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1. 发明授权

US06452050B1 Synthesis and use of &agr;-ketoamide derivatives and arrays 失效
标题翻译： α-酮酰胺衍生物和阵列的合成和应用
公开(公告)号：US06452050B1
公开(公告)日：2002-09-17
申请号：US09531737
申请日：2000-03-21
申请人： Carmen M. Baldino , David L. Coffen , Stewart D. Chipman , Hong Cheng
发明人： Carmen M. Baldino , David L. Coffen , Stewart D. Chipman , Hong Cheng
IPC分类号： C07C23307
CPC分类号： C40B40/04 , C07C275/40 , C07C335/20 , C07D333/60
摘要： The invention is based on new methods for making and using compounds and arrays of novel &agr;-ketoamides, and the arrays and compounds made by these methods. These novel compounds are potential inhibitors of proteolytic enzymes, particularly cysteine proteases such as cruzain. Application of the new methods has led to the identification of a number of new inhibitors, from amongst an array of about 38,000 &agr;-ketoamide derivatives, having specific activity against three cysteine proteases: cruzain, papain, and cathepsin B. These compounds and other compounds identified by the methods described herein can be useful, for example, in developing pharmaceutical agents for the treatment of diseases (e.g., Chagas' disease) associated with these proteases. Although the disclosed compounds have specific activity for cruzain, papain, cathepsin B, the methods described herein can also be used to identify inhibitors of other proteases.
摘要翻译：本发明基于制备和使用新型α-酮酰胺的化合物和阵列的新方法，以及通过这些方法制备的阵列和化合物。这些新型化合物是蛋白水解酶的潜在抑制剂，特别是半胱氨酸蛋白酶如克鲁津。新方法的应用已经导致了一系列新的抑制剂的鉴定，其中有大约38,000个α-酮酰胺衍生物，具有针对三个半胱氨酸蛋白酶：克鲁津，木瓜蛋白酶和组织蛋白酶B的比活性。这些化合物和其它化合物通过本文所述的方法鉴定可用于例如开发用于治疗与这些蛋白酶相关的疾病（例如恰加斯病）的药剂。虽然所公开的化合物对克鲁津，木瓜蛋白酶，组织蛋白酶B具有比活性，但本文所述的方法也可用于鉴定其它蛋白酶的抑制剂。

2. 发明授权

US6143931A Synthesis and use of .alpha.-ketoamide derivatives and arrays 失效
标题翻译： α-酮酰胺衍生物和阵列的合成和应用
公开(公告)号：US6143931A
公开(公告)日：2000-11-07
申请号：US61752
申请日：1998-04-16
申请人： Carmen M. Baldino , David L. Coffen , Stewart D. Chipman , Hong Cheng
发明人： Carmen M. Baldino , David L. Coffen , Stewart D. Chipman , Hong Cheng
IPC分类号： C07B61/00 , C07C275/40 , C07C335/20 , C07D333/60 , C07C233/00
CPC分类号： C40B40/04 , C07C275/40 , C07C335/20 , C07D333/60
摘要： The invention is based on new methods for making and using compounds and arrays of novel .alpha.-ketoamides, and the arrays and compounds made by these methods. These novel compounds are potential inhibitors of proteolytic enzymes, particularly cysteine proteases such as cruzain. Application of the new methods has led to the identification of a number of new inhibitors, from amongst an array of about 38,000 .alpha.-ketoamide derivatives, having specific activity against three cysteine proteases: cruzain, papain, and cathepsin B. These compounds and other compounds identified by the methods described herein can be useful, for example, in developing pharmaceutic agents for the treatment of diseases (e.g., Chagas' disease) associated with these proteases. Although the disclosed compounds have specific activity for cruzain, papain, cathepsin B, the methods described herein can also be used to identify inhibitors of other proteases.
摘要翻译：本发明基于制备和使用新型α-酮酰胺的化合物和阵列的新方法，以及通过这些方法制备的阵列和化合物。这些新型化合物是蛋白水解酶的潜在抑制剂，特别是半胱氨酸蛋白酶如克鲁津。新方法的应用已经导致了一系列新的抑制剂的鉴定，其中有大约38,000种α-酮酰胺衍生物，具有针对三种半胱氨酸蛋白酶：克鲁津，木瓜蛋白酶和组织蛋白酶B的比活性。这些化合物和其它化合物通过本文描述的方法鉴定可用于例如开发用于治疗与这些蛋白酶相关的疾病（例如恰加斯病）的药物制剂。虽然所公开的化合物对克鲁津，木瓜蛋白酶，组织蛋白酶B具有比活性，但本文所述的方法也可用于鉴定其它蛋白酶的抑制剂。

