Abstract: The present invention relates to macrolide compounds endowed with antiinflammatory activity and more particularly relates to new stable crystalline forms of a macrolide derivative with antiinflammatory activity, processes for the preparation of such forms, pharmaceutical compositions containing them as active ingredient and the use of said crystalline forms for the treatment of inflammatory diseases.

Abstract: Macrolide compounds endowed with antiinflammatory activity are described, and more particularly macrolide derivatives lacking cladinose in position 3, with antiinflammatory activity, pharmaceutically acceptable salts thereof and pharmaceutical compositions containing them as active ingredient.

Abstract: Macrolide compounds endowed with antiinflammatory activity are described, and more particularly macrolide derivatives lacking cladinose in position 3, with antiinflammatory activity, pharmaceutically acceptable salts thereof and pharmaceutical compositions containing them as active ingredient.

Abstract: Macrolide compounds lacking cladinose in position 3 having antiinflammatory activity and substantially free of antibiotic properties, pharmaceutically acceptable salts thereof, and pharmaceutical compositions containing them as active ingredient.

Abstract: the present invention relates to macrolide compounds endowed with antiinflammatory activity and more particularly relates to new stable crystalline forms of a macrolide derivative with antiinflammatory activity, processes for the preparation of such forms, pharmaceutical compositions containing them as active ingredient and the use of said crystalline forms for the treatment of inflammatory diseases.

Abstract: The present invention relates to a compound of formula (IA) as defined in the specification or a pharmaceutically acceptable sat thereof, in the preparation of a medicament for both the treatment of inflammatory bowel diseases and the prevention of colon cancer.

Abstract: Macrolides with anti-inflammatory activity are described. Particularly described are 9a-azalides and their anti-inflammatory activity without cladinose in position 3, the pharmaceutically acceptable salts thereof and the pharmaceutical composition that contain them as active principle.

Abstract: Compounds of formula I wherein R and R1 are as defined in the description. The compounds of formula I are PDE 4 inhibitors.

Abstract: Macrolides with anti-inflammatory activity are described, and more particularly, 9a-azalides without cladinose in position 3 with anti-inflammatory activity, their pharmaceutically acceptable salts and pharmaceutical compositions that contain them as active principle.

Abstract: Macrolide compounds endowed with antiinflammatory activity are described, and more particularly macrolide derivatives lacking cladinose in position 3, with antiinflammatory activity, pharmaceutically acceptable salts thereof and pharmaceutical compositions containing them as active ingredient.

Abstract: A process for preparing a compound of formula I: 1

Abstract: Compounds of formula (I) wherein B is alkylene, amino, CONH or a bond; Cy is optionally substituted phenyl or heteroaryl; R is H, phenyl or (C1-4)alkyl optionally substituted; R1 is (C1-6)alkyl or polyfluoro(C1-6)-alkyl; R2 is (C4-7)cycloalkyl optionally containing an oxygen atom and optionally substituted; and the N→O derivatives and pharmaceutically acceptable salt thereof are PDE 4 and TNF&agr; inhibitors.

Abstract: Tricyclic phthalazine compounds of formula (I) wherein A is a 5-7 membered heterocycle containing from 1 to 4 nitrogen atoms, optionally partially or totally unsaturated, and optionally substituted by a (C1-4)alkyl group in turn optionally substituted; Z is NH, methylene, a C2-6 alkylene chain optionally branched and/or unsaturated and/or interrupted by a C5-7 cycloalkyl residue; Cy is phenyl or heterocycle optionally substituted by one or more substituents, or a COR4 group wherein R4 is hydroxy, alkoxy, amino optionally substituted by one or two (C1-6)alkyl groups or by hydroxy; R is a (C1-6)alkyl or polyfluoro(C1-6)alkyl group; R1 is hydrogen; a (C1-8)-alkyl, (C2-8)-alkenyl or (C2-8)-alkynyl group optionally substituted by hydroxy, oxo, aryl or heterocycle, and optionally interrupted by one or more heteroatoms or heterogroups; a (C1-4)alkoxy group or a (C4-7)cycloalkoxy group optionally containing an oxygen atom and optionally substituted by a polar substituent in the cyclic moiety, arylox

Abstract: Phthalazine compounds having formula I wherein , A, B, R, R1, R2 and R3 are as defined herein, useful as phosphodiesterase 4 inhibitors.

