AR114290A1 - Péptidos macrocíclicos contra actinetobacter baumannii - Google Patents
Péptidos macrocíclicos contra actinetobacter baumanniiInfo
- Publication number
- AR114290A1 AR114290A1 ARP190101064A ARP190101064A AR114290A1 AR 114290 A1 AR114290 A1 AR 114290A1 AR P190101064 A ARP190101064 A AR P190101064A AR P190101064 A ARP190101064 A AR P190101064A AR 114290 A1 AR114290 A1 AR 114290A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- formula
- pharmaceutically acceptable
- compound
- carboxy
- Prior art date
Links
- 102000004196 processed proteins & peptides Human genes 0.000 title 1
- 108090000765 processed proteins & peptides Proteins 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 10
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 6
- 150000003839 salts Chemical class 0.000 abstract 5
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 3
- 229910052739 hydrogen Inorganic materials 0.000 abstract 3
- 239000001257 hydrogen Substances 0.000 abstract 3
- 239000008194 pharmaceutical composition Substances 0.000 abstract 3
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 2
- 125000004103 aminoalkyl group Chemical group 0.000 abstract 2
- 201000010099 disease Diseases 0.000 abstract 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 2
- 229910052736 halogen Inorganic materials 0.000 abstract 2
- 150000002367 halogens Chemical group 0.000 abstract 2
- 150000002431 hydrogen Chemical group 0.000 abstract 2
- 208000015181 infectious disease Diseases 0.000 abstract 2
- 125000004739 (C1-C6) alkylsulfonyl group Chemical group 0.000 abstract 1
- IHWDSEPNZDYMNF-UHFFFAOYSA-N 1H-indol-2-amine Chemical compound C1=CC=C2NC(N)=CC2=C1 IHWDSEPNZDYMNF-UHFFFAOYSA-N 0.000 abstract 1
- 241000588626 Acinetobacter baumannii Species 0.000 abstract 1
- 241000894006 Bacteria Species 0.000 abstract 1
- 239000002253 acid Substances 0.000 abstract 1
- 150000001732 carboxylic acid derivatives Chemical class 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 229940079593 drug Drugs 0.000 abstract 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 239000000546 pharmaceutical excipient Substances 0.000 abstract 1
- 230000002265 prevention Effects 0.000 abstract 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
- A61K38/12—Cyclic peptides, e.g. bacitracins; Polymyxins; Gramicidins S, C; Tyrocidins A, B or C
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/08—Tripeptides
- C07K5/0815—Tripeptides with the first amino acid being basic
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
- A61K38/06—Tripeptides
-
- 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
-
- 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
- A61P31/04—Antibacterial agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K1/00—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length
- C07K1/06—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length using protecting groups or activating agents
- C07K1/061—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length using protecting groups or activating agents using protecting groups
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/06—Dipeptides
- C07K5/06086—Dipeptides with the first amino acid being basic
