Patent ID: 6291453
Filing Date: 2001-09-18
Classification: C07D

Abstract:
A compound of formula I: ##STR9##whereR.sup.1 is selected from the group consisting of alkyl, substituted alkyl, aryl, substituted aryl, cycloalkyl, substituted cycloalkyl, heterocyclic, substituted heterocylic, heteroaryl and substituted heteroaryl;R.sup.2 is selected from the group consisting of hydrogen, alkyl, substituted alkyl, cycloalkyl, substituted cycloalkyl, cycloalkenyl, substituted cycloalkenyl, heterocyclic, substituted heterocyclic, aryl, substituted aryl, heteroaryl, substituted heteroaryl, and R.sup.1 and R.sup.2 together with the nitrogen atom bound to R.sup.2 and the SO.sub.2 group bound to R.sup.1 can form a heterocyclic or a substituted heterocyclic group;R.sup.3 is selected from the group consisting of hydrogen, alkyl, substituted alkyl, cycloalkyl, substituted cycloalkyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocyclic, substituted heterocyclic and, when R.sup.2 does not form a heterocyclic group with R.sup.1, R.sup.2 and R.sup.3 together with the nitrogen atom bound to R.sup.2 and the carbon atom bound to R.sup.3 can form a heterocyclic or a substituted heterocyclic group;R.sup.5 is --(CH.sub.2).sub.x --Ar--R.sup.5 ' where R.sup.5 ' is selected from the group consisting of --NR.sup.12 C(Z)NR.sup.8 R.sup.8 ' and --NR.sup.12 C(Z)R.sup.13 wherein R.sup.12 is selected from the group consisting of hydrogen, alkyl and aryl, R.sup.8 and R.sup.8 ' are independently selected from the group consisting of hydrogen, alkyl substituted alkyl, aryl, substituted aryl, cycloalkyl, substituted cycloalkyl, heterocyclic, substituted heterocyclic, heteroaryl and substituted heteroaryl provided that when Z is oxygen, at least one of R.sup.8 and R.sup.8 ' is substituted alkyl, cycloalkyl, substituted cycloalkyl, saturated heterocyclic other than morpholino and thiomorpholino, or substituted heterocyclic, and R.sup.8 and R.sup.8 ' can be joined to form a saturated heterocycle other than morpholino or thiomorpholino, a saturated substituted heterocycle or a saturated/unsaturated heterocycle having an amino group substituted with an alkoxycarbonyl substituent, and further provided that when Z is sulfur, at least one of R.sup.8 and R.sup.8 ' is a group other than aryl, substituted aryl, heteroaryl or substituted heteroaryl, R.sup.13 is selected from the group consisting of saturated heterocycle other than morpholino and thiomorpholino, and substituted heterocycle, and Z is selected from the group consisting of oxygen, sulfur and NR.sup.12 where R.sup.12 is as defined above,Ar is aryl, substituted aryl, heteroaryl or substituted heteroaryl,x is an integer of from 1 to 4;Q is --C(X)NR.sup.7 -- wherein R.sup.7 is selected from the group consisting of hydrogen and alkyl; and X is selected from the group consisting of oxygen and sulfur;and pharmaceutically acceptable salts thereof,with the proviso that when R.sup.1 is p-CH.sub.3 -.phi.-, Q is --NHC(O)--, and R.sup.2 and R.sup.3 are joined to form a pyrrolidinyl group, then R.sup.5 is not p-[--NHC(O)-2-(1-Boc-4-Cbz-piperazinyl)]-benzyl- or p-[--NHC(O)-2-(1-Boc-piperazinyl)]-benzyl-.