Patents by Inventor Roberto Castagnani

Roberto Castagnani 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).

  • Patent number: 9206133
    Abstract: The present invention provides a new process of synthesis of a polymorph of 7-chloro-4-(piperazin-1-yl)-quinoline of Formula I. Said quinoline compound is substantially pure of any impurities. The present invention further provides the use of the above-mentioned polymorph of 7-chloro-4-(piperazin-1-yl)-quinoline in the synthesis of piperaquine or one of its pharmaceutically acceptable salts.
    Type: Grant
    Filed: June 5, 2012
    Date of Patent: December 8, 2015
    Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.
    Inventors: Walter Cabri, Roberto Castagnani, Silvia Armaroli, Gianandrea Quattrociocchi, Vincenzo Colangeli
  • Publication number: 20140200346
    Abstract: The present invention provides a new process of synthesis of a polymorph of 7-chloro-4-(piperazin-1-yl)-quinoline of Formula I. Said quinoline compound is substantially pure of any impurities. The present invention further provides the use of the above-mentioned polymorph of 7-chloro-4-(piperazin-1-yl)-quinoline in the synthesis of piperaquine or one of its pharmaceutically acceptable salts.
    Type: Application
    Filed: June 5, 2012
    Publication date: July 17, 2014
    Applicant: SIGMA-TAU INDUSTRIE FARMACEUTICHE RIUNITE S.p.A.
    Inventors: Walter Cabri, Roberto Castagnani, Silvia Armaroli, Gianandrea Quattrociocchi, Vincenzo Colangeli
  • Patent number: 6953865
    Abstract: A process for the production of (R)- or (S)-aminocarnitine starting respectively from (R)- or (S)-nitryloxycarnitine, through the formation and hydrogenation of the azidocarnitine intermediate with the same absolute configuration is described. (R)-aminocarnitine inner salt is obtained after purification, which is then converted into non-deliquescent salts. Also a process for the preparation of derivatives of (R)- and (S)-aminocarnitine, in particular acylayed or ureic derivatives, having known pharmacological properties, starting from (R)- and (S)-aminocarnitine salts, releasing the aminic function in situ.
    Type: Grant
    Filed: July 17, 2002
    Date of Patent: October 11, 2005
    Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.
    Inventors: Oreste Piccoloi, Roberto Castagnani, Paolo De Witt Scalfaro
  • Publication number: 20040171875
    Abstract: A process for the production of (R)— or (S)-aminocarnitine starting respectively from (R)— or (S)-nitryloxycarnitine, through the formation and hydrogenation of the azidocarnitine intermediate with the same absolute configuration is described. (R)— aminocarnitine inner salt is obtained after purification, which is then converted into non-deliquescent salts. A further subject of the present invention is a process for the preparation of derivatives of (R)— and (S)-aminocarnitine, in particular acylated or ureic derivatives, having known pharmacological properties, starting from (R)— and (S)-aminocarnitine salts, releasing the aminic function in situ.
    Type: Application
    Filed: January 5, 2004
    Publication date: September 2, 2004
    Inventors: Oreste Piccoloi, Roberto Castagnani, Paolo De Witt Scalfaro
  • Patent number: 6593478
    Abstract: A new, more efficient and highly stereospecific process is described for the preparation of compounds with general formula (R)-(I) and of absolute configuration (R), where the groups M, W, Q and Q1 are as defined in the description, starting from compounds of absolute configuration (S) by hydrolysis, in the presence of acids, of the corresponding esterified derivatives. The (R)-(I) products obtained with the process described herein are chiral synthons useful for the production of enanthiomerically pure drugs. The preparation of (R)-carnitine is also provided.
    Type: Grant
    Filed: June 24, 2002
    Date of Patent: July 15, 2003
    Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.
