Patents Assigned to ZaCh System
-
Patent number: 7939676Abstract: A process for the manufacturing of levetiracetam, wherein said process comprises the steps of: (1) reacting the (?)-(S)-alpha-ethyl-2-oxo-1-pyrrolidine acetic acid with a substoichiometric amount of an activating agent in an alcoholic solvent, and (2) subjecting the resulting reaction solution of step (1) to an ammonolysis process with gaseous ammonia.Type: GrantFiled: September 17, 2009Date of Patent: May 10, 2011Assignee: Zach System S.p.A.Inventors: Corrado Colli, Massimiliano Forcato, Livius Cotarca
-
Publication number: 20110065932Abstract: A process for the manufacturing of levetiracetam, wherein said process comprises the steps of: (1) reacting the (?)-(S)-alpha-ethyl-2-oxo-1-pyrrolidine acetic acid with a substoichiometric amount of an activating agent in an alcoholic solvent, and (2) subjecting the resulting reaction solution of step (1) to an ammonolysis process with gaseous ammonia.Type: ApplicationFiled: September 17, 2009Publication date: March 17, 2011Applicant: ZACH SYSTEM S.P.A.Inventors: Corrado Colli, Massimiliano Forcato, Livius Cotarca
-
Patent number: 7884243Abstract: A process for the production of ene-amide derivatives represented by the formula (I) wherein R1 and R2 and R3 are independently a hydrogen atom, an alkyl, a cycloalkyl, a cycloalkylalkyl, an alkylaryl, an aryl, a heterocycle, a cyano, an alkoxy, an aryloxy, a carboxyl, a carbamoyl, —CONR5R6 (in which R5 and R6 are independently an alkyl, arylalkyl or aryl group said ring being substituted or not with a functional group or with R5) or —COOR5 group (in which R5 is an alkyl, alkylaryl or aryl group), said alkyl, cycloalkyl, cycloalkylalkyl, alkylaryl and aryl groups being substituted or not with a functional group or with R5; or R1 and R2 taken together, may form a ring (which terms includes mono-, di- and higher polycyclic ring systems); R4 is a hydrogen atom, an alkyl, an aryl, an alkylaryl, said groups are substituted or not with a halogen atom as Cl, Br, or F; X is an oxygen atom or a leaving group and m is an integer 1 or 2; when m is 1 then X is a leaving group; when m is 2 then X is a oxygen atom, whiType: GrantFiled: December 22, 2004Date of Patent: February 8, 2011Assignee: Zach SystemInventors: Alain Burgos, Blandine Bertrand, Sonia Roussiasse, Jean-François Pluvie, Sylvie Blanchet, Juliette Martin, Florence Perrin, Françoise Bourdeau
-
Publication number: 20110021793Abstract: The present invention relates to a process for reducing a compound of formula (I) wherein X is halogen, a hydroxy group, an alkylsulfoniloxy group or an arylsulfonyloxy group; to give a compound of formula (II) as a di-astereoisomerically pure compound of RS/SR configuration characterized in that said reduction is carried out by the use of (+)-B-chlorodiisopinocampheylborane or (?)-B-chlorodiisopinocampheylborane. The compounds of formula (II) are useful as intermediates for the preparation of Nebivolol.Type: ApplicationFiled: March 16, 2009Publication date: January 27, 2011Applicant: ZACH SYSTEM S.P.A.Inventors: Raffaella Volpicelli, Paolo Maragni, Franco Massaccesi, Ilaria Munari, Livius Cotarca, Johnny Foletto
-
Patent number: 7759517Abstract: The present invention relates to a process for the preparation of gabapentin and, more in particular, to a method of synthesis of 1,1-cyclohexane acetic acid monoamide, an intermediate used in the preparation of gabapentin, comprising the basic hydrolysis reaction of ?, -diaminocarbonyl-?,?-pentamethylene glutarimide.Type: GrantFiled: June 22, 2005Date of Patent: July 20, 2010Assignee: Zach System S.P.A.Inventors: Marco Villa, Maurizio Paiocchi, Katiuscia Arrighi, Francesco Corcella, Vincenzo Cannata, Giorgio Soriato, Massimo Verzini
-
Publication number: 20100160436Abstract: Stable compositions containing gabapentin compositions, methods of preparing such compositions, and methods of using such compositions.Type: ApplicationFiled: March 1, 2010Publication date: June 24, 2010Applicant: ZaCh System S.p.A.Inventors: Vincenzo CANNATA, Francesco Corcella, Andrea Nicoli
-
Publication number: 20100076206Abstract: The present invention relates to a process for preparing Nebivolol and, more particularly, to an improved process for synthesizing enantiomerically enriched 6-fluoro chroman alcohol or epoxide derivatives of formula, wherein R and X is defined in the description; as useful intermediates in the preparation of Nebivolol.Type: ApplicationFiled: November 23, 2007Publication date: March 25, 2010Applicant: ZACH SYSTEM S.P.A.Inventors: Elio Ullucci, Paolo Maragni, Livius Cotarca, Johnny Foletto
