JP2011046700A5 - - Google Patents
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- Publication number
- JP2011046700A5 JP2011046700A5 JP2010171260A JP2010171260A JP2011046700A5 JP 2011046700 A5 JP2011046700 A5 JP 2011046700A5 JP 2010171260 A JP2010171260 A JP 2010171260A JP 2010171260 A JP2010171260 A JP 2010171260A JP 2011046700 A5 JP2011046700 A5 JP 2011046700A5
- Authority
- JP
- Japan
- Prior art keywords
- solvate
- pharmaceutically acceptable
- acceptable salt
- group
- compound
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
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- 150000001875 compounds Chemical class 0.000 claims 48
- 150000003839 salts Chemical class 0.000 claims 48
- 239000012453 solvate Substances 0.000 claims 48
- 239000000126 substance Substances 0.000 claims 17
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 11
- 239000003795 chemical substances by application Substances 0.000 claims 9
- 229940122245 Janus kinase inhibitor Drugs 0.000 claims 6
- 125000004093 cyano group Chemical group *C#N 0.000 claims 6
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 6
- 230000001225 therapeutic effect Effects 0.000 claims 6
- 125000001424 substituent group Chemical group 0.000 claims 5
- 125000005843 halogen group Chemical group 0.000 claims 4
- 229910052757 nitrogen Inorganic materials 0.000 claims 4
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 4
- 230000003449 preventive effect Effects 0.000 claims 4
- 230000000069 prophylactic effect Effects 0.000 claims 4
- 238000002054 transplantation Methods 0.000 claims 4
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 3
- 238000004519 manufacturing process Methods 0.000 claims 3
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 2
- 125000004454 (C1-C6) alkoxycarbonyl group Chemical group 0.000 claims 2
- 125000003161 (C1-C6) alkylene group Chemical group 0.000 claims 2
- 208000023275 Autoimmune disease Diseases 0.000 claims 2
- 125000003320 C2-C6 alkenyloxy group Chemical group 0.000 claims 2
- 208000003556 Dry Eye Syndromes Diseases 0.000 claims 2
- 206010013774 Dry eye Diseases 0.000 claims 2
- 102000015617 Janus Kinases Human genes 0.000 claims 2
- 108010024121 Janus Kinases Proteins 0.000 claims 2
- 201000007224 Myeloproliferative neoplasm Diseases 0.000 claims 2
- 201000004681 Psoriasis Diseases 0.000 claims 2
- 125000005196 alkyl carbonyloxy group Chemical group 0.000 claims 2
- 208000026935 allergic disease Diseases 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 125000002911 monocyclic heterocycle group Chemical group 0.000 claims 2
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 2
- 210000000056 organ Anatomy 0.000 claims 2
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 2
- 229940124597 therapeutic agent Drugs 0.000 claims 2
- 125000006376 (C3-C10) cycloalkyl group Chemical group 0.000 claims 1
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 1
- 206010012438 Dermatitis atopic Diseases 0.000 claims 1
- 102000006503 Janus Kinase 2 Human genes 0.000 claims 1
- 108010019437 Janus Kinase 2 Proteins 0.000 claims 1
- 102000006500 Janus Kinase 3 Human genes 0.000 claims 1
- 108010019421 Janus Kinase 3 Proteins 0.000 claims 1
- 229940121730 Janus kinase 2 inhibitor Drugs 0.000 claims 1
- 229940123241 Janus kinase 3 inhibitor Drugs 0.000 claims 1
- 229940124384 agent for atopic dermatitis Drugs 0.000 claims 1
