Patent ID: 6495336
Filing Date: 2002-12-17
Classification: C07K,C12Q,G01N

Abstract:
A compound which is an oligopeptide derivative of the formula (I) or a salt thereof in whichR1 is (a) a hydrogen atom, a C2-8-alkanoyl group optionally having an amino group in the &ohgr; position, a phenyl-C2-4-alkanoyl group whose phenyl radical is optionally substituted in the p position by an amino group; or (b) a cyclohexylcarbonyl group which is optionally substituted in the 4 position by an aminomethyl radical, a benzoyl group which is optionally substituted in the o or p position by methyl, amino or halogen, a C1-8-alkoxycarbonyl group, a benzyloxycarbonyl group which is optionally substituted in the p position by methoxy, methyl or chlorine; or (c) a radical of the formula â€”SO2â€”R5 where R5 can be a C1-6-alkyl radical, an optionally substituted aryl or heteroaryl radical or a radical of a bicyclic terpene derivative; or (d) a group of the formula â€”COâ€”CH(R6)â€”NHâ€”R7, where R6 is hydrogen, a C1-6-alkyl radical, a 1- or 2-hydroxyethyl radical, a methylmercaptoethyl radical, an aminobutyl radical, a guanidinopropyl radical, a carboxy-C1-4-alkyl radical, a carboxamido-C1-4-alkyl radical, a phenyl-C1-4-alkyl radical whose phenyl radical is optionally substituted by OH, halogen, C1-4-alkyl or methoxy, or a cyclohexyl or cyclohexylmethyl radical whose ring is option-ally substituted by OH, halogen, C1-4-alkyl or methoxy, or a nitrogen-containing heteroaryl-C1-4-alkyl radical with 3 to 8 carbon atoms in the heterocyclic system, where the group â€”COâ€”CH(R6)â€”NHâ€”R7 may be racemic or have the D or L configuration, and R7 can be a group of type (a), (b) or (c); or (e) a group of the formula wherein m can be 1 or 2, and one of the methylene groups can be substituted by hydroxyl, carboxyl, C1-4-alkyl or aryl-C1-4-alkyl; R2 is hydrogen, C1-6-alkyl, C1-2-hydroxyalkyl, C1-4-alkoxy-C1-6-alkyl, benzyloxy-C1-2-alkyl, an &ohgr;-carboxy-C1-3-alkyl radical, an &ohgr;-C1-4-alkoxy-carbonyl-C1-3-alkyl radical, an &ohgr;-benzyloxycarbonyl-C1-3-alkyl radical or a cyclohexyl, cyclohexylmethyl, 4-hydroxycyclohexylmethyl, phenyl, benzyl, 4-hydroxybenzyl or imidazolyl-4-methyl radical; R3 is (a) hydrogen or C1-4-alkyl and R3 is hydrogen; or (b) together with R3 a tri- or tetramethylene group, where one of the methylene groups can be substituted by hydroxyl, carboxyl, C1-4-alkyl or aryl-C1-4-alkyl; and R4 is (a) an aniline residue of the formula where R8 can be hydroxyl and R9 can be hydrogen, halogen, amino, C1-4-alkyl, C1-4-alkoxy or C1-4-alkanoyl; or (b) a quinoline residue of the formula where one of R10, R11 and R12 is an â€”NH group via which the quinoline residue is linked to the Arg residue, another can be hydroxyl or amino, and the other can be hydrogen, hydroxyl or amino.