Patents by Inventor Andrea Castellin

Andrea Castellin 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: 20240033228
    Abstract: A system for the administration and delivery of active ingredients includes a vector or carrier chosen from the mesoporous nanoparticles and one or more pharmacologically active ingredients (API) including molecules with antibacterial, bacteriostatic or bactericidal and/or mucolytic and/or anti-inflammatory activity, loaded and/or supported in said vector, in which said vector is constituted by mesoporous particles of zirconia (MZN).
    Type: Application
    Filed: October 7, 2021
    Publication date: February 1, 2024
    Inventors: Emmanuele Kizito AMBROSI, Benedetta LEONETTI, Andrea CASTELLIN, Gabriele SPONCHIA
  • 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
  • Patent number: 8871953
    Abstract: The present invention relates to a novel process for the preparation of olopatadine hydrochloride starting from an advanced intermediate.
    Type: Grant
    Filed: March 23, 2010
    Date of Patent: October 28, 2014
    Assignee: F.I.S. Fabbrica Italiana Sintetiei S.p.A.
    Inventors: Andrea Castellin, Clark Ferrari, Marco Galvagni
  • 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
  • Patent number: 8680276
    Abstract: The present invention relates to the stereoselective synthesis of (4aS,7aS)-octahydro-1H-pyrrolo[3,4-b]pyridine, as well as the conversion thereof, to give Moxifloxacin. Particularly, the present invention relates to a method for the synthesis of (4aS,7aS)-octahydro-1H-pyrrolo[3,4-b]pyridine of formula (I) comprising: (a) the optical resolution by enzymatic hydrolysis of the intermediate dialkyl-1-alkylcarbonylpiperidine-2,3-dicarboxylate racemate of formula (II) to give, following isolation, the intermediate dialkyl-(2S,3R)-1-alkylcarbonyl-piperidine-2,3-dicarboxylate of formula (III) in which AIk is a straight or branched C1-C5 alkyl group; (b) the conversion of the intermediate (III) to (4aR,7aS)-1-alkylcarbonylhexahydrofuro[3,4-b]pyridine-5,7-dione of formula (IV) in which AIk has the meanings set forth above; (c) the conversion of the intermediate (IV) to (4aS,7as)-octahydro-1H-pyrrolo[3,4-b]pyridine of formula (I) with an optical purity above 99%.
    Type: Grant
    Filed: March 4, 2010
    Date of Patent: March 25, 2014
    Inventors: Riccardo Motterle, Giancarlo Arvotti, Elisabetta Bergantino, Andrea Castellin, Stefano Fogal, Marco Galvagni
  • 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
  • Publication number: 20140024704
    Abstract: A process for the preparation of olopatadine hydrochloride starting from an advanced intermediate.
    Type: Application
    Filed: July 12, 2013
    Publication date: January 23, 2014
    Inventors: Andrea Castellin, Clark Ferrari, Marco Galvagni
  • 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
  • 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: 8344136
    Abstract: The present invention relates to a process for the preparation of Brinzolamide, or 2H-thieno[3,2-e]-1,2-thiazin-6-sulfonamide, 4-(ethyl amino)-3,4-dihydro-2-(3-methoxypropyl)-, 1,1-dioxide, (4R)-via intermediates 2,3-dihydro-4H-thieno[3,2-e]-1,2-thiazin-4-ones, 1,1-dioxide. Further objects of the present invention are the intermediates mentioned above and other intermediates of the synthesis.
    Type: Grant
    Filed: June 15, 2009
    Date of Patent: January 1, 2013
    Assignee: PHF S.A.
    Inventors: Alessandro Falchi, Ottorino De Lucchi, Andrea Castellin
  • Publication number: 20120232281
    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: Application
    Filed: January 11, 2012
    Publication date: September 13, 2012
    Inventors: Andrea Castellin, Paolo Stabile, Francesco Fontana, Ottorino De Lucchi, Andrea Caporale, Stefano Tartaggia
  • 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
  • Publication number: 20120095228
    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: Application
    Filed: October 13, 2011
    Publication date: April 19, 2012
    Inventors: Andrea Castellin, Ottorino De Lucchi, Andrea Caporale
  • Publication number: 20110275799
    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 isomerisation of a 4H-imidazo[1,5-a][1,4]benzodiazepine product.
    Type: Application
    Filed: May 3, 2011
    Publication date: November 10, 2011
    Inventors: Andrea Castellin, Michele Maggini, Paola Donnola
  • Publication number: 20110230661
    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: Application
    Filed: March 18, 2011
    Publication date: September 22, 2011
    Inventors: Andrea Castellin, Pierluigi Padovan, Liu Jiageng, Yibo Zhou, Lin Feng
  • Publication number: 20110207172
    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: Application
    Filed: June 15, 2010
    Publication date: August 25, 2011
    Inventors: Stefano Fogal, Elisabetta Bergantino, Riccardo Motterle, Andrea Castellin, Giancarlo Arvotti
  • 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
  • Publication number: 20110137036
    Abstract: The present invention relates to the stereoselective synthesis of (4aS,7aS)-octahydro-1H-pyrrolo[3,4-b]pyridine, as well as the conversion thereof, to give Moxifloxacin. Particularly, the present invention relates to a method for the synthesis of (4aS,7aS)-octahydro-1H-pyrrolo[3,4-b]pyridine of formula (I) comprising: (a) the optical resolution by enzymatic hydrolysis of the intermediate dialkyl-1-alkylcarbonylpiperidine-2,3-dicarboxylate racemate of formula (II) to give, following isolation, the intermediate dialkyl-(2S,3R)-1-alkylcarbonyl-piperidine-2,3-dicarboxylate of formula (III) in which AIk is a straight or branched C1-C5 alkyl group; (b) the conversion of the intermediate (III) to (4aR,7aS)-1-alkylcarbonylhexahydrofuro[3,4-b]pyridine-5,7-dione of formula (IV) in which AIk has the meanings set forth above; (c) the conversion of the intermediate (IV) to (4aS,7as)-octahydro-1H-pyrrolo[3,4-b]pyridine of formula (I) with an optical purity above 99%.
    Type: Application
    Filed: March 4, 2010
    Publication date: June 9, 2011
    Inventors: Riccardo Motterle, Giancarlo Arvotti, Elisabetta Bergantino, Andrea Castellin, Stefano Fogal, Marco Galvagni