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    • 9. 发明申请
    • DICATIONIC 2,5-DIARYLFURAN AZA-ANALOGS AS ANTI-PROTOZOAN AGENTS
    • 作为抗真菌药物的二异丙基呋喃亚胺类似物
    • WO2004050018A3
    • 2004-07-08
    • PCT/US0337691
    • 2003-11-25
    • UNIV NORTH CAROLINAUNIV GEORGIA STATE RES FOUNDBOYKIN DAVID WTIDWELL RICHARD RISMAIL MOHAMED ABRUN RETO
    • BOYKIN DAVID WTIDWELL RICHARD RISMAIL MOHAMED ABRUN RETO
    • A61K20060101A61K31/4178A61K31/422A61K31/427A61K31/443A61K31/4436A61K31/444A61K31/497A61K31/501A61K31/506C07D405/04C07D409/04
    • C07D307/38C07D307/54C07D333/08C07D405/04C07D405/14C07D407/04C07D407/14C07D409/04C07D409/14
    • A compound of Formula (I): wherein: X is selected from the group consisting of O, S, and NR where R is hydrogen or lower alkyl; C , C , A, and Y are CH, N, NR O, or S, wherein C and C are the same or different; D , D , B, and Z are CH, N, or NR wherein D and D are the same or different; provided that B, Z, or both B and Z are not present when A, Y, or both A and Y are O, S, or NR ; R ,R , R , R , R and R are selected from the group consisting of H, lower alkyl, halogen, alkoxyl, aryloxyl, aralkoxy and hydroxyl; R and R are each independently selected from the group consisting of H, hydroxy, lower alkyl, cycloalkyl, aryl, aralkyl, alkoxyl, hydroxycycloalkyl, alkoxycycloalkyl, hydroxyalkyl, aminoalkyl, acyloxy, acetoxy, and alkylaminoalkyl; and R , R , R and R are each independently selected from the group consisting of H, lower alkyl, alkoxyalkyl, cycloalkyl, aryl, aralkyl, hydroxyalkyl, aminoalkyl, and alkylaminoalkyl, or R and R together or R and R together represent a C2 to C10 alkyl, hydroxyalkyl, or alkylene, or R and R together or R and R together are: wherein n is a number from 1 to 3, and R is H or-CONHR NR R , wherein R , is lower alkyl and R and R are each independently selected from the group consisting of H and lower alkyl.
    • 式(I)的化合物:其中:X选自O,S和NR 17,其中R 17是氢或低级烷基; C 1,C 2,A和Y是CH,N,NR 17,O或S,其中C 1和C 2相同或不同; D 1,D 2,B和Z是CH,N或NR 17,其中D 1和D 2是相同或不同的; 条件是当A,Y或A和Y都为O,S或NR 17时,B,Z或两者均不存在B和Z。 R 13,R 14,R 15,R 16,R 1和R 8选自H,低级烷基,卤素,烷氧基,芳氧基,芳烷氧基和羟基 ; R 3和R 6各自独立地选自H,羟基,低级烷基,环烷基,芳基,芳烷基,烷氧基,羟基环烷基,烷氧基环烷基,羟基烷基,氨基烷基,酰氧基,乙酰氧基和烷基氨基烷基。 和R 2,R 4,R 5和R 7各自独立地选自H,低级烷基,烷氧基烷基,环烷基,芳基,芳烷基,羟基烷基,氨基烷基和烷基氨基烷基,或 R 2和R 4一起或R 5和R 7一起代表C 2至C 10烷基,羟烷基或亚烷基,或R 3和R 4一起或R 6和 R 7一起是:其中n是1至3的数,R 9是H或-CONHR 10 NR 11 R 12,其中R 10是低级烷基和R <11>和R 12各自独立地选自H和低级烷基。