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DE60002769D1 - Wasserhaltiges, kristallines Calcium-Salz der Simvastatin Dihydroxy offene Säure - Google Patents

Wasserhaltiges, kristallines Calcium-Salz der Simvastatin Dihydroxy offene Säure

Info

Publication number
DE60002769D1
DE60002769D1 DE60002769T DE60002769T DE60002769D1 DE 60002769 D1 DE60002769 D1 DE 60002769D1 DE 60002769 T DE60002769 T DE 60002769T DE 60002769 T DE60002769 T DE 60002769T DE 60002769 D1 DE60002769 D1 DE 60002769D1
Authority
DE
Germany
Prior art keywords
hydrous
calcium salt
crystalline calcium
open acid
dihydroxy open
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 - Fee Related
Application number
DE60002769T
Other languages
English (en)
Other versions
DE60002769T2 (de
DE60002769T9 (de
Inventor
Richard D Tillyer
Paul J Reider
Edward J J Grabowski
Feng Xu
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
Application filed by Merck and Co Inc filed Critical Merck and Co Inc
Publication of DE60002769D1 publication Critical patent/DE60002769D1/de
Publication of DE60002769T2 publication Critical patent/DE60002769T2/de
Application granted granted Critical
Publication of DE60002769T9 publication Critical patent/DE60002769T9/de
Expired - Fee Related 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/22—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • C07C69/02—Esters of acyclic saturated monocarboxylic acids having the carboxyl group bound to an acyclic carbon atom or to hydrogen
    • C07C69/22—Esters of acyclic saturated monocarboxylic acids having the carboxyl group bound to an acyclic carbon atom or to hydrogen having three or more carbon atoms in the acid moiety
    • C07C69/30—Esters of acyclic saturated monocarboxylic acids having the carboxyl group bound to an acyclic carbon atom or to hydrogen having three or more carbon atoms in the acid moiety esterified with trihydroxylic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0002—Galenical forms characterised by the drug release technique; Application systems commanded by energy
    • A61K9/0004—Osmotic delivery systems; Sustained release driven by osmosis, thermal energy or gas
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2602/00—Systems containing two condensed rings
    • C07C2602/02—Systems containing two condensed rings the rings having only two atoms in common
    • C07C2602/14—All rings being cycloaliphatic
    • C07C2602/26—All rings being cycloaliphatic the ring system containing ten carbon atoms
    • C07C2602/28—Hydrogenated naphthalenes

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Vascular Medicine (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Urology & Nephrology (AREA)
  • Obesity (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Emergency Medicine (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Medicinal Preparation (AREA)
DE60002769T 1999-03-08 2000-03-07 Wasserhaltiges, kristallines Calcium-Salz der Simvastatin Dihydroxy offene Säure Expired - Fee Related DE60002769T9 (de)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
US12324799P 1999-03-08 1999-03-08
US123247P 1999-03-08
US26474599A 1999-03-09 1999-03-09
US264745 1999-03-09
PCT/US2000/002627 WO2000053566A1 (en) 1999-03-08 2000-02-02 Crystalline hydrated dihydroxy open-acid simvastatin calcium salt
US2627P 2000-02-02

Publications (3)

Publication Number Publication Date
DE60002769D1 true DE60002769D1 (de) 2003-06-26
DE60002769T2 DE60002769T2 (de) 2004-03-18
DE60002769T9 DE60002769T9 (de) 2004-11-04

Family

ID=26821372

Family Applications (1)

Application Number Title Priority Date Filing Date
DE60002769T Expired - Fee Related DE60002769T9 (de) 1999-03-08 2000-03-07 Wasserhaltiges, kristallines Calcium-Salz der Simvastatin Dihydroxy offene Säure

Country Status (16)

Country Link
EP (2) EP1163203A1 (de)
JP (2) JP2002539108A (de)
AR (1) AR022857A1 (de)
AT (1) ATE240934T1 (de)
AU (1) AU764048B2 (de)
CA (1) CA2365869A1 (de)
CO (1) CO5150184A1 (de)
DE (1) DE60002769T9 (de)
DK (1) DK1036783T3 (de)
ES (1) ES2198253T3 (de)
HN (1) HN2000000031A (de)
PE (1) PE20001469A1 (de)
PT (1) PT1036783E (de)
SI (1) SI1036783T1 (de)
SV (1) SV2002000035A (de)
WO (1) WO2000053566A1 (de)

