Patent ID: 6534493
Filing Date: 2003-03-18
Classification: A61K,A61P,C07C,C07D,C07K

Abstract:
Compound represented by the formula: wherein:R represents hydrogen, alkoxycarbonyl, aralkoxycarbonyl, alkylcarbonyl, cycloalkylcarbonyl, cycloalkylalkoxycarbonyl, cycloalkylalkanoyl, alkanoyl, aralkanoyl, aroyl, aryloxycarbonyl, aryloxycarbonylalkyl, aryloxyalkanoyl, heterocyclylcarbonyl, heterocyclyloxycarbonyl, heterocyclylalkanoyl, heterocyclylalkoxycarbonyl, heteroaralkanoyl, heteroaralkoxycarbonyl, heteroaryloxycarbonyl, heteroaroyl, alkyl, alkenyl, cycloalkyl, aryl, aralkyl, aryloxyalkyl, heteroaryloxyalkyl, hydroxyalkyl, aminocarbonyl, aminoalkanoyl, or mono- or disubstituted aminocarbonyl or mono- or disubstituted aminoalkanoyl radicals, wherein the substituents are selected from alkyl, aryl, aralkyl, cycloalkyl, cycloalkylalkyl, heteroaryl, heteroaralkyl, heterocycloalkyl, and heterocycloalkylalkyl radicals, or where said aminoalkanoyl radical is disubstituted, said substituents along with the nitrogen atom to which they are attached form a heterocycloalkyl or heteroaryl radical; Râ€² represents hydrogen or radicals as defined for R3 or R and Râ€² together with the nitrogen to which they are attached represent heterocycloalkyl or heteroaryl radical; R1 represents hydrogen, â€”CH2SO2NH2, â€”CH2CO2CH3, â€”CO2CH3, â€”CONH2, â€”CH2C(O)NHCH3, â€”C(CH3)2(SH), â€”C(CH3)2(SCH3), â€”C(CH3)2(S[O]CH3), â€”C(CH3)2(S[O]2CH3), alkyl, haloalkyl, alkenyl, alkynyl or cycloalkyl radicals, or amino acid side chains selected from asparagine, S-methyl cysteine and the sulfoxide (SO) and sulfone (SO2) derivatives thereof, isoleucine, allo-isoleucine, alanine, leucine, tert-leucine, phenylalanine, omithine, histidine, norleucine, glutamine, threonine, glycine, allo-threonine, serine, O-methyl serine, asparatic acid, beta-cyano alanine and valine side chains; R2 represents (i) alkyl, (ii) aryl, (iii) cycloalkyl, (iv) cycloalkylalkyl or (v) aralkyl radicals, which radicals (i)-(v) are optionally substituted with a group selected from alkyl and halogen radicals, â€”NO2, â€”Câ‰¡N, CF3, â€”OR9, and â€”SR9, wherein R9 represents hydrogen or alkyl radicals, or (vi) halogen radicals; R3 represents alkyl, haloalkyl, alkenyl, alkynyl, hydroxyalkyl, alkoxyalkyl, cycloalkyl, cycloalkylalkyl, heterocycloalkyl, heteroaryl, heterocycloalkylalkyl, aryl, aralkyl, heteroaralkyl, aminoalkyl or mono- or disubstituted aminoalkyl radicals, wherein said substituents are selected from alkyl, aryl, aralkyl, cycloalkyl, cycloalkylalkyl, heteroaryl, heteroaralkyl, heterocycloalkyl, and heterocycloalkylalkyl radicals, or in the case of a disubstituted aminoalkyl radical, said substituents along with the nitrogen atom to which they are attached, form a heterocycloalkyl or a heteroaryl radical; and R4 represents radicals as defined by R3.