JP2008526721A5 - - Google Patents
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- JP2008526721A5 JP2008526721A5 JP2007548895A JP2007548895A JP2008526721A5 JP 2008526721 A5 JP2008526721 A5 JP 2008526721A5 JP 2007548895 A JP2007548895 A JP 2007548895A JP 2007548895 A JP2007548895 A JP 2007548895A JP 2008526721 A5 JP2008526721 A5 JP 2008526721A5
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- -1 NR c Inorganic materials 0.000 claims 64
- 125000001424 substituent group Chemical group 0.000 claims 50
- 229910052760 oxygen Inorganic materials 0.000 claims 30
- 125000000623 heterocyclic group Chemical group 0.000 claims 29
- 125000001183 hydrocarbyl group Chemical group 0.000 claims 23
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 23
- 229910052736 halogen Inorganic materials 0.000 claims 22
- 150000002367 halogens Chemical class 0.000 claims 22
- 125000005842 heteroatom Chemical group 0.000 claims 22
- 229910052717 sulfur Inorganic materials 0.000 claims 22
- 239000001257 hydrogen Substances 0.000 claims 21
- 229910052739 hydrogen Inorganic materials 0.000 claims 21
- 125000002837 carbocyclic group Chemical group 0.000 claims 15
- 125000001072 heteroaryl group Chemical group 0.000 claims 15
- 125000004432 carbon atom Chemical group C* 0.000 claims 14
- 125000003277 amino group Chemical group 0.000 claims 13
- 150000001875 compounds Chemical class 0.000 claims 13
- 150000002431 hydrogen Chemical group 0.000 claims 13
- 229910052757 nitrogen Inorganic materials 0.000 claims 12
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 12
- 125000003118 aryl group Chemical group 0.000 claims 11
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 11
- 229910052799 carbon Inorganic materials 0.000 claims 10
- 125000002950 monocyclic group Chemical group 0.000 claims 9
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 9
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 9
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 8
- 125000004093 cyano group Chemical group *C#N 0.000 claims 8
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 8
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 8
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 7
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 6
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 6
- 229910002091 carbon monoxide Inorganic materials 0.000 claims 6
- 125000001309 chloro group Chemical group Cl* 0.000 claims 5
- 125000001153 fluoro group Chemical group F* 0.000 claims 5
- 125000004043 oxo group Chemical group O=* 0.000 claims 5
- 239000001301 oxygen Chemical group 0.000 claims 5
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 4
- 125000003282 alkyl amino group Chemical group 0.000 claims 4
- 125000006615 aromatic heterocyclic group Chemical group 0.000 claims 4
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 4
- 239000011593 sulfur Substances 0.000 claims 4
- 125000006163 5-membered heteroaryl group Chemical group 0.000 claims 3
- 150000001204 N-oxides Chemical class 0.000 claims 3
- 125000002619 bicyclic group Chemical group 0.000 claims 3
- 125000004122 cyclic group Chemical group 0.000 claims 3
- 125000000753 cycloalkyl group Chemical group 0.000 claims 3
