BRPI0510929A - derivados de n-(1-(1-benzil-4-fenil-1h-imidazol-2-il)-2,2-dimetilpropil) benzamida e compostos relacionados como inibidores de proteìna de eixo de kinesin (ksp) para o tratamento de cáncer - Google Patents
derivados de n-(1-(1-benzil-4-fenil-1h-imidazol-2-il)-2,2-dimetilpropil) benzamida e compostos relacionados como inibidores de proteìna de eixo de kinesin (ksp) para o tratamento de cáncerInfo
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- BRPI0510929A BRPI0510929A BRPI0510929-9A BRPI0510929A BRPI0510929A BR PI0510929 A BRPI0510929 A BR PI0510929A BR PI0510929 A BRPI0510929 A BR PI0510929A BR PI0510929 A BRPI0510929 A BR PI0510929A
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- 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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- 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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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- 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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- C07D401/02—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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- C07D401/02—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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- C07D401/02—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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- C07D403/04—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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- 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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- C07D413/06—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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- 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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- 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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- C07D417/12—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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- 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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- Nuclear Medicine, Radiotherapy & Molecular Imaging (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
DERIVADOS DE N-(1-BENZIL-4FENIL-1H-IMIDAZOL-2-IL)-2,2-DIMETILPROPIL) BENZAMIDA E COMPOSTOS RELACIONADOS COMO INIBIDORES DA PROTEìNA CINESINA DO FUSO (KSP PARA O TRATAMENTO DE CáNCER Esta invenção é dirigida aos compostos imidazol substituídos que modulam a atividade de KSP são úteis para o tratamento de cãncer e são representados pela fórmula (I) em que: R¬ 1¬ é selecionado do grupo que consiste em aminoacil, acilamino, carboxil, éster carboxílico, aril e aquil opcionalmente substituído com hidroxi ou halo; R¬ 2¬ é selecionado do grupo que consiste em hidrogênio, alquil e aril; R¬ 3¬ é selecionado do grupo que consiste em hidrogênioe X-A, em que X é selecionado do grupo que consiste em C (O)-, -C(S)-, -S(O)~ 2~ e -S(O)~ 2~-N (R)-, em que R é hidrogênio ou alquil; e A é selecionado do grupo que consiste em hidrogênio, alquil opcionalmente substituído.alcoxi opcionalmente substituído,aril opcionalmente substituído, carboxil, éster carboxílico, aminoacil, heteroaril opcionalmente substituído, heterocíclico opcionalmente substituído e cicloalquil opcionalmente subistituído em que os grupos opcionalmente substituídos são substituídos com 1 a 4 substituintes; R¬ 5¬ é selecionado do grupo que consiste em L-A, em que L é selecionado do grupo que consiste em -S(O)<sym>-, em que q é um ou dois, e C~ 1~ a C~ 5~ alquileno opcionalmente substituído com hidroxi, halo ou acilamino;e A ¬ 1¬ é selecionado do grupo que consiste em aril, aril substituído,heteroaril, heteroaril substituído, heterocíclico, heterocíclico substituido, cicloaquil e cicloalquil subastituido e um de R¬ 6¬ ou R¬ 7¬ é selecionado do grupo que consiste em heterocíclico, abril e heteroaril, todos os quais podem ser opcionalmente substituídos com (R¬ 8¬)<sym> em que R¬ 8¬ e m é um número inteiro de 1 a 3 e o outro de R¬ 6¬ ou R¬ 7¬ é selecionado do grupo que consiste em hidrogêncio,halo e alquil, ou R¬ 6¬ e R¬ 7¬ são ambos hidrogênio; os outros substituintes são definidos nas reivinicações.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
