利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

19 条记录 (耗时 0.025 秒)

    Adducts of macrocyclic chelants
    6.
    发明授权
    Adducts of macrocyclic chelants 失效
    大环螯合剂的加合物

    公开(公告)号：US5554748A

    公开(公告)日：1996-09-10

    申请号：US175989

    申请日：1993-12-30

    申请人： Paul F. Sieving ,  Alan D. Watson

    发明人： Paul F. Sieving ,  Alan D. Watson

    IPC分类号： A61K47/48 ,  A61K49/08 ,  A61K49/12 ,  A61K51/06 ,  C08G69/48 ,  C07D255/02 ,  C07D257/02 ,  C07D273/00

    CPC分类号： A61K49/143 ,  A61K47/48076 ,  A61K47/48315 ,  A61K49/085 ,  A61K49/106 ,  A61K49/128 ,  A61K49/146 ,  A61K51/065 ,  C08G69/48

    摘要： There are provided polychelants and their metal chelates which are useful in diagnostic imaging and in radiotherapy and which comprise a plurality of macrocyclic chelant moieties, e.g. DOTA residues, conjugated to a polyamine backbone molecule, e.g. polylysine. To produce a site-specific polychelate, one or more of the macrocyclic chelant carrying backbone molecules may be conjugated to a site-directed macromolecule, e.g. a protein. For example, adducts of a macrocyclic chelant can be formed by the process of (a) dispersing a carboxylic macrocyclic chelant in a polar, anhydrous solvent, (b) adding a base with a pKa sufficient to remove all carboxyl protons to create an amine salt of the chelant soluble in the solvent, (c) chilling the reaction mixture to between about 5.degree. C. and 55.degree. C. above the freezing point of the solvent, and (d) adding substantial equimolar amount of chilled alkylhaloformate under anhydrous conditions so as to form a slurry containing the mixture carboxycarbonic anhydride of the chelant.

    摘要翻译： 提供了可用于诊断成像和放射治疗中的多层螯合物及其金属螯合物，其包含多个大环螯合剂部分，例如， 与多胺主链分子缀合的DOTA残基。 聚赖氨酸 为了产生位点特异性聚合物，一种或多种携带骨架分子的大环螯合剂可以与位点定向的大分子结合，例如 蛋白质 例如，大环螯合剂的加合物可以通过以下方法形成：（a）将羧基大环螯合剂分散在极性无水溶剂中，（b）加入足以除去所有羧基质子以产生胺盐的pKa碱 的螯合剂溶于溶剂中，（c）将反应混合物冷却至高于溶剂凝固点的约5℃至55℃，和（d）在无水条件下加入基本上等摩尔量的冷却的卤代烷基卤化物， 以形成含有螯合剂的羧基碳酸酐混合物的浆料。

    Dichelants
    8.
    发明授权
    Dichelants 失效

    公开(公告)号：US5972307A

    公开(公告)日：1999-10-26

    申请号：US898376

    申请日：1997-07-22

    申请人： Joan Carvalho ,  Alan D. Watson ,  Jere D. Fellmann ,  Michael Koo

    发明人： Joan Carvalho ,  Alan D. Watson ,  Jere D. Fellmann ,  Michael Koo

    IPC分类号： A61K49/00 ,  A61K49/06 ,  C07C237/06 ,  C07C237/10 ,  C07C237/12 ,  C07D241/06 ,  C07D257/02 ,  C07D295/185 ,  C07D403/14 ,  C07F9/6524 ,  C07F19/00 ,  A61K51/04 ,  A61B5/055 ,  C07D225/00 ,  C07F5/00

    CPC分类号： C07D241/06 ,  A61K49/0002 ,  A61K49/06 ,  C07C237/06 ,  C07C237/10 ,  C07C237/12 ,  C07D257/02 ,  C07D295/185 ,  C07D403/14 ,  C07F19/005 ,  C07F9/6524

    摘要： This invention relates to dichelants, in particular compounds having two macrocyclic chelant groups linked by a bridge containing an ester or amide bond, especially compounds of formula Vb ##STR1## (wherein each X which may be the same or different is NZ, O or S, at least two Xs being NZ;each Z is a group R.sup.1 or a group CR.sup.1.sub.2 Y, at least one Z, and preferably 2 or 3 Zs, on each macrocyclic ring being a group CR.sup.1.sub.2 Y;each Y is a group CO.sub.2 H, PO.sub.3 H, SO.sub.3 H, CONR.sup.1.sub.2, CON(OR.sup.1)R.sup.1, CNS or CONR.sup.1 NR.sup.1.sub.2, preferably COOH;m is 0 or 1 or 2, preferably 1; each n is 2 or 3, preferably 2; q is 1 or 2, preferably 1;each R.sup.1 which may be the same or different is a hydrogen atom or an alkyl group optionally substituted by one or more hydroxy and/or alkoxy groups;and D is a bridging group having a molecular weight of less than 1000, preferably less than 500, joining two macrocyclic rings via at least one amide or ester bond) and salts and metal chelates thereof.

