申请人:Pfizer Inc.
公开号:US04243666A1
公开(公告)日:1981-01-06
Regulators of the cardiovascular system and, in particular, in the treatment of hypertension having the formula ##STR1## wherein R is lower alkyl; X, is a 3- or 4-position substituent and is --(CH.sub.2).sub.n CONR.sup.1 R.sup.2, --O(CH.sub.2).sub.n CONR.sup.1 R.sup.2 or ##STR2## wherein n is 0, 1 or 2; R.sup.1 is hydrogen or lower alkyl, and R.sup.2 is lower alkyl; lower alkenyl, lower alkynyl, phenyl, substituted phenyl, C.sub.3 -C.sub.7 cycloalkyl; lower alkyl substituted by phenyl, substituted phenyl, C.sub.3 -C.sub.7 cycloalkyl, halogen, trifluoromethyl, hydroxy, lower alkoxy, lower alkoxycarbonyl, phenoxy, substituted phenoxy or --NR.sup.3 R.sup.4 wherein R.sup.3 and R.sup.4 each represent hydrogen, lower alkyl, lower alkanoyl or lower alkylsulfonyl; with the proviso that any O, N or halogen atom in R.sup.2 is separated by at least 2 carbon atoms from the nitrogen atom to which R.sup.2 is attached; or R.sup.1 and R.sup.2 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; the pharmaceutically acceptable bioprecursors therefor, and the pharmaceutically acceptable acid addition salts thereof.
心血管系统的调节剂,尤其是治疗高血压的化合物的公式为##STR1##其中R是较低的烷基;X是3-或4-位取代基,为--(CH.sub.2).sub.n CONR.sup.1 R.sup.2,--O(CH.sub.2).sub.n CONR.sup.1 R.sup.2或##STR2##其中n为0、1或2;R.sup.1为氢或较低的烷基,而R.sup.2为较低的烷基;较低的烯基,较低的炔基,苯基,取代苯基,C.sub.3-C.sub.7环烷基;较低的烷基被苯基,取代苯基,C.sub.3-C.sub.7环烷基,卤素,三氟甲基,羟基,较低的烷氧基,较低的烷氧羰基,苯氧基,取代苯氧基或--NR.sup.3 R.sup.4取代的;其中R.sup.3和R.sup.4分别表示氢,较低的烷基,较低的烷酰基或较低的烷基磺酰基;但R.sup.2中的任何O、N或卤原子与R.sup.2连接的氮原子至少相隔2个碳原子;或R.sup.1和R.sup.2与它们连接的氮原子一起形成一个吗啡基,该吗啡基可以选择地被一个或两个较低的烷基取代,或者一个1,2,3,4-四氢异喹啉基,该基可以选择地在苯环部分被一个或两个较低的烷氧基取代;其药用上可接受的生物前体,以及其药用上可接受的酸加盐。