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1. 发明申请

WO2010011666A3 INDOLINE SCAFFOLD SHP-2 INHIBITORS AND CANCER TREATMENT METHOD 审中-公开
标题翻译： INDOLINE SCAFFOLD SHP-2抑制剂和癌症治疗方法
公开(公告)号：WO2010011666A3
公开(公告)日：2010-04-22
申请号：PCT/US2009051276
申请日：2009-07-21
申请人： UNIV SOUTH FLORIDA , WU JIE , LAWRENCE NICHOLAS J , SEBTI SAID M
发明人： WU JIE , LAWRENCE NICHOLAS J , SEBTI SAID M
IPC分类号： C07D403/12 , A61K31/496 , A61P35/00
CPC分类号： C07D405/06 , C07D209/08 , C07D215/36
摘要： The subject invention concerns methods and compounds for inhibiting Shp2. In one embodiment, a compound of the invention has a chemical structure as shown in formula I or II: wherein X, Y, and Z are independently N or S; R1 is cycloalkyl, heterocycloalkyl, aryl, or heteroaryl, any of which can be optionally substituted with one or more of halogen; alkyl; heteroalkyl; -COOH; -C(R3)3, wherein R3 can independently be any of -H or halogen; or -OR4, wherein R4 can be any of H, alkyl. or heteroalkyl; R2 is alkyl, alkylcarbonyl, heteroalkylcarbonyl, aryl, arylcarbonyl, heterocycloalkylcarbonyl, cycloalkylcarbonyl, or -C(O)NR6R7, any of which can be optionally substituted with one or more of halogen; alkyl; heteroalkyl; carbonyl; -OR4, wherein R4 can be -H, alkyl, or heteroalkyl; -OH; -C(RO3)3, wherein R3 can independently be any of -H or halogen; aryl, which can be substituted with one or more of halogen or - OR4; heterocycloalkyl; or -C(O)OR5, wherein R5 can be -H or alkyl; R6 and R7 are independently -H, alkyl, heteroalkyl, aryl, or heteroaryl; and R1 is H or alkyl; or a pharmaceutically acceptable salt or hydrate thereof.
摘要翻译：本发明涉及用于抑制Shp2的方法和化合物。在一个实施方案中，本发明的化合物具有如式I或II所示的化学结构：其中X，Y和Z独立地为N或S; R 1是环烷基，杂环烷基，芳基或杂芳基，它们中的任何一个可以任选地被一个或多个卤素取代; 烷基; 杂; -COOH; -C（R 3）3，其中R 3可以独立地为-H或卤素中的任何一个; 或-OR 4，其中R 4可以是H，烷基中的任何一个。或杂烷基; R 2是烷基，烷基羰基，杂烷基羰基，芳基，芳基羰基，杂环烷基羰基，环烷基羰基或-C（O）NR 6 R 7，它们中的任何一个可以任选地被一个或多个卤素取代; 烷基; 杂; 羰; -OR 4，其中R 4可以是-H，烷基或杂烷基; -哦; -C（RO 3）3，其中R 3可以独立地为-H或卤素中的任何一个; 芳基，其可以被一个或多个卤素或-OR 4取代; 杂环; 或-C（O）OR 5，其中R 5可以是-H或烷基; R6和R7独立地为-H，烷基，杂烷基，芳基或杂芳基; 并且R1是H或烷基; 或其药学上可接受的盐或水合物。

2. 发明申请

WO2009135000A3 INHIBITION OF SHP2/PTPN11 PROTEIN TYROSINE PHOSPHATASE BY NSC-117199 AND ANALOGS 审中-公开
标题翻译： NSC-117199和模拟物对SHP2 / PTPN11蛋白酪氨酸磷酸化酶的抑制作用
公开(公告)号：WO2009135000A3
公开(公告)日：2010-02-18
申请号：PCT/US2009042305
申请日：2009-04-30
申请人： H LEE MOFFITT CANCER CT AND RE , UNIV SOUTH FLORIDA , WU JIE , LAWRENCE NICHOLAS J , SEBTI SAID M , LAWRENCE HARSHANI R
发明人： WU JIE , LAWRENCE NICHOLAS J , SEBTI SAID M , LAWRENCE HARSHANI R
IPC分类号： A61K31/404 , A61P35/00 , C07D209/34
CPC分类号： C07D209/40
摘要： Protein tyrosine phosphatase (PTP) Shp2 is a non-receptor PTP that involved in cell signaling and regulation of cell proliferation, differentiation, and migration. Shp2 mediates activation of kinases that are involved in the pathogenesis of human carcinoma. NSC-117199 was identified as a porent inhibitor of the protein tyrosine phosphatase (PTPa) Shp2. A focused library of analogs incorporating an isatin scaffold was designed and evaluated for inhibition of Shp2 and Shp1 PTP activities. Several compounds were identified that selectively inhibit Shp2 over Shp1 and PTP1B with low to sub-micromolar activity. Also disclosed are methods of inhibiting a protein tyrosine phosphatase in a cell and treating cancer through selective inhibition of Shp2.
摘要翻译：蛋白酪氨酸磷酸酶（PTP）Shp2是参与细胞信号传导和调节细胞增殖，分化和迁移的非受体PTP。 Shp2介导参与人类癌症发病机制的激酶活化。 NSC-117199被鉴定为蛋白酪氨酸磷酸酶（PTPa）Shp2的细胞抑制剂。设计了一个重点的掺入靛红支架的类似物库，并评估了Shp2和Shp1 PTP活性的抑制作用。鉴定出几种化合物选择性地抑制Shp1与Shp1和PTP1B的低亚微摩尔活性。还公开了抑制细胞中的蛋白质酪氨酸磷酸酶并通过选择性抑制Shp2治疗癌症的方法。

