ECSP18072109A - Derivados de pirazolo[1,5-a]pirazin-4-ilo como inhibidores de jak campo de la invención - Google Patents
Derivados de pirazolo[1,5-a]pirazin-4-ilo como inhibidores de jak campo de la invenciónInfo
- Publication number
- ECSP18072109A ECSP18072109A ECSENADI201872109A ECDI201872109A ECSP18072109A EC SP18072109 A ECSP18072109 A EC SP18072109A EC SENADI201872109 A ECSENADI201872109 A EC SENADI201872109A EC DI201872109 A ECDI201872109 A EC DI201872109A EC SP18072109 A ECSP18072109 A EC SP18072109A
- Authority
- EC
- Ecuador
- Prior art keywords
- alkyl
- hydroxy
- independently
- heteroaryl
- heterocyclic
- Prior art date
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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
- A61K31/33—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
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/14—Drugs for dermatological disorders for baldness or alopecia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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- 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
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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
-
- 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
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
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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
- A61P37/02—Immunomodulators
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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
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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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
- A61P37/08—Antiallergic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- 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)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Immunology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Diabetes (AREA)
- Dermatology (AREA)
- Pulmonology (AREA)
- Rheumatology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Epidemiology (AREA)
- Pain & Pain Management (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Transplantation (AREA)
- Gastroenterology & Hepatology (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Urology & Nephrology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Un compuesto que tiene la siguiente estructura (ver fórmula en imagen adjunta) o una sal de este aceptable desde el punto de vista farmacéutico, o un solvato aceptable desde el punto de vista farmacéutico de un compuesto o una sal aceptable desde el punto de vista farmacéutico, en donde A, A y A son independientemente O, C=O, C-R o N-R, en donde R y R pueden ser independientemente H, amino, -NR7COR6, COR6, -CONR7R8, C1-C6 alquilo o hidroxi(C1-C6 alquilo), y R puede estar presente o ausente, y está presente donde las reglas de valencia lo permiten, y en donde no más de uno de A, A y A es O o C=O; R0 y R son independientemente H, Br, Cl, F o C1-C6 alquilo; R1 es H, C1-C6 alquilo o hidroxi(C1-C6 alquilo); R2 se selecciona del grupo que consiste en H, C1-C6 alquilo, C1-C6 alcoxi, hidroxi(C1-C6 alquilo), fenil(C1-C6 alquilo), formilo, heteroarilo, heterocíclico, -COR6, -OCOR6, -COOR6, -NR7COR6, -CONR7R8 y -(CH2)n-W, en donde W es ciano, hidroxi, C3-C8 cicloalquilo, -SO2NR7R8 y -SO2-R9, en donde R9 es C1-C6 alquilo, C3-C8 cicloalquilo, heteroarilo o heterocíclico; en donde cada uno de alquilo, cicloalquilo, heterocíclico o heteroarilo puede ser no sustituido o sustituido por halo, ciano, hidroxi o C1-C6 alquilo; X es C-R3 o N, en donde R3 puede ser H o C1-C6 alquilo; R4 y R5 son independientemente H, amino, C1-C6 alquilo o hidroxi(C1-C6 alquilo); R6, R7 y R8 son... (el resumen completo se adjunta a los documentos de la solicitud).
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662299130P | 2016-02-24 | 2016-02-24 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ECSP18072109A true ECSP18072109A (es) | 2018-10-31 |
Family
ID=58054385
