公开(公告)号：EP2241567A1

公开(公告)日：2010-10-20

申请号：EP09710649.6

申请日：2009-02-09

申请人： Eisai R&D Management Co., Ltd.

发明人： OZAKI, Fumihiro ,  SOEJIMA, Motohiro ,  ISHIDA, Tasuku ,  NORIMINE, Yoshihiko ,  KURUSU, Nobuyuki ,  DOI, Eriko ,  KANEKO, Toshihiko ,  HASEGAWA, Daiju ,  KOBAYASHI, Kiyoaki ,  YAMAMOTO, Noboru

IPC分类号： C07D451/06 ,  A61K31/439 ,  A61K31/46 ,  A61K31/4985 ,  A61K31/53 ,  A61K31/5377 ,  A61K31/5383 ,  A61K31/55 ,  A61P3/12 ,  A61P15/00 ,  A61P25/00 ,  A61P25/04 ,  A61P25/08 ,  A61P25/20 ,  A61P29/02 ,  A61P43/00 ,  C07D451/14 ,  C07D519/00

CPC分类号： C07D451/06 ,  C07D451/02 ,  C07D451/04 ,  C07D519/00

摘要： Compounds represented by formula (I) and pharmaceutically acceptable salts thereof have excellent sodium channel inhibitory action and are useful as therapeutic agents and analgesics for various kinds of neuralgia, neuropathy, epilepsy, insomnia, premature ejaculation and the like.

wherein Q represents ethylene, etc., R 1 , R 2 and R 3 represent hydrogen, etc., X 1 represents C 1-6 alkylene, etc., X 2 represents C 1-6 alkylene, etc., A 1 represents a 5- to 6-membered heterocyclic group, etc., and A 2 represents C 6-14 aryl, etc.

摘要翻译： 由式（I）表示的化合物及其药学上可接受的盐具有优异的钠通道抑制作用，可用作各种神经痛，神经病，癫痫，失眠，早泄等的治疗剂和止痛剂。 其中Q表示乙烯等，R 1，R 2和R 3表示氢等，X 1表示C 1-6亚烷基等，X 2表示C 1-6亚烷基等，A 1表示 5-至6-元杂环基等，A 2表示C 6-14芳基等

公开(公告)号：EP1254895B1

公开(公告)日：2007-05-23

申请号：EP01901413.3

申请日：2001-01-18

申请人： Eisai R&D Management Co., Ltd.

发明人： YAMAMOTO, Noboru ,  SUZUKI, Yuichi ,  KIMURA, Manami ,  NIIDOME, Tetsuhiro ,  IIMURA, Yoichi ,  TERAMOTO, Tetsuyuki ,  KANEDA, Yoshihisa ,  KANEKO, Toshihiko ,  KURUSU, Nobuyuki ,  SHINMYO, Daisuke ,  YOSHIKAWA, Yukie ,  HATAKEYAMA, Shinji

IPC分类号： C07D333/26 ,  A61K31/495 ,  A61K31/381 ,  A61P9/10

CPC分类号： C07D207/337 ,  C07D207/09 ,  C07D207/14 ,  C07D207/16 ,  C07D209/14 ,  C07D209/42 ,  C07D211/22 ,  C07D211/26 ,  C07D211/32 ,  C07D211/34 ,  C07D211/46 ,  C07D211/58 ,  C07D211/64 ,  C07D213/36 ,  C07D213/57 ,  C07D213/74 ,  C07D215/06 ,  C07D215/12 ,  C07D215/227 ,  C07D215/38 ,  C07D217/04 ,  C07D217/22 ,  C07D235/14 ,  C07D235/30 ,  C07D241/04 ,  C07D243/08 ,  C07D261/08 ,  C07D263/20 ,  C07D263/32 ,  C07D263/58 ,  C07D271/06 ,  C07D277/28 ,  C07D277/42 ,  C07D277/82 ,  C07D295/145 ,  C07D295/185 ,  C07D295/192 ,  C07D295/215 ,  C07D307/52 ,  C07D307/54 ,  C07D307/81 ,  C07D319/20 ,  C07D333/24 ,  C07D333/28 ,  C07D333/38 ,  C07D333/60 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D403/04 ,  C07D405/06 ,  C07D409/06 ,  C07D409/12 ,  C07D409/14 ,  C07D413/04 ,  C07D413/12 ,  C07D413/14 ,  C07D417/04 ,  C07D417/12 ,  C07D471/10 ,  C07D487/08

摘要： Novel compounds exhibiting excellent calcium antagonism, particularly neuroselective calcium antagonism, namely, compounds of the general formula (I), salts of the same, or hydrates of both wherein Ar is a group derived from an optionally substituted 5- to 14-membered aromatic ring, or the like; the ring A is one member selected from among piperazine, homopiperazine, piperidine and so on; the ring B is an optionally substituted C3-14 hydrocarbon ring or the like; E is a single bond, -CO-, or the like; X is a single bond, oxygen, or the like; R1 is hydrogen, halogeno, hydroxyl, or the like; and D?1, D2, W1 and W2¿ are each independently a single bond or optionally substituted C¿1-6? alkylene.

公开(公告)号：EP1375496B1

公开(公告)日：2007-07-04

申请号：EP02707189.3

申请日：2002-03-27

申请人： Eisai R&D Management Co., Ltd.

发明人： OKADA, Toshimi ,  KURUSU, Nobuyuki ,  TANAKA, Keigo ,  YOSHIKAWA, Seiji ,  SHINMYO, Daisuke ,  WATANABE, Nobuhisa ,  IKUTA, Hironori ,  HIYOSHI, Hironobu ,  SAEKI, Takao ,  YANAGIMACHI, Mamoru ,  ITO, Masashi

IPC分类号： C07D401/04 ,  C07D401/14 ,  C07D451/14 ,  C07D453/02 ,  C07D491/113 ,  A61K31/435 ,  A61K31/439

CPC分类号： C07D401/04 ,  A61K31/435 ,  A61K31/439 ,  A61K31/4545 ,  C07D401/14 ,  C07D453/04 ,  C07D491/10

摘要： A compound having excellent squalene synthetase inhibitory activity. It is a compound (I) represented by the following general formula, a salt thereof, or a hydrate of either. (I) In the formula, R1 means optionally substituted vinyl or an optionally substituted aromatic ring; n is an integer of 0 to 2; X, Y, and Z are the same or different and each means optionally substituted carbon, nitrogen, etc.; CyA means an optionally substituted 5- to 14-membered nonaromatic cyclic amino group optionally containing oxygen or sulfur; W means -C=C-, etc.; and A means a group of the formula (II) (wherein R8 represents hydrogen, hydroxy, etc.; B2 represents optionally substituted carbon or nitrogen; and c is 0 or 1), etc.