KR20170102299A - 비-알콜성 지방간 질환의 치료를 위한 acc 억제제 조합 요법 - Google Patents
비-알콜성 지방간 질환의 치료를 위한 acc 억제제 조합 요법 Download PDFInfo
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- KR20170102299A KR20170102299A KR1020177021086A KR20177021086A KR20170102299A KR 20170102299 A KR20170102299 A KR 20170102299A KR 1020177021086 A KR1020177021086 A KR 1020177021086A KR 20177021086 A KR20177021086 A KR 20177021086A KR 20170102299 A KR20170102299 A KR 20170102299A
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Classifications
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- 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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- 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
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- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
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| PCT/US2016/012673 WO2016112305A1 (en) | 2015-01-09 | 2016-01-08 | Acc inhibitor combination therapy for the treatment of non-alcoholic fatty liver disease |
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Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2021040440A1 (ko) * | 2019-08-30 | 2021-03-04 | (주)셀트리온 | 비알콜성 지방간염(nash, nonalcoholic steatohepatitis) 치료 또는 예방을 위한 약학 조성물 |
| KR20210114887A (ko) * | 2020-03-11 | 2021-09-24 | 동아에스티 주식회사 | 비알콜성지방간염의 예방 또는 치료를 위한 약학적 조성물 |
| KR20230110541A (ko) * | 2020-11-17 | 2023-07-24 | 엥방티바 | 간 질환의 치료를 위한 병용 요법 |
Families Citing this family (78)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PT1993360T (pt) | 2005-12-28 | 2017-05-25 | Vertex Pharma | Formas sólidas de n-[2,4-bis(1,1-dimetiletil)-5-hidroxifenil]-1,4-di-hidro-4-oxoquinolina-3-carboxamida |
| TWI625121B (zh) | 2009-07-13 | 2018-06-01 | 基利科學股份有限公司 | 調節細胞凋亡信號之激酶的抑制劑 |
| US9719068B2 (en) | 2010-05-06 | 2017-08-01 | Children's Hospital Medical Center | Methods and systems for converting precursor cells into intestinal tissues through directed differentiation |
| EP2545964A1 (en) | 2011-07-13 | 2013-01-16 | Phenex Pharmaceuticals AG | Novel FXR (NR1H4) binding and activity modulating compounds |
| US11571431B2 (en) | 2013-12-04 | 2023-02-07 | Galmed Research And Development Ltd | Aramchol salts |
| EP3149156B1 (en) | 2014-05-28 | 2021-02-17 | Children's Hospital Medical Center | Methods and systems for converting precursor cells into gastric tissues through directed differentiation |
| JP6804438B2 (ja) | 2014-10-17 | 2020-12-23 | チルドレンズ ホスピタル メディカル センター | 多能性幹細胞を使用するヒト小腸のin vivoモデル、並びにそれを作製、及び使用する方法 |
| CN109879859B (zh) | 2015-07-06 | 2022-01-25 | 吉利德科学公司 | Cot调节剂及其使用方法 |
| US20170166583A1 (en) | 2015-11-25 | 2017-06-15 | Gilead Apollo, Llc | Ester acc inhibitors and uses thereof |
| US20170166582A1 (en) * | 2015-11-25 | 2017-06-15 | Gilead Apollo, Llc | Pyrazole acc inhibitors and uses thereof |
| IL243707A0 (en) | 2016-01-20 | 2016-05-01 | Galmed Res And Dev Ltd | Treatment to regulate the microbiota in the intestine |
| CN112920200A (zh) | 2016-03-02 | 2021-06-08 | 吉利德阿波罗公司 | 噻吩并嘧啶二酮acc抑制剂的固体形式及其制备方法 |
