YU36802A - Postupak za dobijanje amorfnog atorvastatina - Google Patents
Postupak za dobijanje amorfnog atorvastatinaInfo
- Publication number
- YU36802A YU36802A YU36802A YUP36802A YU36802A YU 36802 A YU36802 A YU 36802A YU 36802 A YU36802 A YU 36802A YU P36802 A YUP36802 A YU P36802A YU 36802 A YU36802 A YU 36802A
- Authority
- YU
- Yugoslavia
- Prior art keywords
- atorvastatin
- solvent
- preparation
- type
- amorphous form
- Prior art date
Links
- 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 title abstract 7
- 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 title abstract 7
- 229960005370 atorvastatin Drugs 0.000 title abstract 7
- 238000000034 method Methods 0.000 title abstract 2
- 239000002904 solvent Substances 0.000 abstract 2
- 239000000126 substance Substances 0.000 abstract 2
- 159000000007 calcium salts Chemical class 0.000 abstract 1
- 238000006243 chemical reaction Methods 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- 230000001376 precipitating effect Effects 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
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Diabetes (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Hematology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Engineering & Computer Science (AREA)
- Public Health (AREA)
- Obesity (AREA)
- Pyrrole Compounds (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
Atorvastatin, supstanca poznata po hemijskom nazivu hemi kalcijumova so [R-(R*,R*)]-2-(4-fluorofenil)-Гџ,δ-dihidroksi-5-(1-metiletil)-3-fenil-4-[(fenilamino)karbonil]-1H-pirol-1-heptanske kiseline, jednostavno se može dobaviti u nekom od svojih kristalnih oblika, kao što je poznato iz prethodne prakse. Ovaj pronalazak se odnosi na novi postupak za proizvodnju atorvastatina u amorfnom obliku taloženjem atorvastatina upotrebom rastvarača drugog tipa iz rastvora atorvastatina, koji se dobija sa rastvaračem prvog tipa. Ovaj postupak je koristan za prevodjenje atorvastatina, koji je u kristalnom obliku u atorvastatin, koji je u amorfnom obliku.[Atorvastatin, the substance known by the chemical name [R-(R*,R*)]-2-(4-fluorophenyl)-Гџ,δ-dihydroxy-5-(1-methylethyl)-3-phenyl-4- [(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid hemi calcium salt, is readily available in one of its crystalline forms as it is known from the prior art. The present invention relates to a novel process for preparing atorvastatin in an amorphous form by precipitating the atorvastatin using a solvent of a second type from a solution of atorvastatin which is provided with a solvent of a first type. This process is useful for the conversion of atorvastatin in a crystalline form into atorvastatin in an amorphous form.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| SI9900271A SI20425A (sl) | 1999-12-10 | 1999-12-10 | Priprava amorfnega atorvastatina |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| YU36802A true YU36802A (sh) | 2005-09-19 |
| RS50307B RS50307B (sr) | 2009-09-08 |
Family
ID=20432564
Country Status (22)
| Country | Link |
|---|---|
| US (2) | US6613916B2 (sh) |
| EP (1) | EP1237864B1 (sh) |
| JP (1) | JP5087193B2 (sh) |
| KR (1) | KR100729689B1 (sh) |
| AT (1) | ATE270661T1 (sh) |
| AU (1) | AU776854B2 (sh) |
| BG (1) | BG65719B1 (sh) |
| CA (1) | CA2392025C (sh) |
| CZ (1) | CZ301627B6 (sh) |
| DE (1) | DE60012045T2 (sh) |
| EE (1) | EE05328B1 (sh) |
| ES (1) | ES2223615T3 (sh) |
| HR (1) | HRP20020482B1 (sh) |
| PL (1) | PL208226B1 (sh) |
| PT (1) | PT1237864E (sh) |
| RS (1) | RS50307B (sh) |
| RU (1) | RU2247113C2 (sh) |
| SI (1) | SI20425A (sh) |
| SK (1) | SK287032B6 (sh) |
| TR (1) | TR200402543T4 (sh) |
| UA (1) | UA71041C2 (sh) |
| WO (1) | WO2001042209A1 (sh) |
Families Citing this family (50)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IN191236B (sh) * | 1999-05-25 | 2003-10-11 | Ranbaxy Lab Ltd | |
| 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 |
