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1. 发明申请

US20110190295A1 COMPOSITIONS AND METHODS FOR INHIBITION OF HEPATOCYTE GROWTH FACTOR RECEPTOR C-MET SIGNALING 失效
标题翻译：抑制肝细胞生长因子受体C-MET信号的组合物和方法
公开(公告)号：US20110190295A1
公开(公告)日：2011-08-04
申请号：US12935643
申请日：2009-03-31
申请人： Donald P. Bottaro , Megan Peach , Marc Nicklaus , Terrence Burke, JR. , Gagani Athauda , Sarah Choyke , Alessio Giubellino , Nelly Tan , Zhen-Dan Shi
发明人： Donald P. Bottaro , Megan Peach , Marc Nicklaus , Terrence Burke, JR. , Gagani Athauda , Sarah Choyke , Alessio Giubellino , Nelly Tan , Zhen-Dan Shi
IPC分类号： A61K31/5377 , C07D213/85 , A61K31/44 , C07D413/12 , C07D239/02 , A61K31/505 , A61P35/00
CPC分类号： C07D213/90 , C07D213/85 , C07D239/22 , C07D311/86
摘要： Derivatives and analogs of inhibitors of receptor tyrosine kinase c-Met, pharmaceutical compositions containing derivatives and analogs of c-Met inhibitors are provided. Methods of making derivatives and analogs of c-Met inhibitors and methods of use thereof are provided.
摘要翻译：提供受体酪氨酸激酶c-Met抑制剂的衍生物和类似物，其含有c-Met抑制剂的衍生物和类似物的药物组合物。提供了制备c-Met抑制剂的衍生物和类似物的方法及其使用方法。

2. 发明申请

US20080132469A1 SH2 DOMAIN BINDING INHIBITORS 有权
标题翻译： SH2域绑定抑制剂
公开(公告)号：US20080132469A1
公开(公告)日：2008-06-05
申请号：US11932424
申请日：2007-10-31
申请人： Terrence R. BURKE , Zhen-Dan SHI , Sang-Uk KANG
发明人： Terrence R. BURKE , Zhen-Dan SHI , Sang-Uk KANG
IPC分类号： A61K31/675 , C07D487/00 , C07K2/00 , A61K31/404
CPC分类号： C07K5/021 , A61K38/00 , C07K5/06078
摘要： Disclosed are compounds represented by the formula: or a pharmaceutically acceptable salt or isomer thereof, wherein R1-R6 are as defined in the specification. These compounds are targeted for use as inhibitors of SH2 domain binding with a phosphoprotein, and are contemplated for use in a number of diseases including cancer. Also disclosed are pharmaceutical compositions comprising a compound of the invention and a pharmaceutically acceptable carrier.
摘要翻译：公开了由下式表示的化合物或其药学上可接受的盐或异构体，其中R 1 -R 6如说明书中所定义。这些化合物被靶向用作与磷蛋白SH2结构域结合的抑制剂，并且被预期用于许多疾病，包括癌症。还公开了包含本发明化合物和药学上可接受的载体的药物组合物。

3. 发明授权

US08754081B2 Compositions and methods for inhibition of hepatocyte growth factor receptor c-Met signaling 失效
标题翻译：抑制肝细胞生长因子受体c-Met信号传导的组成和方法
公开(公告)号：US08754081B2
公开(公告)日：2014-06-17
申请号：US12935643
申请日：2009-03-31
申请人： Donald P. Bottaro , Megan Peach , Marc Nicklaus , Terrence Burke, Jr. , Gagani Athauda , Sarah Choyke , Alessio Giubellino , Nelly Tan , Zhen-Dan Shi
发明人： Donald P. Bottaro , Megan Peach , Marc Nicklaus , Terrence Burke, Jr. , Gagani Athauda , Sarah Choyke , Alessio Giubellino , Nelly Tan , Zhen-Dan Shi
IPC分类号： A61K31/5377 , A61K31/4412 , C07D413/02 , C07D221/00
CPC分类号： C07D213/90 , C07D213/85 , C07D239/22 , C07D311/86
摘要： Derivatives and analogs of inhibitors of receptor tyrosine kinase c-Met, pharmaceutical compositions containing derivatives and analogs of c-Met inhibitors are provided. Methods of making derivatives and analogs of c-Met inhibitors and methods of use thereof are provided.
摘要翻译：提供受体酪氨酸激酶c-Met抑制剂的衍生物和类似物，其含有c-Met抑制剂的衍生物和类似物的药物组合物。提供了制备c-Met抑制剂的衍生物和类似物的方法及其使用方法。

