CN105705501B - RORγ调节剂 - Google Patents

RORγ调节剂 Download PDF

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Publication number
CN105705501B
CN105705501B CN201480061168.1A CN201480061168A CN105705501B CN 105705501 B CN105705501 B CN 105705501B CN 201480061168 A CN201480061168 A CN 201480061168A CN 105705501 B CN105705501 B CN 105705501B
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Prior art keywords
base
hexafluoro
fluorophenyl
tetrahydroquinoline
sulfonyl
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Expired - Fee Related
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CN201480061168.1A
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Chinese (zh)
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CN105705501A (zh
Inventor
T·G·M·达尔
段敬武
龚华
江斌
陆忠辉
D·S·温斯坦
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Bristol Myers Squibb Co
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Bristol Myers Squibb Co
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/58—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems with hetero atoms directly attached to the ring nitrogen atom
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • 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
    • C07D279/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one sulfur atom as the only ring hetero atoms
    • C07D279/10—1,4-Thiazines; Hydrogenated 1,4-thiazines
    • C07D279/14—1,4-Thiazines; Hydrogenated 1,4-thiazines condensed with carbocyclic rings or ring systems
    • C07D279/16—1,4-Thiazines; Hydrogenated 1,4-thiazines condensed with carbocyclic rings or ring systems condensed with one six-membered ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic 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
    • C07D413/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D471/10—Spiro-condensed systems
    • 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
    • C07D487/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic 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
    • C07D491/02—Heterocyclic 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
    • C07D491/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic 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
    • C07D491/02—Heterocyclic 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
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic 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
    • C07D491/02—Heterocyclic 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
    • C07D491/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Rheumatology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Pain & Pain Management (AREA)
  • Transplantation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Quinoline Compounds (AREA)
  • Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
CN201480061168.1A 2013-09-09 2014-09-08 RORγ调节剂 Expired - Fee Related CN105705501B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201361875220P 2013-09-09 2013-09-09
US61/875,220 2013-09-09
PCT/US2014/054489 WO2015035278A1 (en) 2013-09-09 2014-09-08 RORγ MODULATORS

Publications (2)

Publication Number Publication Date
CN105705501A CN105705501A (zh) 2016-06-22
CN105705501B true CN105705501B (zh) 2019-04-19

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US (1) US9663469B2 (cg-RX-API-DMAC10.html)
EP (1) EP3044219A1 (cg-RX-API-DMAC10.html)
JP (1) JP6407285B2 (cg-RX-API-DMAC10.html)
CN (1) CN105705501B (cg-RX-API-DMAC10.html)
WO (1) WO2015035278A1 (cg-RX-API-DMAC10.html)

