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    • 5. 发明申请
    • Novel Benzimidazole(Thio)Carbamates with Antiparasitic Activity and the Synthesis Thereof
    • 具有抗寄生虫活性的新型苯并咪唑(Thio)氨基甲酸酯及其合成
    • US20090131369A1
    • 2009-05-21
    • US11997057
    • 2006-07-18
    • Christophe Pierre Alain Chassaing
    • Christophe Pierre Alain Chassaing
    • A61K31/675C07F9/06
    • C07F9/65068
    • This invention relates to benzimidazole carbamates and (thio)carbamates corresponding to Formula I: Here, X1 and X2 are independently O or S, wherein at least one of X1 and X2 is O; Y1 and Y2 are independently O or S, wherein at least one of Y1 and Y2 is O; R1 is alkyl having from 1-4 carbon atoms; R2, R3, and R4 are independently hydrogen or a cation; R5 and R6 are independently hydrogen, halogen, alkyl (having from 1-8 carbon atoms), —OR7, —SR8, —CO—R9, —OSO2—Ar, or —S(O)R10; R7 is alkyl having from 1-8 carbon atoms; R8 is alkyl (having from 1-8 carbon atoms) or aryl; R9 is alkyl (having from 1-8 carbon atoms), cycloalkyl (having from 3-6 carbon atoms), or aryl; Ar is aryl; and R10 is alkyl (having from 1-8 carbon atoms) or aryl. The compounds generally are soluble and stable in water, and have antiparasitic (particularly anthelmintic) activity in vivo that is comparable to known water-insoluble benzimidazole carbamates (e.g., albendazole and fenbendazole).
    • 本发明涉及对应于式I的苯并咪唑氨基甲酸酯和(硫代)氨基甲酸酯:这里,X 1和X 2独立地为O或S,其中X 1和X 2中的至少一个为O; Y1和Y2独立地为O或S,其中Y1和Y2中的至少一个为O; R1是具有1-4个碳原子的烷基; R2,R3和R4独立地为氢或阳离子; R5和R6独立地是氢,卤素,具有1-8个碳原子的烷基,-OR7,-SR8,-CO-R9,-OSO2-Ar或-S(O)R10; R7是具有1-8个碳原子的烷基; R8是烷基(具有1-8个碳原子)或芳基; R9是烷基(具有1-8个碳原子),环烷基(具有3-6个碳原子)或芳基; Ar为芳基; 和R 10是烷基(具有1-8个碳原子)或芳基。 化合物通常在水中是可溶的和稳定的,并且在体内具有与已知的水不溶性苯并咪唑氨基甲酸酯(例如阿苯达唑和芬苯达唑)相当的抗寄生虫(特别是驱肠虫)活性。