SI1848705T1 - Eksoselektivne in diastereoselektivne sinteze himbacinskih analogov - Google Patents

Eksoselektivne in diastereoselektivne sinteze himbacinskih analogov

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Publication number
SI1848705T1
SI1848705T1 SI200630633T SI200630633T SI1848705T1 SI 1848705 T1 SI1848705 T1 SI 1848705T1 SI 200630633 T SI200630633 T SI 200630633T SI 200630633 T SI200630633 T SI 200630633T SI 1848705 T1 SI1848705 T1 SI 1848705T1
Authority
SI
Slovenia
Prior art keywords
diastereo
exo
selective syntheses
himbacine analogs
himbacine
Prior art date
Application number
SI200630633T
Other languages
English (en)
Inventor
George Wu
Anantha Sudhakar
Tao Wang
Ji Xie
Frank Xing Chen
Marc Poirier
Mingsheng Huang
Vijay Sabesan
Daw-Long Kwok
Jian Cui
Xiaojing Yang
Tiruvettipuram K Thiruvengadam
Jing Liao
Ilia Zavialov
Hoa N Nguyen
Ngiap Kie Lim
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
Publication of SI1848705T1 publication Critical patent/SI1848705T1/sl

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    • C07ORGANIC CHEMISTRY
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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
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
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    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • 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
    • C07C201/10Preparation of nitro compounds by substitution of functional groups by nitro groups
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    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • 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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    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C205/00Compounds containing nitro groups bound to a carbon skeleton
    • C07C205/44Compounds containing nitro groups bound to a carbon skeleton the carbon skeleton being further substituted by —CHO groups
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    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • 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
    • C07C309/01Sulfonic acids
    • 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
    • C07C309/08Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton containing oxygen atoms bound to the carbon skeleton containing hydroxy groups bound to the carbon skeleton
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    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C69/00Esters of carboxylic acids; Esters of carbonic or haloformic acids
    • C07C69/52Esters of acyclic unsaturated carboxylic acids having the esterified carboxyl group bound to an acyclic carbon atom
    • C07C69/606Esters of acyclic unsaturated carboxylic acids having the esterified carboxyl group bound to an acyclic carbon atom having only or additionally carbon-to-carbon triple bonds as unsaturation in the carboxylic acid moiety
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    • C07C69/00Esters of carboxylic acids; Esters of carbonic or haloformic acids
    • 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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    • C07DHETEROCYCLIC COMPOUNDS
    • 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
    • C07D277/62Benzothiazoles
    • C07D277/64Benzothiazoles with only hydrocarbon or substituted hydrocarbon radicals attached in position 2
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    • C07DHETEROCYCLIC COMPOUNDS
    • C07D307/00Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/77Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D307/92Naphthofurans; Hydrogenated naphthofurans
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • 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
    • C07D333/56Radicals substituted by oxygen atoms
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    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/06Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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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
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/06Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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
    • 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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    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00Compounds containing elements of Groups 4 or 14 of the Periodic System
    • C07F7/02Silicon compounds
    • C07F7/08Compounds having one or more C—Si linkages
    • C07F7/18Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
    • C07F7/1804Compounds having Si-O-C linkages
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    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic System
    • 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
    • C07F9/576Six-membered rings
    • C07F9/58Pyridine rings
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    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00Systems containing only non-condensed rings
    • C07C2601/12Systems containing only non-condensed rings with a six-membered ring
    • C07C2601/16Systems containing only non-condensed rings with a six-membered ring the ring being unsaturated
    • 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
    • Y02P20/00Technologies relating to chemical industry
    • Y02P20/50Improvements relating to the production of bulk chemicals
    • Y02P20/55Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups
SI200630633T 2005-01-14 2006-01-12 Eksoselektivne in diastereoselektivne sinteze himbacinskih analogov SI1848705T1 (sl)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US64446405P 2005-01-14 2005-01-14
PCT/US2006/000954 WO2006076415A2 (en) 2005-01-14 2006-01-12 Exo- and diastereo- selective syntheses of himbacine analogs
EP06718069A EP1848705B1 (en) 2005-01-14 2006-01-12 Exo- and diastereo- selective syntheses of himbacine analogs

