KR20040081172A - (3알,5알)7-3-페닐-4-페닐카바모일-2-(4-플로로페닐)-5-이소프로필-피롤-1-일!-3,5-디하이드록시헵타노익산(아토르바스타틴)의 반칼슘염의 무정형 제조 방법 - Google Patents
(3알,5알)7-3-페닐-4-페닐카바모일-2-(4-플로로페닐)-5-이소프로필-피롤-1-일!-3,5-디하이드록시헵타노익산(아토르바스타틴)의 반칼슘염의 무정형 제조 방법 Download PDFInfo
- Publication number
- KR20040081172A KR20040081172A KR10-2004-7011960A KR20047011960A KR20040081172A KR 20040081172 A KR20040081172 A KR 20040081172A KR 20047011960 A KR20047011960 A KR 20047011960A KR 20040081172 A KR20040081172 A KR 20040081172A
- Authority
- KR
- South Korea
- Prior art keywords
- salt
- isopropyl
- fluorophenyl
- phenyl
- solution
- 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.)
- Withdrawn
Links
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
- C07D207/32—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 only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
- C07D207/33—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 only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms with substituted hydrocarbon radicals, directly attached to ring carbon atoms
- C07D207/337—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F3/00—Compounds containing elements of Groups 2 or 12 of the Periodic Table
- C07F3/04—Calcium compounds
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Pyrrole Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CZ20020413A CZ296967B6 (cs) | 2002-02-01 | 2002-02-01 | 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) |
| CZPV2002-413 | 2002-02-01 | ||
| PCT/CZ2003/000007 WO2003068739A1 (en) | 2002-02-01 | 2003-01-30 | Method of manufacturing an amorphous form of the hemi-calcium salt of (3r, 5r) 7- 3-phenyl-4-phenylcarbamoyl-2-(4-fluorophenyl)-5-isopropyl-pyrrol-1-yl!-3, 5-dihydroxyheptanoic acid (atorvastatin) |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| KR20040081172A true KR20040081172A (ko) | 2004-09-20 |
Family
ID=27674298
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR10-2004-7011960A Withdrawn KR20040081172A (ko) | 2002-02-01 | 2003-01-30 | (3알,5알)7-3-페닐-4-페닐카바모일-2-(4-플로로페닐)-5-이소프로필-피롤-1-일!-3,5-디하이드록시헵타노익산(아토르바스타틴)의 반칼슘염의 무정형 제조 방법 |
Country Status (15)
| Country | Link |
|---|---|
| US (1) | US7208608B2 (https=) |
| EP (1) | EP1470106B1 (https=) |
| JP (1) | JP2005521685A (https=) |
| KR (1) | KR20040081172A (https=) |
| AT (1) | ATE480516T1 (https=) |
| AU (1) | AU2003213986A1 (https=) |
| CZ (1) | CZ296967B6 (https=) |
| DE (1) | DE60334068D1 (https=) |
| EA (1) | EA007432B1 (https=) |
| ES (1) | ES2347324T3 (https=) |
| HU (1) | HUP0402590A3 (https=) |
| PL (1) | PL209756B1 (https=) |
| PT (1) | PT1470106E (https=) |
| UA (1) | UA76826C2 (https=) |
| WO (1) | WO2003068739A1 (https=) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR100833439B1 (ko) * | 2007-01-02 | 2008-05-29 | 씨제이제일제당 (주) | 비결정형 아토르바스타틴 칼슘의 개선된 제조방법 |
| KR101050722B1 (ko) * | 2008-12-02 | 2011-07-21 | 대웅바이오 주식회사 | 무정형 아토르바스타틴 칼슘염의 제조방법 |
Families Citing this family (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2520740C (en) * | 2003-04-11 | 2012-06-05 | Lek Pharmaceuticals D.D. | Process for the preparation of amorphous calcium salt of atorvastatin |
