New forms and salts of a dihydropyrrolo[1,2-c]imidazolyl aldosterone synthase or aromatase inhibitor 机翻标题: 暂无翻译,请尝试点击翻译按钮。

公开号/公开日
WO2013109514 A1 2013-07-25 [WO2013109514] / 2013-07-25
申请号/申请日
2013WO-US21521 / 2013-01-15
发明人
SUTTON PAUL;LOESER ERIC;
申请人
NOVARTIS;
主分类号
IPC分类号
A61K-031/407A61P-005/38C07D-487/04
摘要
(WO2013109514) The invention relates to a phosphate salt or a nitrate salt of 4-(R)-6,7- dihydro-5H-pyrrolo[l,2-c]imidazol-5-yl-3-fluoro-benzonitrile having following formula: especially in crystalline form, and specific forms of these salts, as well as related invention embodiments.  The salts and salt forms allow for the prophylactic and/or therapeutic treatment of aldosterone synthase and/or aromatase mediated diseases or disorders such as Cushing's disease.
机翻摘要
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地址
代理人
代理机构
;
优先权号
2012US-61587280 2012-01-17
主权利要求
(WO2013109514) 1. A phosphate salt of 4-(R)-(6,7-dihydro-5H-pyrrolo[1,2-c]imidazol-5-yl)-3-fluoro benzonitrile. ' 12. A nitrate salt of 4-(R)-6,7-dihydro-5H-pyrrolo[1,2-c]imidazol-5-yl-3-fluoro-benzonitrile. 13. A process for making a phosphate salt, especially in crystalline form, respectively, of 4-(R)-6,7-dihydro-5H-pyrrolo[1,2-c]imidazol-5-yl-3-fluoro-benzonitrile, the process comprising: (a) providing a solution of 4-(R)-6,7-dihydro-5H-pyrrolo[1,2-c]imidazol-5-yl-3- fluoro-benzonitrile in either a protic or an aprotic polar solvent; (b) adding nitric acid or especially phosphoric acid; and (c) isolating the formed crystalline form of a nitrate salt or especially a phosphate salt of 4-(R)-6,7-dihydro-5H-pyrrolo[1,2-c]imidazol-5-yl-3-fluoro-benzonitrile; . 17. A pharmaceutical composition comprising a phosphate salt of 4-(R)-(6,7-dihydro-5H- pyrrolo[1,2-c]imidazol-5-yl)-3-fluoro-benzonitrile and one or more pharmaceutically acceptable excipients.
法律状态
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