Claims
- 1. A compound of Formula (1):
- 2. The compound claim 1, wherein the compound of Formula (I) comprise a compound of Formula (Ia)
- 3. The compound of Formula (Ia) of claim 2, wherein R1 comprises a hydrogen, methyl, ethyl, propyl, butyl, iso-butyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, 3-butenyl, tert-butyl, 3-cyclohexyl-propyl, 3-phenoxy-propyl, methoxymethyl, 4-fluoro-phenyl, 3-(4-chlorophenoxy)-propyl, 2,4,4-trimethyl-pentyl, 1-ethyl-propyl, 1-propyl-butyl, benzyloxymethyl, 2-cyclopropy-ethyl, 2-phenyl-ethyl, 4-tert-butylphenoxymethyl, 4-tert-butylcyclohexyl, 4-butylcyclohexyl , 4-ethylcyclohexyl, 3-methoxycarbonyl-1-propyl, or 2-(pyridin-3-yl)-ethyl group.
- 4. The compound of Formula (Ia) of claim 2, wherein R2 comprises a phenyl or 1,2,3,4-tetrahydroisoquinoline group, wherein the phenyl group is substituted with at least one substitutent comprising
a) —Y2-alkyl; b) —Y2-aryl; c) —Y2-heteroaryl; d) —Y2-alkylene-heteroarylaryl; e) —Y2-alkylene-aryl; f) —Y2-alkylene-W2—R18; g) —Y3—Y4—NR23R24; h) —Y3—Y4—NH—C(═NR25)NR23R24; i) —Y3—Y4—C(═NR25)NR23R24; or j) —Y3—Y4—Y5—A2; wherein Y2 and W2 independently comprise —CH2—or —O—, and R18 comprises aryl, alkyl, -alkylene-aryl, -alkylene-heteroaryl, or -alkylene-O-aryl; Y3 and Y5independently comprise a direct bond, —CH2—, —O—, —N(H), —S—, SO2—, —C(O)—, —CON(H)—, —NHC(O)—, —NHCON(H)—, —NHSO2—, —SO2N(H)—, —C(O)—O—, —NHSO2NH—, —O—CO—, 645wherein R27 and R26 independently comprise aryl, alkyl, -alkylene-aryl, alkoxy, or -alkyl-O-aryl; Y4 comprises
a) -alkylene; b) -alkenylene; c) -alkynylene; d) -arylene; e) -heteroarylene; f) -cycloalkylene; g) -heterocyclylene; h) -alkylene-arylene; i) -alkylene-heteroarylene; j) -alkylene-cycloalkylene; k) -alkylene-heterocyclylene; l) -arylene-alkylene; m) -heteroarylene-alkylene; n) -cycloalkylene-alkylene; t) -heterocyclylene-alkylene; u) —O—; v) —S—; w) —S(O2)—; or x) —S(O)—; wherein said alkylene groups may optionally contain one or more O, S, S(O), or SO2 atoms; A2 comprises
a) heterocyclyl, fused arylheterocyclyl, or fused heteroarylheterocyclyl, containing at least one basic nitrogen atom, b) -imidazolyl, or c) -pyridyl; and R23, R24, and R25 independently comprise hydrogen, aryl, heteroaryl, -alkylene-heteroaryl, alkyl, -alkylene-aryl, -alkylene-O-aryl, or -alkylene-O-heteroaryl; and R23 and R24 may be taken together to form a ring having the formula —(CH2)s—X3—(CH2)t-bonded to the nitrogen atom to which R23 and R24 are attached wherein s and t are, independently, 1, 2, 3, or 4; X3 comprises direct bond, —CH2—, —O—, —S—, —S(O2)—, —C(O)—, —CON(H)—, —NHC(O)—, —NHCON(H)—, —NHSO2—, —SO2N(H)—, —C(O)—O—, —O—C(O)—, —NHSO2NH—, 646wherein R28 and R29 independently comprise hydrogen, aryl, heteroaryl, alkyl, -alkylene-aryl, or -alkylene-heteroaryl.
