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.)
- Granted
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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 |
|---|---|---|---|---|
| US9388123B2 (en) * | 2012-11-28 | 2016-07-12 | Kyoto University | LSD1-selective inhibitor having lysine structure |
| WO2015021128A1 (en) | 2013-08-06 | 2015-02-12 | Imago Biosciences Inc. | Kdm1a inhibitors for the treatment of disease |
| ES2973286T3 (es) | 2014-11-26 | 2024-06-19 | St Europeo Di Oncologia S R L | Modelos de trastornos del desarrollo neurológico basados en la reprogramación y usos de los mismos |
| PL3256218T3 (pl) | 2015-02-12 | 2025-03-31 | Imago Biosciences Inc. | Inhibitor kdm1a i jego zastosowanie w terapii |
| WO2016198649A1 (en) | 2015-06-12 | 2016-12-15 | Oryzon Genomics, S.A. | Biomarkers associated with lsd1 inhibitors and uses thereof |
| WO2017013061A1 (en) | 2015-07-17 | 2017-01-26 | Oryzon Genomics, S.A. | Biomarkers associated with lsd1 inhibitors and uses thereof |
| KR102710120B1 (ko) | 2015-08-12 | 2024-09-27 | 인사이트 홀딩스 코포레이션 | Lsd1 저해제의 염 |
| RU2726622C2 (ru) | 2015-11-27 | 2020-07-15 | Тайхо Фармасьютикал Ко., Лтд. | Новое соединение бифенила или его соль |
| US20190091256A1 (en) * | 2016-03-02 | 2019-03-28 | Beth Israel Deaconess Medical Center | Therapeutic targets for lin-28-expressing cancers |
| AU2017233898B2 (en) | 2016-03-15 | 2022-12-15 | Oryzon Genomics, S.A. | Combinations of LSD1 inhibitors for use in the treatment of solid tumors |
| ES3042059T3 (en) | 2016-03-16 | 2025-11-18 | Oryzon Genomics Sa | Methods to determine kdm1a target engagement and chemoprobes useful therefor |
| EP4585270A3 (en) * | 2016-06-07 | 2025-09-24 | The J. David Gladstone Institutes | Medium chain fatty acid esters of beta-hydroxybutyrate and butanediol and compositions and methods for using same |
| CN111194306B (zh) * | 2016-08-16 | 2023-05-16 | 伊美格生物科学公司 | 用于制备kdm1a抑制剂的方法和过程 |
| EP3535420A1 (en) | 2016-11-03 | 2019-09-11 | Oryzon Genomics, S.A. | Biomarkers for determining responsiveness to lsd1 inhibitors |
| US20190256929A1 (en) | 2016-11-03 | 2019-08-22 | Oryzon Genomics, S.A. | Pharmacodynamic biomarkers for personalized cancer care using epigenetic modifying agents |
| TWI727173B (zh) | 2017-05-26 | 2021-05-11 | 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 |
| WO2018216800A1 (ja) | 2017-05-26 | 2018-11-29 | 大鵬薬品工業株式会社 | 新規なビフェニル化合物又はその塩 |
| WO2018221555A1 (ja) * | 2017-05-31 | 2018-12-06 | 大鵬薬品工業株式会社 | Ｉｎｓｍ１の発現に基づくｌｓｄ１阻害剤の治療効果の予測方法 |
| EP3654963A4 (en) | 2017-07-21 | 2021-04-14 | Buck Institute for Research on Aging | BETA-HYDROXYBUTYRATE AND BUTANEDIOL S ENANTIOMERS AND THEIR METHODS OF USE |
| MY204406A (en) | 2017-08-03 | 2024-08-27 | Oryzon Genomics Sa | Methods of treating behavior alterations |
| 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 |
| US12037317B2 (en) | 2018-01-25 | 2024-07-16 | Buck Institute For Research On Aging | Synthesis of 3-hydroxybutyryl 3-hydroxybutyrate and related compounds |
| JP7450559B2 (ja) * | 2018-05-11 | 2024-03-15 | イマーゴ バイオサイエンシーズ インコーポレイテッド | 疾患の処置のためのｋｄｍ１ａ阻害剤 |
| US10968200B2 (en) | 2018-08-31 | 2021-04-06 | 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 |
