Patent ID: 6630451
Filing Date: 2003-10-07
Classification: A61K,C07D,C07K,H01L,H05K

Abstract:
A compound of the following formula (I): wherein:A1 and A2 are each independently a D- or L-amino acid selected from the group consisting of alanine, &bgr;-alanine, arginine, homoarginine, cyclohexylalanine, citrulline, cysteine (optionally substituted with C1-C4 alkyl, aryl, or arC1-C4 alkyl), 2,4-diaminobutyric acid (optionally substituted with acyl, C1-C4 alkyl, aroyl, amidino, or MeC(NH)â€”), 2,3 diaminopropionic acid (optionally substituted with acyl, C1-C4 alkyl, aroyl, amidino, or MeC(NH)â€”), glutamine, glycine, indanylglycine, lysine (optionally substituted with acyl, C1-C4 alkyl, aroyl, or MeC(NH)â€”), valine, methionine, proline, serine (optionally substituted with C1-C4 alkyl, aryl, or arC1-C4 alkyl), homoserine (optionally substituted with C1-C4 alkyl, aryl, or arC1-C4 alkyl), tetrahydroisoquinoline-3-COOH, threonine (optionally substituted with C1-C4 alkyl, aryl, or arC1-C4 alkyl), ornithine (optionally substituted with acyl, C1-C4 alkyl, aroyl, or MeC(NH)â€”), and an unsubstituted or substituted aromatic amino acid selected from the group consisting of phenylalanine, heteroarylalanine, naphthylalanine, homophenylalanine, histidine, tryptophan, tyrosine, arylglycine, heteroarylglycine, aryl-&bgr;-alanine, and heteroaryl-&bgr;-alanine wherein one or more of the substituents on the aromatic amino acid are independently selected from the group consisting of halogen, C1-C4 alkyl, C1-C4 alkoxy, hydroxy, C1-C4 alkoxycarbonyl, amino, amidino, guanidino, fluorinated C1-C4 alkyl, fluorinated C1-C4 alkoxy, C1-C4 alkylsulfonyl, C1-C4 alkylcarbonyl, cyano, aryl, heteroaryl, arC1-C4 alkyl, C2-C4 alkenyl, alkynyl, and nitro; R1 is selected from the group consisting of amino, C1-C8 alkylamino, C1-C8 dialkylamino, arylamino, arC1-C8 alkylamino, C3-C8 cycloalkylamino, heteroalkylC1-C8 alkylamino, heteroalkylC1-C8 alkyl-N-methylamino, C1-C8 dialkylaminoC1-C8 alkylamino, â€”N(C1-C8alkyl)â€”C1-C8 alkyl-N(C1-C8alkyl)2, N(C1-C8 alkyl) (C1-C8 alkenyl), â€”N(C1-C8alkyl) (C3-C8cycloalkyl), heteroalkyl and substituted heteroalkyl wherein the substituent on the heteroalkyl is selected from the group consisting of oxo, amino, C1-C8 alkoxyC1-C8 alkyl, C1-C8 alkylamino and C1-C8 dialkylamino; R2 and R3 are each independently selected from the group consisting of hydrogen, C1-C8 alkyl, C3-C8 cycloalkyl, C3-C8 cycloalkylC1-C8 alkyl, aryl, heteroalkyl, substituted heteroalkyl (wherein the substituent on the heteroalkyl is one or more substituents independently selected from the group consisting of C1-C8 alkoxycarbonyl, C1-C8 alkyl, and C1-C4 alkylcarbonyl), heteroalkylC1-C8 alkyl, indanyl, acetamidinoC1-C8 alkyl, aminoC1-C8 alkyl, C1-C8 alkylaminoC1-C8 alkyl, C1-C8 dialkylaminoC1-C8 alkyl, unsubstituted or substituted heteroarylC1-C8 alkyl and unsubstituted or substituted arC1-C8 alkyl, wherein the substituent on the aralkyl or heteroarylalkyl group is one or more substituents independently selected from the group consisting of halogen, nitro, amino, C1-C8 alkyl, C1-C8 alkoxy, hydroxy, cyano, C1-C4 alkylcarbonyl, C1-C8 alkoxycarbonyl, hydroxyC1-C8 alkyl and aminosulfonyl; or R2 and R3, together with the nitrogen to which they are attached, alternatively form an unsubstituted or substituted heteroalkyl group selected from the group consisting of piperidinyl, piperazinyl, morpholinyl and pyrrolidinyl, wherein the substituent is one or more substituents independently selected from the group consisting of C1-C8alkyl C1-C8 alkoxycarbonyl and C1-C4 alkylcarbonyl; R4 is selected from the group consisting of unsubstituted or substituted aryl, arC1-C8 alkyl, C3-C8 cycloalkyl, and heteroaryl, where one or more of the substituents on the aryl, arC1-C8alkyl, cycloalkyl or heteroaryl group are independently selected from the group consisting of halogen, nitro, amino, cyano, hydroxyalkyl, C1-C8 alkyl, C1-C8 alkoxy, hydroxy, C1-C4 alkylcarbonyl, C1-C8 alkoxycarbonyl, fluorinated C1-C4 alkyl, fluorinated C1-C4 alkoxy, and C1-C4 alkylsulfonyl; R5 is selected from the group consisting of hydrogen and C1-C8 alkyl; X is oxygen or sulfur; m is an integer selected from the group consisting of 0, 1, 2 and 3; n is an integer selected from the group consisting of 2 and 3; and p is an integer selected from the group consisting of 0 and 1; or a pharmaceutically acceptable salt thereof.