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1. 发明申请

WO2004003005A3 SH2 DOMAIN BINDING INHIBITORS 审中-公开
标题翻译： SH2域绑定抑制剂
公开(公告)号：WO2004003005A3
公开(公告)日：2007-02-01
申请号：PCT/US0319987
申请日：2003-06-26
申请人： US GOV HEALTH & HUMAN SERV , BURKE TERRENCE R JR , WEI CHANG-QING , VOIGT JOHANNES H , SHI ZHEN-DAN , GAO YANG
发明人： BURKE TERRENCE R JR , WEI CHANG-QING , VOIGT JOHANNES H , SHI ZHEN-DAN , GAO YANG
IPC分类号： A61K38/12 , A61K38/00 , A61K38/02 , A61K38/05 , A61K38/06 , A61K38/08 , A61P35/00 , C07C211/30 , C07F9/40 , C07K1/00 , C07K1/04 , C07K1/06 , C07K1/14 , C07K5/06 , C07K5/08 , C07K5/12 , C07K7/04 , C07K7/56 , G01N33/68
CPC分类号： C07K5/06191 , A61K38/00 , C07K5/0827 , C07K5/123 , C07K5/126 , C07K7/56
摘要： Disclosed are compounds for SH2 domain binding inhibition, for example, a compound of formula (I), wherein R 1 is a lipophile; R 2 , in combination with the phenyl ring, is a phenylphosphate mimic group or a protected phenylphosphate mimic group; R 3 is hydrogen, azido, amino, carboxyalkyl, alkoxycarbonylalkyl, aminocarbonylalkyl, or alkylcarbonylamino, wherein the alkyl portion of R 3 may be optionally substituted with a substituent selected from the group consisting of halo, hydroxy, carboxyl, amino, aminoalkyl, alkyl, alkoxy, and keto; R 6 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。

2. 发明申请

WO0216407A3 SH2 DOMAIN BINDING INHIBITORS 审中-公开
标题翻译： SH2域绑定抑制剂
公开(公告)号：WO0216407A3
公开(公告)日：2003-11-20
申请号：PCT/US0126078
申请日：2001-08-22
申请人： US GOV HEALTH & HUMAN SERV , BURKE TERRENCE R JR , WEI CHANG-QING , VOIGT JOHANNES H , GAO YANG
发明人： BURKE TERRENCE R JR , WEI CHANG-QING , VOIGT JOHANNES H , GAO YANG
IPC分类号： A61K38/00 , A61P35/00 , C07K5/06 , C07K5/065 , C07K5/08 , A61K38/05 , A61K38/06 , C07C211/30 , C07F9/40 , C07K5/087 , G01N33/68
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, 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 compounds of the present invention have the advantage that their conformation is constrained to provide enhanced binding affinity with SH2 domain protein. Also disclosed are a pharmaceutical composition comprising a pharmaceutically or pharmacologically acceptable carrier and a compound of the present invention, a method for inhibiting an SH2 domain from binding with a phosphoprotein comprising contacting an SH2 domain with a compound of the present invention, a method of preventing or treating a disease, state, or condition by the use of one or more of these compounds, and a method for preparing the compounds of the present invention. The present invention further provides intermediates useful in the preparation of the compounds.
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是亲油体; 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; 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R3的烷基部分可以任选地被选自卤素，羟基，羧基，氨基，氨基烷基，烷基，烷氧基，和酮 R6是连接体; AA是氨基酸; n为1〜6; 或其盐。本发明的化合物具有这样的优点：它们的构象被限制以提供与SH2结构域蛋白质的增强的结合亲和力。还公开了包含药学上可接受的载体和本发明化合物的药物组合物，一种抑制SH2结构域与磷蛋白结合的方法，包括使SH2结构域与本发明的化合物接触，一种预防或通过使用一种或多种这些化合物治疗疾病，状态或病症，以及制备本发明化合物的方法。本发明还提供可用于制备化合物的中间体。

