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1.发明公开
公开(公告)号：EP2149561A1
公开(公告)日：2010-02-03
申请号：EP08764654.3
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.摘要翻译： [问题]提供药物，特别是可用作肠易激综合征（IBS）治疗剂的化合物。 解决问题的手段发现在4-位具有酰胺基的四氢异喹啉-1-酮衍生物或其药学上可接受的盐具有优异的铃蟾肽2（BB2）受体拮抗作用。 还发现四氢异喹啉-1-酮衍生物对肠运动障碍高度有效。 从上述可以看出，本发明的四氢异喹啉-1-酮衍生物可用作与BB2受体，特别是IBS相关疾病的治疗剂。
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公开(公告)号：EP3059239B1
公开(公告)日：2018-06-27
申请号：EP14853825.9
申请日：2014-10-17
申请人： Astellas Pharma Inc.
发明人： SHIRAISHI, Nobuyuki , HOSHII, Hiroaki , HAMAGUCHI, Wataru , HONJO, Eriko , TAKUWA, Tomofumi , KONDO, Yuji , GOTO, Takayuki
IPC分类号： C07D495/04 , A61K31/519 , A61K31/5377 , A61K31/541 , A61K31/554 , A61P25/00 , A61P25/18 , A61P25/22 , A61P43/00 , C07D519/00
CPC分类号： A61K31/519 , A61K31/5355 , A61K31/541 , A61K31/554 , C07D495/04 , C07D495/08 , C07D495/10 , C07D513/04 , C07D519/00
摘要： [Problem] Provided is a compound which is useful as a pharmaceutical composition for preventing and/or treating schizophrenia, cognitive impairment associated with schizophrenia (CIAS), cognitive impairment, fragile X syndrome, autism spectrum disorder, spasticity, anxiety disorder, substance addiction, pain, fibromyalgia, Charcot-Marie-Tooth disease, or the like. [Means for Solution] The present inventors have studied that a pharmaceutical composition for preventing and/or treating schizophrenia, cognitive impairment associated with schizophrenia (CIAS), cognitive impairment, fragile X syndrome, autism spectrum disorder, spasticity, anxiety disorder, substance addiction, pain, fibromyalgia, Charcot-Marie-Tooth disease, or the like, which has a positive allosteric modulator (PAM action) of GABA B , and have found that a sulfur-containing bicyclic compound is a PAM of a GABA B receptor, thereby completing the present invention. The sulfur-containing bicyclic compound of the present invention has a PAM action of GABA B , and can be used as an agent for preventing and/or treating schizophrenia, CIAS, cognitive impairment, fragile X syndrome, autism spectrum disorder, spasticity, anxiety disorder, substance addiction, pain, fibromyalgia, or Charcot-Marie-Tooth disease.
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公开(公告)号：EP2261206A1
公开(公告)日：2010-12-15
申请号：EP09729006.8
申请日：2009-03-30
申请人： Astellas Pharma Inc.
IPC分类号： C07D209/34 , A61K31/4045 , A61K31/405 , A61K31/4178 , A61K31/427 , A61K31/4439 , A61K31/5377 , A61P1/04 , A61P1/14 , C07D401/06 , C07D403/06 , C07D405/06 , C07D417/06
CPC分类号： C07D209/34 , C07D209/38 , C07D401/06 , C07D403/06 , C07D405/06 , C07D417/06
摘要： [Problems] A compound, which is useful as an active ingredient for a pharmaceutical composition, for example a pharmaceutical composition for treating constipation-type irritable bowel syndrome, atonic constipation and/or functional gastrointestinal disorder, is provided.
[Means for Solution] The present inventors have extensively studied compounds having TRPA1 channel activation activity, and confirmed that an indolinone compound has a TRPA1 channel activation activity, and thus completed the present invention. The indolinone compound of the present invention has a TRPA1 channel activation activity and can be used as an active ingredient of a pharmaceutical composition for preventing and/or treating constipation-type irritable bowel syndrome, atonic constipation and/or functional gastrointestinal disorder or the like.摘要翻译： [问题]提供了可用作药物组合物的活性成分的化合物，例如用于治疗便秘型肠易激综合征，非便秘便秘和/或功能性胃肠病症的药物组合物。 [解决方案]本发明人广泛研究了具有TRPA1通道活化活性的化合物，并证实了吲哚啉酮化合物具有TRPA1通道活化活性，从而完成了本发明。 本发明的吲哚满酮化合物具有TRPA1通道活化活性，可以用作预防和/或治疗便秘型肠易激综合征，急性便秘和/或功能性胃肠病等的药物组合物的活性成分。
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公开(公告)号：EP3059239A1
公开(公告)日：2016-08-24
申请号：EP14853825.9
申请日：2014-10-17
申请人： Astellas Pharma Inc.
发明人： SHIRAISHI, Nobuyuki , HOSHII, Hiroaki , HAMAGUCHI, Wataru , HONJO, Eriko , TAKUWA, Tomofumi , KONDO, Yuji , GOTO, Takayuki
IPC分类号： C07D495/04 , A61K31/519 , A61K31/5377 , A61K31/541 , A61K31/554 , A61P25/00 , A61P25/18 , A61P25/22 , A61P43/00 , C07D519/00
CPC分类号： A61K31/519 , A61K31/5355 , A61K31/541 , A61K31/554 , C07D495/04 , C07D495/08 , C07D495/10 , C07D513/04 , C07D519/00
摘要： [Problem] Provided is a compound which is useful as a pharmaceutical composition for preventing and/or treating schizophrenia, cognitive impairment associated with schizophrenia (CIAS), cognitive impairment, fragile X syndrome, autism spectrum disorder, spasticity, anxiety disorder, substance addiction, pain, fibromyalgia, Charcot-Marie-Tooth disease, or the like.
[Means for Solution] The present inventors have studied that a pharmaceutical composition for preventing and/or treating schizophrenia, cognitive impairment associated with schizophrenia (CIAS), cognitive impairment, fragile X syndrome, autism spectrum disorder, spasticity, anxiety disorder, substance addiction, pain, fibromyalgia, Charcot-Marie-Tooth disease, or the like, which has a positive allosteric modulator (PAM action) of GABA B , and have found that a sulfur-containing bicyclic compound is a PAM of a GABA B receptor, thereby completing the present invention. The sulfur-containing bicyclic compound of the present invention has a PAM action of GABA B , and can be used as an agent for preventing and/or treating schizophrenia, CIAS, cognitive impairment, fragile X syndrome, autism spectrum disorder, spasticity, anxiety disorder, substance addiction, pain, fibromyalgia, or Charcot-Marie-Tooth disease.
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