Patents Assigned to F.I.S. Fabbrica Italiana Sintetici S.p.A.
  • IMPROVED PROCESS FOR THE PREPARATION OF TRENBOLONE AND/OR TRENBOLONE ACETATE
    Publication number: 20240025941
    Abstract: Object of the present invention is an improved process for the preparation of Trenbolone (I-b) and/or Trenbolone Acetate (I-a) comprising the reaction of the compound of formula (II): wherein R is H or Ac; with an oxidant agent in presence of an acid.
    Type: Application
    Filed: November 18, 2021
    Publication date: January 25, 2024
    Applicant: F.I.S. - FABBRICA ITALIANA SINTETICI S.P.A.
    Inventor: Anna RENCUROSI
  • HIGHLY EFFICIENT PROCESS FOR THE PREPARATION OF 4-FLUORO-1H-PYRAZOLE OR SALTS THEREOF
    Publication number: 20230242489
    Abstract: Highly efficient process for the preparation of 4-Fluoro-1H-pyrazole or salts thereof by reaction of pyrazole with an electrophilic fluorinating reagent is disclosed.
    Type: Application
    Filed: January 27, 2023
    Publication date: August 3, 2023
    Applicant: F.I.S. - Fabbrica Italiana Sintetici S.p.A.
    Inventors: Kexia LOU, Jian DONG
  • HIGHLY STABLE CRYSTALLINE ELTROMBOPAG MONOETHANOLAMINE SALT FORM D1
    Publication number: 20210284611
    Abstract: Object of the present invention is a highly stable crystalline form of Eltrombopag (ETP) monoethanolamine salt, named Form D1, having the highest thermodynamically stability with excellent non-hygroscopicity, and particularly well suitable for pharmaceutical purposes, with related process.
    Type: Application
    Filed: July 25, 2019
    Publication date: September 16, 2021
    Applicant: F.I.S. - FABBRICA ITALIANA SINTETICI S.P.A.
    Inventors: Nicolas TESSON, Jordi DE MIER VINUE, Paolo STABILE, Pierluigi PADOVAN, Matteo DE POLI, Angelo RESTELLI
  • CRYSTALLINE ELTROMBOPAG MONOETHANOLAMINE SALT FORM D
    Publication number: 20210198211
    Abstract: Object of the present invention is a better crystalline form of Eltrombopag (ETP) monoethanolamine salt, named Form D, stable, suitable for pharmaceutical purposes, and with the highest solubility in water and excellent non-hygroscopicity, then the related process and intermediates thereof.
    Type: Application
    Filed: July 25, 2019
    Publication date: July 1, 2021
    Applicant: F.I.S. - FABBRICA ITALIANA SINTETICI S.P.A.
    Inventors: Nicolas TESSON, Jordi DE MIER VINUE, Paolo STABILE, Pierluigi PADOVAN, Matteo DE POLI, Angelo RESTELLI
  • ENZYMATIC PROCESS FOR THE PREPARATION OF DROXIDOPA
    Publication number: 20210163401
    Abstract: The present invention relates to a process for the preparation of Droxidopa by means of an improved enzymatic reduction of a compound of formula (II): (II), wherein R1, R2 is independent hydrogen, acetyl, R3 is hydrogen, a C1-C4 linear or branched alkyl group and R4 is hydrogen or an amine protecting group.
    Type: Application
    Filed: June 7, 2019
    Publication date: June 3, 2021
    Applicant: F.I.S. - FABBRICA ITALIANA SINTETICI S.P.A.
    Inventors: Stefano FOGAL, Paolo STABILE, Pierluigi PADOVAN, Matteo DE POLI, Angelo RESTELLI
  • NEW EFFICIENT PROCESS FOR THE PREPARATION OF SITAGLIPTIN
    Publication number: 20210061808
    Abstract: Object of the present invention is an efficient process for the preparation of the active pharmaceutical ingredient Sitagliptine and the 2,4,5-trifluorophenylacetic acid (TFAA) and salt thereof, which is a key intermediate for the synthesis of Sitagliptine.
    Type: Application
    Filed: January 11, 2019
    Publication date: March 4, 2021
    Applicant: F.I.S. - FABBRICA ITALIANA SINTETICI S.P.A.
