4-hydroxy-4-phenylpiperidine derivatives and pharmaceuticals containing the same
    4.
    发明授权
    4-hydroxy-4-phenylpiperidine derivatives and pharmaceuticals containing the same 失效
    4-羟基-4-苯基哌啶衍生物和含有它们的药物

    公开(公告)号:US06362203B1

    公开(公告)日:2002-03-26

    申请号:US09698041

    申请日:2000-10-30

    IPC分类号: C07D21152

    CPC分类号: C07D211/52

    摘要: Described is a 4-hydroxy-4-phenylpiperidine derivative represented by the following formula (1): [wherein, R1 and R2 are the same or different and each independently represents a hydrogen atom, a lower alkyl, or the like, R3 represents a hydrogen atom or a group —(CR4R5)n—Y (in which, R4 and R5 each represents a hydrogen atom or a lower alkyl group, Y represents a group —COOR6, —CONR7R8, —OR9 or —OCOR10 (in which R6, R9 and R10 each independently represents a hydrogen atom, a lower alkyl group, or the like, R7 and R8 are the same or different and each independently represents a hydrogen atom, a lower alkyl group, or the like), and n stands for 1 to 6)], or salt thereof. The compound exhibits excellent peripheral analgesic action.

    摘要翻译: 描述了由下式(1)表示的4-羟基-4-苯基哌啶衍生物:[其中,R 1和R 2相同或不同,各自独立地表示氢原子,低级烷基等,R 3表示 氢原子或基团 - (CR 4 R 5)n Y(其中,R 4和R 5各自表示氢原子或低级烷基,Y表示-COOR 6,-CONR 7 R 8,-OR 9或-OCOR 10(其中R 6,R 9和 R 10各自独立地表示氢原子,低级烷基等,R 7和R 8相同或不同,各自独立地表示氢原子,低级烷基等),n表示1〜6 )]或其盐。该化合物表现出优异的外周镇痛作用。

    Platinum (IV) complex and pharmaceutical composition comprising the same
    5.
    发明授权
    Platinum (IV) complex and pharmaceutical composition comprising the same 失效
    铂(IV)复合物和包含其的药物组合物

    公开(公告)号:US5902826A

    公开(公告)日:1999-05-11

    申请号:US997061

    申请日:1997-12-23

    IPC分类号: A61K31/55 C07F15/00 A61K31/28

    CPC分类号: C07F15/0093

    摘要: A diamine-platinum (IV) complex represented by the following formula (1): ##STR1## wherein R.sup.1 and R.sup.2 together represent R.sup.5 O--CH(CH.sub.2 NH.sub.2).sub.2 (R.sup.5 represents hydrogen, acetyl, trifluoroacetyl, benzoyl, cycloalkylcarbonyl or methanesulfonyl) or a C.sub.5-8 1,2-cycloalkanediamine; R.sup.3 and R.sup.4 each represents hydrogen or R.sup.6 CO-- (R.sup.6 represents alkyl, halogenoalkyl, cycloalkyl, aryl or aralkyl); and two X's together represent a malonic acid residue or glycolic acid residue which may have a substituent capable of coordinating to the platinum in formula (1) by an O,O-coordination or an N-acylamino acid residue coordinating to the platinum in formula (1) by an O,N-coordination; and a pharmaceutical composition comprising as an active ingredient the above-described diamine-platinum (IV) complex.

    摘要翻译: 由下式(1)表示的二胺 - 铂(IV)络合物:其中R1和R2一起表示R5O-CH(CH2NH2)2(R5代表氢,乙酰基,三氟乙酰基,苯甲酰基,环烷基羰基或甲磺酰基)或C5-8 1,2-环烷二胺; R3和R4各自表示氢或R6CO-(R6表示烷基,卤代烷基,环烷基,芳基或芳烷基); 两个X一起代表丙二酸残基或乙醇酸残基,其可以具有能够通过与式(1)中的铂配位的O,O-配位体或N-酰基氨基酸残基与式(1)中的铂配位的取代基, 1)通过O,N-配位; 以及包含上述二胺 - 铂(IV)络合物作为活性成分的药物组合物。

    Dithiolylidene acetamide derivatives
    8.
    发明授权
    Dithiolylidene acetamide derivatives 失效
    二硫代亚乙酰胺衍生物

    公开(公告)号:US5962509A

    公开(公告)日:1999-10-05

    申请号:US169989

    申请日:1998-10-13

    CPC分类号: C07D339/06

    摘要: Disclosed are dithiolylidene acetamide derivatives represented by the following formula: ##STR1## wherein R.sup.1 and R.sup.2 may be the same or different and each independently represent a hydrogen atom or an alkyl group, or salts thereof; and pharmaceuticals containing them as effective ingredients. The dithiolylidene acetamide derivatives and their salts show AGE formation inhibitory action and are useful as preventives and therapeutics for diabetic complications.

    摘要翻译: 公开了由下式表示的二亚噻吩基乙酰胺衍生物:其中R1和R2可以相同或不同,各自独立地表示氢原子或烷基,或其盐; 和含有它们作为有效成分的药物。 二硫代亚乙酰胺衍生物及其盐显示AGE形成抑制作用,可用作糖尿病并发症的预防药物和治疗剂。