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51. 发明申请

US20100272678A1 ANTI-CANCER DRUGS, AND USES RELATING FOR MALIGNANT MELANOMA AND OTHER CANCERS 有权
标题翻译：抗癌药物及其与恶性肿瘤及其他癌症有关的用途
公开(公告)号：US20100272678A1
公开(公告)日：2010-10-28
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： A61K38/20 , C07C245/12 , A61K31/655 , A61K33/24 , A61K39/395 , A61K38/21 , A61K38/19 , A61P35/00
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。

52. 发明授权

US07608242B2 Peptide-chelate conjugates 失效
标题翻译：肽 - 螯合物
公开(公告)号：US07608242B2
公开(公告)日：2009-10-27
申请号：US10469801
申请日：2002-03-01
申请人： Alan Cuthbertson , Marivi Mendizabal , Mark Dixon , Anthony E. Storey , Edward R. Bacon , Vinay Chandrakant Desai , Sudhakar Kasina , Henry Raphael Wolfe
发明人： Alan Cuthbertson , Marivi Mendizabal , Mark Dixon , Anthony E. Storey , Edward R. Bacon , Vinay Chandrakant Desai , Sudhakar Kasina , Henry Raphael Wolfe
IPC分类号： A61K51/00 , A61M36/14
CPC分类号： C07K7/06 , A61K51/088 , C07K14/245 , G01N33/57419
摘要： A peptide-chelate conjugate with affinity for the ST receptor is disclosed, wherein the chelate is tetradentate. The peptide-chelate conjugate of the invention may be labelled with a radiometal to provide a metal complex. A radiopharmaceutical composition comprising the metal complex is provided. which is suitable for the diagnostic imaging of colorectal cancer. Also provided for in the invention is a kit for the preparation of the radiopharmaceutical preparation.
摘要翻译：公开了对ST受体具有亲和性的肽 - 螯合物缀合物，其中螯合物是四齿酸盐。本发明的肽 - 螯合物缀合物可用放射性金属标记以提供金属络合物。提供了包含金属络合物的放射性药物组合物。这适用于结肠直肠癌的诊断成像。本发明还提供了用于制备放射性药物制剂的试剂盒。

53. 发明申请

US20080227961A1 BRIDGED AROMATIC SUBSTITUTED AMINE LIGANDS WITH DONOR ATOMS 失效
标题翻译：桥梁采用芳香取代的氨基配位体
公开(公告)号：US20080227961A1
公开(公告)日：2008-09-18
申请号：US11849769
申请日：2007-09-04
申请人： Sudhakar Kasina
发明人： Sudhakar Kasina
IPC分类号： C07F13/00 , C07F9/38 , C07D487/00 , C07C55/00
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。

54. 发明申请

US20060084696A1 Compounds and therapies for the prevention of vascular and non-vascular pathologies 失效
公开(公告)号：US20060084696A1
公开(公告)日：2006-04-20
申请号：US11270185
申请日：2005-11-09
申请人： David Grainger , James Metcalfe , Sudhakar Kasina
发明人： David Grainger , James Metcalfe , Sudhakar Kasina
IPC分类号： A61K31/381 , A61K31/275
CPC分类号： A61K31/275 , A61K31/381 , C07D333/38 , G01N33/74 , G01N2333/495 , G01N2333/71 , G01N2800/108 , G01N2800/323
摘要： The invention provides a method of treating a mammal having, or at risk of, an indication associated with a TGF-beta deficiency comprising administering one or more agents that is effective to elevate the level of TGF-beta. The invention also provides novel compounds that elevate TGF-beta levels, as well as pharmaceutical compositions comprising compounds that elevate TGF-beta levels, and methods for detecting diseases associated with endothelial cell activation.

55. 发明申请

US20060029545A1 Radiolabeled annexins 失效
公开(公告)号：US20060029545A1
公开(公告)日：2006-02-09
申请号：US11236272
申请日：2005-09-27
申请人： Sudhakar Kasina , Alan Fritzberg , Jonathan Tait , John Reno
发明人： Sudhakar Kasina , Alan Fritzberg , Jonathan Tait , John Reno
IPC分类号： A61K51/00 , C07K14/47
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.

