CN105518005B - 作为rock抑制剂的三环吡啶-甲酰胺衍生物 - Google Patents

作为rock抑制剂的三环吡啶-甲酰胺衍生物 Download PDF

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CN105518005B
CN105518005B CN201480047826.1A CN201480047826A CN105518005B CN 105518005 B CN105518005 B CN 105518005B CN 201480047826 A CN201480047826 A CN 201480047826A CN 105518005 B CN105518005 B CN 105518005B
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CN105518005A (zh
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陈丽芬
胡子伦
王彩兰
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Bristol Myers Squibb Co
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    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
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    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
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    • C07DHETEROCYCLIC COMPOUNDS
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    • C07D498/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
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CN201480047826.1A 2013-07-02 2014-07-01 作为rock抑制剂的三环吡啶-甲酰胺衍生物 Expired - Fee Related CN105518005B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201361842084P 2013-07-02 2013-07-02
US61/842,084 2013-07-02
PCT/US2014/045008 WO2015002926A1 (en) 2013-07-02 2014-07-01 Tricyclic pyrido-carboxamide derivatives as rock inhibitors

Publications (2)

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CN105518005A CN105518005A (zh) 2016-04-20
CN105518005B true CN105518005B (zh) 2018-07-20

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US (1) US9663529B2 (cg-RX-API-DMAC7.html)
EP (1) EP3016950B1 (cg-RX-API-DMAC7.html)
JP (1) JP6522602B2 (cg-RX-API-DMAC7.html)
CN (1) CN105518005B (cg-RX-API-DMAC7.html)
ES (1) ES2634628T3 (cg-RX-API-DMAC7.html)
WO (1) WO2015002926A1 (cg-RX-API-DMAC7.html)

Families Citing this family (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9708337B2 (en) 2013-02-22 2017-07-18 Bristol-Myers Squibb Company Aryl amide-based kinase inhibitors
WO2014134391A1 (en) 2013-02-28 2014-09-04 Bristol-Myers Squibb Company Phenylpyrazole derivatives as potent rock1 and rock2 inhibitors
TW201444798A (zh) 2013-02-28 2014-12-01 必治妥美雅史谷比公司 作爲強效rock1及rock2抑制劑之苯基吡唑衍生物
JP6522602B2 (ja) 2013-07-02 2019-05-29 ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company Rock阻害剤としての三環式ピリド−カルボキサミド誘導体
TW201506024A (zh) 2013-07-02 2015-02-16 必治妥美雅史谷比公司 作為有效rock抑制劑的三環甲醯胺衍生物
CN105979950A (zh) 2013-10-11 2016-09-28 百时美施贵宝公司 吡咯并三嗪激酶抑制剂
US9902702B2 (en) 2014-07-15 2018-02-27 Bristol-Myers Squibb Company Spirocycloheptanes as inhibitors of rock
EP3242873B1 (en) 2015-01-09 2020-07-22 Bristol-Myers Squibb Company Cyclic ureas as inhibitors of rock
US10112929B2 (en) 2015-03-09 2018-10-30 Bristol-Myers Squibb Company Lactams as inhibitors of rock
EP3292124B1 (en) 2015-04-10 2019-05-22 Bristol-Myers Squibb Company 6h-isochromeno[3,4-c]pyridines and benzo[c][1,7]naphthyridin-6-(5h)-ones as adaptor associated kinase 1 (aak1) inhibitors
TWI730032B (zh) 2016-01-13 2021-06-11 美商必治妥美雅史谷比公司 作為rock抑制劑之螺庚烷水楊酸醯胺及相關化合物
JP6987792B2 (ja) 2016-05-27 2022-01-05 ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company Rock阻害剤としてのトリアゾロンおよびテトラゾロン
JP6903731B2 (ja) 2016-07-07 2021-07-14 ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company 強力で選択的なrock阻害剤としてのラクタム、環状尿素、およびカルバメート、およびトリアゾロン誘導体
KR102449652B1 (ko) 2016-07-07 2022-09-29 브리스톨-마이어스 스큅 컴퍼니 Rock의 억제제로서의 스피로-융합 시클릭 우레아
JP7113810B2 (ja) 2016-07-07 2022-08-05 ブリストル-マイヤーズ スクイブ カンパニー Rock阻害剤としてのスピロラクタム
JP7191826B2 (ja) * 2016-11-30 2022-12-19 ブリストル-マイヤーズ スクイブ カンパニー 三環式rhoキナーゼ阻害剤
TW201908293A (zh) 2017-07-12 2019-03-01 美商必治妥美雅史谷比公司 作為rock抑制劑之5員及雙環雜環醯胺
JP7313331B2 (ja) 2017-07-12 2023-07-24 ブリストル-マイヤーズ スクイブ カンパニー Rock阻害剤としてのスピロヘプタニルヒダントイン
US12060341B2 (en) 2017-07-12 2024-08-13 Bristol-Myers Squibb Company Spiroheptanyl hydantoins as ROCK inhibitors
ES2951212T3 (es) 2017-07-12 2023-10-18 Bristol Myers Squibb Co Fenilacetamidas como inhibidores de ROCK
EP3652165B1 (en) 2017-07-12 2021-08-25 Bristol-Myers Squibb Company Five membered-aminoheterocyclic and 5,6-or 6,6-membered bicyclic aminoheterocyclic inhibitors of rock for the treatment of heart failure
WO2019089868A1 (en) 2017-11-03 2019-05-09 Bristol-Myers Squibb Company Diazaspiro rock inhibitors
AU2019387370A1 (en) 2018-11-30 2021-06-10 Nuvation Bio Inc. Pyrrole and pyrazole compounds and methods of use thereof
CN113354630B (zh) * 2021-06-30 2022-11-01 江南大学 一种5,6-二氢苯并[h]喹唑啉类化合物及其应用
EP4431596A1 (en) 2021-11-11 2024-09-18 The Doshisha Cryopreservation preparation for corneal endothelial cells and method for producing said cryopreservation preparation

