Patents by Inventor Marco Villa

Marco Villa 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).

  • Patent number: 6455710
    Abstract: The present invention relates to the process for the preparation and purification of citalopram (I) in which a compound of formula (II) wherein Z is iodo, bromo, chloro or CF3—(CF2)n—SO2—O—, n being 0, 1, 2, 3, 4, 5, 6, 7 or 8, is subjected to a cyanide exchange reaction with a cyanide source; the resultant crude citalopram product is optionally subjected to some initial purification and subsequently treated with an amide or an amide-like group forming agent; the reaction mixture is then subjected to an acid/base wash and/or crystallisation and recrystallisation of citalopram in order to remove the amides formed from the crude citalopram mixture; and the resulting citalopram product is optionally further purified, worked up and isolated as the base or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: January 8, 2002
    Date of Patent: September 24, 2002
    Assignee: H. Lundbeck A/S
    Inventors: Marco Villa, Federico SbrogiĆ², Robert Dancer
  • Patent number: 6448408
    Abstract: A process for the preparation of heteroaryl-phenylalanines of formula (II) in which R is a hydrogen atom, a straight or branched C1-C4 alkyl groups or a benzyl group; R1 is an optionally substituted 5 or 6 membered aromatic heterocyclic group with one or two heteroatoms selected among nitrogen, oxygen and sulphur; comprising a cross-coupling reaction among heteroaryl-zinc halide and phenylalanine derivatives is described. Compounds of formula (II) are intermediates useful for the preparation of compounds endowed with pharmacological activity.
    Type: Grant
    Filed: June 21, 1999
    Date of Patent: September 10, 2002
    Assignee: Zambon Group S.p.A.
    Inventors: Marco Villa, Maurizio Paiocchi, Katiuscia Arrighi
  • Publication number: 20020120005
    Abstract: The present invention relates to the process for the preparation and purification of citalopram (I) 1
    Type: Application
    Filed: January 8, 2002
    Publication date: August 29, 2002
    Applicant: H. Lundbeck A/S
    Inventors: Marco Villa, Federico Sbrogio, Robert Dancer
  • Publication number: 20020028946
    Abstract: 1
    Type: Application
    Filed: June 21, 1999
    Publication date: March 7, 2002
    Inventors: MARCO VILLA, MAURIZIO PAIOCCHI, KATIUSCIA ARRIGHI
  • Patent number: 6271375
    Abstract: A process of direct metalation of phenyltetrazoles useful for preparing compounds of formula (II) intermediates for the synthesis of angiotensin II antagonists is described.
    Type: Grant
    Filed: April 27, 2000
    Date of Patent: August 7, 2001
    Assignee: Zambon Group S.p.A.
    Inventors: Marco Villa, Pietro Allegrini, Katiuscia Arrighi, Maurizio Paiocchi
  • Patent number: 6239301
    Abstract: A method for the removal of heavy metals from solutions of organic compounds by treatment with cysteine or with an N-acylcysteine is described. Organic compounds with a content of heavy metal, for example palladium, particularly low and suitable for the preparation of compounds with pharmacologic activity can be isolated from the resultant solutions.
    Type: Grant
    Filed: December 30, 1999
    Date of Patent: May 29, 2001
    Assignee: Zambon Group S.p.A.
    Inventors: Marco Villa, Vincenzo Cannata, Alessandro Rosi, Pietro Allegrini
  • Patent number: 6211387
    Abstract: A compound of formula (II), wherein R1 is chloro, fluoro or trifluoromethyl; R2 is hydrogen, chloro, fluoro or trifluoromethyl; and R is hydrogen or a protective group for the hydroxy moiety useful as an intermediate for the synthesis of antimycotic azole compounnds.
    Type: Grant
    Filed: June 5, 2000
    Date of Patent: April 3, 2001
    Assignee: Zambon Group S.p.A.
