ES3042059T3 - Methods to determine kdm1a target engagement and chemoprobes useful therefor - Google Patents
Methods to determine kdm1a target engagement and chemoprobes useful thereforInfo
- Publication number
- ES3042059T3 ES3042059T3 ES17716799T ES17716799T ES3042059T3 ES 3042059 T3 ES3042059 T3 ES 3042059T3 ES 17716799 T ES17716799 T ES 17716799T ES 17716799 T ES17716799 T ES 17716799T ES 3042059 T3 ES3042059 T3 ES 3042059T3
- Authority
- ES
- Spain
- Prior art keywords
- kdm1a
- trans
- compound
- alkyl
- formula
- 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.)
- Active
Links
Classifications
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Molecular Biology (AREA)
- General Health & Medical Sciences (AREA)
- Biomedical Technology (AREA)
- Hematology (AREA)
- Urology & Nephrology (AREA)
- Medicinal Chemistry (AREA)
- Biotechnology (AREA)
- Microbiology (AREA)
- Physics & Mathematics (AREA)
- Analytical Chemistry (AREA)
- Biochemistry (AREA)
- Wood Science & Technology (AREA)
- Zoology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pathology (AREA)
- Food Science & Technology (AREA)
- Cell Biology (AREA)
- General Physics & Mathematics (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Genetics & Genomics (AREA)
- Biophysics (AREA)
- General Engineering & Computer Science (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Investigating Or Analysing Biological Materials (AREA)
- Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP16382119 | 2016-03-16 | ||
| PCT/EP2017/056330 WO2017158136A1 (en) | 2016-03-16 | 2017-03-16 | Methods to determine kdm1a target engagement and chemoprobes useful therefor |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES3042059T3 true ES3042059T3 (en) | 2025-11-18 |
Family
ID=55794924
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES17716799T Active ES3042059T3 (en) | 2016-03-16 | 2017-03-16 | Methods to determine kdm1a target engagement and chemoprobes useful therefor |
Country Status (5)
| Country | Link |
|---|---|
| US (2) | US11034991B2 (https=) |
| EP (1) | EP3430015B9 (https=) |
| JP (1) | JP2019512546A (https=) |
| ES (1) | ES3042059T3 (https=) |
| WO (1) | WO2017158136A1 (https=) |
Families Citing this family (8)
| 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 |
Family Cites Families (67)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1594962B1 (en) | 2003-01-31 | 2014-08-27 | Promega Corporation | Covalent tethering of functional groups to proteins |
| 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 |
| 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 |
| WO2012013728A1 (en) | 2010-07-29 | 2012-02-02 | Oryzon Genomics S.A. | Arylcyclopropylamine based demethylase inhibitors of lsd1 and their medical use |
| 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 |
| 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 |
| 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 |
| MX356344B (es) * | 2011-10-20 | 2018-05-23 | Oryzon Genomics Sa | Compuestos de (hetero)arilciclopropilamina como inhibidores de lsd1. |
| RU2668952C2 (ru) | 2011-10-20 | 2018-10-05 | Оризон Дженомикс, С.А. | (гетеро)арилциклопропиламины в качестве ингибиторов lsd1 |
| CN105051005B (zh) | 2012-10-12 | 2017-06-13 | 武田药品工业株式会社 | 环丙胺化合物及其用途 |
| 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 |
| JP6604938B2 (ja) | 2013-03-15 | 2019-11-13 | プロメガ コーポレイション | タンパク質を官能基または固体表面に共有結合的に係留するための基質 |
| 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 |
-
2017
- 2017-03-16 WO PCT/EP2017/056330 patent/WO2017158136A1/en not_active Ceased
- 2017-03-16 EP EP17716799.6A patent/EP3430015B9/en active Active
- 2017-03-16 ES ES17716799T patent/ES3042059T3/es active Active
- 2017-03-16 US US16/085,024 patent/US11034991B2/en active Active
- 2017-03-16 JP JP2019500019A patent/JP2019512546A/ja active Pending
-
2021
- 2021-12-16 US US17/644,604 patent/US12195783B2/en active Active
Also Published As
| Publication number | Publication date |
|---|---|
| EP3430015B9 (en) | 2025-12-31 |
| 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 |
| JP2019512546A (ja) | 2019-05-16 |
| US11034991B2 (en) | 2021-06-15 |
| EP3430015B1 (en) | 2025-08-06 |
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