Patent ID: 6288077
Filing Date: 2001-09-11
Classification: A61P,C07D,Y02P

Abstract:
A compound selected from those of formula (I): ##STR10##wherein:n represents 2 or 3,R.sub.1 represents (C.sub.3 -C.sub.8)cycloalkyl, optionally substituted phenyl, or linear or branched (C.sub.1 -C.sub.6)alkyl optionally substituted by one or more identical or different groups selected from halogen, (C.sub.3 -C.sub.8)cycloalkyl, and optionally substituted phenyl,R.sub.2 represents:amino,amidino optionally substituted by one or more identical or different goups selected from linear or branched (C.sub.1 -C.sub.6)alkyl and hydroxy,guanidino optionally substituted by linear or branched (C.sub.1 -C.sub.6)alkyl, orisothioureido optionally substituted by linear or branched (C.sub.1 -C.sub.6)alkyl,Ar represents aryl or monocyclic nitrogen-containing heteroaryl,X.sub.1 represents hydroxy, amino or --NHR.sub.3,R.sub.3 represents propargyl, iminomethyl, linear or branched (C.sub.1 -C.sub.6)alkylsulphonyl, linear or branched aryl(C.sub.1 -C.sub.6)alkylsulphonyl, --CONR'.sub.3 R"".sub.3, or linear or branched (C.sub.1 -C.sub.6)alkyl optionally substituted by:--CO.sub.2 R'.sub.3,--CONR'.sub.3 R"".sub.3,a heterocyclic group,aminosulphonyl,aryl, orheteroaryl,R'.sub.3 and R"".sub.3, which may be identical or different, each represents hydrogen, linear or branched (C.sub.1 -C.sub.6)alkylsulphonyl, aryl, linear or branched (C.sub.1 -C.sub.6)alkyl optionally substituted by carboxy, linear or branched (C.sub.1 -C.sub.6)alkoxycarbonyl or carbamoyl or form, with the nitrogen atom carrying them, a heterocyclic group,an isomer thereof, and an addition salt thereof with a pharmaceutically/acceptable acid or base,on the understanding that the term ""optionally substituted phenyl"" means substituted by one or more identical of different groups selected from halogen, linear or branched (C.sub.1 -C.sub.6)alkyl, linear or branched (C.sub.1 -C.sub.6)alkoxy, hydroxy, linear or branched trihalo-(C.sub.1 -C.sub.6)alkyl, and amino optionally substituted by one or more linear or branched (C.sub.1 -C.sub.6)alkyl groups,the term ""heterocyclic group"" denotes a saturated or unsaturated, mono- or bi-cyclic group having 5 to 12 ring members containing one, two, or three hetero atoms selected from oxygen, nitrogen and sulphur, it being understood that the heterocycle may be optionally substituted by one or more identical or different groups selected from halogen, linear or branched (C.sub.1 -C.sub.6)alkyl, linear or branched (C.sub.1 -C.sub.6)alkoxy, oxo, hydroxy, linear or branched trihalo-(C.sub.1 -C.sub.6)alkyl, and amino optionally substituted by one or more linear or branched (C.sub.1 -C.sub.6)alkyl groups,the term ""aryl"" means phenyl, biphenylyl, or naphthyl, each of those groups being optionally substituted by one or more identical or different groups selected from halogen, linear or branched (C.sub.1 -C.sub.6)alkyl, linear or branched (C.sub.1 -C.sub.6)alkoxy, hydroxy, linear or branched trihalo-(C.sub.1 -C.sub.6)alkyl, amino optionally substituted by one or more linear or branched (C.sub.1 -C.sub.6)alkyl groups, and carboxy,and the term ""heteroaryl group"" denotes an aromatic mono- or bicyclic group having 5 to 12 ring members containing one, two or three hetero atoms selected from oxygen, nitrogen and sulphur, it being understood that heteroaryl may be optionally substituted by one or more identical or different groups selected from halogen, linear or branched (C.sub.1 -C.sub.6)alkyl, hydroxy, linear or branched (C.sub.1 -C.sub.6)alkoxy, trihalomethyl, and amino optionally substituted by one or more linear or branched (C.sub.1 -C.sub.6)alkyl groups.