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)
- Microbiology (AREA)
- Biochemistry (AREA)
- Biotechnology (AREA)
- Physics & Mathematics (AREA)
- Analytical Chemistry (AREA)
- Wood Science & Technology (AREA)
- Zoology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Food Science & Technology (AREA)
- General Physics & Mathematics (AREA)
- Pathology (AREA)
- Cell Biology (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Engineering & Computer Science (AREA)
- Biophysics (AREA)
- Genetics & Genomics (AREA)
- Neurology (AREA)
- Neurosurgery (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 (enExample) |
| EP (1) | EP3430015B9 (enExample) |
| JP (1) | JP2019512546A (enExample) |
| ES (1) | ES3042059T3 (enExample) |
| WO (1) | WO2017158136A1 (enExample) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BR112014009306B1 (pt) | 2011-10-20 | 2021-07-20 | Oryzon Genomics S.A. | Compostos de (hetero)aril ciclopropilamina como inibidores de lsd1 |
| EP3090998A1 (en) | 2015-05-06 | 2016-11-09 | F. Hoffmann-La Roche AG | Solid forms |
| EP3307267B1 (en) | 2016-06-10 | 2019-04-10 | Oryzon Genomics, S.A. | Multiple sclerosis treatment |
| SG10201913331VA (en) | 2016-03-15 | 2020-03-30 | Oryzon Genomics Sa | Combinations of lsd1 inhibitors for use in the treatment of solid tumors |
| AU2017233886B2 (en) | 2016-03-15 | 2022-10-20 | Oryzon Genomics, S.A. | Combinations of LSD1 inhibitors for the treatment of hematological malignancies |
| ES3042059T3 (en) * | 2016-03-16 | 2025-11-18 | Oryzon Genomics Sa | Methods to determine kdm1a target engagement and chemoprobes useful therefor |
| 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 |
|---|---|---|---|---|
| AU2004211584B2 (en) * | 2003-01-31 | 2009-11-12 | Promega Corporation | Covalent tethering of functional groups to proteins |
| BRPI0614805A2 (pt) | 2005-08-10 | 2011-04-12 | Univ Johns Hopkins | poliaminas úteis como produtos terapêuticos antiparasìticos e anticáncer e como inibidores de demetilase lisina-especìficos |
| WO2008054827A2 (en) * | 2006-11-03 | 2008-05-08 | 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 |
| WO2010143582A1 (ja) | 2009-06-11 | 2010-12-16 | 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 |
| WO2011022489A2 (en) | 2009-08-18 | 2011-02-24 | The Johns Hopkins University | (bis) urea and (bis) thiourea compounds as epigenic modulators of lysine-specific demethylase 1 and methods of treating disorders |
| CA2812683C (en) * | 2009-09-25 | 2017-10-10 | Oryzon Genomics S.A. | Lysine specific demethylase-1 inhibitors and their use |
| US8946296B2 (en) | 2009-10-09 | 2015-02-03 | Oryzon Genomics S.A. | Substituted heteroaryl- and aryl-cyclopropylamine acetamides and their use |
| HUE030938T2 (en) | 2010-04-19 | 2017-06-28 | Oryzon Genomics Sa | Lysine-specific demethylase-1 inhibitors and their use |
| JP5934184B2 (ja) | 2010-04-20 | 2016-06-15 | ウニヴェルシタ・デグリ・ストゥディ・ディ・ローマ・ラ・サピエンツァ | ヒストンデメチラーゼlsd1及び/又はlsd2の阻害剤としてのトラニルシプロミン誘導体 |
| MX341732B (es) | 2010-07-29 | 2016-08-30 | Oryzon Genomics S A * | Inhibidores de la 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 |
| 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 |
| SG193241A1 (en) * | 2011-03-25 | 2013-10-30 | Glaxosmithkline Ip No 2 Ltd | Cyclopropylamines as lsd1 inhibitors |
| CN103842332B (zh) | 2011-08-09 | 2016-08-17 | 武田药品工业株式会社 | 环丙胺化合物 |
| 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 |
| WO2013033688A1 (en) | 2011-09-01 | 2013-03-07 | The Brigham And Women's Hospital, Inc. | Treatment of cancer |
| WO2013057322A1 (en) | 2011-10-20 | 2013-04-25 | Oryzon Genomics, S.A. | (hetero)aryl cyclopropylamine compounds as lsd1 inhibitors |
| BR112014009306B1 (pt) * | 2011-10-20 | 2021-07-20 | Oryzon Genomics S.A. | Compostos de (hetero)aril ciclopropilamina como inibidores de lsd1 |
| 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 |
| 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 |
| US9144555B2 (en) | 2012-11-30 | 2015-09-29 | Darlene E. McCord | 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 |
| WO2014151282A1 (en) * | 2013-03-15 | 2014-09-25 | Promega Corporation | Substrates for covalent tethering of proteins to functional groups or solid surfaces |
