发明名称 Crystalline form of a quinolinone-carboxamide compound
摘要 The invention provides a crystalline hydrochloride salt of 1-isopropyl-2-oxo-1,2-dihydroquinoline-3-carboxylic acid {(1S,3R,5R)-8-[(R)-2-hydroxy-3-(methanesulfonyl-methyl-amino)propyl]-8-azabicyclo[3.2.1]oct-3-yl}amide or a solvate thereof. The invention also provides pharmaceutical compositions comprising such crystalline salt forms, methods of using such crystalline salt forms to treat diseases associated with 5-HT4 receptor activity, and processes useful for preparing such crystalline salt forms.
申请公布号 US9126994(B2) 申请公布日期 2015.09.08
申请号 US201414150059 申请日期 2014.01.08
申请人 Theravance Biopharma R&D IP, LLC 发明人 Fatheree Paul R.;Turner S. Derek;Goldblum Adam A.;Chao Robert S.;Genov Daniel
分类号 A61K31/46;C07D451/04 主分类号 A61K31/46
代理机构 代理人 Hagenah Jeffrey A.;Saxon Roberta P.
主权项 1. A method of treating a disorder of reduced motility of the gastrointestinal tract in a mammal, wherein the disorder of reduced motility is chronic constipation, constipation-predominant irritable bowel syndrome, gastroparesis, drug-induced delayed transit, or functional dyspepsia, the method comprising administering to the mammal a pharmaceutical composition comprising a pharmaceutical carrier and a crystalline hydrochloride salt of 1-isopropyl-2-oxo-1,2-dihydroquinoline-3-carboxylic acid {(1S,3R,5R)-8-[(R)-2-hydroxy-3-(methanesulfonyl-methyl-amino)propyl]-8-azabicyclo[3.2.1]oct-3-yl}amide which is characterized by a powder x-ray diffraction pattern having two or more diffraction peaks at 2θ values selected from 4.41±0.2, 8.82±0.2, 9.08±0.2, 11.21±0.2, 14.40±0.2, 16.42±0.2, 17.35±0.2, 17.61±0.2, 18.14±0.2, 19.04±0.2, 19.95±0.2, 20.20±0.2, 21.23±0.2, 22.13±0.2, 22.48±0.2, 22.83±0.2, 24.16±0.2, 25.37±0.2, 25.56±0.2, 26.22±0.2, 27.33±0.2, 29.08±0.2, and 29.61±0.2.
地址 South San Francisco CA US