, C3-7 heterocycdoalkyl, aryl optionally substituted by CO2R14, or heteroaryl optionally substituted by hydroxy or C1-6 alkyl.
- 6. A compound according to claim 1 where R3 represents C1-3 alkyl or halogen.
- 7. A compound according to claim 1 where R4, R5 and R6 represent hydrogen or halogen.
- 8. A compound according to claim 1 where R7 is hydrogen.
- 9. A compound according to claim 1 represented by formula (IA) whereR1A represents a group XA represents a bond, C1-6 alkyl: R8A represents hydrogen, C3-7 cycloalkyl, aryl optionally substituted by halogen, or heteroaryl; R2A represents a group where XB represents C1-6 alkyl optionally substituted by CO2R14A; R8B represents hydrogen, phenyl substituted by CO2R14A, oxadiazole substituted by a hydroxy group, or an unsubstituted C-linked tetrazole group; R3A represents C1-3 alkyl, or halogen; or pharmaceutically acceptable salt or solvate thereof.
- 10. N-Cyclohexyl-3,N-dimethyl-5-[2-(pyridin-4-ylamino)-ethoxy]-benzamide;3-Chloro-N-cycohexyl-N-methyl-5-[2-(pyridin-4-ylamino)-ethoxy]-benzamide; 3-Bromo-N-cyclohexyl-N-methyl-5-[2-(pyridin-4-ylamino)-ethoxy]-benzamide; N-Allyl-3-chloro-N-cyclohexyl-5-[2-(pyridin-4-ylamino)-ethoxy]-benzamide; N-Allyl-3-bromo-N-cyclohexyl-5-[2-(pyridin-4-ylamino)-ethoxy]-benzamide; ({3-Chloro-5-[2-(pyridin-4-ylamino)-ethoxy]-benzoyl}-cyclohexyl-amino)-acetic acid; ({3-Bromo-5-[2-(pyridin-4-ylamino)-ethoxy]-benzoyl}-cyclohexyl-amino)-acetic acid; N-Allyl-3-chloro-N-cyclopentyl-5-[2-(pyridin-4-ylamino)-ethoxy]-benzamide; N-Allyl-3-bromo-N-cyclopentyl-5-[2-(pyridin-4-ylamino)-ethoxy]-benzamide; 3-Chloro-N-propyl-5-[2-(pyridin-4-ylamino)-ethoxy]-N-(tetrahydro-pyran-4-yl)-benzamide; 3-Bromo-N-propyl-5-[2-(pyridin-4-ylamino)-ethoxy]-N-(tetrahydro-pyran-4-yl)-benzamide; 3-Chloro-N-propyl-N-pyridin-3-yl-5-[2-(pyridin-4-ylamino)-ethoxy]-benzamide; 3-Bromo-N-propyl-N-pyridin-3-yl-5-[2-(pyridin-4-ylamino)-ethoxy]-benzamide; 3-Chloro-N-(3,5-difluorophenyl)-N-propyl-5-[2-(pyridin-4-ylamino)-ethoxy]-benzamide; 3-Bromo-N-(3,5-difluorophenyl)-N-propyl-5-[2-(pyridin-4-ylamino)-ethoxy]-benzamide; 2-[{3-Chloro-5-[2-(pyridin-4-ylamino)-ethoxy]-benzoyl}-(2,4-difluoro-benzyl)-amino]-butyric acid; 