EA201990818A1 - ПРОИЗВОДНЫЕ ХРОМАНА, ИЗОХРОМАНА И ДИГИДРОИЗОБЕНЗОФУРАНА В КАЧЕСТВЕ НЕГАТИВНЫХ АЛЛОСТЕРИЧЕСКИХ МОДУЛЯТОРОВ РЕЦЕПТОРОВ mGluR2, ИХ КОМПОЗИЦИИ И ПРИМЕНЕНИЕ - Google Patents
ПРОИЗВОДНЫЕ ХРОМАНА, ИЗОХРОМАНА И ДИГИДРОИЗОБЕНЗОФУРАНА В КАЧЕСТВЕ НЕГАТИВНЫХ АЛЛОСТЕРИЧЕСКИХ МОДУЛЯТОРОВ РЕЦЕПТОРОВ mGluR2, ИХ КОМПОЗИЦИИ И ПРИМЕНЕНИЕInfo
- Publication number
- EA201990818A1 EA201990818A1 EA201990818A EA201990818A EA201990818A1 EA 201990818 A1 EA201990818 A1 EA 201990818A1 EA 201990818 A EA201990818 A EA 201990818A EA 201990818 A EA201990818 A EA 201990818A EA 201990818 A1 EA201990818 A1 EA 201990818A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- pharmaceutically acceptable
- mglur2
- acceptable salt
- disorders
- allosteric modulators
- Prior art date
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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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
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- 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
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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
- A61K31/01—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
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Pain & Pain Management (AREA)
- Anesthesiology (AREA)
- Psychology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines Containing Plant Substances (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
Abstract
Настоящее изобретение относится к некоторым замещенным соединениям хромана, изохромана и дигидроизобензофурана формулы (I)или их фармацевтически приемлемой соли, где кольцо A представляет собой фрагмент, выбранный из:а кольцо B, n, R, R, R, Rи Rявляется таким, как определено в настоящем документе. Соединения по изобретению применятся в качестве ингибиторов mGluR2 или негативных аллостерических модуляторов mGluR2 (NAM) и могут применяться в способах лечения у пациента заболеваний или расстройств, в которые вовлечен рецептор mGluR2-NAM, таких как болезнь Альцгеймера, когнитивное нарушение, легкая форма когнитивного нарушения, шизофрения и другие расстройства настроения, болевые расстройства и расстройства сна, путем введения пациенту терапевтически эффективного количества соединения по изобретению или его фармацевтически приемлемой соли. Изобретение также относится к фармацевтическим композициям, содержащим соединение по изобретению или его фармацевтически приемлемую соль (необязательно в комбинации с одним или несколькими дополнительными активными ингредиентами) и фармацевтически приемлемый носитель, а также к применению соединений и фармацевтических композиций по изобретению в лечении таких заболеваний.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662400150P | 2016-09-27 | 2016-09-27 | |
| PCT/US2017/053155 WO2018063955A1 (en) | 2016-09-27 | 2017-09-25 | CHROMANE, ISOCHROMANE AND DIHYDROISOBENZOFURAN DERIVATIVES AS mGluR2-NEGATIVE ALLOSTERIC MODULATORS, COMPOSITIONS, AND THEIR USE |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| EA201990818A1 true EA201990818A1 (ru) | 2019-08-30 |
| EA038627B1 EA038627B1 (ru) | 2021-09-24 |
Family
ID=60043302
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA201990818A EA038627B1 (ru) | 2016-09-27 | 2017-09-25 | ПРОИЗВОДНЫЕ ХРОМАНА, ИЗОХРОМАНА И ДИГИДРОИЗОБЕНЗОФУРАНА В КАЧЕСТВЕ НЕГАТИВНЫХ АЛЛОСТЕРИЧЕСКИХ МОДУЛЯТОРОВ РЕЦЕПТОРОВ mGluR2, ИХ КОМПОЗИЦИИ И ПРИМЕНЕНИЕ |
Country Status (39)
| Country | Link |
|---|---|
| US (4) | US10335399B2 (ru) |
| EP (1) | EP3519416B1 (ru) |
| JP (3) | JP6681517B2 (ru) |
| KR (1) | KR102296043B1 (ru) |
| CN (1) | CN109983022B (ru) |
| AR (1) | AR109714A1 (ru) |
| AU (2) | AU2017334870C1 (ru) |
| CA (1) | CA3037537C (ru) |
| CL (1) | CL2019000778A1 (ru) |
| CO (1) | CO2019002673A2 (ru) |
| CR (1) | CR20190147A (ru) |
| CY (1) | CY1124346T1 (ru) |
| DK (1) | DK3519416T3 (ru) |
| DO (1) | DOP2019000076A (ru) |
| EA (1) | EA038627B1 (ru) |
| EC (1) | ECSP19020742A (ru) |
| ES (1) | ES2868973T3 (ru) |
| GE (2) | GEP20217266B (ru) |
| HR (1) | HRP20210793T1 (ru) |
| HU (1) | HUE054898T2 (ru) |
| IL (1) | IL265366B (ru) |
| JO (1) | JOP20190058B1 (ru) |
| LT (1) | LT3519416T (ru) |
| MA (1) | MA46342B1 (ru) |
| MD (1) | MD3519416T2 (ru) |
