Multi-substituted imidazolines and method of use thereof

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

Reexamination Certificate

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C514S402000, C548S312100, C548S334500, C548S333500, C548S350100

Reexamination Certificate

active

06878735

ABSTRACT:
A new class of imidazolines as 4-position acids or esters with very potent anti-inflammatory as well as antimicrobial activity is described. The synthesis of these imidazolines includes a multicomponent reaction applicable to a combinatorial synthetic approach. The combination of these two key characteristics provides an effective therapeutic drug in the treatment of septic shock as well as many other inflammatory (arthritis and asthma) and infectious disorders. The use of this novel class of non-steroidal agents as anti-inflammatory agents (for the treatment of asthma etc.), antibacterial agents and antiseptic agents is described. The compounds are also useful in the treatment of tumors (such as cancers). The imidazolines are potent inhibitors of the transcription factor NF-κB as well as potent activity against the Gram (+) bacteriumB. subtillusandB. cereuswith MIC values in the range of 50 μm/mL.

REFERENCES:
patent: 5804374 (1998-09-01), Baltimore
patent: 5821072 (1998-10-01), Schwartz et al.
patent: 6001563 (1999-12-01), Deely et al.
patent: 6318978 (2001-11-01), Burns
patent: 6410516 (2002-06-01), Baltimore
Yamamoto, Y., et al., J. Clin Invest 107 135-142 (2001).
Hart, L.A., et al., Am J Respir Crit Care Med 158 1585-1592 (1998).
Coward, W.R., et al., Clin Exp Allergy 28 Suppl 3, 42-46 (1998).
Badger, A.M., et al., J. Pharmacol Exp Ther 290 587-593 (1999).
Breton, J.J., et al., J Pharmacol Exp Ther 282 459-466 (1997).
Roshak, A., et al., J Pharmacol Exp Ther 283 955-951 (1997).
Kopp, E., et al., Science 265 956-959 (1994).
Ichiyama, T., et al., Brain Res 911 56-61 (2001.
Natarajan, K., et al., Proc Natl Acad Sci USA 93 9090-9095 (1996).
M.P.Boland, Biochemical Society Transactions, vol. 29 part 6, p 674-678 (2001).
Bohrer, H., J. Clin. Invest., 972-985 (1997).
Cusack, J.C., et al., Cancer REs 60 2323-2330 (2000).
Brandes, L.M., et al., Mol Pharmacol, 60, 559-567 (2001).
Arlt, A., et al., Oncogene 20 859-858 (2001).
Cusack, J.C., et al., Cancer Res 61 3535-3540 (2001).
Hershenson, F.M.P., Synthesis, 999-1001 (1988).
Consonni, R.C., et al., J. Chem. Res (S) 188-189 (1991).
Bilodeau, M.T.C., J. Org. Chem. 63 2800-2801 (1998).
Puntener, K., et al., J. Org Chem. 65 8301-8306 (2000).
Hsiao, Y.H., J. Org. Chem. 62 3586-3591 (1997).
Dghaym, R.D. D., et al., Angew. Chem. Int. Ed. Engl. 40 3228-3230 (Sep. 2001).
Viso, A., et al., J. Org. Chem. 62 2316-2317 (1997).
M.Karin, Nature Immunology, 3, 221-227 (2002).
Baldwin, J. Clin. Invest., 3, 241-246 (2001), vol. 107.
Huang, T., et al., J. Biol. Chem., 275, 9501-9509 (2000).
Schunk, S., et al., Organic letters 2, 907-910 (2000).
Sain, B., et al., Heterocycles, 23, 1611-1614 (1985).
Peddibhotla, S., et al., Organic Letters 4 3533-3535 (Oct. 3, 2002).

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