EP0520823A2
Expired / Lapsed
EP
⏱️ 0.0 years remaining
Non-substrate peptide inhibitors of farnesyl protein transferase
Assignee: Merck and Co Inc
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Filing: 1992-06-26
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Granted: —
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Expires: 2012-06-26
Abstract
Abstract The present invention is directed to peptide compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the fanesylation of the oncogene protein Ras.
Inventors
- 👤 Jackson B. Gibbs.
- 👤 Elaine Rands
- 👤 David L. Pompliano
- 👤 Victor M. Garsky
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-10-27 16:28
CPC Classifications
C; C07; C07K; C07K5/00; C07K5/04; C07K5/10; C07K5/1002; C07K5/1005; C07K5/1013; A; A61; A61P; A61P35/00
Claims Analysis
Total Claims: 7
Claim 1
Independent Claim
80 words
A compound which inhibits farnesyl - protein transferase and prevents transformation of normal cells into cancer cells by acting as a non-substrate inhibitor, which compound comprises the amino acid sequence: Cys - Xaa¹-dXaa² - Xaa³ wherein: Cys is a Cysteine amino acid; Xaa¹ is any amino acid in the natural L-isomer form; dXaa² is any amino acid in an unnatural D-isomer form; and Xaa³ is any amino acid in the natural L isomer form; or the pharmaceutically acceptable salts thereof.
Claim 2
Dependent Claim
13 words
A compound according to Claim 1 which is CV(dL)S (SEQ ID NO: 1).
Claim 3
Dependent Claim
13 words
A compound according to Claim 1 which is CV(dF)M (SEQ ID NO: 2).
Claim 4
Dependent Claim
25 words
A chemotherapeutic composition comprising a pharmaceutical carrier, and dispersed therein a therapeutically effective amount of a compound according to any one of the preceding Claims.
Claim 5
Dependent Claim
39 words
The use of a composition of Claim 4 for the manufacture of a medicament for inhibiting farnesyl-protein transferase and plasma membrane Ras protein localization, and preventing transformation of normal cells into cancer cells by acting as a non-substrate inhibitor.
Claim 6
Dependent Claim
17 words
The use of a composition of Claim 4 for the manufacture of a medicament for treating cancer.
Claim 7
Dependent Claim
15 words
The use according to Claim 5 or Claim 6, wherein the mammal is a human.
References Cited (Backward Citations)
No citation records indexed.
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