Abstract: Compounds of formula I or pharmaceutically acceptable salts thereof: wherein R1, R2, R3, R4 and Z are as defined in the specification as well as salts and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain.

Abstract: The present invention relates to compounds that inhibit of a5b1 function, processes for their preparation, pharmaceutical compositions containing them as the active ingredient, to their use as medicaments and to their use in the manufacture of medicaments for use in the treatment in warm-blooded animals such as humans of diseases that have a significant angiogenesis or vascular component such as for treatment of solid tumours. The present invention also relates to compounds that inhibit a5b1 and also that exhibit appropriate selectivity profile(s) against other integrins.

Abstract: The present invention relates to compounds of formula (I) that mediate Edg, including Edg-1, processes for their preparation, pharmaceutical compositions containing them as the active ingredient, to their use as medicaments and to their use in the manufacture of medicaments for use in the treatment in warm-blooded animals such as humans of diseases that have a significant vascularization or inflammatory component such as in tumor-related diseases. The present invention also relates to compounds that inhibit a5bl, and also that exhibit appropriate selectivity profile(s) against other integrins.

Abstract: The present invention is directed to novel compounds, to a process for their preparation, their use in therapy and pharmaceutical compositions comprising the novel compounds.

Abstract: Compounds of formula (I) wherein R1, HET-1 and HET-2 are as described in the specification, and their salts and pro-drugs, are activators of glucokinase (GLK) and are thereby useful in the treatment of, for example, type 2 diabetes. Processes for preparing compounds of formula (I) are also described.

Abstract: The present invention is directed to novel compounds, to a process for their preparation, their use in therapy and pharmaceutical compositions comprising the novel compounds.

Abstract: The present invention is directed to novel compounds, to a process for their preparation, their use in therapy and pharmaceutical compositions comprising the novel compounds.

Abstract: A process for the preparation of a compound of Formula (I) and intermediates useful therein are provided. The process comprises reacting a compound of formula R1—CO—CH2-E with a compound of formula R2—CHX1X2 in the presence of a compound of formula R3R4N—C(?NH)NH2 and a catalyst, thereby to form a dihydropyrimidine; and oxidising the dihydropyrimidine to form the compound of Formula (1). R1 is H or an alkyl group; R2 is H, an alkyl or aryl group; R3 and R4 are each independently H, alkyl or aryl, or R3 and R4 are linked to form, together with the nitrogen to which they are attached to form a 5 to 7 membered heterocyclic ring; E is H, an unsubstituted alkyl group, and aryl group or an electron withdrawing group; and X1 and X2 are each independently leaving groups, or X1 and X2 together represent ?O.

Abstract: The invention relates to the use of a compound of Formula (I) or a salt, solvate or prodrug thereof, wherein R1, R2, R3, n and m are as described in the specification, in the preparation of a medicament for the treatment or prevention of a disease condition mediated through glucokinase (GLK), such as type 2 diabetes. The invention also relates to a novel group of compounds of Formula (I) and to methods for preparing compounds of Formula (I).

Abstract: The invention provides compounds of formula (I) wherein m, R1, n, R2, q, p, X, Y, R3, R4, t and, R5 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.

Abstract: The invention provides sterile glucocorticosteroids and sterile formulations containing glucocorticosteroid and use thereof in the treatment of an allergic and/or inflammatory condition of the nose or the lungs.

Abstract: A compound of formula I or a pharmaceutically acceptable salt thereof, processes for preparing such compounds, their use as Fatty Acid Synthase inhibitors, methods for their therapeutic use, particularly in the treatment of obesity and diabetes mellitus, cancer and infection and pharmaceutical compositions containing them.

Abstract: Compounds of formula I wherein R1, R2, R3, R4, R5, R6, R7, R8 and R9 are as defined in the specification as a base or a pharmaceutically acceptable salt, solvate or solvate of salt thereof, processes for their preparation, new intermediates used therein, pharmaceutical formulations containing said compounds and to the use of said compounds in therapy.

