2-Phenylindole derivatives, their use as complement inhibitors

Details 2-Phenylindole derivatives, their use as complement inhibitors 2-Phenylindole derivatives, their use as complement inhibitors

1984-03-05

1985-04-09

Daus, Donald G.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

548510, 548511, C07D20918, A61K 3140

Patent

active

045101582

ABSTRACT:
4-(1-R'-2-phenyl-1H-indol-3-yl)-3-cyclohexene-1-carboxylic acids, 4-(1'R'-2-phenyl-1H-indol-3-yl)cyclohexane-1-carboxylic acids, 4-(1-R'-2-phenyl-1H-indol-3-yl)benzoic acids, the corresponding cyclohexene- and cyclohexane-1,1-dicarboxylic acids, and lower-alkyl esters thereof, wherein R' is hydrogen or lower-alkyl, are prepared by reacting a 1-R'-2-phenyl-1H-indole with a cyclohexanone-4-carboxylic acid or -4,4-dicarboxylic acid, followed as desired by a hydrogenation or aromatization process. The compounds which are free carboxylic acids or salts thereof are useful as complement inhibitors. The corresponding esters are useful as intermediates.

REFERENCES:
patent: 3551451 (1970-12-01), Szmuszkovicz
Patrick, R. A. & Johnson, R. E., Annual Reports in Medicinal Chemistry, vol. 15, Academic Press, New York, NY, 1980; Chapter 20, pp. 193-201.
Freter, K., J. Org. Chem., vol. 40, 2525-2529 (1975).

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