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公开(公告)号：US5948386A
公开(公告)日：1999-09-07
申请号：US818075
申请日：1997-03-14
CPC分类号： A61K47/48384 , A61K47/48084 , A61K51/0478
摘要： A method of forming phosphine-amine conjugates includes reacting a hydroxymethyl phosphine group of an amine-free first molecule with at least one free amine group of a second molecule to covalently bond the first molecule with the second molecule through an aminomethyl phosphorus linkage and the conjugates formed thereby.
摘要翻译： 形成膦 - 胺共轭物的方法包括使无胺第一分子的羟甲基膦基与至少一个第二分子的游离胺基反应，以通过氨基甲基磷键将第一分子与第二分子共价键合，并且共轭物 由此形成。
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2.发明授权
公开(公告)号：US6054115A
公开(公告)日：2000-04-25
申请号：US33928
申请日：1998-03-03
申请人： Kattesh V. Katti , Srinivasa Rao Karra , Douglas E. Berning , C. Jeffrey Smith , Wynn A. Volkert , Alan R. Ketring
发明人： Kattesh V. Katti , Srinivasa Rao Karra , Douglas E. Berning , C. Jeffrey Smith , Wynn A. Volkert , Alan R. Ketring
IPC分类号： A61K51/00 , A61K51/04 , A61K51/08 , A61K51/10 , A61P9/00 , A61P25/00 , A61P31/00 , A61P31/12 , A61P35/00 , C07F7/00 , C07F9/50 , C07F13/00 , C07F15/00 , C07F5/00 , C07F9/00
CPC分类号： C07F15/008 , A61K51/04 , A61K51/0478 , A61K51/0489 , C07F13/005 , C07F9/5004 , C07F9/5022 , C07F9/5027 , A61K2121/00 , A61K2123/00
摘要： A compound and method of making a compound for use as a diagnostic or therapeutic pharmaceutical comprises at least one functionalized hydroxyalkyl phosphine donor group and one or more sulfur or nitrogen donor and a metal combined with the ligand.
摘要翻译： 制备用作诊断或治疗药物的化合物的化合物和方法包括至少一种官能化羟烷基膦供体基团和一个或多个硫或氮供体和与配体结合的金属。
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3.发明授权
公开(公告)号：US5843993A
公开(公告)日：1998-12-01
申请号：US818078
申请日：1997-03-14
CPC分类号： A61K51/0489 , A61K31/66 , A61K51/0478 , C07F9/5045
摘要： A complex and method for making same for use as a diagnostic or therapeutic pharmaceutical includes a ligand comprising at least one hydroxyalkyl phosphine donor group bound to a gold atom to form a gold-ligand complex that is stable in aqueous solutions containing oxygen, serum and other body fluids.
摘要翻译： 用于制备其作为诊断或治疗性药物的复合物和方法包括配体，其包含与金原子结合的至少一个羟烷基膦供体基团，以形成在含有氧，血清和其它物质的水溶液中稳定的金 - 配体配合物 体液。
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公开(公告)号：US5855867A
公开(公告)日：1999-01-05
申请号：US818080
申请日：1997-03-14
申请人： Kattesh V. Katti , Srinivasa Rao Karra , Douglas E. Berning , C. Jeffrey Smith , Wynn A. Volkert , Alan R. Ketring
发明人： Kattesh V. Katti , Srinivasa Rao Karra , Douglas E. Berning , C. Jeffrey Smith , Wynn A. Volkert , Alan R. Ketring
IPC分类号： A61K51/00 , A61K51/04 , A61K51/08 , A61K51/10 , A61P9/00 , A61P25/00 , A61P31/00 , A61P31/12 , A61P35/00 , C07F7/00 , C07F9/50 , C07F13/00 , C07F15/00 , C07C233/00 , C07F5/00 , C07F9/02
CPC分类号： C07F15/008 , A61K51/04 , A61K51/0478 , A61K51/0489 , C07F13/005 , C07F9/5004 , C07F9/5022 , C07F9/5027 , A61K2121/00 , A61K2123/00
摘要： A compound and method of making a compound for use as a diagnostic or therapeutic pharmaceutical comprises at least one functionalized hydroxyalkyl phosphine donor group and one or more sulfur or nitrogen donor and a metal combined with the ligand.
