Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1997-01-21
1999-11-09
Gerstl, Robert
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
5483361, A61K 31415, C07D23361
Patent
active
059815620
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.
REFERENCES:
patent: 5141851 (1992-08-01), Brown et al.
patent: 5234917 (1993-08-01), Finkelstein et al.
patent: 5238922 (1993-08-01), Graham et al.
patent: 5326773 (1994-07-01), DeSolms et al.
patent: 5340828 (1994-08-01), Graham et al.
patent: 5352705 (1994-10-01), Deana, et al.
patent: 5439918 (1995-08-01), DeSolms et al.
patent: 5468733 (1995-11-01), Desolms et al.
patent: 5480893 (1996-01-01), Graham et al.
patent: 5491164 (1996-02-01), DeSolms et al.
patent: 5504212 (1996-04-01), DeSolms et al
patent: 5534537 (1996-07-01), Ciccarone et al.
patent: 5571792 (1996-11-01), Bolton et al.
patent: 5571835 (1996-11-01), Anthony et al.
patent: 5578629 (1996-11-01), Ciccarone et al.
patent: 5585359 (1996-12-01), Breslin et al.
patent: 5756528 (1998-05-01), Anthony
James, G.L. et al., "Benzodiazepine Peptidomimetic BZA-5B Interrupts the MAP Kinase Activation Pathway in H-Ras-transformed Rat-1 Cells, but Not in Untransformed Cells," The Jour. of Biol. Chem., vol. 269, No. 44, pp. 27705-27714 (1994).
James, G.L. et al., "Benzodiazepine Peptidomimetics: Potent Inhibitors of Ras Farnesylation in Animal Cells", Science, vol. 260, pp. 1937-1942 (1993).
James, G.L., et al., "Polylysine and CVIM Sequences of K-RasB Dictate Specificity of Prenylation and Confer Resistance to Benzodiazepine Peptidomimetic in Vitro", The Jour. of Biol. Chem., vol. 270, No. 11, pp. 6221-6226 (1995).
Kohl, N.E. et al., "Selective Inhibition of ras-Dependent Transformation by a Farnesyltransferase Inhibitor", Science, vol. 260, pp. 1934-1937 (1993).
Kohl, N.E. et al., "Protein farnesyltransferase inhibitors block the growth of ras-dependent tumors in nude mice", Proc. Natl. Acad. Sci. USA, Med. Sciences, vol. 91, pp. 9141-9145 (1994).
Kohl, N.E., et al., "Inhibition of farnesyltransferase induces regression of mammary and salivary carcinomas in ras transgenic mice," Nature Medicine, vol. 1, No. 8, pp. 792-797 (1995).
Pompliano, D.L., "Steady-State Kinetic Mechanism of Ras Farnesyl:Protein Transferase," Biochemistry, vol. 31, pp. 3800-3807 (1992).
Sepp-Lorenzino, L., et al., "A Peptidomimetic Inhibitor of Farnesyl:Protein Transferase Blocks the Anchorage-dependent and -independent Growth of Human Tumor Cell Lines," Cancer Research, vol. 55, pp. 5302-5309 (1995).
Lampe, J.W., et al., "Cardiotonic Agents. 6. Histamine Analogues as Potential Cardiovascular Selective H2 Agonists," J. Med. Chem., vol. 33, pp. 1688-1697 (1990).
PTEA, Gazz. Chim. Ital. 114, 35-40, 1984.
Dinsmore Christopher J.
Hartman George D.
Daniel Mark R.
Gerstl Robert
Merck & Co. , Inc.
Muthard David A.
Pecoraro Dianne
LandOfFree
Inhibitors of farnesyl-protein transferase does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Inhibitors of farnesyl-protein transferase, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Inhibitors of farnesyl-protein transferase will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-1456531