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/08—Tripeptides
- C07K5/0819—Tripeptides with the first amino acid being acidic
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Molecular Biology (AREA)
- Genetics & Genomics (AREA)
- Biophysics (AREA)
- Biochemistry (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Immunology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Gastroenterology & Hepatology (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Analytical Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Peptides Or Proteins (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
La presente proporciona compuestos de fórmula (1), en la que X¹, X², R¹ a R⁶ y A son tal como se indica en la presente memoria, así como sales farmacéuticamente aceptables de los mismos. Además, la presente se refiere a la preparación de los compuestos de fórmula (1), composiciones farmacéuticas que los comprenden y a su utilización como medicamentos destinados al tratamiento de enfermedades e infecciones causadas por bacterias. Reivindicación 1: Un compuesto de fórmula (1), o una sal farmacéuticamente aceptable del mismo, en la que: X¹ es CH o N; X² es CH o N; A se selecciona de los compuestos del grupo de fórmulas (2); R¹ se selecciona de hidrógeno, halógeno, alcoxi C₁₋₆ y alquilo C₁₋₆; R² es hidrógeno o alquilo C₁₋₆; R³ es aminoalquilo C₁₋₆; R⁴ es aminoalquilo C₁₋₆ o carbamoil-alquilo C₁₋₆; R⁵ se selecciona de carboxi, carboxi-alquilo C₁₋₆ y carboxi-alquenilo C₂₋₆; y R⁶ se selecciona de hidrógeno, halógeno, hidroxi, alcoxi C₁₋₆ y alquilsulfonilo C₁₋₆; con la condición de que el compuesto de fórmula (1) no sea: ácido 4-[(11S,14S,17S)-14-(4-amino-butil)-11-(3-amino-propil)-25-cloro-17-(1H-indol-3-ilmetil)-16-metil-12,15,18-trioxo-2-tia-4,10,13,16,19-pentaaza-triciclo[19.4.0.0*3,8*]pentacosa-1(25),3(8),4,6,21,23-hexaén-22-il]-benzoico. Reivindicación 19: Un proceso para la preparación de los compuestos de fórmula (1) según cualquiera de las reivindicaciones 1 a 8, o una sal farmacéuticamente aceptable de los mismos, que comprende: a) cortar todos los grupos protectores de amino, indol y carboxi presentes en un compuesto de fórmula (3), en la que R, R², R⁶, X¹ y X² son tal como se define en cualquiera de las reivindicaciones 1 a 18; R⁵ se selecciona de R⁷, -alquil C₁₋₆-R⁷ y alquenil C₂₋₆-R⁷, en los que R⁷ se selecciona de carboxi y un ácido carboxílico protegido; R³⁰ es -alquil C₁₋₆, -NH-COOᵗBu; y R⁴⁰ es -alquil C₁₋₆, -NH-COOᵗBu o -alquil C₁₋₆-C(O)-NH-CPh₃; para proporcionar dicho compuesto de fórmula (1). Reivindicación 21: Una composición farmacéutica que comprende un compuesto según cualquiera de las reivindicaciones 1 a 18 y 20, o una sal farmacéuticamente aceptable del mismo, y uno o más excipientes farmacéuticamente aceptables. Reivindicación 24: Un compuesto según cualquiera de las reivindicaciones 1 a 18 y 20, o una sal farmacéuticamente aceptable del mismo, o una composición farmacéutica según la reivindicación 21, para la utilización en el tratamiento o la prevención de infecciones y enfermedades resultantes causadas por Acinetobacter baumannii.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNPCT/CN2018/084131 | 2018-04-23 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR114290A1 true AR114290A1 (es) | 2020-08-12 |
