Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1982-06-01
1985-02-19
Love, Ethel G.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
549304, 549459, 549467, A61K 3134, C07D30778
Patent
active
045005435
ABSTRACT:
Disclosed herein are 1-aminomethyl-phthalans represented by the formula ##STR1## wherein R, R.sub.1, and R.sub.2 are independently selected from hydrogen, hydroxy, loweralkoxy of 1 to 3 carbon atoms, loweralkenyloxy of 1 to 3 carbon atoms, thiomethyl, halo, or ##STR2## wherein R.sub.5 and R.sub.6 are independently selected from hydrogen, loweracyl of 1 to 4 carbon atoms or sulfonyl of the formula ##STR3## wherein R.sub.7 is loweralkyl of 1 to 4 carbon atoms; or R and R.sub.1, or R.sub.1 and R.sub.2 can be taken together to form a methylenedioxy or ethylenedioxy bridge; with the proviso that at least one of R, R.sub.1 or R.sub.2 must be other than hydrogen; and R.sub.3 and R.sub.4 are independently selected from hydrogen; loweralkyl of 1 to 4 carbon atoms; halo-substituted loweralkyl of 1 to 4 carbon atoms; arylalkyl of the formula ##STR4## wherein m is 0, 1 or 2, p is 0 or 1, R.sub.8 is hydrogen or loweralkyl of 1 to 4 carbon atoms and R.sub.9 and R.sub.10 are independently selected from hydrogen, hydroxy, methoxy, loweralkyl of 1 to 4 carbon atoms, or halo, or R.sub.9 and R.sub.10 can be taken together to form a methylenedioxy or ethylenedioxy bridge; or 1,4-benzodioxan of the formula ##STR5## wherein q is 1, 2 or 3, and R.sub.11 is hydrogen, methoxy, or halo; or R.sub.3 and R.sub.4 can be taken together to form a piperazino, piperidino or morpholino moiety; and the pharmaceutically acceptable salts thereof. Also disclosed are pharmaceutical compositions comprising compounds of formula (I) and a pharmaceutically acceptable carrier or diluent.
REFERENCES:
patent: 3200132 (1965-08-01), Werner
patent: 3467675 (1969-09-01), Petersen et al.
patent: 3513239 (1970-05-01), Wiley et al.
patent: 3859279 (1975-01-01), Fothergill et al.
Arendsen David L.
DeBernardis John F.
Abbott Laboratories
Katz Martin L.
Love Ethel G.
Shelton Dennis K.
Weinstock Steven F.
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