Patents Assigned to Dipharma Francis S.r.l.
  • Patent number: 8063244
    Abstract: A process for the preparation of a compound of formula (I) is disclosed, which comprises: a) the reaction of a compound of formula (II) with zinc azide of formula (III) Zn(N3)2??(III) in the presence of a solvent of formula R1—OH, wherein R1 is herein defined, to obtain a compound of formula (IV), b) its conversion into a compound of formula (V); c) its enantiomeric enrichment to obtain the (S) enantiomer of formula (VI); and d) the hydrolysis thereof.
    Type: Grant
    Filed: April 29, 2010
    Date of Patent: November 22, 2011
    Assignee: Dipharma Francis S.r.l.
    Inventors: Gabriele Razzetti, Pietro Allegrini, Dario Pastorello
  • Publication number: 20110269962
    Abstract: Process for the preparation of ?-ketoester synthetic intermediates useful in the preparation of statins, in particular Pitavastatin.
    Type: Application
    Filed: April 22, 2011
    Publication date: November 3, 2011
    Applicant: DIPHARMA FRANCIS S.R.L.
    Inventors: Maurizio TADDEI, Evita BALDUCCI, Emanuele ATTOLINO, Simone MANTEGAZZA, Gianmaria DELL'ANNA
  • Patent number: 7989618
    Abstract: Linezolid salts, useful as such and as intermediates in a process for the preparation of novel and known crystalline linezolid forms, in particular known as Form III.
    Type: Grant
    Filed: September 3, 2008
    Date of Patent: August 2, 2011
    Assignee: DiPharma Francis s.r.l.
    Inventors: Chiara Vladiskovic, Emanuele Attolino, Pietro Allegrini, Gabriele Razzetti
  • Patent number: 7982062
    Abstract: A process for the preparation of high purity cholanic acids, typically in purity equal to or higher than 99%.
    Type: Grant
    Filed: September 11, 2007
    Date of Patent: July 19, 2011
    Assignee: Dipharma Francis s.r.l.
    Inventors: Pietro Allegrini, Tiziano Scubla, Fausto Gorassini, Andrea Finco
  • Publication number: 20110152367
    Abstract: Disclosed is a process for the preparation of (R)-2-(3-diisopropylamino-1-phenylpropyl)-4-(hydroxymethyl)-phenol isobutyrate (Fesoterodine) or a pharmaceutically acceptable salt thereof having a low content of impurities such as tolterodine and tolterodine isobutyrate.
    Type: Application
    Filed: December 20, 2010
    Publication date: June 23, 2011
    Applicant: DIPHARMA FRANCIS S.R.L.
    Inventors: Marco ARTICO, Emanuele ATTOLINO, Pietro ALLEGRI
  • Publication number: 20110124917
    Abstract: The present invention relates to a process for the preparation of (R)-(1-Naphthalen-1-yl-ethyl)-[3-(3-trifluoromethyl-phenyl)-propyl]-amine or a salt thereof, in particular the hydrochloride, and intermediates useful in its synthesis.
    Type: Application
    Filed: November 24, 2010
    Publication date: May 26, 2011
    Applicant: DIPHARMA FRANCIS s.r.l.
    Inventors: Pietro ALLEGRINI, Emanuele Attolino, Davide Rossi
  • Publication number: 20110034523
    Abstract: Disclosed is a crystalline form of rufinamide selected from: a substantially anhydrous and approximately monosolvated with trifluoroacetic acid crystalline form, hereinafter designated as Form ?, and a crystalline form, hereinafter designated as Form ?, characterised by an XRPD spectrum as shown in FIG. 3, wherein the most intense peaks fall at 4.5, 9.0, 13.5, 18.0, 18.8, 19.5, 20.6, 24.6, 25.7, 26.5, 27.4, 27.9, 28.7, 30.0 and 31.8±0.2° in 2?.
    Type: Application
    Filed: August 3, 2010
    Publication date: February 10, 2011
    Applicant: DIPHARMA FRANCIS S.R.L.
    Inventors: Gabriele RAZZETTI, Chiara VLADISKOVIC, Pietro ALLEGRINI
  • Publication number: 20110028728
    Abstract: Process for the preparation of crystalline anhydrous (R)-2-[[[3-methyl-4-(2,2,2-trifluoroetoxy)-2-piridyl]methyl]sulphinyl]benzimidazole (dexlansoprazole).
