JP2010505794A5 - - Google Patents
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- Publication number
- JP2010505794A5 JP2010505794A5 JP2009530875A JP2009530875A JP2010505794A5 JP 2010505794 A5 JP2010505794 A5 JP 2010505794A5 JP 2009530875 A JP2009530875 A JP 2009530875A JP 2009530875 A JP2009530875 A JP 2009530875A JP 2010505794 A5 JP2010505794 A5 JP 2010505794A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- amino
- cycloalkyl
- indazol
- alkoxy
- 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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- 125000003453 indazolyl group Chemical group N1N=C(C2=C1C=CC=C2)* 0.000 claims 11
- 125000000217 alkyl group Chemical group 0.000 claims 10
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims 10
- 125000000753 cycloalkyl group Chemical group 0.000 claims 10
- 150000003839 salts Chemical class 0.000 claims 9
- 125000003342 alkenyl group Chemical group 0.000 claims 8
- 125000004183 alkoxy alkyl group Chemical group 0.000 claims 8
- 125000000278 alkyl amino alkyl group Chemical group 0.000 claims 8
- 125000003282 alkyl amino group Chemical group 0.000 claims 8
- 125000004103 aminoalkyl group Chemical group 0.000 claims 8
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 8
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 7
- 125000003545 alkoxy group Chemical group 0.000 claims 6
- 125000004093 cyano group Chemical group *C#N 0.000 claims 6
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 6
- 125000004438 haloalkoxy group Chemical group 0.000 claims 6
- 125000001188 haloalkyl group Chemical group 0.000 claims 6
- 125000001475 halogen functional group Chemical group 0.000 claims 6
- 229910052739 hydrogen Inorganic materials 0.000 claims 6
- 239000001257 hydrogen Substances 0.000 claims 6
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 6
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 6
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 6
- 239000003814 drug Substances 0.000 claims 5
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 4
- -1 2-indazolyl Chemical class 0.000 claims 3
- 206010010904 Convulsion Diseases 0.000 claims 3
- 102000004257 Potassium Channel Human genes 0.000 claims 3
- 125000003806 alkyl carbonyl amino group Chemical group 0.000 claims 3
- 201000010099 disease Diseases 0.000 claims 3
- 208000035475 disorder Diseases 0.000 claims 3
- 230000000694 effects Effects 0.000 claims 3
- 108020001213 potassium channel Proteins 0.000 claims 3
- 241000124008 Mammalia Species 0.000 claims 2
- 125000005119 alkyl cycloalkyl group Chemical group 0.000 claims 2
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 claims 2
- BZRGWNYKWFAOMR-UHFFFAOYSA-N n-(4-chlorophenyl)-2-indazol-2-yl-6-methylpyrimidin-4-amine Chemical compound N=1C(N2N=C3C=CC=CC3=C2)=NC(C)=CC=1NC1=CC=C(Cl)C=C1 BZRGWNYKWFAOMR-UHFFFAOYSA-N 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 125000001424 substituent group Chemical group 0.000 claims 2
- 229910052717 sulfur Inorganic materials 0.000 claims 2
- CZAADHJQSOAANV-UHFFFAOYSA-N 2-[4-(4-chloroanilino)pyrimidin-2-yl]indazol-6-amine Chemical compound N1=C2C=C(N)C=CC2=CN1C(N=1)=NC=CC=1NC1=CC=C(Cl)C=C1 CZAADHJQSOAANV-UHFFFAOYSA-N 0.000 claims 1
