Patents by Inventor Raffaella Volpicelli

Raffaella Volpicelli 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).

  • Process for preparing enantiomerically enriched oxamides
    Patent number: 9481686
    Abstract: The present invention relates to a chiral oxamide of formula (I) useful as an intermediate in the preparation of dorzolamide, and to the preparation thereof. The invention also relates to the preparation of dorzolamide, to the hydrochloride salt thereof, and to the active ingredient contained in a drug useful in the treatment of glaucoma, by means of the intermediate of formula (I).
    Type: Grant
    Filed: June 28, 2013
    Date of Patent: November 1, 2016
    Assignee: ZACH SYSTEM S.P.A.
    Inventors: Raffaella Volpicelli, Antonio Nardi, Mauro Andretto, Ilaria Munari, Roberto Brescello, Anna Smaniotto, Livius Cotarca, Massimo Verzini
  • Process for Preparing Enantiomerically Enriched Oxamides
    Publication number: 20150191485
    Abstract: The present invention relates to a chiral oxamide of formula (I) useful as an intermediate in the preparation of dorzolamide, and to the preparation thereof. The invention also relates to the preparation of dorzolamide, to the hydrochloride salt thereof, and to the active ingredient contained in a drug useful in the treatment of glaucoma, by means of the intermediate of formula (I).
    Type: Application
    Filed: June 28, 2013
    Publication date: July 9, 2015
    Inventors: Raffaella Volpicelli, Antonio Nardi, Mauro Andretto, Ilaria Munari, Roberto Brescello, Anna Smaniotto, Livius Cotarca, Massimo Verzini
  • Process for preparing Bosentan monohydrate and it's intermediates
    Patent number: 8933226
    Abstract: The present invention relates to a process for preparing Bosentan Monohydrate; in particular, the present invention provides the preparation of the novel 4-tert-butyl-N-[6-(2-hydroxy-ethoxy)-5-(2-methoxy-phenoxy)-2-(2-pyrimidinyl)-pyrimidin-4-yl]-benzenesulfonamide sodium salt as an ethylene glycol solvate (Bosentan sodium salt ethylene glycol solvate), which is a useful intermediate for obtaining Bosentan Monohydrate in a pure form.
    Type: Grant
    Filed: September 22, 2011
    Date of Patent: January 13, 2015
    Assignee: Zach Systems S.p.A.
    Inventors: Livius Cotarca, Massimo Verzini, Elisa Melotto, Ivan Michieletto, Alfonso Melloni, Paolo Maragni, Raffaella Volpicelli, Mauro Andretto, Corrado Colli
  • Process for preparing Nebivolol
    Patent number: 8927742
    Abstract: The present invention relates to a process for preparing Nebivolol and, more particularly, to an improved method of debenzylation of a compound of formula (II) useful for preparing nebivolol endowed with high purity.
    Type: Grant
    Filed: October 28, 2009
    Date of Patent: January 6, 2015
    Assignee: Zach Systems S.p.A.
    Inventors: Paolo Maragni, Ivan Michieletto, Raffaella Volpicelli, Giorgio Soriato, Johnny Foletto, Livius Cotarca, Massimo Verzini
  • Asymmetric reduction process
    Patent number: 8927740
    Abstract: The present invention relates to a stereoselective reduction procedure to obtain, by means of catalytic asymmetric hydrogenation by hydrogen transfer, a compound of formula (I) in which X is S or SO2 and R4 is hydrogen or an SO2NH2 group, from the corresponding ketone precursor, said compound of formula (I) being useful as an intermediate in the preparation of dorzolamide or of the hydrochloride salt thereof.
    Type: Grant
    Filed: March 8, 2012
    Date of Patent: January 6, 2015
    Assignee: Zach System S.P.A.
