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)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Neurology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Physical Education & Sports Medicine (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (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)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (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) | EA035068B1 (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) | MA51988A (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) | PL3663296T3 (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 (35)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
UA116981C2 (uk) | 2012-02-10 | 2018-06-11 | ПіТіСі ТЕРАП'ЮТІКС, ІНК. | Сполуки для лікування спінальної м'язової атрофії |
WO2015024876A2 (en) | 2013-08-19 | 2015-02-26 | F. Hoffmann-La Roche Ag | Screening method |
US10882868B2 (en) * | 2014-05-15 | 2021-01-05 | Hoffmann-La Roche Inc. | Compounds for treating spinal muscular atrophy |
EP3298017B1 (en) | 2015-05-20 | 2019-08-14 | H. Hoffnabb-La Roche Ag | Compounds for treating spinal muscular atrophy |
US10668171B2 (en) | 2015-05-30 | 2020-06-02 | Ptc Therapeutics, Inc. | Methods for modulating RNA splicing |
JP6659841B2 (ja) * | 2015-11-12 | 2020-03-04 | エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft | 脊髄性筋萎縮症を処置するための組成物 |
AU2016351919B2 (en) * | 2015-11-12 | 2020-11-12 | F. Hoffmann-La Roche Ag | Compounds for treating amyotrophic lateral sclerosis |
CN108137579B (zh) | 2015-12-10 | 2022-01-07 | 豪夫迈·罗氏有限公司 | 桥连哌啶衍生物 |
MX2021001091A (es) | 2015-12-10 | 2022-04-26 | Ptc Therapeutics Inc | Compuestos para usarse en el tratamiento o mejoramiento de la enfermedad de huntington. |
US11702646B2 (en) | 2016-11-28 | 2023-07-18 | Ptc Therapeutics, Inc. | Methods for modulating RNA splicing |
MX2019014514A (es) | 2017-06-05 | 2020-07-20 | Ptc Therapeutics Inc | Compuestos para tratar la enfermedad de huntington. |
EP3638318A4 (en) | 2017-06-14 | 2021-03-17 | PTC Therapeutics, Inc. | METHOD OF MODULATION OF RNA SPLICING |
EP3644996B1 (en) | 2017-06-28 | 2023-07-26 | PTC Therapeutics, Inc. | Methods for treating huntington's disease |
CA3067592A1 (en) | 2017-06-28 | 2019-01-03 | Ptc Therapeutics, Inc. | Methods for treating huntington's disease |
CA3075968C (en) | 2017-09-22 | 2023-04-04 | F. Hoffmann-La Roche Ag | Process for the preparation of 7-(4,7-diazaspiro[2,5]octan-7-yl)-2-(2,8-dimethylimidazo[1,2-b]pyridazin-6-yl)pyrido[1,2-a]pyrimidin-4-one derivatives |
JP7423515B2 (ja) * | 2017-10-03 | 2024-01-29 | エフ. ホフマン-ラ ロシュ アーゲー | Smaの新たな処置 |
AU2019243048A1 (en) | 2018-03-27 | 2020-10-15 | Ptc Therapeutics, Inc. | Compounds for treating Huntington's disease |
BR112020026637A2 (pt) | 2018-06-27 | 2021-03-30 | Reborna Biosciences, Inc. | Agente profilático ou terapêutico para atrofia muscular espinhal |
EP4434990A1 (en) | 2018-06-27 | 2024-09-25 | PTC Therapeutics, Inc. | Heterocyclic and heteroaryl compounds for treating huntington's disease |
US11685746B2 (en) | 2018-06-27 | 2023-06-27 | Ptc Therapeutics, Inc. | Heteroaryl compounds for treating Huntington's disease |
JP2022505098A (ja) | 2018-10-19 | 2022-01-14 | エフ.ホフマン-ラ ロシュ アーゲー | ピリド[1,2-a]ピリミジン-4-オン誘導体の新規な形態、その製剤およびその製造プロセス |
CN113966219A (zh) | 2019-06-12 | 2022-01-21 | 豪夫迈·罗氏有限公司 | Sma的新治疗方法 |
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 |
EP4308577A1 (en) * | 2021-03-17 | 2024-01-24 | F. Hoffmann-La Roche AG | New thiadiazolopyrimidone derivatives |
CR20230437A (es) | 2021-03-17 | 2023-10-16 | Hoffmann La Roche | Nuevos derivados de tiazolopirimidinona |
AU2022237836B2 (en) | 2021-03-18 | 2024-07-04 | F. Hoffmann-La Roche Ag | Process for preparing risdiplam |
CN118055767A (zh) | 2021-10-06 | 2024-05-17 | 豪夫迈·罗氏有限公司 | 新颖的组合施用 |
WO2023202501A1 (zh) * | 2022-04-18 | 2023-10-26 | 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 |
