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    • 4. 发明申请
    • ARYLETHANOLAMINE DERIVATIVES AND THEIR USE AS AGONISTS OF ATYPICAL BETA-ADRENOCEPTORS
    • 芳香胺衍生物及其作为原子反应的激动剂使用
    • WO1997021665A1
    • 1997-06-19
    • PCT/EP1996005469
    • 1996-12-06
    • GLAXO GROUP LIMITEDGREEN, Richard, HowardFOXTON, Michael, Walter
    • GLAXO GROUP LIMITED
    • C07C229/42
    • C07D209/08C07C217/84C07C229/42C07D215/04
    • The present invention relates to phenethanolamine derivatives of formula (I) wherein R represents an aryl group optionally substituted by one or more substituents selected from halogen, hydroxy, C1-6alkoxy, C1-6alkyl, nitro, cyano, hydroxymethyl and trifluoromethyl; R represents hydrogen or C1-6alkyl; R represents a group (A) where the ring is substituted by one to four further substituents selected from C1-6alkyl, halogen, trifluoromethyl, and C1-6alkoxy; or R represents a group (B) where the aromatic ring is optionally substituted by up to three further substituents selected from C1-6alkyl, halogen, trifluoromethyl, and C1-6alkoxy; R represents hydrogen, or C1-6alkyl; R represents ZCH2CO2H wherein Z represents a bond, or O; Y represents (CH2)n where n is 1-3; and physiologically acceptable derivatives thereof; to processes for their preparation; and their use in the treatment of conditions susceptible of amelioration by an atypical beta-adrenoceptor agonist.
    • 本发明涉及式(I)的苯乙醇胺衍生物,其中R 1表示任选被一个或多个选自卤素,羟基,C 1-6烷氧基,C 1-6烷基,硝基,氰基,羟甲基和三氟甲基的取代基取代的芳基; R 2表示氢或C 1-6烷基; R 3表示其中环被1-4个其它取代基取代的基团(A),所述取代基选自C 1-6烷基,卤素,三氟甲基和C 1-6烷氧基; 或R 3表示其中芳环任选被至多三个选自C 1-6烷基,卤素,三氟甲基和C 1-6烷氧基的其它取代基取代的基团(B); R 4表示氢或C 1-6烷基; R 5表示ZCH 2 CO 2 H,其中Z表示键或O; Y表示(CH2)n,其中n为1-3; 及其生理上可接受的衍生物; 进行准备; 以及它们用于治疗易受非典型β-肾上腺素受体激动剂改善的病症。