Method of using (H.sup.+ /K.sup.+)ATPase inhibitors as antiviral agents
    3.
    发明授权
    Method of using (H.sup.+ /K.sup.+)ATPase inhibitors as antiviral agents 失效
    使用(H + / K +)ATP酶抑制剂作为抗病毒剂的方法

    公开(公告)号:US5945425A

    公开(公告)日:1999-08-31

    申请号:US737251

    申请日:1996-10-24

    摘要: A class of compounds which are (H.sup.+ /K.sup.+)ATPase inhibitors can be used for the treatment of viral infections. Compounds of particular interest are defined by Formula III: ##STR1## wherein D is N or CH; wherein R.sup.7 is one or more radicals selected from hydrido, alkoxy, amino, cyano, nitro, hydroxyl, alkyl, halo, haloalkyl, carboxyl, alkanoyl, nitro, amino, alkylamino, aminocarbonyl, aminosulfonyl, alkylaminocarbonyl, alkylcarbonylamino, alkoxycarbonyl, alkylaminosulfonyl, alkylsulfonylamino, alkylthio, alkylsulfinyl and alkylsulfonyl; wherein R.sup.8 is selected from hydrido, alkyl and cycloalkyl; wherein R.sup.9 is one or more radicals selected from hydrido, alkoxy, amino, alkyl, halo, cyano, nitro, hydroxyl, haloalkyl, nitro, carboxyl, alkanoyl, amino, alkylamino, dialkylamino, aminocarbonyl, alkylaminocarbonyl, alkylcarbonylamino, aminosulfonyl, alkylaminosulfonyl, alkylsulfonylamino, alkoxycarbonyl, alkylthio, alkylsulfinyl and alkylsulfonyl; and wherein R.sup.10 and R.sup.11 are independently selected from hydrido, alkyl, aryl, alkylcarbonyl and arylcarbonyl wherein the aryl ring may be further substituted with one or more radicals selected from alkyl, halo, hydrazidylcarbonyl, aminocarbonyl and alkoxy; or wherein R.sup.10 and R.sup.11 together with the nitrogen atom form a heterocyclic ring.

    摘要翻译: PCT No.PCT / US95 / 05021 Sec。 371日期1996年10月24日第 102(e)日期1996年10月24日PCT提交1995年5月1日PCT公布。 出版物WO95 / 29897 1995年11月9日,一类(H + / K +)ATP酶抑制剂的化合物可用于治疗病毒感染。 特别感兴趣的化合物由式III定义:其中D是N或CH; 其中R7是一个或多个选自氢,烷氧基,氨基,氰基,硝基,羟基,烷基,卤素,卤代烷基,羧基,烷酰基,硝基,氨基,烷基氨基,氨基羰基,氨基磺酰基,烷基氨基羰基,烷基羰基氨基,烷氧基羰基,烷基氨基磺酰基, ,烷硫基,烷基亚磺酰基和烷基磺酰基; 其中R8选自氢,烷基和环烷基; 其中R9是一个或多个选自氢,烷氧基,氨基,烷基,卤素,氰基,硝基,羟基,卤代烷基,硝基,羧基,烷酰基,氨基,烷基氨基,二烷基氨基,氨基羰基,烷基氨基羰基,烷基羰基氨基,氨基磺酰基,烷基氨基磺酰基, ,烷氧基羰基,烷硫基,烷基亚磺酰基和烷基磺酰基; 并且其中R 10和R 11独立地选自氢,烷基,芳基,烷基羰基和芳基羰基,其中所述芳基环可以进一步被一个或多个选自烷基,卤素,肼基羰基,氨基羰基和烷氧基的基团取代; 或其中R 10和R 11与氮原子一起形成杂环。

    Pharmaceutically useful meso-azacyclic amides of imidazopyridine
carboxylic acids and analogs thereof
    6.
    发明授权
    Pharmaceutically useful meso-azacyclic amides of imidazopyridine carboxylic acids and analogs thereof 失效
    咪唑并吡啶羧酸及其类似物的药学有用的内消旋 - 氮杂环酰胺

    公开(公告)号:US5137893A

    公开(公告)日:1992-08-11

    申请号:US666278

    申请日:1991-03-07

    IPC分类号: C07D519/00

    CPC分类号: C07D519/00

    摘要: The imidazopyridines containing meso-azacycle side chains as described herein find utility as antagonists of the serotonin 5-HT.sub.3 receptor. As such they are useful for the treatment of humans and animals wherein antagonism of 5-HT.sub.3 receptors is benefical. Therapy is indicated for, but not limited to, the treatment of anxiety, psychoses, depression (especially depression accompanied by anxiety), cognitive disorders, substance abuse dependence and/or withdrawal, gastrointestinal motility disturbances (including esophageal reflux, dyspepsia, irritable bowel syndrome), emesis caused by chemotherapeutic agents, and visceral pain. Additionally, the compounds of the present invention may find utility as enhancers of nasal absorption of bioactive compounds.

    摘要翻译: 含有本文所述的内消旋 - 侧链侧链的咪唑并吡啶可用作5-羟色胺5-HT 3受体的拮抗剂。 因此,它们可用于治疗其中5-HT 3受体拮抗作用有益的人和动物。 治疗指示但不限于治疗焦虑症,精神病,抑郁症(特别是伴有焦虑的抑郁症),认知障碍,药物滥用依赖和/或戒断,胃肠蠕动障碍(包括食管反流,消化不良,肠易激综合征 ),由化疗药引起的呕吐和内脏痛。 此外,本发明的化合物可以用作生物活性化合物的鼻吸收增强剂。