EA200400789A1 - КРИСТАЛЛИЧЕСКАЯ КАЛЬЦИЕВАЯ СОЛЬ [R-(R*,R*)]-2-(4-ФТОРФЕНИЛ)-β,δ-ДИГИДРОКСИ-5-(1-МЕТИЛЭТИЛ)-3-ФЕНИЛ-4-[(ФЕНИЛАМИНО)КАРБОНИЛ]-1H-ПИРРОЛГЕПТАНОВОЙ КИСЛОТЫ (2:1) - Google Patents

КРИСТАЛЛИЧЕСКАЯ КАЛЬЦИЕВАЯ СОЛЬ [R-(R*,R*)]-2-(4-ФТОРФЕНИЛ)-β,δ-ДИГИДРОКСИ-5-(1-МЕТИЛЭТИЛ)-3-ФЕНИЛ-4-[(ФЕНИЛАМИНО)КАРБОНИЛ]-1H-ПИРРОЛГЕПТАНОВОЙ КИСЛОТЫ (2:1)

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Publication number
EA200400789A1
EA200400789A1 EA200400789A EA200400789A EA200400789A1 EA 200400789 A1 EA200400789 A1 EA 200400789A1 EA 200400789 A EA200400789 A EA 200400789A EA 200400789 A EA200400789 A EA 200400789A EA 200400789 A1 EA200400789 A1 EA 200400789A1
Authority
EA
Eurasian Patent Office
Prior art keywords
phenyl
pyrrohleptanic
dihydroxi
phenylamino
methylethyl
Prior art date
Application number
EA200400789A
Other languages
English (en)
Other versions
EA008441B1 (ru
Inventor
Иржи Фаустманн
Александр Ергов
Original Assignee
Ивакс Фармасьютикалз С. Р. О.
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
Application filed by Ивакс Фармасьютикалз С. Р. О. filed Critical Ивакс Фармасьютикалз С. Р. О.
Publication of EA200400789A1 publication Critical patent/EA200400789A1/ru
Publication of EA008441B1 publication Critical patent/EA008441B1/ru

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Classifications

    • 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
    • C07D207/32—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 only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D207/325—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 only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms with substituted hydrocarbon radicals directly attached to the ring nitrogen atom
    • C07D207/327—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
    • 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
    • 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
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • C07D207/32—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 only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D207/33—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 only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms with substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D207/337—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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Obesity (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyrrole Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

Новые кристаллические формы кальций аторвастатина, обозначаемые Fa и Je, получают перекристаллизацией из неводного, неполярного растворителей при температуре выше 90°C. Данные кристаллические формы применимы в качестве агентов для лечения гиперлипидемии и гиперхолестеринемии.Международная заявка была опубликована вместе с отчетом о международном поиске.
EA200400789A 2001-12-12 2002-12-11 КРИСТАЛЛИЧЕСКАЯ КАЛЬЦИЕВАЯ СОЛЬ [R-(R*, R*)]-2-(4-ФТОРФЕНИЛ)- β, δ-ДИГИДРОКСИ-5-(1-МЕТИЛЭТИЛ)-3-ФЕНИЛ-4-[(ФЕНИЛАМИНО)КАРБОНИЛ]-1H-ПИРРОЛ-ГЕПТАНОВОЙ КИСЛОТЫ (2:1) EA008441B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US34113301P 2001-12-12 2001-12-12
PCT/US2002/039512 WO2003050085A1 (en) 2001-12-12 2002-12-11 CRYSTALLINE [R-(R*,R*)]-2-(4-FLUOROPHENYL)-β,δ-DIHYDROXY-5-(1-METHYLETHYL)-3-PHENYL-4-[(PHENYLAMINO)CARBONYL]-1H-PYRROLE-HEPTANOIC ACID CALCIUM SALT (2:1)

Publications (2)

Publication Number Publication Date
EA200400789A1 true EA200400789A1 (ru) 2004-12-30
EA008441B1 EA008441B1 (ru) 2007-06-29

Family

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Family Applications (2)

Application Number Title Priority Date Filing Date
EA200400789A EA008441B1 (ru) 2001-12-12 2002-12-11 КРИСТАЛЛИЧЕСКАЯ КАЛЬЦИЕВАЯ СОЛЬ [R-(R*, R*)]-2-(4-ФТОРФЕНИЛ)- β, δ-ДИГИДРОКСИ-5-(1-МЕТИЛЭТИЛ)-3-ФЕНИЛ-4-[(ФЕНИЛАМИНО)КАРБОНИЛ]-1H-ПИРРОЛ-ГЕПТАНОВОЙ КИСЛОТЫ (2:1)
EA200700331A EA009795B1 (ru) 2001-12-12 2002-12-11 КРИСТАЛЛИЧЕСКАЯ КАЛЬЦИЕВАЯ СОЛЬ [R-(R*,R*)]-2-(4-ФТОРФЕНИЛ)-β,δ-ДИГИДРОКСИ-5-(1-МЕТИЛЭТИЛ)-3-ФЕНИЛ-4-[(ФЕНИЛАМИНО)КАРБОНИЛ]-1H-ПИРРОЛГЕПТАНОВОЙ КИСЛОТЫ

Family Applications After (1)

