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    Methods and formulations for the treatment of infectious bursal disease in avian subjects
    61.
    发明授权
    Methods and formulations for the treatment of infectious bursal disease in avian subjects 失效
    用于治疗禽类受试者传染性法氏囊病的方法和配方

    公开(公告)号：US06774144B1

    公开(公告)日：2004-08-10

    申请号：US09703804

    申请日：2000-11-01

    Applicant: Christine C. Dykstra ,  James C. Hudson ,  Sandra Ewald ,  Richard R. Tidwell ,  David W. Boykin

    Inventor： Christine C. Dykstra ,  James C. Hudson ,  Sandra Ewald ,  Richard R. Tidwell ,  David W. Boykin

    IPC: A61K3134

    CPC classification number: A61K31/138 ,  A61K31/19 ,  A61K31/34 ,  A61K31/366 ,  A61K31/56 ,  A61K31/573

    Abstract: In one aspect, the invention relates to a method of treating infectious bursal disease (IBD) in an avian subject in need of such treatment. The method comprises administering to the subject a compound of the formulas (I) through (IV) or a pharmaceutically acceptable salt thereof in an amount sufficient to treat IBD. In another aspect, the invention relates to a method of producing active immunity against infectious bursal virus disease (IBD) in an avian subject. The method comprises administering to a subject an immunogenic-amount of an IBDV vaccine and a compound selected from the compounds of formulas (I) through (IV) described herein. The compound represented by formulas (I) through (IV) is administered in an amount sufficient to induce an immune response in the avian subject.

    Abstract translation: 一方面，本发明涉及在需要这种治疗的禽类受试者中治疗传染性法氏囊病（IBD）的方法。 该方法包括向受试者施用足以治疗IBD的量的式（I）至（IV）化合物或其药学上可接受的盐。 另一方面，本发明涉及在禽类受试者中产生针对传染性法氏囊病毒病（IBD）的主动免疫的方法。 该方法包括向受试者施用免疫原性量的IBDV疫苗和选自本文所述的式（I）至（IV）的化合物的化合物。 由式（I）至（IV）表示的化合物以足以在禽类受试者中诱导免疫应答的量施用。

    Benzamidoxime prodrugs as antipneumocystic agents
    62.
    发明授权
    Benzamidoxime prodrugs as antipneumocystic agents 有权

    公开(公告)号：US06423737B1

    公开(公告)日：2002-07-23

    申请号：US09759664

    申请日：2001-01-12

    Applicant: James E. Hall ,  Richard R. Tidwell ,  David W. Boykin

    Inventor： James E. Hall ,  Richard R. Tidwell ,  David W. Boykin

    IPC: A61K3115

    Abstract: A method of treating Pneumocystis carinii pneumonia in a subject in need of such treatment is disclosed. The method comprises orally administering to the subject a bis-benzamidoxime, or a pharmaceutically acceptable salt thereof, that is reduced in the subject to produce a benzamidine having anti-P. carinii activity. The method of the present invention may alternatively comprise intravenously administering to the subject an active compound as disclosed herein. Pharmaceutical formulations and active compounds useful in the practice of the present invention are also disclosed.

    Benzamidoxime prodrugs as antipneumocystic agents
    65.
    发明授权
    Benzamidoxime prodrugs as antipneumocystic agents 失效
    苯甲酰胺肟前药作为抗肺囊虫药

    公开(公告)号：US5723495A

    公开(公告)日：1998-03-03

    申请号：US558716

    申请日：1995-11-16

    Applicant: James E. Hall ,  Richard R. Tidwell ,  David W. Boykin

    Inventor： James E. Hall ,  Richard R. Tidwell ,  David W. Boykin

    IPC: C07D307/52 ,  A61K31/00 ,  A61K31/15 ,  A61K31/155 ,  A61K31/34 ,  A61K31/341 ,  A61K31/38 ,  A61K31/381 ,  A61P11/00 ,  A61P31/00 ,  A61P31/04 ,  A61P43/00 ,  C07C257/18 ,  C07C259/18 ,  C07D235/24 ,  C07D307/54 ,  C07D307/68 ,  C07D333/24 ,  A61K31/165

    CPC classification number: A61K31/15 ,  A61K31/155 ,  A61K31/341 ,  C07C257/18 ,  C07C259/18 ,  C07D307/54 ,  C07D307/68 ,  C07D333/24

    Abstract: A method of treating Pneumocystis carinii pneumonia in a subject in need of such treatment is disclosed. The method comprises orally administering to the subject a bis-benzamidoxime of formula I: ##STR1## wherein R.sub.1 and R.sub.2 are each independently selected from the group consisting of H, loweralkyl, oxyalkyl, alkoxyalkyl, cycloalkyl, aryl, hydroxyalkyl, aminoalkyl or alkylaminoalkyl; R.sub.3 is H, loweralkyl, oxyalkyl, alkoxyalkyl, hydroxyalkyl, cycloalkyl, aryl, aminoalkyl, alkylaminoalkyl or halogen; n is from 2 to 6; X is O, N, or S; and Y is H or loweralkyl, or a pharmaceutically acceptable salt thereof, that is reduced in the subject to produce a benzamidine having anti-P, carinii activity. The method of the present invention may alternatively comprise intravenously administering to the subject an active compound as disclosed herein. Pharmaceutical formulations and active compounds useful in the practice of the present invention are also disclosed.

    Abstract translation: 公开了在需要这种治疗的受试者中治疗卡氏肺囊虫肺炎的方法。 该方法包括向受试者口服给予式I的双 - 苯甲脒：其中R 1和R 2各自独立地选自H，低级烷基，烷氧基烷基，烷氧基烷基，环烷基，芳基，羟基烷基，氨基烷基 或烷基氨基烷基; R3是H，低级烷基，氧烷基，烷氧基烷基，羟基烷基，环烷基，芳基，氨基烷基，烷基氨基烷基或卤素; n为2至6; X是O，N或S; 并且Y是H或其烷基或其药学上可接受的盐，其在受试者中减少以产生具有抗P，卡尼氏菌活性的苯甲脒。 本发明的方法可以选择性地向受试者静脉内施用本文所公开的活性化合物。 还公开了可用于本发明实践的药物制剂和活性化合物。

    Methods of treating Giardia lamblia
    67.
    发明授权
    Methods of treating Giardia lamblia 失效
    治疗贾第鞭毛虫的方法

    公开(公告)号：US5627184A

    公开(公告)日：1997-05-06

    申请号：US454838

    申请日：1995-05-31

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

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

    IPC: 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 classification number: C07D239/26 ,  A61K31/505 ,  A61K31/506 ,  C07D307/54 ,  C07D403/10 ,  C07D403/14 ,  C07D405/14 ,  C09B23/0075 ,  G01N33/52

    Abstract: 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.

    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。

    Methods of inhibiting Pneumocystis carinii pneumonia, Giardia lamblia, and Cryptosporidium and compounds useful therefor
    69.
    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。

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