专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明申请

WO2010132869A3 PEPTIDE MIMETIC LIGANDS OF POLO-LIKE KINASE 1 POLO BOX DOMAIN AND METHODS OF USE 审中-公开
标题翻译： POLO-like激素的肽类化合物1 POLO BOX域及其使用方法
公开(公告)号：WO2010132869A3
公开(公告)日：2011-04-07
申请号：PCT/US2010035069
申请日：2010-05-17
申请人： US GOV HEALTH & HUMAN SERV , BURKE TERRENCE R , LIU FA , LEE KYUNG S , PARK JUNG-EUN
发明人： BURKE TERRENCE R , LIU FA , LEE KYUNG S , PARK JUNG-EUN
IPC分类号： C07K7/06 , C12N9/12
CPC分类号： C07K7/06 , A61K38/00
摘要： Found in various eukaryotic organisms, polo-like kinases (collectively, Plks) are a conserved subfamily of Ser/Thr protein kinases that play critical roles in cell proliferation. Provided herein are compounds that specifically inhibit the activity of Plks, specifically Plkl. Further provided herein are methods for use of the compounds for the treatment of hyperprolif erative disorders, particularly cancer. Also provided are uses of the compounds for the preparation of a medicament.
摘要翻译：在各种真核生物中发现，polo样激酶（统称为Plks）是Ser / Thr蛋白激酶的保守亚家族，在细胞增殖中起关键作用。本文提供了特异性抑制Plks，特别是Plk1活性的化合物。本文进一步提供的是使用该化合物治疗过度扩张性疾病，特别是癌症的方法。还提供了化合物用于制备药物的用途。

2. 发明申请

WO2012142245A2 PEPTIDE MIMETIC LIGANDS OF POLO-LIKE KINASE 1 POLO BOX DOMAIN AND METHODS OF USE 审中-公开
标题翻译： POLO-like激素的肽类化合物1 POLO BOX域及其使用方法
公开(公告)号：WO2012142245A2
公开(公告)日：2012-10-18
申请号：PCT/US2012033259
申请日：2012-04-12
申请人： US GOV HEALTH & HUMAN SERV , BURKE TERRENCE R , QIAN WENJIAN , LIU FA , LEE KYUNG S , PARK JUNG-EUN
发明人： BURKE TERRENCE R , QIAN WENJIAN , LIU FA , LEE KYUNG S , PARK JUNG-EUN
IPC分类号： C07K14/435 , A61K47/48 , A61P35/00 , C12N9/12
CPC分类号： C07K7/06 , A61K38/00 , A61K47/60 , C07K1/006 , C07K5/0827 , C12N9/12 , C12Y207/11021
摘要： Novel compounds are provided that bind to polo-like kinases through the polo-box domain. In certain embodiments, the novel compounds are PEGylated peptides. The PEGylated peptides in accordance with the invention demonstrate high PBD-binding affinity. In certain embodiments, the PEGylated peptides have also achieved activities in whole cell systems. The invention also provides compounds that bind polo-like kinases through the polo-box domain and possess reduced anionic charge. Further provided are methods of design and/or synthesis of the PEGylated peptides and methods of use thereof. The invention provides methods of use of the compounds and methods of synthesis of the compounds.
摘要翻译：提供了通过polo-box结构域结合polo样激酶的新型化合物。在某些实施方案中，新化合物是PEG化肽。根据本发明的聚乙二醇化肽表现出高PBD结合亲和力。在某些实施方案中，聚乙二醇化肽还在整个细胞系统中获得活性。本发明还提供通过马球结构域结合polo样激酶并具有减少的阴离子电荷的化合物。还提供了聚乙二醇化肽的设计和/或合成方法及其使用方法。本发明提供了化合物的使用方法和化合物的合成方法。

