Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1999-03-31
2000-08-01
Chang, Ceila
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514322, 546198, 546199, A61K 31445
Patent
active
060967633
ABSTRACT:
This invention relates to novel compounds, their synthesis and use as selective .alpha..sub.1a adrenergic receptor antagonists. One application of the compounds is in the treatment of benign prostatic hyperplasia. The compounds are selective in their ability to relax smooth muscle tissue enriched in the .alpha..sub.1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia are achieved.
REFERENCES:
patent: 3982001 (1976-09-01), Heffe et al.
patent: 4066722 (1978-01-01), Vandenberk et al.
patent: 4110449 (1978-08-01), Wade et al.
patent: 4470989 (1984-09-01), Henning et al.
patent: 4980365 (1990-12-01), Davis
patent: 5008264 (1991-04-01), Davis
patent: 5064840 (1991-11-01), Carr et al.
patent: 5141930 (1992-08-01), Nakao et al.
patent: 5143923 (1992-09-01), Hrib et al.
patent: 5192775 (1993-03-01), Malen et al.
patent: 5229399 (1993-07-01), Malen et al.
patent: 5232931 (1993-08-01), Prucher et al.
patent: 5262418 (1993-11-01), Van Daele et al.
patent: 5280030 (1994-01-01), Jegham et al.
patent: 5371094 (1994-12-01), Heine et al.
patent: 5403847 (1995-04-01), Gluchowski et al.
patent: 5462942 (1995-10-01), Hartog et al.
Elde et al. "Distribution of neuropeptide receptors . . . " Medline 95336119, 1995.
A. F. Casey, "Opioid Receptors and their Ligands: Recents Developments", Advances in Drug Research, vol. 18, pp. 179-285, (1989).
J. M. Wetzel et al., "Discovery of Alpha 1a Adrenergic Receptor Antagonists based on the L-Type . . . ", Journal of Medicinal Chemistry, vol. 38, No. 10, pp. 1579-1581, (1995).
C. Chapple, "Medical treatment for benign prostatic hyperplasia: surgery still gives the best results", British Medical Journal, vol. 304, No. 6836, p. 1198(2), May 9, 1992.
T. Resine et al., "Opioid Analgesics and Antagonists", Goodman and Gilman's The Pharmaceutical Basis of Therapeutics, pp. 521-555, (1995).
Chang Raymond S. L.
Hoffman Jacob M.
Chang Ceila
Merck & Co. , Inc.
Walton Kenneth R.
Winokur Melvin
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