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WO2000071703A3 - Inhibition d'histone deacetylase - Google Patents

Inhibition d'histone deacetylase Download PDF

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Publication number
WO2000071703A3
WO2000071703A3 PCT/IB2000/001252 IB0001252W WO0071703A3 WO 2000071703 A3 WO2000071703 A3 WO 2000071703A3 IB 0001252 W IB0001252 W IB 0001252W WO 0071703 A3 WO0071703 A3 WO 0071703A3
Authority
WO
WIPO (PCT)
Prior art keywords
histone deacetylase
inhibition
methods
enzymatic activity
relates
Prior art date
Application number
PCT/IB2000/001252
Other languages
English (en)
Other versions
WO2000071703A2 (fr
Inventor
Alan R Macleod
Zuomei Li
Jeffrey M Besterman
Original Assignee
Methylgene Inc
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Methylgene Inc filed Critical Methylgene Inc
Priority to EP00954830A priority Critical patent/EP1173562A2/fr
Priority to JP2000620080A priority patent/JP2003500052A/ja
Priority to AU67182/00A priority patent/AU6718200A/en
Priority to CA002366408A priority patent/CA2366408A1/fr
Priority to KR1020017014048A priority patent/KR20020007398A/ko
Publication of WO2000071703A2 publication Critical patent/WO2000071703A2/fr
Publication of WO2000071703A3 publication Critical patent/WO2000071703A3/fr

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    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N15/00—Mutation or genetic engineering; DNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purification; Use of hosts therefor
    • C12N15/09—Recombinant DNA-technology
    • C12N15/11—DNA or RNA fragments; Modified forms thereof; Non-coding nucleic acids having a biological activity
    • C12N15/52—Genes encoding for enzymes or proenzymes
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N15/00—Mutation or genetic engineering; DNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purification; Use of hosts therefor
    • C12N15/09—Recombinant DNA-technology
    • C12N15/11—DNA or RNA fragments; Modified forms thereof; Non-coding nucleic acids having a biological activity
    • C12N15/113—Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides; Antisense DNA or RNA; Triplex- forming oligonucleotides; Catalytic nucleic acids, e.g. ribozymes; Nucleic acids used in co-suppression or gene silencing
    • C12N15/1137—Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides; Antisense DNA or RNA; Triplex- forming oligonucleotides; Catalytic nucleic acids, e.g. ribozymes; Nucleic acids used in co-suppression or gene silencing against enzymes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N2310/00—Structure or type of the nucleic acid
    • C12N2310/30—Chemical structure
    • C12N2310/31—Chemical structure of the backbone
    • C12N2310/315—Phosphorothioates
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N2310/00—Structure or type of the nucleic acid
    • C12N2310/30—Chemical structure
    • C12N2310/32—Chemical structure of the sugar
    • C12N2310/321—2'-O-R Modification
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N2310/00—Structure or type of the nucleic acid
    • C12N2310/30—Chemical structure
    • C12N2310/34—Spatial arrangement of the modifications
    • C12N2310/345—Spatial arrangement of the modifications having at least two different backbone modifications
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N2310/00—Structure or type of the nucleic acid
    • C12N2310/30—Chemical structure
    • C12N2310/34—Spatial arrangement of the modifications
    • C12N2310/346—Spatial arrangement of the modifications having a combination of backbone and sugar modifications

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Genetics & Genomics (AREA)
  • Engineering & Computer Science (AREA)
  • Biomedical Technology (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Zoology (AREA)
  • Wood Science & Technology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Engineering & Computer Science (AREA)
  • Molecular Biology (AREA)
  • Biotechnology (AREA)
  • General Health & Medical Sciences (AREA)
  • Physics & Mathematics (AREA)
  • Biochemistry (AREA)
  • Microbiology (AREA)
  • Plant Pathology (AREA)
  • Biophysics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Virology (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
  • Investigating Or Analysing Biological Materials (AREA)
  • Enzymes And Modification Thereof (AREA)

