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    • 28. 发明申请
    • FATTY ACID ANALOGUES FOR THE TREATMENT OF PROLIFERATIVE SKIN DISORDERS
    • 脂肪酸类似物治疗增生性皮肤病
    • WO0226218A3
    • 2002-06-13
    • PCT/NO0100393
    • 2001-09-27
    • THIA MEDICA ASBERGE ROLFKRISTIANSEN KARSTEN
    • BERGE ROLFKRISTIANSEN KARSTEN
    • A61K31/19A61K31/20A61K31/215A61P17/00A61P17/06A61P17/08A61P17/12A61P37/08A61K31/201A61K31/202
    • A61K31/20
    • The present invention relates to fatty acid analogues of the general formula (I): R1- [xi - CH2]n - COOR2 wherein R1 is; a C1-C24 alkene with one or more double bonds and/or with one or more triple bonds, and/or a C1-C24 alkyne, and/or a C1-C24 alkyl, or a C1-C24 alkyl substituted in one or several positions with one or more compounds selected from the group comprising fluoride, chloride, hydroxy, C1-C4 alkoxy, C1-C4 alkylthio, C2-C5 acyloxy or C1-C4 alkyl, and wherein R2 represents hydrogen or C1-C4 alkyl, and wherein n is an integer from 1 to 12, and wherein i is an odd number and indicates the position relative to COOR2, and wherein X1 independent of each other are selected from the group comprising O, S, SO, SO2, Se and CH2, and with the proviso that at least one of the Xi is not CH2, and with the proviso that if R1 is an alkyne or alkene, then the carbon-carbon triple bond or double bond is positioned between the ( omega -1) carbon and the ( omega -2) carbon, or between the ( omega -2) carbon and the ( omega -3) carbon, or between the ( omega -3) carbon and the ( omega -4) carbon, which can be used for the treatment and/or prevention of proliferative skin disorders. More specifically the invention relates to the inhibition of proliferation and/or differentiation of keratinocytes.
    • 本发明涉及通式(I)的脂肪酸类似物:R1- [xi-CH2] n-COOR2其中R1是; 具有一个或多个双键和/或具有一个或多个三键的C1-C24烯烃和/或C1-C24炔烃,和/或C1-C24烷基或被一个或多个 与选自氟化物,氯化物,羟基,C 1 -C 4烷氧基,C 1 -C 4烷硫基,C 2 -C 5酰氧基或C 1 -C 4烷基的组中的一种或多种化合物反应,并且其中R 2表示氢或C 1 -C 4烷基,并且其中 n是1至12的整数,并且其中i是奇数并且表示相对于COOR 2的位置,并且其中彼此独立的X 1选自组 包括O,S,SO,SO 2,Se和CH 2,条件是至少一个X 1不是CH 2,并且条件是如果R 1是炔烃或烯烃,则碳 - 碳三键或双键 键位于(ω-1)碳和(ω-2)碳之间,或(ω-2)碳和(ω-3)碳之间,或(ω-3)碳和(ω- 欧米茄-4)碳,whic h可以用于治疗和/或预防增殖性皮肤病。 更具体地说,本发明涉及抑制角质形成细胞的增殖和/或分化。