| JP6525162B2 (ja) | 2013-06-19 | 2019-06-05 | 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(e)−n’−(1−フェニルエチリデン)ベンゾヒドラジド類似体 |
| 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 |
| MX383590B (es) | 2013-08-06 | 2025-03-11 | 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 |
| WO2015031564A2 (en) | 2013-08-30 | 2015-03-05 | University Of Utah | Substituted-1h-benzo[d]imidazole series compounds as lysine-specfic demethylase 1 (lsd1) inhibitors |
| SI3080100T1 (sl) | 2013-12-11 | 2023-04-28 | Celgene Quanticel Research, Inc. | Inhibitorji lizin specifične demetilaze-1 |
| EP3102034A4 (en) | 2014-02-07 | 2017-07-12 | MUSC Foundation For Research Development | Aminotriazole- and aminotetrazole-based kdm1a inhibitors as epigenetic modulators |
| TWI720451B (zh) | 2014-02-13 | 2021-03-01 | 美商英塞特控股公司 | 作為lsd1抑制劑之環丙胺 |
| US9493442B2 (en) | 2014-02-13 | 2016-11-15 | Incyte Corporation | Cyclopropylamines as LSD1 inhibitors |
| US9527835B2 (en) | 2014-02-13 | 2016-12-27 | Incyte Corporation | Cyclopropylamines as LSD1 inhibitors |
| KR102421235B1 (ko) | 2014-02-13 | 2022-07-15 | 인사이트 코포레이션 | Lsd1 저해제로서 사이클로프로필아민 |
| EP3114109A4 (en) | 2014-03-07 | 2017-10-18 | The Johns Hopkins University | Inhibitors of histone lysine specific demethylase (lsd1) and histone deacetylases (hdacs) |
| 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 |
| CN106459024B (zh) | 2014-04-11 | 2019-11-05 | 武田药品工业株式会社 | 环丙胺化合物及其用途 |
| 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 |
| WO2015168466A1 (en) | 2014-05-01 | 2015-11-05 | Quanticel Pharmaceuticals, Inc. | Inhibitors of lysine specific demethylase-1 |
| JP6320570B2 (ja) | 2014-05-30 | 2018-05-09 | イエオ−イスティトゥート・エウロペオ・ディ・オンコロジア・エッセ・エッレ・エッレ | ヒストンデメチラーゼ阻害剤としてのシクロプロピルアミン化合物 |
| 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 |
| SG11201610975RA (en) | 2014-07-03 | 2017-01-27 | Celgene Quanticel Res Inc | Inhibitors of lysine specific demethylase-1 |
| MX391865B (es) | 2014-07-03 | 2025-03-21 | Celgene Quanticel Res Inc | Inhibidores de demetilasa-1 especifica de lisina. |
| 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 |
| US9758523B2 (en) | 2014-07-10 | 2017-09-12 | Incyte Corporation | Triazolopyridines and triazolopyrazines as LSD1 inhibitors |
| TW201613925A (en) | 2014-07-10 | 2016-04-16 | Incyte Corp | Imidazopyrazines as LSD1 inhibitors |
| WO2016007722A1 (en) | 2014-07-10 | 2016-01-14 | Incyte Corporation | Triazolopyridines and triazolopyrazines as lsd1 inhibitors |
| JP6692350B2 (ja) | 2014-09-05 | 2020-05-13 | セルジーン クオンティセル リサーチ,インク. | リジン特異的なデメチラーゼ−1の阻害剤 |
| EP2993175A1 (en) | 2014-09-05 | 2016-03-09 | IEO - Istituto Europeo di Oncologia Srl | Thienopyrroles as histone demethylase inhibitors |
| JP6636031B2 (ja) | 2015-01-30 | 2020-01-29 | ジェネンテック, インコーポレイテッド | 治療用化合物およびその使用 |
| RS66458B1 (sr) | 2015-02-12 | 2025-02-28 | Imago Biosciences Inc | Kdm1a inhibitor i njegova primena u terapiji |
| SG11201708047UA (en) | 2015-04-03 | 2017-10-30 | Incyte Corp | 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 |
| US10526287B2 (en) | 2015-04-23 | 2020-01-07 | 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 |
| CN110402244B (zh) | 2015-08-12 | 2023-02-03 | 因赛特公司 | Lsd1抑制剂的盐 |
| ES3042059T3 (en) * | 2016-03-16 | 2025-11-18 | Oryzon Genomics Sa | Methods to determine kdm1a target engagement and chemoprobes useful therefor |
-
2017
- 2017-03-16 ES ES17716799T patent/ES3042059T3/es active Active
- 2017-03-16 EP EP17716799.6A patent/EP3430015B9/en active Active
- 2017-03-16 JP JP2019500019A patent/JP2019512546A/ja active Pending
- 2017-03-16 WO PCT/EP2017/056330 patent/WO2017158136A1/en not_active Ceased
- 2017-03-16 US US16/085,024 patent/US11034991B2/en active Active
-
2021
- 2021-12-16 US US17/644,604 patent/US12195783B2/en active Active
Also Published As
| Publication number | Publication date |
|---|---|
| WO2017158136A1 (en) | 2017-09-21 |
| US20220389478A1 (en) | 2022-12-08 |
| EP3430015C0 (en) | 2025-08-06 |
| US11034991B2 (en) | 2021-06-15 |
| EP3430015A1 (en) | 2019-01-23 |
| JP2019512546A (ja) | 2019-05-16 |
| US12195783B2 (en) | 2025-01-14 |
| EP3430015B1 (en) | 2025-08-06 |
| EP3430015B9 (en) | 2025-12-31 |
| US20190085372A1 (en) | 2019-03-21 |
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