CA2610890A1 - Novel 2-azetidinone derivatives and their use as cholesterol absorption inhibitors for the treatment of hyperlipidaemia - Google Patents
Novel 2-azetidinone derivatives and their use as cholesterol absorption inhibitors for the treatment of hyperlipidaemia Download PDFInfo
- Publication number
- CA2610890A1 CA2610890A1 CA002610890A CA2610890A CA2610890A1 CA 2610890 A1 CA2610890 A1 CA 2610890A1 CA 002610890 A CA002610890 A CA 002610890A CA 2610890 A CA2610890 A CA 2610890A CA 2610890 A1 CA2610890 A1 CA 2610890A1
- Authority
- CA
- Canada
- Prior art keywords
- solvate
- formula
- compound
- salt
- pharmaceutically acceptable
- 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.)
- Abandoned
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D205/00—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
- C07D205/02—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
- C07D205/06—Heterocyclic compounds containing four-membered rings with one nitrogen 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
- C07D205/08—Heterocyclic compounds containing four-membered rings with one nitrogen 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 one oxygen atom directly attached in position 2, e.g. beta-lactams
-
- 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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/397—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
-
- 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
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/06—Dipeptides
- C07K5/06008—Dipeptides with the first amino acid being neutral
- C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
- C07K5/06026—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atom, i.e. Gly or Ala
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
SE0501425 | 2005-06-20 | ||
SE0501425-3 | 2005-06-20 | ||
PCT/SE2006/000741 WO2006137782A1 (en) | 2005-06-20 | 2006-06-19 | Novel 2-azetidinone derivatives and their use as cholesterol absorption inhibitors for the treatment of hyperlipidaemia |
Publications (1)
Publication Number | Publication Date |
---|---|
CA2610890A1 true CA2610890A1 (en) | 2006-12-28 |
Family
ID=37570721
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CA002610890A Abandoned CA2610890A1 (en) | 2005-06-20 | 2006-06-19 | Novel 2-azetidinone derivatives and their use as cholesterol absorption inhibitors for the treatment of hyperlipidaemia |
Country Status (18)
Families Citing this family (18)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US7871998B2 (en) | 2003-12-23 | 2011-01-18 | Astrazeneca Ab | Diphenylazetidinone derivatives possessing cholesterol absorption inhibitory activity |
UY29607A1 (es) | 2005-06-20 | 2007-01-31 | Astrazeneca Ab | Compuestos quimicos |
SA06270191B1 (ar) * | 2005-06-22 | 2010-03-29 | استرازينيكا ايه بي | مشتقات من 2- أزيتيدينون جديدة باعتبارها مثبطات لامتصاص الكوليسترول لعلاج حالات فرط نسبة الدهون في الدم |
AR057072A1 (es) | 2005-06-22 | 2007-11-14 | Astrazeneca Ab | Compuestos quimicos derivados de 2-azetidinona, formulacion farmaceutica y un proceso de preparacion del compuesto |
TW200811098A (en) | 2006-04-27 | 2008-03-01 | Astrazeneca Ab | Chemical compounds |
