公开(公告)号：US09562044B2

公开(公告)日：2017-02-07

申请号：US14770648

申请日：2014-02-27

Applicant: ASTELLAS PHARMA INC.

Inventor： Taisuke Takahashi ,  Jun Maeda ,  Yusuke Inagaki ,  Kenji Negoro ,  Hiroaki Tanaka ,  Kazuhiro Yokoyama ,  Hajime Takamatsu ,  Takanori Koike ,  Issei Tsukamoto

IPC: C07D417/14 ,  C07D491/08 ,  A61K31/497 ,  A61K31/5377 ,  C07D491/107

CPC classification number: C07D417/14 ,  A61K31/497 ,  A61K31/5377 ,  A61P13/10 ,  A61P43/00 ,  C07D491/08 ,  C07D491/107

Abstract: Thiazole derivatives having pyrazine-2-carbonylamino substituted at the 2-position of the following formula (I): are excellent muscarinic M3 receptor positive allosteric modulators, and are useful for treating bladder or urinary tract diseases, related to bladder contraction by a muscarinic M3 receptor. The 2-acylaminothiazole derivatives and salts thereof can be used for treating bladder or urinary tract diseases, related to bladder contraction by a muscarinic M3 receptor, for example, voiding dysfunctions such as underactive bladder.

Abstract translation: [问题]提供了用作治疗储存功能障碍，排尿功能障碍和下尿路疾病的药物组合物的活性成分的化合物。 [解决方案]本发明人已经发现，具有2-位取代的吡嗪-2-羰基氨基的噻唑衍生物是优良的毒蕈碱M 3受体正变构调节剂，可用作膀胱的预防和/或治疗剂 或尿路疾病，涉及到毒蕈碱M 3受体的膀胱收缩，从而完成了本发明。 本发明的2-酰氨基噻唑衍生物或其盐可用作预防和/或治疗膀胱或尿路疾病的药物，其与由毒蕈碱M 3受体引起的膀胱收缩有关，例如排空功能障碍如不充分活动 膀胱。

公开(公告)号：US20160002218A1

公开(公告)日：2016-01-07

申请号：US14770648

申请日：2014-02-27

Applicant: ASTELLAS PHARMA INC.

Inventor： Taisuke TAKAHASHI ,  Jun MAEDA ,  Yusuke INAGAKI ,  Kenji NEGORO ,  Hiroaki TANAKA ,  Kazuhiro YOKOYAMA ,  Hajime TAKAMATSU ,  Takanori KOIKE ,  Issei TSUKAMOTO

IPC: C07D417/14 ,  C07D491/107

CPC classification number: C07D417/14 ,  A61K31/497 ,  A61K31/5377 ,  A61P13/10 ,  A61P43/00 ,  C07D491/08 ,  C07D491/107

Abstract: [Problem]A compound which is useful as an active ingredient of a pharmaceutical composition for treating storage dysfunctions, voiding dysfunctions, and lower urinary tract diseases is provided.[Means for Solution]The present inventors have found that a thiazole derivative having pyrazine-2-carbonylamino substituted at the 2-position is an excellent muscarinic M3 receptor positive allosteric modulator, and is useful as an agent for preventing and/or treating bladder or urinary tract diseases, related to bladder contraction by a muscarinic M3 receptor, thereby completing the present invention. The 2-acylaminothiazole derivative or a salt thereof of the present invention can be used as an agent for preventing and/or treating bladder or urinary tract diseases, related to bladder contraction by a muscarinic M3 receptor, for example, voiding dysfunctions such as underactive bladder.

Abstract translation: [问题]提供了用作治疗储存功能障碍，排尿功能障碍和下尿路疾病的药物组合物的活性成分的化合物。 [解决方案]本发明人已经发现，具有2-位取代的吡嗪-2-羰基氨基的噻唑衍生物是优异的毒蕈碱M3受体阳性变构调节剂，可用作预防和/或治疗膀胱或 尿道疾病，涉及到毒蕈碱性M3受体的膀胱收缩，从而完成了本发明。 本发明的2-酰氨基噻唑衍生物或其盐可用作预防和/或治疗与毒蕈碱性M3受体的膀胱收缩有关的膀胱或尿路疾病的药剂，例如排尿功能障碍如膀胱活动不足 。

公开(公告)号：US20140113863A1

公开(公告)日：2014-04-24

申请号：US14143866

申请日：2013-12-30

Applicant: Ferring B.V.

Inventor： Bjarke Mirner Klein ,  Jens Peter Norgaard

IPC: A61K38/11

CPC classification number: A61K38/11 ,  A61K9/0056 ,  A61K38/08 ,  A61P13/10

Abstract: The present disclosure is directed to reducing nocturnal voids by administering a dose of desmopressin over a minimum treatment period compared to before administration, and maintaining or improving the reduction of nocturnal voids over the minimum treatment period.

Abstract translation: 本公开内容涉及通过在施用之前在最小治疗期间施用一定剂量的去氨加压素来减少夜间空隙，并且在最小治疗期间保持或改善夜间空隙的减少。