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Polymorphs
专利权人:
发明人:
지거 페터,켐머 디르크,콜바우어 페터,니콜라 토마스,렌츠 마르틴
申请号:
KR1020087026976
公开号:
KR1014529150000B1
申请日:
2007.04.30
申请国别(地区):
KR
年份:
2014
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.본 발명은 1-((4-메틸-퀴나졸린-2-일)메틸)-3,7-(2-부틴-1-일)-8-(3-(R)-아미노피페리딘-1-일)크산틴의 다형태 결정성 변형물, 이의 제조방법 및 약물을 제조하기 위한 이의 용도에 관한 것이다.
来源网站:
中国工程科技知识中心
来源网址:
http://www.ckcest.cn/home/

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