会员体验
专利管家(专利管理)
工作空间(专利管理)
风险监控(情报监控)
数据分析(专利分析)
侵权分析(诉讼无效)
联系我们
交流群
官方交流:
QQ群: 891211   
微信请扫码    >>>
现在联系顾问~
热词
    • 3. 发明申请
    • NOVEL DIAGNOSTIC AGENTS FOR THE NON-INVASIVE IN VIVO IMAGING OF AMINOPEPTIDASE N (APN/CD13)
    • 用于非侵入性氨基转移酶N(APN / CD13)VIVO成像的新型诊断试剂
    • US20120213702A1
    • 2012-08-23
    • US13393440
    • 2010-08-31
    • Christoph BremerCarsten Höltke
    • Christoph BremerCarsten Höltke
    • A61K51/04C07D207/16C07F15/02C07F3/00C07F13/00A61K49/00A61K49/10A61K31/40A61P35/00A61P29/00A61P19/02A61P35/02A61P13/12A61P9/00G01N33/53C07D403/14
    • A61K51/0446A61K47/545A61K49/0032A61K49/0041A61K49/0043A61K49/0052A61K49/101
    • The present invention relates to aminopeptidase N (APN) inhibitor conjugates of formula I wherein W is a —CO— or an —SO2— group and at least one of R1 or R2 represents (OCH2—CH2)n-X, where n is an integer of 1 to 100 and X represents H or a detectable label or a therapeutic, and the other represents an alkoxy group or OH, and wherein R3, R3′ and R3″ is independently selected from an alkoxy group or (OCH2—CH2)n-X, where n is an integer of 1 to 100 and X represents H or a detectable label or a therapeutic, and R4 is selected from the group comprising: wherein R is an alkyl group. Furthermore, the present invention relates to a diagnostic and/or pharmaceutical composition comprising the conjugate of the invention. The present invention also relates to the conjugate or composition of the invention for use in the diagnosis or treatment of APN-associated diseases like for example angiogenesis in cancer, rheumatoid arthritis, leukemia and diabetic nephropathy, as well as to the use of the conjugate or of the composition of the invention in the diagnosis or treatment of angiogenesis in cancer, rheumatoid arthritis, leukemia and diabetic nephropathy. In a further aspect, the present invention relates to kits comprising the conjugate or composition of the invention. The conjugate or pharmaceutical/diagnostic composition of the invention can also be used in in vivo or in vitro imaging studies of aminopeptidase N.
    • 本发明涉及式I的氨基肽酶N(APN)抑制剂缀合物,其中W是-CO-或-SO 2 - 基,R 1或R 2中的至少一个表示(OCH 2 -CH 2)n X,其中n是 1〜100,X表示H或可检测标记或治疗剂,另一个表示烷氧基或OH,并且其中R3,R3'和R3“独立地选自烷氧基或(OCH2-CH2)nX,其中 n为1〜100的整数,X为H或可检测标记或治疗剂,R4选自:其中R为烷基。 此外,本发明涉及包含本发明缀合物的诊断和/或药物组合物。 本发明还涉及用于诊断或治疗APN相关疾病的本发明的缀合物或组合物,例如癌症,类风湿性关节炎,白血病和糖尿病性肾病中的血管生成,以及该缀合物或 的本发明的组合物在癌症,类风湿性关节炎,白血病和糖尿病肾病中的血管发生的诊断或治疗中的用途。 在另一方面,本发明涉及包含本发明的缀合物或组合物的试剂盒。 本发明的缀合物或药物/诊断组合物也可用于氨基肽酶N的体内或体外成像研究。