3. 发明申请

WO2012142245A8 PEPTIDE MIMETIC LIGANDS OF POLO-LIKE KINASE 1 POLO BOX DOMAIN AND METHODS OF USE 审中-公开
标题翻译： POLO-like激素的肽类化合物1 POLO BOX域及其使用方法
公开(公告)号：WO2012142245A8
公开(公告)日：2013-11-21
申请号：PCT/US2012033259
申请日：2012-04-12
申请人： US GOV HEALTH & HUMAN SERV , BURKE TERRENCE R , QIAN WENJIAN , LIU FA , LEE KYUNG S , PARK JUNG-EUN
发明人： BURKE TERRENCE R , QIAN WENJIAN , LIU FA , LEE KYUNG S , PARK JUNG-EUN
IPC分类号： C07K14/435 , A61K47/48 , A61P35/00 , C12N9/12
CPC分类号： C07K7/06 , A61K38/00 , A61K47/60 , C07K1/006 , C07K5/0827 , C12N9/12 , C12Y207/11021
摘要： Novel compounds are provided that bind to polo-like kinases through the polo -box domain. In certain embodiments, the novel compounds are PEGylated peptides. The PEGylated peptides in accordance with the invention demonstrate high PBD-binding affinity. In certain embodiments, the PEGylated peptides have also achieved activities in whole cell systems. The invention also provides compounds that bind polo- like kinases through the polo -box domain and possess reduced anionic charge. Further provided are methods of design and/or synthesis of the PEGylated peptides and methods of use thereof. The invention provides methods of use of the compounds and methods of synthesis of the compounds. The compounds of the invention have potential therapeutic activity in view of their binding and inhibitory activities towards Plkl. They are based on the amino acid sequence PLHSpT (phosphorylated Thr). The PEG moiety, when present, is covalently attached at the N- terminus. The invention also encompasses derivatives having substituents on the Pro and/or the His side chains, substituents on the phosphate group, the replacement of His with Gln, the replacement of Pro with a N-substituted Gly, the replacement of Ser with Ala, as well as HS-pT fragments with N-terminal alkoxycarbonyl group and PLHS fragments with a C-terminal glyco-imino-alkylxyalkylamide group.
摘要翻译：提供了新的化合物，其通过polo-box结构域结合polo样激酶。在某些实施方案中，新化合物是PEG化肽。根据本发明的聚乙二醇化肽表现出高PBD结合亲和力。在某些实施方案中，聚乙二醇化肽还在整个细胞系统中获得活性。本发明还提供通过马球盒结构域结合polo样激酶并具有减少的阴离子电荷的化合物。还提供了聚乙二醇化肽的设计和/或合成方法及其使用方法。本发明提供了化合物的使用方法和化合物的合成方法。考虑到它们对Plk1的结合和抑制活性，本发明的化合物具有潜在的治疗活性。它们基于氨基酸序列PLHSpT（磷酸化的Thr）。存在时，PEG部分在N末端共价连接。本发明还包括在Pro和/或His侧链上具有取代基的衍生物，磷酸基团上的取代基，用Gln取代His，用N-取代的Gly取代Pro，用Ala取代Ser，作为以及具有N-末端烷氧基羰基的HS-pT片段和具有C-末端糖 - 亚氨基 - 烷基烷基酰胺基团的PLHS片段。

4. 发明专利

AU2012242784A1 Peptide mimetic ligands of polo-like kinase 1 polo box domain and methods of use 未知
公开(公告)号：AU2012242784A1
公开(公告)日：2013-10-31
申请号：AU2012242784
申请日：2012-04-12
申请人： US GOV HEALTH & HUMAN SERV
发明人： BURKE TERRENCE R , QIAN WENJIAN , LIU FA , LEE KYUNG S , PARK JUNG-EUN
IPC分类号： C07K14/435 , A61K47/48 , A61P35/00 , C12N9/12
摘要： Novel compounds are provided that bind to polo-like kinases through the polo -box domain. In certain embodiments, the novel compounds are PEGylated peptides. The PEGylated peptides in accordance with the invention demonstrate high PBD-binding affinity. In certain embodiments, the PEGylated peptides have also achieved activities in whole cell systems. The invention also provides compounds that bind polo- like kinases through the polo -box domain and possess reduced anionic charge. Further provided are methods of design and/or synthesis of the PEGylated peptides and methods of use thereof. The invention provides methods of use of the compounds and methods of synthesis of the compounds. The compounds of the invention have potential therapeutic activity in view of their binding and inhibitory activities towards Plkl. They are based on the amino acid sequence PLHSpT (phosphorylated Thr). The PEG moiety, when present, is covalently attached at the N- terminus. The invention also encompasses derivatives having substituents on the Pro and/or the His side chains, substituents on the phosphate group, the replacement of His with Gln, the replacement of Pro with a N-substituted Gly, the replacement of Ser with Ala, as well as HS-pT fragments with N-terminal alkoxycarbonyl group and PLHS fragments with a C-terminal glyco-imino-alkylxyalkylamide group.

