DK2206697T3 - Exo- og diastereo-selektive synteser af himbacinanaloger - Google Patents

Exo- og diastereo-selektive synteser af himbacinanaloger

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Publication number
DK2206697T3
DK2206697T3 DK10001844.9T DK10001844T DK2206697T3 DK 2206697 T3 DK2206697 T3 DK 2206697T3 DK 10001844 T DK10001844 T DK 10001844T DK 2206697 T3 DK2206697 T3 DK 2206697T3
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DK
Denmark
Prior art keywords
diastereo
exo
selective syntheses
himbacin
analogs
Prior art date
Application number
DK10001844.9T
Other languages
English (en)
Inventor
George G Wu
Anantha Sudhakar
Tao Wang
Ji Xie
Frank Xing Chen
Marc Poirier
Mingsheng Huang
Vijay Sabesen
Daw-Long Kwok
Jian Cui
Xiaojing Yang
Tiruvettipuram K Thiruvengadam
Jing Liao
Original Assignee
Schering Corp
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 Schering Corp filed Critical Schering Corp
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Publication of DK2206697T3 publication Critical patent/DK2206697T3/da

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    • C07D263/00Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/52Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings condensed with carbocyclic rings or ring systems
    • C07D263/54Benzoxazoles; Hydrogenated benzoxazoles
    • C07D263/56Benzoxazoles; Hydrogenated benzoxazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
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    • C07C201/00Preparation of esters of nitric or nitrous acid or of compounds containing nitro or nitroso groups bound to a carbon skeleton
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    • C07C201/10Preparation of nitro compounds by substitution of functional groups by nitro groups
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    • C07C201/00Preparation of esters of nitric or nitrous acid or of compounds containing nitro or nitroso groups bound to a carbon skeleton
    • C07C201/06Preparation of nitro compounds
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    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
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    • C07C205/00Compounds containing nitro groups bound to a carbon skeleton
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    • C07C205/55Compounds containing nitro groups bound to a carbon skeleton the carbon skeleton being further substituted by carboxyl groups having nitro groups or carboxyl groups bound to carbon atoms of rings other than six-membered aromatic rings of the carbon skeleton
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    • C07C231/00Preparation of carboxylic acid amides
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    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
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    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C235/00Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
    • C07C235/02Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton
    • C07C235/28Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton being acyclic and unsaturated
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    • C07C303/00Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides
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    • C07C309/00Sulfonic acids; Halides, esters, or anhydrides thereof
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    • C07C309/02Sulfonic acids having sulfo groups bound to acyclic carbon atoms
    • C07C309/03Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
    • C07C309/07Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton containing oxygen atoms bound to the carbon skeleton
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    • C07C69/52Esters of acyclic unsaturated carboxylic acids having the esterified carboxyl group bound to an acyclic carbon atom
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    • C07C69/66Esters 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
    • C07C69/73Esters 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
    • C07C69/732Esters 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
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    • C07D277/00Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/60Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
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    • C07D307/92Naphthofurans; Hydrogenated naphthofurans
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    • C07D333/00Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/50Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D333/52Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes
    • C07D333/54Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
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    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
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    • C07D417/06Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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    • C07F7/00Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02Silicon compounds
    • C07F7/08Compounds having one or more C—Si linkages
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    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/553Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
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    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02PCLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
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  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Urology & Nephrology (AREA)
  • Pain & Pain Management (AREA)
  • Vascular Medicine (AREA)
  • Hematology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Rheumatology (AREA)
  • Cardiology (AREA)
  • Diabetes (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Furan Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Peptides Or Proteins (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
DK10001844.9T 2005-01-14 2006-01-12 Exo- og diastereo-selektive synteser af himbacinanaloger DK2206697T3 (da)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US64446405P 2005-01-14 2005-01-14
EP06718069A EP1848705B1 (en) 2005-01-14 2006-01-12 Exo- and diastereo- selective syntheses of himbacine analogs

Publications (1)

Publication Number Publication Date
DK2206697T3 true DK2206697T3 (da) 2012-02-13

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DK10001844.9T DK2206697T3 (da) 2005-01-14 2006-01-12 Exo- og diastereo-selektive synteser af himbacinanaloger
DK06718069.5T DK1848705T3 (da) 2005-01-14 2006-01-12 EXO- og diastereoselektive synteser af himbacin-analoger

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Country Status (22)

