Abstract: The present invention relates to novel oxadiazole derivatives having pharmacological activity, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders.

Abstract: A compound of formula (I): wherein A1 represents 2,3-dihydro-1-benzofuran-7-yl, 5-fluoro-2-methoxy-phenyl or 5-fluoro-2-hydroxy-phenyl; X represents —C(R3)— or nitrogen; when X represents —C(R3)—, R2 represents hydrogen and R1 represents fluorine, R3 represents hydrogen or fluorine, when X represents —C(R3)— and R2 and R1 each represent hydrogen, R3 represents hydrogen, hydroxy, methoxy or fluorine, when X represents —C(R3)— and R2 represents hydroxy, methoxy, —CO2CH3 or —CO2CH2CH3, R1 and R3 each represent hydrogen, when X represents nitrogen, R1 and R2 each represent hydrogen; and Y represents H or methyl; or a physiologically functional derivative thereof.

Abstract: The present invention relates to novel oxadiazole derivatives having pharmacological activity, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders.

Abstract: The present invention relates to novel piperazine and azepine derivatives having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of neurodegenerative disorders including Alzheimer's disease.

Abstract: There are provided according to the invention novel compounds of formula (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, R19, R20, and R34 are as described in the specification, processes for preparing them, formulations containing them and their use in therapy for the treatment of inflammatory diseases.

Abstract: Compounds of formula (I): wherein: R1 represents substituted or unsubstituted heteroaryl; Y represents —(CRnaRnb)n—; Rna and Rnb are each independently hydrogen or C1-6alkyl; n is an integer from 0 to 5; R2 represents unsubstituted or substituted aryl or unsubstituted or substituted heteroaryl; R3 and R4 each independently represent hydrogen or C1-6-alkyl; R7 represents hydrogen or C1-6alkyl; R8 represents hydrogen or C1-6alkyl; and salts and solvates thereof; are CCR3 antagonists and are thus indicated to be useful in therapy.

Abstract: There are provided according to the invention novel compounds of formula (I) and pharmaceutically acceptable salts and solvates thereof, wherein: R1 is phenyl which may be unsubstituted or substituted by one or two substituents selected from fluorine, chlorine, C1-2alkoxy-, —CN; phenyl fused to a 5-membered saturated ring containing one oxygen atom; pyridinyl which may be unsubstituted or substituted by one or two substituents selected from fluorine or chlorine; or C-linked pyrazolyl which may be unsubstituted or substituted by the substituent C1-2alkyl; R2 is C1-4alkyl; R3 is C1-2alkyl; and n is 0, 1 or 2.

Abstract: There are provided according to the invention novel compounds of formula (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, R19, R20, and R34 are as described in the specification, processes for preparing them, formulations containing them and their use in therapy for the treatment of inflammatory diseases.

Abstract: A compound of formula (I): wherein A1 represents 2,3-dihydro-1-benzofuran-7-yl, 5-fluoro-2-methoxy-phenyl or 5-fluoro-2-hydroxy-phenyl; X represents —C(R3)— or nitrogen; when X represents —C(R3)—, R2 represents hydrogen and R1 represents fluorine, R3 represents hydrogen or fluorine, when X represents —C(R3)— and R2 and R1 each represent hydrogen, R3 represents hydrogen, hydroxy, methoxy or fluorine, when X represents —C(R3)— and R2 represents hydroxy, methoxy, —CO2CH3 or —CO2CH2CH3, R1 and R3 each represent hydrogen, when X represents nitrogen, R1 and R2 each represent hydrogen; and Y represents H or methyl; or a physiologically functional derivative thereof.

Abstract: There are provided according to the invention novel compounds of formula (I) and pharmaceutically acceptable salts and solvates thereof: wherein R1 is selected from the group consisting of C1-4alkyl, C4-6cycloalkyl(CH2)m—, methoxyC2-4alkyl, HOCH2CH2—, R3(O)2S(CH2)2—, R5R4NCO(CH2)n—, and heterocyclyl(CH2)m— wherein any nitrogen heteroatom of the heterocyclyl radical may be unsubstituted or substituted by methyl; R2 is hydrogen or methyl; R3 is methyl or NH2; R4-5 independently represent methyl, m is 0, 1 or 2; and n is 1 or 2; or R1 and R2 together with the nitrogen atom to which they are attached may form a heterocyclyl ring, which may be unsubstituted or substituted by one or two substituents selected from the group consisting of; methyl, ?O and (CH3)2N—.

Abstract: Compounds of formula (I) or pharmaceutically acceptable salts thereof are inhibitors of phosphodiesterase type IV (PDE4) and are of use in the treatment of inflammatory and/or allergic diseases.

Abstract: There are provided according to the invention, novel compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, X, a, b and Z are as defined in the specification, processes for preparing them, formulations containing them and their use in therapy for the treatment of inflammatory diseases.

