公开(公告)号：EP4177257A1

公开(公告)日：2023-05-10

申请号：EP21837478.3

申请日：2021-07-05

申请人： Kissei Pharmaceutical Co., Ltd.

发明人： TAKEUCHI, Hideki ,  JO, Kazumichi

IPC分类号： C07D495/04 ,  A61K31/4365 ,  A61P5/10 ,  A61P25/00 ,  A61P25/16

摘要： [Problem] An object of the present invention is to provide a compound which has high storage stability and is suitable for use as a drug substance.
[Solution] The present invention relates to a succinate salt of 1-{[(4aR,6R,8aR)-2-amino-3-cyano-8-methyl-4,4a, 5,6,7,8,8a,9-octahydrothieno[3,2-g]quinolin-6-yl]carbonyl}-3-[2-(dimethylamino)ethyl]-1-propylurea, which is suitable as a drug substance having excellent storage stability and crystallinity and is useful for the treatment or prevention of Parkinson's disease, restless legs syndrome, hyperprolactinemia or the like.

公开(公告)号：EP2535342B1

公开(公告)日：2014-08-06

申请号：EP11742250.1

申请日：2011-02-09

申请人： Kissei Pharmaceutical Co., Ltd.

发明人： JO, Kazumichi ,  TAKEUCHI, Hideki

IPC分类号： C07D495/04 ,  A61K31/519 ,  A61P5/04 ,  A61P15/08 ,  A61P15/16 ,  A61P15/18 ,  A61P35/00

CPC分类号： A61K31/519 ,  A61K9/0053 ,  A61K31/14 ,  C07B2200/13 ,  C07D495/04

摘要： An objective of the present invention is to improve the solubility of 3-[2-fluoro-5-(2,3-difluoro-6-methoxybenzyloxy)-4-methoxyphenyl]-2,4-dioxo-1,2,3,4-tetrahydrothieno[3,4-d]pyrimidine-5-carboxylic acid. The present invention provides 3-[2-fluoro-5-(2,3-difluoro-6-methoxybenzyl-oxy)-4-methoxyphenyl]-2,4-dioxo-1,2,3,4-tetrahydrothieno[3,4-d]pyrimidine-5-carboxy lic acid choline salt has excellent solubility and storage stability.

公开(公告)号：EP2535342A1

公开(公告)日：2012-12-19

申请号：EP11742250.1

申请日：2011-02-09

申请人： Kissei Pharmaceutical Co., Ltd.

发明人： JO, Kazumichi ,  TAKEUCHI, Hideki

IPC分类号： C07D495/04 ,  A61K31/519 ,  A61P5/04 ,  A61P15/08 ,  A61P15/16 ,  A61P15/18 ,  A61P35/00

CPC分类号： A61K31/519 ,  A61K9/0053 ,  A61K31/14 ,  C07B2200/13 ,  C07D495/04

摘要： An objective of the present invention is to improve the solubility of 3-[2-fluoro-5-(2,3-difluoro-6-methoxybenzyloxy)-4-methoxyphenyl]-2,4-dioxo-1,2,3,4-tetrahydrothieno[3,4-d]pyrimidine-5-carboxylic acid.
The present invention provides 3-[2-fluoro-5-(2,3-difluoro-6-methoxybenzyl-oxy)-4-methoxyphenyl]-2,4-dioxo-1,2,3,4-tetrahydrothieno[3,4-d]pyrimidine-5-carboxy lic acid choline salt has excellent solubility and storage stability.

摘要翻译： 本发明的一个目标是提高的3- [2-氟-5-（2,3-二氟-6-甲氧基苄基氧基）-4-甲氧基苯基] -2,4-二氧代-1,2,3-溶解度， 4四氢噻吩[3,4-d]嘧啶-5-羧酸。 本发明提供了3- [2-氟-5-（2,3-二氟-6-甲氧基苄基氧基）-4-甲氧基苯基] -2,4-二氧代-1,2,3,4-四氢噻吩并[3， 4-d]嘧啶-5-羧基LIC酸胆碱盐具有优异的溶解性和储存稳定性。