Family
ID=66290410
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP190101064A AR114290A1 (es) | 2018-04-23 | 2019-04-23 | Péptidos macrocíclicos contra actinetobacter baumannii |
Country Status (20)
| Country | Link |
|---|---|
| US (2) | US11819532B2 (es) |
| EP (1) | EP3784262A1 (es) |
| JP (2) | JP7460541B2 (es) |
| KR (1) | KR20210005574A (es) |
| CN (1) | CN111886020B (es) |
| AR (1) | AR114290A1 (es) |
| AU (1) | AU2019260124A1 (es) |
| BR (1) | BR112020021729A2 (es) |
| CA (1) | CA3089688A1 (es) |
| CL (1) | CL2020002695A1 (es) |
| CR (1) | CR20200488A (es) |
| IL (2) | IL278053B2 (es) |
| MA (1) | MA52352A (es) |
| MX (1) | MX2020007633A (es) |
| PE (1) | PE20210855A1 (es) |
| PH (1) | PH12020551762A1 (es) |
| SG (1) | SG11202007219PA (es) |
| TW (1) | TWI833748B (es) |
| UA (1) | UA126943C2 (es) |
| WO (1) | WO2019206853A1 (es) |
Families Citing this family (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CR20180232A (es) | 2015-10-27 | 2018-05-31 | Hoffmann La Roche | Macrociclos peptídicos contra acinetobacter baumannii |
| US11505573B2 (en) | 2018-03-28 | 2022-11-22 | Hoffmann-La Roche Inc. | Peptide macrocycles against Acinetobacter baumannii |
| US11819532B2 (en) * | 2018-04-23 | 2023-11-21 | Hoffmann-La Roche Inc. | Peptide macrocycles against Acinetobacter baumannii |
| WO2019209692A1 (en) | 2018-04-23 | 2019-10-31 | Celgene Corporation | Substituted 4-aminoisoindoline-1,3-dione compounds and their use for treating lymphoma |
| EP3934756A1 (en) | 2019-03-08 | 2022-01-12 | F. Hoffmann-La Roche AG | Novel imidazole-pyrazole derivatives |
| JP2023510971A (ja) | 2020-01-22 | 2023-03-15 | エフ． ホフマン－ラ ロシュ アーゲー | 新規複素環式化合物 |
| WO2021219578A1 (en) | 2020-04-29 | 2021-11-04 | F. Hoffmann-La Roche Ag | Antibacterial 8-phenylamino-3-(pyrazol-4-yl)imidazo[1,2-a]pyrazine derivatives |
| JP2023527479A (ja) | 2020-06-01 | 2023-06-28 | エフ． ホフマン－ラ ロシュ アーゲー | 新規イミダゾピラジン誘導体 |
| CN115667264A (zh) | 2020-06-08 | 2023-01-31 | 豪夫迈·罗氏有限公司 | 新型咪唑并-吡嗪衍生物 |
| CN115916784A (zh) | 2020-06-09 | 2023-04-04 | 豪夫迈·罗氏有限公司 | 新型咪唑并吡嗪衍生物 |
| EP4204090A1 (en) | 2020-08-31 | 2023-07-05 | F. Hoffmann-La Roche AG | Imidazole-pyrazole derivatives as antibacterials |
| CN115989227A (zh) | 2020-09-01 | 2023-04-18 | 豪夫迈·罗氏有限公司 | 具有抗菌性的咪唑-吡唑衍生物 |
| WO2022049272A1 (en) | 2020-09-07 | 2022-03-10 | F. Hoffmann-La Roche Ag | Novel heterocyclic antibiotics |
| JP2024506021A (ja) | 2021-02-07 | 2024-02-08 | エフ． ホフマン－ラ ロシュ アーゲー | 新規ヘテロアリール置換イミダゾール誘導体 |
| EP4367102A1 (en) | 2021-07-06 | 2024-05-15 | F. Hoffmann-La Roche AG | Quaternary ammonium cation substituted compounds for the treatment of bacterial infections |
| WO2023285497A1 (en) | 2021-07-15 | 2023-01-19 | F. Hoffmann-La Roche Ag | Imidazole derivatives and their use as antibiotics |
| AR128501A1 (es) * | 2022-02-14 | 2024-05-15 | Hoffmann La Roche | Proceso para fabricar péptidos macrocíclicos |
| CN118632842A (zh) | 2022-02-25 | 2024-09-10 | 豪夫迈·罗氏有限公司 | 两性离子抗细菌化合物 |
| AU2023250008A1 (en) | 2022-04-07 | 2024-10-03 | F. Hoffmann-La Roche Ag | Crystalline forms of a macrocyclic peptide antibiotic |