| EP4177335A1 (en) | 2016-05-05 | 2023-05-10 | Children's Hospital Medical Center | Methods for the in vitro manufacture of gastric fundus tissue and compositions related to same |
| SI3730487T1 (sl) | 2016-06-13 | 2022-08-31 | Gilead Sciences, Inc. | Azetidinski derivati kot modulatorji FXR (NR1H4) |
| CA3252823A1 (en) | 2016-06-13 | 2025-02-25 | Gilead Sciences Inc | Fxr (nr1h4) modulating compounds |
| EP3534976A4 (en) | 2016-11-04 | 2020-09-16 | Children's Hospital Medical Center | PATHOLOGICAL MODELS OF HEPATIC ORGANOIDS AND ASSOCIATED METHODS OF MANUFACTURE AND USE |
| US11197870B2 (en) | 2016-11-10 | 2021-12-14 | Galmed Research And Development Ltd | Treatment for hepatic fibrosis |
| MA46786A (fr) * | 2016-11-10 | 2019-09-18 | Galmed Res And Development Ltd | Inhibition de la fibrose chez des patients atteints d'une stéatose hépatique non alcoolique |
| MA47558A (fr) * | 2016-11-10 | 2019-09-18 | Galmed Res And Development Ltd | Traitement de la fibrose |
| EP3548507A4 (en) | 2016-12-05 | 2020-07-15 | Children's Hospital Medical Center | COLON ORGANOIDS AND PROCESSES FOR THE PREPARATION AND USE THEREOF |
| WO2018134254A1 (en) | 2017-01-17 | 2018-07-26 | Heparegenix Gmbh | Protein kinase inhibitors for promoting liver regeneration or reducing or preventing hepatocyte death |
| KR102577824B1 (ko) * | 2017-01-22 | 2023-09-13 | 선샤인 레이크 파르마 컴퍼니 리미티드 | 티에노피리미딘 유도체 및 의약에서 이의 용도 |
| WO2018171699A1 (zh) * | 2017-03-24 | 2018-09-27 | 浙江海正药业股份有限公司 | 氰基取代的杂芳基并嘧啶酮类衍生物及其制备方法和用途 |
| TW201900167A (zh) * | 2017-03-28 | 2019-01-01 | 美商基利科學股份有限公司 | 治療肝疾病之方法 |
| JP6906626B2 (ja) * | 2017-03-28 | 2021-07-21 | ギリアード サイエンシーズ, インコーポレイテッド | 肝疾患を処置するための治療的組み合わせ |
| CA3059883A1 (en) * | 2017-04-12 | 2018-10-18 | Gilead Sciences, Inc. | Methods of treating liver disease |
| EP3609997A4 (en) | 2017-04-14 | 2021-03-03 | Children's Hospital Medical Center | COMPOSITIONS OF STEM CELLS FROM MULTIPLE DONOR CELLS AND THEIR PREPARATION PROCEDURES |
| MX2019012535A (es) * | 2017-04-18 | 2020-08-17 | Genfit | Combinacion que comprende un agonista de ppar tal como elafibranor y un inhibidor de la acetil-coa carboxilasa (acc). |
| WO2018195727A1 (en) * | 2017-04-24 | 2018-11-01 | Tsinghua University | Use of autoinducer-related pathway in inducing apoptosis and anti-infective therapy |
| WO2018236896A1 (en) * | 2017-06-19 | 2018-12-27 | Arena Pharmaceuticals, Inc. | Compounds and methods for treatment of nafld and nash |
| WO2019015583A1 (en) | 2017-07-17 | 2019-01-24 | Nanjing Ruijie Pharmatech Co., Ltd. | NOVEL COMPOUNDS AND THEIR USES AS ACC INHIBITORS |
| EP3660023B1 (en) * | 2017-07-26 | 2023-03-08 | Nanjing Sanhome Pharmaceutical Co., Ltd. | Thienopyrimidinedione compounds as acc inhibitors and use thereof |
| CN109316601B (zh) * | 2017-07-31 | 2021-11-09 | 武汉朗来科技发展有限公司 | 药物组合物及其用途 |
| EP3676262A4 (en) | 2017-09-03 | 2021-03-31 | Angion Biomedica Corp. | VINYLHETEROCYCLENE AS RHO-ASSOCIATED COILED COIL KINASE (ROCK) INHIBITORS |
| US11033601B2 (en) * | 2017-09-14 | 2021-06-15 | The Regents Of The University Of Colorado, A Body Corporate | Selective inhibition of V1b for treating fatty liver |
