Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1994-02-14
1996-02-27
Jordan, Kimberly
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514859, 514864, A61K 3144
Patent
active
054949149
ABSTRACT:
Inhibitors of testosterone 5.alpha.-reductase activity, for example those of formula: ##STR1## wherein novel substituents are provided at the R.sup.4, R.sup.6, R.sup.7, R.sup.17.alpha. and/or R.sup.17.beta. positions are useful for the treatment of diseases whose progress is aided by activation of androgen receptors, e.g., prostate cancer, benign prostatic hyperplasia, acne, seborrhea, hirsutism, androgenic alopecia and the like.
REFERENCES:
patent: 3001988 (1961-09-01), Nysted
patent: 3300523 (1967-01-01), Brown
patent: 3995060 (1976-11-01), Neri et al.
patent: 4024248 (1977-05-01), Konig et al.
patent: 4055641 (1977-10-01), Benson et al.
patent: 4087461 (1978-05-01), Robinson
patent: 4100274 (1978-07-01), Dutta et al.
patent: 4118483 (1978-10-01), Konig et al.
patent: 4139638 (1979-02-01), Neri et al.
patent: 4161540 (1979-07-01), Neri et al.
patent: 4191759 (1980-03-01), Johnston et al.
patent: 4220775 (1980-09-01), Rasmusson et al.
patent: 4235893 (1980-11-01), Brodie et al.
patent: 4329364 (1982-05-01), Neri et al.
patent: 4377584 (1983-03-01), Rasmusson
patent: 4386080 (1983-05-01), Crossley et al.
patent: 4472382 (1984-09-01), Labrie et al.
patent: 4481190 (1984-11-01), Nestor et al.
patent: 4547493 (1985-10-01), Teutsch et al.
patent: 4634696 (1987-01-01), Teutsch et al.
patent: 4659516 (1987-04-01), Bowler et al.
patent: 4659695 (1987-04-01), Labrie
patent: 4732912 (1988-03-01), Pilgrim et al.
patent: 4751240 (1988-06-01), Bowler et al.
patent: 4760053 (1988-07-01), Labrie
patent: 4760061 (1988-07-01), Edwards et al.
patent: 4822528 (1989-04-01), Columbo et al.
patent: 4859681 (1989-08-01), Rasmusson et al.
patent: 4904661 (1990-02-01), Pilgrim et al.
patent: 4937237 (1990-06-01), Holt et al.
patent: 5021414 (1991-06-01), Pilgrim et al.
patent: 5023234 (1991-06-01), Labrie
patent: 5026882 (1991-06-01), Holt et al.
patent: 5053403 (1991-10-01), Orentreich et al.
patent: 5061801 (1991-10-01), Williams et al.
patent: 5061802 (1991-10-01), Steinberg et al.
patent: 5061803 (1991-10-01), Williams
patent: 5064813 (1991-11-01), Labrie
patent: 5204337 (1993-04-01), Labrie
patent: 5237064 (1993-08-01), Bakshi et al.
Voigt et al., Endo, (1973), 92(4), pp. 1216-1922.
Green et al., Nature, 320(13) Mar. 1986, pp. 134-139.
Lubahn et al., Science, (1988) 240 pp. 327-330.
Lubahn et al. Proc. Natl Acad. Sci. USA 86, 9534-9538, Dec. 1989.
Neri et al., J. Steroidal Biochem., 1975, (6), pp. 815-819.
Chang, et al., Biochemistry, 1982, 21(17) 4302-4109.
Gyorki, et al., J. Steroidal Biochem. 25(3), 355-358, 1986.
Macaulay, et al., J. Steroidal Biochem. 26(5) 535-538, 1987.
Grunwell, et al., Steroids, 27(6), 1976, pp. 759-771.
Chin, et al., J. Biol. Chem., 250(19), 1975, pp. 1682-1686.
Auchus et al., Biochemistry, 1986, 25, 7295-7300.
