AR100442A1 - Derivados de pirido[1,2-a]pirimidin-4-ona para tratar atrofia muscular espinal - Google Patents
Derivados de pirido[1,2-a]pirimidin-4-ona para tratar atrofia muscular espinalInfo
- Publication number
- AR100442A1 AR100442A1 ARP150101500A ARP150101500A AR100442A1 AR 100442 A1 AR100442 A1 AR 100442A1 AR P150101500 A ARP150101500 A AR P150101500A AR P150101500 A ARP150101500 A AR P150101500A AR 100442 A1 AR100442 A1 AR 100442A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- heterocycloalkyl
- cycloalkyl
- hydrogen
- amino
- Prior art date
Links
- 208000002320 spinal muscular atrophy Diseases 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 4
- 239000001257 hydrogen Substances 0.000 abstract 4
- 229910052739 hydrogen Inorganic materials 0.000 abstract 4
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 4
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract 3
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 abstract 3
- 125000001424 substituent group Chemical group 0.000 abstract 3
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 abstract 2
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 2
- 125000004103 aminoalkyl group Chemical group 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 2
- 125000002947 alkylene group Chemical group 0.000 abstract 1
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 125000001188 haloalkyl group Chemical group 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
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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
- 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
- A61K31/50—Pyridazines; Hydrogenated pyridazines
- A61K31/5025—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring 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
- A61K31/495—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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- 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
- A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
-
- 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
-
- 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
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Neurology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Physical Education & Sports Medicine (AREA)
- Epidemiology (AREA)
- Pain & Pain Management (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Steroid Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
Además, se refiere a la fabricación de compuestos de fórmula (1), a composiciones farmacéuticas que los comprenden y a su uso como medicamentos para tratar o prevenir la AME. Reivindicación 1: El compuesto de fórmula (1) en la que R¹ es hidrógeno o alquilo C₁₋₇; R² es hidrógeno, ciano, alquilo C₁₋₇, haloalquilo C₁₋₇ o cicloalquilo C₃₋₈; R³ es hidrógeno, alquilo C₁₋₇, o cicloalquilo C₃₋₈; A es N-heterocicloalquilo o NR¹²R¹³, en el que N-heterocicloalquilo comprende 1 ó 2 átomos de anillo de nitrógeno y está opcionalmente sustituido con 1, 2, 3 ó 4 sustituyentes seleccionados de R¹⁴; R¹² es heterocicloalquilo que comprende 1 átomo de anillo de nitrógeno, en el que heterocicloalquilo está opcionalmente sustituido con 1, 2, 3 ó 4 sustituyentes seleccionados de R¹⁴; R¹³ es hidrógeno, alquilo C₁₋₇₀ cicloalquilo C₃₋₈; R¹⁴ se selecciona independientemente de nitrógeno, alquilo C₁₋₇, amino, amino-alquilo C₁₋₇, cicloalquilo y heterocicloalquilo C₃₋₈ o dos R¹⁴ juntos forman alquileno C₁₋₇; con la salvedad de que si A es N-heterocicloalquilo que comprende solo 1 átomo de anillo de nitrógeno, entonces al menos un sustituyente R¹⁴ es amino o amino-alquilo C₁₋₇; y sales farmacéuticamente aceptables de los mismos.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201461993839P | 2014-05-15 | 2014-05-15 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR100442A1 true AR100442A1 (es) | 2016-10-05 |
