CR20180372A - Derivados de pirazolo [1,5-a] pirazin-4-ilo - Google Patents
Derivados de pirazolo [1,5-a] pirazin-4-iloInfo
- Publication number
- CR20180372A CR20180372A CR20180372A CR20180372A CR20180372A CR 20180372 A CR20180372 A CR 20180372A CR 20180372 A CR20180372 A CR 20180372A CR 20180372 A CR20180372 A CR 20180372A CR 20180372 A CR20180372 A CR 20180372A
- Authority
- CR
- Costa Rica
- Prior art keywords
- alkyl
- hydroxy
- independently
- cycloalkyl
- halo
- Prior art date
Links
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
-
- 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
-
- 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
Abstract
Un compuesto que tiene la siguiente estructura 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, cada uno independientemente, H, C1-C6 alquilo, C1-C4 alcoxi(C1-C6 alquilo) o C3-C8 cicloalquilo, dicho C1-C6 alquilo se sustituye opcionalmente con halo, CN o hidroxi; o R7 y R8, junto con el átomo unido a estos, forman un anillo de 5 o 6 miembros, en donde el anillo se sustituye opcionalmente con halo, hidroxi, CN o C1-C6 alquilo; y n es 0, 1, 2 o 3. También se proporcionan métodos de tratamiento tales como inhibidores de quinasas Janus y composiciones farmacéuticas que contienen los compuestos de la invención y combinaciones de estos con otros agentes terapéuticos.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201662299130P | 2016-02-24 | 2016-02-24 | |
PCT/IB2017/050748 WO2017144995A1 (en) | 2016-02-24 | 2017-02-10 | Pyrazolo[1,5-a]pyrazin-4-yl derivatives as jak-inhibitors |
Publications (1)
Publication Number | Publication Date |
---|---|
CR20180372A true CR20180372A (es) | 2018-09-19 |
Family
ID=58054385
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CR20180372A CR20180372A (es) | 2016-02-24 | 2017-02-10 | Derivados de pirazolo [1,5-a] pirazin-4-ilo |
Country Status (45)
Families Citing this family (19)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
RU2718902C2 (ru) | 2016-02-24 | 2020-04-15 | Пфайзер Инк. | Производные пиразоло[1,5-а]пиразин-4-ила в качестве jak-ингибиторов |
TW202000666A (zh) | 2018-02-27 | 2020-01-01 | 美商英塞特公司 | 作為a2a/a2b抑制劑之咪唑并嘧啶及***并嘧啶 |
TW201940483A (zh) | 2018-03-12 | 2019-10-16 | 美商艾伯維有限公司 | 酪胺酸激酶2介導的傳訊之抑制劑 |
EA202092779A1 (ru) | 2018-05-17 | 2021-02-02 | Байер Акциенгезельшафт | Замещенные дигидропиразолопиразинкарбоксамидные производные |
CA3100731A1 (en) | 2018-05-18 | 2019-11-21 | Incyte Corporation | Fused pyrimidine 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***并吡啶 |
MX2021012487A (es) * | 2019-04-12 | 2021-11-12 | Primegene Beijing Co Ltd | Compuestos derivados de pirazolopirazina, composicion farmaceutica y uso de la misma. |
CA3138473A1 (en) | 2019-04-30 | 2020-11-05 | Celgene Corporation | Combination therapies comprising apremilast and tyk2 inhibitors |
CN114667148A (zh) * | 2019-09-11 | 2022-06-24 | 辉瑞公司 | 用jak抑制剂治疗汗腺炎 |
WO2021124095A1 (en) * | 2019-12-18 | 2021-06-24 | Pfizer Inc. | Treatment of ulcerative colitis with kinase inhibitors |
CN115715194A (zh) | 2020-04-04 | 2023-02-24 | 辉瑞公司 | 治疗冠状病毒疾病2019的方法 |
CA3179566A1 (en) * | 2020-04-08 | 2021-10-14 | 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 |
US20230330083A1 (en) * | 2020-09-11 | 2023-10-19 | 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 |
WO2022165530A1 (en) * | 2021-02-01 | 2022-08-04 | Janssen Biotech, Inc. | Small molecule inhibitors of salt inducible kinases |
KR20230152087A (ko) | 2021-03-30 | 2023-11-02 | 화이자 인코포레이티드 | 백반증을 치료하는 방법 |
WO2023076161A1 (en) | 2021-10-25 | 2023-05-04 | Kymera Therapeutics, Inc. | Tyk2 degraders and uses thereof |
WO2023083200A1 (zh) * | 2021-11-12 | 2023-05-19 | 南京明德新药研发有限公司 | 吡唑并环化合物及其应用 |
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JP5442448B2 (ja) | 2006-12-22 | 2014-03-12 | アステックス、セラピューティックス、リミテッド | Fgfrインヒビターとしての二環式ヘテロ環式化合物 |
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. |
