Claims
- 1. A compound of Formula I
- 2. The compound according to claim 1, or a pharmaceutically acceptable salt thereof, wherein V1 is
- 3. The compound according to claim 1, or a pharmaceutically acceptable salt thereof, wherein V1 is
- 4. The compound according to claim 1, or a pharmaceutically acceptable salt thereof, wherein Q is N(R6)C(O).
- 5. The compound according to claim 1, or a pharmaceutically acceptable salt thereof, wherein Q is C≡C.
- 6. The compound according to any one of claims 1 to 5, or a pharmaceutically acceptable salt thereof, wherein at least one of R1 and R2 is independently selected from:
Phenyl-(C1-C6 alkylenyl); and Substituted phenyl-(C1-C6 alkylenyl); wherein each group and each substituent is independently selected.
- 7. The compound according to according to any one of claims 1 to 5, or a pharmaceutically acceptable salt thereof, wherein at least one of R1 and R2 is independently selected from:
5-, 6-, 9-, and 10-membered heteroaryl-(C1-C6 alkylenyl); and Substituted 5-, 6-, 9-, and 10-membered heteroaryl-(C1-C6 alkylenyl); wherein each heteroaryl contains carbon atoms and from 1 to 4 heteroatoms independently selected from 1 O, 1 S, 1 N(H), 1 N(C1-C6 alkyl), and 4 N, and 5- and 6-membered heteroaryl are monocyclic rings and 9- and 10-membered heteroaryl are 6,5-fused and 6,6-fused bicyclic rings, respectively, wherein at least 1 of the 2 fused rings of a bicyclic ring is aromatic, and wherein when the O and S atoms both are present, the O and S atoms are not bonded to each other; and wherein each group and each substituent is independently selected.
- 8. A compound of Formula II, III, IV, V, or VI
- 9. The compound of Formula II according to claim 8, selected from:
4-[5-(3-Benzylcarbamoyl-2,6-dioxo-3,6-dihydro-2H-pyrazin-1-yl)-tetrazol-2-yl]-benzoic acid; 4-(5-{2,6-Dioxo-3-[(pyridin-4-ylmethyl)-carbamoyl]-3,6-dihydro-2H-pyrazin-1-yl}-tetrazol-2-yl)-benzoic acid; 4-[3-(3-Benzylcarbamoyl-2,6-dioxo-3,6-dihydro-2H-pyrazin-1-yl)-prop-2-ynyl]-benzoic acid; 4-(3-{2,6-Dioxo-3-[(pyridin-4-ylmethyl)-carbamoyl]-3,6-dihydro-2H-pyrazin-1-yl}-prop-2-ynyl)-benzoic acid; 4-{2-[2,6-Dioxo-3-(3-phenyl-prop-1-ynyl)-3,6-dihydro-2H-pyrazin-1-yl]-oxazol-5-yl}-benzoic acid; 4-{2-[3-(3-Imidazol-1-yl-prop-1-ynyl)-2,6-dioxo-3,6-dihydro-2H-pyrazin-2H-pyrazin-1-yl]-oxazol-4-yl}-benzoic acid; 4-{3-[2,6-Dioxo-3-(3-phenyl-prop-1-ynyl)-3,6-dihydro-2H-pyrazin-1-yl]-prop-2-ynyl}-benzoic acid; 4-{3-[3-(3-Imidazol-1-yl-prop-1-ynyl)-2,6-dioxo-3,6-dihydro-2H-pyrazin-1-yl]-prop-2-ynyl}-benzoic acid; 4-({[2,6-Dioxo-3-(5-phenyl-oxazol-2-yl)-3,6-dihydro-2H-pyrazine-1-carbonyl]-amino}-methyl)-benzoic acid; 4-{3-[2,6-Dioxo-3-(5-phenyl-oxazol-2-yl)-3,6-dihydro-2H-pyrazin-1-yl]-prop-2-ynyl}-benzoic acid; 4-{5-[2,6-Dioxo-3-(4-phenyl-oxazol-2-yl)-3,6-dihydro-2H-pyrazin-1-yl]-tetrazol-2-yl}-benzoic acid; and 4-{3-[2,6-Dioxo-3-(4-phenyl-oxazol-2-yl)-3,6-dihydro-2H-pyrazin-1-yl]-prop-2-ynyl}-benzoic acid; or a pharmaceutically acceptable salt thereof.
- 10. The compound of Formula III according to claim 8, selected from:
4-[5-(5-Benzylcarbamoyl-6-oxo-6H-pyridazin-1-yl)-tetrazol-2-yl]-benzoic acid; 4-(5-{6-Oxo-5-[(pyridin-4-ylmethyl)-carbamoyl]-6H-pyridazin-1-yl}-tetrazol-2-yl)-benzoic acid; 4-[3-(5-Benzylcarbamoyl-6-oxo-6H-pyridazin-1-yl)-prop-2-ynyl]-benzoic acid; 4-(3-{6-Oxo-5-[(pyridin-4-ylmethyl)-carbamoyl]-6H-pyridazin-1-yl}-prop-2-ynyl)-benzoic acid; 4-{2-[6-Oxo-5-(3-phenyl-prop-1-ynyl)-6H-pyridazin-1-yl]-oxazol-5-yl}-benzoic acid; 4-{2-[5-(3-Imidazol-1-yl-prop-1-ynyl)-6-oxo-6H-pyridazin-1-yl]-oxazol-4-yl}-benzoic acid; 4-{3-[6-Oxo-5-(3-phenyl-prop-1-ynyl)-6H-pyridazin-1-yl]-prop-2-ynyl}-benzoic acid; 4-{3-[5-(3-Imidazol-1-yl-prop-1-ynyl)-6-oxo-6H-pyridazin-1-yl]-prop-2-ynyl}-benzoic acid; 4-({[6-Oxo-5-(5-phenyl-oxazol-2-yl)-6H-pyridazine-1-carbonyl]-amino}-methyl)-benzoic acid; 4-{3-[6-Oxo-5-(5-phenyl-oxazol-2-yl)-6H-pyridazin-1-yl]-prop-2-ynyl}-benzoic acid; 4-{5-[6-Oxo-5-(4-phenyl-oxazol-2-yl)-6H-pyridazin-1-yl]-tetrazol-2-yl}-benzoic acid; and 4-{3-[6-Oxo-5-(4-phenyl-oxazol-2-yl)-6H-pyridazin-1-yl]-prop-2-ynyl}-benzoic acid; or a pharmaceutically acceptable salt thereof.
- 11. A pharmaceutical composition, comprising a compound according to claim 1, or a pharmaceutically acceptable salt thereof, admixed with a pharmaceutically acceptable carrier, excipient, or diluent.
- 12. The pharmaceutical composition according to claim 11, comprising a compound according to claim 9 or 10, or a pharmaceutically acceptable salt thereof, admixed with a pharmaceutically acceptable carrier, excipient, or diluent.
- 13. A method for treating osteoarthritis or rheumatoid arthritis, comprising administering to a patient suffering from osteoarthritis or rheumatoid arthritis a nontoxic effective amount of a compound according to claim 1, or a pharmaceutically acceptable salt thereof.
- 14. The method according to claim 13, wherein the compound administered is a compound according to claim 9 or 10, or a pharmaceutically acceptable salt thereof.
CROSS-REFERENCE TO RELATED APPLICATIONS
[0001] This application claims benefit of priority from U.S. Provisional Patent Application No. 60/403,040, filed Aug. 13, 2002.
Provisional Applications (1)
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Number |
Date |
Country |
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60403040 |
Aug 2002 |
US |