USE OF CBX CANNABINOID RECEPTOR MODULATORS AS POTASSIUM CHANNEL MODULATORS
    1.
    发明申请
    USE OF CBX CANNABINOID RECEPTOR MODULATORS AS POTASSIUM CHANNEL MODULATORS 审中-公开
    CBX CANNABINOID受体调节剂作为钾通道调节剂的使用

    公开(公告)号:WO2007125049A1

    公开(公告)日:2007-11-08

    申请号:PCT/EP2007/053915

    申请日:2007-04-20

    摘要: The invention is directed to the use of at least one CB x modulator wherein the CB x modulator is selected from the group consisting of CB 1 agonists; CB 2 agonists; CB 2 partial agonists; CB 2 antagonists; CB 2 inverse agonists; and dually acting compounds which are both a CB 1 agonist and a CB 2 agonist; and mixtures thereof, as K ATP channel modulator for the prophylaxis, treatment, delayed progression, delayed onset and/or inhibition of a variety of disease conditions including obesity, diabetes mellitus, metabolic syndrome, syndrome X, insulinoma, familial hyperinsulemic hypoglycemia, male pattern baldness, detrusor hyperreactivity, asthma, neuroprotection, epilepsy, analgesia, cardioprotection, angina, cardioplegia, arrhythmia, coronary spasm, peripheral vascular disease, cerebral vasospasm, appetite regulation, neurodegeneration, pain - including neuropathic pain and chronic pain - and impotence in mammals and humans. The invention further relates to methods of treating, preventing, delaying progression of, delaying onset of and/or inhibiting a variety of disease conditions including obesity, diabetes mellitus, metabolic syndrome, syndrome X, insulinoma, familial hyperinsulemic hypoglycemia, male pattern baldness, detrusor hyperreactivity, asthma, neuroprotection, epilepsy, analgesia, cardioprotection, angina, cardioplegia, arrhythmia, coronary spasm, peripheral vascular disease, cerebral vasospasm, appetite regulation, neurodegeneration, pain - including neuropathic pain and chronic pain - and impotence in mammals and humans comprising administering to a subject in need thereof an effective amount of at least one CB x modulator having K ATP channel modulating properties.

    摘要翻译: 本发明涉及使用至少一种CB-X调节剂,其中CB调节剂选自CB 1激动剂 ; CB 2激动剂; CB 2/2部分激动剂; CB 2拮抗剂; CB 2反向激动剂; 和作为CB 1激动剂和CB 2 N 2激动剂的双作用化合物; 和其混合物,作为用于预防,治疗,延迟进展,延迟发作和/或抑制多种疾病状况(包括肥胖症,糖尿病,代谢综合征,综合征X,胰岛素瘤)的K ATP通道调节剂 ,家族性高胰岛素低血糖,男性型秃发,逼尿肌反应性过高,哮喘,神经保护,癫痫,镇痛,心脏保护,心绞痛,心跳停搏,心律失常,冠状动脉痉挛,外周血管疾病,脑血管痉挛,食欲调节,神经变性,疼痛 - 包括神经性疼痛和慢性 疼痛和哺乳动物和人类的阳。。 本发明还涉及治疗,预防,延缓发病和/或抑制各种疾病状况(包括肥胖症,糖尿病,代谢综合征,综合征X,胰岛素瘤,家族性高胰岛素低血糖,男性型秃发,逼尿肌)的进展, 高反应性,哮喘,神经保护,癫痫,止痛,心脏保护,心绞痛,心脏停跳,心律失常,冠状动脉痉挛,外周血管疾病,脑血管痉挛,食欲调节,神经变性,疼痛 - 包括神经性疼痛和慢性疼痛 - 以及哺乳动物和人的阳humans 涉及有需要的受试者有效量的至少一种具有K ATP通道调节特性的CB调节剂。

    METHOD OF USING POTASSIUM CHANNEL INHIBITING COMPOUNDS
    4.
    发明申请
    METHOD OF USING POTASSIUM CHANNEL INHIBITING COMPOUNDS 审中-公开
    使用钾通道抑制化合物的方法

