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PE20040768A1 - Derivados de arilen-(2-amino-fenil)-carboxamida como inhibidores de la histona desacetilasa (hdac) - Google Patents

Derivados de arilen-(2-amino-fenil)-carboxamida como inhibidores de la histona desacetilasa (hdac)

Info

Publication number
PE20040768A1
PE20040768A1 PE2003001241A PE2003001241A PE20040768A1 PE 20040768 A1 PE20040768 A1 PE 20040768A1 PE 2003001241 A PE2003001241 A PE 2003001241A PE 2003001241 A PE2003001241 A PE 2003001241A PE 20040768 A1 PE20040768 A1 PE 20040768A1
Authority
PE
Peru
Prior art keywords
alkyl
phenyl
amino
carboxamide
desacetilase
Prior art date
Application number
PE2003001241A
Other languages
English (en)
Inventor
Michael Weidner
Georg Fertig
Fran Herting
Matthias Koerner
Anja Limberg
Manfred Kubbies
Ulrike Reiff
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 PE20040768A1 publication Critical patent/PE20040768A1/es

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D333/00Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04Heterocyclic 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
    • C07D333/26Heterocyclic 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
    • C07D333/38Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D333/40Thiophene-2-carboxylic acid
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic 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
    • C07D213/02Heterocyclic 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
    • C07D213/04Heterocyclic 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
    • C07D213/60Heterocyclic 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
    • C07D213/78Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81Amides; Imides
    • C07D213/82Amides; Imides in position 3
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00Carboxylic acid amides
    • C07C233/64Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings
    • C07C233/77Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/28Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a non-condensed six-membered aromatic ring of the carbon skeleton
    • C07C237/42Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a non-condensed six-membered aromatic ring of the carbon skeleton having nitrogen atoms of amino groups bound to the carbon skeleton of the acid part, further acylated
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C275/00Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups
    • C07C275/04Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to acyclic carbon atoms
    • C07C275/20Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to acyclic carbon atoms of an unsaturated carbon skeleton
    • C07C275/24Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing six-membered aromatic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D333/00Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04Heterocyclic 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
    • C07D333/26Heterocyclic 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
    • C07D333/38Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00Systems containing only non-condensed rings
    • C07C2601/02Systems containing only non-condensed rings with a three-membered ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00Systems containing only non-condensed rings
    • C07C2601/06Systems containing only non-condensed rings with a five-membered ring
    • C07C2601/08Systems containing only non-condensed rings with a five-membered ring the ring being saturated
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00Systems containing only non-condensed rings
    • C07C2601/06Systems containing only non-condensed rings with a five-membered ring
    • C07C2601/10Systems containing only non-condensed rings with a five-membered ring the ring being unsaturated
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00Systems containing only non-condensed rings
    • C07C2601/12Systems containing only non-condensed rings with a six-membered ring
    • C07C2601/14The ring being saturated

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)
  • 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)
  • Pyridine Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Compounds Containing Sulfur Atoms (AREA)

Abstract

SE REFIERE A UN COMPUESTO DE LA FORMULA GENERAL I, DONDE A ES TIOFEN-DIILO, FENILENO O PIRIDENDIILO; R1 ES ALQUILO, ALQUENILO, ALQUINILO OPCIONALMENTE SUSTITUIDOS, O CH2-(O-CH2-CH2-)mO-ALQUILO, (CH2)n-O-ALQUILO, ENTRE OTROS, O NR3R4, DONDE R3 Y R4 SON H, ALQUILO, ALQUENILO O ALQUINILO OPCIONALMENTE SUSTITUIDOS, O CH2-(O-CH2-CH2-)mO-ALQUILO, (CH2)n-O-ALQUILO, (CH2)n-C(O)-NH-ALQUILO, ENTRE OTROS; n ES 1 A 6, m ES 1 A 4. ADEMAS SE REFIERE A COMPUESTOS DE FORMULA I-A, EN DONDE A ES TIOFEN-2,5-DIILO, PIRIDEN-2,5-DIILO O 1-4-FENILENO; R5 ES (CH2)k-CICLOPROPILO, ENTRE OTROS; k ES 0 A 6. SON COMPUESTOS PREFERIDOS: 5-[(2-ETOXI-ACETILAMINO)-METIL]-TIOFEN-2-(2-AMINO-FENIL)-CARBOXAMIDA, 5-(PENT-4-ENOILAMINO-METIL)-TIOFEN-2-(2-AMINO-FENIL)-CARBOXAMIDA, 5-[3-(2-DIMETILAMINO-ETIL)-UREIDOMETIL]-TIOFEN-2-(2-AMINO-FENIL)-CARBOXAMIDA; ENTRE OTROS. TAMBIEN SE REFIERE A UN PROCESO PARA ELABORACION DE Y A UNA COMPOSICION FARMACEUTICA. ESTOS COMPUESTOS SON INHIBIDORES DE LA HISTONA DESACETILASA (HDAC) Y POR CONSIGUIENTE MUESTRAN UNA ACTIVIDAD QUE INDUCE LA DIFERENCIACION Y ANTIPROLIFERACION, QUE RESULTA EN LA INHIBICION DE LA PROLIFERACION DE CELULAS TUMORALES, INDUCCION DE LA APTOSIS E INHIBICION DE LA INVASION
PE2003001241A 2002-12-10 2003-12-09 Derivados de arilen-(2-amino-fenil)-carboxamida como inhibidores de la histona desacetilasa (hdac) PE20040768A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP02027579 2002-12-10

Publications (1)

