JP2016531121A5 - - Google Patents
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- JP2016531121A5 JP2016531121A5 JP2016533392A JP2016533392A JP2016531121A5 JP 2016531121 A5 JP2016531121 A5 JP 2016531121A5 JP 2016533392 A JP2016533392 A JP 2016533392A JP 2016533392 A JP2016533392 A JP 2016533392A JP 2016531121 A5 JP2016531121 A5 JP 2016531121A5
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- JP
- Japan
- Prior art keywords
- compound according
- groups
- alkyl
- optionally
- nitrogen
- 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.)
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- 150000001875 compounds Chemical class 0.000 claims 24
- 125000000217 alkyl group Chemical group 0.000 claims 13
- 125000003118 aryl group Chemical group 0.000 claims 9
- 125000001072 heteroaryl group Chemical group 0.000 claims 8
- 229910052739 hydrogen Inorganic materials 0.000 claims 6
- 239000001257 hydrogen Substances 0.000 claims 6
- 229910005965 SO 2 Inorganic materials 0.000 claims 5
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 5
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 4
- 125000003710 aryl alkyl group Chemical group 0.000 claims 4
- 125000000753 cycloalkyl group Chemical group 0.000 claims 4
- ZUOUZKKEUPVFJK-UHFFFAOYSA-N diphenyl Chemical compound C1=CC=CC=C1C1=CC=CC=C1 ZUOUZKKEUPVFJK-UHFFFAOYSA-N 0.000 claims 4
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims 4
- 229910052760 oxygen Inorganic materials 0.000 claims 4
- 125000003545 alkoxy group Chemical group 0.000 claims 3
- 229910052736 halogen Inorganic materials 0.000 claims 3
- 150000002367 halogens Chemical class 0.000 claims 3
- RAXXELZNTBOGNW-UHFFFAOYSA-N imidazole Natural products C1=CNC=N1 RAXXELZNTBOGNW-UHFFFAOYSA-N 0.000 claims 3
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- KAESVJOAVNADME-UHFFFAOYSA-N Pyrrole Chemical compound C=1C=CNC=1 KAESVJOAVNADME-UHFFFAOYSA-N 0.000 claims 2
- 125000003342 alkenyl group Chemical group 0.000 claims 2
- 125000003282 alkyl amino group Chemical group 0.000 claims 2
- 125000000304 alkynyl group Chemical group 0.000 claims 2
- 235000010290 biphenyl Nutrition 0.000 claims 2
- 239000004305 biphenyl Substances 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 2
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims 2
- 150000002431 hydrogen Chemical group 0.000 claims 2
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- 239000000651 prodrug Substances 0.000 claims 2
- 229940002612 prodrug Drugs 0.000 claims 2
- 229910052717 sulfur Inorganic materials 0.000 claims 2
- 101100516568 Caenorhabditis elegans nhr-7 gene Proteins 0.000 claims 1
- WTKZEGDFNFYCGP-UHFFFAOYSA-N Pyrazole Chemical compound C=1C=NNC=1 WTKZEGDFNFYCGP-UHFFFAOYSA-N 0.000 claims 1
- 125000004183 alkoxy alkyl group Chemical group 0.000 claims 1
- 125000004688 alkyl sulfonyl alkyl group Chemical group 0.000 claims 1
- 125000004103 aminoalkyl group Chemical group 0.000 claims 1
- 125000001769 aryl amino group Chemical group 0.000 claims 1
- 125000004429 atom Chemical group 0.000 claims 1
- 125000004093 cyano group Chemical group *C#N 0.000 claims 1
- 125000006310 cycloalkyl amino group Chemical group 0.000 claims 1
- 125000004663 dialkyl amino group Chemical group 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000004438 haloalkoxy group Chemical group 0.000 claims 1
