PH12019550050A1 - Isoxazole analogs as fxr agonists and methods of use thereof - Google Patents
Isoxazole analogs as fxr agonists and methods of use thereofInfo
- Publication number
- PH12019550050A1 PH12019550050A1 PH12019550050A PH12019550050A PH12019550050A1 PH 12019550050 A1 PH12019550050 A1 PH 12019550050A1 PH 12019550050 A PH12019550050 A PH 12019550050A PH 12019550050 A PH12019550050 A PH 12019550050A PH 12019550050 A1 PH12019550050 A1 PH 12019550050A1
- Authority
- PH
- Philippines
- Prior art keywords
- methods
- fxr agonists
- isoxazole
- analogs
- isoxazole analogs
- Prior art date
Links
Classifications
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- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/439—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring forming part of a bridged ring system, e.g. quinuclidine
-
- 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
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- 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
- 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
- A61P3/08—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
-
- 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
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
-
- 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
- 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
- C07D261/08—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 only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
-
- 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
- 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
- C07D417/14—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 three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
- C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
- C07D451/04—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof with hetero atoms directly attached in position 3 of the 8-azabicyclo [3.2.1] octane or in position 7 of the 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring system
-
- 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
- C07D487/08—Bridged systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/04—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Diabetes (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Gastroenterology & Hepatology (AREA)
- Urology & Nephrology (AREA)
- Epidemiology (AREA)
- Child & Adolescent Psychology (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Hospice & Palliative Care (AREA)
- Vascular Medicine (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)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662404059P | 2016-10-04 | 2016-10-04 | |
| PCT/US2017/055147 WO2018067704A1 (en) | 2016-10-04 | 2017-10-04 | Isoxazole analogs as fxr agonists and methods of use thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PH12019550050A1 true PH12019550050A1 (en) | 2019-07-24 |
Family
ID=61830059
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PH12019550050A PH12019550050A1 (en) | 2016-10-04 | 2019-03-28 | Isoxazole analogs as fxr agonists and methods of use thereof |
Country Status (13)
| Country | Link |
|---|---|
| US (2) | US10450306B2 (https=) |
| EP (1) | EP3523298A4 (https=) |
| JP (1) | JP2019537557A (https=) |
| KR (1) | KR20190056436A (https=) |
| CN (1) | CN109906223A (https=) |
| AU (1) | AU2017338853A1 (https=) |
| BR (1) | BR112019006651A2 (https=) |
| CA (1) | CA3039124A1 (https=) |
| IL (1) | IL265803A (https=) |
