MX2020011049A - Oxadiazolopirazinas y oxadiazolopiridinas útiles como desacopladores mitocondriales. - Google Patents
Oxadiazolopirazinas y oxadiazolopiridinas útiles como desacopladores mitocondriales.Info
- Publication number
- MX2020011049A MX2020011049A MX2020011049A MX2020011049A MX2020011049A MX 2020011049 A MX2020011049 A MX 2020011049A MX 2020011049 A MX2020011049 A MX 2020011049A MX 2020011049 A MX2020011049 A MX 2020011049A MX 2020011049 A MX2020011049 A MX 2020011049A
- Authority
- MX
- Mexico
- Prior art keywords
- formula
- compounds
- useful
- mitochondrial
- salts
- Prior art date
Links
Classifications
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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
- C07D241/14—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 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 carbon atoms
- C07D241/18—Oxygen or sulfur atoms
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- 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
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
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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
- A61K31/495—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
- A61K31/4965—Non-condensed pyrazines
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- 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
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- 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
-
- 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
- A61P3/04—Anorexiants; Antiobesity agents
-
- 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
- A61P3/06—Antihyperlipidemics
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- 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
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
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- 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
- C07D213/60—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 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 carbon atoms
- C07D213/72—Nitrogen atoms
- C07D213/73—Unsubstituted amino or imino radicals
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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
- C07D241/14—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 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 carbon atoms
- C07D241/16—Halogen atoms; Nitro radicals
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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
- C07D241/14—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 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 carbon atoms
- C07D241/20—Nitrogen atoms
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- 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
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic Table
- C07F5/02—Boron compounds
- C07F5/025—Boronic and borinic acid compounds
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Diabetes (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Epidemiology (AREA)
- Child & Adolescent Psychology (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Psychology (AREA)
- Immunology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Gastroenterology & Hepatology (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Pyridine Compounds (AREA)
Abstract
La descripción proporciona compuestos de Fórmula I:(VER FORMULA) y las sales farmacéuticamente aceptables de estos. Las variables, R1, R2, R3, X1, X2, y Z se definen en la presente. Determinados compuestos de Fórmula I actúan como desacopladores de protonóforos mitocondriales selectivos que no afectan el potencial de la membrana plasmática. Los compuestos y sales de Fórmula I son útiles para tratar o reducir el riesgo de afecciones que responden al desacoplamiento mitocondrial, tales como cáncer, obesidad, diabetes de tipo II, enfermedad de hígado graso, resistencia a la insulina, enfermedad de Parkinson, lesión por isquemia-reperfusión, insuficiencia cardíaca, enfermedad del hígado graso no alcohólico (NALFD) y esteatohepatitis no alcohólica (NASH). Debido a que los desacopladores mitocondriales reducen la producción de especies reactivas de oxígeno (ROS), que se sabe contribuyen al daño celular relacionado con la edad, los compuestos de Fórmula I son útiles para aumentar la esperanza de vida. Los compuestos y sales de Fórmula I también son útiles para regular la homeostasis de glucosa o la acción de la insulina en un paciente.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862660880P | 2018-04-20 | 2018-04-20 | |
| PCT/US2019/028544 WO2019204813A1 (en) | 2018-04-20 | 2019-04-22 | Oxadiazolopyrazines and oxadiazolopyridines useful as mitochondrial uncouplers |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| MX2020011049A true MX2020011049A (es) | 2021-01-08 |
Family
ID=67139787
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2020011050A MX2020011050A (es) | 2018-04-20 | 2019-04-22 | Imidazopiridinas útiles como desacopladores mitocondriales. |
| MX2020011049A MX2020011049A (es) | 2018-04-20 | 2019-04-22 | Oxadiazolopirazinas y oxadiazolopiridinas útiles como desacopladores mitocondriales. |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2020011050A MX2020011050A (es) | 2018-04-20 | 2019-04-22 | Imidazopiridinas útiles como desacopladores mitocondriales. |
Country Status (12)
| Country | Link |
|---|---|
| US (3) | US11708376B2 (es) |
| EP (3) | EP3781567B1 (es) |