    Type: Application
    Filed: July 6, 2010
    Publication date: February 3, 2011
    Applicant: DIPHARMA FRANCIS S.r.l.
    Inventors: Chiara VLADISKOVIC, Alessandro Restelli, Gabriele Razzetti
  • Publication number: 20100331541
    Abstract: A process for the preparation of 2(R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]-7(8H)-pyrazinyl]-1-(2,4,5-trifluorophenyl)-2-butanamine and intermediates useful for the synthesis thereof.
    Type: Application
    Filed: March 19, 2010
    Publication date: December 30, 2010
    Applicant: DIPHARMA FRANCIS S.R.L.
    Inventors: Pietro ALLEGRINI, Emanuele ATTOLINO, Gianmaria DELL'ANNA, Mario MICHIELETTI
  • Publication number: 20100297711
    Abstract: Process for the preparation of intermediates useful in the synthesis of [1[S(R)],2?,4?]-4-cyclohexyl-1-[[[(2-methyl-1-oxypropoxy)propoxy](4-phenylbutyl)phosphinyl]acetyl]-L-proline, and the synthesis thereof, in particular as sodium salt.
    Type: Application
    Filed: May 24, 2010
    Publication date: November 25, 2010
    Applicant: DIPHARMA FRANCIS S.r.l.
    Inventors: Gabriele RAZZETTI, Sergio Riva, Pietro Allegrini, Mario Michieletti, Emanuele Attolino
  • Publication number: 20100292506
    Abstract: A process for the preparation of a compound of formula (I) is disclosed, which comprises: a) the reaction of a compound of formula (II) with zinc azide of formula (III) Zn(N3)2??(III) in the presence of a solvent of formula R1—OH, wherein R1 is herein defined, to obtain a compound of formula (IV), b) its conversion into a compound of formula (V); c) its enantiomeric enrichment to obtain the (S) enantiomer of formula (VI); and d) the hydrolysis thereof.
    Type: Application
    Filed: April 29, 2010
    Publication date: November 18, 2010
    Applicant: DIPHARMA FRANCIS S.r.l.
    Inventors: Gabriele RAZZETTI, Pietro Allegrini, Dario Pastorello
  • Publication number: 20100267954
    Abstract: Process for the purification of paliperidone by formation of a salt thereof, such as the hydrochloride.
    Type: Application
    Filed: April 19, 2010
    Publication date: October 21, 2010
    Applicant: DIPHARMA FRANCIS S.r.l.
    Inventors: Simone Mantegazza, Emanuele Attolino, Gabriele Razzetti, Pietro Allegrini
  • Publication number: 20100234616
    Abstract: The invention provides a novel process for the regioselective preparation of a compound of formula (I)
    Type: Application
    Filed: March 12, 2010
    Publication date: September 16, 2010
    Applicant: DIPHARMA FRANCIS S.R.L.
    Inventors: Emanuele ATTOLINO, Lino COLOMBO, Ilaria MORMINO, Pietro ALLEGRINI
  • Patent number: 7790891
    Abstract: A process for the preparation of a compound of formula (I), or a salt thereof, wherein Q is ?CR8— or ?N—; and R1-R8 are as herein defined; comprising the reaction of a compound of formula (II), or a salt thereof, wherein Q, R1-R7 are as herein defined; with a reducing agent selected from a trivalent phosphorous compound, an oxidizable solvent and a sulfonic acid chloride; and, if desired, the conversion of a compound of formula (I) to another compound of formula (I) or a salt thereof.
    Type: Grant
    Filed: October 29, 2007
    Date of Patent: September 7, 2010
    Assignee: Dipharma Francis S.R.L.
    Inventors: Pietro Allegrini, Marcello Rasparini, Gabriele Razzetti, Simone Mantegazza, Vittorio Lucchini, Alberto Bologna
  • Patent number: 7750177
    Abstract: A process for the preparation of entacapone, in particular as the polymorphic form A, comprising the preparation of a compound of formula (V), wherein R is C1-C6 alkyl, by condensation of N,N-diethyl-cyano-acetamide with a compound of formula (IV), wherein R is C1-C6 alkyl, in the presence of a strong basic agent; the dealkylation of the compound of formula (V) to obtain entacapone, and the crystallization thereof from methyl ethyl ketone is performed to yield the polymorphic form A. The polymorphic form A of entacapone may be used to treat Parkinson's disease and/or to enhance effectiveness of muscle control.
    Type: Grant
    Filed: December 18, 2007
    Date of Patent: July 6, 2010
    Assignee: Dipharma Francis s.r.l.