4. 发明授权

US07767645B2 SH2 domain binding inhibitors 有权
标题翻译： SH2结构域结合抑制剂
公开(公告)号：US07767645B2
公开(公告)日：2010-08-03
申请号：US11932424
申请日：2007-10-31
申请人： Terrence R. Burke, Jr. , Zhen-Dan Shi , Sang-Uk Kang
发明人： Terrence R. Burke, Jr. , Zhen-Dan Shi , Sang-Uk Kang
IPC分类号： A61K38/12
CPC分类号： C07K5/021 , A61K38/00 , C07K5/06078
摘要： Disclosed are compounds represented by the formula: or a pharmaceutically acceptable salt or isomer thereof, wherein R1-R6 are as defined in the specification. These compounds are targeted for use as inhibitors of SH2 domain binding with a phosphoprotein, and are contemplated for use in a number of diseases including cancer. Also disclosed are pharmaceutical compositions comprising a compound of the invention and a pharmaceutically acceptable carrier.
摘要翻译：公开了由下式表示的化合物或其药学上可接受的盐或异构体，其中R 1 -R 6如说明书中所定义。这些化合物被靶向用作与磷蛋白SH2结构域结合的抑制剂，并且被预期用于许多疾病，包括癌症。还公开了包含本发明化合物和药学上可接受的载体的药物组合物。

5. 发明授权

US07425537B2 SH2 domain binding inhibitors 失效
标题翻译： SH2结构域结合抑制剂
公开(公告)号：US07425537B2
公开(公告)日：2008-09-16
申请号：US10517717
申请日：2003-06-26
申请人： Terrence R Burke, Jr. , Chang-Qing Wei , Zhen-Dan Shi , Yang Gao
发明人： Terrence R Burke, Jr. , Chang-Qing Wei , Zhen-Dan Shi , Yang Gao
IPC分类号： A61K38/12 , C07K5/12 , C07K1/00
CPC分类号： C07F9/6515 , C07K5/06026 , C07K5/06191
摘要： Disclosed are compounds for SH2 domain binding inhibition, for example, a compound of formula (I), wherein R1 is a lipophile; R2, in combination with the phenyl ring, is a phenylphosphate mimic group or a protected phenylphosphate mimic group; R3 is hydrogen, azido, amino, carboxyalkyl, alkoxycarbonylalkyl, aminocarbonylalkyl, or alkylcarbonylamino, wherein the alkyl portion of R3 may be optionally substituted with a substituent selected from the group consisting of halo, hydroxy, carboxyl, amino, aminoalkyl, alkyl, alkoxy, and keto; R6 is a linker; AA is an amino acid; and n is 1 to 6; or a salt thereof. The conformationally compounds provide enhanced binding affinity with SH2 domain protein. Also disclosed are a pharmaceutical compositions and a method for inhibiting an SH2 domain from binding with a phosphoprotein.
摘要翻译：公开了用于SH2结构域结合抑制的化合物，例如式（I）的化合物，其中R 1是亲脂体; R 2与苯环组合是苯基磷酸酯模拟基团或被保护的苯基磷酸酯模拟基团; R 3是氢，叠氮基，氨基，羧基烷基，烷氧基羰基烷基，氨基羰基烷基或烷基羰基氨基，其中R 3的烷基部分可以任选地被选自由卤素，羟基，羧基，氨基，氨基烷基，烷基，烷氧基和酮基组成; R 6是连接体; AA是氨基酸; n为1〜6; 或其盐。构象化合物提供与SH2结构域蛋白质增强的结合亲和力。还公开了用于抑制SH2结构域与磷蛋白结合的药物组合物和方法。

6. 发明申请

US20080139456A1 Macrocyclic Sh2 Domain Binding Inhibitors 审中-公开
标题翻译：大环Sh2结构域结合抑制剂
公开(公告)号：US20080139456A1
公开(公告)日：2008-06-12
申请号：US11575723
申请日：2005-09-30
申请人： Terrence R. Burke , Zhen-Dan Shi , Shinya Oishi , Fa Liu
发明人： Terrence R. Burke , Zhen-Dan Shi , Shinya Oishi , Fa Liu
IPC分类号： A61K38/12 , C07K5/12
CPC分类号： C07K5/06113 , A61K38/00 , C07K5/06191 , C07K5/0812 , C07K5/0827
摘要： Disclosed are compounds for inhibiting the binding of an SH2 domain-containing protein, for example, a compound of formula (I): FORMULA (I) wherein R1 is a lipophile; R2, in combination with the phenyl ring, is a phenylphosphate mimic group or a protected phenylphosphate mimic group; R3 is, for example, hydrogen, azido, amino, oxalylamino, carboxy alkyl, alkoxycarbonyl alkyl, aminocarbonyl alkyl, or alkyl carbonylamino; R6 is a linker; AA is an amino acid; and n is 1 to 6; or a pharmaceutically acceptable salt, stereoisomer, solvate, or hydrate thereof. Also disclosed are pharmaceutical compositions and methods of use of such compounds.
摘要翻译：公开了用于抑制含SH2结构域的蛋白质，例如式（I）的化合物：式（I）的化合物：其中R1是亲油性物质; R2与苯环组合是苯基磷酸酯模拟基团或被保护的苯基磷酸酯模拟基团; R3是例如氢，叠氮基，氨基，草酰氨基，羧基烷基，烷氧基羰基烷基，氨基羰基烷基或烷基羰基氨基; R6是连接体; AA是氨基酸; n为1〜6; 或其药学上可接受的盐，立体异构体，溶剂合物或水合物。还公开了药物组合物和这些化合物的使用方法。