- 125000001188 haloalkyl group Chemical group 0.000 claims 1
- 125000005241 heteroarylamino group Chemical group 0.000 claims 1
- 125000000623 heterocyclic group Chemical group 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361862759P | 2013-08-06 | 2013-08-06 | |
| US61/862,759 | 2013-08-06 | ||
| US201461954276P | 2014-03-17 | 2014-03-17 | |
| US61/954,276 | 2014-03-17 | ||
| PCT/US2014/049906 WO2015021128A1 (en) | 2013-08-06 | 2014-08-06 | Kdm1a inhibitors for the treatment of disease |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2016531121A JP2016531121A (ja) | 2016-10-06 |
| JP2016531121A5 true JP2016531121A5 (enExample) | 2017-09-14 |
| JP6521967B2 JP6521967B2 (ja) | 2019-05-29 |
Family
ID=52461899
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016533392A Active JP6521967B2 (ja) | 2013-08-06 | 2014-08-06 | 疾患の治療のためのｋｄｍ１ａ阻害剤 |
Country Status (14)
| Country | Link |
|---|---|
| US (4) | US9790195B2 (enExample) |
| EP (1) | EP3030323B1 (enExample) |
| JP (1) | JP6521967B2 (enExample) |
| KR (1) | KR102255778B1 (enExample) |
| CN (1) | CN105592888A (enExample) |
| AU (1) | AU2014306149B2 (enExample) |
| BR (1) | BR112016002496B1 (enExample) |
| CA (1) | CA2920257C (enExample) |
| DK (1) | DK3030323T3 (enExample) |
| ES (1) | ES2734209T3 (enExample) |
| IL (1) | IL243976B (enExample) |
| MX (1) | MX383590B (enExample) |
| WO (1) | WO2015021128A1 (enExample) |
| ZA (1) | ZA201600901B (enExample) |
Families Citing this family (35)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP6238908B2 (ja) * | 2012-11-28 | 2017-11-29 | 京都府公立大学法人 | リシン構造を有するｌｓｄ１選択的阻害薬 |
| CA2920257C (en) | 2013-08-06 | 2023-02-21 | Imago Biosciences Inc. | Kdm1a inhibitors for the treatment of disease |
| EP3224352B1 (en) * | 2014-11-26 | 2024-01-03 | Istituto Europeo di Oncologia S.r.l. | Reprogramming-based models of neurodevelopmental disorders and uses thereof |
| BR112017017074A2 (pt) | 2015-02-12 | 2018-04-10 | Imago Biosciences Inc | Compostos; sal; bis-tosilatos de n-((s)-5-((1r,2s)-2-(4- fluorofenil)ciclopropilamino)-1-(4-metilpiperazin-1- il)-1-oxopentan-2-il)-4-(1h-1,2,3-triazol-1-il)benzamida; sal de tosilato de um composto; sal de bis- tosilato de um composto; compostos, sais, polimorfos ou solvatos; composições farmacêuticas, método para inibição de kdm1a; métodos para tratamento de uma doença mediada por kdm1a ou globina; método para atingir um efeito em um paciente; método para inibir pelo menos uma função de kdm1a |
| KR20180011331A (ko) | 2015-06-12 | 2018-01-31 | 오리존 지노믹스 에스.에이. | Lsd1 억제제와 관련된 바이오마커 및 그의 용도 |
| WO2017013061A1 (en) | 2015-07-17 | 2017-01-26 | Oryzon Genomics, S.A. | Biomarkers associated with lsd1 inhibitors and uses thereof |
| UA126277C2 (uk) | 2015-08-12 | 2022-09-14 | Інсайт Корпорейшн | Солі інгібітору lsd1 |
| TWI679195B (zh) | 2015-11-27 | 2019-12-11 | 日商大鵬藥品工業股份有限公司 | 新穎聯苯化合物或其鹽 |
| WO2017151732A1 (en) * | 2016-03-02 | 2017-09-08 | Beth Israel Deaconess Medical Center Technology Venture Office, Br2 | Therapeutic targets for lin-28-expressing cancers |
| WO2017157825A1 (en) | 2016-03-15 | 2017-09-21 | F. Hoffmann-La Roche Ag | Combinations of lsd1 inhibitors for use in the treatment of solid tumors |
| JP2019512546A (ja) | 2016-03-16 | 2019-05-16 | オリゾン・ゲノミクス・ソシエダッド・アノニマ | Ｋｄｍ１ａ標的会合を決定するための方法、およびそれに有用な化学プローブ |