    Inventors: Simone Mantegazza, Pietro Allegrini, Gabriele Razzetti
  • Patent number: 7662610
    Abstract: A process for the preparation of an acid of formula (I), as the individual (R) enantiomer or (S), or a salt thereof wherein R is a protected amino group; and the asterisk * denotes the stereogenic carbon atom, comprising contacting an ester of formula (II), as mixture of (R,S) enantiomers, or a salt thereof, wherein R1 is straight or branched C1-C6 alkyl, optionally substituted with phenyl; (the asterisk * and R defined above), with a lipase from Candida antarctica, under conditions effective to obtain a mixture comprising an acid of formula (I), as the individual (R) enantiomer, and an ester of formula (II), as the individual (S) enantiomer; the subsequent hydrolysis of the latter to obtain an acid of formula (I), as the individual (S) enantiomer; and, if desired, the conversion of an acid of formula (I), either as the (R) or (S) enantiomer, to a salt thereof.
    Type: Grant
    Filed: January 11, 2007
    Date of Patent: February 16, 2010
    Assignee: Dipharma Francis s.r.l.
    Inventors: Sergio Riva, Paola Fassi, Michele Scarpellini, Pietro Allegrini, Gabriele Razzetti
  • Patent number: 7605268
    Abstract: A process for preparation of a compound of formula (I), both as the isomeric mixture and individual isomers, wherein Q is ?CR8— or ?N—; each R1, R2, R3, R4 is independently selected from hydrogen, halogen, hydroxy; nitro; C1-C6 alkyl optionally substituted with hydroxy; alkylthio C1-C6; C1-C6 alkoxy optionally substituted with halogen or C1-C6 alkoxy; phenyl-C1-C6 alkyl; phenyl-C1-C6 alkoxy; and —N(RaRb) wherein each Ra and Rb is independently hydrogen or C1-C6 alkyl or Ra and Rb, taken together with the nitrogen atom they are linked to, form a saturated heterocyclic ring; and each R5, R6, R7, R8 is independently selected from hydrogen, halogen, hydroxy; C1-C6 alkyl optionally substituted with hydroxy; alkylthio C1-C6; C1-C6 alkoxy optionally substituted with halogen; C1-C6 alkyl-carbonyl, C1-C6 alkoxy-carbonyl, and oxazol-2-yl; comprising converting a compound of formula (IV), to said compound of formula (I), in the presence of a catalyst, if necessary in an organic solvent.
    Type: Grant
    Filed: April 20, 2007
    Date of Patent: October 20, 2009
    Assignee: Dipharma Francis s.r.l.
    Inventors: Pietro Allegrini, Marcello Rasparini, Gabriele Razzetti, Roberto Rossi, Gianpiero Ventimigla
  • Publication number: 20090203915
    Abstract: A process for the preparation of (1S,3?R)-quiniclidin-3?-yl-1-phenyl-3,4-dihydro-1H-isoquinolin-2-carboxylate, namely solifenacin, comprising the reaction of a compound of formula (IV) with a compound of formula (V), as herein defined, and the subsequent reaction with 3-quinuclidinol.
    Type: Application
    Filed: January 30, 2009
    Publication date: August 13, 2009
    Applicant: Dipharma Francis S.r.l.
    Inventors: Pietro Allegrini, Lino Colombo, Marco Brusasca, Chiara Vladiskovic, Gabriele Razzetti, Emanuele Attolino
  • Patent number: 7563794
    Abstract: Ziprasidone base or a pharmaceutically acceptable salt thereof free from colored impurities, in particular those giving the product a “slightly pink to pink” coloration.
    Type: Grant
    Filed: March 7, 2006
    Date of Patent: July 21, 2009
    Assignee: Dipharma Francis S.r.l.
    Inventors: Gianpiero Ventimiglia, Pietro Allegrini, Gabriele Razzetti, Domenico Magrone, Alberto Bologna
  • Publication number: 20090156855
    Abstract: Novel crystalline hydrate form of (S)-1-phenylethylammonium (R)-diphenyl-methanesulphinyl-acetate and its use in a process for the preparation of (R)-benzhydrylsulphinylacetamide.
    Type: Application
    Filed: November 4, 2008
    Publication date: June 18, 2009
    Applicant: DIPHARMA FRANCIS S.R.L.
    Inventors: Giuseppe Barreca, Pietro Allegrini, Gabriele Razzetti