US20240173325A1 (en) | 2022-10-14 | 2024-05-30 | 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 |
WO2024218207A1 (en) | 2023-04-20 | 2024-10-24 | F. Hoffmann-La Roche Ag | Thieno[3,2-b]pyridine derivatives |
Family Cites Families (10)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN1093130C (zh) * | 1996-08-06 | 2002-10-23 | 辉瑞大药厂 | 被取代的吡啶并6,6-二环衍生物 |
EP2215074B1 (en) | 2007-09-27 | 2014-02-19 | The United States of America, as Represented by the Secretary, Department of Health and Human Services | 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 |
US8932818B2 (en) | 2008-08-13 | 2015-01-13 | Ptc Therapeutics, Inc. | Screening assays for compounds that modulate programmed ribosomal frameshifting |
JP2011529722A (ja) * | 2008-08-14 | 2011-12-15 | カーディアック ペースメイカーズ, インコーポレイテッド | 音響通信リンクの性能評価および適合 |
CN104244944B (zh) * | 2011-12-30 | 2018-06-08 | Ptc医疗公司 | 用于治疗脊髓性肌萎缩症的化合物 |
UA116981C2 (uk) * | 2012-02-10 | 2018-06-11 | ПіТіСі ТЕРАП'ЮТІКС, ІНК. | Сполуки для лікування спінальної м'язової атрофії |
WO2014012050A2 (en) | 2012-07-13 | 2014-01-16 | Indiana University Research & Technology Corporation | Compounds for treatment of spinal muscular atrophy |
JP6659841B2 (ja) | 2015-11-12 | 2020-03-04 | エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft | 脊髄性筋萎縮症を処置するための組成物 |
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2015
- 2015-05-11 EA EA201692280A patent/EA035068B1/ru active Protection Beyond IP Right Term
- 2015-05-11 SI SI201531021T patent/SI3143025T1/sl unknown
- 2015-05-11 NZ NZ72500815A patent/NZ725008A/en unknown
- 2015-05-11 CN CN201580027306.9A patent/CN106459092B/zh active Active
- 2015-05-11 CR CR20160518A patent/CR20160518A/es unknown
- 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 KR KR1020167034983A patent/KR102213740B1/ko active IP Right Grant
- 2015-05-11 DK DK15721701T patent/DK3143025T3/da active
- 2015-05-11 EP EP19200058.6A patent/EP3663296B1/en active Active
- 2015-05-11 EP EP23169721.0A patent/EP4241772A3/en not_active Withdrawn
- 2015-05-11 MA MA051988A patent/MA51988A/fr unknown
- 2015-05-11 WO PCT/EP2015/060343 patent/WO2015173181A1/en active Application Filing
- 2015-05-11 EP EP15721701.9A patent/EP3143025B1/en active Active
- 2015-05-11 MY MYPI2016001903A patent/MY174284A/en unknown
- 2015-05-11 UA UAA201612716A patent/UA119670C2/uk unknown
- 2015-05-11 SI SI201531952T patent/SI3663296T1/sl unknown
- 2015-05-11 EA EA202090486A patent/EA202090486A3/ru unknown
- 2015-05-11 JP JP2016567816A patent/JP6236173B2/ja active Active
- 2015-05-11 ES ES15721701T patent/ES2761423T3/es active Active
- 2015-05-11 PE PE2016002128A patent/PE20170128A1/es unknown
- 2015-05-11 PL PL15721701T patent/PL3143025T3/pl unknown
- 2015-05-11 RS RS20191541A patent/RS59718B1/sr unknown
- 2015-05-11 CA CA2948561A patent/CA2948561C/en active Active
- 2015-05-11 BR BR112016026205-0A patent/BR112016026205B1/pt active IP Right Grant
- 2015-05-11 AU AU2015261046A patent/AU2015261046C1/en active Active
- 2015-05-11 KR KR1020217002966A patent/KR102256013B1/ko active IP Right Grant
- 2015-05-11 MA MA39995A patent/MA39995B1/fr unknown
- 2015-05-11 SG SG11201609497TA patent/SG11201609497TA/en unknown
- 2015-05-11 PT PT157217019T patent/PT3143025T/pt unknown
- 2015-05-11 ES ES19200058T patent/ES2949660T3/es active Active
- 2015-05-11 HU HUE15721701A patent/HUE046491T2/hu unknown
- 2015-05-11 HR HRP20230637TT patent/HRP20230637T1/hr unknown
- 2015-05-14 AR ARP150101500A patent/AR100442A1/es not_active Application Discontinuation
- 2015-05-14 TW TW104115433A patent/TWI667239B/zh active
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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 LT LTPA2021010C patent/LTPA2021010I1/lt unknown
- 2021-09-14 HU HUS2100037C patent/HUS2100037I1/hu unknown
- 2021-09-15 NL NL301128C patent/NL301128I2/nl unknown
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