Tricyclic .delta.3-piperidines as .alpha.2-antagonists

Details Tricyclic .delta.3-piperidines as .alpha.2-antagonists Tricyclic .delta.3-piperidines as .alpha.2-antagonists

C - Chemistry, Metallurgy

07

D

C07D 519/00 (2006.01) A61K 31/415 (2006.01) A61K 31/42 (2006.01) A61K 31/425 (2006.01) A61K 31/505 (2006.01) A61K 31/54 (2006.01) C07D 491/04 (2006.01) C07D 495/04 (2006.01) C07D 513/00 (2006.01)

Patent

CA 2345622

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; X1 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 optionally substituted mono, bi- or tricyclic nitrogen containing heterocycle, a 2H-benzopyranone, a benzamide, a benzophenone or a phenoxyphenyl having central .alpha.2-adrenoceptor antagonist activity. It further relates to their preparation, pharmaceutical use and compositions.

La présente invention concerne les composés de la formule (I), leurs formes N-oxyde, 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; X1 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 éventuellement un azote mono, bi ou tricyclique substitué et contenant un hétérocycle, un 2H-benzopyranone, un benzamide, un benzophénone ou un phénoxyphényle possédant une activité d'antagoniste d'adrénorécepteur alpha 2 central. L'invention concerne en outre la préparation de ces composés, leur usage pharmaceutique et leurs compositions.

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