Patent ID: 6242422
Filing Date: 2001-06-05
Classification: A61P,C07C,C07D,C07F,C07K

Abstract:
An isolated compound of the following formula: ##STR56##wherein:n is 0, 1 or 2;X is CH.sub.2, C.dbd.O, O, S or NH;A is a moiety of Formula IIa-i: ##STR57## ##STR58##B is a hydrogen atom, a deuterium atom, C.sub.1-10 straight chain branched alkyl, cycloalkyl, phenyl, substituted phenyl, naphthyl, substituted naphthyl, 2-benzoxazolyl, substituted 2-oxazolyl, (CH.sub.2).sub.m cycloalkyl, (CH.sub.2).sub.m phenyl, (CH.sub.2).sub.m (substituted phenyl), (CH.sub.2).sub.m (1 or 2-naphthyl), (CH.sub.2).sub.m heteroaryl, halomethyl, CO.sub.2 R.sup.13, CONR.sup.14 R.sup.15, CH.sub.2 ZR.sup.16, CH.sub.2 OCO(aryl), CH.sub.2 OCO(heteroaryl), or CH.sub.2 OPO(R.sup.17)R.sup.18, where Z is an oxygen or a sulfur atom, or B is a group of the Formula IIIa-c: ##STR59##R.sup.1 is phenyl, substituted phenyl, naphthyl, substituted naphthyl, heteroaryl, or substituted heteroaryl;R.sup.2 is hydrogen, alkyl, cycloalkyl, phenyl, substituted phenyl, (CH.sub.2).sub.m NH.sub.2, (CH.sub.2).sub.m NHCOR.sup.10, (CH.sub.2).sub.m N(C.dbd.NH)NH.sub.2, (CH.sub.2).sub.p CO.sub.2 R.sup.3, (CH.sub.2).sub.p OR.sup.11, (CH.sub.2).sub.p SR.sup.12, (CH.sub.2).sub.m cycloalkyl, (CH.sub.2).sub.m phenyl, (CH.sub.2).sub.m (substituted phenyl), (CH.sub.2).sub.m (1 or 2-naphthyl), or (CH.sub.2).sub.m heteroaryl, wherein heteroaryl includes (but is not limited to) pyridyl, thienyl, furyl, thiazolyl, imidazolyl, pyrazolyl, isoxazolyl, pyrazinyl, pyrimidyl, triazinyl, tetrazolyl, and indolyl;R.sup.3 is hydrogen, alkyl, cycloalkyl, (cycloalkyl)alkyl, phenylalkyl, or substituted phenylalkyl; and whereinR.sup.4 is alkyl, cycloalkyl, phenyl, substituted phenyl, (CH.sub.2).sub.m NH.sub.2, (CH.sub.2).sub.m NHCOR.sup.10, (CH.sub.2).sub.m N(C.dbd.NH)NH.sub.2, (CH.sub.2).sub.p CO.sub.2 R.sup.3,(CH.sub.2).sub.p OR.sup.11, (CH.sub.2).sub.p SR.sup.12, (CH.sub.2).sub.m cycloalkyl, (CH.sub.2).sub.m phenyl, (CH.sub.2).sub.m (substituted phenyl), (CH.sub.2).sub.m (1 or 2-naphthyl), or (CH.sub.2).sub.m heteroaryl, wherein heteroaryl includes (but is not limited to) pyridyl, thienyl, furyl, thiazolyl, imidazolyl, pyrazolyl, isoxazolyl, pyrazinyl, pyrimidyl, triazinyl, tetrazolyl, and indolyl;R.sup.4a is hydrogen, or methyl, or R.sup.4 and R.sup.4a taken together are --(CH.sub.2).sub.d -- where d is an interger from 2 to 6;R.sup.5 is phenyl, substituted phenyl, (CH.sub.2).sub.p phenyl, (CH.sub.2).sub.p (substituted phenyl), cycloalkyl, or benzofused cycloalkyl;R.sup.6 is hydrogen, alkyl, cycloalkyl, phenyl, substituted phenyl, (CH.sub.2).sub.m cycloalkyl, (CH.sub.2).sub.m phenyl, (CH.sub.2).sub.m (substituted phenyl), or (CH.sub.2).sub.m (1 or 2-naphthyl);R.sup.7 is hydrogen, fluorine, oxo, alkyl, cycloalkyl, phenyl, substituted phenyl, naphthyl, (CH.sub.2).sub.m