5. 发明专利

CA2832073A1 PEPTIDE MIMETIC LIGANDS OF POLO-LIKE KINASE 1 POLO BOX DOMAIN AND METHODS OF USE 未知
公开(公告)号：CA2832073A1
公开(公告)日：2012-10-18
申请号：CA2832073
申请日：2012-04-12
申请人： US GOV HEALTH & HUMAN SERV
发明人： BURKE TERRENCE R , QIAN WENJIAN , LIU FA , LEE KYUNG S , PARK JUNG-EUN
IPC分类号： C07K14/435 , A61K47/48 , A61P35/00 , C12N9/12
摘要： Novel compounds are provided that bind to polo-like kinases through the polo -box domain. In certain embodiments, the novel compounds are PEGylated peptides. The PEGylated peptides in accordance with the invention demonstrate high PBD-binding affinity. In certain embodiments, the PEGylated peptides have also achieved activities in whole cell systems. The invention also provides compounds that bind polo- like kinases through the polo -box domain and possess reduced anionic charge. Further provided are methods of design and/or synthesis of the PEGylated peptides and methods of use thereof. The invention provides methods of use of the compounds and methods of synthesis of the compounds. The compounds of the invention have potential therapeutic activity in view of their binding and inhibitory activities towards Plkl. They are based on the amino acid sequence PLHSpT (phosphorylated Thr). The PEG moiety, when present, is covalently attached at the N- terminus. The invention also encompasses derivatives having substituents on the Pro and/or the His side chains, substituents on the phosphate group, the replacement of His with Gln, the replacement of Pro with a N-substituted Gly, the replacement of Ser with Ala, as well as HS-pT fragments with N-terminal alkoxycarbonyl group and PLHS fragments with a C-terminal glyco-imino-alkylxyalkylamide group.

6. 发明专利

CA2582908A1 MACROCYCLIC SH2 DOMAIN BINDING INHIBITORS 未知
公开(公告)号：CA2582908A1
公开(公告)日：2006-04-13
申请号：CA2582908
申请日：2005-09-30
申请人： US GOV HEALTH & HUMAN SERV
发明人： OISHI SHINYA , SHI ZHEN-DAN , BURKE TERRENCE R JR , LIU FA
IPC分类号： A61K38/12 , A61K31/675 , A61P35/00 , C07F9/553 , C07K5/12

7. 发明专利

IL278171D0 Gip derivatives and uses thereof 未知
公开(公告)号：IL278171D0
公开(公告)日：2020-11-30
申请号：IL27817120
申请日：2020-10-20
申请人： NOVO NORDISK AS , HOGENDORF WOUTER FREDERIK JOHAN , TH?GERSEN HENNING , COX NICHOLAS RAYMOND , KNERR PATRICK J , DIMARCHI RICHARD , FINAN BRIAN , LAU JESPER F , REEDTZ RUNGE STEFFEN , LIU FA
发明人： HOGENDORF WOUTER FREDERIK JOHAN , TH?GERSEN HENNING , COX NICHOLAS RAYMOND , KNERR PATRICK J , DIMARCHI RICHARD , FINAN BRIAN , LAU JESPER F , REEDTZ-RUNGE STEFFEN , LIU FA
IPC分类号： A61K38/00 , A61K38/22 , A61K38/26 , A61P3/10 , C07K14/575 , C07K14/605 , C07K14/645
摘要： The present invention relates to novel peptides that are derivatives of glucose-dependent insulinotropic polypeptide (GIP) analogues having improved physical stability in solution and a protracted profile of action. More particularly the invention relates to such peptides that are agonists at the GIP receptor and to their use in weight management or for treatment of diseases such as obesity, diabetes or non-alcoholic steatohepatitis (NASH). The peptides comprise a lysine residue at a position corresponding to position 24 of hGIP(1-31), and comprise a negatively charged modifying group attached to the epsilon amino group of the lysine residue.

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式