Salt and polymorph of benzopyrimidinone compound and pharmaceutical composition and use thereof

Patent metadata

Field	Value
Publication number	US-11434226-B2
Application number	US-202016736300-A
Country	US
Kind code	B2
Filing date	Jan 7, 2020
Priority date	Jul 7, 2017
Publication date	Sep 6, 2022
Grant date	Sep 6, 2022

Abstract

The present disclosure relates to a salt of phenyl pyrimidinone compound, a polymorph thereof and a pharmaceutical composition comprising the same and a use thereof, particularly relates to the hydrochlorate of phenyl pyrimidinone compound of following formula (I-A) and a pharmaceutically acceptable polymorph, solvate, hydrate, co-crystal, anhydrous substance, or amorphous form thereof, a pharmaceutical composition and a pharmaceutical unit dosage comprising the same, the preparing method and use thereof.

First claim

The invention claimed is:

1. A compound of the following formula:

wherein the compound is a crystalline form A which has peaks at a diffraction angle 2θ of 6.1°±0.2°, 9.3°±0.2°, 11.1°±0.2°, 12.2°±0.2°, 15.3°±0.2°, 16.7°±0.2°, 21.6°±0.2°, 22.9°±0.2° in X-ray diffraction pattern.

2. The compound according to claim 1 , wherein the crystalline form A has characteristic peaks at least at 3482.81 cm −1 , 3405.67 cm −1 , 3293.82 cm −1 , 3046.98 cm −1 , 2967.91 cm −1 , 2871.49 cm −1 , 1656.55 cm −1 , 1604.48 cm −1 , 1579.41 cm −1 , 1494.56 cm −1 , 1226.50 cm −1 , 973.88 cm −1 , 813.81 cm −1 , in the infrared absorption spectrum as measured by the potassium bromide pellet technique.

3. The compound according to claim 1 , wherein the crystalline form A belongs to monoclinic crystal system and space group Pc, with axis length a=9.935(4) Å, b=14.44(6) Å, c=9.147(5) Å, and the angle of the lattice plane α=90°, β=106.47(5°), γ=90°.

4. A pharmaceutical composition comprising the compound according to claim 1 and a pharmaceutically acceptable adjuvant.

Assignees

• Shanghai Inst Materia Medica Cas
• Suzhou Vigonvita Life Sciences Co Ltd
• Topharman Shanghai Co Ltd

Inventors

• Shen Jingshan
• He Yang
• Chen Weiming
• Li Jianfeng
• Tian Guanghui
• Gong Xudong
• Wang Zhen
• Zhang Rongxia
• Liu Yongjian
• Jiang Hualiang

Classifications

• A61K45/06

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

• A61K31/506

  not condensed and containing further heterocyclic rings · CPC title

• C07D239/36 Primary

  as doubly bound oxygen atom or as unsubstituted hydroxy radical · CPC title

• C07B2200/13

  Crystalline forms, e.g. polymorphs · CPC title

• A61P15/10

  for impotence · CPC title