专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明申请

WO2009152340A2 2,3-SUBSTITUTED THIOPHENES IN LUNG INFLAMMATION THERAPIES 审中-公开
标题翻译：肺取暖治疗中的2,3代替噻吩类药物
公开(公告)号：WO2009152340A2
公开(公告)日：2009-12-17
申请号：PCT/US2009/047051
申请日：2009-06-11
申请人： OSI PHARMACEUTICALS, INC. , GARTON, Andrew , GIBSON, Neil , GRIFFIN, Graeme
发明人： GARTON, Andrew , GIBSON, Neil , GRIFFIN, Graeme
IPC分类号： A61K31/381 , A61P11/06
CPC分类号： A61K31/381
摘要： Methods of treating inflammatory lung conditions comprising administering 2,3- substituted thiophenes of the formula (I).
摘要翻译：治疗炎症性肺病的方法包括给予式（I）的2,3-取代的噻吩。

2. 发明申请

WO2009073139A2 COMBINED TREATMENT WITH AN EGFR KINASE INHIBITOR AND AN INHIBITOR OF C-KIT 审中-公开
标题翻译：与EGFR激酶抑制剂和C-kit的抑制剂联合治疗
公开(公告)号：WO2009073139A2
公开(公告)日：2009-06-11
申请号：PCT/US2008/013172
申请日：2008-11-26
申请人： OSI PHARMACEUTICALS, INC. , GARTON, Andrew, John , FRANKLIN, Maryland, Rosenfeld
发明人： GARTON, Andrew, John , FRANKLIN, Maryland, Rosenfeld
IPC分类号： A61K31/4709 , A61K31/517 , A61K45/06 , A61P35/00
CPC分类号： A61K31/517 , A61K31/4709 , A61K39/39541 , A61K45/06 , A61K2300/00
摘要： The present invention provides a composition and a method for treating tumors or tumor metastases in a patient, comprising administering to the patient simultaneously or sequentially a therapeutically effective amount of a combination of an EGFR kinase inhibitor and a KIT kinase inhibitors, with or without additional agents or treatments, such as other anti-cancer drugs or radiation therapy. A preferred example of an EGFR kinase inhibitor that can be used in practicing this invention is the compound erlotinib HCl (also known as TARCEV A ® ). A preferred example of a KIT kinase inhibitor that can be used in practicing this invention is OSI-930 and OSI-817.
摘要翻译：本发明提供了一种用于治疗患者的肿瘤或肿瘤转移的组合物和方法，其包括向所述患者同时或依次施用治疗有效量的EGFR激酶抑制剂和KIT激酶抑制剂的组合，或治疗，如其他抗癌药物或放射治疗。可用于实施本发明的EGFR激酶抑制剂的优选实例是化合物厄洛替尼HCl（也称为TARCEV A？）。可用于实施本发明的KIT激酶抑制剂的优选实例是OSI-930和OSI-817。

3. 发明申请

WO2007084667A3 FUSED HETEROBICYCLIC KINASE INHIBITORS 审中-公开
标题翻译：融合的杂环类激酶抑制剂
公开(公告)号：WO2007084667A3
公开(公告)日：2007-12-06
申请号：PCT/US2007001439
申请日：2007-01-18
申请人： OSI PHARMACEUTICAL INC , ARNOLD LEE D , CHEN XIN , DONG HANPING , GARTON ANDREW , MULVIHILL MARK JOSEPH , SMITH COLIN PETER SAMBROOK , THOMAS GERARD HUGH , KRULLE THOMAS MARTIN , WANG JING
发明人： ARNOLD LEE D , CHEN XIN , DONG HANPING , GARTON ANDREW , MULVIHILL MARK JOSEPH , SMITH COLIN PETER SAMBROOK , THOMAS GERARD HUGH , KRULLE THOMAS MARTIN , WANG JING
IPC分类号： C07D471/04 , A61K31/437 , A61P35/00
CPC分类号： C07D471/04
摘要： Compounds of the formula (I) and pharmaceutically acceptable salts thereof, wherein X 1 , X 2 , X 3 , X 4 , X 5 , X 6 , X 7 , R 1 , and Q 1 are defined herein, inhibit kinase enzymes and are useful for the treatment and/or prevention of hyperproliferative diseases such as cancer. The compounds are also useful in the treatment of inflammation, allergy, asthma, disease and conditions of the immune system, disease and conditions of the nervous system, cardiovascular diseases, disease and conditions of the eye, dermatological diseases, osteoporosis, diabetes, multiple sclerosis, and infections.
摘要翻译：式（I）化合物及其药学上可接受的盐，其中X 1，X 2，X 3，X 4， X SUB 5，SUB 6，SUB 7，SUB 1和SUP 1 本文定义为抑制激酶，并可用于治疗和/或预防过度增殖性疾病如癌症。这些化合物还可用于治疗炎症，变态反应，哮喘，疾病和免疫系统疾病和病症，神经系统疾病和病症，心血管疾病，眼睛疾病和病症，皮肤病，骨质疏松症，糖尿病，多发性硬化症和感染。