- 125000003118 aryl group Chemical group 0.000 claims 1
- 125000004429 atom Chemical group 0.000 claims 1
- 201000008937 atopic dermatitis Diseases 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 125000004432 carbon atom Chemical group C* 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 229910052731 fluorine Inorganic materials 0.000 claims 1
- 125000001153 fluoro group Chemical group F* 0.000 claims 1
- 125000005842 heteroatom Chemical group 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 125000004430 oxygen atom Chemical group O* 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
- 125000004434 sulfur atom Chemical group 0.000 claims 1
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2010171260A JP5520158B2 (ja) | 2009-07-31 | 2010-07-30 | 含窒素スピロ環化合物及びその医薬用途 |
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2009179502 | 2009-07-31 | ||
| JP2009179502 | 2009-07-31 | ||
| JP2010171260A JP5520158B2 (ja) | 2009-07-31 | 2010-07-30 | 含窒素スピロ環化合物及びその医薬用途 |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014077850A Division JP2014141516A (ja) | 2009-07-31 | 2014-04-04 | 含窒素スピロ環化合物及びその医薬用途 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2011046700A JP2011046700A (ja) | 2011-03-10 |
| JP2011046700A5 true JP2011046700A5 (enExample) | 2014-02-13 |
| JP5520158B2 JP5520158B2 (ja) | 2014-06-11 |
Family
ID=43529436
Family Applications (9)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010171260A Active JP5520158B2 (ja) | 2009-07-31 | 2010-07-30 | 含窒素スピロ環化合物及びその医薬用途 |
| JP2014077850A Pending JP2014141516A (ja) | 2009-07-31 | 2014-04-04 | 含窒素スピロ環化合物及びその医薬用途 |
| JP2015224910A Ceased JP2016029104A (ja) | 2009-07-31 | 2015-11-17 | 含窒素スピロ環化合物及びその医薬用途 |
| JP2016214954A Ceased JP2017019877A (ja) | 2009-07-31 | 2016-11-02 | 含窒素スピロ環化合物及びその医薬用途 |
| JP2018028525A Ceased JP2018111701A (ja) | 2009-07-31 | 2018-02-21 | 含窒素スピロ環化合物及びその医薬用途 |
| JP2019219283A Withdrawn JP2020033384A (ja) | 2009-07-31 | 2019-12-04 | 含窒素スピロ環化合物及びその医薬用途 |
| JP2021144545A Withdrawn JP2021183653A (ja) | 2009-07-31 | 2021-09-06 | 含窒素スピロ環化合物及びその医薬用途 |
| JP2023128376A Withdrawn JP2023138641A (ja) | 2009-07-31 | 2023-08-07 | 含窒素スピロ環化合物及びその医薬用途 |
| JP2025077764A Pending JP2025109780A (ja) | 2009-07-31 | 2025-05-08 | 含窒素スピロ環化合物及びその医薬用途 |
Family Applications After (8)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014077850A Pending JP2014141516A (ja) | 2009-07-31 | 2014-04-04 | 含窒素スピロ環化合物及びその医薬用途 |
| JP2015224910A Ceased JP2016029104A (ja) | 2009-07-31 | 2015-11-17 | 含窒素スピロ環化合物及びその医薬用途 |
| JP2016214954A Ceased JP2017019877A (ja) | 2009-07-31 | 2016-11-02 | 含窒素スピロ環化合物及びその医薬用途 |
| JP2018028525A Ceased JP2018111701A (ja) | 2009-07-31 | 2018-02-21 | 含窒素スピロ環化合物及びその医薬用途 |
| JP2019219283A Withdrawn JP2020033384A (ja) | 2009-07-31 | 2019-12-04 | 含窒素スピロ環化合物及びその医薬用途 |
| JP2021144545A Withdrawn JP2021183653A (ja) | 2009-07-31 | 2021-09-06 | 含窒素スピロ環化合物及びその医薬用途 |
| JP2023128376A Withdrawn JP2023138641A (ja) | 2009-07-31 | 2023-08-07 | 含窒素スピロ環化合物及びその医薬用途 |
| JP2025077764A Pending JP2025109780A (ja) | 2009-07-31 | 2025-05-08 | 含窒素スピロ環化合物及びその医薬用途 |
Country Status (36)
Families Citing this family (37)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI466885B (zh) * | 2009-07-31 | 2015-01-01 | Japan Tobacco Inc | 含氮螺環化合物及其醫藥用途 |
| EP2485589A4 (en) * | 2009-09-04 | 2013-02-06 | Biogen Idec Inc | HETEROARYL-BTK INHIBITORS |
| EP2606051B1 (en) * | 2010-08-20 | 2016-10-05 | Hutchison Medipharma Limited | Pyrrolopyrimidine compounds and uses thereof |
