Patent EP0528486A2 successfully refreshed from Google Patents.
EP0528486A2
Expired / Lapsed
EP
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Non-substrate inhibitors of farnesyl protein transferase
Assignee: Merck and Co Inc
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Filing: 1992-08-08
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Granted: —
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Expires: 2012-08-08
Abstract
Abstract The present invention is directed to 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 farnesylation 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
2026-10-23 22:16
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: 6
Claim 1
Independent Claim
105 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 - Xaa² - Xaa³ - NRR¹ wherein: Cys is the amino acid Cysteine; Xaa¹ is any amino acid in the natural L-isomer form; Xaa² is any amino acid in the natural L-isomer form; and Xaa³-NRR¹ is an amide of any amino acid in the natural L-isomer form, wherein R and R¹ are independently selected from hydrogen, C₁ - C₁₂ alkyl, aralkyl, or unsubstituted or substituted aryl; or the pharmaceutically acceptable salts thereof.
Claim 2
Dependent Claim
13 words
A compound according to Claim 1 which is CVLS-NH₂ (SEQ ID NO: 1).
Claim 3
Dependent Claim
13 words
A compound according to Claim 1 which is CVFM-NH₂ (SEQ ID NO: 2).
Claim 4
Dependent Claim
23 words
A chemotherapeutic composition comprising a pharmaceutical carrier, and dispersed therein, a therapeutically effective amount of a compound according to Claims 1 through 3.
Claim 5
Dependent Claim
41 words
The use of a compound as claimed in claim 1 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
21 words
The use of a compound as claimed in claim 1 for the manufacture of a medicament for the treatment of cancer.
References Cited (Backward Citations)
No citation records indexed.
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