CA2666193A1 (en) | 2006-08-08 | 2008-02-14 | Sanofi-Aventis | Arylaminoaryl-alkyl-substituted imidazolidine-2,4-diones, process for preparing them, medicaments comprising these compounds, and their use |
EP2025674A1 (de) | 2007-08-15 | 2009-02-18 | sanofi-aventis | Substituierte Tetrahydronaphthaline, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel |
DE102007054497B3 (de) | 2007-11-13 | 2009-07-23 | Sanofi-Aventis Deutschland Gmbh | Neue kristalline Diphenylazetidinonhydrate und Verfahren zu deren Herstellung |
EP2310372B1 (en) | 2008-07-09 | 2012-05-23 | Sanofi | Heterocyclic compounds, processes for their preparation, medicaments comprising these compounds, and the use thereof |
WO2010068601A1 (en) | 2008-12-08 | 2010-06-17 | Sanofi-Aventis | A crystalline heteroaromatic fluoroglycoside hydrate, processes for making, methods of use and pharmaceutical compositions thereof |
US9212175B2 (en) | 2009-03-06 | 2015-12-15 | Lipideon Biotechnology Ag | Pharmaceutical hypocholesterolemic compositions |
DK2470552T3 (en) | 2009-08-26 | 2014-02-17 | Sanofi Sa | NOVEL, CRYSTALLINE, heteroaromatic FLUORGLYCOSIDHYDRATER, MEDICINES COVERING THESE COMPOUNDS AND THEIR USE |
US8933024B2 (en) | 2010-06-18 | 2015-01-13 | Sanofi | Azolopyridin-3-one derivatives as inhibitors of lipases and phospholipases |
US8828994B2 (en) | 2011-03-08 | 2014-09-09 | Sanofi | Di- and tri-substituted oxathiazine derivatives, method for the production thereof, use thereof as medicine and drug containing said derivatives and use thereof |
WO2012120055A1 (de) | 2011-03-08 | 2012-09-13 | Sanofi | Di- und trisubstituierte oxathiazinderivate, verfahren zu deren herstellung, ihre verwendung als medikament sowie sie enthaltendes arzneimittel und deren verwendung |
EP2683700B1 (de) | 2011-03-08 | 2015-02-18 | Sanofi | Tetrasubstituierte oxathiazinderivate, verfahren zu deren herstellung, ihre verwendung als medikament sowie sie enthaltendes arzneimittel und deren verwendung |
US8901114B2 (en) | 2011-03-08 | 2014-12-02 | Sanofi | Oxathiazine derivatives substituted with carbocycles or heterocycles, method for producing same, drugs containing said compounds, and use thereof |
WO2012120053A1 (de) | 2011-03-08 | 2012-09-13 | Sanofi | Verzweigte oxathiazinderivate, verfahren zu deren herstellung, ihre verwendung als medikament sowie sie enthaltendes arzneimittel und deren verwendung |
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LT3300B (en) * | 1992-12-23 | 1995-06-26 | Schering Corp | Combination of a cholesterol biosynhtesis inhibitor and a beta- lactam cholesterol absorbtion inhibitor |
US5633246A (en) * | 1994-11-18 | 1997-05-27 | Schering Corporation | Sulfur-substituted azetidinone compounds useful as hypocholesterolemic agents |
DK1413331T3 (da) | 2001-01-26 | 2007-12-10 | Schering Corp | Kombinationer af peroxisomproliferatoraktiveret receptor (PPAR)-aktivatoren fenofibrat og sterolabsorptionsinhibitoren ezetimib til vaskulære indikationer |
TWI291957B (en) | 2001-02-23 | 2008-01-01 | Kotobuki Pharmaceutical Co Ltd | Beta-lactam compounds, process for repoducing the same and serum cholesterol-lowering agents containing the same |
US7053080B2 (en) * | 2001-09-21 | 2006-05-30 | Schering Corporation | Methods and therapeutic combinations for the treatment of obesity using sterol absorption inhibitors |
