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    • 8. 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。
    • 9. 发明授权
    • Quinazolinone derivative, hair growth promoter and external composition
for skin using the same
    • 喹唑啉酮衍生物,毛发生长促进剂和皮肤外用组合物
    • US5972929A
    • 1999-10-26
    • US137148
    • 1998-08-20
    • Koji KobayashiHirotada FukunishiTsunao Magara
    • Koji KobayashiHirotada FukunishiTsunao Magara
    • A61K8/49A61Q7/00C07D239/90A61K31/495
    • C07D239/90A61K8/4953A61Q7/00
    • A quinazolinone derivative or a salt thereof expressed by the following Formula (I); ##STR1## wherein each of A and B is R.sup.1 or --(CH.sub.2).sub.n -NR.sup.2 R.sup.3 ; wherein R.sup.1 represents a hydrocarbon group of C.sub.10-30 ; wherein R.sup.2 and R.sup.3 individually represent a hydrogen atom, a lower alkyl group, a phenyl group, or a benzyl group, or together represent a heterocyclic ring having 3-7 members; and n represents an integer of 1-5; wherein when A is R.sup.1, B is --(CH.sub.2).sub.n -NR.sup.2 R.sup.3 and when A is --(CH.sub.2).sub.n -NR.sup.2 R.sup.3, B is R.sup.1 ; and wherein R.sup.4 is selected from the group consisting of a hydrogen atom, a halogen atom, a lower alkyl group, a lower acyl group, a nitro group, a cyano group, an amino group, a lower alkoxycarbonyl group, a lower alkylamino group, a lower alkoxy group, a lower acyloxy group, a carbamoyl group, a lower alkylcarbamoyl group, and a lower acylamino group. The quinazolinone 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 humans.
    • 由下式(I)表示的喹唑啉酮衍生物或其盐; 其中A和B各自为R 1或 - (CH 2)n -NR 2 R 3; 其中R1表示C10-30的烃基; 其中R2和R3各自表示氢原子,低级烷基,苯基或苄基,或一起表示具有3-7个成员的杂环; n表示1-5的整数, 其中当A为R1时,B为 - (CH2)n-NR2R3,当A为 - (CH2)n-NR2R3时,B为R1; 并且其中R 4选自氢原子,卤素原子,低级烷基,低级酰基,硝基,氰基,氨基,低级烷氧基羰基,低级烷基氨基, 低级烷氧基,低级酰氧基,氨基甲酰基,低级烷基氨基甲酰基和低级酰氨基。 喹唑啉酮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,特别是人类的护发,改善或预防脱发。