申请人:Sankyo Company, Limited
公开号:US05616599A1
公开(公告)日:1997-04-01
Compounds of the following formula (I) or the formula (I).sub.p : ##STR1## wherein R.sup.1 is alkyl or alkenyl; R.sup.2 and R.sup.3 are hydrogen, alkyl, alkenyl, cycloalkyl, aralkyl, aryl, or aryl fused to cycloalkyl; R.sup.4 is hydrogen, alkyl, alkanoyl, alkenoyl, arylcarbonyl, alkoxycarbonyl, tetrahydropyranyl, tetrahydrothiopyranyl, tetrahydrothienyl, tetrahydrofuryl, a group of formula --SiR.sup.a R.sup.b R.sup.c, in which R.sup.a, R.sup.b and R.sup.c are alkyl or aryl, alkoxymethyl, (alkoxyalkoxy)methyl, haloalkoxymethyl, aralkyl, aryl or alkanoyloxymethoxycarbonyl; R.sup.5 is carboxy or --CONR.sup.8 R.sup.9, wherein R.sup.8 and R.sup.9 hydrogens or alkyl, or R.sup.8 and R.sup.9 together form alkylene; R.sup.6 is hydrogen, alkyl, alkoxy or halogen; R.sup.7 is carboxy or tetrazol-5-yl; R.sub.p.sup.1 is hydrogen, alkyl, cycloalkyl or alkanoyl; R.sub.p.sup.2 is a single bond, alkylene or alkylidene; R.sub.p.sup.3 and R.sub.p.sup.4 are each hydrogen or alkyl; R.sub.p.sup.6 is carboxy or tetrazol-5-yl; and X.sub.p is oxygen or sulfur; and pharmaceutically acceptable salts and esters thereof. The compounds are AII receptor antagonists and thus have hypotensive activity and can be used for the treatment and prophylaxis of hypertension. The compounds may be prepared by reacting a biphenylmethyl compound with an imidazole compound.
以下式(I)或式(I).sub.p的化合物:其中R.sup.1是烷基或
烯基;R.sup.2和R.sup.3是
氢、烷基、
烯基、
环烷基、芳基烷基、芳基或与
环烷基融合的芳基;R.sup.4是
氢、烷基、烷酰基、
烯酰基、芳基羰基、烷
氧羰基、
四氢吡喃基、四
氢硫代
吡喃基、
四氢噻吩基、
四氢呋喃基,具有式--SiR.sup.a R.sup.b R.sup.c的基团,其中R.sup.a、R.sup.b和R.sup.c是烷基或芳基、烷
氧甲基、(烷
氧基烷
氧基)
甲基、卤代烷
氧甲基、芳基烷基、芳基或烷酰
氧甲
氧羰基;R.sup.5是羧基或--CONR.sup.8 R.sup.9,其中R.sup.8和R.sup.9是
氢或烷基,或R.sup.8和R.sup.9一起形成亚烷基;R.sup.6是
氢、烷基、烷
氧基或卤素;R.sup.7是羧基或
四唑-5-基;R.sub.p.sup.1是
氢、烷基、
环烷基或烷酰基;R.sub.p.sup.2是单键、烷基或烷基亚
甲基;R.sub.p.sup.3和R.sub.p.sup.4分别是
氢或烷基;R.sub.p.sup.6是羧基或
四唑-5-基;X.sub.p是
氧或
硫;以及其药学上可接受的盐和
酯。这些化合物是AII受体
拮抗剂,因此具有降压活性,可用于治疗和预防高血压。这些化合物可以通过将
联苯甲基化合物与
咪唑化合物反应制备而成。