Organic compounds -- part of the class 532-570 series – Organic compounds – Nitriles
Reexamination Certificate
2006-04-11
2006-04-11
Kumar, Shailendra (Department: 1621)
Organic compounds -- part of the class 532-570 series
Organic compounds
Nitriles
C564S153000, C564S157000, C564S175000, C514S522000, C514S524000, C514S616000, C514S617000
Reexamination Certificate
active
07026500
ABSTRACT:
This invention provides a class of androgen receptor targeting agents (ARTA). The agents define a new subclass of compounds, which are selective androgen receptor modulators (SARM). Several of the SARM compounds have been found to have an unexpected androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. Other SARM compounds have been found to have an unexpected antiandrogenic activity of a nonsteroidal ligand for the androgen receptor. The SARM compounds, either alone or as a composition, are useful for a) male contraception; b) treatment of a variety of hormone-related conditions, for example conditions associated with Androgen Decline in Aging Male (ADAM), such as fatigue, depression, decreased libido, sexual dysfunction, erectile dysfunction, hypogonadism, osteoporosis, hair loss, anemia, obesity, sarcopenia, osteopenia, osteoporosis, benign prostate hyperplasia, alterations in mood and cognition and prostate cancer; c) treatment of conditions associated with Androgen Decline in Female (ADIF), such as sexual dysfunction, decreased sexual libido, hypogonadism, sarcopenia, osteopenia, osteoporosis, alterations in cognition and mood, depression, anemia, hair loss, obesity, endometriosis, breast cancer, uterine cancer and ovarian cancer; d) treatment and/or prevention of acute and/or chronic muscular wasting conditions; e) preventing and/or treating dry eye conditions; f) oral androgen replacement therapy; and/or g) decreasing the incidence of, halting or causing a regression of prostate cancer.
REFERENCES:
patent: 3875229 (1975-04-01), Gold
patent: 4139638 (1979-02-01), Neri et al.
patent: 4191775 (1980-03-01), Glen
patent: 4239776 (1980-12-01), Glen et al.
patent: 4282218 (1981-08-01), Glen et al.
patent: 4386080 (1983-05-01), Crossley et al.
patent: 4465507 (1984-08-01), Konno et al.
patent: 4636505 (1987-01-01), Tucker
patent: 4880839 (1989-11-01), Tucker
patent: 5162504 (1992-11-01), Horoszewicz
patent: 5609849 (1997-03-01), Kung
patent: 5656651 (1997-08-01), Sovak et al.
patent: 6019957 (2000-02-01), Miller et al.
patent: 6071957 (2000-06-01), Miller et al.
patent: 6160011 (2000-12-01), Miller et al.
patent: 6482861 (2002-11-01), Miller et al.
patent: 6492554 (2002-12-01), Dalton et al.
patent: 6569896 (2003-05-01), Dalton et al.
patent: 0 040 932 (1981-12-01), None
patent: 0 100 172 (1984-02-01), None
patent: 000 2892 (1985-02-01), None
patent: 0 253 503 (1988-01-01), None
patent: 1360001 (1970-03-01), None
patent: 52-128329 (1977-10-01), None
patent: 54-63047 (1980-12-01), None
patent: WO 95/19770 (1995-07-01), None
patent: WO 98 05962 (1998-02-01), None
patent: WO 98/53826 (1998-12-01), None
patent: WO 98/55153 (1998-12-01), None
patent: WO 01 27622 (2001-04-01), None
patent: WO 01 28990 (2001-04-01), None
patent: WO 01 34563 (2001-05-01), None
patent: WO 02 00617 (2002-01-01), None
patent: WO 02/016310 (2002-02-01), None
patent: WO 03 011302 (2003-02-01), None
U.S. Appl. No. 10/298,229, filed Nov. 28, 2002, Miller et al.
U.S. Appl. No. 10/270,232, filed Oct. 15, 2002, Dalton et al.
U.S. Appl. No. 10/277,108, filed Oct. 23, 2002, Dalton et al.
U.S. Appl. No. 10/270,233, filed Oct. 15, 2002, Dalton et al.
U.S. Appl. No. 10/270,732, filed Oct. 15, 2002, Dalton et al.
U.S. Appl. No. 10/371,155, filed Feb. 24, 2003, Dalton et al.
U.S. Appl. No. 10/371,209, filed Feb. 24, 2003, Dalton et al.
U.S. Appl. No. 10/371,211, filed Feb. 24, 2003, Dalton et al.
U.S. Appl. No. 10/371,210, filed Feb. 24, 2003, Dalton et al.
U.S. Appl. No. 10/359,270, filed Feb. 6, 2003, Steiner et al.
U.S. Appl. No. 10/310,150, filed Dec. 5, 2002, Steiner et al.
Eliason et al., “High Throughput Fluorescence Polarization-Based Screening Assay for the Identification of Novel Nuclear Receptor Ligands,” Abstracts of Papers, 223rd ACS National Meeting, Orlando, FL, United States, (2002), Apr. 7, 2002.
