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1. 发明授权

US09174969B2 Indoline scaffold SHP-2 inhibitors and cancer treatment method 有权
标题翻译：吲哚酚支架SHP-2抑制剂和癌症治疗方法
公开(公告)号：US09174969B2
公开(公告)日：2015-11-03
申请号：US13055113
申请日：2009-07-21
申请人： Jie Wu , Nicholas J. Lawrence , Said M. Sebti
发明人： Jie Wu , Nicholas J. Lawrence , Said M. Sebti
IPC分类号： A61K31/496 , C07D209/08 , C07D215/36 , C07D405/06
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(R3)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 R′ is H or alkyl; or a pharmaceutically acceptable salt or hydrate thereof.
摘要翻译：本发明涉及抑制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，其中任何一个可以任选被一个或多个卤素取代; 烷基; 杂烷基; -COOH; -C（R 3）3，其中R 3可以独立地为-H或卤素; 或-OR 4，其中R 4可以是H，烷基或杂烷基中的任何一个; 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，其中任何一个可以任选被一个或多个卤素取代; 烷基; 杂烷基; 羰; -OR4，其中R4可以是-H，烷基或杂烷基; -哦; -C（R 3）3，其中R 3可以独立地为-H或卤素; 芳基，其可被一个或多个卤素或-OR 4取代; 杂环烷基; 或-C（O）OR 5，其中R 5可以是-H或烷基; R6和R7独立地是-H，烷基，杂烷基，芳基或杂芳基; 和R'是H或烷基; 或其药学上可接受的盐或水合物。

2. 发明授权

US08987474B2 Inhibition of Shp2/PTPN11 protein tyrosine phosphatase by NSC-87877, NSC-117199 and their analogs 有权
标题翻译： NSC-87877，NSC-117199及其类似物抑制Shp2 / PTPN11蛋白酪氨酸磷酸酶
公开(公告)号：US08987474B2
公开(公告)日：2015-03-24
申请号：US11733023
申请日：2007-04-09
申请人： Jie Wu , Nicholas J. Lawrence , Said M. Sebti , Harshani R. Lawrence
发明人： Jie Wu , Nicholas J. Lawrence , Said M. Sebti , Harshani R. Lawrence
IPC分类号： A61K31/404 , A61K31/405 , C07D209/40
CPC分类号： A61K31/405 , C07D209/40
摘要： Compounds and associated methods for inhibiting a protein tyrosine phosphatase. By a combination of experimental and virtual screenings of the NCI Diversity Set chemical library, NSC-87877 and NSC-117199 have been identified as Shp2 PTP inhibitors. Significantly, NSC-87877 is active in cell-based assays and has no detectable off-target effects in the EGF-stimulated Erk 1/2 activation pathway. Additionally, a number of analogs of NSC-117199 have been produced. These analogs exhibit enhanced protein tyrosine phosphatase inhibition and are found to be potent and/or selective inhibitors of Shp1 and/or Shp2 protein tyrosine phosphatases.
摘要翻译：用于抑制蛋白质酪氨酸磷酸酶的化合物和相关方法。通过NCI多样性集化学库的实验和虚拟筛选的组合，NSC-87877和NSC-117199已被鉴定为Shp2 PTP抑制剂。显着地，NSC-87877在基于细胞的测定中是有活性的，并且在EGF刺激的Erk 1/2激活途径中没有检测到的脱靶作用。此外，已经生产了许多NSC-117199的类似物。这些类似物表现出增强的蛋白酪氨酸磷酸酶抑制，并且被发现是Shp1和/或Shp2蛋白酪氨酸磷酸酶的有效和/或选择性抑制剂。

