公开(公告)号：EP0940387A4

公开(公告)日：2000-07-05

申请号：EP96935424

申请日：1996-10-24

申请人： MITSUBISHI TOKYO PHARM INC

发明人： TSUCHIYA SUSUMU ,  YASUDA NOBUYUKI ,  MATSUMOTO TOSHIFUMI ,  HIRATSUKA KOZO ,  IIZUKA HIROYUKI ,  HUKUZAKI ATSUSI ,  MATSUNAGA KOUICHI

IPC分类号： C07C215/42 ,  C07C217/74 ,  C07C219/24 ,  C07C235/36 ,  C07D235/08 ,  C07D295/185 ,  C07D317/46 ,  A61K31/135 ,  C07C49/255 ,  C07C49/753 ,  C07C211/40 ,  C07C213/02 ,  C07C213/04 ,  C07C213/08

CPC分类号： C07D295/185 ,  C07C215/42 ,  C07C217/74 ,  C07C219/24 ,  C07C235/36 ,  C07C2601/08 ,  C07C2601/14 ,  C07D235/08 ,  C07D317/46 ,  Y10S514/866 ,  Y10S514/909

摘要： Phenylethanolamine compounds represented by general formula (I) and pharmacologically acceptable salts thereof which have a potent effect of stimulating β3 adrenaline receptors and a high selectivity for β3 adrenaline receptors, wherein R1 represents hydrogen or halogeno; R2 represents hydrogen, hydroxy, lower alkoxy, lower alkoxy substituted by one or two lower alkoxycarbonyl or carboxy groups, lower alkoxy substituted by lower alkylaminocarbonyl optionally substituted by lower alkoxy, lower alkoxy substituted by cyclic C4-6 aminocarbonyl, lower alkoxycarbonyl, or carboxy; R3 represents hydrogen, hydroxy, lower alkoxy, or lower alkoxy substituted by one or two lower alkoxycarbonyl or carboxy groups, or R2 and R3 may be bonded to each other to thereby form methylenedioxy substituted by carboxy or lower alkoxycarbonyl; and m and n are each 0 or 1.

摘要翻译： 本发明涉及由通式AIU代表phenylethanolamines化合物：（其中R1 darstellt氢或卤素; R 2 darstellt氢，羟基，低级烷氧基，低级烷氧基substituiertem被一个或两个低级烷氧基羰基或羧基，低级烷氧基substituiertem与 低级烷基氨基羰该管道可与低级烷氧基，低级烷氧基substituiertem具有4至6个碳原子的环状氨基羰基，低级烷氧基羰或羧基; R 3 darstellt氢，羟基，低级烷氧基或低级烷氧基substituiertem被一个或两个低级烷氧基羰基或羧基; R2和R3可键合到彼此，以形成具有羧基或低级烷氧羰基亚甲二氧基substituiertem;和m和n是0或1），和它们的药理学上可接受的盐，它们具有有效的β3肾上腺素能刺激作用和高的β3肾上腺素能受体 选择性，以及其生产方法及其生产中间体的方法。