JP7174709B2 - ファルネソイドx受容体アゴニストおよびその使用 - Google Patents
ファルネソイドx受容体アゴニストおよびその使用 Download PDFInfo
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- JP7174709B2 JP7174709B2 JP2019547662A JP2019547662A JP7174709B2 JP 7174709 B2 JP7174709 B2 JP 7174709B2 JP 2019547662 A JP2019547662 A JP 2019547662A JP 2019547662 A JP2019547662 A JP 2019547662A JP 7174709 B2 JP7174709 B2 JP 7174709B2
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- substituted
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Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three 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
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- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/415—1,2-Diazoles
-
- 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0014—Skin, i.e. galenical aspects of topical compositions
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
- A61K9/0029—Parenteral nutrition; Parenteral nutrition compositions as drug carriers
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/06—Ointments; Bases therefor; Other semi-solid forms, e.g. creams, sticks, gels
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4841—Filling excipients; Inactive ingredients
- A61K9/4866—Organic macromolecular compounds
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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
-
- 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
-
- 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
- C07D401/12—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
- 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
- C07D403/12—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 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
- C07D405/02—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
- C07D405/02—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
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Nutrition Science (AREA)
- Dermatology (AREA)
- Gastroenterology & Hepatology (AREA)
- Physiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762471517P | 2017-03-15 | 2017-03-15 | |
| US62/471,517 | 2017-03-15 | ||
| PCT/US2018/022489 WO2018170166A1 (en) | 2017-03-15 | 2018-03-14 | Farnesoid x receptor agonists and uses thereof |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2020514333A JP2020514333A (ja) | 2020-05-21 |
| JP2020514333A5 JP2020514333A5 (enExample) | 2021-04-15 |
| JP7174709B2 true JP7174709B2 (ja) | 2022-11-17 |
Family
ID=63522667
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019547662A Active JP7174709B2 (ja) | 2017-03-15 | 2018-03-14 | ファルネソイドx受容体アゴニストおよびその使用 |
Country Status (10)
| Country | Link |
|---|---|
| US (3) | US10961198B2 (enExample) |
| EP (1) | EP3596053B1 (enExample) |
| JP (1) | JP7174709B2 (enExample) |
| CN (1) | CN110637011B (enExample) |
| AR (1) | AR111284A1 (enExample) |
| CA (1) | CA3055990A1 (enExample) |
| DK (1) | DK3596053T3 (enExample) |
| IL (1) | IL269068B (enExample) |
| TW (1) | TWI803482B (enExample) |
| WO (1) | WO2018170166A1 (enExample) |
Families Citing this family (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3350166A4 (en) | 2015-09-16 | 2019-05-01 | Metacrine, Inc. | FARNESOID-X RECEPTOR AGONISTS AND USES THEREOF |
| US10626081B2 (en) | 2015-09-16 | 2020-04-21 | Metacrine, Inc. | Farnesoid X receptor agonists and uses thereof |