Publications (1)

Publication Number Publication Date
SI1848705T1 true SI1848705T1 (sl) 2010-06-30

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SI200630633T SI1848705T1 (sl) 2005-01-14 2006-01-12 Eksoselektivne in diastereoselektivne sinteze himbacinskih analogov
SI200631234T SI2206697T1 (sl) 2005-01-14 2006-01-12 Ekso- in diastereo-selektivne sinteze himbacinskih analogov

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US (4) US7605275B2 (sl)
EP (4) EP2196468B1 (sl)
JP (3) JP4681616B2 (sl)
CN (2) CN101193880B (sl)
AR (1) AR056919A1 (sl)
AT (2) ATE530516T1 (sl)
CA (2) CA2875768C (sl)
CY (2) CY1109896T1 (sl)
DE (1) DE602006012450D1 (sl)
DK (2) DK2206697T3 (sl)
ES (3) ES2412981T3 (sl)
HK (1) HK1108893A1 (sl)
HR (2) HRP20100218T1 (sl)
ME (1) ME01967B (sl)
MX (1) MX2007008665A (sl)
PL (2) PL1848705T3 (sl)
PT (2) PT1848705E (sl)
RS (2) RS52117B (sl)
SG (2) SG192505A1 (sl)
SI (2) SI1848705T1 (sl)
WO (1) WO2006076415A2 (sl)
ZA (1) ZA200706711B (sl)

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US7488742B2 (en) * 2000-06-15 2009-02-10 Schering Corporation Thrombin receptor antagonists
DK2206697T3 (da) 2005-01-14 2012-02-13 Schering Corp Exo- og diastereo-selektive synteser af himbacinanaloger
AR052871A1 (es) * 2005-01-14 2007-04-11 Schering Corp Una sintesis exo-selectiva de analogos de himbacina
WO2006076564A1 (en) * 2005-01-14 2006-07-20 Schering Corporation Synthesis of himbacine analogs
WO2007075964A2 (en) * 2005-12-22 2007-07-05 Schering Corporation Thrombin receptor antagonists as prophylaxis to complications from cardiopulmonary surgery
US7553987B2 (en) * 2006-06-30 2009-06-30 Schering Corporation Synthesis of 3-(5-nitrocyclohex-1-enyl) acrylic acid and esters thereof
AR061727A1 (es) * 2006-06-30 2008-09-17 Schering Corp Sintesis de dietil [[ 5- ( 3-fluorofenil) -piridin -2il] metil] fosfonato
WO2008076316A2 (en) * 2006-12-15 2008-06-26 Schering Corporation Bisulfite purification of an alpha-keto amide
CN101918019B (zh) 2007-10-08 2014-11-26 奥里尼亚制药有限公司 包含钙调神经磷酸酶抑制剂或mTOR抑制剂的眼科组合物
JP5432910B2 (ja) * 2007-10-24 2014-03-05 メルク・シャープ・アンド・ドーム・コーポレーション ドデカヒドロ−ナフト−フラニル−カルバミン酸エステル中間体調製のための高純度合成プロセス
JP5945593B2 (ja) * 2011-06-21 2016-07-05 ブルースター・シリコーンズ・フランス・エスアエス ヒドロシリル化反応抑制剤及び安定な硬化性シリコーン組成物を調製するためのその使用
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
US11339094B2 (en) 2017-08-14 2022-05-24 The Regents Of The University Of California Mitigation of alkali-silica reaction in concrete using readily-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
CN1290265A (zh) * 1997-11-25 2001-04-04 先灵公司 凝血酶受体拮抗剂
TR200003203T2 (tr) * 1998-05-05 2001-03-21 Eli Lilly And Company Karboksaldehitin saflaştırılması
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
ES2291323T3 (es) 2000-06-15 2008-03-01 Schering Corporation Antagonistas de receptores de trombina.
US7235567B2 (en) 2000-06-15 2007-06-26 Schering Corporation Crystalline polymorph of a bisulfate salt of a thrombin receptor antagonist
US8124625B2 (en) * 2001-09-14 2012-02-28 Shionogi & Co., Ltd. Method of enhancing the expression of apolipoprotein AI using olefin derivatives
KR100960170B1 (ko) * 2001-10-18 2010-05-26 쉐링 코포레이션 트롬빈 수용체 길항제로서의 힘바신 동족체
DE60317493T3 (de) * 2002-04-16 2018-07-12 Merck Sharp & Dohme Corp. Trizyklische thrombin rezeptor antagonisten
ES2311996T3 (es) * 2004-05-28 2009-02-16 Schering Corporation Analogos retringidos 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
WO2006076564A1 (en) * 2005-01-14 2006-07-20 Schering Corporation Synthesis of himbacine analogs
US7541471B2 (en) * 2005-01-14 2009-06-02 Schering Corporation Synthesis of himbacine analogs
DK2206697T3 (da) 2005-01-14 2012-02-13 Schering Corp Exo- og diastereo-selektive synteser af himbacinanaloger

