| 摘要 |
<p>New benzoxadiazole and benzothiadiazole derivs. are of formula (I) : R1 is H, 1-6C alkyl, 2-6c hydroxyalkyl, 3-6c alkoxyalkyl, 3-6C alkenyl, 3-6C alkyalkyl, 3-7C cycloalkyl, 4-8C cycloalkyl-alkyl, or 7-9C phenylalkyl or 9-12C phenylalkenyl in which the phenyl group is substituted by 1,2 or 3 substituents from halogen, OH, 1-4C alkyl and 1-4C alkoxy; R2 and R3 are H, 1-6C alkyl, 7-10C phenylakyl, 3-7C cycloalkyl or 4-8C cycloalkyl-alkyl; R3 and R4 are CN, COR7, COOR7, S(O)nR7 or COO-A-NR8R9; n is 0, 1 or 2. R7 is 1-6C alkyl, 3-6C alkenyl, 3-6C alkynyl, 3-7C cycloalkyl, 4-8C cycloalkylalkyl, 2-6C hydroxyalkyl, 3-6C alkoxyalkyl, 4-8C hydroxyalkoxyalkyl, 2-6C aminoalkyl, (1-4C alkylamino)-(2-6C alkyl), di(1-4C alkyl)amino-alkyl, phenyl, 7-10C phenylalkyl, a 5- or 6-membered heterocyclic ring contg. an N-, O- or S-atom as hetero atom and opt. contg. a further 1,2, or 3 ring N-atoms, or 1-4C alkyl substd. by such a heterocyclic ring; A is 1-6C alkylene; R8 and R9 are 1-6C alkyl, 3-6C alkenyl, 3-6C alkynyl, 3-7C cycloalkyl, 4-8c cycloalkylalkyl, 2-6C hydroxyalkyl, 3-6C alkoxyalkyl, 4-8C hydroxyalkoxy lkyl, 2-6C aminoalkyl, (1-4C alkylamino)(2-6C alkyl), di (1-4C alkyl) aminoalkyl, phenyl or 7-10C phenylalkyl, or NR8R9 is 5- to 7-membered ring opt. contg. 0, S or NR10 (R10 = 1-4C alky alkyl) as a further hetero atom; R6 is H, halogen, 1-4C alkyl, 1-4C alkoxy, 1-4C alkylthio, 1-4C alkylsulphonyl, CF3, NO2, OH, N3, NH2, 1-4C alkylamino, di(1-4C alkyl) amino, 1-5C alkanamido, 2-5C carbalkoxy, aminocarbonyl, OCF3, CN, sulphamoyl, 1-4C alkylsulphamoyl or di(1-4C alkyl)sulphamoyl; and X is O or S; with provisos. (I) are coronary vasodilators and have a favourable activity against angina pectoris. They also increase blood flow in the brain and in the legs. In addition, (I) have calcium antagonistic and antihypertensive activities.</p> |
