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1.发明授权Metal chelates as pharmaceutical imaging agents, processes of making such and uses thereof 失效金属螯合物作为药物成像剂，制备方法及其用途
公开(公告)号：US5986074A
公开(公告)日：1999-11-16
申请号：US993219
申请日：1997-12-18
CPC分类号： A61K51/04 , C07F13/005
摘要： The present invention relates to novel metal chelates, exemplified as technetium-99m or rhenium chelates, and to the process of preparing such metal chelates from corresponding ligands. These ligands and their corresponding metal chelates are synthesized to have a cysteinylethylene (EC) structure, a monothiourea (MTU) structure, or a dithiourea (DTU) structure. The present invention further relates to a pharmaceutical composition comprising a metal chelate, for example, a .sup.99m Tc-chelate, to the use of the composition for renal imaging and examination of renal function, and to a kit for preparing such a composition prior to use.
摘要翻译： 本发明涉及以锝-99m或铼螯合物为例的新型金属螯合物，以及由相应配体制备这种金属螯合物的方法。 这些配体及其相应的金属螯合物被合成以具有半胱氨酸乙烯（EC）结构，一硫脲（MTU）结构或二硫脲（DTU）结构。 本发明还涉及包含金属螯合物，例如99mTc螯合物的药物组合物，用于肾脏成像和肾功能检查的组合物，以及用于在使用前制备该组合物的试剂盒。
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公开(公告)号：US5116831A
公开(公告)日：1992-05-26
申请号：US560394
申请日：1990-07-31
IPC分类号： C07F15/00
CPC分类号： C07F15/0093
摘要： Square-planar four-coordinate complexes of cis-platinum (II) with neutral bidentate aminoalkyl-substituted cycloalkylamine ligands and bromo-, chloro-, iodo-, nitrato-, oxalato-, or malanato-ligands possess antimicrobial activity as well as activity against transplanted L1210 and P388 murine leukemia cell lines.
摘要翻译： 顺式铂（II）与中性二齿氨基烷基取代的环烷基胺配体和溴 - ，氯 - ，碘 - ，硝基 - ，草酸 - 或马拉那那 - 配体的平面四坐标络合物具有抗菌活性和抗 移植L1210和P388鼠白血病细胞系。
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公开(公告)号：US5281616A
公开(公告)日：1994-01-25
申请号：US873415
申请日：1992-04-24
摘要： Compositions for the inhibition of replication of human immunodeficiency virus containing one or more "porphyrins" possessing antiviral activity. As used herein "porphyrins" includes porphyrins, phthalocyanines, chlorins, metallo derivatives thereof, and other porphyrin-like compounds. Examples of natural and synthetic, positively, negatively, and neutrally charged porphyrins, phthalocyanines, and derivatives thereof have been found to exhibit selective anti-HIV activity which is not dependent on the presence of light.
摘要翻译： 用于抑制含有一种或多种具有抗病毒活性的“卟啉”的人类免疫缺陷病毒复制的组合物。 如本文所用，“卟啉”包括卟啉，酞菁，二氢卟酚，其金属衍生物和其它卟啉样化合物。 已经发现天然和合成，正，负和中性带电的卟啉，酞菁及其衍生物的实例表现出不依赖于光的选择性抗HIV活性。
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公开(公告)号：US5192788A
公开(公告)日：1993-03-09
申请号：US197764
申请日：1988-05-23
摘要： Compositions for the treatment or prevention of AIDS or other diseases resulting from infection with the Human Immunodeficiency Virus containing one or more porphyrins.Porphyrins are tetrapyrrole macrocyle compounds with bridges of one carbon joining the pyrroles. Porphyrins occur naturally and are made synthetically. Derivatives of porphyrins include porphyrins with one or more substituents on one or more of the rings, porphyrins in which the conjugation of the ring has been altered by addition of substituents, porphyrins in which one or more center nitrogens is attached to substituents such as metals, liganded metals, and organic moieties, metalloporphyrins and metalloporphyrin-ligand complexes.Examples of natural and synthetic, positively, negatively, and neutrally charged porphyrins and porphyrin derivatives have been found to exhibit selective anti-HIV activity which is not dependent on the presence of light. Most of the compounds did not inhibit replication of herpes simplex virus type 1 or type 2 or Coxsackievirus strain B4. Effective concentrations for inhibition of HIV-1, as measured in vitro by inhibition of replication range from 0.01 to greater than 100 .mu.M. None of the compounds were toxic to unifected PBM cells.
摘要翻译： 用于治疗或预防由含有一种或多种卟啉的人类免疫缺陷病毒感染而引起的AIDS或其他疾病的组合物。 卟啉是具有连接吡咯的一个碳原子的桥的四吡咯大环化合物。 卟啉自然发生并合成。 卟啉的衍生物包括在一个或多个环上具有一个或多个取代基的卟啉，其中通过加成取代基改变环的缀合的卟啉，其中一个或多个中心氮连接到取代基如金属上的卟啉， 配体金属和有机部分，金属卟啉和金属卟啉 - 配体络合物。 已经发现天然和合成，正，负和中性带电的卟啉和卟啉衍生物的实例表现出不依赖于光的存在的选择性抗HIV活性。 大多数化合物不抑制1型或2型或柯萨奇病毒株B4的单纯疱疹病毒的复制。 如通过抑制复制而在体外测量的HIV-1的有效浓度范围为0.01至大于100μM。这些化合物对单个PBM细胞无毒。
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5.发明授权Method for inhibiting infection or replication of human immunodeficiency virus with porphyrin and phthalocyanine antiviral compositions 失效用卟啉和酞菁抗病毒组合物抑制人类免疫缺陷病毒感染或复制的方法
公开(公告)号：US5109016A
公开(公告)日：1992-04-28
申请号：US355499
申请日：1989-05-22
摘要： Compositions for the inhibition of replication of human immunodeficiency virus containing one or more "porphyrins" possessing antiviral activity. As used herein "porphyrins" includes porphyrins, phthalocyanines, chlorins, metallo derivatives thereof, and other porphyrin-like compounds. Examples of natural and synthetic, positively, negatively, and neutrally charged porphyrins, phthalocyanines, and derivatives thereof have been found to exhibit selective anti-HIV activity which is not dependent on the presence of light.
摘要翻译： 用于抑制含有一种或多种具有抗病毒活性的“卟啉”的人类免疫缺陷病毒复制的组合物。 如本文所用，“卟啉”包括卟啉，酞菁，二氢卟酚，其金属衍生物和其它卟啉样化合物。 已经发现天然和合成，正，负和中性带电的卟啉，酞菁及其衍生物的实例表现出不依赖于光的选择性抗HIV活性。
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公开(公告)号：US4970324A
公开(公告)日：1990-11-13
申请号：US142151
申请日：1988-01-08
IPC分类号： C07F15/00
CPC分类号： C07F15/0093
摘要： Square-planar four-coordinate complexes of cis-platinum(II) with neutral bidentate aminoalkyl-substituted cycloalkylamine ligands and bromo-, chloro-, iodo-, nitrato-, oxalato-, or malanato-ligands possess antimicrobial activity as well as activity against transplanted L1210 and P388 murine leukemia cell lines.
摘要翻译： 顺式铂（II）与中性二齿氨基烷基取代的环烷基胺配体和溴 - ，氯 - ，碘 - ，硝基 - ，草酸 - 或马拉那那 - 配体的平面四坐标络合物具有抗菌活性和抗 移植L1210和P388鼠白血病细胞系。
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