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    Therapeutic agent for pain disease
    3.
    发明授权
    Therapeutic agent for pain disease 有权
    疼痛病治疗剂

    公开(公告)号：US08492350B2

    公开(公告)日：2013-07-23

    申请号：US12449152

    申请日：2008-02-06

    Applicant: Yoshitaka Nakazawa

    Inventor： Yoshitaka Nakazawa

    IPC: A61K31/70 ,  C07H5/04 ,  C07H5/06 ,  C08B37/00 ,  A01N43/04

    CPC classification number: A61K31/7012 ,  C07H7/027

    Abstract: A method for treating neuropathic pain by administering a pharmaceutical preparation containing N-acetylneuraminic acid or a pharmaceutically acceptable salt thereof to a person in need of treatment of neuropathic pain. Examples of neuropathic pain include trigeminal neuralgia, postherpetic neuralgia, strangulated neuropathy, complex regional pain syndrome (CRPS), diabetic neuropathy, neuropathy caused by trauma, phantom limb pain, central pain, and neuropathic pain caused by drug therapy or radiation therapy.

    Abstract translation: 一种通过向需要治疗神经性疼痛的人施用含有N-乙酰神经氨酸或其药学上可接受的盐的药物制剂来治疗神经性疼痛的方法。 神经性疼痛的例子包括三叉神经痛，带状疱疹后神经痛，窒息性神经病变，复杂区域性疼痛综合征（CRPS），糖尿病性神经病变，由创伤引起的神经病变，幻肢疼痛，中枢性疼痛和药物治疗或放射治疗引起的神经性疼痛。

    THERAPEUTIC AGENT FOR PAIN DISEASE
    6.
    发明申请
    THERAPEUTIC AGENT FOR PAIN DISEASE 有权
    用于治疗疼痛的治疗剂

    公开(公告)号：US20100121040A1

    公开(公告)日：2010-05-13

    申请号：US12449152

    申请日：2008-02-06

    Applicant: Yoshitaka Nakazawa

    Inventor： Yoshitaka Nakazawa

    IPC: C07H7/027

    CPC classification number: A61K31/7012 ,  C07H7/027

    Abstract: 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.

    Abstract translation: 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。

    Method for the production of 2=-keto-l-gulonic acid C4C10 alkyl esters
    8.
    发明授权
    Method for the production of 2=-keto-l-gulonic acid C4C10 alkyl esters 失效
    制备2 =酮-1-古洛糖酸C 4 C 10烷基酯的方法

    公开(公告)号：US07091375B2

    公开(公告)日：2006-08-15

    申请号：US10534334

    申请日：2003-11-07

    Applicant: Thomas Domschke ,  Martin Merger ,  Georg Grossmann ,  Tillmann Faust

    Inventor： Thomas Domschke ,  Martin Merger ,  Georg Grossmann ,  Tillmann Faust

    IPC: C07D305/12

    CPC classification number: C07H7/027 ,  Y02P20/127

    Abstract: 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.

    Abstract translation: 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。

    Process for producing sugar chain asparagine derivative
    9.
    发明申请
    Process for producing sugar chain asparagine derivative 有权
    制备糖链天冬酰胺衍生物的方法

    公开(公告)号：US20040181054A1

    公开(公告)日：2004-09-16

    申请号：US10481246

    申请日：2003-12-18

    Inventor： Yasuhiro Kajihara ,  Ken Sasaki

    IPC: C13K005/00

    CPC classification number: C07H13/10 ,  C07H5/06 ,  C07H7/027 ,  C07H15/12 ,  C12P13/04 ,  C12P19/04 ,  C12P19/28 ,  Y02P20/55

    Abstract: The present invention provides a process for preparing a sugar chain asparagine derivative. According to the process, various isolated sugar chain asparagine derivatives useful in the field of the development of pharmaceuticals and the like can be conveniently obtained in a large amount as compared to that of the prior art. The present invention also provides a process for preparing a sugar chain asparagine and a process for preparing a sugar chain via a step for preparing a sugar chain asparagine derivative. The present invention further provides a novel sugar chain asparagine derivative, a sugar chain asparagine and a sugar chain.

    Abstract translation: 本发明提供了制备糖链天冬酰胺衍生物的方法。 根据该方法，与现有技术相比，可以方便地获得与药物开发领域有用的各种分离的糖链天冬酰胺衍生物。 本发明还提供了制备糖链天冬酰胺的方法和通过制备糖链天冬酰胺衍生物的步骤制备糖链的方法。 本发明还提供了一种新型的糖链天冬酰胺衍生物，糖链天冬酰胺和糖链。

    Chromogenic substrates of sialidase and methods of making and using the same
    10.
    发明授权
    Chromogenic substrates of sialidase and methods of making and using the same 有权
    唾液酸酶的显色底物及其制备和使用方法

    公开(公告)号：US06512100B1

    公开(公告)日：2003-01-28

    申请号：US09651622

    申请日：2000-08-30

    Applicant: Stephen C Johnson ,  Ashraf Saeed ,  Ming Luo

    Inventor： Stephen C Johnson ,  Ashraf Saeed ,  Ming Luo

    IPC: C07H1504

    CPC classification number: C07H15/203 ,  C07H7/027 ,  C07H15/24 ,  C07H17/02 ,  C07H17/075

    Abstract: The subject invention discloses materials and methods for the design, synthesis, and biochemical evaluation of chromogenic substrate compounds for sialidases of bacterial, viral, protozoa, and vertebrate (including humans) origin. In particular, this invention provides a novel class of effective compounds as chromogenic substrates of these sialidases which yield chromogenic products after reactions catalyzed by sialidase take place. Also provided are methods of making these substrate compounds, methods of diagnosis and prognosis of sialidase related diseases using these substrate compounds.

    Abstract translation: 本发明公开了用于细菌，病毒，原生动物和脊椎动物（包括人）起源的唾液酸酶的显色底物化合物的设计，合成和生物化学评估的材料和方法。 特别地，本发明提供了一种新型的有效化合物作为这些唾液酸酶的显色底物，其在由唾液酸酶催化的反应发生后产生显色产物。 还提供了使用这些底物化合物制备这些底物化合物的方法，唾液酸酶相关疾病的诊断和预后的方法。

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