PE20040913A1 - Enantiomeros (r) y (s) de derivados del acido tiofeno hidroxamico como inhibidores de desacetilasa histona (hdac) - Google Patents

Enantiomeros (r) y (s) de derivados del acido tiofeno hidroxamico como inhibidores de desacetilasa histona (hdac)

Info

Publication number
PE20040913A1
PE20040913A1 PE2003001262A PE2003001262A PE20040913A1 PE 20040913 A1 PE20040913 A1 PE 20040913A1 PE 2003001262 A PE2003001262 A PE 2003001262A PE 2003001262 A PE2003001262 A PE 2003001262A PE 20040913 A1 PE20040913 A1 PE 20040913A1
Authority
PE
Peru
Prior art keywords
thiophene
hydroxamic
inhibitors
desacetilase
hdac
Prior art date
Application number
PE2003001262A
Other languages
English (en)
Inventor
Klaus-Peter Kunkele
Anja Limberg
Adelbert Grossmann
Frank Herting
Ulrich Tibes
Matthias Koerner
Olaf Mundigl
Original Assignee
Hoffmann La Roche
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 Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of PE20040913A1 publication Critical patent/PE20040913A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/26—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur 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
    • C07D333/38—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links

Landscapes

  • 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)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Compounds Containing Sulfur Atoms (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

SE REFIERE A LOS ENANTIOMEROS (R) Y (S) DE DERIVADOS DEL ACIDO TIOFENO HIDROXAMICO DE FORMULA I, INCLUYENDO SUS SALES FISIOLOGICAMENTE ACEPTABLES, EN DONDE Ar ES UN GRUPO ARILO O HETEROARILO QUE PUEDE ESTAR SUSTITUIDO HASTA 3 VECES O NO POR HALOGENO, FENILO, ALQUILO, ENTRE OTROS; R1 ES H, FENILO, ALQUILO O ALQUENILO QUE PUEDEN ESTAR SUSTITUIDO UNA O VARIAS VECES O NO SUSTITUIDO POR HALOGENO, OH, NO2, NH2, ENTRE OTROS; O R1 Y Ar FORMAN UN ANILLO DE TETRAHIDRONAFTALENO, INDANO o DIBENZOSUBERANO; R2 ES H o ALQUILO; n ES 1, 2 o 3. SON COMPUESTOS PREFERIDOS: 2-HIDROXIAMIDA 5-[(1-TIOFENO-2-IL-ETIL)-AMIDA] DEL ACIDO (R)-TIOFENO-2,5-DICARBOXILICO; 2-HIDROXIAMIDA 5-[(1-TIOFENO-2-IL-ETIL)-AMIDA] DEL ACIDO (S)-TIOFENO-2,5-DICARBOXILICO; 2-HIDROXIAMIDA 5-{[1-(5-METIL-TIOFENO-2-IL)-ETIL]-AMIDA} DEL ACIDO (R)-TIOFENO-2,5-DICARBOXILICO; ENTRE OTROS. TAMBIEN SE REFIERE A UN PROCEDIMIENTO PARA LA ELABORACION ESTEREOSELECTIVA DE ESTOS COMPUESTOS Y UN MEDICAMENTO QUE LOS CONTIENE. ESTOS COMPUESTOS SON INHIBIDORES DE LA DESACETILASA HISTONA (HDAC) SON UTILES COMO INHIBIDORES DE LA PROLIFERACION DE CELULAS TUMORALES
PE2003001262A 2002-12-16 2003-12-11 Enantiomeros (r) y (s) de derivados del acido tiofeno hidroxamico como inhibidores de desacetilasa histona (hdac) PE20040913A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP02028038 2002-12-16

Publications (1)

Publication Number Publication Date
PE20040913A1 true PE20040913A1 (es) 2005-01-18

Family

ID=32524005

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2003001262A PE20040913A1 (es) 2002-12-16 2003-12-11 Enantiomeros (r) y (s) de derivados del acido tiofeno hidroxamico como inhibidores de desacetilasa histona (hdac)

Country Status (18)

