Compositions comprising 2-hydroxycarboxylic acids and related compounds, and methods for alleviating signs of dermatological aging
    1.
    发明授权
    Compositions comprising 2-hydroxycarboxylic acids and related compounds, and methods for alleviating signs of dermatological aging 失效
    包含2-羟基羧酸和相关化合物的组合物,以及减轻皮肤病学老化症状的方法

    公开(公告)号:US06384079B1

    公开(公告)日:2002-05-07

    申请号:US09224949

    申请日:1999-01-04

    IPC分类号: A61K317048

    摘要: Uses of topical compositions comprising a 2-hydroxycarboxylic acid or related compound to alleviate or improve signs of skin, nail and hair changes associated with intrinsic or extrinsic aging are disclosed. 2-Hydroxycarboxylic acids and their related compounds include, for example, 2-hydroxyethanoic acid, hydroxypropanoic acid, 2-methyl 2-hydroxypropanoic acid, 2-phenyl 2-hydroxyethanoic acid, 2-phenyl 2-methyl 2-hydroxyethanoic acid, 2-phenyl 3-hydroxypropanoic acid, 2,2-diphenyl 2-hydroxyethanoic acid, 2-hydroxybutane-1,4-dioic acid, 2,3-hihydroxybutane-1,4-dioic acid, 2-carboxy 2-hydroxypentane-1,5-dioic acid, 2-ketopropanoic acid, methyl 2-ketopropanoate, ethyl 2-ketopropanoate, and gluconolactone. Topical application of compositions comprising 2-hydroxycarboxylic acid and/or related compounds has been found to alleviate or improve skin lines; blotches; blemishes; nodules; wrinkles; pigmented spots; atrophy; precancerous lesions; elastotic changes characterized by leathery, coarse, rough, dry and yellowish skin; and other skin changes associated with intrinsic aging or skin damages caused by extrinsic factors such as sunlight, radiations, air pollution, wind, cold, dampness, heat, chemicals, smoke and cigarette smoking. Topical applications of such compositions have also been found to improve the overall qualities of nail and hair affected by intrinsic aging or damaged by extrinsic factors.

    摘要翻译: 公开了包含2-羟基羧酸或相关化合物的局部组合物用于缓解或改善与内在或外在老化相关的皮肤,指甲和毛发变化的迹象。 2-羟基羧酸及其相关化合物包括例如2-羟基乙酸,羟丙酸,2-甲基-2-羟基丙酸,2-苯基2-羟基乙酸,2-苯基2-甲基2-羟基乙酸,2-苯基2-羟基乙酸, 苯基3-羟基丙酸,2,2-二苯基2-羟基乙酸,2-羟基丁烷-1,4-二酸,2,3-羟基丁烷-1,4-二酸,2-羧基-2-羟基戊烷-1,5- 二酮酸,2-酮戊酸,2-酮基丙酸甲酯,2-酮丙酸乙酯和葡萄糖酸内酯。 发现包含2-羟基羧酸和/或相关化合物的组合物的局部施用可减轻或改善皮肤线; 斑点 瑕疵 结节; 皱纹 着色点; 萎缩 癌前病变 弹性变化以皮革,粗糙,粗糙,干燥和淡黄色皮肤为特征; 以及与外部因素如阳光,辐射,空气污染,风,寒冷,潮湿,热,化学品,烟雾和吸烟引起的内在衰老或皮肤损伤相关的其他皮肤变化。 也已经发现这些组合物的局部应用可以改善受内在老化影响的指甲和头发的整体质量或由外在因素损坏。

    Use of harpagid-related compounds for prevention and treatment of osteoporosis, arthritis and ruptured disc and pharmaceutical composition containing the same
    2.
    发明授权
    Use of harpagid-related compounds for prevention and treatment of osteoporosis, arthritis and ruptured disc and pharmaceutical composition containing the same 失效
    使用与标签相关的化合物预防和治疗骨质疏松症,关节炎和破裂的椎间盘以及含有它们的药物组合物

    公开(公告)号:US06812214B2

    公开(公告)日:2004-11-02

    申请号:US09995691

    申请日:2001-11-29

    IPC分类号: A61K317048

    CPC分类号: A61K31/7048

    摘要: In the present invention, it is discovered that a compound of formula (I) has a potent effect for treatment of osteoporosis, arthritis and ruptured disc: in which R1 represents hydrogen atom or alkyl group and R2 represents hydrogen atom r cinnamoyl group. Therefore, the compound of formula (I) can be used for prevention and treatment of osteoporosis, arthritis and ruptured disc. Thus, the present invention provides a pharmaceutical preparation containing as an effective component a compound of formula (I) in combination with a pharmaceutically acceptable auxiliary, diluent, isotonic agent, preservative, lubricant and solubilizing aid, which is formulated in the form of a pharmaceutically acceptable preparation and has a potent effect for osteoporosis, arthritis and ruptured disc.

    摘要翻译: 在本发明中,发现式(I)化合物对治疗骨质疏松症,关节炎和破裂盘具有有效的作用:其中R1表示氢原子或烷基,R2表示氢原子肉桂酰基。 因此,式(I)化合物可用于预防和治疗骨质疏松症,关节炎和破裂性椎间盘。 因此,本发明提供了药物制剂,其含有式(I)化合物作为有效成分与药学上可接受的助剂,稀释剂,等渗剂,防腐剂,润滑剂和增溶助剂的组合,其以药学上可接受的形式配制 可接受的制剂,对骨质疏松,关节炎和破裂性椎间盘具有有效的作用。

    23-O-substituted 5-O-mycaminosyltylonide derivatives
    3.
    发明授权
    23-O-substituted 5-O-mycaminosyltylonide derivatives 失效
    23-O-取代的5-O-碳霉糖基海藻衍生物

    公开(公告)号:US06753415B2

    公开(公告)日:2004-06-22

    申请号:US10126076

    申请日:2002-04-19

    IPC分类号: A61K317048

    CPC分类号: C07H17/08

    摘要: There are described novel 5-O-mycaminosyltylonide (OMT) analogs possessing increased antibacterial activity toward Gram positive and Gram negative bacteria as well as macrolide resistant Gram positives and pharmaceutically acceptable compositions comprising a therapeutically effective amount of a compound of the invention in combination with a pharmaceutically acceptable carrier. Also described are a method for treating bacterial infections by administering to a patient a pharmaceutical composition containing a therapeutically-effective amount of a compound of the invention, and processes for the preparation of such compounds

    摘要翻译: 描述了具有对革兰氏阳性和革兰氏阴性细菌以及大环内酯抗性革兰氏阳性和药学上可接受的组合物具有增加的抗细菌活性的新型5-O-碳霉糖基托伦(OMT)类似物,其包含治疗有效量的本发明化合物与 药学上可接受的载体。 还描述了通过向患者施用含有治疗有效量的本发明化合物的药物组合物和用于制备这些化合物的方法来治疗细菌感染的方法