CA2201351A1 - Inhibiteurs de farnesyle-proteine transferase - Google Patents

Inhibiteurs de farnesyle-proteine transferase

Info

Publication number
CA2201351A1
CA2201351A1 CA 2201351 CA2201351A CA2201351A1 CA 2201351 A1 CA2201351 A1 CA 2201351A1 CA 2201351 CA2201351 CA 2201351 CA 2201351 A CA2201351 A CA 2201351A CA 2201351 A1 CA2201351 A1 CA 2201351A1
Authority
CA
Canada
Prior art keywords
aryl
substituted
alkyl
unsubstituted
heterocycle
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.)
Abandoned
Application number
CA 2201351
Other languages
English (en)
Inventor
Gerald E. Stokker
Samuel L. Graham
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Merck and Co Inc
Original Assignee
Individual
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 claimed from US08/315,046 external-priority patent/US5523456A/en
Application filed by Individual filed Critical Individual
Publication of CA2201351A1 publication Critical patent/CA2201351A1/fr
Abandoned legal-status Critical Current

Links

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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

La présente invention se rapporte à des analogues du motif CAAX de la protéine Ras qui est modifiée par farnésylation in vivo. Ces analogues de CAAX inhibent la farnésylation de Ras. De plus, ils diffèrent de ceux précédemment décrits se présentant sous forme d'inhibiteurs de farnésyle transférase de Ras modifiée en ce qu'ils ne possèdent pas de fraction thiol. L'absence de thiol offre des avantages uniques sur le plan du comportement pharmacocinétique amélioré chez les animaux, de la prévention des réactions chimiques dépendant de thiol, telle que l'auto-oxydation rapide et la formation de bisulfure avec des thiols endogènes, et de la toxicité systémique réduite. L'invention se rapporte en outre à des compositions chimiothérapeutiques contenant ces inhibiteurs de farnésyle transférase et à leurs procédés de production.
CA 2201351 1994-09-29 1995-09-25 Inhibiteurs de farnesyle-proteine transferase Abandoned CA2201351A1 (fr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US315,046 1994-09-29
US08/315,046 US5523456A (en) 1994-09-29 1994-09-29 Inhibitors of farnesyl-protein transferase
PCT/US1995/012321 WO1996010011A1 (fr) 1994-09-29 1995-09-25 Inhibiteurs de farnesyle-proteine transferase

Publications (1)

Publication Number Publication Date
CA2201351A1 true CA2201351A1 (fr) 1996-04-04

Family

ID=29405755

Family Applications (1)

Application Number Title Priority Date Filing Date
CA 2201351 Abandoned CA2201351A1 (fr) 1994-09-29 1995-09-25 Inhibiteurs de farnesyle-proteine transferase

Country Status (1)

Country Link
CA (1) CA2201351A1 (fr)

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Legal Events

Date Code Title Description
FZDE Dead