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    • 54. 发明申请
    • Method and composition for the control of hair growth
    • 用于控制头发生长的方法和组成
    • US20040131574A1
    • 2004-07-08
    • US10467366
    • 2004-01-20
    • Raymond J Bergeron JR.
    • A61K007/06A61K007/11
    • A61Q7/00A61K8/84A61K31/13A61K31/133A61K31/785
    • Disclosed are pharmaceutical compositions and methods for controlling the growth of hair by topically applying to a human or non-human mammal a polyamine or a salt thereof with a pharmaceutically acceptable acid, the polyamine having formula (I) wherein: R1-R6 may be the same or different and are hydrogen, alkyl, hydrocarbyl aryl, hydrocarbyl aryl alkyl, cycloalkyl, or any of the foregoing wherein the alkyl chain is interrupted by at least one etheric oxygen atom with the proviso that R1 and R6 may not both be hydrogen; N1, N2, N3 and N4 are nitrogen atoms capable of protonation at physiological pHs; a and b may be the same or different and are integers from 0 to 6; A, B and C may be the same or different and are integers from 0 to 6; A, B and C may be the same or different and are bridging groups of variable length, including unsubstituted heterocyclic bridging groups which incorporate as a hetero atom therein said N1 or N4; and further wherein said A, B, C are selected such that they effectively maintain the distance between the nitrogen atoms such that the polyamine: (i) is capable of uptake by a target cell upon topical application of the polyamine to said human or non-human mammal; and (ii) upon uptake by the target cell, competitively binds via an electrostatic interaction between the positively charged nitrogen atoms to substantially the same biological counter-anions as the intracellular natural polyamines in the target cell; the polyamine, upon binding to the biological counter-anion in the cell, functions to inhibit the formation therein of the enzyme, ornithine decarboxylase. 1
    • 公开了用于通过向药物或非人哺乳动物将多胺或其盐与药学上可接受的酸局部施用来控制毛发生长的药物组合物和方法,所述多胺具有式(I),其中:R 1 -R 6可以是 相同或不同的是氢,烷基,烃基芳基,烃基芳基烷基,环烷基或前述的任何一种,其中烷基链被至少一个醚性氧原子间隔,条件是R 1和R 6不能都是氢; N 1,N 2,N 3和N 4是能够在生理pH下质子化的氮原子; a和b可以相同或不同,为0至6的整数; A,B和C可以相同或不同,为0至6的整数; A,B和C可以相同或不同,并且是可变长度的桥连基团,包括在其中引入其中所述N 1或N 4的杂原子的未取代的杂环桥基; 并且进一步地,其中所述A,B,C被选择为使得它们有效地保持氮原子之间的距离,使得多胺:(i)在将多胺局部施用于所述人或非多胺时能够被靶细胞摄取, 人类哺乳动物 和(ii)被靶细胞吸收后,通过正电荷的氮原子之间的静电相互作用与目标细胞中细胞内天然多胺的基本相同的生物反阴离子竞争性结合; 多胺在与细胞中的生物反阴离子结合时发挥功能,抑制其中的鸟氨酸脱羧酶的形成。