Tetrahydro-benzo ¬e| isoindolines

C - Chemistry – Metallurgy – 07 – D

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260/317, 260/306

C07D 209/62 (2006.01) C07D 209/66 (2006.01) C07D 405/02 (2006.01) C07D 405/06 (2006.01)

Patent

CA 1215376

ABSTRACT OF THE DISCLOSURE Disclosed herein are tetrahydro-benzo [e] isoindolines useful in the treatment of hypertension 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, benzyloxy, benzoyloxy, thiomethyl, halo, or Image wherein R4 and R5 are independently selected from hydrogen, loweracyl of 1 to 4 carbon atoms or sulfonyl of the formula wherein R6 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 is 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, R7 is hydrogen or loweralkyl of 1 to 4 carbon atoms and R8 and R9 are independently selected from hydrogen, hydroxy, methoxy, loweralkyl of 1 to 4 carbon atoms, or halo, or R8 and R9 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 R10 is hydrogen, methoxy, or halo; and the pharmaceutically acceptable salts thereof, and pharmaceutical compositions comprising compounds of formula (I) and a pharmaceutically accepta- ble carrier or diluent.

429181

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