Patent ID: 6596728
Filing Date: 2003-07-22
Classification: A61P,C07D

Abstract:
A compound of the formula (I), or a salt thereof, in whichZ is â€”NHâ€”(C1-C16-alkyl)-(C&boxH;O)â€”; â€”(C&boxH;O)â€”(C1-C16-alkyl)-(C&boxH;O)â€”; or â€”(C&boxH;O)-phenyl-(C&boxH;O)â€”; A1, A2, A3, A4, each independently of one another is the D- or L-form of alanine, glycine, proline, cysteine, histidine, glutamine, aspartic acid, isoleucine, arginine, glutamic acid, lysine, serine, phenylalanine, leucine, threonine, tryptophan, methionine, valine, tyrosine, asparagine, 2-aminoadipic acid, 2-aminoisobutyric acid, 3-aminoadipic acid, 3-aminoisobutyric acid, beta-alanine, 2-aminopimelic acid, 2-aminobutyric acid, 2,4-diaminobutyric acid, 4-aminobutyric acid, desmosine, piperidic acid, 2,2-diaminopimelic acid, 6-aminocaproic acid, 2,3-diaminopropionic acid, 2-aminoheptanoic acid, N-ethylglycine, 2-(2-thienyl)-glycine, 3-(2-thienyl)-alanine, penicillamine, sarcosine, N-ethylasparagine, N-methylisoleucine, hydroxylysine, 6-N-methyllysine, allo-hydroxylysine, N-methylvaline, 3-hydroxyproline, norvaline, 4-hydroxyproline, norleucine, isodesmosine, ornithine, allo-isoleucine, 3-(2-naphthyl)alanine, azaglycine, N-cyclohexylglycine, or 2,4-diaminobutyric acid, E is â€”SO2â€”R4, â€”COâ€”R4; R is phenyl, thiazolyl, oxazolyl, thienyl, thiophenyl, furanyl, pyridyl, or pyrimidyl, wherein the rings are unsubstituted, or are substituted up to 3 times by F, Cl, Br, OH, CF3, NO2, CN, OCF3, â€”(C1-C6)-alkyl, â€”Oâ€”(C1-C6)-alkyl, â€”Sâ€”(C1-C6)-alkyl, â€”SOâ€”(C1-C6)-alkyl, â€”SO2â€”(C1-C6)-alkyl, â€”(C1-C6)-alkyl, â€”(C3-C6)-cycloalkyl, â€”COOH, â€”COO(C1-C6)alkyl, â€”COO(C3-C6)cycloalkyl, â€”CONH2, â€”CONH(C1-C6)alkyl, â€”CON[(C1-C6)alkyl]2, â€”CONH(C3-C6)cycloalkyl, â€”NH2, â€”NHâ€”COâ€”(C1-C6)-alkyl, or â€”NHâ€”CO-phenyl; R2 is H, â€”OH, â€”CH2OH, or â€”OMe; R3 is H, F, methyl, or â€”OMe; R4 is â€”(C1-C16-alkyl), â€”(C0-C16-alkylene)-R5, â€”(C&boxH;O)â€”(C0-C16-alkylene)-R5, â€”(C&boxH;O)â€”(C0-C16-alkylene)-NHâ€”R5, â€”(C1-C8-alkenylene)-R5, â€”(C1-C8-alkynyl), â€”(C1-C4-alkylene)-S(O)râ€”R5, â€”(C1-C4-alkylene)-Oâ€”R5, or â€”(C1-C4-alkylene)-NHâ€”R5; R5 is â€”COOâ€”R6, â€”(C&boxH;O)â€”R6, â€”(C1-C6-alkylene)-R7, â€”(C1-C6-alkenylene)-R7, â€”(C1-C7)-cycloalkyl, phenyl, naphthyl, thienyl, thiophenyl, furanyl, pyridyl, pyrimidyl, dihydropyrimidine-2,4-dion-6-yl, chromanyl, phthalimidoyl, or thiazolyl, wherein the rings are unsubstituted, or are substituted up to 3 times by F, Cl, Br, â€”OH, â€”CF3, â€”NO2, â€”CN, â€”OCF3, â€”(C1-C6)-alkyl, â€”Oâ€”(C1-C6)-alkyl, â€”Sâ€”(C1-C6)-alkyl, â€”SOâ€”(C1-C6)-alkyl, â€”SO2â€”(C1-C6)-alkyl, â€”(C1-C6)-alkyl, â€”(C3-C6)-cycloalkyl, â€”COOH, â€”COO(C1-C6)alkyl, â€”COO(C3-C6)cycloalkyl, â€”CONH2, â€”CONH(C1-C6)alkyl, â€”CON[(C1-C6)alkyl]2, â€”CONH(C3-C6)cycloalkyl, â€”NH2, â€”NHâ€”COâ€”(C1-C6)-alkyl, â€”NHâ€”CO-phenyl, or pyridyl; R6 is H or â€”(C1-C6)alkyl; R7 is H, â€”(C1-C7)-cycloalkyl, phenyl, naphthyl, thienyl, thiophenyl, furanyl, pyridyl, pyrimidyl, dihydropyrimidine-2,4-dion-6-yl, chromanyl, phthalimidoyl, or thiazolyl, wherein the rings are unsubstituted, or are substituted up to 3 times by F, Cl, Br, OH, CF3, NO2, CN, OCF3, â€”(C1-C6)-alkyl, â€”Oâ€”(C1-C6)-alkyl, â€”Sâ€”(C1-C6)-alkyl, â€”SOâ€”(C1-C6)-alkyl, â€”SO2â€”(C1-C6)-alkyl, â€”(C1-C6)-alkyl, â€”(C3-C6)-cycloalkyl, â€”COOH, â€”COO(C1-C6)alkyl, â€”COO(C3-C6)cycloalkyl, â€”CONH2, â€”CONH(C1-C6)alkyl, â€”CON[(C1-C6)alkyl]2, â€”CONH(C3-C6)cycloalkyl, â€”NH2, â€”NHâ€”COâ€”(C1-C6)-alkyl, or â€”NHâ€”CO-phenyl; l, q, m, n, o, p each independently of one another is 0 or 1, where l+q+m+n+o+p is greater than or equal to 1; r is 0, 1, or 2; with the proviso that in formula (I), when R1 is unsubstituted phenyl, R2 is H, R3 is H, and l, m, n, o, and p are all zero, then R4 is other than â€”CH3 or â€”C(CH3)3.