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CY1112371T1 (el) 2015-12-09
CN102757423A (zh) 2012-10-31
ZA200706711B (en) 2014-01-29
SG158888A1 (en) 2010-02-26
US8618314B2 (en) 2013-12-31
US20110251392A1 (en) 2011-10-13
CN101193880A (zh) 2008-06-04
CA2875768C (en) 2018-03-06
RS52117B (en) 2012-08-31
HK1108893A1 (en) 2008-05-23
ES2412981T3 (es) 2013-07-15
US8258319B2 (en) 2012-09-04
DE602006012450D1 (de) 2010-04-08
SG192505A1 (en) 2013-08-30
EP1848705B1 (en) 2010-02-24
JP2011098967A (ja) 2011-05-19
EP2206697B1 (en) 2011-10-26
JP2013177407A (ja) 2013-09-09
JP5911447B2 (ja) 2016-04-27
US20060247450A1 (en) 2006-11-02
SI2206697T1 (sl) 2012-02-29
JP2008526972A (ja) 2008-07-24
US20090281321A1 (en) 2009-11-12
ATE458726T1 (de) 2010-03-15
EP2196454A2 (en) 2010-06-16
AR056919A1 (es) 2007-11-07
WO2006076415A2 (en) 2006-07-20
CA2875768A1 (en) 2006-07-20
ES2339696T3 (es) 2010-05-24
ME01967B (me) 2012-08-31
CA2594871C (en) 2015-04-07
JP5388231B2 (ja) 2014-01-15
PT2206697E (pt) 2012-01-10
EP2196454A3 (en) 2010-09-22
JP4681616B2 (ja) 2011-05-11
CY1109896T1 (el) 2014-09-10
US7989653B2 (en) 2011-08-02
ES2374379T3 (es) 2012-02-16
EP2196468B1 (en) 2013-04-10
US20120296093A1 (en) 2012-11-22
PT1848705E (pt) 2010-05-10
HRP20100218T1 (hr) 2010-05-31
HRP20110963T1 (hr) 2012-01-31
EP2196468A1 (en) 2010-06-16
ATE530516T1 (de) 2011-11-15
EP1848705A2 (en) 2007-10-31
CN102757423B (zh) 2016-04-20
PL1848705T3 (pl) 2010-07-30
WO2006076415A3 (en) 2006-11-16
EP2196454B1 (en) 2014-08-27
DK2206697T3 (da) 2012-02-13
DK1848705T3 (da) 2010-06-14
PL2206697T3 (pl) 2012-03-30
MX2007008665A (es) 2008-03-04
EP2206697A1 (en) 2010-07-14
CA2594871A1 (en) 2006-07-20
RS51315B (sr) 2010-12-31
CN101193880B (zh) 2012-08-22
US7605275B2 (en) 2009-10-20

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