- 125000000842 isoxazolyl group Chemical group 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- 239000012453 solvate Substances 0.000 claims 3
- 125000002941 2-furyl group Chemical group O1C([*])=C([H])C([H])=C1[H] 0.000 claims 2
- 125000004442 acylamino group Chemical group 0.000 claims 2
- 125000004423 acyloxy group Chemical group 0.000 claims 2
- 125000004466 alkoxycarbonylamino group Chemical group 0.000 claims 2
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 2
- 239000000460 chlorine Substances 0.000 claims 2
- 229910052801 chlorine Inorganic materials 0.000 claims 2
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 2
- 125000002541 furyl group Chemical group 0.000 claims 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 2
- 125000001620 monocyclic carbocycle group Chemical group 0.000 claims 2
- 125000001064 morpholinomethyl group Chemical group [H]C([H])(*)N1C([H])([H])C([H])([H])OC([H])([H])C1([H])[H] 0.000 claims 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 2
- 125000002971 oxazolyl group Chemical group 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- OCTYSLJDFYIKNR-UHFFFAOYSA-N 1-(2,6-difluorophenyl)-3-[3-[6-(morpholin-4-ylmethyl)-1H-benzimidazol-2-yl]-1,2-thiazol-4-yl]urea Chemical compound FC1=CC=CC(F)=C1NC(=O)NC1=CSN=C1C1=NC2=CC(CN3CCOCC3)=CC=C2N1 OCTYSLJDFYIKNR-UHFFFAOYSA-N 0.000 claims 1
- WTPHPNVGUMVTQE-UHFFFAOYSA-N 1-(2,6-difluorophenyl)-3-[3-[6-(morpholin-4-ylmethyl)-1h-benzimidazol-2-yl]-2h-1,3-thiazol-5-yl]urea Chemical compound FC1=CC=CC(F)=C1NC(=O)NC1=CN(C=2NC3=CC=C(CN4CCOCC4)C=C3N=2)CS1 WTPHPNVGUMVTQE-UHFFFAOYSA-N 0.000 claims 1
- URJTVZKSCYVLMF-UHFFFAOYSA-N 1-cyclopropyl-3-[3-[6-(morpholin-4-ylmethyl)-1H-benzimidazol-2-yl]-1,2-thiazol-4-yl]urea Chemical compound C=1SN=C(C=2NC3=CC=C(CN4CCOCC4)C=C3N=2)C=1NC(=O)NC1CC1 URJTVZKSCYVLMF-UHFFFAOYSA-N 0.000 claims 1
- UIJXCTPSHQCPOY-UHFFFAOYSA-N 1-cyclopropyl-3-[3-[6-(morpholin-4-ylmethyl)-1h-benzimidazol-2-yl]-2h-1,3-thiazol-5-yl]urea Chemical compound C=1N(C=2NC3=CC=C(CN4CCOCC4)C=C3N=2)CSC=1NC(=O)NC1CC1 UIJXCTPSHQCPOY-UHFFFAOYSA-N 0.000 claims 1
- LFDAPUZYRQHWPS-UHFFFAOYSA-N 2,6-difluoro-N-[3-[5-(morpholin-4-ylmethyl)-1H-indol-2-yl]-1,2-thiazol-4-yl]benzamide Chemical compound FC1=CC=CC(F)=C1C(=O)NC1=CSN=C1C1=CC2=CC(CN3CCOCC3)=CC=C2N1 LFDAPUZYRQHWPS-UHFFFAOYSA-N 0.000 claims 1
- 125000006508 2,6-difluorobenzyl group Chemical group [H]C1=C([H])C(F)=C(C(F)=C1[H])C([H])([H])* 0.000 claims 1
- XWDJLAUIRRHHIL-UHFFFAOYSA-N 2-chloro-4-morpholin-4-yl-n-[4-[6-(morpholin-4-ylmethyl)-1h-benzimidazol-2-yl]-1,3-thiazol-5-yl]benzamide Chemical compound ClC1=CC(N2CCOCC2)=CC=C1C(=O)NC=1SC=NC=1C(NC1=C2)=NC1=CC=C2CN1CCOCC1 XWDJLAUIRRHHIL-UHFFFAOYSA-N 0.000 claims 1
- 125000001622 2-naphthyl group Chemical group [H]C1=C([H])C([H])=C2C([H])=C(*)C([H])=C([H])C2=C1[H] 0.000 claims 1
- 125000004105 2-pyridyl group Chemical group N1=C([*])C([H])=C([H])C([H])=C1[H] 0.000 claims 1
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 claims 1
- 125000001397 3-pyrrolyl group Chemical group [H]N1C([H])=C([*])C([H])=C1[H] 0.000 claims 1
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical group [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims 1
- 241000124008 Mammalia Species 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- XSQUKJJJFZCRTK-UHFFFAOYSA-N Urea Chemical compound NC(N)=O XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 claims 1
