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AR078776A1 - Derivados de (1,1,1,3,3,3-hexafluoro-2-hidroxipropan-2-il)-fenilo - Google Patents

Derivados de (1,1,1,3,3,3-hexafluoro-2-hidroxipropan-2-il)-fenilo

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Publication number
AR078776A1
AR078776A1 ARP100103925A ARP100103925A AR078776A1 AR 078776 A1 AR078776 A1 AR 078776A1 AR P100103925 A ARP100103925 A AR P100103925A AR P100103925 A ARP100103925 A AR P100103925A AR 078776 A1 AR078776 A1 AR 078776A1
Authority
AR
Argentina
Prior art keywords
alkyl
ring
phenyl
present
optionally substituted
Prior art date
Application number
ARP100103925A
Other languages
English (en)
Inventor
Emma Louise Carswell
David Jonathan Bennett
Andrew John Cooke
Original Assignee
Organon Nv
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Organon Nv filed Critical Organon Nv
Publication of AR078776A1 publication Critical patent/AR078776A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/08—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D211/18—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D211/26—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by nitrogen atoms
    • C07D211/28—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by nitrogen atoms to which a second hetero atom is attached
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • 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
    • C07D213/60—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 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
    • C07D213/72—Nitrogen atoms
    • C07D213/75—Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
    • C07D237/02—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings
    • C07D237/06—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D237/10—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three 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
    • C07D237/20—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three 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, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/42—One nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D261/00—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
    • C07D261/02—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
    • 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
    • C07D261/12—Oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C07D295/08—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
    • C07D295/096—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 separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C07D295/192—Radicals derived from carboxylic acids from aromatic carboxylic acids

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Diabetes (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyrrole Compounds (AREA)
  • Hydrogenated Pyridines (AREA)

Abstract

Composiciones farmacéuticas que los comprenden y al uso de estos derivados de (1,1,1,3,3,3-hexafluoro-2-hidroxipropan-2-il)fenilo en el tratamiento de la ateroesclerosis. Reivindicacion 1: Un derivado de (1,1,1,3,3,3-hexafluoro-2-hidroxipropan-2-il)fenilo que tiene la formula general (1), caracterizado porque: n es 0 o 1; X es NR4, O o un enlace; Y es O, CHR5, C(OR6)R5, CO, S, SO, SO2, NR5, CONR5 o un enlace, y el enlace de puntos representa un enlace simple; o Y es CR5, y el enlace de puntos representa un enlace doble; Y tiene un patron de substitucion meta o para en el anillo fenilo con relacion a la posicion fenilo-NH; Z es CH2 o CO; el substituyente hexafluoroisopropanol tiene un patron de substitucion orto, meta o para en el anillo fenilo con relacion a la posicion fenilo-Z; R1 es alquilo C1-8, cicloalquilo C3-8 o cicloalquilo C3-8-alquilo C1-4, cada uno de los grupos alquilo es substituido opcionalmente por 1 o 2 substituyentes seleccionados entre hidroxi, hidroximetilo, alquiloxi C1-3, ciano, halogeno, CF3, NR7R8, NR7R8CO y R9OCO; o R1 es un anillo aromático de 5 o 6 miembros, que comprende opcionalmente 1 a 3 heteroátomos seleccionados entre O, S y N, el anillo es substituido opcionalmente por alquilo C1-3, cicloalquilo C3-6, alquiloxi C1-3, alquilsulfonilo C1-3, ciano, CF3, OCF3, halogeno o R9OCO, y el anillo es ligado opcionalmente a X a través de un grupo alquileno C1-3 que es opcionalmente substituido por hidroxi; o R1 es un anillo heterocíclico de 4, 5 o 6 miembros saturado o insaturado, que comprende 1 o 2 heteroátomos seleccionados entre NR10, O, S, SO y SO2, el anillo es substituido opcionalmente por alquilo C1-3, hidroxi, oxo, NR11R12 o R9OCO, y el anillo es ligado opcionalmente a X a través de un grupo alquileno C1-3 que es substituido opcionalmente por hidroxi; o cuando X es NR4, R1 junto con R4 y el N al cual están unidos pueden formar un anillo de 4 a 8 miembros, que puede ser substituido opcionalmente con hidroxilo o hidroximetilo; R2 es H o 1 a 3 halogenos; o cuando Y es NR5, R2 y R5 junto con los 2 átomos de carbono adyacentes a los cuales están unidos pueden formar un anillo heteroaromático de 5 miembros fusionado, que comprende opcionalmente 1 o 2 átomos de N adicionales; R3 es H o alquilo C1-3; R4, cuando está presente, es H o alquilo C1-3; R5, cuando está presente, es H o alquilo C1-3; R6, cuando está presente, es H o alquilo C1-3; R7 y R8, cuando están presentes, son independientemente H o alquilo C1-3; R9, cuando está presente, es H o alquilo C1-3; R10, cuando está presente, es H o alquilo C1-3; R11 y R12, cuando están presentes, son independientemente H o alquilo C1-3; o una sal farmacéuticamente aceptable del mismo.
ARP100103925A 2009-10-27 2010-10-26 Derivados de (1,1,1,3,3,3-hexafluoro-2-hidroxipropan-2-il)-fenilo AR078776A1 (es)

