申请人:Solvay Pharmaceuticals GmbH
公开号:US06040303A1
公开(公告)日:2000-03-21
Neurokinin-antagonistic compounds corresponding to formula I: ##STR1## in which R.sup.1 is hydrogen or lower alkyl, R.sup.2 is hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl, and R.sup.3 is hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl, or R.sup.2 and R.sup.3 together are alkylenedioxy with 1 to 2 carbon atoms, bonded to adjacent carbon atoms of the phenyl ring, R.sup.4 is hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl, and R.sup.5 is hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl, or R.sup.4 and R.sup.5 together are alkylenedioxy with 1 to 2 carbon atoms, bonded to adjacent carbon atoms of the phenyl ring, R.sup.6 is lower alkyl, halogen or trifluoromethyl, R.sup.7 is lower alkyl, halogen or trifluoromethyl, A is a --(CH.sub.2).sub.n -- group in which n represents an integer from 1 to 3, or an --NH--(CH.sub.2).sub.m -- group in which m represents an integer from 2 to 3, and B is an alkylene chain with 1 to 3 carbon atoms optionally substituted by lower alkyl, and physiologically acceptable salts thereof and processes for the preparation of these compounds.
公式I对应的神经激肽拮抗化合物:##STR1##其中R.sup.1是氢或较低的烷基,R.sup.2是氢、较低的烷基、较低的烷氧基、卤素或三氟甲基,R.sup.3是氢、较低的烷基、较低的烷氧基、卤素或三氟甲基,或者R.sup.2和R.sup.3一起是1至2个碳原子的亚烷二氧基,与苯环的相邻碳原子相结合,R.sup.4是氢、较低的烷基、较低的烷氧基、卤素或三氟甲基,R.sup.5是氢、较低的烷基、较低的烷氧基、卤素或三氟甲基,或者R.sup.4和R.sup.5一起是1至2个碳原子的亚烷二氧基,与苯环的相邻碳原子相结合,R.sup.6是较低的烷基、卤素或三氟甲基,R.sup.7是较低的烷基、卤素或三氟甲基,A是一个--(CH.sub.2).sub.n--基团,其中n表示1至3的整数,或者一个--NH--(CH.sub.2).sub.m--基团,其中m表示2至3的整数,B是一个含有1至3个碳原子的烷基链,可选择地被较低的烷基取代,以及这些化合物的生理学上可接受的盐和制备这些化合物的方法。