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1. 发明申请

US20070197509A1 Compositions and methods for modulating gated ion channels 审中-公开
公开(公告)号：US20070197509A1
公开(公告)日：2007-08-23
申请号：US11643640
申请日：2006-12-21
申请人： Kazimierz Babinski , Rahul Vohra , Jean-Louis Brochu , Deogratias Ntirampebura , Chang-Qing Wei , Robert Zamboni
发明人： Kazimierz Babinski , Rahul Vohra , Jean-Louis Brochu , Deogratias Ntirampebura , Chang-Qing Wei , Robert Zamboni
IPC分类号： A61K31/551 , A61K31/5377 , A61K31/517 , A61K31/4709 , C07D413/02 , C07D401/02 , C07D403/02
CPC分类号： C07D239/91 , A61K31/47 , A61K31/4709 , A61K31/496 , A61K31/517 , A61K31/5377 , A61K31/551 , C07D215/233 , C07D215/44 , C07D215/46 , C07D215/52 , C07D239/94 , C07D401/12 , C07D401/14 , C07D405/12
摘要： The present invention relates to compositions and methods to modulate the activity of gated ion channels.

2. 发明申请

US20080004282A1 Compositions and methods for modulating gated ion channels 审中-公开
公开(公告)号：US20080004282A1
公开(公告)日：2008-01-03
申请号：US11786415
申请日：2007-04-10
申请人： Rahul Vohra , Zhonghong Gan , Chang-Qing Wei , Stephen Price , Hazel Dyke , Elsa Dechaux
发明人： Rahul Vohra , Zhonghong Gan , Chang-Qing Wei , Stephen Price , Hazel Dyke , Elsa Dechaux
IPC分类号： A61K31/50 , A61K31/47 , A61P1/00 , C07D217/00 , C07D401/02 , C12N5/00 , C07D401/10 , C07D217/14 , A61P13/00 , A61K31/4965
CPC分类号： C07D471/04 , C07D209/40
摘要： The present invention relates to compositions and methods to modulate the activity of gated ion channels.

3. 发明申请

US20080004272A1 Compositions and methods for modulating gated ion channels 审中-公开
标题翻译：用于调节门控离子通道的组合物和方法
公开(公告)号：US20080004272A1
公开(公告)日：2008-01-03
申请号：US11786439
申请日：2007-04-10
申请人： Rahul Vohra , Chang-Qing Wei , Zhonghong Gan , Joachim Demnitz , Philip Ahring
发明人： Rahul Vohra , Chang-Qing Wei , Zhonghong Gan , Joachim Demnitz , Philip Ahring
IPC分类号： A61K31/535 , A61K31/40 , A61K31/44 , C07D209/00 , C07D403/00 , C07D413/00 , C07D401/00 , A61P1/00 , A61K31/497
CPC分类号： C07D471/04 , C07D209/40
摘要： The present invention relates to compositions and methods to modulate the activity of gated ion channels.
摘要翻译：本发明涉及调节门控离子通道活性的组合物和方法。

4. 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。

5. 发明授权

US06977241B2 SH2 domain binding inhibitors 失效
标题翻译： SH2结构域结合抑制剂
公开(公告)号：US06977241B2
公开(公告)日：2005-12-20
申请号：US10362231
申请日：2001-08-22
申请人： Terrence R. Burke, Jr. , Chang-Qing Wei , Johannes H. Voigt , Yang Gao
发明人： Terrence R. Burke, Jr. , Chang-Qing Wei , Johannes H. Voigt , Yang Gao
IPC分类号： A61K38/00 , A61P35/00 , C07K5/06 , C07K5/065 , C07K5/08 , A61K38/02 , C07K2/00
CPC分类号： C07K5/06078 , A61K38/00 , C07K5/06191 , C07K5/0827
摘要： Disclosed are compounds for SH2 domain binding inhibition. For example, disclosed is a compound of formula (I) wherein R1 is a lipophile; R2, in combination with the phenyl ring, forms 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. Also disclosed are a pharmaceutical composition, a method for inhibiting an SH2 domain from binding with a phosphoprotein and a method of treating breast cancer.
摘要翻译：公开了用于SH2结构域结合抑制的化合物。例如，公开了式（I）的化合物，其中R 1是亲脂体; R 2与苯环组合形成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。还公开了药物组合物，抑制SH2结构域与磷蛋白结合的方法和治疗乳腺癌的方法。

6. 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。

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