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1. 发明申请

WO1996040117A1 METHODS OF TREATING MICROBIAL INFECTIONS 审中-公开
标题翻译：治疗微生物感染的方法
公开(公告)号：WO1996040117A1
公开(公告)日：1996-12-19
申请号：PCT/US1996008972
申请日：1996-06-03
申请人： THE UNIVERSITY OF NORTH CAROLINA AT CHAPEL HILL , GEORGIA STATE UNIVERSITY RESEARCH FOUNDATION, INC. , DUKE UNIVERSITY , AUBURN UNIVERSITY , TIDWELL, Richard, R. , HALL, James, E. , BOYKIN, David, W. , DYKSTRA, Christine, C. , PERFECT, John, R. , BLAGBURN, Byron, L.
发明人： THE UNIVERSITY OF NORTH CAROLINA AT CHAPEL HILL , GEORGIA STATE UNIVERSITY RESEARCH FOUNDATION, INC. , DUKE UNIVERSITY , AUBURN UNIVERSITY
IPC分类号： A61K31/40
CPC分类号： C07D403/04 , A61K31/403 , A61K31/4178 , A61K31/4184 , A61K31/506 , C07D209/86 , C07D209/88 , C07D403/14 , Y02A50/488
摘要： The present invention provides methods for treating Cryptococcus neoformans, Cryptosporidium parvum, and Candida albicans in a subject in need of such treatment. The methods comprise administering to the subject a compound of Formula (I), wherein X is located in the para or meta positions and is loweralkyl, loweralkoxy, alkoxyalkyl, hydroxyalkyl, aminoalkyl, alkylaminoalkyl, cycloalkyl, aryl, alkylaryl, halogen, or (a), wherein each R2 is independently selected from the group consisting of H, loweralkyl, alkoxyalkyl, hydroxyalkyl, aminoalkyl, alkylaminoalkyl, cycloalkyl, aryl, or alkylaryl or two R2 groups together represent C2-C10 alkylene, or two R2 groups together represent (b), wherein m is from 1-3 and R4 is H, (c) or -CONHR5NR6R7, wherein R5 is loweralkyl, R6 and R7 are each independently selected from the group consisting of H and lower alkyl; each R8 is independently selected from the group consisting of H, loweralkyl, alkoxyalkyl, hydroxyalkyl, aminoalkyl, alkylaminoalkyl, cycloalkyl, aryl, or alkylaryl, or two R8 groups together represent C2-C10 alkylene; R9 is H, hydroxy, loweralkyl, alkoxyalkyl, hydroxyalkyl, aminoalkyl, alkylaminoalkyl, cycloalkyl, aryl, or alkylaryl; R3 is H, hydroxy, loweralkyl, alkoxyalkyl, hydroxyalkyl, aminoalkyl, alkylaminoalkyl, cycloalkyl, aryl, or alkylaryl; R1 is H, loweralkyl, alkoxyalkyl, hydroxyalkyl, aminoalkyl, alkylaminoalkyl, cycloalkyl, aryl, alkylaryl, or halogen; or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明提供了在需要这种治疗的受试者中治疗隐球菌新隐球蛋白，小隐孢子虫和白色念珠菌的方法。所述方法包括向受试者施用式（I）化合物，其中X位于对位或间位，且为低级烷基，低级烷氧基，烷氧基烷基，羟烷基，氨基烷基，烷基氨基烷基，环烷基，芳基，烷基芳基，卤素或（），其中每个R 2独立地选自H，低级烷基，烷氧基烷基，羟基烷基，氨基烷基，烷基氨基烷基，环烷基，芳基或烷基芳基或两个R 2基团一起表示C 2 -C 10亚烷基，或两个R 2基团一起表示（b ），其中m为1-3，R4为H，（c）或-CONHR5NR6R7，其中R5为低级烷基，R6和R7各自独立地选自H和低级烷基; 每个R 8独立地选自H，低级烷基，烷氧基烷基，羟基烷基，氨基烷基，烷基氨基烷基，环烷基，芳基或烷基芳基，或两个R 8基团一起表示C 2 -C 10亚烷基; R9是H，羟基，低级烷基，烷氧基烷基，羟基烷基，氨基烷基，烷基氨基烷基，环烷基，芳基或烷基芳基; R3是H，羟基，低级烷基，烷氧基烷基，羟基烷基，氨基烷基，烷基氨基烷基，环烷基，芳基或烷基芳基; R1是H，低级烷基，烷氧基烷基，羟基烷基，氨基烷基，烷基氨基烷基，环烷基，芳基，烷基芳基或卤素; 或其药学上可接受的盐。

