WO2010011296A3 - Deacetylase inhibitors and uses thereof - Google Patents

Deacetylase inhibitors and uses thereof Download PDF

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Publication number
WO2010011296A3
WO2010011296A3 PCT/US2009/004235 US2009004235W WO2010011296A3 WO 2010011296 A3 WO2010011296 A3 WO 2010011296A3 US 2009004235 W US2009004235 W US 2009004235W WO 2010011296 A3 WO2010011296 A3 WO 2010011296A3
Authority
WO
WIPO (PCT)
Prior art keywords
deacetylase inhibitors
inventive compounds
useful
inhibitors
compounds
Prior art date
Application number
PCT/US2009/004235
Other languages
French (fr)
Other versions
WO2010011296A2 (en
Inventor
Weiping Tang
James Elliot Bradner
Stuart L. Schreiber
Original Assignee
President And Fellows Of Harvard College
Dana-Farber Cancer Institute, 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
Priority to KR1020117004046A priority Critical patent/KR101708946B1/en
Application filed by President And Fellows Of Harvard College, Dana-Farber Cancer Institute, Inc. filed Critical President And Fellows Of Harvard College
Priority to AU2009274549A priority patent/AU2009274549B2/en
Priority to CN200980137438.1A priority patent/CN102164888B/en
Priority to EP09800666.1A priority patent/EP2321264B1/en
Priority to CA2731730A priority patent/CA2731730C/en
Priority to US13/055,241 priority patent/US8440716B2/en
Priority to JP2011520034A priority patent/JP5665740B2/en
Priority to RU2011106799/04A priority patent/RU2515611C2/en
Publication of WO2010011296A2 publication Critical patent/WO2010011296A2/en
Publication of WO2010011296A3 publication Critical patent/WO2010011296A3/en
Priority to IL210804A priority patent/IL210804A/en
Priority to HK12101694.3A priority patent/HK1161583A1/en
Priority to US13/861,519 priority patent/US9434686B2/en

Links

Classifications

    • 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
    • C07C259/06—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 hydrogen atoms or to acyclic carbon atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C251/00—Compounds containing nitrogen atoms doubly-bound to a carbon skeleton
    • C07C251/72—Hydrazones
    • C07C251/86—Hydrazones having doubly-bound carbon atoms of hydrazone groups bound to carbon atoms of six-membered aromatic rings

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

The present invention provides novel compounds of formula (I) and pharmaceutical compositions thereof. The inventive compounds are useful as deacetylase inhibitors (e.g., histone deacetylase inhibitors) and may be useful in the treatment of proliferative diseases such as cancer. In particular, the inventive compounds are HDAC6 inhibitors. The invention also provide synthetic methods for preparing the inventive compounds.
PCT/US2009/004235 2008-07-23 2009-07-22 Deacetylase inhibitors and uses thereof WO2010011296A2 (en)

Priority Applications (11)

Application Number Priority Date Filing Date Title
US13/055,241 US8440716B2 (en) 2008-07-23 2009-07-22 Deacetylase inhibitors and uses thereof
AU2009274549A AU2009274549B2 (en) 2008-07-23 2009-07-22 Deacetylase inhibitors and uses thereof
CN200980137438.1A CN102164888B (en) 2008-07-23 2009-07-22 Deacetylase inhibitors and uses thereof
EP09800666.1A EP2321264B1 (en) 2008-07-23 2009-07-22 Deacetylase inhibitors and uses thereof
CA2731730A CA2731730C (en) 2008-07-23 2009-07-22 Deacetylase inhibitors and uses thereof
KR1020117004046A KR101708946B1 (en) 2008-07-23 2009-07-22 Deacetylase inhibitors and uses thereof
JP2011520034A JP5665740B2 (en) 2008-07-23 2009-07-22 Deacetylase inhibitors and uses thereof
RU2011106799/04A RU2515611C2 (en) 2008-07-23 2009-07-22 Deacetylase inhibitors and their application
IL210804A IL210804A (en) 2008-07-23 2011-01-23 Benzylidenehydrazides and uses thereof
HK12101694.3A HK1161583A1 (en) 2008-07-23 2012-02-21 Deacetylase inhibitors and uses thereof
US13/861,519 US9434686B2 (en) 2008-07-23 2013-04-12 Deacetylase inhibitors and uses thereof