3. 发明授权

US08901145B2 Aminopyrimidine kinase inhibitors 有权
标题翻译：氨基嘧啶激酶抑制剂
公开(公告)号：US08901145B2
公开(公告)日：2014-12-02
申请号：US13452250
申请日：2012-04-20
申请人： Carmen M. Baldino , Justin L. Caserta , Stephane A. Dumas , Chee-Seng Lee , Yvonne L. Flanders
发明人： Carmen M. Baldino , Justin L. Caserta , Stephane A. Dumas , Chee-Seng Lee , Yvonne L. Flanders
IPC分类号： A01N43/54 , A61K31/505 , C07D417/14
CPC分类号： C07D417/14
摘要： Disclosed are compounds, pharmaceutical compositions containing those compounds, and uses of the compounds and compositions as modulators of casein kinase 1 (e.g., CK1γ), casein kinase 2 (CK2), Pim-1, Pim-2, Pim-3, the TGFβ pathway, the Wnt pathway, the JAK/STAT pathway, and/or the mTOR pathway. Uses are also disclosed for the treatment or prevention of a range of therapeutic indications due at least in part to aberrant physiological activity of casein kinase 1 (e.g., CK1γ), casein kinase 2 (CK2), Pim-1, Pim-2, Pim-3, the TGFβ pathway, the Wnt pathway, the JAK/STAT pathway, and/or the mTOR pathway.
摘要翻译：公开了化合物，含有这些化合物的药物组合物，以及化合物和组合物作为酪蛋白激酶1（例如CK1γ），酪蛋白激酶2（CK2），Pim-1，Pim-2，Pim-3，TGFβb的调节剂的用途 ; 途径，Wnt途径，JAK / STAT途径和/或mTOR途径。还公开了用于治疗或预防一系列治疗适应症的用途，至少部分地由于酪蛋白激酶1（例如CK1γ），酪蛋白激酶2（CK2），Pim-1，Pim-2，Pim的异常生理活性 -3，TGF＆bgr; 途径，Wnt途径，JAK / STAT途径和/或mTOR途径。

4. 发明授权

US09073903B2 Imidazole-2,4-dione inhibitors of casein kinase 1 有权
标题翻译：咪唑-2,4-二酮抑制剂酪蛋白激酶1
公开(公告)号：US09073903B2
公开(公告)日：2015-07-07
申请号：US13577535
申请日：2011-02-17
申请人： Carmen M. Baldino , Justin L. Caserta , Chee-Seng Lee , Robert B. Nicewonger
发明人： Carmen M. Baldino , Justin L. Caserta , Chee-Seng Lee , Robert B. Nicewonger
IPC分类号： A61K31/506 , A61K31/497 , A61K31/5377 , A61K31/551 , C07D403/06 , C07D403/14 , C07D401/14 , C07D413/14 , C07D409/14 , C07D405/14
CPC分类号： C07D401/14 , C07D403/14 , C07D405/14 , C07D413/14
摘要： Disclosed are compounds, pharmaceutical compositions containing those compounds, and uses of the compounds and compositions as modulators of casein kinase 1 (e.g., CK1γ), the TGFβ pathway and/or the Wnt pathway. Uses are also disclosed for the treatment or prevention of a range of therapeutic indications due at least in part to aberrant physiological activity of casein kinase 1 (e.g., CK1γ), the TGFβ pathway and/or the Wnt pathway.
摘要翻译：公开了化合物，含有那些化合物的药物组合物，以及化合物和组合物作为酪蛋白激酶1（例如CK1γ）的调节剂的用途，TGFβb 途径和/或Wnt途径。还公开了用于治疗或预防一系列治疗适应症的用途，至少部分地由于酪蛋白激酶1（例如CK1γ），TGFβb的异常生理活性。途径和/或Wnt途径。

