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US 8,569,334 B2Granted
P2X7R antagonists and their use
AssigneeAffectis Pharmaceuticals AG
InventorMichael Bös
Life of this patent
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Abstract
The present application is directed to novel P2X7R antagonists that are indol-3-carboxamide or azaindole-3-carboxamide compounds, pharmaceutical compositions comprising the same and their use for the prophylactic or therapeutic treatment of diseases mediated by P2X7R activity.
Claims11
A compound of the general formula:
- wherein,
- R1 is a mono- or bicycloalkylalkyl group;
- R2 is selected from straight or branched C1-C5 alkyl which may optionally substituted with —OH, C1-C5 alkoxy, NH2—, N(Ra)2—,NHRa—, CN—, CF3, halogen, piperidino, morpholino, pyrrolidino, 5H-tetrazolylpropyl, methylcarbamoyl, dimethylcarbamoyl, or ethylmethylcarbamoyl, wherein Ra is hydrogen or C1-C5 alkyl;
- R3, R4, R5, R6, are at each occurrence independently selected from hydrogen, halogen, methyl, hydroxy, methoxy, cyano, or trifluoromethyl;
- and
- a, b, c, and d are carbon and x is nitrogen, or
- a, c, d, and x are carbon and b is nitrogen, or
- a, b, d, and x are carbon and c is nitrogen, or
- b, c, d, and x are carbon and a is nitrogen;
- or a pharmaceutically acceptable salt or solvate thereof.
7 more elements
A compound selected from the group consisting of
- 4-chloro-N-(cycloheptylmethyl)- 1-methyl-1H-indazole-3-carboxamide,
- 4-bromo-N-(cycloheptylmethyl)-1-methyl-1H-indazole-3-carboxamide,
- N-(bicyclo [2.2.2]octan-1-ylmethyl)-4-chloro-1-methyl-1H-indazole-3-carboxamide,
- N-(bicyclo [2.2.2]octan-1-ylmethyl)-4-bromo-1-methyl-1H-indazole-3-carboxamide,
- 4-chloro-N-(cycloheptylmethyl)-1-methyl-1H-pyrrolo [2,3-b]pyridine-3-carboxamide),
- 4-bromo-N-(cycloheptylmethyl)-1-methyl-1H-pyrrolo [2,3-b]pyridine-3-carboxamide,
- N-(bicyclo [2.2.2]octan-1-ylmethyl)-4-chloro-1-methyl-1H-pyrrolo [2,3-b]pyridine-3carboxamide,
- N-(bicyclo [2.2.2]octan-1-ylmethyl)-4-bromo-1-methyl-1H-pyrrolo [2,3-b]pyridine-3carboxamide,
- 4-chloro-N-(cycloheptylmethyl)-1-methyl-1H-pyrrolo [3,2-c]pyridine-3-carboxamide,
- 4-bromo-N-(cycloheptylmethyl)-1-methyl-1H-pyrrolo [3,2-c]pyridine-3-carboxamide),
- N-(bicyclo [2.2.2]octan-1-ylmethyl)-4-chloro-1-methyl-1H-pyrrolo [3,2-c]pyridine-3carboxamide,
- N-(bicyclo [2.2.2]octan-1-ylmethyl)-4-bromo-1-methyl-1H-pyrrolo [3,2-c]pyridine-3carboxamide,
- 4-chloro-N-(cycloheptylmethyl)-1-methyl-1H-pyrrolo [2,3-c]pyridine-3-carboxamide,
- 4-bromo-N-(cycloheptylmethyl)-1-methyl-1H-pyrrolo [2,3-c]pyridine-3-carboxamide,
- N-(bicyclo [2.2.2]octan-1-ylmethyl)-4-chloro-1-methyl-1H-pyrrolo [2,3-c]pyridine-3carboxamide, and
- N-(bicyclo [2.2.2]octan-1-ylmethyl)-4-bromo-1-methyl-1H-pyrrolo [2,3-c]pyridine-3carboxamide.
13 more elements
Dependencies are inferred from the claim text.