Schwarz, Organic Synthesis Collective, vol. 3: 332-333 (1955).
Cooke, Jr.., Tetrahedron Letters, 22 pp. 1983-1986, 191.
Gibson, et al., Angew Chem. Int. Ed. 7 (1968) No. 12, pp. 919-930.
Raucher, et al., J. Org. Chem., 1981, 46, 3558-3559.
Weiss, et al., Angew Chem. Int. Ed. 12 (1973) No. 10, p. 841.
Bull, et al., Chem. Soc. Chem. Commun. 1986, pp. 451-453.
Wang, et al., Can J. Chem., 65, 2121-2131, 1987.
Jordan, et al., Endocrinology, 124 (4), 1989, pp. 1717-1726.
Musto, et al., Endo. Res. Comm. (1977), vol. 4, No. 2, pp. 141-158.
Solo, et al., Steroids, vol. 40, No. 6 (1982), pp. 603-614.
De Larminat, et al., The Prostate, vo. 5 (1984), pp. 123-140.
Beardwell, et al., (1983) Cancer Chemother. Pharmacol. 10, No. 3, 158-160.
Brooks, et al., (1982) The Prostate, 3, No. 1, 35-44.
Bruchovsky, et al., (1968) J. Biol. Chem. 243, No. 8, 2012-2021.
Coy, et. al., (1982) Endocrinology, 110, 1445-1447.
Debruyne, F. (1988) Bailliere's Clin. Oncol. Int'l. Practice & Res., pp. 559-570.
Gohring et al., World Patent Information, vol. 11, No. 1., pp. 5-10, 1988.
Salman, et al., J. Steroid Biochem, vol. 33, No. 1, pp. 25-31 (1989).
Lefebvre, et al. Prostate 1982, 3(6), 569-578.
Lee et al., Steroids 22, 677-685, 1973.
Mobbs, et al., 71th An. Meeting of the Endocrine Soc., No. 1410, 1989.
Mobbs et al., J. Steroidal Biochem., 19(3), 1279-1290, 1983.
Donnelly, "Continuous Subcutaneous Administration of `Zoladex` (ICI 118,630--An LH-RH Analogue) to Patients with advanced Prostatic Cancer", ICI Pharmaceuticals Division, Macclesfield, U.K., 1988.
Tora, et al. EMBO 8(7) 1981-1986, 1989.
Nayfeh, et al., Steroids 14:3, 1969, pp. 269-283.
Luthy, et al., J. Steroid Biochem. 31(5) 845-52, 1988.
Labrie, et al., The Prostate, 4, 579-594, 1983.
Begin, et al., Molecular and Cellular Endocrinology, 58 (1988) 213-219.
Lee et al., J. Androl. 2(6) 293-299, 1981.
Belis et al., J. Androl. 4, 144-149, 1983.
Schally, et al., Cancer Treatment Reports, 68(a), 281-288 (1984).
Levesque, et al., J. Med. Chem. 1991, 34 1624-1630.
Santen, et al. LHRH and Its Analogues, MTP Press, pp. 351-364, (1984).
Labrie et al., J. Steroid Biochem. 19(1) 999-1007, 1983.
Labrie, et al., (1984) 7th International Congress of Endocrinology 1984, p. 98.
Lambert, et al., (1986) Ann. Clin. Biochem., 23, 225-229.
Potts, et al., (1978) Steroids, 32, No. 2, 257-267.
Wilson, J. (1975) Handbk of Physio., Sec. 7, Endo. V, Amer. Physio. Soc. pp.491-508.
Farnsworth, W. E. (1969) Investigative Urology, 6, No. 4, 423-427.
Groom, et al., (1971) Biochem. J., 122, 125-126.
Geller, et al., (1989) 71st Ann. Endo. Soc. Meet. (Seattle, 6/21-24). No. 1640, p. 432.
Gormley, et. al., (1989) 71st Ann. Endo. Soc. Meet. (Seattle, 6/21-24). No. 1225, p. 329.
