Patent ID: 6302837
Filing Date: 2001-10-16
Classification: A61P,C07D

Abstract:
A compound selected from those of formula (I): ##STR36##wherein:X represents sulphur,Y represents oxygen, sulphur, NR.sub.3 wherein R.sub.3 is hydrogen, linear or branched (C.sub.1 -C.sub.6)alkyl, linear or branched (C.sub.1 -C.sub.6)acyl, aryl, aryl-(C.sub.1 -C.sub.6)alkyl in which alkyl is linear or branched or heteroaryl-(C.sub.1 -C.sub.6)alkyl in which alkyl is linear or branched,T represents nitrogen when bond that links it to adjacent carbon atom is single (--), and, carbon or CH depending on whether the bond that links it to adjacent carbon is single (--) or double ({character pullout}),A represents single bond, or a group selected from (C.sub.1 -C.sub.6)alkylene (optionally substituted by one or more groups selected from linear or branched (C.sub.1 -C.sub.6)alkyl, aryl, aryl-(C.sub.1 -C.sub.6)alkyl in which alkyl is linear or branched, cycloalkyl, heterocycloalkyl, and heteroaryl), arylene, cycloalkylene, heterocycloalkylene, heteroarylene, and --SO.sub.2 --R.sub.4 -- (SO.sub.2 being linked to T) wherein R.sub.4 represents a group selected from linear or branched (C.sub.1 -C.sub.6)alkylene, arylene, aryl-(C.sub.1 -C.sub.6)alkylene in which alkylene is linear or branched, cycloalkylene, heterocycloalkylene, and heteroarylene,W represents a group selected from hydroxy, linear or branched (C.sub.1 -C.sub.6)alkoxy, aryloxy, aryl-(C.sub.1 -C.sub.6)alkoxy in which alkoxy is linear or branched, cycloalkyloxy, heterocycloalkyloxy, heteroaryloxy, amino (which may itself be substituted by one or two, identical or different, groups each independently of the other selected from linear or branched (C.sub.1 -C.sub.6)alky, aryl, aryl-(C.sub.1 -C.sub.6)alkyl in which alkyl is linear or branched, and cycloalkyl), and hydroxyamino,U.sub.1 represents oxygen, sulphur, or linear or branched (C.sub.1 -C.sub.6)alkylene wherein one or more carbon atoms may optionally be replaced by one or more hetero atoms selected from oxygen, nitrogen, and sulphur, the said alkylene being optionally substituted by one or more, identical or different, groups selected from halogen, hydroxy, linear or branched (C.sub.1 -C.sub.6)alkyl, and linear or branched (C.sub.1 -C.sub.6)alkoxy,V.sub.1 represents arylene,U.sub.2 represents a single bond, oxygen, nitrogen, sulphur, linear or branched (C.sub.1 -C.sub.6)alkylene wherein one or more carbon may optionally be replaced by one or more, identical or different, groups selected from oxygen, sulphur, and nitrogen (nitrogen being substituted by a group selected from hydrogen, and linear or branched (C.sub.1 -C.sub.6)alkyl), and SO.sub.2,V.sub.2 represents aryl,Ra, Rb, and Rc, which may be identical or different, each independently of the others represents a group selected from:hydrogen, halogen,hydroxy, cyano, nitro,linear or branched (C.sub.1 -C.sub.6)alkyl, linear or branched (C.sub.1 -C.sub.6)alkoxy, linear or branched (C.sub.1 -C.sub.6)acyl, carboxy, linear or branched (C.sub.1 -C.sub.6)alkoxycarbonyl, linear or branched (C.sub.1 -C.sub.6)trihaloalkyl,amino optionally substituted by one or two groups, which may be identical or different, each independently of the other selected from linear or branched (C.sub.1 -C.sub.6)alkyl, aryl, and aryl-(C.sub.1 -C.sub.6)alkyl in which alkyl is linear or branched,aryloxy, aryl-(C.sub.1 -C.sub.6)alkoxy in which alkoxy is linear or branched, heteroaryloxy, heteroaryl-(C.sub.1 -C.sub.6)alkoxy in which alkoxy is linear or branched,and a group of formula --U.sub.1 --V.sub.1 --U.sub.2 --V.sub.2 wherein U.sub.1, U.sub.2, V.sub.1 and V.sub.2 are as defined hereinbefore,or two of them together form methylenedioxy, or ethylenedioxy each of those groups being optionally substituted by one or two linear or branched (C.sub.1 -C.sub.6)alkyl, aryl, or aryl-(C.sub.1 -C.sub.6)alkyl in which alkyl is linear or branched,R.sub.1 represents:aryl substituted by from one to five, identical or different, substituents each independently of the others selected from halogen, hydroxy, cyano, nitro, carboxy, linear or branched (C.sub.1 -C.sub.6)alkyl, linear or branched (C.sub.1 -C.sub.6)alkoxy, linear or branched (C.sub.1 -C.sub.6)acyl, linear or branched (C.sub.1 -C.sub.6)alkoxycarbonyl, linear or branched (C.sub.1 -C.sub.6)trihaloalkyl (optionally substituted by hydroxy), linear or branched (C.sub.1 -C.sub.6)trihaloalkoxy, amino (optionally substituted by one or two, linear or branched (C.sub.1 -C.sub.6)alkyl, one of which alkyl may be optionally substituted by a group selected from amino, linear or branched (C.sub.1 -C.sub.6)alkylamino, and di-(C.sub.1 -C.sub.6)alkylamino in which each alkyl are each linear or branched), amino-(C.sub.1 -C.sub.6)alkoxy (in which alkoxy is linear or branched, and amino is optionally substituted by one or two, identical or different, linear or branched (C.sub.1 -C.sub.6)alkyl), (C.sub.1 -C.sub.6)alkoxycarbonyl(C.sub.1 -C.sub.6)alkyl in which each alkoxy and alkyl are each linear or branched, linear or branched (C.sub.1 -C.sub.6)alkylcarbonylamino, aryl-(C.sub.1 -C.sub.6)alkyl in which each alkyl is linear or branched, aryloxy, aryl-(C.sub.1 -C.sub.6)alkoxy in which alkoxy is linear or branched, arylamino, aryl-(C.sub.1 -C.sub.6)alkylamino in which each alkyl is linear or branched, arylsulphanyl, aryl-(C.sub.1 -C.sub.6)alkylsulphanyl in which each alkyl is linear or branched, heteroaryl, heteroaryl-(C.sub.1 -C.sub.6)alkyl in which each alkyl is linear or branched, heteroaryloxy, heteroaryl-(C.sub.1 -C.sub.6)alkoxy in which each alkoxy is linear or branched, heteroarylamino, heteroaryl-(C.sub.1 -C.sub.6)alkylamino in which each alkyl is linear or branched, heteroarylsulphanyl, heteroaryl-(C.sub.1 -C.sub.6)alkylsulphanyl in which each alkyl is linear or branched,1,3-dihydro-2H-indol-2-one, 3,4-dihydro-2(1H)-quinolinone, 1-hydroxy-2(1H)-pyridinone,or optionally substituted heteroaryl,R.sub.2 represents a group selected from hydrogen, linear or branched (C.sub.1 -C.sub.6)alkyl, aryl, aryl-(C.sub.1 -C.sub.6)alkyl in which each alkyl is linear or branched, cycloalkyl, heterocycloalkyl, heterocycloalkyl-(C.sub.1 -C.sub.6)alkyl in which each alkyl is linear or branched, heteroaryl, and heteroaryl-(C.sub.1 -C.sub.6)alkyl in which each alkyl is linear or branched,wherein:aryl is understood to be phenyl, biphenyl, naphthyl, tetrahydronaphthyl, or dihydronaphthyl, each of those groups being optionally substituted by one or more, identical or different, groups selected from halogen, hydroxy, cyano, nitro, linear or branched (C.sub.1 -C.sub.6)alkyl (optionally substituted by one or more groups selected from hydroxy, amino, mono (C.sub.1 -C.sub.6)alkylamino and di-(C.sub.1 -C.sub.6)alkylamino in which each alkyl is each linear or branched), linear or branched (C.sub.1 -C.sub.6)trihaloalkyl, linear or branched (C.sub.1 -C.sub.6)alkoxy, aryloxy, linear or branched (C.sub.1 -C.sub.6)acyl, carboxy, linear or branched (C.sub.1 -C.sub.6)alkoxycarbonyl, and amino (amino being optionally substituted by one or two, identical or different, linear or branched (C.sub.1 -C.sub.6)alkyl),cycloalkyl is understood to be a mono- or bi-cyclic group containing from 3 to 8 atoms carbon,heterocycloalkyl is understood to be mono- or bi-cyclic, saturated, or unsaturated group, of non-aromatic character, having from 5 to 12 ring members containing one, two, or three, identical or different, hetero atoms selected from oxygen, nitrogen, and sulphur, it being understood that heterocycloalkyl may be optionally substituted by one or more, identical or different, groups selected from halogen, hydroxy, linear or branched (C.sub.1 -C.sub.6)alkyl, linear or branched (C.sub.1 -C.sub.6)trihaloalkyl, linear or branched (C.sub.1 -C.sub.6)alkoxy, aryloxy, aryl-(C.sub.1 -C.sub.6)alkoxy in which alkoxy is linear or branched, amino (optionally substituted by one or two linear or branched (C.sub.1 -C.sub.6)alkyl), linear or branched (C.sub.1 -C.sub.6)acyl, linear or branched (C.sub.1 -C.sub.6)alkoxycarbonyl, nitro, and oxo,heteroaryl is understood to be mono-, or bi-cyclic heterocycloalkyl as defined hereinbefore, at least one of the rings of which has aromatic character, it being possible for hetero atom(s) to be located, in the case of bicyclic system, on the ring having aromatic character or on the partially unsaturated ring, it being understood that heteroaryl may be optionally substituted by one or more, identical or different, groups as defined for the substituents of heterocycloalkyl,its optical isomers, and pharmaceutically-acceptable acid or base addition salts thereof.