JP2019512546A - 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 - Google Patents

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 Download PDF

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JP2019512546A
JP2019512546A JP2019500019A JP2019500019A JP2019512546A JP 2019512546 A JP2019512546 A JP 2019512546A JP 2019500019 A JP2019500019 A JP 2019500019A JP 2019500019 A JP2019500019 A JP 2019500019A JP 2019512546 A JP2019512546 A JP 2019512546A
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kdm1a
trans
cyclyl
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カルセリャール・ゴンサレス，エレナ
マエス，タマラ
マスカーロ・クルサット，クリスティナ
オルテガ・ムニョス，アルベルト
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オリゾン・ゲノミクス・ソシエダッド・アノニマ
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    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12Q—MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
    • C12Q1/00—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions
    • C12Q1/26—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving oxidoreductase
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/58—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving labelled substances

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JP2019500019A 2016-03-16 2017-03-16 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 Pending JP2019512546A (ja)

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EP16382119 2016-03-16
EP16382119.2 2016-03-16
PCT/EP2017/056330 WO2017158136A1 (en) 2016-03-16 2017-03-16 Methods to determine kdm1a target engagement and chemoprobes useful therefor

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JP2019512546A true JP2019512546A (ja) 2019-05-16
JP2019512546A5 JP2019512546A5 (https=) 2020-04-30

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US (2) US11034991B2 (https=)
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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MX356344B (es) 2011-10-20 2018-05-23 Oryzon Genomics Sa Compuestos de (hetero)arilciclopropilamina como inhibidores de lsd1.
EP3090998A1 (en) 2015-05-06 2016-11-09 F. Hoffmann-La Roche AG Solid forms
CN109462980B (zh) 2016-03-15 2022-02-08 奥莱松基因组股份有限公司 用于治疗血液恶性肿瘤的lsd1抑制剂的组合
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
RS58951B1 (sr) 2016-06-10 2019-08-30 Oryzon Genomics Sa Lečenje multiple skleroze
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
WO2021197371A1 (zh) * 2020-03-31 2021-10-07 南京金斯瑞生物科技有限公司 一种含有刚性连接子的生物偶联物

Citations (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2007524357A (ja) * 2003-01-31 2007-08-30 プロメガ　コーポレイション タンパク質に対する官能基の共有結合的テザリング
WO2013022047A1 (ja) * 2011-08-09 2013-02-14 武田薬品工業株式会社 シクロプロパンアミン化合物
JP2013505903A (ja) * 2009-09-25 2013-02-21 オリゾン・ジェノミックス・ソシエダッド・アノニマ リジン特異的デメチラーゼ−１阻害剤およびその使用
JP2013525331A (ja) * 2010-04-19 2013-06-20 オリゾン・ジェノミックス・ソシエダッド・アノニマ リジン特異的脱メチル化酵素１阻害薬およびその使用
JP2013535460A (ja) * 2010-07-29 2013-09-12 オリゾン・ジェノミックス・ソシエダッド・アノニマ Ｌｓｄ１のアリールシクロプロピルアミンをベースとしたデメチラーゼ阻害剤およびそれらの医学的使用
WO2014058071A1 (ja) * 2012-10-12 2014-04-17 武田薬品工業株式会社 シクロプロパンアミン化合物およびその用途
JP2014515013A (ja) * 2011-03-25 2014-06-26 グラクソスミスクライン、インテレクチュアル、プロパティー、ナンバー２、リミテッド Ｌｓｄ１阻害剤としてのシクロプロピルアミン
WO2014151282A1 (en) * 2013-03-15 2014-09-25 Promega Corporation Substrates for covalent tethering of proteins to functional groups or solid surfaces
JP2014532619A (ja) * 2011-10-20 2014-12-08 オリゾン・ジェノミックス・ソシエダッド・アノニマＯｒｙｚｏｎ Ｇｅｎｏｍｉｃｓ Ｓ．Ａ． 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
JP2015502335A (ja) * 2011-10-20 2015-01-22 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