| JP7479278B2 (ja) * | 2017-10-06 | 2024-05-08 | ギリアード サイエンシーズ, インコーポレイテッド | Acc阻害剤を含む併用療法 |
| EP3694603A4 (en) | 2017-10-10 | 2021-07-14 | Children's Hospital Medical Center | ESOPHAGUS TISSUE AND / OR ORGANOID COMPOSITIONS AND METHOD FOR MANUFACTURING THEREOF |
| EP3708577B1 (en) * | 2017-11-06 | 2024-09-04 | Shenzhen Turier Biotech Co., Ltd. | Treatment of biliary cirrhosis based on oxyntomodulin analogue glp-1r/gcgr dual-target agonist peptide |
| CN107693514A (zh) * | 2017-12-04 | 2018-02-16 | 威海贯标信息科技有限公司 | 一种鲁格列净组合物 |
| US12379372B2 (en) | 2017-12-21 | 2025-08-05 | Children's Hospital Medical Center | Digitalized human organoids and methods of using same |
| SG11202007143UA (en) | 2018-01-31 | 2020-08-28 | Heparegenix Gmbh | Protein kinase mkk4 inhibitors for promoting liver regeneration or reducing or preventing hepatocyte death |
| AU2019254371A1 (en) * | 2018-04-17 | 2020-10-08 | Boehringer Ingelheim International Gmbh | Pharmaceutical composition, methods for treating and uses thereof |
| EP3784657A4 (en) * | 2018-04-24 | 2022-02-09 | pH Pharma Co., Ltd. | USE OF NEUTROPHIL ELASTASE INHIBITORS IN LIVER DISEASE |
| EP3810139A1 (en) | 2018-06-21 | 2021-04-28 | HepaRegeniX GmbH | Tricyclic protein kinase inhibitors for promoting liver regeneration or reducing or preventing hepatocyte death |
| AU2019303986B2 (en) | 2018-07-16 | 2024-02-22 | Heparegenix Gmbh | Protein kinase inhibitors for promoting liver regeneration or reducing or preventing hepatocyte death |
| KR102887406B1 (ko) | 2018-07-26 | 2025-11-19 | 칠드런즈 호스피탈 메디칼 센터 | 간-담도-췌장 조직 및 이를 제조하는 방법 |
| US20210322324A1 (en) * | 2018-08-14 | 2021-10-21 | Avolynt | Method for treating primary sclerosing cholangitis |
| US11254660B2 (en) | 2018-08-31 | 2022-02-22 | Pfizer Inc. | Combinations for treatment of NASH/NAFLD and related diseases |
| WO2020049556A1 (en) * | 2018-09-06 | 2020-03-12 | Galmed Research And Development Ltd | Combination therapy for the treatment of liver disease |
| WO2020056158A1 (en) | 2018-09-12 | 2020-03-19 | Children's Hospital Medical Center | Organoid compositions for the production of hematopoietic stem cells and derivatives thereof |
| CN110950884B (zh) * | 2018-09-27 | 2024-03-26 | 上海翰森生物医药科技有限公司 | 含二并环类衍生物抑制剂、其制备方法和应用 |
| JP2022513101A (ja) * | 2018-11-20 | 2022-02-07 | 中国医▲薬▼研究▲開▼▲発▼中心有限公司 | スピロ環系化合物及びその医薬用途 |
| US11225473B2 (en) | 2019-01-15 | 2022-01-18 | Gilead Sciences, Inc. | FXR (NR1H4) modulating compounds |
| EP3927683A1 (en) | 2019-02-19 | 2021-12-29 | Gilead Sciences, Inc. | Solid forms of fxr agonists |
| US12458612B2 (en) * | 2019-04-10 | 2025-11-04 | Genfit | Combination therapy comprising compounds of formula (I) and GLP-1 receptor agonists |
| SG11202111552YA (en) | 2019-05-08 | 2021-11-29 | Aligos Therapeutics Inc | MODULATORS OF THR-ß AND METHODS OF USE THEREOF |
| TWI770527B (zh) | 2019-06-14 | 2022-07-11 | 美商基利科學股份有限公司 | Cot 調節劑及其使用方法 |
| JP7374233B2 (ja) * | 2019-07-02 | 2023-11-06 | ▲広▼▲東▼▲東▼▲陽▼光▲薬▼▲業▼有限公司 | 立体配置を有するチエノピリミジン誘導体及び薬物におけるその応用 |
