Quinazolinone derivative, hair growth promoter and external composition
for skin using the same
    3.
    发明授权
    Quinazolinone derivative, hair growth promoter and external composition for skin using the same 有权
    喹唑啉酮衍生物,毛发生长促进剂和皮肤外用组合物

    公开(公告)号:US5972929A

    公开(公告)日:1999-10-26

    申请号:US137148

    申请日:1998-08-20

    摘要: 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.

    摘要翻译: 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。

    Alkylenediamine derivative anti-ulcer drug and antibacterial drug
    5.
    发明授权
    Alkylenediamine derivative anti-ulcer drug and antibacterial drug 失效
    烷二胺衍生物抗溃疡药和抗菌药

    公开(公告)号:US5814634A

    公开(公告)日:1998-09-29

    申请号:US842891

    申请日:1997-04-17

    CPC分类号: C07D295/13

    摘要: The invention provides a compound which has anti-ulcer effect and antibacterial activity against Helicobacter pyroli. This compound is an alkylenediamine derivative or salt which has a general formula of (1): ##STR1## wherein each of R.sub.4, R.sub.5, and R.sub.6 is hydrogen or lower alkyl; n represents an integer of 1 to 6; Y is --CH.sub.2 --, --O--, or --N(R.sub.7)--, wherein R.sub.7 is lower alkyl, aryl, carbamoyl lower alkyl, aralkyl, or a heterocyclic group having 5 to 9 carbon numbers; and, W is a group expressed by formulas 2 or 3: ##STR2## wherein (1) in formula 2: each of R.sub.1 and R.sub.2 is hydrogen, lower alkoxy, alkenyloxy, or a halogen atom; each of R.sub.3 and R.sub.3 is methyl, prenyl, or geranyl; when one of R.sub.3 and R.sub.3 is prenyl or geranyl, the other must be a methyl group; and X is oxygen or sulfur; and (2) in formula 3, R.sub.10 is a lower alkyl, and R.sub.11 is a halogen atom.

    摘要翻译: 本发明提供了一种对幽门螺杆菌具有抗溃疡作用和抗菌活性的化合物。 该化合物是具有通式(1):式1的亚烷基二胺衍生物或盐,其中R 4,R 5和R 6各自为氢或低级烷基; n表示1〜6的整数, Y是-CH 2 - , - O-或-N(R 7) - ,其中R 7是低级烷基,芳基,氨基甲酰基低级烷基,芳烷基或具有5至9个碳数的杂环基; 式3中,式(1)中,R 1和R 2各自为氢,低级烷氧基,链烯氧基或卤素原子,式中,(1)表示2或3表示的基团。 R 3和R 3各自为甲基,异戊烯基或香叶基; 当R3和R3之一是异戊烯基或香叶基时,另一个必须是甲基; X为氧或硫; 和(2)在式3中,R 10是低级烷基,R 11是卤素原子。

    N-acylpiperazine derivative, antibacterial drug and anti-ulcer drug
    6.
    发明授权
    N-acylpiperazine derivative, antibacterial drug and anti-ulcer drug 失效
    N-酰基哌嗪衍生物,抗菌药物和抗溃疡药

    公开(公告)号:US5756505A

    公开(公告)日:1998-05-26

    申请号:US625992

    申请日:1996-04-01

    CPC分类号: C07D295/185 C07D295/192

    摘要: An N-acylpiperazine derivative or a salt thereof in accordance with the present invention is represented by the following formula 1: ##STR1## wherein R.sub.1 represents a lower alkyl, hydroxy lower alkyl, lower acyl, or arylcarbonyloxy lower alkyl group; R.sub.2 represents hydrogen atom or a lower alkyl, lower alkoxy, lower alkenyl, amino, or nitro group; R.sub.3 and R.sub.4, which are identical to or different from each other, represent hydrogen atoms, halogen atoms, or cyano, nitro, lower alkyl, or lower alkoxy groups; and n represents 0 or 1. The N-acylpiperazine derivative has anti-ulcer effect or an antibacterial activity against Helicobacter pyroli to be available for prevention or cure of ulsers.

