BR0010923A - Processo para a produção de atorvastatina de cálcio amorfa - Google Patents
Processo para a produção de atorvastatina de cálcio amorfaInfo
- Publication number
 - BR0010923A BR0010923A BR0010923-1A BR0010923A BR0010923A BR 0010923 A BR0010923 A BR 0010923A BR 0010923 A BR0010923 A BR 0010923A BR 0010923 A BR0010923 A BR 0010923A
 - Authority
 - BR
 - Brazil
 - Prior art keywords
 - atorvastatin
 - solvent
 - calcium
 - production
 - atorvastatin calcium
 - Prior art date
 
Links
- OJRHUICOVVSGSY-RXMQYKEDSA-N (2s)-2-chloro-3-methylbutan-1-ol Chemical compound CC(C)[C@H](Cl)CO OJRHUICOVVSGSY-RXMQYKEDSA-N 0.000 title abstract 3
 - 229960001770 atorvastatin calcium Drugs 0.000 title abstract 3
 - 238000000034 method Methods 0.000 title abstract 3
 - 238000004519 manufacturing process Methods 0.000 title abstract 2
 - XUKUURHRXDUEBC-KAYWLYCHSA-N Atorvastatin Chemical compound C=1C=CC=CC=1C1=C(C=2C=CC(F)=CC=2)N(CC[C@@H](O)C[C@@H](O)CC(O)=O)C(C(C)C)=C1C(=O)NC1=CC=CC=C1 XUKUURHRXDUEBC-KAYWLYCHSA-N 0.000 abstract 2
 - XUKUURHRXDUEBC-UHFFFAOYSA-N Atorvastatin Natural products C=1C=CC=CC=1C1=C(C=2C=CC(F)=CC=2)N(CCC(O)CC(O)CC(O)=O)C(C(C)C)=C1C(=O)NC1=CC=CC=C1 XUKUURHRXDUEBC-UHFFFAOYSA-N 0.000 abstract 2
 - 239000012296 anti-solvent Substances 0.000 abstract 2
 - 229960005370 atorvastatin Drugs 0.000 abstract 2
 - BWFCZHDTTAYGNN-CNZCJKERSA-N calcium;(3r,5r)-7-[2-(4-fluorophenyl)-3-phenyl-4-(phenylcarbamoyl)-5-propan-2-ylpyrrol-1-yl]-3,5-dihydroxyheptanoic acid Chemical compound [Ca].C=1C=CC=CC=1C1=C(C=2C=CC(F)=CC=2)N(CC[C@@H](O)C[C@@H](O)CC(O)=O)C(C(C)C)=C1C(=O)NC1=CC=CC=C1 BWFCZHDTTAYGNN-CNZCJKERSA-N 0.000 abstract 2
 - 239000002904 solvent Substances 0.000 abstract 2
 - 238000004090 dissolution Methods 0.000 abstract 1
 - 238000001914 filtration Methods 0.000 abstract 1
 - 150000004677 hydrates Chemical class 0.000 abstract 1
 - 238000002360 preparation method Methods 0.000 abstract 1
 
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
 
 
Landscapes
- 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 (en:Method) | 1999-05-25 | 1999-05-25 | |
| PCT/IB2000/000014 WO2000071116A1 (en) | 1999-05-25 | 2000-01-06 | Process for the production of amorphous atorvastatin calcium | 
Publications (1)
| Publication Number | Publication Date | 
|---|---|
| BR0010923A true BR0010923A (pt) | 2002-07-16 | 
Family
ID=11091180
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date | 
|---|---|---|---|
| BR0010923-1A BR0010923A (pt) | 1999-05-25 | 2000-01-06 | Processo para a produção de atorvastatina de cálcio amorfa | 
Country Status (15)
| Country | Link | 
|---|---|
| US (2) | US6528660B1 (en:Method) | 
| EP (1) | EP1185264B1 (en:Method) | 
| CN (2) | CN1196679C (en:Method) | 
| AT (1) | ATE362759T1 (en:Method) | 
| AU (1) | AU778962B2 (en:Method) | 
| BR (1) | BR0010923A (en:Method) | 
| DE (1) | DE60034946T2 (en:Method) | 
| DK (1) | DK1185264T3 (en:Method) | 
| ES (1) | ES2284472T3 (en:Method) | 
