KR100781420B1 - [Ｒ-(Ｒ*,Ｒ*)]-2-(4-플루오로페닐)-β,δ-다이하이드록시-5-(1-메틸에틸)-3-페닐-4-[(페닐아미노)카보닐]-1Ｈ-피롤-1-헵탄산의 결정성 형태 - Google Patents

[Ｒ-(Ｒ*,Ｒ*)]-2-(4-플루오로페닐)-β,δ-다이하이드록시-5-(1-메틸에틸)-3-페닐-4-[(페닐아미노)카보닐]-1Ｈ-피롤-1-헵탄산의 결정성 형태 Download PDF

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KR100781420B1
KR100781420B1 KR1020067005316A KR20067005316A KR100781420B1 KR 100781420 B1 KR100781420 B1 KR 100781420B1 KR 1020067005316 A KR1020067005316 A KR 1020067005316A KR 20067005316 A KR20067005316 A KR 20067005316A KR 100781420 B1 KR100781420 B1 KR 100781420B1
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free acid
crystalline form
atorvastatin
atorvastatin free
solid
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KR20060037467A (ko
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안소니 마이클 캄페타
조셉 프란시스 크르지자니악
제이슨 알버트 레오나르드
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워너-램버트 캄파니 엘엘씨
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    • 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
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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

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  • Organic Chemistry (AREA)
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  • Pharmacology & Pharmacy (AREA)
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  • Neurology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Diabetes (AREA)
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyrrole Compounds (AREA)
KR1020067005316A 2003-09-17 2004-09-06 [Ｒ-(Ｒ*,Ｒ*)]-2-(4-플루오로페닐)-β,δ-다이하이드록시-5-(1-메틸에틸)-3-페닐-4-[(페닐아미노)카보닐]-1Ｈ-피롤-1-헵탄산의 결정성 형태 Expired - Fee Related KR100781420B1 (ko)

Applications Claiming Priority (2)

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US50359203P 2003-09-17 2003-09-17
US60/503,592 2003-09-17

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KR20060037467A KR20060037467A (ko) 2006-05-03
KR100781420B1 true KR100781420B1 (ko) 2007-12-03

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KR1020067005316A Expired - Fee Related KR100781420B1 (ko) 2003-09-17 2004-09-06 [Ｒ-(Ｒ*,Ｒ*)]-2-(4-플루오로페닐)-β,δ-다이하이드록시-5-(1-메틸에틸)-3-페닐-4-[(페닐아미노)카보닐]-1Ｈ-피롤-1-헵탄산의 결정성 형태

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US (1) US20070276027A1 (enExample)
EP (1) EP1663969A1 (enExample)
JP (1) JP2007505885A (enExample)
KR (1) KR100781420B1 (enExample)
CN (2) CN101318923A (enExample)
AR (1) AR045654A1 (enExample)
AU (1) AU2004272365A1 (enExample)
BR (1) BRPI0414457A (enExample)
CA (1) CA2539158A1 (enExample)
IL (1) IL173651A0 (enExample)
MX (1) MXPA06003003A (enExample)
NO (1) NO20060716L (enExample)
RU (1) RU2315755C2 (enExample)
TW (1) TW200524862A (enExample)
WO (1) WO2005026116A1 (enExample)
ZA (1) ZA200602222B (enExample)

Families Citing this family (6)

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Publication number Priority date Publication date Assignee Title
KR20080007561A (ko) 2005-12-13 2008-01-22 테바 파마슈티컬 인더스트리즈 리미티드 아토바스타틴 헤미칼슘의 결정형 및 이의 제조 방법
MX2009011009A (es) * 2007-04-13 2009-10-30 Nicox Sa Formas cristalinas de atorvastatin 4-(nitrooxi)butil ester.
US8697740B2 (en) 2009-01-12 2014-04-15 Merck Sharp & Dohme Corp. Crystalline polymorphic forms of an antidiabetic compound
CA3065589C (en) 2010-06-03 2022-04-26 Catalent Ontario Limited Multi phase soft gel capsules, apparatus and method thereof
CA2706270C (en) * 2010-06-03 2020-01-07 Accucaps Industries Limited Pharmaceutical formulations of statins and omega-3 fatty acids for encapsulation
KR20120011249A (ko) 2010-07-28 2012-02-07 주식회사 경보제약 아토바스타틴 헤미칼슘염의 신규한 결정형, 이의 수화물, 및 그의 제조방법

Citations (3)

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US4681893A (en) 1986-05-30 1987-07-21 Warner-Lambert Company Trans-6-[2-(3- or 4-carboxamido-substituted pyrrol-1-yl)alkyl]-4-hydroxypyran-2-one inhibitors of cholesterol synthesis
WO2002043667A2 (en) * 2000-11-16 2002-06-06 Teva Pharmaceutical Industries Ltd. 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
US6583295B1 (en) 1998-09-18 2003-06-24 Lek Pharmaceuticals D.D. Salts of HMG-CoA reductase inhibitors