| WO2017213999A1 (en) | 2016-06-07 | 2017-12-14 | The J. David Gladstone Institutes | Medium chain fatty acid esters of beta-hydroxybutyrate and butanediol and compositions and methods for using same |
| US11390590B2 (en) | 2016-08-16 | 2022-07-19 | Imago Biosciences, Inc. | Methods and processes for the preparation of KDM1A inhibitors |
| US20190256930A1 (en) | 2016-11-03 | 2019-08-22 | Oryzon Genomics, S.A. | Biomarkers for determining responsiveness to lsd1 inhibitors |
| WO2018083138A1 (en) | 2016-11-03 | 2018-05-11 | Oryzon Genomics, S.A. | Pharmacodynamic biomarkers for personalized cancer care using epigenetic modifying agents |
| CN110740991B (zh) | 2017-05-26 | 2023-07-04 | 大鹏药品工业株式会社 | 新型联苯化合物或其盐 |
| TWI770925B (zh) | 2017-05-26 | 2022-07-11 | 日商大鵬藥品工業股份有限公司 | 使用有新穎聯苯化合物之抗腫瘤效果增強劑 |
| TWI749235B (zh) | 2017-05-31 | 2021-12-11 | 日商大鵬藥品工業股份有限公司 | 基於insm1表現之lsd1抑制劑之治療效果的預測方法 |
| MX2020000734A (es) | 2017-07-21 | 2020-07-29 | Buck Inst Res Aging | Enantiómeros s de beta-hidroxibutirato y butanodiol, y métodos para usarlos. |
| CN110996949A (zh) | 2017-08-03 | 2020-04-10 | 奥瑞泽恩基因组学股份有限公司 | 用于治疗行为改变的方法 |
| CN107828747B (zh) * | 2017-10-23 | 2020-11-03 | 中山大学附属第六医院 | 一种多肽及其编码基因和用途 |
| WO2019147503A1 (en) | 2018-01-25 | 2019-08-01 | Buck Institute For Research On Aging | Synthesis of 3-hydroxybutyryl 3-hydroxybutyrate and related compounds |
| ES2977656T3 (es) | 2018-05-11 | 2024-08-28 | Imago Biosciences Inc | Inhibidores de KDM1A para el tratamiento de enfermedades |
| WO2020047198A1 (en) | 2018-08-31 | 2020-03-05 | Incyte Corporation | Salts of an lsd1 inhibitor and processes for preparing the same |
| WO2020152280A1 (en) * | 2019-01-24 | 2020-07-30 | Fundación Pública Andaluza Progreso Y Salud | Lsd1 inhibitors for use in the treatment of type 2 diabetes |
| JP7536316B2 (ja) | 2019-03-20 | 2024-08-20 | オリソン ヘノミクス，ソシエダ アノニマ | 境界性パーソナリティ障害の処置方法 |
| US20220151999A1 (en) | 2019-03-20 | 2022-05-19 | Oryzon Genomics, S.A. | Methods of treating attention deficit hyperactivity disorder using kdm1a inhibitors such as the compound vafidemstat |
| JP2022546908A (ja) | 2019-07-05 | 2022-11-10 | オリゾン・ゲノミクス・ソシエダッド・アノニマ | Ｋｄｍ１ａ阻害剤を使用した小細胞肺がんの個別化された処置のためのバイオマーカーおよび方法 |
| EP4058151B1 (en) | 2019-11-13 | 2025-05-21 | Taiho Pharmaceutical Co., Ltd. | Novel salt of terphenyl compound |
| JP2023524328A (ja) * | 2019-12-09 | 2023-06-12 | イマーゴ バイオサイエンシーズ インコーポレイテッド | 骨髄増殖性新生物の治療のためのリシン特異的ヒストンデメチラーゼ阻害剤 |
| WO2022214303A1 (en) | 2021-04-08 | 2022-10-13 | Oryzon Genomics, S.A. | Combinations of lsd1 inhibitors for treating myeloid cancers |
| US20250032454A1 (en) * | 2021-10-18 | 2025-01-30 | Imago Biosciences, Inc. | Kdm1a inhibitors for the treatment of disease |
| JP2025516647A (ja) | 2022-05-09 | 2025-05-30 | オリゾン・ゲノミクス・ソシエダッド・アノニマ | Ｌｓｄ１阻害薬を用いる悪性末梢神経鞘腫（ｍｐｎｓｔ）の治療法 |
| CN119497613A (zh) | 2022-05-09 | 2025-02-21 | 奥莱松基因组股份有限公司 | 使用lsd1抑制剂治疗nf1-突变肿瘤的方法 |
| JP2025538876A (ja) | 2022-11-24 | 2025-12-02 | オリゾン・ゲノミクス・ソシエダッド・アノニマ | がん治療のためのｌｓｄ１阻害薬とメニン阻害薬の組合せ |
Family Cites Families (41)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1804811A4 (en) | 2004-09-24 | 2011-04-27 | Idenix Cayman Ltd | METHOD AND COMPOSITION FOR THE TREATMENT OF FLAVIVERS, PESTIVERS AND HEPACIVIRES |
| WO2008103277A2 (en) | 2007-02-16 | 2008-08-28 | Amgen Inc. | Nitrogen-containing heterocyclyl ketones and their use as c-met inhibitors |
| UA98961C2 (uk) | 2007-06-27 | 2012-07-10 | Астразенека Аб | Похідні піразинону та їх застосування у лікуванні легеневих захворювань |
