Abstract: The present application relates to internally cyclized naphthamide compounds of the formula Ia (wherein R1a, R1b, R1c, R2, R3, R4, R5, R6, R7, R8, X1, X2, Y, Z, and n are as defined herein), which are useful, for example, for antagonizing the pharmacological actions of the neurokinin 1 (NK1) receptor.

Abstract: A compound of formula (I) or a salt, ester, amide or prodrug thereof; where X is O, or S, S(O), S(O)2 or NR6 where R6 is hydrogen of C1-6alkyl; R5 is an optionally substituted 6-membered aromatic ring containing at least one nitrogen atom, and R1, R2, R3, R4 are independently selected from halogeno, cyano, nitro, C1-3alkylsulphanyl, —N(OH)R7— (wherein R7 is hydrogen, or C1-3alkyl), or R9X1— (wherein X1 represents a direct bond, —O—, —CH2—, —OC(O), —C(O)—, —S—, —SO—, —SO2—, —NR10C(O)—, —C(O)NR11—, —SO2NR12—, —NR13SO2— or NR14— (wherein R10, R11, R12, R13 and R14 each independently represents hydrogen, C1-3alkyl or C1-3alkoxyC2-3alkyl), and R9 is hydrogen, optionally substituted hydrocarbyl, optionally substituted heterocyclyl or optionally substituted alkoxy; provided that at least one of R2 or R3 is other than hydrogen. These compounds inhibit aurora 2 kinase and are useful in the preparation of medicaments for the treatment of proliferative disease such as cancer.

Abstract: An immediate release pharmaceutical composition comprising 4-(3?-chloro-4?-fluoroanilino)-7-methoxy-6-(3-mor-pholinopropoxy)quinazoline or a pharmaceutically-acceptable salt thereof (the Agent); a water-soluble acid; and a water-soluble cellulose ether or an ester of a water-soluble cellulose ether. The claimed compositions inhibit the rate of precipitation of the Agent from solution and/or provide enhanced solubilisation of the agent at pH levels similar to those of the upper GI tract. The claimed compositions are expected to be useful in reducing inter-patient and/or intra-patient variability in exposure to the Agent.

Abstract: There are disclosed novel compounds of formula (I) wherein A, R1, R2, R3 and X are as defined in the specification, and pharmaceutically acceptable salts thereof, together with processes for their preparation, pharmaceutical compositions comprising them and their use in therapy. The compounds of formula (I) are CX3CR1 receptor antagonists and are thereby particularly useful in the treatment or prophylaxis of neurodegenerative disorders, demyelinating disease, atherosclerosis and pain.

Abstract: The invention provides certain pteridinone compounds of formula (I), processes and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapy.

Abstract: This invention relates to novel compounds having the structural formula I below: and their pharmaceutically acceptable salts, tautomers or in vivo-hydrolysable precursors, compositions and methods of use thereof. These novel compounds provide a treatment or prophylaxis of anxiety disorders, cognitive disorders, and/or mood disorders.

Abstract: This invention relates to novel compounds having the structural formula I below: and their pharmaceutically acceptable salts, tautomers or in vivo-hydrolysable precursors, compositions and methods of use thereof. These novel compounds provide a treatment or prophylaxis of anxiety disorders, cognitive disorders, and/or mood disorders.

Abstract: Compounds according to Formula (I) below: wherein R1, R2, R3, and R4 are as defined in the specification, pharmaceutically-acceptable salts, methods of making, pharmaceutical compositions containing and methods for using the same.

Abstract: Compounds of general formula I R1 is selected from any one of phenyl, pyridinyl, thienyl, furanyl, imidazolyl, pyrrolyl, triazolyl, thiazolyl, and pyridine N-oxide; R2 is independently selected from ethyl and isopropyl; R3 is independently selected from hydrogen and fluoro; R4 is independently selected from —OH, —NH2 and —NHSO2R5; and R5 is independently selected from hydrogen, —CF3 and C1–C6 alkyl, or salts thereof or separate enantiomers and salts thereof; where each R1 heteroaromatic ring may optionally and independently be further substituted by 1, 2 or 3 substituents selected from straight and branched C1–C6 alkyl, NO2, CF3, C1–C6 alkoxy, chloro, fluoro, bromo, and iodo.

