公开(公告)号：EP1445253B1

公开(公告)日：2009-08-05

申请号：EP02781759.2

申请日：2002-11-13

申请人： Astellas Pharma Inc.

发明人： KOSHIO, Hiroyuki ,  TSUKAMOTO, Issei ,  KURAMOCHI, Takahiro ,  AKAMATSU, Seijiro ,  SAITOH, Chikashi

IPC分类号： C07D223/16 ,  C07D401/12 ,  C07D401/14 ,  C07D403/10 ,  C07D403/12 ,  C07D403/14 ,  C07D409/14 ,  C07D417/14 ,  C07D401/06 ,  C07D403/06 ,  C07D405/14 ,  A61K31/55 ,  A61P7/12 ,  A61P13/00 ,  A61P43/00

CPC分类号： C07D223/16 ,  C07D401/12 ,  C07D401/14 ,  C07D403/10 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D417/14

摘要： 4,4-Difluoro-1,2,3,4-tetrahydro-5H-1-benzazepine derivatives represented by the general formula (I), which have excellent arginine vasopressin V2 activity and are useful in the treatment of central diabetes insipidus and/or night pollakisuria: (I) wherein R1 is -OH, -O-lower alkyl, or optionally substituted amino; R2 is lower alkyl which may be substituted with one or more halogen atoms, or halogeno; one of R3 and R4 is -H, lower alkyl, or halogeno, and the other is optionally substituted nonaromatic cyclic amino or optionally substituted aromatic cyclic amino; and R5 is -H, lower alkyl, or halogeno.

公开(公告)号：EP1955697B1

公开(公告)日：2012-05-02

申请号：EP06833666.8

申请日：2006-11-29

申请人： Astellas Pharma Inc.

发明人： KURAMOCHI, Takahiro ,  HIRABAYASHI, Ryoji ,  KOGANEMARU, Yohei ,  MUNAKATA, Ryosuke ,  YONEZAWA, Koichi ,  KISO, Tetsuo

IPC分类号： C07D215/38 ,  C07D401/12 ,  C07D405/12 ,  C07D413/12 ,  C07D265/36 ,  C07D209/34 ,  C07D277/62 ,  C07D279/16 ,  C07D277/64 ,  C07D405/14 ,  C07C237/40 ,  C07D417/12 ,  C07D235/26 ,  C07D319/18 ,  C07D321/10 ,  C07D403/12 ,  C07D453/02 ,  C07D217/02 ,  C07D401/14 ,  A61K31/4704 ,  A61P29/00

CPC分类号： C07D295/135 ,  A61K31/167 ,  C07C37/18 ,  C07C237/40 ,  C07C2601/14 ,  C07C2602/10 ,  C07D207/09 ,  C07D207/14 ,  C07D209/34 ,  C07D209/48 ,  C07D209/96 ,  C07D211/58 ,  C07D213/38 ,  C07D213/74 ,  C07D213/80 ,  C07D215/227 ,  C07D215/38 ,  C07D217/02 ,  C07D265/36 ,  C07D277/64 ,  C07D279/16 ,  C07D295/13 ,  C07D295/185 ,  C07D307/14 ,  C07D307/22 ,  C07D309/14 ,  C07D319/12 ,  C07D319/18 ,  C07D321/10 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D413/04 ,  C07D413/12 ,  C07D417/12 ,  C07D453/02 ,  C07C39/27

摘要： Disclosed is a novel and excellent therapeutic or prophylactic agent for nociceptive pain, neuropathic pain, cancer pain, headache, bladder dysfunction or the like, which relies on a preventive activity on capsaicin receptor VR1 activation. It is found that a benzamide derivative having a benzene ring fused with a monocyclic ring on a nitrogen atom in the amide group and an amino group substituted by a lower alkylamino or cyclic group at a position adjacent to the amide group has a potent preventive activity on VR1 activation and an excellent pharmacological activity relying on the preventive activity, and therefore the derivative can be used as a good therapeutic or prophylactic agent for a VR1-related disease, such as nociceptive pain, neuropathic pain, cancer pain, headache and bladder dysfunction.

