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41. 发明申请

US20050036948A1 Radiolabeled annexins 失效
标题翻译：放射性标记的膜联蛋白
公开(公告)号：US20050036948A1
公开(公告)日：2005-02-17
申请号：US10820653
申请日：2004-04-08
申请人： Sudhakar Kasina , John Reno , Louis Theodore
发明人： Sudhakar Kasina , John Reno , Louis Theodore
IPC分类号： A61K47/48 , A61K51/08 , C07K1/13 , C07K7/06 , C07K14/47 , G01N33/53 , A61K49/00 , G01N33/567
CPC分类号： C07K7/06 , A61K47/54 , A61K47/547 , A61K47/549 , A61K51/087 , A61K51/088 , A61K2123/00 , C07K1/13 , C07K14/4721
摘要： Radiolabeled annexin and modified annexin conjugates useful for imaging vascular thrombi are described. Methods for making and using such radiolabeled annexin conjugates are also provided.
摘要翻译：描述了可用于成像血管血栓的放射性标记的膜联蛋白和修饰的膜联蛋白缀合物。还提供了制备和使用这种放射性标记的膜联蛋白缀合物的方法。

42. 发明授权

US5405966A Trichothecene conjugates 失效
标题翻译：三氯乙烯共轭物
公开(公告)号：US5405966A
公开(公告)日：1995-04-11
申请号：US73118
申请日：1993-06-07
申请人： Louis J. Theodore , John M. Reno , Sudhakar Kasina , James A. Sanderson , Paul G. Abrams
发明人： Louis J. Theodore , John M. Reno , Sudhakar Kasina , James A. Sanderson , Paul G. Abrams
IPC分类号： A61K31/35 , A61K31/365 , A61K47/48 , G01N33/532 , C07D209/76
CPC分类号： A61K31/365 , A61K31/35 , A61K47/48492 , G01N33/532
摘要： Conjugates of trichothecenes and agents that bind to a defined population of cells are disclosed. Preferred are conjugates of trichothecene molecules with polyclonal or monoclonal antibodies or fragments thereof that recognize antigens that are present only on tumor cells or are augmented in their expression on tumor cells as compared to normal tissues. Trichothecene molecules are coupled to the agent through non-covalent and covalent linkages, such as peptide bonds, disulfide bonds, thioester bonds, or thioether bonds. A method for inhibiting the growth and metabolism of antigen-positive cells is also disclosed. Derivatized trichothecene compounds prepared for conjugation to targeting agents are also disclosed.
摘要翻译：公开了与定义的细胞群结合的单端孢霉烯和试剂的缀合物。优选的是头孢霉烯分子与多克隆或单克隆抗体或其片段的缀合物，其识别仅存在于肿瘤细胞上的抗原，或者与正常组织相比增强其在肿瘤细胞上的表达。三氯甲炔类分子通过非共价键和共价键（如肽键，二硫键，硫酯键或硫醚键）与试剂偶联。还公开了抑制抗原阳性细胞生长和代谢的方法。还公开了制备用于与靶向剂缀合的衍生化的单端孢霉烯化合物。

