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EP0461869A2 Expired / Lapsed EP ⏱️ 0.0 years remaining

Chemotherapeutic agents

Assignee: Merck and Co Inc
•
Filing: 1991-06-12
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Granted: —
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Expires: 2011-06-12
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Abstract

Abstract Compounds which inhibit farnesylation of Ras protein, chemotherapeutic compositions comprising one or more compounds of the invention, and methods for inhibiting farnesylation of Ras protein.

Inventors

  • 👤 Jackson B. Gibbs
  • 👤 Richard A.F. Dixon
  • 👤 Victor M. Garsky
  • 👤 Michael D. Schraber

Bibliographic Details

Application Number —
Jurisdiction EP
Data Source google_patents
Last Synchronized 2026-10-29 18:40
CPC Classifications
C; C07; C07K; C07K5/00; C07K5/04; C07K5/10; C07K5/1002; C07K5/1005; C07K5/1013; A; A61; A61P; A61P35/00; A61K; A61K38/00

Claims Analysis

Total Claims: 11
Claim 1
Independent Claim 45 words
A compound which inhibits plasma membrane Ras protein localization and prevents transformation of normal cells into cancer cells, which compound comprises the amino acid sequence. cys-Aaa¹-Aaa²-Xaa wherein Aaa¹ is an aliphatic amino acid; Aaa² is an aliphatic amino acid; and Xaa is any amino acid.
Claim 2
Dependent Claim 26 words
A compound of Claim 1 wherein Aaa¹ is Ala, Val, Leu or Ile; Aaa² is Ala, Val, Leu or Ile, and Xaa is Ser or Met.
Claim 3
Dependent Claim 8 words
A compound of Claim 2 which is Cys-Val-Leu-Ser.
Claim 4
Dependent Claim 8 words
A compound of claim 2 which is cys-Val-Ile-Met.
Claim 5
Dependent Claim 8 words
A compound of Claim 2 which is cys-Val-Val-Met.
Claim 6
Dependent Claim 9 words
A chemotherapeutic composition comprising a compound of Claim 1.
Claim 7
Dependent Claim 22 words
The use of a compound as claimed in Claim 1 for the manufacture of a medicament for inhibiting farnesylation of Ras protein.
Claim 8
Dependent Claim 9 words
A chemotherapeutic composition comprising a compound of Claim 2.
Claim 9
Dependent Claim 22 words
The use of a compound as claimed in Claim 2 for the manufacture of a medicament for inhibiting farnesylation of Ras protein.
Claim 10
Dependent Claim 50 words
A compound of claim 1 which inhibits plasma membrane Ras protein localization and prevents transformation of normal cells into cancer cells, which compound comprises the sequence: S-( trans, trans ̲ )farnesyl-Cys-Aaa¹-Aaa²-Xaa wherein Aaa¹ is an aliphatic amino acid; Aaa² is an aliphatic amino acid; and Xaa is an amino acid.
Claim 11
Dependent Claim 27 words
A compound of claim 10 selected from the group consisting of: S - (trans, trans) farnesyl-cys-Val-Leu-Ser; S - (trans, trans) farnesyl-cys-Val-Ile-Met; and S - (trans, trans) farnesyl-cys-Val-Val-Met.

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