利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

200 条记录 (耗时 0.027 秒)

    Method for preparation of sulphostin and its analogue or intermediates thereof
    92.
    发明申请
    Method for preparation of sulphostin and its analogue or intermediates thereof 失效
    磺普钠及其类似物或其中间体的制备方法

    公开(公告)号：US20050020834A1

    公开(公告)日：2005-01-27

    申请号：US10498272

    申请日：2002-12-16

    申请人： Masashi Nagai ,  Hiroko Yamazaki ,  Keichirou Yamamoto ,  Masatoshi Abe

    发明人： Masashi Nagai ,  Hiroko Yamazaki ,  Keichirou Yamamoto ,  Masatoshi Abe

    IPC分类号： C07C215/30 ,  C07F9/553 ,  C07F9/568 ,  C07F9/572 ,  C07F9/59 ,  C07F9/547

    CPC分类号： C07C215/30 ,  C07B2200/07 ,  C07F9/5532 ,  C07F9/568 ,  C07F9/572 ,  C07F9/59 ,  Y02P20/55

    摘要： A method for preparing a compound represented by the following general formula (5) where, n is an integer of 0 to 3; and Y represents a protecting group for an amino group, the method including the steps of reacting a compound represented by the following general formula (3) where n and Y are as described above, with a silylating agent, and subsequently reacting it with P (═O) T3, where T represents a halogen atom, and further with ammonia. A method for preparing an optically active intermediate of sulphostin or an analogue thereof, which is an optically active amine salt of an optically active compound represented by the following general formula (8) where n is an integer of 0 to 3; Y represents a protecting group for the amino group; and each configuration at C* and P* may be the same or different and indicates S or R, the method including reacting a compound represented by the following general formula (7) where n and Y are as described above; and the configuration of C* indicates either of S or R, with an optically active amine, and resolving the formed diastereomeric salt by fractional crystallization.

    摘要翻译： 一种制备由以下通式（5）表示的化合物的方法，其中n为0-3的整数; Y表示氨基的保护基，该方法包括使下述通式（3）表示的化合物（其中n和Y如上所述）与甲硅烷基化剂反应，然后使其与P（ = O）T3，其中T表示卤素原子，并且还含有氨。 一种制备磺普钠或其类似物的光学活性中间体的方法，其为由以下通式（8）表示的光学活性化合物的光学活性胺盐，其中n为0-3的整数; Y表示氨基的保护基; 并且C *和P *的每个构型可以相同或不同，表示S或R，该方法包括使由以下通式（7）表示的化合物，其中n和Y如上所述; 并且C *的构型表示S或R中的任一个与光学活性胺，并且通过分级结晶拆分形成的非对映体盐。

    N-oxides and derivatives of chlorambucil for treating hypoxic tumor cells
    97.
    发明授权
    N-oxides and derivatives of chlorambucil for treating hypoxic tumor cells 失效
    用于治疗缺氧性肿瘤细胞的N-氧化物和苯丁酸氮芥的衍生物

    公开(公告)号：US5602278A

    公开(公告)日：1997-02-11

    申请号：US326327

    申请日：1994-10-20

    申请人： Lynn Kirkpatrick

    发明人： Lynn Kirkpatrick

    IPC分类号： C07C239/18 ,  C07F9/6584 ,  C07C229/28 ,  C07F9/547

    CPC分类号： C07F9/65846 ,  C07C239/18

    摘要： This invention relates to compounds which are N-oxides and derivatives of chlorambucil and which, under certain conditions, (1) are stable in hypoxic and oxic cells, (2) are toxic in cells having varying degrees of hypoxia, and (3) show little toxicity to oxic cells. These compounds have the general formula set out below and are used to treat tumorous cells: ##STR1## wherein R is an alkyl, aryl, or derivatives thereof, such as CH.sub.3 OCH.sub.2 CH.sub.2 --; CH.sub.3 CH.sub.2 OCH.sub.2 CH.sub.2 --; C.sub.6 H.sub.5 OCH.sub.2 CH.sub.2 --; C.sub.6 H.sub.5 CH.sub.2 --; CH.sub.3 (CH.sub.2).sub.3 OCH.sub.2 CH.sub.2 Cl; or any one of the following: ##STR2##

    摘要翻译： 本发明涉及N-氧化物和苯丁酸氮芥衍生物的化合物，并且在某些条件下，（1）在缺氧和氧细胞中是稳定的，（2）在具有不同程度的缺氧的细胞中是有毒的，和（3）显示 对氧细胞毒性小。 这些化合物具有下列通式，用于治疗肿瘤细胞：其中R为烷基，芳基或其衍生物，例如CH 3 OCH 2 CH 2 - ; CH3CH2OCH2CH2-; C6H5OCH2CH2-; C6H5CH2-; CH3（CH2）3OCH2CH2Cl; 或以下任何一种：

    Crop-protection formulations
    99.
    发明授权
    Crop-protection formulations 失效
    作物保护制剂

    公开(公告)号：US5512534A

    公开(公告)日：1996-04-30

    申请号：US131289

    申请日：1993-10-04

    申请人： Gerhard Frisch ,  Thomas Maier

    发明人： Gerhard Frisch ,  Thomas Maier

    IPC分类号： A01N25/30 ,  A01N25/04 ,  A01N57/10 ,  C07F9/09 ,  C07F9/547 ,  C08G65/327 ,  C08G65/332 ,  C08G65/333 ,  C09K19/40 ,  A01N57/12

