公开(公告)号：US09643940B2

公开(公告)日：2017-05-09

申请号：US14424215

申请日：2013-08-30

申请人： ONO PHARMACEUTICAL CO., LTD.

发明人： Kousuke Tani ,  Akihiro Kinoshita ,  Keisuke Hanada ,  Yoshiyuki Aratani ,  Takahiro Nekado ,  Atsushi Shimabukuro

IPC分类号： C07D277/56 ,  A61K47/40 ,  C07D277/20 ,  C07D211/22 ,  A61K31/426 ,  C08B37/16 ,  C08L5/16

CPC分类号： C07D277/56 ,  A61K31/426 ,  A61K47/40 ,  C07B2200/13 ,  C07D211/22 ,  C07D277/20 ,  C08B37/0015 ,  C08L5/16

摘要： A compound that can be a therapeutic agent for underactive bladder which has low risk of side effects and can be administered orally is provided. Furthermore, a crystal which is advantageous in view of the stability, long-term storage, handleability, easiness of the drug preparation or the like as a drug substance of medicaments is provided. Since a salt of 2-[(2-{(1R,5R)-2-oxo-5-[(1E,4S)-7,8,8-trifluoro-4-hydroxy-4-methyl-1,7-octadien-1-yl]cyclopentyl}ethyl)thio]-1,3-thiazole-4-carboxylic acid or a diastereomeric mixture thereof and 4-piperidinemethanol is a chemically very stable crystal, it can be stored for a long time, and is very useful as a drug substance of medicaments.

公开(公告)号：US20150218114A1

公开(公告)日：2015-08-06

申请号：US14424215

申请日：2013-08-30

申请人： ONO PHARMACEUTICAL CO., LTD.

发明人： Kousuke Tani ,  Akihiro Kinoshita ,  Keisuke Hanada ,  Yoshiyuki Aratani ,  Takahiro Nekado ,  Atsushi Shimabukuro

IPC分类号： C07D277/56 ,  C08B37/16 ,  C07D211/22

CPC分类号： C07D277/56 ,  A61K31/426 ,  A61K47/40 ,  C07B2200/13 ,  C07D211/22 ,  C07D277/20 ,  C08B37/0015 ,  C08L5/16

摘要： A compound that can be a therapeutic agent for underactive bladder which has low risk of side effects and can be administered orally is provided. Furthermore, a crystal which is advantageous in view of the stability, long-term storage, handleability, easiness of the drug preparation or the like as a drug substance of medicaments is provided. Since a salt of 2-[(2-{(1R,5R)-2-oxo-5-[(1E,4S)-7,8,8-trifluoro-4-hydroxy-4-methyl-1,7-octadien-1-yl]cyclopentyl}ethyl)thio]-1,3-thiazole-4-carboxylic acid or a diastereomeric mixture thereof and 4-piperidinemethanol is a chemically very stable crystal, it can be stored for a long time, and is very useful as a drug substance of medicaments.

摘要翻译： 提供可以作为副作用低的口服低剂量膀胱用治疗剂的化合物。 此外，提供了鉴于药物的药物物质的稳定性，长期储存，可操作性，药物制备容易度等方面是有利的晶体。 由于2 - [（2 - {（1R，5R）-2-氧代-5 - [（1E，4S）-7,8,8-三氟-4-羟基-4-甲基-1,7- 辛二烯-1-基]环戊基}乙基）硫代] -1,3-噻唑-4-羧酸或其非对映异构体混合物和4-哌啶甲醇是化学上非常稳定的晶体，它可以长时间储存​​，并且是 作为药物的药物物质非常有用。