Benzodiazepine compounds and their use as pharmaceuticals

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

CPC

260/239.5

IPC codes

C07D 487/04 (2006.01)

Type

Patent

Patent number

CA 1164457

Description

ABSTRACT OF THE DISCLOSURE The present invention provides compounds of formula Image where R1, R2 and R3 independently represent hydrogen, halogen or C1-4haloalkyl, R6 is C1-6alkyl, C3-7cycloalkyl or C3-7cycloalkylC1-6alkyl , and Q is -OH or -NH2. These compounds, which are useful as intermediates for the preparation of compounds of formula (I): Image wherein R1, R2, R3 and R6 are defined above; and in which R5 is a group of the formula Image where R9 is hydrogen, C1-14 alkyl, C3-7 cycloalkyl, C3-7 cycloalkyl, C1-4 alkyl, C1-4 haloalkyl, C2-4 alkenyl, C1-4 alkanoul, benzyl, cyano or optionally substituted phenyl, where R10 is hydrogen, C1-4 alkyl or optionally substituted phenyl, and where n is 0 or 1; are prepared by ring closing a compound of formula Image where Z is CN, COOH or COOR12, R12 being a C1-4 alkyl group. The compounds of formula (I) as defined above have neuroleptic, sedative, relaxant, anxiolytic or anti-emetic properties, and low toxicity, and are useful in the treatment of disorders of the central nervous system.

Application Number

433655

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