| WO2024033278A1 (en) | 2022-08-09 | 2024-02-15 | F. Hoffmann-La Roche Ag | Process for manufacturing an antibiotic macrocyclic peptide |
Family Cites Families (35)
| Publication number | Priority date | Publication date | Assignee | Title |
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| US6660832B1 (en) | 1999-08-20 | 2003-12-09 | Isis Pharmaceuticals, Inc. | Macrocyclic compounds and preparation methods thereof |
| DE10226921A1 (de) | 2002-06-17 | 2003-12-24 | Bayer Ag | Antibakterielle Amid-Makrozyklen |
| DE10234422A1 (de) | 2002-07-29 | 2004-02-12 | Bayer Ag | Antibakterielle Ester-Makrozyklen |
| ES2281692T3 (es) | 2002-08-23 | 2007-10-01 | Sloan-Kettering Institute For Cancer Research | Sintesis de epotilones, sus intermediarios, sus analogos y sus usos. |
| US7521420B2 (en) | 2003-06-18 | 2009-04-21 | Tranzyme Pharma, Inc. | Macrocyclic antagonists of the motilin receptor |
| US7491695B2 (en) | 2003-06-18 | 2009-02-17 | Tranzyme Pharma Inc. | Methods of using macrocyclic modulators of the ghrelin receptor |
| US7476653B2 (en) | 2003-06-18 | 2009-01-13 | Tranzyme Pharma, Inc. | Macrocyclic modulators of the ghrelin receptor |
| EP1498422A1 (de) | 2003-07-17 | 2005-01-19 | Jerini AG | C5a-Rezeptor-Antagonisten |
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| WO2005090388A1 (en) | 2004-03-19 | 2005-09-29 | The University Of Queensland | Alpha helical mimics, their uses and methods for their production |
| DE102004025731A1 (de) | 2004-05-26 | 2005-12-15 | Bayer Healthcare Ag | Antibakterielle Amid-Makrozyklen III |
| US20060004185A1 (en) | 2004-07-01 | 2006-01-05 | Leese Richard A | Peptide antibiotics and peptide intermediates for their prepartion |
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| EP2350031A2 (en) | 2008-08-20 | 2011-08-03 | Ensemble Therapeutics Corporation | Macrocyclic compounds for inhibition of tumor necrosis factor alpha |
| CA2778503A1 (en) | 2009-10-23 | 2011-04-28 | Tranzyme Pharma, Inc. | Macrocyclic inhibitors of serine protease enzymes |
| AU2010313282A1 (en) | 2009-10-30 | 2012-05-24 | Ocera Therapeutics, Inc. | Macrocyclic ghrelin receptor antagonists and inverse agonists and methods of using the same |
| SI2603600T1 (sl) | 2010-08-13 | 2019-04-30 | Aileron Therapeutics, Inc. | Peptidomimetični makrocikli |
| US20130123196A1 (en) | 2011-08-31 | 2013-05-16 | New York University | Thioether-, ether-, and alkylamine-linked hydrogen bond surrogate peptidomimetics |
| KR102112373B1 (ko) | 2012-02-15 | 2020-05-18 | 에일러론 테라퓨틱스 인코포레이티드 | 펩티드모방체 마크로사이클 |
| CN103387601B (zh) | 2012-05-11 | 2017-01-11 | 南开大学 | 抗登革热病毒(denv)杂环肽类化合物及其制备方法和用途 |
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| CA2892027A1 (en) | 2012-11-21 | 2014-05-30 | Rqx Pharmaceuticals, Inc. | Macrocyclic broad spectrum antibiotics |
| WO2014110420A1 (en) | 2013-01-10 | 2014-07-17 | Noliva Therapeutics Llc | Peptidomimetic compounds |
| EP2942389A1 (en) * | 2014-05-05 | 2015-11-11 | Servicio Andaluz De Salud | Vaccine against Acinetobacter baumannii based on lipopolysaccharide-deficient cellular components |
