Patent ID: 6140333
Filing Date: 2000-10-31
Classification: A61P,C07D

Abstract:
A compound represented by the formula (I): ##STR16## or a pharmaceutically acceptable salt thereof, whereinAr represents an unsubstituted aryl group, an unsubstituted heteroaryl group, a substituted aryl group or a substituted heteroaryl group, wherein the substituent for the aryl group and heteroaryl group is selected from the group consisting of a halogen atom, a lower alkyl group, and a lower alkoxy group;R.sup.1 represents an unsubstituted C.sub.3 -C.sub.6 cycloalkyl group or a fluorine atom substituted C.sub.3 -C.sub.6 cycloalkyl group;R.sup.2 represents a hydrogen atom or a group having the formula --(A.sup.1).sub.m --NH--B or,R.sup.2 combined with R.sup.3, is(i) a group represented by the formula .dbd.A.sup.2 --NH--B, or(ii) together with the adjoining one of the carbon atoms on the ring, represents a C.sub.2 -C.sub.8 aliphatic nitrogen-containing heterocyclic group containing an imino group, and wherein said nitrogen-containing heterocyclic group is unsubstituted or substituted with a lower alkyl group, or(iii) together with the adjoining one of the carbon atoms on the ring, represents a C.sub.3 -C.sub.8 aliphatic carbocyclic group having on the ring a group --(A.sup.1).sub.m --NH--B, or having on the ring both said group --(A.sup.1).sub.m --NH--B and a lower alkyl group, orR.sup.2 combined with R.sup.4, and the adjoining two carbon atoms to which R.sup.2 and R.sup.4 are bonded, represents a C.sub.2 -C.sub.8 aliphatic nitrogen-containing heterocyclic group containing an imino group, and wherein said nitrogen-containing heterocyclic group is unsubstituted or substituted with a lower alkyl group;R.sup.3 represents a hydrogen atom, an unsubstituted C.sub.1 -C.sub.8 aliphatic hydrocarbon group or a lower alkyl-substituted C.sub.1 -C.sub.8 aliphatic hydrocarbon group or,R.sup.3 combined with R.sup.5 represents a single bond or,R.sup.3 together with an adjoining one of the carbon atoms on the ring, represents(i) a C.sub.2 -C.sub.8 aliphatic nitrogen-containing heterocyclic group containing an imino group, and wherein said nitrogen-containing heterocyclic group is unsubstituted or substituted with a lower alkyl group, or(ii) a C.sub.3 -C.sub.8 aliphatic carbocyclic group having on the ring a group --(A.sup.1).sub.m --NH--B, or having on the ring both said group --(A.sup.1).sub.m --NH--B and a lower alkyl group;R.sup.4 represents a hydrogen atom or a group having the formula --(A.sup.1).sub.m --NH--B, or,R.sup.4 combined with R.sup.5 is a group represented by the formula .dbd.A.sup.2 --NH--B, or,R.sup.4 together with an adjoining one of the carbon atoms on the ring, represents(i) a C.sub.2 -C.sub.8 aliphatic nitrogen-containing heterocyclic group containing an imino group, and wherein said nitrogen-containing heterocyclic group is unsubstituted or substituted with a lower alkyl group or,(ii) a C.sub.3 -C.sub.8 carbocyclic group having on the ring a group --(A.sup.1).sub.m --NH--B, or having on the ring both said group --(A.sup.1).sub.m --NH--B and a lower alkyl group;R.sup.5 represents a hydrogen atom or an unsubstituted C.sub.1 -C.sub.6 aliphatic hydrocarbon group or a lower alkyl group-substituted C.sub.1 -C.sub.6 aliphatic hydrocarbon group, orR.sup.5 together with an adjoining one of the carbon atoms on the ring, represents(i) a C.sub.2 -C.sub.8 aliphatic nitrogen-containing heterocyclic group containing an imino group, and wherein said nitrogen-containing heterocyclic group is unsubstituted or substituted with a lower alkyl group, or,(ii) a C.sub.3 -C.sub.8 aliphatic carbocyclic group having on the ring a group --(A.sup.1).sub.m --NH--B, or having on the ring both said group --(A.sup.1).sub.m --NH--B and a lower alkyl group;A.sup.1 represents an unsubstituted C.sub.1 -C.sub.8 bivalent aliphatic hydrocarbon group or a lower alkyl group-substituted C.sub.1 -C.sub.8 bivalent aliphatic hydrocarbon group;A.sup.2 represents an unsubstituted C.sub.1 -C.sub.8 trivalent aliphatic hydrocarbon group or a lower alkyl group-substituted C.sub.1 -C.sub.8 trivalent aliphatic hydrocarbon group;B represents a hydrogen atom, an unsubstituted C.sub.1 -C.sub.6 aliphatic hydrocarbon group or a substituted C.sub.1 -C.sub.6 aliphatic hydrocarbon group, wherein said substituent is a lower alkyl group or aryl group;m represents 0 or 1;n represents 0 or 1; andX represents an oxygen atom or a sulfur atom,with the provisos that:(a) R.sup.2 and R.sup.4 do not simultaneously represent a hydrogen atom;(b) when either R.sup.2 or R.sup.4 represents the group --(A.sup.1).sub.m --NH--B, the other represents a hydrogen atom;(c) when R.sup.2 and R.sup.3 combine to form said group .dbd.A.sup.2 --NH--B or together with the carbon atom to which they are bonded combine to form said C.sub.2 -C.sub.8 aliphatic nitrogen-containing heterocyclic group or said C.sub.3 -C.sub.8 aliphatic carbocyclic group, R.sup.4 represents a hydrogen atom; and(d) when R.sup.4 and R.sup.5 combine to form said group .dbd.A.sup.2 --NH--B or together with the carbon atom to which they are bonded combine to form said C.sub.2 -C.sub.8 aliphatic nitrogen-containing heterocyclic group or said C.sub.3 -C.sub.8 aliphatic carbocyclic group, R.sup.2 represents a hydrogen atom.