申请人:Nelson Research & Development Co.
公开号:US04652573A1
公开(公告)日:1987-03-24
Compounds having calcium channel antagonist activity of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are each independently amino, trifluoromethyl, pentafluoroethyl, alkoxy, lower alkenyl, or lower alkynyl or branched or unbranched lower alkyl, which is unsubstituted or is substituted with cyano, hydroxy, acyloxy, hydrazino, lower alkyl amino, or di(lower alkyl)-amino or 5 or 6 membered saturated nitrogen-containing heterocyclic-1-yl, which is unsubstituted or is substituted with oxo, hydroxy, alkyl, and hydroxy (lower alkyl) R.sub.3 is straight- or branched-chain C.sub.1 to C.sub.12 alkyl, alkenyl, alkynyl, or cycloalkyl, and is either unsubstituted or substituted with hydroxy, acyloxy, cyano, di(lower alkyl) amino 5- or 6-membered saturated nitrogen-containing heterocyclic-1-yl or R.sub.3 is --A-R.sub.4, A is a straight- or branched-chain hydrocarbon moiety containing from 2 to 12 carbon atoms and from 0 to 2 double bonds, R.sub.4 is selected from the group consisting of: ##STR2## R.sub.5 is hydrogen, nitro, cyano, azido, amino, trifluoromethyl, alkylamino, dialkylamino, halo, carboxyl, carbalkoxy, alkyl, alkenyl, alkynyl, cycloalkyl, acylamino, carboxamido, sulfonamide, and SO.sub.m -(lower)alkyl where m is 0, 1, or 2 and R.sub.6 is aryl or heteroaryl or a pharmaceutically-acceptable salt thereof are disclosed. Also disclosed is a method of treating hypertension and other disorders by administering an effective amount of a compound of the present invention.
具有钙通道拮抗活性的化合物的结构式:##STR1##其中R.sub.1和R.sub.2分别独立地是氨基,三氟甲基,五氟乙基,烷氧基,较低烯基,或较低炔基,或者是支链或非支链较低烷基,未取代或取代有氰基,羟基,酰氧基,叠氮基,较低烷基氨基,或二(较低烷基)-氨基,或未取代或取代有氧代基,羟基,烷基和羟基(较低烷基)的5或6元饱和氮杂环基-1-基,R.sub.3是直链或支链C.sub.1至C.sub.12烷基,烯基,炔基或环烷基,未取代或取代有羟基,酰氧基,氰基,二(较低烷基)氨基,5-或6-元饱和氮杂环基-1-基,或R.sub.3是--A-R.sub.4,A是含有2至12个碳原子和0至2个双键的直链或支链碳氢基团,R.sub.4选自以下群体之一:##STR2##R.sub.5是氢,硝基,氰基,偶氮基,氨基,三氟甲基,烷基氨基,二烷基氨基,卤素,羧基,羧酰氧基,烷基,烯基,炔基,环烷基,酰氨基,羧胺基,磺酰胺基,和SO.sub.m -(较低)烷基,其中m为0,1或2,R.sub.6是芳基或杂环芳基,或其药用可接受盐。还公开了通过给予本发明的化合物的有效量来治疗高血压和其他疾病的方法。