DK1429756T3 (da) | 2001-09-21 | 2007-03-19 | Schering Corp | Behandling af xanthoma med azetidinonderivater som sterolabsorptionsinhibitorer |
DE60229406D1 (de) * | 2001-09-21 | 2008-11-27 | Schering Corp | Verfahren zur behandlung oder verhinderung von vaskulärer entzündung mit sterol-absorbierungs- inhibitor(en) |
GB0215579D0 (en) * | 2002-07-05 | 2002-08-14 | Astrazeneca Ab | Chemical compounds |
US6761509B2 (en) * | 2002-07-26 | 2004-07-13 | Jan Erik Jansson | Concrete module for retaining wall and improved retaining wall |
US6960047B2 (en) * | 2002-08-02 | 2005-11-01 | Innovative Technology Application, Inc. | Protection barrier apparatus |
MXPA05004811A (es) | 2002-11-06 | 2005-07-22 | Schering Corp | Inhibidores de absorcion de colesterol para el tratamiento de trastornos autoinmunes. |
US7235543B2 (en) * | 2003-03-07 | 2007-06-26 | Schering Corporation | Substituted azetidinone compounds, processes for preparing the same, formulations and uses thereof |
CN1805926A (zh) | 2003-05-05 | 2006-07-19 | 兰贝克赛实验室有限公司 | 二苯基氮杂环丁酮衍生物的反式异构体的制备方法 |
US20040259179A1 (en) | 2003-05-30 | 2004-12-23 | Gerd Assmann | Sterol markers as diagnostic tools in the prevention of atherosclerotic diseases and as tools to aid in the selection of agents to be used for the prevention and treatment of atherosclerotic disease |
US7002008B2 (en) * | 2003-06-16 | 2006-02-21 | Bomi Patel Framroze | Process for the preparation of 1-(4-fluorophenyl)-4(S)-(4-hydroxyphenyl)-azetidin-2-one |
JP2005015434A (ja) | 2003-06-27 | 2005-01-20 | Kotobuki Seiyaku Kk | 血清コレステロール低下剤或はアテローム性硬化症の予防又は治療剤 |
US20070072812A1 (en) | 2003-08-25 | 2007-03-29 | Microbia, Inc. | Quaternary salt derivatives of 1,4-diphenylazetidin-2-ones |
WO2005021497A2 (en) | 2003-08-28 | 2005-03-10 | Microbia, Inc. | Tethered dimers and trimers of 1,4-diphenylazetidn-2-ones |
EP1522541A1 (en) | 2003-10-07 | 2005-04-13 | Lipideon Biotechnology AG | Novel hypocholesterolemic compounds |
WO2005044256A1 (en) | 2003-10-30 | 2005-05-19 | Merck & Co., Inc. | 2-azetidinones as anti-hypercholesterolemic agents |
WO2005042692A2 (en) | 2003-10-31 | 2005-05-12 | Forbes Medi-Tech Inc. | A method of inhibiting the expression of genes which mediate cellular cholesterol influx in animal cells and inhibiting the production of proteins resulting from the expression of such genes using cholesterol absorption inhibitors |
EP1680189A2 (en) * | 2003-11-05 | 2006-07-19 | Schering Corporation | Combinations of lipid modulating agents and substituted azetidinones and treatments for vascular conditions |
PL380414A1 (pl) | 2003-11-10 | 2007-01-22 | Microbia, Inc. | 4-Diarylo-1- fenyloazetydyn-2-ony |
US7067675B2 (en) | 2003-11-24 | 2006-06-27 | Hetero Drugs Limited | Process for ezetimibe intermediate |
AU2004298375A1 (en) | 2003-12-17 | 2005-06-30 | Dainippon Sumitomo Pharma Co., Ltd. | Medicinal compositions and combinations |
US20050171080A1 (en) | 2003-12-23 | 2005-08-04 | Dr. Reddy's Laboratories, Inc. | Polymorphs of ezetimibe and process for preparation thereof |
GB0329778D0 (en) * | 2003-12-23 | 2004-01-28 | Astrazeneca Ab | Chemical compounds |
US7871998B2 (en) * | 2003-12-23 | 2011-01-18 | Astrazeneca Ab | Diphenylazetidinone derivatives possessing cholesterol absorption inhibitory activity |