- 230000002159 abnormal effect Effects 0.000 claims 1
- 239000002671 adjuvant Substances 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 150000001408 amides Chemical class 0.000 claims 1
- BNBQRQQYDMDJAH-UHFFFAOYSA-N benzodioxan Chemical group C1=CC=C2OCCOC2=C1 BNBQRQQYDMDJAH-UHFFFAOYSA-N 0.000 claims 1
- 125000006367 bivalent amino carbonyl group Chemical group [H]N([*:1])C([*:2])=O 0.000 claims 1
- 239000000872 buffer Substances 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 239000004202 carbamide Substances 0.000 claims 1
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 claims 1
- 230000010261 cell growth Effects 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000001301 ethoxy group Chemical group [H]C([H])([H])C([H])([H])O* 0.000 claims 1
- 239000000945 filler Substances 0.000 claims 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 1
- 125000005647 linker group Chemical group 0.000 claims 1
- 239000000314 lubricant Substances 0.000 claims 1
- 125000000250 methylamino group Chemical group [H]N(*)C([H])([H])[H] 0.000 claims 1
- 125000004170 methylsulfonyl group Chemical group [H]C([H])([H])S(*)(=O)=O 0.000 claims 1
- 125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 claims 1
- 125000006518 morpholino carbonyl group Chemical group [H]C1([H])OC([H])([H])C([H])([H])N(C(*)=O)C1([H])[H] 0.000 claims 1
- 125000002757 morpholinyl group Chemical group 0.000 claims 1
- STZPSNUPCHFSMK-UHFFFAOYSA-N n-[4-(1h-benzimidazol-2-yl)-1,3-thiazol-5-yl]-2,6-difluorobenzamide Chemical compound FC1=CC=CC(F)=C1C(=O)NC1=C(C=2NC3=CC=CC=C3N=2)N=CS1 STZPSNUPCHFSMK-UHFFFAOYSA-N 0.000 claims 1
- XCMYPPZEMCUEPD-UHFFFAOYSA-N n-[4-(5,6-dimethoxy-1h-benzimidazol-2-yl)-1,3-thiazol-5-yl]-1-methylpiperidine-4-carboxamide Chemical compound N1C=2C=C(OC)C(OC)=CC=2N=C1C=1N=CSC=1NC(=O)C1CCN(C)CC1 XCMYPPZEMCUEPD-UHFFFAOYSA-N 0.000 claims 1
- LQSHTJUGHPOZMC-UHFFFAOYSA-N n-[4-(5,6-dimethoxy-1h-benzimidazol-2-yl)-1,3-thiazol-5-yl]pyrrolidine-2-carboxamide Chemical compound N1C=2C=C(OC)C(OC)=CC=2N=C1C=1N=CSC=1NC(=O)C1CCCN1 LQSHTJUGHPOZMC-UHFFFAOYSA-N 0.000 claims 1
- OICRXGWDCJOVOB-UHFFFAOYSA-N n-[4-[6-(morpholin-4-ylmethyl)-1h-benzimidazol-2-yl]-1,3-thiazol-5-yl]-2,3-dihydro-1-benzofuran-5-carboxamide Chemical compound C=1C=C2OCCC2=CC=1C(=O)NC=1SC=NC=1C(NC1=C2)=NC1=CC=C2CN1CCOCC1 OICRXGWDCJOVOB-UHFFFAOYSA-N 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000004193 piperazinyl group Chemical group 0.000 claims 1
- 125000000587 piperidin-1-yl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C([H])([H])C1([H])[H] 0.000 claims 1
- 125000004482 piperidin-4-yl group Chemical group N1CCC(CC1)* 0.000 claims 1
- 239000003755 preservative agent Substances 0.000 claims 1
- 230000000069 prophylactic effect Effects 0.000 claims 1
- 125000004307 pyrazin-2-yl group Chemical group [H]C1=C([H])N=C(*)C([H])=N1 0.000 claims 1
- 125000003226 pyrazolyl group Chemical group 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 125000004527 pyrimidin-4-yl group Chemical group N1=CN=C(C=C1)* 0.000 claims 1
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 1
- 125000002112 pyrrolidino group Chemical group [*]N1C([H])([H])C([H])([H])C([H])([H])C1([H])[H] 0.000 claims 1