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ECSENADI201872109A ECSP18072109A (es) | 2016-02-24 | 2018-09-24 | Derivados de pirazolo[1,5-a]pirazin-4-ilo como inhibidores de jak campo de la invención |
Country Status (45)
Families Citing this family (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| UA119835C2 (uk) | 2016-02-24 | 2019-08-12 | Пфайзер Інк. | ПОХІДНІ ПІРАЗОЛО[1,5-а]ПІРАЗИН-4-ІЛУ ЯК JAK-ІНГІБІТОРИ |
| BR112020017421A2 (pt) | 2018-02-27 | 2020-12-22 | Incyte Corporation | Imidazopirimidinas e triazolopirimidinas como inibidores de a2a/a2b |
| UY38144A (es) | 2018-03-12 | 2019-10-31 | Abbvie Inc | Inhibidores de la señalización mediada por tirosina cinasa |
| WO2019219517A1 (en) | 2018-05-17 | 2019-11-21 | Bayer Aktiengesellschaft | Substituted dihydropyrazolo pyrazine carboxamide derivatives |
| MA52940A (fr) | 2018-05-18 | 2021-04-28 | Incyte Corp | Dérivés de pyrimidine fusionnés utilisés en tant qu'inhibiteurs de a2a/a2b |
| GEP20237560B (en) | 2018-07-05 | 2023-10-25 | Incyte Corp | Fused pyrazine derivatives as a2a / a2b inhibitors |
| TW202033198A (zh) | 2018-10-17 | 2020-09-16 | 美商美國禮來大藥廠 | 以巴瑞克替尼(baricitinib)治療原發性膽汁性膽管炎及原發性硬化性膽管炎 |
| TWI829857B (zh) | 2019-01-29 | 2024-01-21 | 美商英塞特公司 | 作為a2a / a2b抑制劑之吡唑并吡啶及三唑并吡啶 |
| AU2020256720B2 (en) * | 2019-04-12 | 2022-09-01 | PrimeGene (Beijing) Co. Ltd. | Pyrazolopyrazine derived compounds, pharmaceutical composition and use thereof |
| AU2019443366A1 (en) | 2019-04-30 | 2021-12-02 | Celgene Corporation | Combination therapies comprising apremilast and Tyk2 inhibitors |
| CA3153676A1 (en) | 2019-09-11 | 2021-03-18 | Pfizer Inc. | Treatment of hidradenitis with jak inhibitors |
| TW202135816A (zh) * | 2019-12-18 | 2021-10-01 | 美商輝瑞股份有限公司 | 以激酶抑制劑治療潰瘍性結腸炎 |
| BR112022020020A2 (pt) | 2020-04-04 | 2022-11-22 | Pfizer | Métodos de tratamento da doença do coronavírus 2019 |
| US20230159539A1 (en) * | 2020-04-08 | 2023-05-25 | Pfizer Inc. | Crystalline forms of 3-cyano-1-[4-[6-(1-methyl-1h-pyrazol-4-yl)pyrazolo[1,5-a]pyrazin-4-yl]-1h-pyrazol-1-yl]cyclobutaneacetonitrile, and use thereof |
| WO2022056196A1 (en) * | 2020-09-11 | 2022-03-17 | Pulmosim Therapeutics Llc | Compositions and methods for treating or preventing pulmonary hypertension |
| CN112592345A (zh) * | 2020-12-07 | 2021-04-02 | 嘉兴特科罗生物科技有限公司 | 一种三氮唑并吡嗪类化合物及其用途 |
| EP4284802A1 (en) * | 2021-02-01 | 2023-12-06 | Janssen Biotech, Inc. | Small molecule inhibitors of salt inducible kinases |
| US20240156822A1 (en) | 2021-03-30 | 2024-05-16 | Pfizer Inc. | Methods For Treatment of Vitiligo |
| WO2023076161A1 (en) | 2021-10-25 | 2023-05-04 | Kymera Therapeutics, Inc. | Tyk2 degraders and uses thereof |
| CA3237632A1 (en) * | 2021-11-12 | 2023-05-19 | Changqing WEI | Pyrazolo fused ring compound and use thereof |
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| CN101679408B (zh) | 2006-12-22 | 2016-04-27 | Astex治疗学有限公司 | 作为fgfr抑制剂的双环杂环化合物 |
| AR066879A1 (es) * | 2007-06-08 | 2009-09-16 | Novartis Ag | Derivados de quinoxalina como inhibidores de la actividad de cinasa de tirosina de las cinasas janus |
| CL2008001709A1 (es) | 2007-06-13 | 2008-11-03 | Incyte Corp | Compuestos derivados de pirrolo [2,3-b]pirimidina, moduladores de quinasas jak; composicion farmaceutica; y uso en el tratamiento de enfermedades tales como cancer, psoriasis, artritis reumatoide, entre otras. |
| TWI527819B (zh) | 2008-06-10 | 2016-04-01 | 艾伯維有限公司 | 新穎三環化合物 |
| WO2010016005A1 (en) | 2008-08-06 | 2010-02-11 | Pfizer Inc. | 6 substituted 2-heterocyclylamino pyrazine compounds as chk-1 inhibitors |
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| UY33213A (es) * | 2010-02-18 | 2011-09-30 | Almirall Sa | Derivados de pirazol como inhibidores de jak |
| CN102985424B (zh) * | 2010-04-14 | 2015-03-11 | 阵列生物制药公司 | 5,7-取代的-咪唑并[1,2-c]嘧啶 |
| EP2397482A1 (en) | 2010-06-15 | 2011-12-21 | Almirall, S.A. | Heteroaryl imidazolone derivatives as jak inhibitors |
| RU2014118954A (ru) * | 2011-10-12 | 2015-11-20 | Эррэй Биофарма Инк. | 5,7-ЗАМЕЩЕННЫЕ-ИМИДАЗО[1,2-c]ПИРИМИДИНЫ |
| EP2832734A4 (en) * | 2012-03-28 | 2015-08-26 | Takeda Pharmaceutical | HETEROCYCLIC CONNECTION |