AU2004308332B2 (en) * | 2003-12-23 | 2008-04-10 | Merck Sharp & Dohme Corp. | Anti-hypercholesterolemic compounds |
WO2005066120A2 (en) | 2003-12-30 | 2005-07-21 | Ranbaxy Laboratories Limited | Process for asymmetric synthesis of hydroxy-alkyl substituted azetidinone derivatives |
EP1723414A4 (en) | 2004-01-16 | 2008-03-26 | Merck & Co Inc | NPC1L1 (NPC3) AND METHOD FOR IDENTIFYING ITS LIGANDS |
ZA200609584B (en) | 2004-01-20 | 2008-06-25 | Panacea Biotec Ltd | Pharmaceutical compositions comprising higher primary alcohols and ezetimibe and process of preparation thereof |
KR100725758B1 (ko) * | 2004-03-30 | 2007-06-08 | 삼성광주전자 주식회사 | 전동 송풍기 및 이를 이용한 자동차용 전동 과급기 |
JP2007538042A (ja) | 2004-05-21 | 2007-12-27 | サノフィ−アベンティス・ドイチュラント・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツング | 1,4−ジフェニルアゼチジノン誘導体の製造方法 |
DE102004025072A1 (de) | 2004-05-21 | 2005-12-15 | Sanofi-Aventis Deutschland Gmbh | Verfahren zur Herstellung von Diphenyl-azetidinon-Derivaten |
WO2006017257A2 (en) | 2004-07-12 | 2006-02-16 | Phenomix Corporation | Azetidinone derivatives |
US20060046996A1 (en) * | 2004-08-31 | 2006-03-02 | Kowa Co., Ltd. | Method for treating hyperlipidemia |
MX2007003732A (es) * | 2004-09-29 | 2007-04-23 | Schering Corp | Combinaciones de azetidononas sustituidas y antagonistas de receptor de canabinoide 1. |
EP1817280A1 (en) | 2004-12-03 | 2007-08-15 | Teva Pharmaceutical Industries Ltd. | Ezetimibe polymorphs |
CA2591564A1 (en) | 2004-12-20 | 2006-06-29 | Schering Corporation | Process for the synthesis of azetidinones |
IL166149A0 (en) | 2005-01-05 | 2006-01-15 | Hadasit Med Res Service | Use of ezetimibe and amiodarone in protection against beta-amyloid neurotoxicity |
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WO2006102674A2 (en) | 2005-03-24 | 2006-09-28 | Microbia, Inc. | Diphenylheterocycle cholesterol absorption inhibitors |
MX2007012253A (es) | 2005-04-04 | 2007-12-07 | Univ Pontificia Catolica Chile | Uso de ezetimibe para la prevencion y tratamiento de calculos de colesterol en la via biliar. |
WO2006116499A1 (en) | 2005-04-26 | 2006-11-02 | Microbia, Inc. | 4-biarylyl-1-phenylazetidin-2-one glucuronide derivatives for hypercholesterolemia |
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WO2006122186A2 (en) | 2005-05-10 | 2006-11-16 | Microbia, Inc. | 1,4-diphenyl-3-hydroxyalkyl-2-azetidinone derivatives for treating hypercholestrolemia |
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SA06270191B1 (ar) | 2005-06-22 | 2010-03-29 | استرازينيكا ايه بي | مشتقات من 2- أزيتيدينون جديدة باعتبارها مثبطات لامتصاص الكوليسترول لعلاج حالات فرط نسبة الدهون في الدم |
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US20070049748A1 (en) * | 2005-08-26 | 2007-03-01 | Uppala Venkata Bhaskara R | Preparation of ezetimibe |
WO2007030721A2 (en) | 2005-09-08 | 2007-03-15 | Teva Pharmaceutical Industries Ltd. | Processes for the preparation of (3r,4s)-4-((4-benzyloxy)phenyl)-1-(4-fluorophenyl)-3-((s)-3-(4-fluorophenyl)-3-hydroxypropyl)-2-azetidinone, an intermediate for the synthesis of ezetimibe |
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WO2007058335A1 (en) | 2005-11-15 | 2007-05-24 | Takeda Pharmaceutical Company Limited | Use of tak-475 together with ezetimibe for treating hyperlipidemia |