43. 发明授权

US4980147A Radiolabeled technetium chelates for use in renal function determinations 失效
标题翻译：放射性标记的锝螯合物用于肾功能测定
公开(公告)号：US4980147A
公开(公告)日：1990-12-25
申请号：US733481
申请日：1985-05-14
申请人： Alan Fritzberg , Sudhakar Kasina , Dennis L. Johnson
发明人： Alan Fritzberg , Sudhakar Kasina , Dennis L. Johnson
IPC分类号： A61K51/00 , A61K51/08 , C07C233/56 , C07C237/22 , C07C309/15 , C07C311/45 , C07C323/60 , C07F13/00 , C07K5/02
CPC分类号： C07C233/56 , A61K51/0478 , A61K51/08 , C07F13/005 , C07K5/0202 , A61K2123/00 , Y02P20/55
摘要： The present invention is directed to novel radiopharmaceutical imaging agents incorporating Tc-99m as a radiolabel. In particular, the novel imaging agents disclosed herein have relatively high renal extraction efficiencies, and hence are useful for conducting renal function imaging procedures. The novel Tc-99m compounds of a present invention have the following general formula: ##STR1## wherein X is S or N; and wherein Y is--H or wherein Y is ##STR2## and where R.sub.1 is --H, --CH.sub.3, or --CH.sub.2 CH.sub.3 ; R.sub.2 is --H, --CH.sub.2 CO.sub.2 H, --CH.sub.2 CONH.sub.2, --CH.sub.2 CH.sub.2 CO.sub.2 H, --CH.sub.2 CH.sub.2 CONH.sub.2, --CH.sub.3, --CH.sub.2 CH.sub.3, CH.sub.2 C.sub.6 H.sub.5, or --CH.sub.2 OH; and Z is --H, --CO.sub.2 H, --CONH.sub.2, --SO.sub.3 H, --SO.sub.2 NH.sub.2, or --CONHCH.sub.2 CO.sub.2 H; and the Tc is Tc-99m; and water-soluble salts thereof. Of the foregoing, the presently preferred Tc-99m compound of the present invention is Tc-99m-mercaptoacetylglycylglycylglycine (Tc-99m-MAGGG). The present invention is also directed to novel chelating agents that may be reacted with Tc-99m to form the foregoing compounds. Such novel chelating agents have the following general formula. ##STR3## where X and Y have the same definitions as above, and wherein Y' is --H.sub.2 when X is N, or wherein Y' is --H, or a suitable protective group such as --COCH.sub.3, --COC.sub.6 H.sub.5, --CH.sub.2 NHCOCH.sub.3, --COCF.sub.3, or --COCH.sub.2 OH when X is S. The present invention also provides methods for preparing and using the novel Tc-99m compounds.
摘要翻译：本发明涉及包含Tc-99m作为放射性标记的新型放射性药物显像剂。特别地，本文公开的新型成像剂具有相对高的肾提取效率，因此可用于进行肾功能成像过程。本发明的新型Tc-99m化合物具有以下通式：其中X为S或N; 并且其中Y是-H或其中Y是＆lt; IMAGE＆gt;其中R 1是-H，-CH 3或-CH 2 CH 3; R2是-H，-CH2CO2H，-CH2CONH2，-CH2CH2CO2H，-CH2CH2CONH2，-CH3，-CH2CH3，CH2C6H5或-CH2OH; Z是-H，-CO 2 H，-CONH 2，-SO 3 H，-SO 2 NH 2或-CONHCH 2 CO 2 H; Tc为Tc-99m; 及其水溶性盐。在上述中，本发明优选的Tc-99m化合物是Tc-99m-巯基乙酰基甘氨酰甘氨酰甘氨酸（Tc-99m-MAGGG）。本发明还涉及可与Tc-99m反应形成前述化合物的新型螯合剂。这种新型螯合剂具有以下通式。其中X和Y具有与上述相同的定义，并且其中当X是N时Y'是-H2，或其中Y'是-H，或合适的保护基如-COCH 3，-COC 6 H 5，-CH 2 NHCOCH 3， -COCF 3或-COCH 2 OH。本发明还提供了制备和使用新型Tc-99m化合物的方法。

44. 发明授权

US08143237B2 Anti-cancer drugs, and uses relating for malignant melanoma and other cancers 有权
标题翻译：抗癌药物，以及与恶性黑素瘤和其他癌症相关的用途
公开(公告)号：US08143237B2
公开(公告)日：2012-03-27
申请号：US12767647
申请日：2010-04-26
申请人： Ganga Raju Gokaraju , Sudhakar Kasina , Rama Raju Gokaraju , Venkata Kanaka Ranga Raju Gokaraju , Venkateswarlu Somepalli , Trimurtulu Golakoti , Kiran Bhupathiraju , Sengupta Krishanu , Venkata Krishna Raju Alluri
发明人： Ganga Raju Gokaraju , Sudhakar Kasina , Rama Raju Gokaraju , Venkata Kanaka Ranga Raju Gokaraju , Venkateswarlu Somepalli , Trimurtulu Golakoti , Kiran Bhupathiraju , Sengupta Krishanu , Venkata Krishna Raju Alluri
IPC分类号： C07D517/04 , A61K31/53 , A61K31/655 , A61P31/00
CPC分类号： A61K31/655 , A61K38/193 , A61K38/20 , A61K38/21 , A61K45/06 , C07D253/04 , C07D517/14 , A61K2300/00
摘要： Selenopheno triazene analogs, their compositions, tautomeric forms, stereoisomers, polymorphs, hydrates, solvates, and pharmaceutically acceptable salts and mixtures thereof are useful for the treatment of metastatic malignant melanoma and other cancers. The selenopheno triazene analogs have the general formulae (I) or (II): wherein the substituents R1, R2, R3, R6, and R7 are as described in the specification. Other cancers include which may be treated with these compounds include, but are not limited to, malignant melanoma, leukemia, lymphomas (Hodgkins and non-Hodgkins), sarcomas (Ewing's sarcoma), brain tumors, central nervous system (CNS) metastases, gliomas, carcinomas such as breast cancer, prostate cancer, lung cancer (small cell and non-small cell), colon cancer, pancreatic cancer, Head and Neck cancers and oropharyngeal squamous cell carcinoma.
摘要翻译：硒代苯三氮烯类似物，它们的组合物，互变异构形式，立体异构体，多晶型物，水合物，溶剂合物及其药学上可接受的盐和混合物可用于治疗转移性恶性黑素瘤和其它癌症。硒代苯并三氮烯类似物具有通式（I）或（II）：其中取代基R 1，R 2，R 3，R 6和R 7如说明书中所述。可以用这些化合物治疗的其它癌症包括但不限于恶性黑素瘤，白血病，淋巴瘤（霍奇金淋巴瘤和非霍奇金淋巴瘤），肉瘤（尤文氏肉瘤），脑肿瘤，中枢神经系统（CNS）转移瘤，胶质瘤，癌症如乳腺癌，前列腺癌，肺癌（小细胞和非小细胞），结肠癌，胰腺癌，头颈部癌症和口咽鳞状细胞癌。

