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    Radiohalogenated for proteins
    1.
    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。

    Radiohalogenated small molecules for protein labeling
    5.
    发明授权
    Radiohalogenated small molecules for protein labeling 失效
    用于蛋白标记的放射性卤代小分子

    公开(公告)号：US5045303A

    公开(公告)日：1991-09-03

    申请号：US137952

    申请日：1987-11-23

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

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

    IPC分类号： C07F3/12 ,  C07F7/22

    CPC分类号： C07F7/2212 ,  C07F3/12

    摘要： Haloaryl compounds are lithiated and thereafter metalated with one of the following organometallic groups: Sn(n-Bu).sub.3 or SnMe.sub.3. The resulting aryltin compound can be transmetalated in site-specific reaction with one of the following organometallic groups: HgX, Hg(OAc).sub.2, BX.sub.3, or BZ.sub.2, wherein X is Cl, Br, or I, and Z is alkyl or alkoxy. The metalated compounds are subsequently radiohalogenated via a demetalation reaction. A functional group suitable for conjugation to protein can be added subsequent of 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 activate the aromatic ring and that bears a functional group, or a precursor thereof, suitable for conjugation to protein under conditions that preserve the biological activity of the protein.The radiohalogenated small molecules are conjugated to proteins such as monoclonal antibodies for use in diagnosis and therapy.

    摘要翻译： 卤代芳基化合物被锂化，然后用以下有机金属组之一金属化：Sn（n-Bu）3或SnMe 3。 所得的芳基锡化合物可以在以下有机金属基团之一的位置特异性反应中转金属：HgX，Hg（OAc）2，BX3或BZ2，其中X为Cl，Br或I，Z为烷基或烷氧基。 金属化合物随后通过脱金属反应放射卤化。 适合于与蛋白质缀合的官能团可以随后优选在放射性卤化之前加入。 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何一个，Ar是芳族或杂芳族环，R2是不活化芳环的短链取代基 并且在保持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或其前体。 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。

    Radiohalogenated small molecules for protein labeling
    6.
    发明授权
    Radiohalogenated small molecules for protein labeling 失效
    放射性蛋白标记的小分子

    公开(公告)号：US5213787A

    公开(公告)日：1993-05-25

    申请号：US627806

    申请日：1990-12-12

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

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

    IPC分类号： C07F3/12 ,  C07F7/22

    CPC分类号： C07F7/2212 ,  C07F3/12

    摘要： Haloaryl compounds are lithiated and thereafter metalated with one of the following organometallic groups: Sn(n-Bu).sub.3 or SnMe.sub.3. The resulting aryltin compound can be transmetalated in site-specific reaction with one of the following organometallic groups: HgX, Hg(OAc).sub.2, BX.sub.3, or BZ.sub.2, wherein X is Cl, Br, or I, and Z is alkyl or alkoxy. The metalated compounds are subsequently radiohalogenated via a demetalation reaction. A functional group suitable for conjugation to protein can be added subsequent or 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 activate the aromatic ring and that bears a functional group, or a precursor thereof, suitable for conjugation to protein under conditions that preserve the biological activity of the protein.The radiohalogenated small molecules are conjugated to proteins such as monoclonal antibodies for use in diagnosis and therapy.

    摘要翻译： 卤代芳基化合物被锂化，然后用以下有机金属组之一金属化：Sn（n-Bu）3或SnMe 3。 所得的芳基锡化合物可以在以下有机金属基团之一的位置特异性反应中转金属：HgX，Hg（OAc）2，BX3或BZ2，其中X为Cl，Br或I，Z为烷基或烷氧基。 金属化合物随后通过脱金属反应放射卤化。 适于与蛋白质缀合的官能团可以随后或优选在放射性卤化之前添加。 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何一个，Ar是芳族或杂芳族环，R2是不活化芳环的短链取代基 并且在保持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或其前体。 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。

    Metal radionuclide chelating compounds for improved chelation kinetics
    10.
    发明授权
    Metal radionuclide chelating compounds for improved chelation kinetics 失效
    用于改善螯合动力学的金属放射性核素螯合化合物

    公开(公告)号：US4988496A

    公开(公告)日：1991-01-29

    申请号：US201134

    申请日：1988-05-31

    申请人： Ananthachari Srinivasan ,  Alan R. Fritzberg ,  David S. Jones

    发明人： Ananthachari Srinivasan ,  Alan R. Fritzberg ,  David S. Jones

    IPC分类号： A61K47/48 ,  A61K51/10 ,  C07C327/30 ,  C07C327/32 ,  C07D207/46 ,  C07D209/48 ,  C07D307/18 ,  C07D405/12

    CPC分类号： C07D209/48 ,  A61K47/48707 ,  A61K51/1093 ,  C07C327/30 ,  C07C327/32 ,  C07D207/46 ,  C07D307/18 ,  C07D405/12 ,  A61K2121/00 ,  A61K2123/00

    摘要： The present invention provides metal chelating compounds, to chelates and chelate-targeting agent conjugates formed from the chelating compounds, and to methods for making and using these compositions. The chelating compounds incorporate two nitrogen atoms and three sulfur atoms ("N.sub.2 S.sub.3 "), two nitrogen atoms and four sulfur atoms ("N.sub.2 S.sub.4 "), or three nitrogen atoms and three sulfur atoms ("N.sub.3 S.sub.3 "). Metals, and metal oxides, capable of being chelated by the compounds include those that are radionuclides, such as .sup.99m Tc and .sup.186/188 Re.The targeting agent portion of the chelate-targeting agent conjugates provided includes antibodies, peptides, hormones, enzymes and biological response modifiers. Methods for making the conjugates are provided and encompass the addition of a metal, or metal oxide, to a chelating compound prior to attachment to a targeting agent as well as subsequent to the attachment.Another aspect of the invention provides kits for producing chelate-targeting agent comjugates for radiopharmaceutical use.An additional aspect of the invention provides methods for using the chelate-targeting agent conjugates for diagnostic and therapeutic purposes, such as detection of a target site and delivery of a radionuclide to the site, respectively.