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2001068648A1 (en) * 2000-03-15 2001-09-20 Aventis Pharma Deutschland Gmbh Substituted beta-carbolines with ikb-kinase inhibiting activity

Family Cites Families (101)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
HU168776B (cg-RX-API-DMAC7.html) 1973-11-09 1976-07-28
HU168036B (cg-RX-API-DMAC7.html) 1973-11-09 1976-02-28
US3962448A (en) * 1974-03-11 1976-06-08 Smithkline Corporation 8-Alkyl and alkenyl-10-hydroxy-5H[1]benzopyranopyridine derivatives having polyphagic activity
CA1098910A (en) 1978-06-15 1981-04-07 Robert N. Schut 3-amino-2-(5-fluoro and 5-methoxy-1h-indol-3-yl) propanoic acid derivatives
JPS57116067A (en) 1981-01-12 1982-07-19 Sankyo Kagaku Kk Novel 8-quinolinesulfonyl derivative, its synthesis and use
DE3703435A1 (de) 1987-02-05 1988-08-18 Thomae Gmbh Dr K Neue thiazole, diese verbindungen enthaltende arzneimittel und verfahren zu ihrer herstellung
IE68593B1 (en) 1989-12-06 1996-06-26 Sanofi Sa Heterocyclic substituted acylaminothiazoles their preparation and pharmaceutical compositions containing them
WO1996037493A1 (de) 1995-05-26 1996-11-28 Bayer Aktiengesellschaft Pyridyl-thiazole und deren verwendung zum schutz von pflanzen gegen befall durch mikroorganismen
WO1998028282A2 (en) 1996-12-23 1998-07-02 Du Pont Pharmaceuticals Company OXYGEN OR SULFUR CONTAINING 5-MEMBERED HETEROAROMATICS AS FACTOR Xa INHIBITORS
US6187797B1 (en) 1996-12-23 2001-02-13 Dupont Pharmaceuticals Company Phenyl-isoxazoles as factor XA Inhibitors
JPH11193281A (ja) 1997-10-27 1999-07-21 Takeda Chem Ind Ltd アデノシンa3受容体拮抗剤およびチアゾール化合物
WO1999052906A1 (de) 1998-04-08 1999-10-21 Bayer Aktiengesellschaft Substituierte oxazolyl- und thiazolyl-uracil herbizide
US7026334B1 (en) 1999-07-26 2006-04-11 Shionogi & Co., Ltd. Thiazolidine compounds and pharmaceutical compositions exhibiting thrombopoietin receptor agonism
YU65502A (sh) * 2000-03-15 2005-11-28 Aventis Pharma Deutschland Gmbh. Supstituisani beta-karbolini sa ikb-kinaza inhibirajućim dejstvom
GB0010183D0 (en) 2000-04-26 2000-06-14 Ferring Bv Inhibitors of dipeptidyl peptidase IV
WO2002014291A1 (fr) 2000-08-11 2002-02-21 Nippon Chemiphar Co.,Ltd. ACTIVATEURS DE PPAR$G(d)
JP2002053566A (ja) 2000-08-11 2002-02-19 Japan Tobacco Inc チアゾール化合物及びその医薬用途
US20020173507A1 (en) 2000-08-15 2002-11-21 Vincent Santora Urea compounds and methods of uses
US20020103192A1 (en) 2000-10-26 2002-08-01 Curtin Michael L. Inhibitors of histone deacetylase
EP1354603A1 (en) 2000-12-26 2003-10-22 Takeda Chemical Industries, Ltd. Concomitant drugs
JPWO2002062775A1 (ja) 2001-02-02 2004-06-10 山之内製薬株式会社 2−アシルアミノチアゾール誘導体又はその塩
MY130778A (en) 2001-02-09 2007-07-31 Vertex Pharma Heterocyclic inhibitiors of erk2 and uses thereof
US20020177594A1 (en) 2001-03-14 2002-11-28 Curtin Michael L. Inhibitors of histone deacetylase
JP4157381B2 (ja) 2001-03-23 2008-10-01 日本ケミファ株式会社 ペルオキシソーム増殖剤応答性受容体の活性化剤
US20050009843A1 (en) 2001-04-26 2005-01-13 Kiyoshi Nakayama Medicine for inhibiting drug elimination pump
US20050080113A1 (en) 2001-06-11 2005-04-14 Shigenori Ohkawa Medicinal compositions
