Soluble tachykinin antagonists, the preparation and use thereof
    1.
    发明授权
    Soluble tachykinin antagonists, the preparation and use thereof 失效
    可溶性速激肽拮抗剂,其制备及应用

    公开(公告)号:US6075006A

    公开(公告)日:2000-06-13

    申请号:US125542

    申请日:1998-08-28

    摘要: The compounds of formula (I) cyclo[X.sub.1.sup.1 --Z.sub.1.sup.2 --X.sub.2.sup.3 --X.sub.3.sup.4 --Z.sub.2.sup.5 --X.sub.4.sup.6 ]cyclo(2.beta.-5.beta.) wherein: X.sub.1 =(D or L)Cys(Y) or (D or L)SeCys(Y), Z.sub.1 =Asp and Z.sub.2 =Dap or Z.sub.1 =Dap and Z.sub.2 =Asp and X.sub.2, X.sub.3 and X.sub.4 =natural or synthetic hydrophobic amino acids, having Z.sub.1, Z.sub.2, X.sub.2, X.sub.3 and X.sub.4 the same D or L configuration; Y=is a glycosidic group selected from the aldo and keto hexoses in the furanose or pyranose form bound to the cysteine with an .alpha. or .beta. thioacetalic bond or a cyclithol or a polyvinyl alcohol or PEG, constituted of 5 to 10 monomeric unities, bound to the cysteine with a thioether bond, are endowed of high solubility and of potent tachykinin-antagonistic activity.

    摘要翻译: PCT No.PCT / EP97 / 00917 Sec。 371日期1998年8月28日 102(e)1998年8月28日PCT 1997年2月26日PCT PCT。 第WO97 / 31941号公报 日期:1997年9月4日式(I)环[X11-Z12-X23-X34-Z25-X46]环(2β-5β)的化合物其中:X1 =(D或L)Cys(Y)或(D 或L)SeCys(Y),Z1 = Asp和Z2 = Dap或Z1 = Dap和Z2 = Asp,X2,X3和X4 =天然或合成疏水性氨基酸,具有Z1,Z2,X2,X3和X4相同的D 或L配置; Y =是选自醛糖或吡喃糖形式的醛糖和酮糖己糖的糖苷基,其与α或β硫代缩醛键结合到半胱氨酸,或者由5至10个单体单体组成的环戊醇或聚乙烯醇或PEG结合 具有硫醚键的半胱氨酸具有高溶解度和有效的速激肽拮抗活性。

    Eutectic mixtures in cosmetic compositions
    2.
    发明授权
    Eutectic mixtures in cosmetic compositions 失效
    化妆品组合物中的共晶混合物

    公开(公告)号:US06410036B1

    公开(公告)日:2002-06-25

    申请号:US09564218

    申请日:2000-05-04

    IPC分类号: A61K700

    摘要: The present invention relates to a liquid, substantially anhydrous eutectic mixture comprising a principal acid component, such as a hydroxy acid, and at least one other component selected from the group consisting of a carbohydrate, a polyol, an amino acid, and a carboxylic acid. The mixtures remain liquid at room temperature, are relatively non-irritating, and can be used to deliver higher levels of the principal acid than would ordinarily be possible. The invention also provides a method of making such a mixture comprising heating the component having the lowest melting point to the temperature at which it melts, dissolving the remaining component or components in the melted component, and allowing the mixture to cool.

    摘要翻译: 本发明涉及一种液体,基本上无水的共晶混合物,其包含主要酸组分,例如羟基酸,和至少一种选自碳水化合物,多元醇,氨基酸和羧酸的其它组分 。 混合物在室温下保持液体,相对不刺激,并且可以用于递送比通常可能的更高水平的主要酸。 本发明还提供一种制备这种混合物的方法,包括将具有最低熔点的组分加热至其熔融的温度,将剩余的组分溶解在熔融组分中,并使混合物冷却。