Abstract

L'invention concerne l'inhibition de l'expression et de l'activité enzymatique d'histone déacétylase et, en particulier, l'inhibition d'une histone déacétylase spécifique. L'invention concerne également des compositions comprenant des oligonucléotides antisens, ainsi que des procédés d'utilisation de celles-ci pour inhiber une histone déacétylase. Enfin, l'invention concerne également des procédés permettant d'identifier une histone déacétylase intervenant dans l'induction de la prolifération cellulaire, ainsi que des procédés permettant d'identifier des composés qui réagissent mutuellement avec l'activité enzymatique d'une telle histone déacétylase et réduisent cette activité.
PCT/IB2000/001252 1999-05-03 2000-05-03 Inhibition d'histone deacetylase WO2000071703A2 (fr)

Priority Applications (5)

Application Number Priority Date Filing Date Title
EP00954830A EP1173562A2 (fr) 1999-05-03 2000-05-03 Inhibition d'histone deacetylase
JP2000620080A JP2003500052A (ja) 1999-05-03 2000-05-03 ヒストン脱アセチル酵素の抑制
AU67182/00A AU6718200A (en) 1999-05-03 2000-05-03 Inhibition of histone deacetylase
CA002366408A CA2366408A1 (fr) 1999-05-03 2000-05-03 Inhibition d'histone deacetylase
KR1020017014048A KR20020007398A (ko) 1999-05-03 2000-05-03 히스톤 탈아세틸화효소의 억제

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US13228799P 1999-05-03 1999-05-03
US60/132,287 1999-05-03

Publications (2)

Publication Number Publication Date
WO2000071703A2 WO2000071703A2 (fr) 2000-11-30
WO2000071703A3 true WO2000071703A3 (fr) 2001-07-19

Family

ID=22453318

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/IB2000/001252 WO2000071703A2 (fr) 1999-05-03 2000-05-03 Inhibition d'histone deacetylase

Country Status (6)

Country Link
EP (1) EP1173562A2 (fr)
JP (1) JP2003500052A (fr)
KR (1) KR20020007398A (fr)
AU (1) AU6718200A (fr)
CA (1) CA2366408A1 (fr)
WO (1) WO2000071703A2 (fr)

Cited By (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7154002B1 (en) 2002-10-08 2006-12-26 Takeda San Diego, Inc. Histone deacetylase inhibitors
US7169801B2 (en) 2003-03-17 2007-01-30 Takeda San Diego, Inc. Histone deacetylase inhibitors
US7250514B1 (en) 2002-10-21 2007-07-31 Takeda San Diego, Inc. Histone deacetylase inhibitors
US7642253B2 (en) 2005-05-11 2010-01-05 Takeda San Diego, Inc. Histone deacetylase inhibitors
US7642275B2 (en) 2004-12-16 2010-01-05 Takeda San Diego, Inc. Histone deacetylase inhibitors
US7732475B2 (en) 2005-07-14 2010-06-08 Takeda San Diego, Inc. Histone deacetylase inhibitors