Family Cites Families (57)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2619005A1 (en) 2005-08-10 2007-02-22 Johns Hopkins University Polyamines useful as anti-parasitic and anti-cancer therapeutics and as lysine-specific demethylase inhibitors
CA2668286C (en) * 2006-11-03 2014-09-16 Pharmacyclics, Inc. Bruton's tyrosine kinase activity probe and method of using
WO2008127734A2 (en) 2007-04-13 2008-10-23 The Johns Hopkins University Lysine-specific demethylase inhibitors
EP2361242B1 (en) 2008-10-17 2018-08-01 Oryzon Genomics, S.A. Oxidase inhibitors and their use
WO2010084160A1 (en) 2009-01-21 2010-07-29 Oryzon Genomics S.A. Phenylcyclopropylamine derivatives and their medical use
US8389580B2 (en) 2009-06-02 2013-03-05 Duke University Arylcyclopropylamines and methods of 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
EP2467359A4 (en) 2009-08-18 2013-01-09 Univ Johns Hopkins (BIS-) UREA- AND (BIS-) THIOMINE COMPOUNDS AS EPIGENE MODULATORS OF THE LYSINE-SPECIFIC DEMETHYLASE 1 AND METHODS OF DISEASE TREATMENT THEREWITH
US8946296B2 (en) 2009-10-09 2015-02-03 Oryzon Genomics S.A. Substituted heteroaryl- and aryl-cyclopropylamine acetamides 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
EP2598480B1 (en) 2010-07-29 2019-04-24 Oryzon Genomics, S.A. Cyclopropylamine derivatives useful as lsd1 inhibitors
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
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
JP6122006B2 (ja) 2011-08-15 2017-04-26 ザ ユニバーシティ オブ ユタ リサーチ ファウンデイション ヒストン脱メチル化酵素阻害剤としての、置換された（ｅ）−ｎ’−（１−フェニルエチリデン）ベンゾヒドラジド類似体
US9289415B2 (en) 2011-09-01 2016-03-22 The Brigham And Women's Hospital, Inc. Treatment of cancer
EP2927212A4 (en) 2012-11-28 2016-06-08 Univ Kyoto LSD1-SELECTIVE HEMMER WITH LYSINE STRUCTURE
WO2014085613A1 (en) 2012-11-30 2014-06-05 Mccord Darlene E Hydroxytyrosol and oleuropein compositions for induction of dna damage, cell death and lsd1 inhibition
EP2740474A1 (en) 2012-12-05 2014-06-11 Instituto Europeo di Oncologia S.r.l. Cyclopropylamine derivatives useful as inhibitors of histone demethylases kdm1a
CN103054869A (zh) 2013-01-18 2013-04-24 郑州大学 含三唑基的氨基二硫代甲酸酯化合物在制备以lsd1为靶标药物中的应用
WO2014164867A1 (en) 2013-03-11 2014-10-09 Imago Biosciences Kdm1a inhibitors for the treatment of disease
NZ715331A (en) 2013-06-19 2019-09-27 The Univ Of Utah Research Foundation Substituted (e)-n’-(1-phenylethylidene) benzohydrazide analogs as histone demethylase inhibitors
CN103319466B (zh) 2013-07-04 2016-03-16 郑州大学 含香豆素母核的1,2,3-三唑-氨基二硫代甲酸酯化合物、制备方法及其应用
ES2734209T3 (es) 2013-08-06 2019-12-04 Imago Biosciences Inc Inhibidores de KDM1A para el tratamiento de enfermedades
US9186391B2 (en) 2013-08-29 2015-11-17 Musc Foundation For Research Development Cyclic peptide inhibitors of lysine-specific demethylase 1
US9556170B2 (en) 2013-08-30 2017-01-31 University Of Utah Research Foundation Substituted-1H-benzo[d]imidazole series compounds as lysine-specific demethylase 1 (LSD1) inhibitors
SI3080100T1 (sl) 2013-12-11 2023-04-28 Celgene Quanticel Research, Inc. Inhibitorji lizin specifične demetilaze-1
WO2015120281A1 (en) 2014-02-07 2015-08-13 Musc Foundation For Research Development Aminotriazole- and aminotetrazole-based kdm1a inhibitors as epigenetic modulators
SI3105218T1 (sl) 2014-02-13 2019-11-29 Incyte Corp Ciklopropilamini kot inhibitorji LSD1
EP3105219B9 (en) 2014-02-13 2018-10-03 Incyte Corporation Cyclopropylamines as lsd1 inhibitors
US9527835B2 (en) 2014-02-13 2016-12-27 Incyte Corporation Cyclopropylamines as LSD1 inhibitors
MX373103B (es) 2014-02-13 2020-04-17 Incyte Holdings Corp Ciclopropilaminas como inhibidores de desmetilasa específica de lisina 1 (lsd1).
JP2017508798A (ja) 2014-03-07 2017-03-30 ザ ジョンズ ホプキンス ユニバーシティ ヒストンリジン特異的デメチラーゼ（ｌｓｄ１）およびヒストンデアセチラーゼ（ｈｄａｃ）の阻害剤
CN103893163B (zh) 2014-03-28 2016-02-03 中国药科大学 2-([1，1′-联苯]-4-基)2-氧代乙基4-((3-氯-4-甲基苯基)氨基)-4-氧代丁酸酯在制备lsd1抑制剂药物中的应用
AR099994A1 (es) 2014-04-11 2016-08-31 Takeda Pharmaceuticals Co Compuesto de ciclopropanamina y sus usos
CN103961340B (zh) 2014-04-30 2019-06-25 南通中国科学院海洋研究所海洋科学与技术研究发展中心 一类lsd1抑制剂及其应用
SI3137169T1 (sl) 2014-05-01 2022-04-29 Celgene Quanticel Research, Inc. Inhibitorji lizin specifične demetilaze-1
US10233165B2 (en) 2014-05-30 2019-03-19 Istituto Europeo Di Oncologia S.R.L. Cyclopropylamine compounds as histone demethylase inhibitors
CN104119280B (zh) 2014-06-27 2016-03-16 郑州大学 含氨基类脲与端炔结构单元的嘧啶衍生物、制备方法及应用
RS60658B1 (sr) 2014-06-27 2020-09-30 Celgene Quanticel Research Inc Inhibitori lizin specifične demetilaze-1
EA201891526A3 (ru) 2014-07-03 2019-05-31 Селджен Квонтисел Рисёрч, Инк. Ингибиторы лизин-специфической деметилазы-1
US10414750B2 (en) 2014-07-03 2019-09-17 Celgene Quanticel Research, Inc. Inhibitors of lysine specific demethylase-1
TWI687419B (zh) 2014-07-10 2020-03-11 美商英塞特公司 作為ｌｓｄ１抑制劑之咪唑并吡啶及咪唑并吡嗪
TW201613925A (en) 2014-07-10 2016-04-16 Incyte Corp Imidazopyrazines as LSD1 inhibitors
WO2016007727A1 (en) 2014-07-10 2016-01-14 Incyte Corporation Triazolopyridines and triazolopyrazines as lsd1 inhibitors
WO2016007722A1 (en) 2014-07-10 2016-01-14 Incyte Corporation Triazolopyridines and triazolopyrazines as lsd1 inhibitors
EA201790376A1 (ru) 2014-09-05 2017-08-31 Селджен Квонтисел Рисёрч, Инк. Ингибиторы лизин-специфической деметилазы-1
EP2993175A1 (en) 2014-09-05 2016-03-09 IEO - Istituto Europeo di Oncologia Srl Thienopyrroles as histone demethylase inhibitors
WO2016123387A1 (en) 2015-01-30 2016-08-04 Genentech, Inc. Therapeutic compounds and uses thereof
PL3256218T3 (pl) 2015-02-12 2025-03-31 Imago Biosciences Inc. Inhibitor kdm1a i jego zastosowanie w terapii
EP3277689B1 (en) 2015-04-03 2019-09-04 Incyte Corporation Heterocyclic compounds as lsd1 inhibitors
CN106045862B (zh) 2015-04-10 2019-04-23 上海迪诺医药科技有限公司 环丙胺类螺(杂)环化合物、其药物组合物及应用
WO2016172496A1 (en) 2015-04-23 2016-10-27 Constellation Pharmaceuticals, Inc. Lsd1 inhibitors and uses thereof
EP3090998A1 (en) 2015-05-06 2016-11-09 F. Hoffmann-La Roche AG Solid forms
WO2017004519A1 (en) 2015-07-02 2017-01-05 University Of Utah Research Foundation Substituted benzohydrazide analogs as histone demethylase inhibitors
LT3334709T (lt) 2015-08-12 2025-03-10 Incyte Holdings Corporation Lsd1 inhibitoriaus druskos
WO2017158136A1 (en) * 2016-03-16 2017-09-21 Oryzon Genomics, S.A. Methods to determine kdm1a target engagement and chemoprobes useful therefor

