ES2251292B1 - Procedimiento para la obtencion de un compuesto farmaceuticamente activo y de sus intermedios de sintesis. - Google Patents

Procedimiento para la obtencion de un compuesto farmaceuticamente activo y de sus intermedios de sintesis. Download PDF

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Publication number
ES2251292B1
ES2251292B1 ES200400949A ES200400949A ES2251292B1 ES 2251292 B1 ES2251292 B1 ES 2251292B1 ES 200400949 A ES200400949 A ES 200400949A ES 200400949 A ES200400949 A ES 200400949A ES 2251292 B1 ES2251292 B1 ES 2251292B1
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ES
Spain
Prior art keywords
formula
compound
group
temperature
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Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Expired - Fee Related
Application number
ES200400949A
Other languages
English (en)
Spanish (es)
Other versions
ES2251292A1 (es
Inventor
Jorge Bessa Bellmunt
Juan Huguet Clotet
Juan Antonio Perez Andres
Pere Dalmases Barjoan
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Inke SA
Original Assignee
Inke SA
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority to ES200400949A priority Critical patent/ES2251292B1/es
Application filed by Inke SA filed Critical Inke SA
Priority to PL05733764T priority patent/PL1747190T3/pl
Priority to US11/568,054 priority patent/US7728021B2/en
Priority to AT05733764T priority patent/ATE401300T1/de
Priority to SI200530408T priority patent/SI1747190T1/sl
Priority to KR1020067024308A priority patent/KR20060135959A/ko
Priority to PT05733764T priority patent/PT1747190E/pt
Priority to PCT/IB2005/001100 priority patent/WO2005102987A1/en
Priority to JP2007509005A priority patent/JP2007533727A/ja
Priority to DE602005008224T priority patent/DE602005008224D1/de
Priority to TW094112179A priority patent/TWI283576B/zh
Priority to ES05733764T priority patent/ES2309741T3/es
Priority to ZA200608986A priority patent/ZA200608986B/en
Priority to EP05733764A priority patent/EP1747190B1/en
Publication of ES2251292A1 publication Critical patent/ES2251292A1/es
Application granted granted Critical
Publication of ES2251292B1 publication Critical patent/ES2251292B1/es
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

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Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D257/00—Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms
    • C07D257/02—Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D257/04—Five-membered rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C227/00—Preparation of compounds containing amino and carboxyl groups bound to the same carbon skeleton
    • C07C227/14—Preparation of compounds containing amino and carboxyl groups bound to the same carbon skeleton from compounds containing already amino and carboxyl groups or derivatives thereof
    • C07C227/18—Preparation of compounds containing amino and carboxyl groups bound to the same carbon skeleton from compounds containing already amino and carboxyl groups or derivatives thereof by reactions involving amino or carboxyl groups, e.g. hydrolysis of esters or amides, by formation of halides, salts or esters
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C229/00—Compounds containing amino and carboxyl groups bound to the same carbon skeleton
    • C07C229/02—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton
    • C07C229/34—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton containing six-membered aromatic rings
    • C07C229/36—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton containing six-membered aromatic rings with at least one amino group and one carboxyl group bound to the same carbon atom of the carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C231/00—Preparation of carboxylic acid amides
    • C07C231/02—Preparation of carboxylic acid amides from carboxylic acids or from esters, anhydrides, or halides thereof by reaction with ammonia or amines
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00—Carboxylic acid amides
    • C07C233/01—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C233/45—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups
    • C07C233/46—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom
    • C07C233/47—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom having the carbon atom of the carboxamide group bound to a hydrogen atom or to a carbon atom of an acyclic saturated carbon skeleton

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Catalysts (AREA)
  • Pyrrole Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Peptides Or Proteins (AREA)
ES200400949A 2004-04-20 2004-04-20 Procedimiento para la obtencion de un compuesto farmaceuticamente activo y de sus intermedios de sintesis. Expired - Fee Related ES2251292B1 (es)

Priority Applications (14)

