Solid form of dihydropyrimidine compound and preparation method therefor and use thereof

Patent metadata

Field	Value
Publication number	US-11434235-B2
Application number	US-201916981430-A
Country	US
Kind code	B2
Filing date	May 6, 2019
Priority date	May 16, 2018
Publication date	Sep 6, 2022
Grant date	Sep 6, 2022

Abstract

Disclosed are a solid form of (E)-3-((R)-4-(((R)-6-(2-chloro-4-fluorophenyl)-5-(methoxycarbonyl)-2-(thiazol-2-yl)-3,6-dihydropyrimidin-4-yl)methyl)morpholin-2-yl)acrylic acid, a preparation method therefor, a pharmaceutical composition comprising same, and the use thereof in the preparation of drugs for preventing or treating viral diseases.

First claim

What is claimed is:

1. A crystalline form A of the compound of Formula (I) characterized in that the X-ray powder diffraction pattern of the crystalline form A has characteristic peaks at diffraction angles of 8.7±0.2°, 17.5±0.2°, 19.3±0.2°, 20.3±0.2° and 21.4±0.2°,

2. The crystalline form A according to claim 1 , further comprising peaks at diffraction angles of 16.0±0.2°, 17.8±0.2°, 22.3±0.2° and 23.1±0.2°.

3. The crystalline form A according to claim 1 , characterized in that the endothermic peak in a differential scanning calorimetry (DSC) graph of the crystalline form A of the compound of Formula (I) appears at 173±2° C.

4. The crystalline form A according to claim 1 , characterized in that the crystalline form A of the compound of Formula (I) starts to decompose at 190±2° C. measured using thermogravimetric analysis (TGA).

5. A pharmaceutical composition comprising the crystalline form A according to claim 1 , and one or more pharmaceutically acceptable carriers or one or more additional therapeutic agents.

6. A pharmaceutical formulation comprising the crystalline form A according to claim 1 , and one or more pharmaceutically acceptable carriers.

7. The crystalline form A according to claim 2 , wherein the X-ray powder diffraction pattern of the crystalline form A is as shown in FIG. 1 .

8. The crystalline form A according to claim 3 , wherein the DSC graph of the crystalline form A is as shown in FIG. 2 .

9. The crystalline form A according to claim 4 , wherein the TGA graph of the crystalline form A is as shown in FIG. 3 .

Assignees

• Sichuan Kelun Biotech Biopharmaceutical Co Ltd

Inventors

• Wang Tianming
• Yang Chengxi
• Cai Jiaqiang
• Liu Wei
• Zhang Baolei
• Tian Qiang
• Song Shuai
• Hu Hao
• Han Weibiao
• Li Youqiang
• Chen Xing
• Wang Lichun
• Wang Jingyi

Classifications

• A61P31/18

  for HIV · CPC title

• C07D417/14 Primary

  containing three or more hetero rings · CPC title

• A61P31/20

  for DNA viruses · CPC title

• A61K45/06

  Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca · CPC title

• A61P31/14

  for RNA viruses · CPC title