利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

27 条记录 (耗时 0.037 秒)

    Process for the preparation of iopamidol and the new intermediates therein
    9.
    发明授权
    Process for the preparation of iopamidol and the new intermediates therein 有权
    碘帕醇及其中间体的制备方法

    公开(公告)号：US07368101B2

    公开(公告)日：2008-05-06

    申请号：US11316559

    申请日：2005-12-21

    申请人： Pier Lucio Anelli ,  Marino Brocchetta ,  Giovanna Lux ,  Enrico Cappelletti

    发明人： Pier Lucio Anelli ,  Marino Brocchetta ,  Giovanna Lux ,  Enrico Cappelletti

    IPC分类号： A61K49/04 ,  C07C233/00 ,  C07D407/00

    CPC分类号： C07C231/02 ,  C07C237/46

    摘要： A process for the preparation of (S)-N,N′-bis[2-hydroxy-1-(hydroxymethyl)ethyl]-5-[(2-hydroxy-1-oxo-propyl)amino]-2,4,6-triiodo-1,3-benzendicarboxamide (iopamidol) starting from 5-amino-N,N′-bis[2-hydroxy-1-(hydroxymethyl)ethyl]-2,4,6-triiodo-1,3-benzenedicarboxamide (II) which process comprises a) reacting the compound of formula (II) with a suitable protecting agent, to give a compound of formula (III) wherein R is a group of formula A or B wherein R1 is a hydrogen atom, a C1÷C4 straight or branched alkoxy group, R2 is hydrogen, a C1÷C4 straight or branched alkoy group and R3 ?is a C1÷C4 straight or branched alkyl group, a trifuoromethyl or a trichloromethyl group; b) acylating the amino group in position 5 of the intermediate compound of formula (III), by reaction with a (S)-2-(acetyloxy)propanoyl chloride to give a compound of formula (IV) wherein R is as defined above; and c) removing all the acyl groups present in the compound of formula (IV) under basic conditions, with prior cleavage of the cyclic protections of the hydroxy groups in the carboxamido substituents under acidic conditions, when R is a group of formula A carboxamido hydroxy groups under acidic conditions. The invention also refers to the new intermediates of formula (III) and (IV) wherein —R is a group A.

    摘要翻译： 制备（S）-N，N'-双[2-羟基-1-（羟甲基）乙基] -5 - [（2-羟基-1-氧代 - 丙基）氨基] -2,4， 5-氨基-N，N'-双[2-羟基-1-（羟甲基）乙基] -2,4,6-三碘-1,3-苯二甲酰胺的6-三碘-1,3-苯二甲酰胺（碘帕醇） （II）所述方法包括a）使式（II）化合物与合适的保护剂反应，得到其中R为式A或B的基团的式（III）化合物，其中R 1 >是氢原子，C 1或C 4直链或支链烷氧基，R 2是氢，C 1 直线或支链烷基，R 3？是C / C 直链或支链烷基，三氟甲基或三氯甲基; b）通过与（S）-2-（乙酰氧基）丙酰氯反应，酰化式（III）中间体化合物的第5位的氨基，得到其中R如上定义的式（Ⅳ）化合物; 和c）在碱性条件下除去存在于式（Ⅳ）化合物中的所有酰基，在R是式A的基团时，先前在酸性条件下，在甲酰氨基取代基中羟基的环保保护被切割。 在酸性条件下。 本发明还涉及式（III）和（IV）的新中间体，其中-R是基团A.

    Gastrin Releasing Peptide Compounds
    10.
    发明申请
    Gastrin Releasing Peptide Compounds 审中-公开
    胃泌素释放肽化合物

    公开(公告)号：US20080008649A1

    公开(公告)日：2008-01-10

    申请号：US11751337

    申请日：2007-05-21

    申请人： Enrico Cappelletti ,  Luciano Lattuada ,  Karen Linder ,  Edmund Marinelli ,  Palaniappa Nanjappan ,  Adrian Nunn ,  Natarajan Raju ,  Kondareddiar Ramalingam ,  Rolf Swenson ,  Michael Tweedle ,  Mary Maddalena

    发明人： Enrico Cappelletti ,  Luciano Lattuada ,  Karen Linder ,  Edmund Marinelli ,  Palaniappa Nanjappan ,  Adrian Nunn ,  Natarajan Raju ,  Kondareddiar Ramalingam ,  Rolf Swenson ,  Michael Tweedle ,  Mary Maddalena

    IPC分类号： A61K51/08 ,  A61P35/04

    CPC分类号： C07K14/57572 ,  A61K49/085 ,  A61K49/122 ,  A61K49/14 ,  A61K51/088

    摘要： New and improved compounds for use in diagnostic imaging or therapy having the formula M-N—O—P-G, wherein M is a metal chelator having the structure: wherein R1-R5 and FG are as defined herein (in the form complexed with a metal radionuclide or not), N—O—P is the linker containing at least one non-alpha amino acid with a cyclic group, at least one substituted bile acid or at least one non-alpha amino acid, and G is the GRP receptor targeting peptide. In the preferred embodiment, M is an Aazta metal chelator or a derivative thereof. Methods for imaging a patient and/or providing radiotherapy or phototherapy to a patient using the compounds of the invention are also provided. Methods and kits for preparing a diagnostic imaging agent from the compound is further provided. Methods and kits for preparing a radiotherapeutic agent are further provided. Novel methods of treating prostate tumors or of delaying the progression of prostate tumors are also provided, including, methods of treating bone or soft tissue metastases of prostate cancer, methods for treating hormone sensitive and hormone refractory prostate cancer, methods for delaying the progression of hormone sensitive prostate cancer, for facilitating combination therapy in patients with hormone sensitive prostate cancer and for decreasing aberrant vascular permeability in patients with hormone sensitive prostate cancer.

    摘要翻译： 用于具有式MNOPG的诊断成像或治疗的新的和改进的化合物，其中M是具有以下结构的金属螯合剂：其中R 1 -R 5和FG如本文所定义（以与金属放射性核素复合的形式） NOP是含有至少一个具有环状基团，至少一个取代的胆汁酸或至少一个非α氨基酸的非α氨基酸的接头，G是GRP受体靶向肽。 在优选的实施方案中，M是Aazta金属螯合剂或其衍生物。 还提供了使用本发明的化合物对患者成像和/或向患者提供放射治疗或光疗的方法。 还提供了用于从该化合物制备诊断显像剂的方法和试剂盒。 还提供了用于制备放射治疗剂的方法和试剂盒。 还提供了治疗前列腺肿瘤或延缓前列腺肿瘤进展的新方法，包括治疗前列腺癌骨或软组织转移的方法，治疗激素敏感性和激素难治性前列腺癌的方法，延迟激素进展的方法 敏感前列腺癌，用于促进激素敏感性前列腺癌患者的联合治疗，并减少激素敏感性前列腺癌患者异常血管通透性。