发明名称 Polymorphs
摘要 Anhydrous Polymorphic Forms A, B, D and E and polymorphic form C of 1-[(4-methyl-quinazolin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-amino-piperidin-1-yl)-xanthine (I), are new. Form A has a melting point of 206+-[deg]C; Form D melts at 150+-3[deg]C; and Form E melts at 175+-3[deg]C. Form B transforms reversibly into the polymorph A at 10-40[deg]C. Form C loses water at 30-100[deg]C. An independent claim is included for a method (M1) of preparing polymorph form C involving refluxing (I) in methanol; cooling the methanolic solution to 40-60[deg]C; adding a solvent such as tert-butylmethylether; cooling the resulting suspension to 15-25[deg]C and then to 0-5[deg]C; filtering the crystals by suction and drying in vacuo at 70[deg]C. ACTIVITY : Antidiabetic; Anorectic; Antarthritic; Antirheumatoid; Osteopathic; Immunosuppressive. No biological data is given. MECHANISM OF ACTION : Dipeptidyl peptidase (DPP)-IV inhibitor.
申请公布号 ZA200808224(B) 申请公布日期 2009.05.27
申请号 ZA20080008224 申请日期 2008.09.26
申请人 BOEHRINGER INGELHEIM INTERNATIONAL GMBH 发明人 SIEGER, PETER;KEMMER, DIRK;KOHLBAUER, PETER;NICOLA, THOMAS;RENZ, MARTIN
分类号 A61K;A61P;C07D 主分类号 A61K
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