JP2010514681A - 抗凝血剤として有用な大環状第ｖｉｉａ因子阻害剤 - Google Patents
抗凝血剤として有用な大環状第ｖｉｉａ因子阻害剤 Download PDFInfo
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- JP2010514681A JP2010514681A JP2009543158A JP2009543158A JP2010514681A JP 2010514681 A JP2010514681 A JP 2010514681A JP 2009543158 A JP2009543158 A JP 2009543158A JP 2009543158 A JP2009543158 A JP 2009543158A JP 2010514681 A JP2010514681 A JP 2010514681A
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- JJNCRKLSAULKQR-UHFFFAOYSA-N Cc1cc(C(C(O)=O)Nc(cc2)cc3c2C=CNC3=O)cc(C)c1CCO Chemical compound Cc1cc(C(C(O)=O)Nc(cc2)cc3c2C=CNC3=O)cc(C)c1CCO JJNCRKLSAULKQR-UHFFFAOYSA-N 0.000 description 1
- VSXCTCMFQVDJTB-UHFFFAOYSA-N NC(c(cc(cc1)[N+]([O-])=O)c1OC(F)(F)F)N Chemical compound NC(c(cc(cc1)[N+]([O-])=O)c1OC(F)(F)F)N VSXCTCMFQVDJTB-UHFFFAOYSA-N 0.000 description 1
- GSQUVIBWTKWASE-UHFFFAOYSA-N NN(CCc1ccccc11)C1=O Chemical compound NN(CCc1ccccc11)C1=O GSQUVIBWTKWASE-UHFFFAOYSA-N 0.000 description 1
- PAEMWNBWAKIGLQ-UHFFFAOYSA-N Nc(cc1)cc2c1C(F)=CNC2=O Chemical compound Nc(cc1)cc2c1C(F)=CNC2=O PAEMWNBWAKIGLQ-UHFFFAOYSA-N 0.000 description 1
- KKPITLYHSOXPTM-UHFFFAOYSA-N Nc1cc(C2NCCC2)ccc1 Chemical compound Nc1cc(C2NCCC2)ccc1 KKPITLYHSOXPTM-UHFFFAOYSA-N 0.000 description 1
- POQDPPCZQPFEDZ-DNVCBOLYSA-N O=C(Cc(ccc([BrH+])c1)c1Cl)N([C@](C1)(CO2)[C@H]1c1ccccc1)C2=O Chemical compound O=C(Cc(ccc([BrH+])c1)c1Cl)N([C@](C1)(CO2)[C@H]1c1ccccc1)C2=O POQDPPCZQPFEDZ-DNVCBOLYSA-N 0.000 description 1
- UBQKCCHYAOITMY-UHFFFAOYSA-N O=C1NC=CC=C1 Chemical compound O=C1NC=CC=C1 UBQKCCHYAOITMY-UHFFFAOYSA-N 0.000 description 1
- YWPMKTWUFVOFPL-UHFFFAOYSA-N O=C1NCCc2ccccc12 Chemical compound O=C1NCCc2ccccc12 YWPMKTWUFVOFPL-UHFFFAOYSA-N 0.000 description 1
- XGYCWCIGCYGQFU-UHFFFAOYSA-N O=S1(NCCC1)=O Chemical compound O=S1(NCCC1)=O XGYCWCIGCYGQFU-UHFFFAOYSA-N 0.000 description 1
- DNGMYXZLJGHHOM-UHFFFAOYSA-N O=S1(NCCCC1)=O Chemical compound O=S1(NCCCC1)=O DNGMYXZLJGHHOM-UHFFFAOYSA-N 0.000 description 1
- ZDPJGAWPRHNQHI-QMMMGPOBSA-N OC[C@@H](c(cc1)ccc1Br)O Chemical compound OC[C@@H](c(cc1)ccc1Br)O ZDPJGAWPRHNQHI-QMMMGPOBSA-N 0.000 description 1
- WVDDGKGOMKODPV-UHFFFAOYSA-N OCc1ccccc1 Chemical compound OCc1ccccc1 WVDDGKGOMKODPV-UHFFFAOYSA-N 0.000 description 1
- MOBNCKURXDGQCB-UHFFFAOYSA-N [O-][N+](c(cc1)cc2c1N=CNC2=O)=O Chemical compound [O-][N+](c(cc1)cc2c1N=CNC2=O)=O MOBNCKURXDGQCB-UHFFFAOYSA-N 0.000 description 1
- PPXUVXCYQWPGGE-UHFFFAOYSA-N [O-][N+](c(cc1C=O)cc(F)c1O)=O Chemical compound [O-][N+](c(cc1C=O)cc(F)c1O)=O PPXUVXCYQWPGGE-UHFFFAOYSA-N 0.000 description 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D271/00—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
- C07D271/12—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms condensed with carbocyclic rings or ring systems
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
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- A—HUMAN NECESSITIES
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- A61P3/06—Antihyperlipidemics
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- A—HUMAN NECESSITIES
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- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
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- A—HUMAN NECESSITIES
