KR101886945B1 - 감마-세크레타제 조절제로서의 크로멘 및 1,1a,2,7b-테트라히드로시클로프로파[c]크로멘 피리도피라진디온 - Google Patents
감마-세크레타제 조절제로서의 크로멘 및 1,1a,2,7b-테트라히드로시클로프로파[c]크로멘 피리도피라진디온 Download PDFInfo
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- KR101886945B1 KR101886945B1 KR1020167030135A KR20167030135A KR101886945B1 KR 101886945 B1 KR101886945 B1 KR 101886945B1 KR 1020167030135 A KR1020167030135 A KR 1020167030135A KR 20167030135 A KR20167030135 A KR 20167030135A KR 101886945 B1 KR101886945 B1 KR 101886945B1
- Authority
- KR
- South Korea
- Prior art keywords
- alkyl
- alkoxy
- hydroxy
- halo
- cycloalkyl
- 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.)
- Expired - Fee Related
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- OUMWLQJVSPGNBK-UHFFFAOYSA-N CCOC(C1C2c3cc(C(F)(F)F)ccc3OCC12)=O Chemical compound CCOC(C1C2c3cc(C(F)(F)F)ccc3OCC12)=O OUMWLQJVSPGNBK-UHFFFAOYSA-N 0.000 description 1
- FCZFPMKLLXTSNP-UHFFFAOYSA-N CCOC(C=N)=O Chemical compound CCOC(C=N)=O FCZFPMKLLXTSNP-UHFFFAOYSA-N 0.000 description 1
- 0 C[n]1cnc(I*)c1 Chemical compound C[n]1cnc(I*)c1 0.000 description 1
- QQHZHEKUWRRTFH-UHFFFAOYSA-N FC(c(cc1)cc2c1OCC=C2)(F)F Chemical compound FC(c(cc1)cc2c1OCC=C2)(F)F QQHZHEKUWRRTFH-UHFFFAOYSA-N 0.000 description 1
- RFAXTTXXUMLASD-UHFFFAOYSA-N OCC1C2c3cc(C(F)(F)F)ccc3OCC12 Chemical compound OCC1C2c3cc(C(F)(F)F)ccc3OCC12 RFAXTTXXUMLASD-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic 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
- C07D471/02—Heterocyclic 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
- C07D471/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4375—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201461973436P | 2014-04-01 | 2014-04-01 | |
| US61/973,436 | 2014-04-01 | ||
| PCT/IB2015/051988 WO2015150957A1 (en) | 2014-04-01 | 2015-03-18 | Chromene and 1,1 a,2,7b-tetrahydrocyclopropa[c]chromene pyridopyrazinediones as gamma-secretase modulators |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| KR20160137635A KR20160137635A (ko) | 2016-11-30 |
| KR101886945B1 true KR101886945B1 (ko) | 2018-08-08 |
Family
ID=52815058
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020167030135A Expired - Fee Related KR101886945B1 (ko) | 2014-04-01 | 2015-03-18 | 감마-세크레타제 조절제로서의 크로멘 및 1,1a,2,7b-테트라히드로시클로프로파[c]크로멘 피리도피라진디온 |
Country Status (29)
| Country | Link |
|---|---|
| US (2) | US20150274721A1 (enExample) |
| EP (1) | EP3126361B1 (enExample) |
| JP (1) | JP6643247B2 (enExample) |
| KR (1) | KR101886945B1 (enExample) |
| CN (1) | CN106211770B (enExample) |
| AP (1) | AP2016009465A0 (enExample) |
| AR (1) | AR099874A1 (enExample) |
| AU (1) | AU2015242330B2 (enExample) |
| BR (1) | BR112016022519A8 (enExample) |
| CA (1) | CA2944308A1 (enExample) |
| CL (1) | CL2016002422A1 (enExample) |
| CR (1) | CR20160454A (enExample) |
| CU (1) | CU20160140A7 (enExample) |
| DK (1) | DK3126361T3 (enExample) |
| DO (1) | DOP2016000266A (enExample) |
| EA (1) | EA031419B1 (enExample) |
| EC (1) | ECSP16078289A (enExample) |
| ES (1) | ES2759277T3 (enExample) |
| IL (1) | IL248154B (enExample) |
| MD (1) | MD20160102A2 (enExample) |
| MX (1) | MX369074B (enExample) |
| NI (1) | NI201600149A (enExample) |
| PE (1) | PE20161364A1 (enExample) |
| PH (1) | PH12016501864A1 (enExample) |
| SG (1) | SG11201607465UA (enExample) |
| TW (1) | TWI568733B (enExample) |
| UY (1) | UY36054A (enExample) |
| WO (1) | WO2015150957A1 (enExample) |
