公开(公告)号：EP3095781B1

公开(公告)日：2018-10-03

申请号：EP15737185.7

申请日：2015-01-13

申请人： Astellas Pharma Inc.

发明人： MATSUMOTO, Shunichiro ,  SHIMIZU, Takafumi ,  SAITO, Tomoyuki ,  KANAYAMA, Takatoshi ,  TANAKA, Hiroaki ,  MORI, Chiharu ,  YOKOYAMA, Kazuhiro ,  MATSUI, Shigeo

IPC分类号： C07D209/16 ,  A61K31/4045 ,  A61K31/4155 ,  A61K31/422 ,  A61K31/427 ,  A61K31/454 ,  A61K31/497 ,  A61K31/506 ,  A61P13/10 ,  A61P43/00 ,  C07D401/12 ,  C07D403/12 ,  C07D417/12

CPC分类号： C07D209/16 ,  C07D401/12 ,  C07D403/12 ,  C07D413/12 ,  C07D417/12

摘要： [Problem] To provide a compound useful as a MT 1 and/or MT 2 receptor agonist. [Solution] The present inventors have studied on MT 1 and/or MT 2 receptor agonists, and have confirmed that indole compounds have the activity. As a result, the present invention is accomplished. That is, a compound represented by formula (I) or a salt thereof according to the present invention has a MT 1 and/or MT 2 receptor agonistic activity and has a low ability of migrating into the central nervous system. Therefore, the compound or a salt thereof can be used as a peripheral MT 1 and/or MT 2 receptor agonist, and therefore can be used as a therapeutic and/or prophylactic agent for urinary incontinence, particularly stress urinary incontinence and mixed urinary incontinence.

公开(公告)号：EP2546255A1

公开(公告)日：2013-01-16

申请号：EP11753475.0

申请日：2011-03-11

申请人： Astellas Pharma Inc.

发明人： KOSHIO, Hiroyuki ,  ASAI, Norio ,  TAKAHASHI, Taisuke ,  SHIMIZU, Takafumi ,  NAGAI, Yasuhito ,  KAWABATA, Keiko ,  THOR, Karl Bruce

IPC分类号： C07D487/04 ,  A61K31/55 ,  A61P3/04 ,  A61P13/00 ,  A61P13/02 ,  A61P15/10 ,  A61P43/00 ,  C07D498/04

CPC分类号： C07D498/04 ,  A61K31/55 ,  C07D471/04 ,  C07D487/04

摘要： [Problem] Provided is a compound which is useful as an agent for treating or preventing 5-HT 2C receptor-related diseases, particularly incontinence such as stress urinary incontinence, urge urinary incontinence, mixed urinary incontinence, and the like, sexual dysfunction such as erectile dysfunction syndrome and the like, obesity, and the like.
[Means for Solution] The present inventors have investigated compounds having a 5-HT 2C receptor agonist activity, which is promising as an active ingredient of a pharmaceutical composition for treating or preventing incontinence such as stress urinary incontinence, urge urinary incontinence, mixed urinary incontinence, and the like, sexual dysfunction such as erectile dysfunction syndrome and the like, obesity, and the like, and have found that the benzazepine compounds of the present invention have an excellent 5-HT 2C receptor agonist activity, thereby completing the present invention. That is, the benzazepine compounds of the present invention have a 5-HT 2C receptor agonist activity and can be used as an agent for treating or preventing 5-HT 2C receptor-related diseases, particularly incontinence such as stress urinary incontinence, urge urinary incontinence, mixed urinary incontinence, and the like, sexual dysfunction such as erectile dysfunction syndrome and the like, obesity, and the like.

公开(公告)号：EP2546255B1

公开(公告)日：2016-08-31

申请号：EP11753475.0

申请日：2011-03-11

申请人： Astellas Pharma Inc.

发明人： KOSHIO, Hiroyuki ,  ASAI, Norio ,  TAKAHASHI, Taisuke ,  SHIMIZU, Takafumi ,  NAGAI, Yasuhito ,  KAWABATA, Keiko ,  THOR, Karl Bruce

IPC分类号： C07D487/04 ,  A61K31/55 ,  A61P3/04 ,  A61P13/00 ,  A61P13/02 ,  A61P15/10 ,  A61P43/00 ,  C07D498/04

CPC分类号： C07D498/04 ,  A61K31/55 ,  C07D471/04 ,  C07D487/04

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。

公开(公告)号：EP3095781A1

公开(公告)日：2016-11-23

申请号：EP15737185.7

申请日：2015-01-13

申请人： Astellas Pharma Inc.