45. 发明授权

US07674886B2 Bridged aromatic substituted amine ligands with donor atoms 失效
标题翻译：具有供体原子的桥连的芳族取代的胺配体
公开(公告)号：US07674886B2
公开(公告)日：2010-03-09
申请号：US11849769
申请日：2007-09-04
申请人： Sudhakar Kasina
发明人： Sudhakar Kasina
IPC分类号： A61K51/04
CPC分类号： C07F13/005 , A61K51/04 , A61K51/0478 , A61K51/0482 , A61K51/0489 , A61K51/0497 , A61K51/087 , A61K51/088 , C07B2200/05 , C07C229/16 , C07C323/34 , C07D257/10 , C07D265/32 , C07D285/00 , C07D333/36 , C07D495/04 , C07D495/14 , C07F9/3817 , C07F9/6524 , C07F9/655345 , C07F9/6561
摘要： The present invention provides for substituted metal chelating compounds in which at least two of the chelating atoms are nitrogen which are directly attached to aromatic rings and one or more of those nitrogen atoms has attached thereto a substituent other than hydrogen, and methods for making and using these compounds.
摘要翻译：本发明提供了取代的金属螯合化合物，其中至少两个螯合原子是直接连接到芳环上的氮，并且一个或多个这些氮原子连接有除氢之外的取代基，以及制备和使用方法这些化合物。

46. 发明授权

US07268220B2 Bridged aromatic substituted amine ligands with donor atoms 失效
标题翻译：具有供体原子的桥连的芳族取代的胺配体
公开(公告)号：US07268220B2
公开(公告)日：2007-09-11
申请号：US11061110
申请日：2005-02-18
申请人： Sudhakar Kasina
发明人： Sudhakar Kasina
IPC分类号： C07F13/00
CPC分类号： C07F13/005 , A61K51/04 , A61K51/0478 , A61K51/0482 , A61K51/0489 , A61K51/0497 , A61K51/087 , A61K51/088 , C07B2200/05 , C07C229/16 , C07C323/34 , C07D257/10 , C07D265/32 , C07D285/00 , C07D333/36 , C07D495/04 , C07D495/14 , C07F9/3817 , C07F9/6524 , C07F9/655345 , C07F9/6561
摘要： The present invention provides for substituted metal chelating compounds in which at least two of the chelating atoms are nitrogen which are directly attached to aromatic rings and one or more of those nitrogen atoms has attached thereto a substituent other than hydrogen, and methods for making and using these compounds.
摘要翻译：本发明提供了取代的金属螯合化合物，其中至少两个螯合原子是直接连接到芳环上的氮，并且一个或多个这些氮原子连接有除氢之外的取代基，以及制备和使用方法这些化合物。

47. 发明授权

US07115248B2 Radiolabeled annexins 失效
公开(公告)号：US07115248B2
公开(公告)日：2006-10-03
申请号：US10820653
申请日：2004-04-08
申请人： Sudhakar Kasina , John M Reno , Louis J Theodore
发明人： Sudhakar Kasina , John M Reno , Louis J Theodore
IPC分类号： A61K51/00 , A61M36/14
CPC分类号： C07K7/06 , A61K47/54 , A61K47/547 , A61K47/549 , A61K51/087 , A61K51/088 , A61K2123/00 , C07K1/13 , C07K14/4721
摘要： Radiolabeled annexin and modified annexin conjugates useful for imaging vascular thrombi are described. Methods for making and using such radiolabeled annexin conjugates are also provided.

