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    • 15. 发明授权
    • Vitronectin receptor antagonist pharmaceuticals
    • Vitronectin受体拮抗剂药物
    • US07018611B2
    • 2006-03-28
    • US10281015
    • 2002-10-26
    • Thomas D. HarrisJohn A. BarrettAlan P. Carpenter, Jr.Milind Rajopadhye
    • Thomas D. HarrisJohn A. BarrettAlan P. Carpenter, Jr.Milind Rajopadhye
    • A61K51/00A61M36/14
    • A61K49/0002A61K49/04A61K49/085A61K49/10A61K49/223A61K51/0455A61K51/0459A61K51/0497C07D401/12C07D401/14
    • The present invention describes novel compounds of the formula: (Q)d—Ln—Ch, useful for the diagnosis and treatment of cancer, methods of imaging tumors in a patient, and methods of treating cancer in a patient. The present invention also provides novel compounds useful for monitoring therapeutic angiogenesis treatment and destruction of new angiogenic vasculature. The present invention further provides novel compounds useful for imaging atherosclerosis, restenosis, cardiac ischemia, and myocardial reperfusion injury. The present invention still further provides novel compounds useful for the treatment of rheumatoid arthritis. The pharmaceuticals are comprised of a targeting moiety that binds to a receptor that is upregulated during angiogenesis, an optional linking group, and a therapeutically effective radioisotope or diagnostically effective imageable moiety. The imageable moiety is a gamma ray or positron emitting radioisotope, a magnetic resonance imaging contrast agent, an X-ray contrast agent, or an ultrasound contrast agent.
    • 本发明描述了新的下式化合物:<?in-line-formula description =“In-line Formulas”end =“lead”?>(Q) 对于癌症的诊断和治疗有用的<?in-line-formula description =“在线公式”end =“tail”?>,肿瘤成像方法 患者,以及在患者中治疗癌症的方法。 本发明还提供了可用于监测治疗性血管生成治疗和破坏新的血管生成脉管系统的新型化合物。 本发明还提供可用于成像动脉粥样硬化,再狭窄,心脏缺血和心肌再灌注损伤的新型化合物。 本发明还提供了可用于治疗类风湿性关节炎的新化合物。 药物由与血管发生期间上调的受体结合的靶向部分,任选的连接基团和治疗有效的放射性同位素或诊断上有效的可成像部分组成。 可成像部分是伽马射线或正电子发射放射性同位素,磁共振成像造影剂,X射线造影剂或超声造影剂。