- 5. The compound of Formula (Ia) of claim 2, wherein R2 comprises 4-[3-(N,N′-diethylamino)-propoxy]-phenyl, 4-[3-(N,N′-dimethylamino)-propoxy]-phenyl, 3-[3-(N,N′-diethylamino)-propoxy]-phenyl, 4-(3-fluoro-4-trifluoromethyl-phenoxy)-phenyl, 4-(4-fluoro-3-trifluoromethyl-phenoxy)-phenyl, 4-(4-trifluoromethoxy-phenoxy)-phenyl, 4-(3,4-dichloro-phenoxy)-phenyl, 4-(3,5-bis-trifluoromethyl-phenoxy)-phenyl, 4-benzyloxy-phenyl, 4-(4-methyloxy-phenoxy)-phenyl, 4-(2-hexyl-4-chloro-phenoxy)-phenyl, 4-(4-phenyl-phenoxy)-phenyl, 4-(4-acetamido-phenoxy)-phenyl, 4-(4-methyl-phenoxy)-phenyl, 4-(4-fluoro-phenoxy)-phenyl, 4-(4-bromo-phenoxy)-phenyl, 4-(4-chloro-phenoxy)-phenyl, 4-(4-amino-phenoxy)-phenyl, 4-(3-ethyl-4-chloro-phenoxy)-phenyl, 4-[2-(N-ethylamino)-ethoxy]-phenyl, 4-[2,2′-dimethyl-3-(N,N′-dimethylamino)-propoxy]-phenyl, 1,2,3,4-tetrahydroisoquinolin-7-yl, 4-(4-benzamido-phenoxy)-phenyl, 4-(4-isonicotinamido-phenoxy)-phenyl, 4-[2-(N-methyl-N′-pyrid-4-yl)-ethoxy]-phenyl, 4-[3-(diethylmethyl ammonium)-propoxy)]-phenyl, 4-(2,5-di-fluoro-benzyloxy)-phenyl, 4-(2,4-dichloro-phenoxy)-phenyl, 4-(naphthalen-2-yloxy)-phenyl, 4-(6-methoxy-naphthalen-2-yloxy)-phenyl, 4-(4-methoxy-naphthalen-2-yloxy)-phenyl, 4-(6-hydroxy-naphthalen-2-yloxy)-phenyl, 4-(dibenzofuran-2-yloxy)-phenyl, 4-[2-(1-methyl-pyrrolidin-2-yl)-ethoxy]-phenyl, 4-[2-(piperazin-1-yl)-ethoxy]-phenyl, or 4-(4-tert-butyl-phenoxy)-phenyl.
- 6. The compound of Formula (Ia) of claim 2, wherein R3 comprises hydrogen; and R4 comprises a phenyl group, wherein the phenyl group is substituted with at least one substituent comprising
a) —Y2-alkyl; b) —Y2-aryl; c) —Y2-heteroaryl; d) —Y2-alkylene-heteroarylaryl; e) —Y2-alkylene-aryl; f) —Y2-alkylene-W2—R18; g) —Y3—Y4—NR23R24; h) —Y3—Y4—NH—C(═NR25)NR23R24; i) —Y3—Y4—C(═NR25)NR23R24; or j) —Y3—Y4—Y5—A2; wherein Y2 and W2 independently comprise —CH2—or —O—; R18 comprises aryl, alkyl, -alkylene-aryl, -alkylene-heteroaryl, or -alkylene-O-aryl; Y3 and Y5independently comprise a direct bond, —CH2—, —O—, —N(H), —S—, SO2—, —C(O)—, —CON(H)—, —NHC(O)—, —NHCON(H)—, —NHSO2—, —SO2N(H)—, —C(O)—O—, —NHSO2NH—, —O—CO—, 647wherein R27 and R26 independently comprise aryl, alkyl, -alkylene-aryl, alkoxy, or -alkyl-O-aryl; Y4 comprises
a) -alkylene; b) -alkenylene; c) -alkynylene; d) -arylene; e) -heteroarylene; f) -cycloalkylene; g) -heterocyclylene; h) -alkylene-arylene; i) -alkylene-heteroarylene; j) -alkylene-cycloalkylene; k) -alkylene-heterocyclylene; l) -arylene-alkylene; m) -heteroarylene-alkylene; n) -cycloalkylene-alkylene; o) -heterocyclylene-alkylene; p) —O—; q) —S—; r) —S(O2)—; or s) —S(O)—; wherein said alkylene groups may optionally contain one or more O, S, S(O), or SO2 atoms; A2comprises
a) heterocyclyl, fused arylheterocyclyl, or fused heteroarylheterocyclyl, containing at least one basic nitrogen atom, b) -imidazolyl, or c) -pyridyl; R23, R24, and R25 independently comprise hydrogen, aryl, heteroaryl, -alkylene-heteroaryl, alkyl, -alkylene-aryl, -alkylene-O-aryl, or -alkylene-O-heteroaryl; and R23and R24 may be taken together to form a ring having the formula —(CH2)s—X3—(CH2)t-bonded to the nitrogen atom to which R23 and R24 are attached wherein s and t are, independently, 1, 2, 3, or 4; X3 comprises direct bond, —CH2—, —O—, —S—, —S(O2)—, —C(O)—, —CON(H)—, —NHC(O)—, —NHCON(H)—, —NHSO2—, —SO2N(H)—, —C(O)—O—, —O—C(O)—, —NHSO2NH—, 648wherein R28 and R29 independently comprise hydrogen, aryl, heteroaryl, alkyl, -alkylene-aryl, or -alkylene-heteroaryl.
