CA1199322A - Antihypercholesterolemic compounds - Google Patents

Antihypercholesterolemic compounds

Info

Publication number
CA1199322A
CA1199322A CA000369992A CA369992A CA1199322A CA 1199322 A CA1199322 A CA 1199322A CA 000369992 A CA000369992 A CA 000369992A CA 369992 A CA369992 A CA 369992A CA 1199322 A CA1199322 A CA 1199322A
Authority
CA
Canada
Prior art keywords
compound
prepared
double bonds
stirring
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.)
Expired
Application number
CA000369992A
Other languages
English (en)
French (fr)
Inventor
Robert L. Smith
William F. Hoffman
Alvin K. Willard
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Merck and Co Inc
Original Assignee
Merck and 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.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=27494171&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=CA1199322(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Priority claimed from US06/175,232 external-priority patent/US4293496A/en
Application filed by Merck and Co Inc filed Critical Merck and Co Inc
Application granted granted Critical
Publication of CA1199322A publication Critical patent/CA1199322A/en
Expired legal-status Critical Current

Links

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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Obesity (AREA)
  • Diabetes (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Hematology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Steroid Compounds (AREA)
  • Pyrane Compounds (AREA)
CA000369992A 1980-02-04 1981-02-03 Antihypercholesterolemic compounds Expired CA1199322A (en)

Applications Claiming Priority (8)

Application Number Priority Date Filing Date Title
US11805180A 1980-02-04 1980-02-04
US11804980A 1980-02-04 1980-02-04
US118,049 1980-02-04
US118,051 1980-02-04
US17546080A 1980-08-05 1980-08-05
US175,232 1980-08-05
US06/175,232 US4293496A (en) 1980-02-04 1980-08-05 6(R)-[2-(8-Hydroxy-2,6-dimethylpolyhydronaphthyl-1)-ethyl]-4(R)-hydroxy-3,4,5,6-tetrahydro-2H-pyran-2-ones
US175,460 1988-04-13

Publications (1)

Publication Number Publication Date
CA1199322A true CA1199322A (en) 1986-01-14

Family

ID=27494171

Family Applications (1)

Application Number Title Priority Date Filing Date
CA000369992A Expired CA1199322A (en) 1980-02-04 1981-02-03 Antihypercholesterolemic compounds

Country Status (22)

Country Link
EP (1) EP0033538B1 (enFirst)
AU (1) AU548996B2 (enFirst)
CA (1) CA1199322A (enFirst)
CY (1) CY1404A (enFirst)
DD (1) DD155989A5 (enFirst)
DE (1) DE3173042D1 (enFirst)
DK (1) DK157292C (enFirst)
ES (1) ES499079A0 (enFirst)
FI (1) FI78082C (enFirst)
GR (1) GR74798B (enFirst)
HK (1) HK16488A (enFirst)
IE (1) IE51478B1 (enFirst)
IL (1) IL62044A (enFirst)
MA (1) MA19054A1 (enFirst)
MY (1) MY8700745A (enFirst)
NL (1) NL930009I2 (enFirst)
NO (2) NO154229C (enFirst)
NZ (1) NZ196172A (enFirst)
PT (1) PT72441B (enFirst)
RO (1) RO82367B (enFirst)
SG (1) SG61087G (enFirst)
YU (1) YU28181A (enFirst)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6307066B1 (en) 1996-09-19 2001-10-23 Brantford Chemicals Inc. Process for producing simvastatin
US6506929B1 (en) 1998-06-18 2003-01-14 Apotex Inc. Process to manufacture simvastatin and intermediates
WO2010043748A1 (es) 2008-10-15 2010-04-22 Neuron Biopharma, S.A. Biosíntesis de derivados de monacolina j