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US8289908P 2008-07-23 2008-07-23
US61/082,899 2008-07-23

Related Child Applications (2)

Application Number Title Priority Date Filing Date
US13/055,241 A-371-Of-International US8440716B2 (en) 2008-07-23 2009-07-22 Deacetylase inhibitors and uses thereof
US13/861,519 Continuation US9434686B2 (en) 2008-07-23 2013-04-12 Deacetylase inhibitors and uses thereof

Publications (2)

Publication Number Publication Date
WO2010011296A2 WO2010011296A2 (en) 2010-01-28
WO2010011296A3 true WO2010011296A3 (en) 2010-04-22

Family

ID=41570773

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2009/004235 WO2010011296A2 (en) 2008-07-23 2009-07-22 Deacetylase inhibitors and uses thereof

Country Status (11)

Country Link
US (2) US8440716B2 (en)
EP (1) EP2321264B1 (en)
JP (2) JP5665740B2 (en)
KR (1) KR101708946B1 (en)
CN (1) CN102164888B (en)
AU (1) AU2009274549B2 (en)
CA (1) CA2731730C (en)
HK (1) HK1161583A1 (en)
IL (1) IL210804A (en)
RU (1) RU2515611C2 (en)
WO (1) WO2010011296A2 (en)

Families Citing this family (34)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6777217B1 (en) * 1996-03-26 2004-08-17 President And Fellows Of Harvard College Histone deacetylases, and uses related thereto
US20030129724A1 (en) 2000-03-03 2003-07-10 Grozinger Christina M. Class II human histone deacetylases, and uses related thereto
US7244853B2 (en) * 2001-05-09 2007-07-17 President And Fellows Of Harvard College Dioxanes and uses thereof
CA2937005A1 (en) 2005-03-22 2006-09-28 President And Fellows Of Harvard College Treatment of protein degradation disorders
US8222423B2 (en) * 2006-02-14 2012-07-17 Dana-Farber Cancer Institute, Inc. Bifunctional histone deacetylase inhibitors
CA2654540C (en) * 2006-05-03 2017-01-17 President And Fellows Of Harvard College Histone deacetylase and tubulin deacetylase inhibitors
CA2731730C (en) 2008-07-23 2017-06-13 President And Fellows Of Harvard College Deacetylase inhibitors and uses thereof
WO2011019393A2 (en) 2009-08-11 2011-02-17 President And Fellows Of Harvard College Class- and isoform-specific hdac inhibitors and uses thereof
NZ601655A (en) 2010-01-22 2014-10-31 Acetylon Pharmaceuticals Inc Reverse amide compounds as protein deacetylase inhibitors and methods of use thereof
EA025345B1 (en) 2010-11-16 2016-12-30 Эситайлон Фармасьютикалз, Инк. Pyrimidine hydroxy amide compounds as protein deacetylase inhibitors and pharmaceutical compositions thereof for treating a disease related to hdac6
GB201110546D0 (en) * 2011-06-22 2011-08-03 Imp Innovations Ltd Compositions
WO2014011713A2 (en) * 2012-07-10 2014-01-16 Dana-Farber Cancer Institue, Inc. Anti-proliferative compounds and uses thereof
JP6626437B2 (en) 2013-10-08 2019-12-25 アセチロン ファーマシューティカルズ インコーポレイテッドＡｃｅｔｙｌｏｎ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ，Ｉｎｃ． Combination of histone deacetylase inhibitor and either Her2 inhibitor or PI3K inhibitor
WO2015054474A1 (en) 2013-10-10 2015-04-16 Acetylon Pharmaceuticals, Inc. Pyrimidine hydroxy amide compounds as histone deacetylase inhibitors
EP3060217B1 (en) 2013-10-24 2022-06-08 Mayo Foundation for Medical Education and Research Treatment of polycystic diseases with an hdac6 inhibitor
WO2015084905A1 (en) 2013-12-03 2015-06-11 Acetylon Pharmaceuticals, Inc. Combinations of histone deacetylase inhibitors and immunomodulatory drugs
US9464073B2 (en) 2014-02-26 2016-10-11 Acetylon Pharmaceuticals, Inc. Pyrimidine hydroxy amide compounds as HDAC6 selective inhibitors