| DK2831077T3 (en) | 2012-03-28 | 2016-08-15 | Merck Patent Gmbh | BICYCLIC PYRAZINO DERIVATIVES |
| JP6159028B2 (ja) | 2013-07-31 | 2017-07-05 | ギリアード サイエンシーズ， インコーポレイテッド | Ｓｙｋ阻害剤 |
| WO2015086693A1 (en) | 2013-12-11 | 2015-06-18 | Almirall, S.A. | Pyrazolopyrimidin-2-yl derivatives as jak inhibitors |
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| WO2016009028A1 (fr) | 2014-07-17 | 2016-01-21 | Valeo Systèmes d'Essuyage | Balai plat caréné d'essuie-glace |
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| CA2976109A1 (en) | 2015-02-13 | 2016-08-18 | Dana-Farber Cancer Institute, Inc. | Substituted pyrrolopyrimidine, pyrazolopyrimidine and purine derivatives and use thereof as lrrk2 inhibitors |
| GB201504565D0 (en) | 2015-03-18 | 2015-05-06 | Takeda Pharmaceutical | Novel compounds |
| PT3290418T (pt) | 2015-04-29 | 2019-07-16 | Wuxi Fortune Pharmaceutical Co Ltd | Inibidores de janus quinase (jak) |
| EP3394066A2 (en) | 2015-12-22 | 2018-10-31 | H. Hoffnabb-La Roche Ag | PYRAZOLO[1,5a]PYRIMIDINE DERIVATIVES AS IRAK4 MODULATORS |
| UA119835C2 (uk) | 2016-02-24 | 2019-08-12 | Пфайзер Інк. | ПОХІДНІ ПІРАЗОЛО[1,5-а]ПІРАЗИН-4-ІЛУ ЯК JAK-ІНГІБІТОРИ |
| US10703757B2 (en) | 2016-12-23 | 2020-07-07 | Plexxikon Inc. | Compounds and methods for CDK8 modulation and indications therefor |
| US11168090B2 (en) | 2017-01-18 | 2021-11-09 | Array Biopharma Inc. | Substituted pyrazolo[1,5-a]pyrazines as RET kinase inhibitors |
| WO2018234342A1 (en) | 2017-06-21 | 2018-12-27 | F. Hoffmann-La Roche Ag | ISOINDOLINONE DERIVATIVES AS MODULATORS OF IRAK4 |
| EP3668858A1 (en) | 2017-08-14 | 2020-06-24 | Pfizer Inc | Pyrazolo[1,5-a]pyrazin-4-yl and related derivatives |
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2017
- 2017-02-10 UA UAA201808148A patent/UA119835C2/uk unknown
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- 2017-02-10 KR KR1020187024431A patent/KR102128671B1/ko active IP Right Grant
- 2017-02-10 ME MEP-2020-97A patent/ME03743B/me unknown
- 2017-02-10 DK DK17705705.6T patent/DK3419978T3/da active
- 2017-02-10 SI SI201730289T patent/SI3419978T1/sl unknown
- 2017-02-10 RS RS20200584A patent/RS60261B1/sr unknown
- 2017-02-10 HU HUE17705705A patent/HUE049305T2/hu unknown
- 2017-02-10 MD MDE20190031T patent/MD3419978T2/ro unknown
- 2017-02-10 PL PL17705705T patent/PL3419978T3/pl unknown
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- 2017-02-10 CU CU2018000078A patent/CU24511B1/es unknown
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- 2017-02-10 AU AU2017222417A patent/AU2017222417B2/en active Active
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- 2017-02-10 EP EP17705705.6A patent/EP3419978B1/en active Active
- 2017-02-21 US US15/437,618 patent/US10144738B2/en active Active
- 2017-02-21 CA CA2958490A patent/CA2958490C/en active Active
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- 2017-02-22 UY UY0001037133A patent/UY37133A/es unknown
- 2017-02-23 AR ARP170100462A patent/AR107714A1/es unknown
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2018
- 2018-07-18 SV SV2018005726A patent/SV2018005726A/es unknown
- 2018-07-24 ZA ZA2018/04972A patent/ZA201804972B/en unknown
- 2018-08-01 IL IL260923A patent/IL260923B/en unknown
- 2018-08-03 NI NI201800080A patent/NI201800080A/es unknown
- 2018-08-17 CL CL2018002358A patent/CL2018002358A1/es unknown
- 2018-08-23 PH PH12018501788A patent/PH12018501788A1/en unknown
- 2018-08-24 DO DO2018000187A patent/DOP2018000187A/es unknown
- 2018-09-24 EC ECSENADI201872109A patent/ECSP18072109A/es unknown
- 2018-11-06 US US16/181,596 patent/US10822341B2/en active Active
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2019
- 2019-01-14 HK HK19100512.8A patent/HK1258157A1/zh unknown
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2020
- 2020-05-13 HR HRP20200781TT patent/HRP20200781T1/hr unknown
- 2020-05-15 CY CY20201100470T patent/CY1122949T1/el unknown
- 2020-09-08 US US17/014,533 patent/US11472809B2/en active Active
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2022
- 2022-09-07 US US17/939,375 patent/US20230045252A1/en active Pending
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