Abstract: The pyrimidinone compounds are disclosed. Methods of preparing the pyrimidinone compounds are also disclosed.

Abstract: Muscarinic Acetylcholine Receptor Antagonists and methods of using them are provided.

Abstract: Compounds having a benzodiazepinyl core structure are disclosed which are vitronectin receptor antagonists useful in the treatment of osteoporosis, angiogenesis, tumor growth and metastasis, atherosclerosis, restenosis and inflammation.

Abstract: A polymorphic form of 5-[4-[2-(N-methyl-N-(2-pyridyl)amino)ethoxy]-benzyl]thiazolidine-2,4-dione, maleic acid salt (the “Polymorph”) characterized in that it: (i) provides an infra red spectrum containing peaks at 1360, 1326, 1241, 714 and 669 cm−1; and/or (ii) provides a Raman spectrum containing peaks at 1581, 768, 670, 271 and 226 cm−1; and/or (iii) provides a solid-state nuclear magnetic resonance spectrum containing peaks at chemical shifts substantially as set out in Table I; and/or (iv) provides an X-ray powder diffraction (XRPD) pattern containing peaks substantially as set out in Table II; a process for preparing such a compound, a pharmaceutical composition containing such a compound and the use of such a compound in medicine.

Abstract: A polymorphic form of 5-[4-[2-(N-methyl-N-(2-pyridyl)amino)ethoxy]benzyl]-thiazolidine-2, 4-dione, maleic acid salt (the “Polymorph”) characterized in that it provides: (i) an infra red spectrum containing peaks at 1763, 912, 856 and 709 cm−1; and/or (ii) a Raman spectrum containing peaks at 1762, 1284, 912 and 888 cm−1; and/or (iii) a solid-state 13C nuclear magnetic resonance spectrum containing peaks at 111.0, 113.6, 119.8, 129.1, 130.9, 131.8, 134.7, 146.5, 152.7, 157.5, 169.5, 171.0, 178.7 ppm; and/or (v) an X-ray powder diffraction (XRPD) pattern which gives calculated lattice spacings at 5.87, 5.30, 4.69, 4.09, 3.88, 3.61, 3.53 and 3.46 Angstroms; a process for preparing such a compound, a pharmaceutical composition containing such a compound and the use of such a compound in medicine.

Abstract: This invention relates, in part, to newly identified methods of using quinolone antibiotics, particularly a gemifloxacin compound against certain pathogenic bacteria, particularly quinolone resistant S. pnemoniae and rare H. influenzae strains.

Abstract: A novel method for the determination of amino acids by HPLC using pre-column derivatization is described. In this procedure, the aminno acids are derivatized with 2-chlorobenzoxazole to yield highly fluroresent N-(2-benzoxazolyl)-amino acids (BOX-AAs) for detection at very high sensitivity. Derivatives can also be detected using conventional UV detection methods. The BOX-AAs can be separated on a C18 reversed phase column for quantitative estimation. This method can be used for the preparation of N-(2-benzoxazolyl)-amino acids in large amounts.

Abstract: This invention relates to novel compounds of Formula (I) to (VII), and compositions thereof, useful in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).

Abstract: A compound which acts as an antagonist at 5-HT4 receptors is of potential use in the treatment of conditions associated with bladder hypersensitivity, such as urinary incontinence, which is often associated with irritable bowel syndrome (IBS) and a compound which acts as an agonist at 5-HT4 receptors is of potential use in the treatment of conditions associated with a poorly functioning bladder, such as urinary bladder hypoactivity following prostectomy.

Abstract: This invention relates to the use of compounds as inhibitors of the fatty acid synthase FabH.

Abstract: Novel anti-infective and methods of using them are provided.

Abstract: The present invention provides phenyl urea and phenyl thiourea derivatives which are non-peptide antagonists of human orexin receptors, in particular orexin-1 receptors, of formula (I) in which: Z represents oxygen or sulfur; and R1 to R7 represent various substituent groups; and pharmaceutically acceptable salts thereof. In particular, these compounds are of potential use in the treatment of obesity including obesity observed in Type 2(non-insulin-dependent) diabetes patients and/or sleep disorders.

Abstract: A method for reducing post-ischaemic injury of the heart and/or improving the functional recovery of the heart following myocardial ischaemia which method comprises administration of an effective, non-toxic amount of a glucose uptake enhancer to a human or non-human mammal in need thereof.

Abstract: Heterocycle condensed morphinoid derivatives of formula (I) have therapeutic utility as analgesics, in collagen disease, as anti-allergic and anti-inflammatory agents, brain cell protectants, in gastritis, diarrhoea, cardiovascular and respiratory diseases, cough, mental illness, epilepsy, for the preservation of organs during transplant operations, and for the treatment of those pathological conditions which customarily can be treated with agonists of the delta opioid receptor.

Abstract: Compounds of formula (I): or a tautomeric form thereof, or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate thereof, wherein: A1 represents a substituted or unsubstituted aromatic heterocyclyl group; R1 represents a hydrocarbon atom, an alkyl group, an acyl group, an aralkyl group, wherein the aryl moiety may be substituted or unsubstituted, or a substituted or unsubstituted aryl group; R2 and R3 each represent hydrogen, or R2 and R3 together represent a bond; A2 represents a benzene ring having a total up to five substituents; and n represents an integer in the range of from 2 to 6; pharmaceutical compositions containing such compounds and the use of such compounds and compositions in medicine.

Abstract: This invention relates to novel compounds of Formula (I), and compositions thereof, useful in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).

Abstract: Disclosed are compounds of formula (I): wherein: Y represents a group (CH2)n, wherein n represents 0, 1 or 2; R1 is phenyl, naphthyl, a mono or bicyclic heteroaryl group containing up to 3 heteroatoms selected from N, O and S; or a group NR3R4 wherein one of R3 and R4 is hydrogen or optionally substituted (C1-4)alkyl and the other is phenyl, naphthyl or a mono or bicyclic heteroaryl group containing up to 3 heteroatoms selected from N, O and S, or R3 and R4 together with the N atom to which they are attached form a 5 to 7-membered cyclic amine which has an optionally fused phenyl ring; any of which R1 groups may be optionally substituted; R2 represents phenyl or a 5- or 6-membered heteroaryl group containing up to 3 heteroatoms selected from N, O and S, wherein the phenyl or heteroaryl group is substituted by R5, and further optional substituents; or R2 represents an optionally substituted bicyclic aromatic or bicyclic heteroaromatic group containing up to 3 heteroatoms selected from N, O

Abstract: A compound of formula (I) wherein: R isopropyl; n is 0; R1 is naphthylmethyl; R2 is t-butyl; and R3 is methyl; is useful in the treatment of disorders mediated by s-CD23.

Abstract: This invention relates to the use of compounds as inhibitors of the fatty acid synthase FabH.

Abstract: The present invention provides a novel hydrate of 5-[4-[2-(N-methyl-N-(2-pyridyl)amino)ethoxy]benzyl]thiazolidine-2,4-dione, maleic acid.