JP6952602B2 (en) 2014-07-07 2021-10-20 アセチロン ファーマシューティカルズ インコーポレイテッドＡｃｅｔｙｌｏｎ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ，Ｉｎｃ． Treatment of leukemia with histone deacetylase inhibitors
US9937174B2 (en) 2014-12-05 2018-04-10 University of Modena and Reggio Emilia Combinations of histone deacetylase inhibitors and bendamustine
US10272084B2 (en) 2015-06-01 2019-04-30 Regenacy Pharmaceuticals, Llc Histone deacetylase 6 selective inhibitors for the treatment of cisplatin-induced peripheral neuropathy
ES2769255T3 (en) 2015-06-08 2020-06-25 Acetylon Pharmaceuticals Inc Methods for making protein deacetylase inhibitors
WO2016200919A1 (en) 2015-06-08 2016-12-15 Acetylon Pharmaceuticals, Inc. Crystalline forms of a histone deacetylase inhibitor
EP3328844B1 (en) * 2015-07-27 2019-11-27 Chong Kun Dang Pharmaceutical Corp. 1,3,4-oxadiazole sulfamide derivatives as histone deacetylase 6 inhibitor and pharmaceutical composition comprising the same
MY197262A (en) * 2015-07-27 2023-06-08 Chong Kun Dang Pharmaceutical Corp 1,3,4-oxadiazole sulfonamide derivative compounds as histone deacetylase 6 inhibitor, and the pharmaceutical composition comprising the same
PL3330259T3 (en) 2015-07-27 2021-02-08 Chong Kun Dang Pharmaceutical Corp. 1,3,4-oxadiazole amide derivative compound as histone deacetylase 6 inhibitor, and pharmaceutical composition containing same
MY197738A (en) 2015-08-04 2023-07-12 Chong Kun Dang Pharmaceutical Corp 1,3,4-oxadiazole derivative compounds as histone deacetylase 6 inhibitor, and the pharmaceutical composition comprising the same
NZ740809A (en) 2015-10-12 2019-04-26 Chong Kun Dang Pharmaceutical Corp Oxadiazole amine derivative compounds as histone deacetylase 6 inhibitor, and the pharmaceutical composition comprising the same
JP2019515909A (en) 2016-04-19 2019-06-13 アセチロン ファーマシューティカルズ インコーポレイテッドＡｃｅｔｙｌｏｎ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ，Ｉｎｃ． HDAC inhibitor alone or in combination with a BTK inhibitor for the treatment of chronic lymphocytic leukemia
CA3026763A1 (en) * 2016-06-07 2017-12-14 Dermavant Sciences GmbH Topical formulations of pde-4 inhibitors and their methods of use
US11324744B2 (en) 2016-08-08 2022-05-10 Acetylon Pharmaceuticals Inc. Methods of use and pharmaceutical combinations of histone deacetylase inhibitors and CD20 inhibitory antibodies
KR102316234B1 (en) 2018-07-26 2021-10-22 주식회사 종근당 1,3,4-Oxadiazole Derivative Compounds as Histone Deacetylase 6 Inhibitor, and the Pharmaceutical Composition Comprising the same
KR20240013098A (en) 2021-04-23 2024-01-30 테나야 테라퓨틱스, 인코포레이티드 HDAC6 inhibitors for use in the treatment of dilated cardiomyopathy
TW202308619A (en) 2021-05-04 2023-03-01 美商特納亞治療股份有限公司 Hdac6 inhibitors for treatment of metabolic disease and hfpef
CN115192714A (en) * 2022-07-08 2022-10-18 沈阳药科大学 Application of HDAC6 inhibitor in preparation of medicine for treating DNMT3A gene deletion cancer

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1998047869A1 (en) * 1997-04-22 1998-10-29 Cocensys, Inc. Carbocyclic and heterocyclic substituted semicarbazones and thiosemicarbazones and the use thereof
US20040092598A1 (en) * 2000-09-29 2004-05-13 Watkins Clare J. Carbamic acid compounds comprising an amide linkage as hdac inhibitors
US20060079528A1 (en) * 2003-02-25 2006-04-13 Finn Paul W Carbamic acid compounds comprising a bicyclic heteroaryl group as hdac inhibitors

