申请人:Yamanouchi Pharmaceutical Co., Ltd.
公开号:US06083955A1
公开(公告)日:2000-07-04
Novel arylethenesulfonamide derivative having a high affinity for drugs, especially endoserine receptors, and represented by general formula (I); pharmaceutically acceptable salts thereof; and drugs comprising the same as the active ingredient, especially endoserine receptor antagonist, wherein Ar: optionally substituted aryl group or optionally substituted five- to six-membered heteroaryl group; X: oxygen atom, sulfur atom or a group represented by a formula --NH--; Y: oxygen atom or sulfur atom; R.sub.1 : hydrogen atom, optionally halogen-substituted lower alkyl group, cycloalkyl group, optionally substituted aryl group or optionally substituted five- to six-membered heteroaryl group. R.sub.2 : lower alkyl group, lower alkenyl group or lower alkynyl group where each of which may be substituted with one to three substituent(s) selected from a group consisting of hydroxyl group, lower alkoxy group, cycloalkyl group, halogen atom, carboxyl group and lower alkoxycarbonyl group; R.sub.3 : phenyl group which may be substituted with one to four substituent(s) selected from a group consisting of optionally halogen-substituted lower alkyl group, lower alkoxy group, halogen atom, lower alkylthio group, lower alkylsulfinyl group, lower alkanesulfonyl group, carboxyl group, lower alkoxycarbonyl group and carbamoyl group; and R.sub.4 and R.sub.5 : they may be same or different and each is hydrogen atom or lower alkyl.
具有对药物,尤其是内源性丝氨酸受体高亲和力的新型芳基乙烯磺酰胺衍生物,其通式表示为(I); 其药学上可接受的盐; 以及作为活性成分的药物,尤其是内源性丝氨酸受体拮抗剂,其中Ar:可选取代芳基或可选取代的五至六元杂环芳基; X:氧原子,硫原子或由公式--NH--表示的基团; Y:氧原子或硫原子; R.sub.1:氢原子,可选取代的卤代低烷基,环烷基,可选取代的芳基或可选取代的五至六元杂环芳基。R.sub.2:低烷基,低烯基或低炔基,其中每个基团可能被选自羟基,低烷氧基,环烷基,卤原子,羧基和低烷氧羰基基团的一个到三个取代基所取代; R.sub.3:苯基,其可能被选自一个到四个取代基所取代,所选取代基包括可选取代的卤代低烷基,低烷氧基,卤原子,低烷硫基,低烷基硫醇基,低烷基磺酰基,羧基,低烷氧羰基基团和氨基甲酰基; R.sub.4和R.sub.5:它们可能相同或不同,每个都是氢原子或低烷基。