Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1992-08-07
1994-04-12
Daus, Donald G.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
514183, 514213, 514218, 514219, 5142222, 5142242, 5142245, 5142295, 514243, 514248, 514253, 514257, 514279, 514280, 514281, 514375, 514410, 540468, 540471, 540476, 540488, 540492, 540576, 544 14, 544 89, 544 99, 544125, 544233, 544245, 544342, 544361, 546 14, 546 38, 546 42, 546 77, 548217, 548419, 548420, 549333, A61K 31435
Patent
active
053025890
ABSTRACT:
The present invention relates to certain substituted 17 .beta.-substituted carbonyl-6-azaandrost-4-en-3-ones of formula (I): ##STR1## wherein R.sup.1 and R.sup.2 are
REFERENCES:
patent: 3138584 (1964-06-01), Zderic
patent: 4191759 (1980-03-01), Johnston et al.
patent: 4361578 (1982-11-01), Alig et al.
patent: 4377584 (1983-03-01), Rasmusson et al.
patent: 4882319 (1989-11-01), Holt et al.
patent: 4888336 (1989-12-01), Holt et al.
patent: 4937237 (1990-06-01), Holt et al.
patent: 5017568 (1991-05-01), Holt et al.
patent: 5061801 (1991-10-01), Williams et al.
patent: 5061802 (1991-10-01), Steinberg et al.
patent: 5061803 (1991-10-01), Williams et al.
patent: 5098908 (1992-03-01), Steinberg et al.
patent: 5110939 (1992-05-01), Holt et al.
Diani et al. Jour. Clin. Endoc. vol. 74, pp. 345-350 (1992).
Helliker, Wall St. Jour., Jun. 7, 1991 pp. A1, A7.
Stinson, Chem. & Eng. News, Jun. 7, 1992, pp. 7-8.
Hsia, et al, J. Invest. Derm., 1974, pp. 224-227.
Robaine, et al, J. Steroid Biochem., 8, 1977, pp. 307-310.
Petrow, et al, Steroids, 38, 1981, pp. 121-140.
Lian, et al, J. Steroid Biochem., 19, 1983, p. 395.
Holt, et al, J. Med. Chem., 33, 1990, 937-942, "Steroidal A Ring Aryl Carboxylic Acids: A New Class of Steroid 5.alpha.-Reductase Inhibitors".
Stoner, et al, J. Steroid Biochem. Molec. Biol., 37, 1990, pp. 375-378.
Brooks, et al, Steroids, 47, 1986, pp. 1-19.
Velthuysen, et al, Tetrahedron Letters, 27, 1966, 3081-3086, "Synthesis of (.+-.)-N-Methyl-6-aza-8(14)-dehydro-19-nor-testosterone".
Speckamp, et al, Tetrahedron, 24, 1968, 5893-5898, "The Synthesis of N-Methyl-6-Aza-8(14)-Dehydro-19-Nor-Testosterone".
Kutney, et al, Candian J. of Chem., 41, 1963, 613-619, "Synthesis of 6-Aza Steroids--A Novel Class of Azaandrostane Analogues".
Sampson, et al, Biochimica et Biophysica Acta, 960, 1988, 268-274, "The Efects of 6-Azacholest-4-en-3.beta.-ol-7-one, an Inhibitor of Cholesterol 7.alpha.-Hydroxylase, on Cholesterol Metabolism and Bile Acid Synthesis in Primary Cultures of Rat Hepatocytes".
Kutney, et al, Tetrahedron, 24, 1968, 845-857, "Synthesis of Ring A-Oxygenated 6-Aza Steroids".
Brown, et al, J. Chem. Soc., 1987, 595-599, "The Synthesis of Some Cholesterol Derivatives as Probes for Mechanisms of Cholesterol Metabolism".
Jacobs, et al., 1960, 4033-4039, "The Introduction of Oxyen and Bitrogen into the B Ring of the Steroid Nucleus".
Speckamp, et al, Tetrahedron, 24, 1968, 5881-5891, "Synthesis of N-Methyl and N-Ethyl-6-Aza-8(14)-Dehydroestrone Methyl Ether".
Hugl, et al, Tetrahedron, vol. 29, 1973, 759-767, "Umsetzungen Von .DELTA..sup.5 -Steroidolefinen Mit Pb(OAc).sub.4-n (N.sub.3).sub.n.sup.1 ".
Kutney, et al, Chem. and Ind, 1961, 1713-1714, "Synthesis of 6-Aza-Steroids: A Novel Class of Steroidal Hormones".
Rasmusson, et al, J. Med. Chem, 29, 1986, 2298-2315, "Steroids: Structure-Activity Relationships for Inhibition of 5.alpha.-Reductase and Androgen Receptor Binding".
H. Lettre et al., Liebig's Ann. Chem, 703, 1967, 147-151, "Verbesserung der Darstellung von 6-Aza-Steroiden".
Rasmusson, et al, J. Med. Chem., 27, 1984, 1690-1701, "Azasteroids as Inhibitors of Rat Prostatic 5.alpha.-Reductase".
Imperato-McGinley, et al, TIG, 1986, 130-133, "Inherited 5.alpha.-Reductase Deficiency in Man".
Jones, et al, British J. of Urology, 66, 1990, 506-508, "Origin and Structure of Benign Prostatic Hyperplasia".
Bhattacharya, et al, Synthetic Communications, 30(17), 1990, 2683-2690, "Acylimidazolides as Versatile Synthesis Intermediates for the Preparation of Sterically Congested Amides and Ketones: A Practical Synthesis of Proscar.RTM.".
Fang Francis G.
Frye Stephen V.
Middlemiss David
Daus Donald G.
Glaxo Inc.
Joyner Charles T.
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