EP1425287A4 - Procedes permettant de preparer des formes salines calciques de statines - Google Patents

Procedes permettant de preparer des formes salines calciques de statines

Info

Publication number
EP1425287A4
EP1425287A4 EP02759374A EP02759374A EP1425287A4 EP 1425287 A4 EP1425287 A4 EP 1425287A4 EP 02759374 A EP02759374 A EP 02759374A EP 02759374 A EP02759374 A EP 02759374A EP 1425287 A4 EP1425287 A4 EP 1425287A4
Authority
EP
European Patent Office
Prior art keywords
statins
processes
calcium salt
salt forms
preparing calcium
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.)
Withdrawn
Application number
EP02759374A
Other languages
German (de)
English (en)
Other versions
EP1425287A1 (fr
Inventor
Valerie Niddam-Hildesheim
Revital Lifshitz-Liron
Rami Lidor-Hadas
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.)
Teva Pharmaceutical Industries Ltd
Original Assignee
Teva Pharmaceutical Industries Ltd
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 claimed from US10/037,412 external-priority patent/US6528661B2/en
Application filed by Teva Pharmaceutical Industries Ltd filed Critical Teva Pharmaceutical Industries Ltd
Publication of EP1425287A1 publication Critical patent/EP1425287A1/fr
Publication of EP1425287A4 publication Critical patent/EP1425287A4/fr
Withdrawn legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/42—One nitrogen atom
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • 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
    • 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
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
    • C07D207/34—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/18—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D209/24—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with an alkyl or cycloalkyl radical attached to the ring nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/54—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/55—Acids; Esters
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/12—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D215/14—Radicals substituted by oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D309/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
    • C07D309/16—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D309/28—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D309/30—Oxygen atoms, e.g. delta-lactones
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pyrane Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Quinoline Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Pyrrole Compounds (AREA)
  • Indole Compounds (AREA)
EP02759374A 2001-08-16 2002-08-16 Procedes permettant de preparer des formes salines calciques de statines Withdrawn EP1425287A4 (fr)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US31281201P 2001-08-16 2001-08-16
US312812P 2001-08-16
US37412 2001-10-24
US10/037,412 US6528661B2 (en) 2000-11-16 2001-10-24 Hydrolysis of [R(R*,R*)]-2-(4-fluorophenyl)-β,δ-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino) carbonyl]-1H-pyrrole-1-heptanoic acid esters with calcium hydroxide
PCT/US2002/026012 WO2003016317A1 (fr) 2001-08-16 2002-08-16 Procedes permettant de preparer des formes salines calciques de statines

Publications (2)

Publication Number Publication Date
EP1425287A1 EP1425287A1 (fr) 2004-06-09
EP1425287A4 true EP1425287A4 (fr) 2005-09-07

Family

ID=26714105

Family Applications (1)

Application Number Title Priority Date Filing Date
EP02759374A Withdrawn EP1425287A4 (fr) 2001-08-16 2002-08-16 Procedes permettant de preparer des formes salines calciques de statines

Country Status (17)

Country Link
EP (1) EP1425287A4 (fr)
JP (2) JP4188826B2 (fr)
CN (1) CN100430405C (fr)
AU (1) AU2002324715B2 (fr)
CA (1) CA2450820C (fr)
CZ (1) CZ2004337A3 (fr)
HR (1) HRPK20040255B3 (fr)
HU (1) HUP0500616A3 (fr)
IL (2) IL160077A0 (fr)
IS (1) IS7148A (fr)
MX (1) MXPA04001451A (fr)
NO (1) NO20041082L (fr)
NZ (1) NZ529913A (fr)
PL (1) PL370407A1 (fr)
SK (1) SK1402004A3 (fr)
TR (1) TR200302281T2 (fr)
WO (1) WO2003016317A1 (fr)

Families Citing this family (55)

