2-polysubstituted aromatic ring-pyrimidine derivatives, preparation and medical application thereof
US11591325B2 · kind B2 · utility
Assignees
Inventors
Key dates
| Filing date | Nov 8, 2017 |
| Grant date | Feb 28, 2023 |
| Priority date | — |
| Expiry date | Oct 15, 2039 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07D417/14
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
The present invention provides a 2-polysubstituted aromatic ring-pyrimidine derivative and an optical isomer thereof, or a pharmaceutically acceptable salt or solvate thereof, the compound, and an optical isomer thereof or a pharmaceutically thereof acceptable salts or solvates can be used in the preparation of anti-tumor drugs. The invention designs and synthesizes a series of novel small molecule Chk1 inhibitors by using N-substituted pyridin-2-aminopyrimidine obtained by structure-based virtual screening as a lead compound, and carries out Chk1 kinase inhibitory activity test. The experiment confirmed that said compounds possess potent anticancer activity, Chk1 kinase inhibitory activity, and are promising Chk1 inhibitors, and can be used as new cancer therapeutic drugs, which can be applied to treat solid tumors or hematologic tumors related to proliferative disease of human or animal. The 2-polysubstituted aromatic ring-pyrimidine derivatives provided by the present invention has the structure of the formula I:
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.