| MX (1) | MX2019003790A (https=) |
| PH (1) | PH12019550050A1 (https=) |
| RU (1) | RU2019113066A (https=) |
| WO (1) | WO2018067704A1 (https=) |
Families Citing this family (51)
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|---|---|---|---|---|
| EP2545964A1 (en) | 2011-07-13 | 2013-01-16 | Phenex Pharmaceuticals AG | Novel FXR (NR1H4) binding and activity modulating compounds |
| US10208081B2 (en) | 2014-11-26 | 2019-02-19 | Enanta Pharmaceuticals, Inc. | Bile acid derivatives as FXR/TGR5 agonists and methods of use thereof |
| WO2016161003A1 (en) | 2015-03-31 | 2016-10-06 | Enanta Phamraceuticals, Inc. | Bile acid derivatives as fxr/tgr5 agonists and methods of use thereof |
| WO2017189651A1 (en) | 2016-04-26 | 2017-11-02 | Enanta Pharmaceuticals, Inc. | Isoxazole derivatives as fxr agonists and methods of use thereof |
| WO2017189663A1 (en) | 2016-04-26 | 2017-11-02 | Enanta Pharmaceuticals, Inc. | Isoxazole derivatives as fxr agonists and methods of use thereof |
| US10080741B2 (en) | 2016-04-26 | 2018-09-25 | Enanta Pharmaceuticals, Inc. | Isoxazole derivatives as FXR agonists and methods of use thereof |
| WO2017201152A1 (en) | 2016-05-18 | 2017-11-23 | Enanta Pharmaceuticals, Inc. | Isoxazole derivatives as fxr agonists and methods of use thereof |
| WO2017201150A1 (en) | 2016-05-18 | 2017-11-23 | Enanta Pharmaceuticals, Inc. | Isoxazole analogs as fxr agonists and methods of use thereof |
| WO2017201155A1 (en) | 2016-05-18 | 2017-11-23 | Enanta Pharmaceuticals, Inc. | lSOXAZOLE DERIVATIVES AS FXR AGONISTS AND METHODS OF USE THEREOF |
| MX385718B (es) | 2016-06-13 | 2025-03-18 | Gilead Sciences Inc | Compuestos moduladores de fxr (nr1h4). |
| CA3252823A1 (en) | 2016-06-13 | 2025-02-25 | Gilead Sciences, Inc. | Substituted tert-butyl-3-(2-chloro-phenyl)-3-hydroxyazetidine-1-carboxylate compounds |
| TW201808283A (zh) | 2016-08-05 | 2018-03-16 | 廣東東陽光藥業有限公司 | 含氮三環化合物及其在藥物中的應用 |
| US10450306B2 (en) | 2016-10-04 | 2019-10-22 | Enanta Pharmaceuticals, Inc. | Isoxazole analogs as FXR agonists and methods of use thereof |
| WO2018081285A1 (en) | 2016-10-26 | 2018-05-03 | Enanta Pharmaceuticals, Inc. | Urea-containing isoxazole derivatives as fxr agonists and methods of use thereof |
| CN108017636A (zh) * | 2016-11-04 | 2018-05-11 | 合帕吉恩治疗公司 | 作为fxr调节剂的含氮杂环化合物 |
| PT3600309T (pt) | 2017-03-28 | 2022-10-03 | Gilead Sciences Inc | Combinações terapêuticas para o tratamento de doenças hepáticas |
| WO2019118571A1 (en) | 2017-12-12 | 2019-06-20 | Enanta Pharmaceuticals, Inc. | Isoxazole analogs as fxr agonists and methods of use thereof |
| CN110128432B (zh) | 2018-02-02 | 2021-03-02 | 广东东阳光药业有限公司 | 含氮三环化合物及其在药物中的应用 |
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| WO2020029908A1 (zh) * | 2018-08-08 | 2020-02-13 | 广州市恒诺康医药科技有限公司 | 螺桥环化合物、其药物组合物及其用途 |
| WO2020114307A1 (zh) * | 2018-12-07 | 2020-06-11 | 四川科伦博泰生物医药股份有限公司 | 异噁唑衍生物及其制备方法和用途 |
| EP3911647B1 (en) | 2019-01-15 | 2023-12-13 | Gilead Sciences, Inc. | Isoxazole compound as fxr agonist and pharmaceutical compositions comprising same |
| KR20210123337A (ko) * | 2019-01-31 | 2021-10-13 | 더 내셔널 인스티튜츠 오브 파마슈티컬 알앤디 컴퍼니 리미티드 | 방향족 고리 또는 헤테로방향족 고리 화합물, 이의 제조 방법 및 이의 의학 용도 |
| CA3233305A1 (en) | 2019-02-19 | 2020-08-27 | Gilead Sciences, Inc. | Solid forms of fxr agonists |
| CN111825595A (zh) * | 2019-04-15 | 2020-10-27 | 山东轩竹医药科技有限公司 | 钠通道阻滞剂 |
| US12528796B2 (en) | 2019-04-15 | 2026-01-20 | Tosk, Inc. | Modulators of RAS GTPase |