3. 发明申请

WO2004065411A3 PEPTIDES 审中-公开
标题翻译：肽
公开(公告)号：WO2004065411A3
公开(公告)日：2005-01-27
申请号：PCT/US2004000669
申请日：2004-01-12
申请人： US GOV HEALTH & HUMAN SERV , BURKE TERRENCE R JR , LEE KYEONG , GAO YANG , PHAN JASON , WAUGH DAVID S
发明人： BURKE TERRENCE R JR , LEE KYEONG , GAO YANG , PHAN JASON , WAUGH DAVID S
IPC分类号： A61K38/00 , C07K5/093 , C07K38/00
CPC分类号： C07K5/0819 , A61K38/00 , Y02P20/55
摘要： Disclosed are compounds which are tripeptides of the formula P-A-B-C or prodrugs thereof, wherein A is an amino acid having a carboxy alkyl group (e.g., carboxy C1-C6 alkyl group), B is tyrosine, phenylalanine, or a substituted tyrosine or phenylalanine, C is a hydrophobic amino acid, and P is an amine protecting group protecting the amine end of A. Also disclosed are pharmaceutical compositions comprising such a compound and a pharmaceutically acceptable carrier, and a method of treating an animal, e.g., a human, exposed to or infected by Yersihia pestis. The compounds find use as anti-bioterrorism agents.
摘要翻译：公开了作为式PABC或其前药的三肽的化合物，其中A是具有羧基烷基的氨基酸（例如羧基C 1 -C 6烷基），B是酪氨酸，苯丙氨酸或取代的酪氨酸或苯丙氨酸，C 是疏水性氨基酸，P是保护A的胺末端的胺保护基。还公开了包含这种化合物和药学上可接受的载体的药物组合物，以及治疗动物（例如人）暴露于或感染鼠疫耶尔氏酵母。该化合物可用作抗生物恐怖剂。

4. 发明申请

WO0128577A3 INHIBITION OF CELL MOTILITY AND ANGIOGENESIS BY INHIBITORS OF THE GRB2 SH2-DOMAIN 审中-公开
标题翻译： GRB2 SH2域的抑制剂抑制细胞动力学和抗血管生成
公开(公告)号：WO0128577A3
公开(公告)日：2001-12-13
申请号：PCT/US0041423
申请日：2000-10-20
申请人： US GOV HEALTH & HUMAN SERV , BURKE TERRENCE R JR , BOTTARO DONALD P , ATABEY SAFIYE N , SORIANO JESUS V , BRECKENRIDGE DIANE E , YAO ZHU JUN , GAO YANG
发明人： BOTTARO DONALD P , ATABEY SAFIYE N , SORIANO JESUS V , BRECKENRIDGE DIANE E , YAO ZHU-JUN , GAO YANG
IPC分类号： C12Q1/02 , A61K38/00 , A61P35/00 , A61P35/02 , A61P35/04 , A61P43/00 , C07K5/08 , C07K5/093 , C12Q1/48 , A61K38/04 , A61K38/05 , A61K38/06 , A61K38/07
CPC分类号： A61K38/07 , A61K38/05 , A61K38/06 , C07K5/0819 , C07K5/0827
摘要： Disclosed are methods of inhibiting cell motility, for example, by inhibiting the binding between an intracellular transducer and a receptor protein tyrosine kinase, and more particularly by inhibiting hepatocyte growth factor (HGF) induced cell motility. The present invention also provides a method of inhibiting angiogenesis. The methods of the present invention employ peptides such as phosphotyrosyl mimetics. The present invention further provides methods of preventing and/or treating diseases, disorders, states, or conditions such as cancer, particularly metastatic cancer comprising administering to a mammal of interest one or more peptides of the present invention. Also disclosed are methods of blocking HGF, VEGF, or bFGF-stimulated migration, cell proliferation, and formation of capillary-like structures.
摘要翻译：公开了抑制细胞运动性的方法，例如通过抑制细胞内换能器和受体蛋白酪氨酸激酶之间的结合，更具体地通过抑制肝细胞生长因子（HGF）诱导的细胞运动性。本发明还提供抑制血管发生的方法。本发明的方法使用诸如磷酸二甲酰基模拟物之类的肽。本发明还提供了预防和/或治疗诸如癌症，特别是转移性癌症的疾病，病症，状态或病症的方法，其包括对感兴趣的哺乳动物施用本发明的一种或多种肽。还公开了阻断HGF，VEGF或bFGF刺激的迁移，细胞增殖和毛细血管样结构的形成的方法。

