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1. 发明专利

CA2031528A1 RADIONUCLIDE METAL CHELATES FOR THE RADIOLABELING OF PROTEINS 未知
公开(公告)号：CA2031528A1
公开(公告)日：1990-12-17
申请号：CA2031528
申请日：1990-06-15
申请人： GUSTAVSON LINDA M , SRINIVASAN ANANTHACHARI , KASINA SUDHAKER , FRITZBERG ALAN R
发明人： GUSTAVSON LINDA M , SRINIVASAN ANANTHACHARI , KASINA SUDHAKER , FRITZBERG ALAN R
IPC分类号： C07D307/18 , A61K39/395 , A61K51/00 , A61K51/10 , C07C323/60 , C07D263/26 , C07D309/08 , C07D327/04 , C07F13/00 , C07K5/06 , C07K14/705 , C07K14/715 , C07K16/00

2. 发明专利

AU6338000A Labeled neurotensin derivatives 未知
公开(公告)号：AU6338000A
公开(公告)日：2001-01-09
申请号：AU6338000
申请日：2000-06-22
申请人： ERION JACK L , MALLINCKRODT INC , SCHMIDT MICHELLE A , SRINIVASAN ANANTHACHARI
发明人： SRINIVASAN ANANTHACHARI , ERION JACK L , SCHMIDT MICHELLE A
IPC分类号： A61K38/00 , A61K47/48 , A61K51/00 , A61K51/08 , C07K7/06 , C07K7/08 , C07K7/00
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.

3. 发明申请

WO0078796A3 LABELED NEUROTENSIN DERIVATIVES WITH IMPROVED RESISTANCE TO ENZYMATIC DEGRADATION 审中-公开
标题翻译：标记的神经递质衍生物具有改善的抗酶降解能力
公开(公告)号：WO0078796A3
公开(公告)日：2001-05-17
申请号：PCT/US0017509
申请日：2000-06-22
申请人： MALLINCKRODT INC , SRINIVASAN ANANTHACHARI , ERION JACK L , SCHMIDT MICHELLE A
发明人： SRINIVASAN ANANTHACHARI , ERION JACK L , SCHMIDT MICHELLE A
IPC分类号： A61K38/00 , A61K47/48 , A61K51/00 , A61K51/08 , C07K7/06 , C07K7/08 , G01N33/68
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。

4. 发明申请

WO0018440A9 SOMATOSTATIN RECEPTOR RADIOLIGAND WITH INCREASED UPTAKE 审中-公开
公开(公告)号：WO0018440A9
公开(公告)日：2000-10-12
申请号：PCT/US9922337
申请日：1999-09-24
申请人： MALLINCKRODT INC , JONG MARION DE , BREEMAN WOUT A , VISSER THEOFILUS JOHANNES , KRENNING ERIC PAUL , SRINIVASAN ANANTHACHARI
发明人： DE JONG MARION , BREEMAN WOUT A , VISSER THEOFILUS JOHANNES , KRENNING ERIC PAUL , SRINIVASAN ANANTHACHARI
IPC分类号： G01N33/534 , A61K47/48 , A61K51/00 , A61K51/08 , A61P35/00 , C07K7/06 , C07K7/08 , C07K14/00 , C07K14/575 , G01N33/566
CPC分类号： A61K51/088 , A61K51/083
摘要： A radioligand comprising a peptide capable of binding to a receptor wherein the peptide is coupled to at least one chelating agent, which chelating agent is not coordinated to a metal ion under physiological conditions and a composition comprising said radioligand as a diagnostic or pharmaceutical and a kit for the detection of receptors.