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
-
- 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
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- 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
- A61P9/06—Antiarrhythmics
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- 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
- A61P9/08—Vasodilators for multiple indications
-
- A—HUMAN NECESSITIES
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- 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
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- 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
- A61P9/12—Antihypertensives
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D255/00—Heterocyclic compounds containing rings having three nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D249/00 - C07D253/00
- C07D255/04—Heterocyclic compounds containing rings having three nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D249/00 - C07D253/00 condensed with carbocyclic rings or ring systems
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
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- Endocrinology (AREA)
- Child & Adolescent Psychology (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Pulmonology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
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| US87086406P | 2006-12-20 | 2006-12-20 | |
| US98446007P | 2007-11-01 | 2007-11-01 | |
| PCT/US2007/088032 WO2008079836A2 (en) | 2006-12-20 | 2007-12-19 | Macrocyclic factor viia inhibitors useful as anticoagulants |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2010514681A true JP2010514681A (ja) | 2010-05-06 |
| JP2010514681A5 JP2010514681A5 (enExample) | 2010-09-16 |
Family
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| Application Number | Title | Priority Date | Filing Date |
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| Country | Link |
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| US (1) | US8420830B2 (enExample) |
| EP (1) | EP2102176A2 (enExample) |
| JP (1) | JP2010514681A (enExample) |
| AR (1) | AR064471A1 (enExample) |
| AU (1) | AU2007337025A1 (enExample) |
| CA (1) | CA2673598A1 (enExample) |
| CL (1) | CL2007003718A1 (enExample) |
| MX (1) | MX2009006689A (enExample) |
| NO (1) | NO20092279L (enExample) |
| PE (1) | PE20081775A1 (enExample) |
| TW (1) | TW200836735A (enExample) |
| WO (1) | WO2008079836A2 (enExample) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2015506934A (ja) * | 2011-12-27 | 2015-03-05 | バイオ−ファーム ソリューションズ カンパニー リミテッド | フェニルアルキルカルバメート誘導体化合物およびこれを含む薬学組成物 |
Families Citing this family (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2099783A1 (en) | 2006-12-20 | 2009-09-16 | Brystol-Myers Squibb Company | Bicyclic lactam factor viia inhibitors useful as anticoagulants |
| EA201200820A1 (ru) * | 2009-12-08 | 2013-01-30 | Бёрингер Ингельхайм Интернациональ Гмбх | Способ синтеза промежуточных продуктов, применимых для получения замещенных индазолов и азаиндазолов |
| TWI520965B (zh) | 2010-02-11 | 2016-02-11 | 必治妥美雅史谷比公司 | 作為因子ｘｉａ抑制劑之巨環類 |
| CN102993065B (zh) * | 2011-09-13 | 2015-07-29 | 中国科学院上海药物研究所 | 含手性叔丁基亚磺酰基的α-芳基氨基酸酯类化合物、其制备方法及用途 |
