JP6983225B2 - 窒素含有三環式化合物、および医薬におけるその使用 - Google Patents
窒素含有三環式化合物、および医薬におけるその使用 Download PDFInfo
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- JP6983225B2 JP6983225B2 JP2019506117A JP2019506117A JP6983225B2 JP 6983225 B2 JP6983225 B2 JP 6983225B2 JP 2019506117 A JP2019506117 A JP 2019506117A JP 2019506117 A JP2019506117 A JP 2019506117A JP 6983225 B2 JP6983225 B2 JP 6983225B2
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- 0 C*c(cc1*)c(*)c(*)c1Ic1n[o]c(I)c1C Chemical compound C*c(cc1*)c(*)c(*)c1Ic1n[o]c(I)c1C 0.000 description 10
- ASCAIQNTTTXVOU-UHFFFAOYSA-N C=NC1=Cc2ccccc2Oc(cc2)c1nc2ON Chemical compound C=NC1=Cc2ccccc2Oc(cc2)c1nc2ON ASCAIQNTTTXVOU-UHFFFAOYSA-N 0.000 description 1
- ACQLAZWSLWBDRC-UHFFFAOYSA-N OC(c1cc(F)c(CCc2nc(OCc3c(C4CC4)[o]nc3-c(c(Cl)ccc3)c3Cl)ccc2O2)c2c1)=O Chemical compound OC(c1cc(F)c(CCc2nc(OCc3c(C4CC4)[o]nc3-c(c(Cl)ccc3)c3Cl)ccc2O2)c2c1)=O ACQLAZWSLWBDRC-UHFFFAOYSA-N 0.000 description 1
- ZSULLEPJCHLLGN-UHFFFAOYSA-N OC(c1cc(Oc(c(CC2)n3)ccc3OCc3c(C4CC4)[o]nc3-c(c(Cl)ccc3)c3Cl)c2cc1F)=O Chemical compound OC(c1cc(Oc(c(CC2)n3)ccc3OCc3c(C4CC4)[o]nc3-c(c(Cl)ccc3)c3Cl)c2cc1F)=O ZSULLEPJCHLLGN-UHFFFAOYSA-N 0.000 description 1
- SKYRJSUNKSZONZ-UHFFFAOYSA-N OC(c1ccc(C2=C=C2c(nc(cc2)OCc3c(C4CC4)[o]nc3-c(c(Cl)ccc3)c3Cl)c2O2)c2c1)=O Chemical compound OC(c1ccc(C2=C=C2c(nc(cc2)OCc3c(C4CC4)[o]nc3-c(c(Cl)ccc3)c3Cl)c2O2)c2c1)=O SKYRJSUNKSZONZ-UHFFFAOYSA-N 0.000 description 1
Classifications
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- 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
-
- 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
- A61K31/41—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
- A61K31/4164—1,3-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
- A61K31/41—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
- A61K31/42—Oxazoles
-
- 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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
- A61P5/50—Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
-
- 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
-
- 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
- A61P9/12—Antihypertensives
-
- 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
-
- 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
- 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
- C07D491/056—Ortho-condensed systems with two or more oxygen atoms as ring hetero atoms 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
- C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Cardiology (AREA)
- Epidemiology (AREA)
- Diabetes (AREA)
- Heart & Thoracic Surgery (AREA)
- Endocrinology (AREA)
- Hematology (AREA)
- Hospice & Palliative Care (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
- Reproductive Health (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610640043.5 | 2016-08-05 | ||
| CN201610640043 | 2016-08-05 | ||