4-[({3-Chloro-5-[2-(pyridin-4-ylamino)-ethoxy]-benzoyl}-isobutyl-amino)-methyl]-benzoic acid; 4-[2-({3-Chloro-5-[2-(pyridin-4-ylamino)-ethoxy]-benzoyl}-isobutyl-amino)-ethyl]-benzoic acid; 3-Chloro-N-cyclopentyl-5-[2-(pyridin-4-ylamino)-ethoxy]-N-(3-trifluoromethanesulfonylamino-propyl)-benzamide; 3-Chloro-N-isopropyl-N-methyl-5-[2-(pyridin-4-ylamino)-ethoxy]-benzamide; N-[2-(3-Amino-[1,2,4]oxadiazol-5-yl)-ethyl]-3-chloro-N-isopropyl-5-[2-(pyridin-4-ylamino)-ethoxy]-benzamide; N-(2-Carbamoyl-ethyl)-N-isopropyl-3-methyl-5-[2-(pyridin-4-ylamino)-ethoxy]-benzamide; N-(2-Carbamoyl-ethyl)-3-chloro-N-cyclopropylmethyl-5-[2-(pyridin-4-ylamino)-ethoxy]-benzamide; N-(2-Carbamoyl-ethyl)-3-chloro-5-[2-(pyridin-4-ylamino)-ethoxy]-N-tetrahydrofuran-2-ylmethyl)-benzamide; N-(2-Carbamoyl-ethyl)-3-chloro-N-(2,2-dimethyl-propyl)-5-[2-(pyridin-4-ylamino)-ethoxy]-benzamide; N-(2-Carbamoyl-ethyl)-3-chloro-N-isopropyl-5-[2-(pyridin-4-ylamino)-ethoxy]-benzamide; N-(2-Carbamoyl-ethyl)-3-chloro-N-isobutyl-5-[2-(pyridin-4-ylamino)-ethoxy]-benzamide; 6-[{3-Chloro-5-[2-(pyridin-4-ylamino)-ethoxy]-benzoyl}-(2-fluoro-benzyl)-amino]-hexanoic acid; 6-({3-Chloro-5-[2-(pyridin-4-ylamino)-ethoxy]-benzoyl}-isobutyl-amino)-hexanoic acid; 6-[{3-Chloro-5-[2-(pyridin-4-ylamino)-ethoxy]-benzoyl}-(2-methoxy-ethyl)-amino]-hexanoic acid; 6-[{3-Chloro-5-(2-(pyridin-4-ylamino)-ethoxy]-benzoyl}-cyclohexylmethyl-amino)-hexanoic acid; 6-[{3-Chloro-5-[2-(pyridin-4-ylamino)-ethoxy]-benzoyl}-(3-fluoro-benzyl)-amino]-hexanoic acid; 6-({3-Chloro-5-[2-(pyridin-4-ylamino)-ethoxy]-benzoyl}-pyridin-4-ylmethyl-amino)-hexanoic acid; N-(5-Carbamoyl-pentyl)-3-chloro-N-furan-2-ylmethyl-5-[2-(pyridin-4-ylamino)-ethoxy]-benzamide; N-(5-Carbamoyl-pentyl)-3-chloro-5-[2-(pyridin-4-ylamino)-ethoxy]-N-(2,2,2-trifluoroethyl)-benzamide; N-(5-Carbamoyl-pentyl)-3-chloro-N-(2-fluoro-benzyl)-5-[2-(pyridin-4-ylamino)-ethoxy]-benzamide; N-(5-Carbamoyl-pentyl)-3-chloro-N-(2-methoxy-ethyl)-5-[2-(pyridin-4-ylamino)-ethoxy]-benzamide; N-(5-Carbamoyl-pentyl)-3-chloro-N-cyclohexylmethyl-5-[2-(pyridin-4-ylamino)-ethoxy]-benzamide; N-(5-Carbamoyl-pentyl)-3-chloro-N-isobutyl-5-[2-(pyridin-4-ylamino)-ethoxy]-benzamide; N-(5-Carbamoyl-pentyl)-3-chloro-5-[2-(pyridin-4-ylamino)-ethoxy]-N-thiophen-2-ylmethyl-benzamide; 