- 239000003381 stabilizer Substances 0.000 claims 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 1
- 125000000147 tetrahydroquinolinyl group Chemical group N1(CCCC2=CC=CC=C12)* 0.000 claims 1
- 230000001225 therapeutic effect Effects 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US64050904P | 2004-12-30 | 2004-12-30 | |
| GB0428549A GB0428549D0 (en) | 2004-12-30 | 2004-12-30 | Pharmaceutical compounds |
| PCT/GB2005/005089 WO2006070192A1 (en) | 2004-12-30 | 2005-12-30 | Thiazole and isothiazole derivatives that modulate the acivity of cdk, gsk and aurora kynases |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2008526721A JP2008526721A (ja) | 2008-07-24 |
| JP2008526721A5 true JP2008526721A5 (https=) | 2009-03-05 |
Family
ID=36101705
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2007548895A Withdrawn JP2008526721A (ja) | 2004-12-30 | 2005-12-30 | Ｃｄｋ、ｇｓｋ及びオーロラキナーゼの活性を調節するチアゾールおよびイソチアゾール誘導体 |
Country Status (4)
| Country | Link |
|---|---|
| US (1) | US20080312223A1 (https=) |
| EP (1) | EP1836199A1 (https=) |
| JP (1) | JP2008526721A (https=) |
| WO (1) | WO2006070192A1 (https=) |
Families Citing this family (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI372050B (en) * | 2003-07-03 | 2012-09-11 | Astex Therapeutics Ltd | (morpholin-4-ylmethyl-1h-benzimidazol-2-yl)-1h-pyrazoles |
| EP1833819A1 (en) | 2004-12-30 | 2007-09-19 | Astex Therapeutics Limited | Pyrazole compounds that modulate the activity of cdk, gsk and aurora kinases |
| US8119655B2 (en) | 2005-10-07 | 2012-02-21 | Takeda Pharmaceutical Company Limited | Kinase inhibitors |
| EP1968579A1 (en) * | 2005-12-30 | 2008-09-17 | Astex Therapeutics Limited | Pharmaceutical compounds |
| EP2049119A2 (en) * | 2006-06-29 | 2009-04-22 | Astex Therapeutics Limited | Pharmaceutical combinations of 1-cyclopropyl-3-[3-(5-morphoolin-4-ylmethyl-1h-benzoimidazol-2-yl)-1h-1-pyrazol-4-yl]-urea |
| SG158147A1 (en) | 2006-10-09 | 2010-01-29 | Takeda Pharmaceutical | Kinase inhibitors |
| EP2330894B8 (en) | 2008-09-03 | 2017-04-19 | BioMarin Pharmaceutical Inc. | Compositions including 6-aminohexanoic acid derivatives as hdac inhibitors |
| RU2535032C2 (ru) | 2008-12-22 | 2014-12-10 | Милленниум Фармасьютикалз, Инк. | Сочетание ингибиторов аврора киназы и анти-cd 20 антител |
| WO2010135411A2 (en) * | 2009-05-19 | 2010-11-25 | The Regents Of The University Of Colorado | Aurora-a copy number and sensitivity to inhibitors |
| US10059723B2 (en) | 2011-02-28 | 2018-08-28 | Biomarin Pharmaceutical Inc. | Histone deacetylase inhibitors |
| US8957066B2 (en) | 2011-02-28 | 2015-02-17 | Biomarin Pharmaceutical Inc. | Histone deacetylase inhibitors |
| US9540395B2 (en) | 2011-02-28 | 2017-01-10 | Biomarin Pharmaceutical Inc. | Histone deacetylase inhibitors |
| RU2015117950A (ru) * | 2012-10-26 | 2016-12-20 | Ф. Хоффманн-Ля Рош Аг | 3,4-дизамещенный 1н-пиразол и 4,5-дизамещенный тиазол в качестве ингибиторов тирозинкиназы syk |
| WO2014143666A1 (en) | 2013-03-15 | 2014-09-18 | Biomarin Pharmaceutical Inc. | Hdac inhibitors |
| EP3076963A4 (en) | 2013-12-06 | 2017-09-13 | Millennium Pharmaceuticals, Inc. | Combination of aurora kinase inhibitors and anti-cd30 antibodies |
| JP2018524292A (ja) | 2015-07-21 | 2018-08-30 | ミレニアム ファーマシューティカルズ， インコーポレイテッドＭｉｌｌｅｎｎｉｕｍ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ， Ｉｎｃ． | オーロラキナーゼインヒビターと化学療法剤の投与 |
