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Title:
CRYSTAL MORPHOLOGY OF 1-[(4-METHYL-QUINAZOLINE-2-YL)METHYL]-3-METHYL-7-(2-BUTYN-1-YL)-8-(3-(R)-AMINO-PEPERIDINE-1-YL)-XANTHINE
Document Type and Number:
WIPO Patent Application WO/2021/250995
Kind Code:
A1
Abstract:
The purpose of the present invention is to provide a crystal morphology of 1-[(4-methyl-quinazoline-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-amino-peperidine-1-yl)-xanthine, which exhibits superior stability. The above problem can be solved by: the crystal morphology of 1-[(4-methyl-quinazoline-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-amino-peperidine-1-yl)-xanthine, which exhibits at least three peaks selected from the group consisting of 6.9° ± 0.2°, 7.6° ± 0.2°, 9.3° ± 0.2°, 14.5° ± 0.2°, and 20.8° ± 0.2° in X-ray powder diffraction (diffraction angle 2θ) by Cu-Ka radiation; or the crystal morphology of 1-[(4-methyl-quinazoline-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-amino-peperidine-1-yl)-xanthine, which exhibits at least four peaks selected from the group consisting of 6.9°±0.2°, 10.4°±0.2°, 15.4°±0.2°, 17.9°±0.2°, 20.8°±0.2°, and 23.8°±0.2° in X-ray powder diffraction (diffraction angle 2θ) by Cu-Ka radiation.

Inventors:
TANAKA YUMIKO (JP)
SHIMIZU YUMIKA (JP)
ONAGA TOMOTSUNE (JP)
Application Number:
PCT/JP2021/015338
Publication Date:
December 16, 2021
Filing Date:
April 13, 2021
Export Citation:
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Assignee:
YUKI GOSEI YAKUHIN KOGYO KK (JP)
International Classes:
A61P3/10; A61K31/522; C07D473/04
Domestic Patent References:
WO2013128379A22013-09-06
Foreign References:
JP2009535375A2009-10-01
JP2018177769A2018-11-15
CN108017638A2018-05-11
CN107043376A2017-08-15
Other References:
HIRAYAMA, NORIAKI: "HANDBOOK FOR ORGANIC COMPOUND CRYSTAL PREPARATION - PRINCIPLES AND KNOW-HOW", 2008, pages: 58 - 59
Attorney, Agent or Firm:
YAMAGUCHI Kenjiro et al. (JP)
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