CN1196679C - 无定形阿托伐斯汀钙的制备方法 - Google Patents
无定形阿托伐斯汀钙的制备方法 Download PDFInfo
- Publication number
- CN1196679C CN1196679C CNB008080275A CN00808027A CN1196679C CN 1196679 C CN1196679 C CN 1196679C CN B008080275 A CNB008080275 A CN B008080275A CN 00808027 A CN00808027 A CN 00808027A CN 1196679 C CN1196679 C CN 1196679C
- Authority
- CN
- China
- Prior art keywords
- solvent
- atorvastatin calcium
- atorvastatin
- amorphous
- tetrahydrofuran
- Prior art date
- Legal status (The legal status 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 status listed.)
- Expired - Fee Related
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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
- C07D207/34—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
- A61P3/06—Antihyperlipidemics
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (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)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pyrrole Compounds (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IN775DE1999 IN191236B (enExample) | 1999-05-25 | 1999-05-25 | |
| IN775/DEL/99 | 1999-05-25 |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNA2005100525833A Division CN1680315A (zh) | 1999-05-25 | 2000-01-06 | 无定形阿托伐斯汀钙的制备方法 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1351493A CN1351493A (zh) | 2002-05-29 |
| CN1196679C true CN1196679C (zh) | 2005-04-13 |
Family
ID=11091180
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNB008080275A Expired - Fee Related CN1196679C (zh) | 1999-05-25 | 2000-01-06 | 无定形阿托伐斯汀钙的制备方法 |
| CNA2005100525833A Pending CN1680315A (zh) | 1999-05-25 | 2000-01-06 | 无定形阿托伐斯汀钙的制备方法 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNA2005100525833A Pending CN1680315A (zh) | 1999-05-25 | 2000-01-06 | 无定形阿托伐斯汀钙的制备方法 |
Country Status (15)
| Country | Link |
|---|---|
| US (2) | US6528660B1 (enExample) |
| EP (1) | EP1185264B1 (enExample) |
| CN (2) | CN1196679C (enExample) |
| AT (1) | ATE362759T1 (enExample) |
| AU (1) | AU778962B2 (enExample) |
| BR (1) | BR0010923A (enExample) |
| DE (1) | DE60034946T2 (enExample) |
| DK (1) | DK1185264T3 (enExample) |
| ES (1) | ES2284472T3 (enExample) |
| HK (1) | HK1045118A1 (enExample) |
| IN (1) | IN191236B (enExample) |
| MY (1) | MY133511A (enExample) |
| PT (1) | PT1185264E (enExample) |
| WO (1) | WO2000071116A1 (enExample) |
| ZA (1) | ZA200109656B (enExample) |
Families Citing this family (45)
| 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 |
| SI20425A (sl) * | 1999-12-10 | 2001-06-30 | LEK tovarna farmacevtskih in kemi�nih izdelkov d.d. | Priprava amorfnega atorvastatina |
| 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 |
| WO2002057228A1 (en) * | 2001-01-17 | 2002-07-25 | Biocon India Limited | Atorvastatin calcium |
| SI20814A (sl) * | 2001-01-23 | 2002-08-31 | LEK, tovarna farmacevtskih in kemi�nih izdelkov, d.d. | Priprava amorfnega atorvastatina |
| IN190564B (enExample) * | 2001-04-11 | 2003-08-09 | Cadila Heathcare Ltd | |
| EP1423364B1 (en) | 2001-06-29 | 2015-11-04 | Warner-Lambert Company LLC | 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 calcium salt (2:1) (atorvastatin) |
| WO2003018547A2 (en) * | 2001-08-31 | 2003-03-06 | Morepen Laboratories Ltd. | An improved process for the preparation of amorphous atorvastatin calcium salt (2:1) |
| UA77990C2 (en) * | 2001-12-12 | 2007-02-15 | Crystalline calcium salt of (2:1) [r-(r*,r*)]-2-(4-fluorophenyl)-?,?-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1h-pyrroleheptanic acid | |
| CZ296967B6 (cs) * | 2002-02-01 | 2006-08-16 | Zentiva, A.S. | Zpusob výroby amorfní formy hemivápenaté soli (3R,5R) 7-[3-fenyl-4-fenylkarbamoyl-2-(4-fluorfenyl)-5-isopropylpyrrol-1-yl]-3,5-dihydroxyheptanové kyseliny (atorvastatinu) |
| ITMI20020907A1 (it) * | 2002-04-29 | 2003-10-29 | Chemi Spa | Processo di preparazione della forma amorfa del sale di calcio della atorvastatina |
