19-norbufalin derivatives, their preparation and...

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

Reexamination Certificate

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C514S174000, C540S094000

Reexamination Certificate

active

07087590

ABSTRACT:
A 19-norbufalin derivative compound of formula (I):wherein the R groups are as defined by the present specification. The compounds are Na+K−-ATPase inhibitors and can be used in the treatment of cardiac and/or vascular malfunction, renal malfunction, as digoxin antagonists, for treatment of CNS disorders and for the treatment of malignant and proliferative cell diseases.

REFERENCES:
patent: 5874423 (1999-02-01), Lichtstein et al.
patent: WO-94/05305 (1994-03-01), None
Bohl, et al., “Quantitative Structure-Activity Relationships Of Cardiotonic Steroids Using Empirical Molecular Electrostatic Potentials And Semiempirical Molecular Orbital Calculations”, J. Steroid Biochem., vol. 21, No. 4, pp. 373-379, 1984.
Sen, et al., “A Simple And Efficient Synthesis of Bufalin”, J. Chem. Commun., pp. 1213-1214, 1982.
Tsai, et al., “On Cardioactive Steriods.IX. The Conversion Of Digitoxigenin To Bufalin”, Can. J. Chem., vol. 60, pp. 2161-2163, 1982.
Wiesner, et al., “On Cardioactive Steriods. XII. The Synthesis Of (Natural) Bufalin And x'-Isobufalin”, Helvetica Chimica Acta, vol. 66, Fasc. 8, pp. 2632-2640, 1983.
Wiesner, et al., “On Cardioactive Steriods. VIII. The Synthesis Of Bufalin And Resibufogenin Isomers”, Helvetica Chimica Acta, vol 65, Fasc 7, pp. 2049-2060, 1982.
Han, et al., “Neurosteroids Analogues. 4. The Effect Of Methyl Substitution At The C-5 and C-10 Positions of Neurosteroids On Electrophysiological Activity at GABAa”, J. Med.Chem., vol. 39, pp. 4218-4232, 1996.
Tsai, et al., “A Simple Synthesis Of Cardenolides And Their Less Toxic Isomers Via Furyl Intermediates”, Heterocycles, vol. 12, No. 11, pp. 1397-1402, 1979.
Lichtstein, et al., “Identification Of Digitalis-like Compounds in Human Cataractous Lenses”, Eur. J. Biochem., vol. 216, pp. 261-268, 1993.
Sondheimer, et al., “Synthesis Of Bufadienotides. The Synthesis Of Bufalin And Resibufogenin”, J. Am.Chem. Soc., vol. 91, No. 5, pp. 1228-1230, 1969.
Stache, et al., “Synthesen Von Bufadienoliden Synthese Von Scillarenin”, Tetrahedron Letters, No. 35, pp. 3033-3038, 1969.
Pettit, et al., Synthesis Of buf-20(21)-enlides And bufa-20,22-dienolides, Can. J. of Chem., vol. 47, pp. 2511-2513, 1969.
Pettit, et al., “Bufadienolides. 1. Introduction and Base-Catalyzed Condensation of Methyl Ketones With Glyoxylic Acid”, J. of Org. Chem., vol. 35, No. 5, pp. 1367-1376, 1970.
Almirante, et al., “Stereoselective Synthesis of New Digitalis-like Perhydroindene Derivatives From The Hajos-Parrish Ketone”, Synlett, 22, pp. 1234-1236, 1998.
Wiesner, et al., “Some Resent Progress In The Synthetic And Medicinal Chemistry Of Cardioactive Steroid Glycosides”, Pure & Appl. Chem., vol. 58, No. 5, pp. 799-810, 1986.
Di-Capua, et al., “Mass Spectral Determination Of the Configuration Of 17β-Tetrahydropranloxy-19-norandrostan-3β-ol”, Int. J. Mass. Spectrom, 167/168, pp.
Han, et al., “An Improved Synthesis Of 18-Nor-ketosteroids And Application Of The Method For The Preparation Of (3b,5b,13b)-3-Hydroxygonan-17-one”, J. Org. Chem., vol. 61. pp. 7614-7616, 1996.
Somay, et al., “Synthese de bromofurannes et de derives furanniques mono et disubstitues”, Bull. Soc. Chem., No. 3, pp. 990-1000, 1971.
Chiarello, et al., “Synthetic Routes To Cristatic Acid And Derivatives”, Tetruhedron, vol. 44, No. 1, pp. 41-48, 1988.
Kelly, et al., “Pharmacological Treatment Of Heart Failure”, Goodman & Gilman's The Pharmacological Basis of Therapeutics, 8th ed., pp. 809-838, 1990.
Zhang, et al., “Induction by Bufalin Of Differentiation Of Human Leukemia Cells HL60, U937 and ML1 Toward Macrophage/Monocyte-like Cells And its Potent Synergistic Effect On The Differentiation Of Human Leukemia Cells In Combination with Other Inducers”, Cancer research 52, pp. 4634-4641, 1992.
Numazawa, et al., “A Cardiotonic Steroid Bufalin-Induced Differentiation Of THP-1 Cells”, Biochem. Pharma., vol. 52, pp. 321-329, 1996.
Watabe, et al., “The Cooperative Interaction Of Two Different Signaling Pathways In Response To Bufalin induces Apoptosis In Human Leukemia U937 Cells”, J. Bio.Chem., vol. 271, Issue of Jun. 14, pp. 14067-14073, 1996.

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