CA2585490A1 - Composes heteroaromatiques de l'azote qui se lient au site actif d'enzymes de type proteines kinases - Google Patents
Composes heteroaromatiques de l'azote qui se lient au site actif d'enzymes de type proteines kinases Download PDFInfo
- Publication number
- CA2585490A1 CA2585490A1 CA002585490A CA2585490A CA2585490A1 CA 2585490 A1 CA2585490 A1 CA 2585490A1 CA 002585490 A CA002585490 A CA 002585490A CA 2585490 A CA2585490 A CA 2585490A CA 2585490 A1 CA2585490 A1 CA 2585490A1
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- Prior art keywords
- alkyl
- aryl
- heteroaryl
- alkoxy
- nr4r5
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Abandoned
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- -1 Nitrogen heteroaromatic compounds Chemical class 0.000 title claims description 124
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 title claims description 16
- 229910052757 nitrogen Inorganic materials 0.000 title claims description 11
- 102000001253 Protein Kinase Human genes 0.000 title abstract description 13
- 108060006633 protein kinase Proteins 0.000 title abstract description 13
- 150000001875 compounds Chemical class 0.000 claims abstract description 126
- 238000011282 treatment Methods 0.000 claims abstract description 35
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- 125000004890 (C1-C6) alkylamino group Chemical group 0.000 claims description 79
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- CDBYLPFSWZWCQE-UHFFFAOYSA-L Sodium Carbonate Chemical compound [Na+].[Na+].[O-]C([O-])=O CDBYLPFSWZWCQE-UHFFFAOYSA-L 0.000 claims description 8
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- RIOQSEWOXXDEQQ-UHFFFAOYSA-N triphenylphosphine Chemical compound C1=CC=CC=C1P(C=1C=CC=CC=1)C1=CC=CC=C1 RIOQSEWOXXDEQQ-UHFFFAOYSA-N 0.000 claims description 8
- ZADPBFCGQRWHPN-UHFFFAOYSA-N boronic acid Chemical compound OBO ZADPBFCGQRWHPN-UHFFFAOYSA-N 0.000 claims description 7
- 125000000623 heterocyclic group Chemical group 0.000 claims description 7
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims description 5
- KZPYGQFFRCFCPP-UHFFFAOYSA-N 1,1'-bis(diphenylphosphino)ferrocene Chemical compound [Fe+2].C1=CC=C[C-]1P(C=1C=CC=CC=1)C1=CC=CC=C1.C1=CC=C[C-]1P(C=1C=CC=CC=1)C1=CC=CC=C1 KZPYGQFFRCFCPP-UHFFFAOYSA-N 0.000 claims description 5
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- VYYVWKHKMVUYOC-UHFFFAOYSA-N n-[(4-chloro-3-fluorophenyl)methyl]-5-(2-chloropyridin-4-yl)pyridin-3-amine Chemical compound C1=C(Cl)C(F)=CC(CNC=2C=C(C=NC=2)C=2C=C(Cl)N=CC=2)=C1 VYYVWKHKMVUYOC-UHFFFAOYSA-N 0.000 claims description 3
- UYEDPJPWLBUCNZ-UHFFFAOYSA-N n-[(4-chloro-3-fluorophenyl)methyl]-5-(3-chloropyridin-4-yl)pyridin-3-amine Chemical compound C1=C(Cl)C(F)=CC(CNC=2C=C(C=NC=2)C=2C(=CN=CC=2)Cl)=C1 UYEDPJPWLBUCNZ-UHFFFAOYSA-N 0.000 claims description 3
- CQGGCIDBPAJPHX-UHFFFAOYSA-N n-[(4-chloro-3-fluorophenyl)methyl]-5-(3-fluoropyridin-4-yl)pyridin-3-amine Chemical compound C1=C(Cl)C(F)=CC(CNC=2C=C(C=NC=2)C=2C(=CN=CC=2)F)=C1 CQGGCIDBPAJPHX-UHFFFAOYSA-N 0.000 claims description 3
- 229910052763 palladium Inorganic materials 0.000 claims description 3
- YJVFFLUZDVXJQI-UHFFFAOYSA-L palladium(ii) acetate Chemical compound [Pd+2].CC([O-])=O.CC([O-])=O YJVFFLUZDVXJQI-UHFFFAOYSA-L 0.000 claims description 3
- 238000000527 sonication Methods 0.000 claims description 3
- 125000006291 3-hydroxybenzyl group Chemical group [H]OC1=C([H])C([H])=C([H])C(=C1[H])C([H])([H])* 0.000 claims description 2
