ATE141584T1 - Verfahren zum herstellen von simvastatin - Google Patents

Verfahren zum herstellen von simvastatin

Info

Publication number: ATE141584T1
Authority: AT; Austria
Prior art keywords: simvastatin; producing simvastatin; producing; lactone; formation
Prior art date: 1991-05-01

Application number

AT92303920T

Other languages

English (en)

Inventor

Rebecca L Dabora

Gregory L Tewalt

Original Assignee

Merck & Co Inc

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.)

1991-05-01

Filing date

1992-04-30

Publication date

1996-09-15

Family has litigation

First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=24787670&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=ATE141584(T1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.

1992-04-30 Application filed by Merck & Co Inc filed Critical Merck & Co Inc

1996-09-15 Application granted granted Critical

1996-09-15 Publication of ATE141584T1 publication Critical patent/ATE141584T1/de

Links

RYMZZMVNJRMUDD-UHFFFAOYSA-N SJ000286063 Natural products C12C(OC(=O)C(C)(C)CC)CC(C)C=C2C=CC(C)C1CCC1CC(O)CC(=O)O1 RYMZZMVNJRMUDD-UHFFFAOYSA-N 0.000 title abstract 3
RYMZZMVNJRMUDD-HGQWONQESA-N simvastatin Chemical compound C([C@H]1[C@@H](C)C=CC2=C[C@H](C)C[C@@H]([C@H]12)OC(=O)C(C)(C)CC)C[C@@H]1C[C@@H](O)CC(=O)O1 RYMZZMVNJRMUDD-HGQWONQESA-N 0.000 title abstract 3
229960002855 simvastatin Drugs 0.000 title abstract 3
238000004519 manufacturing process Methods 0.000 title 1
230000010933 acylation Effects 0.000 abstract 1
238000005917 acylation reaction Methods 0.000 abstract 1
230000015572 biosynthetic process Effects 0.000 abstract 1
230000020176 deacylation Effects 0.000 abstract 1
238000005947 deacylation reaction Methods 0.000 abstract 1
-1 diol lactone Chemical class 0.000 abstract 1
150000002596 lactones Chemical group 0.000 abstract 1
238000000034 method Methods 0.000 abstract 1
238000006798 ring closing metathesis reaction Methods 0.000 abstract 1

Classifications

- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D309/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
- C07D309/16—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
- C07D309/28—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member 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
- C07D309/30—Oxygen atoms, e.g. delta-lactones
- 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
- A61P9/00—Drugs for disorders of the cardiovascular system
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C69/00—Esters of carboxylic acids; Esters of carbonic or haloformic acids
- C07C69/66—Esters of carboxylic acids having esterified carboxylic groups bound to acyclic carbon atoms and having any of the groups OH, O—metal, —CHO, keto, ether, acyloxy, groups, groups, or in the acid moiety
- C07C69/73—Esters of carboxylic acids having esterified carboxylic groups bound to acyclic carbon atoms and having any of the groups OH, O—metal, —CHO, keto, ether, acyloxy, groups, groups, or in the acid moiety of unsaturated acids
- C07C69/732—Esters of carboxylic acids having esterified carboxylic groups bound to acyclic carbon atoms and having any of the groups OH, O—metal, —CHO, keto, ether, acyloxy, groups, groups, or in the acid moiety of unsaturated acids of unsaturated hydroxy carboxylic acids

Landscapes

Chemical & Material Sciences (AREA)
Organic Chemistry (AREA)
Health & Medical Sciences (AREA)
Engineering & Computer Science (AREA)
Bioinformatics & Cheminformatics (AREA)
Pharmacology & Pharmacy (AREA)
General Health & Medical Sciences (AREA)
Chemical Kinetics & Catalysis (AREA)
General Chemical & Material Sciences (AREA)
Medicinal Chemistry (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
Veterinary Medicine (AREA)
Public Health (AREA)
Life Sciences & Earth Sciences (AREA)
Animal Behavior & Ethology (AREA)
Heart & Thoracic Surgery (AREA)
Cardiology (AREA)
Diabetes (AREA)
Hematology (AREA)
Urology & Nephrology (AREA)
Vascular Medicine (AREA)
Obesity (AREA)
Pyrane Compounds (AREA)
Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Saccharide Compounds (AREA)

AT92303920T 1991-05-01 1992-04-30 Verfahren zum herstellen von simvastatin ATE141584T1 (de)