Family Cites Families (142)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7014A (en) * 1850-01-15 Folding bedstead
US4009A (en) * 1845-04-22 Sawmill-carriage
HU165117B (en) 1971-08-12 1974-06-28
US4160866A (en) 1976-04-30 1979-07-10 Imperial Chemical Industries Limited Carbamates
DE3242252A1 (en) 1982-11-15 1984-05-17 Bayer Ag, 5090 Leverkusen HETEROCYCLICALLY SUBSTITUTED HYDROXYALKYL-AZOLYL DERIVATIVES
NL194579C (en) 1983-01-21 2002-08-05 Schering Ag Diagnostic.
US4631211A (en) 1985-03-25 1986-12-23 Scripps Clinic & Research Foundation Means for sequential solid phase organic synthesis and methods using the same
US4683202A (en) 1985-03-28 1987-07-28 Cetus Corporation Process for amplifying nucleic acid sequences
US4683195A (en) 1986-01-30 1987-07-28 Cetus Corporation Process for amplifying, detecting, and/or-cloning nucleic acid sequences
US4608390A (en) 1985-04-26 1986-08-26 Abbott Laboratories Lipoxygenase inhibiting compounds
US4833080A (en) 1985-12-12 1989-05-23 President And Fellows Of Harvard College Regulation of eucaryotic gene expression
CA1319101C (en) 1986-09-03 1993-06-15 Marta Iris Sabara Rotavirus nucleocapsid protein with or without binding peptides as immunologic carriers for macromolecules
US4861798A (en) 1986-12-29 1989-08-29 Bristol-Myers Company Lipoxygenase inhibitory compounds
US4820828A (en) 1987-03-04 1989-04-11 Ortho Pharmaceutical Corporation Cinnamohydroxamic acids
US5080891A (en) 1987-08-03 1992-01-14 Ddi Pharmaceuticals, Inc. Conjugates of superoxide dismutase coupled to high molecular weight polyalkylene glycols
ES2008962A6 (en) 1987-12-17 1989-08-16 Marga Investigacion New-quanidino-thiazol compounds, their preparation, and use as intermediates of famotidine process.
EP0323590A3 (en) 1987-12-24 1990-05-02 Ono Pharmaceutical Co., Ltd. Carbazoyl derivatives
JPH01224381A (en) 1988-03-04 1989-09-07 Japan Tobacco Inc Trichostatic acid, novel synthetic intermediate for trichostatin a and production of trichostatic acid and trichostatin a
DE58900825D1 (en) 1988-06-13 1992-03-26 Ciba Geigy Ag UNSATURATED BETA KETOESTER ACETALS AND THEIR APPLICATIONS.
US5223409A (en) 1988-09-02 1993-06-29 Protein Engineering Corp. Directed evolution of novel binding proteins
WO1991000257A1 (en) 1989-06-30 1991-01-10 The Trustees Of Columbia University In The City Of New York Novel potent inducers of terminal differentiation and methods of use thereof
US5175191A (en) 1988-11-14 1992-12-29 Sloan-Kettering Institute For Cancer Research Potent inducers of terminal differentiation and methods of use thereof
US5176996A (en) 1988-12-20 1993-01-05 Baylor College Of Medicine Method for making synthetic oligonucleotides which bind specifically to target sites on duplex DNA molecules, by forming a colinear triplex, the synthetic oligonucleotides and methods of use
US5198346A (en) 1989-01-06 1993-03-30 Protein Engineering Corp. Generation and selection of novel DNA-binding proteins and polypeptides
US5096815A (en) 1989-01-06 1992-03-17 Protein Engineering Corporation Generation and selection of novel dna-binding proteins and polypeptides
US5328470A (en) 1989-03-31 1994-07-12 The Regents Of The University Of Michigan Treatment of diseases by site-specific instillation of cells or site-specific transformation of cells and kits therefor
US5256775A (en) 1989-06-05 1993-10-26 Gilead Sciences, Inc. Exonuclease-resistant oligonucleotides
US5143854A (en) 1989-06-07 1992-09-01 Affymax Technologies N.V. Large scale photolithographic solid phase synthesis of polypeptides and receptor binding screening thereof