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5.发明授权New multifunctional ligands for potential use in the design therapeutic or diagnostic radiopharmaceutical imaging agents 失效用于设计治疗或诊断性放射性药物成像剂的新的多功能配体
公开(公告)号：US5601800A
公开(公告)日：1997-02-11
申请号：US211905
申请日：1994-07-29
IPC分类号： A61K51/00 , A61K49/00 , A61K51/10 , C07B59/00 , C07F9/50 , C07F9/6587 , C07F9/80 , C07F13/00 , C07F15/00 , C07F15/02 , A61K51/04
CPC分类号： C07F15/0013 , A61K51/1093 , C07B59/004 , C07F13/005 , A61K2123/00
摘要： A class of diagnostic and therapeutic compounds derived from phosphinimines that include ligands containing either a single phosphinimine functionality or both a phosphinimine group and a phosphine or arsine group, or an aminato group, or a second phosphinimine moiety. These phosphinimine ligands are complexed to early transition metal radionuclides (e.g. .sup.99m Tc or .sup.186 Re/.sup.188 Re) or late transition metals (e.g., .sup.105 Rh or .sup.109 Pd). The complexes with these metals .sup.186 Re/.sup.188 Re, .sup.99m Tc and .sup.109 Pd exhibit a high in vitro and high in vivo stability. The complexes are formed in high yields and can be neutral or charged. These ligands can also be used to form stable compounds with paramagnetic transition metals (e.g. Fe and Mn) for potential use as MRI contrast agents. Applications for the use of ligands and making the ligands are also disclosed.
摘要翻译： PCT No.PCT / US92 / 09742 Sec。 371日期1994年7月29日第 102（e）日期1994年7月29日PCT 1991年11月9日PCT PCT。 公开号WO93 / 08839 日期1993年5月13日一类衍生自次膦酰亚胺的诊断和治疗化合物，其包括含有单次膦亚胺官能团的配体或膦亚胺基和膦或胂基，或氨基或第二次膦酰亚胺部分。 这些膦亚胺配体与早期过渡金属放射性核素（例如99mTc或186Re / 188Re）或后过渡金属（例如，105Rh或109Pd）络合。 与这些金属186Re / 188Re，99mTc和109Pd的配合物具有高体外和高体内稳定性。 络合物以高产率形成并且可以是中性的或带电的。 这些配体也可以用于形成具有顺磁性过渡金属（例如Fe和Mn）的稳定化合物，用于潜在的用作MRI造影剂。 还公开了使用配体和制备配体的应用。
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6.发明授权
公开(公告)号：US5516940A
公开(公告)日：1996-05-14
申请号：US235355
申请日：1994-04-29
IPC分类号： A61K38/00 , A61K31/047 , A61K31/28 , A61K31/66 , A61K31/675 , A61K31/695 , A61K39/395 , A61K49/00 , A61K49/06 , A61K49/08 , A61K51/00 , A61K51/04 , A61P35/00 , A61P43/00 , C07B59/00 , C07F7/00 , C07F7/30 , C07F9/06 , C07F9/22 , C07F9/24 , C07F9/44 , C07F9/535 , C07F13/00 , C07F15/00 , C07F15/06 , C07F19/00 , C07F9/50 , C07D241/04 , C07F9/53
CPC分类号： A61K49/103 , A61K31/28 , A61K31/66 , A61K31/675 , A61K51/0478 , C07B59/004 , C07F13/00 , C07F13/005 , C07F15/0066 , C07F15/065 , C07F19/005 , C07F7/003 , C07F7/30 , C07F9/065 , C07F9/228 , C07F9/2491 , C07F9/4496 , C07F9/5355
摘要： A compound and method of making a compound for use as a diagnostic or therapeutic pharmaceutical comprises either a phosphorous or germanium core and at least two hydrazine groups forming a ligand for bonding to a metal extending from the phosphorous or germanium core.
摘要翻译： 制备用作诊断或治疗药物的化合物的化合物和方法包括磷或锗核和形成用于键合到从磷或锗核延伸的金属的配体的至少两个肼基团。
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7.发明授权
公开(公告)号：US5876693A
公开(公告)日：1999-03-02
申请号：US902829
申请日：1997-07-30
申请人： Kattesh V. Katti , Prahlad R. Singh , V. Sreenivasa Reddy , Kavita K. Katti , Wynn A. Volkert , Alan R. Ketring
发明人： Kattesh V. Katti , Prahlad R. Singh , V. Sreenivasa Reddy , Kavita K. Katti , Wynn A. Volkert , Alan R. Ketring
IPC分类号： A61K51/00 , A61K51/04 , A61K51/08 , A61K51/10 , A61P9/00 , A61P25/00 , A61P31/12 , A61P35/00 , C07F9/50 , C07F13/00 , C07F15/00 , C07F5/00
CPC分类号： A61K51/0478 , A61K51/0489 , C07F13/005 , C07F15/008 , C07F9/5004 , C07F9/5022 , C07F9/5027 , A61K2121/00 , A61K2123/00
摘要： A compound and method of making a compound for use as a diagnostic or therapeutic pharmaceutical comprises a functionalized hydroxyalkyl phosphine ligand and a metal combined with the ligand.
