Patent ID: 6297354
Filing Date: 2001-10-02
Classification: A61K,C07K

Abstract:
A compound of the formula: ##STR9##or a pharmaceutically acceptable salt, ester, or prodrug thereof, wherein:R is of the formula: ##STR10##wherein X is hydrogen, lower alkyl, alkoxy, or a halide selected from the group consisting of bromide, chloride, fluoride, and iodide; Y is hydrogen or loweralkyl; and n is 1-3;A is an amino acid residue selected from the group consisting of:3-(1-naphthyl)-D-alanyl,3-(1-naphthyl)-L-alanyl,D-tryptyl,D-3-(4,4'-biphenyl)alanylD-(benzthienyl)alanyl, andglycyl;B is seryl or glycyl;C is an amino acid residue selected from the group consisting of:(N-epsilon-nicotinyl)lysyl,N-methylphenylalanyl,(4-N-nitro)-N-methylphenylalanyl,[4-(3-amino-1,2,4-triazol-5-yl)]phenylalanyl,[4-(3-amino-1,2,4-triazol-5-yl)]-N-methylphenylalanyl,(4-N-acetyl)-N-methylphenylalanyl,(4-N-acetyl)-N-phenylalanyl,1,2,3,4-tetrahydroisoquinoline-7-hydroxy-3-carbonyl1,2,3,4-tetrahydroisoquinoline-3-carbonylarginyl,sarcosyl,tyrosyl, andN-methyltyrosyl;or where B and C taken together form an amino acid derivative having the formula: ##STR11##D is an amino acid residue selected from the group consisting of:D-arginyl,D-citrullyl,glycyl,D-homocitrullyl,D-diethyl-homoarginyl,D-(N-epsilon-nicotinyl)lysyl,N-methylphenylalanyl,phenylalanyl,D-phenylalanyl,D-tryptyl,D-[4-(3-amino-1,2,4-triazol-5-yl)]-phenylalanyl, andD-(4-N-acetyl)-phenylalanyl;E is an amino acid residue selected from the group consisting of:cyclohexylalanyl,glycyl,leucyl, andN-methylleucyl;or where D and E taken together form an amino acid derivative having the formula: ##STR12##R.sub.1 is selected from the group consisting of --NH(CH.sub.2).sub.l R.sup.2, --NR.sup.3 --(CH.sub.2).sub.m --NHR.sup.4, --NH--(CH.sub.2).sub.n --NR.sup.5 R.sup.6 and --NH--(CH.sub.2).sub.p --NH--C(.dbd.NH)--NH.sub.2 ; wherein:l is 0-10, m is 1-2, n is 1-10, p is 1-10;R.sup.2 is hydrogen, hydroxy, amino, amido, methyl, or phenyl;R.sup.3 is hydrogen, methyl, or ethyl;R.sup.4 is hydrogen, methyl, amino or amido; andR.sup.5 and R.sup.6 taken together with the nitrogen atom to which each is attachedform an aromatic or non-aromatic ring, having at least one nitrogen atom, selected from the group consisting of morpholinyl, piperidinyl, pyridyl, pyridinyl, pyrrolyl, pyrrolidinyl, pyrrolidinonyl, and quinuclidinyl.