- 7. The compound of Formula (Ia) of claim 2, wherein R3 comprises hydrogen and R4 comprises 4-{2-[(4-chlorophenyl)-ethoxy]}-phenyl, 4-[3-(N,N′-diethylamino)-propoxy]-phenyl, 4-(2-amino-ethoxy)-phenyl, 4-[2-(N-methyl-N′-pyridin-4-yl-amino)-ethoxy]-phenyl, 4-[2-(N-ethyl-N′-pyridin-4-yl-amino)-ethoxy]-phenyl, 4-[2-(N-pyridin-4-yl-amino)-ethoxy]-phenyl, 4-(4-amino-pyridin-3-yl-oxy)-phenyl, 4-[(pyridin-4-yl)-amino]-phenyl, 4-[2-(N,N′-bis-pyridin-2-ylmethyl-amino)-ethoxy]-phenyl, 4-[2-(guanidinyl)-ethoxy]-phenyl, 4-{2-[4-(pyridin-4-yl)-piperazin-1-yl]-2-oxo-ethoxy}-phenyl, 4-[2-(N-methyl-N′-3-methylpyridin-4-yl-amino)-ethoxy]-phenyl, 4-(4-hydroxy-pyrrolidin-2-ylmethyloxy)-phenyl, 4-(4-amino-3,5-dimethyl-pyrrolidin-2-ylmethyloxy)-phenyl, dibenzofuran-2-yl, 4-[3-(piperazin-1-yl)-propoxy]-phenyl, 4-(piperazin-4-yloxy)-phenyl, 4-[5-(piperazin-1-yl)-pentoxy]-phenyl, 4-[3-(N,N′-dimethylamino)-propoxy]-phenyl, 4-(3-fluoro-4-trifluoromethyl-phenoxy)-phenyl, 4-(4-fluoro-3-trifluoromethyl-phenoxy)-phenyl, 4-(4-phenyl-phenoxy)-phenyl, 4-(3-trifluoromethoxy-phenoxy)-phenyl, 4-(4-trifluoromethyl-benzyloxy)-phenyl, 4-(3,4-dichloro-phenoxy)-phenyl, 4-(2,4-dichloro-phenoxy)-phenyl, 4-(1-ethyl-piperidin-3-yloxy)-phenyl, 4-benzyloxy-phenyl, 4-[(1-ethyl-piperidin-3-yl)-methoxy]-phenyl, 4-(4-phenoxy-benzyloxy)-phenyl, 4-(4-benzyloxy-benzyloxy)-phenyl, 4-(2-benzenesulfonylmethyl-benzyloxy)-phenyl, 4-(3,4,5-trimethoxybenzyloxy)-phenyl, 4-[2-(pyrrolidin-1-yl)-ethoxy]-phenyl, 4-[2-(piperidin-1-yl)-ethoxy]-phenyl, 4-[2,2′-dimethyl-3-(N,N′-dimethylamino)-propoxy]-phenyl, 4-[2-(N,N′-diisopropylamino)-ethoxy]-phenyl, 4-(adamantan-1-ylmethoxy)-phenyl, 3-[(2,6-dichlorophenyl)-4-methyl-isoxazol-5-ylmethyloxy]-phenyl, 4-(4-bromo-benzyloxy)-phenyl, 4-(4-chlorophenoxy)-phenyl, 4-[4-{(1-ethyl-piperidin-4-yl)-methylamino}-phenoxy]-phenyl, 4-(3,3-diphenylpropoxy)-phenyl, 4-[3,3-Bis-(4-fluorophenyl)-propoxy]-phenyl, 4-[3,3-Bis-(4-chlorophenyl)-allyoxy]-phenyl, 4-(4-chlorophenoxy)-naphthalenyl, 4-[2-(biphenyl-4-yl)-acetamido]-phenyl, 4-(2-(9H-carbazole)-ethoxy]-phenyl, 4-[4-methoxyphenyoxy]-phenyl, 4-(4-tert-butyl-phenoxy)-phenyl, or 4-(naphthylen-2-ylmethoxy)-phenyl.