| AU2002356423A1 (en) * | 2002-05-28 | 2003-12-12 | Cadila Healthcare Limited | Process for the preparation of amorphous atorvastatin calcium |
| US8367848B2 (en) | 2003-04-11 | 2013-02-05 | Lek Pharmaceuticals D.D. | Process for the preparation of amorphous calcium salt of atorvastatin |
| JP5207432B2 (ja) * | 2003-04-29 | 2013-06-12 | エム・エス・ディー・オス・ベー・フェー | アンチ溶媒凝固プロセス |
| US7790197B2 (en) | 2003-06-09 | 2010-09-07 | Warner-Lambert Company Llc | Pharmaceutical compositions of atorvastatin |
| US20050271717A1 (en) | 2003-06-12 | 2005-12-08 | Alfred Berchielli | Pharmaceutical compositions of atorvastatin |
| US7655692B2 (en) | 2003-06-12 | 2010-02-02 | Pfizer Inc. | Process for forming amorphous atorvastatin |
| CA2456430A1 (en) * | 2004-01-28 | 2005-07-28 | Brantford Chemicals Inc. | Improved process for the preparation of amorphous atorvastatin calcium |
| CZ298382B6 (cs) * | 2004-03-10 | 2007-09-12 | Zentiva, A. S. | Zpusob prípravy amorfní formy hemivápenaté soli atorvastatinu a její stabilizace |
| SI1727795T1 (sl) | 2004-03-17 | 2012-05-31 | Ranbaxy Lab Ltd | Postopek za pripravo atorvastatin kalcija v amorfni obliki |
| US7241800B2 (en) * | 2004-03-17 | 2007-07-10 | Mai De Ltd. | Anhydrous amorphous form of fluvastatin sodium |
| CA2562844A1 (en) * | 2004-04-16 | 2005-10-27 | Pfizer Products Inc. | Process for forming amorphous atorvastatin calcium |
| EP1745020A2 (en) | 2004-05-05 | 2007-01-24 | Pfizer Products Incorporated | Salt forms of atorvastatin |
| RU2412191C2 (ru) * | 2004-07-16 | 2011-02-20 | Лек Фармасьютиклз Д.Д. | Продукты окислительной деструкции кальций аторвастатина |
| MX2007000765A (es) | 2004-07-20 | 2007-03-28 | Warner Lambert Co | Formas cristalinas de sal de calcio del acido (r-(r*, r*))-2- (4-fluorofenil)- beta,gama- dihidroxi-5- (1-metiletil)-3 -fenil-4-((fenilamino) (carbonil)-1ih -pirrol-1- heptanoico (2:1). |
| 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 |
| MX2007004425A (es) * | 2004-10-18 | 2007-06-07 | Teva Pharma | Proceso para preparar hemi-calcio de atorvastatina amorfo disolviendo la sal en un solvente organico que es una mezcla de un alcohol y una cetona y/o un ester y removiendo el solvente. |
| KR20070067175A (ko) * | 2004-10-28 | 2007-06-27 | 워너-램버트 캄파니 엘엘씨 | 무정형 아토르바스타틴 형성 방법 |
| WO2006048888A1 (en) * | 2004-11-01 | 2006-05-11 | Jubilant Organosys Limited | Novel process for the preparation of amorphous atorvastatin calcium salt |
| CA2588216A1 (en) | 2004-11-22 | 2006-05-26 | Dexcel Pharma Technologies Ltd. | Stable atorvastatin formulations |
| WO2007052296A2 (en) * | 2005-08-23 | 2007-05-10 | Kopran Research Laboratories Ltd | A process of preparing amorphous atorvastatin calcium |
| US20090216029A1 (en) * | 2005-09-16 | 2009-08-27 | Yatendra Kumar | Process for the production of atorvastatin calcium in amorphous form |
| CA2547216A1 (en) | 2005-09-21 | 2007-03-21 | Renuka D. Reddy | Process for annealing amorphous atorvastatin |
| 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 |
| US20100113802A1 (en) * | 2006-11-02 | 2010-05-06 | Cadila Pharmaceuticals Limited | Process for preparing amorphous atorvastatin hemi calcium salt and its itermediate |
| US7834195B2 (en) | 2007-01-24 | 2010-11-16 | Apotex Pharmachem Inc. | Atorvastatin calcium propylene glycol solvates |
| EP2182925A2 (en) * | 2007-07-27 | 2010-05-12 | Cipla Limited | Pharmaceutical compositions and process for making them |
| EP2075246A1 (en) | 2007-12-27 | 2009-07-01 | M. J. Institute of Research | A process for preparation of amorphous form of atorvastatin hemi-calcium salt |
| CN101684090B (zh) * | 2008-09-27 | 2012-12-05 | 广东东阳光药业有限公司 | 一种制备无定形阿托伐他汀钙的方法 |
| US8115015B2 (en) | 2009-01-26 | 2012-02-14 | Cadila Healthcare Limited | Process for the preparation of amorphous atorvastatin calcium |
| CZ201039A3 (cs) | 2010-01-19 | 2011-07-27 | Zentiva, K. S | Zpusob prumyslové výroby amorfní formy hemivápenaté soli (3R,5R) 7-[3-fenyl-4-fenylkarbamoyl-2-(4-fluorfenyl)-5-isopropylpyrrol-1-yl]-3,5-dihydroxyheptanové kyseliny (atorvastatinu) s vysokým specifickým povrchem a jeho použití v lékové forme |
