AZAADAMANTANE FORMATE ESTER AND PROCESS PREPARING AZAADAMANTANE DERIVATIVES
    7.
    发明申请
    AZAADAMANTANE FORMATE ESTER AND PROCESS PREPARING AZAADAMANTANE DERIVATIVES 审中-公开
    亚胺丹酸酯和制备亚胺丹衍生物的方法

    公开(公告)号:WO2014164682A1

    公开(公告)日:2014-10-09

    申请号:PCT/US2014023204

    申请日:2014-03-11

    申请人: ABBVIE INC

    IPC分类号: C07D451/14 A61K31/439

    摘要: A compound, (4s)-1-azaadamantane-4yl formate ester, is described. In addition, a process is described for preparing (4s)-1-azaadamantane-4yl formate ester, aminothiadiazole-phenyl phosphate salt, bromothiadizole-phenyl or (4s)-4-(5-phenyl-1,3,4-thiadiazol-2-yloxy)-1- azatricyclo[3.3.1.13,7 ]-decane dihydrogen citrate. Furthermore, a process is described, comprising step of hydrolyzing (4s)-1-azaadamantane-4yl formate ester to form (4s)-1-azaadamantan-4-ol HBr salt.

    摘要翻译: 描述了化合物(4s)-1-氮杂金刚烷-4-基甲酸酯。 此外,描述了制备(4s)-1-氮杂金刚烷-4-基甲酸酯,氨基噻二唑 - 苯基磷酸盐,溴噻嗪 - 苯基或(4s)-4-(5-苯基-1,3,4-噻二唑-2-基) 吡啶-2-基氧基)-1-氮杂三环[3.3.1.13.7] - 癸烷二氢柠檬酸二氢盐。 此外,描述了包括水解(4s)-1-氮杂金刚烷-4-基甲酸酯以形成(4s)-1-氮杂金刚烷-4-醇HBr盐的步骤。

    NOVEL BENZAMIDE DERIVATIVE AND USE THEREOF
    10.
    发明申请
    NOVEL BENZAMIDE DERIVATIVE AND USE THEREOF 审中-公开
    新的苯甲酰衍生物及其用途

    公开(公告)号:WO2013081400A3

    公开(公告)日:2013-08-22

    申请号:PCT/KR2012010257

    申请日:2012-11-29

    申请人: VIVOZON INC

    发明人: LEE DOO HYUN

    摘要: The present invention relates to a novel benzamide derivative and a pharmaceutical use thereof, and more specifically, to a novel benzamide derivative of formula 1 or a pharmaceutically acceptable salt thereof, and a composition containing same for the prevention and treatment of pain and itching. The benzamide derivative and the pharmaceutically acceptable salt according to the present invention have a remarkable effect on the suppression of pain. The benzamide derivative and the pharmaceutically acceptable salt have an effect on the suppression of pain not only in a neuropathic animal model but also in a formalin model and other pain-induced models, and thus can be used for the suppression of various kinds of pain such as nociceptive pain and chronic pain. Further, it is confirmed that the present invention has an antipruriginous effect on an itch model in which an established mechanism of pain and concept of treatment is applied, and therefore the antipruriginous composition is useful since the composition can be used for the radical treatment of atopy by suppressing and treating the early itching phase to prevent skin damage and inflammatory response after the scratching phase.

    摘要翻译: 本发明涉及一种新颖的苯甲酰胺衍生物及其药物用途,更具体地说,涉及一种新型的式1的苯甲酰胺衍生物或其药学上可接受的盐,以及含有其的组合物,用于预防和治疗疼痛和瘙痒。 根据本发明的苯甲酰胺衍生物和药学上可接受的盐对抑制疼痛具有显着的作用。 苯甲酰胺衍生物和药学上可接受的盐不仅对神经病性动物模型而且在福尔马林模型和其它疼痛诱导的模型中也具有抑制疼痛的作用,因此可用于抑制各种疼痛 作为伤害性疼痛和慢性疼痛。 此外,证实本发明对于其中应用已建立的疼痛机制和治疗概念的瘙痒模型具有止痒作用,因此该止痒药组合物是有用的,因为该组合物可用于特应性的根治性治疗 通过抑制和治疗早期瘙痒期以防止皮肤损伤和搔抓阶段后的炎症反应。