DE102005055726A1 (de) | 2005-11-23 | 2007-08-30 | Sanofi-Aventis Deutschland Gmbh | Hydroxy-substituierte Diphenylazetidinone, Verfahren zu deren Herstellung, diese Verbindungen enthaltende Arzneimittel und deren Verwendung |
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HUP0501164A2 (en) | 2005-12-20 | 2007-07-30 | Richter Gedeon Nyrt | New industrial process for the production of ezetimibe |
CA2634940A1 (en) | 2005-12-21 | 2007-07-05 | Schering Corporation | Treatment of nonalcoholic fatty liver disease using cholesterol lowering agents and h3 receptor antagonist/inverse agonist |
TW200811098A (en) * | 2006-04-27 | 2008-03-01 | Astrazeneca Ab | Chemical compounds |
MX2009002924A (es) * | 2006-09-15 | 2009-05-28 | Schering Corp | Derivados de azetidinona espirociclica para el tratamiento de trastornos del metabolismo de los lipidos, el dolor, la diabetes y otros trastornos. |
EP2133347A4 (en) * | 2007-03-06 | 2010-03-17 | Teijin Pharma Ltd | 1-BIARYLAZETIDINONDERIVATE |
-
2006
- 2006-06-16 UY UY29607A patent/UY29607A1/es unknown
- 2006-06-19 BR BRPI0612254A patent/BRPI0612254A2/pt not_active IP Right Cessation
- 2006-06-19 CA CA002610890A patent/CA2610890A1/en not_active Abandoned
- 2006-06-19 RU RU2007147338/04A patent/RU2007147338A/ru not_active Application Discontinuation
- 2006-06-19 AU AU2006259949A patent/AU2006259949A1/en not_active Abandoned
- 2006-06-19 CN CNA2006800264766A patent/CN101228123A/zh active Pending
- 2006-06-19 KR KR1020087001031A patent/KR20080019710A/ko not_active Application Discontinuation
- 2006-06-19 EP EP06747933A patent/EP1896407A4/en not_active Withdrawn
- 2006-06-19 US US11/993,033 patent/US7863265B2/en not_active Expired - Fee Related
- 2006-06-19 MX MX2007016483A patent/MX2007016483A/es not_active Application Discontinuation
- 2006-06-19 WO PCT/SE2006/000741 patent/WO2006137782A1/en active Application Filing
- 2006-06-19 JP JP2008518077A patent/JP2008546766A/ja active Pending
- 2006-06-20 AR ARP060102624A patent/AR054484A1/es unknown
- 2006-06-20 TW TW095122114A patent/TW200730493A/zh unknown
-
2007
- 2007-11-28 IL IL187736A patent/IL187736A0/en unknown
- 2007-11-28 NO NO20076137A patent/NO20076137L/no not_active Application Discontinuation
- 2007-11-30 ZA ZA200710415A patent/ZA200710415B/xx unknown
-
2008
- 2008-01-17 EC EC2008008114A patent/ECSP088114A/es unknown
Also Published As
Publication number | Publication date |
---|---|
EP1896407A4 (en) | 2010-06-16 |
AU2006259949A1 (en) | 2006-12-28 |
IL187736A0 (en) | 2008-08-07 |
KR20080019710A (ko) | 2008-03-04 |
US7863265B2 (en) | 2011-01-04 |
AR054484A1 (es) | 2007-06-27 |
BRPI0612254A2 (pt) | 2016-09-06 |
WO2006137782A1 (en) | 2006-12-28 |
UY29607A1 (es) | 2007-01-31 |
JP2008546766A (ja) | 2008-12-25 |
CN101228123A (zh) | 2008-07-23 |
ECSP088114A (es) | 2008-02-20 |
TW200730493A (en) | 2007-08-16 |
RU2007147338A (ru) | 2009-07-27 |
NO20076137L (no) | 2008-01-18 |
EP1896407A1 (en) | 2008-03-12 |
MX2007016483A (es) | 2008-03-10 |
ZA200710415B (en) | 2008-10-29 |
US20100216759A1 (en) | 2010-08-26 |
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Legal Events
Date | Code | Title | Description |
---|---|---|---|
FZDE | Discontinued |