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1. WO1996039137 - INHIBITORS OF FARNESYL-PROTEIN TRANSFERASE

Publication Number WO/1996/039137
Publication Date 12.12.1996
International Application No. PCT/US1996/008740
International Filing Date 03.06.1996
Chapter 2 Demand Filed 17.12.1996
IPC
C07D 233/54 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
233Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
54having two double bonds between ring members or between ring members and non-ring members
C07D 401/14 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
401Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
14containing three or more hetero rings
CPC
C07D 233/64
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
233Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
54having two double bonds between ring members or between ring members and non-ring members
64with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
C07D 401/14
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
401Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
14containing three or more hetero rings
Applicants
  • MERCK & CO., INC. [US]/[US] (AllExceptUS)
  • ANTHONY, Neville, J. [GB]/[US] (UsOnly)
  • SOLINSKY, Kelly, M. [US]/[US] (UsOnly)
  • GOMEZ, Robert, P. [US]/[US] (UsOnly)
  • WILLIAMS, Theresa, M. [US]/[US] (UsOnly)
  • BERGMAN, Jeffrey, M. [US]/[US] (UsOnly)
  • DeSOLMS, S., Jane [US]/[US] (UsOnly)
  • DINSMORE, Christopher, J. [US]/[US] (UsOnly)
  • MacTOUGH, Suzanne, C. [US]/[US] (UsOnly)
Inventors
  • ANTHONY, Neville, J.
  • SOLINSKY, Kelly, M.
  • GOMEZ, Robert, P.
  • WILLIAMS, Theresa, M.
  • BERGMAN, Jeffrey, M.
  • DeSOLMS, S., Jane
  • DINSMORE, Christopher, J.
  • MacTOUGH, Suzanne, C.
Common Representative
  • MERCK & CO., INC.
Priority Data
08/468,16006.06.1995US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) INHIBITORS OF FARNESYL-PROTEIN TRANSFERASE
(FR) INHIBITEURS DE LA FARNESYL TRANSFERASE
Abstract
(EN)
The present invention comprises low molecular weight peptidyl compounds that inhibit the farnesyl-protein transferase. Furthermore, these compounds differ from the mono- or dipeptidyl analogs previously described as inhibitors of farnesyl-protein transferase in that they do not have a thiol moiety. The lack of the thiol offers unique advantages in terms of improved pharmacokinetic behavior in animals, prevention of thiol-dependent chemical reactions, such as rapid autoxidation and disulfide formation with endogenous thiols, and reduced systemic toxicity. Further contained in this invention are chemotherapeutic compositions containing these farnesyl transferase inhibitors and methods for their production.
(FR)
L'invention porte sur des composés peptidyliques de faible poids moléculaire inhibiteurs de la farnésyl transférase. Lesdits composés diffèrent de leurs analogues mono et di-peptidilyques préalablement décrits comme inhibiteurs de la farnésyl transférase en ce qu'ils ne présentent pas de fraction thiol. Cette absence de thiol offre de grands avantages: amélioration du comportement pharmacocinétique chez l'animal, prévention des réactions chimiques suscitées par le thiol tels qu'une auto-oxydation rapide et la formation de bisulfure avec les thiols endogènes, ainsi que réduction de la toxicité systémique. L'invention porte également sur des compositions chimiothérapeutiques contenant lesdits inhibiteurs, et leurs procédés d'obtention.
Also published as
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