7. 发明申请

US20060167222A1 Sh2 domain binding inhibitors 失效
标题翻译： Sh2结构域结合抑制剂
公开(公告)号：US20060167222A1
公开(公告)日：2006-07-27
申请号：US10517717
申请日：2003-06-26
申请人： Terrence Burke , Chang-Qing Wei , Zhen-DaN Shi , Yang Gao
发明人： Terrence Burke , Chang-Qing Wei , Zhen-DaN Shi , Yang Gao
IPC分类号： C07K5/12 , C07D245/02
CPC分类号： C07F9/6515 , C07K5/06026 , C07K5/06191
摘要： Disclosed are compounds for SH2 domain binding inhibition, for example, a compound of formula (I), wherein R1 is a lipophile; R2, in combination with the phenyl ring, is a phenylphosphate mimic group or a protected phenylphosphate mimic group; R3 is hydrogen, azido, amino, carboxyalkyl, alkoxycarbonylalkyl, aminocarbonylalkyl, or alkylcarbonylamino, wherein the alkyl portion of R3 may be optionally substituted with a substituent selected from the group consisting of halo, hydroxy, carboxyl, amino, aminoalkyl, alkyl, alkoxy, and keto; R6 is a linker; AA is an amino acid; and n is 1 to 6; or a salt thereof. The conformationally compounds provide enhanced binding affinity with SH2 domain protein. Also disclosed are a pharmaceutical compositions and a method for inhibiting an SH2 domain from binding with a phosphoprotein.
摘要翻译：公开了用于SH2结构域结合抑制的化合物，例如式（I）的化合物，其中R 1是亲脂体; R 2与苯环组合是苯基磷酸酯模拟基团或被保护的苯基磷酸酯模拟基团; R 3是氢，叠氮基，氨基，羧基烷基，烷氧基羰基烷基，氨基羰基烷基或烷基羰基氨基，其中R 3的烷基部分可以任选地被选自由卤素，羟基，羧基，氨基，氨基烷基，烷基，烷氧基和酮基组成; R 6是连接体; AA是氨基酸; n为1〜6; 或其盐。构象化合物提供与SH2结构域蛋白质增强的结合亲和力。还公开了用于抑制SH2结构域与磷蛋白结合的药物组合物和方法。

8. 发明申请

US20050119163A1 SH2 domain binding inhibitors 审中-公开
标题翻译： SH2结构域结合抑制剂
公开(公告)号：US20050119163A1
公开(公告)日：2005-06-02
申请号：US10944699
申请日：2004-09-17
申请人： Terrence Burke , Zhen-Dan Shi , Sang-Uk Kang
发明人： Terrence Burke , Zhen-Dan Shi , Sang-Uk Kang
IPC分类号： A61K38/00 , C07K5/02 , C07K5/065 , A61K38/16 , A61K38/12 , C07K5/12
CPC分类号： C07K5/021 , A61K38/00 , C07K5/06078
摘要： Disclosed are compounds represented by the formula: or a pharmaceutically acceptable salt or isomer thereof, wherein R1-R6 are as defined in the specification. These compounds are targeted for use as inhibitors of SH2 domain binding with a phosphoprotein, and are contemplated for use in a number of diseases including cancer. Also disclosed are pharmaceutical compositions comprising a compound of the invention and a pharmaceutically acceptable carrier.
摘要翻译：公开了由下式表示的化合物或其药学上可接受的盐或异构体，其中R 1 -R 6如说明书中所定义。这些化合物被靶向用作与磷蛋白SH2结构域结合的抑制剂，并且被预期用于许多疾病，包括癌症。还公开了包含本发明化合物和药学上可接受的载体的药物组合物。

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