    Inventors: Mauro Napoletano, Marco Villa, Aldo Belli, Giancarlo Grancini, Biase Continanza
  • Patent number: 6194584
    Abstract: Process for the preparation of a compound of formula (VII) wherein R1 is Cl, F or CF3; R2 is H, Cl, F or CF3; and R3 is C1-4 alkyl; characterized in that an olefin of formula (II) is epoxidized to give an oxirane of formula (III) which treated with alkyl-magnesium halide gives a triol of formula (IV) which is turned into an epoxide of formula (V), then treated with 1,2,4-triazole. The compounds (VII) are useful for preparing azole derivatives active as antifungal agent.
    Type: Grant
    Filed: June 2, 2000
    Date of Patent: February 27, 2001
    Assignee: Zambon Group S.p.A.
    Inventors: Marco Villa, Mauro Napoletano, Aldo Belli, Francesco Ponzini, Fabio Rondina
  • Patent number: 6187936
    Abstract: A process for the preparation of I: in which R and R1 have the meanings reported in the description, that comprises the enzymatic kinetic resolution by transesterification with aminoalcohols of 3-phenylglycidates of formula I: is described.
    Type: Grant
    Filed: September 20, 1999
    Date of Patent: February 13, 2001
    Assignee: Zambon Group S.p.A.
    Inventors: Marco Villa, Dario Tentorio, Angelo Restelli, Sergio Riva
  • Patent number: 6114523
    Abstract: A process which allows the re-use of compounds of formula ##STR1## in diltiazem synthesis through a process of conversion to a mixture of enantiomers III-(2R,3R) and III-(2S,3S) is described.
    Type: Grant
    Filed: October 21, 1998
    Date of Patent: September 5, 2000
    Assignee: Zamon Group S.p.A.
    Inventors: Pietro Allegrini, Gaetano Marchioro, Giuseppe Barreca, Marco Villa, Laura Russo
  • Patent number: 6100425
    Abstract: A process for the preparation of the compound L-5-(2-acetoxypropionylamino)-2,4,6-triiodoisophthaloyl dichloride by reacting 5-amino-2,4,6-triiodoisophthaloyl dichloride with L-2-acetoxypropionyl chloride in N,N-dimethylacetamide as a solvent, characterized in that a catalytic amount of a lower alcohol is added to the reaction mixture.
    Type: Grant
    Filed: December 19, 1997
    Date of Patent: August 8, 2000
    Assignee: Bracco International, B.V.
    Inventors: Marco Villa, Maurizio Paiocchi
  • Patent number: 5922917
    Abstract: A process for the preparation of 2-amino-1,3-propanediol comprising the catalytic hydrogenation of 1,3-dihydroxyacetone oxime in the presence of rhodium supported on alumina is described.
    Type: Grant
    Filed: September 19, 1996
    Date of Patent: July 13, 1999
    Assignee: Bracco International B.V.
    Inventors: Antonio Nardi, Marco Villa
  • Patent number: 5817861
    Abstract: A process for the preparation of (S)-N,N'-bis?2-hydroxy-1-(hydroxymethyl)ethyl!-5-(2-acetoxy-propionylamino )-2,4,6-triiodo-isophthalamide, an intermediate useful for the synthesis of iopamidol, by reaction between L-5-(2-acetoxy-propionylamino)-2,4,6-triiiodoisophthaloyl dichloride and 2-amino-1 ,3-propanediol in N-methylpyrrolidone and in the presence of a base, is described.
    Type: Grant
    Filed: March 21, 1997
    Date of Patent: October 6, 1998
    Assignee: Bracco International BV
    Inventors: Marco Villa, Antonio Nardi, Maurizio Paiocchi
  • Patent number: 5770773
    Abstract: A process for the preparation of 5-amino-1,3-dioxanes of formula (I), comprising the catalytic hydrogenation of the new oximes of formula (II) is described.
    Type: Grant
    Filed: March 28, 1997
    Date of Patent: June 23, 1998
    Assignee: Zambon Group S.p.A.
