AR061629A1 - Quinoxalinil macrociclicos inhibidores de serina proteasa del virus de la hepatitis c. proceso de obtencion y composiciones farmaceuticas - Google Patents
Quinoxalinil macrociclicos inhibidores de serina proteasa del virus de la hepatitis c. proceso de obtencion y composiciones farmaceuticasInfo
- Publication number
- AR061629A1 AR061629A1 ARP070102807A ARP070102807A AR061629A1 AR 061629 A1 AR061629 A1 AR 061629A1 AR P070102807 A ARP070102807 A AR P070102807A AR P070102807 A ARP070102807 A AR P070102807A AR 061629 A1 AR061629 A1 AR 061629A1
- Authority
- AR
- Argentina
- Prior art keywords
- substituted
- heteroaryl
- aryl
- cycloalkyl
- heterocycloalkyl
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D245/00—Heterocyclic compounds containing rings of more than seven members having two nitrogen atoms as the only ring hetero atoms
- C07D245/04—Heterocyclic compounds containing rings of more than seven members having two nitrogen atoms as the only ring hetero atoms condensed with carbocyclic rings or ring systems
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/4965—Non-condensed pyrazines
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- A61K38/19—Cytokines; Lymphokines; Interferons
- A61K38/21—Interferons [IFN]
- A61K38/212—IFN-alpha
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- A61K38/19—Cytokines; Lymphokines; Interferons
- A61K38/21—Interferons [IFN]
- A61K38/215—IFN-beta
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Gastroenterology & Hepatology (AREA)
- Epidemiology (AREA)
- Immunology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Zoology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Virology (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Molecular Biology (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Peptides Or Proteins (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
Composiciones farmacéuticas que comprenden los compuestos anteriormente mencionados para administrar a un sujeto que sufre de una infeccion por HCV, y métodos de tratar una infeccion por HCV en un sujeto administrando una composicion farmacéutica que comprende los compuestos de la presente. Reivindicacion 1: Un compuesto caracterizado porque responde a la formula 1; así como sus sales aceptables para uso farmacéutico, ésteres y prodrogas, en donde: A se selecciona entre H, -(C=O)-O-R1, - (C=O)-R2, -C(=O)-NH-R2, o - S(O)-R1, -S(O)2NHR2; cada R1se selecciona en forma independiente entre el grupo formado por: arilo; arilo sustituido; heteroarilo; heteroarilo sustituido; heterocicloalquilo o heterocicloalquilo sustituido; alquilo C1-8, alquenilo C2-8, o alquinilo C2-8 cada uno con 0, 1, 2, o 3 heteroátomos seleccionados entre O, S, o N; alquilo C1-8 sustituido, alquenilo C2-8 sustituido, o alquinilo C2-8 sustituido cada uno con 0, 1, 2, o 3 heteroátomos seleccionados entre O, S o N; cicloalquilo C3-12, o cicloalquilo C3-12 sustituido; cicloalquenilo C3-12, o cicloalquenilo C3-12 sustituido; cada R2 se selecciona en forma independiente entre el grupo formado por: hidrogeno; arilo; arilo sustituido; heteroarilo; heteroarilo sustituido; heterocicloalquilo o heterocicloalquilo sustituido; alquilo C1-8, alquenilo C2-8, o alquinilo C2-8 cada uno con 0, 1, 2, o 3 heteroátomos seleccionados entre O, S, o N; alquilo C1-8 sustituido, alquenilo C2-8 sustituido, o alquinilo C2-8 sustituido cada uno con 0, 1, 2, o 3 heteroátomos seleccionados entre O, S o N; cicloalquilo C3-12, o cicloalquilo C3-12 sustituido; cicloalquenilo C3-12, o cicloalquenilo C3-12 sustituido; G se selecciona entre -NHS(O)2-R3 o -NH(SO2)NR4R5; donde cada R3 se selecciona en forma independiente entre: arilo; arilo sustituido; heteroarilo; heteroarilo sustituido, heterocicloalquilo o heterocicloalquilo sustituido; y alquilo C1-8, alquenilo C2-8, o alquinilo C2-8 cada uno con 0, 1, 2, o 3 heteroátomos seleccionados entre O, S, o N; alquilo C1-8 sustituido, alquenilo C2-8 sustituido, o alquinilo C2-8 sustituido cada uno con 0, 1, 2, o 3 heteroátomos seleccionados entre O, S o N; cicloalquilo C3-12, o cicloalquilo C3-12 sustituido; cicloalquenilo C3-12, o cicloalquenilo C3-12 sustituido; con la salvedad de que R3 no sea -CH2Ph ni -CH2CH2Ph; cada R4 y R5 se seleccionan en forma independiente entre: hidrogeno; arilo; arilo sustituido; heteroarilo; heteroarilo sustituido, heterocicloalquilo o heterocicloalquilo sustituido; y alquilo C1-8, alquenilo C2-8, o alquinilo C2-8 cada uno con 0, 1, 2, o 3 heteroátomos seleccionados entre O, S, o N; alquilo C1-8 sustituido, alquenilo C2-8 sustituido, o alquinilo C2-8 sustituido cada uno con 0, 1, 2, o 3 heteroátomos seleccionados entre O, S o N; cicloalquilo C3-12, o cicloalquilo C3-12 sustituido; cicloalquenilo C3-12, o cicloalquenilo C3-12 sustituido; L se selecciona entre -CH2-, -O-, -S-, o -S(O)2-; X y Y tomados junto con los átomos de carbono a los cuales están unidos forman una porcion cíclica seleccionada entre arilo, arilo sustituido, heteroarilo, o heteroarilo sustituido: W está ausente o se selecciona entre -O-, -S-, -NH-, -N(Me)-, -C(O)NH-, o -C(O)N(Me)-; como alternativa, W puede ser alquileno C2-4, alquileno C2-4 sustituido; Z se selecciona entre los grupos formados por: hidrogeno; -CN; N3, halogeno; -NH-N=CH(R2), donde R2 tiene los valores que se han definido; arilo, arilo sustituido; heteroarilo, heteroarilo sustituido; cicloalquilo C3-12, cicloalquilo C3-12 sustituido, heterocicloalquilo, heterocicloalquilo sustituido; alquilo C1-6 con 0, 1, 2, o 3 heteroátomos seleccionados entre O, S, o N, opcionalmente sustituido con uno o más sustituyentes seleccionados entre halogeno, arilo, arilo sustituido, heteroarilo, o heteroarilo sustituido; alquenilo C2-6 con 0, 1, 2, o 3 heteroátomos seleccionados entre O, S, o N, opcionalmente sustituido con uno o más sustituyentes seleccionados entre halogeno, arilo, arilo sustituido, heteroarilo, o heteroarilo sustituido; alquinilo C2-6 con 0, 1, 2, o 3 heteroátomos seleccionados entre O, S, o N, opcionalmente sustituido con uno o más sustituyentes seleccionados entre halogeno, arilo, arilo sustituido, heteroarilo, o heteroarilo sustituido; j = 0, 1, 2, 3, o 4; k =1, 2, o 3; m = 0, 1, o 2; y ----- denota un enlace simple o doble carbono-carbono.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US87244206P | 2006-06-26 | 2006-06-26 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR061629A1 true AR061629A1 (es) | 2008-09-10 |
Family
ID=38846474
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP070102807A AR061629A1 (es) | 2006-06-26 | 2007-06-25 | Quinoxalinil macrociclicos inhibidores de serina proteasa del virus de la hepatitis c. proceso de obtencion y composiciones farmaceuticas |
Country Status (18)
Country | Link |
---|---|
US (2) | US8809264B2 (es) |
EP (1) | EP2066326A4 (es) |
JP (1) | JP5520046B2 (es) |
KR (1) | KR101505056B1 (es) |
CN (1) | CN101478970B (es) |
AR (1) | AR061629A1 (es) |
AU (1) | AU2007265157B2 (es) |
BR (1) | BRPI0714074A2 (es) |
CA (1) | CA2654945C (es) |
IL (1) | IL195512A (es) |
MX (1) | MX2008016528A (es) |
NZ (1) | NZ573275A (es) |
PE (1) | PE20080992A1 (es) |
RU (1) | RU2475494C2 (es) |
TW (1) | TWI454264B (es) |