Families Citing this family (33)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB0005199D0 (en) * 2000-03-04 2000-04-26 Imp College Innovations Ltd Modulation of histone deacetylase
EP2093292A2 (fr) * 2000-03-24 2009-08-26 Methylgene, Inc. Inhibition spécifique d'isoformes d'histone deacetylase
WO2002036783A2 (fr) * 2000-10-31 2002-05-10 Bayer Aktiengesellschaft Regulation de l'histone deacetylase chez l'homme
WO2002055688A2 (fr) * 2001-01-10 2002-07-18 Us Gov Health & Human Serv Inhibiteurs de l'histone deacetylase dans le diagnostique et le traitement de neoplasmes de la thyroide
CA2434601A1 (fr) * 2001-01-12 2002-09-12 Methylgene, Inc. Procede permettant d'inhiber specifiquement l'histone deacetylase-4
US6897220B2 (en) 2001-09-14 2005-05-24 Methylgene, Inc. Inhibitors of histone deacetylase
US6706686B2 (en) 2001-09-27 2004-03-16 The Regents Of The University Of Colorado Inhibition of histone deacetylase as a treatment for cardiac hypertrophy
WO2003032921A2 (fr) 2001-10-16 2003-04-24 Sloan-Kettering Institute For Cancer Research Traitement des maladies neurodegeneratives et du cancer du cerveau
CA2632078C (fr) 2002-03-04 2012-08-14 Sloan-Kettering Institute For Cancer Research Procedes d'induction de differenciation terminale
US7456219B2 (en) 2002-03-04 2008-11-25 Merck Hdac Research, Llc Polymorphs of suberoylanilide hydroxamic acid
US7148257B2 (en) 2002-03-04 2006-12-12 Merck Hdac Research, Llc Methods of treating mesothelioma with suberoylanilide hydroxamic acid
ATE458047T1 (de) 2002-03-07 2010-03-15 Univ Delaware Verfahren zur verstärkung der oligonucleotid- vermittelten nucleinsäuresequenzänderung unter verwendung von zusammensetzungen mit einem hydroxyharnstoff
FR2837838B1 (fr) * 2002-03-26 2005-01-28 Exonhit Therapeutics Sa Nouvelle cible moleculaire de la neurotoxicite
US20050009030A1 (en) * 2002-03-26 2005-01-13 Fabien Schweighoffer Histone deacetylase: novel molecular target of neurotoxicity
US20040072770A1 (en) * 2002-07-03 2004-04-15 Besterman Jeffrey M. Methods for specifically inhibiting histone deacetylase-7 and 8
EP1400806A1 (fr) * 2002-09-18 2004-03-24 G2M Cancer Drugs AG Criblage pour inhibiteurs de l'histone déacétylase
AU2003288433B2 (en) * 2002-12-05 2009-06-25 Imperial College Innovations Limited Control of apoptosis using a complex of an oligonucleotide and a regulatory peptide
AU2004266169B9 (en) 2003-08-26 2007-05-10 Merck Hdac Research, Llc Method of treating cancer with HDAC inhibitors
WO2005023179A2 (fr) 2003-08-29 2005-03-17 Aton Pharma, Inc. Methodes combinees de traitement du cancer
US20080076138A1 (en) 2005-03-02 2008-03-27 Astellas Pharma Inc. Novel Pd Marker for Histone Deacetylase Inhibitor
TWI365068B (en) 2005-05-20 2012-06-01 Merck Sharp & Dohme Formulations of suberoylanilide hydroxamic acid and methods for producing same
JP5148499B2 (ja) 2005-05-20 2013-02-20 メチルジーン インコーポレイテッド Ｖｅｇｆ受容体およびｈｇｆ受容体シグナル伝達の阻害剤
EP2012801A4 (fr) 2006-04-24 2009-08-05 Gloucester Pharmaceuticals Inc Thérapie de combinaison de gemcitabine
WO2007146730A2 (fr) 2006-06-08 2007-12-21 Gloucester Pharmaceuticals Thérapie à base d'inhibiteurs de désacétylase (dac)
US8030344B2 (en) 2007-03-13 2011-10-04 Methylgene Inc. Inhibitors of histone deacetylase
RU2011119478A (ru) 2008-10-14 2012-11-27 Нин Си Соединения и способы применения
US9133162B2 (en) 2011-02-28 2015-09-15 Sunshine Lake Pharma Co., Ltd. Substituted quinoline compounds and methods of use
JP6342392B2 (ja) 2012-07-28 2018-06-13 カリター・サイエンシーズ・エルエルシー 置換型ピラゾロン化合物及び使用方法
TWI574962B (zh) 2012-11-14 2017-03-21 加拓科學公司 作爲ｐｉ３激酶調節劑的芳雜環化合物及其使用方法和用途
JP6389829B2 (ja) 2013-02-21 2018-09-12 カリター・サイエンシーズ・エルエルシー Ｐｉ３キナーゼモジュレータとしてのヘテロ芳香族化合物、及びその使用方法
WO2015051035A1 (fr) 2013-10-01 2015-04-09 The J. David Gladstone Institutes Compositions, systèmes et procédés pour le criblage de médicament de bruit d'expression génétique et leurs utilisations
US9636298B2 (en) 2014-01-17 2017-05-02 Methylgene Inc. Prodrugs of compounds that enhance antifungal activity and compositions of said prodrugs
EP3365344B1 (fr) 2015-10-19 2020-12-09 Sunshine Lake Pharma Co., Ltd. Sél du acide (3-chloro-4-fluoro-phényl)-(6-((4ar,7as)-3-(héxahydro-(1,4)dioxino(2,3-c)pyrrol-6-yl)-propoxy)-7-méthoxy-quinazolin-4-yl)-amine di(methanesulfonique) et forme crystalline form du monohydrate (un inhibiteur d'egfr)

