JP2006513220A5 - - Google Patents
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- JP2006513220A5 JP2006513220A5 JP2004563916A JP2004563916A JP2006513220A5 JP 2006513220 A5 JP2006513220 A5 JP 2006513220A5 JP 2004563916 A JP2004563916 A JP 2004563916A JP 2004563916 A JP2004563916 A JP 2004563916A JP 2006513220 A5 JP2006513220 A5 JP 2006513220A5
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- 150000001875 compounds Chemical class 0.000 claims 41
- 125000000217 alkyl group Chemical group 0.000 claims 32
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 30
- 239000008194 pharmaceutical composition Substances 0.000 claims 29
- 229910052739 hydrogen Inorganic materials 0.000 claims 27
- 201000010099 disease Diseases 0.000 claims 23
- 125000001475 halogen functional group Chemical group 0.000 claims 22
- 239000001257 hydrogen Substances 0.000 claims 22
- 150000002431 hydrogen Chemical class 0.000 claims 17
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 11
- 125000003342 alkenyl group Chemical group 0.000 claims 10
- 125000000304 alkynyl group Chemical group 0.000 claims 10
- 125000000753 cycloalkyl group Chemical group 0.000 claims 10
- 230000001404 mediated effect Effects 0.000 claims 8
- -1 trifluorophenoxy Chemical group 0.000 claims 8
- 238000004519 manufacturing process Methods 0.000 claims 7
- 230000006907 apoptotic process Effects 0.000 claims 6
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 6
- 238000000034 method Methods 0.000 claims 6
- 210000000056 organ Anatomy 0.000 claims 6
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 6
- 208000020084 Bone disease Diseases 0.000 claims 5
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 5
- 208000034578 Multiple myelomas Diseases 0.000 claims 5
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 5
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- 125000003118 aryl group Chemical group 0.000 claims 5
- 229910052799 carbon Inorganic materials 0.000 claims 5
- 125000004432 carbon atom Chemical group C* 0.000 claims 5
- 125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 5
- 208000024827 Alzheimer disease Diseases 0.000 claims 4
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- 208000011231 Crohn disease Diseases 0.000 claims 3
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 3
- 206010018364 Glomerulonephritis Diseases 0.000 claims 3
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- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 2
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- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims 2
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- 208000015023 Graves' disease Diseases 0.000 claims 2
- 208000031886 HIV Infections Diseases 0.000 claims 2
- 208000037357 HIV infectious disease Diseases 0.000 claims 2
- 208000005176 Hepatitis C Diseases 0.000 claims 2
- 206010019773 Hepatitis G Diseases 0.000 claims 2
- 101000960954 Homo sapiens Interleukin-18 Proteins 0.000 claims 2
- 102000000589 Interleukin-1 Human genes 0.000 claims 2
- 108010002352 Interleukin-1 Proteins 0.000 claims 2
- 102100039898 Interleukin-18 Human genes 0.000 claims 2
- 208000007766 Kaposi sarcoma Diseases 0.000 claims 2
- 208000027747 Kennedy disease Diseases 0.000 claims 2
- 201000009906 Meningitis Diseases 0.000 claims 2
- 201000003793 Myelodysplastic syndrome Diseases 0.000 claims 2
- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 claims 2
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims 2
- 208000024777 Prion disease Diseases 0.000 claims 2
