Biphenyl derivatives and medicinal compositions

Details Biphenyl derivatives and medicinal compositions Biphenyl derivatives and medicinal compositions

C - Chemistry, Metallurgy

07

D

C07D 487/04 (2006.01) A61K 31/505 (2006.01) A61K 31/55 (2006.01) C07D 513/04 (2006.01)

Patent

CA 2285343

Biphenyl derivatives represented by general formula (1) and pharmacologically acceptable salts thereof wherein A represents a single bond, -CH2-, -CO-, -CS- or -SO2-; B represents a single bond or -CH2; R1 represents hydrogen, -OH, - NR11R12 (wherein R11 and R12 independently represent each hydrogen or C1-4 alkyl), -OCOCH3 or halogen and R2 represents hydrogen, or R1 and R2 may form together =O; and R3 represents hydrogen or C1-4 alkyl. In said formula, the absolute configuration at the position a may be any of R- and S- configurations. These compounds are highly excellent in safety and efficacy and useful, in particular, as vasopressin receptor antagonists.

L'invention concerne les dérivés de biphényle représentés par la formule générale (1) et leurs sels pharmaceutiquement acceptables. Dans ladite formule, A est une liaison unique, -CH¿2?-, -CO-, -CS- ou -SO¿2?-; B est une liaison unique ou -CH¿2?-; R?1¿ est hydrogène, -OH, -NR?11¿R?12¿ (R?11¿ et R?12¿ représentant indépendamment chacun hydrogène ou alkyle C¿1-4?), -OCOCH¿3? ou halogène, et R?2¿ est hydrogène, ou R?1¿ et R?2¿ peuvent former ensemble =O; et R?3¿ est hydrogène ou alkyle C¿1-4?. Dans cette formule, la configuration absolue en position a peut être l'une quelconque des configurations R- et S-. Les composés considérés sont très intéressants en termes de sécurité et d'efficacité, et ils sont utiles, en particulier, comme antagonistes de récepteur de vasopressine.

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