    摘要翻译： 本发明涉及双耳，特别是具有通过含有酯或酰胺键的桥连接的两个大环螯合剂基团的化合物，特别是式Vb化合物（其中每个X可以相同或不同，为至少NZ，O或S，至少 两个X为NZ;每个Z为基团R 1或基团CR 12 Y，至少一个Z，优选2或3个Z，每个大环上为基团CR 12Y;每个Y为CO 2 H，PO 3 H，SO 3 H，CONR 12， CON（OR1）R1，CNS或CONR1NR12，优选COOH; m为0或1或2，优选1;每个n为2或3，优选2; q为1或2，优选1;每个R 1可以相同 或不同的是氢原子或任选被一个或多个羟基和/或烷氧基取代的烷基; D是分子量小于1000，优选小于500的桥连基团，至少通过至少连接两个大环 一个酰胺或酯键）及其盐和金属螯合物。

    Macrocyclic polyaza dichelates linked through ring nitrogens via an amide or ester functionality
    9.
    发明授权
    Macrocyclic polyaza dichelates linked through ring nitrogens via an amide or ester functionality 失效
    通过环氮化合物通过酰胺或酯官能团连接的大环多氮化合物

    公开(公告)号：US5650133A

    公开(公告)日：1997-07-22

    申请号：US226760

    申请日：1994-04-12

    申请人： Joan Carvalho ,  Alan D. Watson ,  Jere D. Fellmann ,  Michael David Koo

    发明人： Joan Carvalho ,  Alan D. Watson ,  Jere D. Fellmann ,  Michael David Koo

    IPC分类号： A61K49/00 ,  A61K49/06 ,  C07D257/02 ,  C07D403/14 ,  C07F9/6524 ,  A61K51/04 ,  A61B5/055 ,  C07D225/00 ,  C07F5/00

    CPC分类号： C07D403/14 ,  A61K49/0002 ,  A61K49/06 ,  C07D257/02 ,  C07F9/6524

    摘要： This invention relates to dichelants, in particular compounds having two macrocyclic chelant groups linked by a bridge containing an ester or amide bond, especially compounds of formula Vb ##STR1## (wherein each X which may be the same or different is NZ, O or S, at least two Xs being NZ;each Z is a group R.sup.1 or a group CR.sup.1.sub.2 Y, at least one Z, and preferably 2 or 3 Zs, on each macrocyclic ring being a group CR.sup.1.sub.2 Y;each Y is a group CO.sub.2 H, PO.sub.3 H, SO.sub.3 H, CONR.sup.1.sub.2, CON(OR.sup.1)R.sup.1, CNS or CONR.sup.1 NR.sup.1.sub.2, preferably COOH;m is 0 or 1 or 2, preferably 1; each n is 2 or 3, preferably 2; q is 1 or 2, preferably 1;each R.sup.1 which may be the same or different is a hydrogen atom or an alkyl group optionally substituted by one or more hydroxy and/or alkoxy groups;and D is a bridging group having a molecular weight of less than 1000, preferably less than 500, joining two macrocyclic rings via at least one amide or ester bond) and salts and metal chelates thereof.

    摘要翻译： 本发明涉及双耳，特别是具有通过含有酯或酰胺键的桥连接的两个大环螯合剂基团的化合物，特别是具有式Vb的化合物（其中每个可以相同或不同的X可以是NZ，O或S ，至少两个X为NZ;每个Z为基团R 1或基团CR 12 Y，至少一个Z，优选2或3个Z，每个大环上为基团CR 12Y;每个Y为CO 2 H，PO 3 H，SO 3 H ，CONR12，CON（OR1）R1，CNS或CONR1NR12，优选COOH; m为0或1或2，优选1;每个n为2或3，优选2; q为1或2，优选1; 相同或不同的是氢原子或任选被一个或多个羟基和/或烷氧基取代的烷基; D是分子量小于1000，优选小于500的桥连基，连接两个大环 通过至少一个酰胺或酯键）及其盐和金属螯合物。