KR20190080935A - Magl 억제제 - Google Patents
Magl 억제제 Download PDFInfo
- Publication number
- KR20190080935A KR20190080935A KR1020197017201A KR20197017201A KR20190080935A KR 20190080935 A KR20190080935 A KR 20190080935A KR 1020197017201 A KR1020197017201 A KR 1020197017201A KR 20197017201 A KR20197017201 A KR 20197017201A KR 20190080935 A KR20190080935 A KR 20190080935A
- Authority
- KR
- South Korea
- Prior art keywords
- pharmaceutically acceptable
- solvate
- acceptable salt
- formula
- compound
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Ceased
Links
- 229940122357 Monoacylglycerol lipase inhibitor Drugs 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims abstract description 1055
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract description 25
- 208000002193 Pain Diseases 0.000 claims abstract description 24
- 238000011282 treatment Methods 0.000 claims abstract description 9
- 150000003839 salts Chemical class 0.000 claims description 1116
- 239000012453 solvate Substances 0.000 claims description 1072
- 125000000217 alkyl group Chemical group 0.000 claims description 483
- 229910052739 hydrogen Inorganic materials 0.000 claims description 217
- 229910052799 carbon Inorganic materials 0.000 claims description 187
- 229910052736 halogen Inorganic materials 0.000 claims description 124
- 150000002367 halogens Chemical class 0.000 claims description 116
- 238000000034 method Methods 0.000 claims description 102
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims description 95
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 60
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 46
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 44
- 125000001072 heteroaryl group Chemical group 0.000 claims description 37
- 201000010099 disease Diseases 0.000 claims description 36
- 125000003545 alkoxy group Chemical group 0.000 claims description 35
- 125000003118 aryl group Chemical group 0.000 claims description 35
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- 208000035475 disorder Diseases 0.000 claims description 24
- XEEYBQQBJWHFJM-UHFFFAOYSA-N Iron Chemical compound [Fe] XEEYBQQBJWHFJM-UHFFFAOYSA-N 0.000 claims description 21
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- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 17
- 229910052757 nitrogen Inorganic materials 0.000 claims description 16
- 206010015037 epilepsy Diseases 0.000 claims description 14
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 12
- HEDRZPFGACZZDS-UHFFFAOYSA-N Chloroform Chemical compound ClC(Cl)Cl HEDRZPFGACZZDS-UHFFFAOYSA-N 0.000 claims description 12
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- 125000001475 halogen functional group Chemical group 0.000 claims 1
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- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 35
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 33
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- 238000005481 NMR spectroscopy Methods 0.000 description 19
- 235000019439 ethyl acetate Nutrition 0.000 description 19
- 229940124597 therapeutic agent Drugs 0.000 description 19
- 125000002947 alkylene group Chemical group 0.000 description 18
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- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 description 16
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 description 15
- 125000004446 heteroarylalkyl group Chemical group 0.000 description 15
- NSGXIBWMJZWTPY-UHFFFAOYSA-N 1,1,1,3,3,3-hexafluoropropane Chemical compound FC(F)(F)CC(F)(F)F NSGXIBWMJZWTPY-UHFFFAOYSA-N 0.000 description 14