Publication Number Publication Date
PE20040768A1 true PE20040768A1 (es) 2004-11-20

Family

ID=32479720

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2003001241A PE20040768A1 (es) 2002-12-10 2003-12-09 Derivados de arilen-(2-amino-fenil)-carboxamida como inhibidores de la histona desacetilasa (hdac)

Country Status (18)

Country Link
US (1) US7098247B2 (es)
EP (1) EP1572625A1 (es)
JP (1) JP2006509021A (es)
KR (1) KR100759744B1 (es)
CN (2) CN1723192A (es)
AR (1) AR042341A1 (es)
AU (1) AU2003289992A1 (es)
BR (1) BR0317027A (es)
CA (1) CA2507137A1 (es)
GT (1) GT200300274A (es)
MX (1) MXPA05005977A (es)
PA (1) PA8590901A1 (es)
PE (1) PE20040768A1 (es)
PL (1) PL377504A1 (es)
RU (1) RU2345061C2 (es)
TW (1) TW200426138A (es)
UY (1) UY28108A1 (es)
WO (1) WO2004052838A1 (es)

Families Citing this family (19)

* 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
US7250514B1 (en) 2002-10-21 2007-07-31 Takeda San Diego, Inc. Histone deacetylase inhibitors
EP1608628A2 (en) 2003-03-17 2005-12-28 Takeda San Diego, Inc. Histone deacetylase inhibitors
US9115090B2 (en) 2003-12-02 2015-08-25 The Ohio State University Research Foundation Zn2+-chelating motif-tethered short-chain fatty acids as a novel class of histone deacetylase inhibitors
JP2008524246A (ja) * 2004-12-16 2008-07-10 タケダ サン ディエゴ インコーポレイテッド ヒストンデアセチラーゼ阻害剤
US7642253B2 (en) 2005-05-11 2010-01-05 Takeda San Diego, Inc. Histone deacetylase inhibitors
CA2615105A1 (en) 2005-07-14 2007-01-25 Takeda San Diego, Inc. Histone deacetylase inhibitors
JP2009528354A (ja) * 2006-02-28 2009-08-06 メルク エンド カムパニー インコーポレーテッド ヒストン脱アセチル化酵素のインヒビター
KR20090128513A (ko) 2007-03-28 2009-12-15 산텐 세이야꾸 가부시키가이샤 우레아 구조를 갖는 신규 피리딘카르복실산(2-아미노페닐)아미드 유도체
WO2008123395A1 (ja) 2007-03-28 2008-10-16 Santen Pharmaceutical Co., Ltd. ヒストン脱アセチル化酵素阻害作用を有する化合物を有効成分として含有する眼圧下降剤
WO2009047615A2 (en) * 2007-10-10 2009-04-16 Orchid Research Laboratories Limited Novel histone deacetylase inhibitors
EP2292611B1 (en) * 2008-05-23 2012-07-25 Santen Pharmaceutical Co., Ltd Novel thiophenediamine derivative having urea structure
WO2010028192A1 (en) 2008-09-03 2010-03-11 Repligen Corporation Compositions including 6-aminohexanoic acid derivatives as hdac inhibitors
AU2010259042A1 (en) * 2009-06-08 2011-12-15 Gilead Sciences, Inc. Cycloalkylcarbamate benzamide aniline HDAC inhibitor compounds
US10059723B2 (en) 2011-02-28 2018-08-28 Biomarin Pharmaceutical Inc. Histone deacetylase inhibitors
US8957066B2 (en) 2011-02-28 2015-02-17 Biomarin Pharmaceutical Inc. Histone deacetylase inhibitors
US9540395B2 (en) 2011-02-28 2017-01-10 Biomarin Pharmaceutical Inc. Histone deacetylase inhibitors
ES2680224T3 (es) 2013-03-15 2018-09-05 Biomarin Pharmaceutical Inc. Inhibidores de HDAC
PL237497B1 (pl) * 2018-09-17 2021-04-19 Univ Medyczny Im Piastow Slaskich We Wroclawiu Hydrazyd kwasu N’-[(antracen-9-ylo)metyleno]-2-[4,6-dimetylo- 2-sulfanylopirydyn-3-ylo-karboksamido]octowego, sposób jego otrzymywania i zastosowanie

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DE2201062A1 (de) 1972-01-11 1973-07-26 Bayer Ag N-alkoxycarbonyl- bzw. n-alkylthiocarbonyl-2-(2'-thienyl)-benzimidazole, ein verfahren zu ihrer herstellung und ihre verwendung als fungizide
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Also Published As

Publication number Publication date
KR20050088421A (ko) 2005-09-06
RU2005121662A (ru) 2006-01-27
CN1723192A (zh) 2006-01-18
PL377504A1 (pl) 2006-02-06
US7098247B2 (en) 2006-08-29
AR042341A1 (es) 2005-06-15
TW200426138A (en) 2004-12-01
US20040138270A1 (en) 2004-07-15
CA2507137A1 (en) 2004-06-24
WO2004052838A1 (en) 2004-06-24
KR100759744B1 (ko) 2007-10-04
RU2345061C2 (ru) 2009-01-27
BR0317027A (pt) 2005-10-25
CN101279927A (zh) 2008-10-08
AU2003289992A1 (en) 2004-06-30
JP2006509021A (ja) 2006-03-16
PA8590901A1 (es) 2004-11-26
GT200300274A (es) 2004-09-02
EP1572625A1 (en) 2005-09-14
UY28108A1 (es) 2004-06-30
MXPA05005977A (es) 2005-08-18

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