| BR112021016064A2 (pt) | 2019-03-20 | 2021-10-05 | Oryzon Genomics, S.A. | Métodos de tratamento do transtorno de personalidade borderline |
| CN120837494A (zh) | 2019-03-20 | 2025-10-28 | 奥莱松基因组股份有限公司 | 使用kdm1a抑制剂如化合物伐菲德司他治疗注意缺陷多动症的方法 |
| 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 |
| MX2022005812A (es) | 2019-11-13 | 2022-08-16 | Taiho Pharmaceutical Co Ltd | Metodos de tratamiento de enfermedades y trastornos relacionados con desmetilasa 1 especifica de lisina con inhibidores de desmetilasa 1 especifica de lisina. |
| CN115397820A (zh) * | 2019-12-09 | 2022-11-25 | 伊美格生物科学公司 | 用于治疗骨髓增生性肿瘤的赖氨酸特异性组蛋白脱甲基化酶抑制剂 |
| CA3231846A1 (en) | 2021-04-08 | 2022-10-13 | Tamara Maes | Combinations of lsd1 inhibitors for treating myeloid cancers |
| EP4419504A4 (en) * | 2021-10-18 | 2025-09-03 | Imago Biosciences Inc | KDM1A INHIBITORS FOR THE TREATMENT OF DISEASE |
| EP4522136A1 (en) | 2022-05-09 | 2025-03-19 | Oryzon Genomics, S.A. | Methods of treating malignant peripheral nerve sheath tumor (mpnst) using lsd1 inhibitors |
| 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 |
| AU2023385514A1 (en) | 2022-11-24 | 2025-07-10 | Oryzon Genomics, S.A. | Combinations of lsd1 inhibitors and menin inhibitors for treating cancer |
Family Cites Families (41)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20070073805A (ko) | 2004-09-24 | 2007-07-10 | 이데닉스 (케이만) 리미티드 | 플라비바이러스, 페스티바이러스 및 헤파시바이러스를치료하기 위한 방법 및 조성물 |
| EP2114898A2 (en) | 2007-02-16 | 2009-11-11 | Amgen Inc. | Nitrogen-containing heterocyclyl ketones and their use as c-met inhibitors |
| HRP20141174T1 (hr) | 2007-06-27 | 2015-02-13 | Astrazeneca Ab | Derivati pirazinona i njihova uporaba za lijeäśenje bolesti pluä†a |
| CN101855342B (zh) | 2007-09-13 | 2013-07-10 | 科德克希思公司 | 用于还原苯乙酮的酮还原酶多肽 |
| EP2205727B1 (en) | 2007-10-01 | 2015-06-24 | Codexis, Inc. | Ketoreductase polypeptides for the production of azetidinone |
| US8288141B2 (en) | 2008-08-27 | 2012-10-16 | 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 |
| KR101736218B1 (ko) | 2009-09-25 | 2017-05-16 | 오리존 지노믹스 에스.에이. | 라이신 특이적 디메틸라아제-1 억제제 및 이의 용도 |
| EP2486002B1 (en) | 2009-10-09 | 2019-03-27 | Oryzon Genomics, S.A. | Substituted heteroaryl- and aryl- cyclopropylamine acetamides and their use |
| ES2607081T3 (es) | 2010-04-19 | 2017-03-29 | Oryzon Genomics, S.A. | Inhibidores de desmetilasa específica de lisina-1 y su uso |
| EA022459B1 (ru) | 2010-04-20 | 2016-01-29 | Университа' Дельи Студи Ди Рома "Ла Сапиенца" | Производные транилципромина в качестве ингибиторов гистон деметилаз lsd1 и/или lsd2 |
| US9006449B2 (en) | 2010-07-29 | 2015-04-14 | Oryzon Genomics, S.A. | Cyclopropylamine derivatives useful as LSD1 inhibitors |
| LT2598482T (lt) | 2010-07-29 | 2018-07-10 | Oryzon Genomics, S.A. | Demetilazės lsd1 inhibitoriai arilciklopropilamino pagrindu ir jų medicininis panaudojimas |
| US9527805B2 (en) | 2010-09-10 | 2016-12-27 | Robert A. Casero | 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 |
| US9061966B2 (en) | 2010-10-08 | 2015-06-23 | 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 |
| US20140163041A1 (en) | 2011-02-08 | 2014-06-12 | Oryzon Genomics S.A. | Lysine demethylase inhibitors for myeloproliferative or lymphoproliferative diseases or disorders |
