Indoles
AssigneeHoffmann-La Roche Inc.
InventorsCaterina Bissantz, Christophe Grundschober, Raffaello Masciadri, Hasane Ratni, Mark Rogers-Evans, Patrick Schnider
Life of this patent
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Abstract
The present invention is concerned with novel indol-2-yl-carbonyl-piperidine derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are useful in the prevention and/or treatment of anxiety and depressive disorders and other diseases. Present invention is concerned with compounds of the general formula (I) wherein R1 to R6, R8 to R14, R12,, R13,, X and Y are as defined in the specification.
Claims13
The compound of the formula (Ic)
- wherein
- R1 is hydrogen, or
- C1-6-alkyl, optionally substituted by CN or OH;
- R2 is hydrogen,
- C1-6-alkyl, or
- C1-6-alkoxy,
- R3 is hydrogen,
- halo, or
- C1-6-alkyl;
- R4 is hydrogen,
- halo,
- C1-6-alkyl,
- halo-C1-6-alkyl,
- C1-6-alkoxy, or
- halo-C1-6-alkoxy
- R5 is hydrogen,
- halo,
- C1-6-alkyl, or
- C1-6-alkoxy;
- R6 is hydrogen,
- C1-6-alkyl, optionally substituted by CN or OH,
- nitro,
- halo,
- cyano,
- C1-6-alkoxy,
- halo-C1-6-alkoxy, or
- halo-C1-6-alkyl,
- R12, R12′, R13, R13′, and R14 are each independently hydrogen, C1-6-alkoxy, C1-6-alkyl, halo, halo-C1-6-alkoxy, halo-C1-6-alkyl, or nitro;
- or a pharmaceutically acceptable salt thereof.
The compound of formula (I), which is (3,7-Dimethyl-1H-indol-2-yl)-(4-phenyl-3,6-dihydro-2H-pyridin-1-yl)-methanone.
A pharmaceutical composition comprising a therapeutically effective amount of a compound of formula (Ic)
- wherein
- R1 is hydrogen, or
- C1-6-alkyl, optionally substituted by CN or OH
- R2 is hydrogen,
- C1-6-alkyl, or
- C1-6-alkoxy;
- R3 is hydrogen,
- halo, or
- C1-6-alkyl;
- R4 is hydrogen,
- halo,
- C1-6-alkyl,
- halo-C1-6-alkyl,
- C1-6-alkoxy, or
- halo-C1-6-alkoxy;
- R5 is hydrogen,
- halo,
- C1-6-alkyl, or
- C1-6-alkoxy;
- R6 is hydrogen,
- C1-6-alkyl, optionally substituted by CN or OH,
- nitro,
- halo,
- cyano,
- C1-6-alkoxy,
- halo-C1-6-alkoxy, or
- halo-C1-6-alkyl,
- R12R12′, R13R13′, and R14 are each independently hydrogen, C1-6-alkoxy, C1-6-alkyl, halo, halo-C1-6-alkoxy, halo-C1-6-alkyl, or nitro;
- or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier.
Dependencies are inferred from the claim text.