- RFUMIUICOZSINX-UHFFFAOYSA-N 4-n-(4-chlorophenyl)-2-indazol-2-ylpyrimidine-4,5-diamine Chemical compound NC1=CN=C(N2N=C3C=CC=CC3=C2)N=C1NC1=CC=C(Cl)C=C1 RFUMIUICOZSINX-UHFFFAOYSA-N 0.000 claims 1
- NMDNQKSQYHTRKR-UHFFFAOYSA-N 6-(3-chloroindazol-1-yl)-n-(4-chlorophenyl)pyridin-2-amine Chemical compound C12=CC=CC=C2C(Cl)=NN1C(N=1)=CC=CC=1NC1=CC=C(Cl)C=C1 NMDNQKSQYHTRKR-UHFFFAOYSA-N 0.000 claims 1
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 claims 1
- 201000004384 Alopecia Diseases 0.000 claims 1
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 206010002383 Angina Pectoris Diseases 0.000 claims 1
- 208000019901 Anxiety disease Diseases 0.000 claims 1
- 206010003225 Arteriospasm coronary Diseases 0.000 claims 1
- 206010003591 Ataxia Diseases 0.000 claims 1
- 206010003805 Autism Diseases 0.000 claims 1
- 208000020706 Autistic disease Diseases 0.000 claims 1
- 208000020925 Bipolar disease Diseases 0.000 claims 1
- 206010048994 Bladder spasm Diseases 0.000 claims 1
- 201000006474 Brain Ischemia Diseases 0.000 claims 1
- 206010008120 Cerebral ischaemia Diseases 0.000 claims 1
- 208000003890 Coronary Vasospasm Diseases 0.000 claims 1
- 206010012289 Dementia Diseases 0.000 claims 1
- 206010012735 Diarrhoea Diseases 0.000 claims 1
- 208000005171 Dysmenorrhea Diseases 0.000 claims 1
- 206010013935 Dysmenorrhoea Diseases 0.000 claims 1
- 208000010228 Erectile Dysfunction Diseases 0.000 claims 1
- 206010060378 Hyperinsulinaemia Diseases 0.000 claims 1
- 206010020772 Hypertension Diseases 0.000 claims 1
- 206010062016 Immunosuppression Diseases 0.000 claims 1
- 206010022562 Intermittent claudication Diseases 0.000 claims 1
- 206010026749 Mania Diseases 0.000 claims 1
- 208000019022 Mood disease Diseases 0.000 claims 1
- 208000008238 Muscle Spasticity Diseases 0.000 claims 1
- 206010068871 Myotonic dystrophy Diseases 0.000 claims 1
- 150000001204 N-oxides Chemical class 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 208000002193 Pain Diseases 0.000 claims 1
- 208000018737 Parkinson disease Diseases 0.000 claims 1
- 208000006399 Premature Obstetric Labor Diseases 0.000 claims 1
- 206010036600 Premature labour Diseases 0.000 claims 1
- 208000028017 Psychotic disease Diseases 0.000 claims 1
- 208000003782 Raynaud disease Diseases 0.000 claims 1
- 208000012322 Raynaud phenomenon Diseases 0.000 claims 1
- 208000021386 Sjogren Syndrome Diseases 0.000 claims 1
- 208000030886 Traumatic Brain injury Diseases 0.000 claims 1
- 206010046543 Urinary incontinence Diseases 0.000 claims 1
- 206010047163 Vasospasm Diseases 0.000 claims 1
- 208000028311 absence seizure Diseases 0.000 claims 1
- 231100000360 alopecia Toxicity 0.000 claims 1
- 230000036506 anxiety Effects 0.000 claims 1
- 206010003119 arrhythmia Diseases 0.000 claims 1
- 230000006793 arrhythmia Effects 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 206010008118 cerebral infarction Diseases 0.000 claims 1
- 230000036461 convulsion Effects 0.000 claims 1
- 208000029078 coronary artery disease Diseases 0.000 claims 1
- 201000011634 coronary artery vasospasm Diseases 0.000 claims 1
- 230000006735 deficit Effects 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 206010013781 dry mouth Diseases 0.000 claims 1
- 206010015037 epilepsy Diseases 0.000 claims 1
- 230000007160 gastrointestinal dysfunction Effects 0.000 claims 1
- 230000003451 hyperinsulinaemic effect Effects 0.000 claims 1