US5264564A (en) 1989-10-24 1993-11-23 Gilead Sciences Oligonucleotide analogs with novel linkages
JPH05501611A (en) 1989-11-13 1993-03-25 アフィマックス　テクノロジーズ　ナームロゼ　ベノートスハップ Spatially addressable immobilization of antiligands on surfaces
US5304121A (en) 1990-12-28 1994-04-19 Boston Scientific Corporation Drug delivery system making use of a hydrogel polymer coating
FR2659648B1 (en) 1990-03-13 1993-02-12 Michelin Rech Tech PROCESS FOR PREPARING AN ALKYLATED AROMATIC PRODUCT WITH AN ALKYLATION ZEOLITE AND A DEALKYLATION ZEOLITE.
DE69131509T2 (en) 1990-05-09 1999-11-25 Fuji Photo Film Co Ltd Photographic processing composition and processing method using the same
JPH0422948A (en) 1990-05-18 1992-01-27 Fuji Photo Film Co Ltd Photographic processing composition and processing method
US5045538A (en) 1990-06-28 1991-09-03 The Research Foundation Of State University Of New York Inhibition of wasting and protein degradation of mammalian muscle by tetracyclines
GB9026114D0 (en) 1990-11-30 1991-01-16 Norsk Hydro As New compounds
ES2113940T3 (en) 1990-12-03 1998-05-16 Genentech Inc ENRICHMENT METHOD FOR PROTEIN VARIANTS WITH ALTERED UNION PROPERTIES.
EP0562025B1 (en) 1990-12-06 2001-02-07 Affymetrix, Inc. (a Delaware Corporation) Compounds and their use in a binary synthesis strategy
EP0501919A1 (en) 1991-03-01 1992-09-02 Ciba-Geigy Ag Radiation-sensitive compositions based on polyphenols and acetals
WO1992015694A1 (en) 1991-03-08 1992-09-17 The Salk Institute For Biological Studies Flp-mediated gene modification in mammalian cells, and compositions and cells useful therefor
US5225173A (en) 1991-06-12 1993-07-06 Idaho Research Foundation, Inc. Methods and devices for the separation of radioactive rare earth metal isotopes from their alkaline earth metal precursors
EP0603337A1 (en) 1991-09-13 1994-06-29 New England Deaconess Hospital Erythropoietin potentiating agents and methods for their use
US5369108A (en) 1991-10-04 1994-11-29 Sloan-Kettering Institute For Cancer Research Potent inducers of terminal differentiation and methods of use thereof
US5700811A (en) 1991-10-04 1997-12-23 Sloan-Kettering Institute For Cancer Research Potent inducers of terminal differentiation and method of use thereof
US5239113A (en) 1991-10-15 1993-08-24 Monsanto Company Substituted β-amino acid derivatives useful as platelet aggregation inhibitors and intermediates thereof
DE69233331T3 (en) 1991-11-22 2007-08-30 Affymetrix, Inc., Santa Clara Combinatorial Polymersynthesis Strategies
US5534654A (en) 1991-12-10 1996-07-09 Shionogi & Co., Ltd. Aromatic-sulfonamide-type hydroxamic acid derivative
US5359115A (en) 1992-03-26 1994-10-25 Affymax Technologies, N.V. Methods for the synthesis of phosphonate esters
US5573905A (en) 1992-03-30 1996-11-12 The Scripps Research Institute Encoded combinatorial chemical libraries
WO1993019778A1 (en) 1992-04-07 1993-10-14 The Scripps Research Institute Method for inducing tolerance to an antigen using butyrate
JP3356304B2 (en) 1992-06-16 2002-12-16 財団法人生産開発科学研究所 Anti-inflammatory, anti-ulcer agent
US5288514A (en) 1992-09-14 1994-02-22 The Regents Of The University Of California Solid phase and combinatorial synthesis of benzodiazepine compounds on a solid support
DE69333087T2 (en) 1992-10-01 2004-05-06 The Trustees Of Columbia University In The City Of New York COMPLEX COMBINATORY CHEMICAL BANKS WITH MARKINGS
CA2148252C (en) 1992-10-30 2007-06-12 Roger Brent Interaction trap system for isolating novel proteins
US5480971A (en) 1993-06-17 1996-01-02 Houghten Pharmaceuticals, Inc. Peralkylated oligopeptide mixtures
