Abstract: A compound of formula (I) and pharmaceutically acceptable derivatives thereof, in which R1 is H or C1-4alkyl; R2 is R3 is C1-6alkyl or NH2. Compounds of formula (I) are potent and selective inhibitors of COX-2 and are of use in the treatment of the pain, fever, inflammation of a variety of conditions and diseases.

Abstract: The invention provides the compounds of formula (I) and pharmaceutically acceptable derivatives thereof, in which: R1 and R2 are independently selected from H, or C1-6alkyl, R3 is C1-6alkyl or NH2: R4 is H or C1-6alkyl: A is and 5- or 6-membered aryl, or a 5- or 6-membered aryl substituted by one or more R5; R5 is halogen, C1-6alkyl, C1-6alkyl substituted by one ore more F, C1-6alkoxy, C1-6alkoxy substituted by one or more F, SO2NH2 or SO2C1-6alkyl; and n is 1 to 4. Compounds of formula (I) are potent and selective inhibitors of COX-2 and are of use in the treatment of the pain, fever, inflammation of a variety of conditions and diseases.

Abstract: The invention provides the compounds of formula (I) 1

Abstract: The invention provides a COX-2 inhibitor or a pharmaceutically acceptable derivative thereof for use in the treatment of a disorder ameliorated by a gastroprokinetic.

Abstract: The present invention provides a method of treating conditions associated with pain and alleviating the symptoms associated therewith which comprises administering to a mammal, including man, an adenosine A1 agonist or a physiologically acceptable salt or solvate thereof and a 5HT3 antagonist or a physiologically acceptable salt or solvate thereof. The present invention also provides pharmaceutical formulations and patient packs comprising said combinations.

Abstract: The invention provides a COX-2 inhibitor or a pharmaceutically acceptable derivative thereof for use in the treatment of constipation.

Abstract: The invention provides the compounds of formula (I) 1

Abstract: The present invention provides a method of treating conditions associated with pain and alleviating the symptoms associated therewith which comprises administering to a mammal, including man, an adenosine A1 agonist or a physiologically acceptable salt or solvate thereof and a sodium channel blocker or a physiologically acceptable salt or solvate thereof. The present invention also provides pharmaceutical formulations and patient packs comprising said combinations.

Abstract: The present invention provides a method of treating conditions associated with pain and alleviating the symptoms associated therewith which comprises administering to a mammal, including man, (i) an adenosine A1 agonist or a physiologically acceptable salt or solvate thereof and (ii) gabapentin or pregabalin or a physiologically acceptable salt or solvate thereof. The present invention also provides pharmaceutical formulations and patient packs comprising said combinations.

Abstract: The present invention provides a method of treating conditions associated with pain and alleviating the symptoms associated therewith which comprises administering to a mammal, including man, an adenosine A1 agonist or a physiologically acceptable salt or solvate thereof and an NSAID, e.g. a COX-2 inhibitor, or a physiologically acceptable salt or solvate thereof. The present invention also provides pharmaceutical formulations and patient packs comprising said combinations.

Abstract: The present invention provides a method of treating conditions associated with pain and alleviating the symptoms associated therewith which comprises administering to a mammal, including man, an adenosine A1 agonist or a physiologically acceptable salt or solvate thereof and an opioid or a physiologically acceptable salt or solvate thereof. The present invention also provides pharmaceutical formulations and patient packs comprising said combinations.

Abstract: The present invention provides a method of treating conditions associated with pain and alleviating the symptoms associated therewith which comprises administering to a mammal, including man, an adenosine A1 agonist or a physiologically acceptable salt or solvate thereof and a 5HT1 receptor agonist or a physiologically acceptable salt or solvate thereof. The present invention also provides pharmaceutical formulations and patient packs comprising said combinations.

Abstract: The present invention provides a method of treating conditions associated with pain and alleviating the symptoms associated therewith which comprises administering to a mammal, including man, a adenosine A1 agonist or a physiologically acceptable salt or solvate thereof and an EP1 antagonist or a physiologically acceptable salt or solvate thereof. The present invention also provides pharmaceutical formulations and patient packs comprising said combinations.

Abstract: The invention provides the compounds of formula (I) wherein: R0 and R1 are independently selected from H, halogen, C1-6alkyl, C1-6alkoxy, or C1-6alkoxy substituted by one or more fluorine atoms; R2 is halogen, CN, CONR4R5, CO2H, CO2C1-6alkyl, or NHSO2R4; R3 is C1-6alkyl or NH2; and R4 and R5 are independently selected from H, C1-6alkyl, phenyl, phenyl substituted by one or more atoms or groups (selected from halogen, C1-6alkyl, C1-6alkoxy, or C1-6alkoxy substituted by one or more fluorine atoms), or together with the nitrogen atom to which they are attached form a saturated 4 to 8 membered ring; and pharmaceutically acceptable derivatives thereof. Compounds of formula (I) are potent and selective inhibitors of COX-2 and are of use in the treatment of the pain, fever, inflammation of a variety of conditions and diseases.

