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    Methods of inhibiting Pneumocystis carinii pneumonia, Giardia lamblia, and Cryptosporidium and compounds useful therefor
    52.
    发明授权
    Methods of inhibiting Pneumocystis carinii pneumonia, Giardia lamblia, and Cryptosporidium and compounds useful therefor 失效
    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

    Applicant: David W. Boykin ,  Christine C. Dykstra ,  Richard R. Tidwell ,  James E. Hall ,  W. David Wilson ,  Arvind Kumar ,  Byron L. Blagburn

    Inventor： David W. Boykin ,  Christine C. Dykstra ,  Richard R. Tidwell ,  James E. Hall ,  W. David Wilson ,  Arvind Kumar ,  Byron L. Blagburn

    IPC: A61K31/341 ,  A61K31/4178 ,  A61K31/505 ,  A61K31/506 ,  C07D307/54 ,  C07D307/58 ,  C07D403/10 ,  C07D403/14 ,  C07D405/14 ,  G01N33/52 ,  A61K31/34

    CPC classification number: G01N33/52 ,  A61K31/341 ,  A61K31/4178 ,  A61K31/505 ,  A61K31/506 ,  C07D307/54 ,  C07D307/58 ,  C07D403/10 ,  C07D403/14 ,  C07D405/14

    Abstract: 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.

    Abstract translation: 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。

    Compounds that exhibit specific molecular recognition of mixed nucleic acid sequences and bind in the DNA minor groove as a dimer
    60.
    发明授权
    Compounds that exhibit specific molecular recognition of mixed nucleic acid sequences and bind in the DNA minor groove as a dimer 失效
    显示混合核酸序列的特异性分子识别并在DNA小沟中作为二聚体结合的化合物

    公开(公告)号：US07160914B2

    公开(公告)日：2007-01-09

    申请号：US11035627

    申请日：2005-01-14

    Applicant: W. David Wilson ,  David W. Boykin ,  Richard R. Tidwell

    Inventor： W. David Wilson ,  David W. Boykin ,  Richard R. Tidwell

    IPC: A61K31/4184 ,  A61K31/4164 ,  C07D403/04 ,  C12Q1/04 ,  C12Q1/24

    CPC classification number: C07D207/416 ,  C07D307/54 ,  C07D405/04 ,  C07D405/14 ,  C12Q1/6816 ,  C12Q2563/173

    Abstract: Asymmetric derivatives of furamidines with one of the phenyl rings of furamidine replaced with a benzimidazole have been found by quantitative footprinting analyses to bind GC containing sites on DNA more strongly than to pure AT sequences. These compounds have been shown to bind in the minor groove at specific GC containing sequences of DNA in a highly cooperative manner as a stacked dimer. Compounds of the present invention find use in selectively binding mixed sequence DNA, and may also be used in methods of regulating gene expression, methods of treating opportunistic infections and cancer, as well as in methods of detecting certain sequences of DNA.

    Abstract translation: 已经通过定量印迹分析发现了呋喃脒苯基环之一与呋喃脒苯基环之一取代的不对称衍生物，以比纯AT序列更强地结合含DNA位点的DNA。 已经显示这些化合物以高度协同的方式作为堆叠的二聚体以特定的GC含有DNA序列在小沟中结合。 本发明化合物可用于选择性结合混合序列DNA，也可用于调节基因表达的方法，治疗机会性感染和癌症的方法，以及检测某些DNA序列的方法。

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