CA2216532A1 - Inhibiteurs de la farnesyle transferase - Google Patents

Inhibiteurs de la farnesyle transferase Download PDF

Info

Publication number
CA2216532A1
CA2216532A1 CA002216532A CA2216532A CA2216532A1 CA 2216532 A1 CA2216532 A1 CA 2216532A1 CA 002216532 A CA002216532 A CA 002216532A CA 2216532 A CA2216532 A CA 2216532A CA 2216532 A1 CA2216532 A1 CA 2216532A1
Authority
CA
Canada
Prior art keywords
alkyl
aryl
hydrogen
substituted
alkenyl
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
CA002216532A
Other languages
English (en)
Inventor
S. Jane Desolms
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 US08/600,794 external-priority patent/US5627202A/en
Application filed by Individual filed Critical Individual
Publication of CA2216532A1 publication Critical patent/CA2216532A1/fr
Abandoned legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06139—Dipeptides with the first amino acid being heterocyclic
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Genetics & Genomics (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • General Health & Medical Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

La présente invention comporte des analogues du motif structural CA?1¿A?2¿X de la protéine Ras, laquelle est modifiée par farnésylation in vivo. Ces analogues de CA?1¿A?2¿X inhibent la farnésyle transférase ainsi que la farnésylation de certaines protéines. En outre, ces analogues de CA?1¿A?2¿X diffèrent de ceux précédemment décrits en tant qu'inhibiteurs de la farnésyle transférase, en ce qu'ils sont dépourvus d'une fraction thiol. Cette absence de fraction thiol offre des avantages uniques, en termes d'un meilleur comportement pharmacocinétique de ces analogues chez les animaux, d'une prévention de réactions chimiques dépendant des thiols, telles qu'une autoxydation rapide et une formation de disulfure avec les thiols endogènes, et d'une toxicité systématique réduite. Les composés selon l'invention comprennent également une fraction amine cyclique en position A?2¿ du motif structural. On décrit encore dans cette invention des compositions chimiothérapeutiques contenant ces inhibiteurs de farnésyle transférase, ainsi que des procédés de production de ceux-ci.
CA002216532A 1995-03-29 1996-03-25 Inhibiteurs de la farnesyle transferase Abandoned CA2216532A1 (fr)

Applications Claiming Priority (8)

Application Number Priority Date Filing Date Title
US412,626 1982-08-30
US41282895A 1995-03-29 1995-03-29
US41262695A 1995-03-29 1995-03-29
US412,828 1995-03-29
US441995P 1995-09-27 1995-09-27
US60/004,419 1995-09-27
US08/600,794 US5627202A (en) 1995-03-29 1996-02-13 Inhibitors of farnesyl-protein transferase
US600,794 1996-02-13

Publications (1)

Publication Number Publication Date
CA2216532A1 true CA2216532A1 (fr) 1996-10-31

Family

ID=27485364

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002216532A Abandoned CA2216532A1 (fr) 1995-03-29 1996-03-25 Inhibiteurs de la farnesyle transferase

Country Status (3)

Country Link
EP (1) EP0837875A4 (fr)
AU (1) AU708620B2 (fr)
CA (1) CA2216532A1 (fr)

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2575753B1 (fr) * 1985-01-07 1987-02-20 Adir Nouveaux derives peptidiques a structure polycyclique azotee, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
FR2610934B1 (fr) * 1987-02-13 1989-05-05 Adir Nouveaux derives peptidiques a structure polycyclique azotee, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
CA2091194A1 (fr) * 1992-04-08 1993-10-09 Richard D. Connell Derives 2-oxoethyliques utilises comme immunosuppresseurs
SE9300012D0 (sv) * 1993-01-05 1993-01-05 Astra Ab New peptides
US5385918A (en) * 1993-02-09 1995-01-31 Miles Inc. Aminomethylene-peptides as immunosuppressants
CA2118985A1 (fr) * 1993-04-02 1994-10-03 Dinesh V. Patel Inhibiteurs heterocycliques de la farnesyl proteine transferase
AU1615895A (en) * 1994-03-31 1995-10-12 Bristol-Myers Squibb Company Imidazole-containing inhibitors of farnesyl protein transferase
CA2155448A1 (fr) * 1994-08-11 1996-02-12 Katerina Leftheris Inhibiteurs de la farnesyl-proteine-transferase

Also Published As

Publication number Publication date
AU6895096A (en) 1996-11-18
AU708620B2 (en) 1999-08-05
EP0837875A4 (fr) 1998-10-07
EP0837875A2 (fr) 1998-04-29

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Legal Events

Date Code Title Description
FZDE Dead