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1. 发明授权

US5464934A Metal chelates as spacer compounds in biologically active peptides 失效
标题翻译：金属螯合物作为生物活性肽中的间隔物化合物
公开(公告)号：US5464934A
公开(公告)日：1995-11-07
申请号：US63172
申请日：1993-05-14
申请人： T. Jeffrey Dunn , Ananthachari Srinivasan , Leon R. Lyle , Raghavan Rajagopalan
发明人： T. Jeffrey Dunn , Ananthachari Srinivasan , Leon R. Lyle , Raghavan Rajagopalan
IPC分类号： A61K51/00 , A61K49/04 , A61K49/14 , A61K51/08 , C07K1/04 , C07K5/10 , C07K7/04 , C07K14/815 , C07K5/00 , A61K49/00 , C07K7/00 , C07K17/00
CPC分类号： A61K49/14 , C07K1/04 , C07K14/815
摘要： Ligands that are capable of forming metal complexes are incorporated directly into peptides at nonbiologically active locations. The metal complex serves as a bifunctional agent and as a spacer molecule. In one aspect of the invention, the ligands are prepared by replacing a nonbiologically active peptide spacer sequence with either Cys-Gly-Gly-Glu(.gamma.-)CO- (SEQ ID NO:1) or Cys-Gly-Gly-Lys(.epsilon.-)NH-CO(CH.sub.2).sub.2 -CO- (SEQ ID NO:2). In these examples, unnatural peptide bonds are used to attach the ligand to the terminal end of the peptide. Peptides incorporating such ligands are also disclosed.Other spacer ligands which may be incorporated into peptides include the following natural peptide sequences: -Cys-Gly-His-, -Asp-Gly-Cys-, -Glu-Gly-Cys-, -Gly-Asp-Cys-, and -Gly-Glu-Cys-. Unnatural tripeptides which function as spacer ligands include: -Cys-Gly-(imidazolyl glycyl)-, -isoCys-Gly-(imidazolyl glycyl)-, and -isoCys-Gly-His-. When the above peptide sequences are present in a nonbiologically active peptide spacer, they are able to form metal complexes with desired metal ions, and the resulting complexes serve as bifunctional agents and as spacer molecules in the peptide.
摘要翻译：能够形成金属络合物的配体在非生物活性位置直接并入肽中。金属络合物用作双官能剂和间隔分子。在本发明的一个方面，通过用Cys-Gly-Gly-Glu（γ - ）CO-（SEQ ID NO：1）或Cys-Gly-Gly-Lys（SEQ ID NO：1）替代非生物活性肽间隔序列 ε-）NH-CO（CH 2）2 -CO-（SEQ ID NO：2）。在这些实施例中，使用非天然肽键将配体连接到肽的末端。还公开了掺入这种配体的肽。可以并入肽中的其它间隔配体包括以下天然肽序列：-Cys-Gly-His-，-Asp-Gly-Cys-，-Glu-Gly-Cys-，-Gly-Asp-Cys-和 - Gly-Glu-Cys-。用作间隔基配体的非天然三肽包括：-Cys-Gly-（咪唑基甘氨酰基） - ， - iSysys-Gly-（咪唑基甘氨酰基） - 和-i-Syysys-Gly-His-。当上述肽序列存在于非生物活性肽间隔物中时，它们能够与期望的金属离子形成金属络合物，并且所得复合物用作双功能试剂和肽中的间隔分子。

