Biphenyl diaryl pyrimidine derivative with aromatic heterocyclic structure

Patent metadata

Field	Value
Publication number	US-11912685-B2
Application number	US-202117468447-A
Country	US
Kind code	B2
Filing date	Sep 7, 2021
Priority date	Mar 8, 2021
Publication date	Feb 27, 2024
Grant date	Feb 27, 2024

Abstract

This application provides a biphenyl diaryl pyrimidine derivative with an aromatic heterocyclic structure, a pharmaceutically-acceptable salt, a stereoisomer, a hydrate and a solvate thereof, where the biphenyl diaryl pyrimidine derivative is shown in formula (I). This application also provides a pharmaceutical composition containing the biphenyl diaryl pyrimidine derivative, or a pharmaceutically-acceptable salt, a stereoisomer, a hydrate and a solvate thereof, and a pharmaceutically-acceptable carrier. This application further provides a method of treating AIDS by administering a therapeutically effective amount of the pharmaceutical composition to a patient in need.

First claim

What is claimed is:

1. A compound of formula (I), or a pharmaceutically-acceptable salt, a stereoisomer, a hydrate or a solvate thereof:

wherein R 1 is selected from the group consisting of substituted and unsubstituted furyl, substituted and unsubstituted thienyl, substituted and unsubstituted pyrazolyl, substituted and unsubstituted imidazolyl, substituted and unsubstituted thiazolyl, substituted and unsubstituted pyridyl, substituted and unsubstituted pyrimidinyl, substituted and unsubstituted p-aminophenyl and substituted and unsubstituted C 7 -C 10 aromatic heterocyclic group.

2. The compound of claim 1 , or a pharmaceutically-acceptable salt, a stereoisomer, a hydrate or a solvate thereof, wherein the compound is selected from the group consisting of:

3. The compound of claim 1 , or a pharmaceutically-acceptable salt, a stereoisomer, a hydrate or a solvate thereof, wherein the pharmaceutically-acceptable salt is selected from the group consisting of hydrochloride, hydrobromide, formate, methanesulfonate, trifluoromethanesulfonate, sulfate, phosphate, acetate, p-toluenesulfonate, tartrate, citrate, succinate, maleate, fumarate and malate.

4. A pharmaceutical composition, comprising a pharmaceutically effective amount of the compound of claim 1 , or a pharmaceutically-acceptable salt, a stereoisomer, a hydrate or a solvate thereof, and a pharmaceutically-acceptable carrier.

5. A compound of formula (I), or a polycrystal, a eutectic or a single-enantiomer X-ray diffraction single crystal thereof:

wherein R 1 is selected from the group consisting of substituted and unsubstituted furyl, substituted and unsubstituted thienyl, substituted and unsubstituted pyrazolyl, substituted and unsubstituted imidazolyl, substituted and unsubstituted thiazolyl, substituted and unsubstituted pyridyl, substituted and unsubstituted pyrimidinyl, substituted and unsubstituted p-aminophenyl and substituted and unsubstituted C 7 -C 10 aromatic heterocyclic group.

6. The compound of claim 5 , or a polycrystal, a eutectic or a single-enantiomer X-ray diffraction single crystal thereof, wherein the compound is selected from the group consisting of:

7. A pharmaceutical composition, comprising the compound of claim 5 , or a polycrystal, a eutectic or a single-enantiomer X-ray diffraction single crystal thereof, and a pharmaceutically-acceptable carrier.

Assignees

• Univ Fudan

Inventors

• Chen Fener
• Zhuang Chunlin
• Ding Li

Classifications

• C07D401/12 Primary

  linked by a chain containing hetero atoms as chain links · CPC title

• A61P31/18

  for HIV · CPC title

• C07D239/48 Primary

  Two nitrogen atoms · CPC title

• C07D401/14 Primary

  containing three or more hetero rings · CPC title

• C07D403/12

  linked by a chain containing hetero atoms as chain links · CPC title