Use of 1c specific compounds to treat benign prostatic hyperplasia
Patent 5780485 Issued on July 14, 1998. Estimated Expiration Date: July 14, 2015. Estimated Expiration Date is calculated based on simple USPTO term provisions. It does not account for terminal disclaimers, term adjustments, failure to pay maintenance fees, or other factors which might affect the term of a patent.
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A method of treating benign prostatic hyperplasia in a subject which comprises administering to the subject a therapeutically effective amount of a compound which binds to a human adrenergic receptor with a binding affinity greater than ten-fold higher than the binding affinity with which the compound binds to a human adrenergic receptor, a human adrenergic receptor, and a human histamine H1 receptor, and, binds to a human 댒 adrenergic receptor with a binding affinity which is greater than ten-fold lower than the binding affinity with which the compound binds to such adrenergic receptor. Compounds meeting these criteria are provided.
Other References
Forray, C., et al. "The 1C -Adrenergic Receptor that Mediates Smooth Muscle Contraction in Human Prostate Has the Pharmacological Properties of the Cloned Human 1c Subtype," Molecular Pharmacology, 45, 703-708 (1994); U.S.A. (Exhibit 3)
Forray, C., Chiu, G., et al. Effects of Novel Alpha-1C Adrenergic Receptor Antagonists on the Contraction of Human Prostate Smooth Muscle, American Urological Association Eighty-Ninth Annual Meeting, May 14-19, 1994, The Journal of Urology, 151(5), Abstract #159 (May 1994); U.S.A. (Exhibit 4)
Forray, C., Bard, J.A., et al. "Comparison of the Pharmacological Properties of the Cloned Bovine, Human, and Rat 1C -Adrenergic Receptors," The FASEB Journal, 8(4), Abstract #2042 (1994) U.S.A. (Exhibit 5)
Gong, G., et al. 1C -Adrenergic Antagonists and Orthostatic Hypotension in the Rat, The FASEB Journal, 8(4), Abstract #2043 (1994); U.S.A. (Exhibit 6)
Lepor, H., et al. "Localization of Alpha1c Adrenoceptor (1C AR) Subtypes in the Human Prostate," American Urological Association Eighty-Ninth Annual Meeting, May 14-19, 1994, The Journal of Urology, 151(5), Abstract #614 (May 1994); U.S.A. (Exhibit 7)
Perez, J.-L., et al. "Is the 1C -Adrenergic Receptor the 1A -Subtype?" The FASEB Journal, 8(4), Abstract #2041 (1994); U.S.A. (Exhibit 8)
Tang, R., et al. "Localization of Alpha 1C Adrenoceptor (1C AR) Subtypes in the Human Prostatic Tissue," The FASEB Journal, 8 (5), Abstract #5070 (1994); U.S.A. (Exhibit 9)
Wetzel, J.M., et al. "Structural and Functional Studies of the Human 1C Adrenergic Receptor: The Orientation of Transmembrane Helix 5," The FASEB Journal, 8(4), Abstract #2182 (1994); U.S.A. (Exhibit 10)
Archibald, J.L. et al., "Antihypertensive Ureidopiperidines," Journal of Medicinal Chemistry (1980), vol. 23, pp. 857-861
Boer, R. et al., "(+)-Niguldipine binds with very high affinity to Ca2+ channels and to a subtype of 1 -adrenoreceptors," European Journal of Pharmacology--Molecular Pharmacology Section (1989), vol. 172, pp. 131-145
Gup, D.I. et al., "Autonomic Receptors in Human Prostate Adenomas," Journal of Urology (1990), vol. 143, pp. 179-185
Hieble, J.P. et al., "In vitro characterization of the 1 -adrenoreceptors in human prostate," European Journal of Pharmacology (1985), vol. 107, pp. 111-117
Lepor, H. and Baumann, M. et al., Medline Abstracts (1988), Abst. No. 88317114, "The Alpha Adrenergic Binding Properties of Terazosin in the Human Prostate Adenoma and Canine Brain," Journal of Urology (1988), vol. 140(3), pp. 668-671
Lepor, H. and Knapp-Maloney, G. et al., "A Dose Titration Study Evaluating Terazosin, A Selective, Once-A-Day 댑-Blocker for the Treatment of Symptomatic Benign Prostatic Hyperplasia," Journal of Urology (1990), vol. 144, pp. 1393-1398
Lepor, H. and Shapiro, E. et al., Medline Abstracts (1988), Abst. No. 88317113, "The Effect of Electrocautery on Neurotransmitter Receptor Binding Assays in the Canine Prostate," Journal of Urology (1988), vol. 140(3), pp. 664-667
Lomasney, J.W. et al., "Molecular Cloning and Expression of the cDNA for the 1A -Adrenergic Receptor," Journal of Biological Chemistry (1991), vol. 266, pp. 6365-6369
Marshall, I. et al., "Human Alpha1C -Adrenoceptor: Functional Characterization In Prostate," Meeting of the British Pharmacological Society (1992), Abst. No. C97
Ramarao, C.S. et al., "Genomic Organization and Expression of the Human 1B -Adrenergic Receptor," Journal of Biological Chemistry (1992), vol. 267, pp. 21936-21944
Yamada, S. et al., "1A -Adrenergic Receptors in Human Prostate: Characterization and Alteration in Benign Prostatic Hypertrophy," Journal of Pharmacology and Experimental Therapeutics (1987), vol. 242, pp. 326-330
Chemical Abstracts and 1988:563185, Kaminka et al, 1988
Chemical Abstracts and 1987:513718, Yamada et al, 198
July 14, 2015. Estimated Expiration Date is calculated based on simple USPTO term provisions. It does not account for terminal disclaimers, term adjustments, failure to pay maintenance fees, or other factors which might affect the term of a patent.
