Sodium channel blockers, preparation method thereof and use thereof
    6.
    发明授权
    Sodium channel blockers, preparation method thereof and use thereof 有权
    钠通道阻滞剂及其制备方法及用途

    公开(公告)号:US09376429B2

    公开(公告)日:2016-06-28

    申请号:US14435473

    申请日:2013-10-15

    IPC分类号: C07D417/12 C07D417/14

    CPC分类号: C07D417/12 C07D417/14

    摘要: The present invention relates to a compound having a blocking effect against sodium ion channels, particularly Nav1.7, a preparation method thereof and the use thereof. A compound represented by formula 1 according to the invention, or a pharmaceutically acceptable salt, hydrate, solvate or isomer thereof may be effectively used for the prevention or treatment of pain, for example, acute pain, chronic pain, neuropathic pain, post-surgery pain, migraine, arthralgia, neuropathy, nerve injury, diabetic neuropathy, neuropathic disease, epilepsy, arrhythmia, myotonia, ataxia, multiple sclerosis, irritable bowel syndrome, urinary incontinence, visceral pain, depression, erythromelalgia, or paroxysmal extreme pain disorder (PEPD).

    摘要翻译: 本发明涉及对钠离子通道具有阻塞作用的化合物,特别涉及Nav1.7,其制备方法及其应用。 根据本发明的由式1表示的化合物或其药学上可接受的盐,水合物,溶剂合物或异构体可以有效地用于预防或治疗疼痛,例如急性疼痛,慢性疼痛,神经性疼痛,手术后 疼痛,偏头痛,关节痛,神经病变,神经损伤,糖尿病性神经病变,神经病变,癫痫,心律失常,肌强直,共济失调,多发性硬化症,肠易激综合征,尿失禁,内脏痛,抑郁症,红斑性疼痛或阵发性极度疼痛障碍(PEPD) 。

    Biaryl benzoimidazole derivatives and pharmaceutical composition comprising the same
    9.
    发明授权
    Biaryl benzoimidazole derivatives and pharmaceutical composition comprising the same 有权
    双芳基苯并咪唑衍生物及其组合物

    公开(公告)号:US08940769B2

    公开(公告)日:2015-01-27

    申请号:US13857304

    申请日:2013-04-05

    摘要: Disclosed are biaryl benzoimidazole derivatives. They have an inhibitory effect on calcium influx in HEK cells, thereby showing a powerful antagonistic effect on a vanilloid receptor, and further have an analgesic effect, thereby being useful for preventing or treating pain, acute pain, chronic pain, neuropathic pain, postoperative pain, migraine, arthralgia, neuropathies, nerve injury, diabetic neuropathy, neurological illness, neurodermatitis, stroke, bladder hypersensitivity, irritable bowel syndrome, a respiratory disorder such as cough, asthma, and chronic obstructive pulmonary disease, burning, psoriasis, itching, vomiting, irritation of the skin, eyes, and mucous membranes, gastric-duodenal ulcers, inflammatory intestinal diseases, and inflammatory diseases.

    摘要翻译: 公开了联芳基苯并咪唑衍生物。 它们对HEK细胞中的钙流入具有抑制作用,从而对香草素受体具有强大的拮抗作用,并具有镇痛作用,因此可用于预防或治疗疼痛,急性疼痛,慢性疼痛,神经性疼痛,术后疼痛 ,偏头痛,关节痛,神经病,神经损伤,糖尿病性神经病,神经系统疾病,神经性皮炎,中风,膀胱过敏,肠易激综合征,呼吸障碍如咳嗽,哮喘和慢性阻塞性肺病,灼烧,牛皮癣,瘙痒,呕吐, 刺激皮肤,眼睛和粘膜,胃十二指肠溃疡,炎性肠道疾病和炎性疾病。