GB0123589D0 (en) 2001-10-01 2001-11-21 Syngenta Participations Ag Organic compounds
EP1452530A4 (en) 2001-12-03 2005-11-30 Japan Tobacco Inc AZOL CONNECTION AND THEIR MEDICAL USE
ES2610611T3 (es) 2002-01-18 2017-04-28 Astellas Pharma Inc. Derivado de 2-acilaminotiazol o sal del mismo
WO2003062215A1 (en) 2002-01-25 2003-07-31 Kylix Pharmaceuticals B.V. 4(hetero-) aryl substituted (thia-/oxa-/pyra) zoles for inhibition of tie-2
CA2484233A1 (en) 2002-05-13 2003-11-27 Eli Lilly And Company Multicyclic compounds for use as melanin concentrating hormone antagonists in the treatment of obesity and diabetes
JP2006508042A (ja) 2002-07-18 2006-03-09 ブリストル−マイヤーズ スクイブ カンパニー グルココルチコイド受容体の修飾物質および方法
TW200812986A (en) 2002-08-09 2008-03-16 Nps Pharma Inc New compounds
AU2003265395A1 (en) 2002-08-14 2004-03-03 Ppd Discovery, Inc. Prenylation inhibitors and methods of their synthesis and use
US20040122016A1 (en) 2002-10-30 2004-06-24 Jingrong Cao Compositions useful as inhibitors of rock and other protein kinases
GB0230087D0 (en) 2002-12-24 2003-01-29 Astrazeneca Ab Therapeutic agents
GB0302672D0 (en) 2003-02-06 2003-03-12 Astrazeneca Ab Pharmaceutical formulations
WO2004071509A1 (ja) 2003-02-12 2004-08-26 Nippon Chemiphar Co., Ltd. オリゴデンドロサイト分化促進剤
SI1611088T1 (sl) 2003-04-07 2009-12-31 Pharmacyclics Inc Hidroksamati kot terapevtska sredstva
US7696198B2 (en) 2003-04-16 2010-04-13 Memory Pharmaceuticals Corporation Phosphodiesterase 4 inhibitors
CN100545161C (zh) 2003-08-15 2009-09-30 中国科学院上海药物研究所 一类杂环衍生物、制备方法及其用途
US7351727B2 (en) 2003-09-02 2008-04-01 Bristol-Myers Squibb Company Inhibitors of 15-lipoxygenase
EP1664006A2 (en) 2003-09-06 2006-06-07 Vertex Pharmaceuticals Incorporated Modulators of atp-binding cassette transporters
AR045651A1 (es) 2003-09-19 2005-11-02 Solvay Pharm Bv Derivados de tiazol como moduladores del receptor de cannabinoide
WO2005041879A2 (en) 2003-10-28 2005-05-12 Pharmacia Corporation COMBINATIONS COMPRISING AN Hsp90 INHIBITOR AND A PHOPHODIESTERASE INHIBITOR FOR TREATING OR PREVENTING NEOPLASIA
WO2005044194A2 (en) 2003-10-28 2005-05-19 Pharmacia Corporation TREATMENT OR PREVENTION OF NEOPLASIA BY USE OF AN Hsp90 INHIBITOR
US20080275062A1 (en) 2004-01-30 2008-11-06 David Harold Drewry Chemical Compounds
US8759335B2 (en) 2004-01-30 2014-06-24 Vertex Pharmaceuticals Incorporated Modulators of ATP-binding cassette transporters
WO2005077345A1 (en) 2004-02-03 2005-08-25 Astrazeneca Ab Compounds for the treatment of gastro-esophageal reflux disease
WO2005077373A2 (en) 2004-02-03 2005-08-25 Astrazeneca Ab Treatment of gastro-esophageal reflux disease (gerd)
MY148488A (en) 2004-02-18 2013-04-30 Astrazeneca Ab Additional heteropolycyclic compounds and their use as metabotropic glutamate receptor antagonists
AU2005212073B2 (en) 2004-02-18 2010-07-08 Kyorin Pharmaceutical Co., Ltd. Bicyclic amide derivatives
US7259155B2 (en) 2004-05-05 2007-08-21 Otsuka Pharmaceutical Factory, Inc. Phosphonic diester derivatives
JP3928086B2 (ja) 2005-03-29 2007-06-13 塩野義製薬株式会社 3−プロペニルセフェム誘導体