1-{3-Chloro-5-[2-(pyridin-4-ylamino)-ethoxy]-benzoyl}-piperidine-2-carboxylic acid; 4-({3-Chloro-5-[2-(pyridin-4-ylamino)-ethoxy]-benzoyl}-cyclobutyl-amino)-butyric acid; 4-({3-Chloro-5-[2-(pyridin-4-ylamino)-ethoxy]-benzoyl}-furan-2-ylmethyl-amino)-butyric acid; 4-[{3-Chloro-5-[2-(pyridin-4-ylamino)-ethoxy]-benzoyl}-(3-fluoro-benzyl)-amino]-butyric acid; {3-Chloro-5-[2-(pyridin-4-ylamino)-ethoxy-phenyl}-(2-methyl-piperidin-1-yl)-methanone; 3-Chloro-N-(2-diethylcarbamoyl-ethyl)-N-isopropyl-5-[2-(pyridin-4-ylamino)-ethoxy]-benzamide; 3-Chloro-N-isopropyl-N-(3-methanesufonylamino-propyl)-5-[2-(pyridin-4-ylamino)-ethoxy]-benzamide; 3-Chloro-N-isopropyl-N-[3-(propane-1-sulfonylamino)-propyl]-5-[2-(pyridin-4-ylamino)-ethoxy]-benzamide; 3-Chloro-N-isopropyl-N-(3-oxo-3-piperidin-1-yl-propyl)-5-[2-(pyridin-4-ylamino)-ethoxy]-benzamide; 3-Chloro-N-[2-(ethyl-methyl-carbamoyl)-ethyl]-N-isopropyl-5-[2-(pyridin-4-ylamino)-ethoxy]-benzamide; 3-Chloro-N-isopropyl-N-(3-oxo-3-pyrrolidin-1-yl-propyl)-5-[2-(pyridin-4-ylamino)-ethoxy]-benzamide; 3-Chloro-N-isopropyl-N-(3-morpholin-4-yl-3-oxo-propyl)-5-[2-(pyridin-4-ylamino)-ethoxy]-benzamide mixture with 3-({3-chloro-5-[2-(pyridin-4-ylamino)-ethoxy]-benzoyl}-isopropyl-amino)-propionic acid (1:2); N-(2-tert-Butylcarbamoyl-ethyl)-3-chloro-N-isopropyl-5-[2-(pyridin-4-ylamino)-ethoxy]-benzamide; 3-Chloro-N-[2-(2,2-dimethyl-propylcarbamoyl)-ethyl]-N-isopropyl-5-[2-(pyridin-4-ylamino)-ethoxy]-benzamide; 3-Chloro-N-isopropyl-N-(3-oxo-3-thiomorpholin-4-yl-propyl)-5-[2-(pyridin-4-ylamino)-ethoxy]-benzamide; 3-Chloro-N-isopropyl-N-(3-oxo-3-thiazolidin-3-yl-propyl)-5-[2-(pyridin-4-ylamino)-ethoxy]-benzamide; 3-Chloro-N-(3-ethanesulfonylamino-propyl)-N-isopropyl-5-[2-(pyridin-4-ylamino)-ethoxy]-enzamide; 3-Chloro-N-isopropyl-N-[3-propane-2-sulfonylamino)-propyl]-5-[2-(pyridin-4-ylamino)-ethoxy]-benzamide; 3-Chloro-N-(4-fluoro-phenyl)-5-[2-(pyridin-4-ylamino)-ethoxy]-N-(3-[1,2,4]triazol-1-yl-propyl)-benzamide; 3-Chloro-N-cyclopentyl-5-[2-(pyridin-4-ylamino)-ethoxy]-N-(2-1,2,4]triazol-1-yl-ethyl)-benzamide; 3-Chloro-N-cyclopentyl-5-[2-(pyridin-4-ylamino)-ethoxy]-N-(4-[1,2,4]triazol-1-yl-butyl)-benzamide; 