Ad: The HairMax Laser Comb

Ad: Hair2Go.com Ad: Revivogen	Ad: LuxuryBarber.com
Substituted 3-phenanthridinone derivatives as 5-alpha-reductase inhibitors United States Patent 5,621,104 Graham, et. al. Apr. 15, 1997 Substituted 3-phenanthridiNone derivatives as 5-alpha-reductase inhibitors useful in the prevention and treatment of hyperandrogenic disorders

Related U.S. Application Data

References Cited | [Referenced By:]

U.S. Patent Documents

Foreign Patent Documents

Other References

Campbell et al., Syn. Commun. (1979), vol. 9, pp. 471-476, "A Novel Synthesis . . . : An Intermediate Useful in Terpene Synthesis".

Vila et al., Tet. Letters (1989), vol. 45, pp. 4951-4960, "Conformational Analysis of the 4a-Methyl Octahydrophenanthrene System".

Iida et al., Heterocycles (1983), vol. 20, pp.227-230, "A New Synthesis of Phenanthridine Derivatives".

Schultz et al., J. Am. Chem. Soc. (1978), vol. 100, pp. 2140-2149, "Heteroatom Directed Photoarylation. Synthetic Potential of the Heteroatom Sulfur".

Neri et al., Endo. (1972), vol. 91, No. 2, pp. 427-437, "A Biological Profile of a Non-steroidal Antiandrogen, SCH 13521 . . . ".

Nayfeh et al., Steroids, vol. 14 (1969), pp. 269-283, "Metabolism of Progesterone by Rat Testicular Homogenates-III".

Voight et al., Endo., vol. 92 (1973), p.1216, "The Antiandrogenic Action of 4-Androsten-3-one-17beta-Carboxylic Acid and its Methyl Ester on Hamster Flank Organ".

Doorenbos et al., J. Pharm. Sci., vol. 62, No. 4 (1973), pp. 638-640, "Synthesis & Antimicrobial Properties of 17Beta-Isopentyloxy-4-Aza-5 Alpha-Androstane and the 4-Methyl Derivative".

Doorenbos et al., J. Pharm. Sci., vol. 60, No. 8 (1971), pp. 1234-1235, "4,17 Alpha-Dimethyl-4-Aza-5 Alpha-Androstan-17 beta-ol Acetate & Related Azasteroids".

Doorenbos et al., J. Pharm. Sci., vol. 63, No. 4 (1974), pp. 620-622, "Synthesis & Evaluation of Antimicrobial Properties of Amidinoazaandrostanes and Guanidinoazaandrostanes".

Rasmusson et al., J. Med. Chem., vol. 29, No.11 (1986), pp. 2298-3115, "Aza Steroids: Structure-Activity Relationships . . . ".

Brooks et al., Prostate, vol. 9, No. 1 (1986), pp. 65-75, "Prostatic Effects Induced in Dogs by . . . 5 alpha-Reductase Inhibitors".

Brooks et al., Steroids, vol. 47, No. 1 (1986), pp. 1-19, "5 Alpha-Reductase Inhibitory . . . Activities of Some 4-Aza-Steroids in the Rat".

Liang et al., Endo., vol. 117, No. 2, (1986), pp. 571-579, "Species Differences in Prostatic Steroidal 5 Alpha-Reductases of Rat, Dog and Human".

Rasmusson et al., J. Med. Chem., vol. 27, No. 12 (1984), pp. 1690-1701, "Azasteroids as Inhibitors of Rat Prostatic 5 Alpha-Reductase".

Back et al., J. Org. Chem, vol. 46, No. 7 (1981), pp. 1442-1446, "N-Chloroazasteroids . . . ".

Liang et al., Chem. Abstracts, vol. 95, 109055j, "Inhibition of 5-Alpha-Receptor Binding . . . by a 4-Methyl-4-Aza-Steroid" (1985).

Kadohama et al., JNCL, vol. 74, No. 2 (Feb. 1985), pp. 475-481, "Retardation of Prostate Tumor Progression in the Noble Rat by 4-Methyl-4-Aza-Steroidal Inhibitors of 5 Alpha-Reductase".

Andriole et al., The Prostate, vol. 10 (1987), pp. 189-197, "The Effect of 4MA . . . on the Growth of . . . Human Tumors . . . ".

Bingham et al., J. Endocr., vol. 57 (1973), pp. 111-121, "The Metabolism of Testosterone by Human Male Scalp Skin".

Kedderis et al., Toxicol. Appl. Pharmacol., vol. 103 (1990), pp. 222-227, "Studies with Nitrogen-Containing Steroids . . . ".

Metcalf et al., Bioinorganic Chemistry, vol. 17 (1986), pp. 372-376, "Patent Inhibition of Human Steroid . . . by 3-Androstene-3-Carboxylic Acid".

Levy et al., Biochemistry, vol. 29 (1990), pp. 2815-2824, "Inhibition of Rat Liver Steroid 5 Alpha-Reductase . . . ".

Holt et al., J. Med. Chem., vol. 33 (1990), pp. 943-950, "Steroidal A Ring Carboxylic Acids . . . ".

Levy et al., J. Steroid Biochem., vol. 34, No. 1-6 (1989), pp. 571-575, "Interaction Between Rat Prostatic 5 Alpha-Reductase . . . ".

