AR063872A1 - Derivados de acetileno como inhibidores de estearoil coa desaturasa - Google Patents
Derivados de acetileno como inhibidores de estearoil coa desaturasaInfo
- Publication number
- AR063872A1 AR063872A1 ARP070105150A ARP070105150A AR063872A1 AR 063872 A1 AR063872 A1 AR 063872A1 AR P070105150 A ARP070105150 A AR P070105150A AR P070105150 A ARP070105150 A AR P070105150A AR 063872 A1 AR063872 A1 AR 063872A1
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- substituted
- unsubstituted
- alkyl
- case
- cycloalkenyl
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D213/72—Nitrogen atoms
- C07D213/74—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
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- 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
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- 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
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- 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
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- 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
- A61P3/04—Anorexiants; Antiobesity agents
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- 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
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- 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
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
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- 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
- A61P3/08—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
- 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
- C07D237/02—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings
- C07D237/06—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
- C07D237/10—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D237/20—Nitrogen atoms
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/32—One oxygen, sulfur or nitrogen atom
- C07D239/42—One nitrogen atom
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
- C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
- C07D277/08—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
- C07D277/12—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D277/18—Nitrogen atoms
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- 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
- C07D401/10—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 aromatic rings
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- 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
- C07D401/12—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 chain containing hetero atoms as chain links
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic 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
- C07D405/02—Heterocyclic 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
- C07D405/06—Heterocyclic 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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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic 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
- C07D405/02—Heterocyclic 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
- C07D405/10—Heterocyclic 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 aromatic rings
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Veterinary Medicine (AREA)
- Diabetes (AREA)
- General Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Animal Behavior & Ethology (AREA)
- Engineering & Computer Science (AREA)
- Life Sciences & Earth Sciences (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Child & Adolescent Psychology (AREA)
- Gastroenterology & Hepatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Thiazole And Isothizaole Compounds (AREA)
- Pyridine Compounds (AREA)
Abstract