3-Chloro-N-(4-fuoro-phenyl)-5-[2-(pyridin-4-ylamino)-ethoxy]-N-(3-tetrazol-2-yl-propyl)-benzamide; 3-Chloro-N-(3-fluoro-phenyl)-5-[2-(pyridin-4-ylamino)-ethoxy]-N-(3-tetrazol-2-yl-propyl)-benzamide; 3-Chloro-(2-fluoro-phenyl)-5-[2-(pyridin -4-ylamino)-ethoxy-]-N-(3-tetrazol-2-yl-propyl)-benzamide; 3-Chloro-N-phenyl-5-[2-(pyridin-4-ylamino)-ethoxy]-N-(2tetrazol-2-yl-ethyl)-benzamide; 3-Chloro-N-phenyl-5-[2-(pyridin-4-ylamino)-ethoxy]-N-(2-[1,2,3]triazol-2-yl-ethyl)-benzamide; 3-Chloro-N-phenyl-5-[2-(pyridin-4-ylamino)-ethoxy]-N-(2-(pyridin-2-yloxy)-ethyl]-benzamide; 3-Chloro-N-isopropyl-N-(2-methoxy-ethyl)-5-[2-(pyridin-4-ylamino)-ethoxy]-benzamide; 6-({3-Chloro-5-[2-(pyridin-4-ylamino)-ethoxy]-benzoyl}-thiophen-2-ylmethyl-amino)-hexanoic acid; 6-[{3-Chloro-5-[2-(pyridin-4-ylamino)-ethoxy]-benzoyl}-(2-methyl-butyl)-amino]-hexanoic acid; {3-Chloro-5-[2-(pyridin-4-ylamino)-ethoxy]-phenyl}-(2,5-dimethyl-pyrrolidin-1-yl)-methanone; 4-({3-Chloro-5-[2-(pyridin-4-ylamino)-ethoxy]-benzoyl}-naphthalen-1-ylmethyl-amino)-butyric acid; 4-[{3-Chloro-5-[2-(pyridin-4-ylamino)-ethoxy]-benzoyl}-(1-methyl-1H-benzoimidazol-2-yl)-amino]-butyric acid; 3-Chloro-N-isopropyl-5-[2-(pyridin-4-ylamino)-ethoxy]-N-(3-trifluoromethanesulfonylamino-propyl)-benzamide; N-(3-Amino-propyl)-3-chloro-N-isopropyl-5-[2-(pyridin-4-ylamino)-ethoxy]-benzamide; ({3-Chloro-5-[2-(pyridin-4-ylamino)-ethoxy]-benzoyl}-cyclopentyl-amino)-acetic acid; 3-Chloro-N-cyclopentyl-N-propyl-5-[2-(pyridin-4-ylamino)-ethoxy]-benzamide; 3-Chloro-N-cyclopentyl-N-(3-hydroxy-propyl)-5-[2-(pyridin-4-ylamino)-ethoxy]-benzamide; 3-Chloro-N-propyl-5-[2-(pyridin-4-ylamino)-ethoxy]-N-(tetrahydro-pyran-4-yl)-benzamide; 3-Chloro-N-cyclopentyl-N-(2,3-dihydroxy-propyl)-5-[2-(pyridin-4-ylamino)-ethoxy]-benzamide; 3-Chloro-N-cyclopentyl-N-(3-morpholin-4-yl-propyl)-5-[2(pyridin-4-ylamino)-ethoxy]-benzamide; 4-({3-Chloro-5-[2-(pyridin-4-ylamino)-ethoxy]-benzoyl}-cyclopentyl-amino)-butyric acid ethyl ester; 3-Chloro-N-cyclopentyl-5-[2-(pyridin-4-ylamino)-ethoxy]-N-(3-pyrrolidin-1-yl-propyl)-benzamide; N-(3-Carbamoyl-propyl)-3-chloro-N-cyclopentyl-5-[2-(pyridin-4-ylamino)-ethoxy]-benzamide; N-(2-Carbamoyl-ethyl)-3-chloro-N-cyclopentyl-5-[2-(pyridin-4-ylamino)-ethoxy]-benzamide; N-Carbamoylmethyl-3-chloro-N-cyclopentyl-5-[2-(pyridin-4-ylamino)-ethoxy]-benzamide; 