    CPC分类号： C09K19/404 ,  A01N25/04 ,  C07F9/091 ,  C08G65/327 ,  C08G65/3322 ,  C08G65/33303

    摘要： The present invention relates to compounds of the formula I ##STR1## in which R.sup.1 is hydrogen,a substituted or unsubstituted aliphatic radicalhaving up to 30 carbon atoms,a substituted or unsubstituted alicyclic radicalhaving up to 30 carbon atoms,a substituted or unsubstituted aromatic radicalhaving up to 24 carbon atoms ora substituted or unsubstituted heteroaromaticradical having up to 20 carbon atoms,R.sup.2 is an amino acid,x'=0-80,y'=0-50,x"=0-80 andy"=0-50,with at least one of the variables x', y', x" and y" being greater than 0. The compounds of the formula I are prepared by reacting the corresponding dihydrogen phosphate with the respective amino acid or salt thereof. The compounds according to the invention can be employed, for example, as surfactants for emulsifying organic solvents in water.

    摘要翻译： 本发明涉及式Ⅰ的化合物，其中R 1为氢，具有至多30个碳原子的取代或未取代的脂族基，取代或未取代的具有至多30个碳原子的脂环基，取代或未取代的 具有至多24个碳原子的未取代芳族基团或具有至多20个碳原子的取代或未取代的杂芳族基团，R2是氨基酸，x'= 0-80，y'= 0-50，x“= 0-80和 y“= 0-50，其中变量x'，y'，x”和y“中的至少一个大于0.式I化合物通过使相应的磷酸二氢酯与相应的 氨基酸或其盐。 根据本发明的化合物可以用作例如在水中乳化有机溶剂的表面活性剂。

    Substituted piperazine-2-carboxylic acids and derivatives thereof
    100.
    发明授权
    Substituted piperazine-2-carboxylic acids and derivatives thereof 失效
    取代的哌嗪-2-羧酸及其衍生物

    公开(公告)号：US5399693A

    公开(公告)日：1995-03-21

    申请号：US469819

    申请日：1990-01-23

    申请人： Jeffrey C. Watkins ,  Arwel W. Jones

    发明人： Jeffrey C. Watkins ,  Arwel W. Jones

    IPC分类号： A61K31/495 ,  A61K31/505 ,  A61K31/66 ,  A61K31/675 ,  A61K31/69 ,  A61P25/00 ,  A61P25/08 ,  C07D241/04 ,  C07D241/44 ,  C07D403/06 ,  C07D413/06 ,  C07F5/02 ,  C07F9/547 ,  C07F9/6509 ,  C07F5/04

    CPC分类号： C07D403/06 ,  C07D241/04 ,  C07F9/650958

    摘要： Compounds of the general formula ##STR1## wherein X is a C.sub.1 -C.sub.6, straight chain saturated or unsaturated hydrocarbyl group, the group R.sup.4 and the group Y are situated in any position in this chain and wherein at least one of the hydrogen atoms in X can be a heavy isotope of hydrogen;R.sup.4 is hydrogen or an alkyl, alkoxy, hydroxy, aryl, aryloxy, aralkyl, aralkoxy, aralkylamino, or morpholino group wherein the alkyl or aryl part of any one of said groups may be substituted by one or more halogeno groups; or R.sup.4, together with at least one carbon atom of the group X, forms a carbocyclic or heterocyclic ring of 5 to 6 ring atoms;Y is an acidic or related group giving rise to one or more electronegative sites in the group; or R.sup.4 --X--Y represents a carboxylic acyl group;R is hydrogen or an alkyl, haloalkyl, aryl, haloaryl, aralkyl or haloaralkyl;R.sup.1 is hydrogen or an alkyl, haloalkyl, aryl, haloaryl, aralkyl or haloaralkyl group;R.sup.2 R.sup.3 and R.sup.5 which may be the same or different is each hydrogen or an alkyl, hydroxy, alkoxy, carboxy, alkyloxycarbonyl, halo, aryl, haloaryl or aryloxycarbonyl group; orR.sup.2 and R.sup.3 together with the carbon atoms to which they are attached form a ring system orR.sup.3 and R.sup.4 together and/or R.sup.3 and X together form one or more than one ring systems, or a physiologically acceptable salt thereof have activity in the central nervous system.

    摘要翻译： 通式为其中X为C 1 -C 6直链饱和或不饱和烃基的化合物，基团R 4和基团Y位于该链中的任何位置，并且其中至少一个氢原子在 X可以是氢的重质同位素; R4是氢或烷基，烷氧基，羟基，芳基，芳氧基，芳烷基，芳烷氧基，芳烷基氨基或吗啉代基，其中任何一个所述基团的烷基或芳基部分可被一个或多个卤代基取代; 或R 4与X基团的至少一个碳原子一起形成5至6个环原子的碳环或杂环; Y是酸性或相关基团，在该组中引起一个或多个电负性位点; 或R 4 -X-Y表示羧酰基; R是氢或烷基，卤代烷基，芳基，卤代芳基，芳烷基或卤代烷基; R 1是氢或烷基，卤代烷基，芳基，卤代芳基，芳烷基或卤代烷基; R 2 R 3和R 5可以相同或不同，各自为氢或烷基，羟基，烷氧基，羧基，烷氧基羰基，卤素，芳基，卤代芳基或芳氧基羰基; 或R 2和R 3与它们所连接的碳原子一起形成环系，或者R 3和R 4一起和/或R 3和X一起形成一个或多于一个环体系，或其生理上可接受的盐在中心具有活性 神经系统。