Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Cyclopentanohydrophenanthrene ring system doai
Patent
1992-11-23
1997-05-20
Tsang, Cecilia
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Cyclopentanohydrophenanthrene ring system doai
514177, 514178, 514179, 514180, 514181, 514182, 540 89, 540 94, 540 95, 540 97, 540 99, 540106, 540107, 540108, 540109, 540110, 540111, 540112, 540113, 540114, 540118, 540119, 540120, 552505, 552540, 552541, 552542, 552544, 552546, 552547, 552612, 548146, 548201, A61K 3156, A61K 3144, A61K 31425, A61K 31445, A61K 3158, A61K 31495, C07J 4100, C07J 700
Patent
active
RE0355178
ABSTRACT:
Method, compositions, and compounds for modulating brain excitability to alleviate stress, anxiety, and seizure activity using certain steroid derivatives that act at a newly identified site on the gamma-ammobutyric acid/benzodiazepine receptor-chloride ionpore (GBR) complex.
REFERENCES:
patent: 2797230 (1957-06-01), Nicholls
patent: 2861089 (1958-11-01), Graham
patent: 3197470 (1965-07-01), Deghenghi et al.
patent: 4213978 (1980-07-01), Bodor et al.
Beard et al., "The Methylenation of Unsaturated Ketones," Tetrahedron 25:1219-1239 (1969).
Besch et al., "A Review of Some Aspects of the Metabolism of Progestational Agents," Metabolism 14(3), Part 2:432-443 (1965).
Chemical Abstracts 52, Abstract for German Patent Appl. No. 927,030, Rosenkranz et al., "Allopregnane-17.alpha.,21-diol,3,11,20-trione and Its Esters" (1958.
Aird, R.B., and Gordon, G.S., "Anticonvulsive Properties of Desoxycorticosterone," J. Am. Med. Assoc. 145(10):715-719 (1951).
Backstrom, T., Bixo, M., and Hammarback, S., "Ovarian steroid hormones: Effects on mood, behaviour, and brain excitability," Acta. Obstet. Gynecol. Scand. Suppl. 130:19-24 (1985).
Barker, J.L., Harrison, N.L., Lange, G.D., and Owen, D.G., "Potentiation of GABA activated chloride conductance by a steroid anaesthetic in cultured rat spinal neurones," J. Physiol. 386:485-501 (1987).
Barnes, D.M., "Steroids may influence changes in mood," Science 23:1344-1345 (Jun., 1986).
Callachan, H., Cotrell, G.A., Hather, N.Y., Lambert, J.J., Nooney, J.M., and Peters, J.A., "Modulation of the GABA.sub.a receptor by progesterone metabolites" (1987).
Craig, C.R. (G.D. Searle), "Anticonvulsive activity of steroids: Separability of anticonvulsant from hormonal effects," J. Pharm. Exper. Ther. 153(2):337-343 (1966).
Crawley, J.N., Glowa, J.R., Majewska, M.D., and Paul, S.M., "Anxiolytic activity of an endogenous adrenal steroid," Brain Research 398:382-395 (1986).
Gee, K.W., Chang, W.C., Brinton, R.E., and McEwen, B.S., "GABA-dependent modulation of the Cl.sup.- ionophore by steroids in rat brain," Eur. J. Pharmacol. 136:419-423 (1987).
Gyermek, L., Iriarte, J., and Grabbe, P., "Steroids. CCCX. Structure-Activity Relationship of Some Steroidal Hypnotic Agents," J. Med. Chem. 11:117-125 (1968).
Harrison, N.L., Majewska, M.D., Harrington, J.W., and Barker, J.L., "Structure-activity relationships for steroid interaction with the .gamma.-Aminobutyric acid receptor complex," J. Pharm. Exper. Ther. 241(1):346-353 (1987).
Hewett, C.L., Savage, D.S., Lewis, J.J., and Sugrue, M.J. (Organon labs Ltd.), "Anticonvulsant and interneuronal blocking activity in some synthetic aminosteroids," J. Pharm. Lond. 16:765-767 (1964).
Hogskilde, S., Wagner, J., Carl., P., Anker, N., Angelo, H.R., and Sorensen, M.B., "Anticonvulsive properties of pregnanolone emulsion compared with Althesin and thiopentone in mice," Br. J. Anaesth. 16:462-467 (1988).
Lambert, J.J., Peters, J.A., and Cottrell, G.A., "Actions of synthetic and endogenous steroids on the GABA.sub.A receptor," TIPS 8:224-227 (1987).
Landgren, S.L., Aasly, J., Backstrom, T., Dubrovsky, D., and Danielson, E., "The effect of progesterone and its metabolites on the interictal epileptiform discharge in the cat's cerebral cortex," Acta. Physiol. Scand. 131:33-42 (1987).
Majewska, M.D., "Steroids and Brain Activity: Essential dialogue between body and mind," Biochem. Pharmacol. 36(22):3781-3788 (1987).
Majewska, M.D., Harrison, N.L., Schwartz, R.D., Barker, J.L., and Paul, S.M., "Steroid hormone metabolites are Barbiturate-Like modulators of the GABA receptor," Science 232:1004-1007 (1986).