| MX (1) | MX2019003492A (ru) |
| MY (1) | MY196807A (ru) |
| NI (1) | NI201900025A (ru) |
| PE (1) | PE20190609A1 (ru) |
| PH (1) | PH12019500597A1 (ru) |
| PL (1) | PL3519416T3 (ru) |
| PT (1) | PT3519416T (ru) |
| RS (1) | RS61890B1 (ru) |
| SI (1) | SI3519416T1 (ru) |
| TN (2) | TN2020000161A1 (ru) |
| TW (1) | TWI764934B (ru) |
| UA (1) | UA123687C2 (ru) |
| WO (1) | WO2018063955A1 (ru) |
| ZA (1) | ZA201901701B (ru) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EA038627B1 (ru) * | 2016-09-27 | 2021-09-24 | Мерк Шарп И Доум Корп. | ПРОИЗВОДНЫЕ ХРОМАНА, ИЗОХРОМАНА И ДИГИДРОИЗОБЕНЗОФУРАНА В КАЧЕСТВЕ НЕГАТИВНЫХ АЛЛОСТЕРИЧЕСКИХ МОДУЛЯТОРОВ РЕЦЕПТОРОВ mGluR2, ИХ КОМПОЗИЦИИ И ПРИМЕНЕНИЕ |
| 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 |
| JP7291426B2 (ja) * | 2019-03-01 | 2023-06-15 | 山東亨利醫藥科技有限責任公司 | 縮合三環式化合物を調製するための方法、及びその中間体 |
| CA3209557A1 (en) | 2021-03-04 | 2022-09-09 | Bradley P. Morgan | 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 |
| AU2006299671A1 (en) | 2005-10-05 | 2007-04-12 | Merck Frosst Canada Ltd | Substituted quinolines as inhibitors of leukotriene biosynthesis |
| AR065093A1 (es) | 2007-02-05 | 2009-05-13 | Merck Frosst Canada Ltd | Compuestos farmacéuticos inhibidores de la biosintesis de leucotrienos |
| CN102186833A (zh) | 2008-08-18 | 2011-09-14 | 耶鲁大学 | Mif调节剂 |
| JP5634506B2 (ja) * | 2009-05-12 | 2014-12-03 | ジャンセン ファーマシューティカルズ， インコーポレイテッド | １，２，３−トリアゾロ［４，３−ａ］ピリジン誘導体ならびに神経障害および精神障害の治療または予防のためのその使用 |
| 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 |
| MY167423A (en) * | 2011-11-03 | 2018-08-27 | Merck Sharp & Dohme | 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 |
| US10538491B2 (en) | 2015-03-16 | 2020-01-21 | Vanderbilt University | 4,5-substituted picolinamide and picolinonitrile metabotropic glutamate receptor 2 negative allosteric modulators |
| 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 |
| EA038627B1 (ru) * | 2016-09-27 | 2021-09-24 | Мерк Шарп И Доум Корп. | ПРОИЗВОДНЫЕ ХРОМАНА, ИЗОХРОМАНА И ДИГИДРОИЗОБЕНЗОФУРАНА В КАЧЕСТВЕ НЕГАТИВНЫХ АЛЛОСТЕРИЧЕСКИХ МОДУЛЯТОРОВ РЕЦЕПТОРОВ mGluR2, ИХ КОМПОЗИЦИИ И ПРИМЕНЕНИЕ |
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2017
- 2017-09-25 EA EA201990818A patent/EA038627B1/ru unknown
- 2017-09-25 SI SI201730727T patent/SI3519416T1/sl unknown
- 2017-09-25 WO PCT/US2017/053155 patent/WO2018063955A1/en unknown
- 2017-09-25 PE PE2019000706A patent/PE20190609A1/es unknown
- 2017-09-25 JP JP2019516203A patent/JP6681517B2/ja active Active
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- 2017-09-25 JO JOP/2019/0058A patent/JOP20190058B1/ar active
- 2017-09-25 UA UAA201904545A patent/UA123687C2/uk unknown
- 2017-09-25 GE GEAP201715056A patent/GEP20217266B/en unknown
- 2017-09-25 US US15/713,769 patent/US10335399B2/en active Active
- 2017-09-25 AU AU2017334870A patent/AU2017334870C1/en active Active
- 2017-09-25 MY MYPI2019001659A patent/MY196807A/en unknown
- 2017-09-25 TN TNP/2020/000161A patent/TN2020000161A1/en unknown
- 2017-09-25 DK DK17781253.4T patent/DK3519416T3/da active
- 2017-09-25 AR ARP170102642A patent/AR109714A1/es unknown
- 2017-09-25 ES ES17781253T patent/ES2868973T3/es active Active
- 2017-09-25 LT LTEP17781253.4T patent/LT3519416T/lt unknown
- 2017-09-25 TW TW106132824A patent/TWI764934B/zh active
- 2017-09-25 CN CN201780071759.0A patent/CN109983022B/zh active Active
- 2017-09-25 PL PL17781253T patent/PL3519416T3/pl unknown
- 2017-09-25 TN TNP/2020/000160A patent/TN2020000160A1/en unknown
- 2017-09-25 EP EP17781253.4A patent/EP3519416B1/en active Active
- 2017-09-25 KR KR1020197011789A patent/KR102296043B1/ko active IP Right Grant
- 2017-09-25 GE GEAP201715310A patent/GEP20217279B/en unknown
- 2017-09-25 RS RS20210649A patent/RS61890B1/sr unknown
- 2017-09-25 MD MDE20190867T patent/MD3519416T2/ro unknown
- 2017-09-25 PT PT177812534T patent/PT3519416T/pt unknown
- 2017-09-25 MX MX2019003492A patent/MX2019003492A/es unknown
- 2017-09-25 HU HUE17781253A patent/HUE054898T2/hu unknown
- 2017-09-25 MA MA46342A patent/MA46342B1/fr unknown
- 2017-09-25 CA CA3037537A patent/CA3037537C/en active Active
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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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