Patent Citations (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2007524357A (ja) * 2003-01-31 2007-08-30 プロメガ　コーポレイション タンパク質に対する官能基の共有結合的テザリング
JP2013505903A (ja) * 2009-09-25 2013-02-21 オリゾン・ジェノミックス・ソシエダッド・アノニマ リジン特異的デメチラーゼ−１阻害剤およびその使用
JP2013525331A (ja) * 2010-04-19 2013-06-20 オリゾン・ジェノミックス・ソシエダッド・アノニマ リジン特異的脱メチル化酵素１阻害薬およびその使用
JP2013535460A (ja) * 2010-07-29 2013-09-12 オリゾン・ジェノミックス・ソシエダッド・アノニマ Ｌｓｄ１のアリールシクロプロピルアミンをベースとしたデメチラーゼ阻害剤およびそれらの医学的使用
JP2014515013A (ja) * 2011-03-25 2014-06-26 グラクソスミスクライン、インテレクチュアル、プロパティー、ナンバー２、リミテッド Ｌｓｄ１阻害剤としてのシクロプロピルアミン
WO2013022047A1 (ja) * 2011-08-09 2013-02-14 武田薬品工業株式会社 シクロプロパンアミン化合物
JP2014532619A (ja) * 2011-10-20 2014-12-08 オリゾン・ジェノミックス・ソシエダッド・アノニマＯｒｙｚｏｎ Ｇｅｎｏｍｉｃｓ Ｓ．Ａ． 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
JP2015502335A (ja) * 2011-10-20 2015-01-22 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
WO2014058071A1 (ja) * 2012-10-12 2014-04-17 武田薬品工業株式会社 シクロプロパンアミン化合物およびその用途
WO2014151282A1 (en) * 2013-03-15 2014-09-25 Promega Corporation Substrates for covalent tethering of proteins to functional groups or solid surfaces