    摘要翻译: 根据本发明的N-酰基哌嗪衍生物或其盐由下式1表示:其中R 1表示低级烷基,羟基低级烷基,低级酰基或芳基羰基氧基低级烷基; R2代表氢原子或低级烷基,低级烷氧基,低级烯基,氨基或硝基; R 3和R 4彼此相同或不同,表示氢原子,卤原子或氰基,硝基,低级烷基或低级烷氧基; 并且n表示0或1. N-酰基哌嗪衍生物具有抗溃疡作用或对幽门螺杆菌具有抗菌活性,可用于预防或治愈酏剂。

    Method for producing pyrimidinylpyrazole compounds
    7.
    发明授权
    Method for producing pyrimidinylpyrazole compounds 有权
    嘧啶基吡唑化合物的制备方法

    公开(公告)号:US08592582B2

    公开(公告)日:2013-11-26

    申请号:US13520203

    申请日:2011-01-05

    IPC分类号: C07D403/04

    CPC分类号: C07D403/04

    摘要: The present invention provides a method for producing a pyrimidinylpyrazole compound (1), wherein aminoguanidine (2) or its salt is reacted with a β-diketone compound (3) to produce the pyrimidinylpyrazole compound: wherein R1 and R3 are each independently an alkyl group having 1 to 4 carbon atoms, and R2 is a hydrogen atom or an alkyl group having 1 to 4 carbon atoms. The method is excellent in the environmental compatibility and economic efficiency.

    摘要翻译: 本发明提供一种制备嘧啶基吡唑化合物(1)的方法,其中氨基胍(2)或其盐与β-二酮化合物(3)反应以产生嘧啶基吡唑化合物:其中R 1和R 3各自独立地为烷基 具有1至4个碳原子,并且R 2是氢原子或具有1至4个碳原子的烷基。 该方法在环境兼容性和经济效益上优异。

    4-alkylresorcinol derivative and external preparation for skin containing the same
    8.
    发明授权
    4-alkylresorcinol derivative and external preparation for skin containing the same 有权
    4-烷基间苯二酚衍生物和含有其的皮肤外用剂

    公开(公告)号:US08486919B2

    公开(公告)日:2013-07-16

    申请号:US13809696

    申请日:2011-06-01

    IPC分类号: A61K31/6615 C07F9/12

    摘要: The present invention provides a compound that has a high whitening effect and is excellent in safety and stability and provides an external preparation for skin comprising the same. The compound of the present invention is a 4-alkylresorcinol derivative represented by formula (1) or a salt thereof: wherein R1 is a branched or cyclic alkyl group of 3 to 7 carbon atoms or a linear alkyl group of 2 to 5 carbon atoms; R2 and R3 are each independently a hydrogen atom or a group represented by —P(O)(OR4)(OR5), and at least one of R2 and R3 is a group represented by —P(O)(OR4)(OR5); and R4 and R5 are each independently a hydrogen atom or a linear or branched alkyl group of 2 to 5 carbon atoms.

    摘要翻译: 本发明提供了具有高白化效果并且安全性和稳定性优异的化合物,并且提供了包含其的皮肤外用剂。 本发明的化合物是式(1)表示的4-烷基间苯二酚衍生物或其盐:其中,R 1为碳原子数3〜7的支链或环状烷基或碳原子数2〜5的直链烷基; R 2和R 3各自独立地为氢原子或由-P(O)(OR 4)(OR 5)表示的基团,R 2和R 3中的至少一个为-P(O)(OR 4)(OR 5) ; R 4和R 5各自独立地为氢原子或2〜5个碳原子的直链或支链烷基。

    Method For Producing Pyrimidinylpyrazole Compounds
    9.
    发明申请
    Method For Producing Pyrimidinylpyrazole Compounds 有权
    产生嘧啶基吡唑化合物的方法

    公开(公告)号:US20120283441A1

    公开(公告)日:2012-11-08

    申请号:US13520203

    申请日:2011-01-05

    IPC分类号: C07D403/04

    CPC分类号: C07D403/04

    摘要: The present invention provides a method for producing a pyrimidinylpyrazole compound (1), wherein aminoguanidine (2) or its salt is reacted with a β-diketone compound (3) to produce the pyrimidinylpyrazole compound: wherein R1 and R3 are each independently an alkyl group having 1 to 4 carbon atoms, and R2 is a hydrogen atom or an alkyl group having 1 to 4 carbon atoms. The method is excellent in the environmental compatibility and economic efficiency.

    摘要翻译: 本发明提供一种嘧啶基吡唑化合物(1)的制备方法,其中使氨基胍(2)或其盐与β-二酮化合物(3)反应以产生嘧啶基吡唑化合物:其中R 1和R 3各自独立地为烷基 具有1至4个碳原子的基团,并且R 2是氢原子或具有1至4个碳原子的烷基。 该方法在环境兼容性和经济效益上优异。