3-hydroxyisothiazole-4-carboxamidine derivatives as CHK2 inhibitors
US8067452B2 · kind B2 · utility
Assignee
Inventors
Key dates
| Filing date | Jun 20, 2008 |
| Grant date | Nov 29, 2011 |
| Priority date | — |
| Expiry date | May 8, 2029 |
Classification
- Technology area (CPC A)Human Necessities
- CPC primaryA61P39/00
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
This invention provides compounds of Formula I which are inhibitors of Chk2 and are useful as a radiation protection agents in anticancer radiotherapy. A method of modulating Chk2 in vitro includes treating a substrate with Chk2 in the presence of compounds of formula I. A method of making a compound of formula I includes: a) forming a biaryl amine having an amino (NH2) group; b) converting the amino group to an isothiocyanate group; c) adding a cyanoacetamide to the isothiocyanate group to form a thioamide adduct; d) cyclizing the thioamide adduct to form an isothiazole having a cyano group; and e) adding an amine to the cyano group to form a carboxamidine group.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.