Application Number Priority Date Filing Date Title
ES200400949A ES2251292B1 (es) 2004-04-20 2004-04-20 Procedimiento para la obtencion de un compuesto farmaceuticamente activo y de sus intermedios de sintesis.
TW094112179A TWI283576B (en) 2004-04-20 2005-04-18 Process for obtaining a pharmaceutically active compound and synthesis intermediates thereof
AT05733764T ATE401300T1 (de) 2004-04-20 2005-04-18 Verfahren zur herstellung von valsartan und vorstufen davon
SI200530408T SI1747190T1 (sl) 2004-04-20 2005-04-18 Postopek za pripravo valsartana in njegovih prekurzorjev
KR1020067024308A KR20060135959A (ko) 2004-04-20 2005-04-18 발사르탄 및 이의 전구체의 제조방법
PT05733764T PT1747190E (pt) 2004-04-20 2005-04-18 Processo para a preparação de valsartan e seus precursores
PCT/IB2005/001100 WO2005102987A1 (en) 2004-04-20 2005-04-18 Process for the preparation of valsartan and precursors thereof
JP2007509005A JP2007533727A (ja) 2004-04-20 2005-04-18 バルサルタンおよびその前駆体の製造方法
PL05733764T PL1747190T3 (pl) 2004-04-20 2005-04-18 Sposób wytwarzania walsartanu oraz jego prekursorów
US11/568,054 US7728021B2 (en) 2004-04-20 2005-04-18 Process for the preparation of Valsartan and precursors thereof
ES05733764T ES2309741T3 (es) 2004-04-20 2005-04-18 Proceso de preparacion de valsartan y de precursores de sintesi de dicho componente.
ZA200608986A ZA200608986B (en) 2004-04-20 2005-04-18 Process for the preparation of Valsartan and precursors thereof
EP05733764A EP1747190B1 (en) 2004-04-20 2005-04-18 Process for the preparation of valsartan and precursors thereof
DE602005008224T DE602005008224D1 (de) 2004-04-20 2005-04-18 Verfahren zur herstellung von valsartan und vorstufen davon

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
ES200400949A ES2251292B1 (es) 2004-04-20 2004-04-20 Procedimiento para la obtencion de un compuesto farmaceuticamente activo y de sus intermedios de sintesis.

Publications (2)

Publication Number Publication Date
ES2251292A1 ES2251292A1 (es) 2006-04-16
ES2251292B1 true ES2251292B1 (es) 2007-07-01

Family

ID=34966329

Family Applications (2)

Application Number Title Priority Date Filing Date
ES200400949A Expired - Fee Related ES2251292B1 (es) 2004-04-20 2004-04-20 Procedimiento para la obtencion de un compuesto farmaceuticamente activo y de sus intermedios de sintesis.
ES05733764T Expired - Lifetime ES2309741T3 (es) 2004-04-20 2005-04-18 Proceso de preparacion de valsartan y de precursores de sintesi de dicho componente.

Family Applications After (1)

Application Number Title Priority Date Filing Date
ES05733764T Expired - Lifetime ES2309741T3 (es) 2004-04-20 2005-04-18 Proceso de preparacion de valsartan y de precursores de sintesi de dicho componente.

Country Status (13)

Country Link
US (1) US7728021B2 (https=)
EP (1) EP1747190B1 (https=)
JP (1) JP2007533727A (https=)
KR (1) KR20060135959A (https=)
AT (1) ATE401300T1 (https=)
DE (1) DE602005008224D1 (https=)
ES (2) ES2251292B1 (https=)
PL (1) PL1747190T3 (https=)
PT (1) PT1747190E (https=)
SI (1) SI1747190T1 (https=)
TW (1) TWI283576B (https=)
WO (1) WO2005102987A1 (https=)
ZA (1) ZA200608986B (https=)

Families Citing this family (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7378531B2 (en) 2003-04-21 2008-05-27 Teva Pharmaceutical Industries Ltd Process for the preparation of valsartan
WO2006067216A2 (en) * 2004-12-22 2006-06-29 Enantia, S. L. Intermediate compounds for the preparation of an angiotensin ii receptor and process for the preparation of valsartan
ES2259909B1 (es) * 2005-02-28 2007-06-16 Inke, S.A. Procedimiento para la obtencion de un compuesto farmaceuticamente activo y de su intermedio de sintesis.
WO2007005967A2 (en) * 2005-07-05 2007-01-11 Teva Pharmaceutical Industries Ltd. Process for preparing valsartan
ITMI20051989A1 (it) * 2005-10-20 2007-04-21 Dipharma Spa Procedimerntyo per la preparazione di composti antagonisti di angiotensina ii
ES2288376B1 (es) * 2005-10-20 2008-11-01 Inke, S.A. Procedimiento para la obtencion de intermedios utiles en la obtencion de un compuesto farmaceuticamente activo.
WO2007071750A1 (en) * 2005-12-22 2007-06-28 Enantia, S.L. Intermediates and processes for the preparation of valsartan
ES2300175B1 (es) * 2006-02-14 2009-06-08 Inke, S.A. Procedimiento para la obtencion de intermedios utiles en la obtencion de un compuesto farmaceuticamente activo.
WO2008007391A2 (en) * 2006-07-10 2008-01-17 Manne Satyanarayana Reddy An improved process for the preparation of valsartan
DE602007000211D1 (de) * 2007-06-07 2008-12-11 Inke Sa Verfahren zur Gewinnung eines zur Gewinnung von Valsartan nützlichen Valsartan-Salzes
US8492577B2 (en) 2008-04-07 2013-07-23 Hetero Research Foundation Process for preparation of valsartan intermediate
KR101012135B1 (ko) * 2008-12-18 2011-02-07 주식회사 대희화학 발사르탄 메틸 에스테르의 제조방법
CN102702118B (zh) * 2012-06-11 2014-04-16 吉林三善恩科技开发有限公司 一种缬沙坦有机药物共晶及其制备方法
CN103804313B (zh) * 2014-01-27 2015-12-09 云南现代民族药工程技术研究中心 一种简洁的低成本高效率制备缬沙坦的方法
US9675585B1 (en) 2016-03-24 2017-06-13 Ezra Pharma Extended release pharmaceutical formulations
US9687475B1 (en) 2016-03-24 2017-06-27 Ezra Pharma Llc Extended release pharmaceutical formulations with controlled impurity levels