Country Link
US (1) US7098241B2 (es)
EP (1) EP1575933A1 (es)
JP (1) JP2006513181A (es)
KR (1) KR100781929B1 (es)
CN (1) CN100391954C (es)
AR (1) AR042459A1 (es)
AU (1) AU2003293882A1 (es)
BR (1) BR0317348A (es)
CA (1) CA2507629A1 (es)
CL (1) CL2003002611A1 (es)
GT (1) GT200300285A (es)
PA (1) PA8592101A1 (es)
PE (1) PE20040913A1 (es)
PL (1) PL377696A1 (es)
RU (1) RU2348625C2 (es)
TW (1) TW200418825A (es)
UY (1) UY28127A1 (es)
WO (1) WO2004054999A1 (es)

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US7435837B2 (en) * 2003-10-24 2008-10-14 Wyeth Dihydrobenzofuranyl alkanamine derivatives and methods for using same
US20050261347A1 (en) * 2003-10-24 2005-11-24 Wyeth Dihydrobenzofuranyl alkanamine derivatives and methods for using same
US7638553B2 (en) * 2004-06-14 2009-12-29 Hoffmann-La Roche Inc. Hydroxamates, their manufacture and use as pharmaceutical agents
JP2008502626A (ja) * 2004-06-14 2008-01-31 エフ．ホフマン−ラ　ロシュ　アーゲー チオフェン誘導体、それらの製造及び医薬物質としての使用
CA2566515A1 (en) * 2004-06-14 2005-12-22 F. Hoffmann-La Roche Ag Thiophene hydroxamic acid derivatives and their use as hdac inhibitors
CA2607359C (en) * 2005-05-13 2011-08-09 Virochem Pharma Inc. Compounds and methods for the treatment or prevention of flavivirus infections
BRPI0613429A2 (pt) 2005-07-14 2009-02-10 Takeda San Diego Inc inibidores de histona desacetilase
GB0518237D0 (en) * 2005-09-07 2005-10-19 Angeletti P Ist Richerche Bio Therapeutic compounds
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WO2011106627A1 (en) * 2010-02-26 2011-09-01 Millennium Pharmaceuticals, Inc. Substituted hydroxamic acids and uses thereof
WO2011106632A1 (en) * 2010-02-26 2011-09-01 Millennium Pharmaceuticals, Inc. Substituted hydroxamic acids and uses thereof
WO2012019772A1 (en) * 2010-08-12 2012-02-16 Institut De Recherche Pour Le Developpement (I.R.D) Method for treating protozoan parasitic diseases
WO2012112447A2 (en) * 2011-02-14 2012-08-23 Dana-Farber Cancer Institute, Inc. Histone deacetylase inhibitors and methods of use thereof
US9499479B2 (en) 2011-10-03 2016-11-22 The Trustees Of Columbia University In The City Of New York Molecules that selectively inhibit histone deacetylase 6 relative to histone deacetylase 1
RS57188B1 (sr) 2013-03-15 2018-07-31 Japan Tobacco Inc Jedinjenje pirazol-amida i njegove medicinske upotrebe
CN103159646B (zh) * 2013-03-19 2014-10-22 广东药学院 一种异羟肟酸类化合物及其制备方法和应用
US9890136B2 (en) 2013-12-23 2018-02-13 The Trustees Of Columbia University In The City Of New York Memorial Sloan-Kettering Cancer Center Selective HDAC6 inhibitors
TWI773657B (zh) 2015-12-18 2022-08-11 美商亞德利克斯公司 作爲非全身ｔｇｒ５促效劑之經取代之4-苯基吡啶化合物
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Also Published As

Publication number Publication date
RU2348625C2 (ru) 2009-03-10
WO2004054999A1 (en) 2004-07-01
CN100391954C (zh) 2008-06-04
PL377696A1 (pl) 2006-02-06
US7098241B2 (en) 2006-08-29
PA8592101A1 (es) 2004-11-02
RU2005122447A (ru) 2006-05-27
BR0317348A (pt) 2005-11-16
AR042459A1 (es) 2005-06-22
AU2003293882A1 (en) 2004-07-09
CA2507629A1 (en) 2004-07-01
US20040122079A1 (en) 2004-06-24
KR100781929B1 (ko) 2007-12-04
KR20050089157A (ko) 2005-09-07
CN1726204A (zh) 2006-01-25
CL2003002611A1 (es) 2005-01-14
UY28127A1 (es) 2004-06-30
EP1575933A1 (en) 2005-09-21
JP2006513181A (ja) 2006-04-20
GT200300285A (es) 2004-07-14
TW200418825A (en) 2004-10-01

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