| WO2002057229A1 (en) | 2001-01-19 | 2002-07-25 | Biocon India Limited | FORM V CRYSTALLINE [R-(R*,R*)]-2-(4-FLUOROPHENYL)-ß,$G(D)-DIHYDROXY-5-(1-METHYLETHYL)-3-PHENYL-4-[(PHENYLAMINO)CARBONYL]-1H-PYRROLE-1- HEPTANOIC ACID HEMI CALCIUM SALT. (ATORVASTATIN) |
| SI20848A (sl) | 2001-03-14 | 2002-10-31 | Lek, Tovarna Farmacevtskih In Kemijskih Izdelkov, D.D. | Farmacevtska formulacija, ki vsebuje atorvastatin kalcij |
| IN190564B (sh) * | 2001-04-11 | 2003-08-09 | Cadila Heathcare Ltd | |
| BR0210666A (pt) | 2001-06-29 | 2004-10-05 | Warner Lambert Co | Formas cristalinas do sal de cálcio do ácido [r-(r*,r*)]-2-(4-fluorofenil)-beta, delta-dihidróxi-5-(1-metiletil)-3-fenil-4-[(fenilamino)c arbonil]-1h-pirrol-1-heptanóico (2:1) (atorvastatina) |
| US7563911B2 (en) * | 2001-08-31 | 2009-07-21 | Morepen Laboratories Ltd. | Process for the preparation of amorphous atorvastin calcium salt (2:1) |
| 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) |
| HUP0500074A3 (en) | 2002-03-18 | 2005-07-28 | Biocon Ltd Bangalore | Amorphous hmg-coa reductase inhibitors of desired particle size and process for producing them |
| RU2309141C2 (ru) * | 2002-03-18 | 2007-10-27 | Байокон Лимитид | АМОРФНЫЕ ИНГИБИТОРЫ ГМГ-КоА-РЕДУКТАЗЫ И СПОСОБ ИХ ПОЛУЧЕНИЯ |
| ITMI20020907A1 (it) * | 2002-04-29 | 2003-10-29 | Chemi Spa | Processo di preparazione della forma amorfa del sale di calcio della atorvastatina |
| WO2003099785A1 (en) * | 2002-05-28 | 2003-12-04 | Cadila Healthcare Limited | Process for the preparation of amorphous atorvastatin calcium |
| HU227041B1 (en) * | 2003-03-24 | 2010-05-28 | Richter Gedeon Nyrt | Process for the synthesis of amorphous atorvastatin calcium |
| AU2004228607B2 (en) * | 2003-04-11 | 2011-01-27 | Lek Pharmaceuticals D.D. | Process for the preparation of amorphous calcium salt of atorvastatin |
| US7790197B2 (en) | 2003-06-09 | 2010-09-07 | Warner-Lambert Company Llc | Pharmaceutical compositions of atorvastatin |
| US7655692B2 (en) * | 2003-06-12 | 2010-02-02 | Pfizer Inc. | Process for forming amorphous atorvastatin |
| US20050271717A1 (en) | 2003-06-12 | 2005-12-08 | Alfred Berchielli | Pharmaceutical compositions of atorvastatin |
| US8987322B2 (en) * | 2003-11-04 | 2015-03-24 | Circ Pharma Research And Development Limited | Pharmaceutical formulations for carrier-mediated transport statins and uses thereof |
| CA2456430A1 (en) * | 2004-01-28 | 2005-07-28 | Brantford Chemicals Inc. | Improved process for the preparation of amorphous atorvastatin calcium |
| WO2005090301A1 (en) * | 2004-03-17 | 2005-09-29 | Ranbaxy Laboratories Limited | Crystalline form of atorvastatin hemi calcium |
| WO2005092852A1 (en) * | 2004-03-17 | 2005-10-06 | Ranbaxy Laboratories Limited | Process for the production of atorvastatin calcium in amorphous form |
| CN1960972A (zh) * | 2004-04-16 | 2007-05-09 | 辉瑞产品公司 | 用于形成无定形阿托伐它汀钙的方法 |
| CA2649054A1 (en) | 2004-05-05 | 2005-11-10 | Pfizer Products Inc. | Salt forms of [r-(r*,r*)]-2-(4-fluorophenyl)-.beta., .delta.-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1h-pyrrole-1-heptanoic acid |
| CA2573969C (en) * | 2004-07-16 | 2014-02-04 | Lek Pharmaceuticals D.D. | Oxidative degradation products of atorvastatin calcium |
| 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 |
| 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 |
| WO2006046109A1 (en) | 2004-10-28 | 2006-05-04 | Warner-Lambert Company Llc | Process for forming amorphous atorvastatin |
| WO2006048888A1 (en) * | 2004-11-01 | 2006-05-11 | Jubilant Organosys Limited | Novel process for the preparation of amorphous atorvastatin calcium salt |
| WO2006048893A2 (en) * | 2004-11-05 | 2006-05-11 | Morepen Laboratories Limited | A process for synthesis of large particle size statin compounds |
| ES2263370B1 (es) * | 2005-02-16 | 2007-12-01 | Ercros Industrial, S.A. | Atorvastatina calcica amorfa estabilizada y procedimiento para su obtencion. |
| 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 |
| ATE466840T1 (de) | 2005-11-21 | 2010-05-15 | Warner Lambert Co | Neue formen von är-(r*,r*)ü-2-(4-fluorphenyl)-b,d-dihydroxy-5-( -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 |