* Cited by examiner, † Cited by third party
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US7411075B1 (en) 2000-11-16 2008-08-12 Teva Pharmaceutical Industries Ltd. Polymorphic form of atorvastatin calcium
AU2002232891B2 (en) * 2000-11-16 2006-12-14 Teva Pharmaceutical Industries Ltd. Hydrolysis of [R(R*,R*)]-2-(4-fluorophenyl)-beta,delta -dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino) carbonyl]-1H-pyrrole-1-heptanoic acid esters with calcium hydroxide
US7501450B2 (en) 2000-11-30 2009-03-10 Teva Pharaceutical Industries Ltd. Crystal forms of atorvastatin hemi-calcium and processes for their preparation as well as novel processes for preparing other forms
IL156055A0 (en) 2000-11-30 2003-12-23 Teva Pharma Novel crystal forms of atorvastatin hemi calcium and processes for their preparation as well as novel processes for preparing other forms
WO2002057229A1 (fr) 2001-01-19 2002-07-25 Biocon India Limited FORME V CRISTALLINE DE SEL HEMICALCIQUE D'ACIDE [R-(R*,R*)]-2-(4-FLUOROPHENYL)-ß,$G(D)-DIHYDROXY-5-(1-METHYLETHYL)-3-PHENYL-4-[(PHENYLAMINO)CARBONYL]-1H-PYRROLE-1-HEPTANOIQUE (ATORVASTATINE)
US7361772B2 (en) 2001-08-16 2008-04-22 Biocon Limited Process for the production of atorvastatin calcium
CA2412012C (fr) 2001-11-20 2011-08-02 Ed. Geistlich Soehne Ag Fuer Chemische Industrie Matrice extracellulaire resorbable contenant du collagene i et du collagene ii pour la reconstruction de cartilage
WO2003078379A1 (fr) 2002-03-18 2003-09-25 Biocon Limited Inhibiteurs de hmg-coa reductase amorphe avec taille souhaitee des particules
AR039836A1 (es) * 2002-05-21 2005-03-02 Ranbaxy Lab Ltd Proceso para la preparacion de un aldehido de pirimidina util para la preparacion de rosuvastatina
US7179942B2 (en) 2002-07-05 2007-02-20 Bicon Limited Halo-substituted active methylene compounds
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PL376557A1 (pl) * 2003-02-12 2006-01-09 Ciba Specialty Chemicals Holding Inc. Postacie krystaliczne pitawastatyny wapnia
EP1631533B1 (fr) 2003-04-22 2009-03-11 Biocon Limited Nouveau procede pour une reduction stereoselective de beta-setoesters
GB0312896D0 (en) 2003-06-05 2003-07-09 Astrazeneca Ab Chemical process
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EP1816126A1 (fr) * 2003-08-28 2007-08-08 Teva Pharmaceutical Industries Limited Procédé pour la préparation de rosuvastatine calcique
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EP1601658A1 (fr) 2003-11-24 2005-12-07 Teva Pharmaceutical Industries Limited Sels d'ammonium cristallins de la rosuvastatine
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EP1689723B1 (fr) 2003-12-02 2011-04-27 Teva Pharmaceutical Industries, Ltd. Norme de reference pour la caracterisation de la rosuvastatine
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WO2010089770A2 (fr) 2009-01-19 2010-08-12 Msn Laboratories Limited Procédé amélioré d'élaboration d'acide (3r,5s)-7-[2-cyclopropyl-4-(4-fluorophényl)quinolin-3-yl]-3,5-dihydroxy-6(e)-heptènoïque de haute pureté, y compris ses sels pharmaceutiquement acceptables
WO2011086584A2 (fr) 2010-01-18 2011-07-21 Msn Laboratories Limited Procédé amélioré pour la préparation d'intermédiaires amides et leur utilisation
HUP1000299A2 (hu) 2010-06-08 2012-02-28 Nanoform Cardiovascular Therapeutics Ltd Nanostrukturált Atorvastatint, gyógyszerészetileg elfogadott sóit és kokristályait tartalmazó készítmény és eljárás elõállításukra
EP3178812A1 (fr) * 2010-11-12 2017-06-14 Hetero Research Foundation Nouveaux polymorphes de calcium de pitavastatine
HU229260B1 (en) * 2010-11-29 2013-10-28 Egis Gyogyszergyar Nyrt Process for preparation of rosuvastatin salts
CN102875504A (zh) * 2011-07-13 2013-01-16 华南理工大学 4,5,6,7-四氢普伐他汀及其盐在心血管上的用途
CN102302452B (zh) * 2011-09-14 2012-11-21 海南美大制药有限公司 匹伐他汀钙脂质体固体制剂
CN102796036B (zh) * 2012-09-12 2014-06-04 江苏阿尔法药业有限公司 一种阿托伐他汀钙的制备方法
CN103724278B (zh) * 2013-12-12 2019-03-29 江苏阿尔法药业有限公司 他汀类中间体及其衍生物的制备方法
EP3103878A4 (fr) * 2014-02-06 2017-08-16 API Corporation Calcium de rosuvastatine et procédé de production d'un intermédiaire de celui-ci
KR20160126700A (ko) 2015-04-24 2016-11-02 미래파인켐 주식회사 스타틴의 중간체, 이의 제조방법 및 이를 이용한 로수바스타틴의 제조방법
CN105111173B (zh) * 2015-06-26 2017-06-23 上海应用技术学院 他汀含氟衍生物及其用途
CN105017231B (zh) * 2015-06-26 2018-01-26 上海应用技术学院 多取代吲哚类他汀含氟修饰物及其用途
EP3333155B1 (fr) 2015-08-05 2023-05-24 API Corporation Procédé de production du sel de calcium de pitavastatine
CN111362856B (zh) * 2020-04-29 2023-08-18 福建海西新药创制股份有限公司 一种利用微反应装置生产阿托伐他汀钙的方法

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CA2450820A1 (fr) 2003-02-27
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SK1402004A3 (sk) 2005-01-03
AU2002324715B2 (en) 2009-03-12
HRPK20040255B3 (en) 2006-02-28
NO20041082L (no) 2004-03-15
CA2450820C (fr) 2011-03-15
IL160077A0 (en) 2004-06-20
PL370407A1 (en) 2005-05-30
IL160077A (en) 2007-10-31
HUP0500616A3 (en) 2011-07-28
EP1425287A1 (fr) 2004-06-09
WO2003016317A1 (fr) 2003-02-27
NZ529913A (en) 2005-03-24
JP2009024008A (ja) 2009-02-05
JP2005500382A (ja) 2005-01-06
HUP0500616A2 (hu) 2005-11-28
TR200302281T2 (tr) 2004-09-21
IS7148A (is) 2004-02-11
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