| EP2766346B1 (en) | 2011-10-14 | 2017-03-29 | Bristol-Myers Squibb Company | Substituted tetrahydroisoquinoline compounds as factor xia inhibitors |
| EP2858977A1 (en) * | 2012-06-08 | 2015-04-15 | Bristol-Myers Squibb Company | Macrocyclic factor viia inhibitors |
| JP6082462B2 (ja) * | 2012-08-03 | 2017-02-15 | ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ | 第ｘｉａ因子阻害剤としてのジヒドロピリドンｐ１ |
| HRP20170506T1 (hr) * | 2012-08-03 | 2017-06-02 | Bristol-Myers Squibb Company | Dihidropiridon p1 kao inhibitori xia faktora |
| TR201807316T4 (tr) | 2012-10-12 | 2018-06-21 | Bristol Myers Squibb Co | Bir faktör XIa inhibitörünün kristalli formları. |
| US9315519B2 (en) | 2012-10-12 | 2016-04-19 | Bristol-Myers Squibb Company | Guanidine substituted tetrahydroisoquinoline compounds as factor XIa inhibitors |
| WO2014059214A1 (en) | 2012-10-12 | 2014-04-17 | Bristol-Myers Squibb Company | Guanidine and amine substituted tetrahydroisoquinoline compounds as factor xia inhibitors |
| JP6479763B2 (ja) | 2013-03-25 | 2019-03-06 | ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ | 第ｘｉａ因子阻害剤としての置換アゾール含有のテトラヒドロイソキノリン |
| US9657006B2 (en) | 2013-06-13 | 2017-05-23 | Bristol-Myers Squibb Company | Macrocyclic factor VIIa inhibitors |
| NO2760821T3 (enExample) | 2014-01-31 | 2018-03-10 | ||
| PE20210470A1 (es) | 2014-01-31 | 2021-03-08 | Bristol Myers Squibb Co | Macrociclos con grupos p2' heterociclicos como inhibidores del factor xia |
| CN107074821B (zh) | 2014-09-04 | 2020-05-22 | 百时美施贵宝公司 | 为fxia抑制剂的二酰胺大环化合物 |
| US9453018B2 (en) | 2014-10-01 | 2016-09-27 | Bristol-Myers Squibb Company | Pyrimidinones as factor XIa inhibitors |
| EP3072943B1 (en) | 2015-03-26 | 2018-05-02 | Idemitsu Kosan Co., Ltd. | Dibenzofuran/carbazole-substituted benzonitriles |
| CN114805365B (zh) * | 2015-07-29 | 2024-07-23 | 百时美施贵宝公司 | 携带非芳族p2′基团的因子xia新大环 |
Family Cites Families (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0028489B1 (en) | 1979-11-05 | 1983-10-05 | Beecham Group Plc | Enzyme derivatives, and their preparation |
| US5023236A (en) | 1988-04-07 | 1991-06-11 | Corvas, Inc. | Factor VII/VIIA active site inhibitors |
| US5843442A (en) | 1990-10-22 | 1998-12-01 | Corvas International, Inc. | Blood coagulation protein antagonists and uses therefor |
| US5866542A (en) | 1994-10-18 | 1999-02-02 | Corvas International, Inc. | Nematode-extracted anticoagulant protein |
| PE121699A1 (es) | 1997-02-18 | 1999-12-08 | Boehringer Ingelheim Pharma | Heterociclos biciclicos disustituidos como inhibidores de la trombina |
| ZA985247B (en) | 1997-06-19 | 1999-12-17 | Du Pont Merck Pharma | Guanidine mimics as factor Xa inhibitors. |
| WO2000076970A2 (en) | 1999-06-14 | 2000-12-21 | Eli Lilly And Company | Serine protease inhibitors |
| DE19962924A1 (de) | 1999-12-24 | 2001-07-05 | Bayer Ag | Substituierte Oxazolidinone und ihre Verwendung |
| HUP0400651A2 (hu) | 2000-11-07 | 2004-06-28 | Bristol-Myers Squibb Company | Szerin proteáz inhibitorokként alkalmazható savszármazékok és ezeket tartalmazó gyógyszerkészítmények |
| AR035216A1 (es) | 2000-12-01 | 2004-05-05 | Astrazeneca Ab | Derivados de acido mandelico ,derivados farmaceuticamente aceptables, uso de estos derivados para la fabricacion de medicamentos, metodos de tratamiento ,procesos para la preparacion de estos derivados, y compuestos intermediarios |