| US8748143B2 (en) | 2007-09-13 | 2014-06-10 | Codexis, Inc. | Ketoreductase polypeptides for the reduction of acetophenones |
| ES2547528T3 (es) | 2007-10-01 | 2015-10-07 | Codexis, Inc. | Polipéptidos de cetorreductasa para la producción de acetidinona |
| WO2010025287A2 (en) | 2008-08-27 | 2010-03-04 | Codexis, Inc. | Ketoreductase polypeptides for the production of 3-aryl-3-hydroxypropanamine from a 3-aryl-3-ketopropanamine |
| EP2361242B1 (en) | 2008-10-17 | 2018-08-01 | Oryzon Genomics, S.A. | Oxidase inhibitors and their use |
| EP2177502A1 (en) | 2008-10-17 | 2010-04-21 | Oryzon Genomics, S.A. | Compounds and their use |
| JPWO2010143582A1 (ja) | 2009-06-11 | 2012-11-22 | 公立大学法人名古屋市立大学 | フェニルシクロプロピルアミン誘導体及びｌｓｄ１阻害剤 |
| EP2480528B1 (en) | 2009-09-25 | 2018-08-29 | Oryzon Genomics, S.A. | Lysine specific demethylase-1 inhibitors and their use |
| WO2011042217A1 (en) | 2009-10-09 | 2011-04-14 | Oryzon Genomics S.A. | Substituted heteroaryl- and aryl- cyclopropylamine acetamides and their use |
| US8722743B2 (en) | 2010-04-19 | 2014-05-13 | Oryzon Genomics S.A. | Lysine specific demethylase-1 inhibitors and their use |
| CN102985402B (zh) | 2010-04-20 | 2015-04-29 | 罗马大学 | 反苯环丙胺衍生物作为组蛋白去甲基酶lsd1和/或lsd2的抑制剂 |
| ES2674747T3 (es) | 2010-07-29 | 2018-07-03 | Oryzon Genomics, S.A. | Inhibidores de demetilasa LSD1 basados en arilciclopropilamina y sus usos médicos |
| WO2012013727A1 (en) | 2010-07-29 | 2012-02-02 | Oryzon Genomics S.A. | Cyclopropylamine derivatives useful as lsd1 inhibitors |
| WO2012034116A2 (en) | 2010-09-10 | 2012-03-15 | The Johns Hopkins University | Small molecules as epigenetic modulators of lysine-specific demethylase 1 and methods of treating disorders |
| US20120108500A1 (en) * | 2010-10-07 | 2012-05-03 | Naoki Sakane | Compositions and Methods for Modulating Immunodeficiency Virus Transcription |
| WO2012045883A1 (en) | 2010-10-08 | 2012-04-12 | Oryzon Genomics S.A. | Cyclopropylamine inhibitors of oxidases |
| WO2012071469A2 (en) | 2010-11-23 | 2012-05-31 | Nevada Cancer Institute | Histone demethylase inhibitors and uses thereof for treatment o f cancer |
| EP2712315B1 (en) | 2011-02-08 | 2021-11-24 | Oryzon Genomics, S.A. | Lysine demethylase inhibitors for myeloproliferative disorders |
| US20140163041A1 (en) | 2011-02-08 | 2014-06-12 | Oryzon Genomics S.A. | Lysine demethylase inhibitors for myeloproliferative or lymphoproliferative diseases or disorders |
| ES2742805T3 (es) | 2011-03-25 | 2020-02-17 | Glaxosmithkline Ip No 2 Ltd | Ciclopropilaminas como inhibidores de LSD1 |
| EA025529B1 (ru) | 2011-08-09 | 2017-01-30 | Такеда Фармасьютикал Компани Лимитед | Циклопропанаминовое соединение |
| JP6046154B2 (ja) | 2011-10-20 | 2016-12-14 | オリソン ヘノミクス エセ． アー． | Ｌｓｄ１阻害剤としての（ヘテロ）アリールシクロプロピルアミン化合物 |
| EP2768805B1 (en) | 2011-10-20 | 2020-03-25 | Oryzon Genomics, S.A. | (hetero)aryl cyclopropylamine compounds as lsd1 inhibitors |
| JP6238908B2 (ja) * | 2012-11-28 | 2017-11-29 | 京都府公立大学法人 | リシン構造を有するｌｓｄ１選択的阻害薬 |
| EP2740474A1 (en) | 2012-12-05 | 2014-06-11 | Instituto Europeo di Oncologia S.r.l. | Cyclopropylamine derivatives useful as inhibitors of histone demethylases kdm1a |
| WO2014164867A1 (en) * | 2013-03-11 | 2014-10-09 | Imago Biosciences | Kdm1a inhibitors for the treatment of disease |
| EP3013424B1 (en) * | 2013-06-25 | 2024-09-25 | EpiAxis Therapeutics Pty Ltd | Lsd inhibitors for modulating cancer stem cells |