Applications Claiming Priority (1)

Application Number	Priority Date	Filing Date	Title
US07/694,164 US5159104A (en)	1991-05-01	1991-05-01	Process to simvastatin ester

Publications (1)

Publication Number	Publication Date
ATE141584T1 true ATE141584T1 (de)	1996-09-15

Family

ID=24787670

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
AT92303920T ATE141584T1 (de)	1991-05-01	1992-04-30	Verfahren zum herstellen von simvastatin

Country Status (10)

Country	Link
US (1)	US5159104A (de)
EP (1)	EP0511867B1 (de)
JP (1)	JPH0764837B2 (de)
AT (1)	ATE141584T1 (de)
CA (1)	CA2067722A1 (de)
DE (1)	DE69212884T2 (de)
DK (1)	DK0511867T3 (de)
ES (1)	ES2090507T3 (de)
GR (1)	GR3021527T3 (de)
IE (1)	IE73439B1 (de)

Families Citing this family (32)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
US5849541A (en)	1993-11-02	1998-12-15	Merck & Co., Inc.	DNA encoding triol polyketide synthase
WO1997006128A1 (en) *	1995-08-03	1997-02-20	Gist-Brocades B.V.	Selective process for the deacylation of acylated compounds
US5763653A (en) *	1997-03-13	1998-06-09	Ranbaxy Laboratories, Ltd.	Key intermediates in the manufacture of simvastatin
CA2185961A1 (en) *	1996-09-19	1998-03-20	K.S. Keshava Murthy	Process for producing simvastatin
US5763646A (en) *	1997-03-13	1998-06-09	Ranbaxy Laboratories, Ltd.	Process for manufacturing simvastatin from lovastatin or mevinolinic acid
ZA9810764B (en) *	1998-04-22	1999-08-13	Ranbaxy Lab Ltd	An improved process of lactonization in the preparation of statins.
CA2240983A1 (en)	1998-06-18	1999-12-18	Yong Tao	Process to manufacture simvastatin and intermediates
US6002021A (en) *	1998-06-29	1999-12-14	Industrial Technology Research Institute	Process for preparing 6(R)-{2-8'(S)-2",2"-dimethylbutyryloxy-2'(S)-6'(R)-dimethyl-1',2',6'7',8' 8'A(R)-hexahydronapthyl-1'(S)-ethyl}-4(R)-hydroxy-3,4,5,6-tetrahydro-2H- pyran-2-one
SI20116A (sl)	1998-12-02	2000-06-30	LEK, tovarna farmacevtskih in kemi�nih izdelkov, d.d.	Nov postopek za pripravo simvastatina in njegovih analogov
US6391583B1 (en)	1998-12-18	2002-05-21	Wisconsin Alumni Research Foundation	Method of producing antihypercholesterolemic agents
WO2001030773A2 (en)	1999-10-27	2001-05-03	Merck & Co., Inc.	Lactonization process
JP2003513036A (ja) *	1999-11-03	2003-04-08	ハワードジェイ．スミスアンドアソシエイツピーティーワイリミテッド	肝臓選択的な治療方法
AU2000234636A1 (en)	2000-03-30	2001-10-08	Cheil Jedang Corporation	A process for producing simvastatin
CZ2003554A3 (cs)	2000-07-27	2003-08-13	Plus Chemicals, B. V.	Vysoce přečištěný simvastatin
NL1017548C2 (nl) *	2001-03-09	2002-09-10	Synthon Bv	Een lactonisatie proces.
KR20040026705A (ko)	2001-08-16	2004-03-31	테바 파마슈티컬 인더스트리즈 리미티드	스타틴의 칼슘 염 형태의 제조 방법
KR100407758B1 (ko) *	2001-08-27	2003-12-01	씨제이 주식회사	스타틴의 제조에 있어서 락톤화 방법
KR100435142B1 (ko) *	2002-01-09	2004-06-09	한미약품 주식회사	개선된 심바스타틴의 제조방법
WO2004071456A2 (en)	2003-02-11	2004-08-26	Plus Chemicals, B.V.	Process for preparing simvastatin having controlled ranges of simvastatin dimer content
CA2521095A1 (en) *	2003-04-01	2004-10-21	Plus Chemicals, B.V.	Amorphous simvastatin calcium and methods for the preparation thereof
CN102703539A (zh) *	2003-10-21	2012-10-03	维莱尼姆公司	制备新伐他汀及中间体的方法
DE602004023004D1 (de) *	2004-09-08	2009-10-15	Jubilant Organosys Ltd	Verbessertes verfahren zur lactonisierung bei der herstellung von statinen
CN1754870A (zh) *	2004-09-30	2006-04-05	淮北市辉克药业有限公司	辛伐他汀的制备方法
GB0427491D0 (en)	2004-12-16	2005-01-19	Avecia Ltd	Process and compounds
WO2007020079A2 (en) *	2005-08-17	2007-02-22	Synthon B.V.	Orally disintegratable simvastatin tablets
US20110059493A1 (en) *	2007-08-27	2011-03-10	Brian Morgan	Methods for Making Simvastatin and Intermediates
CN101575286B (zh) *	2008-05-09	2013-06-19	上海医药工业研究院	一种辛伐他汀铵盐的合成方法及所用中间体及其制备方法
CN102690254B (zh) *	2008-05-09	2014-06-04	上海医药工业研究院	辛伐他汀铵盐中间体及其制备方法
ES2343049B1 (es)	2008-10-15	2011-06-10	Neuron Biopharma, S.A.	Biosintesis de derivados de monacolina j.
US8470805B2 (en)	2009-04-30	2013-06-25	Kaohsiung Medical University	Processes for preparing piperazinium salts of KMUP and use thereof
TWI462739B (zh)	2010-11-02	2014-12-01	Univ Kaohsiung Medical	Ｓｉｌｄｅｎａｆｉｌ－同族物四級銨哌嗪鹽類之製備及醫療用途
US9499621B2 (en)	2013-04-08	2016-11-22	Cytodyn, Inc.	Felinized antibodies and methods of treating retroviral infections in felines

