Tricyclic compounds

Details Tricyclic compounds Tricyclic compounds

C - Chemistry, Metallurgy

07

D

167/227, 260/270

C07D 453/02 (2006.01) A61K 31/47 (2006.01) C07D 451/04 (2006.01) C07D 451/14 (2006.01) C07D 453/06 (2006.01) C07D 471/06 (2006.01) C07D 471/08 (2006.01)

Patent

CA 2030718

The present invention is directed to new pharmaceutically active compounds of Formula I: Image in which the dashed line denotes an optional double bond; n is 1, 2 or 3; p is 0, 1, 2 or 3; q is 0, 1 or 2; each R1 is independently selected from halogen, hydroxy, lower alkoxy (optionally substituted with phenyl), lower alkyl, nitro, amino, amino carbonyl, (lower alkyl)amino, di(lower alkyl)amino, and (lower alkanoyl)amino; each R2 is lower alkyl; and R3 is selected from Image (a) Image (b) Image (c) Image (d) in which u, x, y and z are each independently an integer from 1 to 3; and R4 and R5 are independently C1-7 alkyl, C3-8 cycloalkyl, C3-8 cycloalkyl-C1-2 alkyl, or a group (CH2)tR6 where t is 1 or 2 and R6 is thienyl, pyrrolyl or furyl optionally further substituted by one or two substituents selected from C1-6 alkyl, C1-6 alkoxy, trifluoromethyl or halogen, or is phenyl optionally substituted by one or two substituents selected from C1-4 alkoxy, trifluoromethyl, halogen, nitro, carboxy, esterified carboxy, and C1-4 alkyl (optionally substituted by hydroxy, C1-4 alkoxy, carboxy, esterified carboxy or in vivo hydrolyzable acyloxy); or a pharmaceutically acceptable salt thereof or N-oxide derivative thereof, or an individual isomer or mixture of isomers thereof, as well as compositions containing them and their methods of use and production.

L'invention porte sur de nouveaux composés actifs en pharmacie, de formule I Image , où la ligne en pointillé représente une double liaison facultative; n est 1, 2 ou 3; p estApp# 0, 1, 2 ou 3; q estApp# 0, 1 ou 2; chaque R1 est choisi indépendamment parmi un halogène, hydroxy, alcoxy inf. (avec substitution facultative par un phényle), alkyle inf., nitro, amino, aminocarbonyle, (alkyle inf.)amino, di(alkyle inf.)amino et (alcanoyle inf.)amino; chaque R2 est un alkyle inf.; R3 est choisi parmi Image (a) Image (b) Image (c) Image (d), où u, x, y et z sont chacun indépendamment un entier de 1 à 3; R4 et R5 sont indépendamment un alkyle C1-7, cycloalkyle C3-8, cycloalkyle C3-8-alkyle C1-2, ou un groupe (CH2)tR6 où t est 1 ou 2 et R6 est un thiényle, pyrrolyle ou furyle avec substitution facultative par un ou deux substituants choisis parmi un alkyle C1-6, alcoxy C1-6, trifluorométhyle, halogène ou phényle avec substitution facultative par un ou deux substituants choisis parmi un halogène, alcoxy C1-4, trifluorométhyle, nitro, carboxy, carboxy estérifié et alkyle C1-4 (avec substitution facultative par un hydroxy, alcoxy C1-4, carboxy, carboxy estérifié ou acyloxy hydrolysable in vivo); ou sur leurs dérivés N-oxydés, leurs isomères individuels ou mélanges d'isomères et leurs sels acceptables en pharmacie; compositions qui en renferment; méthodes de production et d'utilisation.

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