- 201000008980 hyperinsulinism Diseases 0.000 claims 1
- 230000001506 immunosuppresive effect Effects 0.000 claims 1
- 201000001881 impotence Diseases 0.000 claims 1
- 208000021156 intermittent vascular claudication Diseases 0.000 claims 1
- 208000002551 irritable bowel syndrome Diseases 0.000 claims 1
- 208000028867 ischemia Diseases 0.000 claims 1
- 208000017169 kidney disease Diseases 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 208000031225 myocardial ischemia Diseases 0.000 claims 1
- GOOFDKIMFIZGRV-UHFFFAOYSA-N n-(4-chlorophenyl)-2-(5-nitroindazol-2-yl)pyrimidin-4-amine Chemical compound C1=C2C=C([N+](=O)[O-])C=CC2=NN1C(N=1)=NC=CC=1NC1=CC=C(Cl)C=C1 GOOFDKIMFIZGRV-UHFFFAOYSA-N 0.000 claims 1
- BUKLUWFZTMICFQ-UHFFFAOYSA-N n-(4-chlorophenyl)-2-(6-nitroindazol-2-yl)pyrimidin-4-amine Chemical compound N1=C2C=C([N+](=O)[O-])C=CC2=CN1C(N=1)=NC=CC=1NC1=CC=C(Cl)C=C1 BUKLUWFZTMICFQ-UHFFFAOYSA-N 0.000 claims 1
- JJDDIEUKPRBQNR-UHFFFAOYSA-N n-(4-chlorophenyl)-2-indazol-1-yl-6-methylpyrimidin-4-amine Chemical compound N=1C(N2C3=CC=CC=C3C=N2)=NC(C)=CC=1NC1=CC=C(Cl)C=C1 JJDDIEUKPRBQNR-UHFFFAOYSA-N 0.000 claims 1
- PGCZVHJXSVRWTL-UHFFFAOYSA-N n-(4-chlorophenyl)-6-indazol-1-ylpyrazin-2-amine Chemical compound C1=CC(Cl)=CC=C1NC1=CN=CC(N2C3=CC=CC=C3C=N2)=N1 PGCZVHJXSVRWTL-UHFFFAOYSA-N 0.000 claims 1
- SGDLUZVNNSOSBZ-UHFFFAOYSA-N n-(4-chlorophenyl)-6-indazol-1-ylpyridin-2-amine Chemical compound C1=CC(Cl)=CC=C1NC1=CC=CC(N2C3=CC=CC=C3C=N2)=N1 SGDLUZVNNSOSBZ-UHFFFAOYSA-N 0.000 claims 1
- XVQDXTZYCOTRLI-UHFFFAOYSA-N n-(4-chlorophenyl)-6-indazol-2-ylpyrazin-2-amine Chemical compound C1=CC(Cl)=CC=C1NC1=CN=CC(N2N=C3C=CC=CC3=C2)=N1 XVQDXTZYCOTRLI-UHFFFAOYSA-N 0.000 claims 1
- SXTZVSCCGYEFOY-UHFFFAOYSA-N n-[(4-chlorophenyl)methyl]-2-indazol-1-ylpyrimidin-4-amine Chemical compound C1=CC(Cl)=CC=C1CNC1=CC=NC(N2C3=CC=CC=C3C=N2)=N1 SXTZVSCCGYEFOY-UHFFFAOYSA-N 0.000 claims 1
- TXGZRDGSNSTOIW-UHFFFAOYSA-N n-[(4-chlorophenyl)methyl]-2-indazol-2-ylpyrimidin-4-amine Chemical compound C1=CC(Cl)=CC=C1CNC1=CC=NC(N2N=C3C=CC=CC3=C2)=N1 TXGZRDGSNSTOIW-UHFFFAOYSA-N 0.000 claims 1
- KRNGNUGXFMBNJY-UHFFFAOYSA-N n-[2-[4-(4-chloroanilino)pyrimidin-2-yl]indazol-6-yl]acetamide Chemical compound N1=C2C=C(NC(=O)C)C=CC2=CN1C(N=1)=NC=CC=1NC1=CC=C(Cl)C=C1 KRNGNUGXFMBNJY-UHFFFAOYSA-N 0.000 claims 1
- BYGNIUVYBFGPQY-UHFFFAOYSA-N n-cyclohexyl-2-indazol-1-yl-6-methylpyrimidin-4-amine Chemical compound N=1C(N2C3=CC=CC=C3C=N2)=NC(C)=CC=1NC1CCCCC1 BYGNIUVYBFGPQY-UHFFFAOYSA-N 0.000 claims 1
- QIWUMMHCYOXAED-UHFFFAOYSA-N n-cyclohexyl-2-indazol-1-ylpyrimidin-4-amine Chemical compound C1CCCCC1NC1=CC=NC(N2C3=CC=CC=C3C=N2)=N1 QIWUMMHCYOXAED-UHFFFAOYSA-N 0.000 claims 1
- JUIOOVGJSHADDZ-UHFFFAOYSA-N n-cyclohexyl-2-indazol-1-ylquinazolin-4-amine Chemical compound C1CCCCC1NC1=NC(N2C3=CC=CC=C3C=N2)=NC2=CC=CC=C12 JUIOOVGJSHADDZ-UHFFFAOYSA-N 0.000 claims 1
- 201000003631 narcolepsy Diseases 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 208000030761 polycystic kidney disease Diseases 0.000 claims 1
- 208000026440 premature labor Diseases 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 239000000651 prodrug Substances 0.000 claims 1
- 229940002612 prodrug Drugs 0.000 claims 1
- 208000023504 respiratory system disease Diseases 0.000 claims 1
- 201000000980 schizophrenia Diseases 0.000 claims 1