| PCT/CN2017/095724 WO2018024224A1 (en) | 2016-08-05 | 2017-08-02 | Nitrogen-containing tricyclic compounds and uses thereof in medicine |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019524784A JP2019524784A (ja) | 2019-09-05 |
| JP2019524784A5 JP2019524784A5 (enExample) | 2020-07-30 |
| JP6983225B2 true JP6983225B2 (ja) | 2021-12-17 |
Family
ID=61072781
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019506117A Active JP6983225B2 (ja) | 2016-08-05 | 2017-08-02 | 窒素含有三環式化合物、および医薬におけるその使用 |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US10562910B2 (enExample) |
| EP (1) | EP3494118B1 (enExample) |
| JP (1) | JP6983225B2 (enExample) |
| KR (1) | KR102368298B1 (enExample) |
| CN (1) | CN107686486B (enExample) |
| AR (1) | AR109295A1 (enExample) |
| AU (1) | AU2017306605B2 (enExample) |
| CA (1) | CA3030377C (enExample) |
| ES (1) | ES2950412T3 (enExample) |
| TW (1) | TW201808283A (enExample) |
| WO (1) | WO2018024224A1 (enExample) |
Families Citing this family (34)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2545964A1 (en) | 2011-07-13 | 2013-01-16 | Phenex Pharmaceuticals AG | Novel FXR (NR1H4) binding and activity modulating compounds |
| WO2016057549A1 (en) | 2014-10-06 | 2016-04-14 | Aurasense Therapeutics, Llc | Anti-tnf compounds |
| NZ735126A (en) | 2015-03-31 | 2022-10-28 | Enanta Pharm Inc | Bile acid derivatives as fxr/tgr5 agonists and methods of use thereof |
| CA3026512A1 (en) | 2016-06-13 | 2017-12-21 | Gilead Sciences, Inc. | Fxr (nr1h4) modulating compounds |
| CA2968836C (en) | 2016-06-13 | 2025-09-02 | Gilead Sciences Inc | Fxr (nr1h4) modulating compounds |
| JP2019537557A (ja) | 2016-10-04 | 2019-12-26 | エナンタ ファーマシューティカルズ インコーポレイテッド | Ｆｘｒアゴニストとしてのイソキサゾール類似体およびその使用方法 |
| US10597391B2 (en) | 2016-10-26 | 2020-03-24 | Enanta Pharmaceuticals, Inc. | Urea-containing isoxazole derivatives as FXR agonists and methods of use thereof |
| EP4122464B1 (en) | 2017-03-28 | 2024-05-15 | Gilead Sciences, Inc. | Therapeutic combinations for treating liver diseases |
| AU2018360575A1 (en) * | 2017-11-01 | 2020-06-18 | Bristol-Myers Squibb Company | Alkene spirocyclic compounds as farnesoid X receptor modulators |
| US10689391B2 (en) | 2017-12-12 | 2020-06-23 | 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 |
| WO2019160813A1 (en) | 2018-02-14 | 2019-08-22 | Enanta Pharmaceuticals, Inc. | Isoxazole derivatives as fxr agonists and methods of use thereof |
| LT3911647T (lt) | 2019-01-15 | 2024-03-25 | Gilead Sciences, Inc. | Izoksazolo junginys kaip fxr agonistas ir jį apimančios farmacinės kompozicijos |
| CA3129949C (en) | 2019-02-19 | 2024-04-30 | Gilead Sciences, Inc. | Solid forms of fxr agonists |
| US11555032B2 (en) | 2019-05-13 | 2023-01-17 | Enanta Pharmaceuticals, Inc. | Isoxazole derivatives as FXR agonists and methods of use thereof |
| CN110028443B (zh) * | 2019-05-29 | 2022-03-04 | 济南周行医药科技有限公司 | 一种调节fxr活性的三环化合物类药物中间体的制备方法 |
| WO2021014349A1 (en) | 2019-07-23 | 2021-01-28 | Novartis Ag | Treatment comprising fxr agonists |
| TW202114672A (zh) | 2019-07-23 | 2021-04-16 | 瑞士商諾華公司 | 使用fxr促效劑的肝臟疾病之組合治療 |
