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多晶型
专利权人:
Boehringer Ingelheim International GmbH;勃林格殷格翰國際有限公司
发明人:
SIEGER, Peter,KEMMER, Dirk,KOHLBAUER, Peter,NICOLA, Thomas,RENZ, Martin,彼得‧科爾鮑爾,NICOLA, Thomas,托馬斯‧尼古拉,RENZ, Martin,馬丁‧倫茲
申请号:
HK18104664.7
公开号:
HK1245264A
申请日:
2018.04.10
申请国别(地区):
HK
年份:
2018
代理人:
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.
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中国工程科技知识中心
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