- 201000009881 secretory diarrhea Diseases 0.000 claims 1
- 208000018198 spasticity Diseases 0.000 claims 1
- 230000009529 traumatic brain injury Effects 0.000 claims 1
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US82794006P | 2006-10-03 | 2006-10-03 | |
| DKPA200601280 | 2006-10-03 | ||
| PCT/EP2007/060493 WO2008040753A1 (en) | 2006-10-03 | 2007-10-03 | Indazolyl derivatives useful as potassium channel modulating agents |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2010505794A JP2010505794A (ja) | 2010-02-25 |
| JP2010505794A5 true JP2010505794A5 (enExample) | 2010-11-11 |
Family
ID=38959688
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2009530875A Abandoned JP2010505794A (ja) | 2006-10-03 | 2007-10-03 | カリウムチャネル調節剤として有用なインダゾリル誘導体 |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US8222262B2 (enExample) |
| EP (1) | EP2074113A1 (enExample) |
| JP (1) | JP2010505794A (enExample) |
| AU (1) | AU2007304195A1 (enExample) |
| CA (1) | CA2665398A1 (enExample) |
| MX (1) | MX2009003142A (enExample) |
| WO (1) | WO2008040753A1 (enExample) |
Families Citing this family (28)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| LT4193B (en) | 1994-04-01 | 1997-07-25 | Microcide Pharmaceuticals Inc | Cephalosporin antibiotics |
| EP2066655A2 (en) * | 2006-09-07 | 2009-06-10 | Neurosearch A/S | Pyridinyl-pyrimidine derivatives useful as potassium channel modulating agents |
| WO2008092942A2 (en) * | 2007-02-02 | 2008-08-07 | Neurosearch A/S | Pyridinyl-pyrazole derivatives and their use as potassium channel modulators |
| EP2142545A1 (en) | 2007-03-28 | 2010-01-13 | NeuroSearch A/S | Purinyl derivatives and their use as potassium channel modulators |
| WO2009037247A1 (en) | 2007-09-17 | 2009-03-26 | Neurosearch A/S | Pyrazine derivatives and their use as potassium channel modulators |
| RU2011105810A (ru) | 2008-07-17 | 2012-08-27 | Асахи Касеи Фарма Корпорейшн (Jp) | Азотсодержащие бициклические гетероциклические соединения |
| EP2331527A1 (en) * | 2008-09-02 | 2011-06-15 | NeuroSearch A/S | Pyrazolyl-pyrimidine derivatives and their use as potassium channel modulators |
| US8268838B2 (en) | 2008-09-26 | 2012-09-18 | Neurosearch A/S | Substituted purinyl-pyrazole derivatives and their use as potassium channel modulators |
| EP2344501A1 (en) * | 2008-09-26 | 2011-07-20 | NeuroSearch A/S | Substituted purinyl-pyrazol derivatives and their use as potassium channel modulators |
| AU2009322836B2 (en) * | 2008-11-25 | 2013-04-04 | Merck Sharp & Dohme Corp. | Soluble guanylate cyclase activators |
| EP2549875B1 (en) | 2010-03-25 | 2015-05-13 | Merck Sharp & Dohme Corp. | Soluble guanylate cyclase activators |
| KR20140019004A (ko) | 2010-05-27 | 2014-02-13 | 머크 샤프 앤드 돔 코포레이션 | 가용성 구아닐레이트 시클라제 활성화제 |
| US8895583B2 (en) | 2010-10-28 | 2014-11-25 | Merck Sharp & Dohme Corp. | Soluble guanylate cyclase activators |
| JP6223443B2 (ja) | 2012-06-26 | 2017-11-01 | サニオナ・エイピイエス | フェニルトリアゾール誘導体及びｇａｂａａ受容体複合体を調節するための該フェニルトリアゾール誘導体の使用 |
| KR20220143164A (ko) * | 2012-11-21 | 2022-10-24 | 피티씨 테라퓨틱스, 인크. | 치환된 리버스 피리미딘 ｂｍｉ-1 저해제 |
| JP2016504365A (ja) * | 2012-12-28 | 2016-02-12 | アメリカ合衆国 | Ｕｓｐ１／ｕａｆ１デユビキチナーゼ複合体阻害剤及びその使用 |
| CA2922657C (en) | 2013-08-30 | 2022-04-12 | Ptc Therapeutics, Inc. | Substituted pyrimidine bmi-1 inhibitors |