| EP1905424A3 (en) * | 2006-02-02 | 2008-04-30 | Ranbaxy Laboratories Limited | Process for the preparation of a pharmaceutical composition comprising stabilized statin particles |
| CN100429202C (zh) * | 2006-06-30 | 2008-10-29 | 浙江新东港药业股份有限公司 | 一种无定形氟伐他汀钠的制备方法 |
| WO2008053312A2 (en) * | 2006-11-02 | 2008-05-08 | Cadila Pharmaceuticals Limited | Process for preparing amorphous atorvastatin hemi calcium salt and its intermediate |
| KR100833439B1 (ko) * | 2007-01-02 | 2008-05-29 | 씨제이제일제당 (주) | 비결정형 아토르바스타틴 칼슘의 개선된 제조방법 |
| JP2010520273A (ja) * | 2007-03-02 | 2010-06-10 | ドン・ア・ファーム・カンパニー・リミテッド | ピロリルヘプタン酸誘導体の新規な結晶形態 |
| WO2009007856A2 (en) * | 2007-07-11 | 2009-01-15 | Actavis Group Ptc Ehf | Novel polymorph of atorvastatin calcium and use thereof for the preparation of amorphous atorvastatin calcium |
| 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 |
| WO2010066846A2 (en) * | 2008-12-11 | 2010-06-17 | Dsm Ip Assets B.V. | Method for the isolation of atorvastatin |
| JP5414884B2 (ja) * | 2009-03-30 | 2014-02-12 | ボエグリ − グラビュル ソシエテ アノニム | 硬質材料をコーティングした物体の表面をレーザーによって構造化する方法及び装置 |
| 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 |
| US9951009B2 (en) * | 2013-08-29 | 2018-04-24 | Cadila Healthcare Limited | Polymorphic form of pyrrole derivative and intermediate thereof |
| CN106432033B (zh) * | 2016-10-21 | 2018-07-27 | 江苏阿尔法药业有限公司 | 一种无定形阿托伐他汀钙的制备方法 |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| ATE123020T1 (de) * | 1990-05-11 | 1995-06-15 | American Cyanamid Co | N-acylierte arylpyrrole als insektizide, akarizide, nematizide und molluskizide wirkstoffe. |
| US5385929A (en) * | 1994-05-04 | 1995-01-31 | Warner-Lambert Company | [(Hydroxyphenylamino) carbonyl] pyrroles |
| 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) |
| 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) |
| 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) |
| IN191236B (sh) * | 1999-05-25 | 2003-10-11 | Ranbaxy Lab Ltd | |
| HU226640B1 (en) * | 1999-10-18 | 2009-05-28 | Egis Gyogyszergyar Nyilvanosan | Process for producing amorphous atorvastatin calcium salt |
| SI20425A (sl) * | 1999-12-10 | 2001-06-30 | LEK tovarna farmacevtskih in kemi�nih izdelkov d.d. | Priprava amorfnega atorvastatina |
-
1999
- 1999-12-10 SI SI9900271A patent/SI20425A/sl not_active IP Right Cessation
-
2000
- 2000-05-12 UA UA2002054418A patent/UA71041C2/uk unknown
- 2000-12-05 AT AT00977807T patent/ATE270661T1/de active
- 2000-12-05 AU AU15438/01A patent/AU776854B2/en not_active Ceased
- 2000-12-05 ES ES00977807T patent/ES2223615T3/es not_active Expired - Lifetime
- 2000-12-05 RU RU2002115272/04A patent/RU2247113C2/ru not_active IP Right Cessation
- 2000-12-05 JP JP2001543510A patent/JP5087193B2/ja not_active Expired - Fee Related
- 2000-12-05 EE EEP200200293A patent/EE05328B1/xx not_active IP Right Cessation
- 2000-12-05 WO PCT/IB2000/001797 patent/WO2001042209A1/en not_active Ceased
- 2000-12-05 KR KR1020027007167A patent/KR100729689B1/ko not_active Expired - Fee Related
- 2000-12-05 RS YUP-368/02A patent/RS50307B/sr unknown
- 2000-12-05 SK SK783-2002A patent/SK287032B6/sk not_active IP Right Cessation
- 2000-12-05 DE DE60012045T patent/DE60012045T2/de not_active Expired - Lifetime
- 2000-12-05 TR TR2004/02543T patent/TR200402543T4/xx unknown
- 2000-12-05 CA CA002392025A patent/CA2392025C/en not_active Expired - Fee Related
- 2000-12-05 PT PT00977807T patent/PT1237864E/pt unknown
- 2000-12-05 EP EP00977807A patent/EP1237864B1/en not_active Expired - Lifetime
- 2000-12-05 PL PL356184A patent/PL208226B1/pl unknown
- 2000-12-05 HR HR20020482A patent/HRP20020482B1/xx not_active IP Right Cessation
- 2000-12-05 CZ CZ20021838A patent/CZ301627B6/cs not_active IP Right Cessation
- 2000-12-05 US US10/149,348 patent/US6613916B2/en not_active Expired - Lifetime
-
2002
- 2002-06-07 BG BG106786A patent/BG65719B1/bg unknown
-
2003
- 2003-07-07 US US10/614,534 patent/US6891047B2/en not_active Expired - Fee Related
Also Published As
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