Patent ID: 6683648
Filing Date: 2004-01-27
Classification: C07C,C07D,C07K

Abstract:
A compound represented by the formula: or a pharmaceutically acceptable salt, or ester thereof wherein:R and Râ€² together with the nitrogen to which they are attached form a pyrrolidinyl; R1 represents hydrogen, â€”CH2SO2NH2, â€”CH2CO2 CH3, â€”CO2CH3, â€”CONH2, â€”CH2 C(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 and cycloalkyl radicals, and amino acid side chains selected from asparagine, S-methyl cysteine and methionine and the sulfoxide (SO) and sulfone (SO2) derivatives thereof, isoleucine, allo-isoleucine, alanine, leucine, tert-leucine, phenylalanine, ornithine, histidine, norleucine, glutamine, threonine, glycine, allo-threonine, serine, O-alkyl serine, aspartic acid, beta-cyanoalanine and valine side chains; R2 represents alkyl, aryl, cycloalkyl, cycloalkylalkyl and aralkyl radicals, which radicals are optionally substituted with a group selected from alkyl and halogen radials, â€”NO2, â€”CN, â€”CF3, â€”OR9 and â€”SR9, wherein R9 represents hydrogen and alkyl radicals, and halogen radicals; R3 represents 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, and thioalkyl, alkylthioalkyl and arylthioalkyl radicals and the sulfone and sulfoxide derivatives thereof; and R4 represents hydrogen and radicals as defined by R3; R6 represents hydrogen and alkyl radicals; R7 and R7â€² independently represent hydrogen and radicals as defined for R3; amino acid side chains selected from the group consisting of valine, isoleucine, glycine, alanine, allo-isoleucine, asparagine, leucine, glutamine, and t-butylglycine; radicals represented by the formulas â€”C(O)R16, â€”CO2R16, â€”SO2R16, â€”SR16, â€”CONR16R17, â€”CF3 and â€”NR16R17; or R7 and R7â€² together with the carbon atom to which they are attached form a cycloalkyl radical; R8 represents cyano, hydroxyl, alkyl, alkoxy, cycloalkyl, aryl, aralkyl, heterocycloalkyl and heteroaryl radicals and radicals represented by the formulas C(O)R16, CO2R16, SO2R16, SR16, CONR16R17, CF3 and NR16R17; wherein R16 and R17 independently represent hydrogen and radicals as defined for R3, or R16 and R17 together with a nitrogen to which they are attached in the formula NR16R17 represent heterocycloalkyl and heteroaryl radicals; x represents 1 or 2; n represents an integer of from 0 to 6.