    Inventors: Antonio Nardi, Marco Villa
  • Patent number: 5663432
    Abstract: A process for the preparation of 5-amino-2,4,6-triiodoisophthalic acid dichloride by chlorination of 5-amino-2,4,6-triiodoisophthalic acid with thionyl chloride in the presence of a suitable solvent characterized in that the reaction is carried out in the presence of catalytic amounts of a tetraalkylammonium salt of formulaR.sub.1 R.sub.2 R.sub.3 R.sub.4 NX (I)wherein X is halogen, mesylate or tosylate; R.sub.1, R.sub.2, R.sub.3 and R.sub.4, the same or different, are C.sub.1 -C.sub.20 alkyl groups so that the total number of carbon atoms of the groups R.sub.1, R.sub.2, R.sub.3 and R.sub.4 is higher than 16.The 5-amino-2,4,6-triiodoisophthalic acid dichloride obtained according to the process of the present invention is useful as intermediate in the synthesis of iodinated contrast media.
    Type: Grant
    Filed: May 17, 1996
    Date of Patent: September 2, 1997
    Assignee: Zambon Group S.p.A.
    Inventors: Marco Villa, Claudio Pozzoli, Laura Russo, Graziano Castaldi
  • Patent number: 5663372
    Abstract: Described herein is a process for the preparation of 5-amino-1,3-dioxanes of formula (I), wherein R and R.sub.1 have the meanings reported in the description, comprising the catalytic hydrogenation of the new oximes of formula (II).
    Type: Grant
    Filed: October 10, 1996
    Date of Patent: September 2, 1997
    Assignee: Zambon Group S.p.A.
    Inventors: Antonio Nardi, Marco Villa
  • Patent number: 5580993
    Abstract: A process for the preparation of Iopamidol and 5-amino-2,2-dialkyl-1,3-dioxanes of formula ##STR1## wherein R and R.sub.1 are the same or different and represent a straight or branched C.sub.1 and C.sub.2 alkyl group or together with the carbon atom to which they are bonded, form a C.sub.5 -C.sub.6 cycloaliphatic ring; comprising the transformation of a 2,2-dialkyl-1,3-dioxane-5-carboxylic acid ester of formula ##STR2## wherein R.sub.2 represents a straight or branched C.sub.1 -C.sub.2 alkyl group, a phenyl optionally substituted by nitro groups or a benzyl; by treatment with ammonia into the corresponding amides and the subsequent rearrangement of the latter into the compounds of formula I, by treatment with a hypohalogenite. The resultant ketals may be used as is, or be converted to 2-amino-1,3-propanediol, and reacted with 5-amino-2,4,6-triiodo-isophthalic acid dichloride or, alternatively,L-5-(2-acetoxy-propionylamino)-2,4,6-triido-isophthalic acid dichloride, to produce Iopamidol.
    Type: Grant
    Filed: September 12, 1994
    Date of Patent: December 3, 1996
    Assignee: Zambon Group S.p.A.
    Inventors: Marco Villa, Antonio Nardi
  • Patent number: 5571941
    Abstract: A process for purifying Iopamidol which uses a butanol as solvent is described. Iopamidol is obtained with high yields, also starting from aqueous solutions of the same and has characteristics in accordance with those required by pharmacopoeia.
    Type: Grant
    Filed: July 29, 1994
    Date of Patent: November 5, 1996
    Assignee: Zambon Group S.p.A.
    Inventors: Marco Villa, Maurizio Paiocchi
  • Patent number: 5401852
    Abstract: Intermediates for transforming (2S,3S)-2-amino-3-phenyl-1,3-propanediols into their (2R,3R)-enantiomers are described. The final compounds are useful intermediates for the synthesis of antibiotics like chloramphenicol, Thiamphenicol and Florfenicol.
    Type: Grant
    Filed: September 28, 1993
    Date of Patent: March 28, 1995
    Assignee: Zambon Group S.p.A.
    Inventors: Marco Villa, Claudio Giordano, Silvia Cavicchioli, Silvio Levi
  • Patent number: RE36433
    Abstract: A process for purifying Iopamidol which uses a butanol as solvent is described. Iopamidol is obtained with high yields, also starting from aqueous solutions of the same and has characteristics in accordance with those required by pharmacopoeia.
    Type: Grant
    Filed: February 7, 1997
    Date of Patent: December 7, 1999
    Assignee: Bracco International B.V.
    Inventors: Marco Villa, Maurizio Paiocchi