Substituted azasteroids

Details Substituted azasteroids Substituted azasteroids

1975-05-02

1978-06-20

Daus, Donald G.

Chemistry of carbon compounds

Miscellaneous organic carbon compounds

C-metal

260283R, 260283SY, 260287D, 260289D, 260289AZ, 260465R, 2605708R, 260650R, 560103, 568715, 568814, C07D45506

Patent

active

040961478

ABSTRACT:
Compounds of the following general formula are useful as antidepressant and antiparkinson agents: ##STR1## WHEREIN R represents hydrogen, hydroxy, halogen, trifluoromethyl, straight or branched lower alkyl of from 1 to 6 carbon atoms, straight or branched lower alkoxy of from 1 to 6 carbon atoms, acyloxy, alkoxycarbonyloxy, carbamoyloxy, benzoyloxy, or benzoyloxy substituted with straight or branched lower alkyl of from 1 to 6 carbon atoms, straight or branched lower alkoxy of from 1 to 6 carbon atoms or halogen; R.sub.1 represents hydrogen, straight or branched lower alkyl of from 1 to 6 carbon atoms, phenyl or benzyl; R.sub.2 represents hydrogen, straight or branched lower alkyl of from 1 to 6 carbon atoms, ethynyl, ethynyl substituted with straight or branched lower alkyl of from 1 to 6 carbon atoms; aryl, or aralkyl wherein each aryl moiety may be substituted with straight or branched lower alkyl of from 1 to 6 carbon atoms, straight or branched lower alkoxy of from 1 to 6 carbon atoms or halogen; R.sub.3 represents hydroxy, acyloxy, alkoxycarbonyloxy, carbamoyloxy, benzoyloxy or benzoyloxy substituted with straight or branched lower alkyl of from 1 to 6 carbon atoms, straight or branched lower alkoxy of from 1 to 6 carbon atoms or halogen; or R.sub.2 and R.sub.3 taken together form an oxo group; m is an integer of 1 or 2; and n is an integer of from 1 to 3. Individual optical and geometric isomers and pharmaceutically acceptable acid addition salts of the compounds are also included within the scope of this invention.

REFERENCES:
patent: 3219668 (1965-11-01), Brown et al.
patent: 3346582 (1967-10-01), Brown et al.
patent: 3378560 (1968-04-01), Brown et al.
Tietz, "Clinical Chemistry," 1971, pp. 496-497.
White et al., "Principles of Biochemistry," 1968, pp. 522-524.
Burger, Medicinal Chemistry, 1963, p. 42.
Morrison et al., Organic Chemistry, (1966), pp. 790-791.
Strandtmann et al., "J. of Org. Chem.," 31, p. 797, (1966).
Meyers et al., "Tetrahedron Letters," (1965), No. 4, pp. 255-260.

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