Abstract: The invention provides the compounds of formula (I) and pharmaceutically acceptable derivatives thereof in which: R0 is halogen, C1-6alkyl, C1-6alkoxy, C1-6alkoxy substituted by one or more fluorine atoms, or O(CH2)nNR4R5; R1 and R2 are independently selected from H, C1-6alkyl, C1-6alkyl, substituted by one or more fluorine atoms, C1-6alkoxy, C1-6hydroxyalkyl, SC1-6alkyl, C(O)H, C(O)C1-6alkyl, C1-6alkylsulphonyl, C1-6alkoxy substituted by one or more fluorine atoms, O(CH2)nCO2C1-6alkyl, O(CH2)nSC1-6alkyl, (CH2)nNR4R5, (CH2)nSC1-6alkyl or C(O)NR4R5; with the proviso that when R0 is at the 4-position and is halogen, at least one of R1 and R2 is C1-6alkylsulphonyl, C1-6alkoxy substituted by one or more fluorine atoms, O(CH2)nCO2C1-6alkyl, O(CH2)nSC1-6alkyl, (CH2)nNR4R5 or (CH2)nSC1-6alkyl, C(O)NR4R5; R3 is C1-6alkyl or NH2; R4 and R5 are independently selected from H, or C1-6alkyl or, together with the nitrogen atom to which they are attached, form a 4-8 membered saturated ring; and n is 1-4.

Abstract: The present invention relates to benzofuran derivatives of formula (I) as shown below. ##STR1## The invention also relates to pharmaceutically acceptable salts and solvates of the derivatives of formula (I) as well as to processes for their preparation and to their use in the treatment of conditions mediated by tachykinins.

Abstract: The present invention relates to piperidine derivatives of formula (I) ##STR1## wherein R.sup.1 is a C.sub.1-4 alkoxy group; R.sup.2 is ##STR2## R.sup.3 is a hydrogen or halogen atom; R.sup.4 and R.sup.5 may each independently represent a hydrogen or halogen atom, or a C.sub.1-4 alkyl, C.sub.1-4 alkoxy or trifluoromethyl group;R.sup.6 is a hydrogen atom, a C.sub.1-4 alkyl, (CH.sub.2).sub.m cyclopropyl, --S(O).sub.n C.sub.1-4 alkyl, phenyl, NR.sup.7 R.sub.8, CH.sub.2 C(O)CF.sub.3 or trifluoromethyl group;R.sup.7 and R.sup.8 may each independently represent a hydrogen atom, or a C.sub.1-4 alkyl or acyl group;x represents zero or 1;n represents zero, 1 or 2;m represents zero or 1;and pharmaceutically acceptable salts and solvates thereof; to processes for their preparation; and their use in the treatment of conditions mediated by tachykinins.

Abstract: The present invention relates to piperidine derivatives of formula (I) ##STR1## wherein R.sup.1 is a C.sub.1-4 alkoxy group; R.sup.2 is ##STR2## R.sup.3 is a hydrogen or halogen atom; R.sup.4 and R.sup.5 may each independently represent a hydrogen or halogen atom, or aC.sub.1-4 alkyl, C.sub.1-4 alkoxy or trifluoromethyl group;R.sup.6 is a hydrogen atom, a C.sub.1-4 alkyl, (CH.sub.2).sub.m cyclopropyl, --S(O).sub.n C.sub.1-4 alkyl, phenyl,NR.sup.7 R.sup.8, CH.sub.2 C(O)CF.sub.3 or trifluoromethyl group;R.sup.7 and R.sup.8 may each independently represent a hydrogen atom, or a C.sub.1-4 alkyl or acyl group;x represents zero or 1;n represents zero, 1 or 2;m represents zero or 1;and pharmaceutically acceptable salts and solvates thereof; to processes for their preparation; and their use in the treatment of conditions mediated by tachykinins.

Abstract: The present invention relates to the use of tachykinin antagonists, including substance P antagonists and other neurokinin antagonists, in the treatment of emesis. Also described are novel tachykinin antagonists of formula (I), processes for their preparation, pharmaceutical compositions containing them and their medical use. ##STR1## wherein R represents the ring A ##STR2## or 2-pyridinyl or 2-pyridinyl-N-oxide; R.sup.1 is selected from halogen atoms and C.sub.1-4 alkyl, C.sub.1-4 alkoxy, trifluoromethyl, and S(O).sub.n C.sub.1-4 alkyl groups;R.sup.2 and R.sup.3, which may be the same or different, each independently are selected from hydrogen and halogen atoms and C.sub.1-4 alkyl, C.sub.1-4 alkoxy, trifluoromethyl and cyano groups;n represents zero, 1 or 2;and pharmaceutically acceptable salts and solvates thereof.

Abstract: The invention provides compounds of the general formula (I) ##STR1## or a physiologically acceptable salt or solvate thereof, wherein Q represents a 1- or 2-naphthalenyl group.The compounds have a stimulant action at .beta..sub.2 -adrenoreceptors and may be used in the treatment of diseases associated with reversible airways obstruction such as asthma and chronic bronchitis.