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- 125000003709 fluoroalkyl group Chemical group 0.000 description 12
- 125000004435 hydrogen atom Chemical group [H]* 0.000 description 12
- BWHMMNNQKKPAPP-UHFFFAOYSA-L potassium carbonate Chemical compound [K+].[K+].[O-]C([O-])=O BWHMMNNQKKPAPP-UHFFFAOYSA-L 0.000 description 12
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- IAZDPXIOMUYVGZ-UHFFFAOYSA-N Dimethylsulphoxide Chemical compound CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 description 9
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 9
- 102000005398 Monoacylglycerol Lipase Human genes 0.000 description 9
- 108020002334 Monoacylglycerol lipase Proteins 0.000 description 9
- 125000000304 alkynyl group Chemical group 0.000 description 9
- 125000001309 chloro group Chemical group Cl* 0.000 description 9
- 125000002704 decyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 description 9
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- 238000003786 synthesis reaction Methods 0.000 description 9
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Classifications
-
- 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
- C07D471/10—Spiro-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
- A61K31/435—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
- A61K31/438—The ring being spiro-condensed with carbocyclic or heterocyclic ring systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular 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
-
- 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
- A61P25/28—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
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Neurology (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662423102P | 2016-11-16 | 2016-11-16 | |
| US62/423,102 | 2016-11-16 | ||
| PCT/US2017/061870 WO2018093949A1 (en) | 2016-11-16 | 2017-11-15 | Magl inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| KR20190080935A true KR20190080935A (ko) | 2019-07-08 |
Family
ID=62145825
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020197017201A Ceased KR20190080935A (ko) | 2016-11-16 | 2017-11-15 | Magl 억제제 |
Country Status (27)
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US10030020B2 (en) * | 2016-05-12 | 2018-07-24 | Abide Therapeutics, Inc. | Spirocycle compounds and methods of making and using same |
| JOP20190107A1 (ar) | 2016-11-16 | 2019-05-09 | Lundbeck La Jolla Research Center Inc | مثبطات أحادي أسيل جليسرول ليباز (magl) |
| JOP20190105A1 (ar) * | 2016-11-16 | 2019-05-09 | Lundbeck La Jolla Research Center Inc | مثبطات أحادي أسيل جليسرول ليباز (magl) |
| HUE056973T2 (hu) | 2016-11-16 | 2022-04-28 | H Lundbeck As | MAGL inhibitor kristályos formája |
| CA3043609A1 (en) | 2016-11-16 | 2018-05-24 | Abide Therapeutics, Inc. | Pharmaceutical formulations |
| US10927105B1 (en) | 2017-05-23 | 2021-02-23 | Lundbeck La Jolla Research Center, Inc. | Pyrazole MAGL inhibitors |
| JOP20190262B1 (ar) | 2017-05-23 | 2023-09-17 | H Lundbeck As | مثبطات بيرازول magl |
| EP3675848B1 (en) | 2017-08-29 | 2022-03-23 | H. Lundbeck A/S | Spirocycle compounds and methods of making and using same |
| EP3675847B1 (en) | 2017-08-29 | 2023-07-12 | H. Lundbeck A/S | Spirocycle compounds and methods of making and using same |
| US20210309669A1 (en) * | 2018-07-19 | 2021-10-07 | Pfizer Inc. | Heterocyclic Spiro Compounds As MAGL Inhibitors |
| WO2020035424A1 (en) | 2018-08-13 | 2020-02-20 | F. Hoffmann-La Roche Ag | New heterocyclic compounds as monoacylglycerol lipase inhibitors |
| MX2022013224A (es) | 2020-04-21 | 2022-11-14 | H Lundbeck As | Sintesis de un inhibidor de la monoacilglicerol lipasa. |
