公开(公告)号：US06307070B1

公开(公告)日：2001-10-23

申请号：US09122257

申请日：1998-07-24

申请人： Wai-Lam Alex Chu ,  Flemming R. Jensen ,  Thomas B. Jensen ,  James B. McAlpine ,  Birgitte Søkilde ,  Alexandra M. SantAna-Sørensen ,  Sunil Ratnayake ,  Jack B. Jiang ,  Catharine Noble ,  Angela M. Stafford

发明人： Wai-Lam Alex Chu ,  Flemming R. Jensen ,  Thomas B. Jensen ,  James B. McAlpine ,  Birgitte Søkilde ,  Alexandra M. SantAna-Sørensen ,  Sunil Ratnayake ,  Jack B. Jiang ,  Catharine Noble ,  Angela M. Stafford

IPC分类号： C07D30783

CPC分类号： C07D307/82 ,  A61K31/343 ,  C07D307/83

摘要： A method for treating a fungal infection is disclosed. The method includes administering to a patient a pharmaceutical composition containing a compound of formula (IA): where each R is independently H, OH, Br, Cl, I, amino, thiol, nitro, C1-4 alkoxy, C1-4 alkenyloxy, C2-6 alkoxyalkyleneoxy, C1-4 alkylthio, C3-18 alkyl, or C3-18 alkenyl; or two adjacent R's, taken together, are a C2-18 bivalent moiety containing at least one oxgen atom, substituted or disubstituted with A or B or both, A being H, OH, Br, Cl, I, amino, or thiol, and B being H, C1-10 alkyl, C2-18 alkenyl, or C6-18 aryl; provided at least two Rs are not H; X is C4-10 alkyl, C4-20 alkenyl, or a C4-20 single, C6-20 bridged, or C6-20 fused ring moiety containing cycloalkyl, cycloalkenyl, aryl, heterocycle, or heteroaryl, where X is substituted with H, OH, Cl, Br, I, amino, cyano, nitro, alkyl, alkoxy, alkenyl, or alkenyloxy; provided that if X is a heteroaryl or heterocyclic moiety where two Rs are each OH and meta to each other, then the remaining R is H and ortho to each of the two hydroxyls, and Y and Z are each O and a ring atom of X is linked directly to the sp2 carbon atom adjacent to X, then substituted with H, OH, Cl, Br, I, amino, cyano, alkyl, alkoxy, alkenyl, or alkenyloxy; and each of Y and Z is independently selected from O, S, and NH; or a pharmaceutically acceptable salt or ester thereof.

摘要翻译： 公开了一种治疗真菌感染的方法。 该方法包括向患者施用含有式（IA）化合物的药物组合物：其中每个R独立地为H，OH，Br，Cl，I，氨基，硫醇，硝基，C 1-4烷氧基，C 1-4链烯氧基， C 2-6烷氧基亚烷基氧基，C 1-4烷硫基，C 3-8烷基或C 3-8烯基; 或两个相邻的R一起是含有至少一个被A或B或两者取代或二取代的氧原子的C2-18二价部分，A是H，OH，Br，Cl，I，氨基或硫醇，以及 B是H，C 1-10烷基，C 2-8烯基或C 6-18芳基; 提供至少两个R不是H; X是C 4-10烷基，C 4-20链烯基，或含有环烷基，环烯基，芳基，杂环或碳原子的C 4-20单-C6-20桥环或C6-20稠环部分 杂芳基，其中X被H，OH，Cl，Br，I，氨基，氰基，硝基，烷基，烷氧基，烯基或烯氧基取代; 条件是如果X是杂芳基或杂环部分，其中两个R 5各自为OH并且彼此相互间隔，则剩余的R是H和两个羟基中的每一个的邻位，Y和Z各自为O，X为环原子 直接与X相邻的sp2碳原子连接，然后用H，OH，Cl，Br，I，氨基，氰基，烷基，烷氧基，烯基或烯氧基取代; Y和Z各自独立地选自O，S和NH; 或其药学上可接受的盐或酯。