EA202092586A1 - Ингибиторы magl - Google Patents
Ингибиторы maglInfo
- Publication number
- EA202092586A1 EA202092586A1 EA202092586A EA202092586A EA202092586A1 EA 202092586 A1 EA202092586 A1 EA 202092586A1 EA 202092586 A EA202092586 A EA 202092586A EA 202092586 A EA202092586 A EA 202092586A EA 202092586 A1 EA202092586 A1 EA 202092586A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- compounds
- magl inhibitors
- useful
- compositions
- present
- Prior art date
Links
- 102100029814 Monoglyceride lipase Human genes 0.000 title abstract 2
- 101710116393 Monoglyceride lipase Proteins 0.000 title abstract 2
- 239000003112 inhibitor Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 3
- 239000000203 mixture Substances 0.000 abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- CWPIBZMCMRNFHK-UHFFFAOYSA-N piperazin-1-ium;carbamate Chemical class NC(O)=O.C1CNCCN1 CWPIBZMCMRNFHK-UHFFFAOYSA-N 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
- C07D295/16—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
- C07D295/18—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms by radicals derived from carboxylic acids, or sulfur or nitrogen analogues thereof
- C07D295/182—Radicals derived from carboxylic acids
- C07D295/185—Radicals derived from carboxylic acids from aliphatic carboxylic acids
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
-
- 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
- A61P25/04—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
- A61P25/28—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]
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
- C07D213/54—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D213/55—Acids; Esters
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
- C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
- C07D241/10—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
- C07D241/12—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having 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
- C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
- C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
- C07D263/30—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D263/32—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D305/00—Heterocyclic compounds containing four-membered rings having one oxygen atom as the only ring hetero atoms
- C07D305/02—Heterocyclic compounds containing four-membered rings having one oxygen atom as the only ring hetero atoms not condensed with other rings
- C07D305/04—Heterocyclic compounds containing four-membered rings having one oxygen atom as the only ring hetero atoms not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
- C07D305/06—Heterocyclic compounds containing four-membered rings having one oxygen atom as the only ring hetero atoms not condensed with other rings having no 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 the ring atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D305/00—Heterocyclic compounds containing four-membered rings having one oxygen atom as the only ring hetero atoms
- C07D305/02—Heterocyclic compounds containing four-membered rings having one oxygen atom as the only ring hetero atoms not condensed with other rings
- C07D305/04—Heterocyclic compounds containing four-membered rings having one oxygen atom as the only ring hetero atoms not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
- C07D305/08—Heterocyclic compounds containing four-membered rings having one oxygen atom as the only ring hetero atoms not condensed with other rings having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing aromatic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/10—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing aromatic rings
-
- 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