| US9045485B2 (en) | 2010-12-16 | 2015-06-02 | Convergence Pharmaceuticals Limited | ASK 1 inhibiting pyrrolopyrimidine derivatives |
| SMT201800497T1 (it) | 2011-12-21 | 2018-11-09 | Shanghai hengrui pharmaceutical co ltd | Derivato di pirrolo ad anello eteroarilico a sei elementi, relativo metodo di preparazione, e relativi usi medicinali |
| US20140343034A1 (en) * | 2013-04-25 | 2014-11-20 | Japan Tobacco Inc. | Skin barrier function improving agent |
| JP6427497B2 (ja) * | 2013-10-21 | 2018-11-21 | 日本たばこ産業株式会社 | 眼疾患の治療剤又は予防剤 |
| US9879017B2 (en) * | 2014-05-28 | 2018-01-30 | Astrazeneca Ab | Processes for the preparation of AZD5363 and intermediate used therein |
| KR20180025940A (ko) * | 2015-07-07 | 2018-03-09 | 니뽄 다바코 산교 가부시키가이샤 | 7H-피롤로[2,3-d]피리미딘 유도체의 제조 방법 및 그의 중간체 |
| WO2017013270A1 (en) | 2015-07-23 | 2017-01-26 | Universite De Strasbourg | Use of leptin signaling inhibitor for protecting kidneys from patients having ciliopathy |
| HRP20200472T1 (hr) * | 2015-09-24 | 2020-09-18 | Leo Pharma A/S | Liječenje alopecije areate |
| CN111848586B (zh) * | 2015-09-25 | 2024-05-03 | 迪哲(江苏)医药股份有限公司 | 用于抑制jak的化合物和方法 |
| CN117159553A (zh) | 2016-01-21 | 2023-12-05 | 利奥制药有限公司 | 慢性手部湿疹的治疗 |
| WO2018026798A1 (en) | 2016-08-01 | 2018-02-08 | Aptinyx Inc. | Spiro-lactam nmda modulators and methods of using same |
| CN108884100B (zh) * | 2016-11-23 | 2021-04-06 | 江苏恒瑞医药股份有限公司 | 吡咯并六元杂芳环类衍生物的制备方法及中间体 |
| IL288080B2 (en) * | 2016-12-21 | 2024-03-01 | Leo Pharma As | A process for the preparation of H7-pyrrolo[3,2-d]pyrimidine derivatives and their artificial intermediates |
| MX2019007452A (es) | 2016-12-21 | 2019-08-29 | Japan Tobacco Inc | Proceso para preparar derivados de 7h-pirrolo[2,3-d]pirimidina y co-cristales de los mismos. |
| JP2020502224A (ja) | 2016-12-21 | 2020-01-23 | 日本たばこ産業株式会社 | ヤヌスキナーゼ阻害剤の結晶形 |
| US10851116B2 (en) | 2017-01-20 | 2020-12-01 | Leo Pharma A/S | Bicyclic amines as novel JAK kinase inhibitors |
| WO2018141842A1 (en) * | 2017-02-03 | 2018-08-09 | Leo Pharma A/S | 5-(7H-PYRROLO[2,3-d]PYRIMIDIN-4-YL)-5-AZASPIRO[2.5]OCTANE-8-CARBOXYLIC ACID DERIVATIVES AS NOVEL JAK KINASE INHIBITORS |
| JP2020536898A (ja) * | 2017-10-10 | 2020-12-17 | バイオジェン インコーポレイテッド | スピロ誘導体を調製するためのプロセス |
| SG11202007251XA (en) * | 2018-01-31 | 2020-08-28 | Aptinyx Inc | Spiro-lactam nmda receptor modulators and uses thereof |
| WO2020007698A1 (en) * | 2018-07-06 | 2020-01-09 | Leo Pharma A/S | Novel amino-imidazopyrimidine derivatives as janus kinase inhibitors and pharmaceutical use thereof |
| WO2020092015A1 (en) | 2018-11-02 | 2020-05-07 | University Of Rochester | Therapeutic mitigation of epithelial infection |
| MX2021012874A (es) | 2019-05-15 | 2021-11-17 | Leo Pharma As | Tratamiento del lupus eritematoso cutaneo. |
| CN118903144A (zh) * | 2019-08-07 | 2024-11-08 | 乐敦制药株式会社 | 泪液分泌促进用眼科组合物 |
| CN119367282A (zh) * | 2019-12-27 | 2025-01-28 | 乐敦制药株式会社 | 水性组合物 |
| CN111560021B (zh) * | 2020-06-30 | 2023-05-26 | 上海鲲博玖瑞医药科技发展有限公司 | 一种德高替尼中间体及其制备方法 |
| CN111574540B (zh) * | 2020-06-30 | 2023-08-29 | 云南华派医药科技有限公司 | 一种德高替尼的制备方法 |
| CN111606929B (zh) * | 2020-06-30 | 2023-07-07 | 中瀚(齐河县)生物医药科技有限公司 | 德高替尼的制备方法 |
| CN114591321A (zh) * | 2020-12-04 | 2022-06-07 | 广州费米子科技有限责任公司 | 氮杂并环化合物、其制备方法及其用途 |
| TW202241439A (zh) * | 2020-12-29 | 2022-11-01 | 大陸商上海岸闊醫藥科技有限公司 | 治療與抗腫瘤劑相關的皮膚疾病或病症的試劑和方法 |