Holt et al., J. Med. Chem., vol. 33 (1990), pp. 937-942, "Steroidal A Ring Aryl Carboxylic Acids . . . ".

Metcalf et al., TIPS (Dec. 1989), vol. 10, pp. 491-495, "Inhibitors of . . . 5 Alpha-Reductase in Benign Prostatic Hyperplasia . . . ".

Murphy et al., Steroids, vol. 35, No. 3 (Mar. 1980), pp. 1-7, "Effect of Estradiol on a . . . Binding Protein in the Uterus of the Mouse".

Stone et al., Prostate, vol. 9 (1986), pp. 311-318, "Estrogen Formation in Human Prostatic Tissue . . . ".

Brooks et al., Steroids, vol. 47, No. 1 (1986), pp. 1-19, "5 Alpha-Reductase Inhibitory . . . Activities of Some 4-Azasteroids . . . ".

Labrie et al., Lancet, No. 8515 (1986), pp. 1095-1096, "Combination Therapy in Prostate Cancer".

Rittmaster et al., J. Clin. Endocrin & Metab., vol. 55, No. 1 (1987), pp. 188-193, "The Effects of . . . a 5 Alpha-Reductase Inhibitor . . . ".

Diani et al., J. Clin. Endoc. & Metab., vol. 74, No. 2 (1990), pp. 345-350, "Hair Growth Effects of Oral Administration of Finasteride . . . ".

Bruchovsky et al., J. Clin. Endoc. Metab., vol. 67, No. 4 (1988), pp. 808-816, "Kinetic Parameters of 5 Alpha-Reductase Activity in Stroma & Epithelium of Normal, Hyperplastic & Carcinomatous Human Prostates".

Hudson, J. Steroid Biochem., vol. 26, No. 3 (1987), pp. 349-353, "Comparison of Nuclear 5 Alpha-Reductase Activities in the Stromal and Epithelial Fractions of Human Prostatic Tissue".

Moore et al., J. Biol. Chem., vol. 251, No. 19 (1976), pp. 5895-5900, "Steroid 5 Alpha-Reductase in Cultured Human Fibroblasts".

Andersson et al., J. Biol. Chem., vol. 264, No. 27 (1989), pp. 16249-16255, "Expession Cloning & Regulation of Steroid 5 Alpha-Reductase, an Enzyme Essential for Male Sexual Differentiation".

Andersson et al., Proc. Nat'l Acad. Science, vol. 87 (1990), pp. 3640-3644, "Structural & Biochemical Properties of Cloned and Expressed Human and Rat Steroid 5 Alpha-Reductases".

Andersson et al., Nature, vol. 354 (Nov. 14, 1991), pp. 159-161, "Deletion of Steroid 5 Alpha-Reductase-2 Gene in Male Pseudohermaphroditism".

Wilson, Biol. of Reproduction, vol. 46 (1992), pp. 168-173, "Syndromes of Androgen Resistance".

Geldolf et al., Eur. J. Cancer, vol. 26, No. 2 (1990), pp. 188, "Enzyme Inhibitors in Hormone Dependent Prostate Cancer Growth".

Geldolf et al., J. Cancer Res. Clin. Oncol., vol. 118 (1992), pp. 50-55, "Consideration of the Use of . . . 4MA . . . in Prostate Cancer Research".

Brooks et al., The Prostate, vol. 18 (1991), pp. 215-227, "Effect of Castration, DES, Flutamide, and MK-906 on Growth of the Dunning Rat Prostatic Carcinoma".

Jones et al., J. Med. Chem., vol. 36 (1993), pp. 421-423, "Nonsteroidal Inhibitors of Human Type 1 Steroid 5alpha-Reductase".

Masubuchi et al., Eur. J. Pharm., vol. 183, No. 5 (1990), p. 1757, "Lack of DHT Inhibition . . . by Treatment of 4MA . . . ".

Primary Examiner: Rotman; Alan L.
Assistant Examiner: Rotman; A.
Attorney, Agent or Firm: Fitch; Catherine D., Winokur; Melvin

Abstract

The present invention provides for the preparation of compounds,namely, 3-phenanthridiNones and their derivatives and their unique ability to inhibit 5-alpha-reductase or their isozymes thereof in mammals enabling said compounds for treating hyperandrogenic conditions of acne, androgenic alopecia, male pattern baldness,female hirsutism,benign prostatic hyperplasia, prostatitis and prostatic cancer.

1 Claim, No Drawings

Ad: Propecia, Avodart, Spectral DNC and more!

content2

Ad: Hair2Go.com

Location: Unknown Location wrong? Click here What's This?

Web regrowth.com

Ad: ProMox combination therapy!

Ad: The HairMax Laser Comb

More Info: Home | About Regrowth.com | How to Advertise | Privacy Policy | Advertising Policy | Contact Us
Site Map | Copyright © 2007 The Regrowth Network. All rights reserved. Legal Disclaimer

Other Cool Sites: Hair Loss Treatments - Body for Life Tracker - MedSpert

Propecia ® is a registered trademark of Merck. Avodart ® is a registered trademark of GlaxoSmithKline.
Rogaine ® is a registered trademark of Pfizer. Nizoral ® is a registered trademark of McNeil Consumer & Specialty Pharmaceuticals.