- C07D413/10—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 carbon chain containing aromatic rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Pain & Pain Management (AREA)
- Epidemiology (AREA)
- Rheumatology (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Epoxy Compounds (AREA)
- Pyridine Compounds (AREA)
Abstract
В изобретении предусмотрены карбаматы пиперазина и фармацевтические композиции, содержащие указанные соединения. Соединения и композиции по настоящему изобретению являются пригодными в качестве модуляторов MAGL. Кроме того, соединения и композиции по настоящему изобретению являются пригодными для устранения боли.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201862671985P | 2018-05-15 | 2018-05-15 | |
PCT/US2019/032289 WO2019222266A1 (en) | 2018-05-15 | 2019-05-14 | Magl inhibitors |
Publications (1)
Publication Number | Publication Date |
---|---|
EA202092586A1 true EA202092586A1 (ru) | 2021-03-10 |
Family
ID=68534223
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EA202092586A EA202092586A1 (ru) | 2018-05-15 | 2019-05-14 | Ингибиторы magl |
Country Status (25)
Country | Link |
---|---|
US (3) | US11332453B2 (ru) |
EP (1) | EP3793547A4 (ru) |
JP (1) | JP2021523200A (ru) |
KR (1) | KR20210010475A (ru) |
CN (1) | CN112088001A (ru) |
AR (1) | AR115092A1 (ru) |
AU (1) | AU2019271123A1 (ru) |
BR (1) | BR112020000863A2 (ru) |
CA (1) | CA3097063A1 (ru) |
CL (1) | CL2020002927A1 (ru) |
CO (1) | CO2020013550A2 (ru) |
CR (1) | CR20200545A (ru) |
DO (1) | DOP2020000207A (ru) |
EA (1) | EA202092586A1 (ru) |
GE (1) | GEP20227443B (ru) |
JO (1) | JOP20200276A1 (ru) |
MA (1) | MA52635A (ru) |
MX (1) | MX2020012158A (ru) |
NI (1) | NI202000080A (ru) |
PE (1) | PE20211385A1 (ru) |
PH (1) | PH12020551934A1 (ru) |
SG (1) | SG11202011228TA (ru) |
TW (1) | TW201946906A (ru) |
WO (1) | WO2019222266A1 (ru) |
ZA (1) | ZA202006327B (ru) |
Families Citing this family (13)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
SG11201403876RA (en) | 2012-01-06 | 2014-08-28 | Abide Therapeutics Inc | Carbamate compounds and of making and using same |
ES2892952T3 (es) | 2016-09-19 | 2022-02-07 | H Lundbeck As | Carbamatos de piperazina como moduladores del MAGL y/o ABHD6 y su uso |
PL3793565T3 (pl) | 2018-05-14 | 2022-05-02 | Gilead Sciences, Inc. | Inhibitory MCL-1 |
CA3097063A1 (en) | 2018-05-15 | 2019-11-21 | Lundbeck La Jolla Research Center, Inc. | Magl inhibitors |
AU2019294256B2 (en) | 2018-06-27 | 2024-06-20 | Eth Zuerich | Novel pyridine and pyrazine compounds as inhibitors of cannabinoid receptor 2 |
WO2020002314A1 (en) | 2018-06-27 | 2020-01-02 | F. Hoffmann-La Roche Ag | Radiolabeled cannabinoid receptor 2 ligand |
WO2020154683A1 (en) * | 2019-01-25 | 2020-07-30 | Lundbeck La Jolla Research Center, Inc. | Methods of treating disease with magl inhibitors |
TWI778443B (zh) | 2019-11-12 | 2022-09-21 | 美商基利科學股份有限公司 | Mcl1抑制劑 |
BR112021013917A2 (pt) * | 2019-11-15 | 2022-05-24 | H Lundbeck As | Forma cristalina de um inibidor de magl, composição farmacêutica e uso |
EP4065567B1 (en) | 2019-11-26 | 2024-09-11 | Gilead Sciences, Inc. | Processes and intermediates for preparing mcl1 inhibitors |
AU2021259496A1 (en) | 2020-04-21 | 2022-11-10 | H. Lundbeck A/S | Synthesis of a monoacylglycerol lipase inhibitor |
EP4198023A1 (en) | 2021-12-16 | 2023-06-21 | Basf Se | Pesticidally active thiosemicarbazone compounds |
WO2023156402A1 (en) | 2022-02-17 | 2023-08-24 | Basf Se | Pesticidally active thiosemicarbazone compounds |
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EP1201298A1 (en) | 2000-10-24 | 2002-05-02 | Urea Casale S.A. | Carbamate condensation unit |
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WO2005063698A1 (en) | 2003-12-31 | 2005-07-14 | Council Of Scientific & Industrial Research | Process for preparing carbamates |
