Farnesyl transferase inhibitors

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

Reexamination Certificate

Rate now

  [ 0.00 ] – not rated yet Voters 0   Comments 0

Details

C548S336100

Reexamination Certificate

active

07323484

ABSTRACT:
The present invention is directed to compounds of the formulawherein the variables are as defined in the specification. The compounds are useful for inhibiting farnesyl transferase and for the treatment of tumors and restenosis.

REFERENCES:
patent: 5229386 (1993-07-01), Takasugi et al.
patent: 6673927 (2004-01-01), Gordon et al.
patent: 7022704 (2006-04-01), Gordon et al.
patent: 388 909 (1990-09-01), None
patent: H03-14569 (1991-01-01), None
patent: WO94/26723 (1994-11-01), None
patent: WO95/00497 (1995-01-01), None
patent: WO97/19075 (1997-05-01), None
Khosravi-Far et al., Cell Growth & Differentiation, vol. 3;461-469.
Shide et al., “Rational—Design of Potent Carboxylic Acid Based Bisubstrate Inhibitors of Ras Farnesyl Protein Transferase”, Bioorganic & Medicinal Chemistry Letters, 4:2107-2112, 1994.
Bishop et al., “Novel Tricyclic Inhibitors of Farnesyl Protein Transferase”, The Journal of Biological Chemistry, 270:30611-30618, 1995.
Buss et al., “Farnesyl Transferase Inhibitors: the Successes and Surprises of a New Class of Potential Cancer Chemotherapeutics”, Chemistry & Biology, 2:787-791, 1995.
Clerc et al., “Constrained Analogs of KCVFM with Improved Inhibitory Properties Against Farnesyl Transferase” Bioorganic & Medicinal Chemistry Letters, 5:1779-1784, 1995.
deSolms et al., “Pseudodipeptide Inhibitors of Protein Farnesyltransferase”, J. Ned. Chem.,38:3967-3971, 1995.
Garcia et al., “Peptidomimetic Inhibitors of Ras Farnesylation and Function in Whole Cells”, The Journal of Biological Chemistry, 268:18415-18418, 1993.
Gibbs et al., “Farnesyltransferase Inhibitors: Ras Research Yields a Potential Cancer Therapeutic”, Cell, 77:175-178, 1994.
Graham et al., “Pseudopeptide Inhibitors of Ras Farnesyl-Protein Transferase”, J. Med. Chem. 37:725-732, 1994.
Harrington et al., “Cysteine and Methionine Linked by Carbon Pseudopeptides Inhibit Farnesyl Transferase”, Bioorganic & Medicinal Chemistry Letters, 4:2775-2780, 1994.
Hunt et al., “Potent, Cell Active, Non-Thiol Tetrapeptide Inhibitors of Farnesyltransferase”, J. Med. Chem. 39:353-358, 1996.
James et al., “Senzodiazepine Peptidomimetics: Potent Inhibitors of Ras Farnesylation in Animal Cells”, Science, 260:1937-1942, 1993.
James et al., “Polylysine and CVIM Sequences of K-RasB Dictate Specificity of Prenylation and Confer Resistance to Benzodiazepine Peptidomimetic in Vitro”, The Journal of Biological Chem., 270:6221-6226, 1995.
Koblan et al.,11NMR Studies of Novel Inhibitors Bound to FarnesyL-Protein Transferase, Protein Science, 4:681-688, 1995.
Kohl et al., “Development of Inhibitors of Protein Farnesylation as Potential Chemotherapeutic Agents”, Journal of Cellular Biochemistry, 22:145-150, 1995.
Kohl et al., “Inhibition of Farnesyltransferase Induces Regression of Mammary and Salivary Carcinomas in Ras Transgenic Mice”, Nature Medicine, 1:792-797, 1995.
Kohl et al., “Inhibition of Ras Function in Vitro and In Vivo Using Inhibitors of Farnesyl-Protein Transferase”, Methods in Enzymology, 255:378-386, 1995.
Kohl et al., “Selective Inhibition of ras-Dependent Transformation by a Farnesyltransferase Inhibitor”, Science, 260:1934-1937, 1993.
Leftheris et al., “Development of Highly Potent Inhibitors of Ras Farnesyltransferase Possessing Cellular and in Vivo Activity”, J. Med. Chem., 39:224-236, 1996.
Lerner et al., “Ras CAAX Peptidomimetic FTI-277 Selectively Blocks Oncogenic Ras Signaling by Inducing Cytoplasmic Accumulation of Inactive Ras-Raf Complexes”, The J. of Biological Chem., 270:26802-26806, 1995.
Nagasu et al., Inhibition of Hunan Tumor Xenograft Growth by Treatment with the Farnesyl.Transferase Inhibitor 895611, Cancer Research, 55:5310-5314, 1995.
Nigam et al., “Potent Inhibition of Human Tumor p21rasFarnesyltransferase by AIAz-Lacking p21rasCA1A2X Peptidomimetics”, The Journal of Biological Chemistry, 268:20695-20698, 1993.
Patel et al., “Phenol Based Tripeptide Inhibitors of Ras Farnesyl Protein Transferase”, Sioorganic & Medicinal Chemistry Letters, 4:1883-1888, 1994.
Wan et al., “Design and Synthesis of Non-Peptide Ras CAAX Mimetics as Potent Farnesyltransferase Inhibitors”, J. Med. Chem., 39:217-223, 1996.
Oian et al., “Design and Structural Requirements of Potent Peptidomimetic Inhibitors of p21ras Farnesyltransferase”, The Journal of Biological Chemistry, 269:12410-12413, 1994.
Reiss et al., “Sequence Requirement for Peptide Recognition by Rat Brain p21r,sProtein Farnesyltransferase”,I Proc. Matt. Aced. Sci., 88:732-736, 1991.
Sepp-Lorenzino et al., “A Peptidomimetic Inhibitor of Farnesyl: Protein Transferase Blocks the Anchorage Dependent and -Independent Growth of Human Tumor Cell Lines”, Cancer Research, 55:5302-5309, 1995.
Singh et al., “Fusidienot: A Novel Inhibitor of Ras Farnesyl-Protein Transferase from Fusidiua Griseum”, Pergamon Tetrahedron Letters, 35:4693-4696, 1994.
Vogt et al., “A Non-Peptide Mimetic of Ras-CAAX: Selective Inhibition of Farnesyltransferase and Ras Processing”, The Journal of Biological Chemistry, 270:660-664, 1995.
Williams et al.,112-Substituted Piperazines as Constrained Amino Acids. Application to the Synthesis of Potent, Non Carboxylic Acid Inhibitors of Farnesyltransferase, J. Med. Chem., 39:1345-1348, 1996.
Cohen et al Biochemical Pharmacology, vol. 60, pp. 1061-1068 (2000).

LandOfFree

Say what you really think

Search LandOfFree.com for the USA inventors and patents. Rate them and share your experience with other people.

Rating

Farnesyl transferase inhibitors does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Farnesyl transferase inhibitors, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Farnesyl transferase inhibitors will most certainly appreciate the feedback.

Rate now

     

Profile ID: LFUS-PAI-O-2809576

  Search
All data on this website is collected from public sources. Our data reflects the most accurate information available at the time of publication.