Abstract: A compound of formula (I): and pharmaceutically-acceptable salts thereof wherein the variable groups are defined within; their use in the inhibition of 11?HSD1, processes for making them and pharmaceutical compositions comprising them are also described.

Abstract: The present invention relates to compounds and compositions for treating diseases associated with cysteine protease activity. The compounds are reversible inhibitors of cysteine proteases S, K, F, L and B. Of particular interest are diseases associated with Cathepsin S. In addition this invention also discloses processes for the preparation of such inhibitors.

Abstract: A combination comprising an aurora kinase inhibitor and an efflux transporter inhibitor wherein the aurora kinase inhibitor is a compound of formula (I) or pharmaceutically acceptable salt thereof for use in the treatment of hyperproliferative diseases such as cancer.

Abstract: Compounds of Formula (I): wherein: R1 is hydroxymethyl; R2 is selected from —C(O)NR4R5, —SO2NR4R5, —S(O)pR4 and HET-2; HET-1 is a 5- or 6-membered, optionally substituted C-linked heteroaryl ring; HET-2 is a 4-, 5- or 6-membered, C- or N-linked optionally substituted heterocyclyl ring; R3 is selected from halo, fluoromethyl, difluoromethyl, trifluoromethyl, methyl, methoxy and cyano; R4 is selected from for example hydrogen, optionally substituted (1-4C)alkyl and HET-2; R5 is hydrogen or (1-4C)alkyl; or R4 and R5 together with the nitrogen atom to which they are attached may form a heterocyclyl ring system as defined by HET-3; HET-3 is for example an optionally substituted N-linked, 4, 5 or 6 membered, saturated or partially unsaturated heterocyclyl ring; p is (independently at each occurrence) 0, 1 or 2; m is 0 or 1; n is 0, 1 or 2; provided that when m is 0, then n is 1 or 2; or a salt, pro-drug or solvate thereof, are described.

Abstract: A method for identifying compounds capable of modulating the Notch pathway. The test compound is either administered to an animal or is brought into contact with a cell in culture, after which the expression of the basic helix-loop-helix transcription factor Math1 in a sample from said animal or cell is directed. A change in Math1 expression in the presence of said test compound as compared to in the absence of said compound indicates that said compound modulates the Notch pathway.

Abstract: Compounds of formula (I) and their pharmaceutically acceptable salts are described. Processes for their preparation, pharmaceutical compositions containing them, their use as medicaments and their use in the treatment of bacterial infections are also described.

Abstract: The administration of at least one drug in the form of dry powder by inhalation through an air flow path may be accomplished by an inhalation system including a delivery device having a mouthpiece through which the powder is inhaled. The inhalation system includes a dose cassette defining at least one drug cavity containing dry powder of a dose to be delivered and being sealed by a lid. Further, the inhalation system includes a resilient member configured to be introduced into the air flow path to guide/direct the air flow into the drug cavity upon removal of the lid.

Abstract: The present invention concerns a compound of formula (I): wherein R1 is C1-4 alkyl, or benzyl optionally substituted by halogen, C1-4alkyl (optionally substituted by halogen or C1-4 alkoxy), C1-4 alkoxy, C1-4 alkoxycarbonyl, nitro or cyano; and a process for preparing a compound of formula (I).

Abstract: The present invention relates to selective inhibitors of phosphoinositide (PI) 3-kinase ?, use of the selective inhibitors in anti-thrombotic therapy, and a method for screening compounds useful for the new anti-thrombotic therapy by detecting selective inhibitory activity of PI 3-kinase ? of the compound. The invention also relates to novel compounds that are inhibitors of PI 3-kinase.

Abstract: The invention concerns pharmaceutical compositions containing a hydrogen sulphate salt of 6-(4-bromo-2-chloro-phenylamino)-7-fluoro-3-methyl-3H-benzoimidazole-5-carboxylic acid (2-hydroxy-ethoxy)-amide and solvates, crystalline forms and amorphous forms thereof, to the use of said compositions as a medicament; and to processes for the preparation of said compositions.

Abstract: There are disclosed novel 5,7-disubstituted [1,3]thiazolo[4,5-d]pyrimidin-2(3H)-one derivatives of formula (I) wherein R1, R2, R3, R4, R5, R6, and R7 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, cardio- and cerebrovascular atherosclerotic disorders, peripheral artery disease, rheumatoid arthritis, is pulmonary diseases such as COPD, asthma or pain.

Abstract: Selective phenyl substituted aminopyrazine inhibitors of GSK3 useful for the prevention and/or treatment of cognitive disorders.

Abstract: The present invention relates to new compounds of formula (I) wherein Z is N; Y is CONR5, NR5CO, SO2NR5, NR5SO2, CH2NR5, NR5, NR5CONR5, CH2CO, CO, O or CH2O; X is CH or N; P is phenyl or a 5 or 6 membered heteroaromatic ring containing one or more heteroatoms selected from N, O or S and said phenyl ring or 5 or 6 membered heteroaromatic ring may optionally be fused with a 5 or 6 membered saturated, partially saturated or unsaturated ring containing one or more atoms selected from C, N, O or S; Q is C1-6alkyl, C2-6alkenyl or C2-6alkynyl, a process for their preparation and new intermediates used therein, pharmaceutical formulations containing said therapeutically active compounds and to the use of said active compounds in therapy, such as provide compounds having a selective inhibiting effect at GSK3.

Abstract: A compound of formula (I), or a pharmaceutically acceptable salt, or solvate thereof; and pharmaceutical compositions comprising these, all for use in the treatment of chemokine mediated diseases and disorders.

Abstract: There is provided a process for the preparation of a compound of formula I, or a pharmaceutically acceptable derivative thereof, wherein A, B, G, R1, R2, R3, R4 and R41 to R46 have meanings given in the description, which process comprises the dehydrative cyclisation of a compound of formula II,

Abstract: The present invention provides a compound of a formula (I): wherein the variables are defined herein; to a process for preparing such a compound; and to the use of such a compound in the treatment of a PDE 4 mediated disease state.

Abstract: This invention relates to novel compounds having the structural formula I below: and to their pharmaceutically acceptable salt, compositions and methods of use. These novel compounds provide a treatment or prophylaxis of cognitive impairment, Alzheimer Disease, neurodegeneration and dementia.

Abstract: The invention concerns pyrimidine derivatives of Formula (I), wherein each of p, R1, R2, q, R3, r, R4, X1 and Q1 have any of the meanings defined in the description; processes for their preparation, pharmaceutical compositions containing them and their use in a method for producing an anti-proliferative effect in a warm blooded animal such as man.

Abstract: The invention provides compounds of formula (I), wherein R1, R2, R3, R4, R5 and X are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them, a process for preparing pharmaceutical compositions and their use in therapy (I).

Abstract: This invention relates to novel compounds having the structural formula I below: and to their pharmaceutically acceptable salt, compositions and methods of use. These novel compounds provide a treatment or prophylaxis of cognitive impairment, Alzheimer Disease, neurodegeneration and dementia.