Patents by Inventor Giorgio Bertolini

Giorgio Bertolini 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: 20180258028
    Abstract: Subject-matter of the invention is a process for the preparation of key intermediates in the synthesis of indacaterol. Subject-matter of the invention are also new synthesis intermediates.
    Type: Application
    Filed: September 28, 2016
    Publication date: September 13, 2018
    Inventors: Corrado COLLI, Alessandro AGOSTI, Stefano MAIORANA, Federica COLOMBO, Giorgio BERTOLINI
  • Patent number: 10059653
    Abstract: Subject-matter of the invention is a process for the preparation of a key intermediate in the synthesis of indacaterol. Subject-matter of the invention are also new synthesis intermediates.
    Type: Grant
    Filed: January 19, 2016
    Date of Patent: August 28, 2018
    Assignee: OLON S.P.A.
    Inventors: Giorgio Bertolini, Paolangelo Cerea, Corrado Colli, Lazzaro Feliciani, Federico Gassa, Aldo Bianchi, Federica Colombo, Stefano Maiorana, Filippo Nisic
  • Publication number: 20180222909
    Abstract: Subject-matter of the invention is a process for the preparation of ibrutinib and intermediate compound.
    Type: Application
    Filed: July 27, 2016
    Publication date: August 9, 2018
    Inventors: Giorgio BERTOLINI, Ilaria FERRANDO, Mara SADA
  • Patent number: 10023535
    Abstract: The present invention refers to a process for the preparation of 1-(2-halogen-ethyl)-4-piperidinecarboxylic acid ethyl esters, in particular of 1-(2-chloroethyl)-4 piperidinecarboxylic acid ethyl ester, a versatile synthesis intermediate, particularly useful as an intermediate compound in the synthesis of umeclidinium.
    Type: Grant
    Filed: October 22, 2015
    Date of Patent: July 17, 2018
    Assignee: OLON S.P.A.
    Inventors: Giorgio Bertolini, Corrado Colli, Aldo Bianchi, Federica Colombo, Stefano Maiorana, Filippo Nisic
  • Publication number: 20170362161
    Abstract: Subject-matter of the invention is a process for the preparation of a key intermediate in the synthesis of indacaterol. Subject-matter of the invention are also new synthesis intermediates.
    Type: Application
    Filed: January 19, 2016
    Publication date: December 21, 2017
    Applicant: OLON S.P.A.
    Inventors: Giorgio BERTOLINI, Paolangelo CEREA, Corrado COLLI, Lazzaro FELICIANI, Federico GASSA, Aldo BIANCHI, Federica COLOMBO, Stefano MAIORANA, Filippo NISIC
  • Patent number: 9809554
    Abstract: The invention refers to a process for preparing ivabradine, in particular a process for preparing an ivabradine salt.
    Type: Grant
    Filed: May 19, 2014
    Date of Patent: November 7, 2017
    Assignee: OLON S.p.A.
    Inventors: Mara Sada, Faris Garis, Giorgio Bertolini
  • Publication number: 20170313657
    Abstract: The present invention refers to a process for the preparation of 1-(2-halogen-ethyl)-4-piperidinecarboxylic acid ethyl esters, in particular of 1-(2-chloroethyl)-4 piperidinecarboxylic acid ethyl ester, a versatile synthesis intermediate, particularly useful as an intermediate compound in the synthesis of umeclidinium.
    Type: Application
    Filed: October 22, 2015
    Publication date: November 2, 2017
    Applicant: OLON S.P.A.
    Inventors: Giorgio BERTOLINI, Corrado COLLI, Aldo BIANCHI, Federica COLOMBO, Stefano MAIORANA, Filippo NISIC
  • Publication number: 20170165247
    Abstract: The present invention relates to new crystalline compounds of dabigatran etexilate, namely to crystalline compounds comprising mixtures of dabigatran etexilate and an acid. The invention also relates to processes for the preparation of the new crystalline compounds, pharmaceutical compositions comprising them and their use in therapy.
    Type: Application
    Filed: July 17, 2015
    Publication date: June 15, 2017
    Inventors: Giorgio BERTOLINI, Lazzaro FELICIANI, Ilaria FERRANDO
  • Publication number: 20170158645
    Abstract: The present invention relates to the amorphous form of macitentan and to new crystalline forms thereof. The invention also relates to processes for the preparation of the new compounds, to the pharmaceutical compositions comprising them and to the use thereof in the therapy.
    Type: Application
    Filed: July 13, 2015
    Publication date: June 8, 2017
    Inventors: Giorgio BERTOLINI, Lazzaro FELICIANI, Ilaria FERRANDO
  • Publication number: 20170100408
    Abstract: The subject-matter of the present invention is a novel, non-salified ivabradine solid form, in particular an ivabradine form adsorbed on an inert carrier. The subject-matter of the invention is also a process for preparing said solid form, its use in therapy and pharmaceutical compositions comprising it.
    Type: Application
    Filed: March 24, 2015
    Publication date: April 13, 2017
    Inventors: Giorgio BERTOLINI, Cinzia BIAGGI, Ilaria FERRANDO
  • Patent number: 9410169
    Abstract: The present invention relates to an enantioselective enzymatic process for the preparation of an optically active 3-hydroxypiperidinecarboxylic acid derivative.
    Type: Grant
    Filed: June 18, 2012
    Date of Patent: August 9, 2016
    Assignee: LABORATORIO CHIMICO INTERNAZIONALE S.P.A.