- 8. The compound claim 1, wherein the compound of Formula (I) comprise a compound of Formula (Ib)
- 9. The compound of Formula (Ib) of claim 8, wherein R1 comprises comprises a hydrogen, methyl, ethyl, propyl, butyl, iso-butyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, 3-butenyl, tert-butyl, 3-cyclohexyl-propyl, 3-phenoxy-propyl, methoxymethyl, 4-fluoro-phenyl, 3-(4-chlorophenoxy)-propyl, 2,4,4-trimethyl-pentyl, 1-ethyl-propyl, 1-propyl-butyl, benzyloxymethyl, 2-cyclopropy-ethyl, 2-phenyl-ethyl, 4-tert-butylphenoxymethyl, 4-tert-butylcyclohexyl, 4-ethylcyclohexyl, 4-butylcyclohexyl, 3-methoxycarbonyl-1-propyl, or 2-(pyridin-3-yl)-ethyl group, and R3 comprises hydrogen.
- 10. The compound of Formula (Ib) of claim 8, wherein R102 and R104 independently comprise 2-(4-chlorophenyl)-ethyl, 3-(N,N′-diethylamino)-propyl, 2-amino-ethyl, 2-(N-methyl-N′-pyridin-4-yl-amino)-ethyl, 2-(N-ethyl-N′-pyridin-4-yl-amino)-ethyl, 2-(N-pyridin-4-yl-amino)-ethoxy, 4-(4-amino-pyridin-3-yl-oxy), 4-(pyridin-4-yl)-amino, 2-(N,N′-bis-pyridin-2-ylmethyl-amino)-ethyl, 2-(guanidinyl)-ethyl, 2-[4-(pyridin-4-yl)-piperazin-1-yl]-2-oxo-ethyl, 2-(N-methyl-N′-3-methylpyridin-4-yl-amino)-ethyl, 4-hydroxy-pyrrolidin-2-ylmethyl, 4-amino-3,5-dimethyl-pyrrolidin-2-ylmethyl, dibenzofuran-2-yl, 3-(piperazin-1-yl)-propyl, piperazin-4-yl, 5-(piperazin-1-yl)-pentyl, 3-(N,N′-dimethylamino)-propyl, 3-fluoro-4-trifluoromethyl-phenyl, 4-fluoro-3-trifluoromethyl-phenyl, 4-phenyl-phenyl, 3-trifluoromethoxy-phenyl, 4-trifluoromethyl-benzyl, 3,4-dichloro-phenyl, 2,4-dichloro-phenyl, 1-ethyl-piperidin-3-yl, benzyl, (1-ethyl-piperidin-3-yl)-methyl, 4-phenoxy-benzyl, 4-benzyloxy-benzyl, 2-benzenesulfonylmethyl-benzyl, 3,4,5-trimethoxybenzyl, 2-(pyrrolidin-1-yl)-ethyl, 2-(piperidin-1-yl)-ethyl, 2,2′-dimethyl-3-(N,N′-dimethylamino)-propyl, 2-(N,N′-diisopropylamino)-ethyl, 3-(2,6-dichlorophenyl)-4-methyl-isoxazol-5-ylmethyl, 4-bromo-benzyl, 4-chlorophenyl, 4-{(1-ethyl-piperidin-4-yl)-methylamino}-phenyl, 3,3-diphenylpropyl, 3,3-Bis-(4-fluorophenyl)-propyl, 3,3-Bis-(4-chlorophenyl)-allyl, 4-(4-chlorophenoxy)-naphthalenyl, 4-[2-(biphenyl-4-yl)-acetamido]-phenyl, 2-(9H-carbazole)-ethyl, 4-methoxyphenyl, 4-tert-butyl-phenyl, or naphthylen-2-ylmethyl.
