HRP20231475T1 - Derivat p-fenilendiamina kao regulator kalijevih kanala i postupak priprave i njegova medicinska primjena. - Google Patents

Derivat p-fenilendiamina kao regulator kalijevih kanala i postupak priprave i njegova medicinska primjena. Download PDF

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HRP20231475T1
HRP20231475T1 HRP20231475TT HRP20231475T HRP20231475T1 HR P20231475 T1 HRP20231475 T1 HR P20231475T1 HR P20231475T T HRP20231475T T HR P20231475TT HR P20231475 T HRP20231475 T HR P20231475T HR P20231475 T1 HRP20231475 T1 HR P20231475T1
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ring
alkyl
image
halogenated
substituent
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HRP20231475TT
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Huanming Chen
Bo Liang
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Shanghai Zhimeng Biopharma, Inc.
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Publication of HRP20231475T1 publication Critical patent/HRP20231475T1/hr

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    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D267/00—Heterocyclic compounds containing rings of more than six members having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D267/02—Seven-membered rings
    • C07D267/08—Seven-membered rings having the hetero atoms in positions 1 and 4
    • C07D267/12—Seven-membered rings having the hetero atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
    • C07D267/14—Seven-membered rings having the hetero atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems condensed with one six-membered ring
    • 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
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/536—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines ortho- or peri-condensed with carbocyclic ring systems
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/554—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one sulfur as ring hetero atoms, e.g. clothiapine, diltiazem
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/06—Antimigraine agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/08—Antiepileptics; Anticonvulsants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A61P3/12—Drugs for disorders of the metabolism for electrolyte homeostasis
    • 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
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/56—Ring systems containing three or more rings
    • C07D209/80—[b, c]- or [b, d]-condensed
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D221/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00
    • C07D221/02—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00 condensed with carbocyclic rings or ring systems
    • C07D221/22—Bridged ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D225/00—Heterocyclic compounds containing rings of more than seven members having one nitrogen atom as the only ring hetero atom
    • C07D225/04—Heterocyclic compounds containing rings of more than seven members having one nitrogen atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D225/06—Heterocyclic compounds containing rings of more than seven members having one nitrogen atom as the only ring hetero atom condensed with carbocyclic rings or ring systems condensed with one six-membered ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/28—1,4-Oxazines; Hydrogenated 1,4-oxazines
    • C07D265/34—1,4-Oxazines; Hydrogenated 1,4-oxazines condensed with carbocyclic rings
    • C07D265/36—1,4-Oxazines; Hydrogenated 1,4-oxazines condensed with carbocyclic rings condensed with one six-membered ring
    • 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
    • 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
    • C07D487/04—Ortho-condensed systems
    • 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
    • C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
    • 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
    • C07D495/08—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

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  • Organic Chemistry (AREA)
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  • Bioinformatics & Cheminformatics (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Pain & Pain Management (AREA)
  • Psychology (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Urology & Nephrology (AREA)
  • Rheumatology (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Claims (7)

