Amino alcohol derivative, medicinal composition containing...

C - Chemistry – Metallurgy – 07 – C

Patent

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C07C 233/43 (2006.01) A61K 31/18 (2006.01) A61K 31/192 (2006.01) A61K 31/216 (2006.01) A61K 31/235 (2006.01) A61K 31/36 (2006.01) A61K 31/4184 (2006.01) A61P 1/14 (2006.01) A61P 1/16 (2006.01) A61P 3/04 (2006.01) A61P 3/06 (2006.01) A61P 3/10 (2006.01) A61P 13/02 (2006.01) A61P 25/24 (2006.01) A61P 43/00 (2006.01) C07C 311/08 (2006.01) C07D 235/24 (2006.01)

Patent

CA 2541894

A compound having potent irritative activity against a human .beta.3- adrenergic receptor and high selectivity therefor and represented by the general formula (I) (wherein R1 is hydrogen or lower alkyl; R2 and R3 each independently is hydrogen or lower alkyl; R4, R5, and R6 each independently is hydrogen, halogeno, lower alkyl, or lower alkoxy; R7 is hydrogen or lower alkyl; R8 is hydrogen, halogeno, lower alkyl, lower alkoxy, etc.; R9 is - COR10, -A1-COR10, -O-A2-COR10, etc.; Ar is optionally substituted phenyl or heteroaryl; and A is a bond, -OCH2, etc.), a prodrug of the compound, or a pharmacologically acceptable salt of either.

L'invention concerne un composé présentant une puissante activité stimulante vis-à-vis du récepteur .beta.¿3?-adrénergique humain et une sélectivité élevée pour ce dernier, ledit composé étant représenté par la formule générale (I), (dans laquelle R?1¿ représente hydrogène ou alkyle inférieur; R?2¿ et R?3¿ représentent indépendamment l'un de l'autre hydrogène ou alkyle inférieur; R?4¿, R?5¿ et R?6¿ représentent indépendamment l'un de l'autre hydrogène, halogéno, alkyle inférieur, ou alcoxy inférieur; R?7¿ représente hydrogène ou alkyle inférieur; R?8¿ représente hydrogène, halogéno, alkyle inférieur, alcoxy inférieur, etc.; R?9¿ représente -COR?10¿, -A?1¿-COR?10¿, -O-A?2¿-COR?10¿, etc.; Ar représente phényle ou hétéroaryle éventuellement substitués; et A représente une liaison, -OCH¿2?, etc.). L'invention concerne également un promédicament dudit composé ou un sel pharmacologiquement acceptable dudit composé ou dudit promédicament.

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