- 11. The compound of Formula (Ib) of claim 8, wherein R1 comprises -alkyl, -alkylene-cycloalkylene-alkyl, -cycloalkyl, -heterocyclyl, -alkylene-cycloalkyl, -alkylene-heteroaryl, -alkylene-heterocyclyl, or -alkylene-heterocyclylene-alkyl; R3 comprises hydrogen; R102 comprises -aryl or -alkylene-aryl substituted with at least one of a halogen, a perhaloalkyl, or an alkoxy group; and R104 comprises —Y4—NR23R24 or —Y4—Y5—A2.
- 12. The compound of Formula (Ib) of claim 8, wherein R1 comprises -heterocyclyl, heterocyclylene-heteroaryl, -alkylene-cycloalkyl, -alkylene-heteroaryl, -alkylene-heterocyclyl, or -alkylene-heterocyclylene-alkyl; R3 comprises hydrogen; and R102 and R104 independently comprise -aryl or -alkylene-aryl, wherein the alkyl or ary groups are optionally substituted with at least one of a halogen, a perhaloalkyl, or an alkoxy group, and wherein at least one of R102 and R104 comprise —Y4—NR23R24 or —Y4—Y5—A2, wherein Y4 comprises alkylene.
- 13. The compound claim 1, wherein the compound of Formula (I) comprise a compound of Formula (Ic)
- 14. The compound of Formula (Ic) of claim 13, wherein R2 comprises hydrogen or alkyl.
- 15. The compound of Formula (Ic) of claim 13, wherein R1 comprises a phenyl group substituted by one or more substituents comprising
a) —Y2-alkyl; b) —Y2-aryl; c) —Y2-heteroaryl; d) —Y2-alkylene-heteroarylaryl; e) —Y2-alkylene-aryl; f) —Y2-alkylene-W2—R18; g) —Y3—Y4—NR23R24 h) —Y3—Y4—NH—C(═NR25)NR23R24 i) —Y3—Y4—C(═NR25)NR23R24 j) —Y3—Y4—Y5—A2 wherein Y2 and W2 independently comprise —CH2—, —O—, and R18 comprises aryl, alkyl, -alkylene-aryl, -alkylene-heteroaryl, or -alkylene-O-aryl; Y3 and Y5independently comprise a direct bond, —CH2—, —O—, —N(H), —S—, SO2—, —C(O)—, —CON(H)—, —NHC(O)—, —NHCON(H)—, —NHSO2—, —SO2N(H)—, —C(O)—O—, —NHSO2NH—, —O—CO—, 657wherein R27 and R26 independently comprise aryl, alkyl, -alkylene-aryl, alkoxy, or -alkyl-O-aryl; Y4 comprises
a) -alkylene; b) -alkenylene; c) -alkynylene; d) -arylene; e) -heteroarylene; f) -cycloalkylene; g) -heterocyclylene; h) -alkylene-arylene; i) -alkylene-heteroarylene; j) -alkylene-cycloalkylene; k) -alkylene-heterocyclylene; l) -arylene-alkylene; m) -heteroarylene-alkylene; n) -cycloalkylene-alkylene; o) -heterocyclylene-alkylene; p) —O—; q) —S—; r) —S(O2)—; or s) —S(O)—; wherein said alkylene groups may optionally contain one or more O, S, S(O), or SO2 atoms; A2 comprises
a) heterocyclyl, fused arylheterocyclyl, or fused heteroarylheterocyclyl, containing at least one basic nitrogen atom, b) -imidazolyl, or c) -pyridyl; R23, R24, and R25 independently comprise hydrogen, aryl, heteroaryl, -alkylene-heteroaryl, alkyl, -alkylene-aryl, -alkylene-O-aryl, or -alkylene-O-heteroaryl; and R23 and R24 may be taken together to form a ring having the formula —(CH2)s—X3—(CH2)t-bonded to the nitrogen atom to which R23 and R24 are attached wherein s and t are, independently, 1, 2, 3, or 4; X3 comprises direct bond, —CH2—, —O—, —S—, —S(O2)—, —C(O)—, —CON(H)—, —NHC(O)—, —NHCON(H)—, —NHSO2—, —SO2N(H)—, —C(O)—O—, —O—C(O)—, —NHSO2NH—, 658wherein R28 and R29 independently comprise hydrogen, aryl, heteroaryl, alkyl, -alkylene-aryl, or -alkylene-heteroaryl.