56. 发明申请

US20050020667A1 Compounds and therapies for the prevention of vascular and non-vascular pathologies 失效
标题翻译：用于预防血管和非血管病变的化合物和疗法
公开(公告)号：US20050020667A1
公开(公告)日：2005-01-27
申请号：US10827602
申请日：2004-04-19
申请人： David Grainger , James Metcalfe , Sudhakar Kasina
发明人： David Grainger , James Metcalfe , Sudhakar Kasina
IPC分类号： A61K31/381 , C07D333/38 , G01N33/74 , A61K31/4025 , A61K31/34 , A61K31/38
CPC分类号： A61K31/275 , A61K31/381 , C07D333/38 , G01N33/74 , G01N2333/495 , G01N2333/71 , G01N2800/108 , G01N2800/323
摘要： The invention provides a method of treating a mammal having, or at risk of, an indication associated with a TGF-beta deficiency comprising administering one or more agents that is effective to elevate the level of TGF-beta. The invention also provides novel compounds that elevate TGF-beta levels, as well as pharmaceutical compositions comprising compounds that elevate TGF-beta levels, and methods for detecting diseases associated with endothelial cell activation.
摘要翻译：本发明提供了治疗具有或具有与TGF-β缺乏相关的指征的哺乳动物的方法，包括施用一种或多种有效提高TGF-β水平的试剂。本发明还提供了提高TGF-β水平的新化合物，以及包含提高TGF-β水平的化合物的药物组合物，以及用于检测与内皮细胞活化相关的疾病的方法。

57. 发明授权

US06534037B1 Non-steroidal compounds for steroid receptors and uses relating thereto 失效
标题翻译：用于类固醇受体的非类固醇化合物及其相关用途
公开(公告)号：US06534037B1
公开(公告)日：2003-03-18
申请号：US09644186
申请日：2000-08-22
申请人： Sudhakar Kasina , D. Mark Gleave
发明人： Sudhakar Kasina , D. Mark Gleave
IPC分类号： A61K4900
CPC分类号： A61K51/0493
摘要： Steroid receptor analogs having good binding affinity for steroid receptors and “binding arms” for chelation to metal species such as radionuclides are prepared with all carbon backbones. The analogs very closely approximate the geometries present in natural steroids which are important for effective binding to receptor sites. In addition, metal species binding arms are strategically incorporated into the analog structure in a manner that does not disrupt the analog's receptor binding efficacy. Furthermore, the metal species binding arms may be designed to chelate one or more radionuclides, including radionuclides effective in diagnostic or therapeutic applications. With incorporation of an appropriate steroid receptor binding group, these metal species-bound analogs may be used, for example, to bind androgen receptor sites in the diagnosis or treatment of prostate cancer, or estrogen receptor sites in the diagnosis or treatment of breast and ovarian cancers.
摘要翻译：对于类固醇受体具有良好的结合亲和力的类固醇受体类似物和用于螯合金属物质如放射性核素的“结合臂”用所有碳骨架制备。类似物非常接近存在于天然类固醇中的几何形状，其对于有效结合受体位点是重要的。此外，金属物质结合臂以不破坏类似物的受体结合功效的方式战略性地并入到类似物结构中。此外，金属物质结合臂可以设计成螯合一种或多种放射性核素，包括在诊断或治疗应用中有效的放射性核素。通过掺入适当的类固醇受体结合基团，可以使用这些金属物质结合的类似物，例如在诊断或治疗乳腺和卵巢中的前列腺癌或雌激素受体位点的诊断或治疗中结合雄激素受体位点癌症

58. 发明授权

US6005083A Bridged aromatic substituted amine ligands with donor atoms 失效
公开(公告)号：US6005083A
公开(公告)日：1999-12-21
申请号：US829533
申请日：1997-03-28
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 , C07F9/30
CPC分类号： C07F13/005 , A61K51/04 , A61K51/0478 , A61K51/0482 , A61K51/0489 , A61K51/0497 , A61K51/087 , A61K51/088 , C07C229/16 , C07C323/34 , C07D257/10 , C07D265/32 , C07D285/00 , C07D333/36 , C07D495/04 , C07D495/14 , C07F9/3817 , C07F9/6524 , C07F9/655345 , C07F9/6561 , C07B2200/05
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.

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