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    • 1. 发明授权
    • Methods of inhibiting Pneumocystis carinii pneumonia, Giardia lamblia,
and Cryptosporidium and compounds useful therefor
    • 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
    • US5602172A
    • 1997-02-11
    • US453276
    • 1995-05-30
    • David W. BoykinChristine C. DykstraRichard R. TidwellJames E. HallW. David WilsonArvind KumarByron L. Blagburn
    • David W. BoykinChristine C. DykstraRichard R. TidwellJames E. HallW. David WilsonArvind KumarByron L. Blagburn
    • A61K31/341A61K31/4178A61K31/505A61K31/506C07D307/54C07D307/58C07D403/10C07D403/14C07D405/14G01N33/52A61K31/34
    • G01N33/52A61K31/341A61K31/4178A61K31/505A61K31/506C07D307/54C07D307/58C07D403/10C07D403/14C07D405/14
    • 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.
    • 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。
    • 4. 发明授权
    • Methods of treating Giardia lamblia
    • 治疗贾第鞭毛虫的方法
    • US5627184A
    • 1997-05-06
    • US454838
    • 1995-05-31
    • David W. BoykinChristine C. DykstraRichard R. TidwellJames E. HallW. David WilsonArvind Kumar
    • David W. BoykinChristine C. DykstraRichard R. TidwellJames E. HallW. David WilsonArvind Kumar
    • G01N33/50A61K31/505A61K31/506C07D239/26C07D307/52C07D307/54C07D307/58C07D403/10C07D403/14C07D405/14C09B23/01C12Q1/68G01N21/78G01N33/52G01N33/58
    • C07D239/26A61K31/505A61K31/506C07D307/54C07D403/10C07D403/14C07D405/14C09B23/0075G01N33/52
    • The present invention provides methods for treating Pneumocystis carinii pneumonia and Giardia lamblia in a subject in need of such treatment. The methods comprises administering to the subject a compound of Formula I: ##STR1## wherein: X and Y are located in the para or meta positions and are selected from the group consisting of H, loweralkyl, loweralkoxy, and ##STR2## wherein: each R.sub.1 is independently selected from the group consisting of H, loweralkyl, alkoxyalkyl, hydroxyalkyl, aminoalkyl, alkylaminoalkyl, cycloalkyl, aryl, or alkylaryl or two R.sub.1 groups together represent C.sub.2 -C.sub.10 alkyl, hydroxyalkyl, or alkylene, or two R.sub.1 groups together represent ##STR3## wherein m is from 1-3 and R.sub.7 is H or --CONHCR.sub.8 NR.sub.9 R.sub.10, wherein R.sub.8 is loweralkyl, and R.sub.9 and R.sub.10 are each independently selected from the group consisting of H and lower alkyl;R.sub.2 is H, hydroxy, loweralkyl, alkoxyalkyl, hydroxyalkyl, aminoalkyl, alkylaminoalkyl, cycloalkyl, aryl, or alkylaryl;n is a number from 0 to 2;R.sub.3 and R.sub.4 are each independently selected from the group consisting of H, loweralkyl, loweralkoxy, alkylaryl, aryl, oxyaryl, aminoalkyl, aminoaryl, or halogen; andR.sub.5 and R.sub.6 are each independently selected from the group consisting of H, loweralkyl, aryl, alkylaryl, aminoalkyl, aminoaryl, halogen, oxyalkyl, oxyaryl, or oxyarylalkyl; or a phamaceutically acceptable salt thereof. The compound of Formula I is administered in an amount effective to treat the condition.The present invention also provides compounds useful for the treatment of Pneumocystis carinii pneumonia and Giardia lamblia.
    • 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和贾第鞭毛虫的方法。 所述方法包括向受试者施用式I化合物:其中:X和Y位于对位或间位,并且选自H,低级烷基,低级烷氧基和低级烷氧基, 其中:每个R 1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 1基团一起表示C 2 -C 10烷基,羟基烷基或亚烷基或两个R 1基团 一起代表,其中m为1-3,R7为H或-CONHCR8NR9R10,其中R8为低级烷基,R9和R10各自独立地选自H和低级烷基; R2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; n是从0到2的数字; R 3和R 4各自独立地选自H,低级烷基,低级烷氧基,烷基芳基,芳基,氧芳基,氨基烷基,氨基芳基或卤素; 并且R 5和R 6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; 或其药学上可接受的盐。 以有效治疗病症的量施用式I化合物。 本发明还提供了可用于治疗卡氏肺囊虫肺炎和贾第鞭毛虫的化合物。