Wagner, et al., (1975) Acta Endocr. (Kbh), Suppl. 193, 52 (abst).
Robinson, et al., (1984) J. Steroid Biochem., 21, No. 5, 601-605.
Swaneck, et al., (1982) Biochem. Biophysical Res. Comm., 106, No. 4, 1441-1447.
Petrow, et al., (1982) J. Endocr., 95, 311-313.
Kadohma, et al., (1985) J. Natl. Cancer Inst., 74, No. 2, 475-486.
Earnshaw, et al., (1984) Clin. Invest., 21, 13-21.
Corbin, et al., (1984) J. Steroid Biochem., 20 (6B), 1369, No. A9.
Dutta et al., (1978) J. Med. Chem., 21, No. 10, 1018-1024.
Erchegyi, et al., (1981) Blochem. & Biophysical Res. Comm. 100, No. 3, 915-920.
Nestor, et al., (1984) J. Steroid Blochem., 20 (6B), 1366, No. A3.
Faure, et al., LHRH and Its Analogs, pp. 337-349, 1988.
Walsh, et al., The Journal of Clinical Investigation, vol. 57, Apr. 1976, pp. 1093-1097.
Brooks, et al. Proc. of the Soc. for Exp. Biology and Medicine, 169, 67-73 (1982).
George, et al., "The Effect of A 5-.alpha.-Reductase Inhibitor on Androgen Physiology in the Prepubertal Male Rat", 1165, Department of Cell Biology and Anatomy, University of Texas Southwestern Medical Center, Dallas, TX 75235, 1988.
Tenover, et al., "Effects of 24-Week Administration of a 5.alpha.-Alpha Reductase Inhibitor (MK-906) on Serum Levels of Testosterone (T), Free T, and Gonadotropins in Men", 583, Department of Medicine, University of Washintton, Seattle, WA 98103, 1988.
Liang, et al., Endocrinology, vol. 112, No. 4, pp. 1460-1468, 1988.
Sharpless, et al., Tetrahedron Letters, 1979 (1973).
Riess, Institut de Chimie. Strasbourg, France (Jul. 31, 1964).
Fujimoto, J. Pharm. Soc. Jap, 87:270 (1967).
Toth, et al. (1982) J. Steroid Biochem 17:653-660.
Junkmann, K. (1957) Recent Progr. Horm. Res., 13:1389-1427.
Weinbauer, et al. (1986) Acta Endocrinologica 113:128-132.
Seguin, et. al. Mol. Cell. Endocrinol., 21, 37-41 1981.
Neumann et al., In: Clinics in Oncology, vol. 1, pp. 41-64, 1982.
Simard, et al., Mol. Cell. Endocrinol., 44, 261-270, 1986.
Poyet and Labrie, Mol. Cell. Endocrinol., 42, 283-288, 1985.
Furr, et al. J. Endocr., 113, R7-R9, 1987.
Labrie, et al., Important Advances in Oncology, Philadelphia, pp. 193-217, 1985.
Wakeling, et al. J. Endocr., 112, R7-R10, 1987.
Wakeling, et al. J. Steroid Biochem., 30, 141-147, 1987.
Bhatnager, et al. Biol. Chem. 253, 811-815, 1978.
Chin, et al. J. Biol. Chem., 255, 3660-3664, 1980.
Thomas, et al. J. Biol. Chem., 258, 1587-1590, 1983.
Tobias, et al. J. Biol. Chem., 257, 2783-2786, 1982.
Thomas, et al. J. Biol. Chem., 258, 11500, 1983.
Labrie, et al. Endocrinology 123: 1412-1417, 1988.
Plante, et al., J. Steroid Biochem., 31(1), 61-64 (1988).
Rivier, et al., LHRH Analogs as Antiovulator
Labrie Fernand
Merand Yves M.
Singh Shankar M.
Endorecherche
Jordan Kimberly
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