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 (https=) | 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 (https=) |
| EP (1) | EP3030323B1 (https=) |
| JP (1) | JP6521967B2 (https=) |
| KR (1) | KR102255778B1 (https=) |
| CN (1) | CN105592888A (https=) |
| AU (1) | AU2014306149B2 (https=) |
| BR (1) | BR112016002496B1 (https=) |
| CA (1) | CA2920257C (https=) |
| DK (1) | DK3030323T3 (https=) |
| ES (1) | ES2734209T3 (https=) |
| IL (1) | IL243976B (https=) |
| MX (1) | MX383590B (https=) |
| WO (1) | WO2015021128A1 (https=) |
| ZA (1) | ZA201600901B (https=) |
Families Citing this family (35)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2927212A4 (en) * | 2012-11-28 | 2016-06-08 | Univ Kyoto | LSD1-SELECTIVE HEMMER WITH LYSINE STRUCTURE |
| ES2734209T3 (es) | 2013-08-06 | 2019-12-04 | Imago Biosciences Inc | Inhibidores de KDM1A para el tratamiento de enfermedades |
| 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 |
| CA2987876A1 (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 |
| LT3334709T (lt) | 2015-08-12 | 2025-03-10 | Incyte Holdings Corporation | Lsd1 inhibitoriaus druskos |
| PL3381896T3 (pl) | 2015-11-27 | 2023-05-08 | Taiho Pharmaceutical Co., Ltd. | Związek bifenylowy lub jego sól |
| WO2017151732A1 (en) * | 2016-03-02 | 2017-09-08 | Beth Israel Deaconess Medical Center Technology Venture Office, Br2 | Therapeutic targets for lin-28-expressing cancers |
| ES3057783T3 (en) | 2016-03-15 | 2026-03-04 | Oryzon Genomics Sa | Combinations of lsd1 inhibitors for use in the treatment of neoplastic diseases |
| WO2017158136A1 (en) | 2016-03-16 | 2017-09-21 | Oryzon Genomics, S.A. | Methods to determine kdm1a target engagement and chemoprobes useful therefor |
| 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 |
| WO2018035259A1 (en) * | 2016-08-16 | 2018-02-22 | Imago Biosciences, Inc. | Methods and processes for the preparation of kdm1a inhibitors |
| WO2018083138A1 (en) | 2016-11-03 | 2018-05-11 | Oryzon Genomics, S.A. | Pharmacodynamic biomarkers for personalized cancer care using epigenetic modifying agents |
| WO2018083189A1 (en) | 2016-11-03 | 2018-05-11 | Oryzon Genomics, S.A. | Biomarkers for determining responsiveness to lsd1 inhibitors |
| JP6738962B2 (ja) | 2017-05-26 | 2020-08-12 | 大鵬薬品工業株式会社 | 新規なビフェニル化合物を用いた抗腫瘍効果増強剤 |
| 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 |
| US12435128B2 (en) | 2017-05-31 | 2025-10-07 | Taiho Pharmaceutical Co., Ltd. | Method for predicting therapeutic effect of LSD1 inhibitor based on expression of INSM1 |
| WO2019018683A1 (en) | 2017-07-21 | 2019-01-24 | Buck Institute For Research On Aging | BETA-HYDROXYBUTYRATE AND BUTANEDIOL ENANTIOMERS AND METHODS OF USE THEREOF |
| MX2020001323A (es) | 2017-08-03 | 2020-03-20 | Oryzon Genomics Sa | Metodos para tratar alteraciones del comportamiento. |
| 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 |
| BR112021001066A2 (pt) * | 2018-05-11 | 2021-04-20 | Imago Biosciences, Inc. | composto, método de tratamento de uma doença mediada por kdm1a, método de tratamento de uma doença mediada por globina, composição farmacêutica; método de inibição de kdm1a, método para obter um efeito em um paciente, e método para inibir pelo menos uma função de kdm1a |