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
US4293496A (en) *	1980-02-04	1981-10-06	Merck & Co., Inc.	6(R)-[2-(8-Hydroxy-2,6-dimethylpolyhydronaphthyl-1)-ethyl]-4(R)-hydroxy-3,4,5,6-tetrahydro-2H-pyran-2-ones
US4444784A (en) *	1980-08-05	1984-04-24	Merck & Co., Inc.	Antihypercholesterolemic compounds
JPH0692381B2 (ja) *	1980-03-31	1994-11-16	三共株式会社	Ｍｂ−５３０ａ誘導体
US4584389A (en) *	1983-10-11	1986-04-22	Merck & Co., Inc.	Processes for preparing 6(R)-[2-[8(S)(2,2-dimethylbutyryloxy)-2(S),6(S)-dimethyl-1,2,3,4,4a(S),5,6,7,8,8a(S)-decahydronaphthyl-1(S)]ethyl]-4(R)-hydroxy-3,4,5,6-tetrahydro-2H-pyran-2-one
US4582915A (en) *	1983-10-11	1986-04-15	Merck & Co., Inc.	Process for C-methylation of 2-methylbutyrates
JPH0749393B2 (ja) *	1987-06-03	1995-05-31	旭電化工業株式会社	新規化合物及びこれを用いた高脂血症治療薬
US4820850A (en) *	1987-07-10	1989-04-11	Merck & Co., Inc.	Process for α-C-alkylation of the 8-acyl group on mevinolin and analogs thereof
PT88364A (pt) *	1987-09-02	1989-07-31	Merck & Co Inc	Process for preparing novel hmg-coa reductase inhibitors
US4866090A (en) *	1988-01-07	1989-09-12	Merck & Co., Inc.	Novel HMG-CoA reductase inhibitors

1991
- 1991-05-01 US US07/694,164 patent/US5159104A/en not_active Expired - Lifetime
1992
- 1992-04-30 DE DE69212884T patent/DE69212884T2/de not_active Expired - Fee Related
- 1992-04-30 ES ES92303920T patent/ES2090507T3/es not_active Expired - Lifetime
- 1992-04-30 EP EP92303920A patent/EP0511867B1/de not_active Expired - Lifetime
- 1992-04-30 AT AT92303920T patent/ATE141584T1/de not_active IP Right Cessation
- 1992-04-30 CA CA002067722A patent/CA2067722A1/en not_active Abandoned
- 1992-04-30 DK DK92303920.0T patent/DK0511867T3/da active
- 1992-05-01 JP JP4157239A patent/JPH0764837B2/ja not_active Expired - Fee Related
- 1992-07-01 IE IE921399A patent/IE73439B1/en not_active IP Right Cessation
1996
- 1996-10-31 GR GR960402890T patent/GR3021527T3/el unknown

