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1. WO1996009821 - INHIBITORS OF FARNESYL-PROTEIN TRANSFERASE

Publication Number WO/1996/009821
Publication Date 04.04.1996
International Application No. PCT/US1995/012320
International Filing Date 25.09.1995
Chapter 2 Demand Filed 19.04.1996
IPC
A61K 38/00 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
38Medicinal preparations containing peptides
C07D 207/09 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
207Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
02with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
04having no double bonds between ring members or between ring members and non-ring members
08with hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms
09Radicals substituted by nitrogen atoms not forming part of a nitro radical
C07K 5/065 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
5Peptides having up to four amino acids in a fully defined sequence; Derivatives thereof
04containing only normal peptide links
06Dipeptides
065the side chain of the first amino acid containing carbocyclic rings, e.g. Phe, Tyr
CPC
A61K 38/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
38Medicinal preparations containing peptides
A61P 35/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
A61P 43/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
43Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
C07D 207/09
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
207Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
02with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
04having no double bonds between ring members or between ring members and non-ring members
08with hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms
09Radicals substituted by nitrogen atoms, not forming part of a nitro radical
C07K 5/06078
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
5Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
04containing only normal peptide links
06Dipeptides
06008with the first amino acid being neutral
06078and aromatic or cycloaliphatic
Applicants
  • MERCK & CO., INC. [US]/[US] (AllExceptUS)
  • ANTHONY, Neville, J. [GB]/[US] (UsOnly)
  • deSOLMS, S., Jane [US]/[US] (UsOnly)
  • GRAHAM, Samuel, L. [US]/[US] (UsOnly)
Inventors
  • ANTHONY, Neville, J.
  • deSOLMS, S., Jane
  • GRAHAM, Samuel, L.
Common Representative
  • MERCK & CO., INC.
Priority Data
315,05929.09.1994US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) INHIBITORS OF FARNESYL-PROTEIN TRANSFERASE
(FR) INHIBITEURS DE FARNESYLE-PROTEINE TRANSFERASE
Abstract
(EN)
The present invention comprises analogs of the CA1A2X motif of the protein Ras that is modified by farnesylation $i(in vivo). These CA1A2X analogs inhibit the farnesylation of Ras. Furthermore, these CA1A2X analogs differ from those previously described as inhibitors of Ras farnesly transferase in that they have a prolyl like moiety in the A1 position. Further contained in this invention are chemotherapeutic compositions containing these farnesyl transferase inhibitors and methods for their production.
(FR)
La présente invention se rapporte à des analogues du motif CA1A2X de la protéine Ras qui est modifiée par farnésylation $i(in vivo). Ces analogues de CA1A2X inhibent la farnésylation de Ras. De plus, ils diffèrent des autres analogues précédemment décrits comme étant des inhibiteurs de Ras-farnésyle transférase en ce qu'ils possèdent une fraction de type prolyle en position A1. Cette invention se rapporte également à des compositions chimiothérapiques contenant ces inhibiteurs de farnésyle transférase et à leurs procédés de production.
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