Abstract: Tri-substituted phenyl derivatives having the general formula (I): ##STR1## In a preferred embodiment, Y is preferably an --XR.sup.a group, X is preferably --O--, Z is preferably an --XR.sup.5 group, R.sup.a is preferably hydrogen or an optionally substituted alkyl group, R.sup.1 is preferably an --NHC(--NCN)NHR.sup.13 or --NHC(.dbd.CHNO.sub.2)NHR.sup.13 group, R.sup.2, R.sup.3 and R.sup.4 are preferably hydrogen, R.sup.5 is preferably an optionally substituted alkyl, alkenyl, cycloalkyl, cycloalkenyl or heterocycloalkyl group, R.sup.12 is preferably hydrogen or a C.sub.1-3 alkyl group, R.sup.13 is preferably hydrogen, a C.sub.1-3 alkyl group, an optionally substituted phenyl group or an optionally substituted phenylC.sub.1-3 alkyl group, Ar.sup.1 is preferably an optionally substituted nitrogen containing heteroaryl group, and Ar is preferably a phenyl group.

Abstract: Tri-substituted phenyl derivatives and pharmaceutical compositions containing them. In a preferred embodiment, the compounds have the general formula (2): ##STR1## wherein L is preferably --OR; R.sup.a is preferably an optionally substituted alkyl group; R is preferably an optionally substituted cycloalkyl group; R.sup.3 is preferably hydrogen; R.sup.4 is preferably hydrogen, --(CH.sub.2).sub.t --Ar or --(CH.sub.2).sub.t --Ar--(L.sup.1).sub.n --Ar'; R.sup.5 is preferably --(CH.sub.2).sub.t --Ar or --(CH.sub.2).sub.t ---Ar--(L.sup.1).sub.n --Ar'; R.sup.6 and R.sup.7 are preferably hydrogen, L.sup.1 is preferably a divalent linking group; Ar is preferably a monocyclic or bicyclic aryl or heteroaryl group; and Ar' is preferably Ar or an Ar containing group. Compounds of the invention are potent and selective phosphodiesterase type IV inhibitors and are useful in the prophylaxis and treatment of various diseases, such as asthma, which are associated with an unwanted inflammatory response or muscular spasm.

Abstract: Tri-substituted phenyl derivatives and processes for their preparation. In a preferred embodiment, the compounds have the general formula (2) ##STR1## wherein L is preferably --OR; Z is preferably --C(R.sup.3)(R.sup.4)--C(R.sup.5)(R.sup.6)(R.sup.7); R is preferably an optionally substituted cycloalkyl group: R.sup.3 is preferably hydrogen; R.sup.4 is hydrogen, --(CH.sub.2).sub.t Ar or --(CH.sub.2).sub.t --Ar--(L.sup.1).sub.n --Ar'; R.sup.5 is --(CH.sub.2).sub.t Ar or --(CH.sub.2).sub.t --Ar--(L.sup.1).sub.n --Ar'; R.sup.6 and R.sup.7 are preferably hydrogen or methyl; Ar is a monocyclic or bicyclic aryl or heteroaryl group; L.sup.1 is a divalent linking group; and Ar' is Ar or an Ar containing group. Compounds of the invention are potent and selective phosphodiesterase type IV inhibitors and are useful in the prophylaxis and treatment of various diseases, such as asthma, which are associated with an unwanted inflammatory response or muscular spasm.

Abstract: Compounds of general formula (1) ##STR1## are described wherein .dbd.W-- is (1) .dbd.C(Y)-- where Y is a halogen atom, or an alkyl, (2) .dbd.N--; L is a --XR, ?where R is an optionally substituted alkyl, alkenyl, cycloalkyl or cyloalkenyl group!, Z is (1) a group --C(R.sup.3)(R.sup.4)C(R.sup.5)(R.sup.6)(R.sup.7) or --C(R.sup.4).dbd.C(R.sup.5)(R.sup.6) where R.sup.3 is a hydrogen or a fluorine atom or an optionally substituted straight or branched alkyl group; R.sup.4 is a group selected from --X.sup.a L.sup.1 R.sup.12 ?where X.sup.a is as defined above for X, L.sup.1 is a linker group and R.sup.12 is a hydrogen atom or a cycloaliphatic, bicyclic aryl group --Alk.sup.1 R.sup.12 ?where Alk.sup.1 is an optionally substituted straight or branched alkenyl or alkynyl chain or Z is (2) a group --C(R.sup.4)C(R.sup.5)(R.sup.6)(R.sup.7) where R.sup.4 is a group .dbd.CH.sub.2, or .dbd.CH(L.sup.1).sub.n --R.sup.12 ; and the salts, solvates, hydrates, prodrugs and N-oxides thereof.

