3-hydroxyisothiazole-4-carboxamidine derivatives as CHK2...

Details 3-hydroxyisothiazole-4-carboxamidine derivatives as CHK2... 3-hydroxyisothiazole-4-carboxamidine derivatives as CHK2...

2008-06-20

2011-11-29

Nolan, Jason M (Department: 1626)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

C548S213000

Reexamination Certificate

active

08067452

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.

REFERENCES:
patent: 7429667 (2008-09-01), Abdellaoui et al.
patent: 7652047 (2010-01-01), Abdellaoui et al.
El Abdellaoui et al. Bioorganic & Medicinal Chem. Lett. 2006, 16(21), 5561-66.
Carlessi et al. Molecular Cancer Therapeutics 2007, 6(3), 935-44.
Larson, et al., “Identification of novel, selective and potent Chk2 inhibitors,”Bioorganic&Med. Chem Ltrs12:172-175 (2007).

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