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE4313747A1 (de) * 1993-04-27 1994-11-03 Bayer Ag Verfahren zur Herstellung von substituierten Biphenyltetrazolen
WO2003020721A1 (en) * 2001-08-30 2003-03-13 Novartis Ag Pyrrolo pyrimidines as agents for the inhibition of cystein proteases

Family Cites Families (8)

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IL97219A (en) * 1990-02-19 1995-12-08 Ciba Geigy Ag Biphenyl substituted aliphatic amino compounds process for their preparation and pharmaceutical compositions containing them
DE4319041A1 (de) * 1992-10-23 1994-04-28 Bayer Ag Trisubstituierte Biphenyle
DE4319040A1 (de) 1992-10-23 1994-04-28 Bayer Ag Alkoxymethylsubstituierte Pyridonbiphenyle
DE4320432A1 (de) * 1993-06-21 1994-12-22 Bayer Ag Substituierte Mono- und Bipyridylmethylderivate
DE4407488A1 (de) 1994-03-07 1995-09-14 Bayer Ag Verwendung von Biphenyl- und Pyridylmethylpyridonen
US5965738A (en) 1994-09-20 1999-10-12 Wakunaga Seiyaku Kabushiki Kaisha Process for producing N-biphenylmethylthiadiazoline derivative or salt thereof and intermediate for producing the same
US6207665B1 (en) * 1997-06-12 2001-03-27 Schering Aktiengesellschaft Piperazine derivatives and their use as anti-inflammatory agents
DE60201415T2 (de) * 2001-01-19 2006-02-09 Pharmacopeia, Inc. Bisarylderivate mit fsh rezeptor modulierender aktivität

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE4313747A1 (de) * 1993-04-27 1994-11-03 Bayer Ag Verfahren zur Herstellung von substituierten Biphenyltetrazolen
WO2003020721A1 (en) * 2001-08-30 2003-03-13 Novartis Ag Pyrrolo pyrimidines as agents for the inhibition of cystein proteases

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
MOENIUS, T. et al. "Carbon-14 Labelling of DIOVAN in its Valine-Moiety". Journal of Labelled Compounds and Radiopharmaceuticals, 2000, Volumen 43, páginas 1245-1252. Ver especialmente esquema 6. *
ÖHBERG, L. & WESTMAN. J. "One-pot Three-step Solution Phase Syntheses of Thiohydantoins using Microwave Heating". Synlett, 2001, Número 12, páginas 1893-1896. Tabla 2, compuesto 7. *

Also Published As

Publication number Publication date
TWI283576B (en) 2007-07-11
WO2005102987A1 (en) 2005-11-03
SI1747190T1 (sl) 2008-12-31
ES2251292A1 (es) 2006-04-16
ATE401300T1 (de) 2008-08-15
PL1747190T3 (pl) 2009-01-30
TW200539873A (en) 2005-12-16
JP2007533727A (ja) 2007-11-22
PT1747190E (pt) 2008-09-29
ES2309741T3 (es) 2008-12-16
EP1747190B1 (en) 2008-07-16
US20090221836A1 (en) 2009-09-03
DE602005008224D1 (de) 2008-08-28
ZA200608986B (en) 2008-02-27
KR20060135959A (ko) 2006-12-29
EP1747190A1 (en) 2007-01-31
US7728021B2 (en) 2010-06-01

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