| MX2022002636A (es) | 2019-09-03 | 2022-03-25 | Novartis Ag | Tratamiento de la enfermedad o trastorno hepatico que comprende los antagonistas del receptor de actrii. |
| US20220347190A1 (en) | 2019-09-19 | 2022-11-03 | Novartis Ag | Treatment comprising fxr agonists |
| JP2022550312A (ja) | 2019-09-30 | 2022-12-01 | ノバルティス アーゲー | Ｆｘｒアゴニストの使用を含む処置 |
| JP7750836B2 (ja) * | 2019-11-29 | 2025-10-07 | ▲広▼▲東▼▲東▼▲陽▼光▲薬▼▲業▼有限公司 | 三環式含窒素化合物の非晶質及びその用途 |
| CN112876493B (zh) * | 2019-11-29 | 2023-05-09 | 广东东阳光药业有限公司 | 含氮三环化合物的盐及其用途 |
| CN112876490A (zh) * | 2019-11-29 | 2021-06-01 | 广东东阳光药业有限公司 | 含氮三环化合物的晶型及其用途 |
| JP2023505116A (ja) * | 2019-11-29 | 2023-02-08 | ▲広▼▲東▼▲東▼▲陽▼光▲薬▼▲業▼有限公司 | 三環式含窒素化合物の結晶形及びその用途 |
| IL293894A (en) | 2019-12-20 | 2022-08-01 | Novartis Ag | Combination treatment of liver diseases using integrin inhibitors |
| WO2022101853A1 (en) | 2020-11-16 | 2022-05-19 | Novartis Ag | Method of determining liver fibrosis |
| CN115974885A (zh) * | 2021-10-15 | 2023-04-18 | 广东东阳光药业有限公司 | 含氮三环化合物的新晶型及其用途 |
| WO2023061477A1 (zh) | 2021-10-15 | 2023-04-20 | 广东东阳光药业有限公司 | 含氮三环化合物的新晶型及其用途 |
| CN115974884A (zh) * | 2021-10-15 | 2023-04-18 | 广东东阳光药业有限公司 | 含氮三环化合物的新晶型及其用途 |
| CN115974887A (zh) * | 2021-10-15 | 2023-04-18 | 广东东阳光药业有限公司 | 含氮三环化合物的新晶型及其用途 |
| WO2024140868A1 (zh) * | 2022-12-30 | 2024-07-04 | 广东东阳光药业股份有限公司 | 三环化合物的晶型及其用途 |
| CN118772166A (zh) * | 2023-04-10 | 2024-10-15 | 广东东阳光药业股份有限公司 | 含氮三环化合物的新晶型及其用途 |
| CN119320393A (zh) * | 2023-07-17 | 2025-01-17 | 上海枢境生物科技有限公司 | 双环[5,6]咪唑嘧啶酮类衍生物、其制备方法和应用 |
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| EP1285914B1 (en) | 2001-08-13 | 2007-12-19 | PheneX Pharmaceuticals AG | Nr1h4 nuclear receptor binding compounds |
| AU2003290700A1 (en) | 2002-11-22 | 2004-06-18 | Smithkline Beecham Corporation | Farnesoid x receptor agonists |
| ATE526318T1 (de) | 2005-12-19 | 2011-10-15 | Glaxosmithkline Llc | Farnesoid-x-rezeptor-agonisten |
| EP1984360B1 (en) | 2006-02-03 | 2014-01-15 | Eli Lilly & Company | Compounds and methods for modulating FX-receptors |
| JP2007230909A (ja) | 2006-03-01 | 2007-09-13 | Univ Of Tokyo | 置換イソキサゾール誘導体 |
| ATE460403T1 (de) | 2006-05-24 | 2010-03-15 | Lilly Co Eli | Verbindungen und verfahren zur modulierung von fx-rezeptoren |
| PL2029547T3 (pl) * | 2006-05-24 | 2010-09-30 | Lilly Co Eli | Agoniści FXR |
| EP1894924A1 (en) * | 2006-08-29 | 2008-03-05 | Phenex Pharmaceuticals AG | Heterocyclic FXR binding compounds |
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| CL2007003035A1 (es) | 2006-10-24 | 2008-05-16 | Smithkline Beechman Corp | Compuestos derivados de isoxazol sustituidos, agonistas de receptores farnesoid x; procedimiento de preparacion; composicion farmaceutica que lo comprende; y uso del compuesto en el tratamiento de la obesidad, diabetes mellitus, fibrosis en organos, |
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| JP2019524784A (ja) | 2019-09-05 |
| ES2950412T3 (es) | 2023-10-09 |
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