- 125000006283 4-chlorobenzyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1Cl)C([H])([H])* 0.000 claims description 2
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- 125000004203 4-hydroxyphenyl group Chemical group [H]OC1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 125000000339 4-pyridyl group Chemical group N1=C([H])C([H])=C([*])C([H])=C1[H] 0.000 claims 1
- CPFXIMAVAHVWDM-UHFFFAOYSA-N ClC1=C(C=C(CNC2=CC(=CC=C2)C2=CC=NC=C2)C=C1)F.N1=CC(=CC(=C1)NC(CC1=CC=C(C=C1)Cl)=O)C1=CC=NC=C1 Chemical compound ClC1=C(C=C(CNC2=CC(=CC=C2)C2=CC=NC=C2)C=C1)F.N1=CC(=CC(=C1)NC(CC1=CC=C(C=C1)Cl)=O)C1=CC=NC=C1 CPFXIMAVAHVWDM-UHFFFAOYSA-N 0.000 claims 1
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Classifications
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- 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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- C—CHEMISTRY; METALLURGY
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- 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
- C07D213/75—Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
-
- 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
- C07D401/04—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
-
- 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
- C07D401/14—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 three or more hetero rings
-
- 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
- C07D405/14—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 three or more hetero rings
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Biomedical Technology (AREA)
- Heart & Thoracic Surgery (AREA)
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- Cardiology (AREA)
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- Physical Education & Sports Medicine (AREA)
- Ophthalmology & Optometry (AREA)
- Virology (AREA)
- Orthopedic Medicine & Surgery (AREA)
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- AIDS & HIV (AREA)
- Vascular Medicine (AREA)
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- Endocrinology (AREA)
- Reproductive Health (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Pyridine Compounds (AREA)
Applications Claiming Priority (5)
Application Number | Priority Date | Filing Date | Title |
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GB0425026A GB0425026D0 (en) | 2004-11-12 | 2004-11-12 | Compounds which bind to the active site of protein kinase enzymes |
GB0425026.2 | 2004-11-12 | ||
GBGB0500245.6A GB0500245D0 (en) | 2004-11-12 | 2005-01-07 | Compounds which bind to the active site of protein kinase enzymes |
GB0500245.6 | 2005-01-07 | ||
PCT/GB2005/004358 WO2006051311A1 (fr) | 2004-11-12 | 2005-11-11 | Composés hétéroaromatiques de l'azote qui se lient au site actif d'enzymes de type protéines kinases |
Publications (1)
Publication Number | Publication Date |
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CA2585490A1 true CA2585490A1 (fr) | 2006-05-18 |
Family
ID=35788166
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
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CA002585490A Abandoned CA2585490A1 (fr) | 2004-11-12 | 2005-11-11 | Composes heteroaromatiques de l'azote qui se lient au site actif d'enzymes de type proteines kinases |
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EP (1) | EP1814856A1 (fr) |
JP (1) | JP2008519814A (fr) |
CA (1) | CA2585490A1 (fr) |
WO (1) | WO2006051311A1 (fr) |
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US8211919B2 (en) | 2005-09-02 | 2012-07-03 | Astellas Pharma Inc. | Amide derivatives as rock inhibitors |
