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    Phenylacetonitrile derivatives and hair tonics and external preparations for skin containing the derivatives
    4.
    发明申请
    Phenylacetonitrile derivatives and hair tonics and external preparations for skin containing the derivatives 审中-公开
    苯乙腈衍生物和头发滋养物以及含有衍生物的皮肤外用制剂

    公开(公告)号：US20050176822A1

    公开(公告)日：2005-08-11

    申请号：US10509246

    申请日：2003-03-28

    申请人： Naoto Hanyu ,  Koji Kobayashi ,  Masahiro Tajima ,  Akihiro Ishino

    发明人： Naoto Hanyu ,  Koji Kobayashi ,  Masahiro Tajima ,  Akihiro Ishino

    IPC分类号： A61K8/40 ,  A61K8/41 ,  A61P17/14 ,  A61Q7/00 ,  A61Q19/00 ,  C07C255/42 ,  C07C255/43 ,  A61K31/277

    CPC分类号： A61Q19/00 ,  A61K8/40 ,  A61K8/41 ,  A61Q7/00 ,  C07C255/42 ,  C07C255/43

    摘要： A hair growth promoting composition comprising, as an effective ingredient, a phenylacetonitrile derivative or a pharmacologically acceptable salt thereof expressed by the following Formula (I): wherein each of R1 and R2 is hydrogen atom, a C1-10 alkyl group, a C2-10 alkenyl group or C2-10 acyl group, or NR1R2 may be a heterocycle having 3-7 members; R3 is a C1-5 alkyl group; and each of R4, R5 and R6 is hydrogen atom or a C1-4 alkoxy group. The present invention provides a hair growth promoting composition having excellent effects on promoting hair regrowth, preventing or inhibiting hair loss, and the like in human by compounding above-specified phenylacetonitrile derivative as a effective ingredient thereto.

    摘要翻译： 一种毛发生长促进组合物，其包含由下式（I）表示的苯乙腈衍生物或其药理学上可接受的盐作为有效成分：其中R 1和R 2各自表示， SUP>是氢原子，C 1-10烷基，C 2-10链烯基或C 2-10酰基， 或NR 1 R 2可以是具有3-7个成员的杂环; R 3是C 1-5烷基; R 4，R 5和R 6中的每一个为氢原子或C 1-4烷氧基 。 本发明提供一种通过将上述规定的苯乙腈衍生物作为有效成分配合而具有对促进毛发再生，预防或抑制脱发等的效果的毛发生长促进组合物。

    1,2-DI-substituted piperidine derivative, hair growth promoter and external composition for skin using the same
    5.
    发明授权
    1,2-DI-substituted piperidine derivative, hair growth promoter and external composition for skin using the same 有权
    1,2-DI取代的哌啶衍生物，毛发生长促进剂和使用其的皮肤外用组合物

    公开(公告)号：US6057337A

    公开(公告)日：2000-05-02

    申请号：US239960

    申请日：1999-01-29

    申请人： Koji Kobayashi ,  Hirotada Fukunishi ,  Kenichi Umishio ,  Akihiro Ishino

    发明人： Koji Kobayashi ,  Hirotada Fukunishi ,  Kenichi Umishio ,  Akihiro Ishino

    IPC分类号： C07D211/22 ,  C07D211/26 ,  C07D401/12 ,  C07D521/00 ,  A61K7/06

    CPC分类号： C07D231/12 ,  C07D211/22 ,  C07D211/26 ,  C07D233/56 ,  C07D249/08 ,  C07D401/12

    摘要： A 1,2-di-substituted piperidine derivative or a salt thereof expressed by the following Formula (I): ##STR1## wherein one of A and B is a hydrocarbon group of C.sub.1-30 expressed by R.sup.1 and the other is --(CH.sub.2)n-NR.sup.2 R.sup.3 ; Y is --CO--, --CONR.sup.5 -- or --COO--; Z is --O--, --OCO--, --OCONR.sup.6 -- or --NR.sup.6 --; R.sup.2 and R.sup.3 individually represent a hydrogen a lower alkyl, a phenyl or a benzyl group, or together represent a heterocycle having 3-7 members; --NR.sup.5 --(CH.sub.2)n-NR.sup.2 R.sup.3 and --NR.sup.6 --(CH.sub.2)n-NR.sup.2 R.sup.3 of --(Y).sub.1 --A and --Z--B may be the following Group W: ##STR2## wherein ring E is a heterocycle of 6 or 7 members including two nitrogen atoms and R.sup.2 is a hydrogen, a lower alkyl, a phenyl or a benzyl group; R.sup.4 is a hydrogen, a halogen, a lower alkyl, a lower acyl, a nitro, a cyano, a lower alkoxycarbonyl, a carbamoyl, a lower alkylcarbamoyl, a lower alkylamino, a lower acylamino, a lower alkoxy or a lower acyloxy group; each of R.sup.5 and R.sup.6 is a hydrogen, a lower alkyl, a lower acyl, a lower alkylcarbamoyl group, or a part of said ring E; l is 0 or 1; m is an integer of 2-5; and n is an integer of 0-5. The 1,2-di-substituted piperidine derivative or the salt thereof has excellent hair growth and regrowth promoting effects, which are useful for care, improvement or prevention of hair loss in mammals and, in particular, in human.

    摘要翻译： 由下式（I）表示的1,2-二取代的哌啶衍生物或其盐：其中A和B中的一个为由R1表示的C1-30的烃基，另一个为 - （CH 2）n - NR2R3; Y是-CO - ， - CONR 5 - 或-COO-; Z是-O - ， - OCO - ， - OCONR 6 - 或-NR 6 - ; R2和R3各自表示氢，低级烷基，苯基或苄基，或一起表示具有3-7个成员的杂环; - （Y）1-A和-ZB的-NR 5 - （CH 2）n -NR 2 R 3和-NR 6 - （CH 2）n -NR 2 R 3可以是以下W组：其中环E是6或7个成员的杂环，包括两个 氮原子，R 2为氢，低级烷基，苯基或苄基; R4是氢，卤素，低级烷基，低级酰基，硝基，氰基，低级烷氧基羰基，氨基甲酰基，低级烷基氨基甲酰基，低级烷基氨基，低级酰基氨基，低级烷氧基或低级酰氧基。 R5和R6各自为氢，低级烷基，低级酰基，低级烷基氨基甲酰基或所述环E的一部分; l为0或1; m为2-5的整数; n为0-5的整数。 1,2-二取代的哌啶衍生物或其盐具有优异的毛发生长和再生长促进效果，其可用于哺乳动物，特别是人的护发，改善或预防脱发。