5. 发明专利

AU2916601A Inhibition of cell motility and angiogenesis 未知
公开(公告)号：AU2916601A
公开(公告)日：2001-04-30
申请号：AU2916601
申请日：2000-10-20
申请人： US GOV HEALTH & HUMAN SERV , BURKE TERRENCE R JR
发明人： BOTTARO DONALD P , ATABEY SAFIYE N , SORIANO JESUS V , BRECKENRIDGE DIANE E , YAO ZHU-JUN , GAO YANG
IPC分类号： C12Q1/02 , A61K38/00 , A61P35/00 , A61P35/02 , A61P35/04 , A61P43/00 , C07K5/08 , C07K5/093 , C12Q1/48
摘要： Disclosed are methods of inhibiting cell motility, for example, by inhibiting the binding between an intracellular transducer and a receptor protein tyrosine kinase, and more particularly by inhibiting hepatocyte growth factor (HGF) induced cell motility. The present invention also provides a method of inhibiting angiogenesis. The methods of the present invention employ peptides such as phosphotyrosyl mimetics. The present invention further provides methods of preventing and/or treating diseases, disorders, states, or conditions such as cancer, particularly metastatic cancer comprising administering to a mammal of interest one or more peptides of the present invention. Also disclosed are methods of blocking HGF, VEGF, or bFGF-stimulated migration, cell proliferation, and formation of capillary-like structures

6. 发明专利

CA2387922C INHIBITION OF CELL MOTILITY AND ANGIOGENESIS 未知
公开(公告)号：CA2387922C
公开(公告)日：2011-12-06
申请号：CA2387922
申请日：2000-10-20
申请人： US GOV HEALTH & HUMAN SERV
发明人： BOTTARO DONALD P , ATABEY SAFIYE N , SORIANO JESUS V , BRECKENRIDGE DIANE E , YAO ZHU-JUN , GAO YANG , BURKE TERRENCE R JR
IPC分类号： A61K38/04 , C12Q1/02 , A61K38/00 , A61K38/05 , A61K38/06 , A61K38/07 , A61P35/00 , A61P35/02 , A61P35/04 , A61P43/00 , C07K5/08 , C07K5/093 , C12Q1/48
摘要： Disclosed are methods of inhibiting cell motility, for example, by inhibiting the binding between an intracellular transducer and a receptor protein tyrosine kinase, and more particularly by inhibiting hepatocyte growth factor (HGF) induced cell motility. The present invention also provides a method of inhibiting angiogenesis. The methods of the present invention employ peptides such as phosphotyrosyl mimetics. The present invention further provides methods of preventing and/or treating diseases, disorders, states, or conditions such as cancer, particularly metastatic cancer comprising administering to a mammal of interest one or more peptides of the present invention. Also disclosed are methods of blocking HGF, VEGF, or bFGF-stimulated migration, cell proliferation, and formation of capillary-like structures.

7. 发明专利

AU8513301A Sh2 domain binding inhibitors 未知
公开(公告)号：AU8513301A
公开(公告)日：2002-03-04
申请号：AU8513301
申请日：2001-08-22
申请人： US GOV HEALTH & HUMAN SERV
发明人： BURKE TERRENCE R JR , WEI CHANG-QING , VOIGT JOHANNES H , GAO YANG
IPC分类号： A61K38/00 , A61P35/00 , C07K5/06 , C07K5/065 , C07K5/08 , A61K38/05 , A61K38/06 , C07C211/30 , C07F9/40 , C07K5/087 , G01N33/68

8. 发明专利

DE60034959T2 未知
公开(公告)号：DE60034959T2
公开(公告)日：2008-01-17
申请号：DE60034959
申请日：2000-10-20
申请人： US GOV HEALTH & HUMAN SERV
发明人： BOTTARO DONALD P , ATABEY SAFIYE N , SORIANO JESUS V , BRECKENRIDGE DIANE E , YAO ZHU-JUN , GAO YANG , BURKE TERRENCE R JR
IPC分类号： A61K38/04 , C12Q1/02 , A61K38/00 , A61K38/05 , A61K38/06 , A61K38/07 , A61P35/00 , A61P35/02 , A61P35/04 , A61P43/00 , C07K5/08 , C07K5/093 , C12Q1/48
摘要： Disclosed are methods of inhibiting cell motility, for example, by inhibiting the binding between an intracellular transducer and a receptor protein tyrosine kinase, and more particularly by inhibiting hepatocyte growth factor (HGF) induced cell motility. The present invention also provides a method of inhibiting angiogenesis. The methods of the present invention employ peptides such as phosphotyrosyl mimetics. The present invention further provides methods of preventing and/or treating diseases, disorders, states, or conditions such as cancer, particularly metastatic cancer comprising administering to a mammal of interest one or more peptides of the present invention. Also disclosed are methods of blocking HGF, VEGF, or bFGF-stimulated migration, cell proliferation, and formation of capillary-like structures

