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58 条记录 (耗时 0.021 秒)

    Radiohalogenated for proteins
    29.
    发明授权
    Radiohalogenated for proteins 失效
    放射性卤化蛋白质

    公开(公告)号：US4885153A

    公开(公告)日：1989-12-05

    申请号：US338497

    申请日：1989-04-13

    申请人： Daniel S. Wilbur ,  Alan R. Fritzberg ,  David S. Jones

    发明人： Daniel S. Wilbur ,  Alan R. Fritzberg ,  David S. Jones

    IPC分类号： C07F3/12 ,  C07F7/22

    CPC分类号： C07F7/2212 ,  C07F3/12

    摘要： Haloaryl compounds bearing a defined functional group or precursor are metalated with either Sn(n-Bu).sub.3 or SnMe.sub.3. The resulting aryltin compound may be transmetalated in site-specific reaction with one of the following organometallic groups: HgX.sub.2, Hg(OAc).sub.2, BX.sub.3, or BZ.sub.3, wherein X is Cl, Br, or I, and Z is alkyl or alkoxy. The stannylated or otherwise metalated compounds are subsequently radiohalogenated via a demetalation reaction. The Stannylated or otherwise metalated compounds are subsequently radiohalogenated via a demetalation reaction. The functional group is suitable for conjugation to protein and can be present or be added subsequent, but most preferably prior, to the radiohalogenation.Also compounds of the formula: R.sub.1 --Ar--R.sub.2, wherein R.sub.1 is either a radiohalogen or any one of the organometallic groups stated above, Ar is aromatic or heteroaromatic ring, and R.sub.2 is a short-chain substituent that does not highly activate the aromatic ring an that bears a functional group suitable for conjugation to protein under conditions that preserve the biological activity of the protein. The radiohalogenated small nolecules are conjugated to proteins such as monoclonal antibodies for use in diagnosis and therapy.

    摘要翻译： 带有限定官能团或前体的卤代芳基化合物与Sn（n-Bu）3或SnMe 3金属化。 所得的芳基锡化合物可以与以下有机金属基团之一的位置特异性反应转金属：HgX2，Hg（OAc）2，BX3或BZ3，其中X为Cl，Br或I，Z为烷基或烷氧基。 然后通过脱金属反应使经卤化或其它金属化的化合物放射性卤化。 然后通过脱金属反应使经卤化或其它金属化的化合物放射性卤化。 该官能团适用于与蛋白质缀合，并且可以存在或随后添加，但最优选之前为放射性卤化。 还有下式的化合物：R1-Ar-R2，其中R1是放射性卤素或上述有机金属基团中的任一个，Ar是芳族或杂芳族环，R2是不高度活化芳族的短链取代基 在保护蛋白质的生物活性的条件下，具有适合于与蛋白质缀合的官能团。 放射性卤化的小分子与蛋白质缀合，例如用于诊断和治疗的单克隆抗体。

    Skeletal-targeted radiation to treat bone-associated pathologies
    30.
    发明授权
    Skeletal-targeted radiation to treat bone-associated pathologies 失效
    骨骼靶向辐射治疗骨相关病变

    公开(公告)号：US07691985B2

    公开(公告)日：2010-04-06

    申请号：US12043757

    申请日：2008-03-06

    申请人： Alan R. Fritzberg

    发明人： Alan R. Fritzberg

    IPC分类号： C07F5/00

    CPC分类号： A61K51/0478 ,  A61K51/0489

    摘要： The present invention relates to a method of suppressing bone marrow (BM) and treating conditions that arise in or near bone such as cancer, myeloproliferative diseases, autoimmune diseases, infectious diseases, metabolic diseases or genetic diseases, with compositions having as their active ingredient a radionuclide complexed with a chelating agent such as macrocyclic aminophosphonic acid.

    摘要翻译： 本发明涉及一种抑制骨髓（BM）的治疗方法，并且治疗在诸如癌症，骨髓增生性疾病，自身免疫性疾病，传染病，代谢疾病或遗传疾病之类的骨附近或附近产生的病症，组合物具有作为其活性成分的组合物 与螯合剂如大环氨基膦酸络合的放射性核素。