    公开(公告)号:WO2007020286A3

    公开(公告)日:2007-05-10

    申请号:PCT/EP2006065418

    申请日:2006-08-17

    摘要: The present invention relates to the use of an effective amount of at least one potassium KvI.3 channel inhibitor or of an effective amount of at least one compound having in addition to its potassium KvI.3 channel inhibiting properties also CBx modulating properties and/or potassium K(atp) channel opening properties for the manufacture of a medicament for the prophylaxis, treatment, delayed progression, delayed onset and/or inhibition of various medical conditions in subjects in need thereof . The diseases are obesity, diabetes mellitus, metabolic syndrome, syndrome X, insulinoma, familial hyperinsulemic hypoglycemia, male pattern baldness, detrusor hyperreactivity, asthma, glucose metabolism - in particular, insulin resistance, hyperglycaemea and/or glucose intolerance - neuroprotection, epilepsy, analgesia, cardioprotection, angina, cardioplegia, arrhythmia, coronary spasm, peripheral vascular disease, cerebral vasospasm, appetite regulation, neurodegeneration, pain - including neuropathic pain and chronic pain - and impotence. The compounds are a.o. 4, 5-dihydropyrazole derivatives, imidazole derivatives, diazoxide, NN414, R(+) -WIN55212-2, HU-308, Rimonaband, SR-147778.

    摘要翻译: 本发明涉及使用有效量的至少一种KvI.3通道抑制剂或有效量的至少一种化合物,除了其KvI.3通道抑制性质之外,还具有CBx调节性质和/或 钾(atp)通道开放性质,用于制备用于在有需要的受试者中预防,治疗,延迟进展,延迟发作和/或抑制各种医学病症的药物。 疾病是肥胖症,糖尿病,代谢综合征,综合征X,胰岛素瘤,家族性高胰岛素血症,男性型秃发,逼尿肌反应性过高,哮喘,葡萄糖代谢 - 特别是胰岛素抵抗,高血糖和/或葡萄糖不耐受 - 神经保护,癫痫,止痛 心脏保护,心绞痛,心脏停搏,心律失常,冠状动脉痉挛,外周血管疾病,脑血管痉挛,食欲调节,神经变性,疼痛 - 包括神经性疼痛和慢性疼痛 - 阳。。 化合物是a.o. 4,5-二氢吡唑衍生物,咪唑衍生物,二氮嗪,NN414,R(+)-WIN55212-2,HU-308,Rimonaband,SR-147778。

    PHARMACEUTICAL COMPOSITIONS COMPRISING CBX CANNABINOID RECEPTOR MODULATORS AND POTASSIUM CHANNEL MODULATORS
    6.
    发明申请
    PHARMACEUTICAL COMPOSITIONS COMPRISING CBX CANNABINOID RECEPTOR MODULATORS AND POTASSIUM CHANNEL MODULATORS 审中-公开
    包含CBX CANNABINOID受体调节剂和钾通道调节剂的药物组合物

    公开(公告)号:WO2007125048A1

    公开(公告)日:2007-11-08

    申请号:PCT/EP2007/053914

    申请日:2007-04-20

    摘要: The invention is directed to pharmaceutical compositions comprising pharmacologically effective quantities of each of a) at least one K ATP channel modulator as a first active agent and b) at least one CB x modulator as a second active agent. The invention further relates to the use of such compositions and to methods of treating, preventing, delaying progression of, delaying onset of and/or inhibiting a variety of disease conditions including obesity, diabetes mellitus, metabolic syndrome, syndrome X, insulinoma, familial hyperinsulemic hypoglycemia, male pattern baldness, detrusor hyperreactivity, asthma, neuroprotection, epilepsy, analgesia, cardioprotection, angina, cardioplegia, arrhythmia, coronary spasm, peripheral vascular disease, cerebral vasospasm, appetite regulation, neurodegeneration, pain - including neuropathic pain and chronic pain - and impotence in mammals and humans by administering such compositions to subjects in need thereof. The invention also is directed to processes of manufacturing such compositions.

    摘要翻译: 本发明涉及药物组合物,其包含药理学有效量的a)至少一种作为第一活性剂的至少一种ATP通道调节剂,和b)至少一种CB 调节剂作为第二活性剂。 本发明还涉及这样的组合物的用途,以及治疗,预防,延缓发病和/或抑制多种疾病状况(包括肥胖症,糖尿病,代谢综合征,综合征X,胰岛素瘤,家族性高胰岛素)的方法 低血糖,男性型秃发,逼尿肌反应过度,哮喘,神经保护,癫痫,止痛,心脏保护,心绞痛,心脏停跳,心律失常,冠状动脉痉挛,外周血管疾病,脑血管痉挛,食欲调节,神经变性,疼痛 - 包括神经性疼痛和慢性疼痛 通过将这些组合物给予有需要的受试者,在哺乳动物和人类中发挥阳。。 本发明还涉及制造这种组合物的方法。