Patent ID: 6777408
Filing Date: 2004-08-17
Classification: A61P,C07D

Abstract:
A compound of the formula in racemic, or enantiomeric or diastereoisomeric form or mixtures thereof,wherein R1 is hydrogen or Râ€²1â€”NHâ€”C(Y)â€”; Râ€²1 is unsubstituted or substituted aryl or heteroaryl; R2 is selected from the group consisting of alkyl of 1 to 6 carbon atoms, trifluoromethyl and phenyl unsubstituted or substituted with at least one member of the group consisting of hydroxy, halo, lower alkyl anrd lower alkoxy of 1 to 6 carbon atoms, X and Y are independently O or S; R3a is selected from the group consisting of hydrogen, alkyl of 1 to 6 carbon atoms, hydroxy and â€”OC(O)Râ€²3a; Râ€²3a is alkyl of 1 to 10 carbon atoms unsubstituted or substituted with at least one member of the group consisting of: cycloalkyl; heterocycloalkyl; aryl; heteroaryl; guanidyl unsubstituted or substituted by nitro or cyano; or â€”NRâ€³3aRâ€²â€³3a; Râ€³3a and Râ€²â€³3a are individually selected from the group consisting of hydrogen, lower alkyl, aryl, lower arylalkyl, lower heteroarylalkyl, alkylcarbonyl and alkoxycarbonyl; R3b is hydrogen or alkyl of 1 to 6 carbon atoms; R4 is â€”(CH2)nâ€”CHRâ€²4Râ€³4; n is an integer from 0 to 6; Râ€²4 and Râ€³4 are individually selected from the group consisting of hydrogen, alkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 6 carbon atoms, lower cycloalkyl alkyl, aryl, lower aralkyl, heteroaryl, lower heteroarylalkyl, arylcarbonyl and adamantyl, all unsubstituted or substituted;Aâ€”B is â€”C&boxH;Nâ€” or â€”Câ€”N(R5)â€”; R5 is selected from the group consisting of hydrogen, alkyl of 1 to 6 carbon atoms, alkenyl of up to 6 carbon atoms and â€”C(O)â€”(CH2)pâ€”Râ€²5; Râ€²5 is selected from the group consisting of hydrogen, amino, lower alkyl amino, di(lower alkyl)amino, cycloalkyl, heterocycloalkyl guanidyl unsubstituted or substituted by nitro or cyano, aryl optionally substituted, heteroaryl and â€”NHâ€”C(O)â€”(CH2)câ€”NHâ€”C(O)â€”(CH2)dâ€”NH2; p is an integer from 0 to 10; c and d are independently 0, 1, 2 or 3; and a non-toxic, pharmaceutically acceptable acid addition salt thereof.