BR0314126A - Ligandos de amida acìclica e sulfonamida para o receptor de estrogênio - Google Patents
Ligandos de amida acìclica e sulfonamida para o receptor de estrogênioInfo
- Publication number
- BR0314126A BR0314126A BR0314126-8A BR0314126A BR0314126A BR 0314126 A BR0314126 A BR 0314126A BR 0314126 A BR0314126 A BR 0314126A BR 0314126 A BR0314126 A BR 0314126A
- Authority
- BR
- Brazil
- Prior art keywords
- pharmaceutically acceptable
- formula
- prodrug
- acceptable salt
- estrogen
- Prior art date
Links
- 102000015694 estrogen receptors Human genes 0.000 title abstract 5
- 108010038795 estrogen receptors Proteins 0.000 title abstract 5
- -1 Acyclic Amide Chemical class 0.000 title abstract 2
- 239000003446 ligand Substances 0.000 title abstract 2
- 229940124530 sulfonamide Drugs 0.000 title abstract 2
- FDDDEECHVMSUSB-UHFFFAOYSA-N sulfanilamide Chemical compound NC1=CC=C(S(N)(=O)=O)C=C1 FDDDEECHVMSUSB-UHFFFAOYSA-N 0.000 title 1
- 239000000651 prodrug Substances 0.000 abstract 6
- 229940002612 prodrug Drugs 0.000 abstract 6
- 150000003839 salts Chemical class 0.000 abstract 6
- 150000001875 compounds Chemical class 0.000 abstract 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 4
- 239000008194 pharmaceutical composition Substances 0.000 abstract 3
- 102000018997 Growth Hormone Human genes 0.000 abstract 2
- 108010051696 Growth Hormone Proteins 0.000 abstract 2
- 201000010099 disease Diseases 0.000 abstract 2
- 208000035475 disorder Diseases 0.000 abstract 2
- 229940011871 estrogen Drugs 0.000 abstract 2
- 239000000262 estrogen Substances 0.000 abstract 2
- 239000000122 growth hormone Substances 0.000 abstract 2
- 230000001404 mediated effect Effects 0.000 abstract 2
- 238000000034 method Methods 0.000 abstract 2
- PUZPDOWCWNUUKD-UHFFFAOYSA-M sodium fluoride Chemical compound [F-].[Na+] PUZPDOWCWNUUKD-UHFFFAOYSA-M 0.000 abstract 2
- 208000024891 symptom Diseases 0.000 abstract 2
- 241000124008 Mammalia Species 0.000 abstract 1
- 102000003982 Parathyroid hormone Human genes 0.000 abstract 1
- 108090000445 Parathyroid hormone Proteins 0.000 abstract 1
- 239000003263 anabolic agent Substances 0.000 abstract 1
- 229940124325 anabolic agent Drugs 0.000 abstract 1
- 210000000988 bone and bone Anatomy 0.000 abstract 1
- 239000000199 parathyroid hormone Substances 0.000 abstract 1
- 229960001319 parathyroid hormone Drugs 0.000 abstract 1
- 230000002265 prevention Effects 0.000 abstract 1
- 239000002089 prostaglandin antagonist Substances 0.000 abstract 1
- 239000002522 prostaglandin receptor stimulating agent Substances 0.000 abstract 1
- 235000013024 sodium fluoride Nutrition 0.000 abstract 1
- 239000011775 sodium fluoride Substances 0.000 abstract 1
Classifications
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- C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
- C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
- C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
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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
- C07D213/24—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 substituted hydrocarbon radicals attached to ring carbon atoms
- C07D213/36—Radicals substituted by singly-bound nitrogen atoms
- C07D213/40—Acylated substituent nitrogen atom
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- C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
- C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms 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
- C07D215/20—Oxygen atoms
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- C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms 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
- C07D215/36—Sulfur atoms
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- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
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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
- C07D233/56—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 only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
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- C07D261/00—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
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- C07D261/06—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members
- C07D261/10—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two 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, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
