Patents by Inventor Mauro Napoletano

Mauro Napoletano has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).

  • Publication number: 20080319057
    Abstract: 2-Phenylethylamino substituted carboxamide derivatives of formula (I); wherein J, W, R0, R1, R2, R3, and R4 have the meanings as defined in the specification and pharmaceutically acceptable salts thereof, pharmaceutical compositions containing them as active ingredient and their use as sodium and/or calcium channel modulators useful in preventing alleviating and curing a wide range of pathologies, including neurological, psychiatric, cardiovascular, inflammatory, ophthalmic, urology, and gastrointestinal diseases where the above mechanisms have been described as playing a pathological role, are described.
    Type: Application
    Filed: November 29, 2006
    Publication date: December 25, 2008
    Inventors: Florian Thaler, Mauro Napoletano, Cibele Sabido-David, Ermanno Moriggi, Carla Caccia, Laura Faravelli, Alessandra Restivo, Patricia Salvati
  • Patent number: 7419961
    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.
    Type: Grant
    Filed: October 28, 2003
    Date of Patent: September 2, 2008
    Assignee: Zambon S.p.A.
    Inventors: Mauro Napoletano, Andrea Mereu, Ermanno Moriggi, Fernando Ornaghi, Gabriele Morazzoni, Franco Pellacini
  • Publication number: 20080108679
    Abstract: The present invention relates to new pharmaceutical uses of an isoxazolic derivative or a pharmaceutically acceptable salt thereof in the preparation of a medicament useful for treating the neuropathic pain.
    Type: Application
    Filed: November 14, 2005
    Publication date: May 8, 2008
    Applicant: ZAMBON S.P.A.
    Inventors: Mauro Napoletano, Ermanno Moriggi
  • Publication number: 20070167381
    Abstract: Macrolide compounds of formula (I) wherein X, R, R1, R2, R3 and R4, have the meanings as defined in the specification, pharmaceutically acceptable salts thereof, pharmaceutical compositions containing them as active ingredient and the use thereof in the treatment and prophylaxis of inflammatory diseases, are described.
    Type: Application
    Filed: January 25, 2005
    Publication date: July 19, 2007
    Inventors: Andrea Mereu, Mauro Napoletano, Fernando Ornaghi, Ermanno Moriggi, Franco Pellacini
  • Publication number: 20060166996
    Abstract: Compounds of formula I wherein R and R1 are as defined in the description. The compounds of formula I are PDE 4 inhibitors.
    Type: Application
    Filed: December 22, 2003
    Publication date: July 27, 2006
    Applicant: Zambon Group S.P.A.
    Inventors: Mauro Napoletano, Franco Pellacini, Gabriele Morazzoni, Jean-Dominique Moriggi, Carlo Riva, Thomas Haack, Leopoldo Allievi, Marco Pauselli
  • Publication number: 20060166904
    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.
    Type: Application
    Filed: October 28, 2003
    Publication date: July 27, 2006
    Applicant: ZAMBON GROUP S.P.A.
    Inventors: Mauro Napoletano, Andrea Mereu, Ermanno Moriggi, Fernando Ornaghi, Gabriele Morazzoni, Franco Pellacini
  • Publication number: 20060058246
    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.
    Type: Application
    Filed: July 29, 2003
    Publication date: March 16, 2006
    Applicant: ZAMBON GROUP S.P.A.
    Inventors: Mauro Napoletano, Ermanno Moriggi, Andrea Mereu, Fernando Ornaghi, Gabriele Morazzoni, Roberto Longoni, Carlo Riva, Luciano Pacchetti, Franco Pellacini
  • Patent number: 6894164
    Abstract: A process for the preparation of phthalazines by preparing intermediate (pyridinylidene)-phthalides starting from 3-oxo-1,3-dihydro-isobenzofuran-1-carboxylic acids and pyridinecarbaldehydes, is described.
    Type: Grant
    Filed: September 29, 2003
    Date of Patent: May 17, 2005
    Assignee: Zambon Group S.p.A.
    Inventor: Mauro Napoletano
  • Publication number: 20040068117
    Abstract: A process for the preparation of phthalazines by preparing intermediate (pyridinylidene)-phthalides starting from 3-oxo-1,3-dihydro-isobenzofuran-1-carboxylic acids and pyridinecarbaldehydes, is described.
    Type: Application
    Filed: September 29, 2003
    Publication date: April 8, 2004
    Applicant: ZAMBON GROUP S.P.A.
