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    • 3. 发明授权
    • Imidazolin-2-ones
    • 咪唑啉-2-酮
    • US4845233A
    • 1989-07-04
    • US96092
    • 1987-09-11
    • Takeru Higuchi, deceasedby Kenji W. Higuchi, co-executorOoi Wong
    • Takeru Higuchi, deceasedby Kenji W. Higuchi, co-executorOoi Wong
    • C07D233/70
    • C07D233/70
    • A compound having the formula: ##STR1## wherein R, R.sub.1 and R.sub.2 are independently selected from hydrogen; hydroxy; fluorine; bromine; chlorine; C.sub.1 -C.sub.20 alkyl; C.sub.2 -C.sub.20 alkenyl; C.sub.2 -C.sub.20 alkynyl; C.sub.3 -C.sub.10 cycloalkyl; C.sub.2 -C.sub.20 (monohydroxy or polyhydroxy)alkyl; C.sub.1 -C.sub.20 (monohalo or polyhalo)alkyl; carboxy; C.sub.1 -C.sub.20 alkylcarboxy; C.sub.1 -C.sub.20 alkenylcarboxy; C.sub.1 -C.sub.20 carboxyalkyl; C.sub.1 -C.sub.20 alkanoyl; C.sub.1 -C.sub.20 alkanoyloxy; C.sub.1 -C.sub.20 alkoxycarbonyl; carbamoyl; carbamyl; C.sub.1 -C.sub.20 alkylcarbamyl; sulfo; C.sub.1 -C.sub.20 alkylsulfonyl; C.sub.1 -C.sub.20 alkylsulfinyl; C.sub.1 -C.sub.20 alkylsulfoxide; C.sub.1 -C.sub.20 alkylsulfone; thio; C.sub.1 -C.sub.20 alkylthio; amino; nitro; C.sub.1 -C.sub.20 alkylamino; C.sub.1 -C.sub.20 aminoalkyl; substituted or unsubstituted phenyl or benzyl, the substituents being selected from hydroxy, fluorine, bromine, chlorine, C.sub.1 -C.sub.20 alkyl, C.sub.2 -C.sub.20 alkenyl, C.sub.2 -C.sub.20 (monohydroxy or polyhydroxy)alkyl, X is methyl or oxygen and n is 0 to 20. The invention is also directed to a method for increasing the topical penetration of a physiologically active agent across the skin or membrane of a mammalian organism. Also claimed is a pharmaceutical composition and a novel method for preparing 1-substituted-4-imidazolin-2-one.
    • 具有下式的化合物:其中R,R 1和R 2独立地选自氢; 羟基; 氟; 溴; 氯; C 1 -C 20烷基; C2-C20烯基; C2-C20炔基; C3-C10环烷基; C2-C20(单羟基或多羟基)烷基; C 1 -C 20(单卤代或多卤代)烷基; 羧基; C 1 -C 20烷基羧基; C1-C20烯基羧基; C 1 -C 20羧基烷基; C1-C20烷酰基; C1-C20烷酰氧基; C1-C20烷氧基羰基; 氨基甲酰基; 氨基甲酰 C1-C20烷基氨基甲酰基; 磺基 C 1 -C 20烷基磺酰基; C1-C20烷基亚磺酰基; C1-C20烷基亚砜; C1-C20烷基砜; 硫代 C 1 -C 20烷硫基; 氨基; 硝基 C1-C20烷基氨基; C1-C20氨基烷基; 取代或未取代的苯基或苄基,取代基选自羟基,氟,溴,氯,C 1 -C 20烷基,C 2 -C 20烯基,C 2 -C 20(单羟基或多羟基)烷基,X为甲基或氧,n为0至 本发明还涉及增加生理活性剂穿过哺乳动物生物体的皮肤或膜的局部渗透的方法。 还要求保护的是药物组合物和制备1-取代-4-咪唑啉-2-酮的新方法。