JP6109934B2 - 脂質合成の複素環モジュレーター - Google Patents

脂質合成の複素環モジュレーター Download PDF

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JP6109934B2
JP6109934B2 JP2015520627A JP2015520627A JP6109934B2 JP 6109934 B2 JP6109934 B2 JP 6109934B2 JP 2015520627 A JP2015520627 A JP 2015520627A JP 2015520627 A JP2015520627 A JP 2015520627A JP 6109934 B2 JP6109934 B2 JP 6109934B2
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alkyl
compound
halogen
cycloalkyl
item
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JP2015522036A (ja
JP2015522036A5 (cg-RX-API-DMAC7.html
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ヨハン ディー． オスロブ，
ヨハン ディー． オスロブ，
ロバート エス． マクドウェル，
ロバート エス． マクドウェル，
ラッセル ジョンソン，
ラッセル ジョンソン，
ハンビャオ ヤン，
ハンビャオ ヤン，
マーク エバンチック，
マーク エバンチック，
クリスティアナ エー． ザハリア，
クリスティアナ エー． ザハリア，
ハイイン カイ，
ハイイン カイ，
リリー ダブリュー． フー，
リリー ダブリュー． フー，
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Sagimet Biosciences Inc
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3V Biosciences Inc
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero 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
    • 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D205/00—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
    • C07D205/02—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D205/04—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • 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
    • C07D211/10—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 radicals containing only carbon and hydrogen atoms attached to ring carbon atoms
    • C07D211/16—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 radicals containing only carbon and hydrogen atoms attached to ring carbon atoms with acylated ring nitrogen atom
    • 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
    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D401/10—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 aromatic rings
    • 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
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing aromatic 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
    • C07D405/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • 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
    • C07D413/14—Heterocyclic 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
    • 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
    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Virology (AREA)
  • Reproductive Health (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Endocrinology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pregnancy & Childbirth (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic 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)
  • Plural Heterocyclic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
JP2015520627A 2012-07-03 2013-07-01 脂質合成の複素環モジュレーター Active JP6109934B2 (ja)

Applications Claiming Priority (9)

Application Number Priority Date Filing Date Title
US201261667894P 2012-07-03 2012-07-03
US61/667,894 2012-07-03
US201261698511P 2012-09-07 2012-09-07
US61/698,511 2012-09-07
US201261699819P 2012-09-11 2012-09-11
US61/699,819 2012-09-11
US201361785933P 2013-03-14 2013-03-14
US61/785,933 2013-03-14
PCT/US2013/048950 WO2014008197A1 (en) 2012-07-03 2013-07-01 Heterocyclic modulators of lipid synthesis

Publications (3)

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JP2015522036A JP2015522036A (ja) 2015-08-03
JP2015522036A5 JP2015522036A5 (cg-RX-API-DMAC7.html) 2016-08-18
JP6109934B2 true JP6109934B2 (ja) 2017-04-05

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US (3) US9428502B2 (cg-RX-API-DMAC7.html)
EP (1) EP2870150B1 (cg-RX-API-DMAC7.html)
JP (1) JP6109934B2 (cg-RX-API-DMAC7.html)
KR (1) KR102071095B1 (cg-RX-API-DMAC7.html)
CN (1) CN104507928B (cg-RX-API-DMAC7.html)
AU (2) AU2013286894B2 (cg-RX-API-DMAC7.html)
BR (1) BR112015000106B1 (cg-RX-API-DMAC7.html)
CA (1) CA2877999C (cg-RX-API-DMAC7.html)
ES (1) ES2738823T3 (cg-RX-API-DMAC7.html)
IL (1) IL236407A (cg-RX-API-DMAC7.html)
IN (1) IN2015DN00137A (cg-RX-API-DMAC7.html)
MX (1) MX364815B (cg-RX-API-DMAC7.html)
NZ (2) NZ703162A (cg-RX-API-DMAC7.html)
PL (1) PL2870150T3 (cg-RX-API-DMAC7.html)
SG (1) SG11201500024YA (cg-RX-API-DMAC7.html)
WO (1) WO2014008197A1 (cg-RX-API-DMAC7.html)
ZA (1) ZA201409477B (cg-RX-API-DMAC7.html)

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JP2017502083A (ja) * 2014-01-07 2017-01-19 ３−ブイ・バイオサイエンシーズ・インコーポレイテッド３−Ｖ Ｂｉｏｓｃｉｅｎｃｅｓ，Ｉｎｃ． 癌及びウイルス感染症に対する使用のための脂質合成の複素環式モジュレータ

