首页> 外国专利> New calcium complex of oxa-diaza-phosphaundecane derivative MS-325, useful as stabilizer for diagnostic compositions containing gadolinium complex of MS-325 and as antidote for heavy metal poisoning

New calcium complex of oxa-diaza-phosphaundecane derivative MS-325, useful as stabilizer for diagnostic compositions containing gadolinium complex of MS-325 and as antidote for heavy metal poisoning

机译:氧杂-重氮-磷十一碳烷衍生物MS-325的新型钙络合物,可用作含MS-325 ado络合物的诊断组合物的稳定剂和重金属中毒的解毒剂

摘要

The calcium complex (I) of ((4R)-4-(bis-(carboxy-.kappa.O)-methyl)-amino-kappa.N)-6,9-bis-((carbo xy.kappa.O)-methyl)-1-((4,4-diphenylcyclohexyl)oxy)-1-hydroxy-2-oxa-6, 9-diaza-1-phosphaundecan-11-yl acid-.kappa.N6,.kappa.N9,.kappa.011) 1-oxidato(6-))-hexahydrogen (MS-325) and its salts with cations are new. Independent claims are included for: (a) pharmaceutical compositions containing (I), optionally together with conventional galenic additives and/or gadolinate (3-) ((4R)-4-(bis-(carboxy-.kappa.O)-methyl)-amino-kappa.N)-6,9-bis-((carbo xy.kappa.O)-methyl)-1-((4,4-diphenylcyclohexyl)oxy)-1-hydroxy-2-oxa-6, 9-diaza-1-phosphaundecan-11-yl acid-.kappa.N6,.kappa.N9,.kappa.011) 1-oxidato(6-))-trihydrogen (Gd-MS-325); and (b) the preparation of a galenic formulation of Gd-MS-325 by: (i) reacting gadolinium oxide, MS-325, a buffer and an organic base with (I); or (ii) reacting gadolinium oxide, a salt of MS-325, Tris buffer and sodium oxide to give Gd-MS-325 then adding (I).
机译:((4R)-4-(双-(羧基-κO)-甲基)-氨基-κN)-6,9-双-((羰基xk.O )-甲基)-1-(((4,4-二苯基环己基)氧基)-1-羟基-2-氧杂-6,9-二氮杂-1-膦十一烷-11-基酸-κN6,κN9 ,kappa.011)1-氧化(6-))-六氢(MS-325)及其与阳离子的盐是新的。包括以下独立权利要求:(a)药物组合物,其包含(I),任选地与常规盖伦酸酯添加剂和/或g磺酸酯(3-)((4R)-4-(双-(羧基-κ.O)-甲基)-氨基-κN)-6,9-双-(((羰基xk.O)-甲基)-1-((4,4-二苯基环己基)氧基)-1-羟基-2-氧杂-6 ,9-二氮杂-1-磷酸金刚烷-11-基酸-κN6,κN9,κ011)1-氧化(6-))-三氢(Gd-MS-325); (b)通过以下方式制备Gd-MS-325的盖伦制剂:(i)使氧化g,MS-325,缓冲剂和有机碱与(I)反应; (ii)使氧化oxide,MS-325的盐,Tris缓冲液和氧化钠反应,得到Gd-MS-325,然后添加(I)。

著录项

  • 公开/公告号DE19964224A1

    专利类型

  • 公开/公告日2001-06-28

    原文格式PDF

  • 申请/专利权人 SCHERING AG;

    申请/专利号DE19991064224

  • 申请日1999-09-09

  • 分类号A61K49/00;

  • 国家 DE

  • 入库时间 2022-08-22 01:10:06

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