5. 发明授权

US08563539B2 Aminopyrimidine kinase inhibitors 有权
标题翻译：氨基嘧啶激酶抑制剂
公开(公告)号：US08563539B2
公开(公告)日：2013-10-22
申请号：US12978089
申请日：2010-12-23
申请人： Carmen M. Baldino , Justin L. Caserta , Chee-Seng Lee , Robert B. Nicewonger , Yvonne L. Flanders , Stephane A. Dumas
发明人： Carmen M. Baldino , Justin L. Caserta , Chee-Seng Lee , Robert B. Nicewonger , Yvonne L. Flanders , Stephane A. Dumas
IPC分类号： A61K31/33 , A61K31/55 , A61K31/497 , A61K31/535 , A61K31/4965 , C07D243/08 , C07D413/06 , C07D417/06 , C07D239/02 , C07D403/02 , C07D409/02
CPC分类号： C12N9/99 , C07D417/06 , C07D417/14 , C07D471/04 , C07D487/04
摘要： Disclosed are compounds, pharmaceutical compositions containing those compounds, and uses of the compounds and compositions as modulators of casein kinase 1 (e.g., CK1γ), casein kinase 2 (CK2), Pim 1, Pim2, Pim3, the TGFβ pathway, the Wnt pathway, the JAK/STAT pathway, and/or the mTOR pathway. Uses are also disclosed for the treatment or prevention of a range of therapeutic indications due at least in part to aberrant physiological activity of casein kinase 1 (e.g., CK1γ), casein kinase 2 (CK2), Pim 1, Pim2, Pim3, the TGFβ pathway, the Wnt pathway, the JAK/STAT pathway, and/or the mTOR pathway.
摘要翻译：公开了化合物，含有这些化合物的药物组合物，以及化合物和组合物作为酪蛋白激酶1（例如CK1gamma），酪蛋白激酶2（CK2），Pim1，Pim2，Pim3，TGFbeta途径，Wnt途径的调节剂的用途，JAK / STAT途径和/或mTOR途径。还公开了用于治疗或预防一系列治疗适应症的用途，至少部分地由于酪蛋白激酶1（例如CK1gamma），酪蛋白激酶2（CK2），Pim1，Pim2，Pim3，TGFbeta的异常生理活性途径，Wnt途径，JAK / STAT途径和/或mTOR途径。

