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    • 2. 发明授权
    • 1,2,4-triazine-3, 5-dione derivatives, their production and use thereof
    • 1,2,4-三嗪-3,5-二酮衍生物,其制备和用途
    • US5985875A
    • 1999-11-16
    • US921047
    • 1997-08-29
    • Hideki MikiIsao AokiKoichi IwanagaToshikatsu Hayashi
    • Hideki MikiIsao AokiKoichi IwanagaToshikatsu Hayashi
    • C07D253/075C07D401/10A61K31/53
    • C07D253/075C07D401/10
    • The present invention relates to compounds represented by the formula: ##STR1## wherein R.sup.1 is (1) an optionally substituted alkyl group which may be bonded through a hetero atom, (2) an optionally substituted acyl group, (3) an alkylsulfonyl group, (4) an alkylsulfinyl group, or (5) an optionally substituted sulfamoyl group; A is --N.dbd. or -CH.dbd.; R.sup.2 is a hydrogen atom or an alkyl group which may optionally be substituted with halogen and which may be bonded through a hetero atom;X.sup.1 is halogen or a lower alkyl group;X.sup.2 is a hydrogen atom or a fluorine atom;R.sup.3 is a hydrogen atom, halogen or a lower alkyl group;and R.sup.4 is a hydrogen atom, an optionally substituted alkyl group or an acyl group, provided that when R.sup.1 is (1) a C.sub.1-4 alkanoyl group, (2) benzoyl, (3) trifluoroacetyl, (4) sulfamoyl which may optionally be substituted with a C.sub.1-4 alkyl group, (5) a C.sub.1-4 alkyl group which may optionally be substituted with hydroxy, halogen or a C.sub.1-3 alkoxy group, (6) amino which is substituted with a C.sub.14 alkyl group, A is --CH.dbd., R.sup.2 is a hydrogen atom, X.sup.1 is a chlorine atom, R.sup.3 is a chlorine atom, and X.sup.2 is a hydrogen atom, then R.sup.4 is an optionally substituted alkyl group or an optionally substituted acyl group; or salts thereof, their production and use thereof. These compounds and salts thereof are useful as anti-protozoal agents.
    • 本发明涉及由下式表示的化合物:其中R1是(1)可以通过杂原子键合的任选取代的烷基,(2)任选取代的酰基,(3)烷基磺酰基,(4) 烷基亚磺酰基,或(5)任选取代的氨磺酰基; A是-N =或-CH =; R2是氢原子或可以被卤素取代的烷基,可以通过杂原子键合; X1是卤素或低级烷基; X2是氢原子或氟原子; R3是氢原子,卤素或低级烷基; 并且R 4为氢原子,任选取代的烷基或酰基,条件是当R 1为(1)C 1-4烷酰基时,(2)苯甲酰基,(3)三氟乙酰基,(4)氨磺酰基,其可任选地为 被C 1-4烷基取代,(5)可任意被羟基,卤素或C 1-3烷氧基取代的C 1-4烷基,(6)被C 14烷基取代的氨基,A是 -CH =,R2为氢原子,X1为氯原子,R3为氯原子,X2为氢原子,R4为任意取代的烷基或任选取代的酰基; 或其盐,其生产和使用。 这些化合物及其盐可用作抗原生动物剂。