公开(公告)号：EP1000935A4

公开(公告)日：2001-03-21

申请号：EP98933924

申请日：1998-07-24

申请人： TSUMURA & CO

发明人： HASEGAWA YOSHIHIRO ,  SHINDOU SHOUICHIROU ,  HATTORI TOMOHISA ,  YAMAZAKI YOUSUKE ,  OBATA TATSUHIRO ,  HORIUCHI FUMIKO ,  HAYAKAWA HIROYUKI ,  KUMAZAWA HIROAKI

IPC分类号： C07D213/56 ,  C07D213/57 ,  A61K31/44 ,  A61K31/535 ,  C07D213/59 ,  C07D213/61 ,  C07D213/65 ,  C07D213/80 ,  C07D405/12

CPC分类号： C07D213/56

摘要： Compounds represented by general formula (I), and nephritis remedies and TGF-β inhibitors containing the same, wherein Ar1 is (substituted) pyridyl; Ar2 is (substituted) phenyl; R1 is H, alkyl or aryl; R2 is H, alkyl, cyano or alkoxycarbonyl; R3 is H or (substituted) alkyl; X is O or S; A and B are each H, OH, alkoxy or alkylthio, or alternatively they together form oxo, thioxo, =N-Y (wherein Y is dialkylamino, OH, aralkyloxy or alkoxy) or -Z1-M-Z2- (wherein Z?1 and Z2¿ are each O, S or optionally alkyl-substituted imino; and M is alkylene or phenylene), or B may be 1-alkylimidazol-2-yl with A being OH; and n is an integer of 1 to 3.

公开(公告)号：EP1142875A4

公开(公告)日：2003-03-26

申请号：EP00900175

申请日：2000-01-11

申请人： TSUMURA & CO

发明人： HASEGAWA YOSHIHIRO ,  SHINDOU SHOUICHIROU ,  HATTORI TOMOHISA ,  OBATA TATSUHIRO ,  HORIUCHI FUMIKO ,  HAYAKAWA HIROYUKI ,  KUMAZAWA HIROAKI

IPC分类号： A61P9/00 ,  A61P11/00 ,  A61P13/12 ,  A61P37/02 ,  C07D213/40 ,  A61K31/44 ,  A61K31/4406

CPC分类号： C07D213/40

摘要： Cinnamamide derivatives represented by general formula (I); and immunomodulators and preventive and therapeutic agents for nephrotic syndrome, circulatory disturbance and respiratory diseases, containing the same, wherein R1 is hydroxyl, C¿1?-C6 alkoxy, arylalkoxy or (substituted) amino; R?2 and R3¿ are each halogeno or C¿1?-C4 alkyl; R?4¿ is hydrogen or C¿1?-C6 alkyl; R?5¿ is hydrogen, C¿1?-C6 alkyl or aryl; R?6¿ is hydrogen, C¿1?-C6 alkyl, cyano or C1-C6 alkoxycarbonyl; W is O, S, imino, methylene, hydroxymethylene or carbonyl; X and Y are each O or S; m is an integer of 0 to 2; and n is an integer of 1 to 3, or alternatively the -C(R?2)(R3¿)-W- group may be vinylene when m is 0.

摘要翻译： 本发明涉及具有下式（I）的肉桂酰胺衍生物：其中R 1表示羟基，C 1-6 - 烷氧基，芳基烷氧基或取代或未取代的氨基的 R 2和R 3相同或不同，各自表示氢原子，卤素原子或C 1-4 - 烷基; R 4表示氢原子或C 1-6 - 烷基; R 5表示氢原子，C 1-6 - 烷基或芳基; R 6表示氢原子，C 1-6 - 烷基，氰基或C 1-6 - 烷氧基 - 羰基; W表示氧原子，硫原子，亚氨基，亚甲基，羟基亚甲基或羰基; X和Y相同或不同，各自表示氧原子或硫原子; m表示0〜2的整数， n表示1〜3的整数， 当m为0时，基团-C（R 2）（R 3）-W-可以表示亚乙烯基; 或其药学上可接受的盐; 以及含有上述化合物，特别是免疫调节剂，肾病综合征，循环障碍或呼吸系统疾病的预防或治疗剂的药物组合物。