5. 发明申请

WO9747329A2 RADIOPHARMACEUTICAL COMPOSITIONS CAPABLE OF LOCALIZING AT SITES OF THROMBUS 审中-公开
标题翻译：放射性物质组合物可以在THROMBUS的位点定位
公开(公告)号：WO9747329A2
公开(公告)日：1997-12-18
申请号：PCT/US9709292
申请日：1997-06-05
申请人： SEARLE & CO , MALLINCKRODT MEDICAL INC , FEIGEN LARRY P , FLYNN DANIEL LEE , NEEDLEMAN PHILIP , SRINIVASAN ANANTHACHARI , ZABLOCKI JEFFERY ALAN
发明人： FEIGEN LARRY P , FLYNN DANIEL LEE , NEEDLEMAN PHILIP , SRINIVASAN ANANTHACHARI , ZABLOCKI JEFFERY ALAN
IPC分类号： A61K38/00 , A61K51/00 , A61K51/08 , C07K5/072 , A61K51/58
CPC分类号： C07K5/06113 , A61K51/088 , A61K2121/00 , A61K2123/00
摘要： A radiopharmaceutical capable of localizing at a site of thrombus containing activated platelets within a mammalian body is provided wherein the radiopharmaceutical comprises a linear peptidomimetic containing ligand capable of specifically binding to the GPIIb/IIIa integrin receptor of platelets in the thrombus and a radionuclide covalently bound to the peptidomimetic containing ligand. The ligand compositions of the invention are provided complexed with a selected metal radionuclide to form a diagnostic or therapeutic radiopharmaceutical to image a site of thrombus or provide radiotherapy to the site of thrombus, respectively. Methods of imaging a site of thrombus in a mammalian body by administering a diagnostically effective amount of the radiopharmaceutical composition of this invention complexed with a selected diagnostic metal radionuclide and methods of providing therapy to a site of thrombus in a mammalian body by administering a therapeutically effective amount of the radiopharmaceutical composition of this invention complexed with a selected therapeutic metal radionuclide are also provided as well as kits for preparing such radiopharmaceutical compositions.
摘要翻译：提供能够定位在哺乳动物体内含有活化血小板的血栓部位的放射性药物，其中放射性药物包含能够特异性结合血栓中血小板的GPIIb / IIIa整联蛋白受体的线性拟肽含量配体和共价结合的放射性核素含拟肽的配体。提供本发明的配体组合物与所选择的金属放射性核素复合以形成诊断或治疗性放射性药物以分别对血栓位点成像或向血栓部位提供放射治疗。通过施用诊断上有效量的本发明的放射性药物组合物与选定的诊断性金属放射性核素复合而在哺乳动物体内成像血栓位点的方法和通过施用治疗有效的方法向哺乳动物体内的血栓位点提供治疗还提供了与选定的治疗性金属放射性核素复合的本发明的放射性药物组合物的量以及用于制备这种放射性药物组合物的试剂盒。

6. 发明申请

WO0220610A2 CONFORMATIONALLY CONSTRAINED LABELED PEPTIDES FOR IMAGING AND THERAPY 审中-公开
标题翻译：用于成像和治疗的一致的约束标签肽
公开(公告)号：WO0220610A2
公开(公告)日：2002-03-14
申请号：PCT/US0127708
申请日：2001-09-07
申请人： MALLINCKRODT INC , SCHMIDT MICHELLE A , ERION JACK L , SRINIVASAN ANANTHACHARI
发明人： SCHMIDT MICHELLE A , ERION JACK L , SRINIVASAN ANANTHACHARI
IPC分类号： A61K38/00 , A61K47/48 , A61K49/00 , A61K51/08 , C07K7/06 , C07K14/655 , A61K38/08 , A61K38/22 , C07K14/575
CPC分类号： C07K7/06 , A61K38/00 , A61K47/6425 , A61K49/0002 , A61K51/083 , A61K51/088 , C07K14/6555
摘要： Conformational constraints in diagnostic and therapeutic agents in peptides have been introduced by utilization of disulfide bonds and amide cyclizations. These constraints are responsible for altering the stability and specificity of these receptor-targeted agents. Conformationally constrained peptides containing secondary and primary amines, ethers, thioethers, amidines, esters and other functionalities have been synthesized. Methods are disclosed which incorporate multiple features of the above functionalities in the macrocyclic ring of the peptides.
摘要翻译：已经通过利用二硫键和酰胺环化引入肽中诊断和治疗剂中的构象约束。这些限制是改变这些受体靶向药物的稳定性和特异性的原因。已经合成了含有仲胺和伯胺，醚，硫醚，脒，酯和其他官能团的构象约束肽。公开了在肽的大环中并入上述功能的多个特征的方法。