US5440016A (en) 1993-06-18 1995-08-08 Torrey Pines Institute For Molecular Studies Peptides of the formula (KFmoc) ZZZ and their uses
US20030203976A1 (en) 1993-07-19 2003-10-30 William L. Hunter Anti-angiogenic compositions and methods of use
US5994341A (en) 1993-07-19 1999-11-30 Angiogenesis Technologies, Inc. Anti-angiogenic Compositions and methods for the treatment of arthritis
US5362899A (en) 1993-09-09 1994-11-08 Affymax Technologies, N.V. Chiral synthesis of alpha-aminophosponic acids
US5659016A (en) 1994-09-22 1997-08-19 Cancer Institute RPDL protein and DNA encoding the same
US6231600B1 (en) 1995-02-22 2001-05-15 Scimed Life Systems, Inc. Stents with hybrid coating for medical devices
US5837313A (en) 1995-04-19 1998-11-17 Schneider (Usa) Inc Drug release stent coating process
US6099562A (en) 1996-06-13 2000-08-08 Schneider (Usa) Inc. Drug coating with topcoat
JP3330781B2 (en) 1995-05-22 2002-09-30 三菱エンジニアリングプラスチックス株式会社 Polycarbonate resin composition
EP0855024A4 (en) 1995-09-20 2001-08-22 Merck & Co Inc Histone deacetylase as target for antiprotozoal agents
JPH09124918A (en) 1995-10-30 1997-05-13 Mitsubishi Eng Plast Kk Polycarbonate resin composition
US6030945A (en) 1996-01-09 2000-02-29 Genentech, Inc. Apo-2 ligand
US6273912B1 (en) * 1996-02-28 2001-08-14 Impra, Inc. Flanged graft for end-to-side anastomosis
US6777217B1 (en) 1996-03-26 2004-08-17 President And Fellows Of Harvard College Histone deacetylases, and uses related thereto
US6068987A (en) 1996-09-20 2000-05-30 Merck & Co., Inc. Histone deacetylase as target for antiprotozoal agents
WO1998016830A2 (en) 1996-10-16 1998-04-23 The President And Fellows Of Harvard College Droplet assay system
ZA9710342B (en) 1996-11-25 1998-06-10 Alza Corp Directional drug delivery stent and method of use.
US6273913B1 (en) 1997-04-18 2001-08-14 Cordis Corporation Modified stent useful for delivery of drugs along stent strut
AUPO721997A0 (en) 1997-06-06 1997-07-03 Queensland Institute Of Medical Research, The Anticancer compounds
US6190619B1 (en) 1997-06-11 2001-02-20 Argonaut Technologies, Inc. Systems and methods for parallel synthesis of compounds
US5891507A (en) 1997-07-28 1999-04-06 Iowa-India Investments Company Limited Process for coating a surface of a metallic stent
US6195612B1 (en) 1998-01-05 2001-02-27 Tama L. Pack-Harris Pharmacy benefit management system and method of using same
US6503708B1 (en) 1998-01-26 2003-01-07 Incyte Genomics, Inc. Microtubule-associated protein
US6428960B1 (en) 1998-03-04 2002-08-06 Onyx Pharmaceuticals, Inc. Selection method for producing recombinant baculovirus
US6037361A (en) 1998-03-09 2000-03-14 Warner-Lambert Company Fluorinated butyric acids and their derivatives as inhibitors of matrix metalloproteinases
US6153252A (en) 1998-06-30 2000-11-28 Ethicon, Inc. Process for coating stents
US6248127B1 (en) 1998-08-21 2001-06-19 Medtronic Ave, Inc. Thromboresistant coated medical device
DE19846008A1 (en) 1998-10-06 2000-04-13 Bayer Ag Phenylacetic acid heterocyclylamide
TR200101663T2 (en) 1998-12-10 2001-11-21 F.Hoffmann-La Roche Ag Pro-collagen c-proteinase inhibitors
AU3118200A (en) 1998-12-14 2000-07-03 Merck & Co., Inc. Hiv integrase inhibitors
DE69903976T2 (en) 1998-12-16 2003-07-24 Aventis Pharma Ltd HETEROARYL CYCLIC ACETALS
AR035313A1 (en) 1999-01-27 2004-05-12 Wyeth Corp ACETILENIC TACE INHIBITORS OF HYDROXAMIC ACID OF SULFONAMIDE BASED ON ALFA-AMINO ACIDS, PHARMACEUTICAL COMPOSITIONS AND THE USE OF THE SAME FOR THE MANUFACTURE OF MEDICINES.