UY (1) | UY30437A1 (es) |
WO (1) | WO2008002924A2 (es) |
ZA (1) | ZA200810519B (es) |
Families Citing this family (51)
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JP2003007697A (ja) * | 2001-06-21 | 2003-01-10 | Hitachi Kokusai Electric Inc | 半導体装置の製造方法、基板処理方法および基板処理装置 |
MY140680A (en) | 2002-05-20 | 2010-01-15 | Bristol Myers Squibb Co | Hepatitis c virus inhibitors |
US20090148407A1 (en) | 2005-07-25 | 2009-06-11 | Intermune, Inc. | Novel Macrocyclic Inhibitors of Hepatitis C Virus Replication |
ATE493409T1 (de) | 2005-10-11 | 2011-01-15 | Intermune Inc | Verbindungen und verfahren zur inhibierung der replikation des hepatitis-c-virus |
RU2008152171A (ru) | 2006-07-05 | 2010-08-10 | Интермьюн, Инк. (Us) | Новые ингибиторы вирусной репликации гепатита с |
KR101615500B1 (ko) | 2006-10-27 | 2016-04-27 | 머크 샤프 앤드 돔 코포레이션 | Hcv ns3 프로테아제 억제제 |
EP2185524A1 (en) | 2007-05-10 | 2010-05-19 | Intermune, Inc. | Novel peptide inhibitors of hepatitis c virus replication |
US20090005387A1 (en) * | 2007-06-26 | 2009-01-01 | Deqiang Niu | Quinoxalinyl macrocyclic hepatitis c virus serine protease inhibitors |
AR067180A1 (es) * | 2007-06-29 | 2009-09-30 | Gilead Sciences Inc | Compuestos antivirales |
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US8372802B2 (en) * | 2008-03-20 | 2013-02-12 | Enanta Pharmaceuticals, Inc. | Fluorinated macrocyclic compounds as hepatitis C virus inhibitors |
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US8207341B2 (en) | 2008-09-04 | 2012-06-26 | Bristol-Myers Squibb Company | Process or synthesizing substituted isoquinolines |
UY32099A (es) * | 2008-09-11 | 2010-04-30 | Enanta Pharm Inc | Inhibidores macrocíclicos de serina proteasas de hepatitis c |
AR075584A1 (es) | 2009-02-27 | 2011-04-20 | Intermune Inc | COMPOSICIONES TERAPEUTICAS QUE COMPRENDEN beta-D-2'-DESOXI-2'-FLUORO-2'-C-METILCITIDINA Y UN DERIVADO DE ACIDO ISOINDOL CARBOXILICO Y SUS USOS. COMPUESTO. |
TW201040181A (en) | 2009-04-08 | 2010-11-16 | Idenix Pharmaceuticals Inc | Macrocyclic serine protease inhibitors |
US8936781B2 (en) | 2009-05-13 | 2015-01-20 | Enanta Pharmaceuticals, Inc. | Macrocyclic compounds as hepatitis C virus inhibitors |
US8232246B2 (en) | 2009-06-30 | 2012-07-31 | Abbott Laboratories | Anti-viral compounds |
TW201117812A (en) | 2009-08-05 | 2011-06-01 | Idenix Pharmaceuticals Inc | Macrocyclic serine protease inhibitors |
SI2477980T1 (sl) | 2009-09-15 | 2017-01-31 | Taigen Biotechnology Co., Ltd. | Inhibitorji HCV proteaze |
WO2011049908A2 (en) * | 2009-10-19 | 2011-04-28 | Enanta Pharmaceuticals, Inc. | Bismacrokyclic compounds as hepatitis c virus inhibitors |
JP2013511562A (ja) * | 2009-11-24 | 2013-04-04 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | C型肝炎阻害化合物 |
JP5717768B2 (ja) * | 2010-03-10 | 2015-05-13 | アッヴィ・バハマズ・リミテッド | 固体組成物 |
JP5911476B2 (ja) | 2010-05-26 | 2016-04-27 | スノビオン プハルマセウトイカルス インコーポレイテッド | ヘテロアリール化合物及びその使用方法 |
MX2012014301A (es) * | 2010-06-07 | 2013-04-29 | Enanta Pharm Inc | Inhibidores macrociclicos de serina proteasa de hepatitis c. |
NZ608720A (en) | 2010-09-21 | 2015-03-27 | Enanta Pharm Inc | Macrocyclic proline derived hcv serine protease inhibitors |
US20120101032A1 (en) * | 2010-10-22 | 2012-04-26 | Intermune, Inc. | Novel macrocyclic inhibitors of hepatitis c virus replication |
CN103380132B (zh) * | 2010-12-30 | 2016-08-31 | 益安药业 | 菲啶大环丙型肝炎丝氨酸蛋白酶抑制剂 |
CA2822556A1 (en) * | 2010-12-30 | 2012-07-05 | Enanta Pharmaceuticals, Inc | Macrocyclic hepatitis c serine protease inhibitors |