- 16. The compound of Formula (Ic) of claim 13, wherein R1 comprises 2-methoxy-3,5-dimethyoxy-phenyl, 3-(4-tert-butyl-phenoxy)-phenyl, 4-[3-(N,N′-diethylamino)-propoxy]-phenyl, 4-[3-(N,N′-dimethylamino)-propoxy]-phenyl, 4-[(pyrrolidin-1-yl)-ethoxy]-phenyl, 3-[(pyrrolidin-1-yl)-ethoxy]-phenyl, 2-[(pyrrolidin-1-yl)-ethoxy]-phenyl, 3-(naphthalen-2-yloxy)-phenyl, 4-biphenyl, 3-(3,3-dimethylbutoxy)-phenyl, 3-(phenoxy)-phenyl, 3-(3,4-dichloro-phenoxy)-phenyl, 3-(3,5-dichloro-phenoxy)-phenyl, 4-tert-butyl-phenyl, 4-(dibutylamino)-phenyl, 4-[2-(4-methoxy-phenyl)-ethoxy]-phenyl, 2-naphthyl, 2-benzofuranyl, 3-(3-trifluoromethyl-phenoxy)-phenyl, 4-chloro-phenyl, 2-benzhydryl, 4-isopropoxy-phenyl, 3-(4-tertbutyl-phenoxy)-phenyl, 4-[2-(4-chloro-phenyl)-ethoxy]-phenyl, 3-[2-(4-chloro-phenyl)-ethoxy]-phenyl, 2-{3-[2-(4-chloro-phenyl)-ethoxy]-phenyl]-ethyl, 2-{4-[2-(4-methoxy-phenyl)-ethoxy]-phenyl}-ethyl, or 2-[3-(N,N-diethylamino)-propoxy)]-4-[2-(4-chloro-phenyl)-ethoxy]-phenyl.
- 17. The compound of Formula (Ic) of claim 13, wherein R1 comprises 4-[2-(4-chloro-phenyl)-ethoxy]-phenyl, 3-[2-(4-chloro-phenyl)-ethoxy]-phenyl, 2-{3-[2-(4-chloro-phenyl)-ethoxy]-phenyl]-ethyl, 2-{4-[2-(4-methoxy-phenyl)-ethoxy]-phenyl}-ethyl, or 2-[3-(N,N-diethylamino)-propoxy)]-4-[2-(4-chloro-phenyl)-ethoxy]-phenyl.
- 18. The compound of Formula (Ic) of claim 13, wherein R111, R112 and R114 comprise hygrogen; and R113 comprises —Y3—Y4—NR23R24, or —Y3—Y4—Y5—A2 .
- 19. The compound of Formula (Ic) of claim 13, wherein R1 comprises 4-[2-(4-chloro-phenyl)-ethoxy]-phenyl, 3-[2-(4-chloro-phenyl)-ethoxy]-phenyl, 2-{3-[2-(4-chloro-phenyl)-ethoxy]-phenyl]-ethyl, 2-{4-[2-(4-methoxy-phenyl)-ethoxy]-phenyl}-ethyl, or 2-[3-(N,N-diethylamino)-propoxy)]-4-[2-(4-chloro-phenyl)-ethoxy]-phenyl; R2 comprises alkyl; R112 and R114 comprise hygrogen; and R111 and R113 comprise —Y3—Y4—NR23R24, or —Y3—Y4—Y5—A2.
- 20. A pharmaceutical composition comprising the compound of Formula (I) as claimed in claim 1, and one or more pharmaceutically acceptable carriers, excipients, or diluents.
- 21. The pharmaceutical composition of to claim 20, in the form of an oral dosage or parenteral dosage unit.
- 22. The pharmaceutical composition of claim 20, wherein said compound is administered as a dose in a range from about 0.01 to 500 mg/kg of body weight per day.
