4 h-3, 1-benzoxazin-4-ones and related compounds

Details 4 h-3, 1-benzoxazin-4-ones and related compounds 4 h-3, 1-benzoxazin-4-ones and related compounds

C - Chemistry, Metallurgy

07

D

167/215, 530/5.0

C07D 265/24 (2006.01) A61K 31/535 (2006.01) C07C 273/18 (2006.01) C07K 5/06 (2006.01) C07K 5/078 (2006.01) C07K 5/08 (2006.01) C07K 5/097 (2006.01) C07K 5/103 (2006.01) C07K 7/06 (2006.01) A61K 38/00 (2006.01) C07C 275/42 (2006.01)

Patent

CA 1269800

24220-FF ABSTRACT OF THE DISCLOSURE Novel 2-amino-4H-3,1-benzoxazin-4-ones represented by the formula Image and the pharmaceutically acceptable esters and salts thereof wherein R1 is hydrogen or lower alkyl; R2 and R3 are each independently hydrogen, halo, lower alkyl, hydroxy, lower alkoxy, lower thioalkyl, -NO2, -N(R')2, -NR'COR', -NHCON(R')2 or -NHCOOR', with the proviso that at least one of R1, R2 and R3 is not hydrogen when X is NHR or NR'COR''; and X is a radical chosen from the group consisting of: Image -AN(R')2 and -AOR' (A) (B) (C) (D) in which: R is lower alkyl, lower alkenyl, lower alkynyl, optionally substituted lower cycloalkyl or optionally substituted phenyl lower alkyl; each R' is independently hydrogen or lower alkyl, or lower alkenyl or lower alkynyl where the unsaturated bond is at least one carbon removed from the O or N atom; each R'' is independently R, lower alkoxy, NHR' or AOR'; and A is an amino acid residue, or a peptide of 2 to amino acid residues, are useful as enzyme inhibitors in animals.

470962

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