Topical Lightening Composition and Uses Thereof
    1.
    发明申请
    Topical Lightening Composition and Uses Thereof 有权
    局部减光成分及用途

    公开(公告)号:US20120003168A1

    公开(公告)日:2012-01-05

    申请号:US12975415

    申请日:2010-12-22

    IPC分类号: A61K8/46 A61Q19/02

    CPC分类号: A61K31/74 A61K8/46 A61Q19/02

    摘要: The disclosure relates to novel topical lightening compositions a skin depigmenting agent and a vehicle. There is provided a topical lightening composition comprising a substituted-4-oxobutanoic acid, ester, or amide tyrosinase inhibitor, and a vehicle. The depigmenting agents of this disclosure can be used as such or as a pharmaceutically acceptable salt including conventional non-toxic salts which include a metal salt or an alkaline earth metal salt, an ammonium salt, or an organic base salt. The depigmenting agents of this disclosure can be incorporated into any cosmetically-, dermatologically-, or cosmeticatically-acceptable vehicle or carrier normally used for topical application. The compositions and methods of the disclosure are effective to lighten skin, hair, lips, and/or nails.

    摘要翻译: 本公开涉及新颖的局部减光组合物皮肤色素沉着剂和载体。 提供了包含取代的-4-氧代丁酸,酯或酰胺酪氨酸酶抑制剂和载体的局部减轻组合物。 本公开的脱色剂可以原样使用或作为药学上可接受的盐使用,包括常规无毒盐,包括金属盐或碱土金属盐,铵盐或有机碱盐。 本公开的脱色剂可以并入通常用于局部应用的美容,皮肤病学或化妆品可接受的载体或载体中。 本公开的组合物和方法有效地减轻皮肤,头发,嘴唇和/或指甲。

    Topical lightening composition and uses thereof
    2.
    发明授权
    Topical lightening composition and uses thereof 有权
    局部减光组合物及其用途

    公开(公告)号:US08329149B2

    公开(公告)日:2012-12-11

    申请号:US12975415

    申请日:2010-12-22

    IPC分类号: A61K31/74 A61K8/46

    CPC分类号: A61K31/74 A61K8/46 A61Q19/02

    摘要: The disclosure relates to novel topical lightening compositions a skin depigmenting agent and a vehicle. There is provided a topical lightening composition comprising a substituted-4-oxobutanoic acid, ester, or amide tyrosinase inhibitor, and a vehicle. The depigmenting agents of this disclosure can be used as such or as a pharmaceutically acceptable salt including conventional non-toxic salts which include a metal salt or an alkaline earth metal salt, an ammonium salt, or an organic base salt. The depigmenting agents of this disclosure can be incorporated into any cosmetically-, dermatologically-, or cosmeticatically-acceptable vehicle or carrier normally used for topical application. The compositions and methods of the disclosure are effective to lighten skin, hair, lips, and/or nails.

    摘要翻译: 本公开涉及新颖的局部减光组合物皮肤色素沉着剂和载体。 提供了包含取代的-4-氧代丁酸,酯或酰胺酪氨酸酶抑制剂和载体的局部减轻组合物。 本公开的脱色剂可以原样使用或作为药学上可接受的盐使用,包括常规无毒盐,包括金属盐或碱土金属盐,铵盐或有机碱盐。 本公开的脱色剂可以并入通常用于局部应用的美容,皮肤病学或化妆品可接受的载体或载体中。 本公开的组合物和方法有效地减轻皮肤,头发,嘴唇和/或指甲。

    Computer Aided Ligand-Based and Receptor-Based Drug Design Utilizing Molecular Shape and Electrostatic Complementarity
    8.
    发明申请
    Computer Aided Ligand-Based and Receptor-Based Drug Design Utilizing Molecular Shape and Electrostatic Complementarity 失效
    基于计算机辅助配体和基于受体的药物设计利用分子形态和静电互补

    公开(公告)号:US20080294404A1

    公开(公告)日:2008-11-27

    申请号:US11870279

    申请日:2007-10-10

    IPC分类号: G06G7/48

    摘要: Methods related to the generation of shape signatures representing molecular shape, and using shape signatures in both ligand-based and receptor-based molecular design. Ray-tracing is used to explore the volume interior to a ligand, or the space exterior to a receptor site. Shape signatures are then probability distributions derived from the ray-traces. Shape signatures provide condensed descriptors of shape properties readily compared to each other to test for shape similarity or complementarity.

    摘要翻译: 与代表分子形状的形状特征的产生相关的方法,以及基于配体和受体的分子设计中的形状特征。 光线跟踪用于探索配体内部的体积,或受体位点外部的空间。 形状特征就是衍射自射线轨迹的概率分布。 形状特征提供形状特征的简明描述,容易相互比较,以测试形状相似性或互补性。

    Estrogen receptor modulators and uses thereof
    9.
    发明授权
    Estrogen receptor modulators and uses thereof 有权
    雌激素受体调节剂及其用途

    公开(公告)号:US08455537B2

    公开(公告)日:2013-06-04

    申请号:US13165431

    申请日:2011-06-21

    摘要: A method for preventing, diagnosing, or treating a condition mediated by an estrogen receptor by administering to a patient in need thereof an effective amount of a compound of formula I, II, or a combination thereof: wherein R1, R3, R4, and R5 are independently selected from H, OH, and ORa; R2 is selected from H, OH, and (C═O) (C1-7)alkyl; Ra is (C1-7)alkyl or (C═O)(C1-7)alkyl; or a derivative of the compound selected from N-oxide derivatives, prodrug derivatives, protected derivatives, isomers, and mixtures of isomers of the compound; or a pharmaceutically acceptable salt or solvate of the compound or the derivative. Compounds of formula I and II and pharmaceuticals compositions thereof are also presented.

    摘要翻译: 一种通过向有需要的患者施用有效量的式I,II化合物或其组合来预防,诊断或治疗由雌激素受体介导的病症的方法,其中R1,R3,R4和R5 独立地选自H,OH和ORa; R 2选自H,OH和(C = O)(C 1-7)烷基; R a为(C 1-7)烷基或(C = O)(C 1-7)烷基; 或选自所述化合物的N-氧化物衍生物,前药衍生物,保护的衍生物,异构体和异构体混合物的化合物的衍生物; 或化合物或其衍生物的药学上可接受的盐或溶剂化物。 还提供了式I和II的化合物及其药物组合物。