-
Publication number: 20100076204Abstract: The present invention relates to a process for the preparation of levetiracetam and, more particularly, to an improved process for the preparation of levetiracetam characterized by a crystallization-induced dynamic resolution of a diastereoisomeric mixture of an (±)-alpha-ethyl-2-oxo-1-pyrrolidine acetamide derivative.Type: ApplicationFiled: July 20, 2007Publication date: March 25, 2010Applicant: ZACH SYSTEM S.P.A.Inventors: Massimiliano FORCATO, Ivan MICHIELETTO, Paolo MARAGNI, Franco MASSACCESI, Livius COTARCA
-
Publication number: 20100069652Abstract: The present invention relates to a process for the preparation of Nebivolol and, more particularly, to an improved method of synthesizing 6-fluoro chroman epoxides of formula (I) key intermediates in preparing nebivolol.Type: ApplicationFiled: October 2, 2007Publication date: March 18, 2010Applicant: ZACH SYSTEM S.P.A.Inventor: Raffaella Volpicelli
-
Publication number: 20100068770Abstract: The invention relates to a synthesis process. This process relates to the synthesis of the compound of formula (I) according to Scheme A below: in which R1, R2 and R3, which may be identical or different, represent, individually and independently, an alkyl group, characterized by an enzymatic hydrolysis reaction that involves placing the compound of formula (II) in contact with an enzyme that performs a chemoselective hydrolysis of only one of the two ester functions of the compound of formula (II) to obtain the compound of formula (I). The invention allows the industrial preparation of the intermediate of formula (I), which may be used for the preparation of the pharmaceutical active principle repaglinide.Type: ApplicationFiled: January 22, 2008Publication date: March 18, 2010Applicants: ZACH SYSTEM, NOVACTA BIOSYSTEMS LIMITEDInventors: Alain Burgos, Jean-Claude Caille, Michelle Lorraine Gradley
-
Publication number: 20100056813Abstract: The present invention relates to a process for preparing nebivolol and, more particularly, to a process for preparing d-nebivolol and its enantiomer l-nebivolol or acid addition salts thereof starting from commercially available or easily obtainable 2,2-dimethyl-1,3 dioxolane-4-carbaldehyde and a vinyl Grignard reagent.Type: ApplicationFiled: November 23, 2007Publication date: March 4, 2010Applicant: ZACH SYSTEM S.P.A.Inventors: Raffaella Volpicelli, Paolo Maragni, Livius Cotarca, Johnny Foletto, Franco Massaccesi
-
Publication number: 20090326266Abstract: A process for the preparation of 1,1-cyclohexanediacetic acid monoamide comprising the amination of 1,1-cyclohexanediacetic acid anhydride by reaction with aqueous NH3 at a temperature lower than 30° C. by using a NH3/anhydride molar ratio lower than 3, and the product precipitation through the acidification of the reaction mixture; a precipitation process of 1,1-cyclohexanediacetic acid monoamide; and a process for the synthesis of gabapentin comprising the above preparation of 1,1-cyclohexanediacetic acid monoamide, the Hofmann transposition of the same monoamide, the purification of a gabapentin salt and the crystallization from organic solvent.Type: ApplicationFiled: March 9, 2009Publication date: December 31, 2009Applicant: ZACH SYSTEM S.p.A.Inventors: Katiuscia ARRIGHI, Vincenzo CANNATA, Francesco CORCELLA, Gaetano MARCHIORO, Andrea NICOLI, Maurizio PAIOCCHI, Marco VILLA
-
Publication number: 20090292138Abstract: The present invention relates to a process for the purification of gabapentin. The process relates to the addition of hydrochloric acid to an aqueous solution or suspension of gabapentin, before, during or after the concentration step of that solution, and the subsequent slurry of the gabapentin by the addition of an alcoholic solvent. The so obtained gabapentin has an high purity degree and, in particular, is characterized by a low content of lactam.Type: ApplicationFiled: December 15, 2005Publication date: November 26, 2009Applicant: ZACH SYSTEM S.P.A.Inventors: Roberto Giovanetti, Andrea Nicoli, Livius Cotarca
-
Publication number: 20090275759Abstract: A process for resolving dorzolamide trans racemate, which comprises reacting said racemate with (1S)-(+)-10-camphorsulfonic acid so obtaining the (4S,6S) enantiomer by selectively precipitating and recovering the camphorsulfonic acid salt thereof (dorzolamide camphorsulfonate), and neutralizing dorzolamide camphorsulfonate to obtain dorzolamide.Type: ApplicationFiled: April 16, 2007Publication date: November 5, 2009Applicant: ZACH SYSTEM S.P.A.Inventors: Paolo Maragni, Ivan Michieletto, Livius Cotarca
