ECSP077183A - Derivados de la n-(1-bencil-4-fenil-1h-imidazol-2-il)-2,2-dimetilpropil)benzamida y los compuestos relacionados como inhibidores de la proteína de quiinesina del huso (ksp) para el tratamiento del cáncer - Google Patents
Derivados de la n-(1-bencil-4-fenil-1h-imidazol-2-il)-2,2-dimetilpropil)benzamida y los compuestos relacionados como inhibidores de la proteína de quiinesina del huso (ksp) para el tratamiento del cáncerInfo
- Publication number
- ECSP077183A ECSP077183A EC2007007183A ECSP077183A ECSP077183A EC SP077183 A ECSP077183 A EC SP077183A EC 2007007183 A EC2007007183 A EC 2007007183A EC SP077183 A ECSP077183 A EC SP077183A EC SP077183 A ECSP077183 A EC SP077183A
- Authority
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- Prior art keywords
- group
- substituted
- optionally substituted
- hydrogen
- aryl
- Prior art date
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
- C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- 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
- 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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- C07D—HETEROCYCLIC COMPOUNDS
- C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
- C07D233/04—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
- C07D233/20—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with substituted hydrocarbon radicals, directly attached to ring carbon atoms
- C07D233/24—Radicals substituted by nitrogen atoms not forming part of a nitro radical
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- C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
- C07D233/64—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
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- 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
- C07D401/04—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 directly linked by a ring-member-to-ring-member bond
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- 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
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- 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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- 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
- C07D403/04—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 directly linked by a ring-member-to-ring-member bond
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- 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
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- 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
- C07D403/14—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 three or more hetero rings
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- 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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- 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
- C07D405/12—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 chain containing hetero atoms as chain links
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- C07D413/02—Heterocyclic 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
- C07D413/06—Heterocyclic 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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- C07D413/02—Heterocyclic 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
- C07D413/12—Heterocyclic 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 chain containing hetero atoms as chain links
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- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
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- C07D417/00—Heterocyclic 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
- C07D417/02—Heterocyclic 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
- C07D417/04—Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
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- C07—ORGANIC CHEMISTRY
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- C07D417/00—Heterocyclic 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
- C07D417/02—Heterocyclic 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
- C07D417/06—Heterocyclic 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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- C07D417/02—Heterocyclic 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
- C07D417/12—Heterocyclic 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 chain containing hetero atoms as chain links
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic 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
- C07D417/14—Heterocyclic 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 three or more hetero rings
