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：US11319296B2

公开(公告)日：2022-05-03

申请号：US17276284

申请日：2019-09-19

申请人： ONO PHARMACEUTICAL CO., LTD.

发明人： Masaki Asada ,  Keisuke Hanada ,  Satonori Higuchi ,  Atsushi Naganawa ,  Yasuhiro Takeda

IPC分类号： C07D309/06 ,  C07C235/64 ,  C07C233/81 ,  C07C327/48 ,  A61P25/20

摘要： An object of the present invention is to provide a DP receptor antagonist. A compound represented by general formula (I): (wherein all symbols are as shown in the specification) and a pharmaceutically acceptable salt thereof have DP receptor antagonistic activity and are also highly safe, and thus are useful as active ingredients of pharmaceuticals for DP receptor-mediated diseases. In addition, the compound represented by the general formula (I) and the pharmaceutically acceptable salt thereof also have good transferability to the central nervous system, and thus are particularly useful as a preventive and/or therapeutic agent for diseases associated with DP receptors present in the central nervous system among DP receptor-mediated diseases, that is, sleep-wake disorders.

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。