发明人： MATSUMOTO, Shunichiro ,  SHIMIZU, Takafumi ,  SAITO, Tomoyuki ,  KANAYAMA, Takatoshi ,  TANAKA, Hiroaki ,  MORI, Chiharu ,  YOKOYAMA, Kazuhiro ,  MATSUI, Shigeo

IPC分类号： C07D209/16 ,  A61K31/4045 ,  A61K31/4155 ,  A61K31/422 ,  A61K31/427 ,  A61K31/454 ,  A61K31/497 ,  A61K31/506 ,  A61P13/10 ,  A61P43/00 ,  C07D401/12 ,  C07D403/12 ,  C07D417/12

CPC分类号： C07D209/16 ,  C07D401/12 ,  C07D403/12 ,  C07D413/12 ,  C07D417/12

摘要： [Problem] To provide a compound useful as a MT 1 and/or MT 2 receptor agonist. [Solution] The present inventors have studied on MT 1 and/or MT 2 receptor agonists, and have confirmed that indole compounds have the activity. As a result, the present invention is accomplished. That is, a compound represented by formula (I) or a salt thereof according to the present invention has a MT 1 and/or MT 2 receptor agonistic activity and has a low ability of migrating into the central nervous system. Therefore, the compound or a salt thereof can be used as a peripheral MT 1 and/or MT 2 receptor agonist, and therefore can be used as a therapeutic and/or prophylactic agent for urinary incontinence, particularly stress urinary incontinence and mixed urinary incontinence.

公开(公告)号：EP2873660B1

公开(公告)日：2016-10-26

申请号：EP13816547.7

申请日：2013-07-09

申请人： Astellas Pharma Inc.

发明人： KANAYAMA, Takatoshi ,  KUBOTA, Hideki ,  MATSUMOTO, Shunichiro ,  SAITO, Tomoyuki ,  SHIMIZU, Takafumi ,  KATOH, Naoto ,  MATSUI, Shigeo

IPC分类号： C07D209/42 ,  A61K31/4045 ,  A61K31/407 ,  A61K31/437 ,  A61P13/10 ,  C07D471/04 ,  C07D491/048

CPC分类号： C07D491/052 ,  C07D209/42 ,  C07D471/04 ,  C07D491/048

公开(公告)号：EP3333165A1

公开(公告)日：2018-06-13

申请号：EP16833012.4

申请日：2016-08-02

申请人： Astellas Pharma Inc.

发明人： SUGANE, Takashi ,  MAKINO, Takuya ,  YAMASHITA, Daisuke ,  YONETOKU, Yasuhiro ,  TANABE, Daisuke ,  MIHARA, Hisashi ,  ASAI, Norio ,  OSODA, Kazuhiko ,  SHIMIZU, Takafumi ,  MORITOMO, Hiroyuki ,  SUGASAWA, Keizo ,  MAENO, Kyoichi ,  HOSOGAI, Naomi

IPC分类号： C07D401/14 ,  A61K31/496 ,  A61K31/501 ,  A61P13/10 ,  C07D403/06 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D417/14

摘要： [Problem]
To provide a compound which can be used as an MC 4 receptor agonist.
[Means for Solution]
The present inventors have investigated MC 4 receptor agonists, and have found that a piperazine derivative has an action related to the agonists, thereby completing the present invention. That is, the piperazine derivative of the present invention has an MC 4 receptor agonistic action, and can be used as an agent for preventing or treating bladder and/or urinary tract diseases, in particular, underactive bladder, hypotonic bladder, acontractile bladder, detrusor underactivity, neurogenic bladder, urethral relaxation failure, detrusor-external urethral sphincter dyssynergia, and voiding dysfunctions in benign prostatic hyperplasia.

公开(公告)号：EP2873660A1

公开(公告)日：2015-05-20

申请号：EP13816547.7

申请日：2013-07-09

申请人： Astellas Pharma Inc.

发明人： KANAYAMA, Takatoshi ,  KUBOTA, Hideki ,  MATSUMOTO, Shunichiro ,  SAITO, Tomoyuki ,  SHIMIZU, Takafumi ,  KATOH, Naoto ,  MATSUI, Shigeo

IPC分类号： C07D209/42 ,  A61K31/4045 ,  A61K31/407 ,  A61K31/437 ,  A61P13/10 ,  C07D471/04 ,  C07D491/048

CPC分类号： C07D491/052 ,  C07D209/42 ,  C07D471/04 ,  C07D491/048

摘要： [Problem]
To provided a compound which is useful as an MT1 and/or MT2 receptor agonist.
[Means for Solution]
The present inventors have conducted studies on MT1 and/or MT2 receptor agonists, and have found that an indole carboxamide compound has an MT1 and/or MT2 receptor agonistic action, thereby completing the present invention. The indole carboxamide compound of the present invention has the MT1 and/or MT2 receptor agonistic action as well as a low CNS penetration, and therefore, it can be used as an agent for preventing and/or treating urological diseases; in one embodiment, lower urinary tract symptoms; in another embodiment, urine storage symptom, in another embodiment, urinary incontinence; in a still another embodiment, stress urinary incontinence; and the like.

摘要翻译： [问题]提供可用作MT1和/或MT2受体激动剂的化合物。 [解决方法]本发明人对MT1和/或MT2受体激动剂进行了研究，发现吲哚甲酰胺化合物具有MT1和/或MT2受体激动作用，从而完成了本发明。 本发明的吲哚甲酰胺化合物具有MT1和/或MT2受体激动作用以及低CNS渗透，因此它可以用作预防和/或治疗泌尿疾病的药剂; 在一个实施方案中，下尿路症状; 在另一个实施方案中，尿液贮存症状，在另一个实施方案中，尿失禁; 在又一个实施方案中，压力性尿失禁; 等等。