| 摘要 |
<p>This invention provides novel antihypertensives which are 4-amino-2-piperidinoquinazolines of the formula < IMG > (I) wherein R is lower alkyl; and X, which is attached to the 3- or 4- position of the piperidino group, is a group of the formula: (i) -CH2)nCONR1R2, (ii) -O(CH2)nCONR1R2 or (iii) -< IMG >, wherein n is 0, 1 or 2; and either R1 is hydrogen or lower alkyl, and R2 is lower alkyl; phenyl, lower alkylphenyl, lower alkoxyphenyl or halophenyl; C3-C7 cycloalkyl; or lower alkyl substituted by phenyl, lower alkylphenyl, lower alkoxyphenyl, halophenyl, C3-C7 cycloalkyl, halogen, trifluoromethyl, hydroxy, lower alkoxy, lower alkenyl, lower alkynyl, lower alkoxycarbonyl, phenoxy, lower alkylphenoxy, lower alkoxyphenoxy, halophenoxy or a group of the formula: -NR3R4 wherein R3 and R4 each independently represent hydrogen, lower alkyl, lower alkanoyl or lower alkylsulfonyl; with the proviso that any O, N or halogen atom in R2 is separated by at least 2 carbon atoms from the nitrogen atom to which R2 is attached; or R1 and R2 taken together with the nitrogen atom to which they are attached form a morpholino group optionally substituted by one or two lower alkyl groups, or a 1,2,3,4-tetrahydroisoquinolyl group optionally substituted on the benzene ring portion by one or two lower alkoxy groups; and the pharmaceutically acceptable acid addition salts thereof.</p> |