    Inventors: Terry SHI, Sam LOU, Ottorino DE LUCCHI, Pierluigi PADOVAN
  • PROCESS FOR THE PREPARATION OF CYCLOPROPYLDIKETOPIPERAZINES AND OF A KEY INTERMEDIATE OF DS-5272
    Publication number: 20200377521
    Abstract: Object of the present invention is an improved process for the preparation of cyclopropyldiketopiperazines and thereof key intermediates.
    Type: Application
    Filed: August 20, 2020
    Publication date: December 3, 2020
    Applicant: F.I.S. - Fabbrica Italiana Sintetici S.P.A.
    Inventors: Pierluigi PADOVAN, Kexia Lou
  • EFFICIENT PROCESS FOR THE PREPARATION OF SITAGLIPTIN THROUGH A VERY EFFECTIVE PREPARATION OF THE INTERMEDIATE 2,4,5-TRIFLUOROPHENYLACETIC ACID
    Publication number: 20200157109
    Abstract: Object of the present invention is an efficient process for the preparation of the active pharmaceutical ingredient Sitagliptine and the 2,4,5-trifluorophenylacetic acid (TFAA) and salt thereof, which is a key intermediate for the synthesis of Sitagliptine.
    Type: Application
    Filed: May 15, 2018
    Publication date: May 21, 2020
    Applicant: F.I.S. - FABBRiCA ITALIANA SINTETICI S.P.A.
    Inventors: Ottorino DE LUCCHI, Pierluigi PADOVAN, Elena BRASOLA
  • Dimer impurities of Apixaban and method to remove them
    Patent number: 10590133
    Abstract: Object of the present invention are dimer impurities of the active ingredient Apixaban, analytical methods for identifying and/or quantifying them and a synthetic method for removing or limiting said impurities from Apixaban and synthetic precursors thereof.
    Type: Grant
    Filed: June 28, 2019
    Date of Patent: March 17, 2020
    Assignee: F.I.S.-FABBRICA ITALIANA SINTETICI S.P.A.
    Inventors: Elena Brasola, Filippo Tomasi, Loris Peruzzi
  • PROCESS FOR THE PREPARATION OF CYCLOPROPYLDIKETOPIPERAZINES AND OF A KEY INTERMEDIATE OF DS-5272
    Publication number: 20190389881
    Abstract: Object of the present invention is an improved process for the preparation of cyclopropyldiketopiperazines and thereof key intermediates.
    Type: Application
    Filed: January 15, 2018
    Publication date: December 26, 2019
    Applicant: F.I.S. - Fabbrica Italiana Sintetici S.p.A.
    Inventors: Pierluigi PADOVAN, Kexia Lou
  • PROCESS FOR THE PREPARATION OF CHIRAL 3-AMINO-PIPERIDINS, USEFUL INTERMEDIATES FOR THE PREPARATION OF TOFACITINIB
    Publication number: 20190002407
    Abstract: Object of the present invention is an improved process for the preparation of (3R,4R)-1-benzyl-4-methylpiperidin-3-amine by means of chiral Rhodium catalysts.
    Type: Application
    Filed: June 25, 2018
    Publication date: January 3, 2019
    Applicant: F.I.S. - Fabbrica Italiana Sintetici S.p.A.
    Inventors: Mireia Pastó Aguilà, Sara Preciado Gallego, Emanuele Miserazzi
  • PROCESS FOR THE PREPARATION OF PURE NILOTINIB AND ITS SALT
    Publication number: 20180334449
    Abstract: Object of the present invention is a process for the preparation of the pharmaceutical active ingredient Nilotinib free base or Nilotinib dihydrochloride dihydrate by means of an improved crystallization procedure.
    Type: Application
    Filed: May 15, 2018
    Publication date: November 22, 2018
    Applicant: F.I.S. - Fabbrica Italiana Sintetici S.p.A.
    Inventors: JinPu SHI, Roberto PROFETA
  • Key intermediates and impurities of the synthesis of Apixaban: Apixaban glycol esters
    Patent number: 10040793
    Abstract: Object of the present invention is an improved process for the preparation of Apixaban, through new intermediates which undergo to a faster amidation reaction. Impurities of Apixaban are also identified and quantified.
    Type: Grant
    Filed: November 30, 2017
    Date of Patent: August 7, 2018
    Assignee: F.I.S. FABBRICA ITALIANA SINTETICI S.P.A.