| NZ785221A (en) | 2019-07-29 | 2025-08-29 | Heparegenix Gmbh | Heteroaryl-substituted pyrazolo-pyridine protein kinase inhibitors for promoting liver regeneration or reducing or preventing hepatocyte death |
| AR119594A1 (es) | 2019-08-09 | 2021-12-29 | Gilead Sciences Inc | Derivados de tienopirimidina como inhibidores acc y usos de los mismos |
| CN110628810B (zh) * | 2019-08-13 | 2022-06-28 | 浙江大学 | 一种提高植物光合效率的方法 |
| US20230105984A1 (en) | 2019-12-23 | 2023-04-06 | Svetlana Marukian | Compositions and methods for the treatment of liver diseases and disorders |
| JP7639008B2 (ja) | 2020-01-15 | 2025-03-04 | ヘパリジェニックス ゲーエムベーハー | 肝再生促進又は肝細胞死の抑制もしくは防止のためのプロテインキナーゼ阻害剤 |
| JP2021134211A (ja) | 2020-02-24 | 2021-09-13 | ファイザー・インク | Nafld/nashおよび関連疾患の処置のための組合せ |
| JP2022058085A (ja) | 2020-02-24 | 2022-04-11 | ファイザー・インク | ジアシルグリセロールアシルトランスフェラーゼ2阻害剤とアセチル-CoAカルボキシラーゼ阻害剤との組合せ |
| EP4126231A1 (en) | 2020-03-30 | 2023-02-08 | Gilead Sciences, Inc. | Solid forms of (s)-6-(((1-(bicyclo[1.1.1]pentan-1-yl)-1h-1,2,3-triazol-4-yl)2-methyl-1-oxo-1,2- dihydroisoquinolin-5-yl)methyl)))amino)8-chloro-(neopentylamino)quinoline-3-carb onitrile a cot inhibitor compound |
| CN115397824B (zh) | 2020-04-02 | 2024-10-22 | 吉利德科学公司 | 用于制备cot抑制剂化合物的方法 |
| CN111407892A (zh) * | 2020-04-08 | 2020-07-14 | 中国药科大学 | Acsl4及其在nash中的应用 |
| US11478533B2 (en) | 2020-04-27 | 2022-10-25 | Novo Nordisk A/S | Semaglutide for use in medicine |
| CN115666558A (zh) | 2020-05-21 | 2023-01-31 | 盐野义制药株式会社 | 脂肪性肝病的治疗用药物 |
| US12091404B2 (en) | 2021-03-11 | 2024-09-17 | Gilead Sciences, Inc. | GLP-1R modulating compounds |
| WO2022212194A1 (en) | 2021-03-29 | 2022-10-06 | Gilead Sciences, Inc. | Khk inhibitors |
| TW202345826A (zh) | 2021-06-04 | 2023-12-01 | 美商基利科學股份有限公司 | 治療nash之方法 |
| TW202311256A (zh) | 2021-06-18 | 2023-03-16 | 美商基利科學股份有限公司 | 用於治療fxr誘發之搔癢之il-31調節劑 |
| WO2023034381A1 (en) * | 2021-08-31 | 2023-03-09 | University Of Pittsburgh-Of The Commonwealth System Of Higher Education | Quantitative systems pharmacology methods for identifying therapeutics for disease states |
| WO2023047203A1 (en) * | 2021-09-25 | 2023-03-30 | Torrent Pharmaceuticals Ltd | Combination of omzotirome and antidiabetic agent, antihypertensive agent or anti-dyslipidemic agent |
| US20250041279A1 (en) | 2021-11-19 | 2025-02-06 | Shionogi & Co., Ltd. | Therapeutic medicine for heart disease or skeletal muscle disease |
| US20250017938A1 (en) * | 2023-06-20 | 2025-01-16 | Sagimet Biosciences Inc. | Combination therapies of fasn inhibitors with thyroid hormone receptor agonists |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2009155611A1 (en) * | 2008-06-20 | 2009-12-23 | Kinemed, Inc. | Compositions for the treatment of fibrotic diseases or conditions |
| US20100113473A1 (en) * | 2008-10-30 | 2010-05-06 | Player Mark R | Aryl amide compound as an acetyl coenzyme a carboxylase inhibitor |
| WO2012090219A2 (en) * | 2010-12-31 | 2012-07-05 | Jubilant Biosys Ltd. | Thiazole compounds useful as acetyl-coa carboxylase (acc) inhibitors |
