Patent ID: 6172044
Filing Date: 2001-01-09
Classification: A61K,C07K,Y10S

Abstract:
A compound of the formulae ##STR42##whereinR.sub.1 is (C.sub.1 -C.sub.4)alkyl;R.sub.2 is (C.sub.1 -C.sub.4)alkyl, phenyl, benzyl, cyclohexyl or cyclohexylmethyl;X is --CO.sub.2 R.sub.3 wherein R.sub.3 is (C.sub.1 -C.sub.4)alkyl, phenyl, benzyl, cyclohexyl or cyclohexylmethyl;P.sub.2 Gly or Ala where the nitrogen of the .alpha.-amino group is optionally substituted with an R group where R is (C.sub.1 -C.sub.6)alkyl, (C.sub.3 -C.sub.12)cycloalkyl, (C.sub.3 -C.sub.12)cycloalkyl(C.sub.1 -C.sub.6)alkyl, (C.sub.4 -C.sub.11)bicycloalkyl, (C.sub.4 -C.sub.11)bicycloalkyl(C.sub.1 -C.sub.6)alkyl, (C.sub.6 -C.sub.10)aryl, (C.sub.6 -C.sub.10)aryl(C.sub.1 -C.sub.6)alkyl, (C.sub.3 -C.sub.7)heterocycloalkyl, (C.sub.3 -C.sub.7)heterocycloalkyl(C.sub.1 -C.sub.6)alkyl, (C.sub.5 -C.sub.9)heteroaryl, (C.sub.5 -C.sub.9)heteroaryl(C.sub.1 -C.sub.6)alkyl, fused (C.sub.6 -C.sub.10)aryl(C.sub.3 -C.sub.12)cycloalkyl, fused (C.sub.6 -C.sub.10)aryl(C.sub.3 -C.sub.12)cycloalkyl(C.sub.1 -C.sub.6)alkyl, fused (C.sub.5 -C.sub.9)heteroaryl(C.sub.3 -C.sub.12)cycloalkyl, or fused (C.sub.5 -C.sub.9)heteroaryl(C.sub.3 -C.sub.12)cycloalkyl(C.sub.1 -C.sub.6)alkyl, or P.sub.2 is Pro, Aze, Ind, Tic, Pip, Tca, Pro(4-OBzl), Pro(4-OAc), Pro(4-OH);P.sub.3 is Ala, bAla, Leu, Ile, Nle, Val, Nva, Lys or bVal;P.sub.4 is Ala, bAla, Val, Nva, bVal, Pro or is deleted;K is hydrogen, acetyl, succinyl, benzoyl, t-butyloxycarbonyl, carbobenzyloxy, dansyl, isovaleryl, methoxysuccinyl, 1-adamantanesulphonyl, 1-adamantaneacetyl, 2-carboxybenzoyl, --C(O)N(CH.sub.3).sub.2, 4-((chlorophenyl)sulfonylaminocarbonyl)-phenylcarbonyl, 4-((4-bromophenyl)sulfonylaminocarbonyl)phenylcarbonyl, 4-(sulfonylaminocarbonyl)phenylcarbonyl or is a group of the formulae ##STR43##wherein Z is N or CH, B is a group of the formulae ##STR44##R' is a hydrogen or a (C.sub.1 -C.sub.4)alkyl group;n is zero or the integers 1 or 2;or a hydrate or a pharmaceutically acceptable salt thereof.