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    • 10. 发明申请
    • METHOD FOR THE CONTROL OF HYPERLIPIDEMIA
    • 控制高脂血症的方法
    • WO1990000897A1
    • 1990-02-08
    • PCT/US1989003246
    • 1989-07-27
    • UNIVERSITY OF NORTH CAROLINA AT CHAPEL HILLNORTH CAROLINA CENTRAL UNIVERSITY
    • UNIVERSITY OF NORTH CAROLINA AT CHAPEL HILLNORTH CAROLINA CENTRAL UNIVERSITYIZYDORE, Robert, A.HALL, Iris, H.
    • A61K31/53
    • A61K31/53A61K31/41
    • The invention provides pharmaceutical compositions comprising hypolipidemically active derivatives of 1,2,4-triazolidine-3,5-diones, 1,3,5-triazabicyclo[3.1.0]hexane-2,4-diones, and 1,3,5-triazine-2,4(1H,3H)-diones in a pharmaceutically acceptable carrier for treating hyperlipidemia in mammals, particularly humans. The present invention is also directed to a method of controlling hyperlipidemia in mammals which comprises administering to a mammal an amount effective to control hyperlipidemia of a compound having hypolipidemic activity and structural formula (I), wherein R is hydrogen, a C1 to C18 alkyl or substituted alkyl, a C2 to C18 alkenyl or substituted alkenyl, a C2 to C18 alkynyl or substituted alkynyl, a C4 to C10 cycloalkyl or substituted cycloalkyl, a C4 to C10 cycloalkenyl or substituted cycloalkenyl, phenyl, a substituted phenyl, cyano, phenalkyl, -CO-R or -Y-CO-R ; R is (a), (b), (c), R and R can be the same or different and are each the same as R ; R , R and R can be the same or different and are each hydrogen, a C1 to C18 alkyl or substituted alkyl, a C2 to C18 alkenyl or substituted alkenyl, a C1 to C18 alkynyl or substituted alkynyl, a C4 to C10 cycloalkyl or substituted cycloalkyl, a C4 to C10 cycloalkenyl or substituted cycloalkenyl, phenyl or substituted phenyl, phenalkyl, -CO-R , or -Y-CO-R , with the proviso that R5 and R together cannot be so bulky as to cause the compound to decompose; R is hydrogen, a C1 to C5 alkyl, a C4 to C10 cycloalkyl, -CO-R , or -Y-CO-R ; R is hydrogen, a C1 to C5 alkyl or substituted alkyl, a C2 to C5 alkenyl or substituted alkenyl, a C2 to C5 alkynyl or substituted alkynyl, phenyl or substituted phenyl, phenoxy or substituted phenoxy, a C1 to C5 alkoxy or substituted alkoxy, a C4 to C10 cycloalkyl or substituted cycloalkyl, a C4 to C10 cycloalkenyl or substituted cycloalkenyl, -NHC6C5, -NR R wherein R and R can be the same or different and are each hydrogen, a C1 to C5 alkyl or substituted alkyl, phenyl or substituted phenyl; Y is a C1 to C10 alkylene or substituted alkylene; R is -CO, -COH, -CS, -CSH, or a C1 to C4 alkylene group; and the pharmaceutically acceptable salts, and mixtures thereof.
    • 本发明提供药物组合物,其包含1,2,4-三唑烷-3,5-二酮,1,3,5-三氮杂双环[3.1.0]己烷-2,4-二酮的降血脂活性衍生物和1,3,5 - 三嗪-2,4(1H,3H) - 二酮在用于治疗哺乳动物,特别是人类的高脂血症的药学上可接受的载体中。 本发明还涉及一种控制哺乳动物高脂血症的方法,其包括向哺乳动物施用有效控制具有降血脂活性的化合物的高脂血症的量和结构式(I),其中R 1是氢,C1至 C18烷基或取代的烷基,C2至C18烯基或取代的烯基,C2至C18炔基或取代的炔基,C4至C10环烷基或取代的环烷基,C4至C10环烯基或取代的环烯基,苯基,取代的苯基,氰基, 苯基烷基,-CO-R 9或-Y-CO-R 9; R 2是(a),(b),(c),R 3和R 4可以相同或不同,并且各自与R 1相同; R 5,R 6和R 7可以相同或不同,各自为氢,C1至C18烷基或取代的烷基,C2至C18烯基或取代的烯基,C1至C18炔基或取代的 炔基,C4至C10环烷基或取代的环烷基,C4至C10环烯基或取代的环烯基,苯基或取代的苯基,苯基烷基,-CO-R9或-Y-CO-R9,条件是 R 5和R 6一起不能如此庞大,导致化合物分解; R 8是氢,C 1至C 5烷基,C 4至C 10环烷基,-CO-R 9或-Y-CO-R 9; R 9是氢,C 1至C 5烷基或取代的烷基,C 2至C 5烯基或取代的烯基,C 2至C 5炔基或取代的炔基,苯基或取代的苯基,苯氧基或取代的苯氧基,C 1至C 5的烷氧基或 取代的烷氧基,C 4至C 10环烷基或取代的环烷基,C 4至C 10环烯基或取代的环烯基,-NHC 6 C 5,-NR 10 R 11其中R 10和R 11可以相同或不同, 各自为氢,C1至C5烷基或取代的烷基,苯基或取代的苯基; Y是C1至C10亚烷基或取代的亚烷基; R 12是-CO,-COH,-CS,-CSH或C1〜C4亚烷基; 及其药学上可接受的盐及其混合物。