3. 发明申请

WO2012135697A3 NOVEL RHO KINASE INHIBITORS AND METHODS OF USE 审中-公开
标题翻译：新型RHO激酶抑制剂及其使用方法
公开(公告)号：WO2012135697A3
公开(公告)日：2013-01-17
申请号：PCT/US2012031575
申请日：2012-03-30
申请人： H LEE MOFFITT CANCER CT & RES , LAWRENCE NICHOLAS J , SEBTI SAID M , PIREDDU ROBERTA
发明人： LAWRENCE NICHOLAS J , SEBTI SAID M , PIREDDU ROBERTA
IPC分类号： C07D239/48 , A61K31/506 , A61P35/00 , C07D403/04
CPC分类号： A61K31/52 , A61K31/505 , A61K31/506 , A61K45/06 , C07D239/48 , C07D401/04 , C07D403/04 , C07D403/12 , C07D403/14 , C07D417/12 , C07D473/34 , A61K2300/00
摘要： The subject invention concerns materials and methods for treating diseases and disorders associated with expression of Rho associated kinases (ROCKs). Examples of diseases and disorders contemplated within the scope of the invention include, but are not limited to, oncological disorders, cardiovascular diseases, CNS disorders, and inflammatory disorders. In one embodiment, a method of the invention comprises administering a therapeutically effective amount of one or more compounds of the present invention, or a composition comprising the compounds, to a person or animal in need of treatment. The subject invention also concerns compounds that inhibit ROCKs, and compositions that comprise the inhibitor compounds of the invention. Compounds contemplated within the scope of the invention include, but are not limited to, those compounds shown in Table (5).
摘要翻译：本发明涉及用于治疗与Rho相关激酶（ROCK）的表达相关的疾病和病症的材料和方法。在本发明范围内考虑的疾病和病症的实例包括但不限于肿瘤疾病，心血管疾病，中枢神经系统疾病和炎症性疾病。在一个实施方案中，本发明的方法包括将治疗有效量的一种或多种本发明化合物或包含该化合物的组合物施用于需要治疗的人或动物。本发明还涉及抑制ROCK的化合物，以及包含本发明的抑制剂化合物的组合物。涵盖在本发明范围内的化合物包括但不限于表（5）所示的那些化合物。

4. 发明申请

WO2012135641A3 AURORA KINASE INHIBITORS AND METHODS OF MAKING AND USING THEREOF 审中-公开
标题翻译： AURORA激酶抑制剂及其制备和使用方法
公开(公告)号：WO2012135641A3
公开(公告)日：2012-12-27
申请号：PCT/US2012031494
申请日：2012-03-30
申请人： H LEE MOFFITT CANCER CT AND RES INST , SEBTI SAID M , SCHOENBRUNN ERNST , LAWRENCE NICHOLAS J , LAWRENCE HARSHANI R , MARTIN MATTHEW P
发明人： SEBTI SAID M , SCHOENBRUNN ERNST , LAWRENCE NICHOLAS J , LAWRENCE HARSHANI R , MARTIN MATTHEW P
IPC分类号： C07D239/32 , A61K31/506 , A61P35/00 , C07D403/12 , C07D413/12
CPC分类号： A61K31/505 , A61K31/506 , A61K31/5377 , A61K31/635 , C07D239/48 , C07D295/135 , C07D401/12 , C07D403/12 , C07D413/12 , G01N33/5011
摘要： Described herein are inhibitors of Aurora kinase and their use in the treatment of cancer. Methods of screening for selective inhibitors of Aurora kinases are also disclosed.
摘要翻译：本文描述了极光激酶的抑制剂及其在治疗癌症中的用途。还公开了筛选Aurora激酶的选择性抑制剂的方法。

5. 发明申请

WO2011130740A2 PYRIDYLTHIAZOLE-BASED UREAS AS INHIBITORS OF RHO ASSOCIATED PROTEIN KINASE (ROCK) AND METHODS OF USE 审中-公开
标题翻译：作为RHO相关蛋白激酶（ROCK）的抑制剂的基于吡啶并噻唑的UREAS和使用方法
公开(公告)号：WO2011130740A2
公开(公告)日：2011-10-20
申请号：PCT/US2011032893
申请日：2011-04-18
申请人： H LEE MOFFITT CANCER CT & RES , LAWRENCE NICHOLAS J , PIREDDU ROBERTA , SEBTI SAID M
发明人： LAWRENCE NICHOLAS J , PIREDDU ROBERTA , SEBTI SAID M
IPC分类号： C07D417/04 , A61K31/4436 , A61K31/4439 , A61P9/00 , A61P29/00 , C07D417/14
CPC分类号： C07D417/04 , C07D417/14
摘要： Compounds and compositions having activity as inhibitors of Rho-associated proteinkinases (ROCKs), and methods of making and using the subject compounds are disclosed.
摘要翻译：公开了具有作为Rho相关蛋白激酶（ROCK）的抑制剂活性的化合物和组合物，以及制备和使用本发明化合物的方法。

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