Disubstituted acetylenes bearing heteroaromatic and heterobicycl

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...

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514252, 514253, 514255, 514256, 514269, 514314, 514337, 514432, 514444, 514456, 514461, 514863, A61K 31505, A61K 31495, A61K 3138, A61K 3147

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056021305

ABSTRACT:
Retinoid-like activity is exhibited by compounds of the formula ##STR1## where X is S, O, or NR' where R' is hydrogen or lower alkyl; R is hydrogen or lower alkyl; A is pyridyl, thienyl, furyl, pyridazinyl, pyrimidinyl or pyrazinyl; n is 0-4; and B is H, --COOH or a pharmaceutically acceptable salt, ester or amide thereof, --CH.sub.2 OH or an ether or ester derivative, or --CHO or an acetal derivative, or --COR.sub.1 or a ketal derivative where R.sub.1 is --(CH.sub.2).sub.m CH.sub.3 where m is 0-4, or a pharmaceutically acceptable salt thereof.

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: 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: 4826984 (1989-05-01), Berlin et al.
patent: 4855320 (1989-08-01), Chatterjee et al.
patent: 4895868 (1990-01-01), Chandraratna
patent: 4927947 (1990-05-01), Chandraratna
patent: 4980369 (1990-12-01), Chandraratna
patent: 4992468 (1991-02-01), Chandraratna
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: 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
patent: 5231113 (1993-07-01), Chandraratna
patent: 5234926 (1993-08-01), Chandraratna
patent: 5248777 (1993-09-01), Chandraratna
patent: 5264456 (1993-11-01), Chandraratna
patent: 5264578 (1993-11-01), Chandraratna
patent: 5272156 (1993-12-01), Chandraratna
patent: 5278318 (1994-01-01), Chandraratna
patent: 5324744 (1994-06-01), Chandraratna
patent: 5324840 (1994-06-01), Chandraratna
patent: 5326898 (1994-07-01), Chandraratna
patent: 5344959 (1994-09-01), Chandraratna
patent: 5346895 (1994-09-01), Chandraratna
patent: 5346915 (1994-09-01), Chandraratna
patent: 5348972 (1994-09-01), Chandraratna
patent: 5348975 (1994-09-01), Chandraratna
patent: 5349105 (1993-09-01), Chandraratna
patent: 5354752 (1994-10-01), Chandraratna
Eur.J. Med. Chem. vol. No. 30, no. spl., 1995 pp. 505S-517 S, by Chandraratna et al.
Biopharm. Drug. Dispos. vol. 15, No. 5, 1994, pp. 347-357.
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.
Davis et al. J. Organomettalic Chem 387 (1990) 381-390.
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, vol. 96, No. 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, Vo. 95, 1990, pp. 125-136.
Characterization of Human Sebaceous Cells In Vitro, Thomas I. Doran, et al., The Journal of Investigative Dermatology, vol. 96, No. 3, Mar. 1991.
Synthesis and Evaluation of Stilbene and Dihydrostilbene Derivatives as Potential Anticancer Agents That Inhibit Tubulin Polymerization by Cushman, Mark et.al. J.Med. Chem 1991, 34, 2579-2588.
Synthesis and Evaluation of New Protein-Tyrosine Kinase Inhibitors. Part 1. Pyridine-Containing Stilbenes and Amides by Cushman, Mark et al. Bioorganic & Medicinal Chemistry Letters, vol. 1, No.4, pp. 211-214, 1991.
Di-and Tri-methoxystyryl Derivatives of Heterocyclic Nitrogen Compounds by Bahner, C. T. et al. Arzneim-Forsch./Drug Res, 31 (I), Nr. 3 (1981).
Retinobenzoic acids. 3. Structure-Activity Relationships of retinoidal Azobenzene-4-carboxylic acids and Stilbene-4-carboxylic acids by H. Kagechika et al., Journal of Medicinal Chemistry, 1989 , 32, pp. 1098-1108 .

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