| ZA (1) | ZA201606252B (enExample) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| UA110688C2 (uk) | 2012-09-21 | 2016-01-25 | Пфайзер Інк. | Біциклічні піридинони |
| MX368391B (es) * | 2015-02-03 | 2019-09-30 | Pfizer | Ciclopropabenzofuranil-piridopirazindionas novedosas. |
| CN106580997B (zh) * | 2016-12-09 | 2018-01-19 | 张田 | 一种治疗先兆流产的药物组合物 |
| EP3554502A4 (en) | 2016-12-16 | 2021-01-06 | Pipeline Therapeutics, Inc. | METHOD FOR TREATMENT OF COCHLEA SYNAPTOPATHY |
| EP3849979A1 (en) | 2018-09-12 | 2021-07-21 | Novartis AG | Antiviral pyridopyrazinedione compounds |
| CN110907542A (zh) * | 2018-09-17 | 2020-03-24 | 复旦大学 | 一种液质联用检测唾液中司来吉兰及其代谢物的方法 |
| EP3870292A4 (en) | 2018-10-26 | 2022-11-09 | The Research Foundation for The State University of New York | COMBINATION OF SEROTONIN-SPECIFIC RESUPPUT INHIBITOR AND SEROTONIN 1A RECEPTOR PARTIAL AGONIST TO REDUCE L-DOPA-INDUCED DYSKINESIA |
| CN113543852A (zh) | 2019-03-06 | 2021-10-22 | 第一三共株式会社 | 吡咯并吡唑衍生物 |
| TW202535873A (zh) | 2019-09-26 | 2025-09-16 | 瑞士商諾華公司 | 抗病毒吡唑并吡啶酮化合物 |
| JP2025535295A (ja) | 2022-10-18 | 2025-10-24 | ファイザー・インク | パタチン様ホスホリパーゼドメイン含有タンパク質3(pnpla3)修飾因子 |
| EP4604955A1 (en) | 2022-10-18 | 2025-08-27 | Pfizer Inc. | Use of patatin-like phospholipase domain-containing protein 3 compounds |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2013171712A1 (en) * | 2012-05-16 | 2013-11-21 | Janssen Pharmaceuticals, Inc. | Substituted 3, 4 - dihydro - 2h - pyrido [1, 2 -a] pyrazine - 1, 6 - dione derivatives useful for the treatment of (inter alia) alzheimer's disease |
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| US5750349A (en) | 1993-01-25 | 1998-05-12 | Takeda Chemical Industries Ltd. | Antibodies to β-amyloids or their derivatives and use thereof |
| DE19709877A1 (de) | 1997-03-11 | 1998-09-17 | Bayer Ag | 1,5-Dihydro-pyrazolo[3,4-d]-pyrimidinon-derivate |
| CA2286305A1 (en) | 1997-04-09 | 1998-10-15 | Mindset Ltd. | Recombinant antibodies specific for beta-amyloid ends, dna encoding and methods of use thereof |
| US8173127B2 (en) | 1997-04-09 | 2012-05-08 | Intellect Neurosciences, Inc. | Specific antibodies to amyloid beta peptide, pharmaceutical compositions and methods of use thereof |
| GB9722520D0 (en) | 1997-10-24 | 1997-12-24 | Pfizer Ltd | Compounds |
| US6743427B1 (en) | 1997-12-02 | 2004-06-01 | Neuralab Limited | Prevention and treatment of amyloidogenic disease |
| TWI239847B (en) | 1997-12-02 | 2005-09-21 | Elan Pharm Inc | N-terminal fragment of Abeta peptide and an adjuvant for preventing and treating amyloidogenic disease |
| DE1257584T1 (de) | 2000-02-24 | 2003-05-28 | Lilly Co Eli | Humanisierte antikörper, die amyloid beta peptid demarkieren |
| DE10045112A1 (de) | 2000-09-11 | 2002-03-21 | Merck Patent Gmbh | Verwendung von Indolderivaten zur Behandlung von Erkrankungen des zentralen Nervensystems |
| JP4708675B2 (ja) | 2000-11-03 | 2011-06-22 | プロテオテック・インコーポレーテッド | ウンカリア・トメントーサおよび関連植物からアミロイド阻害化合物を単離する方法ならびに単離した化合物の使用 |
| JP2005503789A (ja) | 2001-08-17 | 2005-02-10 | イーライ・リリー・アンド・カンパニー | 抗Aβ抗体 |
| US20030195205A1 (en) | 2001-11-02 | 2003-10-16 | Pfizer Inc. | PDE9 inhibitors for treating cardiovascular disorders |
| NZ534466A (en) * | 2002-02-28 | 2006-04-28 | Sanofi Aventis | Heteroaryl substituted 2-pyridinyl and 2-pyrimidinyl - 6,7,8,9- tetrahydropyrimido[1,2-a] pyrimidin-4-one derivatives |
| DE10238723A1 (de) | 2002-08-23 | 2004-03-11 | Bayer Ag | Phenyl-substituierte Pyrazolyprimidine |
