Imidazole and imidazoline derivatives and uses thereof

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

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514300, 514301, 514302, 514310, 514312, 514313, 514401, 514402, 546112, 546114, 546115, 546122, 546143, 546153, 546155, 546156, 546157, 546159, 546183, 5483114, 5483121, 5483315, A61K 3144, A61K 3147, C07D22104, C07D21538

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active

060937270

ABSTRACT:
This invention is directed to novel imidazole and imidazoline derivatives which are selective agonists for cloned human a, adrenergic receptors. This invention is also related to the use of these compounds for the treatment of any disease where modulation of the .alpha..sub.2 receptors may be useful. The invention further provides for a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.

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Kretzschmar, von R. et al., "Zur Pharmakologie von N-(2-Imizadolin-2-yl)-N-(4-indanyl)amin (Indanazolin), einer neuen vasokonstriktorisch wirksamen Imidavolinverbindung," Arzneim.-Forsch./Drug Res. (1980) 30: 1746-1760.
Timmermans, P.B.M.W.M. et al., "Characterization of Alpha-adrenoceptor populations. Quantitative relationships between cardiovascular effects initiated at central and peripheral Alpha-adrenoceptors," J. Med. Chem. (1981) 24: 502-507.
Amemiya, Y., et al., "Synthesis and Alpha-Adrenergic Activities of 2- and 4-Substituted Imidazoline and Imidazole Analogues," J. Med. Chem. (1992) 35:750-755.
Hong, S., et al., "A Structure-Activity Relationship Study of Benzylic Modifications of 4-[1-(1-Napththyl)ethyl]-1H-imidazoles on Alpha 1-and Alpha 2-Adrenergic Receptors," J. Med. Chem. (1994) 37: 2328-2333.
Wong, W.C., et al., "Design and Synthesis of Alpha 2 Adrenoceptor Agonists," 213th American Chemical Society Meeting, San Francisco, CA, Apr. 13-17, 1997, Abstract No. 023, which was mailed to subscribers Mar. 8, 1997.

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