Crystal form of 1-[(4-methyl-quinazoline-2-yl)methyl]-3-methyl-7-(2-butyne-1-yl)-8-(3-(R)-amino-piperidine-1-yl)-xanthine

JP7872225B2Active Publication Date: 2026-06-09YUKI GOSEI IND
View PDF 9 Cites 0 Cited by

Patent Information

Authority / Receiving Office
JP · JP
Patent Type
Patents
Current Assignee / Owner
YUKI GOSEI IND
Filing Date
2021-06-10
Publication Date
2026-06-09

AI Technical Summary

Benefits of technology

【0006】 本発明のリナグリプチンの結晶形態によれば、不純物の生成が少なく優れた安定性を示すことができる。また、本発明のリナグリプチンの結晶形態は、優れた水への溶解性を示すことができる。

✦ Generated by Eureka AI based on patent content.

Smart Images

  • Figure 0007872225000012
    Figure 0007872225000012
  • Figure 0007872225000013
    Figure 0007872225000013
  • Figure 0007872225000001
    Figure 0007872225000001
Patent Text Reader

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.
Need to check novelty before this filing date? Find Prior Art

Claims

1. Crystals of 1-[(4-methyl-quinazolin-2-yl)methyl]-3-methyl-7-(2-butyne-1-yl)-8-(3-(R)-amino-piperidine-1-yl)-xanthine, showing peaks at 6.9°±0.2°, 7.3°±0.2°, 7.6°±0.2°, 9.3°±0.2°, 14.5°±0.2°, 17.7°±0.2°, and 20.8°±0.2° in powder X-ray diffraction (diffraction angle 2θ) induced by Cu-Kα irradiation.

2. The crystal according to claim 1, having the powder X-ray diffraction pattern shown in the figure below.

3. A pharmaceutical composition for the treatment of diabetes, comprising crystals of 1-[(4-methyl-quinazolin-2-yl)methyl]-3-methyl-7-(2-butyne-1-yl)-8-(3-(R)-amino-piperidine-1-yl)-xanthine as an active ingredient.

4. Use of the crystals of 1-[(4-methyl-quinazolin-2-yl)methyl]-3-methyl-7-(2-butyne-1-yl)-8-(3-(R)-amino-piperidine-1-yl)-xanthine according to claim 1 or 2 in the manufacture of a pharmaceutical composition for the treatment of diabetes.

5. Crystals of 1-[(4-methyl-quinazolin-2-yl)methyl]-3-methyl-7-(2-butyne-1-yl)-8-(3-(R)-amino-piperidine-1-yl)-xanthine according to claim 1 or 2, for use in a method for treating diabetes.