-
Patent number: 7586015Abstract: A process is used for the preparation of 1,3,2-oxazaborolidine compounds. This process prepares compounds of formula (I) or (IA): in which: R1 is an alkyl or an aryl; and R2, R3, R4 and R5 are especially a hydrogen atom or an alkyl, wherein the following are reacted in two steps: a) a boric precursor compound with an acetal compound to give a boronate compound; and b) the boronate compound with an amino alcohol compound. This process avoids by-products and exhibits a very good stereospecificity.Type: GrantFiled: January 25, 2007Date of Patent: September 8, 2009Assignee: Zach SystemInventors: Alain Burgos, Stëphane Frein
-
Publication number: 20090131688Abstract: The invention concerns a novel method for synthesis of 4-benzofuran-carboxylic acid or alkyl ester thereof. This method is characterized in that a reaction for aromatization of a compound of formula (II) is performed for the synthesis of the compound of formula (I), according to the scheme A2 below: wherein R independently represents hydrogen or a linear or branched C1-15 alkyl group. With the invention, it is possible to industrially synthesize 4-benzofuran-carboxylic acid or alkyl ester thereof with good yield and very good purity.Type: ApplicationFiled: February 25, 2008Publication date: May 21, 2009Applicant: ZACH SYSTEMInventors: Alain Burgos, Martine Maruani, Florence Perrin, Stephane Frein
-
Publication number: 20090005429Abstract: The present invention relates to a process for the preparation of carvedilol as well as of the optically active R and S enantiomers thereof and of mixtures of these enantiomers and, more particularly, relates to an improved process for the preparation of carvedilol and its enantiomers characterized by the use of ethyl acetate as reaction solvent.Type: ApplicationFiled: December 5, 2005Publication date: January 1, 2009Applicant: ZACH SYSTEM S.P.A.Inventors: Elisenda Trepat Guixer, Anna Munoz Alvarez, Marta Pomares Marco, Francisco Marquillas Olondriz
-
Publication number: 20090005567Abstract: A process and new oxazolinic intermediates for the preparation of 4-(8-chloro-5,6-dihydro-11H-benzo-[5,6]-clohepta-[1,2-b]-pyridin-11-ylide-ne)-1-piperidinecarboxylic acid ethyl ester (loratadine) is described. The process starts from 2-(4,4-dimethyl-4,5-dihydrooxazol-2-yl)-3-methyl-pyridine, a new intermediate to obtain loratadine. 2-(4,4-dimethyl-4,5-dihydro-oxazol-2-yl)-3-methyl-pyridine is condensed with 3-chloro-benzyl-chloride and the resultant product is treated with Grignard reagent of 4-chloro-N-methyl-piperidine. [3-(2-(3-chloro-phenyl)-ethyl]-pyridin-2-yl-]-1-(methyl-piperidin-4-yl)-methanone is obtained for subsequent hydrolysis. Starting from this last compound it is possible to obtain loratadine with known methods.Type: ApplicationFiled: September 9, 2008Publication date: January 1, 2009Applicant: ZaCH System S.p.A.Inventors: Vincenzo CANNATA, Livius Cotarca, Ivan Michieletto, Stefano Poli
-
Patent number: 7462742Abstract: An in situ or one-pot process for the preparation of the compounds of formula (I) uses a compound of general formula (I): and includes: a) the hydrogenation of a nitrile group of the compound of general formula (II): in which R1 to R4 are especially H or alkyl and n varies from 0 to 4, in the presence of a hydrogenation catalyst, a methylating agent and an organic acid as solvent, and at a temperature Ta below the initiation temperature of a reductive amination reaction, to give a primary amine from the nitrile group; and b) the reductive amination of the primary amine in the presence of hydrogen, at a temperature Tb above Ta, to give the dimethylated amine of general formula (I) by activation of the methylating age.Type: GrantFiled: January 23, 2007Date of Patent: December 9, 2008Assignee: Zach SystemInventors: Alain Burgos, Jacques Tonnel, Valéry Dambrin, Denis Lucet, Patricia Poirier
-
Publication number: 20080300307Abstract: Stable compositions containing gabapentin compositions, methods of preparing such compositions, and methods of using such compositions.Type: ApplicationFiled: August 12, 2008Publication date: December 4, 2008Applicant: ZaCh System S.p.A.Inventors: Vincenzo Cannata, Francesco Corcella, Andrea Nicoli