Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1993-03-11
1995-03-21
Evans, Joseph E.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514438, 549 71, A61K 3138, A61K 3119
Patent
active
053995864
ABSTRACT:
Retinoid-like compounds which act as agonists of the RXR retinoid receptor sites induce apoptosis of tumor cells in cell cultures, and are used as drugs to treat tumors in mammals including humans. Compounds which are specific agonists of RXR receptors and also compounds which are agonists of both RAR and RXR agonist (pan-agonists) induce apoptosis, although the RXR agonist compounds are preferred as drugs to avoid undesirable side effects associated with RAR agonist activity. The RXR agonists compounds are administered to mammals afflicted with tumors in pharmaceutical compositions adapted for systemic topical or for intralesional administration. The range of concentration of the active ingredient RXR agonist compound in the pharmaceutical compositions is approximately between 0.001 and 5 percent by weight, and such that the composition delivers approximately 0.1 mg to 100 mg of the active ingredient per kg body weight of the patient, per day of treatment.
REFERENCES:
patent: 4096341 (1978-06-01), Frazer
patent: 4326055 (1982-04-01), Loeliger
patent: 4391731 (1983-07-01), Boller et al.
patent: 4695649 (1987-09-01), Magami et al.
patent: 4705802 (1987-11-01), Lautenschlager et al.
patent: 4723028 (1988-02-01), Shudo
patent: 4739098 (1988-04-01), Chandraratna
patent: 4740519 (1988-04-01), Shroot et al.
patent: 4810804 (1989-03-01), Chandraratna
patent: 4826969 (1989-05-01), Maignan et al.
patent: 4855320 (1989-08-01), Chatterjee et al.
patent: 4895868 (1990-01-01), Chandraratna
patent: 4980369 (1990-12-01), Chandraratna
patent: 4992468 (1991-02-01), Chandraratna
patent: 4994491 (1991-02-01), Purcell et al.
patent: 5006550 (1991-04-01), Chandraratna
patent: 5013744 (1991-05-01), Chandraratna
patent: 5015658 (1991-05-01), Chandraratna
patent: 5023341 (1991-06-01), Chandraratna
patent: 5037825 (1991-08-01), Klaus et al.
patent: 5045551 (1991-09-01), Chandraratna
patent: 5049584 (1991-09-01), Purcell et al.
patent: 5053523 (1991-10-01), Chandraratna
patent: 5068252 (1991-11-01), Chandraratna
patent: 5089509 (1992-02-01), Chandraratna
patent: 5130335 (1992-07-01), Chandraratna
patent: 5134159 (1992-07-01), Chandraratna
patent: 5162546 (1992-11-01), Chandraratna
patent: 5175185 (1992-12-01), Chandraratna
patent: 5183827 (1993-02-01), Chandraratna
patent: 5202471 (1993-04-01), Chandraratna
Ursula M. Ney, et al. "Anti-Inflammatory Effects of Synthetic Retinoids May Be Related to their Immunomodulatory Action", Dermatologica (Suppl. 1), vol. 175, 1987, pp. 93-99.
A General Synthesis of Terminal and Internal Arylalkynes by the Palladium-Catalyzed Reaction of Alkynylzinc Reagents with Aryl Halides by Anthony O. King and Ei-ichi Negishi, J. Org. Chem. 43 No. 2, (1978) p. 358.
Conversion of Methyl Ketones into Terminal Acetylenes and (E)-Tri-substituted Olefins of Terpenoid Origin by Ei-ichi, Anthony O. King, and William L. Klima, J. Org. Chem. 45 No. 12, (1980) p. 2526.
Sporn et. al. in J. Amer. Acad. Derm. 15:756-764 (1986).
A Convenient Synthesis of Ethynylarenes and Diethynylarenes by S. Takahashi, Y. Kuroyama, K. Sonogashira, N. Hagihara, Synthesis (1980) pp. 627-630.
Shudo et al. in Chem. Phar. Bull. 33:404-407 (1985).
Kagechika et. al. in J. Med. Chem. 31:2182-2192 (1988).
Chemistry and Biology of Synthetic Retinoids by Marcia I. Dawson and William H. Okamura, published by CRC Press Inc., (1990), pp. 334-335, 354.
Synthesis of 2,2'-Diacyl-1,1'-biaryls. Regiocontrolled Protection of . . . by Mervic, et al, J. Org. Chem., No. 45, pp. 4720-4725, (1980).
A Dopamine Receptor Model and Its Application in the Design of a New Class of Rigid Pyrrolo[2,3-g]isoquinoline Antipsychotics, Gary L. Olson, et al. American Chemical Society, 1981, Vo. 24, No. 9, pp. 1026-1031.
6.2.3 Conformational Restriction, Williams, et al., Drug Discovery and Development, (1987) The Humana Press, pp. 54-55.
V. Retinoid Structure-Biological Activity Relationships, Chemistry and Biology of Synthetic Retinoids, pp. 324-356 (1990).
Davis et al. J. Organomettalic Chem 387 (1990) 381-390.
Nuclear receptor that identifies a novel retinoic acid response pathway, David J. Mangelsdorf, et al., Nature, vol. 345, 17 May (1990), pp. 224-229.
A Retinoic Acid-responsive Element in the Apoliprotein AI Gene Distinguishes between Two Different Retinoic Acid Response Pathways J. N. Rottman et al., Molecular and Cellular Biology, Jul. 1991, pp. 3814-3820.
A human retinoic acid receptor which belongs to the family of nuclear receptors, M. Petkovich, et al., Nature, vol. 330, 3 Dec. 1987, pp. 444-450.
Identification of a receptor for the morphogen retinoic acid, V. Giguere, et al., Nature, vol. 330, 17 Dec. 1987, pp. 624-629.
Identification of a second human retinoic acid receptor, Nigel Brand, et al., Nature, vol. 332, 28 Apr. 1988, pp. 850-853.
A third human retinoic acid receptor, hRAR- , A. Krust, et al., Proc. Nat'l. Acad, Sci, USA, vol. 86, Jul. 1989, pp. 5310-5314.
Characterization of three RXR genes that mediate the action of 9-cis retinoic acid, D. J. Mangelsdorft, et al., Genes & Devlopment, vol. 6, (1992), pp. 329-344.
Effects of 13-Cis-Retinoic Acid, All-Trans-Retinoic Acid, and Acitretin on the Proliferation, Lipid Synthesis and Keratin Expression of Cultured Human Sebocytes In Vitro, C. C. Zouboulis, The Journal of Investigative Dermatology, Inc., vol. 96, No. 5, 5 May 1991, pp. 792-797.
Organ maintenance of human sebaceous glands: in vitro effects of 13-cis retinoic acid and testosterone, John Ridden, et al., Journal of Cell Science, vol. 95, (1990), pp. 125-136.
Characterization of Human Sebaceous Cells In Vitro, T. I. Doran, et al., The Journal of Investigative Dermatology, vol. 96, No. 3, Mar. 1991, pp. 341-348.
Retinoids as Generalized Regulators of Cellular Growth and Differentiation Peter J. A. Davies, et al., The American Journal of the Medical Sciences, vol. 296, No. 3, Sep. 1988, pp. 164-170.
The Molecular Basis of Retinoic Acid Action, E. Antonio Chiocca, The Journal of Biological Chemistry, vol. 263, No. 23, Aug. 15, 1988, pp. 11584-11589.
Chandraratna Roshantha A.
Davies Peter A. J.
Allergan Inc.
Baran Robert J.
Evans Joseph E.
Szekeres Gabor L.
Voet Martin A.
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