CA2176720C - Nouveaux inhibiteurs d'enzymes, leur synthese et leurs procedes d'utilisation - Google Patents

Nouveaux inhibiteurs d'enzymes, leur synthese et leurs procedes d'utilisation Download PDF

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Publication number
CA2176720C
CA2176720C CA002176720A CA2176720A CA2176720C CA 2176720 C CA2176720 C CA 2176720C CA 002176720 A CA002176720 A CA 002176720A CA 2176720 A CA2176720 A CA 2176720A CA 2176720 C CA2176720 C CA 2176720C
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CA
Canada
Prior art keywords
hydroxyethoxy
pyrimidine
methyl
phenylthio
barbituric acid
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Fee Related
Application number
CA002176720A
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English (en)
Other versions
CA2176720A1 (fr
Inventor
Mahmoud H. El Kouni
Fardos N. M. Naguib
Raymond F. Schinazi
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Individual
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Individual
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Filing date
Publication date
Priority claimed from US08/146,838 external-priority patent/US5476855A/en
Application filed by Individual filed Critical Individual
Publication of CA2176720A1 publication Critical patent/CA2176720A1/fr
Application granted granted Critical
Publication of CA2176720C publication Critical patent/CA2176720C/fr
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/60—Three or more oxygen or sulfur atoms

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

L'invention concerne des nouveaux composés efficaces pour inhiber l'activité de la DHUDase et l'UrdPase. Lesdits composés sont représentés par la formule (I) ou (II) dans lesquelles X correspond à S ou Se; Y à I, F, Cl, Br, méthoxy, benzyle, sélénylphényle, ou thiophényle, et R¿1? à une terminaison acyclo représentée par la formule (III) dans laquelle R¿2? correspond à H, CH¿2?OH ou CH¿2?NH¿2?; R¿3? à OH, NH¿2?, ou à OCOCH¿2?CH¿2?CO¿2?H; et R¿4? à O, S, ou CH¿2?. Les composés selon l'invention peuvent être utilisés dans des compositions pharmaceutiques ainsi qu'avec divers agents chimiothérapeutiques de manière à augmenter l'efficacité du traitement. Ils peuvent également être utilisés dans des méthodes de traitement de patients par coadministration ou administration séquentielle des composés inhibant les enzymes avec un agent chimiothérapeutique efficace pour traiter des cancers, ou des infections virales, fongiques, bactériennes ou parasitaires. Lesdits composés sont également utiles pour améliorer l'imagerie. Ils peuvent aussi être administrés seuls pour prévenir et/ou traiter les troubles du catabolisme de la pyrimidine et d'autres troubles physiologiques.
CA002176720A 1993-11-02 1994-09-30 Nouveaux inhibiteurs d'enzymes, leur synthese et leurs procedes d'utilisation Expired - Fee Related CA2176720C (fr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US08/146,838 US5476855A (en) 1993-11-02 1993-11-02 Enzyme inhibitors, their synthesis and methods for use
US08/146,838 1993-11-02
PCT/US1994/011173 WO1995012400A1 (fr) 1993-11-02 1994-09-30 Nouveaux inhibiteurs d'enzymes, leur synthese et leurs procedes d'utilisation

Publications (2)

Publication Number Publication Date
CA2176720A1 CA2176720A1 (fr) 1995-05-11
CA2176720C true CA2176720C (fr) 2006-08-01

Family

ID=36764225

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002176720A Expired - Fee Related CA2176720C (fr) 1993-11-02 1994-09-30 Nouveaux inhibiteurs d'enzymes, leur synthese et leurs procedes d'utilisation

Country Status (1)

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CA (1) CA2176720C (fr)

Also Published As

Publication number Publication date
CA2176720A1 (fr) 1995-05-11

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