CA2660560A1 (fr) * | 2006-08-16 | 2008-02-21 | Boehringer Ingelheim International Gmbh | Composes de pyrazine, leur utilisation et procedes de preparation |
US8071779B2 (en) * | 2006-12-18 | 2011-12-06 | Inspire Pharmaceuticals, Inc. | Cytoskeletal active rho kinase inhibitor compounds, composition and use |
GEP20125379B (en) | 2007-05-03 | 2012-01-10 | Pfizer Ltd | 2 -pyridine carboxamide derivatives as sodium channel modulators |
WO2009026276A1 (fr) | 2007-08-22 | 2009-02-26 | Irm Llc | Composés et compositions de 5- (4- (haloalkoxy) phényl) pyrimidine-2-amine utilisés comme inhibiteurs de kinases |
TWI504395B (zh) | 2009-03-10 | 2015-10-21 | Substituted 3-amino-2-mercaptoquinoline as a KCNQ2 / 3 modifier | |
TWI461197B (zh) | 2009-03-12 | 2014-11-21 | 2-mercaptoquinoline-3-carboxamide as a KCNQ2 / 3 modifier | |
TW201038565A (en) | 2009-03-12 | 2010-11-01 | Gruenenthal Gmbh | Substituted 2-mercapto-3-aminopyridines as KCNQ2/3 modulators |
TWI475020B (zh) | 2009-03-12 | 2015-03-01 | The substituted nicotine amide as a KCNQ2 / 3 modifier | |
MX2011012198A (es) | 2009-05-15 | 2011-12-08 | Novartis Ag | Aril-piridinas como inhibidoras de sintasa de aldosterona. |
JP6041671B2 (ja) * | 2009-06-12 | 2016-12-14 | アビバックス | ガンを治療する為に有用な化合物 |
US10253020B2 (en) | 2009-06-12 | 2019-04-09 | Abivax | Compounds for preventing, inhibiting, or treating cancer, AIDS and/or premature aging |
PL2531492T3 (pl) | 2010-02-05 | 2016-10-31 | Pochodne 1,2,4-triazyno-4-aminy | |
JP5605727B2 (ja) * | 2010-04-06 | 2014-10-15 | Jnc株式会社 | セレンテラジン類縁体及びセレンテラミド類縁体 |
BR112013004766A2 (pt) | 2010-08-27 | 2016-08-02 | Gruenenthal Gmbh | 2-amino-quinolina-3-carboxamidas substituídas como moduladores de kcnq2/3 |
EP2609086B1 (fr) | 2010-08-27 | 2015-02-25 | Grünenthal GmbH | 2-oxo- et 2-thioxo-dihydroquinoléine-3-carboxamides substitués comme modulateurs de kcnq2/3 |
TWI522349B (zh) | 2010-08-27 | 2016-02-21 | 歌林達股份有限公司 | 作為kcnq2/3調節劑之被取代之2-氧基-喹啉-3-甲醯胺 |
BR112013005056A2 (pt) | 2010-09-01 | 2016-05-31 | Gruenenthal Gmbh | 1-oxo-di-hidroisoquinolina-3-carboxamidas substituídas como moduladores kcnq2/3 |
EA201390717A1 (ru) * | 2010-11-17 | 2013-10-30 | Новартис Аг | 3-(аминоарил)пиридиновые соединения |
WO2013126608A1 (fr) * | 2012-02-22 | 2013-08-29 | Sanford-Burnham Medical Research Institute | Composés sulfonamides et leurs utilisations en tant qu'inhibiteurs de tnap |
EP2757161A1 (fr) | 2013-01-17 | 2014-07-23 | Splicos | miRNA-124 comme biomarqueur de l'infection virale |
EP3626245B1 (fr) * | 2013-04-24 | 2021-05-05 | Kyushu University, National University Corporation | Agent thérapeutique pour maladie du fond de l'oeil |
WO2015108861A1 (fr) | 2014-01-14 | 2015-07-23 | Millennium Pharmaceuticals, Inc. | Hétéroaryles et utilisations de ceux-ci |
WO2015108881A1 (fr) | 2014-01-14 | 2015-07-23 | Millennium Pharmaceuticals, Inc. | Hétéroaryles et utilisations de ceux-ci |
EP2974729A1 (fr) | 2014-07-17 | 2016-01-20 | Abivax | Dérivés de quinoléine utilisés dans le traitement de maladies inflammatoires |
WO2017007755A1 (fr) | 2015-07-06 | 2017-01-12 | Rodin Therapeutics, Inc. | N-aminophényl-amides hétérocycliques en tant qu'inhibiteurs de l'histone désacétylase |
PT3319959T (pt) | 2015-07-06 | 2021-12-06 | Alkermes Inc | Inibidores hetero-halo de histona desacetilase |
EP4088719A1 (fr) | 2015-10-13 | 2022-11-16 | Institut National de la Santé et de la Recherche Médicale (INSERM) | Procédés et compositions pharmaceutiques pour le traitement de non-perfusion capillaire rétinienne |