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US58092704P | 2004-06-18 | 2004-06-18 | |
PCT/US2005/022062 WO2006002236A1 (en) | 2004-06-18 | 2005-06-20 | N- (1- (1-benzyl -4-phenyl-1h-imidazol-2-yl) -2,2-dymethylpropyl) benzamide derivatives and related compounds as kinesin spindle protein (ksp) inhibitors for the treatment of cancer |
Publications (1)
Publication Number | Publication Date |
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BRPI0510929A true BRPI0510929A (pt) | 2007-07-17 |
Family
ID=34980173
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
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BRPI0510929-9A BRPI0510929A (pt) | 2004-06-18 | 2005-06-20 | derivados de n-(1-(1-benzil-4-fenil-1h-imidazol-2-il)-2,2-dimetilpropil) benzamida e compostos relacionados como inibidores de proteìna de eixo de kinesin (ksp) para o tratamento de cáncer |
Country Status (21)
Country | Link |
---|---|
US (3) | US7576221B2 (pt) |
EP (1) | EP1765789B1 (pt) |
JP (2) | JP4836280B2 (pt) |
KR (1) | KR101170925B1 (pt) |
CN (1) | CN1993331A (pt) |
AU (1) | AU2005258135B2 (pt) |
BR (1) | BRPI0510929A (pt) |
CA (1) | CA2571002A1 (pt) |
EC (1) | ECSP077183A (pt) |
ES (1) | ES2409345T3 (pt) |
IL (1) | IL180147A0 (pt) |
MA (1) | MA28739B1 (pt) |
MX (1) | MXPA06014909A (pt) |
NO (1) | NO20070343L (pt) |
NZ (1) | NZ552510A (pt) |
RU (1) | RU2427572C2 (pt) |
SG (1) | SG153851A1 (pt) |
TN (1) | TNSN06419A1 (pt) |
TW (1) | TW200612958A (pt) |
WO (1) | WO2006002236A1 (pt) |
ZA (1) | ZA200700481B (pt) |
Families Citing this family (31)
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KR101170925B1 (ko) * | 2004-06-18 | 2012-08-07 | 노바티스 백신즈 앤드 다이아그노스틱스 인코포레이티드 | 암 치료용 키네신 방추 단백질 (ksp) 억제제로서의n-(1-(1-벤질-4-페닐-1h-이미다졸-2-일)-2,2-디메틸프로필)벤자미드 유도체 및 관련 화합물 |
MX2007001953A (es) | 2004-08-18 | 2007-05-09 | Astrazeneca Ab | Enantiomeros de pirimidonas fusionadas seleccionadas y usos en el tratamiento y prevencion del cancer. |
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 |
MX2008013427A (es) | 2006-04-19 | 2008-11-04 | Novartis Ag | Compuestos de benzoxazole y benzotiazole sustituidos-6-0 y metodos para inhibir la señalizacion csf-1r. |
ES2376668T3 (es) | 2006-09-05 | 2012-03-15 | Kyowa Hakko Kirin Co., Ltd. | Derivado de imidazol. |
US20100120717A1 (en) | 2006-10-09 | 2010-05-13 | Brown Jason W | Kinase inhibitors |
CA2668661A1 (en) * | 2006-11-13 | 2008-05-29 | Novartis Ag | Substituted pyrazole and triazole compounds as ksp inhibitors |
MX2009007260A (es) * | 2007-01-05 | 2009-07-10 | Novartis Ag | Derivados de imidazol como inhibidores de proteina de huso de cinesina (eg-5). |
US8252832B2 (en) * | 2007-12-14 | 2012-08-28 | Novartis Ag | Kinesin inhibitors as cancer therapeutics |
WO2010084186A1 (en) | 2009-01-26 | 2010-07-29 | Novartis Ag | Salts and polymorphs of a kinesin inhibitor compound |
CN103153970A (zh) * | 2010-04-15 | 2013-06-12 | 诺瓦提斯公司 | 作为ksp抑制剂的*唑和噻唑化合物 |
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 |
EP2968591A1 (en) * | 2013-03-15 | 2016-01-20 | Novartis AG | Cell proliferation inhibitors and conjugates thereof |
NZ720736A (en) * | 2013-12-23 | 2020-08-28 | Bayer Pharma AG | Antibody drug conjugates (adcs) with kinesin spindel protein (ksp) |
WO2016020791A1 (en) | 2014-08-05 | 2016-02-11 | Novartis Ag | Ckit antibody drug conjugates |
EP3233127A1 (de) | 2014-12-15 | 2017-10-25 | Bayer Pharma Aktiengesellschaft | Antikörper-wirkstoff-konjugate (adcs) von ksp-inhibitoren mit aglycosylierten anti-tweakrantikörpern |
IS2977B (is) | 2015-02-23 | 2017-07-15 | Actavis Group Ptc Ehf. | Aðferð til framleiðslu á milliefnum sem eru nytsamleg við nýsmíði á elúxadólíni |