Abstract: The present invention relates to novel morpholin-acetamide compounds of formula (I) useful for the treatment of inflammatory diseases. Compounds of formula (I) wherein R1, R2, R3, R4, R5, X, a, b and Z are as defined in the specification, processes for preparing them, formulations containing them and their use in therapy for the treatment of inflammatory diseases.

Abstract: A compound of formula (I), wherein R2 represents C1-3alkyl, halogen or hydrogen; R3 represents straight or branched alkyl group of 1-6 carbon atoms; with the proviso that, when R3 represents C1-3alkyl, R2 represents C1-3alkyl, R1 cannot represent phenyl optionally substituted by one or more substituents selected from halogen, C1-3alkyl, trifluoromethyl, nitro, cyano, —CO2Rc, —CONRcRd, —CORc, —SORe, —SO2Re, —SO3H, —SO2NRcRd, —ORc, —NHSO2Re, —NHCORc and —NRcRd; and salts and solvates thereof, in particular, physiologically acceptable solvates and salts thereof. These compounds are agonists at the Adenosine A1 receptor.

Abstract: There are provided according to the invention, novel compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, X a, b, and Z are as defined in the specification, processes for preparing them, formulations containing them and their use in therapy for the treatment of inflammatory diseases.

Abstract: Compounds of formula (I) wherein: R1 represents C1-16 alkyl, C2-6alkenyl, C2-6alkynyl, C2-6alkynyl-Y1—, aryl-Y1—, heteroaryl-Y1—, aryl-(O)t-aryl-Y1—, aryl-(O)t-heteroaryl-Y1—, heteroaryl-(O)t-aryl-Y1—, heteroaryl-(O)t-heteroaryl-Y1—, C2-6 alkenyl-Y1—, aryl-O—Y1—, heteroaryl-O—Y1—, C1-16 alkyl-SO2—Y1—,M—Y1—,J2-Y1—, —CN or C3-8 cycloalkyl-Y1— or C3-8 cycloalkenyl-Y1—, which cycloalkyl or cycloalkenyl may be optionally substituted by one or more hydroxyl or C1-16 Alkyl groups; R2 represents hydrogen or C1-16 alkyl; X represents ethylene or a group of formula CReRf wherein Re and Rf independently represent hydrogen or C1-14 alkyl or Re and Rf may together with the carbon atom to which they are attached form a C3-8 cycloalkyl group; R3 and R4 independently represent hydrogen or C1-14 alkyl; Z represents a bond, CO, SO2, CR9R6(CH2)n, (CH2)nCR9R6, CHR6(CH2)nO, CHR6(CH2)nS, CHR6(CH2)nOCO, CHR6(CH2)n

Abstract: A method of treating a patient suffering from or susceptible to ischemic heart disease, peripheral vascular disease or stroke or which subject is suffering pain, a CNS disorder or sleep apnea which comprises administering a therapeutically effective amount of an adenosine derivative which is an agonist at the adenosine A1 receptor and which exhibits little or no agonist activity of the A3 receptor.

Abstract: A compound of formula (I), wherein R2 represents C1-3alkyl, halogen or hydrogen; R3 represents straight or branched alkyl group of 1-6 carbon atoms; with the proviso that, when R3 represents C1-3alkyl, R2 represents C1-3alkyl, R1 cannot represent phenyl optionally substituted by one or more substituents selected from halogen, C1-3alkyl, trifluoromethyl, nitro, cyano, —CO2Rc, —CONRcRd, —CORc, —SORe, —SO2Re, —SO3H, —SO2NRcRd, —ORc, —NHSO2Re, —NHCORc and —NRcRd; and salts and solvates thereof, in particular, physiologically acceptable solvates and salts thereof. These compounds are agonists at the Adenosine A1 receptor.

Abstract: A method of treating a patient suffering from or susceptible to ischemic heart disease, peripheral vascular disease or stroke or which subject is suffering pain, a CNS disorder or sleep apnea which comprises administering a therapeutically effective amount of an adenosine derivative which is an agonist at the adenosine A1 receptor and which exhibits little or no agonist activity of the A3 receptor.

Abstract: A compound of formula (I), wherein R2 represents C1-3alkyl, halogen or hydrogen; R3 represents straight or branched alkyl group of 1-6 carbon atoms; with the proviso that, when R3 represents C1-3alkyl, R2 represents C1-3alkyl, R1 cannot represent phenyl optionally substituted by one or more substituents selected from halogen, C1-3alkyl, trifluoromethyl, nitro, cyano, —CO2Rc, —CONRcRd, —CORc, —SORe, SO2Re, —SO3H, —SO2NRcRd, —ORc, —NHSO2Re, —NHCORc and —NRcRd; and salts and solvates thereof, in particular, physiologically acceptable solvates and salts thereof. These compounds are agonists at the Adenosine Al receptor.