    Inventors: Raffaella Volpicelli, Mauro Andretto, Livius Cotarca, Antonio Nardi, Massimo Verzini
  • ASYMMETRIC REDUCTION PROCESS
    Publication number: 20130338377
    Abstract: The present invention relates to a stereoselective reduction procedure to obtain, by means of catalytic asymmetric hydrogenation by hydrogen transfer, a compound of formula (I) in which X is S or SO2 and R4 is hydrogen or an SO2NH2 group, from the corresponding ketone precursor, said compound of formula (I) being useful as an intermediate in the preparation of dorzolamide or of the hydrochloride salt thereof.
    Type: Application
    Filed: March 8, 2012
    Publication date: December 19, 2013
    Applicant: ZACH SYSTEM S.P.A.
    Inventors: Raffaella Volpicelli, Mauro Andretto, Livius Cotarca, Antonio Nardi, Massimo Verzini
  • PROCESS FOR PREPARING BOSENTAN MONOHYDRATE AND ITS INTERMEDIATED
    Publication number: 20130253195
    Abstract: The present invention relates to a process for preparing Bosentan Monohydrate; in particular, the present invention provides the preparation of the novel 4-tert-butyl-N-[6-(2-hydroxy-ethoxy)-5-(2-methoxy-phenoxy)-2-(2-pyrimidinyl)-pyrimidin-4-yl]-benzenesulfonamide sodium salt as an ethylene glycol solvate (Bosentan sodium salt ethylene glycol solvate), which is a useful intermediate for obtaining Bosentan Monohydrate in a pure form.
    Type: Application
    Filed: September 22, 2011
    Publication date: September 26, 2013
    Applicant: ZACH SYSTEM SPA
    Inventors: Livius Cotarca, Massimo Verzini, Elisa Melotto, Ivan Michieletto, Alfonso Melloni, Paolo Maragni, Raffaella Volpicelli, Mauro Andretto, Corrado Colli
  • Process for preparing nebivolol
    Patent number: 8258323
    Abstract: The present invention relates to a process for preparing nebivolol and, more particularly, to a process for preparing d-nebivolol and its enantiomer l-nebivolol or acid addition salts thereof starting from commercially available or easily obtainable 2,2-dimethyl-1,3 dioxolane-4-carbaldehyde and a vinyl Grignard reagent.
    Type: Grant
    Filed: April 29, 2011
    Date of Patent: September 4, 2012
    Assignee: Zach System S.p.A.
    Inventors: Raffaella Volpicelli, Paolo Maragni, Livius Cotarca, Johnny Foletto, Franco Massaccesi
  • Process for preparing nebivolol
    Patent number: 8084629
    Abstract: The present invention relates to a process for reducing a compound of formula (I) wherein X is halogen, a hydroxy group, an alkylsulfoniloxy group or an arylsulfonyloxy group; to give a compound of formula (II) as a diastereoisomerically pure compound of RS/SR configuration characterized in that said reduction is carried out by the use of (+)-B-chlorodiisopinocampheylborane or (?)-B-chlorodiisopinocampheylborane. The compounds of formula (II) are useful as intermediates for the preparation of Nebivolol.
    Type: Grant
    Filed: March 16, 2009
    Date of Patent: December 27, 2011
    Assignee: Zach System S.p.A.
    Inventors: Raffaella Volpicelli, Paolo Maragni, Franco Massaccesi, Ilaria Munari, Livius Cotarca, Johnny Foletto
  • PROCESS FOR PREPARING NEBIVOLOL
    Publication number: 20110207948
    Abstract: The present invention relates to a process for preparing Nebivolol and, more particularly, to an improved method of debenzylation of a compound of formula (II) useful for preparing nebivolol endowed with high purity.
    Type: Application
    Filed: October 28, 2009
    Publication date: August 25, 2011
    Applicant: ZACH SYSTEM S.P.A.