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- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/10—Spiro-condensed systems
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- Organic Chemistry (AREA)
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- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
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- Hematology (AREA)
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- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
Esta invención se dirige a los compuestos substituidos del imidazol, los cuales, modulan la actividad de la KSP representado por la fórmula I: en donde: R1 se selecciona del grupo que consiste de acilamino, carboxilo, éster de carboxilo, arilo, y alquilo opcionalmente sustituido con hidroxi o halo; R2 se seleccionan del grupo que consiste de hidrógeno, alquilo, y arilo; R3 se seleccionan del grupo que consiste del hidrógeno y - X-A, en donde X se selecciona del grupo que consiste de -C(O) -, - C(S) -, - S(O) -, - S(O)2, y - S(O)2-N(R)-, donde R es hidrógeno o alquilo y A se selecciona del grupo que consiste de hidrógeno, alquilo opcionalmente substituido, del arilo alkoxy, opcionalmente substituido opcionalmente substituido, del éster carboxilo, carboxilo, del aminoacilo, del heteroarilo opcionalmente substituido, del cycloalquilo heterocíclico, y opcionalmente substituido opcionalmente substituido, en donde substituyen a los grupos opcionalmente substituidos con 1 a 4 sustitutos; R5 es seleccionado del grupo que consiste de L-A1, en donde L es seleccionado del grupo que consiste de -S(O)q- donde q es uno ó dos, y el alquenilo de C1 a C5 opcionalmente sustituido con hidroxi, halo, o acilamino; y A1 es seleccionado del grupo que consiste de arilo, arilo sustituido, heteroarilo, heteroarilo sustituido, heterocíclico, heterocíclico sustituido, cicloalquilo, y cicloalquilo sustituido; y uno de tanto R6 ó R7 es seleccionado del grupo que consiste de heterocíclico, arilo y heteroarilo, todos de los cuales pueden estar opcionalmente sustituidos con-(R8)m donde R8 es como se define aquí y m es un número entero de 1 a 3, y los otros de R6 ó R7 es seleccionado del grupo que consiste de hidrógeno, halo, y alquilo; ó R6 y R7 son ambos hidrógeno;
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
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US58092704P | 2004-06-18 | 2004-06-18 |
Publications (1)
Publication Number | Publication Date |
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ECSP077183A true ECSP077183A (es) | 2007-02-28 |
Family
ID=34980173
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
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EC2007007183A ECSP077183A (es) | 2004-06-18 | 2007-01-18 | Derivados de la n-(1-bencil-4-fenil-1h-imidazol-2-il)-2,2-dimetilpropil)benzamida y los compuestos relacionados como inhibidores de la proteína de quiinesina del huso (ksp) para el tratamiento del cáncer |
Country Status (21)
Country | Link |
---|---|
US (3) | US7576221B2 (es) |
EP (1) | EP1765789B1 (es) |
JP (2) | JP4836280B2 (es) |
KR (1) | KR101170925B1 (es) |
CN (1) | CN1993331A (es) |
AU (1) | AU2005258135B2 (es) |
BR (1) | BRPI0510929A (es) |
CA (1) | CA2571002A1 (es) |
EC (1) | ECSP077183A (es) |
ES (1) | ES2409345T3 (es) |
IL (1) | IL180147A0 (es) |
MA (1) | MA28739B1 (es) |
MX (1) | MXPA06014909A (es) |
NO (1) | NO20070343L (es) |
NZ (1) | NZ552510A (es) |
RU (1) | RU2427572C2 (es) |
SG (1) | SG153851A1 (es) |
TN (1) | TNSN06419A1 (es) |
TW (1) | TW200612958A (es) |
WO (1) | WO2006002236A1 (es) |
ZA (1) | ZA200700481B (es) |
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JP4836280B2 (ja) * | 2004-06-18 | 2011-12-14 | ノバルティス バクシンズ アンド ダイアグノスティックス,インコーポレーテッド | 癌を治療するためのキネシンスピンドルタンパク質(ksp)阻害剤としてのn−(1−(1−ベンジル−4−フェニル−1h−イミダゾール−2−イル)−2,2−ジメチルプロピル)ベンズアミド誘導体および関連化合物 |
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WO2007011647A2 (en) * | 2005-07-15 | 2007-01-25 | Kalypsys, Inc. | Inhibitors of mitotic kinesin ksp |
TW200800951A (en) * | 2005-08-09 | 2008-01-01 | Novartis Ag | Substituted imidazole compounds as KSP inhibitors |
US8119655B2 (en) | 2005-10-07 | 2012-02-21 | Takeda Pharmaceutical Company Limited | Kinase inhibitors |
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US8273738B2 (en) | 2006-09-05 | 2012-09-25 | Kyowa Hakko Kirin Co., Ltd. | Imidazole derivatives |
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KR20090081020A (ko) * | 2006-11-13 | 2009-07-27 | 노파르티스 아게 | Ksp 억제제로서의 치환된 피라졸 및 트리아졸 화합물 |
CA2674318A1 (en) | 2007-01-05 | 2008-07-17 | Novartis Ag | Cyclized derivatives as eg-5 inhibitors |
US8252832B2 (en) * | 2007-12-14 | 2012-08-28 | Novartis Ag | Kinesin inhibitors as cancer therapeutics |
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JP2013525290A (ja) * | 2010-04-15 | 2013-06-20 | ノバルティス アーゲー | Ksp阻害剤としてのオキサゾールおよびチアゾール化合物 |