FR2885129B1 (fr) 2005-04-29 2007-06-15 Proskelia Sas Nouveaux derives de l'ureee substituee parun thiazole ou benzothiazole, leur procede de preparation, leur application a titre de medicaments, les compositions pharmaceutiques les renfermant et utilisation.
EA200702445A1 (ru) 2005-05-09 2008-04-28 Ачиллион Фармасьютикалз, Инк. Соединения тиазола и способы их применения
US7655446B2 (en) 2005-06-28 2010-02-02 Vertex Pharmaceuticals Incorporated Crystal structure of Rho-kinase I kinase domain complexes and binding pockets thereof
US20100168102A9 (en) * 2005-07-11 2010-07-01 Devgen Nv Amide Derivatives as Kinase Inhibitors
EP1962892A4 (en) 2005-11-22 2011-10-12 Univ South Florida INHIBITION OF CELL PROLIFERATION
WO2007075896A2 (en) 2005-12-22 2007-07-05 Kemia, Inc. Heterocyclic cytokine inhibitors
JP2009524677A (ja) 2006-01-25 2009-07-02 シンタ ファーマシューティカルズ コーポレーション 炎症および免疫関連使用用のチアゾールおよびチアジアゾール化合物
WO2007116106A1 (es) 2006-04-12 2007-10-18 Palobiofarma, S.L. Nuevos compuestos como antagonistas de los receptores a1 de adenosina
EP2032562B1 (en) 2006-05-12 2010-08-25 Vertex Pharmaceuticals Incorporated Selective inhibitors of rock protein kinase and uses thereof
US7935715B2 (en) 2006-07-28 2011-05-03 Boehringer Ingelheim International Gmbh Compounds which modulate the CB2 receptor
JP5030114B2 (ja) 2006-09-25 2012-09-19 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング Cb2受容体をモジュレートする化合物
TW200831081A (en) 2006-12-25 2008-08-01 Kyorin Seiyaku Kk Glucokinase activator
WO2008124000A2 (en) 2007-04-02 2008-10-16 Ligand Pharmaceuticals Incorporated Thiazole derivatives as androgen receptor modulator compounds
GB0706793D0 (en) 2007-04-05 2007-05-16 Evotec Ag Compounds
EP2170309B1 (en) 2007-06-22 2016-10-26 Hydra Biosciences, Inc. 2,6-dioxo,-2,3-dihydro-1h-purine compounds useful for treating disorders related to the activity of the trpa1 channel
US8445686B2 (en) 2007-08-27 2013-05-21 Abbvie Inc. 4-(4-pyridinyl)-benzamides and their use as rock activity modulators
TW200916447A (en) 2007-08-29 2009-04-16 Methylgene Inc Sirtuin inhibitors
ES2331220B1 (es) 2007-10-02 2010-09-23 Palobiofarma, S.L. Nuevos compuestos como antagonistas de los receptores a1 de adenosina.
AU2008319735A1 (en) 2007-10-31 2009-05-07 Nissan Chemical Industries, Ltd. Pyridazinone derivatives and use thereof as P2X7 receptor inhibitors
JP5492092B2 (ja) 2007-11-07 2014-05-14 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング Cb2受容体を調節する化合物
WO2009067607A2 (en) 2007-11-20 2009-05-28 Memory Pharmaceuticals Corporation Combinations of pde4 inhibitors and antipsychotics for the treatment of psychotic disorders
WO2009081222A1 (en) 2007-12-21 2009-07-02 Glenmark Pharmaceuticals, S.A. Substituted tricyclic pyridine or pyrimidine vanilloid receptor ligands
CA2709784A1 (en) 2007-12-21 2009-07-09 University Of Rochester Method for altering the lifespan of eukaryotic organisms
US20100316584A1 (en) 2008-02-08 2010-12-16 Shiseido Company Ltd. Whitening Agent And Skin External Preparation
US20110105436A1 (en) 2008-03-10 2011-05-05 Auckland Uniservices Limited Heteroaryl compounds, compositions, and methods of use in cancer treatment
