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。

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：EP2206707B1

公开(公告)日：2014-07-23

申请号：EP08842145.8

申请日：2008-10-23

申请人： Astellas Pharma Inc.

发明人： SUGASAWA, Keizo ,  KAWAGUCHI, Kenichi ,  NOMURA, Takaho ,  MATSUMOTO, Shunichiro ,  SHIN, Takashi ,  AZAMI, Hidenori ,  ABE, Tomoaki ,  SUGA, Akira ,  SEO, Ryushi ,  TANAHASHI, Masayuki ,  WATANABE, Toru

IPC分类号： C07D277/20 ,  A61K31/421 ,  A61K31/422 ,  A61K31/426 ,  A61K31/427 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/5377 ,  A61P13/02 ,  A61P43/00 ,  C07D263/34 ,  C07D277/56 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D413/04 ,  C07D417/04 ,  C07D263/48 ,  C07D401/14

CPC分类号： C07D263/34 ,  C07D263/48 ,  C07D277/20 ,  C07D277/56 ,  C07D401/14 ,  C07D403/12 ,  C07D407/12 ,  C07D413/04 ,  C07D413/12 ,  C07D413/14 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14 ,  C07D491/08 ,  C07D491/107 ,  C07D491/113 ,  C07D491/20 ,  C07D495/04 ,  C07D498/10

公开(公告)号：EP2206707A1

公开(公告)日：2010-07-14

申请号：EP08842145.8

申请日：2008-10-23

申请人： Astellas Pharma Inc.

发明人： SUGASAWA, Keizo ,  KAWAGUCHI, Kenichi ,  NOMURA, Takaho ,  MATSUMOTO, Shunichiro ,  SHIN, Takashi ,  AZAMI, Hidenori ,  ABE, Tomoaki ,  SUGA, Akira ,  SEO, Ryushi ,  TANAHASHI, Masayuki ,  WATANABE, Toru

IPC分类号： C07D277/20 ,  A61K31/421 ,  A61K31/422 ,  A61K31/426 ,  A61K31/427 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/5377 ,  A61P13/02 ,  A61P43/00 ,  C07D263/34 ,  C07D277/56 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14

CPC分类号： C07D263/34 ,  C07D263/48 ,  C07D277/20 ,  C07D277/56 ,  C07D401/14 ,  C07D403/12 ,  C07D407/12 ,  C07D413/04 ,  C07D413/12 ,  C07D413/14 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14 ,  C07D491/08 ,  C07D491/107 ,  C07D491/113 ,  C07D491/20 ,  C07D495/04 ,  C07D498/10

摘要： [Object] To provide a therapeutic and/or prophylactic agent for urinary frequency, urinary urgency, and urinary incontinence associated with various lower urinary tract diseases including overactive bladder, various lower urinary tract diseases accompanied by lower urinary tract pain, such as interstitial cystitis, chronic prostatitis, and the like, and various diseases accompanied by pain, based on an excellent trkA receptor inhibitory action.
[Means for Solution] A novel azolecarboxamide compound in which a thiazole ring or an oxazole ring is bonded to a benzene ring, a pyridine ring, a pyridazine ring, a thiophene ring, a pyrazole ring or a pyrrole ring through carboxamide, or a salt thereof is confirmed to have a potent trkA receptor inhibitory activity, and found to be capable of being used as a therapeutic and/or prophylactic agent which is excellent in efficacy and safety for urinary frequency, urinary urgency, and urinary incontinence associated with various lower urinary tract diseases including overactive bladder, various lower urinary tract diseases accompanied by lower urinary tract pain, such as interstitial cystitis, chronic prostatitis, and the like, and various diseases accompanied by pain, thereby completing the present invention.

摘要翻译： 本发明提供与膀胱过度活动症等各种下尿路疾病相伴的尿频，尿急，尿失禁的治疗和/或预防剂，伴有间质性膀胱炎等下尿路疼痛的各种下尿路疾病， 慢性前列腺炎等，以及伴随疼痛的各种疾病，基于优良的trkA受体抑制作用。 [溶液的方法]噻唑环或恶唑环经由羧酰胺与苯环，吡啶环，哒嗪环，噻吩环，吡唑环或吡咯环键合的新型偶氮苯甲酰胺化合物或其盐 证实其具有有效的trkA受体抑制活性，并且发现其能够用作与各种下泌尿相关的尿频，尿急和尿失禁的功效和安全性优异的治疗和/或预防剂 包括膀胱过度活动症，伴有下尿路疼痛的各种下尿路疾病，诸如间质性膀胱炎，慢性前列腺炎等，以及伴有疼痛的各种疾病，由此完成本发明。

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：EP2009005A1

公开(公告)日：2008-12-31

申请号：EP07742444.8

申请日：2007-04-19

申请人： Astellas Pharma Inc.

发明人： SUGASAWA, Keizo ,  KAWAGUCHI, Kenichi ,  MATSUZAWA, Takaho ,  SEO, Ryushi ,  HARADA, Hironori ,  SUGA, Akira ,  ABE, Tomoaki ,  AZAMI, Hidenori ,  MATSUMOTO, Shunichiro ,  SHIN, Takashi ,  TANAHASHI, Masayuki ,  WATANABE, Toru

IPC分类号： C07D263/34 ,  A61K31/427 ,  A61K31/438 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/4985 ,  A61K31/501 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/55 ,  A61K31/551 ,  A61K31/553 ,  A61P13/02 ,  A61P13/08 ,  A61P13/10 ,  A61P19/02 ,  A61P25/04 ,  A61P43/00

CPC分类号： C07D277/56 ,  C07D263/34 ,  C07D263/48 ,  C07D413/04 ,  C07D413/12 ,  C07D413/14 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D471/10 ,  C07D487/08 ,  C07D491/08

摘要： Provided is an agent for treating or preventing urinary frequency, urinary urgency and urinary, incontinence which are associated with overactive bladder, a lower urinary tract disease such as interstitial cystitis and chronic prostatitis accompanied by lower urinary tract pain, and various diseases accompanied by pain. A novel azolecarboxamide derivative in which an azole ring such as thioazole or oxazole is bonded to a benzene ring, pyridine ring or pyrimidine ring through carboxamide was confirmed to have a potent trkA receptor-inhibitory activity and found to be an agent for treating or preventing lower urinary tract disease and various diseases accompanied by pain, which is excellent in efficacy and safety, and thus the present invention was accomplished.

摘要翻译： 本发明提供一种治疗或预​​防伴有膀胱过度活动症的尿频，尿急尿失禁，下尿路疾病如间质性膀胱炎和伴有下尿路疼痛的慢性前列腺炎，以及伴有疼痛的各种疾病。 确认噻唑或恶唑等吡咯环通过羧酰胺与苯环，吡啶环或嘧啶环结合的新型偶氮羧酰胺衍生物具有强烈的trkA受体抑制活性，被发现是治疗或预防剂 泌尿系统疾病和各种伴有疼痛的疾病，其效力和安全性优异，从而完成了本发明。