Abstract: Compounds of general formula (1): ##STR1## are described wherein .dbd.W-- is (1) .dbd.C(Y)-- where Y is a halogen atom, or an alkyl, or --X.sup.a R.sup.1 group where X.sup.a is --O--, --S(O).sub.m -- ?where m is zero or an integer of value 1 or 2!, or --N(R.sup.a)-- ?where R.sup.a is a hydrogen atom or an optionally substituted alkyl group! and R.sup.1 is a hydrogen atom or an optionally substituted alkyl group or, (2) .dbd.N--; X is as described above for X.sup.a or is a chain --CR.dbd.C(R.sup.b)-- or ?--CH(R)!.sub.q --CH(R.sup.b)-- where R is a hydrogen or a fluorine atom or a methyl group, R.sup.b is as described below for R.sup.2 and q is zero or the integer 1; R.sup.2 is (1) an optionally substituted alkyl, alkenyl, cycloalkyl or cycloalkenyl group when X is --O--, --S(O).sub.m -- or --N(R.sup.a)--; atoms or groups; R.sup.3 is an atom or group R.sup.13 ;R.sup.4 is a hydrogen atom or is as defined for R.sup.6 ; R.sup.5 is a hydrogen or a fluorine atom; R.sup.6 is a group --(CH.sub.2).sub.

Abstract: Compounds of general formula (1): ##STR1## wherein Y is a halogen atom or a group --OR.sup.1 where R.sup.1 is an optionally substituted alkyl group;X is --O--, --S-- or --N(R.sup.8)--, where R.sup.8 is a hydrogen atom or an alkyl group;R.sup.2 is an optionally substituted alkyl, alkenyl, cycloalkyl or cycloalkenyl group;R.sup.3 is a hydrogen or halogen atom or an --OR.sup.9 group, where R.sup.9 is a hydrogen atom or an optionally substituted alkyl, alkenyl, alkoxyalkyl, or alkanoyl group, or a formyl, carboxamido or thiocarboxamido group;R.sup.4 is a group --(CH.sub.2).sub.n Ar, where Ar is a monocyclic or bicyclic aryl group optionally containing one or more heteroatoms selected from oxygen, sulphur or nitrogen atoms and n is zero or an integer 1,2 or 3;R.sup.5 is a C.sub.3-9 carbocyclic ketone optionally containing one or more heteroatoms selected from oxygen, sulphur or nitrogen atoms;R.sup.6 is a hydrogen atom or an optionally substituted alkyl group;R.sup.

Abstract: Compounds of general formula (1) ##STR1## are described wherein Y is a halogen atom or a group --OR.sup.1, where R.sup.1 is an optionally substituted alkyl group; X is --O--, --S-- or --N(R.sup.7)--, where R.sup.7 is a hydrogen atom or an alkyl group; R.sup.2 is an optionally substituted cycloalkyl or cycloalkenyl group; R.sup.3 and R.sup.4, which may be the same or different, is each a hydrogen atom or an alkyl, --CO.sub.2 R.sup.8 (where R.sup.8 is a hydrogen atom or an alkyl, aryl, or aralkyl group), --CONR.sup.9 R.sup.10 (where R.sup.9 and R.sup.10 which may be the same or different is each a hydrogen atom or an alkyl, aryl or aralkyl group), --CSNR.sup.9 R.sup.10, --CN, --CH.sub.2 CN group; Z is --(CH.sub.2).sub.n -- (where n is zero or an integer 1, 2 or 3; R.sup.5 is an optionally substituted monocyclic or bicyclic aryl group optionally containing one or more heteroatoms selected from oxygen, sulphur or nitrogen atoms; R.sup.

