BR0206637A - Processo para preparação de atorvastatina em forma não cristalina e de formulação farmacêutica - Google Patents

Processo para preparação de atorvastatina em forma não cristalina e de formulação farmacêutica

Info

Publication number
BR0206637A
BR0206637A BR0206637-8A BR0206637A BR0206637A BR 0206637 A BR0206637 A BR 0206637A BR 0206637 A BR0206637 A BR 0206637A BR 0206637 A BR0206637 A BR 0206637A
Authority
BR
Brazil
Prior art keywords
atorvastatin
calcium
crystalline
denotes
preparation
Prior art date
Application number
BR0206637-8A
Other languages
English (en)
Inventor
Gorazd Sorsak
Original Assignee
Lek Tovarna Farmacevtskih
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 Tovarna Farmacevtskih filed Critical Lek Tovarna Farmacevtskih
Publication of BR0206637A publication Critical patent/BR0206637A/pt

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic 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
    • C07D207/30Heterocyclic 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
    • C07D207/34Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • YGENERAL 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
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02PCLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00Technologies relating to chemical industry
    • Y02P20/50Improvements relating to the production of bulk chemicals
    • Y02P20/55Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Medicinal Chemistry (AREA)
  • Diabetes (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Hematology (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (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

"PROCESSO PARA PREPARAçãO DE ATORVASTATINA EM FORMA NãO CRISTALINA E DE FORMULAçãO FARMACêUTICA". Atorvastatina cálcica, a substância conhecida pelo nome químico sal semi cálcio de [(R-(R*,R*)]-2-(4-fluorfenil)-b,d-dihidróxi-5-(1-metil-etil)-3-fenil-4-[(fenila mino)carbonil]-1H-pirrolo-1-ácido heptanóico, é conhecida como inibidora de HMG-CoA redutase e é usada como um agente antihipercolesterolêmico. A atorvastatina é normalmente preparada como seu sal de cálcio, uma vez que ele permite que a atorvastatina seja convenientemente formulada nas formulações farmacêuticas, por exemplo, comprimidos, cápsulas, pós e similares para administração oral. A atorvastatina cálcica pode existir em uma forma amorfa ou em uma das fórmulas cristalinas (Forma I, Forma II, Forma III e Forma IV). A atorvastatina cálcica é a substância que é ligeiramente solúvel em água e concluiu-se que as formas cristalinas são menos prontamente solúveis do que a forma amorfa, o que pode causar problemas na biodisponibilidade de atorvastatina no corpo. A presente invenção se refere a um novo processo para converter o intermediário da síntese de atorvastatina da fórmula seguinte (I) ou atorvastatina lactose na atorvastatina cálcica não cristalina: em que A denota um grupo protetor comum ou grupos protetores separados para o grupo di-hidróxi e B denota um grupo protetor de ácido carboxílico.
BR0206637-8A 2001-01-23 2002-01-22 Processo para preparação de atorvastatina em forma não cristalina e de formulação farmacêutica BR0206637A (pt)

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 (1)

Publication Number Publication Date
BR0206637A true BR0206637A (pt) 2004-08-03

Family

ID=20432812

Family Applications (1)

Application Number Title Priority Date Filing Date
BR0206637-8A BR0206637A (pt) 2001-01-23 2002-01-22 Processo para preparação de atorvastatina em forma não cristalina e de formulação farmacêutica

Country Status (27)

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

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CA2626317A1 (en) 2000-12-27 2002-07-04 Teva Pharmaceutical Industries Ltd. Crystalline forms of atorvastatin
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HU227124B1 (en) * 2001-09-14 2010-07-28 Egis Gyogyszergyar Nyilvanosan Polymorphs of 1-pyrrole derivative, intermediate for the preparation of atorvastatin
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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
US7645888B2 (en) 2004-08-27 2010-01-12 Biocon Limited Process for the production of amorphous atorvastatin calcium
BRPI0519996A2 (pt) 2004-10-28 2009-04-07 Warner Lambert Co processo para formar atorvastatina amorfa
ES2270722B1 (es) * 2005-09-15 2008-03-01 Ercros Industrial, S.A. Procedimiento para la obtencion de atorvastatina calcica amorfa.
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CA2547216A1 (en) 2005-09-21 2007-03-21 Renuka D. Reddy Process for annealing amorphous atorvastatin
ES2304335T3 (es) 2005-11-21 2010-05-19 Warner-Lambert Company Llc Formas nuevas del acido (r-(r*,r*))-2-(4-fluorofenil)-b,b-dihidroxi-5-(1-metiletil)-3-fenil-4-((fenilamino)carbonil)1h-pirrol-1-heptanoico, de magnesio.
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WO2009052246A1 (en) * 2007-10-17 2009-04-23 Ovokaitys, Todd, F. Process for the modification of the solid state of a compound and co-amorphous compositions produced with same
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
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HUE030160T2 (en) * 2010-04-19 2017-05-29 Dsm Sinochem Pharm Nl Bv Preparation of atorvastatin with low dietary contamination
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Also Published As

Publication number Publication date
IL157068A0 (en) 2004-02-08
RU2003124962A (ru) 2005-01-10
SI1373202T1 (sl) 2005-12-31
IL157068A (en) 2009-09-01
JP4336106B2 (ja) 2009-09-30
CZ20031988A3 (cs) 2003-11-12
DE60203894D1 (de) 2005-06-02
PL209428B1 (pl) 2011-08-31
ES2240748T3 (es) 2005-10-16
YU56803A (sh) 2006-05-25
BG108017A (bg) 2004-08-31
SK9082003A3 (en) 2003-12-02
EP1373202A1 (en) 2004-01-02
SI20814A (sl) 2002-08-31
US7074940B2 (en) 2006-07-11
US6750353B2 (en) 2004-06-15
CN1260213C (zh) 2006-06-21
SK286593B6 (sk) 2009-01-07
EE05270B1 (et) 2010-02-15
HUP0302797A3 (en) 2009-09-28
CN1487921A (zh) 2004-04-07
AU2002219455B2 (en) 2007-04-26
ATE294159T1 (de) 2005-05-15
WO2002059087A1 (en) 2002-08-01
ZA200305307B (en) 2004-07-09
RS51010B (sr) 2010-10-31
HU227535B1 (en) 2011-08-29
US20040072895A1 (en) 2004-04-15
HRP20030575B1 (en) 2011-10-31
RU2324679C2 (ru) 2008-05-20
HUP0302797A2 (hu) 2003-11-28
EP1373202B1 (en) 2005-04-27
HRP20030575A2 (en) 2005-06-30
PL361763A1 (en) 2004-10-04
KR100882066B1 (ko) 2009-02-10
DK1373202T3 (da) 2005-05-17
CA2435954C (en) 2008-06-03
JP2005503997A (ja) 2005-02-10
UA73829C2 (en) 2005-09-15
DE60203894T2 (de) 2006-01-19
KR20030077003A (ko) 2003-09-29
US20030109569A1 (en) 2003-06-12
MXPA03006548A (es) 2004-10-15
EE200300333A (et) 2003-10-15
CA2435954A1 (en) 2002-08-01

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B06F Objections, documents and/or translations needed after an examination request according [chapter 6.6 patent gazette]
B07D Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette]
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