摘要翻译： 制备用作诊断或治疗药物的化合物的化合物和方法包括官能化羟烷基膦配体和与配体结合的金属。
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公开(公告)号：US5478474A
公开(公告)日：1995-12-26
申请号：US165373
申请日：1993-12-10
CPC分类号： G21F9/12 , C22B3/205 , C22B3/42 , G21C19/46 , Y02P10/234 , Y02W30/883
摘要： The method of treating liquid waste in a media is accomplished by exposing the media to phosphinimines and sequestering .sup.99 Tc from the media by the phosphinimine (PN) functionalities. The system for treating the liquid waste in the media includes extraction of .sup.99 TcO.sub.4.sup.- from aqueous solutions into organic solvents or mixed organic/polar media, extraction of .sup.99 Tc from solutions on a solid matrix by using a container containing PN functionalities on solid matrices including an inlet and outlet for allowing flow of media through an immobilized phosphinimine ligand system contained within the container. Also, insoluble suspensions of phosphinimine functionalities on solid matrices in liquid solutions or present on supported liquid membranes (SLM) can be used to sequester .sup.99 Tc from those liquids.
摘要翻译： 通过将介质暴露于次膦酰亚胺并通过膦亚胺（PN）官能团从介质中螯合99Tc来实现处理介质中废液的方法。 用于处理介质中的液体废物的系统包括将99TcO4-从水溶液中萃取到有机溶剂或混合有机/极性介质中，通过使用在包括入口的固体基质上含有PN官能团的容器从固体基质上的溶液中提取99Tc 和用于允许介质流过包含在容器内的固定化膦酰亚胺配体系统的出口。 此外，膦酰亚胺功能性在液体溶液中固体基质上的不溶性悬浮液或存在于载体液膜（SLM）上的不溶性悬浮液可用于从这些液体中螯合99Tc。
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9.发明授权Procedure for isolating and purifying radioactive ligated rhenium pharmaceuticals and use thereof and kit 失效用于分离和纯化放射性结扎铼药物的方法及其用途和试剂盒
公开(公告)号：US4935222A
公开(公告)日：1990-06-19
申请号：US873990
申请日：1986-06-13
CPC分类号： A61K51/1282 , A61K51/1241 , A61K2123/00
摘要： A sterile pyrogen free Re.sup.196 or Re.sup.188 radiopharmaceutical is prepared by reducing radioactive perrhenate in the presence of a bone seeking ligand to form a solution including complexed Re-ligand compound together with impurities such as uncomplexed perrhenate, ReO.sub.2 and free ligand. The radiopharmaceutical is obtained by a low pressure purification method. The solution is added to a separation column, preferably an ion exchange column, and a first portion is eluted and discarded. The radiopharmaceutical is collected in a second eluted portion defined as having 25-85% of the activity of the Re on the column, less than 10% unligated perrhenate and less than 1% ReO.sub.2. This can be used as is to image and treat metastatic bone leasions. A simple kit is also disclosed.
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公开(公告)号：US4732974A
公开(公告)日：1988-03-22
申请号：US836535
申请日：1986-03-05
IPC分类号： C07K16/00 , A61K39/395 , A61K51/00 , A61K51/08 , A61K51/10 , C07K1/107 , C07K1/113 , C07K1/13 , C07K14/00 , G01N33/532 , G01N33/534 , G01N33/574 , C07K3/08 , A61K39/00 , A61K39/42 , A61K43/00
CPC分类号： G01N33/534 , A61K51/1048 , A61K51/1093 , C07K1/1077 , G01N33/532 , A61K2121/00 , A61K2123/00
摘要： A conjugate of a protein or polypeptide and a metal ion is prepared by reacting a metal ion transfer complex comprising a chelate of 4,5-dihydroxyl-m-benzenedisulfonic acid or a salt thereof with a protein or polypeptide that is covalently bound to an exogenous chelating group having a greater affinity than 4,5-dihydroxyl-m-benzenedisulfonic acid for the metal ion.
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