1. Spoj predstavljen formulom A ili njegova farmaceutski prihvatljiva sol: [image] pri čemu: prsten B je [image] ili [image] prsten A je tiofenski prsten; ili prsten B je [image] ili [image] prsten A je benzenski prsten; R1 je supstituent na prstenu A; R2 je supstituent na prstenu B; R3 i R4 su supstituenti na šesteročlanom prstenu; R1 i R2 su svaki neovisno vodik, halogen, nitro, cijano, C1-6 alkil, C1-6 alkoksi, halogenirani C1-6 alkil, halogenirani C1-6 alkoksi, C3-6 cikloalkil, C1-6 alkanamino; R3 i R4 su svaki neovisno C1-6 alkil; Y je CH; Z je (CH2)n, n je 1; R5 je C1-6 alkil.
2. Spoj prema patentnom zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, pri čemu: prsten B je [image] ili [image] prsten A je tiofenski prsten; R1 je supstituent na prstenu A; R2 je supstituent na prstenu B; R3 i R4 su supstituenti na šesteročlanom prstenu; R1 i R2 su svaki neovisno vodik, halogen, nitro, cijano, C1-6 alkil, C1-6 alkoksi, halogenirani C1-6 alkil, halogenirani C1-6 alkoksi, C3-6 cikloalkil, C1-6 alkanamino; R3 i R4 su svaki neovisno C1-6 alkil; Y je CH; Z je (CH2)n, n je 1; R5 je C1-6 alkil.
3. Spoj prema patentnom zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, pri čemu: prsten B je [image] ili [image] prsten A je benzenski prsten; R1 je supstituent na prstenu A; R2 je supstituent na prstenu B; R3 i R4 su supstituenti na šesteročlanom prstenu; R1 i R2 su svaki neovisno vodik, halogen, nitro, cijano, C1-6 alkil, C1-6 alkoksi, halogenirani C1-6 alkil, halogenirani C1-6 alkoksi, C3-6 cikloalkil, C1-6 alkanamino; R3 i R4 su svaki neovisno C1-6 alkil; Y je CH; Z je (CH2)n, n je 1; R5 je C1-6 alkil.
4. Spoj prema patentnom zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, pri čemu: prsten B je [image] ili [image] prsten A je tiofenski prsten; R1 je supstituent na prstenu A; R2 je supstituent na prstenu B; R3 i R4 su supstituenti na šesteročlanom prstenu; R1 i R2 su svaki neovisno vodik, halogen, nitro, cijano, C1-6 alkil, C1-6 alkoksi, halogenirani C1-6 alkil, halogenirani C1-6 alkoksi, C3-6 cikloalkil, C1-6 alkanamino; R3 i R4 su svaki neovisno C1-6 alkil; Y je CH; Z je CH2; R5 je C1-6 alkil.
5. Spoj prema patentnom zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, pri čemu je spoj odabran iz skupine koju čine: [image]
6. Farmaceutski pripravak koji sadrži jednog ili više farmaceutski prihvatljivih nosača ili razrjeđivača i spoj prema patentnom zahtjevu 1 ili njegovu farmaceutski prihvatljivu sol.
7. Upotreba spoja prema patentnom zahtjevu 1 ili njegove farmaceutski prihvatljive soli ili farmaceutskog pripravka prema patentnom zahtjevu 6 za pripravu lijeka koji regulira ionsku struju u kalijevom kanalu kod sisavaca.
HRP20231475TT 2018-05-22 2019-05-22 Derivat p-fenilendiamina kao regulator kalijevih kanala i postupak priprave i njegova medicinska primjena. HRP20231475T1 (hr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN201810493023 2018-05-22
EP19808475.8A EP3798220B1 (en) 2018-05-22 2019-05-22 P-phenylenediamine derivative as potassium channel regulator and preparation method and medical application thereof
PCT/CN2019/088012 WO2019223732A1 (zh) 2018-05-22 2019-05-22 作为钾通道调节剂的对二氨基苯衍生物、其制备方法及其在医药上的应用

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HRP20231475T1 true HRP20231475T1 (hr) 2024-03-01

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HRP20231475TT HRP20231475T1 (hr) 2018-05-22 2019-05-22 Derivat p-fenilendiamina kao regulator kalijevih kanala i postupak priprave i njegova medicinska primjena.

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US (2) US11365181B2 (hr)
EP (1) EP3798220B1 (hr)
JP (1) JP7294681B2 (hr)
KR (1) KR102599761B1 (hr)
CN (2) CN110511220B (hr)
AU (1) AU2019272383B2 (hr)
BR (1) BR112020023861A2 (hr)
CA (1) CA3101226C (hr)
ES (1) ES2963614T3 (hr)
HR (1) HRP20231475T1 (hr)
PL (1) PL3798220T3 (hr)
RS (1) RS64710B1 (hr)
RU (1) RU2762562C9 (hr)
WO (1) WO2019223732A1 (hr)

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CN114057641A (zh) * 2020-08-07 2022-02-18 上海挚盟医药科技有限公司 作为钾通道调节剂的四氢异喹啉类化合物及其制备和应用
WO2023025276A1 (zh) * 2021-08-26 2023-03-02 杭州和正医药有限公司 一种钾通道调节剂、组合物及应用
CN113698345B (zh) * 2021-10-27 2022-02-01 上海挚盟医药科技有限公司 作为钾通道调节剂的化合物及其制备和应用
CN116535353A (zh) * 2022-01-25 2023-08-04 上海挚盟医药科技有限公司 作为钾通道调节剂的酰胺类化合物及其制备和应用
WO2024067819A1 (zh) * 2022-09-30 2024-04-04 上海翰森生物医药科技有限公司 含哌啶多环类衍生物调节剂、其制备方法和应用

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JP2021525241A (ja) 2021-09-24
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AU2019272383B2 (en) 2021-09-23
US20210163429A1 (en) 2021-06-03
CA3101226A1 (en) 2019-11-28
CN110511220B (zh) 2022-04-01
CN112119079A (zh) 2020-12-22
EP3798220A1 (en) 2021-03-31
WO2019223732A1 (zh) 2019-11-28
ES2963614T3 (es) 2024-04-01
EP3798220A4 (en) 2022-02-23
KR20210011968A (ko) 2021-02-02
PL3798220T3 (pl) 2024-02-26
EP3798220C0 (en) 2023-08-23
RU2762562C1 (ru) 2021-12-21
BR112020023861A2 (pt) 2021-04-13
CN110511220A (zh) 2019-11-29
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