| US11434222B2 (en) | 2020-11-13 | 2022-09-06 | H. Lundbeck A/S | MAGL inhibitors |
| KR20240128870A (ko) | 2021-12-29 | 2024-08-27 | 싸이 테라퓨틱스, 인크. | 모노아실글리세롤 리파아제(magl) 억제 |
| AU2023264787A1 (en) | 2022-05-04 | 2024-10-31 | H. Lundbeck A/S | Crystalline form of 1,1,1,3,3,3-hexafluoropropan-2-yl (s)-1-(pyridazin-3-ylcarbamoyl)-6 azaspiro[2.5]octane-6-carboxylate as monoacylglycerol lipase inhibitor. |
| WO2024168426A1 (en) | 2023-02-13 | 2024-08-22 | Apogee Pharmaceuticals, Inc. | Small molecules as monoacylglycerol lipase (magl) inhibitors, compositions and use thereof |
Family Cites Families (37)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US1003002A (en) | 1910-10-10 | 1911-09-12 | Gustave J Martel | Tire-patching device. |
| EP1368354A1 (en) | 2001-03-07 | 2003-12-10 | Pfizer Products Inc. | Modulators of chemokine receptor activity |
| 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 |
| EP2065369A4 (en) | 2006-08-23 | 2011-12-28 | Astellas Pharma Inc | UREA CONNECTION OR SALT THEREOF |
| CA2716863A1 (en) | 2008-03-05 | 2009-09-11 | Targacept, Inc. | Sub-type selective amides of diazabicycloalkanes |
| FR2941696B1 (fr) | 2009-02-05 | 2011-04-15 | Sanofi Aventis | Derives d'azaspiranyl-alkylcarbamates d'heterocycles a 5 chainons, leur preparation et leur application en therapeutique |
| US20120083476A1 (en) | 2009-06-05 | 2012-04-05 | Janssen Pharmaceutica Nv | Heteroaryl-substituted spirocyclic diamine urea modulators of fatty acid amide hydrolase |
| WO2011040905A1 (en) | 2009-09-29 | 2011-04-07 | Polyone Corporation | Polyester articles having simulated metallic or pearlescent appearance |
| MX2012004753A (es) | 2009-10-23 | 2012-09-07 | Janssen Pharmaceutica Nv | Octahidropirrolo[3,4-c]pirrolos disustituidos como moduladores del receptor de orexina. |
| JP2013521290A (ja) | 2010-03-04 | 2013-06-10 | メルク・シャープ・エンド・ドーム・コーポレイション | Ｍｇｌｕｒ２の正のアロステリックモジュレータ |
| FR2960875B1 (fr) | 2010-06-04 | 2012-12-28 | Sanofi Aventis | Derives de carbamates d'hexafluoroisopropyle, leur preparation et leur application en therapeutique |
| EP2444084A1 (en) | 2010-10-21 | 2012-04-25 | Centro Nacional de Investigaciones Oncológicas (CNIO) | Use of PI3K inibitors for the treatment of obesity |
| ES2982694T3 (es) * | 2012-01-06 | 2024-10-17 | H Lundbeck As | Compuestos de carbamato para su uso en tratamiento |
| JP2014005245A (ja) * | 2012-06-26 | 2014-01-16 | Dainippon Sumitomo Pharma Co Ltd | 二環性ピリミジン誘導体を含有する医薬組成物 |
| PL2900669T3 (pl) | 2012-09-25 | 2020-01-31 | F. Hoffmann-La Roche Ag | Pochodne heksahydropirolo[3,4-C]pirolu i związki pokrewne jako inhibitory autotaksyny (ATX) oraz inhibitory produkcji kwasu lizofosfatydowego (LPA) do leczenia np. chorób nerek |
| WO2015003002A1 (en) | 2013-07-03 | 2015-01-08 | Abide Therapeutics, Inc. | Pyrrolo-pyrrole carbamate and related organic compounds, pharmaceutical compositions, and medical uses thereof |
| SG11201607920RA (en) * | 2014-04-04 | 2016-10-28 | X Rx Inc | Substituted spirocyclic inhibitors of autotaxin |
| WO2015179559A2 (en) | 2014-05-21 | 2015-11-26 | Abide Therapeutics, Inc. | Pyrazole compounds and methods of making and using same |
| US9771341B2 (en) | 2015-03-18 | 2017-09-26 | Abide Therapeutics, Inc. | Piperazine carbamates and methods of making and using same |
| BR112017024253A2 (pt) | 2015-05-11 | 2018-07-24 | Abide Therapeutics Inc | métodos de tratamento de inflamação ou dor neuropática. |
| JP6832914B2 (ja) | 2015-07-31 | 2021-02-24 | ファイザー・インク | Ｍａｇｌ阻害薬としての１，１，１−トリフルオロ−３−ヒドロキシプロパン−２−イルカルバマート誘導体および１，１，１−トリフルオロ−４−ヒドロキシブタン−２−イルカルバマート誘導体 |
| WO2017087858A1 (en) | 2015-11-20 | 2017-05-26 | Abide Therapeutics, Inc. | Pyrazole compounds and methods of making and using same |
