DOP2019000076A - DERIVADOS DE CROMANO, ISOCROMANO Y DIHIDROISOBENZOFURANOS COMO MODULADORES ALOSTÉRICOS NEGATIVOS DE mGluR2, COMPOSICIONES Y SU USO - Google Patents
DERIVADOS DE CROMANO, ISOCROMANO Y DIHIDROISOBENZOFURANOS COMO MODULADORES ALOSTÉRICOS NEGATIVOS DE mGluR2, COMPOSICIONES Y SU USOInfo
- Publication number
- DOP2019000076A DOP2019000076A DO2019000076A DO2019000076A DOP2019000076A DO P2019000076 A DOP2019000076 A DO P2019000076A DO 2019000076 A DO2019000076 A DO 2019000076A DO 2019000076 A DO2019000076 A DO 2019000076A DO P2019000076 A DOP2019000076 A DO P2019000076A
- Authority
- DO
- Dominican Republic
- Prior art keywords
- mglur2
- disorders
- compounds
- pharmaceutically acceptable
- negative
- Prior art date
Links
Classifications
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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
- A61K31/16—Amides, e.g. hydroxamic acids
- A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
- A61K31/166—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the carbon of a carboxamide group directly attached to the aromatic ring, e.g. procainamide, procarbazine, metoclopramide, labetalol
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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
- A61K31/435—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
- A61K31/436—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 the heterocyclic ring system containing a six-membered ring having oxygen as a ring hetero atom, e.g. rapamycin
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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
- A61K31/435—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
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- 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
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- 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
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- 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
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
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- 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
- A61P25/20—Hypnotics; Sedatives
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- 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
- A61P25/24—Antidepressants
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- 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
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- 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
- C07D221/24—Camphidines
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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
-
- 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
- C07D491/12—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 three hetero rings
- C07D491/18—Bridged 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
- A61K31/01—Hydrocarbons
- A61K31/015—Hydrocarbons carbocyclic
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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
- A61K31/02—Halogenated hydrocarbons
- A61K31/025—Halogenated hydrocarbons carbocyclic
- A61K31/03—Halogenated hydrocarbons carbocyclic aromatic
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Anesthesiology (AREA)
- Psychology (AREA)
- Pain & Pain Management (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines Containing Plant Substances (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
La presente invención proporciona ciertos compuestos de cromano, isocromano y dihidroisobenzofurano sustituidos de fórmula (I): o una sal farmacéuticamente aceptable de los mismos, en la que el anillo A es un resto seleccionado de: y el anillo B, n, R1, R2, R2A, R3 y R3A son como se definen en la presente memoria. Los compuestos de la invención son útiles como inhibidores de mGluR2, o moduladores alostéricos negativos de mGluR2 (NAM), y pueden ser útiles en procedimientos de tratamiento de un paciente para enfermedades o trastornos en los que está implicado el receptor mGluR2-NAM, tales como la enfermedad de Alzheimer, deterioro cognitivo, deterioro cognitivo leve, esquizofrenia y otros trastornos del estado de ánimo, trastornos del dolor y trastornos del sueño, mediante la administración al paciente de una cantidad terapéuticamente eficaz de un compuesto de la invención, o una sal farmacéuticamente aceptable del mismo. La invención también se refiere a composiciones farmacéuticas que comprenden un compuesto de la invención, o una sal farmacéuticamente aceptable del mismo, (opcionalmente en combinación con uno o más ingredientes activos adicionales), y un vehículo farmacéuticamente aceptable, y al uso de los compuestos y composiciones farmacéuticas de la invención en el tratamiento de tales enfermedades.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662400150P | 2016-09-27 | 2016-09-27 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| DOP2019000076A true DOP2019000076A (es) | 2019-07-15 |
