Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Cyclopentanohydrophenanthrene ring system doai
Patent
1996-06-21
2000-11-07
Dees, Jose' G.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Cyclopentanohydrophenanthrene ring system doai
552523, A61K 3157, C07J 3100
Patent
active
061437379
ABSTRACT:
The present invention is directed to compounds of formula I ##STR1## wherein the substituents are as defined in the specification. Also disclosed are compositions and method of use of the compounds.
REFERENCES:
patent: 3816624 (1974-06-01), Davis et al.
patent: 3998829 (1976-12-01), Phillips et al.
Beyer et al., "Synthesis of potential antiprogestins II", Steroids, vol. 35(5), pp. 481-488, 1990.
Brueggemeier et al., "Biochemican and pharmacological development of steroidal inhibitors of aromatase", J. Steroid Biochem. Molec. Biol., vol. 37(3), pp. 379-385, 1990.
Berenbaum, M.C., "Synergy, additivism, and antagonism in immunosuppression," Clin. Exp. Immunol. 28:1-18 (1977).
Berenbaum, M.C., "The Expected Effect of a Combination of Agents: the General Solution," J. Theor. Biol. 114:413-431 (1985).
Berenbaum, M.C., "What is Synergy?" Pharmacol. Rev. 41:93-141 (1989).
Bourgain, C. et al., "Human endometrial maturation is markedly improved after luteal supplementation of gonadotropin-releasing hormone analogue/human menopausal gonadotropin stimulated cycles," Human Reproduction 9:32-40 (Jan. 1994).
Brueggemeier, R.W. & Katlic, N.E., "Effects of the Aromatase Inhibitor 7.alpha.-(4'-Amino)phenylthio-4-androstene-3,17-dione in MCF-7 Human Mammary Carcinoma Cell Culture," Cancer Research 47:4548-4551 (1987).
Brueggemeier, R.W. et al., "Biochemical and Pharmacological Development of Steroidal Inhibitors of Aromatase," J. Steroid Biochem. Molec. Biol. 37:379-385 (1990).
Clarke, R. et al., "Effect of P-glycoprotein Expression on Sensitivity to Hormones in MCF-7 Human Breast Cancer Cells," J. Natl. Cancer Inst. 84:1506-1512 (1992).
Clarke, R. & Lippman, M., "Acquisition of Antiestrogen Resistance in Breast Cancer," Drug Resistance in Oncology, Teicher, B.A., ed. Marcel Dekker, Inc., New York (1992) pp. 501-536.
Escriba, P. et al., "Role of Membrane Lipids in the Interaction of Daunomycin with Plasma Membranes from Tumor Cells: Implications in Drug-Resistance Phenomena," Biochemistry 29:7275-7282 (1990).
Fleming, G.F. et al., "Megestrol acetate reverses multidrug resistance and interacts with P-glycoprotein," Cancer Chemother. Pharmacol. 29:445-449 (1992).
Gruol, D.J. et al., "Reversal of Multidrug Resistance by RU 486," Cancer Research 54:3088-3091 (Jun. 1994).
Gulino, A. et al., "Calmodulin Antagonism and Growth-inhibiting Activity of Triphenylethylene Antiestrogens in MCF-7 Human Breast Cancer Cells," Cancer Research 46:6274-6278 (1986).
Ichikawa-Haraguchi, M. et al., "Progesterone and its metabolites: the potent inhibitors of the transporting activity of P-glycoprotein in the adrenal gland," Biochimica et Biophysica Acta 1158:201-208 (1993).
Kessel, D., "Interactions among membrane transport systems: anthracyclines, calcium antagonists and anti-estrogens," Biochem. Pharmacol. 35:2825-2826 (1986).
Lecureur, V. et al., "The antiprogestatin drug RU 486 potentiates doxorubicin cytotoxicity in multidrug resistant cells through inhibition of P-glycoprotein function," FEBS Letters 355:187-191 (Oct. 1994).
Lehnert, M. et al., "Identification of Agents for Clinical Reversal of Multidrug Resistance," Eur. J. Clin. Invest. 22:A38, No. 214 (1992).
Leonessa, F. et al., "Effect of Tamoxifen on the Multidrug-resistant Phenotype in Human Breast Cancer Cells: Isobologram, Drug Accumulation, and M.sub.r 170,000 Glycoprotein (gp170) Binding Studies," Cancer Research 54:441-447 (Jan. 1994).
Loewe, S. "Antagonisms and Antagonists," Pharmacol. Rev. 9:237-242 (1957).
Piekarz, R.L. et al., "Progesterone Regulates the Murine Multidrug Resistance mdr1b Gene," J. Biol. Chem. 268:7613-7616 (1993).
Reichstein, T. & Montigel, C., "Uber Bestandteile der Nebennierenrinde und verwandte Stoffe. Einwirkung von Bleitetra-acetat auf Allopregnanolon-acetat, Pregnenolon-acetat und Progesteron," Helv. Chim. Acta. 22:1212-1259 (1939).
Wang, L. et al., "Reversal of the Multidrug Resistance (MDR) Phenotype with Megestrol Acetate (MA)," Proceedings of the American Association for Cancer Research 32:377, No. 2239 (1991).
Yang, C.-P. H., et al., "Progesterone Interacts with P-Glycoprotein in Multidrug-resistant Cells and in the Endometrium of Gravid Uterus," J. Biol. Chem. 264:782-788 (1989).
Clarke Robert
Ghiorghis Alem
Hammer Charles
Leonessa Fabio
Talebian Abdel H.
Badio Barbara
Dees Jos,e G.
Georgetown University
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