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AR077908A1 - Compuestos de oxadiazol como moduladores de s1p - Google Patents

Compuestos de oxadiazol como moduladores de s1p

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Publication number
AR077908A1
AR077908A1 ARP100103076A ARP100103076A AR077908A1 AR 077908 A1 AR077908 A1 AR 077908A1 AR P100103076 A ARP100103076 A AR P100103076A AR P100103076 A ARP100103076 A AR P100103076A AR 077908 A1 AR077908 A1 AR 077908A1
Authority
AR
Argentina
Prior art keywords
optionally substituted
alkyl
phenyl
cyclohexyl
optionally
Prior art date
Application number
ARP100103076A
Other languages
English (en)
Inventor
Shannon R Fixx-Stenzel
Adrian D Hobson
Kevin R Woller
Kevin P Cusack
Eric C Breinlinger
Robert H Stoffel
Shannon R Fix-Stenzel
Original Assignee
Abbott Lab
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Filing date
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Application filed by Abbott Lab filed Critical Abbott Lab
Publication of AR077908A1 publication Critical patent/AR077908A1/es

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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
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    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
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    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/14Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/38Drugs for disorders of the endocrine system of the suprarenal hormones
    • A61P5/40Mineralocorticosteroids, e.g. aldosterone; Drugs increasing or potentiating the activity of mineralocorticosteroids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P7/06Antianaemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/08Vasodilators for multiple indications
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D271/00Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
    • C07D271/02Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms not condensed with other rings
    • C07D271/061,2,4-Oxadiazoles; Hydrogenated 1,2,4-oxadiazoles
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/10Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
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  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Pulmonology (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Rheumatology (AREA)
  • Transplantation (AREA)
  • Ophthalmology & Optometry (AREA)
  • Emergency Medicine (AREA)
  • Obesity (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Dermatology (AREA)
  • Urology & Nephrology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Compuestos de oxadiazol, composiciones farmacéuticas que contienen dichos compuestos y uso de dichos compuestos o de dichas composiciones como agonistas o antagonistas de los receptores unidos a la proteína G de la familia S1P, para tratar enfermedades asociadas con la modulacion de la actividad de los receptores de la S1P, particularmente al proveer un efecto de inmunosupresion beneficioso. Reivindicacion 1: Un compuesto caracterizado porque es de formula (1) sales aceptables farmacéuticamente, metabolitos biologicamente activos, solvatos, hidratos, prodrogas, racematos, enantiomeros o estereoisomeros del mismo, donde L es una union o alquilo C1-3 opcionalmente sustituido; R1 es -C(O)-NH-fenilo, -NH-C(O)-furanilo, -NH-S(O)2-fenilo opcionalmente sustituido, -O-alquilo C1-3 opcionalmente sustituido, -S-alquilo C1-3 opcionalmente sustituido, alquilo C2-6 opcionalmente sustituido, amino opcionalmente sustituido, cicloalquilo C3-6 opcionalmente sustituido, -(CH2)alquilo C3, tetrahidrobenzofuranilo opcionalmente sustituido, furanilo opcionalmente sustituido, tetrahidrofuranilo opcionalmente sustituido, 2,3-dihidroisoindolilo opcionalmente sustituido, isoindolinilo opcionalmente sustituido, imidazolilo opcionalmente sustituido, 5,6-dihidro imidazo[1,2-a]pirazinilo opcionalmente sustituido, imidazo[1,2-a]pirazinilo opcionalmente sustituido, indolilo opcionalmente sustituido, isoxazolilo opcionalmente sustituido, morfolinilo opcionalmente sustituido, naftilo opcionalmente sustituido, fenilo opcionalmente sustituido, -O-CH2-fenilo opcionalmente sustituido, -O-fenilo opcionalmente sustituido, -O-fenilo opcionalmente sustituido, piperidinilo opcionalmente sustituido, pirazolilo opcionalmente sustituido, piridinilo opcionalmente sustituido, pirimidinilo opcionalmente sustituido, pirrolidinilo opcionalmente sustituido, 1,2,3,4-tetrahidroisoquinolinilo opcionalmente sustituido, quinolinilo opcionalmente sustituido, 3,4-dihidroquinolinilo opcionalmente sustituido, 3,4-dihidroisoquinolinilo opcionalmente sustituido, 5,6,7,8-tetrahidroimidazo[1,2-a]pirazinilo opcionalmente sustituido, pirrolilo opcionalmente sustituido, pirrolo[2,3-b]piridinilo opcionalmente sustituido, quinolinilo opcionalmente sustituido, tiazolilo opcionalmente sustituido o tienilo opcionalmente sustituido; R2 es Br, Cl, CF3, CN, o -O-alquilo C1-2; R3 es alquilo C3-8 opcionalmente sustituido, alquilo C2-6deuterado, alquenilo C4-5, alquinilo C4-5, cicloalquilo C3-6 opcionalmente sustituido, alquilo C2-3 opcionalmente sustituido-O-alquilo C1-3 opcionalmente sustituido, alquilo C1-3 opcionalmente sustituido-imidazolilo, alquilo C1-3opcionalmente sustituido-morfolinilo, alquilo C1-3 opcionalmente sustituido-fenilo opcionalmente sustituido, alquilo C1-3 opcionalmente sustituido-piperazinilo opcionalmente sustituido, alquilo C1-3 opcionalmente sustituido-pirrolidinilo, alquilo C1-3 opcionalmente sustituido-piperidinilo, alquilo C1-3 opcionalmente sustituido-tienilo, tetrahidrofuranilo o tiazolilo opcionalmente sustituido; y R6 es H; con las siguientes condiciones R1 no está sustituido con ciclohexilo opcionalmente sustituido, -C(O)ciclohexilo o -NH-ciclohexilo; cuando L es alquilo C1-3, R1 no es isoxazolilo opcionalmente sustituido; cuando R3 es (C1)alquilo opcionalmente sustituido, L-R1 no es ciclohexilo o -CH2-ciclohexilo; y con la condicion de que el compuesto no sea un compuesto de formula (2) o (3).
ARP100103076A 2009-12-08 2010-08-23 Compuestos de oxadiazol como moduladores de s1p AR077908A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US26767909P 2009-12-08 2009-12-08

