Novel benzylaminoethoxybenzene derivatives, production...

C - Chemistry – Metallurgy – 07 – C

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C07C 217/14 (2006.01) A61K 31/135 (2006.01) A61K 31/16 (2006.01) A61K 31/195 (2006.01) A61K 31/24 (2006.01) C07C 217/18 (2006.01) C07C 217/58 (2006.01) C07C 217/84 (2006.01) C07C 219/28 (2006.01) C07C 225/16 (2006.01) C07C 229/38 (2006.01) C07C 233/18 (2006.01) C07C 233/25 (2006.01)

Patent

CA 2160019

A novel benzylaminoethoxybenzene derivative represented by general formula (I), a salt thereof, or a solvate thereof; wherein R1 represents hydrogen, lower alkyl, lower hydroxyalkyl, lower alkoxyalkyl, aryl or benzyl; R2 represents hydrogen, lower alkyl, lower acyl, aryl or benzyl; R3 represents hydrogen, lower alkyl, lower alkoxyalkyl, lower dialkylaminoalkyl or lower acyl; and R4 represents hydrogen, halogen, lower alkoxy, amino, lower acylamino, hydroxy, lower acyloxy, lower acyl, carboxy or lower alkoxycarbonyl. An alpha-1 blocker prepared from this compound has a potent blocking effect and is reduced in the side effect of orthostatic hypotension.

Nouveau dérivé du benzylaminoéthoxybenzène de formule générale (I), l'un de ses sels ou l'un de ses solvates. Dans la formule (I), R?1¿ représente hydrogène, alkyle inférieur, hydroxyalkyle inférieur, alcoxyalkyle inférieur, aryle ou benzyle; R?2¿ représente hydrogène, alkyle inférieur, acyle inférieur, aryle ou benzyle; R?3¿ représente hydrogène, alkyle inférieur, alcoxyalkyle inférieur, dialkylaminoalkyle inférieur ou acyle inférieur; R?4¿ représente hydrogène, halogène, alcoxy inférieur, amino, acylamino inférieur, hydroxy, acyloxy inférieur, acyle inférieur, carboxy ou alcoxycarbonyle inférieur. Un bloqueur alpha-1 préparé à partir de ce composé présente un puissant effet de blocage et des effets secondaires, tels que l'hypotension orthostatique réduits.

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