| US20250275974A1 (en) | 2022-04-20 | 2025-09-04 | Leo Pharma A/S | Treatment of frontal fibrosing alopecia |
| IL322047A (en) | 2023-02-28 | 2025-09-01 | Assia Chem Ind Ltd | Solid forms of dalgocitinib and processes for their preparation |
| AU2024238918A1 (en) | 2023-03-17 | 2025-10-09 | Leo Pharma A/S | A method for the treatment of chronic hand eczema in patients with moderate to severe chronic hand eczema |
| WO2024225445A1 (en) | 2023-04-27 | 2024-10-31 | Japan Tobacco Inc. | Crystalline form of delgocitinib |
| WO2025085050A1 (en) * | 2023-10-16 | 2025-04-24 | Leo Pharma A/S | Treatment of frontal fibrosing alopecia |
Family Cites Families (28)
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| JP4611524B2 (ja) | 1998-06-02 | 2011-01-12 | オーエスアイ・ファーマスーティカルズ・インコーポレーテッド | ピロロ[2,3d]ピリミジン組成物およびその使用 |
| PA8474101A1 (es) * | 1998-06-19 | 2000-09-29 | Pfizer Prod Inc | Compuestos de pirrolo [2,3-d] pirimidina |
| RS50087B (sr) * | 1998-06-19 | 2009-01-22 | Pfizer Products Inc., | Pirolo (2,3-d) pirimidin jedinjenja |
| CZ303875B6 (cs) | 1999-12-10 | 2013-06-05 | Pfizer Products Inc. | Pyrrolo[2,3-d]pyrimidinová sloucenina a farmaceutická kompozice s jejím obsahem |
| WO2004005293A2 (en) * | 2002-07-05 | 2004-01-15 | Targacept, Inc. | N-aryl diazaspiracyclic compounds and methods of preparation and use thereof |
| JPWO2005047286A1 (ja) | 2003-11-13 | 2007-05-31 | 小野薬品工業株式会社 | スピロ複素環化合物 |
| AR054416A1 (es) * | 2004-12-22 | 2007-06-27 | Incyte Corp | Pirrolo [2,3-b]piridin-4-il-aminas y pirrolo [2,3-b]pirimidin-4-il-aminas como inhibidores de las quinasas janus. composiciones farmaceuticas. |
| EP1858902A1 (en) | 2005-02-24 | 2007-11-28 | Pfizer Products Incorporated | Bicyclic heteroaromatic derivatives useful as anticancer agents |
| RU2435769C2 (ru) * | 2005-05-20 | 2011-12-10 | Вертекс Фармасьютикалз Инкорпорейтед | Пирролопиридины, полезные в качестве ингибиторов протеинкиназы |
| KR20080026654A (ko) | 2005-07-14 | 2008-03-25 | 아스텔라스세이야쿠 가부시키가이샤 | 헤테로시클릭 야누스 키나제 3 억제제 |
| KR101391900B1 (ko) | 2005-12-13 | 2014-05-02 | 인사이트 코포레이션 | 야누스 키나아제 억제제로서의 헤테로아릴 치환된 피롤로[2,3-b]피리딘 및 피롤로[2,3-b]피리미딘 |
| GB0526246D0 (en) | 2005-12-22 | 2006-02-01 | Novartis Ag | Organic compounds |
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| JP2010513385A (ja) | 2006-12-22 | 2010-04-30 | エフ.ホフマン−ラ ロシュ アーゲー | スピロ−ピペリジン誘導体 |
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| GB0913342D0 (en) | 2009-07-31 | 2009-09-16 | Astrazeneca Ab | Compounds - 801 |
| TWI466885B (zh) * | 2009-07-31 | 2015-01-01 | Japan Tobacco Inc | 含氮螺環化合物及其醫藥用途 |
| EP2485589A4 (en) | 2009-09-04 | 2013-02-06 | Biogen Idec Inc | HETEROARYL-BTK INHIBITORS |
| JP2018028525A (ja) * | 2016-08-15 | 2018-02-22 | 小野 信行 | イオンレーザーと重水素を利用した核融合炉 |
| JP6229778B2 (ja) * | 2016-09-21 | 2017-11-15 | サミー株式会社 | 遊技機 |
-
2010
- 2010-07-22 TW TW99124110A patent/TWI466885B/zh active
- 2010-07-23 AR ARP100102681A patent/AR077497A1/es active IP Right Grant
- 2010-07-30 RS RS20170305A patent/RS55913B1/sr unknown
- 2010-07-30 PL PL10804531T patent/PL2460806T3/pl unknown
- 2010-07-30 EP EP10804531.1A patent/EP2460806B1/en active Active
- 2010-07-30 HU HUE10804531A patent/HUE033070T2/hu unknown
- 2010-07-30 SI SI201031426A patent/SI2460806T1/sl unknown
- 2010-07-30 HR HRP20170447TT patent/HRP20170447T1/hr unknown
- 2010-07-30 CN CN201080034068.1A patent/CN102510865B/zh active Active
- 2010-07-30 LT LTEP10804531.1T patent/LT2460806T/lt unknown