| US11874276B2 (en) | 2018-04-05 | 2024-01-16 | Dana-Farber Cancer Institute, Inc. | STING levels as a biomarker for cancer immunotherapy |
| US20220305048A1 (en) | 2019-08-26 | 2022-09-29 | Dana-Farber Cancer Institute, Inc. | Use of heparin to promote type 1 interferon signaling |
| WO2026024674A1 (en) | 2024-07-22 | 2026-01-29 | Genesis Therapeutics, Inc. | Methods of treating skp2-associated cancers |
Family Cites Families (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5852011A (en) | 1994-05-31 | 1998-12-22 | Mitsui Chemicals, Inc. | Benzimidazole derivatives |
| EP0854722B1 (en) | 1995-10-06 | 2006-11-02 | University of Medicine and Dentistry of New Jersey | Proteins involved in targeting of peptidyl transfer center, and corresponding therapeutic agents and methods |
| NZ503788A (en) | 1997-10-27 | 2002-11-26 | Agouron Pharma | 4-aminothiazole derivatives and their use as inhibitors of cyclin-dependent kinases |
| DE19920936A1 (de) * | 1999-05-07 | 2000-11-09 | Basf Ag | Heterozyklisch substituierte Benzimidazole, deren Herstellung und Anwendung |
| SI1194425T1 (sl) * | 1999-06-23 | 2005-12-31 | Sanofi Aventis Deutschland | Substituirani benzimidazoli |
| US6632815B2 (en) * | 1999-09-17 | 2003-10-14 | Millennium Pharmaceuticals, Inc. | Inhibitors of factor Xa |
| US20040087798A1 (en) | 2000-03-14 | 2004-05-06 | Akira Yamada | Novel amide compounds |
| US6645990B2 (en) | 2000-08-15 | 2003-11-11 | Amgen Inc. | Thiazolyl urea compounds and methods of uses |
| EP1256578B1 (en) | 2001-05-11 | 2006-01-11 | Pfizer Products Inc. | Thiazole derivatives and their use as cdk inhibitors |
| FR2831536A1 (fr) * | 2001-10-26 | 2003-05-02 | Aventis Pharma Sa | Nouveaux derives de benzimidazoles, leur procede de preparation, leur application a titre de medicament, compositions pharmaceutiques et nouvelle utilisation notamment comme inhibiteurs de kdr |
| AU2002349477A1 (en) | 2001-11-26 | 2003-06-10 | Takeda Chemical Industries, Ltd. | Bicyclic derivative, process for producing the same, and use |
| EP1472245A2 (en) | 2002-02-06 | 2004-11-03 | Vertex Pharmaceuticals Incorporated | Heteroaryl compounds useful as inhibitors of gsk-3 |
| EP1581217A4 (en) | 2002-11-01 | 2007-07-11 | Merck & Co Inc | CARBONYLAMINO-BENZIMIDAZOLE DERIVATIVES AS MODULATORS OF ANDROGENIC RECEPTORS |
| TWI372050B (en) | 2003-07-03 | 2012-09-11 | Astex Therapeutics Ltd | (morpholin-4-ylmethyl-1h-benzimidazol-2-yl)-1h-pyrazoles |
| US7932281B2 (en) * | 2004-03-10 | 2011-04-26 | Kureha Corporation | Amine-based compound and use thereof |
| EP1833819A1 (en) * | 2004-12-30 | 2007-09-19 | Astex Therapeutics Limited | Pyrazole compounds that modulate the activity of cdk, gsk and aurora kinases |
| EP1899299B1 (en) * | 2005-06-27 | 2010-10-20 | Bristol-Myers Squibb Company | C-linked cyclic antagonists of p2y1 receptor useful in the treatment of thrombotic conditions |
-
2005
- 2005-12-30 WO PCT/GB2005/005089 patent/WO2006070192A1/en not_active Ceased
- 2005-12-30 EP EP05823660A patent/EP1836199A1/en not_active Withdrawn
- 2005-12-30 JP JP2007548895A patent/JP2008526721A/ja not_active Withdrawn
- 2005-12-30 US US11/813,173 patent/US20080312223A1/en not_active Abandoned
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