WO2012109398A1 (en) | 2011-02-10 | 2012-08-16 | Idenix Pharmaceuticals, Inc. | Macrocyclic serine protease inhibitors, pharmaceutical compositions thereof, and their use for treating hcv infections |
US8957203B2 (en) | 2011-05-05 | 2015-02-17 | Bristol-Myers Squibb Company | Hepatitis C virus inhibitors |
US10201584B1 (en) | 2011-05-17 | 2019-02-12 | Abbvie Inc. | Compositions and methods for treating HCV |
US8691757B2 (en) | 2011-06-15 | 2014-04-08 | Bristol-Myers Squibb Company | Hepatitis C virus inhibitors |
EP2802595B1 (en) | 2012-01-11 | 2016-01-06 | AbbVie Inc. | Processes for making hcv protease inhibitors |
JP2015533124A (ja) | 2012-10-08 | 2015-11-19 | アッヴィ・インコーポレイテッド | Hcvプロテアーゼ阻害剤を作製するのに有用な化合物 |
EA025560B1 (ru) | 2012-10-19 | 2017-01-30 | Бристол-Майерс Сквибб Компани | Ингибиторы вируса гепатита с |
US9643999B2 (en) * | 2012-11-02 | 2017-05-09 | Bristol-Myers Squibb Company | Hepatitis C virus inhibitors |
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CN111689951A (zh) * | 2020-06-11 | 2020-09-22 | 西北师范大学 | 一种1-苄基-3-烷基喹喔啉-2(1h)-酮的合成方法 |
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2007
- 2007-06-25 UY UY30437A patent/UY30437A1/es not_active Application Discontinuation
- 2007-06-25 TW TW096122888A patent/TWI454264B/zh not_active IP Right Cessation
- 2007-06-25 AR ARP070102807A patent/AR061629A1/es unknown
- 2007-06-25 PE PE2007000815A patent/PE20080992A1/es active IP Right Grant
- 2007-06-26 NZ NZ573275A patent/NZ573275A/en unknown
- 2007-06-26 CN CN200780024107.8A patent/CN101478970B/zh active Active
- 2007-06-26 CA CA2654945A patent/CA2654945C/en not_active Expired - Fee Related
- 2007-06-26 JP JP2009518517A patent/JP5520046B2/ja active Active
- 2007-06-26 KR KR1020097001503A patent/KR101505056B1/ko not_active IP Right Cessation
- 2007-06-26 US US11/768,723 patent/US8809264B2/en not_active Expired - Fee Related
- 2007-06-26 MX MX2008016528A patent/MX2008016528A/es active IP Right Grant
- 2007-06-26 US US11/768,712 patent/US8501681B2/en not_active Expired - Fee Related
- 2007-06-26 WO PCT/US2007/072140 patent/WO2008002924A2/en active Application Filing
- 2007-06-26 EP EP07784548A patent/EP2066326A4/en not_active Withdrawn
- 2007-06-26 BR BRPI0714074-6A patent/BRPI0714074A2/pt not_active Application Discontinuation
- 2007-06-26 AU AU2007265157A patent/AU2007265157B2/en active Active
- 2007-06-26 RU RU2009102252/04A patent/RU2475494C2/ru active
-
2008
- 2008-11-25 IL IL195512A patent/IL195512A/en active IP Right Grant
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Also Published As
Publication number | Publication date |
---|---|
JP2009541491A (ja) | 2009-11-26 |
US20070299078A1 (en) | 2007-12-27 |
US8809264B2 (en) | 2014-08-19 |
WO2008002924A2 (en) | 2008-01-03 |
KR101505056B1 (ko) | 2015-03-23 |
TWI454264B (zh) | 2014-10-01 |
KR20090023732A (ko) | 2009-03-05 |
IL195512A (en) | 2014-05-28 |
PE20080992A1 (es) | 2008-08-06 |
IL195512A0 (en) | 2009-09-01 |
TW200810777A (en) | 2008-03-01 |
JP5520046B2 (ja) | 2014-06-11 |
CN101478970A (zh) | 2009-07-08 |
BRPI0714074A2 (pt) | 2012-12-18 |
AU2007265157A1 (en) | 2008-01-03 |
CA2654945C (en) | 2013-08-06 |
RU2475494C2 (ru) | 2013-02-20 |
CA2654945A1 (en) | 2008-01-03 |
ZA200810519B (en) | 2009-08-26 |
UY30437A1 (es) | 2008-01-31 |
RU2009102252A (ru) | 2010-08-10 |
CN101478970B (zh) | 2014-07-02 |
WO2008002924A3 (en) | 2008-04-03 |
US8501681B2 (en) | 2013-08-06 |
EP2066326A2 (en) | 2009-06-10 |
AU2007265157B2 (en) | 2013-06-27 |
EP2066326A4 (en) | 2010-09-29 |
US20080008681A1 (en) | 2008-01-10 |
NZ573275A (en) | 2011-12-22 |
MX2008016528A (es) | 2009-03-31 |
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