48. 发明申请

US20050276754A1 Bridged aromatic substituted amine ligands with donor atoms 失效
公开(公告)号：US20050276754A1
公开(公告)日：2005-12-15
申请号：US11061110
申请日：2005-02-18
申请人： Sudhakar Kasina
发明人： Sudhakar Kasina
IPC分类号： A61K51/00 , A61K51/04 , A61K51/08 , A61P35/00 , C07C229/16 , C07C229/18 , C07C323/34 , C07D257/10 , C07D265/32 , C07D285/00 , C07D333/36 , C07D495/04 , C07D495/14 , C07F5/00 , C07F9/22 , C07F9/38 , C07F9/6524 , C07F9/6553 , C07F9/6561 , C07F13/00
CPC分类号： C07F13/005 , A61K51/04 , A61K51/0478 , A61K51/0482 , A61K51/0489 , A61K51/0497 , A61K51/087 , A61K51/088 , C07B2200/05 , C07C229/16 , C07C323/34 , C07D257/10 , C07D265/32 , C07D285/00 , C07D333/36 , C07D495/04 , C07D495/14 , C07F9/3817 , C07F9/6524 , C07F9/655345 , C07F9/6561
摘要： The present invention provides for substituted metal chelating compounds in which at least two of the chelating atoms are nitrogen which are directly attached to aromatic rings and one or more of those nitrogen atoms has attached thereto a substituent other than hydrogen, and methods for making and using these compounds.

49. 发明授权

US06528627B1 Bridged aromatic substituted amine ligands with donor atoms 失效
公开(公告)号：US06528627B1
公开(公告)日：2003-03-04
申请号：US09724834
申请日：2000-11-28
申请人： Sudhakar Kasina
发明人： Sudhakar Kasina
IPC分类号： C07F938
CPC分类号： C07F13/005 , A61K51/04 , A61K51/0478 , A61K51/0482 , A61K51/0489 , A61K51/0497 , A61K51/087 , A61K51/088 , C07B2200/05 , C07C229/16 , C07C323/34 , C07D257/10 , C07D265/32 , C07D285/00 , C07D333/36 , C07D495/04 , C07D495/14 , C07F9/3817 , C07F9/6524 , C07F9/655345 , C07F9/6561
摘要： The present invention provides for substituted metal chelating compounds in which at least two of the chelating atoms are nitrogen which are directly attached to aromatic rings and one or more of those nitrogen atoms has attached thereto a substituent other than hydrogen, and methods for making and using these compounds.

50. 发明授权

US6024937A Aromatic amine substituted bridged nitrogen and sulfur donor atom ligands for imaging 失效
标题翻译：用于成像的芳族胺取代的桥连氮和硫供体原子配体
公开(公告)号：US6024937A
公开(公告)日：2000-02-15
申请号：US463232
申请日：1995-06-05
申请人： Sudhakar Kasina , Eric Yau , John M. Reno
发明人： Sudhakar Kasina , Eric Yau , John M. Reno
IPC分类号： C07D239/42 , A61K51/00 , A61K51/04 , C07B59/00 , C07C211/50 , C07C211/53 , C07C229/56 , C07C229/60 , C07C229/64 , C07C229/76 , C07C233/43 , C07C239/16 , C07C239/18 , C07C255/24 , C07C271/20 , C07C319/00 , C07C323/34 , C07C323/63 , C07D213/00 , C07D257/10 , C07D285/00 , C07D513/04 , C07F1/08 , C07F1/12 , C07F7/24 , C07F9/94 , C07F13/00 , C07F15/00 , C07D39/02
CPC分类号： C07C211/50 , A61K51/0478 , C07C229/60 , C07C229/64 , C07C233/43 , C07C239/16 , C07C239/18 , C07C323/34 , C07C323/63 , C07D257/10 , C07D285/00 , C07D513/04 , A61K2121/00 , A61K2123/00
摘要： The present invention provides aromatic amine substituted metal chelating compounds, chelates and chelate-targeting moiety conjugates formed from the chelating compounds, and methods for making and using these compounds. Metals capable of being chelated by the chelating compounds include radionuclides, such as .sup.99m Tc and .sup.186188 Re.
摘要翻译：本发明提供由螯合化合物形成的芳族胺取代的金属螯合化合物，螯合物和螯合靶向部分缀合物，以及制备和使用这些化合物的方法。能够被螯合化合物螯合的金属包括放射性核素，例如99mTc和186188Re。

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