4-(Phenylmethyl and substituted phenylmethyl)-imidazole-2-thiones acting as specific alpha2 adrenergic agonists
    5.
    发明授权
    4-(Phenylmethyl and substituted phenylmethyl)-imidazole-2-thiones acting as specific alpha2 adrenergic agonists 失效
    作为特定α2肾上腺素能激动剂的4-(苯基甲基和取代的苯基甲基) - 咪唑-2-硫酮

    公开(公告)号:US07683089B1

    公开(公告)日:2010-03-23

    申请号:US11232341

    申请日:2005-09-20

    IPC分类号: A61K31/4164 C07D233/30

    CPC分类号: C07D233/84

    摘要: Compounds of Formula 1 where the variables have the meaning defined in the specification are agonists of alpha2 adrenergic receptors. Several compounds of the disclosure are specific or selective to alpha2B and/or alpha2C adrenergic receptors in preference over alpha2A adrenergic receptors. Additionally some of the claimed compounds have no or only minimal cardivascular and/or sedatory activity. The compounds of Formula 1 are useful as medicaments in mammals, including humans, for treatment of diseases and or alleviations of conditions which are responsive to treatment by agonists of alpha2 adrenergic receptors. Compounds of Formula 1 which have no significant cardiovascular and/or sedatory activity are useful for treating pain and other conditions with minimal side effects.

    摘要翻译: 变量具有本说明书中定义的含义的式1化合物是α2肾上腺素能受体的激动剂。 本公开的几种化合物优选α2B和/或α2C肾上腺素能受体是优于α2A肾上腺素能受体的特异性或选择性的。 另外一些要求保护的化合物没有或仅有最小的心血管和/或镇静活性。 式1的化合物可用作哺乳动物(包括人)中用于治疗疾病的药物和/或缓解对α2肾上腺素能受体激动剂治疗有反应的病症。 没有明显的心血管和/或镇静作用的式1化合物可用于治疗疼痛和其他具有最小副作用的病症。

    Imidazole-2-thiones
    6.
    发明授权
    Imidazole-2-thiones 失效
    咪唑-2-硫酮

    公开(公告)号:US08063086B2

    公开(公告)日:2011-11-22

    申请号:US11873500

    申请日:2007-10-17

    IPC分类号: A61K31/4164 C07D233/30

    摘要: Compounds of Formula 1 where X is S and the variables have the meaning defined in the specification are specific or selective to alpha2B and/or alpha2C adrenergic receptors in preference over alpha2A adrenergic receptors, and as such have no or only minimal cardiovascular and/or sedatory activity. These compounds of Formula 1 are useful as medicaments in mammals, including humans, for treatment of diseases and or alleviations of conditions which are responsive to treatment by agonists of alpha2B adrenergic receptors. Compounds of Formula 1 where X is O also have the advantageous property that they have no or only minimal cardiovascular and/or sedatory activity and are useful for treating pain and other conditions with no or only minimal cardiovascular and/or sedatory activity.

    摘要翻译: 式1的化合物,其中X为S且变量具有本说明书中定义的含义,优先选择α2B和/或α2C肾上腺素能受体,优于α2A肾上腺素能受体,因此没有或只有最小的心血管和/或镇静剂 活动。 式1的这些化合物可用作哺乳动物(包括人)中用于治疗疾病的药物和/或缓解对α2B肾上腺素能受体的激动剂治疗有反应的病症。 其中X为O的式1的化合物也具有它们没有或只有最小的心血管和/或镇静活性的有利特性,并且可用于治疗没有或仅有最小的心血管和/或镇静活性的疼痛和其它状况。

    4-(Condensed cyclicmethyl)-imidazole-2-thiones acting as α2 adrenergic agonists
    10.
    发明授权
    4-(Condensed cyclicmethyl)-imidazole-2-thiones acting as α2 adrenergic agonists 失效
    作为α2肾上腺素能激动剂的4-(缩合环状甲基) - 咪唑-2-硫酮

    公开(公告)号:US07396849B2

    公开(公告)日:2008-07-08

    申请号:US11232383

    申请日:2005-09-20

    IPC分类号: A61K31/4174 C07D233/42

    摘要: Compounds of Formula 1 where the variables have the meaning defined in the specification are agonists of alpha2 adrenergic receptors. Several compounds of the disclosure are specific or selective to alpha2B and/or alpha2C adrenergic receptors in preference over alpha2A adrenergic receptors. Additionally some of the claimed compounds have no or only minimal cardivascular and/or sedatory activity. The compounds of Formula 1 are useful as medicaments in mammals, including humans, for treatment of diseases and or alleviations of conditions which are responsive to treatment by agonists of alpha2 adrenergic receptors. Compounds of Formula 1 which have no significant cardiovascular and/or sedatory activity are useful for treating pain and other conditions with minimal side effects.

    摘要翻译: 变量具有本说明书中定义的含义的式1化合物是α2肾上腺素能受体的激动剂。 本公开内容的若干化合物优先于α2A2肾上腺素能受体是特异性或选择性的α2B2和/或α2C2N2肾上腺素能受体。 另外一些要求保护的化合物没有或仅有最小的心血管和/或镇静活性。 式1的化合物可用作哺乳动物(包括人)中的药物,用于治疗疾病和/或减轻对α2肾上腺素能受体的激动剂治疗有反应的病症。 没有明显的心血管和/或镇静作用的式1化合物可用于治疗疼痛和其他具有最小副作用的病症。