    Inventors: Oreste Piccolo, Roberto Castagnani, Paolo De Witt
  • Patent number: 6548693
    Abstract: Carnitine derivatives of formula (I) are described in racemic and/or optically active form, as well as the process for their preparation and their use as pharmaceutical anti-angina active ingredients for the treatment of ischaemic heart disease. Also described is a process for producing the (R)-carnitine enantiomer from (S)-carnitine (or vice versa), using the derivatives of formula (I).
    Type: Grant
    Filed: April 11, 2002
    Date of Patent: April 15, 2003
    Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.
    Inventors: Oreste Piccolo, Roberto Castagnani, Paolo De Witt
  • Publication number: 20030032818
    Abstract: 1 A new, more efficient and highly stereospecific process is described for the preparation of compounds with general formula (R)-(I) and of absolute configuration (R), where the groups M, W, Q and Q1 are as defined in the description, starting from compounds of absolute configuration (S) by hydrolysis, in the presence of acids, of the corresponding esterified derivatives. The (R)-(I) products obtained with the process described herein are chiral synthons useful for the production of enanthiomerically pure drugs. The preparation of (R)-carnitine is also provided.
    Type: Application
    Filed: June 24, 2002
    Publication date: February 13, 2003
    Inventors: Oreste Piccolo, Roberto Castagnani, Paolo De Witt
  • Publication number: 20020119965
    Abstract: Carnitine derivatives of formula (I) are described in racemic and/or optically active form, as well as the process for their preparation and their use as pharmaceutical anti-angina active ingredients for the treatment of ischaemic heart disease.
    Type: Application
    Filed: April 11, 2002
    Publication date: August 29, 2002
    Applicant: SIGMA-TAU INDUSTRIE FARMACEUTICHE RIUNITE S.p.A.
    Inventors: Oreste Piccolo, Roberto Castagnani, Paolo De Witt
  • Patent number: 6395923
    Abstract: Carnitine derivatives of formula (I) are described in racemic and/or optically active form, as well as the process for their preparation and their use as pharmaceutical anti-angina active ingredients for the treatment of ischaemic heart disease. Also described is a process for producing the (R)-carnitine enantiomer from (S)-carnitine (or vice versa), using the derivatives of formula (I).
    Type: Grant
    Filed: March 13, 2001
    Date of Patent: May 28, 2002
    Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.
    Inventors: Oreste Piccolo, Roberto Castagnani, Paolo De Witt
  • Publication number: 20010011074
    Abstract: New camitine derivatives of general formula (I) are described in racemic and/or optically active form, as well as the process for their preparation and their use as pharmaceutical anti-angina active ingredients for the treatment of ischaemic heart disease.
    Type: Application
    Filed: March 13, 2001
    Publication date: August 2, 2001
    Inventors: Oreste Piccolo, Roberto Castagnani, Paolo De Witt
  • Patent number: 5532409
    Abstract: A process for producing aminocarnitine is described, wherein methanesulfonylcarnitine is converted to a lactone which is reacted with an azide to give azidocarnitine. The catalytic hydrogenation of azidocarnitine gives aminocarnitine.
    Type: Grant
    Filed: September 30, 1994
    Date of Patent: July 2, 1996
    Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.
    Inventors: Fabio Giannessi, Roberto Castagnani, Francesco De Angelis, Maria O. Tinti, Domenico Misiti
  • Patent number: 5491260
    Abstract: A Process for Preparing L-(-)-carnitine is disclosed which comprises acylating D-(+)-carnitinenitrile or D-(+)-carnitineamide to their respective acyl derivatives which, via acid hydrolysis, yield D-(+)-carnitine which is converted to the lactone of L-(-)-carnitine. The lactone when in base yields L-(-)-carnitine.
    Type: Grant
    Filed: April 7, 1994
    Date of Patent: February 13, 1996
    Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.
    Inventors: Fabio Giannessi, Roberto Castagnani, Maria O. Tinti, Francesco De Angelis, Paolo De Witt, Domenico Misiti