2. 发明申请

WO1996015126A1 FURAN DERIVATIVES FOR INHIBITING PNEUMOCYSTIS CARINII PNEUMONIA, GIARDIA LAMBLIA AND CRYPTOSPORIDIUM PARVUM 审中-公开
标题翻译：用于抑制肺炎球菌CARINII PNEUMONIA，GIARDIA LAMBLIA和CRYPTOSPORIDIUM PARVUM的FURAN衍生物
公开(公告)号：WO1996015126A1
公开(公告)日：1996-05-23
申请号：PCT/US1995014893
申请日：1995-11-13
申请人： GEORGIA STATE UNIVERSITY RESEARCH FOUNDATION, INC. , THE UNIVERSITY OF NORTH CAROLINA AT CHAPEL HILL , AUBURN UNIVERSITY , BOYKIN, David, W. , DYKSTRA, Christine, C. , TIDWELL, Richard, R. , HALL, James, E. , WILSON, W., David , KUMAR, Arvind , BLAGBURN, Byron, L.
发明人： GEORGIA STATE UNIVERSITY RESEARCH FOUNDATION, INC. , THE UNIVERSITY OF NORTH CAROLINA AT CHAPEL HILL , AUBURN UNIVERSITY
IPC分类号： C07D405/14
CPC分类号： A61K31/506 , A61K31/341 , A61K31/4178 , C07D307/54 , C07D307/58 , C07D405/14 , Y02A50/488 , Y02A50/491
摘要： The present invention provides methods for treating Pneumocystis carinii pneumonia, Giardia lamblia, and Cryptosporidium parvum in a subject in need of such treatment. The methods comprise administering to the subject a compound of formula (I), wherein R1 and R2 are each independently selected from the group consisting of H, loweralkyl, aryl, alkylaryl, aminoalkyl, aminoaryl, halogen, oxyalkyl, oxyaryl, or oxyarylalkyl; R3 and R4 are each independently selected from the group consisting of H, loweralkyl, oxyalkyl, alkylaryl, aryl, oxyaryl, aminoalkyl, aminoaryl, or halogen; and X and Y are located in the para or meta positions and are selected from the group consisting of H, loweralkyl, oxyalkyl, and (a) wherein each R5 is independently selected from the group consisting of H, loweralkyl, alkoxyalkyl, hydroxyalkyl, aminoalkyl, alkylaminoalkyl, cycloalkyl, aryl, or alkylaryl or two R5 groups together represent C2-C10 alkyl, hydroxyalkyl, or alkylene; and R6 is H, hydroxy, loweralkyl, alkoxyalkyl, hydroxyalkyl, aminoalkyl, alkylamino, alkylaminoalkyl, cycloalkyl, hydroxycycloalkyl, alkoxycycloalkyl, aryl, or alkylaryl; or a pharmaceutically acceptable salt thereof. The compounds are administered in an amount effective to treat the condition. The present invention also includes novel compounds useful in the treatment of Pneumocystis carinii pneumonia, Giardia lamblia, and Cryptosporidium parvum.
摘要翻译：本发明提供了在需要这种治疗的受试者中治疗卡氏肺囊虫肺炎，贾第鞭毛虫和隐孢子虫的方法。所述方法包括向受试者施用式（I）化合物，其中R 1和R 2各自独立地选自H，低级烷基，芳基，烷基芳基，氨基烷基，氨基芳基，卤素，氧烷基，氧芳基或氧芳基烷基; R 3和R 4各自独立地选自H，低级烷基，烷氧基烷基，烷基芳基，芳基，氧芳基，氨基烷基，氨基芳基或卤素; 并且X和Y位于对位或间位，并且选自H，低级烷基，烷氧基和（a），其中每个R 5独立地选自H，低级烷基，烷氧基烷基，羟基烷基，氨基烷基，烷基氨基烷基，环烷基，芳基或烷基芳基或两个R 5基团一起表示C 2 -C 10烷基，羟基烷基或亚烷基; 烷基氨基，烷基氨基烷基，环烷基，羟基环烷基，烷氧基环烷基，芳基或烷基芳基; R 6是H，羟基，低级烷基，烷氧基烷基，羟基烷基，或其药学上可接受的盐。以有效治疗病症的量施用化合物。本发明还包括可用于治疗卡氏肺囊虫肺炎，贾第鞭毛虫和隐孢子虫的新型化合物。

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