公开(公告)号：EP1632477B1

公开(公告)日：2017-03-01

申请号：EP04736576.2

申请日：2004-06-10

申请人： Astellas Pharma Inc.

发明人： KURAMOCHI, Takahiro ,  ASAI, Norio ,  IKEGAI, Kazuhiro ,  AKAMATSU, Seijiro ,  HARADA, Hironori ,  ISHIKAWA, Noriko ,  SHIRAKAMI, Shohei ,  MIYAMOTO, Satoshi ,  WATANABE, Toshihiro ,  KISO, Tetsuo

IPC分类号： A61K31/33

CPC分类号： C07C237/40 ,  A61K31/167 ,  A61K31/428 ,  A61K31/4453 ,  A61K31/454 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/55 ,  C07D209/08 ,  C07D209/34 ,  C07D213/75 ,  C07D215/38 ,  C07D217/04 ,  C07D223/16 ,  C07D231/56 ,  C07D235/06 ,  C07D241/42 ,  C07D249/18 ,  C07D263/58 ,  C07D265/36 ,  C07D277/64 ,  C07D277/82 ,  C07D279/16 ,  C07D295/155 ,  C07D307/79 ,  C07D317/66 ,  C07D333/54 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04

公开(公告)号：EP1955697A1

公开(公告)日：2008-08-13

申请号：EP06833666.8

申请日：2006-11-29

申请人： Astellas Pharma Inc.

发明人： KURAMOCHI, Takahiro ,  HIRABAYASHI, Ryoji ,  KOGANEMARU, Yohei ,  MUNAKATA, Ryosuke ,  YONEZAWA, Koichi ,  KISO, Tetsuo

IPC分类号： A61K31/167

CPC分类号： C07D295/135 ,  A61K31/167 ,  C07C37/18 ,  C07C237/40 ,  C07C2601/14 ,  C07C2602/10 ,  C07D207/09 ,  C07D207/14 ,  C07D209/34 ,  C07D209/48 ,  C07D209/96 ,  C07D211/58 ,  C07D213/38 ,  C07D213/74 ,  C07D213/80 ,  C07D215/227 ,  C07D215/38 ,  C07D217/02 ,  C07D265/36 ,  C07D277/64 ,  C07D279/16 ,  C07D295/13 ,  C07D295/185 ,  C07D307/14 ,  C07D307/22 ,  C07D309/14 ,  C07D319/12 ,  C07D319/18 ,  C07D321/10 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D413/04 ,  C07D413/12 ,  C07D417/12 ,  C07D453/02 ,  C07C39/27

摘要： To provide a novel and excellent agent for treating or preventing nociceptive pain, neuropathic pain, cancer pain, headache, bladder function disorder and the like, based on the inhibitory action on the capsaicin receptor VR1 activation.
The present invention was accomplished by confirming that a benzamide derivative characterized by the possession of a benzene ring in which a single ring is condensed on the nitrogen atom of amido group and possession of a lower alkylamino or an amino group substituted with a ring group at the neighboring position of said amido group has a strong inhibitory action on VR1 activation and excellent pharmacological actions based on this and by finding that it can become an excellent agent for treating or preventing VR1-involved diseases such as nociceptive pain, neuropathic pain, cancer pain, headache, bladder function disorder and the like.

摘要翻译： 为了用于治疗或预防伤害性疼痛，神经性疼痛，癌性疼痛，头痛，膀胱功能障碍等的基础上，对辣椒素受体VR1活化抑制作用提供一种新颖和优良剂。 本发明什么通过确认完成做由一个苯环的占有，其中单个环在上酰氨基和拥有一个低级烷基氨基的或氨基substituiertem具有环基团的氮原子稠合为特征的苯甲酰胺衍生物 说酰氨基的相邻位置具有基于这一点，并通过寻找并它可以成为优良的药剂用于治疗或预防VR1参与的疾病上VR1活化和优异的药理作用很强的抑制作用：如伤害性疼痛，神经性疼痛，癌症疼痛， 头痛，膀胱功能障碍等。