9. 发明专利

ES2287048T3 INHBICION DE LA MOTILIDAD CELULAR Y LA ANGIOGNESIS MEDIANTE NHIBIDORES DEL DOMINIO GBR2SH2. 未知
公开(公告)号：ES2287048T3
公开(公告)日：2007-12-16
申请号：ES00992431
申请日：2000-10-20
申请人： US GOV HEALTH & HUMAN SERV
发明人： BOTTARO DONALD P , ATABEY SAFIYE N , SORIANO JESUS V , BRECKENRIDGE DIANE E , YAO ZHU-JUN , GAO YANG
IPC分类号： A61K38/04 , C12Q1/02 , A61K38/00 , A61K38/05 , A61K38/06 , A61K38/07 , A61P35/00 , A61P35/02 , A61P35/04 , A61P43/00 , C07K5/08 , C07K5/093 , C12Q1/48
摘要： Uso de un compuesto que inhibe la actividad de señalización celular y la actividad de motilidad celular, para la fabricación de un medicamento para tratar el cáncer, donde dicho cáncer se selecciona del grupo constituido por cáncer de colon, cáncer de pulmón, cáncer de tiroides, cáncer renal, sarcoma, glioblastoma, melanoma y metástasis de cáncer, donde dicho constituido carece sustancialmente de citotoxicidad, y posee la fórmula I: en la que n es de 0 a 15 y PTI es un radical de fenilalanina que posee un anillo fenilo, un extremo amino y un extremo carboxilo, donde el anillo fenilo posee uno o más sustituyentes seleccionados del grupo constituido por formilo, carboxialquilo, dicarboxialquilo, dicarboxihaloalquilo y dicarboxihaloalquiloxi, donde la porción alquilo de los sustituyentes puede estar insustituida o sustituida con un sustituyente seleccionado del grupo constituido por halo, hidroxi, carboxilo, amino, aminoalquilo, alquilo, alcoxi y ceto; y X es un resto unido al nitrógeno de PTIy se selecciona del grupo constituido por alquilcarbonilo, oxalilo, alquilaminocarbonilo, arilaminooxalilo, arilalquilaminooxalilo, alcoxioxalilo, carboxialquilo, carbonilo, heterociclil carbonilo, heterociclilalquil carbonilo, arilalquil heterociclilalquil carbonilo, ariloxicarbonilo y arilalcoxicarbonilo, donde las porciones arilo y alquilo de los sustituyentes pueden estar insustituidos o sustituidos con un sustituyente seleccionado del grupo constituido por halo, hidroxi, carboxilo, amino, aminoalquilo, alquilo, alcoxi y ceto; y la porción heterociclilo de Y contiene al menos 4 heteroátomos seleccionados del grupo constituido por O, N y S; AA es un aminoácido, cuyo extremo amino está unido al extremo carboxilo de PTI; e Y es un arilaquilamino o arilheterociclil alquilamino; o una sal del mismo.

10. 发明专利

DE60034959D1 未知
公开(公告)号：DE60034959D1
公开(公告)日：2007-07-05
申请号：DE60034959
申请日：2000-10-20
申请人： US GOV HEALTH & HUMAN SERV
发明人： BOTTARO DONALD P , ATABEY SAFIYE N , SORIANO JESUS V , BRECKENRIDGE DIANE E , YAO ZHU-JUN , GAO YANG , BURKE TERRENCE R JR
IPC分类号： A61K38/04 , C12Q1/02 , A61K38/00 , A61K38/05 , A61K38/06 , A61K38/07 , A61P35/00 , A61P35/02 , A61P35/04 , A61P43/00 , C07K5/08 , C07K5/093 , C12Q1/48
摘要： Disclosed are methods of inhibiting cell motility, for example, by inhibiting the binding between an intracellular transducer and a receptor protein tyrosine kinase, and more particularly by inhibiting hepatocyte growth factor (HGF) induced cell motility. The present invention also provides a method of inhibiting angiogenesis. The methods of the present invention employ peptides such as phosphotyrosyl mimetics. The present invention further provides methods of preventing and/or treating diseases, disorders, states, or conditions such as cancer, particularly metastatic cancer comprising administering to a mammal of interest one or more peptides of the present invention. Also disclosed are methods of blocking HGF, VEGF, or bFGF-stimulated migration, cell proliferation, and formation of capillary-like structures

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