| HK (1) | HK1045118A1 (en:Method) | 
| IN (1) | IN191236B (en:Method) | 
| MY (1) | MY133511A (en:Method) | 
| PT (1) | PT1185264E (en:Method) | 
| WO (1) | WO2000071116A1 (en:Method) | 
| ZA (1) | ZA200109656B (en:Method) | 
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 | 
| 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 | 
| 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 | 
| 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 (en:Method) * | 2001-04-11 | 2003-08-09 | Cadila Heathcare Ltd | |
| HUP0400381A2 (hu) * | 2001-06-29 | 2004-09-28 | Warner-Lambert Company Llc | [R-(R*,R*)]-2-(4fluorfenil)-béta, delta-dihidroxi-5-(1-metiletil)-3-fenil-4-[(fenilamino)karbonil]-1H-pirrol-1-heptánsav 2:1 arányú kalciumsójának (atorvasztatin) kristályos formái | 
| US7563911B2 (en) | 2001-08-31 | 2009-07-21 | Morepen Laboratories Ltd. | Process for the preparation of amorphous atorvastin 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 | 
| BRPI0409292A (pt) | 2003-04-11 | 2006-04-11 | Lek Pharmaceuticals | processo para a preparação de sal de cálcio amorfo de atorvastatina | 
| CN100434133C (zh) * | 2003-04-29 | 2008-11-19 | 欧加农股份有限公司 | 反溶剂凝固方法 | 
| 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 | 
| EP1727795B1 (en) | 2004-03-17 | 2012-02-15 | Ranbaxy Laboratories Limited | Process for the production of atorvastatin calcium in amorphous form | 
| US7241800B2 (en) * | 2004-03-17 | 2007-07-10 | Mai De Ltd. | Anhydrous amorphous form of fluvastatin sodium | 
| RU2330840C1 (ru) * | 2004-04-16 | 2008-08-10 | Пфайзер Продактс Инк. | Способ получения аморфного кальций аторвастатина | 
| JP2007536373A (ja) | 2004-05-05 | 2007-12-13 | ファイザー・プロダクツ・インク | アトルバスタチンの塩形態 | 
| HUE029911T2 (en) * | 2004-07-16 | 2017-04-28 | Lek Pharmaceuticals | Products of atorvastatin calcium oxidative degradation | 
| JP2008506764A (ja) | 2004-07-20 | 2008-03-06 | ワーナー−ランバート カンパニー リミテッド ライアビリティー カンパニー | [R−(R*,R*)]−2−(4−フルオロフェニル)−β、δ−ジヒドロキシ−5−(1−メチルエチル)−3−フェニル−4−[(フェニルアミノ)カルボニル]−1H−ピロール−1−ヘプタン酸カルシウム塩(2:1)の新規形態 | 
| EP1784389A4 (en) | 2004-08-27 | 2009-03-25 | Biocon Ltd | PROCESS FOR THE PREPARATION OF AMORPHIC ATORVASTATIN CALCIUM | 
| CN101039906A (zh) * | 2004-10-18 | 2007-09-19 | 特瓦制药工业有限公司 | 通过将盐溶解于有机溶剂并除去该溶剂来制备无定形阿托伐他汀半钙的方法,所述有机溶剂为醇和酮和 /或酯的混合物 | 
| CN101048141A (zh) * | 2004-10-28 | 2007-10-03 | 沃尼尔·朗伯有限责任公司 | 形成非晶形的阿托伐他汀的方法 | 
| WO2006048888A1 (en) * | 2004-11-01 | 2006-05-11 | Jubilant Organosys Limited | Novel process for the preparation of amorphous atorvastatin calcium salt | 
| WO2006054308A2 (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 | 
| 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. | 
| 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 | 
| JP2010534644A (ja) * | 2007-07-27 | 2010-11-11 | シプラ・リミテッド | 医薬組成物およびその製造方法 | 
| 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 | 
| WO2016055934A1 (en) * | 2014-10-09 | 2016-04-14 | 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 | 