| EP3350165B1 (en) | 2015-09-16 | 2023-07-26 | Organovo, Inc. | Farnesoid x receptor agonists and uses thereof |
| AU2018236275B2 (en) | 2017-03-15 | 2022-05-12 | Eli Lilly And Company | Farnesoid X receptor agonists and uses thereof |
| DK3596053T3 (da) | 2017-03-15 | 2023-09-25 | Organovo Inc | Farnesoid-x-receptoragonister og anvendelser deraf |
| US11286252B2 (en) | 2017-11-01 | 2022-03-29 | Bristol-Myers Squibb Company | Alkene spirocyclic compounds as farnesoid X receptor modulators |
| KR102731925B1 (ko) | 2017-11-01 | 2024-11-18 | 브리스톨-마이어스 스큅 컴퍼니 | 파르네소이드 x 수용체 조정제로서의 멀티시클릭 화합물 |
| JP7478142B2 (ja) | 2018-06-07 | 2024-05-02 | ディスアーム セラピューティクス, インコーポレイテッド | Sarm1阻害剤 |
| US20220047553A1 (en) * | 2018-09-18 | 2022-02-17 | Metacrine, Inc. | Farnesoid x receptor agonists for the treatment of disease |
| EP3852748B1 (en) | 2018-09-18 | 2025-09-03 | Eli Lilly and Company | Farnesoid x receptor agonists and uses thereof |
| AU2019387370A1 (en) | 2018-11-30 | 2021-06-10 | Nuvation Bio Inc. | Pyrrole and pyrazole compounds and methods of use thereof |
| CA3123215C (en) | 2018-12-19 | 2024-04-02 | Disarm Therapeutics, Inc. | Inhibitors of sarm1 in combination with neuroprotective agents |
| US12319676B2 (en) | 2019-02-15 | 2025-06-03 | Bristol-Myers Squibb Company | Substituted amide compounds useful as farnesoid X receptor modulators |
| AR118050A1 (es) * | 2019-02-15 | 2021-09-15 | Bristol Myers Squibb Co | Compuestos bicíclicos sustituidos como moduladores del receptor farnesoide x |
| JP7449300B2 (ja) * | 2019-02-15 | 2024-03-13 | ブリストル-マイヤーズ スクイブ カンパニー | ファルネソイドx受容体モジュレータとして有用な置換アミド化合物 |
| JP7465883B2 (ja) * | 2019-02-15 | 2024-04-11 | ブリストル-マイヤーズ スクイブ カンパニー | ファルネソイドx受容体モジュレータとしての置換二環式化合物 |
| MX2021009570A (es) * | 2019-02-15 | 2021-09-08 | Bristol Myers Squibb Co | Compuestos biciclicos sustituidos como moduladores del receptor de farnesoide x. |
| WO2021009332A1 (en) | 2019-07-18 | 2021-01-21 | Enyo Pharma | Method for decreasing adverse-effects of interferon |
| 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 |
| JP7664278B2 (ja) * | 2020-03-18 | 2025-04-17 | オルガノボ,インク. | ファルネソイドx受容体アゴニストの結晶質形態 |
| KR20220154801A (ko) * | 2020-03-18 | 2022-11-22 | 메타크린, 인크. | 질환의 치료를 위한 파르네소이드 x 수용체 작용제 |
| WO2021188690A1 (en) * | 2020-03-18 | 2021-09-23 | Metacrine, Inc. | Farnesoid x receptor agonists for the treatment of disease |
| CN120227340A (zh) * | 2020-03-18 | 2025-07-01 | 伊莱利利公司 | 法尼醇x受体激动剂的制剂 |
| MX2023008365A (es) | 2021-01-14 | 2023-10-04 | Enyo Pharma | Efecto sinérgico de un agonista de fxr e ifn para el tratamiento de infección por hbv. |
| TW202308629A (zh) | 2021-04-28 | 2023-03-01 | 法商Enyo製藥公司 | 使用fxr激動劑作為組合治療以增強tlr3激動劑之療效 |
Citations (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2004046162A2 (en) | 2002-11-14 | 2004-06-03 | The Scripps Research Institute | Non-steroidal fxr agonists |
| WO2004045511A2 (en) | 2002-11-15 | 2004-06-03 | The Salk Institute For Biological Studies | Non-steroidal farnesoid x receptor modulators |
| WO2015138969A1 (en) | 2014-03-13 | 2015-09-17 | Salk Institute For Biological Studies | Analogs of fexaramine and methods of making and using |
| WO2016149111A1 (en) | 2015-03-13 | 2016-09-22 | Salk Institute For Biological Studies | Treating latent autoimmune diabetes of adults with farnesoid x receptor agonists to activate intestinal receptors |
| WO2018170182A1 (en) | 2017-03-15 | 2018-09-20 | Metacrine, Inc. | Farnesoid x receptor agonists and uses thereof |
