Benzimidazolone derivatives as 5-ht1a and 5-ht2 antagonists

Details Benzimidazolone derivatives as 5-ht1a and 5-ht2 antagonists Benzimidazolone derivatives as 5-ht1a and 5-ht2 antagonists

C - Chemistry, Metallurgy

07

D

C07D 403/06 (2006.01) A61K 31/415 (2006.01) A61K 31/495 (2006.01) A61K 31/55 (2006.01) C07D 235/26 (2006.01) C07D 403/12 (2006.01) C07D 403/14 (2006.01) C07D 405/12 (2006.01) C07D 405/14 (2006.01)

Patent

CA 2114542

Image Pharmacologically active benzimidazolone derivatives as 5-HT1A and 5-HT2 receptors, useful in the treatment of CNS disorders of formula (I), wherein R1 and R2 may be at the same time or not a hydrogen atom, halogen, trifluoromethyl, C1-6 alkyl, C1-6 alkoxy, C1-6 alkylthio, C1-6 acyl, carboxyl, C1-6 alkoxy- carbonyl, hydroxy, nitro, amino optionally C1-4 alkyl N-mono or di-substituted, C1-6 acylamino, C1-6 alkoxycarbonylamino, carbamoyl optionally C1-4 alkyl N-mono or di-substituted, cyano, C1-6 alkylsulphinyl, C1-6 alkylsulphonyl, amino sulphonyl optionally C1-4 alkyl N-mono or di-substituted, Ct.~ al- kyl N-mono or di-substituted aminosulphonylamino, aminosulphonylamino; R3 is hydrogen, C1-6 alkyl, C2-6 alkenyl or C2-6 alkynyl; A is -CO- or -CONH- or it is absent; B is a straight or branched, saturated or unsaturated C2-6 alkyl; m and n are both independently an integer from 1 to 3; R4 is an aryl, aralkyl, a heteroaryl, or heteroaralkyl group, each group being optionally substituted by one or more substituents selected from halogen, trifluoromethyl, cyano, C1-3 alkoxy, C1-4 alkyl and acid addition salts thereof. The process for the preparation of the compounds of formula (I) as well as pharmaceutical compositions containing them are also described.

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