Pyridinylcyanoguanidine derivative and use thereof
US11873284B2 · kind B2 · utility
Assignees
Inventors
Key dates
| Filing date | Dec 13, 2022 |
| Grant date | Jan 16, 2024 |
| Priority date | — |
| Expiry date | Dec 13, 2042 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07D409/14
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
The present invention discloses a pyridinylcyanoguanidine derivative or a pharmaceutically acceptable salt thereof, which is useful as an NAMPT inhibitor, and useful as a potential agent for the chemotherapy of a variety of diseases associated with abnormal NAD+ expression. The pyridinylcyanoguanidine derivative has a parent structure including cyanoguanidine attached to piperazine or pyrrolidine by an intermediate aliphatic chain, to which a side arylformyl (or heterocyclylformyl) group and pyridinyl (or substituted pyridinyl) group are attached. This structure comes from the structural optimization of FK866, a high-efficiency NAMPT inhibitor. In the structure, the substituted formyl piperazine and substituted formyl pyrrolidine are the further optimizations on the basis of FK866, which strengthens the interaction with NAMPT. The introduction of cyanoguanidine structure not only further enhances the affinity with NAMPT, but also improves the disadvantage of poor water solubility of FK866, which is more conducive to the subsequent drug test.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.