-
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- C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
- C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
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- C07D295/084—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
- C07D295/088—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
-
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- C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
- C07D295/12—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms
- C07D295/135—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
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- C07—ORGANIC CHEMISTRY
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- C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
- C07D295/16—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
- C07D295/18—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms by radicals derived from carboxylic acids, or sulfur or nitrogen analogues thereof
- C07D295/182—Radicals derived from carboxylic acids
- C07D295/185—Radicals derived from carboxylic acids from aliphatic carboxylic acids
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
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- C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
- C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
- C07D307/04—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
- C07D307/10—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms
- C07D307/12—Radicals substituted by oxygen atoms
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
- C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
- C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
- C07D333/26—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur 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
- C07D333/30—Hetero atoms other than halogen
- C07D333/34—Sulfur atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C2601/00—Systems containing only non-condensed rings
- C07C2601/02—Systems containing only non-condensed rings with a three-membered ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C2601/00—Systems containing only non-condensed rings
- C07C2601/06—Systems containing only non-condensed rings with a five-membered ring
- C07C2601/08—Systems containing only non-condensed rings with a five-membered ring the ring being saturated
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C2601/00—Systems containing only non-condensed rings
- C07C2601/12—Systems containing only non-condensed rings with a six-membered ring
- C07C2601/14—The ring being saturated
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| US7265145B2 (en) * | 2003-05-28 | 2007-09-04 | Bristol-Myers Squibb Company | Substituted piperidines and pyrrolidines as calcium sensing receptor modulators and method |
| US7318925B2 (en) | 2003-08-08 | 2008-01-15 | Amgen Fremont, Inc. | Methods of use for antibodies against parathyroid hormone |
| JP2007521232A (ja) | 2003-08-08 | 2007-08-02 | アブジェニックス・インコーポレーテッド | 副甲状腺ホルモン(pth)に対する抗体およびその使用 |
| WO2005087710A1 (ja) | 2004-03-15 | 2005-09-22 | Takeda Pharmaceutical Company Limited | アミノフェニルプロパン酸誘導体 |
| US7504431B2 (en) * | 2004-04-16 | 2009-03-17 | Bristol-Myers Squibb Company | Sulfonyl amide inhibitors of calcium channel function |
| US20090082322A1 (en) * | 2004-10-09 | 2009-03-26 | The Regents Of The University Of Michigan | Gender Differences in Experimental Aortic Aneurysm Formation |
| WO2007055374A1 (ja) * | 2005-11-14 | 2007-05-18 | Mitsubishi Tanabe Pharma Corporation | 骨粗鬆症治療剤 |
| US9409856B2 (en) | 2005-11-28 | 2016-08-09 | Gtx, Inc. | Estrogen receptor ligands and methods of use thereof |
| US8546451B2 (en) | 2005-11-28 | 2013-10-01 | Gtx, Inc. | Estrogen receptor ligands and methods of use thereof |
| US8158828B2 (en) | 2005-11-28 | 2012-04-17 | Gtx, Inc. | Nuclear receptor binding agents |
| US8637706B2 (en) | 2005-11-28 | 2014-01-28 | Gtx, Inc. | Nuclear receptor binding agents |
| DE102006013957A1 (de) * | 2006-03-27 | 2007-10-04 | Bayer Healthcare Aktiengesellschaft | Substituierte N-Benzyl-N-phenylbenzolsulfonamide |
| US9623021B2 (en) | 2007-01-22 | 2017-04-18 | Gtx, Inc. | Nuclear receptor binding agents |
| US9604931B2 (en) | 2007-01-22 | 2017-03-28 | Gtx, Inc. | Nuclear receptor binding agents |
| EA026578B1 (ru) | 2007-01-22 | 2017-04-28 | ДЖиТиЭкс, ИНК. | Вещества, связывающие ядерные рецепторы |