Abstract: Compounds of formula (I), wherein is a single or double bond; Z is NH, methylene, a (C2-C6)alkylene chain optionally branched and/or unsaturated and/or interrupted by a (C5-C7)cycloalkyl residue; A is phenyl or heterocycle optionally substituted or a COR4 group wherein R4 is hydroxy, (C1-C6)-alkoxy, amino optionally substituted; R is a (C1-C6)alkyl or polyfluoro(C1-C6)alkyl group; R1 is absent when is a double bond or, when is a single bond, is (a) hydrogen; (b) (C1-C6)alkyl optionally substituted; (c) —COR6 wherein R6 is hydrogen, aryl, aryl-(C1-C6)alkyl, amino optionally alkylated or monohydroxylated, hydroxy, (C1-C4)alkoxy, carboxy, (C1-C4)alkoxycarbonyl, formula (1), or (C1-C4)alkyl optionally substituted by heterocycle; (d) (C1-C4)-alkylsulfonyl; R2 represents two hydrogen atoms or a group —O when is a single bond, or, when is a double bond, R2 is hydrogen, cyano, (C1-C4)alkoxycarbonyl, amido, optionally substituted aryl or heterocycle, (C1-C8)alkyl, (C2-C8)alkenyl or (

Abstract: The present invention relates to phthalazine derivatives, pharmaceutical compositions containing them, and to their use as phosphodiesterase 4 inhbitors.

Abstract: Compounds of formula I: wherein A is a heterocycle containing a nitrogen atom and optionally saturated or unsaturated and optionally further substituted by an oxo group (═O); R is: hydrogen, cyano, (C1-4)alkoxycarbonyl, carbamoyl; optionally substituted (C4-7)-cycloalkyl, aryl or heterocycle; (C1-8)alkyl, (C2-8)alkenyl or (C2-8)alkynyl optionally branched and/or substituted by (C4-7) cycloalkyl, aryl or heterocycle; aryloxy, heterocyclyloxy, aryl(C1-4)alkoxy, heterocyclyl(C1-4)alkoxy, amino substituted by one or two (C1-4)alkyl group(s), aryl-amino, heterocyclyl-amino, aryl(C1-4)alkyl-amino, or heterocyclyl(C1-4)alkylamino; Y is methylene or ethylene; W is an optionally substituted aryl or heterocycle; R1 is hydrogen, (C4-7)cycloalkyl or a (C2-8)alkyl, (C2-8)alkenyl or (C2-8)alkynyl group optionally substituted by hydroxy, oxo, (C4-7)cycloalkyl, aryl or heterocycle, and optionally interrupted by one or more heteroatom(s) or heterogroup(s); R2 is a (C1-6)alkyl or polyfluoro(C1-6)alkyl gr

Abstract: The present invention provides a compound selected from the group including: N-3-acetyl-1-(3,5-dichloropyridin-4-ylmethyl)-5-cyclopentyloxy-6-methoxy-4H-phthalazine; 6,7-dimethoxy-1-pyridin-4-ylmethyl-4-thiazol-2-yl-phthalazine; 1-(6,7-dimethoxy-4-pyridin-4-ylmethyl-1H-phthalazin-2-yl)ethanone; 2-methanesulphonyl-6,7-dimethoxy-4-pyridin-4-ylmethyl-1,2-dihydrophthalazine; 2-formyl-6,7-dimethoxy-4-pyridin-4-ylmethyl-1,2-dihydrophthalazine; 1-(6,7-dimethoxy-4-pyridin-4-ylmethyl-1H-phthalazin-2-yl)-1-imidazol-1-ylmethanone; 1-(3,5-dichloro-pyridin-4-ylmethyl)-3-methansulphonyl-6-difluoromethoxy-5-(tetrahydro-furan-2-yloxy)-4H-phthalazine; N→O derivatives thereof; and pharmaceutically acceptable salts thereof. The invention also provides a pharmaceutical composition, which contains a therapeutically effective amount of the above compound in admixture with a pharmaceutically acceptable carrier.

Abstract: The present invention provides a compound selected from the group including: 1-(3,5-dichloro-pyridin-4-ylmethyl)-6-methoxy-4-phenyl-phthalazine; 4-(3,5-dichloro-pyridin-4-ylmethyl)-7-methoxy-1H-phthalazin-2-carboxylic acid methyl ester; benzyl-{3-{1-(3,5-dichloro-pyridin-4-ylmethyl)-6-methoxy-phthalazin-5-yl}-prop-2-ynyl}-methyl-amine; 1-(3,5-dichloro-pyridin-4-ylmethyl)-6-methoxy-5-(5-morpholin-4-yl-pent-1-ynyl)-phthalazine dihydrochloride; 3-{1-(3,5-dichloro-pyridin-4-ylmethyl)-6-methoxy-phthalazin-5-yl}-prop-2-yn-1-ol; 1-(3,5-dichloro-pyridin-4-ylmethyl)-6-methoxy-4-morpholin-4-yl-phthalazine; 1-(3,5-dichloro-pyridin-4-ylmethyl)-6-methoxy-4-(1,2,4)triazol-1-yl-phthalazine; N→O derivatives thereof; and pharmaceutically acceptable salts thereof. The invention also provides a pharmaceutical composition which includes a therapeutically effective amount of the above compound in admixture with a suitable carrier.

Abstract: Compounds of formula (I) wherein A is an orthocondensed heterocycle optionally substituted by certain substituents and necessarily substituted by a —B—Cy group where the variables are as defined in the specification and the N→O derivatives and pharmaceutically acceptable salts thereof are phosphodiesterase-4 inhibitors.