La presente proporciona inhibidores de estearoil CoA desaturasa (SCD). En particular, los compuestos descriptos en la presente son útiles en el tratamiento o la prevención de enfermedades, condiciones y/o trastornos modulados por inhibidores de estearoil CoA desaturasa 1 (SCD1). También se proporcionan en la presente, procesos para preparar los compuestos descriptos en ella, los compuestos intermedios y su síntesis, composiciones farmacéuticas de éstas, y métodos para el tratamiento o prevención de enfermedades, condiciones y/o trastornos modulados por inhibidores de estearoil CoA desaturasa, como obesidad, trastorno del apetito, glucosa, insulina, lípidos, síndrome metabólico, enfermedad hígado adiposo. Reivindicación 1: Un compuesto de fórmula (1) A-U-B'-s-Q o una sal de ésta, un solvato de ésta, un profármaco de ésta, un estereoisómero de ésta o un N-óxido de ésta farmacéuticamente aceptables; donde: A es R'W-; R' se selecciona de alquilo sustituido o no sustituido, alquenilo sustituido o no sustituido, alquinilo sustituido o no sustituido, cicloalquilo sustituido o no sustituido, cicloalquilalquilo sustituido o no sustituido, cicloalquenilo sustituido o no sustituido, cicloalquenilalquilo sustituido o no sustituido, arilo sustituido o no sustituido, arilalquilo sustituido o no sustituido, heteroarilo sustituido o no sustituido, heteroarilalquilo sustituido o no sustituido, heterocíclico sustituido o no sustituido y heterociclilalquilo sustituido o no sustituido; W se selecciona de (CR1R2)p, C(=Y) , C(=Y)O, OC(=Y), O, CONR1, S(O)r, S(O)rNR1, NR1(CH2)nO, NR1 o NR1C(=Y)NR2; Q se selecciona de hidrógeno, hidroxilo, alquilo sustituido o no sustituido, alquenilo sustituido o no sustituido, alquinilo sustituido o no sustituido, cicloalquilo sustituido o no sustituido, cicloalquilalquilo sustituido o no sustituido, cicloalquenilo sustituido o no sustituido, cicloalquenilalquilo sustituido o no sustituido, arilo sustituido o no sustituido, arilalquilo sustituido o no sustituido, heteroarilo sustituido o no sustituido, heteroarilalquilo sustituido o no sustituido, heterocíclico sustituido o no sustituido y heterociclilalquilo sustituido o no sustituido; (CR1R2)nOR5, COR1, COOR1, CONR1R2, S(O)rNR1R2, NR1R2, (CH2)nNR1R2, (CH2)nCHR1R2, (CR1R2)NR5R6, (CR1R2)NR5CONR6R7, (CH)nNHCOR1 y (CH2)nNHSO2R1; U se selecciona de un enlace y el grupo de fórmula (2), donde V es CR y N y B es CR o N, o B junto con un átomo de carbono con anillo adyacente y A forman un anillo seleccionado de fórmulas (3), B' se selecciona de fórmulas (4); U y V son independientemente CR o N; en cada caso, R se selecciona independientemente de hidrógeno, hidroxilo, alquilo sustituido o no sustituido, alquenilo sustituido o no sustituido, alquinilo sustituido o no sustituido, cicloalquilo sustituido o no sustituido, cicloalquilalquilo sustituido o no sustituido, cicloalquenilo sustituido o no sustituido, cicloalquenilalquilo sustituido o no sustituido, arilo sustituido o no sustituido, arilalquilo sustituido o no sustituido, heteroarilo sustituido o no sustituido, heterociclilo sustituido o no sustituido, heterociclialquilo sustituido o no sustituido, heteroarilalquilo sustituido o no sustituido; en cada caso, m es independientemente un entero 0-4; en cada caso, n, n' y r son independientemente 0, 1 o 2; p es 0, 1, 2, 3, o 4; en cada caso, R1, R2, R5, R6 y R7 pueden ser idénticos o diferentes y se seleccionan independientemente de hidrógeno, halógeno, alquilo sustituido o no sustituido, alquenilo sustituido o no sustituido, alquinilo sustituido o no sustituido, cicloalquilo sustituido o no sustituido, cicloalquilalquilo sustituido o no sustituido, cicloalquenilo sustituido o no sustituido, cicloalquenilalquilo sustituido o no sustituido, arilo sustituido o no sustituido, arilalquilo sustituido o no sustituido, heteroarilo sustituido o no sustituido, heterocíclico sustituido o no sustituido, heterociclialquilo sustituido o no sustituido, heteroarilalquilo sustituido o no sustituido; o, cuando R1 y R2 están unidos a un átomo común, forman con el átomo común un heterociclilo de 3-7 miembros; en cada caso X1 a X4 son independientemente N o CR; en cada caso, X y X5 a X7 son independientemente CHR4, CO, CS, O, S(O)r, N, o NR4; en cada caso, R4 se selecciona independientemente de hidrógeno, hidroxilo, alquilo sustituido o no sustituido, cicloalquilo sustituido o no sustituido, arilo sustituido o no sustituido, heteroarilo sustituido o no sustituido, y heterociclilo sustituido o no sustituido; en cada caso, R3 se selecciona de hidrógeno, nitro, ciano, halógeno, COR1, alquilo sustituido o no sustituido, arilo sustituido o no sustituido, heteroarilo sustituido o no sustituido, alcoxi sustituido o no sustituido, COOR1, CONR1R2, S(O)rR1, S(O)rNR1R2 y NR1R2, y en cada caso, Y es O o S.
