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Title:
Polymorph
Document Type and Number:
Japanese Patent JP6309589
Kind Code:
B2
Abstract:
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.

Inventors:
Siegel Peter
Kemmer Dirk
Call Bauer Peter
Nikola Thomas
Lenz Martin
Application Number:
JP2016197147A
Publication Date:
April 11, 2018
Filing Date:
October 05, 2016
Export Citation:
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Assignee:
Boehringer Ingelheim International GmbH
International Classes:
C07D473/04
Domestic Patent References:
JP2006503013A
JP5323684B2
JP5800773B2
JP6022513B2
Attorney, Agent or Firm:
Takaki Nishijima
Disciple Maru Ken
Shinichiro Tanaka
Atsushi Hakoda
Kenji Asai
Kazuo Yamazaki
Satsuki Ichikawa
Hironobu Hattori