WO2000046089A1 (en) * 1999-02-01 2000-08-10 Continental Teves Ag & Co. Ohg Pressure control device
US6258121B1 (en) 1999-07-02 2001-07-10 Scimed Life Systems, Inc. Stent coating
US6203551B1 (en) 1999-10-04 2001-03-20 Advanced Cardiovascular Systems, Inc. Chamber for applying therapeutic substances to an implant device
DK1233958T3 (en) 1999-11-23 2011-10-17 Methylgene Inc Inhibitors of histone deacetylase
US6251136B1 (en) 1999-12-08 2001-06-26 Advanced Cardiovascular Systems, Inc. Method of layering a three-coated stent using pharmacological and polymeric agents
US6797820B2 (en) 1999-12-17 2004-09-28 Vicuron Pharmaceuticals Inc. Succinate compounds, compositions and methods of use and preparation
US20030129724A1 (en) 2000-03-03 2003-07-10 Grozinger Christina M. Class II human histone deacetylases, and uses related thereto
PE20020354A1 (en) 2000-09-01 2002-06-12 Novartis Ag HYDROXAMATE COMPOUNDS AS HISTONE-DESACETILASE (HDA) INHIBITORS
GB0023983D0 (en) 2000-09-29 2000-11-15 Prolifix Ltd Therapeutic compounds
US6495719B2 (en) 2001-03-27 2002-12-17 Circagen Pharmaceutical Histone deacetylase inhibitors
AR035455A1 (en) 2001-04-23 2004-05-26 Hoffmann La Roche TRICYCLE DERIVATIVES OF ALQUILHIDROXAMATO, PROCESSES FOR THEIR DEVELOPMENT, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM, AND THE USE OF SUCH COMPOUNDS IN THE PREPARATION OF MEDICINES
US7244853B2 (en) 2001-05-09 2007-07-17 President And Fellows Of Harvard College Dioxanes and uses thereof
US20030187027A1 (en) 2001-05-09 2003-10-02 Schreiber Stuart L. Dioxanes and uses thereof
US6897220B2 (en) 2001-09-14 2005-05-24 Methylgene, Inc. Inhibitors of histone deacetylase
JP2003221398A (en) 2001-11-22 2003-08-05 Japan Science & Technology Corp Method for measuring histone deacetylase activity using fluorescent or chromophoric substrate
US6517889B1 (en) 2001-11-26 2003-02-11 Swaminathan Jayaraman Process for coating a surface of a stent
AU2002362030A1 (en) 2001-11-27 2003-06-10 Fred Hutchinson Cancer Research Center Methods for inhibiting deacetylase activity
US7148257B2 (en) 2002-03-04 2006-12-12 Merck Hdac Research, Llc Methods of treating mesothelioma with suberoylanilide hydroxamic acid
RU2320331C2 (en) 2002-03-04 2008-03-27 МЕРК ЭйчДиЭйСи Рисерч, ЛЛС. Method of induction of terminal differentiation
EP1362914A3 (en) 2002-05-15 2004-05-06 Schering AG Histone deacetylase inhibitor and use thereof
JP2004043446A (en) 2002-05-15 2004-02-12 Schering Ag Histone deacetylase inhibitor and use thereof
WO2003101481A1 (en) 2002-06-03 2003-12-11 Als Therapy Development Foundation Treatment of neurodegenerative diseases using proteasome modulators
TW200401638A (en) 2002-06-20 2004-02-01 Bristol Myers Squibb Co Heterocyclic inhibitors of kinases
TW200420573A (en) 2002-09-26 2004-10-16 Rib X Pharmaceuticals Inc Bifunctional heterocyclic compounds and methods of making and using same
US7282608B2 (en) 2002-10-17 2007-10-16 Methylgene, Inc. Inhibitors of histone deacetylase
JP5354836B2 (en) 2002-11-06 2013-11-27 デイナ ファーバー キャンサー インスティチュート，インコーポレイテッド Methods and compositions for treating cancer using proteasome inhibitors
EP1567142A4 (en) 2002-11-20 2005-12-14 Errant Gene Therapeutics Llc Treatment of lung cells with histone deacetylase inhibitors
CN102267924A (en) 2003-01-08 2011-12-07 诺华疫苗和诊断公司 Antibacterial agents
US7365963B2 (en) * 2003-03-17 2008-04-29 Tdk Corporation Capacitor element, solid electrolytic capacitor, processes for their production and capacitor element combination
PE20050206A1 (en) 2003-05-26 2005-03-26 Schering Ag PHARMACEUTICAL COMPOSITION CONTAINING AN INHIBITOR OF HISTONE DEACETILASE
