Patents Assigned to F.I.S. Fabbrica Italiana Sintetici S.p.A.
  • Patent number: 8815862
    Abstract: Methods for the preparation of Rosuvastatin by co-crystals of Rosuvastatin or intermediates are provided. Also provided are co-crystals, pharmaceutical compositions which include such co-crystals and methods for treating conditions associated with hypercholesterolemia by administering such compositions.
    Type: Grant
    Filed: December 3, 2012
    Date of Patent: August 26, 2014
    Assignee: F.I.S. Fabbrica Italiana Sintetici S.p.A.
    Inventors: Clark Ferrari, Andrea Castellin, Marco Galvagni, Nicolas Tesson, Jordi De Mier, Llorenç Rafecas
  • Publication number: 20140135501
    Abstract: Methods for producing moxifloxacin hydrochloride compounds having very low levels of impurities are provided. Compounds produced using such methods and pharmaceutical compositions including such compounds are also provided.
    Type: Application
    Filed: January 20, 2014
    Publication date: May 15, 2014
    Applicant: F.I.S. - FABBRICA ITALIANA SINTETICI S.p.A.
    Inventors: Gianni Gottardo, Pierluigi Padovan, Sergio Osti
  • Patent number: 8664402
    Abstract: A process for preparing 1-(6-methylpyridin-3-yl)-2-[4-(methyl sulfonyl)phenyl]ethanone, an intermediate of the synthesis of Etoricoxib. The synthesis of the intermediates useful for such preparation is also described.
    Type: Grant
    Filed: January 11, 2012
    Date of Patent: March 4, 2014
    Assignee: F.I.S. Fabbrica Italiana Sintetici S.p.A.
    Inventors: Andrea Castellin, Paolo Stabile, Francesco Fontana, Ottorino De Lucchi, Andrea Caporale, Stefano Tartaggia
  • Patent number: 8609841
    Abstract: An alternative method for the preparation of Erlotinib through a new chemical reaction for the preparation of the 4-(3-aminophenyl)-2-methyl-3-butyn-2-ol key intermediate of formula (IV) according to the following scheme.
    Type: Grant
    Filed: October 13, 2011
    Date of Patent: December 17, 2013
    Assignee: F.I.S. Fabbrica Italiana Sintetici S.p.A.
    Inventors: Andrea Castellin, Ottorino De Lucchi, Andrea Caporale
  • Patent number: 8592178
    Abstract: The present invention relates to an industrial process for the reduction of 4-androstene-3,17-dione in order to obtain testosterone using a particularly stable and selective enzyme produced in a recombinant manner.
    Type: Grant
    Filed: June 15, 2010
    Date of Patent: November 26, 2013
    Assignee: F.I.S. Fabbrica Italiana Sintetici S.p.A.
    Inventors: Stefano Fogal, Elisabetta Bergantino, Riccardo Motterle, Andrea Castellin, Giancarlo Arvotti
  • Patent number: 8557981
    Abstract: The present invention refers to a process for the preparation of 4H-imidazo[1,5-a][1,4]benzodiazepines, in particular Midazolam, through an efficient and selective decarboxylation reaction of the derivative compound of the 5-aminomethyl-1-phenyl-1H-imidazole-4-carboxylic acid of formula (II) avoiding the formation of the 6H-imidazo[1,5-a][1,4]benzodiazepines by-products and the ensuing process for the isomerization of a 4H-imidazo[1,5-a][1,4]benzodiazepine product.
    Type: Grant
    Filed: May 3, 2011
    Date of Patent: October 15, 2013
    Assignee: F.I.S. Fabbrica Italiana Sintetici S.p.A.
    Inventors: Andrea Castellin, Michele Maggini, Paola Donnola
  • Publication number: 20130165650
    Abstract: A process for the preparation of Efavirenz, (4S)-6-chloro-4-(cyclopropylethynyl)-4-(trifluoromethyl)-1,4-dihydro-2H-3,1-benzoxazin-2-one, of formula (I): comprising reacting the intermediate of formula (II): as a free base or a salt thereof, with diphosgene (TCMCF, trichloromethylchloroformate) Cl3CO—COCl in an organic solvent or in a biphasic medium comprised of an organic solvent and water, preferably but not mandatorily in the presence of a weak base in an amount sufficient to neutralize the reaction mixture or in an up to 30% molar excess of such amount.
    Type: Application
    Filed: February 26, 2013
    Publication date: June 27, 2013
    Applicant: F.I.S. Fabbrica Italiana Sintetici S.p.A
    Inventor: F.I.S. Fabbrica Italiana Sintetici S.p.A
  • Publication number: 20130143890
    Abstract: Methods for the preparation of Rosuvastatin by co-crystals of Rosuvastatin or intermediates are provided. Also provided are co-crystals, pharmaceutical compositions which include such co-crystals and methods for treating conditions associated with hypercholesterolemia by administering such compositions.