| GB0711463D0 (en) * | 2007-06-14 | 2007-07-25 | Opal Drug Discovery Ltd | Trimethylsilylbeneylsulphamates as treatments for diseases of bone loss |
| US20090163586A1 (en) | 2007-12-20 | 2009-06-25 | Astrazeneca Ab | Bis-(Sulfonylamino) Derivatives in Therapy 205 |
| US9624161B2 (en) | 2009-02-23 | 2017-04-18 | Gtx, Inc. | Estrogen receptor ligands and methods of use thereof |
| US9427418B2 (en) | 2009-02-23 | 2016-08-30 | Gtx, Inc. | Estrogen receptor ligands and methods of use thereof |
| US8791100B2 (en) | 2010-02-02 | 2014-07-29 | Novartis Ag | Aryl benzylamine compounds |
| WO2012061698A2 (en) | 2010-11-05 | 2012-05-10 | Senomyx, Inc. | Compounds useful as modulators of trpm8 |
| CN113101292B (zh) | 2014-05-08 | 2023-07-11 | 上海市生物医药技术研究院 | 双炔失碳酯组合物和疾病治疗方法 |
| AU2016323992B2 (en) * | 2015-09-16 | 2021-05-06 | Eli Lilly And Company | Farnesoid X receptor agonists and uses thereof |
| BR112018006471B1 (pt) | 2015-10-01 | 2024-02-27 | Senomyx, Inc | Composto, composição, método de modular o membro de melastina do canal potencial do receptor transitório 8 (trpm8), método de modular a sensação de resfrescância de uma composição e método de induzir uma sensação de refrescância em um ser humano ou animal |
| CA3055990A1 (en) | 2017-03-15 | 2018-09-20 | Metacrine, Inc. | Farnesoid x receptor agonists and uses thereof |
| LT3609888T (lt) | 2017-03-15 | 2025-11-10 | Farnezoidinio x receptoriaus agonistai ir jų panaudojimas | |
| CN113056271B (zh) | 2018-09-18 | 2024-10-29 | 奥加诺沃公司 | 法尼醇x受体激动剂及其用途 |
| CN109651297B (zh) * | 2019-01-22 | 2022-05-27 | 杭州壹瑞医药科技有限公司 | 一种n-苄基-n-芳基磺酰胺类衍生物及制备和应用 |
| TWI872230B (zh) | 2020-03-18 | 2025-02-11 | 美商奧加諾沃公司 | 法尼醇x受體促效劑之調配物 |
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| US156281A (en) * | 1874-10-27 | Improvement in wheels for vehicles | ||
| DE1122076B (de) * | 1955-07-08 | 1962-01-18 | Geigy Ag J R | Verfahren zur Herstellung von neuen, therapeutisch wertvollen, insbesondere antiphlogistisch wirksamen N-acylierten Hydroxybenzylaminophenolen |
| GB811130A (en) * | 1955-07-08 | 1959-04-02 | Geigy Ag J R | Improvements in and relating to n-acylated benzylamino phenols |
| GB1576841A (en) * | 1977-01-22 | 1980-10-15 | Beecham Group Ltd | Substituted n-acyl phenylamine compounds having hypolipidaemic activity |
| US4243804A (en) * | 1978-06-19 | 1981-01-06 | E. R. Squibb & Sons, Inc. | Heterocyclic containing amines |
| GB2124615B (en) * | 1979-07-19 | 1984-07-18 | Shell Int Research | Heterocyclic compounds having fungicidal herbicidal and plant-growth regulating properties |
| JPH04145067A (ja) * | 1990-10-04 | 1992-05-19 | Hokko Chem Ind Co Ltd | ヘテロ酢酸アミド誘導体および農園芸用殺菌剤 |
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| EP0585500A1 (en) * | 1992-09-04 | 1994-03-09 | Merrell Dow Pharmaceuticals Inc. | Diaryl piperazineacetamides as antimuscarinic agents |
| TW257757B (enExample) * | 1993-03-03 | 1995-09-21 | Boehringer Mannheim Gmbh | |
| DE19615262A1 (de) * | 1996-04-18 | 1997-10-23 | Bayer Ag | Heteroverknüpfte Phenylglycinolamide |
| US5958934A (en) * | 1996-05-23 | 1999-09-28 | Syntex (U.S.A.) Inc. | Aryl pyrimidine derivatives and uses thereof |
| TW523506B (en) | 1996-12-18 | 2003-03-11 | Ono Pharmaceutical Co | Sulfonamide or carbamide derivatives and drugs containing the same as active ingredients |
| AU7467398A (en) * | 1997-04-25 | 1998-11-24 | Eli Lilly And Company | Indene compounds having activity as serms |
| JP2000072734A (ja) * | 1998-06-15 | 2000-03-07 | Nippon Nohyaku Co Ltd | アニリン誘導体 |
| US6780883B2 (en) * | 1998-11-05 | 2004-08-24 | Warner-Lambert Company | Amide inhibitors of microsomal triglyceride transfer protein |
| ES2230070T3 (es) * | 1999-02-24 | 2005-05-01 | F. Hoffmann-La Roche Ag | Derivados de 3-fenilpiridina y su empleo como antagonistas receptores de nk-1. |
| DE60014216T2 (de) | 1999-02-24 | 2006-03-02 | F. Hoffmann-La Roche Ag | 4-Phenylpyridinderivate und deren Verwendung als NK-1 Rezeptorantagonisten |
| PL350427A1 (en) | 1999-02-24 | 2002-12-16 | Hoffmann La Roche | Phenyl− and pyridinyl derivatives as neurokinin 1 antagonists |
| AU3859400A (en) * | 1999-03-04 | 2000-09-21 | American Home Products Corporation | N-substituted benzoyl indoles as estrogenic agents |
| US6511980B2 (en) * | 2000-05-05 | 2003-01-28 | Ortho Mcneil Pharmaceutical, Inc. | Substituted diamine derivatives useful as motilin antagonists |
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| JP2006508061A (ja) | 2006-03-09 |
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