Howard Tucker and Glynne J. Chesterson, J. Med. Chem. 1988, 31, pp. 885-887, “Resolution of the Nonsteroidal Antiandrogen—4′-Cyano-3-[(4-fluorophenyl)sulfonyl]-2-hydroxy-2-methyl-3′-(trifluoromethyl)-propionanilide and the Determination of the Absolute Configuration of the Active Enantiomer”.
D. McKillop, et al., “Enantioselective metabolism and pharmacokinetics of Casodex in the male rat”, Xenobiotica, 1995, vol. 25, No. 6, 623-634.
Leonid Kirkovsky, et al., “[125I]-Radionated Bicalutamide Analogs as Potential Imaging Agents for Prostate Cancer”, Poster Presentation MEDI 155, 214th ACS National Meeting, Las Vegas, NV, Sep. 7-11, 1997, Department of Pharmacuetical Sciences, University of Tennessee, Memphis, TN 38163.
David T. Baird and Anna F. Glasier, “Hormonal Contraception—Drug Therapy”, The New England Journal of Medicine, May 27, 1993, pp. 1543-1549.
F.C. W. Wu, “Male Contraception: Current Status and Future Prospects”, Clinical Endocrinology, (1988), 29, pp. 443-465.
Carl Djerassi and S.P. Leibo, “A new look at male contraception”, Nature, vol. 370, pp. 11-12.
World Health Organisation Task Force on Methods for the Regulation of Male Fertility, “Contraceptive efficacy of testosterone-induced azoospermia in normal men”, The Lancet, vol. 336, Oct. 20, 1990, pp. 955-959and 1517-1518.
C. G. Francisco, et al., “Long-acting contraceptive agents: testosterone esters of unsaturated acids”, Steroids, Jan. 1990, vol. 55, Butterworths.
John M. Hoberman and Charles E. Yesalis, “The History of Synthetic Testosterone”, Scientific American, Feb. 1995, pp. 76-81.
Leonid Kirkovsky, et al., “Approaches to Irreversible non-steroidal chiral antiandrogens”, Department of Pharmaceutical Sciences, University of Tennessee, 47th Southeast/51st Southwest Joint Regional Meeting of the American Chemical Society, Memphis, TN, Nov. 29-Dec. 1, 1995.
David J. Handelsman, “Bridging the gender gap in contraception: another hurdle cleared” The Medical Journal of Australia, vol. 154, Feb. 18, 1996, pp. 230-233.
Edwards JP, Higuchi RI, Winn DT, Pooley CLF, Caferro TR, Hamann LG, Zhi L, Marschke KB, Goldman ME, and Jones TK. Nonsteroidal androgen receptor agonists based on 4-(Trifluoromethyl)-2H-pyranol[3,2-g]quionolin-2-one. Bioorg. Med. Chem. Lett., 9:1003, 1999.
Zhi L, Tegley CM, Marschke KB, and Jones TK. Switching androgen receptor antagonists to agonists by modifying C-ring substituents on piperidino[3,2-g]quinolone. Bioorg. Med. Chem. Lett., 9: 1009, 1999.
Higuchi RJ, Edwards JP, Caferro TR, Ringgenberg JD, Kong JW, Hamann LG, Arienti KL, Marschke KB, Davis RL, Farmer LJ, and Jones TK. 4-Alkyl- and 3,4-diaklyl-1,2,3,4-tetrahydro-8-pyridono[5,6-g]quinolines: potent, nonsteroidal androgen receptor agonists. Bioorg. Med. Chem. Lett., 9:1335,1999.
Hamann LG, Mani NS, Davis RL, Wang XN, Marschke KB, and Jones TK. Discovery of a potent, orally active nonsteroidal androgen receptor agonist: 4-ethyl-1,2,3,4-tetrahydro-6-(trifluoromethyl)-8-pyridono[5,6-g]-quinoline (LG121071). J. Med. Chem., 42: 210, 1999.
Rosen J, Day A, Jones TK, Jones ET, Nadzan AM, and Stein RB. Intracellular receptors and signal transducers and activators of transcription superfamilies: novel targets for small-molecule drug discovery. J. Med. Chem., 38:4855, 1995.
Dalton JT, Mukherjee A, Zhu Z, Kirkovsky L, and Miller DD. Discovery of Nonsteroidal Androgens. Biochem. Biophys. Res. Commun.,244(1):1-4, 1998.
Edwards JP, West SJ, Pooley CLF, Marschke KB, Farmer LJ, and Jones TK. New nonsteroidal androgen receptor modulators based on 4-(trifluoromethyl)-2-(1H)-Pyrololidino[3,2-g]quinolone. Bioorg. Med. Chem. Lett., 8: 745, 1998.
Berger et al., “Concepts and limitations in the application of radiolabeled antiandrogens, estrogens, or androgens as isotropic scanning agents for the prostate”, Invest. Urol, (1975), 1391, 10-16.
Dalton James T.
Miller Duane D.
Steiner Mitchell S.
Veverka Karen A.
Cohen Mark
Kumar Shailendra
Pearl Cohen Zedek Latzer LLP
University of Tennessee Research Foundation
LandOfFree
Halogenated selective androgen receptor modulators and... does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Halogenated selective androgen receptor modulators and..., we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Halogenated selective androgen receptor modulators and... will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-3558765