Families Citing this family (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IL152179A (en) 2000-04-10 2009-06-15 Teva Pharma Stable pharmaceutical compositions containing 7-substituted-3,5- dihydroxyheptanoic acids or 7-substituted-3,5-dihydroxyheptenoic acids
USRE44578E1 (en) 2000-04-10 2013-11-05 Teva Pharmaceutical Industries, Ltd. Stable pharmaceutical compositions containing 7-substituted-3,5-dihydroxyheptanoic acids or 7-substituted-3,5-dihydroxyheptenoic acids
CA2421018A1 (en) * 2000-09-06 2002-03-14 Merck & Co., Inc. Dihydroxy open-acid salt of simvastatin
AU2002210521A1 (en) * 2000-09-19 2002-04-02 Novimmune S.A. Use of statins (HMG-CoA reductase inhibitors) for the preparation of medicament as a novel type of immunomodulator, immunosuppressor and anti-inflammatory agent
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)
KR20040026705A (ko) 2001-08-16 2004-03-31 테바 파마슈티컬 인더스트리즈 리미티드 스타틴의 칼슘 염 형태의 제조 방법
CA2479005C (en) * 2002-03-18 2012-05-22 Biocon Limited Amorphous atorvastatin calcium or pravastatin sodium hmg-coa reductase inhibitors of desired particle size
US20030195167A1 (en) * 2002-04-15 2003-10-16 Kowa Co., Ltd. PTX3-gene expression inhibitor
CA2486557A1 (en) * 2002-06-13 2003-12-24 Novartis Ag Calcium salts of indole derived statins
AR040588A1 (es) 2002-07-26 2005-04-13 Schering Corp Formulacion farmaceutica que comprende un inhibidor de la absorcion del colesterol y un inhibidor de una hmg- co a reductasa
US6995277B2 (en) 2003-02-11 2006-02-07 Plus Chemicals, B.V. Process for preparing simvastatin having controlled ranges of simvastatin dimer content
EP1719759A3 (de) 2003-06-18 2007-03-21 Teva Pharmaceutical Industries, Inc. Fluvastatin-Natrium-Kristallmodifikation LXXIII, Verfahren zu deren Herstellung, Zusammensetzungen, die diese enthalten und Verfahren zu deren Anwendung
US7368468B2 (en) 2003-06-18 2008-05-06 Teva Pharmaceutical Industries Ltd. Fluvastatin sodium crystal forms XIV, LXXIII, LXXIX, LXXX and LXXXVII, processes for preparing them, compositions containing them and methods of using them
US7368581B2 (en) 2003-06-18 2008-05-06 Teva Pharmaceutical Industries Ltd. Process for the preparation of fluvastatin sodium crystal from XIV
US7816405B2 (en) 2005-04-19 2010-10-19 Eisai R&D Management Co., Ltd. Calcium bis [(2S)-3-[3-[(2S)-3-(4-chloro-2-cyanophenoxy)-2-fluoropropoxy]phenyl ]-2-isopropoxypropionate] and intermediate thereof
US20090069591A1 (en) * 2005-04-19 2009-03-12 Eisai R & D Management Co., Ltd. Calcium Bis [ (2S) -3- [3-[ (2S) -3- (4-Chloro-2-Cyanophenoxy) -2- Fluoropropoxy]Phenyl] -2- Isopropoxypropionate] and Intermediate Thereof
TWI559387B (zh) * 2010-08-27 2016-11-21 恩特葛瑞斯股份有限公司 預防乾燥期間高縱橫比結構崩塌之方法
WO2014036548A1 (en) * 2012-08-31 2014-03-06 New York Society For The Ruptured And Crippled Maintaining The Hospital For Special Surgery Macromolecular prodrugs for hard tissue and methods of use thereof
GB201704687D0 (en) 2017-03-24 2017-05-10 Wockhardt Uk Ltd Pharmaceutical composition of simvastatin or salt thereof
CN113686991A (zh) * 2021-08-31 2021-11-23 南京西默思博检测技术有限公司 测定人血浆中辛伐他汀、β-羟酸辛伐他汀的方法

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4444784A (en) * 1980-08-05 1984-04-24 Merck & Co., Inc. Antihypercholesterolemic compounds
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
US5223415A (en) * 1990-10-15 1993-06-29 Merck & Co., Inc. Biosynthetic production of 7-[1',2',6',7',8',8a'(R)-hexahydro-2'(S),6'(R)-dimethyl-8'(S)-hydroxy-1'(S)-naphthyl]-3(R),5(R)-dihydroxyheptanoic acid (triol acid)

Also Published As

Publication number Publication date
EP1036783A1 (de) 2000-09-20
DK1036783T3 (da) 2003-06-23
WO2000053566A1 (en) 2000-09-14
DE60002769T2 (de) 2004-03-18
ES2198253T3 (es) 2004-02-01
PE20001469A1 (es) 2000-12-18
PT1036783E (pt) 2003-08-29
ATE240934T1 (de) 2003-06-15
EP1163203A1 (de) 2001-12-19
JP2000281626A (ja) 2000-10-10
JP2002539108A (ja) 2002-11-19
SI1036783T1 (en) 2003-08-31
CA2365869A1 (en) 2000-09-14
AR022857A1 (es) 2002-09-04
SV2002000035A (es) 2002-01-15
CO5150184A1 (es) 2002-04-29
DE60002769T9 (de) 2004-11-04
AU2637000A (en) 2000-09-28
AU764048B2 (en) 2003-08-07
HN2000000031A (es) 2001-09-25
EP1036783B1 (de) 2003-05-21

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Legal Events

Date Code Title Description
8364 No opposition during term of opposition
8339 Ceased/non-payment of the annual fee