Progesterone analogs to reverse multidrug resistance

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Cyclopentanohydrophenanthrene ring system doai

Patent

Rate now

  [ 0.00 ] – not rated yet Voters 0   Comments 0

Details

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).

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

Progesterone analogs to reverse multidrug resistance does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Progesterone analogs to reverse multidrug resistance, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Progesterone analogs to reverse multidrug resistance will most certainly appreciate the feedback.

Rate now

     

Profile ID: LFUS-PAI-O-1641243

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