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US4681873A (en) * 1985-07-29 1987-07-21 Warner-Lambert Company 4-amino-3-halo-2-pyridinone nucleoside and nucleotide compounds
US5216174A (en) * 1988-02-22 1993-06-01 Warner-Lambert Co. Process for trans-6-[12-(substituted-pyrrol-1-yl)alkyl]pyran-2-one inhibitors of cholesterol synthesis
US5149837A (en) * 1988-02-22 1992-09-22 Warner-Lambert Company Process for trans-6-[2-(substituted-pyrrol-1-yl)alkyl]pyran-2-one inhibitors of cholesterol synthesis
US5003080A (en) * 1988-02-22 1991-03-26 Warner-Lambert Company Process for trans-6-(2-(substituted-pyrrol-1-yl)alkyl)pryan-2-one inhibitors of cholesterol synthesis
US5245047A (en) * 1988-02-22 1993-09-14 Warner-Lambert Company Process for trans-6-[2-(substituted-pyrrol-1-yl)alkyl]pyran-2-one inhibitors of cholesterol synthesis
US5124482A (en) * 1988-02-22 1992-06-23 Warner-Lambert Company Process for trans-6-(2-substituted-pyrrol-1-yl)alkyl)pyran-2-one inhibitors of cholesterol synthesis
US5097045A (en) * 1989-02-01 1992-03-17 Warner-Lambert Company Process for trans-6-[2-(substituted-pyrrol-1-yl)alkyl]pyran-2-one inhibitors of cholesterol synthesis
FI94339C (fi) * 1989-07-21 1995-08-25 Warner Lambert Co Menetelmä farmaseuttisesti käyttökelpoisen /R-(R*,R*)/-2-(4-fluorifenyyli)- , -dihydroksi-5-(1-metyylietyyli)-3-fenyyli-4-/(fenyyliamino)karbonyyli/-1H-pyrroli-1-heptaanihapon ja sen farmaseuttisesti hyväksyttävien suolojen valmistamiseksi
US5248793A (en) * 1990-10-17 1993-09-28 Warner-Lambert Company Process for the synthesis of (4R-cis)-1,1-dimethylethyl 6-iodomethyl or 6-(phenyl-substituted)sulfonyloxymethyl-2,2-dimethyl-1,3-dioxane-4-acetate
US5103024A (en) * 1990-10-17 1992-04-07 Warner-Lambert Company Process for the synthesis of (4r-cis)-1,1-dimethylethyl 6-cyanomethyl-2,2-dimethyl-1,3-dioxane-4-acetate
US5155251A (en) * 1991-10-11 1992-10-13 Warner-Lambert Company Process for the synthesis of (5R)-1,1-dimethylethyl-6-cyano-5-hydroxy-3-oxo-hexanoate
US5213995A (en) * 1992-04-16 1993-05-25 At&T Bell Laboratories Method of making an article comprising a periodic heteroepitaxial semiconductor structure
WO1994016693A1 (en) * 1993-01-19 1994-08-04 Warner-Lambert Company Stable oral ci-981 formulation and process of preparing same
US5298627A (en) * 1993-03-03 1994-03-29 Warner-Lambert Company Process for trans-6-[2-(substituted-pyrrol-1-yl)alkyl]pyran-2-one inhibitors of cholesterol synthesis
HRP960313B1 (en) * 1995-07-17 2002-08-31 Warner Lambert Co Form iii crystalline (r- (r*, r*)-2- (4-fluorophenyl) -beta-delta-hydroxy-5-(1-methylethyl) -3-phenyl-4- ((phenylamino) carbonyl -1h-pyrrole-1-heptanoic acid calcium salt (2:1)
ES2167587T3 (es) * 1995-07-17 2002-05-16 Warner Lambert Co Forma cristalina de la sal hemicalcica del acido (r-(r*,r*))-2-(4-fluorofenil)-beta,delta-dihidroxi-5-(1-metiletil)-3-fenil-4-((fenilamino)carbonil)-1h-pirrol-1-heptanoico (atorvastatina).
US6087511A (en) * 1996-07-16 2000-07-11 Warner-Lambert Company Process for the production of amorphous [R-(R*,R*)]-2-(4-fluorophenyl)-β,δ-dihydroxy-5-(1-methylethyl )-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid) calcium salt (2:1)
EP0915866B1 (en) * 1996-07-29 2002-03-27 Warner-Lambert Company Improved process for the synthesis of protected esters of (s)-3,4-dihydroxybutyric acid
HUP0100252A3 (en) * 1997-12-19 2002-12-28 Warner Lambert Exp Ltd Dun Lao Process for the synthesis of 1,3-diols
US6476235B2 (en) * 2001-01-09 2002-11-05 Warner-Lambert Company Process for the synthesis of 5-(4-fluorophenyl)-1-[2-((2R,4R)-4-hydroxy-6-oxo-tetrahydro-pyran-2-yl)-ethyl]-2-isopropyl-4-phenyl-1H-pyrrole-3-carboxylic acid phenylamide

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4681893A (en) 1986-05-30 1987-07-21 Warner-Lambert Company Trans-6-[2-(3- or 4-carboxamido-substituted pyrrol-1-yl)alkyl]-4-hydroxypyran-2-one inhibitors of cholesterol synthesis
US6583295B1 (en) 1998-09-18 2003-06-24 Lek Pharmaceuticals D.D. Salts of HMG-CoA reductase inhibitors
WO2002043667A2 (en) * 2000-11-16 2002-06-06 Teva Pharmaceutical Industries Ltd. 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

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IL173651A0 (en) 2006-07-05
ZA200602222B (en) 2007-07-25
BRPI0414457A (pt) 2006-11-14
EP1663969A1 (en) 2006-06-07
MXPA06003003A (es) 2006-06-23
CN1852894A (zh) 2006-10-25
AR045654A1 (es) 2005-11-02
CN101318923A (zh) 2008-12-10
KR20060037467A (ko) 2006-05-03
RU2006108385A (ru) 2006-08-10
US20070276027A1 (en) 2007-11-29
AU2004272365A1 (en) 2005-03-24
CA2539158A1 (en) 2005-03-24
JP2007505885A (ja) 2007-03-15
TW200524862A (en) 2005-08-01
RU2315755C2 (ru) 2008-01-27
NO20060716L (no) 2006-06-16
WO2005026116A1 (en) 2005-03-24

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