| AU2003247327A1 (en) * | 2003-07-15 | 2005-01-28 | Eos Eczacibasi Ozgun Kimyasal Urunler Sanyi Ve Ticaret A.S. | Process for the preparation of amortphous atorvastatin calcium without interconversion of any crystalline form |
| ATE545629T1 (de) * | 2004-03-17 | 2012-03-15 | Ranbaxy Lab Ltd | Verfahren zur herstellung von atorvastatin- calcium in amorpher form |
| US8044086B2 (en) * | 2004-07-16 | 2011-10-25 | Lek Pharmaceuticals D.D. | Oxidative degradation products of atorvastatin calcium |
| 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 |
| CA2582087A1 (en) * | 2004-10-18 | 2006-04-27 | Teva Pharmaceutical Industries Ltd. | Process for preparing amorphous atorvastatin hemi-calcium by dissolving the salt in an organic solvent which is a mixture of an alcohol and a ketone and/or an ester and removing the solvent |
| WO2006048893A2 (en) * | 2004-11-05 | 2006-05-11 | Morepen Laboratories Limited | A process for synthesis of large particle size statin compounds |
| CA2499047A1 (en) | 2005-03-01 | 2006-09-01 | Apotex Pharmachem Inc. | Process for producing atorvastatin hemicalcium |
| GB2424880A (en) * | 2005-04-06 | 2006-10-11 | Generics | Crystalline forms of atorvastatin sodium, processes for their preparation and their use in inhibiting HMG-CoA reductase |
| WO2007020413A1 (en) | 2005-08-15 | 2007-02-22 | Arrow International Limited | Crystalline and amorphous sodium atorvastatin |
| AU2006281237A1 (en) | 2005-08-15 | 2007-02-22 | Arrow International Limited | Crystalline and amorphous sodium atorvastatin |
| ES2270722B1 (es) * | 2005-09-15 | 2008-03-01 | Ercros Industrial, S.A. | Procedimiento para la obtencion de atorvastatina calcica amorfa. |
| HU227696B1 (en) * | 2006-04-13 | 2011-12-28 | Egyt Gyogyszervegyeszeti Gyar | Zinc salt of rosuvastatin, process for its preparation and pharmaceutical compositions containing it |
| US20100113802A1 (en) * | 2006-11-02 | 2010-05-06 | Cadila Pharmaceuticals Limited | Process for preparing amorphous atorvastatin hemi calcium salt and its itermediate |
| 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 |
| WO2009139730A1 (en) * | 2008-05-13 | 2009-11-19 | Ulkar Kimya San. Ve Tic. A.S. | Preparation of novel non-crystalline forms of atorvastatin calcium |
| EP2327682A1 (en) * | 2009-10-29 | 2011-06-01 | KRKA, D.D., Novo Mesto | Use of amphiphilic compounds for controlled crystallization of statins and statin intermediates |
| WO2010069593A1 (en) * | 2008-12-19 | 2010-06-24 | Krka, D. D., Novo Mesto | Use of amphiphilic compounds for controlled crystallization of statins and statin intermediates |
| 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 |
| US20130041162A1 (en) * | 2010-04-19 | 2013-02-14 | Dsm Sinochem Pharmaceuticals Netherlands B.V. | Production of atorvastatin low in ether impurities |
| CN108774164A (zh) * | 2018-05-29 | 2018-11-09 | 宣城美诺华药业有限公司 | 一种阿托伐他汀钙合成方法 |
Family Cites Families (23)
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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) |
| SI0848704T1 (en) * | 1995-07-17 | 2002-04-30 | Warner-Lambert Company | Form iii 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) |
