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    Allosteric adenosine receptor modulators
    5.
    发明申请
    Allosteric adenosine receptor modulators 审中-公开
    变构腺苷受体调节剂

    公开(公告)号：US20040077630A1

    公开(公告)日：2004-04-22

    申请号：US10663243

    申请日：2003-09-15

    Inventor： Pier Giovanni Baraldi

    IPC: A61K031/55 ,  A61K031/385

    CPC classification number: C07D333/36 ,  A61K31/381 ,  A61K31/382 ,  A61K31/4365 ,  A61K31/4436 ,  C07D333/66 ,  C07D333/78 ,  C07D495/04

    Abstract: The present invention relates to compounds of formulas (IA) and (IB): 1 the preparation thereof, pharmaceutical formulations thereof, and their use in medicine as allosteric adenosine receptor modulators for uses including protection against hypoxia and ischemia induced injury and treatment of adenosine-sensitive cardiac arrhythmias.

    Abstract translation: 本发明涉及式（IA）和（IB）的化合物：其制备方法，其药物制剂及其在医学中作为变构腺苷受体调节剂的用途，包括防止缺氧和缺血诱导的损伤和治疗腺苷敏感 心律失常。

    Methods for preventing and treating loss of balance function due to oxidative stress
    8.
    发明申请
    Methods for preventing and treating loss of balance function due to oxidative stress 审中-公开
    预防和治疗由于氧化应激引起的平衡功能丧失的方法

    公开(公告)号：US20030191064A1

    公开(公告)日：2003-10-09

    申请号：US10401682

    申请日：2003-03-31

    Inventor： Richard D. Kopke

    IPC: A61K038/18 ,  A61K038/06 ,  A61K031/728 ,  A61K031/522 ,  A61K031/426 ,  A61K031/198 ,  A61K031/385 ,  A61K031/05 ,  A61K031/13

    CPC classification number: A61K31/522 ,  A61K31/05 ,  A61K31/13 ,  A61K31/198 ,  A61K31/385 ,  A61K31/426 ,  A61K31/728

    Abstract: The present invention provides methods for preventing and treating loss of, or impairments to, the sense of balance. Specifically, the invention provides methods for preserving the sensory hair cells and neurons of the inner ear vestibular apparatus by preventing or reducing the damaging effects of oxidative stress by administering an effective amount of the following therapeutic agents: antioxidants; compounds utilized by inner ear cells for synthesis of glutathione; antioxidant enzyme inducers; trophic factors; mitochondrial biogenesis factors; and combinations thereof.

    Abstract translation: 本发明提供了预防和治疗平衡感的损失或损害的方法。 具体地，本发明提供了通过施用有效量的以下治疗剂来防止或降低氧化应激的损伤作用来保护内耳前庭装置的感觉毛细胞和神经元的方法：抗氧化剂; 内耳细胞用于合成谷胱甘肽的化合物; 抗氧化酶诱导剂; 营养因素; 线粒体生物发生因子; 及其组合。

    Pharmacological inducement of the fed mode for enhanced drug administration to the stomach
    9.
    发明申请
    Pharmacological inducement of the fed mode for enhanced drug administration to the stomach 有权
    用于增强药物给予胃的喂养模式的药理学诱导

    公开(公告)号：US20030044466A1

    公开(公告)日：2003-03-06

    申请号：US10235076

    申请日：2002-09-04

    Applicant: DEPOMED, INC.

    Inventor： Micheline Markey ,  John W. Shell ,  Bret Berner

    IPC: A61K031/445 ,  A61K031/385 ,  A61K009/26

    CPC classification number: A61K9/0065 ,  A61K9/209 ,  A61K9/5084

    Abstract: Drugs intended for absorption in the stomach or upper intestinal tract are administered in oral drug delivery systems in conjunction with any of various substances that have been discovered to function as potent agents for inducing the fed mode. By inducing the onset of the fed mode, these agents cause the stomach to prolong its retention of the drug delivery system, which is either large enough to be retained in the stomach during the fed mode or swells or expands to such a size upon ingestion. The fed mode inducing agents include the following compounds and their salts: glycine and glycylglycine, xylitol and related sugar alcohols, sodium and other metal docusates, null-casomorphins, null-lipoic acid and similarly structured acids, 2,2-diaryl-4-(4null-aryl-4null-hydroxypipendino)butyramides, arginine, Trp-Trp, alkylpyridinium halides, dihydroxybenzoic acids, and potent sweeteners such as aspartame, aspartic acid, acesulfame, and stevioside.