| 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 | 
| 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 | 
| 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 | 
| 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 | 
| WO1997003959A1 (en) * | 1995-07-17 | 1997-02-06 | Warner-Lambert Company | Crystalline [r-(r*,r*)]-2-(4-fluorophenyl)-beta,delta-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1h-pyrrole-1-heptanoic acid hemi calcium salt (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) | 
| 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) | 
| 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 AT AT00900300T patent/ATE362759T1/de active
 - 2000-01-06 DE DE60034946T patent/DE60034946T2/de not_active Expired - Lifetime
 - 2000-01-06 CN CNB008080275A patent/CN1196679C/zh not_active Expired - Fee Related
 - 2000-01-06 HK HK02106699.9A patent/HK1045118A1/zh unknown
 - 2000-01-06 ES ES00900300T patent/ES2284472T3/es not_active Expired - Lifetime
 - 2000-01-06 PT PT00900300T patent/PT1185264E/pt unknown
 - 2000-01-06 AU AU19967/00A patent/AU778962B2/en not_active Ceased
 - 2000-01-06 CN CNA2005100525833A patent/CN1680315A/zh active Pending
 - 2000-01-06 WO PCT/IB2000/000014 patent/WO2000071116A1/en active IP Right Grant
 - 2000-01-06 BR BR0010923-1A patent/BR0010923A/pt not_active IP Right Cessation
 - 2000-01-06 DK DK00900300T patent/DK1185264T3/da active
 - 2000-01-06 US US09/979,475 patent/US6528660B1/en not_active Expired - Lifetime
 - 2000-01-06 EP EP00900300A patent/EP1185264B1/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 | 
|---|---|
| ZA200109656B (en) | 2002-06-27 | 
| US6528660B1 (en) | 2003-03-04 | 
| US20030149279A1 (en) | 2003-08-07 | 
| AU778962B2 (en) | 2004-12-23 | 
| EP1185264B1 (en) | 2007-05-23 | 
| EP1185264A1 (en) | 2002-03-13 | 
| ES2284472T3 (es) | 2007-11-16 | 
| HK1045118A1 (zh) | 2002-11-15 | 
| WO2000071116A1 (en) | 2000-11-30 | 
| MY133511A (en) | 2007-11-30 | 
| DE60034946T2 (de) | 2008-01-17 | 
| CN1680315A (zh) | 2005-10-12 | 
| DK1185264T3 (da) | 2007-08-20 | 
| DE60034946D1 (de) | 2007-07-05 | 
| IN191236B (en:Method) | 2003-10-11 | 
| CN1196679C (zh) | 2005-04-13 | 
| ATE362759T1 (de) | 2007-06-15 | 
| CN1351493A (zh) | 2002-05-29 | 
| AU1996700A (en) | 2000-12-12 | 
| PT1185264E (pt) | 2007-07-10 | 
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Legal Events
| Date | Code | Title | Description | 
|---|---|---|---|
| B07A | Application suspended after technical examination (opinion) [chapter 7.1 patent gazette] | ||
| B09B | Patent application refused [chapter 9.2 patent gazette] | 
             Free format text: INDEFIRO O PEDIDO DE ACORDO COM O(S) ARTIGO(S) 8O, 13, 24 E 25 DA LPI.  | 
        |
| B12B | Appeal against refusal [chapter 12.2 patent gazette] | ||
| B08F | Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette] | 
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