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1. 发明授权

US5602172A Methods of inhibiting Pneumocystis carinii pneumonia, Giardia lamblia, and Cryptosporidium and compounds useful therefor 失效
标题翻译：抑制卡氏肺囊虫肺炎，贾第鞭毛虫和隐孢子虫的方法及其有用的化合物
公开(公告)号：US5602172A
公开(公告)日：1997-02-11
申请号：US453276
申请日：1995-05-30
申请人： David W. Boykin , Christine C. Dykstra , Richard R. Tidwell , James E. Hall , W. David Wilson , Arvind Kumar , Byron L. Blagburn
发明人： David W. Boykin , Christine C. Dykstra , Richard R. Tidwell , James E. Hall , W. David Wilson , Arvind Kumar , Byron L. Blagburn
IPC分类号： A61K31/341 , A61K31/4178 , A61K31/505 , A61K31/506 , C07D307/54 , C07D307/58 , C07D403/10 , C07D403/14 , C07D405/14 , G01N33/52 , A61K31/34
CPC分类号： G01N33/52 , A61K31/341 , A61K31/4178 , A61K31/505 , A61K31/506 , C07D307/54 , C07D307/58 , C07D403/10 , C07D403/14 , C07D405/14
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 adminstering to the subject a compound of Formula (I): ##STR1## wherein: R.sub.1 and R.sub.2 are each independently selected from the group consisting of H, loweralkyl, aryl, alkylaryl, aminoalkyl, aminoaryl, halogen, oxyalkyl, oxyaryl, or oxyarylalkyl;R.sub.3 and R.sub.4 are each independently selected from the group consisting of H, loweralkyl, oxyalkyl, alkylaryl, aryl, oxyaryl, aminoalkyl, aminoaryl, or halogen; andX and Y are located in the para or meta positions and are selected from the group consisting of H, loweralkyl, oxyalkyl, and ##STR2## wherein: each R.sub.5 is independently selected from the group consisting of H, loweralkyl, alkoxyalkyl, hydroxyalkyl, aminoalkyl, alkylaminoalkyl, cycloalkyl, aryl, or alkylaryl or two R.sub.5 groups together represent C.sub.2 -C.sub.10 alkyl, hydroxyalkyl, or alkylene; andR.sub.6 is H, hydroxy, loweralkyl, alkoxyalkyl, hydroxyalkyl, aminoalkyl, alkylamino, alkylaminoalkyl, cycloalkyl, hydroxycycloalkyl, alkoxycycloalkyl, aryl, or alkylaryl;or a phamaceutically acceptable salt thereof. The compounds ar 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。所述方法包括给予受试者式（I）的化合物：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，烷氧基烷基，芳氧基或氧芳基烷基; 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，氧烷基和其中：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。

2. 发明授权

US5622955A Methods of treating cryptosporidium parvum 失效
标题翻译：处理隐孢子虫的方法
公开(公告)号：US5622955A
公开(公告)日：1997-04-22
申请号：US456164
申请日：1995-05-31
申请人： David W. Boykin , Christine C. Dykstra , Richard R. Tidwell , James E. Hall , W. David Wilson , Arvind Kumar , Byron L. Blagburn
发明人： David W. Boykin , Christine C. Dykstra , Richard R. Tidwell , James E. Hall , W. David Wilson , Arvind Kumar , Byron L. Blagburn
IPC分类号： G01N33/50 , A61K31/505 , A61K31/506 , C07D239/26 , C07D307/52 , C07D307/54 , C07D307/58 , C07D403/10 , C07D403/14 , C07D405/14 , C09B23/01 , C12Q1/68 , G01N21/78 , G01N33/52 , G01N33/58
CPC分类号： C07D239/26 , A61K31/505 , A61K31/506 , C07D307/54 , C07D403/10 , C07D403/14 , C07D405/14 , C09B23/0075 , G01N33/52
摘要： The present invention provides methods for treating Cryptosporidium parvum in a subject in need of such treatment. The methods comprises administering to the subject a compound of Formula I: ##STR1##
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孢子虫的方法。所述方法包括向受试者施用式I化合物：（I）

3. 发明授权

US5668167A Methods of treating microbial infections 失效
标题翻译：治疗微生物感染的方法
公开(公告)号：US5668167A
公开(公告)日：1997-09-16
申请号：US477876
申请日：1995-06-07
申请人： Richard R. Tidwell , James E. Hall , David W. Boykin , Christine C. Dykstra , John Perfect , Byron L. Blagburn
发明人： Richard R. Tidwell , James E. Hall , David W. Boykin , Christine C. Dykstra , John Perfect , Byron L. Blagburn
IPC分类号： A61K31/40 , A61K31/403 , A61K31/415 , A61K31/4178 , A61K31/505 , A61P11/00 , A61P31/00 , C07D209/86 , C07D209/88 , C07D403/14
CPC分类号： C07D403/14 , A61K31/403 , A61K31/4178 , C07D209/88
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 comprises administering to the subject a compound of Formula I: ##STR1## wherein: X is located in the para or meta positions and is loweralkyl, loweralkoxy, alkoxyalkyl, hydroxyalkyl, aminoalkyl, alkylaminoalkyl, cycloalkyl, aryl, alkylaryl, halogen, or ##STR2## wherein: each R.sub.2 is independently selected from the group consisting of H, loweralkyl, alkoxyalkyl, hydroxyalkyl, aminoalkyl, alkylaminoalkyl, cycloalkyl, aryl, or alkylaryl or two R.sub.2 groups together represent C.sub.2 -C.sub.10 alkylene, or two R.sub.2 groups together represent ##STR3## wherein m is from 1-3 and R.sub.4 is H, ##STR4## or --CONHR.sub.5 NR.sub.6 R.sub.7, whereinR.sub.5 is loweralkyl, R.sub.6 and R.sub.7 are each independently selected from the group consisting of H and lower alkyl; each R.sub.8 is independently selected from the group consisting of H, loweralkyl, alkoxyalkyl, hydroxyalkyl, aminoalkyl, alkylaminoalkyl, cycloalkyl, aryl, or alkylaryl, or two R.sub.8 groups together represent C.sub.2 -C.sub.10 alkylene; R.sub.9 is H, hydroxy, loweralkyl, alkoxyalkyl, hydroxyalkyl, aminoalkyl, alkylaminoalkyl, cycloalkyl, aryl, or alkylaryl;R.sub.3 is H, hydroxy, loweralkyl, alkoxyalkyl, hydroxyalkyl, aminoalkyl, alkylaminoalkyl, cycloalkyl, aryl, or alkylaryl;R.sub.1 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，其中m为1-3，R4为H，IMA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。

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