BRPI0507499A (pt) | 2004-02-18 | 2007-07-24 | Astrazeneca Ab | composto ou um sal farmaceuticamente aceitável ou hidrato dos mesmos, composição farmacêutica, uso do composto, e, métodos para tratar distúrbios mediados por mglur 5 e para inibir a ativação de receptores de mglur 5 |
JP2008521768A (ja) | 2004-12-23 | 2008-06-26 | エフ.ホフマン−ラ ロシュ アーゲー | ヘテロ環式カルバミン酸誘導体、それらの製造及び医薬品としての使用 |
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JP2009514935A (ja) | 2005-11-05 | 2009-04-09 | アストラゼネカ・アクチエボラーグ | 新規化合物 |
JP2009523729A (ja) | 2006-01-13 | 2009-06-25 | ピーティーシー セラピューティクス,インコーポレーテッド | C型肝炎の治療方法 |
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CN101711154A (zh) | 2007-02-26 | 2010-05-19 | 科森生物科学公司 | 氨基甲酸酯化合物 |
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AU2010229134A1 (en) | 2009-03-23 | 2011-11-10 | Msd K.K. | Novel aminopyridine derivatives having Aurora A selective inhibitory action |
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EP3271352B1 (en) | 2015-03-18 | 2021-05-12 | H. Lundbeck A/S | Piperazine carbamates and methods of making and using same |
ES2892952T3 (es) | 2016-09-19 | 2022-02-07 | H Lundbeck As | Carbamatos de piperazina como moduladores del MAGL y/o ABHD6 y su uso |
JOP20190105A1 (ar) | 2016-11-16 | 2019-05-09 | Lundbeck La Jolla Research Center Inc | مثبطات أحادي أسيل جليسرول ليباز (magl) |
CR20190242A (es) | 2016-11-16 | 2019-07-09 | Abide Therapeutics Inc | Formas cristalinas de inhibidor de magl |
JOP20190106A1 (ar) | 2016-11-16 | 2019-05-09 | Lundbeck La Jolla Research Center Inc | مثبطات أحادي أسيل جليسرول ليباز (magl) |
BR112020003946A2 (pt) | 2017-08-29 | 2020-09-08 | Lundbeck La Jolla Research Center, Inc. | compostos de espirociclo e métodos para produzir e usar os mesmos |
CA3097063A1 (en) | 2018-05-15 | 2019-11-21 | Lundbeck La Jolla Research Center, Inc. | Magl inhibitors |
WO2020154683A1 (en) | 2019-01-25 | 2020-07-30 | Lundbeck La Jolla Research Center, Inc. | Methods of treating disease with magl inhibitors |
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2019
- 2019-05-14 CA CA3097063A patent/CA3097063A1/en active Pending
- 2019-05-14 CN CN201980031137.4A patent/CN112088001A/zh active Pending
- 2019-05-14 SG SG11202011228TA patent/SG11202011228TA/en unknown
- 2019-05-14 WO PCT/US2019/032289 patent/WO2019222266A1/en active Application Filing
- 2019-05-14 AU AU2019271123A patent/AU2019271123A1/en not_active Abandoned
- 2019-05-14 US US17/055,079 patent/US11332453B2/en active Active
- 2019-05-14 GE GEAP201915479A patent/GEP20227443B/en unknown
- 2019-05-14 MX MX2020012158A patent/MX2020012158A/es unknown
- 2019-05-14 EP EP19803143.7A patent/EP3793547A4/en not_active Withdrawn
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NI202000080A (es) | 2021-02-15 |
KR20210010475A (ko) | 2021-01-27 |
CR20200545A (es) | 2020-12-17 |
US20190352273A1 (en) | 2019-11-21 |
EP3793547A1 (en) | 2021-03-24 |
CN112088001A (zh) | 2020-12-15 |
DOP2020000207A (es) | 2021-02-15 |
JOP20200276A1 (ar) | 2020-11-02 |
US11214557B2 (en) | 2022-01-04 |
MA52635A (fr) | 2021-03-24 |
BR112020000863A2 (pt) | 2020-12-08 |
WO2019222266A1 (en) | 2019-11-21 |
SG11202011228TA (en) | 2020-12-30 |
MX2020012158A (es) | 2021-01-29 |
AR115092A1 (es) | 2020-11-25 |
JP2021523200A (ja) | 2021-09-02 |
GEP20227443B (en) | 2022-11-25 |
US20200148653A1 (en) | 2020-05-14 |
CL2020002927A1 (es) | 2021-03-05 |
US20210206735A1 (en) | 2021-07-08 |
ZA202006327B (en) | 2022-06-29 |
PH12020551934A1 (en) | 2021-06-21 |
EP3793547A4 (en) | 2021-11-17 |
CA3097063A1 (en) | 2019-11-21 |
AU2019271123A1 (en) | 2020-11-26 |
CO2020013550A2 (es) | 2020-11-10 |
US11332453B2 (en) | 2022-05-17 |
TW201946906A (zh) | 2019-12-16 |
PE20211385A1 (es) | 2021-07-27 |
US10570106B2 (en) | 2020-02-25 |
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