| JP (3) | JP2021522327A (es) |
| KR (3) | KR102900692B1 (es) |
| CN (3) | CN112262146A (es) |
| AU (2) | AU2019256719A1 (es) |
| BR (2) | BR112020021466A2 (es) |
| CA (2) | CA3097752A1 (es) |
| IL (2) | IL278070A (es) |
| MX (2) | MX2020011050A (es) |
| WO (3) | WO2019204816A1 (es) |
| ZA (2) | ZA202006296B (es) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2021522327A (ja) * | 2018-04-20 | 2021-08-30 | バージニア・テック・インテレクチュアル・プロパティーズ・インコーポレイテッドＶｉｒｇｉｎｉａ Ｔｅｃｈ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｉｅｓ， Ｉｎｃ． | ミトコンドリア脱共役剤として有用なオキサジアゾロピラジンおよびオキサジアゾロピリジン |
| WO2020191503A1 (en) * | 2019-03-27 | 2020-10-01 | Algernon Pharmaceuticals Inc. | Methods and uses of bromantane and derivatives thereof for treating lung disease, fatty liver disease, and kidney disorders |
| US11351149B2 (en) | 2020-09-03 | 2022-06-07 | Pfizer Inc. | Nitrile-containing antiviral compounds |
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| FR2501680A1 (fr) | 1981-03-12 | 1982-09-17 | Elf Aquitaine | Synthese de tetra mercaptides stanniques |
| US4472840A (en) | 1981-09-21 | 1984-09-25 | Jefferies Steven R | Method of inducing osseous formation by implanting bone graft material |
| US4559157A (en) | 1983-04-21 | 1985-12-17 | Creative Products Resource Associates, Ltd. | Cosmetic applicator useful for skin moisturizing |
| LU84979A1 (fr) | 1983-08-30 | 1985-04-24 | Oreal | Composition cosmetique ou pharmaceutique sous forme aqueuse ou anhydre dont la phase grasse contient un polyether oligomere et polyethers oligomeres nouveaux |
| US4820508A (en) | 1987-06-23 | 1989-04-11 | Neutrogena Corporation | Skin protective composition |
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| JP2668259B2 (ja) * | 1988-02-18 | 1997-10-27 | 塩野義製薬株式会社 | 複素環化合物および抗潰瘍剤 |
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| JPH0327172A (ja) | 1989-06-19 | 1991-02-05 | Nissan Chem Ind Ltd | 布の漂白方法 |
| US5645591A (en) | 1990-05-29 | 1997-07-08 | Stryker Corporation | Synthetic bone matrix |
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| AU783915B2 (en) * | 2000-02-16 | 2005-12-22 | Neurogen Corporation | Substituted arylpyrazines |
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| JP2008515979A (ja) * | 2004-10-14 | 2008-05-15 | コンパス ファーマシューティカルズ リミティド ライアビリティ カンパニー | フラザノ‘３，４−ビピラジン（ｂｉｐｙｒａｚｉｎｅ）及び抗腫瘍剤としてのその使用 |
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| ES2270715B1 (es) * | 2005-07-29 | 2008-04-01 | Laboratorios Almirall S.A. | Nuevos derivados de pirazina. |
| EP1966164B1 (en) * | 2005-12-21 | 2013-03-06 | Janssen Pharmaceutica N.V. | Novel substituted pyrazinone derivatives for use in mch-1 mediated diseases |
| EP2017277A1 (en) * | 2007-06-29 | 2009-01-21 | 4Sc Ag | Thiophene-imidazopyridines |
| WO2009086303A2 (en) | 2007-12-21 | 2009-07-09 | University Of Rochester | Method for altering the lifespan of eukaryotic organisms |
| ES2562957T3 (es) * | 2009-04-30 | 2016-03-09 | Midwestern University | Método y composición para el tratamiento de la cetoacidosis diabética |
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| JP2020520949A (ja) * | 2017-05-22 | 2020-07-16 | ユニバーシティ オブ ヴァージニア パテント ファウンデーションＵｎｉｖｅｒｓｉｔｙ Ｏｆ Ｖｅｒｇｉｎｉａ Ｐａｔｅｎｔ Ｆｏｕｎｄａｔｉｏｎ | 組成物、並びにミトコンドリア脱共役剤を調製及び使用する方法 |
| JP2021522327A (ja) * | 2018-04-20 | 2021-08-30 | バージニア・テック・インテレクチュアル・プロパティーズ・インコーポレイテッドＶｉｒｇｉｎｉａ Ｔｅｃｈ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｉｅｓ， Ｉｎｃ． | ミトコンドリア脱共役剤として有用なオキサジアゾロピラジンおよびオキサジアゾロピリジン |
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2019
- 2019-04-22 JP JP2021506388A patent/JP2021522327A/ja active Pending
- 2019-04-22 BR BR112020021466-3A patent/BR112020021466A2/pt not_active Application Discontinuation
- 2019-04-22 CN CN201980038732.0A patent/CN112262146A/zh active Pending
- 2019-04-22 CN CN201980038852.0A patent/CN112261941A/zh active Pending
- 2019-04-22 WO PCT/US2019/028555 patent/WO2019204816A1/en not_active Ceased
- 2019-04-22 US US17/049,232 patent/US11708376B2/en active Active
- 2019-04-22 CA CA3097752A patent/CA3097752A1/en active Pending
- 2019-04-22 KR KR1020207033356A patent/KR102900692B1/ko active Active
- 2019-04-22 US US17/048,897 patent/US20210253594A1/en not_active Abandoned
- 2019-04-22 WO PCT/US2019/028544 patent/WO2019204813A1/en not_active Ceased
- 2019-04-22 EP EP19735421.0A patent/EP3781567B1/en active Active
- 2019-04-22 US US17/049,145 patent/US20210253538A1/en not_active Abandoned
- 2019-04-22 WO PCT/US2019/028560 patent/WO2019204819A1/en not_active Ceased
- 2019-04-22 EP EP19789309.2A patent/EP3781165A4/en not_active Withdrawn
- 2019-04-22 BR BR112020021469-8A patent/BR112020021469A2/pt not_active Application Discontinuation
- 2019-04-22 KR KR1020207033337A patent/KR102913366B1/ko active Active
- 2019-04-22 CA CA3097751A patent/CA3097751A1/en active Pending
- 2019-04-22 JP JP2021506391A patent/JP2021523934A/ja active Pending
- 2019-04-22 MX MX2020011050A patent/MX2020011050A/es unknown
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- 2019-04-22 EP EP19735420.2A patent/EP3781572A1/en active Pending
- 2019-04-22 AU AU2019256719A patent/AU2019256719A1/en not_active Abandoned
- 2019-04-22 CN CN201980038722.7A patent/CN112262141A/zh active Pending
- 2019-04-22 KR KR1020207033297A patent/KR20210003831A/ko not_active Withdrawn
- 2019-04-22 AU AU2019256722A patent/AU2019256722A1/en not_active Abandoned
- 2019-04-22 JP JP2021506390A patent/JP2021523933A/ja active Pending
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2020
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