3. 发明申请

US20080176309A1 Inhibition of Shp2/PTPN11 Protein Tyrosine Phosphatase by NSC-87877, NSC-117199 and Their Analogs 有权
标题翻译： NSC-87877，NSC-117199及其类似物抑制Shp2 / PTPN11蛋白酪氨酸磷酸酶
公开(公告)号：US20080176309A1
公开(公告)日：2008-07-24
申请号：US11733023
申请日：2007-04-09
申请人： Jie Wu , Nicholas J. Lawrence , Said M. Sebti , Harshani R. Lawrence
发明人： Jie Wu , Nicholas J. Lawrence , Said M. Sebti , Harshani R. Lawrence
IPC分类号： A61K31/404 , C12N9/99
CPC分类号： A61K31/405 , C07D209/40
摘要： Compounds and associated methods for inhibiting a protein tyrosine phosphatase. By a combination of experimental and virtual screenings of the NCI Diversity Set chemical library, NSC-87877 and NSC-117199 have been identified as Shp2 PTP inhibitors. Significantly, NSC-87877 is active in cell-based assays and has no detectable off-target effects in the EGF-stimulated Erk1/2 activation pathway. Additionally, a number of analogs of NSC-117199 have been produced. These analogs exhibit enhanced protein tyrosine phosphatase inhibition and are found to be potent and/or selective inhibitors of Shp1 and/or Shp2 protein tyrosine phosphatases.
摘要翻译：用于抑制蛋白质酪氨酸磷酸酶的化合物和相关方法。通过NCI多样性集化学库的实验和虚拟筛选的组合，NSC-87877和NSC-117199已被鉴定为Shp2 PTP抑制剂。显着地，NSC-87877在基于细胞的测定中是有活性的，并且在EGF刺激的Erk1 / 2激活途径中没有检测到的脱靶作用。此外，已经生产了许多NSC-117199的类似物。这些类似物表现出增强的蛋白酪氨酸磷酸酶抑制，并且被发现是Shp1和/或Shp2蛋白酪氨酸磷酸酶的有效和/或选择性抑制剂。

4. 发明申请

US20110190315A1 INDOLINE SCAFFOLD SHP-2 INHIBITORS AND CANCER TREATMENT METHOD 有权
标题翻译： INDOLINE SCAFFLE SHP-2抑制剂和癌症治疗方法
公开(公告)号：US20110190315A1
公开(公告)日：2011-08-04
申请号：US13055113
申请日：2009-07-21
申请人： Jie Wu , Nicholas J. Lawrence , Said M. Sebti
发明人： Jie Wu , Nicholas J. Lawrence , Said M. Sebti
IPC分类号： A61K31/496 , C07D403/12 , C12N5/071 , C12N5/09 , A61P35/00 , A61P35/02
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(R3)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 R′ is H or alkyl; or a pharmaceutically acceptable salt or hydrate thereof.
摘要翻译：本发明涉及抑制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，其中任何一个可以任选被一个或多个卤素取代; 烷基; 杂烷基; -COOH; -C（R 3）3，其中R 3可以独立地为-H或卤素; 或-OR 4，其中R 4可以是H，烷基或杂烷基中的任何一个; 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，其中任何一个可以任选被一个或多个卤素取代; 烷基; 杂烷基; 羰; -OR4，其中R4可以是-H，烷基或杂烷基; -哦; -C（R 3）3，其中R 3可以独立地为-H或卤素; 芳基，其可被一个或多个卤素或-OR 4取代; 杂环烷基; 或-C（O）OR 5，其中R 5可以是-H或烷基; R6和R7独立地是-H，烷基，杂烷基，芳基或杂芳基; 和R'是H或烷基; 或其药学上可接受的盐或水合物。

5. 发明申请

US20170000787A1 AURORA KINASE INHIBITORS AND METHODS OF MAKING AND USING THEREOF 有权
标题翻译： AURORA激酶抑制剂及其制备和使用方法
公开(公告)号：US20170000787A1
公开(公告)日：2017-01-05
申请号：US15012428
申请日：2016-02-01
申请人： Said M. Sebti , Ernst Schönbrunn , Nicholas J. Lawrence , Harshani R. Lawrence , Matthew P. Martin
发明人： Said M. Sebti , Ernst Schönbrunn , Nicholas J. Lawrence , Harshani R. Lawrence , Matthew P. Martin
IPC分类号： A61K31/505 , A61K31/506 , A61K31/635 , A61K31/5377
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：本文描述的是Aurora激酶的抑制剂及其在治疗癌症中的用途。还公开了选择性抑制Aurora激酶的筛选方法。