- 23. The pharmaceutical composition of claim 20, wherein said compound is administered as a dose in a range from about 0.1 to 200 mg/kg of body weight per day.
- 24. The pharmaceutical composition of claim 20, wherein said compound is administered as a dose in a range from about 0.1 to 100 mg/kg of body weight per day.
- 25. The pharmaceutical composition of to claim 20, in a topical dosage form.
- 26. The pharmaceutical composition of claim 25, wherein said compound is applied to the skin.
- 27. The pharmaceutical composition of claim 26, wherein said compound is administered in a formulation ratio of 0.1% to 99% of compound to topical excipient.
- 28. The pharmaceutical composition of claim 20, wherein said compound is in an inhaled dosage form.
- 29. The pharmaceutical composition of claim 28, wherein said composition is an aerosol formulation.
- 30. The pharmaceutical composition of claim 28, wherein said composition is an inhaled powder dosage form.
- 31. The pharmaceutical composition of claim 20, further comprising one or more therapeutic agents selected from the group consisting of alkylating agents, antimetabolites, plant alkaloids, antibiotics, hormones, biologic response modifiers, analgesics, NSAIDs, DMARDs, glucocorticoids, sulfonylureas, biguanides, insulin, cholinesterase inhibitors, antipsychotics, antidepressants, and anticonvulsants.
- 32. A method for the inhibition of the interaction of RAGE with its physiological ligands, which comprises administering to a subject in need thereof, at least one compound of Formula (I) as claimed in claim 1.
- 33. The method of claim 32, wherein the ligand(s) is(are) selected from advanced glycated end products (AGEs), S100/calgranulin/EN-RAGE, β-amyloid and amphoterin.
- 34. A method for treating a disease state selected from the group consisting of acute and chronic systemic inflammation, acute and skin inflammation, symptoms of diabetes, vascular permeability, nephropathy, atherosclerosis, retinopathy, Alzheimer's disease, erectile dysfunction, tumor invasion and/or metastasis, asthma, or chronic obstructive pulmonary disease, which comprises administering to a subject in need thereof a therapeutically effective amount of at least one compound of Formula (I) as claimed in claim 1.
- 35. A method of prevention and/or treatment of RAGE mediated human diseases, treatment comprising alleviation of one or more symptoms resulting from that disorder, to an outright cure for that particular disorder or prevention of the onset of the disorder, the method comprising administration to a human in need thereof a therapeutically effective amount of a compound of Formula (I) as claimed in claim 1.
- 36. The method of claim 32, further comprising administering to a subject in need thereof at least one adjuvant and/or additional therapeutic agent(s).
- 37. The method of claim 34, further comprising administering to a subject in need thereof at least one adjuvant and/or additional therapeutic agent(s).
- 39. The method of claim 35, further comprising administering to a subject in need thereof at least one adjuvant and/or additional therapeutic agent(s).
- 40. A method of treating RAGE mediated diseases, the method comprising administering to a subject in need thereof, a therapeutically effective amount of a compound of Formula (I) as claimed in claim 1, in combination with one or more therapeutic agents selected from the group consisting of alkylating agents, antimetabolites, plant alkaloids, antibiotics, hormones, biologic response modifiers, analgesics, NSAIDs, DMARDs, glucocorticoids, sulfonylureas, biguanides, insulin, cholinesterase inhibitors, antipsychotics, antidepressants, and anticonvulsants.
- 41. A method for treating acute and/or chronic inflammation, skin inflammatory disease, vascular permeability, nephropathy, atherosclerosis, retinopathy, Alzheimer's disease, erectile dysfunction, tumor invasion and/or metastasis, asthma, or chronic obstructive pulmonary disease, which comprises administering to a subject in need thereof a therapeutically effective amount of a compound of Formula (I) as defined in claim 1.
STATEMENT OF RELATED APPLICATION
[0001] The present application claims priority under 35 USC 119(e) from the following U.S. Provisional Application: Serial No. 60/361,983, filed Mar. 5, 2002, entitled “Azole Derivatives as Therapeutic Agents,” the entirety of which is herein incorporated by reference.
Provisional Applications (1)
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Number |
Date |
Country |
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60361983 |
Mar 2002 |
US |