Patents Assigned to Esteve Química, S.A.
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Patent number: 10221134Abstract: The present invention provides a scalable synthesis of enantiomerically pure brivaracetam, and related derivatives.Type: GrantFiled: May 24, 2016Date of Patent: March 5, 2019Assignee: Esteve Quimica S.A.Inventors: Peng Wang, Pixu Li, Qiang Wei, Yuanhua Liu
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Patent number: 9073899Abstract: It relates to solid forms of dabigatran etexilate mesylate, in particular dabigatran etexilate mesylate in crystalline Form A, and in amorphous form; to processes for their preparation, and to pharmaceutical compositions comprising them. It also relates to a crystalline form of dabigatran etexilate base (Form A), and to a process for its preparation.Type: GrantFiled: February 21, 2013Date of Patent: July 7, 2015Assignee: ESTEVE QUÍMICA, S.A.Inventors: Martí Bartra Sanmartí, Rosa Maria Espinosa Ferrer, Maria del Pilar Lupon Roses, Stephen Benedict David Winter, Silvia Donnici Garcia
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Patent number: 9056864Abstract: Crystalline form of abacavir that is essentially free of solvent of formula (I), in particular crystalline Form I, and its preparation process which comprises the following steps: a) crystallizing abacavir from a solution of said compound in a (C1-C4)-alcohol, dichloromethane, acetonitrile/water, or mixtures thereof; b) isolating the crystalline form of abacavir that appears in the prior step; and c) removing the solvent from the crystalline form of abacavir thus obtained. Crystalline Form I can also be obtained by dispersion of abacavir in acetonitrile. The crystalline form of abacavir that is essentially free of solvent is useful for the preparation of pharmaceutical compositions for use in the treatment and/or prophylaxis of HIV infections.Type: GrantFiled: January 21, 2009Date of Patent: June 16, 2015Assignee: ESTEVE QUIMICA, S.A.Inventors: Marti Bartra Sanmartí, Ramón Berenguer Maimó, Jordi Benet-Buchholz, Lluis Solà I Carandell
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Patent number: 9035070Abstract: The invention relates to a process for preparing 1-aryl-pyrazol-3-one intermediates, tautomers, and salts thereof, to novel intermediates, and to the use of the intermediates in the preparation of sigma receptor inhibitors.Type: GrantFiled: July 28, 2011Date of Patent: May 19, 2015Assignee: ESTEVE QUÍMICA, S.A.Inventors: Martí Bartra Sanmarti, Ramon Berenguer Maimo, Jorge Medrano Ruperez, Jorge Garcia Gomez, Javier Ariza Piquer
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Patent number: 8981105Abstract: A process of preparation of a compound of formula (I), or a pharmaceutically acceptable salt thereof, wherein R1 and R2 represent H; or either R1 represents ethyl and R2 represents n-hexyloxycarbonyl that applies to industrial scale, novel intermediates useful for the preparation thereof, and processes of preparing said intermediates.Type: GrantFiled: July 8, 2011Date of Patent: March 17, 2015Assignee: Esteve Quimica, S.A.Inventors: Antoni Segade Rodríguez, Mireia Pastó Aguilá
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Patent number: 8680284Abstract: A preparation process of esomeprazole sodium substantially free of sulfone impurity including the steps of: a) combining either esomeprazole with a (C3-C8)-ketone or a mixture thereof, a sodium alkoxide, and a (C1-C5)-alcohol, or esomeprazole sodium with a (C3-C8)-ketone or a mixture thereof and a (C1-C5)-alcohol; and b) recovering the esomeprazole sodium formed from the reaction media by filtration.Type: GrantFiled: February 11, 2011Date of Patent: March 25, 2014Assignee: Esteve Quimica, S.A.Inventors: Marti Bartra Sanmartí, Ramón Berenguer Maimó, Joan Gabriel Solsona Rocabert
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Publication number: 20130296558Abstract: It comprises a preparation process of entecavir comprising: submitting a (1S,3R)-3-(tert-butyldimethylsilyloxy)-1-(oxiran-2-yl)pent-4-yn-1-ol (VIII) to a double esterification and to a radicalary cyclization, yielding a compound of formula (V), where either a compound of formula (VIII) is submitted to a first esterification reaction, then to a catalytic radicalary cyclization using titanocene dichloride as catalyst in the presence of Mn/2,4,6-collidine HCl or Zn/2,4,6-collidine/trimethylsilyl chloride, and finally to a second esterification reaction or, alternatively, the compound of formula (VIII) is submitted first to a catalytic radicalary cyclization, and then to an esterification reaction. Entecavir can be obtained by submitting compound (V) to a desilylation reaction to remove the TBS group and then to a Mitsunobu coupling with 2-amino-6-chloroguanine, followed by hydrolysis. It also relates to some new intermediates of the process.Type: ApplicationFiled: December 22, 2011Publication date: November 7, 2013Applicant: ESTEVE QUÍMICA, S.A.Inventors: Martí Bartra Sanmartí, Ramón Berenguer Maimó, Javier Velasco Turbau, Javier Ariza Piquer, Jaime Farrás Soler, Jorge García Gómez