| 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 |
| SG11202109159VA (en) | 2019-03-20 | 2021-10-28 | Oryzon Genomics Sa | Methods of treating borderline personality disorder |
| ES3053813T3 (en) | 2019-03-20 | 2026-01-26 | Oryzon Genomics Sa | Methods of treating attention deficit hyperactivity disorder using kdm1a inhibitors such as the compound vafidemstat |
| CN114341366A (zh) | 2019-07-05 | 2022-04-12 | 奥莱松基因组股份有限公司 | 用于使用kdm1a抑制剂个体化治疗小细胞肺癌的生物标志物和方法 |
| 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. |
| IL293703A (en) * | 2019-12-09 | 2022-08-01 | Imago Biosciences Inc | Lysine-specific histone demethylase inhibitors for the treatment of myeloproliferative neoplasms |
| JP2024513260A (ja) | 2021-04-08 | 2024-03-22 | オリゾン ジェノミックス ソシエダッド アノニマ | 骨髄癌処置のためのｌｓｄ１阻害剤の組み合わせ |
| WO2023069884A1 (en) * | 2021-10-18 | 2023-04-27 | Imago Biosciences, Inc. | Kdm1a inhibitors for the treatment of disease |
| CN119546292A (zh) | 2022-05-09 | 2025-02-28 | 奥莱松基因组股份有限公司 | 使用lsd1抑制剂治疗恶性周围神经鞘瘤(mpnst)的方法 |
| JP2025516648A (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ｎｆ１変異腫瘍の治療法 |
| CN120529900A (zh) | 2022-11-24 | 2025-08-22 | 奥莱松基因组股份有限公司 | 用于治疗癌症的LSD1抑制剂和Menin抑制剂的组合 |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BRPI0515896A (pt) | 2004-09-24 | 2008-08-12 | Idenix Cayman Ltd E Ct Nat De | composto ou um sal ou éster farmaceuticamente aceitável do mesmo, método para o tratamento ou profilaxia de um hospedeiro infectado com uma infecção por flavivìrus, pestivìrus ou hepacivìrus, e, composição farmacêutica para o tratamento de um hospedeiro infectado com uma infecção por flavivìrus, pestivìrus ou hepacivìrus |
| AU2008219166B2 (en) | 2007-02-16 | 2013-05-16 | Amgen Inc. | Nitrogen-containing heterocyclyl ketones and their use as c-Met inhibitors |
| EP2170848B1 (en) | 2007-06-27 | 2014-10-22 | AstraZeneca AB | Pyrazinone derivatives and their use in the treatment of lung diseases |
| KR101586503B1 (ko) | 2007-09-13 | 2016-01-18 | 코덱시스, 인코포레이티드 | 아세토페논의 환원을 위한 케토리덕타제 폴리펩티드 |
| WO2009046153A1 (en) | 2007-10-01 | 2009-04-09 | 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 |
| EP2177502A1 (en) | 2008-10-17 | 2010-04-21 | Oryzon Genomics, S.A. | Compounds and their use |
| EP2361242B1 (en) | 2008-10-17 | 2018-08-01 | Oryzon Genomics, S.A. | Oxidase inhibitors 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 |
| RU2602814C2 (ru) | 2009-09-25 | 2016-11-20 | Оризон Дженомикс С.А. | Лизинспецифические ингибиторы деметилазы-1 и их применение |
| US8946296B2 (en) | 2009-10-09 | 2015-02-03 | Oryzon Genomics S.A. | Substituted heteroaryl- and aryl-cyclopropylamine acetamides and their use |
| RS55348B1 (sr) * | 2010-04-19 | 2017-03-31 | Oryzon Gnomics S A | Inhibitori lizin specifične demetilaze-1 i njihova upotreba |
| 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 |
| EP2598480B1 (en) | 2010-07-29 | 2019-04-24 | Oryzon Genomics, S.A. | Cyclopropylamine derivatives useful as lsd1 inhibitors |
| WO2012013728A1 (en) | 2010-07-29 | 2012-02-02 | Oryzon Genomics S.A. | Arylcyclopropylamine based demethylase inhibitors of lsd1 and their medical use |
| 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 |