- 206010039710 Scleroderma Diseases 0.000 claims 2
- 206010052779 Transplant rejections Diseases 0.000 claims 2
- 201000006704 Ulcerative Colitis Diseases 0.000 claims 2
- 241000700605 Viruses Species 0.000 claims 2
- 208000006269 X-Linked Bulbo-Spinal Atrophy Diseases 0.000 claims 2
- 208000011341 adult acute respiratory distress syndrome Diseases 0.000 claims 2
- 201000000028 adult respiratory distress syndrome Diseases 0.000 claims 2
- 230000032683 aging Effects 0.000 claims 2
- 208000006673 asthma Diseases 0.000 claims 2
- 201000008937 atopic dermatitis Diseases 0.000 claims 2
- 201000005000 autoimmune gastritis Diseases 0.000 claims 2
- 210000003169 central nervous system Anatomy 0.000 claims 2
- 206010012601 diabetes mellitus Diseases 0.000 claims 2
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- 206010014599 encephalitis Diseases 0.000 claims 2
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- 208000002672 hepatitis B Diseases 0.000 claims 2
- 208000033519 human immunodeficiency virus infectious disease Diseases 0.000 claims 2
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- 206010028417 myasthenia gravis Diseases 0.000 claims 2
- 210000004165 myocardium Anatomy 0.000 claims 2
- 230000002062 proliferating effect Effects 0.000 claims 2
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 2
- 231100000241 scar Toxicity 0.000 claims 2
- 201000000596 systemic lupus erythematosus Diseases 0.000 claims 2
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 2
- 125000004360 trifluorophenyl group Chemical group 0.000 claims 2
- 201000008827 tuberculosis Diseases 0.000 claims 2
- 206010007556 Cardiac failure acute Diseases 0.000 claims 1
- 206010007558 Cardiac failure chronic Diseases 0.000 claims 1
- 102000011727 Caspases Human genes 0.000 claims 1
- 108010076667 Caspases Proteins 0.000 claims 1
- 208000001490 Dengue Diseases 0.000 claims 1
- 206010012310 Dengue fever Diseases 0.000 claims 1
- 206010014596 Encephalitis Japanese B Diseases 0.000 claims 1
- 208000012895 Gastric disease Diseases 0.000 claims 1
- 208000009329 Graft vs Host Disease Diseases 0.000 claims 1
- 241000590002 Helicobacter pylori Species 0.000 claims 1
- 206010061216 Infarction Diseases 0.000 claims 1
- 206010061218 Inflammation Diseases 0.000 claims 1
- 201000005807 Japanese encephalitis Diseases 0.000 claims 1
- 241000710842 Japanese encephalitis virus Species 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 206010061876 Obstruction Diseases 0.000 claims 1
- 208000017442 Retinal disease Diseases 0.000 claims 1
- 208000007107 Stomach Ulcer Diseases 0.000 claims 1
- 206010043781 Thyroiditis chronic Diseases 0.000 claims 1
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims 1
- 206010046851 Uveitis Diseases 0.000 claims 1
- 208000003152 Yellow Fever Diseases 0.000 claims 1
- 239000002671 adjuvant Substances 0.000 claims 1
- 230000000919 anti-host Effects 0.000 claims 1
- 239000010836 blood and blood product Substances 0.000 claims 1
- 229940125691 blood product Drugs 0.000 claims 1
- 208000029028 brain injury Diseases 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 210000004720 cerebrum Anatomy 0.000 claims 1
- 230000008878 coupling Effects 0.000 claims 1
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- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 201000005917 gastric ulcer Diseases 0.000 claims 1
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- 229940037467 helicobacter pylori Drugs 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 238000009169 immunotherapy Methods 0.000 claims 1
