Patents Assigned to Lundbeck Pharmaceuticals Italy, S.p.A.
  • Patent number: 10894778
    Abstract: The present invention relates to a new process for producing 2-(3-(4-propylheptyl)morpholino)ethan-1-ol with the INN name Delmopinol. The invention also relates to three key intermediates 1-chloro-4-propylhept-3-ene, 1-iodo-4-propylhept-3-ene and 2-(3-(4-propylhept-3-en-1-yl)morpholino)ethan-1-ol.
    Type: Grant
    Filed: December 20, 2017
    Date of Patent: January 19, 2021
    Assignee: Lundbeck Pharmaceuticals Italy S.P.A.
    Inventors: Carla De Faveri, Mariano Stivanello
  • Patent number: 10815251
    Abstract: The present invention relates to a method for the manufacture of 2-(3-(alkyl or alkenyl)morpholino)-ethan-1-ols by reduction of 8a-(alkyl or alkenyl)hexahydrooxazolo[2,3-c][1,4]oxazines encompassing a process for producing 2-(3-(4-propylheptyl)morpholino)ethan-1-ol with the INN name delmopinol. The invention also relates to 1-chloro-4-propylhept-3-ene, 1-iodo-4-propylhept-3-ene, 8a-(4-propylheptyl)hexahydrooxazolo[2,3-c][1,4]oxazine, 8a-(4-propylhept-3-en-1-yl)hexahydrooxazolo[2,3-c][1,4]oxazine and 2-(3-(4-propylhept-3-en-1-yl)morpholino)ethan-1-ol which are intermediates in the delmopinol process.
    Type: Grant
    Filed: February 14, 2020
    Date of Patent: October 27, 2020
    Assignee: Lundbeck Pharmaceuticals Italy S.P.A.
    Inventors: Carla De Faveri, Mariano Stivanello
  • Patent number: 10717747
    Abstract: The present invention relates to a method for the manufacture of 2-(3-(alkyl or alkenyl)morpholino)-ethan-1-ols by reduction of 8a-(alkyl and alkenyl)hexahydrooxazolo[2,3-c][1,4]oxazines encompassing a process for producing 2-(3-(4-propylheptyl)morpholino)ethan-1-ol with the INN name delmopinol. The invention also relates to 1-chloro-4-propylhept-3-ene, 1-iodo-4-propylhept-3-ene, 8a-(4-5 propylheptyl)hexahydrooxazolo[2,3-c][1,4]oxazine, 8a-(4-propylhept-3-en-1-yl)hexahydrooxazolo[2,3-c][1,4]oxazine and 2-(3-(4-propylhept-3-en-1-yl)morpholino)ethan-1-ol which are intermediates in the delmopinol process.
    Type: Grant
    Filed: December 20, 2017
    Date of Patent: July 21, 2020
    Assignee: Lundbeck Pharmaceuticals Italy S.P.A.
    Inventors: Carla De Faveri, Mariano Stivanello
  • Publication number: 20200181167
    Abstract: The present invention relates to a method for the manufacture of 2-(3-(alkyl or alkenyl)morpholino)-ethan-1-ols by reduction of 8a-(alkyl and alkenyl)hexahydrooxazolo[2,3-c][1,4]oxazines encompassing a process for producing 2-(3-(4-propylheptyllmorpholino)ethan-1-ol with the INN name delmopinol. The invention also relates to 1-chloro-4-propylhept-3-ene, 1-iodo-4-propylhept-3-ene, 8a-(4-5 propylheptyl)hexahydrooxazolo[2,3-c] [1,4]oxazine, 8a-(4-propylhept-3-en-1-yl)hexahydrooxazo-lo[2,3-c][1,4]oxazine and 2-(3-(4-propylhept-3-en-1-yl)morpholino)ethan-1-ol which are intermediates in the delmopinol process.
    Type: Application
    Filed: February 14, 2020
    Publication date: June 11, 2020
    Applicant: Lundbeck Pharmaceuticals Italy S.p.A.
    Inventors: Carla De Faveri, Mariano Stivanello
  • Patent number: 10385020
    Abstract: Methods are provided for the synthesis of key intermediates for the synthesis of Argatroban monohydrate, ethyl (2R,4R)-1-[(2S)-2-amino-5-[[imino(nitroamino)methyl]amino]-1-oxopentyl]-4-methylpiperidine-2-carboxylate compounded with HCl. Such intermediates are also provided.
    Type: Grant
    Filed: May 11, 2018
    Date of Patent: August 20, 2019
    Assignee: LUNDBECK PHARMACEUTICALS ITALY S.P.A.
    Inventors: Mariano Stivanello, Florian Anton Martin Huber, Antonio Ricci
  • Patent number: 10329264
    Abstract: This invention relates to a novel chemical process for the synthesis of N?-benzyl-5-methylisoxazole-3-carbohydrazide (Isocarboxazid) which comprises reacting 5-methyl-3-isoxazole carboxylic acid ester with benzylhydrazine or a salt thereof in an aprotic organic solvent and in the presence of an organic base.
    Type: Grant
    Filed: July 27, 2016
    Date of Patent: June 25, 2019
    Assignee: Lundbeck Pharmaceuticals Italy S.P.A.
    Inventors: Carla De Faveri, Florian Anton Martin Huber, Nicola Antolini
  • Publication number: 20180258041
    Abstract: Methods are provided for the synthesis of key intermediates for the synthesis of Argatroban monohydrate, ethyl (2R,4R)-1-[(2S)-2-amino-5-[[imino(nitroamino)methyl]amino]-1-oxopentyl]-4-methylpiperidine-2-carboxylate compounded with HCl. Such intermediates are also provided.
