Patents Assigned to OLON S.p.A.
  • Patent number: 11498917
    Abstract: The invention relates to a process for the preparation of Lifitegrast of formula (I), which comprises: a) condensation of the compound of formula (II) with the compound of formula (III) to give the compound of formula (IV) wherein R1, R2 and R3 are independently selected from straight or branched C1-C6 alkyl groups; b) chlorination of compound (IV) in the presence of a chlorinating agent (IV), (V), c) condensation of compound (V) with amino acid (VI) to give compound (I), c) condensation of compound (V) with amino acid (VI) to give compound (I), d) optional purification of the crude Lifitegrast in mixtures of polar aprotic solvents and water.
    Type: Grant
    Filed: June 13, 2019
    Date of Patent: November 15, 2022
    Assignee: OLON S.P.A.
    Inventors: Giorgio Bertolini, Lazzaro Feliciani, Davide Longoni, Mara Sada, Matteo Valli
  • Publication number: 20220324831
    Abstract: The present invention relates to a novel non-solvated crystalline form of apalutamide in pure, stable form, and the process for the preparation thereof.
    Type: Application
    Filed: September 7, 2020
    Publication date: October 13, 2022
    Applicant: OLON S.P.A.
    Inventors: Valentina Grande, Alessia Manfredi, Jacopo Bonanomi, Gabriele Ferretti, Barbara Novo, Mara Sada, Giorgio Bertolini
  • Publication number: 20220153718
    Abstract: The present invention relates to a process for the preparation of apalutamide in stable amorphous form. The invention also relates to a novel intermediate crystalline form, called form X, which gives rise to said amorphous form, and a process for obtaining said form X.
    Type: Application
    Filed: March 9, 2020
    Publication date: May 19, 2022
    Applicant: OLON S.P.A.
    Inventors: Valentina Grande, Barbara Novo, Mara SADA, Gabriele Ferretti, Alessia Manfredi
  • Patent number: 11325922
    Abstract: The present invention relates to a process for the preparation of crisaborole of formula (I): by preparing intermediates of formulas (II) and (III):
    Type: Grant
    Filed: July 10, 2020
    Date of Patent: May 10, 2022
    Assignee: OLON S.P.A.
    Inventors: Federico Gassa, Lazzaro Feliciani, Alberto Mazza, Marco Quaroni, Mara Sada, Giorgio Bertolini
  • Patent number: 11319288
    Abstract: Disclosed is a process for the synthesis of pimavanserin base with a high yield and purity, which comprises: a) converting tert-butyl-N-[(4-propan-2-yloxyphenyl)methyl]carbamate (Formula (I)) to 1-(isocyanatomethyl)-4-propan-2-yloxybenzene of formula (II) b) adding N-[(4-fluorophenyl)methyl]-1-methylpiperidin-4-amine (Formula (IV)) to the solution obtained in a) to give pimavanserin base, and c) purifying the pimavanserin base obtained in step b).
    Type: Grant
    Filed: April 24, 2019
    Date of Patent: May 3, 2022
    Assignee: OLON S.P.A.
    Inventors: Barbara Novo, Jacopo Bonanomi, Mattia Bertolotti
  • Patent number: 11279724
    Abstract: Disclosed is a process for the preparation of Cangrelor in salt form by preparation and subsequent hydrolysis of an intermediate of formula (IV): The process is characterized by the high yield and purity of the product, and can be used industrially.
    Type: Grant
    Filed: October 29, 2018
    Date of Patent: March 22, 2022
    Assignee: OLON S.P.A.
    Inventors: Jacopo Bonanomi, Mattia Bertolotti, Barbara Novo
  • Publication number: 20210246123
    Abstract: The invention relates to a process for the preparation of Lifitegrast of formula (I), which comprises: a) condensation of the compound of formula (II) with the compound of formula (III) to give the compound of formula (IV) wherein R1, R2 and R3 are independently selected from straight or branched C1-C6 alkyl groups; b) chlorination of compound (IV) in the presence of a chlorinating agent (IV), (V), c) condensation of compound (V) with amino acid (VI) to give compound (I), c) condensation of compound (V) with amino acid (VI) to give compound (I), d) optional purification of the crude Lifitegrast in mixtures of polar aprotic solvents and water.
    Type: Application
    Filed: June 13, 2019
    Publication date: August 12, 2021
    Applicant: OLON S.P.A.
    Inventors: Giorgio Bertolini, Lazzaro Feliciani, Davide Longoni, Mara Sada, Matteo Valli
  • Publication number: 20210206742
    Abstract: The present invention relates to a process for the preparation of Apalutamide of formula (A) Apalutamide is a latest-generation androgen receptor inhibitor, used to treat non-metastatic castration-resistant prostate cancer.
    Type: Application
    Filed: May 27, 2019
    Publication date: July 8, 2021
    Applicant: OLON S.P.A.