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- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
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- 230000000926 neurological effect Effects 0.000 claims 1
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- 125000003107 substituted aryl group Chemical group 0.000 claims 1
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- 208000035408 type 1 diabetes mellitus 1 Diseases 0.000 claims 1
- 239000003981 vehicle Substances 0.000 claims 1
- 0 *CC(C(CC(*)=O)NC(C(*)N(C=Cc1cc(*)c(*)cc11)C1=O)=O)=O Chemical compound *CC(C(CC(*)=O)NC(C(*)N(C=Cc1cc(*)c(*)cc11)C1=O)=O)=O 0.000 description 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US43513302P | 2002-12-20 | 2002-12-20 | |
| PCT/US2003/040870 WO2004058718A1 (en) | 2002-12-20 | 2003-12-22 | 4-oxo-3-(1-oxo-1h-isoquinolin-2-ylacetylamino)-pentanoic acid ester and amide derivatives and their use as caspase inhibitors |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2006343613A Division JP2007070368A (ja) | 2002-12-20 | 2006-12-20 | ４−オキソ−３−（１−オキソ−１ｈ−イソキノリン−２−イルアセチルアミノ）−ペンタン酸のエステル誘導体およびアミド誘導体、ならびにカスパーゼインヒビターとしてのそれらの使用 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2006513220A JP2006513220A (ja) | 2006-04-20 |
| JP2006513220A5 true JP2006513220A5 (https=) | 2007-02-15 |
| JP4675628B2 JP4675628B2 (ja) | 2011-04-27 |
Family
ID=32682166
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2004563916A Expired - Fee Related JP4675628B2 (ja) | 2002-12-20 | 2003-12-22 | ４−オキソ−３−（１−オキソ−１ｈ−イソキノリン−２−イルアセチルアミノ）−ペンタン酸のエステル誘導体およびアミド誘導体、ならびにカスパーゼインヒビターとしてのそれらの使用 |
| JP2006343613A Pending JP2007070368A (ja) | 2002-12-20 | 2006-12-20 | ４−オキソ−３−（１−オキソ−１ｈ−イソキノリン−２−イルアセチルアミノ）−ペンタン酸のエステル誘導体およびアミド誘導体、ならびにカスパーゼインヒビターとしてのそれらの使用 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2006343613A Pending JP2007070368A (ja) | 2002-12-20 | 2006-12-20 | ４−オキソ−３−（１−オキソ−１ｈ−イソキノリン−２−イルアセチルアミノ）−ペンタン酸のエステル誘導体およびアミド誘導体、ならびにカスパーゼインヒビターとしてのそれらの使用 |
Country Status (8)
| Country | Link |
|---|---|
| US (2) | US7612091B2 (https=) |
| EP (1) | EP1581501A1 (https=) |
| JP (2) | JP4675628B2 (https=) |
| CN (1) | CN100366612C (https=) |
| AU (1) | AU2003303345A1 (https=) |
| CA (1) | CA2511235A1 (https=) |
| TW (1) | TW200500343A (https=) |
| WO (1) | WO2004058718A1 (https=) |
Families Citing this family (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PE20011350A1 (es) | 2000-05-19 | 2002-01-15 | Vertex Pharma | PROFARMACO DE UN INHIBIDOR DE ENZIMA CONVERTIDORA DE INTERLEUCINA-1ß (ICE) |
| PL374598A1 (en) | 2002-06-28 | 2005-10-31 | Vertex Pharmaceuticals Incorporated | Caspase inhibitors and uses thereof |
| US7612091B2 (en) | 2002-12-20 | 2009-11-03 | Vertex Pharmaceuticals Incorporated | Caspase inhibitors and uses thereof |
| PE20050159A1 (es) * | 2003-05-27 | 2005-04-19 | Vertex Pharma | Derivados de acido 3-[2-(3-amino-2-oxo-2h-piridin-1-il)-acetilamino]-4-oxo-pentanoico como inhibidores de caspasa |
| EP2399916B1 (en) * | 2004-03-12 | 2014-12-10 | Vertex Pharmaceuticals Incorporated | Process and intermediates for the preparation of aspartic acetal caspase ihnhibitors |
| WO2005115362A1 (en) * | 2004-05-15 | 2005-12-08 | Vertex Pharmaceuticals Incorporated | Treating seizures using ice inhibitors |
| CA2567080A1 (en) | 2004-05-27 | 2005-12-15 | Vertex Pharmaceuticals Incorporated | Ice inhibitors for the treatment of autoinflammatory diseases |
| EP1791535B1 (en) * | 2004-09-17 | 2008-07-30 | BioMAS Ltd. | Novel tellurium compounds and their use as immunomodulators |