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Publication number: 20130184472Abstract: The invention relates to a process for preparing 1-aryl-pyrazol-3-one intermediates, tautomers, and salts thereof, to novel intermediates, and to the use of the intermediates in the preparation of sigma receptor inhibitors.Type: ApplicationFiled: July 28, 2011Publication date: July 18, 2013Applicant: ESTEVE QUIMICA, S.A.Inventors: Martí Bartra Sanmartí, Ramon Berenguer Maimo, Jorge Medrano Ruperez, Jorge Garcia Gomez, Javier Ariza Piquer
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Publication number: 20130116441Abstract: Process for the preparation of a compound of formula (I), or a pharmaceutically acceptable salt thereof, wherein R1 and R2 represent H; or either R1 represents ethyl and R2 represents n-hexyloxycarbonyl that applies to industrial scale, novel intermediates useful for the preparation thereof, and processes of preparing said intermediates.Type: ApplicationFiled: July 8, 2011Publication date: May 9, 2013Applicant: ESTEVE QUIMICA, S.A.Inventors: Antoni Segade Rodríguez, Mireia Pastó Aguilà
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Publication number: 20120309976Abstract: A preparation process of esomeprazole sodium substantially free of sulfone impurity including the steps of: a) combining either esomeprazole with a (C3-C8)-ketone or a mixture thereof, a sodium alkoxide, and a (C1-C5)-alcohol, or esomeprazole sodium with a (C3-C8)-ketone or a mixture thereof and a (C1-C5)-alcohol; and b) recovering the esomeprazole sodium formed from the reaction media by filtration.Type: ApplicationFiled: February 11, 2011Publication date: December 6, 2012Applicant: ESTEVE QUÍMICA, S.A.Inventors: Marti Bartra Sanmartí, Ramón Berenguer Maimó, Joan Gabriel Solsona Rocabert
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Patent number: 8188285Abstract: It comprises a process for the purification of Montelukast, or its salts or its solvates, including any stereoisomer or mixture thereof, which comprises converting Montelukast acid or a solvate thereof, including any stereoisomer or mixtures thereof, into an amine salt selected from the group consisting of tris-(hydroxymethyl)aminomethane, L-(+)-treo-2-amino-1-phenyl-1,3-propanediol, and L-(+)-?-phenylglycinol salt, in the presence of an appropriate solvent. It also comprises novel salts of Montelukast, in particular, tris-(hydroxymethyl)aminomethane, L-(+)-treo-2-amino-1-phenyl-1,3-propanediol, and L-(+)-?-phenylglycinol salts.Type: GrantFiled: August 7, 2007Date of Patent: May 29, 2012Assignee: Esteve Quimica, S.A.Inventors: Yolanda Gasanz Guillén, Pedro Talavera Escasany, Montserrat Monsalvatje Llagostera
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Patent number: 8097723Abstract: Process for the preparation of abacavir, or its salts or its solvates comprising the step of reacting a compound (IV) where R1 is a (C1-C4)-alkyl radical with anhydrous hydrochloric acid/(C1-C6)-alcohol, and then with tri(C1-C4)-alkyl orthoformate, in the absence of water. The preparation process may include further steps of reacting the compound obtained with cyclopropylamine and subsequently hydrolysis to yield abacavir.Type: GrantFiled: December 20, 2007Date of Patent: January 17, 2012Assignee: Esteve Quimica, S.A.Inventors: Jorge Medrano Rupérez, Julio Campon Pardo, Laia Elías Rius, Ramón Berenguer Maimó
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Patent number: 7968712Abstract: The present invention refers to a process for the resolution into one of its enantiomers of the racemate of compound of formula (I): which comprises separating said one of its enantiomers from a diastereoisomeric salt of formula (II), which is formed by reaction of the racemic mixture with an optically active acetylated amino acid of formula (III). The invention also refers to new intermediates which are useful to carry out the process of the invention.Type: GrantFiled: July 2, 2010Date of Patent: June 28, 2011Assignee: Esteve Quimica, S.A.Inventors: David Fernández Bleda, Jordi Lluis Tous
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Patent number: 7902370Abstract: New solid forms of the active ingredient magnesium salt of S-omeprazole, obtainable by a preparation process including: a) crystallizing a magnesium salt of S-omeprazole from a solution of a magnesium salt of S-omeprazole in a solvent system that includes a mixture of methanol/water with an amount of water equal to or greater than about 0.01 ml/g of the magnesium salt of S-omeprazole starting material; b) isolating the magnesium salt of S-omeprazole that appears in the prior operation; c) separating the free organic solvent from the magnesium salt of S-omeprazole obtained or, alternatively, separating both the free solvent and the solvation solvent. The new solid forms are obtained by a reproducible and robust process, with high yield and elevated optical purity, which is useful for the preparation of pharmaceutical products that contain said active ingredient.Type: GrantFiled: June 29, 2005Date of Patent: March 8, 2011Assignee: Esteve Quimica, S.A.Inventors: Ramón Berenguer Maimó, Laura Coppi, Yolanda Gasanz Guillén, Jorge Medrano Rupérez