3-Chloro-N-ethyl-N-phenyl-5-[2-(pyridin-4-ylamino)-ethoxy]-benzamide; N-(2-Carbamoyl-ethyl)-3-chloro-N-cyclopropyl-5-[2-(pyridin-4-ylamino)-ethoxy]-benzamide; 3-Chloro-N,N-dipropyl-5-[2-(pyridin-4-ylamino)-ethoxy]-benzamide; 4-({3-Chloro-5-[2-(pyridin-4-ylamino)-ethoxy]-benzoyl}-cyclopentyl-amino)-butyric acid; N-(2-Carbamoyl-ethyl)-3-chloro-N-phenyl-5-[(2-(pyridin-4-ylamino)-ethoxy]-benzamide; N-(2-Carbamoyl-ethyl)-3-chloro-N-(2-chloro-phenyl)-5-[2-(pyridin-4-ylamino)-ethoxy]-benzamide; N-(2-Carbamoyl-ethyl)-3-chloro-N-(2-fluoro-phenyl)-5-[2-(pyridin-4-ylamino)-ethoxy]-benzamide; 4-[{3-Chloro-5-[2-(pyridin-4-ylamino)-ethoxy]-benzoyl}-(2-fluoro-phenyl)amino]-butyric acid methyl ester; 4-[{3-Chloro-5-[2-(pyridin-4-ylamino)-ethoxy]-benzoyl}-(2-fluoro-phenyl)-amino]-butyric acid; 3-Chloro-N-(2-fluoro-phenyl)-N-(4-oxo-4-pyrrolidin-1-yl-butyl)-5-[2-(pyridin-4-ylamino)-ethoxy]-benzamide; N-(3-Carbamoyl-propyl)-3-chloro-N-(2-fluoro-phenyl)-5-]2-(pyridin-4-ylamino)-ethoxy]-benzamide; 4-((2-Carbamoyl-phenyl)-{3-chloro-5-[2-(pyridin-4-ylamino)-ethoxy]-benzoyl}-amino)-butyric acid methyl ester; 4-((2-Carbamoyl-phenyl)-{3-chloro-5-[2-(pyridin-4-ylamino)-ethoxy]-benzoyl}-amino)-butyric acid; 3-Chloro-N-(2-fluoro-phenyl)-5-[2-(pyridin-4-ylamino)-ethoxy]-N-[3-(1H-tetrazol-5-yl)-propyl]-benzamide; 3-Chloro-N-[2-(2,3-dihydroxy-propoxy)-ethyl]-N-(2-fluoro-phenyl)-5-[2-(pyridin-4-ylamino)-ethoxy]-benzamide; (R)-1-{3-[{3-Chloro-5-[2-(pyridin-4-ylamino]-ethoxy-benzoyl}-(2-fluoro-phenyl)-amino]-propyl}-pyrrolidine-2-carboxylic acid; 3-Chloro-N-phenyl-5-[2-(pyridin-4-ylamino)-ethoxy]-N-(2-sulfamoyl-ethyl)-benzamide; 3-Chloro-N-[2-(ethyl-methyl-carbamoyl)-ethyl]-N-phenyl-5-[2-(pyridin-4-ylamino)-ethoxy]-benzamide; 3-Chloro-N-[2-(ethyl-methyl-carbamoyl)-ethyl]-N-phenyl-5-[2-(pyridin-4-ylamino)-ethoxy]-benzamide; N-(2-tert-Butylcarbamoyl-ethyl)-3-chloro-N-phenyl-5-[2-(pyridin-4-ylamino)-ethoxy]-benzamide; 3-Chloro-N-[2-(2,2-dimethyl-propylcarbamoyl)-ethyl]-N-phenyl-5-[2-(pyridin-4-ylamino)-ethoxy]-benzamide; 