Azacyclooctadiene compound and pharmaceutical use

Details Azacyclooctadiene compound and pharmaceutical use Azacyclooctadiene compound and pharmaceutical use

1990-02-23

1991-12-24

Ivy, C. Warren

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Heterocyclic carbon compounds containing a hetero ring...

540476, A61K 3133, C07D49822

Patent

active

050752960

ABSTRACT:
An azacyclooctadiene compound having the formula (1) or a pharmacologically acceptable salt thereof is novel and useful as an anti-tumor agent. ##STR1## in which R1 is --CH2R, R being hydrogen, --COCH3, --OH, --NH2, --COOH or --OCOCH3, or may form --CH2--X--Y-- together with R2; R2 is hydrogen, an alkyl having 1 to 4 carbon atoms or --COR10, R10 being hydrogen, an alkyl having 1 to 4 carbon atoms, --OR11 or --NHR11, R11 being an alkyl having 1 to 4 carbon atoms, or may form --CH2--X--Y-- together with R1; R3, R4 and R5 each are hydrogen or methyl; R6 and R7 each are hydrogen or may form the direct bond to each other; R8 is hydrogen or may form the direct bond to R7; and R9 is hydrogen, --N3, --NH2, --OCH3 or .dbd.0; X being oxygen or --NZ--, Z being hydrogen, methyl, --COCH3, --CH2COOH, --CO--CH.dbd.CH2, --CO--CH.dbd.CH--CH3, --CH2C6H5, --CH2OH, --CH2OCOCH3 or --CH2--COOC(CH3)3, Y being --SC--, --CO-- or --CH2--.

REFERENCES:
Devita et al., "Cancer . . . " S. B. Lippincott Co: (1985).
Tomioka et al., "Design, Synthesis and Antitamar . . ." Tetrahedron Lett. 30(22)2949-2952 (1989).

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