Families Citing this family (52)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH0692381B2 (ja) * 1980-03-31 1994-11-16 三共株式会社 Ｍｂ−５３０ａ誘導体
US4432996A (en) * 1980-11-17 1984-02-21 Merck & Co., Inc. Hypocholesterolemic fermentation products and process of preparation
US4343814A (en) * 1980-11-17 1982-08-10 Merck & Co., Inc. Hypocholesterolemic fermentation products
EP0094443A1 (en) * 1982-05-17 1983-11-23 Merck & Co. Inc. 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, process for preparing and pharmaceutical composition containing the same
US4503072A (en) * 1982-12-22 1985-03-05 Merck & Co., Inc. Antihypercholesterolemic compounds
ES8609193A1 (es) * 1983-01-24 1986-07-16 Sandoz Ag Procedimiento para preparar analogos de mevalonolactona y derivados de los mismos
DE3481190D1 (de) * 1983-10-11 1990-03-08 Merck & Co Inc Verfahren zur herstellung von 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-on.
DE3480923D1 (de) * 1983-10-11 1990-02-08 Merck & Co Inc Verfahren zur c-methylierung von 2-methylbutyraten.
US4668699A (en) * 1985-08-05 1987-05-26 Merck & Co., Inc. Novel HMG-CoA reductase inhibitors
US4833258A (en) * 1987-02-17 1989-05-23 Merck & Co., Inc. Intermediates useful in the preparation of HMG-COA reductase inhibitors
US4997848A (en) 1987-10-27 1991-03-05 Sankyo Company, Limited Octahydronaphthalene oxime derivatives for cholesterol synthesis inhibition
US5021451A (en) * 1988-11-14 1991-06-04 Hoffman-La Roche Inc. Method for inhibiting hyperproliferative diseases
GB8915280D0 (en) * 1989-07-04 1989-08-23 British Bio Technology Compounds
US5110825A (en) * 1989-12-28 1992-05-05 Shionogi & Co., Ltd. Benzofuran derivative
GB9100174D0 (en) * 1991-01-04 1991-02-20 British Bio Technology Compounds
NZ250609A (en) * 1992-12-28 1995-07-26 Sankyo Co Hexahydronaphthalene esters and ring closed lactones; preparation and medicaments
US6642268B2 (en) 1994-09-13 2003-11-04 G.D. Searle & Co. Combination therapy employing ileal bile acid transport inhibiting benzothipines and HMG Co-A reductase inhibitors
US6268392B1 (en) 1994-09-13 2001-07-31 G. D. Searle & Co. Combination therapy employing ileal bile acid transport inhibiting benzothiepines and HMG Co-A reductase inhibitors
IL118778A (en) * 1995-07-03 1999-07-14 Sankyo Co Pharmaceutical compositions for the treatment of arteriosclerosis and xanthoma containing an hmg-coa reductase inhibitor
EA000954B1 (ru) * 1995-12-06 2000-08-28 Балканфарма - Разград Ад Способ получения ловастатина
US6083497A (en) 1997-11-05 2000-07-04 Geltex Pharmaceuticals, Inc. Method for treating hypercholesterolemia with unsubstituted polydiallylamine polymers
SI9800057A (sl) * 1998-02-26 1999-08-31 Krka, Tovarna Zdravil, D.D. Postopek za pripravo simvastatina in njegovih derivatov
WO2000038721A1 (en) 1998-12-23 2000-07-06 G.D. Searle Llc Combinations of cholesteryl ester transfer protein inhibitors and nicotinic acid derivatives for cardiovascular indications
IL143949A0 (en) 1998-12-23 2002-04-21 Searle Llc Combinations of cholesteryl ester transfer protein inhibitors and fibric acid derivatives for cardiovascular indications
DK1140185T3 (da) 1998-12-23 2003-09-29 Searle Llc Kombinationer af cholesterylestertransferhæmmere og galdesyre kompleksdannende forbindelser til hjertekar indikationer
WO2000038726A1 (en) 1998-12-23 2000-07-06 G.D. Searle Llc Combinations of ileal bile acid transport inhibitors and cholesteryl ester transfer protein inhibitors for cardiovascular indications
