Zambon Group S.p.a.

Zambon S.p.a.

Gabriele Morazzoni

Mauro Napoletano

Gabriele Pietro Norcini

Franco Pellacini

Giancarlo Grancini

Francesco Santangelo

Daniela Botta

Ermanno Moriggi

Andrea Mereu

Fernando Ornaghi

Roberto Longoni

Carlo Riva

Luciano Pacchetti

Gian Marco Leali

Livius Cotarca

Massimo Verzini

Dario Braga

Paolo Maragni

Roberto Brescello

Ivan Michieletto

Julio Alvarez-Builla

Angelo Restelli

Franco Massaccesi

Elisa Melotto

Lorenzo Pradella

Alessandro Di Maria

Jorge G Siro Herrero

Jos&eacute; Luis Garcia Navaio

Dario Università Di Bologna Braga

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.

Crystalline forms of macrolide compounds endowed with antiinflammatory activity

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.

Macrolide compounds endowed with antiinflammatory activity

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.

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.

9a-azalides with anti-inflammatory activity

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 (C )alkyl optionally substituted; R is (C )alkyl or polyfluoro(C )-alkyl; R is (C )cycloalkyl optionally containing an oxygen atom and optionally substituted; and the N&rarr;O derivatives and pharmaceutically acceptable salt thereof are PDE 4 and TNF&agr; inhibitors.

Phthalazine derivatives as phosphodiesterase 4 inhibitors

Tricyclic phthalazine derivatives as phosphodiesterase 4 inhibitors

Phthalazine derivatives phosphodiesterase 4 inhibitors

Benzazine derivatives as phosphodiesterase 4 inhibitors

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&rarr;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.

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-&lcub;3-&lcub;1-(3,5-dichloro-pyridin-4-ylmethyl)-6-methoxy-phthalazin-5-yl&rcub;-prop-2-ynyl&rcub;-methyl-amine; 1-(3,5-dichloro-pyridin-4-ylmethyl)-6-methoxy-5-(5-morpholin-4-yl-pent-1-ynyl)-phthalazine dihydrochloride; 3-&lcub;1-(3,5-dichloro-pyridin-4-ylmethyl)-6-methoxy-phthalazin-5-yl&rcub;-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&rarr;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.

Benzazine derivatives phosphodiesterase 4 inhibitors

Phosphonyldipeptides useful in the treatment of cardiovascular diseases

Phosphinic acid derivatives with metallopeptidase inhibitory activity

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Lainate, Italy

Gabriele Morazzoni