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CN105705501B (zh) 2013-09-09 2019-04-19 百时美施贵宝公司 RORγ调节剂
JP6397488B2 (ja) 2013-09-20 2018-09-26 ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ ＲＯＲγ調節因子
WO2015103508A1 (en) 2014-01-06 2015-07-09 Bristol-Myers Squibb Company CARBOCYCLIC SULFONE RORγ MODULATORS
US9708253B2 (en) 2014-01-06 2017-07-18 Bristol-Myers Squibb Company Cyclohexyl sulfone RORγ modulators
CN106061956B (zh) 2014-01-06 2021-03-12 百时美施贵宝公司 作为RORγ调节剂的杂环砜
JP6661630B2 (ja) 2014-10-30 2020-03-11 ヤンセン ファーマシューティカ エヌ．ベー． ＲＯＲγｔのモジュレーターとしてのチアゾール
PT3212642T (pt) 2014-10-30 2019-12-19 Janssen Pharmaceutica Nv Tiazóis com amida substituída como moduladores de rorgammat
JOP20200117A1 (ar) 2014-10-30 2017-06-16 Janssen Pharmaceutica Nv كحولات ثلاثي فلوروميثيل كمُعدلات للمستقبل النووي جاما تي المرتبط بحمض الريتيونَويك ROR?t
MA41389A1 (fr) 2015-05-07 2018-06-29 Bristol Myers Squibb Co Utilisation de sulfones tricycliques en tant que modulateurs de rory
HK1253734A1 (zh) * 2015-06-11 2019-06-28 The Regents Of The University Of Michigan 用作RORγ激动剂和用於治疗疾病的芳基二氢-2H-苯并[B][1，4]恶嗪磺酰胺和相关化合物
CN104892546B (zh) * 2015-07-01 2017-03-01 中国科学院南海海洋研究所 一类(2h)1,4‑苯并噻嗪类化合物及其制备方法和应用
EP3330256B1 (en) * 2015-07-07 2021-06-16 Shionogi & Co., Ltd. HETEROCYCLIC DERIVATIVE HAVING TrkA-INHIBITING ACTIVITY
TW201803869A (zh) 2016-04-27 2018-02-01 健生藥品公司 作為ＲＯＲγＴ調節劑之６－胺基吡啶－３－基噻唑
TN2018000385A1 (en) 2016-05-20 2020-06-15 Xenon Pharmaceuticals Inc Benzenesulfonamide compounds and their use as therapeutic agents
WO2017213210A1 (ja) * 2016-06-10 2017-12-14 武田薬品工業株式会社 複素環化合物
SG10201912376VA (en) 2016-12-09 2020-02-27 Xenon Pharmaceuticals Inc Benzenesulfonamide compounds and their use as therapeutic agents
US10822318B2 (en) * 2017-05-24 2020-11-03 Regents Of The University Of Minnesota Lactone-based probes and methods of use thereof
JP2020142989A (ja) * 2017-06-21 2020-09-10 Ｍｅｉｊｉ Ｓｅｉｋａファルマ株式会社 イミダゾール誘導体及びそれを含有する医薬
JP2021517563A (ja) 2018-03-12 2021-07-26 エスカリア バイオサイエンシーズ，ビーブイ 二環式ＲＯＲγモジュレーター
US11242350B2 (en) 2018-03-12 2022-02-08 Escalier Biosciences B.V. Spirocyclic ROR-gamma modulators
BR112020024729A2 (pt) 2018-06-13 2021-03-23 Xenon Pharmaceuticals, Inc. compostos de benzenossulfonamida e seu uso como agentes terapêuticos
US10975057B2 (en) 2018-06-18 2021-04-13 Janssen Pharmaceutica Nv 6-aminopyridin-3-yl pyrazoles as modulators of RORgT
EP3790865A1 (en) 2018-06-18 2021-03-17 Janssen Pharmaceutica NV Phenyl substituted pyrazoles as modulators of roryt
US11345666B2 (en) 2018-06-18 2022-05-31 Janssen Pharmaceutica Nv Phenyl and pyridinyl substituted imidazoles as modulators of RORγT
CN112292373A (zh) 2018-06-18 2021-01-29 詹森药业有限公司 作为RORγt的调节剂的吡啶基吡唑类
CN112119065B (zh) * 2018-07-13 2024-01-23 四川科伦博泰生物医药股份有限公司 苯并二氮杂环类化合物、其制备方法及用途
IL279810B2 (en) 2018-08-31 2025-03-01 Xenon Pharmaceuticals Inc Heteroaryl-modified sulfonamide compounds and their use as medicinal agents
JP7383012B2 (ja) 2018-08-31 2023-11-17 ゼノン・ファーマシューティカルズ・インコーポレイテッド ヘテロアリール置換スルホンアミド化合物、およびナトリウムチャネル阻害剤としてのその使用

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CN105705501B (zh) 2013-09-09 2019-04-19 百时美施贵宝公司 RORγ调节剂
JP6397488B2 (ja) 2013-09-20 2018-09-26 ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ ＲＯＲγ調節因子
WO2015103508A1 (en) 2014-01-06 2015-07-09 Bristol-Myers Squibb Company CARBOCYCLIC SULFONE RORγ MODULATORS
US9708253B2 (en) 2014-01-06 2017-07-18 Bristol-Myers Squibb Company Cyclohexyl sulfone RORγ modulators
CN106061956B (zh) 2014-01-06 2021-03-12 百时美施贵宝公司 作为RORγ调节剂的杂环砜
CN106061971B (zh) 2014-01-06 2019-03-12 百时美施贵宝公司 吡咯烷基砜衍生物及其作为RORγ调节剂的用途

Patent Citations (2)

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WO2012064744A2 (en) * 2010-11-08 2012-05-18 Lycera Corporation Tetrahydroquinoline and related bicyclic compounds for inhibition of rorϒ activity and the treatment of disease

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US20160318870A1 (en) 2016-11-03
JP2016532715A (ja) 2016-10-20
CN105705501A (zh) 2016-06-22
EP3044219A1 (en) 2016-07-20
WO2015035278A1 (en) 2015-03-12
JP6407285B2 (ja) 2018-10-17
US9663469B2 (en) 2017-05-30

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