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Publication number: 20100298354Abstract: Crystalline form of abacavir that is essentially free of solvent of formula (I), in particular crystalline Form I, and its preparation process which comprises the following steps: a) crystallizing abacavir from a solution of said compound in a (C1-C4)-alcohol, dichloromethane, acetonitrile/water, or mixtures thereof; b) isolating the crystalline form of abacavir that appears in the prior step; and c) removing the solvent from the crystalline form of abacavir thus obtained. Crystalline Form I can also be obtained by dispersion of abacavir in acetonitrile. The crystalline form of abacavir that is essentially free of solvent is useful for the preparation of pharmaceutical compositions for use in the treatment and/or prophylaxis of HIV infections.Type: ApplicationFiled: January 21, 2009Publication date: November 25, 2010Applicant: ESTEVE QUIMICA, S.A.Inventors: Marti Bartra Sanmarti, Ramón Berenguer Maimó, Jordi Benet-Buchholz, Luis Sola I Carandell
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Publication number: 20100274018Abstract: The present invention refers to a process for the resolution into one of its enantiomers of the racemate of compound of formula (I): which comprises separating said one of its enantiomers from a diastereoisomeric salt of formula (II), which is formed by reaction of the racemic mixture with an optically active acetylated amino acid of formula (III). The invention also refers to new intermediates which are useful to carry out the process of the invention.Type: ApplicationFiled: July 2, 2010Publication date: October 28, 2010Applicant: ESTEVE QUIMICA, S.A.Inventors: David Fernández Bleda, Jordi Lluis Tous
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Patent number: 7777044Abstract: Process for the preparation of optically active derivatives of 2-(2-piridylmethylsulfinyl)-benzimidazole, or salts thereof, by resolution of the corresponding racemic derivatives of 2-(2-piridylmethylsulfinyl)-benzimidazole. The resolution is performed through the formation of inclusion complexes with (S)-(?) or (R)-(+)-[1,1?-Binaphthalene]-2,2?-diol in the presence of an amine, followed by the break of the inclusion complex by treatment with an hydroxide of an alkaline metal. The enantiomer of the derivative of 2-(2-piridylmethylsulfinyl)-benzimidazole may be obtained by extractions at a particular pH with a suitable organic solvent. The process allows to perform the resolution with high yields and high optical purity, without using neither toxic solvents nor chromatography.Type: GrantFiled: February 22, 2006Date of Patent: August 17, 2010Assignee: Esteve Quimica, S.A.Inventors: Laura Coppi, Ramón Berenguer Maimó, Yolanda Gasanz Guillén, Jorge Medrano Rupérez
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Patent number: 7772396Abstract: The present invention refers to a process for the resolution into one of its enantiomers of the racemate of compound of formula (I): which comprises separating said one of its enantiomers from a diastereoisomeric salt of formula (II), which is formed by reaction of the racemic mixture with an optically active acetylated amino acid of formula (III). The invention also refers to new intermediates which are useful to carry out the process of the invention.Type: GrantFiled: October 3, 2007Date of Patent: August 10, 2010Assignee: Esteve Quimica, S.A. Avda. Mare de deu de MonsterratInventors: David Fernández Bleda, Jordi Lluis Tous
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Patent number: 7671208Abstract: An acetone solvate of phthaloyl amlodipine, as well as a process for its preparation including dissolving phthaloyl amlodipine in acetone and cooling the mixture. The present invention also comprises a method for the synthesis of amlodipine, its salts or solvates, which comprises the use of an acetone solvate of phthaloyl amlodipine.Type: GrantFiled: May 31, 2007Date of Patent: March 2, 2010Assignee: Esteve Quimica, S.A.Inventors: Ramón Berenguer Maimó, Jorge Medrano Rupérez, Juan Francisco Merodio Cabanillas
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Publication number: 20100041883Abstract: Process for the preparation of abacavir, or its salts or its solvates comprising the step of reacting a compound (IV) where R1 is a (C1-C4)-alkyl radical with anhydrous hydrochloric acid/(C1-C6)-alcohol, and then with tri(C1-C4)-alkyl orthoformate, in the absence of water. The preparation process may include further steps of reacting the compound obtained with cyclopropylamine and subsequently hydrolysis to yield abacavir.Type: ApplicationFiled: December 20, 2007Publication date: February 18, 2010Applicant: ESTEVE QUÍMICA, S.A.Inventors: Jorge Medrano Rupérez, Julio Campon Pardo, Laia Elías Rius, Ramón Berenguer Maimó