6. 发明申请

US20120270892A1 Aminopyrimidine Kinase Inhibitors 有权
标题翻译：氨基嘧啶激酶抑制剂
公开(公告)号：US20120270892A1
公开(公告)日：2012-10-25
申请号：US13452250
申请日：2012-04-20
申请人： Carmen M. Baldino , Justin L. Caserta , Stephane A. Dumas , Chee-Seng Lee , Yvonne L. Flanders
发明人： Carmen M. Baldino , Justin L. Caserta , Stephane A. Dumas , Chee-Seng Lee , Yvonne L. Flanders
IPC分类号： A61K31/506 , A61K31/4709 , A61P35/00 , A61P35/02 , A61P25/28 , A61P3/08 , A61P25/00 , A61P19/02 , A61P19/08 , A61P19/10 , A61P3/10 , A61P3/00 , C07D417/14 , A61P29/00
CPC分类号： C07D417/14
摘要： Disclosed are compounds, pharmaceutical compositions containing those compounds, and uses of the compounds and compositions as modulators of casein kinase 1 (e.g., CK1γ), casein kinase 2 (CK2), Pim-1, Pim-2, Pim-3, the TGFβ pathway, the Wnt pathway, the JAK/STAT pathway, and/or the mTOR pathway. Uses are also disclosed for the treatment or prevention of a range of therapeutic indications due at least in part to aberrant physiological activity of casein kinase 1 (e.g., CK1γ), casein kinase 2 (CK2), Pim-1, Pim-2, Pim-3, the TGFβ pathway, the Wnt pathway, the JAK/STAT pathway, and/or the mTOR pathway.
摘要翻译：公开了化合物，含有这些化合物的药物组合物，以及化合物和组合物作为酪蛋白激酶1（例如CK1γ），酪蛋白激酶2（CK2），Pim-1，Pim-2，Pim-3，TGFβb的调节剂的用途 ; 途径，Wnt途径，JAK / STAT途径和/或mTOR途径。还公开了用于治疗或预防一系列治疗适应症的用途，至少部分地由于酪蛋白激酶1（例如CK1γ），酪蛋白激酶2（CK2），Pim-1，Pim-2，Pim的异常生理活性 -3，TGF＆bgr; 途径，Wnt途径，JAK / STAT途径和/或mTOR途径。

7. 发明申请

US20110046362A1 METHODS OF MAKING NUCLEOSIDE TETRAPHOSPHATE 失效
标题翻译：制备核苷四磷酸的方法
公开(公告)号：US20110046362A1
公开(公告)日：2011-02-24
申请号：US12867879
申请日：2009-02-13
申请人： Carmen M. Baldino , Dan P. Cook , Shomir Ghosh , Lazlo Varady , Thomas Andreas Waldbach , Zhongguo Wang
发明人： Carmen M. Baldino , Dan P. Cook , Shomir Ghosh , Lazlo Varady , Thomas Andreas Waldbach , Zhongguo Wang
IPC分类号： C07H19/20
CPC分类号： C07H19/20 , C07H15/203
摘要： The invention provides compounds and methods for making adenosine-ribofuranoside tetraphosphate compounds. The compounds are contemplated to have activity at the P2Y receptor and may be used in the treatment of medical disorders such as cystic fibrosis and upper respiratory disorders.
摘要翻译：本发明提供了制备腺苷 - 呋喃糖苷四磷酸化合物的化合物和方法。该化合物被认为具有P2Y受体的活性，可用于治疗医学病症如囊性纤维化和上呼吸道疾病。

8. 发明申请

US20120316155A1 Imidazole-2,4-Dione Inhibitors of Casein Kinase 1 有权
标题翻译：咪唑-2,4-二酮抑制剂酪蛋白激酶1
公开(公告)号：US20120316155A1
公开(公告)日：2012-12-13
申请号：US13577535
申请日：2011-02-17
申请人： Carmen M. Baldino , Justin L. Caserta , Chee-Seng Lee , Robert B. Nicewonger
发明人： Carmen M. Baldino , Justin L. Caserta , Chee-Seng Lee , Robert B. Nicewonger
IPC分类号： A61K31/506 , A61K31/497 , C07D403/14 , C07D401/14 , C07D413/14 , A61K31/5377 , C07D403/06 , A61K31/551 , C07D409/14 , A61P35/00 , A61P25/28 , A61P29/00 , A61P25/00 , A61P19/08 , A61P19/10 , A61P3/08 , A61P3/10 , C07D405/14
CPC分类号： C07D401/14 , C07D403/14 , C07D405/14 , C07D413/14
摘要： Disclosed are compounds, pharmaceutical compositions containing those compounds, and uses of the compounds and compositions as modulators of casein kinase 1 (e.g., CK1γ), the TGFβ pathway and/or the Wnt pathway. Uses are also disclosed for the treatment or prevention of a range of therapeutic indications due at least in part to aberrant physiological activity of casein kinase 1 (e.g., CK1γ), the TGFβ pathway and/or the Wnt pathway.
摘要翻译：公开了化合物，含有那些化合物的药物组合物，以及化合物和组合物作为酪蛋白激酶1（例如CK1γ）的调节剂的用途，TGFβb 途径和/或Wnt途径。还公开了用于治疗或预防一系列治疗适应症的用途，至少部分地由于酪蛋白激酶1（例如CK1γ），TGFβb的异常生理活性。途径和/或Wnt途径。

