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    • 5. 发明授权
    • 1,2-DI-substituted piperidine derivative, hair growth promoter and
external composition for skin using the same
    • 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
    • US6057337A
    • 2000-05-02
    • US239960
    • 1999-01-29
    • Koji KobayashiHirotada FukunishiKenichi UmishioAkihiro Ishino
    • Koji KobayashiHirotada FukunishiKenichi UmishioAkihiro Ishino
    • C07D211/22C07D211/26C07D401/12C07D521/00A61K7/06
    • C07D231/12C07D211/22C07D211/26C07D233/56C07D249/08C07D401/12
    • 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.
    • 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。
    • 6. 发明授权
    • Benzimidazole derivative, hair growth promoter and external composition for skin using the same
    • 苯并咪唑衍生物,毛发生长促进剂和皮肤外用组合物
    • US06204264B1
    • 2001-03-20
    • US09398200
    • 1999-09-17
    • Koji KobayashiHirotada FukunishiKenichi UmishioMasahiro Tajima
    • Koji KobayashiHirotada FukunishiKenichi UmishioMasahiro Tajima
    • A61R31535
    • C07D235/24A61K8/4946A61Q7/00C07D235/08
    • A benzimidazole derivative or a salt thereof expressed by the following Formula (I): wherein one of A and B is a hydrocarbon group of C10-30 expressed by R1 and the other is —(CH2)n—NR2R3; R2 and R3 individually represent H, lower alkyl, phenyl or benzyl, or —NR2R3 may be a heterocycle having 3-7 members, or —CONR5—(CH2)n—NR2R3 may be the following Group (W): wherein R2 is H, lower alkyl, phenyl or benzyl and ring E is a heterocycle of 6 or 7 members; R4 is selected from the group consisting of H, halogen, cyano, trifluoromethyl, lower alkyl and etc.; R5 is H, lower alkyl, lower acyl or lower alkylcarbamoyl; m is 0 or 1; and n is an integer of 0-5. The benzimidazole 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.
    • 由下式(I)表示的苯并咪唑衍生物或其盐:其中A和B中的一个是由R 1表示的C 10-30的烃基,而另一个是 - (CH 2)n -NR 2 R 3; R 2和R 3各自表示H,低级烷基,苯基或苄基,或-NR 2 R 3可以是具有3-7个成员的杂环,或-CONR 5 - (CH 2)n -NR 2 R 3可以是下列基团(W):其中R 2是H 苯基或苄基,环E是6或7个成员的杂环; R4选自H,卤素,氰基,三氟甲基,低级烷基等; R5是H,低级烷基,低级酰基或低级烷基氨基甲酰基; m为0或1; n为0-5的整数。 苯并咪唑衍生物或其盐具有优异的毛发生长和再生长促进作用,其可用于哺乳动物,特别是人的护发,改善或预防脱发。