CA2990076A1 (en) * | 2015-06-22 | 2016-12-29 | Bayer Pharma Aktiengesellschaft | Antibody drug conjugates (adcs) and antibody prodrug conjugates (apdcs) with enzymatically cleavable groups |
PE20180452A1 (es) | 2015-06-23 | 2018-03-05 | Bayer Pharma AG | Conjugados homogeneos especificos de sitio con inhibidores de ksp |
JP2018525334A (ja) | 2015-06-23 | 2018-09-06 | バイエル ファーマ アクチエンゲゼルシャフト | キネシンスピンドルタンパク質(ksp)阻害剤の抗tweakr抗体との抗体薬物複合体 |
US11071788B2 (en) | 2015-06-23 | 2021-07-27 | Bayer Pharma Aktiengesellschaft | Antibody drug conjugates of kinesin spindel protein (KSP) inhibitors with antiB7H3-antibodies |
EP3471776B1 (en) | 2016-06-15 | 2022-05-04 | Bayer Pharma Aktiengesellschaft | Specific antibody-drug-conjugates with ksp inhibitors and anti-cd123-antibodies |
AU2017380871A1 (en) | 2016-12-21 | 2019-07-11 | Bayer Aktiengesellschaft | Antibody drug conjugates (ADCs) having enzymatically cleavable groups |
JP7030811B2 (ja) | 2016-12-21 | 2022-03-07 | バイエル・ファルマ・アクティエンゲゼルシャフト | Ksp阻害剤を有する特異的抗体-薬物コンジュゲート(adc) |
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AU2019403486A1 (en) * | 2018-12-20 | 2021-06-24 | Amgen Inc. | KIF18A inhibitors |
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-
2005
- 2005-06-20 KR KR1020077000979A patent/KR101170925B1/ko not_active IP Right Cessation
- 2005-06-20 BR BRPI0510929-9A patent/BRPI0510929A/pt not_active IP Right Cessation
- 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 NZ NZ552510A patent/NZ552510A/en not_active IP Right Cessation
- 2005-06-20 CN CNA2005800262037A patent/CN1993331A/zh active Pending
- 2005-06-20 TW TW094120475A patent/TW200612958A/zh unknown
- 2005-06-20 AU AU2005258135A patent/AU2005258135B2/en not_active Ceased
- 2005-06-20 ES ES05760871T patent/ES2409345T3/es active Active
- 2005-06-20 SG SG200904294-6A patent/SG153851A1/en unknown
- 2005-06-20 CA CA002571002A patent/CA2571002A1/en not_active Abandoned
- 2005-06-20 MX MXPA06014909A patent/MXPA06014909A/es active IP Right Grant
- 2005-06-20 JP JP2007516842A patent/JP4836280B2/ja not_active Expired - Fee Related
- 2005-06-20 US US11/158,574 patent/US7576221B2/en not_active Expired - Fee Related
- 2005-06-20 WO PCT/US2005/022062 patent/WO2006002236A1/en active Application Filing
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2006
- 2006-12-18 IL IL180147A patent/IL180147A0/en unknown
- 2006-12-18 TN TNP2006000419A patent/TNSN06419A1/en unknown
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2007
- 2007-01-16 ZA ZA200700481A patent/ZA200700481B/xx unknown
- 2007-01-17 MA MA29617A patent/MA28739B1/fr unknown
- 2007-01-18 NO NO20070343A patent/NO20070343L/no not_active Application Discontinuation
- 2007-01-18 EC EC2007007183A patent/ECSP077183A/es unknown
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2009
- 2009-06-05 US US12/455,798 patent/US8318791B2/en not_active Expired - Fee Related
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- 2011-08-18 JP JP2011179247A patent/JP2011256197A/ja not_active Withdrawn
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---|---|
US7576221B2 (en) | 2009-08-18 |
KR20070106961A (ko) | 2007-11-06 |
IL180147A0 (en) | 2007-06-03 |
SG153851A1 (en) | 2009-07-29 |
AU2005258135B2 (en) | 2011-09-22 |
US20130017196A1 (en) | 2013-01-17 |
US8735599B2 (en) | 2014-05-27 |
ECSP077183A (es) | 2007-02-28 |
JP2011256197A (ja) | 2011-12-22 |
TW200612958A (en) | 2006-05-01 |
MXPA06014909A (es) | 2007-02-28 |
JP4836280B2 (ja) | 2011-12-14 |
US20090258016A1 (en) | 2009-10-15 |
EP1765789B1 (en) | 2013-02-27 |
ZA200700481B (en) | 2008-10-29 |
US20060009472A1 (en) | 2006-01-12 |
RU2007101612A (ru) | 2008-08-10 |
CN1993331A (zh) | 2007-07-04 |
TNSN06419A1 (en) | 2008-02-22 |
CA2571002A1 (en) | 2006-01-05 |
RU2427572C2 (ru) | 2011-08-27 |
ES2409345T3 (es) | 2013-06-26 |
NO20070343L (no) | 2007-03-05 |
JP2008503501A (ja) | 2008-02-07 |
US8318791B2 (en) | 2012-11-27 |
WO2006002236A1 (en) | 2006-01-05 |
MA28739B1 (fr) | 2007-07-02 |
EP1765789A1 (en) | 2007-03-28 |
KR101170925B1 (ko) | 2012-08-07 |
NZ552510A (en) | 2010-12-24 |
AU2005258135A1 (en) | 2006-01-05 |
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