Also Published As

Publication number	Publication date
IE73439B1 (en)	1997-06-04
ES2090507T3 (es)	1996-10-16
IE921399A1 (en)	1992-11-04
JPH0764837B2 (ja)	1995-07-12
CA2067722A1 (en)	1992-11-02
DE69212884T2 (de)	1997-02-27
EP0511867A1 (de)	1992-11-04
DE69212884D1 (de)	1996-09-26
EP0511867B1 (de)	1996-08-21
GR3021527T3 (en)	1997-01-31
US5159104A (en)	1992-10-27
JPH05230052A (ja)	1993-09-07
DK0511867T3 (da)	1996-09-09

Legal Events

Date	Code	Title	Description
2009-01-15	REN	Ceased due to non-payment of the annual fee

Publication	Publication Date	Title
ATE141584T1 (de)	1996-09-15	Verfahren zum herstellen von simvastatin
HUT63419A (en)	1993-08-30	Process for producing mercaptoacetamide derivatives of pyrrolo-, pyrido- and oxazinobenzazepine having encephalinase- and angiotensin-converting enzyme-inhibiting activity
NO303574B1 (no)	1998-08-03	Ny fremgangsmÕte for fremstilling av 9-amino-6-demetyl-6-deoksytetracykliner
DE68913215D1 (de)	1994-03-24	Verfahren zur Herstellung hydraulischer Dämpfungsspalten.
ATE121066T1 (de)	1995-04-15	Verfahren zur herstellung von 6,12-dihydro-6- hydroxy-cannabidiol und dessen anwendung zur herstellung von trans-delta-9- tetrahydrocannabinol.
DE69430215D1 (de)	2002-04-25	Verfahren zum Herstellen von Doppelplüschgeweben
DE69431799D1 (de)	2003-01-09	Verfahren zur erzeugung von russen
AT372975B (de)	1983-12-12	Verfahren zum herstellen von monacolin k
DE59404214D1 (de)	1997-11-06	Verfahren zum herstellen von diglycerin
DE3855208D1 (de)	1996-05-23	Verfahren zur Herstellung von hochschlagfesten Polycarbonaten
ATE137493T1 (de)	1996-05-15	Verfahren zur herstellung von zwischenprodukten zur verwendung in der herstellung von alkoxyiminoacetamide
DE69530592D1 (de)	2003-06-05	Verfahren zur herstellung von (+/-) calanolide a und zwischenprodukte dafür
ATE201025T1 (de)	2001-05-15	Verfahren zur herstellung von cephalosporinen und zwischenprodukte in diesem verfahren
ATE163096T1 (de)	1998-02-15	Verfahren zur herstellung von mikrostrukturkörpern
DE69201380D1 (de)	1995-03-23	Verfahren zum Herstellen von Rohrglas.
DE69013514D1 (de)	1994-11-24	Verfahren zum herstellen von bauelementen einer flüssigkeitskammer.
ATE218131T1 (de)	2002-06-15	Verfahren zur herstellung von mono-n- substituierten tetraazamakrocyclen
DE69208290D1 (de)	1996-03-28	Verfahren zum Herstellen von Formkörpern mittels CVD und daraus hergestellte Formkörper
DE69411254D1 (de)	1998-07-30	Verfahren zum kontinuierlichen Herstellen von Dimethylcarbonat
DE68916760D1 (de)	1994-08-18	Verfahren zur Herstellung von Gamma-Lactonen.
ATE175957T1 (de)	1999-02-15	Verfahren zur herstellung von alkoxyiminoacetamid-verbindungen
ATE130597T1 (de)	1995-12-15	Verfahren zur herstellung von r-aminocarnitin und s-aminocarnitin.
ATE150003T1 (de)	1997-03-15	Verfahren zur herstellung von l-(-)-carnitin aus abfallprodukten mit entgegengesetzter konfiguration
ATE132535T1 (de)	1996-01-15	Verfahren zur diskontinuierlichen herstellung von l-carnitin auf mikrobiologischem weg
DE3582368D1 (de)	1991-05-08	Verfahren zur herstellung von epoxyden mittels mikroorganismen.