Inhibitors of protein farnesyltransferase and squalene synthase

Details Inhibitors of protein farnesyltransferase and squalene synthase Inhibitors of protein farnesyltransferase and squalene synthase

1995-01-24

1997-05-20

Geist, Gary

Organic compounds -- part of the class 532-570 series

Organic compounds

Carboxylic acids and salts thereof

562432, 562441, 562442, 562457, 562505, 560 42, 560123, 560251, 546146, 546189, 546262, 548187, 548561, 549 65, 549 77, 549438, 549460, 549479, 549493, 514307, 514316, 514332, 514369, 514427, 514438, 514445, 514461, 514466, 514468, 514471, 514533, 514548, 514562, 514563, C07C22946, A61K 3119, A61K 31195

Patent

active

056314019

ABSTRACT:
The present invention provides a compound of the formula ##STR1## or a pharmaceutically acceptable salt thereof, which are useful in inhibiting protein farnesyltransferase and the farnesylation of the oncogene protein Ras or inhibiting de novo squalene production resulting in the inhibition of cholesterol biosynthesis, processes for the preparation of the compounds of the invention in addition to intermediates useful in these processes, a pharmaceutical composition, and to methods of using such compounds.

REFERENCES:
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patent: 5260479 (1993-11-01), Singh et al.
patent: 5344962 (1994-09-01), Ahmad
Moore et al., Chem. Mat., 1, pp. 163-166 (1989).
Ortiz de Montellano, Paul R., et al. "Prenyl Substituted Cyclobutanones As Squalene Synthetase Inhibitors" Tetrahedron Letters No. 346, pp. 4115-4118, 1976.

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