Abstract: Therapeutically active anthranilic acid derivatives of Formula (I), processes for the preparation of said derivatives, pharmaceutical formulations containing the compounds and the use of the compounds in therapy, particularly in the treatment of diseases in which under-activation of the HM74A receptor contributes to the disease or in which activation of the receptor will be beneficial, are disclosed.

Abstract: The present invention provides therapeutically active compounds which are xanthine derivatives, processes for the manufacture of said derivatives, pharmaceutical formulations containing the active compounds and the use of the compounds in therapy, particularly in the treatment of diseases where under-activation of the HM74A receptor contributes to the disease or where activation of the receptor will be beneficial, having the formula (II): wherein R1 is selected from: hydrogen and C1-4 alkyl which may be optionally substituted with one or more groups selected from CN and CF3, R2 is selected from: C2-10 unsubstituted alkyl, C1-10 alkyl substituted with one or more groups selected from fluorine and CN, C5 alkenyl, unbranched C4 alkenyl, and C1-4 alkyl substituted with cycloalkyl, and R3 is selected from halogen and CN.

Abstract: The present invention concerns the compounds having the formula (I), N-oxides, salt, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereof, wherein Haryl is an aromatic monocyclic, bicyclic or tricyclic heterocycle having 3 to 14 ring members which contains one or more heteroatom ring members selected from nitrogen, oxygen and sulfur and which may optionally be substituted on (i) one or more carbon atoms by C1-6alkyl, halogen, hydroxy, optionally mono- or disubstituted amino, nitro, cyano, haloC1-6alkyl, carboxyl, C3-7cycloalkyl, optionally mono- or disubstituted aminocarbonyl, methylthio, methylsulfonyl, aryl, (R7a)n-M-R7b, Het1 and Het2; whereby the optional substituents on any amino function are independently selected from R5 and -A-R6; and on (ii) a nitrogen atom if present by hydroxy or -A-R6. It further relates to their use as broadspectrum HIV protease inhibitors, processes for their preparation as well as pharmaceutical compositions and diagnostic kits comprising them.

Abstract: The invention provides compounds of formula (I) wherein A and B represent the groups —(CH2)m- and —(CH2)n-respectively; R1 represents hydrogen or C1-6alkyl; R2 represents hydrogen, halogen, hydroxy, cyano, nitro, hydroxyC1-6alkyl, trifluoromethyl, trifluoromethoxy, C1-6alkyl, C1-6alkoxy, C1-6alkoxyC1-6alkyl, C3-7cycloalkylC1-6alkoxy, —(CH2)pC3-6cycloalkyl, —(CH2)pC3-6cycloalkyloxy, —COC1-6alkyl, —SO2C1-6alkyl, —SOC1-6alkyl, —S—C1-6alkyl, C1-6alkylsulfonyloxy, C1-6alkylsulfonylC1-6alkyl, —CO2C1-6alkyl, —CO2NR7R8, —SO2NR7R8, C1-6alkylsulfonamido, C1-6alkylsulfonamidoC1-6alkyl, —(CH2)pNR7R8, C1-6alkylamidoC1-6alkyl, —(CH2)pNR7COR8, arylsulfonyl, arylsulfonyloxy, arylsulfonylC1-6alkyl, arylsulfonamido, arylcarboxamido, arylsulfonamidoC1-6alkyl, arylcarboxamidoC1-6alkyl, aroyl, aroylC1-6alkyl, arylC1-6alkanoyl, —SO2NR7R8, optionally substituted aryl, optionally substituted heteroaryl or optionally substituted heterocyclyl, or a group CONR7R8 or SO2NR7R8 wherein R7 and R8 together may be fused to form a 5-

Abstract: The present invention relates to novel sulfonamide compounds having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of CNS and other disorders.

Abstract: A compound of formula (I) or a salt thereof, or a solvate thereof, wherein: X represents oxygen, sulphur, or NRb; Y and Z each independently represent nitrogen, CH, CR1 or CR2; A represents an unsubstituted or substituted aryl group or an unsubstituted or substituted heterocyclyl group; Ra represents —C(O)NRsRt; R1 and R2 each independently represents hydrogen or specific substituents; and the use of such a compound in the treatment and/or prophylaxis of diseases associated with over activity of osteoclasts in mammals.