3-Chloro-N-(3-oxo-3-thiomorpholin-4-yl-propyl)-N-phenyl-5-[2-(pyridin-4-ylamino)-ethoxy]-benzamide; 3-Chloro-N-(3-oxo-3-thiazolidin-3-yl-propyl)-N-phenyl-5-[2-(pyridin-4-ylamino)-ethoxy]-benzamide; N-tert-Butyl-3-chloro-5-[2-(pyridin-4-ylamino)-ethoxy]-benzamide; 3-Chloro-N-isopropyl-N-[2-(1-methyl-1H-tetrazol-5-yl)-ethyl]-5-[2-(pyridin-4-ylamino)-ethoxy]-benzamide; 3-Chloro-N-(3,5-difluoro-phenyl)-N-propyl-5-[2-(pyridin-4-ylamino)-ethoxy]-benzamide; 3-Chloro-N-(3-morpholin-4-yl-propyl)-5-[2-(pyridin-4-ylamino)-ethoxy]-N-(tetrahydro-pyran-4-yl)-benzamide; 3-Chloro-5-[2-(pyridin-4-ylamino)-ethoxy]-N-(3-pyrrolidin-1-yl-propyl)-N-(tetrahydro-pyran-4-yl)-benzamide; N-(2-Carbamoyl-ethyl)-3-chloro-N-(1-propyl-butyl)-5-[2-(pyridin-4-ylamino)-ethoxy]-benzamide; 3-Chloro-N-cyclopentyl-N-(4-oxo-4-pyrrolidin-1-yl-butyl)-5-[2-(pyridin-4-ylamino)-ethoxy]-benzamide; 3-Chloro-N-ethyl-N-(2-fluoro-phenyl)-5-[2-(pyridin-4-ylamino)-ethoxy]-benzamide; 3-Chloro-N-propyl-5-[2-(pyridin-4-ylamino)-ethoxy]-N-[1,3,4]thiadiazol-2-yl-benzamide; 3-Chloro-N-propyl-5-[2-(pyridin-4-ylamino)-ethoxy]-N-thiazol-2-yl-benzamide; 3-Chloro-N-[2-(2,3-dihydroxy-propoxy)-ethyl]-N-phenyl-5-[2-(pyridin-4-ylamino)-ethoxy]-benzamide; N-(2-tert-Butylsulfamoyl-ethyl)-3-chloro-N-phenyl-5-[2-(pyridin-4-ylamino)-ethoxy]-benzamide; 3-Chloro-N-(2-isopropylsulfamoyl-ethyl)-N-phenyl-5-[2-(pyridin-4-ylamino)-ethoxy]-benzamide; 3-Chloro-N-isopropyl-5-[2-(pyridin-4-ylamino)-ethoxy]-N-[2-(pyridin-2-yloxy)-ethyl]-benzamide; 3-Chloro-N-[2-(2,3-dihydroxy-propoxy)-ethyl]-N-(4-fluoro-phenyl)-5-[2-(pyridin-4-ylamino)-ethoxy]-benzamide; 3-Chloro-N-cyclopentyl-5-[2-(pyridin-4-ylamino)-ethoxy]-N-[2-(1H-tetrazol-5-yl)-ethyl]-benzamide; 3-Chloro-N-isopropyl-5-[2-(pyridin-4-ylamino)-ethoxy]-N-(2-[1,2,4]triazol-1-yl-ethyl)-benzamide; 3-Chloro-N-[2-(3-methyl-but-2-yl-carbamoyl)-ethyl]-N-isopropyl-5-[2-(pyridin-4-ylamino)-ethoxy]-benzamide; 3-Chloro-N-[2-(3,3-dimethyl-but-2-yl-carbamoyl)-ethyl]-N-isopropyl-5-[2-(pyridin-4-ylamino)-ethoxy]-benzamide; 3-Chloro-N-[2-(5-hydroxy-[1,2,4]oxadiazol-3-yl)-ethyl]-N-isopropyl-5-[2-(pyridin-4-ylamino)-ethoxy]-benzamide; N-tert-Butyl-N-(2-tert-butylcarbamoyl-ethyl)-3-chloro-5-[2-(pyridin-4-ylamino)-ethoxy]-benzamide; N-(2-tert-Butylcarbamoyl-ethyl)-3-chloro-N-cyclobutyl-5-[2-(pyridin-4-ylamino)-ethoxy]-benzamide; 