    Type: Application
    Filed: December 3, 2012
    Publication date: June 6, 2013
    Applicant: F.I.S. Fabbrica Italiana Sintetici S.p.A.
    Inventor: F.I.S. Fabbrica Italiana Sintetici S.p.A.
  • Patent number: 8426612
    Abstract: The present invention refers to the synthesis of 3-{[(2R)-1-methylpyrrolidin-2-yl]methyl}-5-[2-(phenylsulfonyl)ethyl]-1H-indole, a drug known by the name Eletriptan, or of its salts. In particular, the present invention regards a process for the synthesis of Eletriptan or of its salt, comprising the following steps: a) Salifying the intermediate of Formula (6), using a dicarboxylic acid to obtain a derived salt; b) Optionally, purifying said raw salt obtained according to step a) by solvent crystallization to obtain a purified salt of the intermediate of Formula (6); c) Converting said salt of the intermediate of formula (6) according to step a) or said purified salt according to step b) into an intermediate of formula (10); d) Converting the intermediate of Formula (10) into Eletriptan or its salt.
    Type: Grant
    Filed: November 9, 2009
    Date of Patent: April 23, 2013
    Assignee: F.I.S. Fabbrica Italiana Sintetici S.p.A.
    Inventors: Siro Serafini, Andrea Castellin, Claudio Dal Santo
  • Patent number: 8420808
    Abstract: The present invention is directed to a process for the preparation of Efavirenz, (4S)-6-chloro-4-(cyclopropylethynyl)-4-(trifluoromethyl)-1,4-dihydro-2H-3,1-benzoxazin-2-one, of formula (I) comprising reacting the intermediate of formula (II) [0045] as a free base or a salt thereof, with diphosgene (TCMCF, trichlormethylchloroformate) Cl3CO—COCl in an organic solvent or in a biphasic medium comprised of an organic solvent and water, preferably but not mandatorily in the presence of a weak base in an amount sufficient to neutralise the reaction mixture or in an up to 30% molar excess of such amount.
    Type: Grant
    Filed: January 30, 2009
    Date of Patent: April 16, 2013
    Assignee: F.I.S. Fabbrica Italiana Sintetici S.p.A.
    Inventors: Alessandro Leganza, Marco Galvagni
  • Publication number: 20130059880
    Abstract: Methods for producing moxifloxacin hydrochloride compounds having very low levels of impurities are provided. Compounds produced using such methods and pharmaceutical compositions including such compounds are also provided.
    Type: Application
    Filed: July 9, 2012
    Publication date: March 7, 2013
    Applicant: F.I.S. - FABBRICA ITALIANA SINTETICI S.p.A.
    Inventors: Gianni Gottardo, Pierluigi Padovan, Sergio Osti
  • Patent number: 8389716
    Abstract: The present invention relates to a process for the synthesis of quetiapine. In particular, a process is provided for the synthesis of quetiapine of formula (A) comprising reacting dibenzo[b,f][1,4]thiazepin-11(10H)-one, intermediate (I) with phosphorous oxychloride to give 11-chlorodibenzo[b,f][1,4]thiazepine, intermediate (II) wherein the said reaction of intermediate (I) to intermediate (II) is performed in an organic solvent in the presence of a mixture of an organic base together with an inorganic base.
    Type: Grant
    Filed: January 30, 2009
    Date of Patent: March 5, 2013
    Assignee: F.I.S. Fabbrica Italiana Sintetici S.p.A.
    Inventors: Siro Serafini, Filippo Tomasi, Marco Galvagni
  • Publication number: 20130040958
    Abstract: Methods for making Imatinib mesylate of formula (I): having low levels of organic solvent are provided. Also provided are alpha and beta forms of Imatinib mesylate and methods for treating conditions such as chronic myelogenous leukaemia by administering same.
    Type: Application
    Filed: July 11, 2012
    Publication date: February 14, 2013
    Applicant: F.I.S. Fabbrica Italiana Sintetici S.p.A.
    Inventors: Ennio GRENDELE, Marco GALVAGNI
  • Patent number: 8334381
    Abstract: It is the object of the present invention a process for the preparation of 4-methyl-N3-[4-(3-pyridinyl)-2-pyrimidinyl]-1,3-benzenediamine and analogues thereof, intermediates useful for the synthesis of Imatinib, or 4-[(4-methyl-1-piperazinyl)methyl]-N-[4-methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]phenyl]benzamide.