Family
ID=60043302
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DO2019000076A DOP2019000076A (es) | 2016-09-27 | 2019-03-26 | DERIVADOS DE CROMANO, ISOCROMANO Y DIHIDROISOBENZOFURANOS COMO MODULADORES ALOSTÉRICOS NEGATIVOS DE mGluR2, COMPOSICIONES Y SU USO |
Country Status (39)
| Country | Link |
|---|---|
| US (4) | US10335399B2 (es) |
| EP (1) | EP3519416B1 (es) |
| JP (3) | JP6681517B2 (es) |
| KR (1) | KR102296043B1 (es) |
| CN (1) | CN109983022B (es) |
| AR (1) | AR109714A1 (es) |
| AU (2) | AU2017334870C1 (es) |
| CA (1) | CA3037537C (es) |
| CL (1) | CL2019000778A1 (es) |
| CO (1) | CO2019002673A2 (es) |
| CR (1) | CR20190147A (es) |
| CY (1) | CY1124346T1 (es) |
| DK (1) | DK3519416T3 (es) |
| DO (1) | DOP2019000076A (es) |
| EA (1) | EA038627B1 (es) |
| EC (1) | ECSP19020742A (es) |
| ES (1) | ES2868973T3 (es) |
| GE (2) | GEP20217266B (es) |
| HR (1) | HRP20210793T1 (es) |
| HU (1) | HUE054898T2 (es) |
| IL (1) | IL265366B (es) |
| JO (1) | JOP20190058B1 (es) |
| LT (1) | LT3519416T (es) |
| MA (1) | MA46342B1 (es) |
| MD (1) | MD3519416T2 (es) |
| MX (1) | MX2019003492A (es) |
| MY (1) | MY196807A (es) |
| NI (1) | NI201900025A (es) |
| PE (1) | PE20190609A1 (es) |
| PH (1) | PH12019500597A1 (es) |
| PL (1) | PL3519416T3 (es) |
| PT (1) | PT3519416T (es) |
| RS (1) | RS61890B1 (es) |
| SI (1) | SI3519416T1 (es) |
| TN (2) | TN2020000160A1 (es) |
| TW (1) | TWI764934B (es) |
| UA (1) | UA123687C2 (es) |
| WO (1) | WO2018063955A1 (es) |
| ZA (1) | ZA201901701B (es) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2018063955A1 (en) * | 2016-09-27 | 2018-04-05 | Merck Sharp & Dohme Corp. | CHROMANE, ISOCHROMANE AND DIHYDROISOBENZOFURAN DERIVATIVES AS mGluR2-NEGATIVE ALLOSTERIC MODULATORS, COMPOSITIONS, AND THEIR USE |
| MA51620A (fr) | 2018-01-19 | 2020-11-25 | Cytokinetics Inc | Analogues de dihydrobenzofurane et d'inden en tant qu'inhibiteurs de sarcomes cardiaques |
| US11964967B2 (en) | 2018-06-26 | 2024-04-23 | Cytokinetics, Inc. | Cardiac sarcomere inhibitors |
| US20220144824A1 (en) * | 2019-03-01 | 2022-05-12 | Kbp Biosciences Co., Ltd. | Method for preparing tricyclic compound, and intermediate thereof |
| EP4301760A1 (en) | 2021-03-04 | 2024-01-10 | Cytokinetics, Inc. | Cardiac sarcomere inhibitors |
| WO2023278729A1 (en) * | 2021-06-30 | 2023-01-05 | The General Hospital Corporation | Chromane imaging ligands |
Family Cites Families (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5552437A (en) | 1994-10-27 | 1996-09-03 | Merck Frosst Canada, Inc. | Bisarylcarbinol derivatives as inhibitors of leukotriene biosynthesis |
| US5576338A (en) | 1995-02-15 | 1996-11-19 | Merck Frosst Canada, Inc. | Bis (biaryl) compounds as inhibitors of leukotriene biosynthesis |
| WO2005014543A1 (ja) | 2003-08-06 | 2005-02-17 | Japan Tobacco Inc. | 縮合環化合物及びそのｈｃｖポリメラーゼ阻害剤としての利用 |
| EP1934205A4 (en) | 2005-10-05 | 2010-06-02 | Merck Frosst Canada Ltd | SUBSTITUTED QUINOLINES AS INHIBITORS OF LEUCOTRIENE BIOSYNTHESIS |
| AR065093A1 (es) | 2007-02-05 | 2009-05-13 | Merck Frosst Canada Ltd | Compuestos farmacéuticos inhibidores de la biosintesis de leucotrienos |
| US20120040974A1 (en) | 2008-08-18 | 2012-02-16 | Yale University | Mif modulators |
| CA2760741C (en) * | 2009-05-12 | 2018-05-01 | Addex Pharma S.A. | 1,2,4-triazolo [4,3-a] pyridine derivatives and their use for the treatment or prevention of neurological and psychiatric disorders |
| WO2011075699A2 (en) | 2009-12-18 | 2011-06-23 | Sunovion Pharmaceuticals Inc. | Compounds for treating disorders mediated by metabotropic glutamate receptor 5, and methods of use thereof |
| WO2013066736A1 (en) | 2011-11-03 | 2013-05-10 | Merck Sharp & Dohme Corp. | QUINOLINE CARBOXAMIDE AND QUINOLINE CARBONITRILE DERIVATIVES AS mGluR2-NEGATIVE ALLOSTERIC MODULATORS, COMPOSITIONS, AND THEIR USE |