| HUP1000299A2 (hu) | 2010-06-08 | 2012-02-28 | Nanoform Cardiovascular Therapeutics Ltd | Nanostrukturált Atorvastatint, gyógyszerészetileg elfogadott sóit és kokristályait tartalmazó készítmény és eljárás elõállításukra |
| US10138206B2 (en) * | 2014-10-09 | 2018-11-27 | Glenmark Pharmaceuticals Limited | Amorphous form of lomitapide mesylate |
Family Cites Families (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| YU44680B (en) | 1982-07-30 | 1990-12-31 | Glaxo Lab Ltd | Process for obtaining very pure amorphous form of cephuroxim axetile |
| 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 |
| 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 |
| 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 |
| 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 |
| HRP960312B1 (en) * | 1995-07-17 | 2001-10-31 | Warner Lambert Co | NOVEL PROCESS FOR THE PRODUCTION OF AMORPHOUS /R-(R*, R*)/-2-(4-FLUOROPHENYL)-"beta", "delta"-DIHYDROXY-5-PHENYL-4-/(PHENYLAMINO)CARBONYL/-1H-PYRROLE -1-HEPTANOIC ACID CALCIUM SALT (2 : 1) |
| DE69634054T2 (de) * | 1995-07-17 | 2005-12-08 | Warner-Lambert Co. | Kristalline (R-(R*, R*))-2-(4-Fluorophenyl)-β, δ-Dihydroxy-5-(1-Methylethyl)-3-Phenyl-4-((Phenylamino)Carbonyl)-1H-Pyrrol-1-Heptancarbonsäure Hemi Calcium Salz (Atorvastatin) |
| 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) |
| SI20425A (sl) * | 1999-12-10 | 2001-06-30 | LEK tovarna farmacevtskih in kemi�nih izdelkov d.d. | Priprava amorfnega atorvastatina |
-
1999
- 1999-05-25 IN IN775DE1999 patent/IN191236B/en unknown
-
2000
- 2000-01-06 EP EP00900300A patent/EP1185264B1/en not_active Expired - Lifetime
- 2000-01-06 WO PCT/IB2000/000014 patent/WO2000071116A1/en not_active Ceased
- 2000-01-06 DK DK00900300T patent/DK1185264T3/da active
- 2000-01-06 CN CNB008080275A patent/CN1196679C/zh not_active Expired - Fee Related
- 2000-01-06 AT AT00900300T patent/ATE362759T1/de active
- 2000-01-06 CN CNA2005100525833A patent/CN1680315A/zh active Pending
- 2000-01-06 HK HK02106699.9A patent/HK1045118A1/zh unknown
- 2000-01-06 DE DE60034946T patent/DE60034946T2/de not_active Expired - Lifetime
- 2000-01-06 AU AU19967/00A patent/AU778962B2/en not_active Ceased
- 2000-01-06 PT PT00900300T patent/PT1185264E/pt unknown
- 2000-01-06 BR BR0010923-1A patent/BR0010923A/pt not_active IP Right Cessation
- 2000-01-06 ES ES00900300T patent/ES2284472T3/es not_active Expired - Lifetime
- 2000-01-06 US US09/979,475 patent/US6528660B1/en not_active Expired - Lifetime
- 2000-05-24 MY MYPI20002283A patent/MY133511A/en unknown
-
2001
- 2001-11-23 ZA ZA200109656A patent/ZA200109656B/en unknown
-
2003
- 2003-03-03 US US10/378,574 patent/US20030149279A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| DK1185264T3 (da) | 2007-08-20 |
| ES2284472T3 (es) | 2007-11-16 |
| AU1996700A (en) | 2000-12-12 |
| MY133511A (en) | 2007-11-30 |
| EP1185264A1 (en) | 2002-03-13 |
| ATE362759T1 (de) | 2007-06-15 |
| BR0010923A (pt) | 2002-07-16 |
| PT1185264E (pt) | 2007-07-10 |
| US20030149279A1 (en) | 2003-08-07 |
| CN1351493A (zh) | 2002-05-29 |
| EP1185264B1 (en) | 2007-05-23 |
| AU778962B2 (en) | 2004-12-23 |
| DE60034946D1 (de) | 2007-07-05 |
| IN191236B (enExample) | 2003-10-11 |
| DE60034946T2 (de) | 2008-01-17 |
| WO2000071116A1 (en) | 2000-11-30 |
| ZA200109656B (en) | 2002-06-27 |
| CN1680315A (zh) | 2005-10-12 |
| US6528660B1 (en) | 2003-03-04 |
| HK1045118A1 (zh) | 2002-11-15 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C14 | Grant of patent or utility model | ||
| GR01 | Patent grant | ||
| CF01 | Termination of patent right due to non-payment of annual fee |
Granted publication date: 20050413 Termination date: 20130106 |
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| CF01 | Termination of patent right due to non-payment of annual fee |