    Inventors: Valentina Grande, Gabriele Ferretti, Barbara Novo
  • Patent number: 11053227
    Abstract: Subject-matter of the present invention is a process for preparing intermediates for the synthesis of optically active beta-amino alcohols by enzymatic reduction of the corresponding beta-amino ketones. Subject-matter of the invention are also said novel synthesis intermediates and the use thereof in the preparation of active pharmaceutical ingredients, among which vilanterol and the salts thereof.
    Type: Grant
    Filed: December 19, 2018
    Date of Patent: July 6, 2021
    Assignee: OLON S.P.A.
    Inventors: Corrado Colli, Giorgio Bertolini, Mara Sada, Faris Garis, Filippo Nisic, Aldo Bianchi, Cinzia Biaggi, Romano Di Fabio, Silvano Ronzoni, Stefania Bertuolo, Adolfo Prandi, Stefano Maiorana
  • Patent number: 11028082
    Abstract: The present invention relates to a process for the preparation of a novel and versatile synthesis intermediate and its use in the preparation of umeclidinium. The invention also relates to some reference standards allowing to detect impurity traces recurring in the preparation of umeclidinium and a process for their preparation.
    Type: Grant
    Filed: May 28, 2018
    Date of Patent: June 8, 2021
    Assignee: OLON S.P.A.
    Inventors: Giorgio Bertolini, Corrado Colli, Filippo Nisic, Mara Sada, Stefania Bertuolo, Silvano Ronzoni, Stefano Maiorana, Romano Di Fabio
  • Publication number: 20210130296
    Abstract: Disclosed is a process for the synthesis of pimavanserin base with a high yield and purity, which comprises: a) converting tert-butyl-N-[(4-propan-2-yloxyphenyl)methyl]carbamate (Formula (I)) to 1-(isocyanatomethyl)-4-propan-2-yloxybenzene of formula (II) b) adding N-[(4-fluorophenyl)methyl]-1-methylpiperidin-4-amine (Formula (IV)) to the solution obtained in a) to give pimavanserin base, and c) purifying the pimavanserin base obtained in step b).
    Type: Application
    Filed: April 24, 2019
    Publication date: May 6, 2021
    Applicant: OLON S.P.A.
    Inventors: Barbara Novo, Jacopo Bonanomi, Mattia Bertolotti
  • Publication number: 20200407355
    Abstract: Disclosed are new crystalline forms of venetoclax, a selective Bcl2 inhibitor used as a chemotherapy agent, and the processes for preparation of said crystalline forms by treating venetoclax with suitable solvents.
    Type: Application
    Filed: February 28, 2019
    Publication date: December 31, 2020
    Applicant: Olon S.P.A.
    Inventors: Barbara Novo, Jacopo Bonanomi, Gaia Migliazza
  • Patent number: 10538479
    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: Grant
    Filed: September 28, 2016
    Date of Patent: January 21, 2020
    Assignee: OLON S.P.A.
    Inventors: Corrado Colli, Alessandro Agosti, Stefano Maiorana, Federica Colombo, Giorgio Bertolini
  • Publication number: 20190276399
    Abstract: Disclosed is a partly crystalline form of nintedanib ethanesulphonate and its preparation process.
    Type: Application
    Filed: June 6, 2017
    Publication date: September 12, 2019
    Applicant: Olon S.P.A.
    Inventors: Barbara Novo, Jacopo Bonanomi, Stella De Fiore, Francesco Calogero
  • Patent number: 10329311
    Abstract: The present invention relates to a process for the preparation of crisaborole of formula (I): by preparing intermediates of formulas (II) and (III):
    Type: Grant
    Filed: March 21, 2018
    Date of Patent: June 25, 2019
    Assignee: OLON S.P.A.
    Inventors: Federico Gassa, Lazzaro Feliciani, Alberto Mazza, Marco Quaroni, Mara Sada, 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
  • Patent number: 10035776
    Abstract: Disclosed is a process for the preparation of Enzalutamide comprising the reaction (Scheme 2), wherein R can be alkyl, aryl, aryl-alkyl or heterocyclyl.
    Type: Grant
    Filed: May 24, 2016
    Date of Patent: July 31, 2018
    Assignee: Olon S.P.A.
    Inventors: Samuele Frigoli, Davide Longoni, Marco Alpegiani, Claudio Fuganti, Stefano Serra
  • 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: 20180148416
    Abstract: Disclosed is an efficient method of synthesising Enzalutamide, which comprises the cyclisation reaction of isothiocyanate 1 with acid 3 pre-treated with a silylating agent, or reacting 1 and 3 in the presence of a silylating agent.
    Type: Application
    Filed: May 24, 2016
    Publication date: May 31, 2018
    Applicant: Olon S.P.A.
    Inventors: Samuele Frigoli, Davide Longoni, Marco Alpegiani
  • Patent number: 9981951
    Abstract: Disclosed are a novel crystalline form and an amorphous form of Olaparib, and the process for their preparation.
    Type: Grant
    Filed: December 19, 2016
    Date of Patent: May 29, 2018
    Assignee: OLON S.P.A.
    Inventors: Barbara Novo, Jacopo Bonanomi, Stella Defiore, Francesco Calogero