Patents Assigned to Lundbeck Pharmaceuticals Italy, S.p.A.
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Patent number: 11578043Abstract: The present invention relates to a non-hygroscopic salt of the compound 2-(3-(4-propylheptyl)morpholino)ethan-1-ol having the INN name delmopinol. In particular, the invention relates to the citrate salt of delmopinol. The present invention also relates to pharmaceutical compositions comprising the citrate salt of delmopinol depicted below.Type: GrantFiled: August 23, 2018Date of Patent: February 14, 2023Assignee: Lundbeck Pharmaceuticals Italy S.P.A.Inventors: Carla De Faveri, Mariano Stivanello
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Patent number: 11384056Abstract: The present invention relates to a new process for producing intermediates useful in the manufacture of 2-(3-(4-propylheptyl)morpholino)ethan-1-ol. The invention also relates to intermediates 1-chloro-4-propylhept-3-ene and 1-iodo-4-propyl-hept-3-ene.Type: GrantFiled: December 20, 2017Date of Patent: July 12, 2022Assignee: Lundbeck Pharmaceuticals Italy S.P.A.Inventors: Carla De Faveri, Mariano Stivanello
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Patent number: 10894778Abstract: 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: GrantFiled: December 20, 2017Date of Patent: January 19, 2021Assignee: Lundbeck Pharmaceuticals Italy S.P.A.Inventors: Carla De Faveri, Mariano Stivanello
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Patent number: 10815251Abstract: 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: GrantFiled: February 14, 2020Date of Patent: October 27, 2020Assignee: Lundbeck Pharmaceuticals Italy S.P.A.Inventors: Carla De Faveri, Mariano Stivanello
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Patent number: 10717747Abstract: 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: GrantFiled: December 20, 2017Date of Patent: July 21, 2020Assignee: Lundbeck Pharmaceuticals Italy S.P.A.Inventors: Carla De Faveri, Mariano Stivanello
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Publication number: 20200181167Abstract: 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: ApplicationFiled: February 14, 2020Publication date: June 11, 2020Applicant: Lundbeck Pharmaceuticals Italy S.p.A.Inventors: Carla De Faveri, Mariano Stivanello
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Patent number: 10385020Abstract: 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: GrantFiled: May 11, 2018Date of Patent: August 20, 2019Assignee: LUNDBECK PHARMACEUTICALS ITALY S.P.A.Inventors: Mariano Stivanello, Florian Anton Martin Huber, Antonio Ricci
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Patent number: 10329264Abstract: 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: GrantFiled: July 27, 2016Date of Patent: June 25, 2019Assignee: Lundbeck Pharmaceuticals Italy S.P.A.Inventors: Carla De Faveri, Florian Anton Martin Huber, Nicola Antolini
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Publication number: 20180258041Abstract: 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: ApplicationFiled: May 11, 2018Publication date: September 13, 2018Applicant: LUNDBECK PHARMACEUTICALS ITALY S.p.A.Inventors: Mariano Stivanello, Florian Anton Martin HUBER, Antonio RICCI
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Patent number: 9994526Abstract: 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: GrantFiled: August 12, 2016Date of Patent: June 12, 2018Assignee: LUNDBECK PHARMACEUTICALS ITALY S.p.A.Inventors: Mariano Stivanello, Florian Anton Martin Huber, Antonio Ricci
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Publication number: 20160347711Abstract: 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: ApplicationFiled: August 12, 2016Publication date: December 1, 2016Applicant: LUNDBECK PHARMACEUTICALS ITALY S.p.A.Inventors: Mariano Stivanello, Florian Anton Martin HUBER, Antonio RICCI
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Patent number: 8912360Abstract: Methods for preparing Ritodrine hydrochloride are provided. Also provided is non-hygroscopic, crystalline, polymorphic Ritodrine hydrochloride of Form I.Type: GrantFiled: March 24, 2011Date of Patent: December 16, 2014Assignee: Lundbeck Pharmaceuticals Italy S.p.A.Inventors: Jacopo Zanon, Giovanna Libralon, Carla De Faveri, Florian Anton Martin Huber
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Publication number: 20140088310Abstract: 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: ApplicationFiled: March 26, 2012Publication date: March 27, 2014Applicant: LUNDBECK PHARMACEUTICALS ITALY S.P.A.Inventors: Mariano Stivanello, Florian Anton Martin Huber, Antonio Ricci
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Patent number: 8378106Abstract: 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: GrantFiled: April 6, 2009Date of Patent: February 19, 2013Assignee: Lundbeck Pharmaceuticals Italy S.p.A.Inventors: Jacopo Zanon, Giovanna Libralon, Andrea Nicoleā²
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Patent number: 7531694Abstract: 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: GrantFiled: July 7, 2004Date of Patent: May 12, 2009Assignee: Lundbeck Pharmaceuticals Italy, S.p.A.Inventors: Marco Villa, Carla De Faveri, Riccardo Zanotti, Francesco Ciardella, Fabrizio Borin
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Publication number: 20070225295Abstract: 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: ApplicationFiled: May 10, 2005Publication date: September 27, 2007Applicants: DIPHARMA S.P.A., LUNDBECK PHARMACEUTICALS ITALY S.P.A.Inventors: Gianpiero Ventimiglia, Pietro Allegrini, Graziano Castaldi
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Publication number: 20070117810Abstract: 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: ApplicationFiled: November 13, 2006Publication date: May 24, 2007Applicants: DIPHARMA S. P. A., LUNDBECK PHARMACEUTICALS ITALY S. P. A.Inventors: Jacopo Zanon, Oscar Martini, Francesco Ciardella, Luca Gregori, Federico Sbrogio, Andrea Castellin