Anticonvulsant and central nervous system-depressing bis(fluorophenyl)alkylamides and their uses
    3.
    发明授权
    Anticonvulsant and central nervous system-depressing bis(fluorophenyl)alkylamides and their uses 失效
    抗惊厥和中枢神经系统抑制双(氟苯基)烷基酰胺及其用途

    公开(公告)号:US06617358B1

    公开(公告)日:2003-09-09

    申请号:US09587179

    申请日:2000-06-02

    IPC分类号: A61K31165

    摘要: Bis(Fluorophenyl)alkylamides have been chemically synthesized which possess beneficial pharmacological properties (e.g., anticonvulsant activity) useful for the treatment of neurological diseases or disorders, such as, for example, epilepsy, convulsions, and seizure disorders. The preferred compounds of the invention also cause little sedation and have high therapeutic and protective indices in animal models of epilepsy. These compounds further possess long pharmacological half-lives, which, in practical clinical therapeutic application, should translate into once-a-day dosing, of great benefit to patients suffering from these diseases and/or disorders. These compounds may also be of further clinical utility in the treatment of other diseases and disorders of the central and peripheral nervous systems, or diseases or disorders affected by them, including, but not limited to, spasticity, skeletal muscle spasms and pain, restless leg syndrome, anxiety and stress, and bipolar disorder.

    摘要翻译: 已经化学合成了双(氟苯基)烷基酰胺,其具有可用于治疗神经疾病或病症(例如癫痫,抽搐和癫痫发作)的有益的药理学性质(例如抗惊厥活性)。 本发明优选的化合物在癫痫的动物模型中也引起很少的镇静作用并具有较高的治疗和保护指标。 这些化合物还具有长的药理学半衰期,其在实际临床治疗应用中应该转化为每天一次给药,对患有这些疾病和/或病症的患者是非常有益的。 这些化合物还可用于治疗中枢和周围神经系统的其他疾病和病症,或受其影响的疾病或病症,包括但不限于痉挛性,骨骼肌痉挛和疼痛,不宁腿 综合征,焦虑和压力和双相情感障碍。

    Use of isovaleramide as a mild anxiolytic and sedative agent
    6.
    发明授权
    Use of isovaleramide as a mild anxiolytic and sedative agent 失效
    使用异戊酰胺作为轻度抗焦虑和镇静剂

    公开(公告)号:US5506268A

    公开(公告)日:1996-04-09

    申请号:US075126

    申请日:1993-06-11

    IPC分类号: A61K31/16 A61P25/20 A61P25/22

    CPC分类号: A61K31/16 Y10S514/923

    摘要: Isovaleramide has been found to exhibit mild anxiolytic activity at low to moderate dosage levels and mildly sedative at somewhat higher dosage levels. In contrast to certain other materials thought to be anxiolytic or mildly sedative, isovaleramide is non-cytotoxic and does not paradoxically stimulate the central nervous system. Isovaleramide is therefore useful as a mild anxiolytic and mild sedative which can be made available to the general public.

    摘要翻译: 已经发现异戊酰胺在低至中等剂量水平下表现出轻度的抗焦虑活性,并且在稍高的剂量水平下轻度镇静。 与被认为是抗焦虑或轻度镇静的某些其他物质相反,异戊酰胺是非细胞毒性的,并不矛盾地刺激中枢神经系统。 因此,异戊酰胺可作为轻度抗焦虑和轻度镇静剂而使用,可向公众提供。

    Compositions comprising valerian extracts, isovaleric acid or derivatives thereof with a NSAID
    8.
    发明授权
    Compositions comprising valerian extracts, isovaleric acid or derivatives thereof with a NSAID 失效
    包含缬草提取物,异戊酸或其衍生物与NSAID的组合物

    公开(公告)号:US06383527B1

    公开(公告)日:2002-05-07

    申请号:US09623384

    申请日:2001-02-22

    IPC分类号: A01N6500

    CPC分类号: A61K45/06

    摘要: Preparations and extracts of valerian, as well as isovaleramide, isovaleric acid, and its pharmaceutically acceptable salts, esters, and substituted amides, and other valerian-related compounds, in combination with NSAIDs exhibit clinically significant pharmacological properties which implicate a treatment for acute muscular aches, strains, and sprains which occur from a localized, external insult to a particular muscle or muscle group outside of, or peripheral to, the CNS. The compositions in question generally are non-cytotoxic and do not elicit weakness or sedative activity at doses that are effective for the symptomatic treatment of such pathological conditions.

    摘要翻译: 缬草的制备和提取物以及异戊酰胺,异戊酸及其药学上可接受的盐,酯和取代的酰胺和其他缬草相关化合物与NSAID组合显示出临床显着的药理学性质,其涉及急性肌肉酸痛的治疗 ,菌株和扭伤,其从CNS的外部或周围的特定肌肉或肌肉组的局部外部侮辱发生。 所讨论的组合物通常是非细胞毒性的,并且在对这种病理状况进行症状治疗有效的剂量下不引起无力或镇静作用。