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1. 发明申请

WO2005118601A3 SULFONYLETHYL PHOSPHORODIAMIDATES FOR USE IN THE TREATMENT OF CANCER 审中-公开
标题翻译：用于治疗癌症的磺酰氟磷酰胆碱酯酶
公开(公告)号：WO2005118601A3
公开(公告)日：2006-04-06
申请号：PCT/US2005017880
申请日：2005-05-20
申请人： TELIK INC , ALLEN DAVID R , MA WENLI , PETERSON BRIAN T , ROBINSON LOUISE , SCHOW STEVEN R , SHI SONGYUAN , SIMON REYNA J , WEBER KEVIN T , WICK MICHAEL M
发明人： ALLEN DAVID R , MA WENLI , PETERSON BRIAN T , ROBINSON LOUISE , SCHOW STEVEN R , SHI SONGYUAN , SIMON REYNA J , WEBER KEVIN T , WICK MICHAEL M
IPC分类号： A61K31/66 , C07F9/00 , C07F9/02 , C07F9/24 , C07F9/572 , C07F9/58 , C07F9/59 , C07F9/6509 , C07F9/6533 , C07F9/655 , C07F9/6553 , C07F9/6561 , A61K31/664 , A61P35/04
CPC分类号： C07F9/2458 , C07F9/2408 , C07F9/5721 , C07F9/581 , C07F9/582 , C07F9/591 , C07F9/598 , C07F9/650958 , C07F9/6533 , C07F9/65515 , C07F9/655345 , C07F9/65616
摘要： Sulfonylethyl and thioethyl phosphorodiamidates, their preparation and intermediates in their preparation, formulations containing them, and their pharmaceutical use. The compounds are useful for treating cancer, alone and in combination with other anticancer therapies.
摘要翻译：磺基乙基和硫代乙基磷酰二胺，它们的制备和中间体在制备中，含有它们的制剂及其药物用途。该化合物可用于单独治疗和与其它抗癌疗法组合治疗癌症。

2. 发明申请

WO1991019735A1 LIBRARIES OF MODIFIED PEPTIDES WITH PROTEASE RESISTANCE 审中-公开
标题翻译：具有耐药性的改性肽的图书馆
公开(公告)号：WO1991019735A1
公开(公告)日：1991-12-26
申请号：PCT/US1991004282
申请日：1991-06-14
申请人： BARTLETT, Paul, A. , SANTI, Daniel, V. , SIMON, Reyna, J.
IPC分类号： C07K07/02
CPC分类号： C07K14/001 , A61K38/00 , A61K47/62 , C07K1/047 , C07K5/0207 , C07K7/02
摘要： Peptoids are provided which are polymers comprised of monomer units wherein the monomer units include at least some substitute amino acids and may include conventional amino acids. The peptoids can be synthesized in large numbers so as to provide libraries of peptoids which can be screened in order to isolate peptoids of desired biological activity. Certain peptoids are designed to mimic as closely as possible the activity of known proteins. Other peptoids are designed so as to have greater or lesser activity than known proteins and may be designed so as to block known receptor sites and/or elicit a desired immunogenic response and thereby act as vaccines. A range of different amino acid substitutes are disclosed, as are their methods of synthesis and methods of using such amino acid substitutes in the synthesis of peptoids and peptoid libraries. Methods of screening the libraries in order to obtain desired peptoids of a particular biological activity are also disclosed. The peptoids are preferably linked to a pharmaceutically active drug forming a conjugate with increased binding affinity to a particular biological receptor site.
摘要翻译：提供了由单体单元组成的聚合物，其中单体单元包括至少一些替代氨基酸并且可以包括常规氨基酸。可以大量合成拟肽，以便提供可以筛选的拟肽文库，以分离所需生物活性的拟肽。某些拟肽被设计为尽可能模拟已知蛋白质的活性。其他拟肽被设计为具有比已知蛋白质更大或更小的活性，并且可以被设计成阻断已知的受体位点和/或引发所需的免疫原性应答并由此作为疫苗。公开了一系列不同的氨基酸替代物，以及它们的合成方法以及在合成拟肽和拟肽文库中使用这种氨基酸替代物的方法。还公开了为了获得特定生物活性所需的拟肽而筛选文库的方法。拟肽优选与形成具有对特定生物受体位点的增加的结合亲和力的缀合物的药学活性药物连接。

