Tricyclic .delta.3-piperidines as pharmaceuticals

Details Tricyclic .delta.3-piperidines as pharmaceuticals Tricyclic .delta.3-piperidines as pharmaceuticals

C - Chemistry, Metallurgy

07

D

C07D 495/04 (2006.01) A61K 31/4353 (2006.01) A61K 31/4355 (2006.01) C07D 221/00 (2006.01) C07D 307/00 (2006.01) C07D 333/00 (2006.01) C07D 491/04 (2006.01) C07D 491/048 (2006.01)

Patent

CA 2346082

The present invention concerns the compounds of formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein Alk is C1- 6alkanediyl; n is 1 or 2; X is -O-, -S-, -S(=O)- or -S(=O)2-; each R1 is independently hydrogen, halogen, C1-6alkyl, nitro, hydroxy or C1- 4alkyloxy; D is an indole, a benzisoxazole, a benzisothiazole, a 2H-benzopyranone, a phenoxyphenyl, a benzamide, a benzophenone or a benzopyrimidinone having central .alpha.2-adrenoceptor antagonist activity. It further relates to their preparation, pharmaceutical use and compositions.

La présente invention concerne des composés représentés par la formule (I), leurs formes N-oxydes, leurs sels d'addition acceptables au plan pharmaceutique et leurs formes stéréochimiquement isomères. Dans la formule selon l'invention, Alk représente un alcanediyle en C1-6; n représente 1 ou 2; X représente, -O-, -S-, -S(=O)-, ou -S(=O)2-; chaque R<1> représente indépendamment un hydrogène, un halogène, un alkyle en C1-6, un nitro, un hydroxy ou un alkyloxy en C1-4; D représente un indole, un benzisoxazole, un benzisothiazole, un 2H-benzopyranone, un phénoxyphényle, un benzamide, un benzophénone ou un benzopyrimidinone possédant une activité d'agoniste d' alpha 2-adrénorécepteur central. L'invention concerne également la préparation de ces composés, leur usage pharmaceutique et leurs compositions.

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