Family
ID=53175048
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP150101500A AR100442A1 (es) | 2014-05-15 | 2015-05-14 | Derivados de pirido[1,2-a]pirimidin-4-ona para tratar atrofia muscular espinal |
Country Status (36)
Country | Link |
---|---|
US (1) | US9969754B2 (es) |
EP (3) | EP3663296B1 (es) |
JP (1) | JP6236173B2 (es) |
KR (2) | KR102213740B1 (es) |
CN (1) | CN106459092B (es) |
AR (1) | AR100442A1 (es) |
AU (1) | AU2015261046C1 (es) |
BR (1) | BR112016026205B1 (es) |
CA (1) | CA2948561C (es) |
CL (1) | CL2016002836A1 (es) |
CR (1) | CR20160518A (es) |
DK (1) | DK3143025T3 (es) |
EA (2) | EA202090486A3 (es) |
ES (2) | ES2761423T3 (es) |
FR (1) | FR21C1039I2 (es) |
HR (2) | HRP20230637T1 (es) |
HU (2) | HUE046491T2 (es) |
IL (2) | IL248653B (es) |
LT (1) | LTPA2021010I1 (es) |
MA (2) | MA39995B1 (es) |
MX (1) | MX371050B (es) |
MY (1) | MY174284A (es) |
NL (1) | NL301128I2 (es) |
NO (1) | NO2021035I1 (es) |
NZ (1) | NZ725008A (es) |
PE (1) | PE20170128A1 (es) |
PH (1) | PH12016502081A1 (es) |
PL (2) | PL3143025T3 (es) |
PT (1) | PT3143025T (es) |
RS (1) | RS59718B1 (es) |
SG (1) | SG11201609497TA (es) |
SI (2) | SI3143025T1 (es) |
TW (1) | TWI667239B (es) |
UA (1) | UA119670C2 (es) |
WO (1) | WO2015173181A1 (es) |
ZA (1) | ZA201607026B (es) |
Families Citing this family (34)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
ES2697174T3 (es) | 2012-02-10 | 2019-01-22 | Ptc Therapeutics Inc | Compuestos para tratar atrofia muscular espinal |
EP3035935B1 (en) | 2013-08-19 | 2020-03-11 | F. Hoffmann-La Roche AG | Compounds for use in the prophylaxis and treatment of cancer |
US10882868B2 (en) * | 2014-05-15 | 2021-01-05 | Hoffmann-La Roche Inc. | Compounds for treating spinal muscular atrophy |
WO2016184832A1 (en) | 2015-05-20 | 2016-11-24 | F. Hoffmann-La Roche Ag | Compounds for treating spinal muscular atrophy |
WO2016196386A1 (en) | 2015-05-30 | 2016-12-08 | Ptc Therapeutics, Inc. | Methods for modulating rna splicing |
AU2016353961B2 (en) * | 2015-11-12 | 2019-08-29 | F. Hoffmann-La Roche Ag | Compositions for treating spinal muscular atrophy |
JP2018533594A (ja) * | 2015-11-12 | 2018-11-15 | エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft | 筋萎縮性側索硬化症を処置するための化合物 |
DK3386511T3 (da) | 2015-12-10 | 2021-07-05 | Ptc Therapeutics Inc | Fremgangsmåder til behandling af huntingtons sygdom |
JP6872550B2 (ja) | 2015-12-10 | 2021-05-19 | エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft | 架橋されたピペリジン誘導体 |
JP2019535789A (ja) * | 2016-11-28 | 2019-12-12 | 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 | Rnaスプライシングを調節する方法 |
EP3634953B1 (en) | 2017-06-05 | 2024-01-03 | PTC Therapeutics, Inc. | Compounds for treating huntington's disease |
EA202090034A1 (ru) | 2017-06-14 | 2020-04-16 | ПиТиСи ТЕРАПЬЮТИКС, ИНК. | Способы модификации сплайсинга рнк |
WO2019005980A1 (en) | 2017-06-28 | 2019-01-03 | Ptc Therapeutics, Inc. | METHODS OF TREATING HUNTINGTON'S DISEASE |
EP3645121A4 (en) | 2017-06-28 | 2021-03-17 | PTC Therapeutics, Inc. | HUNTINGTON'S DISEASE TREATMENT METHODS |
