Crystal of diamine derivative and method of producing same
AssigneeDaiichi Sankyo Company, Limited
InventorsTetsuya Suzuki, Makoto Ono
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Abstract
An object of the present invention is to provide a novel crystal form of a compound that has an inhibitory effect on activated blood coagulation factor X and is useful as a pharmaceutical compound for prevention and/or treatment of thrombotic and/or embolic diseases. The present invention provides a novel crystal form of N1-(5-chloropyridin-2-yl)-N2-((1S,2R,4S)-4-[(dimethylamino)carbonyl]-2-{[(5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridin-2-yl)carbonyl]amino}cyclohexyl)ethanediamide p-toluenesulfonate monohydrate, and method for producing the same.
Claims22
Form II crystals of N1-(5-chloropyridin-2-yl)-N2-((1S,2R,4S)-4-[(dimethylamino)carbonyl]-2-{[(5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridin-2-yl)carbonyl]amino}cyclohexyl)ethanediamide p-toluenesulfonate monohydrate represented by the following formula (I):
- comprising peaks at diffraction angles (2θ) of 13.9±0.2, 14.2±0.2, 15.8±0.2, 16.2±0.2, 18.2±0.2, 21.5±0.2, 22.0±0.2, 22.3±0.2, 23.2±0.2, and 24.3±0.2(°) in powder x-ray diffraction obtained using Cu-Kα rays.
A method for producing Form II crystals of N1-(5-chloropyridin-2-yl)-N2-((1S,2R,4S)-4-[(dimethylamino)carbonyl]-2-{[(5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridin-2-yl)carbonyl]amino}cyclohexyl)ethanediamide p-toluenesulfonate monohydrate represented by the following formula (I):
- comprising peaks at diffraction angles (2θ) of 13.9±0.2, 14.2±0.2, 15.8±0.2, 16.2±0.2, 18.2±0.2, 21.5±0.2, 22.0±0.2, 22.3±0.2, 23.2±0.2, and 24.3±0.2(°) in powder x-ray diffraction obtained using Cu-Kα rays, the method comprising the steps of
- (a) converting a compound represented by formula (I) to an amorphous or low crystalline solid by the dissolution of the compound represented by formula (I) in water, dioxane, aqueous dioxane, or dimethyl sulfoxide followed by freeze drying;
- and
- (b) exposing the amorphous or low crystalline solid to solvent vapor.
Dependencies are inferred from the claim text.