Application Number Title Priority Date Filing Date
EA200700331A EA009795B1 (ru) 2001-12-12 2002-12-11 КРИСТАЛЛИЧЕСКАЯ КАЛЬЦИЕВАЯ СОЛЬ [R-(R*,R*)]-2-(4-ФТОРФЕНИЛ)-β,δ-ДИГИДРОКСИ-5-(1-МЕТИЛЭТИЛ)-3-ФЕНИЛ-4-[(ФЕНИЛАМИНО)КАРБОНИЛ]-1H-ПИРРОЛГЕПТАНОВОЙ КИСЛОТЫ

Country Status (16)

Country Link
US (1) US20050209306A1 (ru)
EP (1) EP1472220A4 (ru)
JP (1) JP2005516008A (ru)
KR (1) KR20040091612A (ru)
CN (2) CN101565394A (ru)
AU (1) AU2002351347A1 (ru)
CA (1) CA2470114A1 (ru)
EA (2) EA008441B1 (ru)
HR (1) HRP20040535A2 (ru)
HU (1) HUP0700116A2 (ru)
MX (1) MXPA04005603A (ru)
NO (1) NO20042902L (ru)
NZ (1) NZ533935A (ru)
PL (1) PL370061A1 (ru)
UA (1) UA77990C2 (ru)
WO (1) WO2003050085A1 (ru)

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US7411075B1 (en) 2000-11-16 2008-08-12 Teva Pharmaceutical Industries Ltd. Polymorphic form of atorvastatin calcium
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
WO2003070702A1 (en) * 2002-02-15 2003-08-28 Teva Pharmaceutical Industries Ltd. Novel crystal forms of atorvastatin hemi-calcium and processes for their preparation, as well as novel processes for preparing atorvastatin hemi-calcium forms i, viii and ix
US7655692B2 (en) 2003-06-12 2010-02-02 Pfizer Inc. Process for forming amorphous atorvastatin
US20050271717A1 (en) 2003-06-12 2005-12-08 Alfred Berchielli Pharmaceutical compositions of atorvastatin
BRPI0513396A (pt) * 2004-07-16 2008-05-06 Lek Pharmaceuticals produtos de degradação oxidativa de atorvastatina de cálcio
CA2754932C (en) * 2004-07-20 2014-04-01 Warner-Lambert Company Llc Novel forms of [r-(r*,r*)]-2-(4-fluorophenyl)-.beta.,.delta.-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1h-pyrrole-1-heptanoic acid calcium salt (2:1)
MX2007004722A (es) 2004-10-28 2007-06-15 Warner Lambert Co Procedimiento para formar atorvastatina amorfa.
WO2006048894A1 (en) * 2004-11-05 2006-05-11 Morepen Laboratories Limited Novel crystalline forms of atorvastatin calcium and processes for preparing them.
CA2547216A1 (en) 2005-09-21 2007-03-21 Renuka D. Reddy Process for annealing amorphous atorvastatin
WO2007057755A1 (en) 2005-11-21 2007-05-24 Warner-Lambert Company Llc Novel forms of [r-(r*,r*)]-2-(4-fluorophenyl)-b,b-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1h-pyrrole-1-hept anoic acid magnesium
KR20100023059A (ko) * 2005-12-13 2010-03-03 테바 파마슈티컬 인더스트리즈 리미티드 아토바스타틴 헤미칼슘의 결정형 및 이의 제조 방법
KR20120011249A (ko) * 2010-07-28 2012-02-07 주식회사 경보제약 아토바스타틴 헤미칼슘염의 신규한 결정형, 이의 수화물, 및 그의 제조방법
WO2013174694A1 (en) * 2012-05-25 2013-11-28 Basf Se Crystalline form b of 1,5-dimethyl-6-thioxo-3-(2,2,7-trifluoro-3-oxo-4-(prop-2-ynyl)-3,4-dihydro-2h-benzo[b][1,4]oxazin-6-yl)-1,3,5-triazinane-2,4-dione
CN104945300B (zh) * 2015-06-17 2017-05-10 北京嘉林药业股份有限公司 一种ⅰ型阿托伐他汀钙的纯化方法
CN104983702A (zh) * 2015-07-23 2015-10-21 青岛蓝盛洋医药生物科技有限责任公司 一种治疗高胆固醇血症的药物阿托伐他汀钙组合物片剂

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Also Published As

Publication number Publication date
UA77990C2 (en) 2007-02-15
WO2003050085A8 (en) 2004-11-11
CN101565394A (zh) 2009-10-28
HUP0700116A2 (en) 2007-05-29
KR20040091612A (ko) 2004-10-28
HRP20040535A2 (en) 2005-02-28
CA2470114A1 (en) 2003-06-19
EA009795B1 (ru) 2008-04-28
US20050209306A1 (en) 2005-09-22
JP2005516008A (ja) 2005-06-02
NO20042902L (no) 2004-09-09
NZ533935A (en) 2006-03-31
PL370061A1 (en) 2005-05-16
CN1612859A (zh) 2005-05-04
EP1472220A4 (en) 2005-06-01
MXPA04005603A (es) 2005-10-18
EA008441B1 (ru) 2007-06-29
EP1472220A1 (en) 2004-11-03
WO2003050085A1 (en) 2003-06-19
EA200700331A1 (ru) 2007-06-29
AU2002351347A1 (en) 2003-06-23

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