WO2010043866A3 - Inhibiteurs d’histone lysine déméthylase - Google Patents

Inhibiteurs d’histone lysine déméthylase Download PDF

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Publication number
WO2010043866A3
WO2010043866A3 PCT/GB2009/002465 GB2009002465W WO2010043866A3 WO 2010043866 A3 WO2010043866 A3 WO 2010043866A3 GB 2009002465 W GB2009002465 W GB 2009002465W WO 2010043866 A3 WO2010043866 A3 WO 2010043866A3
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WO
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Prior art keywords
inhibitors
derivative
formula
histone lysine
activation
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PCT/GB2009/002465
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English (en)
Other versions
WO2010043866A2 (fr
Inventor
Christopher Joseph Schofield
Michael Mcdonough
Nathan Rose
Armin Thalhammer
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Isis Innovation Limited
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Publication date
Application filed by Isis Innovation Limited filed Critical Isis Innovation Limited
Publication of WO2010043866A2 publication Critical patent/WO2010043866A2/fr
Publication of WO2010043866A3 publication Critical patent/WO2010043866A3/fr

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/79—Acids; Esters
    • 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
    • A61P25/24—Antidepressants
    • 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
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00—Carboxylic acid amides
    • C07C233/01—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C233/56—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having carbon atoms of carboxamide groups bound to carbon atoms of carboxyl groups, e.g. oxamides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C255/00—Carboxylic acid nitriles
    • C07C255/49—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C255/57—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and carboxyl groups, other than cyano groups, bound to the carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C259/00—Compounds containing carboxyl groups, an oxygen atom of a carboxyl group being replaced by a nitrogen atom, this nitrogen atom being further bound to an oxygen atom and not being part of nitro or nitroso groups
    • C07C259/04—Compounds containing carboxyl groups, an oxygen atom of a carboxyl group being replaced by a nitrogen atom, this nitrogen atom being further bound to an oxygen atom and not being part of nitro or nitroso groups without replacement of the other oxygen atom of the carboxyl group, e.g. hydroxamic acids
    • C07C259/10—Compounds containing carboxyl groups, an oxygen atom of a carboxyl group being replaced by a nitrogen atom, this nitrogen atom being further bound to an oxygen atom and not being part of nitro or nitroso groups without replacement of the other oxygen atom of the carboxyl group, e.g. hydroxamic acids having carbon atoms of hydroxamic groups bound to carbon atoms of six-membered aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/34—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D307/56—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D307/68—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/12—Systems containing only non-condensed rings with a six-membered ring
    • C07C2601/14—The ring being saturated

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)

Abstract

Cette invention concerne un composé qui est un dérivé de iV-oxalylglycine de formule (I) : un dérivé d’acide hydroxamique de formule (II) : ou un dérivé hétéroaryle de formule (III) : n, Z1, Z2, Y1, Y2, A, p, X1, X2, m, R4, B, R5, R6, R7, R8, R9, X3, R10, R11 et R12 étant tels que définis dans la description, ou un de leurs sels pharmaceutiquement acceptables. Ces composés sont des inhibiteurs de la sous-famille des JMJD2 humains à 2-oxoglutarate des histone déméthylases, en particulier les JMJD2E. Ces inhibiteurs sont utilisés pour changer l’état épigénétique des cellules entraînant l’inhibition/l’activation de la recomposition de la chromatine, l’activation/la désactivation de multiples gènes, et dans le traitement du cancer et d’autres maladies caractérisées par une prolifération cellulaire indésirable et des troubles psychiatriques y compris la dépression.
PCT/GB2009/002465 2008-10-15 2009-10-15 Inhibiteurs d’histone lysine déméthylase WO2010043866A2 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GBGB0818907.8A GB0818907D0 (en) 2008-10-15 2008-10-15 Histone lysine demethylase inhibitors
GB0818907.8 2008-10-15

Publications (2)

Publication Number Publication Date
WO2010043866A2 WO2010043866A2 (fr) 2010-04-22
WO2010043866A3 true WO2010043866A3 (fr) 2010-10-07

Family

ID=40084077

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/GB2009/002465 WO2010043866A2 (fr) 2008-10-15 2009-10-15 Inhibiteurs d’histone lysine déméthylase

Country Status (2)

Country Link
GB (1) GB0818907D0 (fr)
WO (1) WO2010043866A2 (fr)

Families Citing this family (24)