| WO2017087854A1 (en) | 2015-11-20 | 2017-05-26 | Abide Therapeutics, Inc. | Pyrazole compounds and methods of making and using same |
| US10323026B2 (en) | 2016-03-31 | 2019-06-18 | Takeda Pharmaceutical Company Limited | Heterocyclic compound |
| US10030020B2 (en) | 2016-05-12 | 2018-07-24 | Abide Therapeutics, Inc. | Spirocycle compounds and methods of making and using same |
| JOP20190050A1 (ar) | 2016-09-23 | 2019-03-20 | Bial Portela & C? S A | مثبطات دوبامين-b-هيدروكسيلاز تخترق حاجز المخ الدموي |
| JOP20190107A1 (ar) | 2016-11-16 | 2019-05-09 | Lundbeck La Jolla Research Center Inc | مثبطات أحادي أسيل جليسرول ليباز (magl) |
| HUE056973T2 (hu) | 2016-11-16 | 2022-04-28 | H Lundbeck As | MAGL inhibitor kristályos formája |
| JOP20190105A1 (ar) * | 2016-11-16 | 2019-05-09 | Lundbeck La Jolla Research Center Inc | مثبطات أحادي أسيل جليسرول ليباز (magl) |
| JOP20190106A1 (ar) | 2016-11-16 | 2019-05-09 | Lundbeck La Jolla Research Center Inc | مثبطات أحادي أسيل جليسرول ليباز (magl) |
| CA3043609A1 (en) | 2016-11-16 | 2018-05-24 | Abide Therapeutics, Inc. | Pharmaceutical formulations |
| HRP20241558T1 (hr) | 2017-03-13 | 2025-03-28 | Lundbeck La Jolla Research Center, Inc. | Dvojni inhibitori magl i faah |
| JOP20190262B1 (ar) | 2017-05-23 | 2023-09-17 | H Lundbeck As | مثبطات بيرازول magl |
| JOP20190267A1 (ar) | 2017-05-23 | 2019-11-18 | Lundbeck La Jolla Research Center Inc | مثبطات بيرازول magl |
| EP3675847B1 (en) | 2017-08-29 | 2023-07-12 | H. Lundbeck A/S | Spirocycle compounds and methods of making and using same |
| EP3675848B1 (en) | 2017-08-29 | 2022-03-23 | H. Lundbeck A/S | Spirocycle compounds and methods of making and using same |
| US11434222B2 (en) | 2020-11-13 | 2022-09-06 | H. Lundbeck A/S | MAGL inhibitors |
-
2017
- 2017-06-16 JO JOP/2019/0107A patent/JOP20190107A1/ar unknown
- 2017-11-15 WO PCT/US2017/061870 patent/WO2018093949A1/en not_active Ceased
- 2017-11-15 CA CA3043617A patent/CA3043617A1/en not_active Abandoned
- 2017-11-15 ES ES17871458T patent/ES2952582T3/es active Active
- 2017-11-15 CR CR20190239A patent/CR20190239A/es unknown
- 2017-11-15 RU RU2019115784A patent/RU2019115784A/ru unknown
- 2017-11-15 UA UAA201905617A patent/UA125523C2/uk unknown
- 2017-11-15 PE PE2019001017A patent/PE20191145A1/es unknown
- 2017-11-15 EA EA201991029A patent/EA038150B1/ru unknown
- 2017-11-15 CN CN201780083651.3A patent/CN110267962B/zh active Active
- 2017-11-15 MA MA046855A patent/MA46855A/fr unknown
- 2017-11-15 KR KR1020197017201A patent/KR20190080935A/ko not_active Ceased
- 2017-11-15 MX MX2019005773A patent/MX389627B/es unknown
- 2017-11-15 EP EP17871458.0A patent/EP3541820B1/en active Active
- 2017-11-15 BR BR112019009880A patent/BR112019009880A2/pt not_active IP Right Cessation
- 2017-11-15 AU AU2017361253A patent/AU2017361253B2/en not_active Ceased
- 2017-11-15 TN TNP/2019/000149A patent/TN2019000149A1/en unknown
- 2017-11-15 JP JP2019523671A patent/JP7042468B2/ja active Active
- 2017-11-15 US US16/349,047 patent/US11059822B2/en active Active
-
2019
- 2019-05-12 IL IL266547A patent/IL266547B/en unknown
- 2019-05-14 CO CONC2019/0004945A patent/CO2019004945A2/es unknown
- 2019-05-14 DO DO2019000118A patent/DOP2019000118A/es unknown
- 2019-05-15 EC ECSENADI201934535A patent/ECSP19034535A/es unknown
- 2019-05-15 PH PH12019501079A patent/PH12019501079A1/en unknown
- 2019-05-16 NI NI201900049A patent/NI201900049A/es unknown
- 2019-05-16 CL CL2019001336A patent/CL2019001336A1/es unknown
- 2019-05-17 ZA ZA2019/03099A patent/ZA201903099B/en unknown
-
2021
- 2021-06-09 US US17/343,227 patent/US11691975B2/en active Active
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