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US9624173B2 (en) * 2011-03-08 2017-04-18 3-V Biosciences, Inc. Heterocyclic modulators of lipid synthesis
US20170119786A1 (en) 2011-03-08 2017-05-04 3-V Biosciences, Inc. Heterocyclic modulators of lipid synthesis
PL2870150T3 (pl) 2012-07-03 2019-12-31 3-V Biosciences, Inc. Heterocykliczne modulatory syntezy lipidów
CA2934251C (en) * 2013-12-20 2024-01-02 3-V Biosciences, Inc. A combination of heterocyclic modulators of lipid synthesis and chemotherapeutic drugs in treatment of cancer
EP3179990B1 (en) * 2014-08-15 2020-10-14 Sagimet Biosciences Inc. Fatty acid synthase inhibitor for use in the treatment of drug resistant cancer
CN107108581B (zh) * 2014-08-21 2020-06-23 百时美施贵宝公司 作为强效rock抑制剂的回接苯甲酰胺衍生物
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AU2016374568B2 (en) 2015-12-18 2020-08-27 Janssen Pharmaceutica Nv Radiolabelled mGluR2/3 PET ligands
HRP20201372T1 (hr) 2015-12-18 2020-11-27 Janssen Pharmaceutica Nv Radioaktivno označeni pet mglur2/3 ligandi
US10435388B2 (en) 2016-01-07 2019-10-08 Cs Pharmatech Limited Selective inhibitors of clinically important mutants of the EGFR tyrosine kinase
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NZ754372A (en) 2016-11-11 2022-11-25 Sagimet Biosciences Inc Heterocyclic modulators of lipid synthesis
CN107954852A (zh) * 2017-11-30 2018-04-24 贝利化学（张家港）有限公司 2，5-二卤代苯甲酸的制备方法
WO2020135483A1 (en) 2018-12-26 2020-07-02 Janssen Pharmaceutica Nv Thienopyridinone compounds
US20220400732A1 (en) * 2019-03-21 2022-12-22 Cornell University Anti-fructose therapy for colorectal and small intestine cancers
CN111592495A (zh) * 2020-07-06 2020-08-28 上海启讯医药科技有限公司 一种2-正丁基-4-氯-5甲酰基咪唑的制备方法
CN114988975A (zh) * 2022-06-28 2022-09-02 江苏科技大学 一种基于有机染料催化的β-三氟甲基烯胺化合物的制备方法
CN116482278B (zh) * 2023-05-06 2024-02-09 广州清瑞生物科技有限责任公司 一种用于检测阿昔洛韦的对照品的制备方法
CN119080742A (zh) * 2023-06-05 2024-12-06 甘莱制药有限公司 脂质合成的杂环调节剂的工业化制备
WO2025086054A1 (zh) * 2023-10-23 2025-05-01 歌礼生物科技（杭州）有限公司 一种包含苯甲腈衍生物的药物组合物
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US8871790B2 (en) * 2011-03-08 2014-10-28 3-V Biosciences, Inc. Heterocyclic modulators of lipid synthesis
US9624173B2 (en) * 2011-03-08 2017-04-18 3-V Biosciences, Inc. Heterocyclic modulators of lipid synthesis
LT2683244T (lt) 2011-03-08 2017-04-10 3-V Biosciences, Inc. Lipidų sintezės heterocikliniai moduliatoriai
PL2870150T3 (pl) 2012-07-03 2019-12-31 3-V Biosciences, Inc. Heterocykliczne modulatory syntezy lipidów
CA2934251C (en) * 2013-12-20 2024-01-02 3-V Biosciences, Inc. A combination of heterocyclic modulators of lipid synthesis and chemotherapeutic drugs in treatment of cancer
CN105980376B (zh) * 2014-01-07 2019-03-22 3-V生物科学股份有限公司 用于针对癌症和病毒感染使用的脂质合成杂环调节剂
EP3179990B1 (en) * 2014-08-15 2020-10-14 Sagimet Biosciences Inc. Fatty acid synthase inhibitor for use in the treatment of drug resistant cancer
CA2979696A1 (en) * 2015-03-19 2016-09-22 3-V Biosciences, Inc. Heterocyclic modulators of lipid synthesis

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2017502083A (ja) * 2014-01-07 2017-01-19 ３−ブイ・バイオサイエンシーズ・インコーポレイテッド３−Ｖ Ｂｉｏｓｃｉｅｎｃｅｓ，Ｉｎｃ． 癌及びウイルス感染症に対する使用のための脂質合成の複素環式モジュレータ

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EP2870150A1 (en) 2015-05-13
BR112015000106A2 (pt) 2017-06-27
IN2015DN00137A (cg-RX-API-DMAC7.html) 2015-06-12
US9428502B2 (en) 2016-08-30
US20150210688A1 (en) 2015-07-30
US10053450B2 (en) 2018-08-21
KR102071095B1 (ko) 2020-01-29
AU2013286894B2 (en) 2017-12-07
CA2877999A1 (en) 2014-01-09
US10118913B2 (en) 2018-11-06
ZA201409477B (en) 2021-05-26
IL236407A (en) 2017-10-31
AU2017265027A1 (en) 2017-12-14
EP2870150B1 (en) 2019-06-19
NZ729443A (en) 2017-11-24
AU2013286894A1 (en) 2015-01-22
KR20150032571A (ko) 2015-03-26
SG11201500024YA (en) 2015-03-30
ES2738823T3 (es) 2020-01-27
US20180222892A1 (en) 2018-08-09
MX2015000151A (es) 2015-04-10
NZ703162A (en) 2017-05-26
HK1208445A1 (en) 2016-03-04
WO2014008197A1 (en) 2014-01-09
US20160311803A1 (en) 2016-10-27
IL236407A0 (en) 2015-02-26
RU2015103345A (ru) 2016-08-20
BR112015000106B1 (pt) 2022-02-22
CN104507928A (zh) 2015-04-08
PL2870150T3 (pl) 2019-12-31
MX364815B (es) 2019-05-08
JP2015522036A (ja) 2015-08-03
CN104507928B (zh) 2016-09-28
CA2877999C (en) 2021-02-23

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