    Inventors: Elena Brasola, Filippo Tomasi
  • Enzymatic process for the preparation of testosterone and esters thereof
    Patent number: 9970042
    Abstract: The present invention relates to a new process for the preparation of testosterone by means of enzymatic hydrolysis of testosterone esters.
    Type: Grant
    Filed: July 11, 2016
    Date of Patent: May 15, 2018
    Assignee: F.I.S.-FABBRICA ITALIANA SINTETICI S.P.A.
    Inventors: Alfredo Paio, Stefano Fogal, Riccardo Motterle
  • DIMER IMPURITIES OF APIXABAN AND METHOD TO REMOVE THEM
    Publication number: 20180118737
    Abstract: Object of the present invention are dimer impurities of the active ingredient Apixaban, analytical methods for identifying and/or quantifying them and a synthetic method for removing or limiting said impurities from Apixaban and synthetic precursors thereof.
    Type: Application
    Filed: July 18, 2016
    Publication date: May 3, 2018
    Applicant: F.I.S. - FABBRICA ITALIANA SINTETICI S.P.A.
    Inventors: Elena BRASOLA, Filippo TOMASI, Loris PERUZZI
  • Efficient Process for the Preparation of Lapatinib and Salts Thereof by Means of New Intermediates
    Publication number: 20150322050
    Abstract: The present invention refers to a new efficient process for the synthesis of the active pharmaceutical ingredient Lapatinib and salts thereof. In particular, the present synthesis is carried out employing new intermediates in which the amine function is protected by a group cleavable in basic milieu that provides a higher overall yield of the synthesis process.
    Type: Application
    Filed: July 21, 2015
    Publication date: November 12, 2015
    Applicant: F.I.S. - Fabbrica Italiana Sintetici S.p.A.
    Inventors: Francesco FONTANA, Alfredo PAIO
  • Efficient Process for the Preparation of Lapatinib and Salts thereof by Means of New Intermediates
    Publication number: 20150225376
    Abstract: The present invention refers to a new efficient process for the synthesis of the active pharmaceutical ingredient Lapatinib and salts thereof. In particular, the present synthesis is carried out employing new intermediates in which the amine function is protected by a group cleavable in basic milieu that provides a higher overall yield of the synthesis process.
    Type: Application
    Filed: February 18, 2015
    Publication date: August 13, 2015
    Applicant: F.I.S. - Fabbrica Italiana Sintetici S.p.A.
    Inventors: Francesco FONTANA, Alfredo Paio
  • Process for the preparation of olopatadine
    Patent number: 8980939
    Abstract: A process for the preparation of olopatadine hydrochloride starting from an advanced intermediate.
    Type: Grant
    Filed: July 12, 2013
    Date of Patent: March 17, 2015
    Assignee: F.I.S. Fabbrica Italiana Sintetici S.p.A.
    Inventors: Andrea Castellin, Clark Ferrari, Marco Galvagni
  • EFFICIENT PROCESS FOR THE PREPARATION OF LAPATINIB AND SALTS THEREOF BY MEANS OF NEW INTERMEDIATES
    Publication number: 20150065710
    Abstract: The present invention refers to a new efficient process for the synthesis of the active pharmaceutical ingredient Lapatinib and salts thereof. In particular, the present synthesis is carried out employing new intermediates in which the amine function is protected by a group cleavable in basic milieu that provides a higher overall yield of the synthesis process.
    Type: Application
    Filed: September 3, 2013
    Publication date: March 5, 2015
    Applicant: F.I.S. - Fabbrica Italiana Sintetici S.p.A.
    Inventors: Francesco Fontana, Alfredo Paio
  • Methods for the preparation of lapatinib and the salts thereof
    Patent number: 8853396
    Abstract: Methods for the synthesis of the pharmaceutically active ingredient Lapatinib and the salts thereof are provided. In particular, such methods utilize intermediates in which the hydroxyl function is protected by a tetrahydropyranyl group providing greater solubility of the intermediates in common organic solvents.
    Type: Grant
    Filed: March 8, 2012
    Date of Patent: October 7, 2014
    Assignee: F.I.S. Fabbrica Italiana Sintetici S.p.A.
    Inventor: Francesco Fontana