    Inventors: Giorgio Bertolini, Paolo Magri′
  • Patent number: 9403770
    Abstract: A process for preparing fexofenadine is described, which provides for the hydrolysis of 4-[4-[4-(hydroxydiphenylmethyl)-1-piperidyl]-1-oxobutyl]-?,?-dimethylbenzeneacetic acid-alkyl ester, in a mixture of water and optionally an organic solvent, in the presence of a base; the carboxylate salt of 4-[4-[4-(hydroxydiphenylmethyl)-1-piperidyl]-1-oxobutyl]-?,?-dimethylbenzeneacetic acid is thus obtained, which is then directly reduced as carboxylate in a basic environment with hydrogen in the presence of a suitable hydrogenation catalyst to give the carboxylate of fexofenadine, which is precipitated by neutralization of the solution.
    Type: Grant
    Filed: July 25, 2007
    Date of Patent: August 2, 2016
    Assignee: Euticals SPA
    Inventors: Giorgio Bertolini, Maurizio Gallina, Giuseppe Motta, Domenico Vergani
  • Publication number: 20160107998
    Abstract: The invention refers to a process for preparing ivabradine, in particular a process for preparing an ivabradine salt.
    Type: Application
    Filed: May 19, 2014
    Publication date: April 21, 2016
    Inventors: Mara SADA, Faris GARIS, Giorgio BERTOLINI
  • Publication number: 20150291508
    Abstract: The invention concerns a new process for the preparation of crystalline form I of agomelatine by freeze-drying.
    Type: Application
    Filed: August 3, 2011
    Publication date: October 15, 2015
    Applicant: LABORATORIO CHIMICO INTERNAZIONALE S.p.A.
    Inventors: Giorgio Bertolini, Bruno De Angelis
  • Publication number: 20150275249
    Abstract: The present invention relates to an enantioselective enzymatic process for the preparation of an optically active 3-hydroxypiperidinecarboxylic acid derivative.
    Type: Application
    Filed: June 18, 2012
    Publication date: October 1, 2015
    Applicant: LABORATORIO cHIMICO INTERNAZIONALE S.p. A.
    Inventors: Giorgio Bertolini, Paolo Magri'
  • Patent number: 9024068
    Abstract: The invention concerns a new process for the preparation of crystalline form of agomelatine from a solution of agomelatine in a solvent, characterized in that the agomelatine is crystallized by instantaneous precipitation from said solution, at a temperature equal to or below ?10° C.
    Type: Grant
    Filed: December 29, 2011
    Date of Patent: May 5, 2015
    Assignee: Laboratorio Chimico Internazionale S.p.A.
    Inventors: Bruno De Angelis, Faris Garis, Salvatore De Gennaro, Giorgio Bertolini
  • Publication number: 20140309293
    Abstract: The invention concerns a new polymorphic form of R-(+)-?-lipoic acid and a process for the preparation thereof, in addition to the compositions that contain it and its use as a medicine or food supplement.
    Type: Application
    Filed: July 6, 2012
    Publication date: October 16, 2014
    Applicant: LABORATORIO CHIMICO INTERNAZIONALE S.P. A.
    Inventors: Antonio Nardi, Annibale Salvi, Flavio Villani, Bruno De Angelis, Giorgio Bertolini
  • Publication number: 20140221690
    Abstract: The invention concerns a new process for the preparation of two crystalline forms of agomelatine, in particular a process for preparation of form I and a new form of agomelatine, here called form VII.
    Type: Application
    Filed: December 29, 2011
    Publication date: August 7, 2014
    Applicant: LABORATORIO CHIMICO
    Inventors: Bruno De Angelis, Faris Garis, Salvatore De Gennaro, Giorgio Bertolini
  • Patent number: 8796488
    Abstract: A novel process for the synthesis of Lacosamide using D,L-serine as starting material is described, where the methylation reaction of hydroxyl is carried out using an inexpensive base such as NaOH and an inexpensive alkylating agent, non-toxic and non-carcinogenic, such as methyl p-toluenesulfonate; the R enantiomer is isolated from the racemic mixture of Lacosamide after selective hydrolysis of the acetamide, salification of the racemic mixture with a chiral acid (HX*) in an organic solvent, resolution of the diastereoisomeric mixture, preferably by precipitation of the R enantiomer, and subsequent acetylation of the optically pure intermediate.
    Type: Grant
    Filed: December 22, 2010
    Date of Patent: August 5, 2014
    Assignee: Euticals S.p.A.
    Inventors: Alberto Bologna, Patrizia Castoldi, Domenico Vergani, Giorgio Bertolini
  • Patent number: 8791287
    Abstract: The object of the present invention is a new process for the synthesis of tapentadol, both as free base and in hydrochloride form, which comprises the step of alkylation of the ketone (VII) to yield the compound (VIII), as reported in Diagram 1, with high stereoselectivity due to the presence of the benzyl group as substituent of the amino group. It was surprisingly found that this substitution shifts the keto-enol equilibrium towards the desired enantiomer and amplifies the capacity of the stereocenter present in the compound (VII) to orient the nucleophilic addition of the organometallic compound at the carbonyl towards the desired stereoisomer. This substitution thus allows obtaining a considerable increase of the yields in this step, and consequently allows significantly increasing the overall yield of the entire tapentadol synthesis process. A further object of the present invention is constituted by the tapentadol free base in solid form, obtainable by means of the process of the invention.
    Type: Grant
    Filed: June 20, 2011
    Date of Patent: July 29, 2014
    Assignee: Euticals S.p.A.
    Inventors: Giuseppe Motta, Domenico Vergani, Giorgio Bertolini, Nicola Landoni