Publications (1)

Publication Number Publication Date
AR077908A1 true AR077908A1 (es) 2011-09-28

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ID=44145850

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP100103076A AR077908A1 (es) 2009-12-08 2010-08-23 Compuestos de oxadiazol como moduladores de s1p

Country Status (9)

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EP (1) EP2509424A4 (es)
JP (1) JP2013512951A (es)
CN (1) CN102762102A (es)
AR (1) AR077908A1 (es)
CA (1) CA2783851A1 (es)
MX (1) MX2012006667A (es)
TW (1) TW201120016A (es)
UY (1) UY32853A (es)
WO (1) WO2011071570A1 (es)

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EP2184989B1 (en) 2007-08-13 2015-05-06 Monsanto Technology LLC Compositions and methods for controlling nematodes
AU2012304661A1 (en) 2011-09-08 2014-04-03 Allergan, Inc. 3-(4-(5-phenyl-1,2,4-oxadiazol-3-yl)phenoxy)propan-2-ol derivatives as sphingosine-1 phosphate receptors modulators
ES2649475T3 (es) 2013-03-15 2018-01-12 Idorsia Pharmaceuticals Ltd Derivados de piridin-4-ilo
US9828351B2 (en) * 2014-06-26 2017-11-28 Monash University Enzyme interacting agents
US12209072B2 (en) 2018-09-18 2025-01-28 Bristol-Myers Squibb Company Cyclopentyl acids as LPA antagonists
CN112702998A (zh) * 2018-09-18 2021-04-23 百时美施贵宝公司 作为lpa拮抗剂的环庚酸
ES2941774T3 (es) 2018-09-18 2023-05-25 Bristol Myers Squibb Co Acidos oxabiciclo como antagonistas de LPA
CN109369620B (zh) * 2018-12-22 2020-04-14 山东大学 吡啶类化合物及其制备方法与抗胃癌应用
CN109776443B (zh) * 2019-03-25 2022-09-27 上海万巷制药有限公司 一种具有抗氧化作用的噁二唑类化合物及其制备方法
CN114728927B (zh) 2019-11-19 2025-08-29 莫达戈有限公司 用于诊断、治疗和预防与α-突触核蛋白的聚集相关的疾病的化合物
UY38964A (es) 2019-11-25 2021-06-30 Novartis Ag Derivados de 1,2,4-oxadiazol como agonistas del receptor hepático x, sus usos y métodos relacionados referencia cruzada a solicitudes relacionadas
CN115260173B (zh) * 2021-04-30 2024-08-30 厦门宝太生物科技股份有限公司 环戊烷并吲哚类支链酸衍生物及其制备方法和应用
CN113662938B (zh) * 2021-09-26 2022-08-16 广西科技大学 一种胺类衍生物在制备抗肿瘤药物组合物中的应用
WO2023118253A1 (en) * 2021-12-23 2023-06-29 Chiesi Farmaceutici S.P.A. Cyclohexane acid derivatives as lpa receptor inhibitors
EP4649080A1 (en) * 2023-01-13 2025-11-19 Oppilan Pharma Ltd. Preparation of an s1p receptor modulator
CN116444454B (zh) * 2023-06-16 2023-09-12 中国医学科学院医药生物技术研究所 N-羟基脒衍生物及制备方法和应用、肿瘤免疫治疗药物

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TWI404706B (zh) * 2006-01-11 2013-08-11 Actelion Pharmaceuticals Ltd 新穎噻吩衍生物
BRPI0711358A2 (pt) * 2006-05-09 2011-09-27 Pfizer Prod Inc derivados do ácido cicloalquilamino e suas composições farmacêuticas
DK2069335T3 (da) * 2006-09-08 2013-02-18 Actelion Pharmaceuticals Ltd Pyridin-3-ylderivater som immunomoduleringsmidler
AU2007334436A1 (en) * 2006-12-15 2008-06-26 Abbott Laboratories Novel oxadiazole compounds
AU2009220893A1 (en) * 2008-03-07 2009-09-11 Actelion Pharmaceuticals Ltd Novel aminomethyl benzene derivatives
GB0911130D0 (en) * 2009-06-26 2009-08-12 Glaxo Group Ltd Novel compounds

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MX2012006667A (es) 2012-10-15
WO2011071570A1 (en) 2011-06-16
JP2013512951A (ja) 2013-04-18
CA2783851A1 (en) 2011-06-16
EP2509424A4 (en) 2013-09-04
UY32853A (es) 2011-06-30
TW201120016A (en) 2011-06-16
EP2509424A1 (en) 2012-10-17
CN102762102A (zh) 2012-10-31

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