| US10584115B2 (en) | 2013-11-21 | 2020-03-10 | Ptc Therapeutics, Inc. | Substituted pyridine and pyrazine BMI-1 inhibitors |
| TW201605832A (zh) * | 2013-12-10 | 2016-02-16 | 克立弗生物科學公司 | 作為ｐ９７錯合物之抑制劑之單環嘧啶／吡啶化合物 |
| NZ722624A (en) | 2014-01-20 | 2017-09-29 | Cleave Biosciences Inc | Fused pyrimidines as inhibitors of p97 complex |
| WO2017133664A1 (en) * | 2016-02-05 | 2017-08-10 | Savira Pharmaceuticals Gmbh | Bicyclic pyridine and pyrimidine derivatives and their use in the treatment， amelioration or prevention of influenza |
| WO2017148995A1 (en) | 2016-03-04 | 2017-09-08 | Bayer Pharma Aktiengesellschaft | 1-(pyrimidin-2-yl)-1h-indazoles having bub1 kinase inhibiting activity |
| US10774064B2 (en) | 2016-06-02 | 2020-09-15 | Cadent Therapeutics, Inc. | Potassium channel modulators |
| JP6997197B2 (ja) | 2017-01-23 | 2022-01-17 | カデント セラピューティクス，インコーポレーテッド | カリウムチャネルモジュレーター |
| US11174248B2 (en) | 2017-10-11 | 2021-11-16 | Merck Sharp & Dohme Corp. | Indazolyl-spiro[2.3]hexane-carbonitrile derivatives as LRRK2 inhibitors, pharmaceutical compositions, and uses thereof |
| EP3694330B1 (en) * | 2017-10-11 | 2023-04-19 | Merck Sharp & Dohme LLC | Indazolyl-spiro[2.2]pentane-carbonitrile derivatives as lrrk2 inhibitors, pharmaceutical compositions, and uses thereof |
| BR112021002630A2 (pt) | 2018-08-17 | 2021-05-11 | Ptc Therapeutics, Inc. | método para tratar câncer pancreático |
| MX2021004647A (es) | 2018-10-22 | 2021-08-16 | Novartis Ag | Formas cristalinas de moduladores de los canales de potasio. |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2002074753A2 (de) * | 2001-03-15 | 2002-09-26 | Basf Aktiengesellschaft | 5-phenylpyrimidine, verfahren und zwischenprodukte zu ihrer herstellung und ihre verwendung zur bekaempfung von schadpilzen |
| CL2004000409A1 (es) | 2003-03-03 | 2005-01-07 | Vertex Pharma | Compuestos derivados de 2-(cilo sustituido)-1-(amino u oxi sustituido)-quinazolina, inhibidores de canales ionicos de sodio y calcio dependientes de voltaje; composicion farmaceutica; y uso del compuesto en el tratamiento de dolor agudo, cronico, neu |
| JP4808628B2 (ja) * | 2003-12-03 | 2011-11-02 | ワイエム・バイオサイエンシズ・オーストラリア・ピーティーワイ・リミテッド | アゾール系キナーゼ阻害剤 |
| JP4966958B2 (ja) | 2005-03-14 | 2012-07-04 | ノイロサーチ アクティーゼルスカブ | カリウムチャネル調節剤及び医療における使用 |
| EP1863796A1 (en) | 2005-03-22 | 2007-12-12 | NeuroSearch A/S | Pyrazolyl-pyrimidines as potassium channel modulating agents and their medical use |
| JP2009511548A (ja) * | 2005-10-14 | 2009-03-19 | ノイロサーチ アクティーゼルスカブ | 新規ピリミジン−２，４−ジアミン誘導体及び小コンダクタンスのカルシウム依存性カリウムチャネルのモジュレーターとしてのこれらの使用 |
| WO2007071632A2 (en) | 2005-12-20 | 2007-06-28 | Neurosearch A/S | 2-pyridin-2-yl-quinazoline derivatives as potassium channel modulating agents for the treatment of respiratory diseases |
-
2007
- 2007-10-03 MX MX2009003142A patent/MX2009003142A/es active IP Right Grant
- 2007-10-03 EP EP07820871A patent/EP2074113A1/en not_active Withdrawn
- 2007-10-03 AU AU2007304195A patent/AU2007304195A1/en not_active Abandoned
- 2007-10-03 WO PCT/EP2007/060493 patent/WO2008040753A1/en not_active Ceased
- 2007-10-03 CA CA002665398A patent/CA2665398A1/en not_active Abandoned
- 2007-10-03 US US12/444,344 patent/US8222262B2/en active Active
- 2007-10-03 JP JP2009530875A patent/JP2010505794A/ja not_active Abandoned
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