6. 发明授权

US09221808B2 Pyridylthiazole-based ureas as inhibitors of Rho associated protein kinase (ROCK) and methods of use 有权
标题翻译：基于吡啶基噻唑的尿素作为Rho相关蛋白激酶（ROCK）的抑制剂和使用方法
公开(公告)号：US09221808B2
公开(公告)日：2015-12-29
申请号：US13640385
申请日：2011-04-18
申请人： Nicholas J. Lawrence , Roberta Pireddu , Said M. Sebti
发明人： Nicholas J. Lawrence , Roberta Pireddu , Said M. Sebti
IPC分类号： C07D417/04 , 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相关蛋白蛋白酶（ROCK）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。

7. 发明授权

US09597329B2 Aurora kinase inhibitors and methods of making and using thereof 有权
公开(公告)号：US09597329B2
公开(公告)日：2017-03-21
申请号：US15012428
申请日：2016-02-01
申请人： Said M. Sebti , Ernst Schönbrunn , Nicholas J. Lawrence , Harshani R. Lawrence , Matthew P. Martin
发明人： Said M. Sebti , Ernst Schönbrunn , Nicholas J. Lawrence , Harshani R. Lawrence , Matthew P. Martin
IPC分类号： A61K31/506 , A61K31/505 , A61K31/5377 , A61K31/635
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.

8. 发明申请

US20110201576A1 Small molecule inhibitors of stat3 with anti-tumor activity 审中-公开
标题翻译： stat3的小分子抑制剂具有抗肿瘤活性
公开(公告)号：US20110201576A1
公开(公告)日：2011-08-18
申请号：US12931607
申请日：2011-02-04
申请人： James Turkson , Said M. Sebti , Wayne Guida , Man Lun Yip , Nicholas J. Lawrence , Harshani Lawrence , Benjamin Greedy
发明人： James Turkson , Said M. Sebti , Wayne Guida , Man Lun Yip , Nicholas J. Lawrence , Harshani Lawrence , Benjamin Greedy
IPC分类号： A61K31/655 , A61K31/235 , A61K31/444 , A61K31/473 , A61K31/195 , A61K31/24 , A61K31/255 , A61P35/00 , C12N5/00
CPC分类号： A61K31/196 , A61K31/00 , A61K31/18 , A61K45/06 , C07C235/84 , C07C309/73 , C07C311/19 , G01N33/5011 , G01N33/5088 , G01N33/574 , G01N33/57407 , G01N33/57484 , A61K2300/00
摘要： The present invention concerns compounds, compositions containing these compounds, and methods of using these compounds and compositions as inhibitors of Stat3 signaling, Stat3 dimerization, Stat3-DNA binding, Stat5-DNA binding, and/or aberrant cell growth in vitro or in vivo, e.g., as anti-cancer agents for treatment of cancer, such as breast cancer. The compounds of the invention include, but are not limited to, NSC 74859 (S3I-201), NSC 42067, NSC 59263, NSC 75912, NSC 11421, NSC 91529, NSC 263435, and pharmaceutically acceptable salts and analogs of the foregoing. Other non-malignant diseases characterized by proliferation of cells that may be treated using the compounds of the invention, but are not limited to, cirrhosis of the liver; graft rejection; restenosis; and disorders characterized by a proliferation of T cells such as autoimmune diseases, e.g., type 1 diabetes, lupus and multiple sclerosis. The invention further includes an in-vitro screening test for the presence of malignant cells in a mammalian tissue; a method of identifying inhibitors of constitutive Stat3 activation, Stat3-DNA binding, Stat5-DNA binding, and/or Stat3 dimerization; and a method of identifying anti-cancer agents.
摘要翻译：本发明涉及化合物，含有这些化合物的组合物，以及在体外或体内使用这些化合物和组合物作为Stat3信号传导，Stat3二聚化，Stat3-DNA结合，Stat5-DNA结合和/或异常细胞生长的抑制剂的方法，例如作为用于治疗癌症的抗癌剂，例如乳腺癌。本发明的化合物包括但不限于NSC 74859（S3I-201），NSC 42067，NSC 59263，NSC 75912，NSC 11421，NSC 91529，NSC 263435及其前述的药学上可接受的盐和类似物。以可用本发明化合物治疗但不限于肝硬化的细胞增殖为特征的其它非恶性疾病; 移植排斥反应再狭窄; 以及以T细胞增殖为特征的疾病，例如自身免疫疾病，例如1型糖尿病，狼疮和多发性硬化。本发明还包括在哺乳动物组织中存在恶性细胞的体外筛选试验; 识别组成型Stat3激活抑制剂，Stat3-DNA结合，Stat5-DNA结合和/或Stat3二聚化的方法; 以及鉴定抗癌剂的方法。