Abstract: Compounds of general formula (1) ##STR1## are described wherein Y is a halogen atom or a group --OR.sup.1, wherein R.sup.1 is an optionally substituted alkyl group; X is --O--, --S--, or --N(R.sup.6), wherein R.sup.6 is a hydrogen atom or an optionally substituted alkyl group; R.sup.2 is an optionally substituted cycloalkyl or cycloalkenyl group; R.sup.3 and R.sup.4, which may be the same or different, is each a hydrogen atom or an optionally substituted alkyl, --CO.sub.2 R.sup.7 (wherein R.sup.7 is a hydrogen atom, am optionally substituted alkyl, aralkyl, aryl, aryloxyalkyl, alkanoyloxyalkyl or aroyloxyalkyl group), --CONR.sup.8 R.sup.9 (where R.sup.8 and R.sup.9, which may be the same or different, is as defined for R.sup.7), --CSNR.sup.8 R.sup.9, --CN or --CH.sub.2 CN group; Z is --(CH.sub.2).sub.n -- where n is zero or an integer 1, 2 or 3; R.sup.

Abstract: Compounds of general formula (1) are described: ##STR1## wherein .dbd.W-- is (1) .dbd.C(Y)-- where Y is a halogen atom, or an alkyl or --XR.sup.a group where X is --O--, --S(O).sub.m -- ?where m is zero or an integer of value 1 or 2!, or --N(R.sup.b)-- ?where R.sup.b is a hydrogen atom or an optionally substituted alkyl group! and R.sup.a is a hydrogen atom or an optionally substituted alkyl group or, (2) .dbd.N--; L is a --XR, ?where R is an optionally substituted alkyl, alkenyl, cycloalkyl or cyloalkenyl group!, --C(R.sup.5).dbd.C(R.sup.1)(R.sup.2) or ?--CH(R.sup.5)!.sub.n CH(R.sup.1)(R.sup.2) group where R.sup.5 is a hydrogen or a fluorine atom or a methyl group, and R.sup.1 and R.sup.2, which may be the same or different, is each a hydrogen or fluorine atom or an optionally substituted alkyl, alkenyl, alkynyl, alkoxy, alkylthio, --CO.sub.2 R.sup.6, ?where R.sup.6 is a hydrogen atom or an optionally substituted alkyl, aralkyl, or aryl group!, --CONR.sup.7 R.sup.8 ?where R.sup.7 and R.sup.

Abstract: Piperazine derivatives of formula (I) and their salts are 5-HT.sub.1A binding agents and may be used, for example, as anxiolytics. In the formula, R, R.sup.2 and R.sup.4 are hydrogen or lower alkyl, R.sup.1 is mono- or bicyclic aryl or heteroaryl, R.sup.3 is lower alkyl or cycloalkyl, A is an alkylene chain and X is --CO--. --CR.sup.5 OH-- (where R.sup.5 is hydrogen, lower alkyl or cycloalkyl), --S--, --SO-- or --SO.sub.2 -- or X can also be --(CH.sub.2).sub.n -- (where n is 0, 1 or 2) when R.sup.3 is cycloalkyl.

Abstract: Compounds of formula (1) ##STR1## are described wherein Y represents a halogen atom or a group --OR.sup.1, where R.sup.1 is an optionally substituted alkyl group; R.sup.2 represents an optionally substituted cycloalkyl or cycloalkenyl group; R.sup.3 is a monocyclic or bicyclic aryl group optionally containing one or more heteroatoms selected from oxygen or sulphur atoms or a group --N(R.sup.4)-- where R.sup.4 is a hydrogen atom or an alkyl group; X is --O--, --S--, or --N(R.sup.4)--, where R.sup.5 is a hydrogen or an alkyl group; with the proviso that when X is --O-- then R.sup.3 is not a 3-cyanamino-6-pyridazinyl or a 3-chloro-6-pyridazinyl group; and the salts, solvates, hydrates and N-oxides thereof.The compounds are selective and potent inhibitors of phosphodiesterase IV and are useful for the prophylaxis and treatment of inflammatory diseases and the alleviation of conditions associated with central nervous malfunction.