    Abstract translation: 预期用于在胃或上肠道中吸收的药物在口服药物递送系统中与已被发现用作诱导喂养模式的有效药剂的任何各种物质一起施用。 通过诱导进食模式的发作，这些药物引起胃部延长其药物递送系统的保留，药物递送系统的大小足以在进食模式期间保留在胃中，或者在摄食时膨胀或膨胀至这样的大小。 饲喂模式诱导剂包括以下化合物及其盐：甘氨酸和甘氨酰甘氨酸，木糖醇和相关糖醇，钠和其他金属多库酯，β-半胱氨酸，α-硫辛酸和类似结构的酸，2,2-二芳基-4- （4'-芳基-4'-羟基磷脂）丁酰胺，精氨酸，Trp-Trp，烷基吡啶鎓卤化物，二羟基苯甲酸，以及强效甜味剂，如阿斯巴甜，天冬氨酸，乙酰磺胺酸和甜菊苷。

    Steroid sulphatase inhibitors
    10.
    发明申请
    Steroid sulphatase inhibitors 失效
    类固醇硫酸酶抑制剂

    公开(公告)号：US20020177619A1

    公开(公告)日：2002-11-28

    申请号：US10082007

    申请日：2002-02-21

    Inventor： Michael John Reed ,  Barry Victor Lloyd Potter

    IPC: A61K031/385 ,  A61K031/255

    CPC classification number: A61K31/37 ,  C07D311/16 ,  C07D311/30 ,  C07D311/32 ,  C07D311/36 ,  C07J41/0072

    Abstract: A method for controlling estrogen production comprising administering a ring system compound comprising a sulphamic acid ester group; wherein said compound is an inhibitor of an enzyme having steroid sulphatase activity (EC 3.1.6.2); and wherein if the sulphamic acid ester group of said compound is replaced with a sulphate group to form a sulphate compound and incubated with a steroid sulphatase enzyme (EC 3.1.6.2) at a pH 7.4 and 37null C. it provides a Km value of less than 50 nullM. A method to target the estrogen metabolic pathway comprising administering a ring system compound comprising a sulphamic acid ester group; wherein said compound is an inhibitor of an enzyme having steroid sulphatase activity (EC 3.1.6.2); and wherein if the sulphamic acid ester group of said compound is replaced with a sulphate group to form a sulphate compound and incubated with a steroid sulphatase enzyme (EC 3.1.6.2) at a pH 7.4 and 37null C. it provides a Km value of less than 50 nullM.

    Abstract translation: 一种控制雌激素产生的方法，包括施用包含氨基磺酸酯基团的环系化合物; 其中所述化合物是具有类固醇硫酸酯酶活性的酶的抑制剂（EC 3.1.6.2）; 并且其中如果所述化合物的氨基磺酸酯基团被硫酸根基团替代以形成硫酸盐化合物，并在pH 7.4和37℃下与类固醇硫酸酶（EC 3.1.6.2）温育，则其提供Km值 小于50亩。 靶向雌激素代谢途径的方法，包括施用包含氨基磺酸酯基团的环系化合物; 其中所述化合物是具有类固醇硫酸酯酶活性的酶的抑制剂（EC 3.1.6.2）; 并且其中如果所述化合物的氨基磺酸酯基团被硫酸根基团替代以形成硫酸盐化合物，并在pH 7.4和37℃下与类固醇硫酸酶（EC 3.1.6.2）温育，则其提供Km值 小于50亩。

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