AU2157400A (en) 1998-12-23 2000-07-31 G.D. Searle & Co. Combinations of cholesteryl ester transfer protein inhibitors and hmg coa reductase inhibitors for cardiovascular indications
EP1140190B1 (en) 1998-12-23 2002-11-20 G.D. Searle LLC. Combinations of ileal bile acid transport inhibitors and bile acid sequestering agents for cardiovascular indications
ATE240120T1 (de) 1998-12-23 2003-05-15 Searle Llc Kombinationen von ileumgallensäuretransports inhibitoren und fibronsäure derivaten für kardiovaskuläre indikationen
HK1052183A1 (zh) 2000-03-10 2003-09-05 Pharmacia Corporation 制造tetrahydrobenzothiepines的方法
SI1323701T1 (sl) 2000-09-07 2009-12-31 Kaneka Corp Postopki za kristalizacijo hidroksikarboksilnih kislin
JP2005518347A (ja) 2001-11-02 2005-06-23 ジー．ディー． サール エルエルシー 頂端ナトリウム共依存性胆汁酸輸送（ａｓｂｔ）およびタウロコール酸塩取り込みの阻害剤としての新規一および二フッ化ベンゾチエピン化合物
BR0306643A (pt) 2002-01-17 2004-10-19 Pharmacia Corp Novos compostos de hidroxi alquil/aril ou ceto tiepina como inibidores do transporte co-dependente de ácido biliar-sódio apical
SI21187A (sl) 2002-03-26 2003-10-31 Krka, Tovarna Zdravil D.D., Novo Mesto Postopek za pripravo 4-oksitetrahidropiran-2-onov
KR20040092790A (ko) * 2003-04-29 2004-11-04 씨제이 주식회사 심바스타틴 중간체 제조방법
EP1741427A1 (en) 2005-07-06 2007-01-10 KRKA, D.D., Novo Mesto Pharmaceutical composition comprising simvastatin and ezetimibe
RS53084B (sr) 2006-07-05 2014-06-30 Takeda Gmbh Kombinacija inhibitora hmg-coa reduktaze rosuvastatina sa inhibitorom fosfodiesteraze 4, kao što je roflumilast, roflumilast-n-oksid za lečenje inflamatornih plućnih obolenja
WO2009013764A2 (en) * 2007-07-24 2009-01-29 Jubilant Organosys Limited Process for producing 6(r)-[2-(8'(s)-2 ',2 '-dimethylbutyryloxy-2'(s),6'(r)-dimethyl-1,2,6,7', 8',8a'(r)- hexahydronaphthyl-l'(s))ethyl]-4(r)-hydroxy-3,4,5,6- tetrahydro-2h-pyran-2-one
JOP20080381B1 (ar) 2007-08-23 2023-03-28 Amgen Inc بروتينات مرتبطة بمولدات مضادات تتفاعل مع بروبروتين كونفيرتاز سيتيليزين ككسين من النوع 9 (pcsk9)
ES2330184B1 (es) 2008-06-03 2010-07-05 Neuron Biopharma, S.A. Uso de estatinas como anticonvulsivantes, antiepilepticos y neuroprotectores.
EP2204170A1 (en) 2008-12-01 2010-07-07 LEK Pharmaceuticals D.D. Pharmaceutical composition comprising ezetimibe and simvastatin
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
SI2373609T1 (sl) 2008-12-19 2013-12-31 Krka, D.D., Novo Mesto Uporaba amfifilnih spojin za kontrolirano kristalizacijo statinov in intermediatov statinov
EP2216016A1 (en) 2009-02-06 2010-08-11 LEK Pharmaceuticals d.d. Process for the preparation of a pharmaceutical composition comprising ezetimibe
EP2241561A1 (en) * 2009-04-16 2010-10-20 Neuron Biopharma, S.A. Neuroprotective, hypocholesterolemic and antiepileptic compound
WO2011002424A2 (en) 2009-07-02 2011-01-06 Bilgic Mahmut Solubility and stability enchancing pharmaceutical formulation
AR079336A1 (es) 2009-12-11 2012-01-18 Irm Llc Antagonistas de la pro-proteina convertasa-subtilisina/quexina tipo 9 (pcsk9)
EP2368543A1 (en) 2010-03-25 2011-09-28 KRKA, tovarna zdravil, d.d., Novo mesto Method of preparing a granulated pharmaceutical composition comprising simvastatin and/or ezetimibe
ES2380473B1 (es) * 2010-10-13 2013-02-19 Neuron Biopharma, S.A. Compuesto neuroprotector, hipocolesterolémico, antiinflamatorio y antiepiléptico.
JOP20200043A1 (ar) 2011-05-10 2017-06-16 Amgen Inc طرق معالجة أو منع الاضطرابات المختصة بالكوليسترول
WO2013102193A1 (en) 2011-12-29 2013-07-04 Trustees Of Tufts College Functionalization of biomaterials to control regeneration and inflammation responses
JP2015530867A (ja) 2012-06-15 2015-10-29 ジェネンテック， インコーポレイテッド 抗ｐｃｓｋ９抗体、製剤、投薬、及び使用方法