Abstract: A compound of the formula (VIII) wherein each X is independently H or F; and R is selected from hydrogen, halogen, cyano, methyl, cyanomethyl, fluoromethyl, difluoromethyl, trifluoromethyl and —Si[(1-4C)alkyl]3; and processes for preparing a compound of formula (VIII) by bromination of a compound of the formula (VII),

Abstract: The invention relates to chemical compounds of formula (I): or pharmaceutically acceptable salts thereof, which possess Edg-1 antagonistic activity and are accordingly useful for their anti cancer activity and thus in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of said chemical compounds, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments of use in the production of an anti-cancer effect in a warm blooded animal such as man.

Abstract: A novel adenine compound represented by the formula (1): wherein A represents an (un)substituted aromatic carbocycle or (un)substituted aromatic heterocycle; L1, L2, and L3 each independently represents linear or branched alkylene, etc.; R1 represents (un)substituted alkyl, (un)substituted aryl, etc.; R2 represents hydrogen or (un) substituted alkyl; R3 represents (un)substituted alkyl, etc., provided that R3 may be bonded to L2 or L3 to form a nitrogenous saturated heterocycle; and X represents oxygen, etc.; or a pharmaceutically acceptable salt of the compound. The compound and salt are useful as a medicine.

Abstract: A compound of formula (I) wherein R1 represents aryl optionally substituted by a heterocyclic group or a heterocyclic group optionally substituted by aryl wherein each aryl or heterocyclic group is optionally substituted; the group —(CH2)m-T-(CH2)n—U—(CH2)p— is attached at either the 3 or 4 position in the phenyl ring as indicated by the numbers in formula (I) and represents a group selected from one or more of the following: O(CH2)2, O(CH2)3, NC(O)NR4(CH2)2, CH2S(O2)NR5(CH2)2, CH2N(R6)C(O)CH2, (CH2)2N(R6)C(O)(CH2)2, C(O)NR7CH2, C(O)NR7(CH2)2, and CH2N(R6)C(O)CH2O; V represents O, S, NR8 or a single bond; q represents 1, 2, or 3; W represents O, S, N(R9)C(O), NR10, or a single bond; R2 represents halo, a C1-4 alkyl group which is optionally substituted by one or more fluoro, a C1-4 alkoxy group which is optionally substituted by one or more fluoro, a C1-4 acyl group, aryl, an aryl C1-4 alkyl group, CN or NO2; r represents 0, 1, 2 or 3; R3 halo, a C1-4 alkyl group which is optionally substutited by one or more

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

Abstract: A novel adenine compound represented by the formula (1): wherein Z represents (un)substituted alkylene, a single bond, etc.; R1 represents an (un)substituted alkyl, alkenyl, alkynyl, cycloalkyl, aryl, or heteroaryl group; R2 represents hydrogen or (un)substituted alkyl; R3, R4 and R5 each independently represents an (un)substituted alkyl, alkenyl, alkynyl, aryl, or heteroaryl group, provided that R3 and R5 may be bonded to each other to form a 3- to 7-membered, saturated carbocycle or heterocycle in cooperation with the adjacent carbon atom; and X represents oxygen, sulfur, SO2, NR6 (R6 represents hydrogen or alkyl), or a single bond, or a pharmaceutically acceptable salt of the compound. The compound and salt are useful as a medicine.

Abstract: This invention relates to a combination product, as defined herein, comprising a MEK inhibitor and a mTOR-selective inhibitor, and to methods for the production of an anti-cancer effect in a patient, which is accordingly useful in the treatment of cancer in a patient. More specifically the present invention relates to; a combination product, as defined herein, comprising a MEK inhibitor and a mTOR-selective inhibitor; a combination product, as defined herein, comprising a kit of parts comprising a MEK inhibitor and a mTOR-selective inhibitor; use of the combination product, as defined herein, in the treatment of cancer; a method of treating cancer comprising administering the combination product, as defined herein, to a patient. The combination product, as defined herein, and methods of the invention are also useful in the treatment of other diseases associated with the activity of MEK, and/or mTOR.