Patents Assigned to F.I.S. Fabbrica Italiana Sintetici S.p.A.
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Patent number: 8815862Abstract: 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: GrantFiled: December 3, 2012Date of Patent: August 26, 2014Assignee: F.I.S. Fabbrica Italiana Sintetici S.p.A.Inventors: Clark Ferrari, Andrea Castellin, Marco Galvagni, Nicolas Tesson, Jordi De Mier, Llorenç Rafecas
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Publication number: 20140135501Abstract: 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: ApplicationFiled: January 20, 2014Publication date: May 15, 2014Applicant: F.I.S. - FABBRICA ITALIANA SINTETICI S.p.A.Inventors: Gianni Gottardo, Pierluigi Padovan, Sergio Osti
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Patent number: 8664402Abstract: 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: GrantFiled: January 11, 2012Date of Patent: March 4, 2014Assignee: F.I.S. Fabbrica Italiana Sintetici S.p.A.Inventors: Andrea Castellin, Paolo Stabile, Francesco Fontana, Ottorino De Lucchi, Andrea Caporale, Stefano Tartaggia
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Patent number: 8609841Abstract: 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: GrantFiled: October 13, 2011Date of Patent: December 17, 2013Assignee: F.I.S. Fabbrica Italiana Sintetici S.p.A.Inventors: Andrea Castellin, Ottorino De Lucchi, Andrea Caporale
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Patent number: 8592178Abstract: 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: GrantFiled: June 15, 2010Date of Patent: November 26, 2013Assignee: F.I.S. Fabbrica Italiana Sintetici S.p.A.Inventors: Stefano Fogal, Elisabetta Bergantino, Riccardo Motterle, Andrea Castellin, Giancarlo Arvotti
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Patent number: 8557981Abstract: 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: GrantFiled: May 3, 2011Date of Patent: October 15, 2013Assignee: F.I.S. Fabbrica Italiana Sintetici S.p.A.Inventors: Andrea Castellin, Michele Maggini, Paola Donnola
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Publication number: 20130165650Abstract: 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: ApplicationFiled: February 26, 2013Publication date: June 27, 2013Applicant: F.I.S. Fabbrica Italiana Sintetici S.p.AInventor: F.I.S. Fabbrica Italiana Sintetici S.p.A
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Publication number: 20130143890Abstract: 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: ApplicationFiled: December 3, 2012Publication date: June 6, 2013Applicant: F.I.S. Fabbrica Italiana Sintetici S.p.A.Inventor: F.I.S. Fabbrica Italiana Sintetici S.p.A.
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Patent number: 8426612Abstract: 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: GrantFiled: November 9, 2009Date of Patent: April 23, 2013Assignee: F.I.S. Fabbrica Italiana Sintetici S.p.A.Inventors: Siro Serafini, Andrea Castellin, Claudio Dal Santo
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Patent number: 8420808Abstract: 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: GrantFiled: January 30, 2009Date of Patent: April 16, 2013Assignee: F.I.S. Fabbrica Italiana Sintetici S.p.A.Inventors: Alessandro Leganza, Marco Galvagni
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Publication number: 20130059880Abstract: 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: ApplicationFiled: July 9, 2012Publication date: March 7, 2013Applicant: F.I.S. - FABBRICA ITALIANA SINTETICI S.p.A.Inventors: Gianni Gottardo, Pierluigi Padovan, Sergio Osti
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Patent number: 8389716Abstract: 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: GrantFiled: January 30, 2009Date of Patent: March 5, 2013Assignee: F.I.S. Fabbrica Italiana Sintetici S.p.A.Inventors: Siro Serafini, Filippo Tomasi, Marco Galvagni
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Publication number: 20130040958Abstract: 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: ApplicationFiled: July 11, 2012Publication date: February 14, 2013Applicant: F.I.S. Fabbrica Italiana Sintetici S.p.A.Inventors: Ennio GRENDELE, Marco GALVAGNI
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Patent number: 8334381Abstract: 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: GrantFiled: May 20, 2010Date of Patent: December 18, 2012Assignee: F.I.S. Fabbrica Italiana Sintetici S.p.A.Inventors: Alessandro Falchi, Ennio Grendele, Riccardo Motterle, Mariano Stivanello
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Publication number: 20120295928Abstract: 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: ApplicationFiled: May 14, 2012Publication date: November 22, 2012Applicant: F.I.S. FABBRICA ITALIANA SINTETICI S.p.A.Inventors: Francesco Fontana, Alessandro Leganza, Sergio Osti
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Publication number: 20120245350Abstract: 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: ApplicationFiled: March 8, 2012Publication date: September 27, 2012Applicant: F.I.S. FABBRICA ITALIANA SINTETICI S.P.A.Inventor: Francesco Fontana
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Patent number: 8207339Abstract: 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: GrantFiled: March 18, 2011Date of Patent: June 26, 2012Assignee: F.I.S. Fabbrica Italiana Sintetici S.p.A.Inventors: Andrea Castellin, Pierluigi Padovan, Liu Jiageng, Yibo Zhou, Lin Feng
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Patent number: 8168787Abstract: 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: GrantFiled: November 15, 2007Date of Patent: May 1, 2012Assignee: F.I.S. Fabbrica Italiana Sintetici S.p.A.Inventors: Alessandro Falchi, Ennio Grendele, Riccardo Motterle, Mariano Stivanello
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Patent number: 8026372Abstract: 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: GrantFiled: August 4, 2006Date of Patent: September 27, 2011Assignee: F.I.S. Fabbrica Italiana Sintetici S.p.A.Inventors: Siro Serafini, Riccardo Motterle, Elena Brasola
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Publication number: 20110166364Abstract: 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: ApplicationFiled: November 9, 2009Publication date: July 7, 2011Applicant: F.I.S. FABBRICA ITALIANA SINTETICI S.P.A.Inventors: Siro Serafini, Andrea Castellin, Claudio Dal Santo