| JP6905530B2 (ja) | 2015-09-16 | 2021-07-21 | メタクリン,インク. | ファルネソイドx受容体アゴニストとその使用 |
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| AU4537900A (en) | 1999-05-17 | 2000-12-05 | Agouron Pharmaceuticals, Inc. | Glucagon antagonists/inverse agonists |
| EP1187810A2 (en) | 1999-05-25 | 2002-03-20 | Sepracor, Inc. | Heterocyclic analgesic compounds and their use |
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| FR2815032B1 (fr) | 2000-10-10 | 2003-08-08 | Pf Medicament | Nouveaux derives d'aminophenyle piperazine ou d'amino phenyle piperide inhibiteurs de proteines prenyl transferase ainsi que leurs preparations |
| FR2825706B1 (fr) | 2001-06-06 | 2003-12-12 | Pf Medicament | Nouveaux derives de benzothienyle ou d'indole, leur preparation et leur utilisation comme inhibiteurs de proteines prenyl transferase |
| FR2839974B1 (fr) | 2002-05-24 | 2004-07-16 | Pf Medicament | Derives de phenyl-furane ou de phenyl-thiophene,leur preparation et leur application a titre de medicament |
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| WO2004046323A2 (en) | 2002-11-15 | 2004-06-03 | The Salk Institute For Biological Studies | Structure of the farnesoid x receptor ligand binding domain and methods of use therefor |
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| RU2543485C2 (ru) | 2013-02-26 | 2015-03-10 | Андрей Александрович Иващенко | Гетероциклические агонисты рецепторов желчных кислот tgr5, фармацевтическая композиция, способы их получения и применения |
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| US20150258052A1 (en) | 2014-03-13 | 2015-09-17 | Salk Institute For Biological Studies | Methods of using fexaramine and agents that increase sympathetic nervous system activity to promote browning of white adipose tissue |
| US10301268B2 (en) | 2014-03-13 | 2019-05-28 | The Salk Institute For Biological Studies | Analogs of fexaramine and methods of making and using |
| US20180116993A1 (en) | 2015-01-22 | 2018-05-03 | Xiamen University | Modulators of farnesoid x receptor and methods for the use thereof |
| WO2017018751A1 (ko) | 2015-07-24 | 2017-02-02 | 동국대학교 산학협력단 | Blt 저해 활성을 갖는 신규 화합물 및 이를 유효성분으로 포함하는 염증성 질환 예방 또는 치료용 조성물 |
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2018
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| WO2004045511A2 (en) | 2002-11-15 | 2004-06-03 | The Salk Institute For Biological Studies | Non-steroidal farnesoid x receptor modulators |
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| WO2018170182A1 (en) | 2017-03-15 | 2018-09-20 | Metacrine, Inc. | Farnesoid x receptor agonists and uses thereof |
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| IL269068A (en) | 2019-11-28 |
| EP3596053B1 (en) | 2023-08-16 |
| US20200290973A1 (en) | 2020-09-17 |
| CN110637011A (zh) | 2019-12-31 |
| AR111284A1 (es) | 2019-06-26 |
| EP3596053A1 (en) | 2020-01-22 |
| CN110637011B (zh) | 2024-05-14 |
| TW201843149A (zh) | 2018-12-16 |
| US20200131134A1 (en) | 2020-04-30 |
| US20210300875A1 (en) | 2021-09-30 |
| US10961198B2 (en) | 2021-03-30 |
| US10927082B2 (en) | 2021-02-23 |
| WO2018170166A1 (en) | 2018-09-20 |
| JP2020514333A (ja) | 2020-05-21 |
| CA3055990A1 (en) | 2018-09-20 |
| TWI803482B (zh) | 2023-06-01 |
| DK3596053T3 (da) | 2023-09-25 |
| EP3596053A4 (en) | 2020-09-02 |
| IL269068B (en) | 2022-09-01 |
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