3. 发明申请

WO2010036873A1 2-[1H-Benzimidazol-2(3H)-ylidene]-2-(pyrimidin-2-yl)acetamides and 2-[benzothiazol-2(3H)-ylidene]-2-(pyrimidin-2-yl)acetamides as kinase inhibitors 审中-公开
标题翻译： 2- [1H-苯并咪唑-2（3H） - 亚基] -2-（嘧啶-2-基）乙酰胺和2- [苯并噻唑-2（3H） - 亚基] -2-（嘧啶-2-基）激酶抑制剂
公开(公告)号：WO2010036873A1
公开(公告)日：2010-04-01
申请号：PCT/US2009/058345
申请日：2009-09-25
申请人： TELIK, INC. , AURRECOECHEA, Natalia , BEROZA, Paul P. , DAMODARAN, Komath V. , PONTIUS, Karen Y. , ROBINSON, Louise , SIMON, Reyna J. , VU, Truong , WEBER, Kevin T.
发明人： AURRECOECHEA, Natalia , BEROZA, Paul P. , DAMODARAN, Komath V. , PONTIUS, Karen Y. , ROBINSON, Louise , SIMON, Reyna J. , VU, Truong , WEBER, Kevin T.
IPC分类号： C07D401/14 , C07D403/06 , C07D403/14 , C07D417/06 , C07D417/14 , A61K31/506 , A61P35/00
CPC分类号： C07D403/06 , C07D401/14 , C07D403/14 , C07D417/06 , C07D417/14
摘要： 2-[1 H -benzimidazol-2(3 H )-ylidene]-2-(pyrimidin-2-yl)acetamides and 2-[benzothiazol-2(3 H )-ylidene]-2-(pyrimidin-2-yl)acetamides and their salts are kinase inhibitors, useful in the treatment of cancer. Formula I
摘要翻译： 2- [1H-苯并咪唑-2（3H） - 亚基] -2-（嘧啶-2-基）乙酰胺和2- [苯并噻唑-2（3H） - 亚基] -2-（嘧啶-2-基）乙酰胺和它们的盐是可用于治疗癌症的激酶抑制剂。一级方程式

4. 发明申请

WO2006074249A1 TRIPEPTIDE AND TETRAPEPTIDE THIOETHERS 审中-公开
标题翻译： TRIPEPTIDE和TETRAPEPTIDE THIOETHERS
公开(公告)号：WO2006074249A1
公开(公告)日：2006-07-13
申请号：PCT/US2006/000219
申请日：2006-01-04
申请人： TELIK, INC. , AURRECOECHEA, Natalia , KELSON, Andrew, B. , MACSATA, Robert, W. , ROBINSON, Louise , SANCHEZ, Anthony, J. , SANTIAGO, Nicholas, M. , SCHOW, Steven, R. , SIMON, Reyna, J.
发明人： AURRECOECHEA, Natalia , KELSON, Andrew, B. , MACSATA, Robert, W. , ROBINSON, Louise , SANCHEZ, Anthony, J. , SANTIAGO, Nicholas, M. , SCHOW, Steven, R. , SIMON, Reyna, J.
IPC分类号： C12P21/02 , C07K5/08 , A61K38/06 , A61P31/00
CPC分类号： C07K5/0215 , A61K38/00
摘要： Tripeptide and tetrapeptide thioethers, pharmaceutical compositions containing them, their pharmaceutical use, and their preparation. The compounds are useful in potentiating the cytotoxic effects of chemotherapeutic agents in tumor cells, selectively exerting toxicity in tumor cells, elevating the production of GM progenitors in bone marrow, stimulating the differentiation of bone marrow, mitigating the myelosuppressive effects of chemotherapeutic agents, and modulating hematopoiesis in bone marrow.
摘要翻译：三肽和四肽硫醚，含有它们的药物组合物，它们的药物用途及其制备。该化合物可用于增强化疗药物在肿瘤细胞中的细胞毒性作用，选择性地在肿瘤细胞中发挥毒性，提高骨髓中转基因祖细胞的产生，刺激骨髓分化，减轻化疗药物的骨髓抑制作用，以及调节骨髓造血。

5. 发明申请

WO2005118601A2 SULFONYLETHYL PHOSPHORODIAMIDATES 审中-公开
标题翻译：用于治疗癌症的磺酰氟磷酰胆碱酯酶
公开(公告)号：WO2005118601A2
公开(公告)日：2005-12-15
申请号：PCT/US2005/017880
申请日：2005-05-20
申请人： TELIK, INC. , ALLEN, David, R. , MA, Wenli , PETERSON, Brian, T. , ROBINSON, Louise , SCHOW, Steven, R. , SHI, Songyuan , SIMON, Reyna, J. , WEBER, Kevin, T. , WICK, Michael, M.
发明人： ALLEN, David, R. , MA, Wenli , PETERSON, Brian, T. , ROBINSON, Louise , SCHOW, Steven, R. , SHI, Songyuan , SIMON, Reyna, J. , WEBER, Kevin, T. , WICK, Michael, M.
IPC分类号： C07F9/00
CPC分类号： C07F9/2458 , C07F9/2408 , C07F9/5721 , C07F9/581 , C07F9/582 , C07F9/591 , C07F9/598 , C07F9/650958 , C07F9/6533 , C07F9/65515 , C07F9/655345 , C07F9/65616
摘要： Sulfonylethyl and thioethyl phosphorodiamidates, their preparation and intermediates in their preparation, formulations containing them, and their pharmaceutical use. The compounds are useful for treating cancer, alone and in combination with other anticancer therapies.
摘要翻译：磺基乙基和硫代乙基磷酰二胺，它们的制备和中间体在制备中，含有它们的制剂及其药物用途。该化合物可用于单独治疗和与其它抗癌疗法组合治疗癌症。

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