Non-Patent Citations (4)

* Cited by examiner, † Cited by third party
Title
OURAILIDOU,MARIA E., BIOORGTANIC & MEDICINAL CHEMISTRY, vol. 25, JPN6021007040, 2017, pages 847 - 856, ISSN: 0004457348 *
SANCHEZ,LAURA M., JOURNAL OF NATURAL PRODUCTS, vol. 76, JPN6021007037, 2013, pages 630 - 641, ISSN: 0004457346 *
SZEWCZUK,LAWRENCE M., BIOCHEMISTRY, vol. 46, JPN6021007039, 2007, pages 6892 - 6902, ISSN: 0004457347 *
WANG,RONGSHENG E., BIOORGANIC & MEDICINAL CHEMISTRY, vol. 19, JPN6021007035, 2011, pages 4710 - 4720, ISSN: 0004457345 *

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Publication number Publication date
EP3430015B9 (en) 2025-12-31
ES3042059T3 (en) 2025-11-18
US12195783B2 (en) 2025-01-14
WO2017158136A1 (en) 2017-09-21
US20220389478A1 (en) 2022-12-08
EP3430015A1 (en) 2019-01-23
EP3430015C0 (en) 2025-08-06
US20190085372A1 (en) 2019-03-21
US11034991B2 (en) 2021-06-15
EP3430015B1 (en) 2025-08-06

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