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1996031600A1 (fr) * 1995-04-03 1996-10-10 Hybridon, Inc. Procede de modulation de l'expression genique sans depletion de complement
WO1997035990A2 (fr) * 1996-03-26 1997-10-02 President And Fellows Of Harvard College Histone-desacetylases et leurs utilisations
WO2000023112A1 (fr) * 1998-10-19 2000-04-27 Methylgene, Inc. Modulation de l'expression genetique par therapie combinee

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1996031600A1 (fr) * 1995-04-03 1996-10-10 Hybridon, Inc. Procede de modulation de l'expression genique sans depletion de complement
WO1997035990A2 (fr) * 1996-03-26 1997-10-02 President And Fellows Of Harvard College Histone-desacetylases et leurs utilisations
WO2000023112A1 (fr) * 1998-10-19 2000-04-27 Methylgene, Inc. Modulation de l'expression genetique par therapie combinee

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
TAUNTON J ET AL: "A MAMMALIAN HISTONE DEACETYLASE RELATED TO THE YEAST TRANSCRIPTIONAL REGULATOR RPD3P", SCIENCE, vol. 272, 19 April 1996 (1996-04-19), pages 408 - 411, XP002038743, ISSN: 0036-8075 *
YOSHIDA M ET AL: "POTENT AND SPECIFIC INHIBITION OF MAMMALIAN HISTONE DEACETYLASE BOTH IN VIVO AND IN VITRO BY TRICHOSTATIN A", JOURNAL OF BIOLOGICAL CHEMISTRY, vol. 265, no. 28, 5 October 1990 (1990-10-05), pages 17174 - 17179, XP000616087, ISSN: 0021-9258 *

Cited By (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7154002B1 (en) 2002-10-08 2006-12-26 Takeda San Diego, Inc. Histone deacetylase inhibitors
US7399884B2 (en) 2002-10-08 2008-07-15 Takeda San Diego, Inc. Histone deacetylase inhibitors
US7250514B1 (en) 2002-10-21 2007-07-31 Takeda San Diego, Inc. Histone deacetylase inhibitors
US7169801B2 (en) 2003-03-17 2007-01-30 Takeda San Diego, Inc. Histone deacetylase inhibitors
US7375228B2 (en) 2003-03-17 2008-05-20 Takeda San Diego, Inc. Histone deacetylase inhibitors
US7381825B2 (en) 2003-03-17 2008-06-03 Takeda San Diego, Inc. Histone deacetylase inhibitors
US7642275B2 (en) 2004-12-16 2010-01-05 Takeda San Diego, Inc. Histone deacetylase inhibitors
US7642253B2 (en) 2005-05-11 2010-01-05 Takeda San Diego, Inc. Histone deacetylase inhibitors
US7732475B2 (en) 2005-07-14 2010-06-08 Takeda San Diego, Inc. Histone deacetylase inhibitors
US7741494B2 (en) 2005-07-14 2010-06-22 Takeda San Diego, Inc. Histone deacetylase inhibitors

Also Published As

Publication number Publication date
JP2003500052A (ja) 2003-01-07
KR20020007398A (ko) 2002-01-26
CA2366408A1 (fr) 2000-11-30
EP1173562A2 (fr) 2002-01-23
AU6718200A (en) 2000-12-12
WO2000071703A2 (fr) 2000-11-30

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