| EA023143B1 (ru) * | 2011-03-25 | 2016-04-29 | Глэксосмитклайн Интеллекчуал Проперти (No.2) Лимитед | Замещенный циклопропиламин в качестве ингибитора lsd1 |
| KR20140052018A (ko) | 2011-08-09 | 2014-05-02 | 다케다 야쿠힌 고교 가부시키가이샤 | 시클로프로판아민 화합물 |
| RU2668952C2 (ru) | 2011-10-20 | 2018-10-05 | Оризон Дженомикс, С.А. | (гетеро)арилциклопропиламины в качестве ингибиторов lsd1 |
| MX356344B (es) | 2011-10-20 | 2018-05-23 | Oryzon Genomics Sa | Compuestos de (hetero)arilciclopropilamina como inhibidores de lsd1. |
| EP2927212A4 (en) | 2012-11-28 | 2016-06-08 | Univ Kyoto | LSD1-SELECTIVE HEMMER WITH 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 |
| CA2916533C (en) * | 2013-06-25 | 2022-12-20 | University Of Canberra | Methods and compositions for modulating cancer stem cells |
| ES2734209T3 (es) | 2013-08-06 | 2019-12-04 | Imago Biosciences Inc | Inhibidores de KDM1A para el tratamiento de enfermedades |
| SI3105218T1 (sl) | 2014-02-13 | 2019-11-29 | Incyte Corp | Ciklopropilamini kot inhibitorji LSD1 |
| EP3134519B1 (en) | 2014-04-22 | 2018-06-06 | c-LEcta GmbH | Ketoreductases |
| RS60658B1 (sr) | 2014-06-27 | 2020-09-30 | Celgene Quanticel Research Inc | Inhibitori lizin specifične demetilaze-1 |
| PL3256218T3 (pl) | 2015-02-12 | 2025-03-31 | Imago Biosciences Inc. | Inhibitor kdm1a i jego zastosowanie w terapii |
| WO2017079753A1 (en) | 2015-11-05 | 2017-05-11 | Imago Biosciences, Inc. | Lysine-specific histone demethylase as a novel therapeutic target in myeloproliferative neoplasms |
| JP6916795B2 (ja) | 2015-12-29 | 2021-08-11 | ミラティ セラピューティクス， インコーポレイテッド | Ｌｓｄ１阻害剤 |
| KR102479789B1 (ko) | 2016-05-09 | 2022-12-22 | 주빌런트 에피코어 엘엘씨 | 이중 lsd1/hdac 억제제로서 사이클로프로필-아마이드 화합물 |
| US20220025424A1 (en) | 2016-08-16 | 2022-01-27 | Imago Biosciences, Inc. | Compositions and methods for producing stereoisomerically pure aminocyclopropanes |
| WO2018035259A1 (en) | 2016-08-16 | 2018-02-22 | 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 |
| BR112021001066A2 (pt) | 2018-05-11 | 2021-04-20 | Imago Biosciences, Inc. | composto, método de tratamento de uma doença mediada por kdm1a, método de tratamento de uma doença mediada por globina, composição farmacêutica; método de inibição de kdm1a, método para obter um efeito em um paciente, e método para inibir pelo menos uma função de kdm1a |
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2014
- 2014-08-06 ES ES14834451T patent/ES2734209T3/es active Active
- 2014-08-06 CN CN201480053762.6A patent/CN105592888A/zh active Pending
- 2014-08-06 CA CA2920257A patent/CA2920257C/en active Active
- 2014-08-06 US US14/910,423 patent/US9790195B2/en active Active
- 2014-08-06 EP EP14834451.8A patent/EP3030323B1/en active Active
- 2014-08-06 MX MX2016001587A patent/MX383590B/es unknown
- 2014-08-06 JP JP2016533392A patent/JP6521967B2/ja active Active
- 2014-08-06 BR BR112016002496-6A patent/BR112016002496B1/pt active IP Right Grant
- 2014-08-06 KR KR1020167005974A patent/KR102255778B1/ko active Active
- 2014-08-06 AU AU2014306149A patent/AU2014306149B2/en active Active
- 2014-08-06 DK DK14834451.8T patent/DK3030323T3/da active
- 2014-08-06 WO PCT/US2014/049906 patent/WO2015021128A1/en not_active Ceased
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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