| KR20250076664A (ko) | 2019-04-19 | 2025-05-29 | 상하이 인스티튜트 오브 마테리아 메디카 차이니즈 아카데미 오브 싸이언시즈 | Fxr 소분자 작용제 및 이의 제조 방법과 용도 |
| WO2020231917A1 (en) | 2019-05-13 | 2020-11-19 | Enanta Pharmaceuticals, Inc. | Isoxazole derivatives as fxr agonists and methods of use thereof |
| KR20220035365A (ko) | 2019-07-18 | 2022-03-22 | 엔요 파마 | 인터페론의 부작용을 감소시키는 방법 |
| KR20220038368A (ko) | 2019-07-23 | 2022-03-28 | 노파르티스 아게 | Fxr 작용제를 이용하는 간 질환의 병용 치료 |
| WO2021014349A1 (en) | 2019-07-23 | 2021-01-28 | Novartis Ag | Treatment comprising fxr agonists |
| JP7663559B2 (ja) | 2019-09-03 | 2025-04-16 | ノバルティス アーゲー | Ａｃｔｒｉｉ受容体拮抗薬を含む肝疾患または肝臓障害の治療 |
| CN114401745A (zh) | 2019-09-19 | 2022-04-26 | 诺华股份有限公司 | 包含fxr激动剂的治疗 |
| WO2021064575A1 (en) | 2019-09-30 | 2021-04-08 | Novartis Ag | Treatment comprising the use of fxr agonists |
| CN110804025B (zh) * | 2019-11-29 | 2022-02-08 | 扬州工业职业技术学院 | 一种卤代苯异噁唑衍生物及其制备方法与应用 |
| KR20220119424A (ko) | 2019-12-20 | 2022-08-29 | 노파르티스 아게 | 인테그린 억제제를 사용한 간 질환의 조합 치료 |
| IL293892A (en) | 2020-01-15 | 2022-08-01 | Inserm Institut National De La Sant? Et De La Rech M?Dicale | Use of fxr agonists for treating an infection by hepatitis d virus |
| TW202208355A (zh) | 2020-05-04 | 2022-03-01 | 美商安進公司 | 作為骨髓細胞觸發受體2促效劑之雜環化合物及使用方法 |
| PE20230609A1 (es) | 2020-05-04 | 2023-04-13 | Amgen Inc | Compuestos heterociclicos como agonistas del receptor de activacion expresado en las celulas mieloides 2 y metodos de uso |
| CN114195786B (zh) * | 2020-09-18 | 2023-08-22 | 凯思凯迪（上海）医药科技有限公司 | 新型fxr小分子激动剂制备及其用途 |
| CN114315830B (zh) * | 2020-09-30 | 2025-08-12 | 中国科学院上海药物研究所 | Fxr小分子激动剂及其制备方法和用途 |
| US12180220B2 (en) | 2020-10-14 | 2024-12-31 | Tosk, Inc. | Heteroaryl modulators of RAS GTPase |
| US20220112178A1 (en) * | 2020-10-14 | 2022-04-14 | Tosk, Inc. | Small Molecule Modulators of RAS GTPase |
| WO2022101853A1 (en) | 2020-11-16 | 2022-05-19 | Novartis Ag | Method of determining liver fibrosis |
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| JP2024502673A (ja) | 2021-01-14 | 2024-01-22 | ウエヌイグレックオ・ファーマ | Ｈｂｖ感染の処置のためのｆｘｒアゴニストとｉｆｎの相乗効果 |
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2017
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- 2017-10-04 CA CA3039124A patent/CA3039124A1/en not_active Abandoned
- 2017-10-04 KR KR1020197012682A patent/KR20190056436A/ko not_active Withdrawn
- 2017-10-04 RU RU2019113066A patent/RU2019113066A/ru not_active Application Discontinuation
- 2017-10-04 CN CN201780068563.6A patent/CN109906223A/zh active Pending
- 2017-10-04 AU AU2017338853A patent/AU2017338853A1/en not_active Abandoned
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- 2017-10-04 EP EP17859120.2A patent/EP3523298A4/en not_active Withdrawn
- 2017-10-04 WO PCT/US2017/055147 patent/WO2018067704A1/en not_active Ceased
- 2017-10-04 MX MX2019003790A patent/MX2019003790A/es unknown
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| BR112019006651A2 (pt) | 2019-07-02 |
| US10450306B2 (en) | 2019-10-22 |
| MX2019003790A (es) | 2019-09-26 |
| CA3039124A1 (en) | 2018-04-12 |
| WO2018067704A1 (en) | 2018-04-12 |
| US20180099957A1 (en) | 2018-04-12 |
| RU2019113066A (ru) | 2020-11-09 |
| US11034684B2 (en) | 2021-06-15 |
| KR20190056436A (ko) | 2019-05-24 |
| EP3523298A1 (en) | 2019-08-14 |
| JP2019537557A (ja) | 2019-12-26 |
| EP3523298A4 (en) | 2020-06-24 |
| US20200079764A1 (en) | 2020-03-12 |
| AU2017338853A1 (en) | 2019-04-18 |
| IL265803A (en) | 2019-06-30 |
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