- 2010-07-30 CA CA2767899A patent/CA2767899C/en active Active
- 2010-07-30 ME MEP-2017-74A patent/ME02667B/me unknown
- 2010-07-30 US US12/847,025 patent/US8609647B2/en active Active
- 2010-07-30 RU RU2012106344A patent/RU2630694C2/ru active
- 2010-07-30 AU AU2010278066A patent/AU2010278066B2/en active Active
- 2010-07-30 BR BR112012002157-5A patent/BR112012002157B1/pt active IP Right Grant
- 2010-07-30 SM SM20170166T patent/SMT201700166T1/it unknown
- 2010-07-30 PE PE2012000097A patent/PE20121276A1/es active IP Right Grant
- 2010-07-30 JP JP2010171260A patent/JP5520158B2/ja active Active
- 2010-07-30 WO PCT/JP2010/062873 patent/WO2011013785A1/ja not_active Ceased
- 2010-07-30 PT PT108045311T patent/PT2460806T/pt unknown
- 2010-07-30 MX MX2012001313A patent/MX2012001313A/es active IP Right Grant
- 2010-07-30 ES ES10804531.1T patent/ES2616705T3/es active Active
- 2010-07-30 SG SG2011094117A patent/SG176918A1/en unknown
- 2010-07-30 MY MYPI2012000155A patent/MY163495A/en unknown
- 2010-07-30 EP EP17150170.3A patent/EP3181570A1/en not_active Withdrawn
- 2010-07-30 EP EP21159390.0A patent/EP3858349A1/en active Pending
- 2010-07-30 NZ NZ597994A patent/NZ597994A/xx unknown
- 2010-07-30 DK DK10804531.1T patent/DK2460806T3/en active
- 2010-07-30 KR KR1020127001455A patent/KR101773208B1/ko active Active
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2011
- 2011-12-18 IL IL217048A patent/IL217048A/en active IP Right Grant
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2012
- 2012-01-18 CO CO12006869A patent/CO6491052A2/es active IP Right Grant
- 2012-01-27 ZA ZA2012/00689A patent/ZA201200689B/en unknown
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2013
- 2013-11-12 US US14/077,446 patent/US20140187534A1/en not_active Abandoned
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2014
- 2014-04-04 JP JP2014077850A patent/JP2014141516A/ja active Pending
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2015
- 2015-11-17 JP JP2015224910A patent/JP2016029104A/ja not_active Ceased
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2016
- 2016-11-02 JP JP2016214954A patent/JP2017019877A/ja not_active Ceased
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2017
- 2017-03-20 CY CY20171100348T patent/CY1118747T1/el unknown
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2018
- 2018-02-21 JP JP2018028525A patent/JP2018111701A/ja not_active Ceased
-
2019
- 2019-12-04 JP JP2019219283A patent/JP2020033384A/ja not_active Withdrawn
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2021
- 2021-09-06 JP JP2021144545A patent/JP2021183653A/ja not_active Withdrawn
- 2021-12-21 US US17/557,174 patent/US20230023377A1/en not_active Abandoned
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2023
- 2023-05-05 US US18/143,720 patent/US20240150367A1/en not_active Abandoned
- 2023-08-07 JP JP2023128376A patent/JP2023138641A/ja not_active Withdrawn
-
2025
- 2025-02-28 FI FIC20250012C patent/FIC20250012I1/fi unknown
- 2025-02-28 FR FR25C1010C patent/FR25C1010I1/fr active Active
- 2025-03-03 LT LTPA2025511C patent/LTPA2025511I1/lt unknown
- 2025-03-03 HU HUS2500013C patent/HUS2500013I1/hu unknown
- 2025-03-04 NL NL301321C patent/NL301321I2/nl unknown
- 2025-03-04 NO NO2025014C patent/NO2025014I1/no unknown
- 2025-05-08 JP JP2025077764A patent/JP2025109780A/ja active Pending
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