| ATE543803T1 (de) * | 2004-11-24 | 2012-02-15 | Vertex Pharma | 3-ä2-(3-azylamino-2-oxo-2h-pyridin-1- yl)acetylaminoü-4-oxopentansäurederivate und deren verwendung als caspase-inhibitoren |
| FR2923160B1 (fr) | 2007-11-02 | 2013-07-26 | Pasteur Institut | Composes destines a prevenir ou traiter une infection virale. |
| WO2012061786A1 (en) | 2010-11-05 | 2012-05-10 | Brandeis University | Ice cleaved alpha-synuclein a biomarker |
| US9956260B1 (en) | 2011-07-22 | 2018-05-01 | The J. David Gladstone Institutes | Treatment of HIV-1 infection and AIDS |
| JP2017515854A (ja) | 2014-05-12 | 2017-06-15 | クオナトウス ファーマシューティカルズ，インコーポレイテッド | カスパーゼ阻害剤による慢性肝疾患の合併症の治療 |
| WO2017079566A1 (en) | 2015-11-05 | 2017-05-11 | Conatus Pharmaceuticals, Inc. | Caspase inhibitors for use in the treatment of liver cancer |
| CA3010286A1 (en) | 2015-12-31 | 2017-07-06 | Conatus Pharmaceuticals Inc. | Methods of using caspase inhibitors in treatment of liver disease |
| CN107286091B (zh) * | 2016-04-11 | 2020-06-19 | 中国海洋大学 | 一种胺基Sclerotiorin衍生物在制备抗结核药物中的应用 |
| RU2019113150A (ru) | 2016-10-05 | 2020-11-06 | Новартис Аг | Комбинация композиций, содержащих агонисты fxr, предназначенная для лечения или предупреждения фиброзирующего, цирротического заболевания или нарушения |
| EP3814327A1 (en) | 2018-06-29 | 2021-05-05 | Histogen, Inc. | (s)-3-(2-(4-(benzyl)-3-oxopiperazin-1-yl)acetamido)-4-oxo-5-(2,3,5,6-tetrafluorophenoxy)pentanoic acid derivatives and related compounds as caspase inhibitors for treating cardiovascular diseases |
| KR102442103B1 (ko) * | 2019-04-30 | 2022-09-08 | 주식회사 엘지화학 | 캐스파제 저해제의 프로드럭 |
| WO2022123062A1 (en) | 2020-12-11 | 2022-06-16 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Blocking caspase and/or fasl for preventing fatal outcome in covid-19 patients |
Family Cites Families (32)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6204261B1 (en) | 1995-12-20 | 2001-03-20 | Vertex Pharmaceuticals Incorporated | Inhibitors of interleukin-1β Converting enzyme inhibitors |
| DD232699A1 (de) | 1983-11-18 | 1986-02-05 | Adw Ddr | Verfahren zur herstellung von chinazolin-4-on-3-alkansaeuren und deren estern |
| FR2582514B1 (fr) | 1985-05-30 | 1988-02-19 | Rhone Poulenc Sante | Medicaments a base d'amides, nouveaux amides et leur preparation |
| US5714484A (en) | 1993-12-08 | 1998-02-03 | Prototek, Inc. | α-(1,3-dicarbonylenol ether) methyl ketones as cysteine protease inhibitors |
| US6420522B1 (en) | 1995-06-05 | 2002-07-16 | Vertex Pharmaceuticals Incorporated | Inhibitors of interleukin-1β converting enzyme |
| US5716929A (en) | 1994-06-17 | 1998-02-10 | Vertex Pharmaceuticals, Inc. | Inhibitors of interleukin-1β converting enzyme |
| US5756466A (en) | 1994-06-17 | 1998-05-26 | Vertex Pharmaceuticals, Inc. | Inhibitors of interleukin-1β converting enzyme |
| US5847135A (en) | 1994-06-17 | 1998-12-08 | Vertex Pharmaceuticals, Incorporated | Inhibitors of interleukin-1β converting enzyme |
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| EP0761680A3 (en) | 1995-09-12 | 1999-05-06 | Ono Pharmaceutical Co., Ltd. | Tetrazole compounds having Interleukin-1beta converting enzyme inhibitory activity |
| CA2268086A1 (en) | 1996-10-11 | 1998-04-23 | Warner-Lambert Company | Sulfonamide interleukin-1.beta. converting enzyme inhibitors |
| AU738341B2 (en) | 1996-10-11 | 2001-09-13 | Abbott Gmbh & Co. Kg | Asparate ester inhibitors of interleukin-1beta converting enzyme |
| US6063794A (en) | 1996-10-11 | 2000-05-16 | Cor Therapeutics Inc. | Selective factor Xa inhibitors |