| JO3368B1 (ar) | 2013-06-04 | 2019-03-13 | Janssen Pharmaceutica Nv | مركبات 6، 7- ثاني هيدرو بيرازولو [5،1-a] بيرازين- 4 (5 يد)- اون واستخدامها بصفة منظمات تفارغية سلبية لمستقبلات ميجلور 2 |
| WO2016029454A1 (en) | 2014-08-29 | 2016-03-03 | Merck Sharp & Dohme Corp. | TETRAHYDRONAPHTHYRIDINE DERIVATIVES AS mGluR2-NEGATIVE ALLOSTERIC MODULATORS, COMPOSITIONS, AND THEIR USE |
| US9382208B1 (en) | 2015-01-26 | 2016-07-05 | Vanderbilt University | Negative allosteric modulators of metabotropic glutamate receptor 2 |
| WO2016149324A1 (en) | 2015-03-16 | 2016-09-22 | Vanderbilt University | Negative allosteric modulators of metabotropic glutamate receptor 2 |
| JP6471614B2 (ja) | 2015-05-29 | 2019-02-20 | 株式会社リコー | 通信端末、通信システム、通信制御方法、及びプログラム |
| JP2018154554A (ja) | 2015-07-29 | 2018-10-04 | 大日本住友製薬株式会社 | 新規リンカー部位を持つ縮合ピラゾール誘導体およびその医薬用途 |
| WO2018063955A1 (en) * | 2016-09-27 | 2018-04-05 | Merck Sharp & Dohme Corp. | CHROMANE, ISOCHROMANE AND DIHYDROISOBENZOFURAN DERIVATIVES AS mGluR2-NEGATIVE ALLOSTERIC MODULATORS, COMPOSITIONS, AND THEIR USE |
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2017
- 2017-09-25 WO PCT/US2017/053155 patent/WO2018063955A1/en active Application Filing
- 2017-09-25 CA CA3037537A patent/CA3037537C/en active Active
- 2017-09-25 EP EP17781253.4A patent/EP3519416B1/en active Active
- 2017-09-25 AU AU2017334870A patent/AU2017334870C1/en active Active
- 2017-09-25 CN CN201780071759.0A patent/CN109983022B/zh active Active
- 2017-09-25 UA UAA201904545A patent/UA123687C2/uk unknown
- 2017-09-25 DK DK17781253.4T patent/DK3519416T3/da active
- 2017-09-25 GE GEAP201715056A patent/GEP20217266B/en unknown
- 2017-09-25 HU HUE17781253A patent/HUE054898T2/hu unknown
- 2017-09-25 MX MX2019003492A patent/MX2019003492A/es unknown
- 2017-09-25 KR KR1020197011789A patent/KR102296043B1/ko active IP Right Grant
- 2017-09-25 TN TNP/2020/000160A patent/TN2020000160A1/en unknown
- 2017-09-25 JO JOP/2019/0058A patent/JOP20190058B1/ar active
- 2017-09-25 TN TNP/2020/000161A patent/TN2020000161A1/en unknown
- 2017-09-25 CR CR20190147A patent/CR20190147A/es unknown
- 2017-09-25 ES ES17781253T patent/ES2868973T3/es active Active
- 2017-09-25 PT PT177812534T patent/PT3519416T/pt unknown
- 2017-09-25 JP JP2019516203A patent/JP6681517B2/ja active Active
- 2017-09-25 MY MYPI2019001659A patent/MY196807A/en unknown
- 2017-09-25 GE GEAP201715310A patent/GEP20217279B/en unknown
- 2017-09-25 MD MDE20190867T patent/MD3519416T2/ro unknown
- 2017-09-25 SI SI201730727T patent/SI3519416T1/sl unknown
- 2017-09-25 MA MA46342A patent/MA46342B1/fr unknown
- 2017-09-25 AR ARP170102642A patent/AR109714A1/es active IP Right Grant
- 2017-09-25 RS RS20210649A patent/RS61890B1/sr unknown
- 2017-09-25 TW TW106132824A patent/TWI764934B/zh active
- 2017-09-25 EA EA201990818A patent/EA038627B1/ru unknown
- 2017-09-25 LT LTEP17781253.4T patent/LT3519416T/lt unknown
- 2017-09-25 PL PL17781253T patent/PL3519416T3/pl unknown
- 2017-09-25 US US15/713,769 patent/US10335399B2/en active Active
- 2017-09-25 PE PE2019000706A patent/PE20190609A1/es unknown
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2019
- 2019-03-13 IL IL265366A patent/IL265366B/en unknown
- 2019-03-19 PH PH12019500597A patent/PH12019500597A1/en unknown
- 2019-03-19 ZA ZA2019/01701A patent/ZA201901701B/en unknown
- 2019-03-20 NI NI201900025A patent/NI201900025A/es unknown
- 2019-03-22 CO CONC2019/0002673A patent/CO2019002673A2/es unknown
- 2019-03-25 CL CL2019000778A patent/CL2019000778A1/es unknown
- 2019-03-26 DO DO2019000076A patent/DOP2019000076A/es unknown
- 2019-03-28 EC ECSENADI201920742A patent/ECSP19020742A/es unknown
- 2019-04-23 US US16/392,131 patent/US10806724B2/en active Active
- 2019-09-30 JP JP2019178232A patent/JP6945605B2/ja active Active
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2020
- 2020-03-23 JP JP2020051049A patent/JP6992109B2/ja active Active
- 2020-09-25 US US17/032,626 patent/US20210015800A1/en not_active Abandoned
- 2020-11-16 AU AU2020270468A patent/AU2020270468B2/en active Active
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2021
- 2021-05-17 HR HRP20210793TT patent/HRP20210793T1/hr unknown
- 2021-05-31 CY CY20211100468T patent/CY1124346T1/el unknown
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2022
- 2022-03-15 US US17/695,262 patent/US20220218676A1/en active Pending
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