ME02340B (me) | 2008-06-10 | 2017-02-20 | Abbvie Inc | Triciklična jedinjenja |
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UA109131C2 (ru) * | 2010-04-14 | 2015-07-27 | Еррей Біофарма Інк. | 5,7-ЗАМЕЩЕННЫЕ ИМИДАЗО[1,2-c]ПИРИМИДИНЫ КАК ИНГИБИТОРЫ JAK-КИНАЗ |
EP2397482A1 (en) | 2010-06-15 | 2011-12-21 | Almirall, S.A. | Heteroaryl imidazolone derivatives as jak inhibitors |
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JPWO2013146963A1 (ja) * | 2012-03-28 | 2015-12-14 | 武田薬品工業株式会社 | 複素環化合物 |
EA027416B1 (ru) | 2012-03-28 | 2017-07-31 | Мерк Патент Гмбх | Бициклические пиразиноновые производные |
EA031601B1 (ru) | 2013-07-31 | 2019-01-31 | Джилид Сайэнс, Инк. | Ингибиторы syk |
TW201605811A (zh) | 2013-12-11 | 2016-02-16 | 阿爾米雷爾有限公司 | 作為jak抑制劑之吡唑并嘧啶-2基衍生物 |
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PT3290418T (pt) | 2015-04-29 | 2019-07-16 | Wuxi Fortune Pharmaceutical Co Ltd | Inibidores de janus quinase (jak) |
JP6895439B2 (ja) | 2015-12-22 | 2021-06-30 | エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft | IRAK4調節因子としてのピラゾロ[1,5a]ピリミジン誘導体 |
RU2718902C2 (ru) | 2016-02-24 | 2020-04-15 | Пфайзер Инк. | Производные пиразоло[1,5-а]пиразин-4-ила в качестве jak-ингибиторов |
AU2017395023B2 (en) | 2016-12-23 | 2022-04-07 | Plexxikon Inc. | Compounds and methods for CDK8 modulation and indications therefor |
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JP2020524663A (ja) | 2017-06-21 | 2020-08-20 | エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft | Irak4調節因子としてのイソインドリノン誘導体 |
WO2019034973A1 (en) | 2017-08-14 | 2019-02-21 | Pfizer Inc. | PYRAZOLO [1,5-A] PYRAZIN-4-YL AND RELATED DERIVATIVES |
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2017
- 2017-02-10 RU RU2018130547A patent/RU2718902C2/ru active
- 2017-02-10 DK DK17705705.6T patent/DK3419978T3/da active
- 2017-02-10 WO PCT/IB2017/050748 patent/WO2017144995A1/en active Application Filing
- 2017-02-10 EA EA201891463A patent/EA035036B1/ru unknown
- 2017-02-10 SG SG11201806307YA patent/SG11201806307YA/en unknown
- 2017-02-10 CR CR20180372A patent/CR20180372A/es unknown
- 2017-02-10 GE GEAP201714864A patent/GEP20217242B/en unknown
- 2017-02-10 NZ NZ744349A patent/NZ744349A/en unknown
- 2017-02-10 PL PL17705705T patent/PL3419978T3/pl unknown
- 2017-02-10 CU CU2018000078A patent/CU24511B1/es unknown
- 2017-02-10 UA UAA201808148A patent/UA119835C2/uk unknown
- 2017-02-10 CO CONC2018/0008799A patent/CO2018008799A2/es unknown
- 2017-02-10 EP EP20168877.7A patent/EP3712153B1/en active Active
- 2017-02-10 AU AU2017222417A patent/AU2017222417B2/en active Active
- 2017-02-10 JP JP2018544300A patent/JP6505956B2/ja active Active
- 2017-02-10 ES ES17705705T patent/ES2794779T3/es active Active
- 2017-02-10 HU HUE17705705A patent/HUE049305T2/hu unknown
- 2017-02-10 MY MYPI2018702937A patent/MY189118A/en unknown
- 2017-02-10 ME MEP-2020-97A patent/ME03743B/me unknown
- 2017-02-10 SI SI201730289T patent/SI3419978T1/sl unknown
- 2017-02-10 MA MA43668A patent/MA43668B1/fr unknown
- 2017-02-10 MD MDE20190031T patent/MD3419978T2/ro unknown
- 2017-02-10 RS RS20200584A patent/RS60261B1/sr unknown
- 2017-02-10 TN TNP/2018/000295A patent/TN2018000295A1/en unknown
- 2017-02-10 KR KR1020187024431A patent/KR102128671B1/ko active IP Right Grant
- 2017-02-10 EP EP17705705.6A patent/EP3419978B1/en active Active
- 2017-02-10 MA MA052987A patent/MA52987A/fr unknown
- 2017-02-10 LT LTEP17705705.6T patent/LT3419978T/lt unknown
- 2017-02-10 PT PT177057056T patent/PT3419978T/pt unknown
- 2017-02-10 MX MX2018010236A patent/MX2018010236A/es unknown
- 2017-02-10 CN CN201780013165.4A patent/CN109071546B/zh active Active
- 2017-02-21 US US15/437,618 patent/US10144738B2/en active Active
- 2017-02-21 CA CA2958490A patent/CA2958490C/en active Active
- 2017-02-21 TW TW106105777A patent/TWI665201B/zh active
- 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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