CA2201348A1 - Inhibiteurs de la transferase de proteines farnesylees exempts de thiol - Google Patents

Inhibiteurs de la transferase de proteines farnesylees exempts de thiol

Info

Publication number
CA2201348A1
CA2201348A1 CA 2201348 CA2201348A CA2201348A1 CA 2201348 A1 CA2201348 A1 CA 2201348A1 CA 2201348 CA2201348 CA 2201348 CA 2201348 A CA2201348 A CA 2201348A CA 2201348 A1 CA2201348 A1 CA 2201348A1
Authority
CA
Canada
Prior art keywords
substituted
alkyl
unsubstituted
aryl
hydrogen
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 2201348
Other languages
English (en)
Inventor
John H. Hutchinson
Gerald E. Stokker
Neville J. Anthony
S. Jane Desolms
Robert P. Gomez
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 US08/526,244 external-priority patent/US5652257A/en
Application filed by Individual filed Critical Individual
Priority claimed from PCT/US1995/012224 external-priority patent/WO1996010034A2/fr
Publication of CA2201348A1 publication Critical patent/CA2201348A1/fr
Abandoned legal-status Critical Current

Links

Landscapes

  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

L'invention porte sur des analogues du motif CAAX de la protéine Ras modifiés in vivo par farnésylation. Lesdits analogues, qui inhibent la farnésylation de la Ras, diffèrent par ailleurs de ceux précédemment décrits comme inhibiteurs de la Ras farnésyle transférase en ce qu'ils ne présentent pas de fraction thiol. Cette absence de thiol offre des avantages uniques en matière d'amélioration du comportement pharmacocinétique chez les animaux, de prévention des réactions chimiques liées aux thiols telles que la rapidité de l'auto-oxydation, la formation de bisulfures avec les thiols endogènes et une toxicité systémique réduite. L'invention porte également sur des compositions chimiothérapeutiques contenant les susdits inhibiteurs et sur leur procédé d'obtention.
CA 2201348 1994-09-29 1995-09-26 Inhibiteurs de la transferase de proteines farnesylees exempts de thiol Abandoned CA2201348A1 (fr)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US526,244 1990-05-18
US31497494A 1994-09-29 1994-09-29
US314,974 1994-09-29
US08/526,244 US5652257A (en) 1994-09-29 1995-09-21 Heterocycle-containing inhibitors of farnesyl-protein transferase
PCT/US1995/012224 WO1996010034A2 (fr) 1994-09-29 1995-09-26 Inhibiteurs de la transferase de proteines farnesylees exempts de thiol

Publications (1)

Publication Number Publication Date
CA2201348A1 true CA2201348A1 (fr) 1996-04-04

Family

ID=29407617

Family Applications (1)

Application Number Title Priority Date Filing Date
CA 2201348 Abandoned CA2201348A1 (fr) 1994-09-29 1995-09-26 Inhibiteurs de la transferase de proteines farnesylees exempts de thiol

Country Status (1)

Country Link
CA (1) CA2201348A1 (fr)

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Legal Events

Date Code Title Description
FZDE Dead