| CA2920257C (en) | 2013-08-06 | 2023-02-21 | Imago Biosciences Inc. | Kdm1a inhibitors for the treatment of disease |
| DK3105218T3 (da) | 2014-02-13 | 2019-11-04 | Incyte Corp | Cyclopropylaminer som lsd1-inhibitorer |
| CN121203988A (zh) | 2014-04-22 | 2025-12-26 | C-乐克塔股份有限公司 | 酮还原酶 |
| SI3160956T1 (sl) | 2014-06-27 | 2020-11-30 | Celgene Quanticel Research, Inc. | Inhibitorji lizin-specifične demetilaze-1 |
| BR112017017074A2 (pt) | 2015-02-12 | 2018-04-10 | Imago Biosciences Inc | Compostos; sal; bis-tosilatos de n-((s)-5-((1r,2s)-2-(4- fluorofenil)ciclopropilamino)-1-(4-metilpiperazin-1- il)-1-oxopentan-2-il)-4-(1h-1,2,3-triazol-1-il)benzamida; sal de tosilato de um composto; sal de bis- tosilato de um composto; compostos, sais, polimorfos ou solvatos; composições farmacêuticas, método para inibição de kdm1a; métodos para tratamento de uma doença mediada por kdm1a ou globina; método para atingir um efeito em um paciente; método para inibir pelo menos uma função de kdm1a |
| US20190070172A1 (en) | 2015-11-05 | 2019-03-07 | Imago Biosciences, Inc. | Lysine-specific histone demethylase as a novel therapeutic target in myeloproliferative neoplasms |
| MX384792B (es) | 2015-12-29 | 2025-03-14 | Mirati Therapeutics Inc | Inhibidores de desmetilasa especifica de lisina 1 (lsd1). |
| WO2017195216A1 (en) | 2016-05-09 | 2017-11-16 | Jubilant Biosys Limited | Cyclopropyl-amide compounds as dual lsd1/hdac inhibitors |
| CN110268067A (zh) | 2016-08-16 | 2019-09-20 | 伊美格生物科学公司 | 用于产生立体异构纯的氨基环丙烷的组合物和方法 |
| US11390590B2 (en) | 2016-08-16 | 2022-07-19 | Imago Biosciences, Inc. | Methods and processes for the preparation of KDM1A inhibitors |
| US20200069677A1 (en) | 2016-12-09 | 2020-03-05 | Constellation Pharmaceuticals, Inc. | Markers for personalized cancer treatment with lsd1 inhibitors |
| ES2977656T3 (es) | 2018-05-11 | 2024-08-28 | Imago Biosciences Inc | Inhibidores de KDM1A para el tratamiento de enfermedades |
-
2014
- 2014-08-06 CA CA2920257A patent/CA2920257C/en active Active
- 2014-08-06 KR KR1020167005974A patent/KR102255778B1/ko active Active
- 2014-08-06 EP EP14834451.8A patent/EP3030323B1/en active Active
- 2014-08-06 AU AU2014306149A patent/AU2014306149B2/en active Active
- 2014-08-06 BR BR112016002496-6A patent/BR112016002496B1/pt active IP Right Grant
- 2014-08-06 ES ES14834451T patent/ES2734209T3/es active Active
- 2014-08-06 CN CN201480053762.6A patent/CN105592888A/zh active Pending
- 2014-08-06 US US14/910,423 patent/US9790195B2/en active Active
- 2014-08-06 WO PCT/US2014/049906 patent/WO2015021128A1/en not_active Ceased
- 2014-08-06 DK DK14834451.8T patent/DK3030323T3/da active
- 2014-08-06 MX MX2016001587A patent/MX383590B/es unknown
- 2014-08-06 JP JP2016533392A patent/JP6521967B2/ja active Active
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2016
- 2016-01-27 ZA ZA2016/00901A patent/ZA201600901B/en unknown
- 2016-02-04 IL IL243976A patent/IL243976B/en active IP Right Grant
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2017
- 2017-08-02 US US15/667,166 patent/US10370346B2/en active Active
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2019
- 2019-06-19 US US16/445,768 patent/US10882835B2/en active Active
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2020
- 2020-12-01 US US17/108,663 patent/US11655226B2/en active Active