HRP20030575B1 - Preparacija nekristalnog atorvastatin kalcija - Google Patents

Preparacija nekristalnog atorvastatin kalcija

Info

Publication number
HRP20030575B1
HRP20030575B1 HR20030575A HRP20030575A HRP20030575B1 HR P20030575 B1 HRP20030575 B1 HR P20030575B1 HR 20030575 A HR20030575 A HR 20030575A HR P20030575 A HRP20030575 A HR P20030575A HR P20030575 B1 HRP20030575 B1 HR P20030575B1
Authority
HR
Croatia
Prior art keywords
atorvastatin
protecting group
water
group
solution
Prior art date
Application number
HR20030575A
Other languages
English (en)
Inventor
Sorsak Gorazd
Original Assignee
Lek Pharmaceutical And Chemical Company D.D.
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 Lek Pharmaceutical And Chemical Company D.D. filed Critical Lek Pharmaceutical And Chemical Company D.D.
Publication of HRP20030575A2 publication Critical patent/HRP20030575A2/hr
Publication of HRP20030575B1 publication Critical patent/HRP20030575B1/hr

Links

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
    • C07D207/34—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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • 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)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Diabetes (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Public Health (AREA)
  • Obesity (AREA)
  • Pyrrole Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

Postupak za preparaciju atorvastatina u nekristaliničnom obliku naznačen time da obuhvaća: a) dobivanje otopine koja sadrži intermedijerni spoj sljedeće formule (1) u nehidroksilnom otapalu: gdje A označava zajedničku zaštitnu skupinu ili odvojene zaštitne skupine za dihidroksi skupinu i B označava zaštitnu skupinu za karboksilnu kiselinu; b) uklanjanje zaštitne skupine sa hidroksilne skupine; c) uklanjanje zaštitne skupine sa karboksilne kiseline; gdje se redoslijed koraka b) i c) može preokrenuti ; d) koncentriranje otopine do oko polovice početnog volumena ili manje: e) dodavanje vode u suvišku volumena koncentrirane otopine; f) dodavanje, uzimanjem oko jednakog ili većeg volumena od volumena vode dodane u koraku e), otapala koje se neznatno miješa s vodom ili se ne miješa s vodom i u kojem atorvastatin kalcij nije topljiv ili je praktički netopljiv; g) opciono provođenje operacije miješanja, i odvajanje dviju faza; h) neutraliziranje vodene faze; i) pretvaranje atorvastatina u obliku dihidroksikarboksilne kiseline u oblik njegove farmaceutski prihvatljive soli; ij) nastajanje taloga atorvastatina koji se prevodi u navedeni oblik farmaceutski prihvatljive soli. Patent sadrži još 21 patentni zahtjev.
HR20030575A 2001-01-23 2003-07-15 Preparacija nekristalnog atorvastatin kalcija HRP20030575B1 (hr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
SI200100010A SI20814A (sl) 2001-01-23 2001-01-23 Priprava amorfnega atorvastatina
PCT/IB2002/000161 WO2002059087A1 (en) 2001-01-23 2002-01-22 Preparation of non-crystalline atorvastatin calcium

Publications (2)

Publication Number Publication Date
HRP20030575A2 HRP20030575A2 (en) 2005-06-30
HRP20030575B1 true HRP20030575B1 (hr) 2011-10-31

Family

ID=20432812

Family Applications (1)

Application Number Title Priority Date Filing Date
HR20030575A HRP20030575B1 (hr) 2001-01-23 2003-07-15 Preparacija nekristalnog atorvastatin kalcija

Country Status (27)

Country Link
US (2) US6750353B2 (hr)
EP (1) EP1373202B1 (hr)
JP (1) JP4336106B2 (hr)
KR (1) KR100882066B1 (hr)
CN (1) CN1260213C (hr)
AT (1) ATE294159T1 (hr)
AU (1) AU2002219455B2 (hr)
BG (1) BG108017A (hr)
BR (1) BR0206637A (hr)
CA (1) CA2435954C (hr)
CZ (1) CZ20031988A3 (hr)
DE (1) DE60203894T2 (hr)
DK (1) DK1373202T3 (hr)
EE (1) EE05270B1 (hr)
ES (1) ES2240748T3 (hr)
HR (1) HRP20030575B1 (hr)
HU (1) HU227535B1 (hr)
IL (2) IL157068A0 (hr)
MX (1) MXPA03006548A (hr)
PL (1) PL209428B1 (hr)
RS (1) RS51010B (hr)
RU (1) RU2324679C2 (hr)
SI (2) SI20814A (hr)
SK (1) SK286593B6 (hr)
UA (1) UA73829C2 (hr)
WO (1) WO2002059087A1 (hr)
ZA (1) ZA200305307B (hr)