| KR20170038822A (ko) | 2014-07-30 | 2017-04-07 | 에이비에이씨 테라퓨틱스, 에스.엘. | 선택적 항균제로서의 2-피리돈 모이어티를 함유하는 아릴하이드라자이드 |
| CR20180232A (es) * | 2015-10-27 | 2018-05-31 | Hoffmann La Roche | Macrociclos peptídicos contra acinetobacter baumannii |
| EP3388444A1 (en) | 2017-04-10 | 2018-10-17 | F. Hoffmann-La Roche AG | Anti-bacterial peptide macrocycles and use thereof |
| US11505573B2 (en) | 2018-03-28 | 2022-11-22 | Hoffmann-La Roche Inc. | Peptide macrocycles against Acinetobacter baumannii |
| US11819532B2 (en) | 2018-04-23 | 2023-11-21 | Hoffmann-La Roche Inc. | Peptide macrocycles against Acinetobacter baumannii |
-
2019
- 2019-04-19 US US16/389,292 patent/US11819532B2/en active Active
- 2019-04-22 TW TW108113979A patent/TWI833748B/zh active
- 2019-04-23 MA MA052352A patent/MA52352A/fr unknown
- 2019-04-23 BR BR112020021729-8A patent/BR112020021729A2/pt unknown
- 2019-04-23 MX MX2020007633A patent/MX2020007633A/es unknown
- 2019-04-23 PE PE2020000996A patent/PE20210855A1/es unknown
- 2019-04-23 UA UAA202007319A patent/UA126943C2/uk unknown
- 2019-04-23 SG SG11202007219PA patent/SG11202007219PA/en unknown
- 2019-04-23 AR ARP190101064A patent/AR114290A1/es unknown
- 2019-04-23 KR KR1020207029322A patent/KR20210005574A/ko not_active Application Discontinuation
- 2019-04-23 JP JP2020558432A patent/JP7460541B2/ja active Active
- 2019-04-23 CN CN201980020627.4A patent/CN111886020B/zh active Active
- 2019-04-23 CR CR20200488A patent/CR20200488A/es unknown
- 2019-04-23 EP EP19719814.6A patent/EP3784262A1/en active Pending
- 2019-04-23 IL IL278053A patent/IL278053B2/en unknown
- 2019-04-23 CA CA3089688A patent/CA3089688A1/en active Pending
- 2019-04-23 IL IL309537A patent/IL309537A/en unknown
- 2019-04-23 WO PCT/EP2019/060272 patent/WO2019206853A1/en active Application Filing
- 2019-04-23 AU AU2019260124A patent/AU2019260124A1/en active Pending
-
2020
- 2020-10-16 CL CL2020002695A patent/CL2020002695A1/es unknown
- 2020-10-23 PH PH12020551762A patent/PH12020551762A1/en unknown
-
2023
- 2023-10-12 US US18/379,626 patent/US20240050516A1/en active Pending
-
2024
- 2024-01-26 JP JP2024010026A patent/JP2024050700A/ja active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| IL278053B1 (en) | 2024-01-01 |
| JP2021522210A (ja) | 2021-08-30 |
| CN111886020B (zh) | 2024-04-05 |
| CL2020002695A1 (es) | 2021-02-19 |
| IL278053A (en) | 2020-11-30 |
| CA3089688A1 (en) | 2019-10-31 |
| US20240050516A1 (en) | 2024-02-15 |
| IL278053B2 (en) | 2024-05-01 |
| JP7460541B2 (ja) | 2024-04-02 |
| JP2024050700A (ja) | 2024-04-10 |
| TWI833748B (zh) | 2024-03-01 |
| MA52352A (fr) | 2021-03-03 |
| AU2019260124A1 (en) | 2020-08-06 |
| CN111886020A (zh) | 2020-11-03 |
| TW201945386A (zh) | 2019-12-01 |
| KR20210005574A (ko) | 2021-01-14 |
| BR112020021729A2 (pt) | 2021-01-26 |
| PE20210855A1 (es) | 2021-05-18 |
| UA126943C2 (uk) | 2023-02-22 |
| IL309537A (en) | 2024-02-01 |
| CR20200488A (es) | 2021-02-26 |
| SG11202007219PA (en) | 2020-08-28 |
| PH12020551762A1 (en) | 2021-06-14 |
| MX2020007633A (es) | 2020-09-14 |
| US11819532B2 (en) | 2023-11-21 |
| EP3784262A1 (en) | 2021-03-03 |
| US20190321440A1 (en) | 2019-10-24 |
| WO2019206853A1 (en) | 2019-10-31 |
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