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US 2011/0212992 A1Published application
Novel p2x7r antagonists and their use
AssigneeAffectis Pharmaceuticals AG
InventorMichael BOES
Life of this patent
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Abstract
The present application is directed to novel P2X7R antagonists that are N-indol-3-yl-acetamide and N-azaindol-3-yl-acetamide compounds, pharmaceutical compositions comprising the same and their use for the prophylactic or therapeutic treatment of diseases mediated by P2X7R activity.
Claims18
-19. (canceled)
A method for the treatment of a disease or disorder mediated by P2X7R or IL-1 in a patient comprising administering to the patient a therapeutically effective amount of a compound of the general formula:
- or a pharmaceutically acceptable salt or solvate thereof;
- wherein,
- R1 is a mono- or bi-cycloalkylalkyl group or mono- or bi-cycloalkyl group;
- R2 is selected from straight or branched C1-C5 alkyl which may optionally substituted with —OH, —CH2—OH, C1-C5 alkoxy, N(Ra)2—, NHRa—, CN—, CF3, halogen, piperidino, morpholine, pyrrolidino, 5H-tetrazolylpropyl, methylcarbamoyl, dimethylcarbamoyl, or ethylmethylcarbamoyl, wherein Ra is C1-C5 alkyl;
- R3, R4, R5, R6 are at each occurrence independently selected from hydrogen, halogen (i.e. Cl, F, Br or I), methyl, methoxy, cyano, or trifluoromethyl;
- and
- a, b, c, d, x are at each occurrence independently selected from carbon, or nitrogen.
4 more elements
Dependencies are inferred from the claim text.