2. 发明授权

US06664367B1 Stable analogs of bioactive peptides containing disulfide linkages 失效
标题翻译：含有二硫键的生物活性肽的稳定类似物
公开(公告)号：US06664367B1
公开(公告)日：2003-12-16
申请号：US08278437
申请日：1994-07-21
申请人： Raghavan Rajagopalan , Ananthachari Srinivasan , Leon R. Lyle
发明人： Raghavan Rajagopalan , Ananthachari Srinivasan , Leon R. Lyle
IPC分类号： C07K1600
CPC分类号： C07K14/655 , C07K1/006 , C07K7/16 , C07K14/52 , C07K14/6555 , C07K14/70 , Y10S930/28
摘要： Stable analogs of cyclic peptides containing disulfide linkages are disclosed. The disulfide linkage is modified by one of four methods: (a) sulfide contraction, (b) isosteric substitution, (c) thioketal expansion, or (d) alkylation expansion. In sulfide contraction the disulfide bond (—S—S—) is replaced with a monosulfide bond (—S—) in which a bifunctional effector molecule, such as a ligand or chemotoxic agent, is bound to the new peptide linkage. In isosteric substitution, one sulfur atom is replaced with a carbon atom and at least one of the carbon atoms at the modified site is a bifunctional effector molecule. In thioketal expansion, an alkylidene unit (—CR1C2—) is inserted between the two sulfur atoms. In alkylation expansion, an alkyl moiety of from C2 to C3, is inserted between the two sulfur atoms.
摘要翻译：公开了含有二硫键的环肽的稳定类似物。二硫键通过四种方法之一进行改性：（a）硫化物收缩，（b）等排取代，（c）硫代缩酮扩展或（d）烷基化扩展。在硫化物收缩中，二硫键（-S-S-）用单硫键（-S-）代替，其中双功能效应分子如配体或化学毒性剂与新的肽键结合。在等排取代中，一个硫原子被碳原子取代，并且在修饰位点处的至少一个碳原子是双功能效应子分子。在硫缩酮扩展中，在两个硫原子之间插入亚烷基单元（-CR1C2-）。在烷基化扩展中，C2至C3的烷基部分插入在两个硫原子之间。

3. 发明授权

US5623077A Imidazole based nitrogen sulfur ligands useful in radiographic imaging agents 失效
标题翻译：用于放射成像剂的咪唑基氮硫配体
公开(公告)号：US5623077A
公开(公告)日：1997-04-22
申请号：US420612
申请日：1995-04-10
申请人： Raghavan Rajagopalan , Ananthachari Srinivasan
发明人： Raghavan Rajagopalan , Ananthachari Srinivasan
IPC分类号： C07D233/64 , A61K51/00 , A61K51/04 , C07D233/54 , C07D233/91 , C07D405/12 , C07F13/00
CPC分类号： C07F13/005 , A61K51/0478 , C07D233/64 , C07D405/12 , A61K2123/00
摘要： The present invention relates particularly to novel imidazole based nitrogen-sulfur ligands that are suitable for complexing with a radionuclide, and are useful as general imaging agents for diagnostic purposes.
摘要翻译：本发明特别涉及适用于与放射性核素络合的新型咪唑基氮硫配体，并且可用作用于诊断目的的一般成像剂。

4. 发明授权

US5633372A Heterocycle based nitrogen sulfur ligands useful in radiographic imaging agents 失效
标题翻译：基于杂环的氮硫配体可用于放射成像剂
公开(公告)号：US5633372A
公开(公告)日：1997-05-27
申请号：US420611
申请日：1995-04-10
申请人： Raghavan Rajagopalan , Ananthachari Srinivasan
发明人： Raghavan Rajagopalan , Ananthachari Srinivasan
IPC分类号： C07D413/12 , A61K49/04 , A61K51/04 , C07D295/13 , C07D309/08 , C07F13/00 , C07D265/30 , C07D295/00
CPC分类号： C07F13/005 , A61K51/0478 , C07D295/13 , C07D309/08 , A61K2123/00
摘要： The present invention relates particularly to novel heterocycle based nitrogen-sulfur ligands that are suitable for complexing with a radionuclide, and are useful as general imaging agents for diagnostic purposes.
摘要翻译：本发明特别涉及适用于与放射性核素络合的新型基于杂环的氮 - 硫配体，并且可用作用于诊断目的的一般成像剂。

