Patent ID: 6469207
Filing Date: 2002-10-22
Classification: C07C

Abstract:
Compound represented by the formula: or a pharmaceutically acceptable salt, prodrug or ester thereof, wherein:R1 represents hydrogen, â€”CH2SO2NH2, â€”CO2CH3, â€”CONHCH3, â€”CON(CH3)2, â€”CH2C(O)NHCH3, â€”CH2C(O)N(CH3)2, â€”CONH2, 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 and cycloalkyl radicals and amino acid side chains selected from asparagine, S-methyl cysteine and the corresponding sulfoxide and sulfone derivatives thereof, glycine, leucine, isoleucine, allo-isoleucine, tert-leucine, phenylalanine, ornithine, alanine, histidine, norleucine, glutamine, valine, threonine, serine, aspartic acid, beta-cyano alanine, and allothreonine; R2 represents alkyl, aryl, cycloalkyl, cycloalkylalkyl, and aralkyl radicals, which radicals are optionally substituted with a group selected from halogen and alkyl radicals, â€”NO2, â€”Câ‰¡N, CF3, â€”OR9 and â€”SR9 wherein R9 represents hydrogen and alkyl radicals; R3 represents hydrogen, alkyl, haloalkyl, alkenyl, alkynyl, hydroxyalkyl, alkoxyalkyl, cycloalkyl, cycloalkylalkyl, heterocycloalkyl, heteroaryl, heterocycloalkylalkyl, aryl, aralkyl, heteroaralkyl, aminoalkyl and mono- and 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; R4 represents radicals as defined by R3 except hydrogen; R30, R31 and R32 represent radicals as defined for R1, or one of R1 and R30 together with one of R31 and R32 and the carbon atoms to which they are attached form a cycloalkyl radical; R33 and R34 independently represent hydrogen and radicals as defined for R3, or R33 and R34 together with the nitrogen atom to which they are attached represent heterocycloalkyl and heteroaryl radicals; and Y and Yâ€² independently represent O, S, and NR15 wherein R15 represents hydrogen and radicals as defined for R3; and wherein the absolute stereochemistry about the hydroxyl group is designated as (R).