7. 发明申请

WO0018440A8 SOMATOSTATIN RECEPTOR RADIOLIGAND WITH INCREASED UPTAKE 审中-公开
标题翻译：增加摄入的生长抑素受体RADIOLIGAND
公开(公告)号：WO0018440A8
公开(公告)日：2000-08-24
申请号：PCT/US9922337
申请日：1999-09-24
申请人： MALLINCKRODT INC , JONG MARION DE , BREEMAN WOUT A , VISSER THEOFILUS JOHANNES , KRENNING ERIC PAUL , SRINIVASAN ANANTHACHARI
发明人： DE JONG MARION , BREEMAN WOUT A , VISSER THEOFILUS JOHANNES , KRENNING ERIC PAUL , SRINIVASAN ANANTHACHARI
IPC分类号： G01N33/534 , A61K47/48 , A61K51/00 , A61K51/08 , A61P35/00 , C07K7/06 , C07K7/08 , C07K14/00 , C07K14/575 , G01N33/566
CPC分类号： A61K51/088 , A61K51/083
摘要： A radioligand comprising a peptide capable of binding to a receptor wherein the peptide is coupled to at least one chelating agent, which chelating agent is not coordinated to a metal ion under physiological conditions and a composition comprising said radioligand as a diagnostic or pharmaceutical and a kit for the detection of receptors.
摘要翻译：包含能够与受体结合的肽的放射性配体，其中所述肽与至少一种螯合剂偶联，所述螯合剂在生理条件下不与金属离子配位，并且包含所述放射性配体作为诊断剂或药物的组合物和试剂盒用于检测受体。

8. 发明申请

WO0152898A9 METHODS FOR INCORPORATING METAL CHELATORS AT CARBOXYL-TERMINAL SITE OF PEPTIDES 审中-公开
标题翻译：金属螯合剂在羧酸酯终端位置的方法
公开(公告)号：WO0152898A9
公开(公告)日：2002-10-31
申请号：PCT/US0101640
申请日：2001-01-18
申请人： MALLINCKRODT INC , ACHILEFU SAMUEL I , SRINIVASAN ANANTHACHARI
发明人： ACHILEFU SAMUEL I , SRINIVASAN ANANTHACHARI
IPC分类号： A61K47/48 , A61K49/14 , A61K51/08
CPC分类号： A61K49/085 , A61K47/62 , A61K49/14 , A61K51/083 , A61K51/088
摘要： Methods for incorporating metal chelators at carboxyl-terminal sites of peptides are presented. In a first method, a metal chelator which is a polyazacarboxylate with two free carboxyl groups is attached to a functionalized resin via one carboxyl group and to a diamine or orthogonally protected diamine via a second carboxyl group. The protecting group is removed and a sequence of amino acids is added to the diamine residue on solid support to form the desired peptide. After addition of the amino acid or peptide, the compound is cleaved from the resin and blocking groups are removed. In a second method, an orthogonally protected polyazacarboxylate with a free carboxyl and protected amine groups is reacted with a functionalized resin. The amine protecting group is removed and amino acids are added to obtain the desired peptide. The compound is then cleaved from the resin and blocking groups are removed. The cleavage from the resin and removal of blocking groups can be performed simultaneously.
摘要翻译：介绍了在肽的羧基末端位点掺入金属螯合剂的方法。在第一种方法中，具有两个游离羧基的多偶氮羧酸盐的金属螯合剂通过一个羧基连接到官能化树脂上，并通过第二个羧基连接到二胺或正交保护的二胺上。除去保护基，并将一系列氨基酸加入到固体支持物上的二胺残基中以形成所需的肽。加入氨基酸或肽后，从树脂中切下化合物，除去封闭基团。在第二种方法中，将具有游离羧基和被保护的胺基的正交保护的聚阿拉伯羧酸酯与官能化树脂反应。除去胺保护基，并加入氨基酸以获得所需的肽。然后将化合物从树脂上切下，除去封闭基团。可以同时进行与树脂的切割和去除封闭基团。

9. 发明申请

WO9962563A3 RADIOLABELED PEPTIDES FOR THE DIAGNOSIS AND TREATMENT OF BREAST AND PROSTATE TUMORS AND METASTASES OF SUCH TUMORS 审中-公开
标题翻译：用于诊断和治疗乳腺和前列腺肿瘤和这种肿瘤的化学物质的放射性肽
公开(公告)号：WO9962563A3
公开(公告)日：2000-02-10
申请号：PCT/US9912414
申请日：1999-06-03
申请人： MALLINCKRODT INC , REUBI JEAN CLAUDE , BREEMAN WOUT A , SRINIVASAN ANANTHACHARI
发明人： REUBI JEAN-CLAUDE , BREEMAN WOUT A , SRINIVASAN ANANTHACHARI
IPC分类号： A61K51/00 , A61K38/00 , A61P35/00 , C07K2/00 , C07K7/02 , C07K7/08 , A61K51/08 , G01N33/68
CPC分类号： C07K7/086 , A61K38/00
摘要： Breast and/or prostate cancer is diagnosed and/or treated with a radiolabeled peptide or peptidomimetic that binds to GRP (Gastrin Releasing Peptide) receptors.
摘要翻译：用与GRP（胃泌素释放肽）受体结合的放射性标记肽或肽模拟物诊断和/或治疗乳腺和/或前列腺癌。

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