Cytotoxic agents

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

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Details

514452, 549510, 549379, C07D30514, A61K 31335

Patent

active

053569288

ABSTRACT:
The invention relates to pharmaceutical compositions comprising an effective cytotoxic amount of: ##STR1## Wherein R represents Ac or H; R' represents: ##STR2## OH; and R" represents: ##STR3## these new compounds demonstrate surprising tubulin binding activity and cytotoxicity.

REFERENCES:
patent: 5200534 (1993-04-01), Rao
Pazdur, R., et al., "Phase I Trial of Taxotere: Five-Day Schedule", Journal of the National Cancer Institute, 1781 (1992).
Rao, Koppaka V., "Taxol and Related Taxanes. I. Taxanes of Taxus brevifolia Bark", Pharmaceutical Research, vol. 10, No. 4, 1993, pp. 521-524.
Georg, G. I., et al., "Synthesis of Biologically Active Taxol Analogs with Modified Phenylisoserine Side Chains", J. Med. Chem., vol. 35: 4230 (1992).
* Applicants do not have a copy of this article. It is cited in the article by Georg, et al., which was co-authored by Himes. Applicants believe it is a duplicate source of the information for which the Georg reference was cited. (See specification at pp. 28 and 29).
Fumoleau, P., et al., "First Line Chemotherapy with Taxotere in Advanced Breast Cancer: A Phase II Study of the EORTC Clinical Screening Group", Proceedings of the American Society of Clinical Oncologists, vol. 12, Mar. 1993, p. 59.
Wanders, J., et al., "The EORTC ECTG Experience with Acute Hypersensitivity Reactions (HSR) in Taxotere Studies", Proceedings of the American Society of Clinical Oncologists, vol. 12, Mar. 1993, p. 73.

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