| DK2776038T3 (en) * | 2011-11-11 | 2018-04-23 | Gilead Apollo Llc | ACC INHIBITORS AND APPLICATIONS THEREOF |
| EA030958B1 (ru) | 2013-05-10 | 2018-10-31 | Джилид Аполло, Ллс | Ингибиторы акк и их применение |
| BR112015028152A2 (pt) * | 2013-05-10 | 2017-07-25 | Nimbus Apollo Inc | inibidores de acc e usos dos mesmos |
| EA201591962A1 (ru) * | 2013-05-10 | 2016-06-30 | Нимбус Аполло, Инк. | Ингибиторы акк и их применение |
| US9988399B2 (en) | 2013-05-10 | 2018-06-05 | Gilead Apollo, Llc | Bicyclic compounds as ACC inhibitors and uses thereof |
-
2016
- 2016-01-08 BR BR112017014341-0A patent/BR112017014341A2/pt not_active Application Discontinuation
- 2016-01-08 CN CN201680004801.2A patent/CN107106873A/zh active Pending
- 2016-01-08 EP EP19176040.4A patent/EP3597271A1/en not_active Withdrawn
- 2016-01-08 EA EA201791258A patent/EA201791258A1/ru unknown
- 2016-01-08 AU AU2016205138A patent/AU2016205138A1/en not_active Abandoned
- 2016-01-08 SG SG11201705361PA patent/SG11201705361PA/en unknown
- 2016-01-08 CA CA2972919A patent/CA2972919A1/en not_active Abandoned
- 2016-01-08 EP EP16735485.1A patent/EP3242722A4/en not_active Withdrawn
- 2016-01-08 HK HK18102859.6A patent/HK1243369A1/zh unknown
- 2016-01-08 EA EA201892625A patent/EA201892625A1/ru unknown
- 2016-01-08 WO PCT/US2016/012673 patent/WO2016112305A1/en not_active Ceased
- 2016-01-08 JP JP2017535411A patent/JP2018501276A/ja not_active Withdrawn
- 2016-01-08 HK HK18105783.0A patent/HK1246232A1/zh unknown
- 2016-01-08 KR KR1020177021086A patent/KR20170102299A/ko not_active Withdrawn
- 2016-01-08 US US15/541,008 patent/US20180021341A1/en not_active Abandoned
- 2016-01-08 MX MX2017008844A patent/MX2017008844A/es unknown
-
2019
- 2019-05-13 US US16/410,894 patent/US20190381045A1/en not_active Abandoned
-
2020
- 2020-04-15 JP JP2020072689A patent/JP2020109130A/ja active Pending
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2021040440A1 (ko) * | 2019-08-30 | 2021-03-04 | (주)셀트리온 | 비알콜성 지방간염(nash, nonalcoholic steatohepatitis) 치료 또는 예방을 위한 약학 조성물 |
| KR20210114887A (ko) * | 2020-03-11 | 2021-09-24 | 동아에스티 주식회사 | 비알콜성지방간염의 예방 또는 치료를 위한 약학적 조성물 |
| KR20230110541A (ko) * | 2020-11-17 | 2023-07-24 | 엥방티바 | 간 질환의 치료를 위한 병용 요법 |
| KR20240131458A (ko) * | 2020-11-17 | 2024-08-30 | 엥방티바 | 간 질환의 치료를 위한 병용 요법 |
Also Published As
| Publication number | Publication date |
|---|---|
| EP3242722A1 (en) | 2017-11-15 |
| EP3242722A4 (en) | 2018-07-11 |
| HK1243369A1 (zh) | 2018-07-13 |
| CN107106873A (zh) | 2017-08-29 |
| AU2016205138A1 (en) | 2017-07-13 |
| US20180021341A1 (en) | 2018-01-25 |
| WO2016112305A1 (en) | 2016-07-14 |
| CA2972919A1 (en) | 2016-07-14 |
| MX2017008844A (es) | 2018-03-14 |
| HK1246232A1 (zh) | 2018-09-07 |
| EP3597271A1 (en) | 2020-01-22 |
| JP2020109130A (ja) | 2020-07-16 |
| EA201892625A1 (ru) | 2019-07-31 |
| US20190381045A1 (en) | 2019-12-19 |
| SG11201705361PA (en) | 2017-08-30 |
| BR112017014341A2 (pt) | 2018-03-27 |
| EA201791258A1 (ru) | 2017-12-29 |
| JP2018501276A (ja) | 2018-01-18 |
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