CN116813648A (zh) * | 2017-09-22 | 2023-09-29 | 豪夫迈·罗氏有限公司 | 制备2-(2,8-二甲基咪唑并[1,2-b]哒嗪-6-基)吡啶并[1,2-a]嘧啶-4-酮衍生物的方法 |
CA3078137A1 (en) * | 2017-10-03 | 2019-04-11 | F. Hoffmann-La Roche Ag | New treatment of sma |
BR112020019373A2 (pt) | 2018-03-27 | 2020-12-29 | Ptc Therapeutics, Inc. | Compostos para o tratamento da doença de hutington |
US11685746B2 (en) | 2018-06-27 | 2023-06-27 | Ptc Therapeutics, Inc. | Heteroaryl compounds for treating Huntington's disease |
AU2019294478B2 (en) | 2018-06-27 | 2023-03-23 | Ptc Therapeutics, Inc. | Heterocyclic and heteroaryl compounds for treating Huntington's disease |
MX2020014116A (es) | 2018-06-27 | 2021-06-15 | Reborna Biosciences Inc | Agente profilactico o terapeutico para atrofia muscular espinal. |
TW202035411A (zh) | 2018-10-19 | 2020-10-01 | 瑞士商赫孚孟拉羅股份公司 | 吡啶并[1,2-a]嘧啶-4-酮衍生物之新型式、及調配物及製備方法 |
JP2022536669A (ja) | 2019-06-12 | 2022-08-18 | エフ.ホフマン-ラ ロシュ アーゲー | Smaの新規治療 |
EP4004003A1 (en) | 2019-07-31 | 2022-06-01 | Teva Pharmaceuticals International GmbH | Solid state forms of risdiplam and process for preparation thereof |
WO2022048675A1 (zh) * | 2020-09-07 | 2022-03-10 | 苏州科睿思制药有限公司 | Risdiplam晶型及其制备方法和用途 |
WO2022162107A1 (en) | 2021-02-01 | 2022-08-04 | Sandoz Ag | Crystalline form of risdiplam |
JP2024510487A (ja) * | 2021-03-17 | 2024-03-07 | エフ. ホフマン-ラ ロシュ アーゲー | 新規なチアジアゾロピリミドン誘導体 |
AU2022240935A1 (en) | 2021-03-17 | 2023-08-24 | F. Hoffmann-La Roche Ag | New thiazolopyrimidinone derivatives |
JP2024509995A (ja) | 2021-03-18 | 2024-03-05 | エフ. ホフマン-ラ ロシュ アーゲー | リスジプラムを調製するための方法 |
EP4426306A1 (en) | 2021-10-06 | 2024-09-11 | F. Hoffmann-La Roche AG | Novel combined administration |
CN118005654A (zh) * | 2022-04-18 | 2024-05-10 | 深圳市塔吉瑞生物医药有限公司 | 取代的吡啶并嘧啶酮类化合物及包含该化合物的组合物及其用途 |
WO2023240236A1 (en) | 2022-06-10 | 2023-12-14 | Voyager Therapeutics, Inc. | Compositions and methods for the treatment of spinal muscular atrophy related disorders |
WO2024069646A1 (en) * | 2022-09-26 | 2024-04-04 | Natco Pharma Limited | Improved process for the preparation of risdiplam and its intermediates |
WO2024081932A1 (en) | 2022-10-14 | 2024-04-18 | Genentech, Inc. | Methods for treating spinal muscular atrophy |
WO2024154148A1 (en) * | 2023-01-21 | 2024-07-25 | Harman Finochem Limited | Process for preparation of risdiplam, novel intermediates, and process for preparation thereof |
Family Cites Families (10)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
DK0920429T3 (da) * | 1996-08-06 | 2003-05-12 | Pfizer | Substituerede pyrido- eller pyrimidoholdige, 6,6- eller 6,7-bicykliske derivater |
AU2008304231A1 (en) | 2007-09-27 | 2009-04-02 | Albany Molecular Research, Inc. | Isoindoline compounds for the treatment of spinal muscular atrophy and other uses |
US8633019B2 (en) * | 2008-05-27 | 2014-01-21 | Ptc Therapeutics, Inc. | Methods for treating spinal muscular atrophy |
KR20100012134A (ko) * | 2008-07-28 | 2010-02-08 | 신호열 | 마우스 |
WO2010019236A1 (en) | 2008-08-13 | 2010-02-18 | Ptc Therapeutics, Inc | Methods for treating spinal muscular atrophy |
WO2010019326A1 (en) * | 2008-08-14 | 2010-02-18 | Cardiac Pacemakers, Inc. | Performance assessment and adaptation of an acoustic communication link |
JP6193881B2 (ja) * | 2011-12-30 | 2017-09-06 | ピーティーシー セラピューティクス, インコーポレイテッド | 脊髄性筋萎縮症を治療するための化合物 |
ES2697174T3 (es) | 2012-02-10 | 2019-01-22 | Ptc Therapeutics Inc | Compuestos para tratar atrofia muscular espinal |
US9212209B2 (en) | 2012-07-13 | 2015-12-15 | Indiana University Research And Technology Corporation | Screening methods for spinal muscular atrophy |