Families Citing this family (45)

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Publication number Priority date Publication date Assignee Title
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
CZ20032019A3 (cs) 2000-12-27 2003-10-15 Ciba Specialty Chemicals Holding Inc. Krystalické formy Atorvastatinu
EP1365995A2 (en) * 2001-02-27 2003-12-03 Council of Scientific and Industrial Research Essential oil composiiton for potable water disinfection
EA005317B1 (ru) 2001-06-29 2004-12-30 УОРНЕР-ЛАМБЕРТ КОМПАНИ Эл-Эл-Си Кристаллические формы [r-(r*,r*)]-2-(4-фторфенил)-бета, дельта-дигидрокси-5-(1-метилэтил)-3-фенил-4-[(фениламино)карбонил]-1h-пиррол-1-гептановой кислоты кальциевой соли (2:1) (аторвастатин)
HU227124B1 (en) * 2001-09-14 2010-07-28 Egis Gyogyszergyar Nyilvanosan Polymorphs of 1-pyrrole derivative, intermediate for the preparation of atorvastatin
MXPA04007995A (es) 2002-02-19 2004-11-26 Teva Pharma Desolvatacion de solvatos de hemicalcio de atorvastatina.
ITMI20020907A1 (it) * 2002-04-29 2003-10-29 Chemi Spa Processo di preparazione della forma amorfa del sale di calcio della atorvastatina
CA2385529A1 (en) * 2002-05-21 2003-11-21 Bernard Charles Sherman Stable dosage forms comprising atorvastatin calcium
BRPI0409292A (pt) 2003-04-11 2006-04-11 Lek Pharmaceuticals processo para a preparação de sal de cálcio amorfo de atorvastatina
US7790197B2 (en) 2003-06-09 2010-09-07 Warner-Lambert Company Llc Pharmaceutical compositions of atorvastatin
US7655692B2 (en) 2003-06-12 2010-02-02 Pfizer Inc. Process for forming amorphous atorvastatin
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CA2530446A1 (en) 2003-07-02 2005-01-13 Egis Gyogyszergyar Rt. Process for the preparation of amorphous form of a platelet aggregation inhibitor drug
AU2003247327A1 (en) * 2003-07-15 2005-01-28 Eos Eczacibasi Ozgun Kimyasal Urunler Sanyi Ve Ticaret A.S. Process for the preparation of amortphous atorvastatin calcium without interconversion of any crystalline form
AU2003272082A1 (en) * 2003-10-07 2005-04-21 Biocon Limited Process for the production of atorvastatin calcium
CA2551549A1 (en) * 2003-12-29 2005-07-14 Lek Pharmaceuticals D.D. Process for preparing amorphous (4r-cis)-6-[2-[3-phenyl-4-(phenylcarbamoyl)-2-(4-fluorophenyl)-5-(1-methylethyl)-pyrrol-1-yl]-ethyl]-2,2-dimethyl-[1,3]-dioxane-4-yl-acetic acid
EP1577297A1 (en) 2004-03-17 2005-09-21 Ranbaxy Laboratories, Ltd. Process for the production of atorvastatin calcium in amorphous form
ES2739493T3 (es) 2004-05-05 2020-01-31 Pfizer Prod Inc Formas de sal de de atorvastatina con benetamina
JP5000502B2 (ja) * 2004-07-16 2012-08-15 レツク・フアーマシユーテイカルズ・デー・デー アトルバスタチンカルシウムの酸化分解生成物
CA2672554C (en) 2004-07-20 2012-01-03 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)
WO2006011155A1 (en) * 2004-07-26 2006-02-02 Apollo International Limited One pot process for amorphous atorvastain calcium
JP2008510798A (ja) * 2004-08-27 2008-04-10 バイオコン・リミテッド 非晶質アトルバスタチンカルシウムのための方法
AU2005298383A1 (en) 2004-10-28 2006-05-04 Warner-Lambert Company Llc Process for forming amorphous atorvastatin
ES2270722B1 (es) * 2005-09-15 2008-03-01 Ercros Industrial, S.A. Procedimiento para la obtencion de atorvastatina calcica amorfa.
US20090216029A1 (en) * 2005-09-16 2009-08-27 Yatendra Kumar Process for the production of atorvastatin calcium in amorphous form
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DE602006014193D1 (de) 2005-11-21 2010-06-17 Warner Lambert Co Neue formen von är-(r*,r*)ü-2-(4-fluorphenyl)-b,d-dihydroxy-5-(1-methylethyl)-3-phenyl-4-ä(phenylamino)carbonylü-1h-pyrrol-1-heptansäure-magnesium
EP1810667A1 (en) 2006-01-20 2007-07-25 KRKA, tovarna zdravil, d.d., Novo mesto Pharmaceutical composition comprising amorphous atorvastatin
EP1979313A1 (en) * 2006-01-31 2008-10-15 Jubilant Organosys Limited Process for the preparation of amorphous atorvastatin calcium salt
CN100406438C (zh) * 2006-06-30 2008-07-30 浙江新东港药业股份有限公司 一种无定型阿伐他汀钙的制备方法
US20100113802A1 (en) * 2006-11-02 2010-05-06 Cadila Pharmaceuticals Limited Process for preparing amorphous atorvastatin hemi calcium salt and its itermediate
KR100833439B1 (ko) * 2007-01-02 2008-05-29 씨제이제일제당 (주) 비결정형 아토르바스타틴 칼슘의 개선된 제조방법
BRPI0818575A2 (pt) * 2007-10-17 2014-10-07 Todd F Ovokaitys Processo para a modificação do estado sólido de um composto e composições co-amorfas produzidas com o mesmo
WO2009139730A1 (en) * 2008-05-13 2009-11-19 Ulkar Kimya San. Ve Tic. A.S. Preparation of novel non-crystalline forms of atorvastatin calcium
KR101050722B1 (ko) 2008-12-02 2011-07-21 대웅바이오 주식회사 무정형 아토르바스타틴 칼슘염의 제조방법
US8115015B2 (en) * 2009-01-26 2012-02-14 Cadila Healthcare Limited Process for the preparation of amorphous atorvastatin calcium
WO2011131605A1 (en) * 2010-04-19 2011-10-27 Dsm Ip Assets B.V. Production of atorvastatin low in ether impurities
HUP1000299A2 (hu) 2010-06-08 2012-02-28 Nanoform Cardiovascular Therapeutics Ltd Nanostrukturált Atorvastatint, gyógyszerészetileg elfogadott sóit és kokristályait tartalmazó készítmény és eljárás elõállításukra
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
US10202598B2 (en) 2014-05-30 2019-02-12 Todd Frank Ovokaitys Methods and systems for generation, use, and delivery of activated stem cells
US10384985B2 (en) 2014-06-06 2019-08-20 B.K. Consultants, Inc. Methods and compositions for increasing the yield of, and beneficial chemical composition of, certain plants
WO2015187974A1 (en) 2014-06-06 2015-12-10 Ovokaitys Todd Frank Methods and compositions for increasing the bioactivity of nutrients
CN113321607A (zh) * 2020-02-28 2021-08-31 北京福元医药股份有限公司沧州分公司 一种阿托伐他汀钙中间体的纯化方法