US12048761B2 (en) | 2015-10-13 | 2024-07-30 | Inserm (Institut National De La Santé Et De La Recherche Medicale) | Methods and pharmaceutical compositions for the treatment of retinal capillary non-perfusion |
US11168068B2 (en) | 2016-07-18 | 2021-11-09 | Janssen Pharmaceutica Nv | Tau PET imaging ligands |
MX2019008302A (es) | 2017-01-11 | 2019-12-02 | Rodin Therapeutics Inc | Inhibidores biciclicos de histona desacetilasa. |
MX2020001484A (es) | 2017-08-07 | 2020-08-20 | Rodin Therapeutics Inc | Inhibidores bicíclicos de la histona desacetilasa. |
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EP3669873A1 (fr) | 2018-12-20 | 2020-06-24 | Abivax | Dérivés de quinoline destinés à être utilisés dans le traitement de maladies inflammatoires |
EA202191890A1 (ru) | 2019-01-18 | 2022-02-03 | Астразенека Аб | Ингибиторы pcsk9 и способы их применения |
US11384083B2 (en) | 2019-02-15 | 2022-07-12 | Incyte Corporation | Substituted spiro[cyclopropane-1,5′-pyrrolo[2,3-d]pyrimidin]-6′(7′h)-ones as CDK2 inhibitors |
US11472791B2 (en) | 2019-03-05 | 2022-10-18 | Incyte Corporation | Pyrazolyl pyrimidinylamine compounds as CDK2 inhibitors |
US11919904B2 (en) | 2019-03-29 | 2024-03-05 | Incyte Corporation | Sulfonylamide compounds as CDK2 inhibitors |
US11447494B2 (en) | 2019-05-01 | 2022-09-20 | Incyte Corporation | Tricyclic amine compounds as CDK2 inhibitors |
WO2020223469A1 (fr) | 2019-05-01 | 2020-11-05 | Incyte Corporation | Dérivés de n-(1-(méthylsulfonyl)pipéridin-4-yl)-4,5-di hydro-1h-imidazo[4,5-h]quinazolin-8-amine et composés apparentés utilisés en tant qu'inhibiteurs de kinase 2 dépendante des cyclines (cdk2) pour le traitement du cancer |
KR20220064369A (ko) | 2019-08-14 | 2022-05-18 | 인사이트 코포레이션 | Cdk2 저해제로서의 이미다졸릴 피리디미딘일아민 화합물 |
US11851426B2 (en) | 2019-10-11 | 2023-12-26 | Incyte Corporation | Bicyclic amines as CDK2 inhibitors |
US11981671B2 (en) | 2021-06-21 | 2024-05-14 | Incyte Corporation | Bicyclic pyrazolyl amines as CDK2 inhibitors |
US11976073B2 (en) | 2021-12-10 | 2024-05-07 | Incyte Corporation | Bicyclic amines as CDK2 inhibitors |
WO2024119067A1 (fr) | 2022-12-02 | 2024-06-06 | Neumora Therapeutics, Inc. | Méthodes de traitement de troubles neurologiques |
WO2024159284A1 (fr) * | 2023-01-30 | 2024-08-08 | Eurofarma Laboratórios S.A. | Hydrazides inhibiteurs de nav 1.7 et/ou de nav 1.8, leurs procédés d'obtention, compositions, utilisations, méthodes de traitement et trousses |
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---|---|---|---|---|
DE60023926T2 (de) * | 1999-09-10 | 2006-07-20 | Merck & Co., Inc. | Tyrosin kinase inhibitoren |
DK1330452T3 (da) * | 2000-09-20 | 2009-03-16 | Ortho Mcneil Janssen Pharm | Pyrazinderivater som modulatorer af tyrosinkinaser |
US7122550B2 (en) * | 2002-05-23 | 2006-10-17 | Cytopia Pty Ltd | Protein kinase inhibitors |
JP2007516196A (ja) * | 2003-07-02 | 2007-06-21 | ガラパゴス エヌブイ | Rhoキナーゼ阻害剤としてのピラジン及びピラリジン誘導体 |
-
2005
- 2005-11-11 CA CA002585490A patent/CA2585490A1/fr not_active Abandoned
- 2005-11-11 JP JP2007540715A patent/JP2008519814A/ja not_active Abandoned
- 2005-11-11 WO PCT/GB2005/004358 patent/WO2006051311A1/fr active Application Filing
- 2005-11-11 EP EP05809312A patent/EP1814856A1/fr not_active Withdrawn
Also Published As
Publication number | Publication date |
---|---|
WO2006051311A1 (fr) | 2006-05-18 |
EP1814856A1 (fr) | 2007-08-08 |
JP2008519814A (ja) | 2008-06-12 |
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