Complexes with .sup.99m Tc suitable for radiolabelling monoclonal
antibodies or other macro molecules
    1.
    发明授权
    Complexes with .sup.99m Tc suitable for radiolabelling monoclonal antibodies or other macro molecules 失效
    与99mTc的复合物适用于放射性标记单克隆抗体或其他大分子

    公开(公告)号:US5350837A

    公开(公告)日:1994-09-27

    申请号:US55312

    申请日:1993-05-03

    摘要: The ligand L, (R.sup.3)(R.sup.4)(R.sup.5)C--N(R)--C(R.sup.1)(R.sup.2)--(CH.sub.2).sub.n --COOH L where R is hydrogen, hydroxy, alkyl, hydroxyalkyl, or alkylcarboxy, or R and R.sup.1 together may form a mono-, di-, tri-, or tetra-methylene radical, or R and R.sup.3 together may form a mono-, di-, tri-, or tetra-methylene radical, and R.sup.1 and R.sub.2 may be the same or different and are selected from hydrogen, hydroxy, alkyl, hydroxyalkyl, carboxy, alkylcarboxy, alkylamine, alkylthiol, aryl or R.sup.1 and R.sup.2 together may form a tetra- or penta-methylene radical, and R.sup.3 and R.sup.4 and R.sup.5 may be the same or different and are selected from hydrogen, hydroxy, alkyl, hydroxyalkyl, carboxy, alkylcarboxy, provided that at least one of R.sup.3, R.sup.4 and R.sup.5 is hydroxyalkyl, and n is equal to 0, 1 or 2, for example tricine, form useful complexes with .sup.99m Tc, for radiolabelling macromolecules such as monoclonal antibodies.

    摘要翻译: 配体L,(R3)(R4)(R5)CN(R)-C(R1)(R2) - (CH2)n-COOHL其中R是氢,羟基,烷基,羟基烷基或烷基羧基,或R和 R1一起可以形成单 - ,二 - ,三 - 或四 - 亚甲基,或者R和R 3一起可以形成单 - ,二 - ,三 - 或四 - 亚甲基,R1和R2可以是 相同或不同,选自氢,羟基,烷基,羟基烷基,羧基,烷基羧基,烷基胺,烷基硫醇,芳基或R 1和R 2一起可以形成四或五亚甲基,R3和R4和R5可以相同 或不同的,并且选自氢,羟基,烷基,羟基烷基,羧基,烷基羧基,条件是R 3,R 4和R 5中的至少一个是羟烷基,n等于0,1或2,例如三羟甲基,形成有用的络合物 具有99mTc,用于放射性标记大分子如单克隆抗体。

    Synthesis of enantiomerically pure amino-substituted fused bicyclic rings
    4.
    发明授权
    Synthesis of enantiomerically pure amino-substituted fused bicyclic rings 有权
    对映体纯氨基取代稠合双环的合成

    公开(公告)号:US07135570B2

    公开(公告)日:2006-11-14

    申请号:US10959823

    申请日:2004-10-06

    IPC分类号: C07D215/00

    摘要: This invention describes various processes for synthesis and resolution of racemic amino-substituted fused bicyclic ring systems. One process utilizes selective hydrogenation of an amino-substituted fused bicyclic aromatic ring system. An alternative process prepares the racemic amino-substituted fused bicyclic ring system via nitrosation. In addition, the present invention describes the enzymatic resolution of a racemic mixture to produce the (R)— and (S)— forms of amino-substituted fused bicyclic rings as well as a racemization process to recycle the unpreferred enantioner. Further provided by this invention is an asymmetric synthesis of the (R)— or (S)— enantiomer of primary amino-substituted fused bicyclic ring systems.

    摘要翻译: 本发明描述了合成和拆分外消旋氨基取代的稠合双环体系的各种方法。 一个方法利用氨基取代的稠合双环芳族环系统的选择性氢化。 另一种方法是通过亚硝化制备外消旋氨基取代的稠合双环体系。 此外,本发明描述了外消旋混合物的酶拆分以产生(R) - 和(S) - 形式的氨基取代的稠合双环,以及外消旋化方法以回收未预期的对映异构体。 本发明进一步提供的是伯氨基取代的稠合双环体系的(R) - 或(S) - 对映异构体的不对称合成。

    Combination Therapy
    6.
    发明申请
    Combination Therapy 审中-公开
    联合治疗

    公开(公告)号:US20100178271A1

    公开(公告)日:2010-07-15

    申请号:US12376591

    申请日:2007-08-07

    IPC分类号: A61K38/19 A61P35/00 A61P35/02

    摘要: Methods to mobilize progenitor and/or stem cells from the bone marrow to the bloodstream by administering a combination of at least one CXCR4 inhibitor, at least one CXCR2 agonist, and G-CSF are described. The combinations may also be used to increase the effectiveness of chemotherapy and radiation therapies for hematopoietic malignancies.

    摘要翻译: 描述了通过施用至少一种CXCR4抑制剂,至少一种CXCR2激动剂和G-CSF的组合将祖细胞和/或干细胞从骨髓移动到血流的方法。 这些组合也可用于增加造血恶性肿瘤的化疗和放射治疗的有效性。

    Synthesis of enantiomerically pure amino-substituted fused bicyclic rings
    7.
    发明授权
    Synthesis of enantiomerically pure amino-substituted fused bicyclic rings 有权
    对映体纯氨基取代稠合双环的合成

    公开(公告)号:US07452994B2

    公开(公告)日:2008-11-18

    申请号:US11598955

    申请日:2006-11-14

    IPC分类号: C07D215/00 C07D217/00

    摘要: This invention describes various processes for synthesis and resolution of racemic amino-substituted fused bicyclic ring systems. One process utilizes selective hydrogenation of an amino-substituted fused bicyclic aromatic ring system. An alternative process prepares the racemic amino-substituted fused bicyclic ring system via nitrosation. In addition, the present invention describes the enzymatic resolution of a racemic mixture to produce the (R)- and (S)-forms of amino-substituted fused bicyclic rings as well as a racemization process to recycle the unpreferred enantioner. Further provided by this invention is an asymmetric synthesis of the (R)- or (S)-enantiomer of primary amino-substituted fused bicyclic ring systems.

    摘要翻译: 本发明描述了合成和拆分外消旋氨基取代的稠合双环体系的各种方法。 一个方法利用氨基取代的稠合双环芳族环系统的选择性氢化。 另一种方法是通过亚硝化制备外消旋氨基取代的稠合双环体系。 此外,本发明描述了外消旋混合物的酶拆分以产生氨基取代的稠合双环的(R) - 和(S)形式,以及外消旋化方法以回收未预期的对映异构体。 本发明进一步提供的是主要氨基取代的稠合双环体系的(R) - 或(S) - 对映体的不对称合成。