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MX2011004570A (es) * 2008-10-31 2011-06-17 Merck Sharp & Dohme Antagonistas del receptor p2x3 para el tratamiento del dolor.
GB0918862D0 (en) * 2009-10-27 2009-12-09 Glaxo Group Ltd Method of treatment
WO2012007008A1 (fr) * 2010-07-15 2012-01-19 Epitherapeutics Aps Inhibiteurs de hdme
EP2595613B1 (fr) * 2010-07-22 2019-01-09 The U.S.A. as represented by the Secretary, Department of Health and Human Services Composés destinés à être utilisés dans une méthode destinée à prévenir ou à traiter une infection virale
GB201112607D0 (en) * 2011-07-22 2011-09-07 Glaxo Group Ltd Novel compounds
TWI429637B (zh) * 2011-04-01 2014-03-11 Nat Univ Tsing Hua 衍生自４，４’－二酸－２，２’－雙吡啶之三牙配位子、金屬錯合物及其應用
WO2012150042A1 (fr) 2011-05-04 2012-11-08 Cellzome Ag Composés et procédés pour identifier des molécules ayant une interaction avec les histones déméthylases et pour purifier des protéines d'histone déméthylase
EP2592154A1 (fr) 2011-11-09 2013-05-15 Cellzome Ag Produits d'immobilisation et procédés d'identification de molécules d'interaction de déméthylase d'histone et de purification des protéines de déméthylase d'histone
WO2013143597A1 (fr) 2012-03-29 2013-10-03 Glaxo Group Limited Inhibiteurs d'enzymes de déméthylase
WO2014089364A1 (fr) 2012-12-06 2014-06-12 Quanticel Pharmaceuticals, Inc Inhibiteurs de l'histone déméthylase
AU2014236711A1 (en) * 2013-03-14 2015-09-17 Celgene Quanticel Research, Inc. Histone demethylase inhibitors
CN109574865A (zh) * 2013-08-30 2019-04-05 英属哥伦比亚大学 单胺氧化酶-b选择性抑制剂化合物、其药物组合物及应用
CN105566145A (zh) * 2014-11-03 2016-05-11 广州德汇行医药科技有限公司 氨基酸衍生物及其应用
JP6980534B2 (ja) 2015-06-25 2021-12-15 ザ チルドレンズ メディカル センター コーポレーション 造血幹細胞の増大、富化、および維持に関する方法および組成物
AU2017235461B2 (en) 2016-03-15 2023-02-23 Children's Medical Center Corporation Methods and compositions relating to hematopoietic stem cell expansion
WO2017207813A1 (fr) 2016-06-03 2017-12-07 Oryzon Genomics, S.A. Acides hétéroaryl-carboxyliques utilisés en tant qu'inhibiteurs de l'histone déméthylase
AU2018219213A1 (en) * 2017-02-10 2019-09-26 Temple Otorongo Llc Treatment of diabetes and associated metabolic conditions with epigenetic modulators
WO2018149986A1 (fr) * 2017-02-16 2018-08-23 Oryzon Genomics, S.A. Dérivés de 2-(bicyclo-hétéroaryl)-isonicotinique en tant qu'inhibiteurs d'histone déméthylase
WO2018219478A1 (fr) 2017-06-02 2018-12-06 Oryzon Genomics, S.A. Hétéroaryl-carboxamides comme inhibiteurs de l'histone déméthylase
CN107540574B (zh) * 2017-09-19 2021-06-11 成都西岭源药业有限公司 R-联苯丙氨醇的制备方法
US20210254006A1 (en) 2018-06-06 2021-08-19 Ideaya Biosciences, Inc. Methods of culturing and/or expanding stem cells and/or lineage committed progenitor cells using lactam compounds
CN109456262A (zh) * 2018-12-22 2019-03-12 山东大学 基于抑制组蛋白去甲基化酶化合物及其制备方法与抗胃癌应用
CN109438339A (zh) * 2018-12-22 2019-03-08 山东大学 Rbp2酶抑制剂小分子化合物wxsa-072a及其制备方法与抗胃癌应用
CN114409557B (zh) * 2022-01-19 2022-08-30 中南民族大学 一种具有神经保护活性的炭角酸及其制备方法和应用

Citations (14)

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Publication number Priority date Publication date Assignee Title
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WO1988008422A1 (fr) * 1987-04-22 1988-11-03 Schering Aktiengesellschaft Complexants cyliques substitues, complexes et sels de complexes, leur procede de production et substances pharmaceutiques les contenant
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US20070208082A1 (en) * 2005-08-10 2007-09-06 John Hopkins University Polyamines useful as anti-parasitic and anti-cancer therapeutics and as lysine-specific demethylase inhibitors
WO2009113320A1 (fr) * 2008-03-13 2009-09-17 株式会社ヤクルト本社 Inhibiteur de mmp

Patent Citations (14)

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EP0848957A1 (fr) * 1995-09-08 1998-06-24 Kanebo Ltd. INHIBITEUR DE SOLUBILISATION DE LIGAND Fas
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WO2009113320A1 (fr) * 2008-03-13 2009-09-17 株式会社ヤクルト本社 Inhibiteur de mmp

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TUSSETSCHLAEGER STEFAN ET AL: "Synthesis of 5-methoxy-4-benzyloxazoles from tyrosine and m-tyrosine under Bischler-Napieralski conditions", ZEITSCHRIFT FUR NATURFORSCHUNG, TEIL B:ANORGANISCHE CHEMIE, ORGANISCHE CHEMIE, VERLAG DER ZEITSCHRIFT FUR NATURFORSCHUNG. TUBINGEN, DE, vol. 61, no. 4, 1 January 2006 (2006-01-01), pages 420 - 426, XP009087383, ISSN: 0932-0776 *
YAMAMOTO M ET AL: "INHIBITION OF MEMBRANE-TYPE 1 MATRIX METALLOPROTEINASE BY HYDROXAMATE INHIBITORS: AN EXAMINATION OF THE SUBSITE POCKET", JOURNAL OF MEDICINAL CHEMISTRY, AMERICAN CHEMICAL SOCIETY, WASHINGTON, US, vol. 41, no. 8, 1 January 1998 (1998-01-01), pages 1209 - 1217, XP000867897, ISSN: 0022-2623 *
YAMAMOTO M ET AL: "Structure-activity relationship of hydroxamate-based inhibitors on membrane-bound Fas ligand and TNF-.alpha. processing", DRUG DESIGN AND DISCOVERY, HARWOOD ACADEMIC PUBLISHERS GMBH, XX, vol. 16, 1 January 1999 (1999-01-01), pages 119 - 130, XP009130971, ISSN: 1055-9612 *

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WO2010043866A2 (fr) 2010-04-22

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