9. 发明授权

US07960434B2 Small molecule inhibitors of STAT3 with anti-tumor activity 有权
标题翻译：具有抗肿瘤活性的STAT3的小分子抑制剂
公开(公告)号：US07960434B2
公开(公告)日：2011-06-14
申请号：US11805217
申请日：2007-05-21
申请人： James Turkson , Said M. Sebti , Wayne Guida , Man Lun Yip , Nicholas J. Lawrence , Harshani Lawrence , Benjamin Greedy
发明人： James Turkson , Said M. Sebti , Wayne Guida , Man Lun Yip , Nicholas J. Lawrence , Harshani Lawrence , Benjamin Greedy
IPC分类号： A01N41/02 , A61K31/255 , A01N37/18 , A61K31/165
CPC分类号： A61K31/196 , A61K31/00 , A61K31/18 , A61K45/06 , C07C235/84 , C07C309/73 , C07C311/19 , G01N33/5011 , G01N33/5088 , G01N33/574 , G01N33/57407 , G01N33/57484 , A61K2300/00
摘要： The present invention concerns compounds, compositions containing these compounds, and methods of using these compounds and compositions as inhibitors of Stat3 signaling, Stat3 dimerization, Stat3-DNA binding, Stat5-DNA binding, and/or aberrant cell growth in vitro or in vivo, e.g., as anti-cancer agents for treatment of cancer, such as breast cancer. The compounds of the invention include, but are not limited to, NSC 74859 (S3I-201), NSC 42067, NSC 59263, NSC 75912, NSC 11421, NSC 91529, NSC 263435, and pharmaceutically acceptable salts and analogs of the foregoing. Other non-malignant diseases characterized by proliferation of cells that may be treated using the compounds of the invention, but are not limited to, cirrhosis of the liver; graft rejection; restenosis; and disorders characterized by a proliferation of T cells such as autoimmune diseases, e.g., type 1 diabetes, lupus and multiple sclerosis. The invention further includes an in-vitro screening test for the presence of malignant cells in a mammalian tissue; a method of identifying inhibitors of constitutive Stat3 activation, Stat3-DNA binding, Stat5-DNA binding, and/or Stat3 dimerization; and a method of identifying anti-cancer agents.
摘要翻译：本发明涉及化合物，含有这些化合物的组合物，以及在体外或体内使用这些化合物和组合物作为Stat3信号传导，Stat3二聚化，Stat3-DNA结合，Stat5-DNA结合和/或异常细胞生长的抑制剂的方法，例如作为用于治疗癌症的抗癌剂，例如乳腺癌。本发明的化合物包括但不限于NSC 74859（S3I-201），NSC 42067，NSC 59263，NSC 75912，NSC 11421，NSC 91529，NSC 263435及其前述的药学上可接受的盐和类似物。以可用本发明化合物治疗但不限于肝硬化的细胞增殖为特征的其它非恶性疾病; 移植排斥反应再狭窄; 以及以T细胞增殖为特征的疾病，例如自身免疫疾病，例如1型糖尿病，狼疮和多发性硬化。本发明还包括在哺乳动物组织中存在恶性细胞的体外筛选试验; 识别组成型Stat3激活抑制剂，Stat3-DNA结合，Stat5-DNA结合和/或Stat3二聚化的方法; 以及鉴定抗癌剂的方法。

10. 发明授权

US09616064B2 Rho kinase inhibitors and methods of use 有权
公开(公告)号：US09616064B2
公开(公告)日：2017-04-11
申请号：US14008678
申请日：2012-03-30
申请人： Nicholas J. Lawrence , Said M. Sebti , Roberta Pireddu
发明人： Nicholas J. Lawrence , Said M. Sebti , Roberta Pireddu
IPC分类号： A61K31/52 , A61K31/505 , A61K31/506 , A61K45/06 , C07D417/12 , C07D473/34 , C07D403/12 , C07D403/14 , C07D239/48 , C07D401/04 , 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.

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