Pyrimidine derivatives, a process for preparing them and a...

C - Chemistry – Metallurgy – 07 – D

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C07D 239/42 (2006.01) C07D 239/70 (2006.01) C07D 405/12 (2006.01)

Patent

CA 1169861

ABSTRACT New 4-anilinopyrimidine derivatives of formula (I): Image (I) (wherein: R1 and R2 are the same or different and each represents a C1 - C6 alkyl group or R1 and R2 together represent a C3 - C5 alkylene group; R3 represents a hydrogen atom or a C1 - C6 alkyl group; n is 0, 1 or 2; and R4 represents a C1 - C6 alkyl group, a C1 C6 alkoxy group, a C1 - C6 haloalkyl group, a halogen atom, a nitro group, a C1 - C6 alkanesulphonyl group, a cyano group, a carboxy group or a C2 - C7 alkoxycarbonyl group and, when n is 2, the two groups represented by R4 may be the same or different or they may together represent a methylenedioxy group) and pharmaceutically acceptable acid addition salts thereof have been found to have strong antidepressant activity, with low toxicity and very few side-effects. The compounds may be formulated in conventional pharmaceutical compositions for admi- nistration by various routes and may be prepared by reacting a 4-halopyrimidine with aniline or an aniline derivative.

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