| 摘要 |
HA486 BENZAZEPINE AND BENZOTHIAZEPINE DERIVATIVES Vasodilating activity is exhibited by compounds having the formula and the pharmaceutically acceptable salts thereof, wherein X is -CH2- or -S-; R1 is or -O-Y3; R2 is heterocyclo or heteroaryl; R3 and R4 are each independently hydrogen, halogen, alkyl, alkoxy, aryloxy, arylalkoxy, arylalkyl, cyano, hydroxy, alkanoyloxy, , fluoro-substituted alkoxy, fluoro-substituted alkyl, (cycloalkyl)alkoxy, -NO2, -NY10Y11, -S(O)kalkyl, -S(O)karyl or ; HA486 n is 0, 1, 2 or 3; m is 0, 1, 2 or 3; k is 0, 1 or 2; Y1 and Y2 are each independently hydrogen or alkyl; or Y1 is hydrogen and Y2 is alkenyl, alkynyl, aryl, heteroaryl, or cycloalkyl; or Y and Y2, together with the carbon atom to which they are attached, are cycloalkyl; Y3 is hydrogen, alkyl, alkanoyl, alkenyl, arylcarbonyl, heteroarylcarbonyl, or ; Y8 and Y9 are each independently hydrogen, alkyl, aryl, or heteroaryl; or Y8 and Y9, together with the nitrogen atom to which they are attached, are pyrrolidinyl, piperidinyl or morpholinyl; Y10 and Y11 are each independently hydrogen, alkyl, alkanoyl, arylcarbonyl, heteroarylcarbonyl, or ; Y12 is hydroxy, alkoxy, aryloxy, amino, alkylamino, or dialkylamino; and Y13 is alkyl, alkoxy or aryloxy.
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