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    • 6. 发明申请
    • ARYLETHENESULFONAMIDE DERIVATIVES AND DRUG COMPOSITION CONTAINING THE SAME
    • 芳香酰胺衍生物和含有其的药物组合物
    • WO1997022595A1
    • 1997-06-26
    • PCT/JP1996003701
    • 1996-12-19
    • YAMANOUCHI PHARMACEUTICAL CO., LTD.HARADA, HironoriKAZAMI, Jun-ichiWATANUKI, SusumuTSUZUKI, RyujiSUDOU, KatsumiTANAKA, Akihiro
    • YAMANOUCHI PHARMACEUTICAL CO., LTD.
    • C07D239/46
    • C07D239/47C07D239/52C07D401/04C07D405/04C07D409/04C07D409/14C07D417/04
    • Novel arylethenesulfonamide derivatives having a high affinity for drugs, especially endoserine receptors, and represented by general formula (I); pharmacologically acceptable salts thereof; and drugs comprising the same as the active ingredient, especially endoserine receptor antagonists, wherein Ar represents optionally substituted aryl or optionally substituted five- or six-membered heteroaryl; X represents oxygen, sulfur, or the group represented by -NH-; Y represents oxygen or sulfur; R1 represents hydrogen, lower alkyl optionally substituted with halogeno, cycloalkyl, optionally substituted aryl, or optionally substituted five- or six-membered heteroaryl; R2 represents lower alkyl, lower alkenyl, or lower alkynyl each optionally substituted with one to three groups selected among hydroxy, lower alkoxys, cycloakyls, halogens, carboxy, and lower alkoxycarbonyls; R3 represents phenyl optionally substituted with one to four groups selected among optionally halogenated lower alkyls, lower alkoxys, halogens, lower alkylthios, lower alkylsulfinyls, lower alkanesulfonyls, carboxy, lower alkoxycarbonyls, and carbamoyl; and R4 and R5 are the same or different and each represents hydrogen or lower alkyl.
    • 用于药物,特别是内啡肽受体的高亲和力的由通式(I)表示的新型芳酰基磺酰胺衍生物; 其药理学上可接受的盐; 和包含与活性成分相同的药物,特别是内啡肽受体拮抗剂,其中Ar表示任选取代的芳基或任选取代的五元或六元杂芳基; X表示氧,硫或-NH-表示的基团; Y表示氧或硫; R 1表示氢,任选被卤代,环烷基,任选取代的芳基或任选取代的五元或六元杂芳基取代的低级烷基; 每个任选被一至三个选自羟基,低级烷氧基,环烷基,卤素,羧基和低级烷氧基羰基的基团取代的低级烷基,低级烯基或低级炔基; R 3表示任选被一至四个选自任选卤代的低级烷基,低级烷氧基,卤素,低级烷硫基,低级烷基亚磺酰基,低级烷磺酰基,羧基,低级烷氧基羰基和氨基甲酰基的基团取代的苯基。 且R 4和R 5相同或不同,各自表示氢或低级烷基。