公开(公告)号：EP1961734B1

公开(公告)日：2011-09-14

申请号：EP06834759.0

申请日：2006-12-15

申请人： Mitsubishi Tanabe Pharma Corporation

发明人： KIUCHI, Masatoshi ,  MARUKAWA, Kaoru ,  KOBAYASHI, Nobutaka ,  SUGAHARA, Kunio

IPC分类号： C07C217/64 ,  C07C255/54 ,  C07C323/32 ,  C07C323/43 ,  C07F9/09 ,  C07F9/40 ,  C07F9/6527 ,  C07F9/653 ,  A61K31/137 ,  A61K31/165 ,  A61K31/222 ,  A61K31/277 ,  A61K31/325 ,  A61K31/351 ,  A61K31/357 ,  A61K31/661 ,  A61K31/675 ,  A61K31/695 ,  A61P37/06

CPC分类号： C07C235/34 ,  C07C217/64 ,  C07C235/78 ,  C07C255/54 ,  C07C271/16 ,  C07C323/32 ,  C07C323/43 ,  C07D319/06 ,  C07F7/1844 ,  C07F9/09 ,  C07F9/091 ,  C07F9/141 ,  C07F9/4056 ,  C07F9/6527 ,  C07F9/653

摘要： Disclosed is a novel amine compound represented by the general formula (I) below, a pharmaceutically acceptable acid addition salt of the compound, or a hydrate or solvate of the compound or the salt, which is excellent in an immunosuppressing effect, a rejection response-suppressing effect and the like and is reduced in adverse side effects such as bradycardia. Also disclosed is a pharmaceutical composition comprising the compound and a pharmaceutically acceptable carrier. (I) wherein R represents a hydrogen atom or P(=O)(OH)2; X represents an oxygen or sulfur atom; Y represents CH2CH2 or CH=CH; R1 represents an alkyl having 1-4 carbon atoms which is substituted by a halogen atom or a cyano; R2 represents an alky having 1-4 carbon atoms which may be substituted by a hydroxyl group or a halogen atom; R3 and R4 independently represent a hydrogen atom or an alkyl having 1-4 carbon atoms; and n represents 5-8.

公开(公告)号：EP1961734A1

公开(公告)日：2008-08-27

申请号：EP06834759.0

申请日：2006-12-15

申请人： Mitsubishi Tanabe Pharma Corporation

发明人： KIUCHI, Masatoshi ,  MARUKAWA, Kaoru ,  KOBAYASHI, Nobutaka ,  SUGAHARA, Kunio

IPC分类号： C07C217/64 ,  A61K31/137 ,  A61K31/165 ,  A61K31/222 ,  A61K31/277 ,  A61K31/325 ,  A61K31/351 ,  A61K31/357 ,  A61K31/661 ,  A61K31/675 ,  A61K31/695 ,  A61P3/10 ,  A61P11/06 ,  A61P13/12 ,  A61P17/00 ,  A61P17/06 ,  A61P19/00 ,  A61P19/02 ,  A61P25/00 ,  A61P27/16

CPC分类号： C07C235/34 ,  C07C217/64 ,  C07C235/78 ,  C07C255/54 ,  C07C271/16 ,  C07C323/32 ,  C07C323/43 ,  C07D319/06 ,  C07F7/1844 ,  C07F9/09 ,  C07F9/091 ,  C07F9/141 ,  C07F9/4056 ,  C07F9/6527 ,  C07F9/653

摘要： A novel amine compound represented by the following formula (I), which is superior in immunosuppressive action, rejection suppressive action and the like, and shows reduced side effects such as bradycardia and the like, or a pharmaceutically acceptable acid addition salt thereof, or hydrates thereof, or solvate, as well as a pharmaceutical composition containing this compound and a pharmaceutically acceptable carrier.

wherein R is a hydrogen atom or P(=O)(OH) 2 , X is an oxygen atom or a sulfur atom, Y is CH 2 CH 2 or CH=CH, R 1 is cyano or alkyl having a carbon number of 1 to 4 and substituted by a halogen atom(s), R 2 is alkyl having a carbon number of 1 to 4 and optionally substituted by a hydroxyl group(s) or a halogen atom(s), R 3 and R 4 may be the same or different and each is a hydrogen atom or alkyl having a carbon number of 1 to 4, and n is 5 - 8.

摘要翻译： 由下式（I）表示的新型胺化合物，其免疫抑制作用优异，排斥抑制作用等，并且显示减少的副作用，例如心动过缓等，或其药学上可接受的酸加成盐或水合物 或溶剂合物，以及含有该化合物和药学上可接受的载体的药物组合物。 其中R是氢原子或P（= O）（OH）2，X是氧原子或硫原子，Y是CH 2 CH 2或CH = CH，R 1是氰基或碳数为1的烷基 至4并且被卤素原子取代，R 2是碳数为1至4的烷基，并且任选被羟基或卤素原子取代，R 3和R 4可以是 相同或不同，各自为氢原子或碳数为1至4的烷基，n为5-8。