Applications Claiming Priority (4)
Application Number | Priority Date | Filing Date | Title |
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IN1917MU2006 | 2006-11-20 | ||
IN2175MU2006 | 2006-12-29 | ||
IN1375MU2007 | 2007-07-17 | ||
US95410807P | 2007-08-06 | 2007-08-06 |
Publications (1)
Publication Number | Publication Date |
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AR063872A1 true AR063872A1 (es) | 2009-02-25 |
Family
ID=39322723
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP070105150A AR063872A1 (es) | 2006-11-20 | 2007-11-20 | Derivados de acetileno como inhibidores de estearoil coa desaturasa |
Country Status (8)
Country | Link |
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US (1) | US20080182851A1 (es) |
EP (1) | EP2099755A2 (es) |
JP (1) | JP2010510201A (es) |
KR (1) | KR20090083477A (es) |
AR (1) | AR063872A1 (es) |
AU (1) | AU2007323193A1 (es) |
TW (1) | TW200831482A (es) |
WO (1) | WO2008062276A2 (es) |
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US20110093574A1 (en) * | 2008-06-19 | 2011-04-21 | Koehler Loren M | Multi-blade interconnector |
US20110184027A1 (en) * | 2008-09-25 | 2011-07-28 | Glenmark Pharmaceuticals S.A. | Tissue selective stearoyl-coa desaturase 1 inhibitors and cell based screening assay for their identification |
WO2010073011A2 (en) | 2008-12-23 | 2010-07-01 | Betagenon Ab | Compounds useful as medicaments |
WO2010075356A1 (en) * | 2008-12-23 | 2010-07-01 | Forest Laboratories Holdings Limited | Novel piperazine derivatives as inhibitors of stearoyl-coa desaturase |
EP2398809B1 (en) | 2009-02-17 | 2015-07-08 | Merck Canada Inc. | Novel spiro compounds useful as inhibitors of stearoyl-coenzyme a delta-9 desaturase |
WO2011011872A1 (en) | 2009-07-28 | 2011-02-03 | Merck Frosst Canada Ltd. | Novel spiro compounds useful as inhibitors of stearoyl-coenzyme a delta-9 desaturase |
AU2010311321B2 (en) | 2009-10-30 | 2014-11-27 | Prexton Therapeutics S.A. | Novel oxime derivatives and their use as allosteric modulators of metabotropic glutamate receptors |
US20120122928A1 (en) | 2010-08-11 | 2012-05-17 | Bayer Cropscience Ag | Heteroarylpiperidine and -Piperazine Derivatives as Fungicides |
US8759527B2 (en) | 2010-08-25 | 2014-06-24 | Bayer Cropscience Ag | Heteroarylpiperidine and -piperazine derivatives as fungicides |
EP2423210A1 (de) | 2010-08-25 | 2012-02-29 | Bayer CropScience AG | Heteroarylpiperidin- und -piperazinderivate als Fungizide |
CN107033139B (zh) | 2010-10-27 | 2019-11-19 | 拜耳知识产权有限责任公司 | 作为杀真菌剂的杂芳基哌啶和杂芳基哌嗪衍生物 |
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KR102015968B1 (ko) | 2011-12-27 | 2019-08-29 | 바이엘 인텔렉쳐 프로퍼티 게엠베하 | 살진균제로서의 헤테로아릴피페리딘 및 피페라진 유도체 |
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PT1942106E (pt) * | 2003-08-01 | 2011-12-22 | Euro Celtique Sa | Agentes terapêuticos úteis para o tratamento da dor |
WO2009048101A1 (ja) * | 2007-10-10 | 2009-04-16 | Takeda Pharmaceutical Company Limited | アミド化合物 |
US20100234383A1 (en) * | 2009-03-13 | 2010-09-16 | Gilles Klopman | Treating, preventing or ameliorating a hyperproliferative disease/disorder |
-
2007
- 2007-11-19 JP JP2009536816A patent/JP2010510201A/ja active Pending
- 2007-11-19 EP EP07858887A patent/EP2099755A2/en not_active Withdrawn
- 2007-11-19 US US11/942,522 patent/US20080182851A1/en not_active Abandoned
- 2007-11-19 AU AU2007323193A patent/AU2007323193A1/en not_active Abandoned
- 2007-11-19 KR KR1020097013023A patent/KR20090083477A/ko not_active Application Discontinuation
- 2007-11-19 WO PCT/IB2007/003551 patent/WO2008062276A2/en active Application Filing
- 2007-11-20 AR ARP070105150A patent/AR063872A1/es unknown
- 2007-11-20 TW TW096143898A patent/TW200831482A/zh unknown
Also Published As
Publication number | Publication date |
---|---|
WO2008062276A2 (en) | 2008-05-29 |
WO2008062276A8 (en) | 2008-10-09 |
US20080182851A1 (en) | 2008-07-31 |
JP2010510201A (ja) | 2010-04-02 |
AU2007323193A1 (en) | 2008-05-29 |
WO2008062276A3 (en) | 2009-03-05 |
KR20090083477A (ko) | 2009-08-03 |
TW200831482A (en) | 2008-08-01 |
EP2099755A2 (en) | 2009-09-16 |
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