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US (4) US7605275B2 (da)
EP (4) EP2206697B1 (da)
JP (3) JP4681616B2 (da)
CN (2) CN101193880B (da)
AR (1) AR056919A1 (da)
AT (2) ATE458726T1 (da)
CA (2) CA2875768C (da)
CY (2) CY1109896T1 (da)
DE (1) DE602006012450D1 (da)
DK (2) DK2206697T3 (da)
ES (3) ES2339696T3 (da)
HK (1) HK1108893A1 (da)
HR (2) HRP20100218T1 (da)
ME (1) ME01967B (da)
MX (1) MX2007008665A (da)
PL (2) PL1848705T3 (da)
PT (2) PT1848705E (da)
RS (2) RS52117B (da)
SG (2) SG192505A1 (da)
SI (2) SI1848705T1 (da)
WO (1) WO2006076415A2 (da)
ZA (1) ZA200706711B (da)

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US7488742B2 (en) * 2000-06-15 2009-02-10 Schering Corporation Thrombin receptor antagonists
MX2007008665A (es) 2005-01-14 2008-03-04 Schering Corp Sintesis exo- y diastereo-selectivas de analogos de himbacina.
AR052870A1 (es) * 2005-01-14 2007-04-11 Schering Corp Sintesis de analogos de himbacina
AR052871A1 (es) * 2005-01-14 2007-04-11 Schering Corp Una sintesis exo-selectiva de analogos de himbacina
CN101384259A (zh) * 2005-12-22 2009-03-11 先灵公司 作为预防来自心肺外科手术的并发症的凝血酶受体拮抗剂
AR061727A1 (es) * 2006-06-30 2008-09-17 Schering Corp Sintesis de dietil [[ 5- ( 3-fluorofenil) -piridin -2il] metil] fosfonato
CN101511770B (zh) * 2006-06-30 2013-05-08 默沙东公司 3-(5-硝基环己-1-烯基)丙烯酸和其酯的合成
CN101610999A (zh) * 2006-12-15 2009-12-23 先灵公司 α-酮酰胺的亚硫酸氢盐纯化方法
CA3014633C (en) 2007-10-08 2022-05-17 Aurinia Pharmaceuticals Inc. Ophthalmic compositions comprising calcineurin inhibitors or mtor inhibitors
ES2398502T3 (es) * 2007-10-24 2013-03-19 Merck Sharp & Dohme Corp. Procedimiento sintético de alta pureza para la preparación de intermediarios de éster de ácido dodecahidro-nafto-furanil carbámico
WO2012175825A1 (fr) * 2011-06-21 2012-12-27 Bluestar Silicones France Inhibiteurs de reaction d'hydrosilylation, et leur application pour la preparation de compositions silicones durcissables stables.
CN105330689B (zh) * 2014-08-08 2018-08-17 博瑞生物医药(苏州)股份有限公司 制备Himbacine类似物中间体的制备方法
CN105985303B (zh) * 2015-02-13 2020-08-14 上海彩迩文生化科技有限公司 抗凝血剂的制备方法、中间体及其制备方法
CN105348241B (zh) * 2015-12-11 2017-09-05 南京华威医药科技开发有限公司 一种硫酸沃拉帕沙中间体的合成方法
US11247940B2 (en) 2016-10-26 2022-02-15 The Regents Of The University Of California Efficient integration of manufacturing of upcycled concrete product into power plants
CN106749138B (zh) * 2016-12-07 2019-08-16 扬子江药业集团四川海蓉药业有限公司 一种硫酸沃拉帕沙中间体醛的制备方法
CN106866450B (zh) * 2017-01-13 2019-01-11 阜阳欣奕华材料科技有限公司 硫酸沃拉帕沙中间体的制备方法
CN108658910B (zh) * 2017-03-29 2020-11-03 北京新领先医药科技发展有限公司 一种沃拉帕沙中间体1-α的制备方法
US20190224275A1 (en) 2017-05-12 2019-07-25 Aurinia Pharmaceuticals Inc. Protocol for treatment of lupus nephritis
WO2019006352A1 (en) * 2017-06-30 2019-01-03 The Regents Of The University Of California CO2 MINERALIZATION IN PRODUTED AND INDUSTRIAL EFFLUENT WATER BY PH CHANGE CARBONATION
WO2019036386A1 (en) 2017-08-14 2019-02-21 The Regents Of The University Of California MITIGATION OF THE ALKALI-SILICA REACTION IN CONCRETE USING EASILY SOLUBLE CHEMICAL ADDITIVES
WO2019057946A1 (en) 2017-09-25 2019-03-28 F. Hoffmann-La Roche Ag MULTI-CYCLIC AROMATIC COMPOUNDS AS D-FACTOR INHIBITORS
US11384029B2 (en) 2019-03-18 2022-07-12 The Regents Of The University Of California Formulations and processing of cementitious components to meet target strength and CO2 uptake criteria