Marshall, C.W., "5-Pregnen-3b-ol-20-one 3-aminoalkanoates," Belg. patent 621,470, Feb. 18, 1963, CA 59:12883.
Morrow, A.L., Suzdak, P.D., and Paul, S.M., "Steroid hormone metabolites potentiate GABA receptor-mediated chloride ion flux with nanomolar potency," Eur. J. Pharm. 142:483-485 (1987).
Munari, C., Casaroli, D., Matteuzzi, G., and Pacifico, L., "The use of Althesin in Drug-Resistant Status Epilepticus," Epilepsia 20:475-482 (1979).
Riu, P.L., Susini, G., and Ruju, P., "Anticonvulsant activity of Althesin on Experimental Epilepsy," Br. J. Anaesth. 54:343-347 (1982).
Roussel-UCLAF, "Antispasmodics," Fr. patent M1764, May 6, 1963, CA 59:12877.
Selye, H., "The antagonism between anesthetic steroid hormones and pentamethylenetetrazol (Metazol)," J. of Lab. and Clin. Med., 27, 1051-1054 (1942).
Werboff, J., Hedlund, L., and Havlena, J., "Audiogenic seizures in Adult Male castrated Rats treated with various hormones," General and Comp. Endo. 3:389-397 (1963).
Woodbury, D.M., "Effect of Adrenocortical Steroids and Adrenocorticotrophic Hormone on Electroshock Seizure Treshold," J.P.E.T. 105:27-36 (1952).
Woodbury, D.M., "Effect of hormones on brain excitability and electrolytes," Recent Prog. Horm. Res. 10:65-107 (1954).
Arafat, E. et al., "Sedative and Hypnotic Effects Of Oral Administration Of Micronized Progesterone May Be Mediated Through Its Metabolites," Am J Obstet Gynecol 159:1203-1209 (1988).
Conney, A.H. et al., "Decreased Central Depressant Of Progesterone And Other Steroids In Rats Pretreated With Drugs and Insecticides," The Journal Of Pharmacology And Experimental Therapeutics 154:310-318 (1966).
Gyermek, L., "Pregnanolone: A Highly Potent, Naturally Occurring Hypnotic-Anesthetic Agent (32276)," Institute Of Hormone Biology Syntex Research, P.S.E.B.M. 125:1058-1062 (1967).
Gyermek, L. et al., "Some Effects Of Progesterone And Related Steroids On The Central Nervous System," Int. J. Neuropharmacol 6:191-198 (1967).
Mendelson, W.B. et al., "Sleep Induction By An Adrenal Steroid In The Rat," Pyschopharmacology 93:226-229 (1987).
Raisinghani, K.H. et al., "Uptake Of Intravenously Administered Progesterone, Pregnanedione And Pregnanolone By The Rat Brain," Acta Endocrinologica 57:395-404 (1968).
Nagata, CA 74: 13317 (1970).
Pfaff D. W. et al. Science, 219:808-814 (1983).
Laidlaw, Laucet, 1235-1237 (1956).
Marker, R.E. et al, J.A.C.S. 59, 616-618 (1937).
Bordor, Drugs of the Future, 6(3):165-182 (1981).
Morrian et al, Biochem. 40: 376-380 (1947).
Lawrence, L.J. et al, Biochem. Biophys. Res. Comm. 123: 1130-1137 (1984).
Backstrom, T. et al., Acta, Endocr. Supp. 256-257, 1983.
Bodor, J. Pharmaceutical Sciences, 73(3):385-389 (1984).
Dalton, K., The Premenstrual Syndrome and Progesterone Therapy, 2nd Edition, 1984.
Notari, R.E., Methods in Enzymology, 112:309-323 (1985).
Rosciszewska, D., et al., J. Neurol. Neurosurg. Psych. 49:47-51 (1986).
Squires, R.F. et al., Mol. Pharmacol., 23;326-336, 1983.
Swinyard, E.A. et al, Antiepileptic Drugs, D. M. Woodbury, J.K. Penry and C.E. Pippenger, eds., p. 111 (Raven Press, New York) 1982.
Wood, P.L., et al, J. Pharmacol. Exp. Ther. 231:572-576 (1984).
Worms, P. L. et al., J. Pharmacol. Exp. Ther. 220:660-671 (1982).
Dennerstein et al, British Medical Journal, 290:1617-1621, 1985.
Gee, K. W. et al., in Drugs In Central Nervous System Disorders, pp. 123-147, D.C. Horvell, ed. 1985.
Gee, K.W. et al., Molecular Pharmacology, 30:218-225, 1986.
Maddocks, S., et al., Obstet. Gynecol., 154:573-81, 1986.
Maksay, G. et al. J. Neurochem., 44:480-486, 1985.
Mattson, R.H. et al, in Advances in Epileptology, XVth Epilepsy Int. Symposium, 279-282, 1984.
Bolger Michael B.
Gee Kelvin W.
Lan Nancy C.
Tsang Cecilia
University of Southern California
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