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Also Published As

Publication number Publication date
PL361763A1 (en) 2004-10-04
ES2240748T3 (es) 2005-10-16
JP2005503997A (ja) 2005-02-10
CA2435954A1 (en) 2002-08-01
JP4336106B2 (ja) 2009-09-30
US20040072895A1 (en) 2004-04-15
KR20030077003A (ko) 2003-09-29
SK286593B6 (sk) 2009-01-07
DE60203894T2 (de) 2006-01-19
YU56803A (sh) 2006-05-25
DK1373202T3 (da) 2005-05-17
SI1373202T1 (sl) 2005-12-31
HUP0302797A2 (hu) 2003-11-28
US7074940B2 (en) 2006-07-11
ATE294159T1 (de) 2005-05-15
IL157068A0 (en) 2004-02-08
BR0206637A (pt) 2004-08-03
US20030109569A1 (en) 2003-06-12
DE60203894D1 (de) 2005-06-02
IL157068A (en) 2009-09-01
AU2002219455B2 (en) 2007-04-26
RU2003124962A (ru) 2005-01-10
CN1260213C (zh) 2006-06-21
BG108017A (bg) 2004-08-31
CA2435954C (en) 2008-06-03
HUP0302797A3 (en) 2009-09-28
HU227535B1 (en) 2011-08-29
CZ20031988A3 (cs) 2003-11-12
UA73829C2 (en) 2005-09-15
MXPA03006548A (es) 2004-10-15
KR100882066B1 (ko) 2009-02-10
US6750353B2 (en) 2004-06-15
EP1373202A1 (en) 2004-01-02
EE05270B1 (et) 2010-02-15
SI20814A (sl) 2002-08-31
RS51010B (sr) 2010-10-31
SK9082003A3 (en) 2003-12-02
HRP20030575A2 (en) 2005-06-30
ZA200305307B (en) 2004-07-09
WO2002059087A1 (en) 2002-08-01
EP1373202B1 (en) 2005-04-27
RU2324679C2 (ru) 2008-05-20
CN1487921A (zh) 2004-04-07
EE200300333A (et) 2003-10-15
PL209428B1 (pl) 2011-08-31

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