| 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) |
| KR100389518B1 (ko) * | 1995-07-17 | 2003-11-15 | 워너-램버트 캄파니 엘엘씨 | 결정질[r-(r*,r*)]-2-(4-플루오로페닐)-베타,델타-디히드록시-5-(1-메틸에틸)-3-페닐-4-[(페닐아미노)카르보닐]-1h-피롤-1-헵탄산헤미칼슘염(아토르바스타틴) |
| IN191236B (https=) * | 1999-05-25 | 2003-10-11 | Ranbaxy Lab Ltd | |
| 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 |
| IN190564B (https=) * | 2001-04-11 | 2003-08-09 | Cadila Heathcare Ltd | |
| WO2003018547A2 (en) * | 2001-08-31 | 2003-03-06 | Morepen Laboratories Ltd. | An improved process for the preparation of amorphous atorvastatin calcium salt (2:1) |
-
2002
- 2002-02-01 CZ CZ20020413A patent/CZ296967B6/cs not_active IP Right Cessation
-
2003
- 2003-01-30 KR KR10-2004-7011960A patent/KR20040081172A/ko not_active Withdrawn
- 2003-01-30 DE DE60334068T patent/DE60334068D1/de not_active Expired - Lifetime
- 2003-01-30 EA EA200400977A patent/EA007432B1/ru not_active IP Right Cessation
- 2003-01-30 AU AU2003213986A patent/AU2003213986A1/en not_active Abandoned
- 2003-01-30 WO PCT/CZ2003/000007 patent/WO2003068739A1/en not_active Ceased
- 2003-01-30 AT AT03709588T patent/ATE480516T1/de not_active IP Right Cessation
- 2003-01-30 PL PL370495A patent/PL209756B1/pl not_active IP Right Cessation
- 2003-01-30 UA UA20040907211A patent/UA76826C2/uk unknown
- 2003-01-30 JP JP2003567871A patent/JP2005521685A/ja active Pending
- 2003-01-30 ES ES03709588T patent/ES2347324T3/es not_active Expired - Lifetime
- 2003-01-30 US US10/502,632 patent/US7208608B2/en not_active Expired - Lifetime
- 2003-01-30 PT PT03709588T patent/PT1470106E/pt unknown
- 2003-01-30 HU HU0402590A patent/HUP0402590A3/hu unknown
- 2003-01-30 EP EP03709588A patent/EP1470106B1/en not_active Expired - Lifetime
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR100833439B1 (ko) * | 2007-01-02 | 2008-05-29 | 씨제이제일제당 (주) | 비결정형 아토르바스타틴 칼슘의 개선된 제조방법 |
| KR101050722B1 (ko) * | 2008-12-02 | 2011-07-21 | 대웅바이오 주식회사 | 무정형 아토르바스타틴 칼슘염의 제조방법 |
Also Published As
| Publication number | Publication date |
|---|---|
| PL209756B1 (pl) | 2011-10-31 |
| EP1470106B1 (en) | 2010-09-08 |
| CZ296967B6 (cs) | 2006-08-16 |
| US7208608B2 (en) | 2007-04-24 |
| EP1470106A1 (en) | 2004-10-27 |
| PT1470106E (pt) | 2010-09-23 |
| US20050131055A1 (en) | 2005-06-16 |
| UA76826C2 (uk) | 2006-09-15 |
| DE60334068D1 (de) | 2010-10-21 |
| JP2005521685A (ja) | 2005-07-21 |
| ES2347324T3 (es) | 2010-10-28 |
| WO2003068739A1 (en) | 2003-08-21 |
| HUP0402590A2 (hu) | 2005-03-29 |
| HUP0402590A3 (en) | 2010-06-28 |
| EA200400977A1 (ru) | 2004-12-30 |
| PL370495A1 (en) | 2005-05-30 |
| EA007432B1 (ru) | 2006-10-27 |
| CZ2002413A3 (cs) | 2003-10-15 |
| ATE480516T1 (de) | 2010-09-15 |
| AU2003213986A1 (en) | 2003-09-04 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PA0105 | International application |
Patent event date: 20040802 Patent event code: PA01051R01D Comment text: International Patent Application |
|
| PG1501 | Laying open of application | ||
| PC1203 | Withdrawal of no request for examination | ||
| WITN | Application deemed withdrawn, e.g. because no request for examination was filed or no examination fee was paid |