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS5612114B2 (enFirst) * 1974-06-07 1981-03-18
US4049495A (en) * 1974-06-07 1977-09-20 Sankyo Company Limited Physiologically active substances and fermentative process for producing the same
US4137322A (en) 1976-11-02 1979-01-30 Sankyo Company Limited ML-236B carboxylic acid derivatives and their use as antihyperlipemic agents
JPS6026094B2 (ja) 1978-07-04 1985-06-21 三共株式会社 テトラヒドロｍｌ↓−２３６ｂおよびその誘導体並びにそれを有効成分とする高脂血症治療剤
JPS5925599B2 (ja) * 1979-02-20 1984-06-19 三共株式会社 新生理活性物質モナコリンｋおよびその製造法
US4231938A (en) * 1979-06-15 1980-11-04 Merck & Co., Inc. Hypocholesteremic fermentation products and process of preparation
IL60219A (en) * 1979-06-15 1985-05-31 Merck & Co Inc Hypocholesteremic fermentation products of the hmg-coa reductase inhibitor type,their preparation and pharmaceutical compositions containing them
PT72394B (en) 1980-02-04 1982-09-06 Merck & Co Inc Process for preparing dihydro and tetrahydromevinoline hypocholesterolimics

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6307066B1 (en) 1996-09-19 2001-10-23 Brantford Chemicals Inc. Process for producing simvastatin
US6506929B1 (en) 1998-06-18 2003-01-14 Apotex Inc. Process to manufacture simvastatin and intermediates
WO2010043748A1 (es) 2008-10-15 2010-04-22 Neuron Biopharma, S.A. Biosíntesis de derivados de monacolina j

Also Published As

Publication number Publication date
NO810358L (no) 1981-08-05
NO1994001I1 (no) 1994-07-01
AU6657381A (en) 1981-08-13
FI78082B (fi) 1989-02-28
PT72441B (pt) 1984-08-01
HK16488A (en) 1988-03-11
DK157292B (da) 1989-12-04
IL62044A0 (en) 1981-03-31
NL930009I1 (nl) 1993-04-01
PT72441A (pt) 1981-03-01
DK46181A (da) 1981-08-05
SG61087G (en) 1987-10-23
IE810204L (en) 1981-08-04
IE51478B1 (en) 1987-01-07
DK157292C (da) 1990-05-07
EP0033538A2 (en) 1981-08-12
DD155989A5 (de) 1982-07-21
EP0033538A3 (en) 1982-02-24
FI78082C (fi) 1989-06-12
ES8609296A1 (es) 1985-10-16
NZ196172A (en) 1985-01-31
IL62044A (en) 1987-03-31
NO154229C (no) 1986-08-13
MY8700745A (en) 1987-12-31
MA19054A1 (fr) 1981-10-01
FI810287L (fi) 1981-08-05
ES499079A0 (es) 1985-10-16
RO82367B (ro) 1984-02-28
GR74798B (enFirst) 1984-07-12
DE3173042D1 (en) 1986-01-09
AU548996B2 (en) 1986-01-09
CY1404A (en) 1988-04-22
YU28181A (en) 1983-10-31
NL930009I2 (nl) 1993-09-16
RO82367A (ro) 1984-02-21
NO154229B (no) 1986-05-05
EP0033538B1 (en) 1985-11-27

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