cycloalkyl, (CH.sub.2).sub.m phenyl, (CH.sub.2).sub.m (substituted phenyl), (CH.sub.2).sub.m (1 or 2-naphthyl), OR.sup.11, SR.sup.12, or NHCOR.sup.10 ;R.sup.8 is hydrogen, oxo, alkyl, cycloalkyl, phenyl, substituted phenyl, naphthyl, (CH.sub.2).sub.m cycloalkyl, (CH.sub.2).sub.m phenyl, (CH.sub.2).sub.m (substituted phenyl), or (CH.sub.2).sub.m (1 or 2-naphthyl);R.sup.9 is alkyl, cycloalkyl, (CH.sub.2).sub.m cycloalkyl, (CH.sub.2).sub.m phenyl, (CH.sub.2).sub.m (substituted phenyl), (CH.sub.2).sub.m (1 or 2-naphthyl), or COR.sup.10 ;R.sup.10 is hydrogen, alkyl, cycloalkyl, phenyl, substituted phenyl, naphthyl, (CH.sub.2).sub.m cycloalkyl, (CH.sub.2).sub.m phenyl, (CH.sub.2).sub.m (substituted phenyl), (CH.sub.2).sub.m (1 or 2-naphthyl), OR.sup.13, or NR.sup.14 R.sup.15 ;R.sup.11 is hydrogen, alkyl, cycloalkyl, phenyl, substituted phenyl, naphthyl, (CH.sub.2).sub.m cycloalkyl, (CH.sub.2).sub.m phenyl, (CH.sub.2).sub.m (substituted phenyl), or (CH.sub.2).sub.m (1 or 2-naphthyl);R.sup.12 is alkyl, cycloalkyl, phenyl, substituted phenyl, naphthyl, (CH.sub.2).sub.m cycloalkyl, (CH.sub.2).sub.m phenyl, (CH.sub.2).sub.m (substituted phenyl), or (CH.sub.2).sub.m (1 or 2-naphthyl);R.sup.13 is alkyl, cycloalkyl, (CH.sub.2).sub.m cycloalkyl, (CH.sub.2).sub.m phenyl, (CH.sub.2).sub.m (substituted phenyl), or (CH.sub.2).sub.m (1 or 2-naphthyl);R.sup.14 is hydrogen, alkyl, cycloalkyl, phenyl, substituted phenyl, naphthyl, substituted naphthyl, (CH.sub.2).sub.m cycloalkyl, (CH.sub.2).sub.m phenyl, (CH.sub.2).sub.m (substituted phenyl), or (CH.sub.2).sub.m (1 or 2-naphthyl);R.sup.15 is hydrogen or alkyl; orR.sup.14 and R.sup.15 taken together form a five, six or seven membered carbocyclic or heterocyclic ring, such as morpholine or N-substituted piperazine;R.sup.16 is phenyl, substituted phenyl, naphthyl, substituted naphthyl, heteroaryl, (CH.sub.2).sub.m phenyl, (CH.sub.2).sub.m (substituted phenyl), (CH.sub.2).sub.m (1 or 2-naphthyl), or (CH.sub.2).sub.m heteroaryl;R.sup.17 and R.sup.18 are independently alkyl, cycloalkyl, phenyl, substituted phenyl, naphthyl, or phenylalkyl, substituted phenylalkyl, or (cycloalkyl)alkyl;R.sup.19 and R.sup.20 are independently hydrogen, alkyl, phenyl, substituted phenyl, (CH.sub.2).sub.m phenyl, or (CH.sub.2).sub.m (substituted phenyl), or R.sup.19 and R.sup.20 taken together are --(CH.dbd.CH).sub.2 --;R.sup.21 is hydrogen, alkyl, phenyl, substituted phenyl, (CH.sub.2).sub.m phenyl, (CH.sub.2).sub.m (substituted phenyl);R.sup.22, R.sup.23 and R.sup.24 are independently hydrogen or alkyl;Y.sup.1 is CH.sub.2, (CH.sub.2).sub.2, (CH.sub.2).sub.3, or S;Y.sup.2 is O or NR.sup.24 ;Y.sup.3 is CH.sub.2, O, or NR.sup.24 ;a is 0 or 1 and b is 1 or 2, provided that when a is 1 then b is 1;c is 1 or 2, provided that when c is 1 then a is 0 and b is 1;m is 1,2,3 or 4; andp is 1 or 2;or a salt thereof.