    Inventors: Paolo Maragni, Ivan Michieletto, Raffaella Volpicelli, Giorgio Soriato, Johnny Foletto, Livius Cotarca, Massimo Verzini
  • PROCESS FOR PREPARING NEBIVOLOL
    Publication number: 20110201831
    Abstract: The present invention relates to a process for preparing nebivolol and, more particularly, to a process for preparing d-nebivolol and its enantiomer l-nebivolol or acid addition salts thereof starting from commercially available or easily obtainable 2,2-dimethyl-1,3 dioxolane-4-carbaldehyde and a vinyl Grignard reagent.
    Type: Application
    Filed: April 29, 2011
    Publication date: August 18, 2011
    Applicant: ZACH SYSTEM S.P.A.
    Inventors: Raffaella VOLPICELLI, Paolo MARAGNI, Livius COTARCA, Johnny FOLETTO, Franco MASSACCESI
  • Process for preparing nebivolol
    Patent number: 7999124
    Abstract: The present invention relates to a process for preparing nebivolol and, more particularly, to a process for preparing d-nebivolol and its enantiomer l-nebivolol or acid addition salts thereof starting from commercially available or easily obtainable 2,2-dimethyl-1,3 dioxolane-4-carbaldehyde and a vinyl Grignard reagent.
    Type: Grant
    Filed: November 23, 2007
    Date of Patent: August 16, 2011
    Assignee: Zach System S.p.A.
    Inventors: Raffaella Volpicelli, Paolo Maragni, Livius Cotarca, Johnny Foletto, Franco Massaccesi
  • Process for preparing nebivolol
    Patent number: 7960572
    Abstract: The present invention relates to a process for the preparation of Nebivolol and, more particularly, to an improved method of synthesizing 6-fluoro chroman epoxides of formula (I) key intermediates in preparing nebivolol.
    Type: Grant
    Filed: October 2, 2007
    Date of Patent: June 14, 2011
    Assignee: Zach System S.p.A.
    Inventors: Raffaella Volpicelli, Paolo Maragni, Livius Cotarca, Johnny Foletto
  • PROCESS FOR PREPARING NEBIVOLOL
    Publication number: 20110021793
    Abstract: The present invention relates to a process for reducing a compound of formula (I) wherein X is halogen, a hydroxy group, an alkylsulfoniloxy group or an arylsulfonyloxy group; to give a compound of formula (II) as a di-astereoisomerically pure compound of RS/SR configuration characterized in that said reduction is carried out by the use of (+)-B-chlorodiisopinocampheylborane or (?)-B-chlorodiisopinocampheylborane. The compounds of formula (II) are useful as intermediates for the preparation of Nebivolol.
    Type: Application
    Filed: March 16, 2009
    Publication date: January 27, 2011
    Applicant: ZACH SYSTEM S.P.A.
    Inventors: Raffaella Volpicelli, Paolo Maragni, Franco Massaccesi, Ilaria Munari, Livius Cotarca, Johnny Foletto
  • The Process for Preparing Nebivolol
    Publication number: 20100069652
    Abstract: The present invention relates to a process for the preparation of Nebivolol and, more particularly, to an improved method of synthesizing 6-fluoro chroman epoxides of formula (I) key intermediates in preparing nebivolol.
    Type: Application
    Filed: October 2, 2007
    Publication date: March 18, 2010
    Applicant: ZACH SYSTEM S.P.A.
    Inventor: Raffaella Volpicelli
  • PROCESS FOR PREPARING NEBIVOLOL
    Publication number: 20100056813
    Abstract: The present invention relates to a process for preparing nebivolol and, more particularly, to a process for preparing d-nebivolol and its enantiomer l-nebivolol or acid addition salts thereof starting from commercially available or easily obtainable 2,2-dimethyl-1,3 dioxolane-4-carbaldehyde and a vinyl Grignard reagent.
    Type: Application
    Filed: November 23, 2007
    Publication date: March 4, 2010
    Applicant: ZACH SYSTEM S.P.A.
    Inventors: Raffaella Volpicelli, Paolo Maragni, Livius Cotarca, Johnny Foletto, Franco Massaccesi