    Type: Grant
    Filed: May 20, 2010
    Date of Patent: December 18, 2012
    Assignee: F.I.S. Fabbrica Italiana Sintetici S.p.A.
    Inventors: Alessandro Falchi, Ennio Grendele, Riccardo Motterle, Mariano Stivanello
  • Publication number: 20120295928
    Abstract: Impurities of lapatinib such as N-{3-chloro-4-[(2-fluorobenzyl)oxy]phenyl}-6-[5-({[2-(methylsulfonyl)ethyl]amino}methyl)furan-2-yl]quinazoline-4-amine compound of formula (I) or a salt thereof: and analytical methods for identifying and quantifying such impurities of Lapatinib and salts thereof are provided. Also provided is Lapatinib containing less than about 0.05 percent of this and related impurities and methods for preparing such pure forms of Lapatinib.
    Type: Application
    Filed: May 14, 2012
    Publication date: November 22, 2012
    Applicant: F.I.S. FABBRICA ITALIANA SINTETICI S.p.A.
    Inventors: Francesco Fontana, Alessandro Leganza, Sergio Osti
  • Publication number: 20120245350
    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: Application
    Filed: March 8, 2012
    Publication date: September 27, 2012
    Applicant: F.I.S. FABBRICA ITALIANA SINTETICI S.P.A.
    Inventor: Francesco Fontana
  • Patent number: 8207339
    Abstract: The present invention relates to a process for the synthesis of Moxifloxacin of Formula (I) and salts thereof by means of a process providing the coupling reaction of 1-cyclopropril-6,7-difluoro-1,4-dihydro-8-methoxy-4-oxo -3-quinolinic acid or ester thereof with (4aS, 7aS) -octahydro-1H-pyrrole[3,4-b]pyridine using a magnesium salt.
    Type: Grant
    Filed: March 18, 2011
    Date of Patent: June 26, 2012
    Assignee: F.I.S. Fabbrica Italiana Sintetici S.p.A.
    Inventors: Andrea Castellin, Pierluigi Padovan, Liu Jiageng, Yibo Zhou, Lin Feng
  • Patent number: 8168787
    Abstract: A process for the preparation of 4-methyl-N3-[4-(3-pyridinyl)-2-pyrimidinyl]-1,3-benzenediamine and analogues thereof, intermediates useful for the synthesis of Imatinib, or 4-[(4-methyl-1-piperazinyl)methyl]-N-[4-methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]phenyl]benzamide.
    Type: Grant
    Filed: November 15, 2007
    Date of Patent: May 1, 2012
    Assignee: F.I.S. Fabbrica Italiana Sintetici S.p.A.
    Inventors: Alessandro Falchi, Ennio Grendele, Riccardo Motterle, Mariano Stivanello
  • Patent number: 8026372
    Abstract: A process for the preparation of ?-alkoxycarbonylamino-?-aminoacids and ?,? orthogonally diprotected diaminoacids from ?,?-diaminoacids using 1-alkoxycarbonylbenzotriazoles as protecting agents is disclosed. In an alternative embodiment, carbamoylating agents in the presence of benzotriazoles are used instead of 1-alkoxycarbonylbenzotriazoles. This reaction is preferably applied to the preparation of ?-alkoxycarbonyllysines from lysine. A process for the preparation of t-butoxycarbonylbenzotriazoles and novel complexes of ?-alkoxycarbonylamino-?-aminoacids with benzotriazoles are also disclosed.
    Type: Grant
    Filed: August 4, 2006
    Date of Patent: September 27, 2011
    Assignee: F.I.S. Fabbrica Italiana Sintetici S.p.A.
    Inventors: Siro Serafini, Riccardo Motterle, Elena Brasola
  • Publication number: 20110166364
    Abstract: The present invention refers to the synthesis of 3-{[(2R)-1-methylpyrrolidin-2-yl]methyl}-5-[2-(phenylsulfonyl)ethyl]-1H-indole, a drug known by the name Eletriptan, or of its salts. In particular, the present invention regards a process for the synthesis of Eletriptan or of its salt, comprising the following steps: a) Salifying the intermediate of Formula (6), using a dicarboxylic acid to obtain a derived salt; b) Optionally, purifying said raw salt obtained according to step a) by solvent crystallization to obtain a purified salt of the intermediate of Formula (6); c) Converting said salt of the intermediate of formula (6) according to step a) or said purified salt according to step b) into an intermediate of formula (10); d) Converting the intermediate of Formula (10) into Eletriptan or its salt.
    Type: Application
    Filed: November 9, 2009
    Publication date: July 7, 2011
    Applicant: F.I.S. FABBRICA ITALIANA SINTETICI S.P.A.
    Inventors: Siro Serafini, Andrea Castellin, Claudio Dal Santo