| WO1998018781A2 (en) | 1996-10-28 | 1998-05-07 | Versicor, Inc. | Fused 2,4-pyrimidinedione combinatorial libraries, their preparation and the use of fused 2,4-pyrimidinediones derivatives as antimicrobial agents |
| US6972296B2 (en) | 1999-05-07 | 2005-12-06 | Encysive Pharmaceuticals Inc. | Carboxylic acid derivatives that inhibit the binding of integrins to their receptors |
| RU2255933C9 (ru) | 1999-05-07 | 2005-11-20 | Тексэс Байотекнолоджи Копэрейшн | ПРОИЗВОДНЫЕ ПРОПИОНОВОЙ КИСЛОТЫ (ВАРИАНТЫ), ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ И СПОСОБ СЕЛЕКТИВНОГО ИНГИБИРОВАНИЯ СВЯЗЫВАНИЯ α4β1 ИНТЕГРИНА |
| ATE383153T1 (de) | 1999-05-07 | 2008-01-15 | Encysive Pharmaceuticals Inc | Carbonsäurederivate die die bindung von integrinen an ihre rezeptoren hemmen |
| AR026748A1 (es) * | 1999-12-08 | 2003-02-26 | Vertex Pharma | Un compuesto inhibidor de caspasas, una composicion farmaceutica que lo comprende, un metodo para la sintesis del mismo y un compuesto intermediario paradicha sintesis |
| KR100322546B1 (ko) | 2000-05-08 | 2002-03-18 | 윤종용 | 독립적인 전원 전압을 사용하는 메모리와 메모리 컨트롤러간의 인터페이스 시스템 |
| WO2001094351A1 (en) * | 2000-06-07 | 2001-12-13 | Vertex Pharmaceuticals Incorporated | Caspase inhibitors and uses thereof |
| CA2418720A1 (en) * | 2000-09-13 | 2002-03-21 | Vertex Pharmaceuticals Incorporated | Caspase inhibitors and uses thereof |
| WO2002094263A2 (en) * | 2001-05-23 | 2002-11-28 | Vertex Pharmaceuticals Incorporated | Caspase inhibitors and uses thereof |
| JP2005509028A (ja) | 2001-10-09 | 2005-04-07 | バーテックス ファーマシューティカルズ インコーポレイテッド | アスパラギン酸およびグルタミン酸誘導体ならびにそのジアゾケトン中間体を合成するための方法 |
| US7410956B2 (en) | 2002-02-11 | 2008-08-12 | Vertex Pharmaceuticals Incorporated | Caspase inhibitor prodrugs |
| AU2003225088A1 (en) | 2002-04-19 | 2003-11-03 | Vertex Pharmaceuticals Incorporated | Regulation of tnf-alpha |
| PL374598A1 (en) * | 2002-06-28 | 2005-10-31 | Vertex Pharmaceuticals Incorporated | Caspase inhibitors and uses thereof |
| US7612091B2 (en) * | 2002-12-20 | 2009-11-03 | Vertex Pharmaceuticals Incorporated | Caspase inhibitors and uses thereof |
| PE20050159A1 (es) | 2003-05-27 | 2005-04-19 | Vertex Pharma | Derivados de acido 3-[2-(3-amino-2-oxo-2h-piridin-1-il)-acetilamino]-4-oxo-pentanoico como inhibidores de caspasa |
| FI117148B (fi) | 2004-07-09 | 2006-06-30 | Kone Corp | Menetelmä ja laitteisto aksiaalivuo-kestomagneettitahtikoneen kokoonpanoa varten |
| US7296449B2 (en) * | 2004-09-21 | 2007-11-20 | Ball Corporation | Dry hydraulic can shaping |
| ATE543803T1 (de) | 2004-11-24 | 2012-02-15 | Vertex Pharma | 3-ä2-(3-azylamino-2-oxo-2h-pyridin-1- yl)acetylaminoü-4-oxopentansäurederivate und deren verwendung als caspase-inhibitoren |
| JP2007040368A (ja) * | 2005-08-02 | 2007-02-15 | Ntn Corp | プーリの固定構造 |
-
2003
- 2003-12-22 US US10/743,563 patent/US7612091B2/en not_active Expired - Fee Related
- 2003-12-22 CA CA002511235A patent/CA2511235A1/en not_active Abandoned
- 2003-12-22 TW TW092136402A patent/TW200500343A/zh unknown
- 2003-12-22 CN CNB2003801092852A patent/CN100366612C/zh not_active Expired - Fee Related
- 2003-12-22 WO PCT/US2003/040870 patent/WO2004058718A1/en not_active Ceased
- 2003-12-22 JP JP2004563916A patent/JP4675628B2/ja not_active Expired - Fee Related
- 2003-12-22 EP EP03814289A patent/EP1581501A1/en not_active Withdrawn
- 2003-12-22 AU AU2003303345A patent/AU2003303345A1/en not_active Abandoned
-
2006
- 2006-12-20 JP JP2006343613A patent/JP2007070368A/ja active Pending
-
2009
- 2009-09-18 US US12/562,277 patent/US8071618B2/en not_active Expired - Fee Related
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