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    • 6. 发明申请
    • THERAPEUTIC AGENT FOR PAIN DISEASE
    • 用于治疗疼痛的治疗剂
    • US20100121040A1
    • 2010-05-13
    • US12449152
    • 2008-02-06
    • Yoshitaka Nakazawa
    • Yoshitaka Nakazawa
    • C07H7/027
    • A61K31/7012C07H7/027
    • Disclosed is an analgesic agent for a non-inflammatory pain disease, which comprises a sialic acid or a pharmaceutically acceptable salt thereof as an active ingredient. The sialic acid which is an active ingredient for the agent has an analgesic effect on a disease model animal of neurogenic pain which is a non-inflammatory pain. Therefore, the analgesic agent is useful as a pharmaceutical agent for the treatment of a non-inflammatory pain disease such as a neurogenic pain disease, e.g. trigeminal neuralgia, postherpetic neuralgia, entrapment neuropathy, complex regional pain syndrome, diabetic neuropathy, traumatic neuropathy, phantom limb pain, central pain after spinal cord injury or stroke, and neuropathy caused by pharmacotherapy or radiation therapy, or the like.
    • 公开了一种非炎症性疼痛疾病的止​​痛剂,其包含唾液酸或其药学上可接受的盐作为活性成分。 作为药剂的活性成分的唾液酸对作为非炎症性疼痛的神经源性疼痛的疾病模型动物具有镇痛作用。 因此,止痛剂可用作治疗非炎性疼痛疾病如神经性疼痛疾病的药剂,例如神经性疼痛疾病。 三叉神经痛,带状疱疹后神经痛,包埋神经病,复杂的局部疼痛综合征,糖尿病性神经病,外伤性神经病,幻肢疼痛,脊髓损伤或中风后的中枢疼痛,以及由药物治疗或放射治疗引起的神经病变等。
    • 8. 发明授权
    • Method for the production of 2=-keto-l-gulonic acid C4C10 alkyl esters
    • 制备2 =酮-1-古洛糖酸C 4 C 10烷基酯的方法
    • US07091375B2
    • 2006-08-15
    • US10534334
    • 2003-11-07
    • Thomas DomschkeMartin MergerGeorg GrossmannTillmann Faust
    • Thomas DomschkeMartin MergerGeorg GrossmannTillmann Faust
    • C07D305/12
    • C07H7/027Y02P20/127
    • The invention relates to a method for producing 2-keto-L-gulonic acid-C4–C10 alkyl ester by esterifying 2-keto-L-gulonic acid (KGS) with an unsaturated, branched or unbranched C4–C10 alcohol. The inventive method is characterized by the fact that an aqueous KGS solution is reacted with a C4–C10 alcohol up to an esterification degree of 20 to 70 percent in a pre-esterification process carried out under acidic catalysis conditions; and the obtained product is dehydrogenated with an unsaturated, branched or unbranched C4–C10 alcohol in a continuous rectification device, whereby the esterification reaction continues, n-butanol preferably being used as the alkyl alcohol. In a preferred embodiment, the aqueous KGS solution is concentrated up to or beyond the limit of solubility prior to the esterification process, preferably by catalyzing a homogeneous or heterogeneous catalyst, especially sulfonic acid, at temperatures of 50 to 120° C. In another embodiment, the produced KGS ester is reacted in one or several additional steps so as to obtain L-ascorbic acid.
    • 本发明涉及通过酯化2-酮-L-古洛糖酸(KGS)制备2-酮-L-古洛糖酸-C 4 -C 10烷基酯的方法 )与不饱和,支链或非支链C 4 -C 10醇。 本发明的方法的特征在于,将KGS水溶液与C 4 -C 10 - 醇反应,直到酯化程度为20至70% 在酸性催化条件下进行酯化过程; 并将得到的产物用连续精馏装置中的不饱和支链或非支链C 4 -C 10醇脱氢,由此继续进行酯化反应,正丁醇优选为 用作烷基醇。 在优选的实施方案中,在酯化过程之前,优选通过在50至120℃的温度下催化均相或多相催化剂,特别是磺酸,将KGS水溶液浓缩至或超过溶解度的极限。在另一个实施方案中 ,所制备的KGS酯在一个或几个附加步骤中反应,以获得L-抗坏血酸。