公开(公告)号：EP1486501A4

公开(公告)日：2006-03-22

申请号：EP03710430

申请日：2003-03-19

申请人： ASTELLAS PHARMA INC

发明人： ITAHANA HIROTSUNE ,  FUJIYASU JIRO ,  HAYASHIBE SATOSHI ,  WATANABE TOSHIHIRO ,  OKADA MASAMICHI ,  TOYA TAKASHI

IPC分类号： A61K31/429 ,  A61K31/5377 ,  A61P9/10 ,  A61P25/00 ,  A61P25/04 ,  A61P25/06 ,  A61P25/08 ,  A61P25/16 ,  A61P25/28 ,  A61P43/00 ,  C07D513/04

CPC分类号： A61K31/429 ,  A61K31/5377 ,  C07D513/04

摘要： A novel aminomethyl-substituted thiazolobenzimidazole derivative represented by the following general formula (I) or a salt thereof. The derivative or salt has metabotropic glutamate receptor activity, has excellent oral activity, and is useful as a medicine. (I) (In the formula, R1 represents oxygenic saturated heterocycle, etc.; Alk1 represents lower alkylene; m is 0 or 1; Alk2 represents lower alkylene optionally substituted by oxo; n is 0 or 1; X represents a bond, oxygen, sulfur, or NR5; R3 represents hydrogen, etc.; and R2, R4, R5, R6, and R7 are the same or different and each represents hydrogen, etc.; provided that when X is a bond and n is 1, then R3 represents neither lower alkyl nor lower halogenoalkyl, and when m is 1, R1 is OH or OMe, Alk1 is C1-3 alkylene, and either 1) X is a bond, n is 1, and R3 is hydrogen or 2) X is a bond, n is 0, and R3 is cyclohexane, then R4 represents a group other than Me.)

公开(公告)号：EP2042480A4

公开(公告)日：2011-11-23

申请号：EP07790834

申请日：2007-07-17

申请人： ASTELLAS PHARMA INC

发明人： HAYASHIBE SATOSHI ,  YAMASAKI SHINGO ,  WATANABE KAZUSHI ,  SHIRAISHI NOBUYUKI ,  SUZUKI DAISUKE ,  HOSHII HIROAKI ,  OHMORI JUNYA ,  KANAYAMA TAKATOSHI

IPC分类号： C07C211/42 ,  A61K31/13 ,  A61K31/381 ,  A61K31/404 ,  A61K31/435 ,  A61K31/4453 ,  A61P25/00 ,  A61P25/04 ,  A61P25/16 ,  A61P25/28 ,  A61P43/00 ,  C07C215/42 ,  C07C215/44 ,  C07C217/52 ,  C07C235/40 ,  C07C255/58 ,  C07D209/40 ,  C07D221/16 ,  C07D295/12 ,  C07D307/82 ,  C07D333/78

CPC分类号： C07C211/42 ,  C07C215/42 ,  C07C215/44 ,  C07C217/52 ,  C07C235/40 ,  C07C255/58 ,  C07C2602/08 ,  C07D209/40 ,  C07D221/16 ,  C07D295/12 ,  C07D307/82 ,  C07D333/78

公开(公告)号：EP2221296A4

公开(公告)日：2011-04-27

申请号：EP08853617

申请日：2008-11-26

申请人： ASTELLAS PHARMA INC

发明人： HAYASHIBE SATOSHI ,  YAMASAKI SHINGO ,  SHIRAISHI NOBUYUKI ,  HOSHII HIROAKI ,  TOBE TAKAHIKO

IPC分类号： C07D209/94 ,  A61K31/403 ,  A61K31/435 ,  A61K31/4365 ,  A61K31/538 ,  A61K31/55 ,  A61P9/10 ,  A61P25/04 ,  A61P25/06 ,  A61P25/16 ,  A61P25/18 ,  A61P25/24 ,  A61P25/28 ,  A61P25/36 ,  A61P43/00 ,  C07D221/16 ,  C07D223/32 ,  C07D265/34 ,  C07D491/048 ,  C07D495/04

CPC分类号： C07D209/94 ,  C07D221/16 ,  C07D223/32 ,  C07D265/34 ,  C07D333/78 ,  C07D401/06 ,  C07D401/12 ,  C07D491/048 ,  C07D495/04 ,  C07D498/04 ,  C07D513/04 ,  C07D513/06

公开(公告)号：EP1795524A4

公开(公告)日：2009-08-05

申请号：EP05785275

申请日：2005-09-20

申请人： ASTELLAS PHARMA INC

发明人： HAYASHIBE SATOSHI ,  KANAYAMA TAKATOSHI ,  OHMORI JUNYA ,  TOBE TAKAHIKO ,  MAENO KYOICHI ,  SHITAKA YOSHITSUGU ,  SUZUKI JOTAROU ,  KAWABATA SHIGEKI ,  SHIRAISHI NOBUYUKI ,  YAMASAKI SHINGO ,  SUZUKI DAISUKE ,  HOSHII HIROAKI

IPC分类号： C07C217/54 ,  A61K31/445 ,  A61P25/28 ,  C07D211/22

CPC分类号： C07C217/74 ,  C07C215/42 ,  C07C2601/08 ,  C07D211/22 ,  C07D295/088 ,  C07D307/94 ,  C07D319/14 ,  C07D401/06 ,  C07D405/04 ,  C07D409/04 ,  C07D409/10 ,  C07D413/04 ,  C07D453/02

摘要： A compound useful as an NMDA antagonist having a wide safety region which is a therapeutic agent for Alzheimer's disease, vascular dementia (vascular agnosia), Parkinson's disease, ischemic apoplexy, and pains or a preventive agent for these. The compound is an amine derivative or salt thereof characterized by comprising an amine-containing structure (A) and a di- or tricyclic fused ring (indane, tetralone, 4,5,6,7-tetrahydrobenzothiophene, 4,5,6,7-tetrahydrobenzofuran, 7,8-dihydro-6H-indeno[4,5-b]furan, 2,3-dihydro-1H-cyclopenta[a]naphthalene, etc.) bonded to the structure (A) through X1 (a bond, lower alkylene, etc.). The NMDA antagonist contains the derivative or salt as an active ingredient.

摘要翻译： 本发明提供作为具有广泛安全性的NMDA拮抗剂的化合物，可用作治疗剂或阿尔茨海默氏病，脑血管性痴呆，帕金森病，缺血性中风，疼痛等的预防剂。具体地提供了胺衍生物或其盐 其特征在于其中含胺结构A与2-或3-环稠合环结合（例如，茚满，四氢萘酮，4,5,6,7-四氢苯并噻吩，4,5,6,7-四氢苯并呋喃， 8-二氢-6H-茚并[4,5-b]呋喃，2,3-二氢-1H-环戊二烯并[1]萘）通过X 1（键或低级亚烷基）; 和含有它作为其活性成分的NMDA拮抗剂。