AU2016353961B2 (en) | 2015-11-12 | 2019-08-29 | F. Hoffmann-La Roche Ag | Compositions for treating spinal muscular atrophy |
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2015
- 2015-05-11 PT PT157217019T patent/PT3143025T/pt unknown
- 2015-05-11 MA MA39995A patent/MA39995B1/fr unknown
- 2015-05-11 HR HRP20230637TT patent/HRP20230637T1/hr unknown
- 2015-05-11 EA EA202090486A patent/EA202090486A3/ru unknown
- 2015-05-11 RS RS20191541A patent/RS59718B1/sr unknown
- 2015-05-11 SG SG11201609497TA patent/SG11201609497TA/en unknown
- 2015-05-11 KR KR1020167034983A patent/KR102213740B1/ko active IP Right Grant
- 2015-05-11 CN CN201580027306.9A patent/CN106459092B/zh active Active
- 2015-05-11 WO PCT/EP2015/060343 patent/WO2015173181A1/en active Application Filing
- 2015-05-11 AU AU2015261046A patent/AU2015261046C1/en active Active
- 2015-05-11 PL PL15721701T patent/PL3143025T3/pl unknown
- 2015-05-11 KR KR1020217002966A patent/KR102256013B1/ko active IP Right Grant
- 2015-05-11 MA MA051988A patent/MA51988A/fr unknown
- 2015-05-11 PE PE2016002128A patent/PE20170128A1/es unknown
- 2015-05-11 UA UAA201612716A patent/UA119670C2/uk unknown
- 2015-05-11 CR CR20160518A patent/CR20160518A/es unknown
- 2015-05-11 EP EP19200058.6A patent/EP3663296B1/en active Active
- 2015-05-11 JP JP2016567816A patent/JP6236173B2/ja active Active
- 2015-05-11 SI SI201531021T patent/SI3143025T1/sl unknown
- 2015-05-11 EP EP23169721.0A patent/EP4241772A3/en active Pending
- 2015-05-11 HU HUE15721701A patent/HUE046491T2/hu unknown
- 2015-05-11 ES ES15721701T patent/ES2761423T3/es active Active
- 2015-05-11 DK DK15721701T patent/DK3143025T3/da active
- 2015-05-11 EP EP15721701.9A patent/EP3143025B1/en active Active
- 2015-05-11 ES ES19200058T patent/ES2949660T3/es active Active
- 2015-05-11 EA EA201692280A patent/EA035068B1/ru active Protection Beyond IP Right Term
- 2015-05-11 CA CA2948561A patent/CA2948561C/en active Active
- 2015-05-11 PL PL19200058.6T patent/PL3663296T3/pl unknown
- 2015-05-11 MX MX2016014547A patent/MX371050B/es active IP Right Grant
- 2015-05-11 SI SI201531952T patent/SI3663296T1/sl unknown
- 2015-05-11 BR BR112016026205-0A patent/BR112016026205B1/pt active IP Right Grant
- 2015-05-11 MY MYPI2016001903A patent/MY174284A/en unknown
- 2015-05-11 NZ NZ72500815A patent/NZ725008A/en unknown
- 2015-05-14 TW TW104115433A patent/TWI667239B/zh active
- 2015-05-14 AR ARP150101500A patent/AR100442A1/es not_active Application Discontinuation
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2016
- 2016-10-12 ZA ZA2016/07026A patent/ZA201607026B/en unknown
- 2016-10-19 PH PH12016502081A patent/PH12016502081A1/en unknown
- 2016-10-31 IL IL24865316A patent/IL248653B/en active IP Right Grant
- 2016-11-08 CL CL2016002836A patent/CL2016002836A1/es unknown
- 2016-11-14 US US15/351,267 patent/US9969754B2/en active Active
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2019
- 2019-10-17 IL IL270027A patent/IL270027B/en active IP Right Grant
- 2019-11-29 HR HRP20192159TT patent/HRP20192159T1/hr unknown
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2021
- 2021-09-09 FR FR21C1039C patent/FR21C1039I2/fr active Active
- 2021-09-10 NO NO2021035C patent/NO2021035I1/no unknown
- 2021-09-14 HU HUS2100037C patent/HUS2100037I1/hu unknown
- 2021-09-14 LT LTPA2021010C patent/LTPA2021010I1/lt unknown
- 2021-09-15 NL NL301128C patent/NL301128I2/nl unknown
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