5. 发明授权

US5656253A Ligands useful in radiographic imaging 失效
标题翻译：配体可用于放射成像
公开(公告)号：US5656253A
公开(公告)日：1997-08-12
申请号：US255148
申请日：1994-06-07
申请人： Raghavan Rajagopalan , Ananthachari Srinivasan , Jean-Luc Vanderheyden
发明人： Raghavan Rajagopalan , Ananthachari Srinivasan , Jean-Luc Vanderheyden
IPC分类号： A61K51/04 , A61K51/08 , C07B59/00 , C07D213/40 , C07D213/64 , C07D213/68 , C07F13/00 , C07K14/655 , C07K14/815 , A61K51/00 , A61K7/32 , C07D211/70 , C07D401/02
CPC分类号： C07K14/815 , A61K51/0478 , A61K51/088 , C07B59/004 , C07D213/40 , C07D213/64 , C07D213/68 , C07F13/005 , C07K14/6555 , A61K2121/00 , A61K2123/00
摘要： The present invention relates particularly to novel pyridine based nitrogen-sulfur ligands that are suitable for complexing with a radionuclide, and are useful as general imaging agents for diagnostic purposes, novel aminothiol ligands that are suitable for complexing with a radionuclide, and are useful as general imaging agents for diagnostic purposes, and amide-thiolate ligands having improved metal chelate formation kinetics. The amide-thiolate ligands include an amine which converts to a vinylogous amide upon complexation, thereby providing rapid complexation and thermodynamic stability. The ligands may be used for post formed labeling of biological substances for use in the fields of diagnosis and therapy.
摘要翻译：本发明特别涉及适用于与放射性核素络合的新型吡啶类氮硫配体，并且可用作诊断目的的一般成像剂，适于与放射性核素络合的新型氨基硫醇配体，并且可用作一般用于诊断目的的成像剂和具有改善的金属螯合物形成动力学的酰胺 - 硫醇酸配体。酰胺 - 硫醇酸酯配体包括在络合时转化为戊烯酰胺的胺，从而提供快速的络合和热力学稳定性。配体可用于生物物质的后期标记用于诊断和治疗领域。

6. 发明授权

US5653958A Imidazole based nitrogen-sulfur ligands useful in radiographic imaging agents 失效
标题翻译：用于放射成像剂的咪唑基氮硫配体
公开(公告)号：US5653958A
公开(公告)日：1997-08-05
申请号：US419319
申请日：1995-04-10
申请人： Raghavan Rajagopalan , Ananthachari Srinivasan
发明人： Raghavan Rajagopalan , Ananthachari Srinivasan
IPC分类号： C07D233/64 , A61K51/00 , A61K51/04 , C07D233/54 , C07D233/91 , C07D405/12 , C07F13/00
CPC分类号： C07F13/005 , A61K51/0478 , C07D233/64 , C07D405/12 , A61K2123/00
摘要： The present invention relates particularly to novel imidazole based nitrogen-sulfur ligands that are suitable for complexing with a radionuclide, and are useful as general imaging agents for diagnostic purposes.
摘要翻译：本发明特别涉及适用于与放射性核素络合的新型咪唑基氮硫配体，并且可用作用于诊断目的的一般成像剂。

7. 发明申请

US20050191240A1 LABELED NEUROTENSIN DERIVATIVES 失效
标题翻译：标记的神经递质衍生物
公开(公告)号：US20050191240A1
公开(公告)日：2005-09-01
申请号：US10036918
申请日：2001-12-21
申请人： Ananthachari Srinivasan , Jack Erion , Michelle Schmidt
发明人： Ananthachari Srinivasan , Jack Erion , Michelle Schmidt
IPC分类号： A61K38/00 , A61K47/48 , A61K51/00 , A61K51/08 , C07K7/06 , C07K7/08
CPC分类号： A61K51/088 , A61K38/00 , A61K47/6425 , A61K51/085 , C07K7/083
摘要： Peptide analogs of neurotensin are disclosed which are resistant to enzymatic degradation and which retain high binding affinity for neurotensin receptors. Pharmaceutical compositions of these compounds are useful for diagnostic and therapeutic purposes.
摘要翻译：公开了对酶促降解具有抗性并且对神经降压素受体保持高结合亲和力的神经降压素的肽类似物。这些化合物的药物组合物可用于诊断和治疗目的。

