Invention Grant
US08067452B2 3-hydroxyisothiazole-4-carboxamidine derivatives as CHK2 inhibitors
有权
3-羟基异噻唑-4-甲脒衍生物作为CHK2抑制剂
- Patent Title: 3-hydroxyisothiazole-4-carboxamidine derivatives as CHK2 inhibitors
- Patent Title (中): 3-羟基异噻唑-4-甲脒衍生物作为CHK2抑制剂
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Application No.: US12143672Application Date: 2008-06-20
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Publication No.: US08067452B2Publication Date: 2011-11-29
- Inventor: Jim Zhen Wu , Huanming Chen
- Applicant: Jim Zhen Wu , Huanming Chen
- Applicant Address: US CA Aliso Viejo
- Assignee: Valeant Pharmaceuticals International
- Current Assignee: Valeant Pharmaceuticals International
- Current Assignee Address: US CA Aliso Viejo
- Agency: Jones Day
- Main IPC: A61K31/425
- IPC: A61K31/425 ; C07D275/03

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.
Public/Granted literature
- US20090137041A1 3-HYDROXYISOTHIAZOLE-4-CARBOXAMIDINE DERIVATIVES AS CHK2 INHIBITORS Public/Granted day:2009-05-28
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