公开(公告)号：EP3006443A4

公开(公告)日：2016-12-21

申请号：EP14807340

申请日：2014-06-06

申请人： ASTELLAS PHARMA INC

发明人： ISHIHARA TSUKASA ,  IKEGAI KAZUHIRO ,  KURIWAKI IKUMI ,  HISAMICHI HIROYUKI ,  TAKESHITA NOBUAKI ,  TAKEZAWA RYUICHI

IPC分类号： C07D409/10 ,  A61K31/4025 ,  A61K31/4535 ,  A61K31/5377 ,  A61K31/551 ,  A61P19/02 ,  A61P21/00 ,  A61P25/04 ,  A61P29/00 ,  A61P43/00 ,  C07D413/10

CPC分类号： A61K31/5377 ,  A61K31/4025 ,  A61K31/4535 ,  A61K31/551 ,  C07D409/10 ,  C07D413/10

摘要： [Problem] A compound which is useful as an IK1 channel activator is provided. [Means for Solution] As a result of studies on the IK1 channel activator, the present inventors have found that a benzothiophene compound shows effectiveness on visceral pain, inflammatory pain, osteoarthritis pain, neuropathic pain, or fibromyalgia, thereby completing the invention. A compound of the invention has an IK1 channel activation effect, and can also be used as an agent for preventing and/or treating visceral pain, inflammatory pain, osteoarthritis pain, neuropathic pain, or fibromyalgia. In addition, the IK1 channel activator can be used as an agent for preventing and/or treating inflammatory pain, osteoarthritis pain, neuropathic pain, and fibromyalgia.

公开(公告)号：EP1864976A4

公开(公告)日：2008-05-07

申请号：EP06730589

申请日：2006-03-30

申请人： ASTELLAS PHARMA INC

发明人： MATSUMOTO SHUNICHIRO ,  KINOYAMA ISAO ,  OSODA KAZUHIKO ,  YAMAMOTO HIROFUMI ,  HIRANO MASAAKI ,  OHNUKI KEI ,  KAWAMINAMI EIJI ,  SHIN TAKASHI ,  TAKAHASHI TATSUHISA ,  KUSAYAMA TOSHIYUKI ,  HISAMICHI HIROYUKI ,  SHIMADA ITSURO ,  KOIKE TAKANORI

IPC分类号： C07D235/12 ,  A61K31/4184 ,  A61K31/4192 ,  A61K31/4196 ,  A61P13/08 ,  A61P35/00 ,  C07D403/06 ,  C07D409/14 ,  C07D413/10

CPC分类号： C07D235/12 ,  C07D401/06 ,  C07D401/12 ,  C07D403/06 ,  C07D403/12 ,  C07D405/06 ,  C07D405/12 ,  C07D409/06 ,  C07D409/12 ,  C07D409/14 ,  C07D413/06 ,  C07D413/10 ,  C07D413/12 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14

摘要： It is intended to provide a compound useful as a GnRH receptor antagonist. The inventors further investigated proane-1,3-dion derivatives and, as a result, they confirmed that a compound having a benzene ring or a thiophene ring substituted with a group represented by -SO2-R3 in a propane-1,3-dion derivative having 2-(1,3-dihydro-2H-benzimidazole-2-ylidene) has an excellent GnRH receptor antagonism and completed the invention. Because the compound of the invention has a potent GnRH receptor antagonism, it is useful for the treatment of sex hormone-dependent diseases, particularly GnRH-related diseases. Further, because the compound of the invention has an excellent metabolic stability in human and few drug interactions, it has preferable characteristics as a pharmaceutical used for the diseases.

公开(公告)号：EP2821402A4

公开(公告)日：2015-08-19

申请号：EP13754501

申请日：2013-02-26

申请人： ASTELLAS PHARMA INC ,  KOTOBUKI PHARMACEUTICAL CO LTD

发明人： KAMEDA MINORU ,  KURIWAKI IKUMI ,  IIKUBO KAZUHIKO ,  HISAMICHI HIROYUKI ,  KAWAMOTO YUICHIRO ,  MORITOMO HIROYUKI ,  SUZUKI TOMOYUKI ,  FUTAMI TAKASHI ,  SUZUKI ATSUSHI ,  TSUNOYAMA KAZUHISA ,  ASAUMI MAKOTO ,  TOMIYAMA HIROSHI ,  NODA ATSUSHI ,  IWAI YOSHINORI ,  TOKUZAKI KAZUO ,  OKADA HARUKI ,  MIYASAKA KOZO

IPC分类号： C07D239/42 ,  A61K31/4545 ,  A61K31/506 ,  A61P35/00 ,  A61P43/00 ,  C07D239/47 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/14 ,  C07D413/12 ,  C07D471/10 ,  C07D487/20

CPC分类号： C07D239/47 ,  C07D239/42 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D451/02 ,  C07D451/04 ,  C07D453/02 ,  C07D471/08 ,  C07D471/10 ,  C07D487/10 ,  C07D491/107

摘要： Provided is a compound useful as a prophylactic and/or therapeutic agent for bladder cancer. As a result of studies on compounds having FGFR inhibitory action, the present inventors have found that the nitrogen-containing aromatic heterocyclic compounds of the present invention have inhibitory action on FGFR1, FGFR2, and/or FGFR3, particularly, mutant FGFR3, and thus, the present invention has been accomplished. The nitrogen-containing aromatic heterocyclic compound of the present invention can be used as a therapeutic agent for various cancers related to FGFR1, FGFR2, and/or FGFR3, such as lung cancer and hormone therapy-resistant breast cancer, stomach cancer, triple negative breast cancer, endometrial cancer, bladder cancer, and glioblastoma, particularly as a prophylactic and/or therapeutic agent for mutant FGFR3-positive bladder cancer.

公开(公告)号：EP2149561A4

公开(公告)日：2011-09-07

申请号：EP08764654

申请日：2008-05-26

申请人： ASTELLAS PHARMA INC

发明人： HISAMICHI HIROYUKI ,  SHIMADA ITSURO ,  ISHIHARA TSUKASA ,  TAKUWA TOMOFUMI ,  SHIMIZU TAKAFUMI ,  ISHIKAWA NORIKO ,  MAENO KYOICHI ,  SEKI NORIO

IPC分类号： C07D217/26 ,  A61K31/472 ,  A61K31/496 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  A61K31/53 ,  A61K31/5377 ,  A61K31/695 ,  A61P1/00 ,  A61P35/00 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D405/04 ,  C07D405/06 ,  C07D405/14 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12

CPC分类号： A61K31/4725 ,  A61K31/435 ,  A61K31/439 ,  A61K31/445 ,  A61K31/472 ,  A61K31/496 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/695 ,  C07D217/26 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D405/04 ,  C07D405/06 ,  C07D405/14 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D453/02 ,  C07D471/04

摘要： [Problems] To provide a pharmaceutical, in particular a compound which can be used as a therapeutic agent for irritable bowel syndrome (IBS). [Means for Solving Problems] It was found that a tetrahydroisoquinolin-1-one derivative having an amide group at the 4-position or a pharmaceutically acceptable salt thereof has an excellent bombesin 2 (BB2) receptor antagonistic action. It is also found that the tetrahydroisoquinolin-1-one derivative is highly effective on bowel movement disorders. From the above, the tetrahydroisoquinolin-1-one derivative of the present invention is useful as a therapeutic agent for diseases associated with a BB2 receptor, in particular IBS.