US7842835B2 (en) 2003-07-07 2010-11-30 Georgetown University Histone deacetylase inhibitors and methods of use thereof
EP1644323B1 (en) 2003-07-07 2015-03-18 Georgetown University Histone deacetylase inhibitors and methods of use thereof
WO2005012247A1 (en) 2003-07-30 2005-02-10 Hôpital Sainte-Justine Compounds and methods for the rapid quantitative analysis of proteins and polypeptides
ATE462426T1 (en) 2003-08-26 2010-04-15 Merck Hdac Res Llc USING SAHA TO TREAT MESOTHELIOMA
DE10346913A1 (en) * 2003-10-09 2005-05-04 Merck Patent Gmbh acylhydrazone
EP1541549A1 (en) 2003-12-12 2005-06-15 Exonhit Therapeutics S.A. Tricyclic hydroxamate and benzaminde derivatives, compositions and methods
US20050137234A1 (en) 2003-12-19 2005-06-23 Syrrx, Inc. Histone deacetylase inhibitors
JP4989976B2 (en) 2004-02-13 2012-08-01 プレジデント アンド フェロウズ オブ ハーバード カレッジ 3-3 Disubstituted oxindoles as translation initiation inhibitors
WO2006060676A1 (en) 2004-12-03 2006-06-08 Dana Farber Cancer Institute Compositions and methods for treating neoplastic diseases
CA2590334A1 (en) 2004-12-03 2006-06-08 Nereus Pharmaceuticals, Inc. Methods of using [3.2.0] heterocyclic compounds and analogs thereof
CA2937005A1 (en) 2005-03-22 2006-09-28 President And Fellows Of Harvard College Treatment of protein degradation disorders
US7438916B2 (en) 2005-10-14 2008-10-21 Virginia Tech Intellectual Properties, Inc. Therapeutic target for protozoal diseases
US8222423B2 (en) 2006-02-14 2012-07-17 Dana-Farber Cancer Institute, Inc. Bifunctional histone deacetylase inhibitors
MX2008010462A (en) 2006-02-14 2009-04-17 Harvard College Histone Deacetylase Inhibitors.
EP2007383A4 (en) 2006-03-22 2010-09-15 Univ California Inhibitors of protein prenyltransferases
CA2654540C (en) 2006-05-03 2017-01-17 President And Fellows Of Harvard College Histone deacetylase and tubulin deacetylase inhibitors
GB0619753D0 (en) 2006-10-06 2006-11-15 Chroma Therapeutics Ltd Enzyme inhibitors
SI2343286T1 (en) 2006-10-28 2015-05-29 Methylgene Inc. Dibenzo(b,f)(1,4)oxazepine derivatives as inhibitors of histone deacetylase
US8088951B2 (en) 2006-11-30 2012-01-03 Massachusetts Institute Of Technology Epigenetic mechanisms re-establish access to long-term memory after neuronal loss
CN101896457A (en) 2007-10-22 2010-11-24 幽兰研究实验室有限公司 Histone deacetylase inhibitors
EP2060565A1 (en) 2007-11-16 2009-05-20 4Sc Ag Novel bifunctional compounds which inhibit protein kinases and histone deacetylases
CA2731730C (en) 2008-07-23 2017-06-13 President And Fellows Of Harvard College Deacetylase inhibitors and uses thereof
CA2733931A1 (en) 2008-08-15 2010-02-18 Burnham Institute For Medical Research Composition and methods for the design and development of metallo-enzyme inhibitors
WO2011019393A2 (en) 2009-08-11 2011-02-17 President And Fellows Of Harvard College Class- and isoform-specific hdac inhibitors and uses thereof
US20130040998A1 (en) 2010-01-08 2013-02-14 Dana-Farber Cancer Institute, Inc. Fluorinated hdac inhibitors and uses thereof

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1998047869A1 (en) * 1997-04-22 1998-10-29 Cocensys, Inc. Carbocyclic and heterocyclic substituted semicarbazones and thiosemicarbazones and the use thereof
US20040092598A1 (en) * 2000-09-29 2004-05-13 Watkins Clare J. Carbamic acid compounds comprising an amide linkage as hdac inhibitors
US20060079528A1 (en) * 2003-02-25 2006-04-13 Finn Paul W Carbamic acid compounds comprising a bicyclic heteroaryl group as hdac inhibitors

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