3-Chloro-N-cyclobutyl-N-[2-(2,2-dimethyl-propylcarbamoyl)-ethyl]-5-[2-(pyridin-4-ylamino)-ethoxy]-benzamide; N-(2-Carbamoyl-ethyl)-3-chloro-N-cyclobutyl-5-[2-(pyridin-4-ylamino)-ethoxy]-benzamide; 3-Chloro-N-isopropyl-5-[2-(pyridin-4-ylamino)-ethoxy]-N-(2-sulfamoyl-ethyl)-benzamide; 3-Chloro-N-(2,2-dimethyl-propylsulfamoyl-ethyl)-N-isopropyl-5-[2-(pyridin-4-ylamino)-ethoxy]-benzamide; 6-({3-Chloro-5-[2-(pyridin-4-ylamino)-ethoxy]-benzoyl}isopropyl-amino)-hexanoic acid; N-(2-tert-Butylcarbamoyl-ethyl)-N-isopropyl-3-methyl-5-[2-(pyridin-4-ylamino)-ethoxy]-enzamide; N-(5-tert-Butylcarbamoyl-pentyl)-N-isopropyl-3-methyl-5-[2-(pyridin-4-ylamino)-ethoxy]-benzamide; 3-Chloro-N-[5-(2,2-dimethyl-propylcarbamoyl)-pentyl]-N-isopropyl-5-[2-(pyridin-4-ylamino)-ethoxy]-benzamide; N-(5-Carbamoyl-pentyl)-N-isopropyl-3-methyl-5-[2-pyridin-4-ylamino)-ethoxy]-benzamide; 3-Chloro-N-(2-(4-tert-butylphenyl)-ethyl)-N-isopropyl-5-[2-(pyridin-4-ylamino)-ethoxy]-benzamide; 3-Chloro-N-isopropyl-5-[2-(pyridin-4-ylamino)ethoxy]-N-[3-(2,2-dimethyl-propionylamino)-propyl]-benzamide; 3-Chloro-N-isopropyl-5-(2-(pyridin-4-ylamino)ethoxy]-N-[3-(3,3-dimethyl-butyrylamino)-propyl]-benzamide; 3-Chloro-N-[2-(1,1-dimethyl-propylcarbamoyl)-ethyl]-N-isopropyl-5-[2-(pyridin-4-ylamino)-ethoxy]-benzamide; N-{2-(2,2-dimethylpropylcarbamoyl)-ethyl}-N-isopropyl-3-methyl-5-[2-(pyridin-4-ylamino)-ethoxy]-benzamide; 3-(Isopropyl-{3-methyl-5-[2-(pyridin-4-ylamino)-ethoxy]-benzoyl}-amino)-propionic acid; 3-(Isopropyl-{3-methyl-5-[2-(pyridin-4-ylamino)-ethoxy]-benzoyl}-amino)-propionic acid methyl ester; N-(5-tert-Butylcarbamoyl-pentyl)-3-chloro-N-isopropyl-5-[2-(pyridin-4-ylamino)-ethoxy]-benzamide; 6-({3-Methyl-5-[2-(pyridin-4-ylamino)-ethoxy]-benzoyl}-isopropyl-amino)-hexanoic acid; N-(2-Cyano-ethyl)-N-isopropyl-3-methyl-5-[2-(pyridin-4-ylamino)-ethoxy]-benzamide; 3-Chloro-N,N-diisopropyl-5-[2-(pyridin-4-ylamino)-ethoxy]-benzamide; 3-Chloro-N-isopropyl-N-(3-oxo-3-thiazolidin-3-yl-propyl)-5-[2-(pyridin-4-ylamino)-ethoxy]-benzamide; or pharmaceutically acceptable salt or solvate thereof.