WO2009140519A1 (en) 2008-05-14 2009-11-19 Hydra Biosciences, Inc. Compounds and compositions for treating chemical warfare agent-induced injuries
WO2010028193A1 (en) 2008-09-03 2010-03-11 Repligen Corporation Compounds including pimelic acid derivatives as hdac inhibitors
US20100063085A1 (en) * 2008-09-11 2010-03-11 University Court Of The University Of Dundee Method of treating learning impairment in down's syndrome subjects
WO2010029300A1 (en) 2008-09-12 2010-03-18 Biolipox Ab Bis aromatic compounds for use in the treatment of inflammation
WO2010036821A1 (en) 2008-09-24 2010-04-01 Hydra Biosciences, Inc. Methods and compositions for treating respiratory disorders
RU2518462C2 (ru) 2008-12-19 2014-06-10 Новартис Аг Органические соединения
EP2370407B1 (en) * 2008-12-19 2014-06-18 Bristol-Myers Squibb Company Carbazole and carboline kinase inhibitors
WO2010075376A2 (en) 2008-12-23 2010-07-01 Abbott Laboratories Anti-viral compounds
JP2012051804A (ja) * 2008-12-26 2012-03-15 Kyoto Univ Eg5阻害剤
UA103918C2 (en) 2009-03-02 2013-12-10 Айерем Элелси N-(hetero)aryl, 2-(hetero)aryl-substituted acetamides for use as wnt signaling modulators
US8362249B2 (en) 2009-04-27 2013-01-29 Boehringer Ingelheim International Gmbh CXCR3 receptor antagonists
EP2440054A4 (en) 2009-06-09 2012-12-12 California Capital Equity Llc PYRIDILTRIA INHIBITOR OF HEDGEHOG SIGNALING
ES2577024T3 (es) 2009-08-25 2016-07-12 Abraxis Bioscience, Llc Terapia combinada con composiciones de nanopartículas de taxano e inhibidores de Hedgehog
AU2010322287B2 (en) 2009-11-17 2014-04-03 The Regents Of The University Of Michigan 1,4-benzodiazepine-2,5-diones and related compounds with therapeutic properties
JP2013515000A (ja) 2009-12-18 2013-05-02 アクティベサイト ファーマシューティカルズ インコーポレイティッド 血漿カリクレインの阻害薬のプロドラッグ
WO2011129095A1 (ja) 2010-04-12 2011-10-20 塩野義製薬株式会社 インテグラーゼ阻害活性を有するピリドン誘導体
US9221808B2 (en) 2010-04-16 2015-12-29 H. Lee Moffitt Cancer Center And Research Institute, Inc. Pyridylthiazole-based ureas as inhibitors of Rho associated protein kinase (ROCK) and methods of use
WO2011159857A1 (en) 2010-06-16 2011-12-22 Bristol-Myers Squibb Company Carboline carboxamide compounds useful as kinase inhibitors
JP5769326B2 (ja) * 2010-10-19 2015-08-26 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング Rhoキナーゼ阻害薬
US8703953B2 (en) 2012-03-09 2014-04-22 Bristol-Myers Squibb Company Aryl ether-base kinase inhibitors
JP6522602B2 (ja) 2013-07-02 2019-05-29 ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company Rock阻害剤としての三環式ピリド−カルボキサミド誘導体
TW201506024A (zh) 2013-07-02 2015-02-16 必治妥美雅史谷比公司 作為有效rock抑制劑的三環甲醯胺衍生物

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2001068648A1 (en) * 2000-03-15 2001-09-20 Aventis Pharma Deutschland Gmbh Substituted beta-carbolines with ikb-kinase inhibiting activity

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
Rho/Rho-kinase and C-reactive protein relationship in hypertension and atherosclerosis;Lorenzo A. Calo`;《Nephrol Dial Transplant》;20061231;第21卷;1131-1132 *

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