| WO2012107498A1 (en) * | 2011-02-08 | 2012-08-16 | Oryzon Genomics S.A. | Lysine demethylase inhibitors for myeloproliferative disorders |
| CN103857393B (zh) * | 2011-03-25 | 2016-08-17 | 葛兰素史密斯克莱知识产权（第2号）有限公司 | 环丙基胺作为lsd1抑制剂 |
| UA114406C2 (uk) | 2011-08-09 | 2017-06-12 | Такеда Фармасьютікал Компані Лімітед | Похідні циклопропанаміну як інгібітори lsd1 |
| EP3736265A1 (en) | 2011-10-20 | 2020-11-11 | Oryzon Genomics, S.A. | (hetero)aryl cyclopropylamine compounds as lsd1 inhibitors |
| SI2776394T1 (sl) | 2011-10-20 | 2019-05-31 | Oryzon Genomics, S.A. | Spojine (hetero)aril ciklopropilamina kot inhibitorji LSD1 |
| US9388123B2 (en) | 2012-11-28 | 2016-07-12 | Kyoto University | LSD1-selective inhibitor having lysine structure |
| 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 |
| US10220053B2 (en) * | 2013-06-25 | 2019-03-05 | University Of Canberra | Methods and compositions for modulating cancer stem cells |
| WO2015021128A1 (en) | 2013-08-06 | 2015-02-12 | Imago Biosciences Inc. | Kdm1a inhibitors for the treatment of disease |
| PE20161573A1 (es) | 2014-02-13 | 2017-01-19 | Incyte Corp | Ciclopropilamina como inhibidor de la lsd1 |
| EP3134519B1 (en) | 2014-04-22 | 2018-06-06 | c-LEcta GmbH | Ketoreductases |
| ES2812626T3 (es) | 2014-06-27 | 2021-03-17 | Celgene Quanticel Res Inc | Inhibidores de la desmetilasa 1 específica de lisina |
| PL3256218T3 (pl) | 2015-02-12 | 2025-03-31 | Imago Biosciences Inc. | Inhibitor kdm1a i jego zastosowanie w terapii |
| US20190070172A1 (en) | 2015-11-05 | 2019-03-07 | Imago Biosciences, Inc. | Lysine-specific histone demethylase as a novel therapeutic target in myeloproliferative neoplasms |
| KR102720551B1 (ko) | 2015-12-29 | 2024-10-21 | 미라티 테라퓨틱스, 인크. | Lsd1 억제제 |
| CA3022561A1 (en) | 2016-05-09 | 2017-11-16 | Sridharan Rajagopal | Cyclopropyl-amide compounds as dual lsd1/hdac inhibitors |
| CN111194306B (zh) | 2016-08-16 | 2023-05-16 | 伊美格生物科学公司 | 用于制备kdm1a抑制剂的方法和过程 |
| 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 |
| WO2018106984A1 (en) | 2016-12-09 | 2018-06-14 | Constellation Pharmaceuticals, Inc. | Markers for personalized cancer treatment with lsd1 inhibitors |
| JP7450559B2 (ja) | 2018-05-11 | 2024-03-15 | イマーゴ バイオサイエンシーズ インコーポレイテッド | 疾患の処置のためのｋｄｍ１ａ阻害剤 |
-
2014
- 2014-08-06 WO PCT/US2014/049906 patent/WO2015021128A1/en not_active Ceased
- 2014-08-06 JP JP2016533392A patent/JP6521967B2/ja active Active
- 2014-08-06 MX MX2016001587A patent/MX383590B/es unknown
- 2014-08-06 US US14/910,423 patent/US9790195B2/en active Active
- 2014-08-06 KR KR1020167005974A patent/KR102255778B1/ko active Active
- 2014-08-06 CA CA2920257A patent/CA2920257C/en active Active
- 2014-08-06 AU AU2014306149A patent/AU2014306149B2/en active Active
- 2014-08-06 EP EP14834451.8A patent/EP3030323B1/en active Active
- 2014-08-06 BR BR112016002496-6A patent/BR112016002496B1/pt active IP Right Grant
- 2014-08-06 CN CN201480053762.6A patent/CN105592888A/zh active Pending
- 2014-08-06 DK DK14834451.8T patent/DK3030323T3/da active
- 2014-08-06 ES ES14834451T patent/ES2734209T3/es active Active
-
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