Abstract: A powder inhaler for administering powder by inhalation comprising: a flow path defined by a plurality of surfaces through which a stream of air is in use drawn on inhalation by a user; and dosing means (18) for providing a dose of powder to the flow path for entrainment in the stream of air; characterized in that the inhaler further comprises dislodging means for dislodging powder accumulated on a surface of the flow path downstream of the dosing means (18).

Abstract: Compounds of formula (I), wherein one of R1 and R2 is selected from a group (IA), ring A is substituted pyridin-z-yl of thiazol-z-yl, the other substituents are as described in the description and their use in the treatment or prevention of a disease or medical conditions mediated through glucokinase

Abstract: The present invention is directed to novel compounds, their use in therapy and pharmaceutical compositions comprising said novel compounds.

Abstract: Compounds useful for the treatment of pain in accord with the following structural diagram, wherein R1, R2 and R3 are any of a number of groups as defined in the specification and pharmaceutical compositions and methods of treatment utilising such compounds.

Abstract: A method for treating a disease associated with the estrogen receptor-?, comprising the step of administiering a therapeutically-effective amount of a compound that satifies the equation: Ki?A/Ki?A>25, optionally having general structure (I).

Abstract: The present invention relates to compounds of formula (I) wherein variable groups are as defined within; pharmaceutically acceptable salts, solvates, solvates of such salts and prodrugs thereof and their use as ileal bile acid transport (IBAT) inhibitors for the treatment of hyperlipidaemia.

Abstract: The present invention relates to a filter device, especially for a fluidised bed system and particularly for use in the pharmaceutical industry, for separating particles larger than a separating grain from an amount of particles in a fluid flow. The filter device includes a housing and at least one filter portion. A part of the housing is mounted for rotational movement, and the filter portion is provided in the housing, whereby the filter portion is movable upon rotation of the housing. The present invention also relates to a method for separating particles using such a filter device.

Abstract: The invention provides compounds of formula in which m, n, R1, R2, R3, R4, and R5, have the meanings defined in the specification; processes for their preparation; pharmaceutical compositions containing them; a process for preparing the pharmaceutical compositions; and their use in therapy.

Abstract: A process for the manufacture of omeprazole or esomeprazole from pyrmethyl alcohol via pyrmethyl chloride and pyrmetazole characterized in that the whole reaction sequence is carried out without any isolation or purification of intermediates. Further, the reaction is carried out in a solvent system common for the whole reaction sequence and inert to the reactants formed during the process and used in the process and comprises a water immiscible organic solvent and a specified amount of water.

Abstract: Compounds of general formula I R1 is selected from any one of phenyl, pyridinyl, pyrrolyl, thienyl, furanyl, imidazolyl, triazolyl, and pyridine N-oxide; where each R1 phenyl ring and R1 heteroaromatic ring may optionally and independently be further substituted by 1, 2 or 3 substituents selected from straight and branched C1–C6alkyl, NO2, CF3, C1–C6alkoxy, chloro, fluoro, bromo, and iodo. The substitutions on the phenyl ring and on the heteroaromatic ring may take place in any position on said ring systems; are disclosed and claimed in the present application, as well as their pharmaceutically acceptable salts and pharmaceutical compositions comprising the novel compounds and their use in therapy, in particular in the management of pain, anxiety and functional gastrointestinal disorders.

Abstract: Heterocyclic amides of formula (1) and pharmaceutically acceptable salts or pro-drugs thereof wherein variable groups are as described herein; which possess glycogen phosphorylase inhibitory activity and accordingly have value in the treatment of disease states associated with increased glycogen phosphorylase activity are described. Processes for the manufacture of said heterocyclic amide derivatives and pharmaceutical compositions containing them are also described.