| 摘要 |
Disclosed herein are 1-aminomethyl-phthalans represented by the formula <IMAGE> (I) wherein R, R1, and R2 are independently selected from hydrogen, hydroxy, loweralkoxy of 1 to 3 carbon atoms, loweralkenyloxy of 1 to 3 carbon atoms, thiomethyl, halo, or <IMAGE> wherein R5 and R6 are independently selected from hydrogen, loweracyl of 1 to 4 carbon atoms or sulfonyl of the formula <IMAGE> wherein R7 is loweralkyl of 1 to 4 carbon atoms; or R and R1, or R1 and R2 can be taken together to form a methylenedioxy or ethylenedioxy bridge; with the proviso that at least one of R, R1 or R2 must be other than hydrogen; and R3 and R4 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 <IMAGE> wherein m is 0, 1 or 2, p is 0 or 1, R8 is hydrogen or loweralkyl of 1 to 4 carbon atoms and R9 and R10 are independently selected from hydrogen, hydroxy, methoxy, loweralkyl of 1 to 4 carbon atoms, or halo, or R9 and R10 can be taken together to form a methylenedioxy or ethylenedioxy bridge; or 1,4-benzodioxan of the formula <IMAGE> wherein q is 1, 2 or 3, and R11 is hydrogen, methoxy, or halo; or R3 and R4 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.
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