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    INHIBITION OF CELL PROLIFERATION
    3.
    发明申请
    INHIBITION OF CELL PROLIFERATION 审中-公开
    抑制细胞增殖

    公开(公告)号：WO2007062222A2

    公开(公告)日：2007-05-31

    申请号：PCT/US2006/045410

    申请日：2006-11-22

    申请人： UNIVERSITY OF SOUTH FLORIDA ,  SEBTI, Said M. ,  CHELLAPPAN, Srikumar ,  LAWRENCE, Nicholas James

    发明人： SEBTI, Said M. ,  CHELLAPPAN, Srikumar ,  LAWRENCE, Nicholas James

    IPC分类号： A61K31/675 ,  A61K31/53

    CPC分类号： C07C323/45 ,  C07C279/06 ,  C07C335/32 ,  C07D213/53 ,  C07D215/12 ,  C07D233/30 ,  C07D233/84 ,  C07D235/28 ,  C07D249/12 ,  C07D249/14 ,  C07D277/40 ,  C07D277/42 ,  C07D317/56 ,  C07D317/58

    摘要： The disclosed modulators of Rb:Raf-1 interactions are potent, selective disruptors of Rb:Raf-1 binding, with IC 50 values ranging from 80 nM to 500 nM. Further, these compounds are surprisingly effective in inhibiting a wide variety of cancer cells, including osteosarcoma, epithelial lung carcinoma, non small cell lung carcinoma, three different pancreatic cancer cell lines, two different glioblastoma cell lines, metastatic breast cancer, melanoma, and prostate cancer. Moreover, the disclosed compounds effectively disrupt angiogenesis and significantly inhibited tumors in nude mice derived from human epithelial lung carcinoma tumors. Accordingly, the disclosed compounds, pharmaceutical compositions comprising the compounds, methods of inhibiting cell proliferation, methods of treating subjects with cancer, and methods of preparing the disclosed compounds are provided.

    摘要翻译： 所公开的Rb：Raf-1相互作用的调节剂是Rb：Raf-1结合的有效的选择性破坏剂，80nM至500nM的IC 50 N值。 此外，这些化合物令人惊奇地有效地抑制多种癌细胞，包括骨肉瘤，上皮性肺癌，非小细胞肺癌，三种不同的胰腺癌细胞系，两种不同的胶质母细胞瘤细胞系，转移性乳腺癌，黑素瘤和前列腺 癌症。 此外，所公开的化合物有效地破坏了血管发生，并显着抑制了源自人上皮性肺癌肿瘤的裸鼠中的肿瘤。 因此，提供了所公开的化合物，包含该化合物的药物组合物，抑制细胞增殖的方法，治疗患有癌症的受试者的方法以及制备所公开的化合物的方法。

    LIGANDS FOR IMAGING CARDIAC INNERVATION
    6.
    发明申请
    LIGANDS FOR IMAGING CARDIAC INNERVATION 审中-公开
    用于成像心脏感染的配对

    公开(公告)号：WO2008083056A3

    公开(公告)日：2009-04-30

    申请号：PCT/US2007088500

    申请日：2007-12-21

    申请人： LANTHEUS MEDICAL IMAGING INC ,  PUROHIT AJAY ,  HARRIS THOMAS D ,  RADEKE HEIKE S ,  ROBINSON SIMON P ,  YU MING ,  CASEBIER DAVID S

    发明人： PUROHIT AJAY ,  HARRIS THOMAS D ,  RADEKE HEIKE S ,  ROBINSON SIMON P ,  YU MING ,  CASEBIER DAVID S

    IPC分类号： C07C279/04 ,  A61K51/04

    CPC分类号： A61K51/04 ,  A61K51/0453 ,  A61K51/0459 ,  C07B59/001 ,  C07B2200/05 ,  C07C215/60 ,  C07C217/70 ,  C07C279/06 ,  C07C279/08

    摘要： Novel compounds that find use as imaging agents within nuclear medicine applications (PET imaging) for imaging of cardiac innervation are disclosed. These PET based radiotracers may exhibit increased stability, decreased NE release (thereby reducing side effects), improved quantitative data, and/or high affinity for VMAT over prior radiotracers. Methods of using the compounds to image cardiac innervation are also provided. In some instances the compounds are developed by derivatizing certain compounds with 18F in a variety of positions: aryl, alkyl, a keto, benzylic, beta-alkylethers, gamma-propylalkylethers and beta-proplylalkylethers. Alternatively or additionally, a methyl group a is added to the amine, and/or the catechol functionality is either eliminated or masked as a way of making these compounds more stable.

    摘要翻译： 公开了用于心脏神经支配成像的核医学应用（PET成像）中用作成像剂的新型化合物。 这些基于PET的放射性示踪剂可能表现出增加的稳定性，减少NE释放（从而减少副作用），改进的定量数据，和/或对先前的放射性示踪剂对VMAT的高亲和力。 还提供了使用化合物成像心脏神经支配的方法。 在某些情况下，化合物通过在各种位置上衍生化某些化合物而形成：芳基，烷基，酮基，苄基，β-烷基醚，γ-丙基烷基醚和β-丙基烷基醚。 或者或另外，将甲基a加入到胺中，和/或儿茶酚官能团被消除或掩蔽，作为使这些化合物更稳定的方式。