- 11. 3-Chloro-N[2-(5-hydroxy-[1,2,4]oxadiazol-3-yl)-ethyl)N-isopropyl-5-[2[(pyridin-4-ylamino)-ethoxyl]-benzamide;4-({3-Chloro-5-[2-(pyridin-4-ylamino)-ethoxy]-benzoyl}-clobutyl-amino)-butyric acid; 6-({3-Chloro-5-[2-(pyridin-4-ylamino)-ethoxy]-benzoyl}-isobutyl-amino)-hexanoic acid; 4-[({3-Chloro-5-[2-(pyridin-4-ylamino)-ethoxy]-benzoyl}-isobutyl-amino)-methyl]-benzoic acid 4-[2-({3-Chloro-5-[2-(pyridin-4-ylamino)-ethoxy]-benzoyl}-isobutyl-amino)-ethyl]-benzoic acid; 4-({3-Chloro-5-[2-(pyridin-4-ylamino)-ethoxy]-benzoyl}-cyclopentyl-amino)-butyric acid ethyl ester; 4-({3-Chloro-5-(pyridin-4-ylamino)-ethoxy]-benzoyl}-cyclopentyl-amino)-butyric acid; 3-Chloro-N-cyclopentyl-5-[2-(pyridin-4-ylamino)-ethoxy]-N-[2-(1H-tetrazol-5-yl)-ethyl]-benzamide; 6-({3-Chloro-5-[2-(pyridin-4-ylamino)-ethoxy]-benzoyl}-cyclohexylmethyl-amino)-hexanoic acid; 6-({3-Chloro-5-[2-(pyridin-4-ylamino)-ethoxy]benzoyl}-thiophen-2-ylmethyl-amino)-hexanoic acid; 4-[{3-Chloro-5-[2-(pyridin-4-ylamino)-ethoxy]-benzoyl}-(2-fluoro-phenyl)-amino]-butyric acid methyl ester; 4-[{3-Chloro-5-[2-(pyridin-4-ylamino)-ethoxy]-benzoyl}-(2-fluoro-phenyl)-amino]-butyric acid; 3-Chloro-N-(2-fluoro-phenyl)-5-[2-(pyridin-4-ylamino)-ethoxy]-N-[3-(1H-tetrazol-5-yl)-propyl]-benzamide; or pharmaceutically acceptable salt or solvate thereof.
- 12. A method of treatment of a mammal, suffering from a condition susceptible of amelioration by a thrombin inhibitor comprising administration of an effective amount of a compound according to claim 1 or a pharmaceutically acceptable derivative thereof.
- 13. A pharmaceutical composition comprising a compound according to claim 1 or a pharmaceutically acceptable derivative thereof together with one or more pharmaceutically acceptable carriers.
- 14. A process for preparing a compound of formula (I) as claimed in claim 1, or a pharmaceutically acceptable derivative thereof which comprises:(A), reaction of a compound of formula (II) with a compound of formula (III), where R7′ represents R7 or a suitable protecting group, (B), reaction of compounds of formula (XIV) and (XV) where L is a suitable leaving group, in the presence of a suitable base, or (C), reaction of compounds of formula (I) with compounds of formula (III) which are bound to a solid phase resin via a carboxamide or carboxylate functional group on R8 or X, by amide coupling techniques, followed by deprotection of any protecting groups and cleavage from the resin under suitable conditions.
Priority Claims (1)
Number |
Date |
Country |
Kind |
9525620 |
Dec 1995 |
GB |
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Parent Case Info
This application is a continuation application of U.S. application Ser. No. 09/077,885, filed Jun. 12, 1998 now abandoned, which is a 371 of PCT/EP96/05743, filed on Dec. 13, 1996.
US Referenced Citations (1)
Number |
Name |
Date |
Kind |
5556977 |
Wayne |
Sep 1996 |
|
Foreign Referenced Citations (1)
Number |
Date |
Country |
WO 94 20467A |
Sep 1994 |
WO |
Non-Patent Literature Citations (1)
Entry |
Chem Rev., 1996, pp. 3170-3171, 3176, XP002027890 Patani et al.: “A Rational Approach in Drug Design”, Reference on p. 2171 show that the general concept of the citations (listed on p. 3176) was known well before the priority date. |
Continuations (1)
|
Number |
Date |
Country |
Parent |
09/077885 |
|
US |
Child |
09/678610 |
|
US |