CA2794406A1 (en) * | 2010-04-15 | 2011-10-20 | Novartis Ag | Triazole compounds as ksp inhibitors |
DE102010025663A1 (de) | 2010-06-30 | 2012-01-05 | Karl-Heinz Glüsenkamp | Neue beta-Aminoaldehyd-Derivate, Verfahren zu ihrer Herstellung und ihre chemische Verwendung als reaktive Intermediate |
US8809372B2 (en) | 2011-09-30 | 2014-08-19 | Asana Biosciences, Llc | Pyridine derivatives |
US9498540B2 (en) | 2013-03-15 | 2016-11-22 | Novartis Ag | Cell proliferation inhibitors and conjugates thereof |
JP2016516035A (ja) * | 2013-03-15 | 2016-06-02 | ノバルティス アーゲー | 細胞増殖阻害剤およびそれらのコンジュゲート |
PT3086814T (pt) * | 2013-12-23 | 2020-09-04 | Bayer Pharma AG | Conjugados de fármaco de anticorpo (adcs) com inibidores de ksp |
US10786578B2 (en) | 2014-08-05 | 2020-09-29 | Novartis Ag | CKIT antibody drug conjugates |
JP6743015B2 (ja) * | 2014-12-15 | 2020-08-19 | バイエル ファーマ アクチエンゲゼルシャフト | Ksp阻害剤の脱グリコシル化抗tweakr抗体との抗体薬物複合体(adc類) |
IS2977B (is) | 2015-02-23 | 2017-07-15 | Actavis Group Ptc Ehf. | Aðferð til framleiðslu á milliefnum sem eru nytsamleg við nýsmíði á elúxadólíni |
SG10201908685QA (en) | 2015-06-22 | 2019-10-30 | Bayer Pharma AG | Antibody drug conjugates (adcs) and antibody prodrug conjugates (apdcs) with enzymatically cleavable groups |
CN108025086A (zh) | 2015-06-23 | 2018-05-11 | 拜耳制药股份公司 | Ksp抑制剂与抗b7h3抗体的抗体-活性物质缀合物(adc) |
CN107921145A (zh) | 2015-06-23 | 2018-04-17 | 拜耳医药股份有限公司 | Ksp抑制剂与抗‑tweakr抗体的抗体药物缀合物(adc) |
EP3313523A2 (en) | 2015-06-23 | 2018-05-02 | Bayer Pharma Aktiengesellschaft | Targeted conjugates of ksp inhibitors |
EP3919518A1 (en) | 2016-06-15 | 2021-12-08 | Bayer Pharma Aktiengesellschaft | Specific antibody-drug-conjugates (adcs) with ksp inhibitors and anti-cd123-antibodies |
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-
2005
- 2005-06-20 JP JP2007516842A patent/JP4836280B2/ja not_active Expired - Fee Related
- 2005-06-20 CA CA002571002A patent/CA2571002A1/en not_active Abandoned
- 2005-06-20 RU RU2007101612/04A patent/RU2427572C2/ru not_active IP Right Cessation
- 2005-06-20 EP EP05760871A patent/EP1765789B1/en not_active Not-in-force
- 2005-06-20 US US11/158,574 patent/US7576221B2/en not_active Expired - Fee Related
- 2005-06-20 MX MXPA06014909A patent/MXPA06014909A/es active IP Right Grant
- 2005-06-20 SG SG200904294-6A patent/SG153851A1/en unknown
- 2005-06-20 TW TW094120475A patent/TW200612958A/zh unknown
- 2005-06-20 WO PCT/US2005/022062 patent/WO2006002236A1/en active Application Filing
- 2005-06-20 NZ NZ552510A patent/NZ552510A/en not_active IP Right Cessation
- 2005-06-20 BR BRPI0510929-9A patent/BRPI0510929A/pt not_active IP Right Cessation
- 2005-06-20 AU AU2005258135A patent/AU2005258135B2/en not_active Ceased
- 2005-06-20 CN CNA2005800262037A patent/CN1993331A/zh active Pending
- 2005-06-20 KR KR1020077000979A patent/KR101170925B1/ko not_active IP Right Cessation
- 2005-06-20 ES ES05760871T patent/ES2409345T3/es active Active
-
2006
- 2006-12-18 TN TNP2006000419A patent/TNSN06419A1/en unknown
- 2006-12-18 IL IL180147A patent/IL180147A0/en unknown
-
2007
- 2007-01-16 ZA ZA200700481A patent/ZA200700481B/xx unknown
- 2007-01-17 MA MA29617A patent/MA28739B1/fr unknown
- 2007-01-18 EC EC2007007183A patent/ECSP077183A/es unknown
- 2007-01-18 NO NO20070343A patent/NO20070343L/no not_active Application Discontinuation
-
2009
- 2009-06-05 US US12/455,798 patent/US8318791B2/en not_active Expired - Fee Related
-
2011
- 2011-08-18 JP JP2011179247A patent/JP2011256197A/ja not_active Withdrawn
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2012
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Also Published As
Publication number | Publication date |
---|---|
MA28739B1 (fr) | 2007-07-02 |
BRPI0510929A (pt) | 2007-07-17 |
KR101170925B1 (ko) | 2012-08-07 |
US7576221B2 (en) | 2009-08-18 |
JP2011256197A (ja) | 2011-12-22 |
RU2427572C2 (ru) | 2011-08-27 |
AU2005258135A1 (en) | 2006-01-05 |
NO20070343L (no) | 2007-03-05 |
WO2006002236A1 (en) | 2006-01-05 |
US20130017196A1 (en) | 2013-01-17 |
EP1765789B1 (en) | 2013-02-27 |
US8318791B2 (en) | 2012-11-27 |
US20090258016A1 (en) | 2009-10-15 |
AU2005258135B2 (en) | 2011-09-22 |
MXPA06014909A (es) | 2007-02-28 |
NZ552510A (en) | 2010-12-24 |
SG153851A1 (en) | 2009-07-29 |
RU2007101612A (ru) | 2008-08-10 |
ES2409345T3 (es) | 2013-06-26 |
IL180147A0 (en) | 2007-06-03 |
US8735599B2 (en) | 2014-05-27 |
CN1993331A (zh) | 2007-07-04 |
KR20070106961A (ko) | 2007-11-06 |
TW200612958A (en) | 2006-05-01 |
EP1765789A1 (en) | 2007-03-28 |
JP4836280B2 (ja) | 2011-12-14 |
TNSN06419A1 (en) | 2008-02-22 |
JP2008503501A (ja) | 2008-02-07 |
CA2571002A1 (en) | 2006-01-05 |
US20060009472A1 (en) | 2006-01-12 |
ZA200700481B (en) | 2008-10-29 |
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