Patent ID: 6281198
Filing Date: 2001-08-28
Classification: A61P,C07D,Y02P

Abstract:
A compound selected from those of formula (I): ##STR29##wherein:R represents:a group of formula (i): ##STR30##wherein:X and Y, which may be identical or different, each represent a group selected from hydrogen, hydroxy, linear or branched (C.sub.1 -C.sub.6)alkoxy, amino, linear or branched (C.sub.1 -C.sub.6)alkylamino and di-(C.sub.1 -C.sub.6)alkylamino in which each alkyl moiety may be linear or branched,W represents hydrogen, linear or branched (C.sub.1 -C.sub.6)alkyl, aryl or heteroaryl,or a group of formula (ii):--A--G (ii)wherein:A represents a single bond or a linear or branched (C.sub.1 -C.sub.6)alkylene chain optionally substituted by one or more identical or different groups selected from halogen and hydroxy and optionally containing an unsaturation,G represents a group selected from hydrogen, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, --OR.sub.2, --O--T.sub.1 --NR.sub.3 R.sub.4, --O--T.sub.1 --NR.sub.2 --T'.sub.1 --NR.sub.3 R.sub.4, --NR.sub.3 R.sub.4, --NR.sub.2 --T.sub.1 --NR.sub.3 R.sub.4, --NR.sub.2 --T.sub.1 --OR.sub.5, --NR.sub.2 --T.sub.1 --CO.sub.2 R.sub.6, --NR.sub.2 --T.sub.1 --C(O)R.sub.6, --C(O)--NR.sub.3 R.sub.4, --C(O)--NR.sub.2 --T.sub.2, --O--C(O)--T.sub.2, --O--C(S)--T.sub.2, --NR.sub.2 -C(O)--T.sub.2, --NR.sub.2 --C(S)--T.sub.2, --O--C(O)--O--T.sub.2, --O--C(O)--NR.sub.2 --T.sub.2, --O--C(S)--O--T.sub.2, --O--C(S)--NR.sub.2 --T.sub.2, --NR.sub.2 -C(O)--O--T.sub.2, --NR.sub.2 --C(O)--NR.sub.6 --T.sub.2, --NR.sub.2 --C(S)--O--T.sub.2, --NR.sub.2 --C(S)--NR.sub.6 --T.sub.2 and --NR.sub.2 --SO.sub.2 --T.sub.3 wherein:R.sub.2 represents hydrogen, linear or branched (C.sub.1 -C.sub.6)alkyl, aryl or aryl-(C.sub.1 -C.sub.6)alkyl in which the alkyl moiety may be linear or branched,T.sub.1 and T'.sub.1, which may be identical or different, each represents a linear or branched (C.sub.1 -C.sub.6)alkylene chain,R.sub.3 and R.sub.4, which may be identical or different, each represent independently of the other:hydrogen, linear or branched (C.sub.1 -C.sub.6)alkyl (optionally substituted by one or more hydroxy), aryl, aryl-(C.sub.1 -C.sub.6)alkyl in which the alkyl moiety may be linear or branched, cycloalkyl, heteroaryl-(C.sub.1 -C.sub.6)alkyl in which the alkyl moiety may be linear or branched, heteroaryl, heterocycloalkyl or heterocycloalkyl-(C.sub.1 -C.sub.6)alkyl in which the alkyl moiety may be linear or branched,or form together with the nitrogen atom carrying them a saturated or unsaturated, 5- to 7-membered, monocyclic heterocycle optionally containing a second hetero atom selected from oxygen and nitrogen, the heterocycle being optionally substituted by one or more groups selected from halogen, hydroxy, linear or branched (C.sub.1 -C.sub.6)alkyl and heterocyclic groups,R.sub.5 represents linear or branched (C.sub.1 -C.sub.6)alkyl, aryl or aryl-(C.sub.1 -C.sub.6)alkyl in which the alkyl moiety may be linear or branched,R.sub.6 represents hydrogen, linear or branched (C.sub.1 -C.sub.6)alkyl, aryl or aryl-(C.sub.1 -C.sub.6)alkyl in which the alkyl moiety may be linear or branched,T.sub.2 represents a group selected from hydrogen, linear or branched (C.sub.1 -C.sub.6)alkyl (optionally substituted by one or more halogen), aryl, aryl-(C.sub.1 -C.sub.6)alkyl in which the alkyl moiety may be linear or branched, cycloalkyl, cycloalkyl-(C.sub.1 -C.sub.6)alkyl in which the alkyl moiety may be linear or branched, heterocycloalkyl and heterocycloalkyl-(C.sub.1 -C.sub.6)alkyl in which the alkyl moiety may be linear or branched, or T.sub.2 represents a linear or branched (C.sub.1 -C.sub.6)alkylene chain, the chain being substituted by one or more identical or different groups selected from --NR.sub.3 R.sub.4, --OR.sub.2, --CO.sub.2 R.sub.6, --NR.sub.2 --C(O)R.sub.6, --NR.sub.2 --CO.sub.2 R.sub.6, --C(O)R.sub.6, --C(O)NR.sub.3 R.sub.4, --NR.sub.2 --T.sub.1 --NR.sub.3 R.sub.4, --NR.sub.2 --T.sub.1 --OR.sub.6 and --O--T.sub.1 --NR.sub.3 R.sub.4 wherein R.sub.2, R.sub.3, R.sub.4, R.sub.6 and T.sub.1 are as defined hereinbefore,T.sub.3 represents a group selected from linear or branched (C.sub.1 -C.sub.20)alkyl (optionally substituted by one or more groups selected from halogen, --OR.sub.2, --NR.sub.2 R.sub.6, nitro, cyano and azide), aryl, aryl-(C.sub.1 -C.sub.6)alkyl in which the alkyl moiety may be linear or branched, cycloalkyl, cycloalkyl-(C.sub.1 -C.sub.6)alkyl in which the alkyl moiety may be linear or branched, heterocycloalkyl, heterocycloalkyl-(C.sub.1 -C.sub.6)alkyl in which the alkyl moiety may be linear or branched, heteroaryl and heteroaryl-(C.sub.1 -C.sub.6)alkyl in which the alkyl moiety may be linear or branched,R.sub.1 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 the alkyl moiety may be linear or branched, heteroaryl, heteroaryl-(C.sub.1 -C.sub.6)alkyl in which the alkyl moiety may be linear or branched, linear or branched (C.sub.1 -C.sub.6)alkylcarbonyl, arylcarbonyl, aryl-(C.sub.1 -C.sub.6)alkylcarbonyl in which the alkyl moiety may be linear or branched, heterocycloalkylcarbonyl, linear or branched (C.sub.1 -C.sub.6)alkylsulphonyl, arylsulphonyl, aryl-(C.sub.1 -C.sub.6)alkylsulphonyl in which the alkyl moiety may be linear or branched, phosphono, linear or branched (C.sub.1 -C.sub.6)alkoxycarbonyl, aryloxycarbonyl and aryl-(C.sub.1 -C.sub.6)alkoxycarbonyl in which the alkoxy moiety may be linear or branched,its isomers, and also addition salts thereof with a pharmaceutically acceptable acid or base,wherein:aryl denotes phenyl, biphenyl, naphthyl, dihydronaphthyl, tetrahydronaphthyl, indenyl or indanyl, each of those groups optionally having one or more identical or different substituents selected from halogen, hydroxy, linear or branched (C.sub.1 -C.sub.6)alkyl, linear or branched (C.sub.1 -C.sub.6)alkoxy, cyano, nitro, amino, linear or branched (C.sub.1 -C.sub.6)alkylamino, di-(C.sub.1 -C.sub.6)alkylamino in which each alkyl moiety may be linear or branched, linear or branched (C.sub.1 -C.sub.6)alkylsulphonyl, linear or branched (C.sub.1 -C.sub.6)alkylsulphonylamino, carboxy, linear or branched (C.sub.1 -C.sub.6)alkoxycarbonyl, aryloxycarbonyl, aryl-(C.sub.1 -C.sub.6)alkoxycarbonyl in which the alkoxy moiety may be linear or branched, linear or branched (C.sub.1 -C.sub.6)hydroxyalkyl, linear or branched (C.sub.1 -C.sub.6)trihaloalkyl, methylenedioxy, ethylenedioxy, morpholinyl, piperidyl, piperazinyl, linear or branched (C.sub.1 -C.sub.6)alkylcarbonyloxy and linear or branched (C.sub.1 -C.sub.6)alkylcarbonyl,heteroaryl denotes an aromatic monocyclic group, an aromatic bicyclic group, or a bicyclic group in which one of the rings is aromatic and the other ring is partially hydrogenated, each of which groups has from 5 to 12 ring members and contains in the ring system one, two or three identical or different hetero atoms selected from oxygen, nitrogen and sulphur, it being possible for the said heteroaryl optionally to be substituted by the same substituents as those decribed in the case of the aryl group,cycloalkyl denotes a monocyclic or bicyclic group that is saturated or unsaturated, but not of aromatic character, that contains from 3 to 10 carbon atoms and is 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)trihaloalkyl, hydroxy, linear or branched (C.sub.1 -C.sub.6)hydroxyalkyl, amino, linear or branched (C.sub.1 -C.sub.6)alkylamino, di-(C.sub.1 -C.sub.6)-alkylamino in which each alkyl moiety may be linear or branched, piperidyl, piperazinyl and morpholinyl,heterocycloalkyl is to be understood as a cycloalkyl group as defined above containing one or two identical or different hetero atoms selected from oxygen, nitrogen and sulphur, the said heterocycloalkyl being optionally substituted by one or more substituents such as those described in the case of the cycloalkyl,with the proviso that R.sub.1 does not represent methyl when R represents a group --A--G in which A represents a single bond and G represents hydrogen.