8. 发明授权

US5606028A Anchimeric radiometal chelating compounds 失效
标题翻译：嵌合型放射金属螯合化合物
公开(公告)号：US5606028A
公开(公告)日：1997-02-25
申请号：US532041
申请日：1995-09-21
申请人： Alan R. Fritzberg , Ananthachari Srinivasan
发明人： Alan R. Fritzberg , Ananthachari Srinivasan
IPC分类号： A61K51/00 , A61K51/04 , A61K51/10 , C07C313/28 , C07C323/25 , C07C323/41 , C07C323/60 , C07C331/28 , C07K1/113 , C07K5/06 , C07K14/00 , C07K16/00 , C09K3/00 , G01N33/534 , G01N33/60 , C07K17/02 , A61K51/08
CPC分类号： G01N33/534 , A61K51/0478 , A61K51/1093 , C07C313/28 , C07C331/28 , A61K2123/00
摘要： Anchimeric chelates are disclosed which are capable of rapidly forming stable chelates with radionuclide metals at or below physiological temperature. Bifunctional anchimeric chelates having these same properties are also disclosed which are useful for radiolabeling target specific molecules such as monoclonal antibodies and fragments thereof.
摘要翻译：公开了能够在或低于生理温度下用放射性核素金属快速形成稳定的螯合物的嵌合螯合物。还公开了具有这些相同特性的双功能锚定螯合物，其可用于放射性标记靶特异性分子，例如单克隆抗体及其片段。

9. 发明授权

US5283342A Biotinylated small molecules 失效
标题翻译：生物素化小分子
公开(公告)号：US5283342A
公开(公告)日：1994-02-01
申请号：US895588
申请日：1992-06-09
申请人： Linda M. Gustavson , Ananthachari Srinivasan , Alan R. Fritzberg , John M. Reno , Donald B. Axworthy
发明人： Linda M. Gustavson , Ananthachari Srinivasan , Alan R. Fritzberg , John M. Reno , Donald B. Axworthy
IPC分类号： A61K47/48 , A61K51/04 , A61K51/12 , A61K43/00 , A61K49/02 , C07D235/00 , C07D495/04
CPC分类号： B82Y5/00 , A61K47/48146 , A61K47/48353 , A61K47/48707 , A61K47/4873 , A61K47/48753 , A61K51/0497 , A61K51/1268 , A61K2121/00 , A61K2123/00 , Y10S436/804 , Y10S436/808
摘要： Methods, compounds, compositions and kits that relate to pretargeted delivery of diagnostic and therapeutic agents are disclosed. In particular, methods for radiometal labeling of biotin and for improved radiohalogenation of biotin, as well as related compounds, are described.
摘要翻译：公开了与诊断和治疗剂的预靶向递送相关的方法，化合物，组合物和试剂盒。特别地，描述了用于生物素的放射性金属标记和改善生物素的放射性卤化的方法以及相关化合物。

10. 发明授权

US5066789A Targeting substance-diagnostic/therapeutic agent conjugates having Schiff base linkages 失效
标题翻译：具有希夫碱连接的靶向物质 - 诊断/治疗剂缀合物
公开(公告)号：US5066789A
公开(公告)日：1991-11-19
申请号：US415154
申请日：1989-09-29
申请人： Ananthachari Srinivasan , Diana I. Brixner , Vivekananda M. Vrudhula
发明人： Ananthachari Srinivasan , Diana I. Brixner , Vivekananda M. Vrudhula
IPC分类号： A61K47/48 , A61K51/10 , C07D207/40 , C07D207/404 , C07D207/44 , C07D207/452 , C07H15/203 , C07H15/252
CPC分类号： C07D207/404 , A61K47/48338 , A61K47/48715 , A61K51/1093 , C07D207/452 , C07H15/203 , C07H15/252 , A61K2123/00
摘要： Targeting substance-diagnostic/therapeutic agent conjugates joined by stabilized Schiff base or hydrazone linkages are disclosed. In addition, slow release carrier-drug pharmaceuticals are described. The diagnostic and therapeutic conjugates and pharmaceuticals of the present invention provide certain advantages relating to in vivo administration, including controlled release of the active agent at a target site.
摘要翻译：公开了通过稳定的席夫碱或腙键连接的靶向物质 - 诊断/治疗剂缀合物。此外，描述了缓释载体药物药物。本发明的诊断和治疗性缀合物和药物提供与体内施用有关的某些优点，包括活性剂在靶位点的受控释放。

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