    Type: Application
    Filed: May 11, 2018
    Publication date: September 13, 2018
    Applicant: LUNDBECK PHARMACEUTICALS ITALY S.p.A.
    Inventors: Mariano Stivanello, Florian Anton Martin HUBER, Antonio RICCI
  • Patent number: 9994526
    Abstract: Methods are provided for the synthesis of key intermediates for the synthesis of Argatroban monohydrate, ethyl (2R,4R)-1-[(2S)-2-amino-5-[[imino(nitroamino)methyl]amino]-1-oxopentyl]-4-methylpiperidine-2-carboxylate compounded with HCl. Such intermediates are also provided.
    Type: Grant
    Filed: August 12, 2016
    Date of Patent: June 12, 2018
    Assignee: LUNDBECK PHARMACEUTICALS ITALY S.p.A.
    Inventors: Mariano Stivanello, Florian Anton Martin Huber, Antonio Ricci
  • Publication number: 20160347711
    Abstract: Methods are provided for the synthesis of key intermediates for the synthesis of Argatroban monohydrate, ethyl (2R,4R)-1-[(2S)-2-amino-5-[[imino(nitroamino)methyl]amino]-1-oxopentyl]-4-methylpiperidine-2-carboxylate compounded with HCl. Such intermediates are also provided.
    Type: Application
    Filed: August 12, 2016
    Publication date: December 1, 2016
    Applicant: LUNDBECK PHARMACEUTICALS ITALY S.p.A.
    Inventors: Mariano Stivanello, Florian Anton Martin HUBER, Antonio RICCI
  • Patent number: 8912360
    Abstract: Methods for preparing Ritodrine hydrochloride are provided. Also provided is non-hygroscopic, crystalline, polymorphic Ritodrine hydrochloride of Form I.
    Type: Grant
    Filed: March 24, 2011
    Date of Patent: December 16, 2014
    Assignee: Lundbeck Pharmaceuticals Italy S.p.A.
    Inventors: Jacopo Zanon, Giovanna Libralon, Carla De Faveri, Florian Anton Martin Huber
  • Publication number: 20140088310
    Abstract: Methods are provided for the synthesis of key intermediates for the synthesis of Argatroban monohydrate, ethyl (2R,4R)-1-[(2S)-2-amino-5-[[imino(nitroamino)methyl]amino]-1-oxopentyl]-4-methylpiperidine-2-carboxylate compounded with HCl. Such intermediates are also provided.
    Type: Application
    Filed: March 26, 2012
    Publication date: March 27, 2014
    Applicant: LUNDBECK PHARMACEUTICALS ITALY S.P.A.
    Inventors: Mariano Stivanello, Florian Anton Martin Huber, Antonio Ricci
  • Patent number: 8378106
    Abstract: A method is described for preparing argatroban monohydrate obtained from (2R,4R)-1-[NG-nitro-N2-(3-methyl-8-quinolinesulphonyl)-L-arginyl]-4-methyl-2-piperidine carboxylic acid by suitably treating crude argatroban. The method either comprises preparation of argatroban monohydrate in a continuous step or an intermediate step of isolating a purified argatroban. Also obtainable from argatroban monohydrate is anhydrous argatroban, shown to have new physico-chemical characteristics. The described argatroban synthesis and purification process hence enables three different forms of argatroban, not previously described, to be obtained, each with distinctive physico-chemical characteristics and in particular enables argatroban monohydrate to be obtained with high yield and with high purity, being therefore a product suitable for use as active principle in proprietary medicines.
    Type: Grant
    Filed: April 6, 2009
    Date of Patent: February 19, 2013
    Assignee: Lundbeck Pharmaceuticals Italy S.p.A.
    Inventors: Jacopo Zanon, Giovanna Libralon, Andrea Nicoleā€²
  • Patent number: 7531694
    Abstract: A new process for the preparation and purification of 4-4?-diamino-diphenyl-sulfone (dapsone) is described. The process described is a three step process comprising a condensation reaction with the synthesis of a thioether intermediate and then steps of oxidation and reduction in suitable conditions in order to obtain a product with good yield and purity.
    Type: Grant
    Filed: July 7, 2004
    Date of Patent: May 12, 2009
    Assignee: Lundbeck Pharmaceuticals Italy, S.p.A.
    Inventors: Marco Villa, Carla De Faveri, Riccardo Zanotti, Francesco Ciardella, Fabrizio Borin
  • Publication number: 20070225295
    Abstract: New crystalline form of ziprasidone hydrochloride hemihydrate, process for its preparation, its use for the purification of ziprasidone, its pharmaceutical compositions and their use in therapy.
    Type: Application
    Filed: May 10, 2005
    Publication date: September 27, 2007
    Applicants: DIPHARMA S.P.A., LUNDBECK PHARMACEUTICALS ITALY S.P.A.
    Inventors: Gianpiero Ventimiglia, Pietro Allegrini, Graziano Castaldi
  • Publication number: 20070117810
    Abstract: A process for the preparation of ziprasidone and a novel intermediate useful in its preparation. The process comprises the reduction of a compound (III) to give a compound (V) which is then reduced to compound (II). This is reacted with compound (IV) to give the desired compound.
    Type: Application
    Filed: November 13, 2006
    Publication date: May 24, 2007
    Applicants: DIPHARMA S. P. A., LUNDBECK PHARMACEUTICALS ITALY S. P. A.
    Inventors: Jacopo Zanon, Oscar Martini, Francesco Ciardella, Luca Gregori, Federico Sbrogio, Andrea Castellin