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EP09174106 2009-10-27

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AR078776A1 true AR078776A1 (es) 2011-11-30

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ARP100103925A AR078776A1 (es) 2009-10-27 2010-10-26 Derivados de (1,1,1,3,3,3-hexafluoro-2-hidroxipropan-2-il)-fenilo

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Country Link
US (1) US9108939B2 (es)
EP (1) EP2493855B1 (es)
JP (1) JP5699156B2 (es)
AR (1) AR078776A1 (es)
AU (1) AU2010311534B2 (es)
CA (1) CA2777671C (es)
TW (1) TWI513695B (es)
WO (1) WO2011051282A1 (es)

Families Citing this family (13)

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Publication number Priority date Publication date Assignee Title
TW201006816A (en) 2008-05-15 2010-02-16 Organon Nv Hexafluoroisopropanol derivatives
US9309221B2 (en) * 2012-04-10 2016-04-12 Sumitomo Dainippon Pharma Co., Ltd. 1-substituted indazole derivative
JP6115214B2 (ja) * 2012-05-22 2017-04-19 株式会社リコー パターン処理装置、パターン処理方法、パターン処理プログラム
JP6088476B2 (ja) * 2013-10-08 2017-03-01 大日本住友製薬株式会社 新規１位置換インダゾール誘導体からなる医薬
WO2015106164A1 (en) 2014-01-10 2015-07-16 Rgenix, Inc. Lxr agonists and uses thereof
MA39822A (fr) 2014-04-03 2018-02-06 Janssen Pharmaceutica Nv Dérivés de pyrimidine bicycle
JP7025022B2 (ja) 2016-01-11 2022-02-24 ザ ロックフェラー ユニバーシティー 骨髄系由来抑制細胞関連障害の治療のための方法
WO2018068296A1 (en) 2016-10-14 2018-04-19 Merck Sharp & Dohme Corp. PIPERIDINE DERIVATIVES AS LIVER X RECEPTOR β AGONISTS, COMPOSITIONS, AND THEIR USE
WO2018068295A1 (en) * 2016-10-14 2018-04-19 Merck Sharp & Dohme Corp. ARYL AND HETEROARYL ETHER DERIVATIVES AS LIVER X RECEPTOR β AGONISTS, COMPOSITIONS, AND THEIR USE
WO2018068297A1 (en) 2016-10-14 2018-04-19 Merck Sharp & Dohme Corp. N-ARYL AND N-HETEROARYL PIPERIDINE DERIVATIVES AS LIVER X RECEPTOR β AGONISTS, COMPOSITIONS, AND THEIR USE
JP2021504315A (ja) 2017-11-21 2021-02-15 ルジェニクス，インコーポレーテッド 多形及びその使用
WO2020056553A1 (zh) * 2018-09-17 2020-03-26 海门华祥医药科技有限公司 杂环化合物及其盐的制备方法
US11174220B2 (en) 2019-12-13 2021-11-16 Inspirna, Inc. Metal salts and uses thereof

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US6316503B1 (en) 1999-03-15 2001-11-13 Tularik Inc. LXR modulators
EA008928B1 (ru) * 2002-11-26 2007-08-31 Пфайзер Продактс Инк. Активаторы рецепторов, активируемых пролифератором пероксисом (ppar )
CA2581945C (en) * 2004-10-01 2011-01-18 Henrietta Dehmlow Hexafluoroisopropanol substituted ether derivatives
TW201006816A (en) * 2008-05-15 2010-02-16 Organon Nv Hexafluoroisopropanol derivatives

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CA2777671A1 (en) 2011-05-05
AU2010311534A1 (en) 2012-05-03
EP2493855B1 (en) 2014-02-26
JP5699156B2 (ja) 2015-04-08
JP2013508438A (ja) 2013-03-07
US20120238574A1 (en) 2012-09-20
EP2493855A1 (en) 2012-09-05
WO2011051282A1 (en) 2011-05-05
US9108939B2 (en) 2015-08-18
CA2777671C (en) 2017-07-04
TWI513695B (zh) 2015-12-21
TW201127825A (en) 2011-08-16
AU2010311534B2 (en) 2015-01-22

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