| DE10238724A1 (de) | 2002-08-23 | 2004-03-04 | Bayer Ag | Alkyl-substituierte Pyrazolpyrimidine |
| BR0315157A (pt) | 2002-10-09 | 2005-08-09 | Rinat Neuroscience Corp | Métodos de tratar doença de alzheimer empregando-se anticorpos direcionados contra peptìdeo beta amilóide e composições deste |
| US20040220186A1 (en) | 2003-04-30 | 2004-11-04 | Pfizer Inc. | PDE9 inhibitors for treating type 2 diabetes,metabolic syndrome, and cardiovascular disease |
| JP2006527756A (ja) | 2003-06-19 | 2006-12-07 | ファイザー・プロダクツ・インク | Nk1拮抗薬 |
| CA2538220A1 (en) | 2003-09-09 | 2005-03-24 | Takeda Pharmaceutical Company Limited | Use of antibody |
| GB0327319D0 (en) | 2003-11-24 | 2003-12-24 | Pfizer Ltd | Novel pharmaceuticals |
| JP2007519707A (ja) | 2004-02-02 | 2007-07-19 | ファイザー・プロダクツ・インク | ヒスタミン−3受容体モジュレーター |
| US7456164B2 (en) | 2004-05-07 | 2008-11-25 | Pfizer, Inc | 3- or 4-monosubtituted phenol and thiophenol derivatives useful as H3 ligands |
| EP1595881A1 (en) | 2004-05-12 | 2005-11-16 | Pfizer Limited | Tetrahydronaphthyridine derivates useful as histamine H3 receptor ligands |
| SG190665A1 (en) | 2004-07-30 | 2013-06-28 | Rinat Neuroscience Corp | Antibodies directed against amyloid-beta peptide and methods using same |
| GB0423356D0 (en) | 2004-10-21 | 2004-11-24 | Merck Sharp & Dohme | Therapeutic agents |
| WO2006069081A2 (en) | 2004-12-22 | 2006-06-29 | Washington University In St. Louis | USE OF ANTI-Aβ ANTIBODY TO TREAT TRAUMATIC BRAIN INJURY |
| MY148086A (en) | 2005-04-29 | 2013-02-28 | Rinat Neuroscience Corp | Antibodies directed against amyloid-beta peptide and methods using same |
| DK1881985T3 (da) | 2005-05-12 | 2011-02-14 | Pfizer | Vandfrie krystalliske former af N-Y1-(2-ethoxyethyl)-5-(N-ethyl-N-methylamino)-7-(4-methylpyridin-2-yl-amino)-1H-pyrazolo[4,3-D]pyrimidin-3-carbonyl¨methansulfonamid |
| CA2603830A1 (en) | 2005-05-24 | 2006-11-30 | Pharmacia & Upjohn Co Llc | PYRIDINE [2,3-B] PYRAZINONES |
| WO2006126082A2 (en) | 2005-05-24 | 2006-11-30 | Pharmacia & Upjohn Company Llc | Pyridine [3,4-b] pyrazinones as pde-5 inhibitors |
| WO2006126083A1 (en) | 2005-05-24 | 2006-11-30 | Pharmacia & Upjohn Company Llc | Pyridine [3 , 4-b] pyrazinone compounds as pde-5 inhibitors |
| ES2354569T3 (es) | 2005-06-22 | 2011-03-16 | Pfizer Products Inc. | Antagonistas del receptor de histamina-3. |
| US8158673B2 (en) | 2005-10-27 | 2012-04-17 | Pfizer Inc. | Histamine-3 receptor antagonists |
| WO2007052124A1 (en) | 2005-11-04 | 2007-05-10 | Pfizer Limited | Tetrahydronaphthyridine derivative |
| WO2007063385A2 (en) | 2005-12-01 | 2007-06-07 | Pfizer Products Inc. | Spirocyclic amine histamine-3 receptor antagonists |
| WO2007069053A1 (en) | 2005-12-14 | 2007-06-21 | Pfizer Products Inc. | Benzimidazole antagonists of the h-3 receptor |
| WO2007088450A2 (en) | 2006-02-01 | 2007-08-09 | Pfizer Products Inc. | Chromane antagonist of the h-3 receptor |
| WO2007088462A1 (en) | 2006-02-01 | 2007-08-09 | Pfizer Products Inc. | Spirochromane antagonists of the h-3 receptor |
| WO2007099423A1 (en) | 2006-03-02 | 2007-09-07 | Pfizer Products Inc. | 1-pyrrolidine indane derivatives as histamine-3 receptor antagonists |
| CA2643055A1 (en) | 2006-03-13 | 2007-09-20 | Pfizer Products Inc. | Tetralines antagonists of the h-3 receptor |
| EP2013208B1 (en) | 2006-04-21 | 2011-06-22 | Pfizer Products Inc. | Pyridin[3,4-b]pyrazinones |