9. 发明申请

US20110152235A1 Aminopyrimidine Kinase Inhibitors 有权
标题翻译：氨基嘧啶激酶抑制剂
公开(公告)号：US20110152235A1
公开(公告)日：2011-06-23
申请号：US12978089
申请日：2010-12-23
申请人： Carmen M. Baldino , Justin L. Caserta , Chee-Seng Lee , Robert B. Nicewonger , Yvonne L. Flanders , Stephane A. Dumas
发明人： Carmen M. Baldino , Justin L. Caserta , Chee-Seng Lee , Robert B. Nicewonger , Yvonne L. Flanders , Stephane A. Dumas
IPC分类号： A61K31/506 , C07D417/14 , A61K31/496 , A61K31/5377 , A61K31/551 , A61K31/55 , A61K31/497 , A61P35/00 , A61P29/00 , C12N9/99
CPC分类号： C12N9/99 , C07D417/06 , C07D417/14 , C07D471/04 , C07D487/04
摘要： Disclosed are compounds, pharmaceutical compositions containing those compounds, and uses of the compounds and compositions as modulators of casein kinase 1 (e.g., CK1γ), casein kinase 2 (CK2), Pim 1, Pim2, Pim3, the TGFβ pathway, the Wnt pathway, the JAK/STAT pathway, and/or the mTOR pathway. Uses are also disclosed for the treatment or prevention of a range of therapeutic indications due at least in part to aberrant physiological activity of casein kinase 1 (e.g., CK1γ), casein kinase 2 (CK2), Pim 1, Pim2, Pim3, the TGFβ pathway, the Wnt pathway, the JAK/STAT pathway, and/or the mTOR pathway.
摘要翻译：公开了化合物，含有这些化合物的药物组合物，以及化合物和组合物作为酪蛋白激酶1（例如CK1γ），酪蛋白激酶2（CK2），Pim1，Pim2，Pim3，TGFβb的调节剂的用途。途径，Wnt途径，JAK / STAT途径和/或mTOR途径。还公开了用于治疗或预防一系列治疗适应症的用途，至少部分地由于酪蛋白激酶1（例如CK1γ），酪蛋白激酶2（CK2），Pim1，Pim2，Pim3，TGFβb的异常生理活性 ; 途径，Wnt途径，JAK / STAT途径和/或mTOR途径。

10. 发明授权

US08546557B2 Methods of making nucleoside tetraphosphate analogs 失效
标题翻译：制备核苷四磷酸类似物的方法
公开(公告)号：US08546557B2
公开(公告)日：2013-10-01
申请号：US12867879
申请日：2009-02-13
申请人： Carmen M. Baldino , Dan P. Cook , Shomir Ghosh , Lazlo Varady , Thomas Andreas Waldbach , Zhongguo Wang
发明人： Carmen M. Baldino , Dan P. Cook , Shomir Ghosh , Lazlo Varady , Thomas Andreas Waldbach , Zhongguo Wang
IPC分类号： C07H19/00 , C07H19/20
CPC分类号： C07H19/20 , C07H15/203
摘要： The invention provides compounds and methods for making adenosine-ribofuranoside tetraphosphate compounds. The compounds are contemplated to have activity at the P2Y receptor and may be used in the treatment of medical disorders such as cystic fibrosis and upper respiratory disorders.
摘要翻译：本发明提供了制备腺苷 - 呋喃糖苷四磷酸化合物的化合物和方法。该化合物被认为具有P2Y受体的活性，可用于治疗医学病症如囊性纤维化和上呼吸道疾病。

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