Patent ID: 6245774
Filing Date: 2001-06-12
Classification: A61P,C07D

Abstract:
A compound of formula (1) ##STR37##wherein.dbd.W-- is (1) .dbd.C(Y)-- or (2) .dbd.N--;L is (1) --C(R).dbd.C(R.sup.1)(R.sup.2) or --(CHR).sub.n CH(R.sup.1)(R.sup.2), (2) --(X.sup.a).sub.n Alk'Ar' or --Alk'X.sup.a Ar' or (3) X.sup.a R';Z is a group (A), (B), (C) or (D): ##STR38##n is zero or the integer 1;t is zero or an integer 1, 2 or 3;Y is halogen or an alkyl or --XR.sup.a group;each of X and X.sup.a is independently --O--, --S(O).sub.m --, or --N(R.sup.b)--;Z.sup.1 is --NR.sup.12 C(O)--, --C(O)NR.sup.12 --, --NR.sup.12 C(S)--, --C(S)NR.sup.12 --, --C.tbd.C--, --NR.sup.12 SO.sub.2 -- or --SO.sub.2 NR.sup.12 --;m is zero or an integer 1 or 2;each of R.sup.a and R.sup.b is independently hydrogen or an optionally substituted alkyl group;R' is Ar' or an optionally substituted polycycloalkyl or polycycloalkenyl group optionally containing one or more --O-- or --S-- atoms or --N(R.sup.b)-- groups;Ar is an optionally substituted monocyclic or bicyclic aryl group optionally containing one or more heteroatoms selected from oxygen, sulphur and nitrogen atoms;Ar' is an optionally substituted heterocycloaliphatic group or an optionally substituted monocyclic or bicyclic aryl group optionally containing one or more heteroatoms selected from oxygen, sulfur and nitrogen atoms;Alk is an optionally substituted straight or branched alkylene chain optionally interrupted by an atom or group X;Alk' is an optionally substituted straight or branched alkylene, alkenylene or alkynylene chain optionally interrupted by one or more linker atoms or groups L.sup.1 ;R is hydrogen, fluorine or a methyl group;each of R.sup.1 and R.sup.2, which may be the same or different, is hydrogen, fluorine, --CN, --NO.sub.2, or an optionally substituted alkyl, alkenyl, alkynyl, alkoxy, alkylthio, --CO.sub.2 R.sup.8, --CONR.sup.9 R.sup.10 or --CSNR.sup.9 R.sup.10 group, or R.sup.1 and R.sup.2, together with the carbon atom to which they are attached, are linked to form an optionally substituted cycloalkyl, cycloalkenyl or heterocycloaliphatic group;R.sup.3 is hydrogen, fluorine, an optionally substituted straight or branched alkyl group, or --OR.sup.11 ;R.sup.4 is hydrogen, --CN, --CH.sub.2 CN or an optionally substituted --CO.sub.2 R.sup.8, --CSNR.sup.9 R.sup.10 or --(CH.sub.2).sub.t Ar group;R.sup.5 is --(CH.sub.2).sub.t Ar;R.sup.6 is hydrogen, fluorine, --CO.sub.2 R.sup.8, --CONR.sup.9 R.sup.10, --CSNR.sup.9 R.sup.10, or an optionally substituted alkyl group;R.sup.7 is hydrogen, fluorine, an optionally substituted straight or branched alkyl group, or --OR.sup.c, where R.sup.c is hydrogen, formyl or an optionally substituted alkyl, alkenyl, alkoxyalkyl, alkanoyl, carboxamido or thiocarboxamido group;each of R.sup.8, R.sup.9 and R.sup.10 is independently hydrogen or an optionally substituted alkyl, aralkyl or aryl group;R.sup.11 is hydrogen, formyl or an optionally substituted alkyl, alkenyl, alkoxyalkyl, alkanoyl, carboxamido or thiocarboxamido group;R.sup.12 is hydrogen or an optionally substituted alkyl or --(Alk).sub.t Ar group; andthe salts, solvates, hydrates, prodrugs and N-oxides thereof;with the provisos that when L is a group (2) or (3), then Z is a group (A) or (B) in which R.sup.4 is --(CH.sub.2).sub.t Ar, when W is .dbd.N--, L is methyl, Z is a group (A) or (B) and R.sup.5 is phenyl, then at least one of R.sup.3, R.sup.4, R.sup.6 and R.sup.7 is other than hydrogen within the atoms or groups defined for R.sup.3, R.sup.4, R.sup.6 R.sup.7 hereinabove, when W is .dbd.N--, L is methyl, Z is a group (D), Z.sup.1 is --C(O)NH-- and Ar is phenyl, then n is 1 and/or t is 1, 2 or 3, when W is C(OCH.sub.3), L is bicyclo(2.2.1)heptyloxy, Z is a group (B), and R.sup.4 and R.sup.6 are hydrogen, then R.sup.5 is other than 4-(methoxycarbonyl)phenyl within the groups defined for R.sup.5 hereinabove, when W is C(OCH.sub.3), L is [exo-8,9,10-trinorbornyl-2-oxy] tricycloalkyloxy or benzyloxy, Z is a group D, Z.sup.1 is --C(O)NH-- and Ar is 3,5-dichloropyrid-4-yl, 2,6-dichlorophenyl or unsubstituted phenyl, then n is 1 and/or t is 1, 2 or 3, and when W is C(OCH.sub.3) and L is benzyloxy, then Z is other than a group (C) in which Ar is an optionally substituted nitrogen-containing monocyclic or bicyclic heterocycle within the groups defined for Ar hereinabove.