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

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: Compounds of formula (I) are disclosed. The compounds inhibit the action of gamma secretase, and hence find use in the treatment and prevention of Alzheimer's disease.

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: Novel sulphones of formula I are disclosed: The compounds modulate the processing of amyloid precursor protein by gamma-secretase, and hence are useful in the treatment or prevention of Alzheimer's disease.

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: The present invention provides a compound of formula (I) wherein A is an optionally substituted C1-4alkylidene group or a bond, R20 and R21 are hydrogen, alkyl groups or heterocyclic groups, R1 and R2 are small substituents or hydrogen, L is O, S or substituted N, X is a 5- or 6-membered heteroaromatic ring, Y is C1-4alkylidene and Z is a 5- or 6-membered heteroaromatic ring; or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising it; its use in therapy; its use in making medicaments for treating neurodegenerative disease and methods of using it to enhance cognition.

Abstract: Compounds of formula I: inhibit the processing of APP by gamma-secretase, and hence are useful in treating or preventing Alzheimer's disease.

Abstract: Gamma-secretase inhibitors, useful in the treatment or prevention of Alzheimer's disease, are disclosed. The preferred compounds have, as the central portion of the molecule, the structure (a) and are di-astereoisomers of known protease inhibitors.

Abstract: The present invention is directed to compounds and pharmaceutical compositions comprising the compounds which are inhibitors of the enzyme gamma secretase and which are useful in the treatment or prevention of diseases in which the beta-amyloid peptide is involved, such as Alzheimer's disease.

Abstract: A metallo-construct, which may be a peptide, is provided for use as a biological, therapeutic, diagnostic imaging, or radiotherapeutic agent, and for use in library or combinatorial chemistry methods. The construct has a conformationally constrained global secondary structure obtained upon complexing with a metal ion. The peptide constructs are of the general formula:R.sub.1 --X--R.sub.2where X is a plurality of amino acids and includes a complexing backbone for complexing metal ions, so that substantially all of the valences of the metal ion are satisfied upon complexation of the metal ion with X, resulting in a specific regional secondary structure forming a part of the global secondary structure; and where R.sub.1 and R.sub.2 each include from 0 to about 20 amino acids, the amino acids being selected so that upon complexing the metal ion with X at least a portion of either R.sub.1 or R.sub.2 or both have a structure forming the balance of the conformationally constrained global secondary structure.