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 the general formula (1) ##STR1## are described wherein Y is halogen or --OR.sup.1, where R.sup.1 is a substituted or unsubstituted alkyl; X is --O--, --S-- or --N(R.sup.8)--, where R.sup.8 is hydrogen or alkyl; R.sup.2 is substituted or unsubstituted alkyl, alkenyl, cycloalkyl or cycloalkenyl; R.sup.3 is hydrogen, halogen or --OR.sup.9, where R.sup.9 is hydrogen or substituted or unsubstituted alkyl, alkenyl, alkoxyalkyl, or alkanoyl, or formyl, carboxamido or thiocarboxamido; R.sup.4 and R.sup.5, which may be the same or different, are each --(CH.sub.2).sub.n Ar, where Ar is a monocyclic or bicyclic aryl group or monocyclic or bicyclic heteroaryl and n is integer of 0 to 3; R.sup.6 is hydrogen or substituted or unsubstituted alkyl; R.sup.7 is hydrogen or substituted or unsubstituted alkyl; and the salts, solvates, hydrates and N-oxides thereof.

Abstract: An enantioselective multi-stage process is described which uses as a starting material an .alpha.,.beta.-unsaturated olefin of formula (1):Ar--CH.dbd.C(R.sup.4)COAux (1)where Ar and R.sup.4, which may be the same or different, is each a monocyclic or bicyclic aryl group optionally containing one or more heteroatoms selected from oxygen, sulphur or nitrogen atoms; and Aux is the residue of a chiral (R- or S-) auxiliary.In the process, the olefin is converted to a chiral triarylethane which is of use in medicine.

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)--, where R.sup.6 is a hydrogen atom or an alkyl group; R.sup.2 is an optionally substituted alkyl, alkenyl, cycloalkyl or cycloalkenyl group; R.sup.3 and R.sup.4, which may be the same or different, is each a group --(CH.sup.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 hydrogen atom or an optionally substituted alkyl group; and the salts, solvates, hydrates and N-oxides. Compounds according to the invention are potent, selective and orally active PDE IV inhibitors and are useful in the prophylaxis and treatment of asthma.

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.5)--, 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.

Abstract: Disclosed herein are piperazine derivatives of the formula ##STR1## or a pharmaceutically acceptable acid addition salt thereof, wherein W is (CH.sub.2).sub.m, CHOH or O,m is one of the integers 1 or 2,A is an alkylene chain of 1 to 3 carbon atoms optionally substituted by one or more (lower)alkyl groups,R is hydrogen or lower alkyl,R.sup.1 and R.sup.2 are each, independently, aryl or heteroaryl radicals with the proviso that R.sup.1 is not an optionally substituted indolyl radical,R.sup.3 is hydrogen or lower alkyl andR.sup.4 is an aryl or heteroaryl radical.The compounds are 5HT.sub.1A binding agents which may be used, for example, in the treatment of CNS disorders such as anxiety.

Abstract: Compounds of formula ##STR1## where A is an alkylene chain of 1 or 2 carbon atoms optionally substituted by one or more lower alkyl groups,R is hydrogen or lower alkyl,R.sup.1 is an aryl or heteroaryl radical,R.sup.2 is a mono- or bicyclic heterocyclic radical,R.sup.3 is hydrogen, lower alkyl or hydroxy andR.sup.4 is a aryl or heteroaryl radical,and their pharmaceutically acceptable acid addition salts are 5-HT.sub.1A binding agents which may be used, for example, for the treatment of CNS--disorders such as anxiety.

Abstract: Piperazine derivative of formula ##STR1## and the pharmaceutically acceptable acid addition salts, where A is an alkylene chain of 1 or 2 carbon atoms optionally substituted by one or more lower alkyl groups, m is 0, 1 or 2, R is hydrogen or lower alkyl, R.sup.1 is aryl or a mono- or bicyclic heteroaryl radical, R.sup.2 is hydrogen or lower alkyl, R.sup.3 is a heteroaryl radical, R.sup.4 is hydrogen, lower alkyl or aryl, and R.sup.5 is hydrogen, lower alkyl, cycloalkyl, cycloalkyl(lower)alkyl, aryl, or aryl(lower)alkyl or R.sup.4 and R.sup.5 together with the nitrogen atom to which they are both attached represent a saturated heterocyclic ring which may contain a further hetero atom are 5--HT.sub.1A -binding agents and may be used, for example, as anxiolytics.