    Inventor: Mauro Napoletano
  • Patent number: 6706882
    Abstract: A process for the preparation of (pyridinylidene)-phthalides starting from 3-oxo-1,3-dihydro-isobenzofuran-1-carboxylic acids and pyridinecarbaldehydes, is described.
    Type: Grant
    Filed: October 16, 2001
    Date of Patent: March 16, 2004
    Assignee: Zambon Group S.p.A.
    Inventor: Mauro Napoletano
  • Publication number: 20040043999
    Abstract: A process for preparing a compound of formula I: 1
    Type: Application
    Filed: May 20, 2003
    Publication date: March 4, 2004
    Applicant: Zambon Group S.p.A
    Inventors: Mauro Napoletano, Gabriele Norcini, Daniela Botta, Giancarlo Grancini, Gabriele Morazzoni, Francesco Santangelo, Jorge G. Siro Herrero, Jose Luis Garcia Navaio, Julio G. Alvarez-Builla
  • Patent number: 6589951
    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.
    Type: Grant
    Filed: August 10, 2000
    Date of Patent: July 8, 2003
    Assignee: Zambon Group S.p.A.
    Inventors: Mauro Napoletano, Gabriele Norcini, Daniela Botta, Giancarlo Grancini, Gabriele Morazzoni, Francesco Santangelo, Jorge G. Siro Herrero, José Luis Garcia Navaio, Julio G. Alvarez-Builla
  • Patent number: 6525055
    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
    Type: Grant
    Filed: April 30, 2001
    Date of Patent: February 25, 2003
    Assignee: Zambon Group S.p.A.
    Inventors: Mauro Napoletano, Gabriele Norcini, Franco Pellacini, Gabriele Morazzoni
  • Publication number: 20030023094
    Abstract: A process for the preparation of (pyridinylidene)-phthalides starting from 3-oxo-1,3-dihydro-isobenzofuran-1-carboxylic acids and pyridinecarbaldehydes, is described.
    Type: Application
    Filed: October 16, 2001
    Publication date: January 30, 2003
    Inventor: Mauro Napoletano
  • Patent number: 6498160
    Abstract: Phthalazine compounds having formula I wherein , A, B, R, R1, R2 and R3 are as defined herein, useful as phosphodiesterase 4 inhibitors.
    Type: Grant
    Filed: November 14, 2001
    Date of Patent: December 24, 2002
    Assignee: Zambon Group S.p.A.
    Inventors: Mauro Napoletano, Gabriele Norcini, Giancarlo Grancini, Franco Pellacini, Gabriele Morazzoni
  • Patent number: 6492360
    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 (
    Type: Grant
    Filed: October 15, 2001
    Date of Patent: December 10, 2002
    Assignee: Zambon Group S.p.A.
    Inventors: Mauro Napoletano, Gabriele Norcini, Giancarlo Grancini, Franco Pellacini, Gian Marco Leali, Gabriele Morazzoni
  • Publication number: 20020058662
    Abstract: The present invention relates to phthalazine derivatives, pharmaceutical compositions containing them, and to their use as phosphodiesterase 4 inhbitors.
    Type: Application
    Filed: November 14, 2001
    Publication date: May 16, 2002
    Applicant: ZAMBON GROUP S.P.A.
    Inventors: Mauro Napoletano, Gabriele Norcini, Giancarlo Grancini, Franco Pellacini, Gabriele Morazzoni
  • Patent number: 6358973
    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
    Type: Grant
    Filed: April 13, 2001
    Date of Patent: March 19, 2002
    Assignee: Zambon Group S.p.A.
    Inventors: Mauro Napoletano, Gabriele Norcini, Giancarlo Grancini, Franco Pellacini, Gabriele Morazzoni, Lorenzo Pradella
  • Patent number: 6340684
    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.
    Type: Grant
    Filed: January 22, 2001
    Date of Patent: January 22, 2002
    Assignee: Zambon Group S.p.A.
    Inventors: Mauro Napoletano, Gabriele Norcini, Giancarlo Grancini, Franco Pellacini, Gabriele Morazzoni
  • Patent number: 6329370
    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.
    Type: Grant
    Filed: January 22, 2001
    Date of Patent: December 11, 2001
    Assignee: Zambon Group S.p.A.
    Inventors: Mauro Napoletano, Gabriele Norcini, Giancarlo Grancini, Franco Pellacini, Gian Marco Leali, Gabriele Morazzoni