4,4-disubstituted piperidine derivatives, pharmaceutical...

C - Chemistry – Metallurgy – 07 – D

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C07D 211/48 (2006.01) A61K 31/445 (2006.01)

Patent

CA 2023017

NOVEL 4,4-DISUBSTITUTED PIPERIOINE DERIVATIVES, PHARMACEU- TICAL COMPOSITIONS CONTAINING THEM AND PROCESS FOR PREPARING SAME Abstract The invention relates to novel, therapeutically active 4,4-disubstituted piperidine derivatives of the formula (I), Image (I) wherein R1 means hydrogen or -CONHR group, wherein R stands for hydrogen, C1-12alkyl, C3-6cycloalkyl, carbocyclic C6-10aryl or carbocyclic C6-10aryl- C1-4alkyl group, the two latter ones being op- tionally substituted on their aromatic part by one or more, same or different halogen(s) or one or more C1-4alkyl or C1-4alkoxy group(s); R2 stands for an ethynyl or acetyl group; R3 and R4, which are the same or different, represent hydro- gen, one or more halogen(s), C1-4alkyl, C1-4alkoxy, trihalomethyl group or hydroxyl group optionally ester- ified by a C1-4alkanoic acid; and n is 1 or 2, as well as their pharmaceutically acceptable acid addition and quaternary ammonium salts. The invention further relates to pharmaceutical compo- sitions containing these compounds and a proces for their preparation. The compounds of the formula (I) are useful for the treatment of psychotic disorders, insomnia, mania, agita- tion, depression, anxiety, emesis, pain and dementia.

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