BRPI0414457A - formas cristalinas do ácido [r-(r*,r*)]-2-(4-fluorofenil)-beta, delta-dihidróxi-5-(1-metiletil)-3-fenil-4-[(fenilamino)-c arbonil]-1h-pirrol-1-heptanóico - Google Patents

formas cristalinas do ácido [r-(r*,r*)]-2-(4-fluorofenil)-beta, delta-dihidróxi-5-(1-metiletil)-3-fenil-4-[(fenilamino)-c arbonil]-1h-pirrol-1-heptanóico

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Publication number
BRPI0414457A
BRPI0414457A BRPI0414457-0A BRPI0414457A BRPI0414457A BR PI0414457 A BRPI0414457 A BR PI0414457A BR PI0414457 A BRPI0414457 A BR PI0414457A BR PI0414457 A BRPI0414457 A BR PI0414457A
Authority
BR
Brazil
Prior art keywords
phenylamino
fluorophenyl
phenyl
heptanoic
pyrrol
Prior art date
Application number
BRPI0414457-0A
Other languages
English (en)
Inventor
Anthony Michael Campeta
Joseph Francis Krzyzaniak
Jason Albert Leonard
Original Assignee
Warner Lambert Co
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 Warner Lambert Co filed Critical Warner Lambert Co
Publication of BRPI0414457A publication Critical patent/BRPI0414457A/pt

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    • 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
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/08Drugs for disorders of the urinary system of the prostate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Animal Behavior & Ethology (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)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Diabetes (AREA)
  • Hospice & Palliative Care (AREA)
  • Obesity (AREA)
  • Psychiatry (AREA)
  • Urology & Nephrology (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyrrole Compounds (AREA)

Abstract

"FORMAS CRISTALINAS DO áCIDO ¢R-(R*,R*)!-2-(4-FLUOROFENIL)-BETA,DELTA-DIHIDRóXI-5-(1-M ETILETIL)-3-FENIL-4¢(FENILAMINO)-CARBONIL!-1H-PIRROL-1 -HEPTANóICO". A presente invenção refere-se a novas formas cristalinas do ácido ¢R-(R*,R*)!-2-(4-fluorofenil)-<225>,<SYM>-dihidróxi-5-(1-metiletil)-3-fe nil-4-¢(fenilamino)-carbonil!-1H-pirrol-l-heptanóico (ácido livre de atorvastatina) designado Forma A e Forma B, caracterizadas pelos seus padrões de difração de raios X de pó e os seus espectros de RMN no estado sólido são descritos, bem como os métodos de preparação de composição farmacêutica do mesmo, que são úteis como agentes para tratar hiperlipidemia, hipercolesterolemia, osteoporose, hiperplasia prostática benigna, e Doença de Alzheimer, e para preparar sais de atorvastatina.
BRPI0414457-0A 2003-09-17 2004-09-06 formas cristalinas do ácido [r-(r*,r*)]-2-(4-fluorofenil)-beta, delta-dihidróxi-5-(1-metiletil)-3-fenil-4-[(fenilamino)-c arbonil]-1h-pirrol-1-heptanóico BRPI0414457A (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US50359203P 2003-09-17 2003-09-17
PCT/IB2004/002919 WO2005026116A1 (en) 2003-09-17 2004-09-06 Crystalline forms of `r-(r*,r*)]-2-(4-fluorophenyl)-beta,delta-dihydroxy-5-(1-methylethyl)-3-phenyl-4-`(phenylamino)carbonyl!-1h-pyrrole-1-heptanoic acid

Publications (1)

Publication Number Publication Date
BRPI0414457A true BRPI0414457A (pt) 2006-11-14

Family

ID=34312443

Family Applications (1)

Application Number Title Priority Date Filing Date
BRPI0414457-0A BRPI0414457A (pt) 2003-09-17 2004-09-06 formas cristalinas do ácido [r-(r*,r*)]-2-(4-fluorofenil)-beta, delta-dihidróxi-5-(1-metiletil)-3-fenil-4-[(fenilamino)-c arbonil]-1h-pirrol-1-heptanóico

Country Status (16)

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

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8080672B2 (en) 2005-12-13 2011-12-20 Teva Pharmaceutical Industries Ltd. Crystal form of atorvastatin hemi-calcium and processes for preparation thereof
MX2009011009A (es) * 2007-04-13 2009-10-30 Nicox Sa Formas cristalinas de atorvastatin 4-(nitrooxi)butil ester.
WO2010080971A1 (en) * 2009-01-12 2010-07-15 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

Family Cites Families (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4681873A (en) * 1985-07-29 1987-07-21 Warner-Lambert Company 4-amino-3-halo-2-pyridinone nucleoside and nucleotide compounds
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
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
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
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
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
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
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
JP3254219B2 (ja) * 1993-01-19 2002-02-04 ワーナー−ランバート・コンパニー 安定な経口用のci−981製剤およびその製法
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)
GEP20002029B (en) * 1995-07-17 2000-04-10 Warner Lambert Company Us (54) Crystalline [R-(R*,R*,]–2-(4-Fluorophenyl)-Beta,Delta-Dihydroxy-5-(1-Methyl-Ethyl)-3-Phenyl–4-{Phenylamino) Carbonyl} - 1H - Pyrrole - 1 - Heptanoic Acid Hemi Calcium Salt (Atorvastatin)
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)
TR199900191T2 (xx) * 1996-07-29 1999-04-21 Warner-Lambert Company (S)-3,4-Dihidroksibutirik asitin korumal� esterlerinin sentezi i�in geli�tirilmi� proses.
EP1054860B1 (en) * 1997-12-19 2007-04-25 Pfizer Ireland Pharmaceuticals Process for the synthesis of 1,3-diols
SI20070A (sl) 1998-09-18 2000-04-30 LEK, tovarna farmacevtskih in kemi�nih izdelkov, d.d. Nove soli inhibitorjev HMG-CoA reduktaze
PL362981A1 (en) * 2000-11-16 2004-11-02 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
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

Also Published As

Publication number Publication date
ZA200602222B (en) 2007-07-25
IL173651A0 (en) 2006-07-05
US20070276027A1 (en) 2007-11-29
CA2539158A1 (en) 2005-03-24
CN1852894A (zh) 2006-10-25
NO20060716L (no) 2006-06-16
TW200524862A (en) 2005-08-01
EP1663969A1 (en) 2006-06-07
JP2007505885A (ja) 2007-03-15
KR100781420B1 (ko) 2007-12-03
WO2005026116A1 (en) 2005-03-24
AR045654A1 (es) 2005-11-02
MXPA06003003A (es) 2006-06-23
RU2315755C2 (ru) 2008-01-27
RU2006108385A (ru) 2006-08-10
AU2004272365A1 (en) 2005-03-24
KR20060037467A (ko) 2006-05-03
CN101318923A (zh) 2008-12-10

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Legal Events

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B08F Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette]

Free format text: REFERENTE AS 6A E 7A ANUIDADES.

B08K Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette]

Free format text: REFERENTE AO DESPACHO 8.6 PUBLICADO NA RPI 2159 DE 22/05/2012.