Abstract: The present invention provides a compound of formula (I) in which R1 is generally hydrogen or CF3, R2 is generally hydrogen, W is a cyclic amine, a heterocycle or a group L-Y—X where L-Y is a linking portion and X is generally an aromatic or non-aromatic heterocycle, alkyl or alkylcarbonyl and Z is generally a heterocycle such as 5-methylisoxazol-3-yl, and pharmaceutically acceptable salts thereof for enhancing cognition in conditions such as Alzheimer's Disease, pharmaceutical compositions comprising them, their use for manufacturing medicaments and methods of treatment using them

Abstract: The present invention relates to sulfone derivatives of formula (I): Ar—SO2—CR2R3-L-N(R1)2I wherein Ar, L, R1, R2 and R3 are as defined herein, and pharmaceutically acceptable salts and N-oxides thereof, useful in the treatment of a condition which is susceptible to treatment by modulation of 5-HT7 receptor activity, such as depression or a sleep disorder.

Abstract: The present invention provides compounds of formula I: in which: one of X and Y is a nitrogen atom substituted by a group R6? and the other is a carbon atom substituted by an isoxazole group substituted on its carbon atoms by groups R3 and R4; one of R6 and R6? is hydrogen; either all of W1, W2, W3 and W4 are carbon or one of W1, W2, W3 and W4 is nitrogen and the rest are carbon; and R1 and R2 are, independently, a small group, heteroaromatic ring or a 4–7 membered cyclic amine ring; processes for making them; pharmaceutical composition containing them; their use in therapy, particularly for enhancing cognition in conditions such as Alzheimer's Disease; and methods of treatment using them.

Abstract: Urea derivatives of formula I are disclosed: The compounds are inhibitors of ?-secretase, and hence useful in the treatment or prevention of Alzheimer's Disease

Abstract: Compounds of formula I are disclosed: in which X is a 5-membered heteroaryl ring and R is as defined herein.

Abstract: A class of imidazo[1,2-?]pyrimidine derivatives, substituted at the 3-position by an optionally substituted five-membered or six-membered heteroaromatic ring, are selective ligands for GABAA receptors, in particular having good affinity for the ?2 and/or ?3 and/or ?5 subunit thereof, and are accordingly of benefit in the treatment and/or prevention of adverse conditions of the central nervous system, including anxiety, convulsions and cognitive disorders.

Abstract: The present invention relates to compounds of formula I: in which R1 is a linear group or a five membered heterocycle optionally fused to a phenyl ring, R2 is a 5-membered heterocycle, R3 is chosen from a range of substituents, m is 0–3 and n is 0 or 1; the compounds are generally inverse agonists at GABA-A receptors containing the alpha 5 subunit and so are useful in methods of enhancing cognition in subjects with diminished cognition in diseases such as Alzheimer's Disease.

Abstract: The compound (I) is a GABAa receptor ligand, functionally selective for the ?2 and/or ?3 subunit, and is useful in the treatment of deleterious mental states, in particular anxiety.

Abstract: A class of 7-phenylimidazo[1,2-b][1,2,4]triazine derivatives, substituted at the meta position of the phenyl ring by an optionally substituted aryl or heteroaryl group which is directly attached or bridged by an oxygen atom or a —NH— linkage, and substituted on the phenyl ring by one or two further substituents as defined herein, being selective ligands for GABAA receptors, in particular having good affinity for the ?2 and/or ?3 and/or ?5 subunit thereof, are accordingly of benefit in the treatment and/or prevention of adverse conditions of the central nervous system, including anxiety, convulsions and cognitive disorders.

Abstract: A class of compounds is disclosed which are diasteroisomers of a known class of protease inhibitors. The compound inhibit gamma-secretase, and find use in the treatment of and/or prevention of Alzheimer's disease.

Abstract: The present invention provides a compound of formula I, or an N-oxide thereof or a pharmaceutically acceptable salt thereof: wherein X1 represents hydrogen, halogen, C1-6 alkyl, trifluoromethyl or C1-6 alkoxy; X2 represents hydrogen or halogen; Z represents hydrogen, halogen, cyano, cyanomethyl, trifluoromethyl, nitro, hydroxy, hydroxy(C1-6)alkyl, C1-6 alkoxy, C1-6 alkoxy(C1-6)alkyl, trifluoromethoxy, trifluoromethylthio, trifluoromethanesulfinyl, formyl, C2-6 alkoxycarbonyl, oxopyrrolidinyl, or an optionally substituted aryl, heteroaryl or heteroaryl(C1-6)alkoxy group; and R1 represents aryl or heteroaryl, either of which groups may be optionally substituted; pharmaceutical compositions comprising it, its use in therapy and methods of treatment of anxiety and/or depression using it.

Abstract: The present invention relates compounds that are NK-1 antagonists and that are of use in the treatment or prevention of depression, anxiety, pain, inflammation, migaine, emesis or postherpetic neuralgia.

Abstract: A class of [1,8] naphthyridine analogues which are substituted in the 4-position by a substituted phenyl ring. These compounds are ligands for GABAA receptors and useful in the therapy of deleterious mental states such as anxiety.

Abstract: A class of substituted imidazolo[5,1-a]phthalazine derivatives as ligands for GABAA receptors of formula I which are partial or full inverse agonists of an ?5 receptor subunit while being relatively free of activity at ?1 and/or ?2 and/or ?3 receptor subunit binding sites are described herein; they are therefore of benefit as a medicament for enhancing cognition but with the reduction or elimination of proconvulsant activity.

Abstract: A class of substituted imadazolo[2,1-a]phthalazine derivatives as ligands for GABAA receptors of formula I: which are partial or full inverse agonists of an ?5 receptor subunit while being relatively free of activity at ?1 and/or ?2 and/or ?3 receptor subunit binding sites are described herein; they are therefore of benefit as a medicament for enhancing cognition but with the reduction or elimination of proconvulsant activity.

Abstract: A class of 7-phenylimidazo[1,2-b][1,2,4]triazine derivatives, substituted at the meta position of the phenyl ring by an optionally substituted aryl or heteroaryl group which is directly attached or bridged by an oxygen atom or a —NH— linkage, being selective ligands for GABAA receptors, in particular having good affinity for the ?2 and/or ?3 and/or ?5 subunit thereof, are accordingly of benefit in the treatment and/or prevention of adverse conditions of the central nervous system, including anxiety, convulsions and cognitive disorders.

Abstract: A class of imidazo[1,2-?]pyrazine analogues substituted in the 3-position by a substituted phenyl ring, being selective ligands for GABAA receptors which interact more favourably with the ?2 and/or ?3 subunit than with the ?1 subunit, are accordingly of benefit in the treatment and/or prevention of a variety of disorders of the central nervous system, including anxiety and convulsions, with a reduced propensity to cause sedation.

Abstract: A class of 3-phenylimidazo[1,2-c]pyrimidine derivatives, of the formula I: (wherein R1, X, Y, and Z are defined herein) are selective ligands for GABA-A receptors and are useful in the treatment or prevention of adverse conditions of the central nervous system, including anxiety and convulsions.

Abstract: The present invention relates to imidazo[2,1-f]triazin-4-one analogues which are substituted in the 7-position by a substituted phenyl ring, being ligands for GABAA receptors and accordingly of benefit in the therapy of deleterious neurological disorders.

Abstract: The present invention relates compounds of the formula (I): wherein R1, R2, R3, R4, R5, R6, R7 and R8 represent a variety of substituents; and pharmaceutically acceptable salts thereof. The compounds are of particular use in the treatment or prevention of depression, anxiety, pain, inflammation, migraine, emesis or postherpetic neuralgia.