| AU2002322802A1 (en) * | 2001-07-27 | 2003-02-17 | Merck And Co., Inc. | Thrombin inhibitors |
| KR100909141B1 (ko) | 2001-09-21 | 2009-07-23 | 브리스톨-마이어스스퀴브컴파니 | 인자 Ｘａ 억제제로서의 락탐-함유 화합물 및 그의 유도체 |
| EP1594845A4 (en) | 2003-02-11 | 2008-05-21 | Bristol Myers Squibb Co | BENZENE ACETAMIDE COMPOUNDS USEFUL AS SERINE PROTEASE INHIBITORS |
| US7122559B2 (en) | 2003-02-11 | 2006-10-17 | Bristol-Myers Squibb Company | Phenylglycine derivatives useful as serine protease inhibitors |
| WO2006076246A2 (en) | 2005-01-10 | 2006-07-20 | Bristol-Myers Squibb Company | Phenylglycinamide derivatives useful as anticoagulants |
| EP1866822A4 (en) * | 2005-03-03 | 2010-09-01 | Burnham Inst Medical Research | SCREENING PROCEDURE FOR PROTEIN KINASE B INHIBITORS USING VIRTUAL DOCKING APPARATUS AND COMPOSITIONS AND COMPOSITIONS DISCOVERED THEREFOR |
| EP1910298B1 (en) | 2005-06-24 | 2010-01-13 | Brystol-Myers Squibb Company | Phenylglycinamide and pyridylglycinamide derivatives useful as anticoagulants |
| PE20071132A1 (es) | 2005-12-23 | 2007-12-14 | Bristol Myers Squibb Co | Compuestos macrociclicos como inhibidores del factor viia |
| WO2007103996A1 (en) | 2006-03-09 | 2007-09-13 | Bristol-Myers Squibb Company | 2-(aryloxy)acetamide factor viia inhibitors useful as anticoagulants |
| EP2099783A1 (en) | 2006-12-20 | 2009-09-16 | Brystol-Myers Squibb Company | Bicyclic lactam factor viia inhibitors useful as anticoagulants |
-
2007
- 2007-12-14 PE PE2007001814A patent/PE20081775A1/es not_active Application Discontinuation
- 2007-12-19 MX MX2009006689A patent/MX2009006689A/es not_active Application Discontinuation
- 2007-12-19 AU AU2007337025A patent/AU2007337025A1/en not_active Abandoned
- 2007-12-19 CA CA002673598A patent/CA2673598A1/en not_active Abandoned
- 2007-12-19 CL CL200703718A patent/CL2007003718A1/es unknown
- 2007-12-19 EP EP07869479A patent/EP2102176A2/en not_active Withdrawn
- 2007-12-19 AR ARP070105750A patent/AR064471A1/es not_active Application Discontinuation
- 2007-12-19 WO PCT/US2007/088032 patent/WO2008079836A2/en not_active Ceased
- 2007-12-19 JP JP2009543158A patent/JP2010514681A/ja not_active Withdrawn
- 2007-12-19 US US12/519,376 patent/US8420830B2/en active Active
- 2007-12-19 TW TW096148731A patent/TW200836735A/zh unknown
-
2009
- 2009-06-12 NO NO20092279A patent/NO20092279L/no not_active Application Discontinuation
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2015506934A (ja) * | 2011-12-27 | 2015-03-05 | バイオ−ファーム ソリューションズ カンパニー リミテッド | フェニルアルキルカルバメート誘導体化合物およびこれを含む薬学組成物 |
Also Published As
| Publication number | Publication date |
|---|---|
| PE20081775A1 (es) | 2008-12-18 |
| NO20092279L (no) | 2009-08-31 |
| AR064471A1 (es) | 2009-04-01 |
| CA2673598A1 (en) | 2008-07-03 |
| WO2008079836A3 (en) | 2009-01-15 |
| TW200836735A (en) | 2008-09-16 |
| WO2008079836A2 (en) | 2008-07-03 |
| US20100113488A1 (en) | 2010-05-06 |
| WO2008079836A4 (en) | 2009-03-12 |
| AU2007337025A1 (en) | 2008-07-03 |
| US8420830B2 (en) | 2013-04-16 |
| CL2007003718A1 (es) | 2008-07-11 |
| MX2009006689A (es) | 2009-06-30 |
| EP2102176A2 (en) | 2009-09-23 |
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