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US6063847A (en) * 1997-11-25 2000-05-16 Schering Corporation Thrombin receptor antagonists
AU747204B2 (en) * 1997-11-25 2002-05-09 Schering Corporation Thrombin receptor antagonists
CN1168694C (zh) * 1998-05-05 2004-09-29 伊莱利利公司 醛的纯化
US7235567B2 (en) * 2000-06-15 2007-06-26 Schering Corporation Crystalline polymorph of a bisulfate salt of a thrombin receptor antagonist
US7488742B2 (en) * 2000-06-15 2009-02-10 Schering Corporation Thrombin receptor antagonists
US20040192753A1 (en) 2000-06-15 2004-09-30 Samuel Chackalamannil Methods of use of thrombin receptor antagonists
ATE368659T1 (de) * 2000-06-15 2007-08-15 Schering Corp Thrombinrezeptorantagonisten
US8124625B2 (en) * 2001-09-14 2012-02-28 Shionogi & Co., Ltd. Method of enhancing the expression of apolipoprotein AI using olefin derivatives
IL160918A0 (en) * 2001-10-18 2004-08-31 Schering Corp Himbacine analogues as thrombin receptor antagonists
DK1495018T3 (da) * 2002-04-16 2008-02-18 Schering Corp Tricykliske trombinreceptorantagonister
MXPA06013903A (es) * 2004-05-28 2007-01-26 Schering Corp Analogos restringidos de himbacina como antagonistas del receptor de trombina.
AR052871A1 (es) * 2005-01-14 2007-04-11 Schering Corp Una sintesis exo-selectiva de analogos de himbacina
US7541471B2 (en) * 2005-01-14 2009-06-02 Schering Corporation Synthesis of himbacine analogs
MX2007008665A (es) 2005-01-14 2008-03-04 Schering Corp Sintesis exo- y diastereo-selectivas de analogos de himbacina.
AR052870A1 (es) * 2005-01-14 2007-04-11 Schering Corp Sintesis de analogos de himbacina

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EP2196454A2 (en) 2010-06-16
CN101193880B (zh) 2012-08-22
EP2196468B1 (en) 2013-04-10
ES2339696T3 (es) 2010-05-24
ME01967B (me) 2012-08-31
EP2196454B1 (en) 2014-08-27
CY1109896T1 (el) 2014-09-10
EP2196468A1 (en) 2010-06-16
JP2013177407A (ja) 2013-09-09
SG192505A1 (en) 2013-08-30
SI2206697T1 (sl) 2012-02-29
ZA200706711B (en) 2014-01-29
US20120296093A1 (en) 2012-11-22
RS51315B (sr) 2010-12-31
EP1848705B1 (en) 2010-02-24
JP2011098967A (ja) 2011-05-19
SG158888A1 (en) 2010-02-26
PL2206697T3 (pl) 2012-03-30
EP1848705A2 (en) 2007-10-31
CY1112371T1 (el) 2015-12-09
US20090281321A1 (en) 2009-11-12
US7605275B2 (en) 2009-10-20
EP2196454A3 (en) 2010-09-22
CA2594871A1 (en) 2006-07-20
PT2206697E (pt) 2012-01-10
EP2206697B1 (en) 2011-10-26
ES2374379T3 (es) 2012-02-16
JP2008526972A (ja) 2008-07-24
AR056919A1 (es) 2007-11-07
CA2594871C (en) 2015-04-07
JP4681616B2 (ja) 2011-05-11
WO2006076415A2 (en) 2006-07-20
SI1848705T1 (sl) 2010-06-30
HRP20100218T1 (hr) 2010-05-31
HRP20110963T1 (hr) 2012-01-31
ATE458726T1 (de) 2010-03-15
CN102757423A (zh) 2012-10-31
ES2412981T3 (es) 2013-07-15
WO2006076415A3 (en) 2006-11-16
US20110251392A1 (en) 2011-10-13
US8258319B2 (en) 2012-09-04
JP5388231B2 (ja) 2014-01-15
US7989653B2 (en) 2011-08-02
US8618314B2 (en) 2013-12-31
MX2007008665A (es) 2008-03-04
ATE530516T1 (de) 2011-11-15
PL1848705T3 (pl) 2010-07-30
CA2875768A1 (en) 2006-07-20
PT1848705E (pt) 2010-05-10
EP2206697A1 (en) 2010-07-14
RS52117B (en) 2012-08-31
CN101193880A (zh) 2008-06-04
US20060247450A1 (en) 2006-11-02
CA2875768C (en) 2018-03-06
DK1848705T3 (da) 2010-06-14
DE602006012450D1 (de) 2010-04-08
CN102757423B (zh) 2016-04-20
HK1108893A1 (en) 2008-05-23
JP5911447B2 (ja) 2016-04-27

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