WO1996031525A3 - Inhibiteurs de la farnesyl-proteine transferase - Google Patents

Inhibiteurs de la farnesyl-proteine transferase Download PDF

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Publication number
WO1996031525A3
WO1996031525A3 PCT/US1996/003974 US9603974W WO9631525A3 WO 1996031525 A3 WO1996031525 A3 WO 1996031525A3 US 9603974 W US9603974 W US 9603974W WO 9631525 A3 WO9631525 A3 WO 9631525A3
Authority
WO
WIPO (PCT)
Prior art keywords
farnesyl
ca1a2x
inhibitors
thiol
analogs
Prior art date
Application number
PCT/US1996/003974
Other languages
English (en)
Other versions
WO1996031525A2 (fr
Inventor
S Jane Desolms
Original Assignee
Merck & Co Inc
S Jane Desolms
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
Application filed by Merck & Co Inc, S Jane Desolms filed Critical Merck & Co Inc
Priority to EP96911382A priority Critical patent/EP0837857A4/fr
Priority to JP53033696A priority patent/JP2002504067A/ja
Priority to AU54285/96A priority patent/AU713698B2/en
Publication of WO1996031525A2 publication Critical patent/WO1996031525A2/fr
Publication of WO1996031525A3 publication Critical patent/WO1996031525A3/fr

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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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/0207—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-(X)4-C(=0), e.g. 'isosters', replacing two amino acids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

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

Abstract

La présente invention concerne des analogues du motif CA1A2X de la protéine Ras modifiés par farnesylation in vivo. Ces analogues CA1A2X ont un effet inhibiteur sur la farnésyl-protéine transférase et sur la farnesylation de certaines protéines. En outre, ces analogues CA1A2X diffèrent de ceux décrits antérieurement en tant qu'inhibiteurs de farnésyl-protéine transférase par le fait qu'ils ne comportent pas de fraction thiol. L'absence de thiol présente des avantages uniques en termes d'amélioration du comportement pharmacocinétique chez les animaux, de prévention de réactions chimiques dépendantes d'un thiol, telle que l'auto-oxidation rapide et les formations de bisulfure avec des thiols endogènes, et une toxicité systémique réduite. Les composants de cette invention renferment également une fraction amine cyclique à la position A2 du motif. Cette invention recouvre également des compositions chimiothérapeutiques renfermant de tels inhibiteurs de farnesyl transférase et leurs procédés de production.
PCT/US1996/003974 1995-03-29 1996-03-25 Inhibiteurs de la farnesyl-proteine transferase WO1996031525A2 (fr)

Priority Applications (3)

Application Number Priority Date Filing Date Title
EP96911382A EP0837857A4 (fr) 1995-03-29 1996-03-25 Inhibiteurs de la farnesyl-proteine transferase
JP53033696A JP2002504067A (ja) 1995-03-29 1996-03-25 ファルネシル−タンパク質トランスフェラーゼ阻害剤
AU54285/96A AU713698B2 (en) 1995-03-29 1996-03-25 Inhibitors of farnesyl-protein transferase

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US41262695A 1995-03-29 1995-03-29
US41282895A 1995-03-29 1995-03-29
US08/412,626 1995-03-29
US08/412,828 1995-03-29

Publications (2)

Publication Number Publication Date
WO1996031525A2 WO1996031525A2 (fr) 1996-10-10
WO1996031525A3 true WO1996031525A3 (fr) 1996-12-27

Family

ID=27021839

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US1996/003974 WO1996031525A2 (fr) 1995-03-29 1996-03-25 Inhibiteurs de la farnesyl-proteine transferase

Country Status (1)

Country Link
WO (1) WO1996031525A2 (fr)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5703241A (en) * 1995-10-16 1997-12-30 Merck & Co., Inc. Inhibitor of farnesyl-protein transferase
US5932590A (en) * 1996-12-05 1999-08-03 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5238922A (en) * 1991-09-30 1993-08-24 Merck & Co., Inc. Inhibitors of farnesyl protein transferase
US5352705A (en) * 1992-06-26 1994-10-04 Merck & Co., Inc. Inhibitors of farnesyl protein transferase

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5238922A (en) * 1991-09-30 1993-08-24 Merck & Co., Inc. Inhibitors of farnesyl protein transferase
US5352705A (en) * 1992-06-26 1994-10-04 Merck & Co., Inc. Inhibitors of farnesyl protein transferase

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
See also references of EP0837857A4 *
THE JOURNAL OF BIOLOGICAL CHEMISTRY, April 1993, Vol. 268, No. 11, GIBBS et al., "Selective Inhibition of Farresyl-Protein Transferase Blocks Ras Process in Vivo", pages 7617-7620. *

Also Published As

Publication number Publication date
WO1996031525A2 (fr) 1996-10-10

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