Patent ID: 6184244
Filing Date: 2001-02-06
Classification: A61K,A61P,C07K

Abstract:
A compound of the following formula: ##STR8##wherein:n is 1 or 2:R.sup.1 is alkyl, cycloalkyl, (cycloalkyl)atkyl, phenyl, substitutedphenyl, phenylalkyl, substitutedphenylalkyl, heteroaryl, (heteroaryl)alkyl of (CH.sub.2).sub.m CO.sub.2 R.sup.4, wherein m=1-4, and R.sup.4 is as defined below;R.sup.2 is a hydrogen atom, chloro, alkyl, cycloalkyl, (cycloalkyl)alkyl, phenyl, substitutedphenyl, phenylalkyl, substitutedphenylalkyl, heteroaryl, (heteroaryl)alkyl or (C.sub.2).sub.p CO.sub.2 R.sup.5, wherein p=0-4, and R.sup.5 is as defined below;R.sup.3 is a hydrogen atom, alkyl, cycloalkyl, (cycloalkyl)alkyl, phenylalkyl, or substitutedphenylalkyl;R.sup.4 is a hydrogen atom, alkyl, cycloalkyl, (cycloalkyl)alkyl, phenylalkyl, or substitutedphenylalkyl;R.sup.5 is a hydrogen atom, alkyl, cycloalkyl, (cycloalkyl)alkyl, phenylalkyl, or substitutedphenylalkyl;A is a natural or unnatural amino acid;B is a hydrogen atom, a deuterium atom, alkyl, cycloalkyl, (cycloalkyl)alkyl, phenyl, substitutedphenyl, phenylalkyl, substitutedphenylalkyl, heteroaryl, (heteroaryl)alkyl, halomethyl, CH.sub.2 ZR.sup.6, CH.sub.2 OCO(aryl), or CH.sub.2 OCO(heteroaryl), or CH.sub.2 OPO(R.sup.7)R.sup.8, where Z is an oxygen, OC(.dbd.O) or a sulfur atom;R.sup.6 is phenyl, substituted phenyl, phenylalkyl, (substituted phenyl)alkyl, heteroaryl or (heteroaryl)alkyl;R.sup.7 and R.sup.8 are independently selected from a group consisting of alkyl, cycloalkyl, phenyl, substituted phenyl, phenylalkyl, (substituted phenyl)alkyl and (cycloalkyl)alkyl; andX and Y are independently selected from the group consisting of a hydrogen atom, halo, trihalomethyl, amino, protected amino, an amino salt, mono-substituted amino, di-substituted amino, carboxy, protected carboxy, a carboxylate salt, hydroxy, protected hydroxy, a salt of a hydroxy group, lower alkoxy, lower alkylthio, alkyl, substituted alkyl, cycloalkyl, substituted cycloalkyl, (cycloalkyl)alkyl, substituted (cycloalkyl)alkyl, phenyl, substituted phenyl, phenylalkyl, and (substituted phenyl)alkyl;or a pharmaceutically acceptable salt or stereoisomer thereof.