| WO2007138431A2 (en) | 2006-05-30 | 2007-12-06 | Pfizer Products Inc. | Azabicyclic ether histamine-3 antagonists |
| SI2124933T1 (sl) | 2007-01-22 | 2012-12-31 | Pfizer Products Inc. | Tosilatna sol terapevtske spojine in farmacevtski sestavi tega |
| WO2010047990A1 (en) * | 2008-10-23 | 2010-04-29 | Merck Sharp & Dohme Corp. | Fused heterocyclic m1 receptor positive allosteric modulators |
| ES2602794T3 (es) * | 2011-03-31 | 2017-02-22 | Pfizer Inc | Piridinonas bicíclicas novedosas |
| UA110688C2 (uk) * | 2012-09-21 | 2016-01-25 | Пфайзер Інк. | Біциклічні піридинони |
| AU2014206834B2 (en) * | 2013-01-17 | 2017-06-22 | Janssen Pharmaceutica Nv | Novel substituted pyrido-piperazinone derivatives as gamma secretase modulators |
| CA2925743C (en) * | 2013-10-04 | 2018-03-06 | Pfizer Inc. | Novel bicyclic pyridinones as gamma-secretase modulators |
-
2015
- 2015-03-18 EP EP15714951.9A patent/EP3126361B1/en active Active
- 2015-03-18 PE PE2016001895A patent/PE20161364A1/es not_active Application Discontinuation
- 2015-03-18 CN CN201580018466.7A patent/CN106211770B/zh not_active Expired - Fee Related
- 2015-03-18 BR BR112016022519A patent/BR112016022519A8/pt not_active IP Right Cessation
- 2015-03-18 CA CA2944308A patent/CA2944308A1/en not_active Withdrawn
- 2015-03-18 CR CR20160454A patent/CR20160454A/es unknown
- 2015-03-18 EA EA201600619A patent/EA031419B1/ru not_active IP Right Cessation
- 2015-03-18 DK DK15714951.9T patent/DK3126361T3/da active
- 2015-03-18 AP AP2016009465A patent/AP2016009465A0/en unknown
- 2015-03-18 SG SG11201607465UA patent/SG11201607465UA/en unknown
- 2015-03-18 MD MDA20160102A patent/MD20160102A2/ro not_active Application Discontinuation
- 2015-03-18 JP JP2016559879A patent/JP6643247B2/ja not_active Expired - Fee Related
- 2015-03-18 AU AU2015242330A patent/AU2015242330B2/en not_active Ceased
- 2015-03-18 ES ES15714951T patent/ES2759277T3/es active Active
- 2015-03-18 MX MX2016012904A patent/MX369074B/es active IP Right Grant
- 2015-03-18 KR KR1020167030135A patent/KR101886945B1/ko not_active Expired - Fee Related
- 2015-03-18 WO PCT/IB2015/051988 patent/WO2015150957A1/en not_active Ceased
- 2015-03-27 AR ARP150100922A patent/AR099874A1/es unknown
- 2015-03-27 US US14/670,746 patent/US20150274721A1/en not_active Abandoned
- 2015-03-27 UY UY0001036054A patent/UY36054A/es not_active Application Discontinuation
- 2015-03-31 TW TW104110551A patent/TWI568733B/zh not_active IP Right Cessation
-
2016
- 2016-09-09 ZA ZA2016/06252A patent/ZA201606252B/en unknown
- 2016-09-22 CU CUP2016000140A patent/CU20160140A7/es unknown
- 2016-09-22 PH PH12016501864A patent/PH12016501864A1/en unknown
- 2016-09-27 CL CL2016002422A patent/CL2016002422A1/es unknown
- 2016-09-29 IL IL248154A patent/IL248154B/en active IP Right Grant
- 2016-09-29 DO DO2016000266A patent/DOP2016000266A/es unknown
- 2016-09-29 NI NI201600149A patent/NI201600149A/es unknown
- 2016-09-30 EC ECIEPI201678289A patent/ECSP16078289A/es unknown
-
2017
- 2017-02-24 US US15/441,882 patent/US20170166566A1/en not_active Abandoned
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2013171712A1 (en) * | 2012-05-16 | 2013-11-21 | Janssen Pharmaceuticals, Inc. | Substituted 3, 4 - dihydro - 2h - pyrido [1, 2 -a] pyrazine - 1, 6 - dione derivatives useful for the treatment of (inter alia) alzheimer's disease |
Non-Patent Citations (1)
| Title |
|---|
| Journal of Medicinal Chemmistry, 57(3), 1046-1062, 2014.02.13 |
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