4. 发明申请

WO2007117507A1 A METHOD FOR THE ASSAY OF ROCK KINASE ACTIVITY IN CELLS 审中-公开
标题翻译：用于细胞中岩石激酶活性测定的方法
公开(公告)号：WO2007117507A1
公开(公告)日：2007-10-18
申请号：PCT/US2007/008399
申请日：2007-04-03
申请人： OSI PHARMACEUTICALS, INC. , GARTON, Andrew, J. , CASTALDO, Linda
发明人： GARTON, Andrew, J. , CASTALDO, Linda
IPC分类号： G01N33/566
CPC分类号： C12Q1/485 , G01N33/5011 , G01N2500/00
摘要： The present invention provides a method for determining the intracellular activity of ROCK kinase comprising, providing a sample of cells to be tested for ROCK kinase activity, determining the level of phosphorylation of MYPT1 in the sample, and determining the intracellular activity of ROCK kinase in the sample of cells, wherein the level of MYPT1 phosphorylation directly correlates with the level of intracellular ROCK kinase activity. The invention further provides a method for identifying an agent that inhibits the intracellular activity of ROCK kinase comprising, providing a sample of cells having ROCK kinase activity, determining the degree of reduction of phosphorylation of MYPT1 in the sample by contacting the sample of cells with a test agent and comparing the MYPT1 phosphorylation level with the phosphorylation level of MYPT1 in an identical control sample of cells that was not contacted with the test agent, determining the degree of inhibition of intracellular activity of ROCK kinase in the sample of cells contacted with the agent, wherein the level of MYPT1 phosphorylation directly correlates with the level of intracellular ROCK kinase activity, and thus determining whether the test agent is an agent that inhibits the intracellular activity of ROCK kinase. The test agent may for example be a compound not known to have ROCK kinase inhibitory activity, or a compound identified by an in vitro ROCK kinase assay as having inhibitory activity.
摘要翻译：本发明提供了一种确定ROCK激酶的细胞内活性的方法，包括：提供待测试的ROCK激酶活性的细胞样品，测定样品中MYPT1的磷酸化水平，以及测定ROCK激酶在细胞内的活性细胞样本，其中MYPT1磷酸化水平与细胞内ROCK激酶活性的水平直接相关。本发明进一步提供了一种鉴定抑制ROCK激酶细胞内活性的试剂的方法，其包括：提供具有ROCK激酶活性的细胞样品，通过将细胞样品接触到样品中的MYPT1的磷酸化程度来确定测试试剂，并将MYPT1磷酸化水平与未与测试试剂接触的相同对照样品的MYPT1的磷酸化水平进行比较，确定与试剂接触的细胞样品中ROCK激酶的细胞内活性的抑制程度其中MYPT1磷酸化水平与细胞内ROCK激酶活性的水平直接相关，从而确定测试试剂是否是抑制ROCK激酶的细胞内活性的试剂。测试剂可以是例如不知道具有ROCK激酶抑制活性的化合物，或通过体外ROCK激酶测定鉴定为具有抑制活性的化合物。

5. 发明申请

WO2007084667A2 FUSED HETEROBICYCLIC KINASE INHIBITORS 审中-公开
标题翻译：融合的异源性激酶抑制剂
公开(公告)号：WO2007084667A2
公开(公告)日：2007-07-26
申请号：PCT/US2007/001439
申请日：2007-01-18
申请人： OSI PHARMACEUTICAL, INC. , ARNOLD, Lee, D. , CHEN, Xin , DONG, Hanping , GARTON, Andrew , MULVIHILL, Mark, Joseph , SMITH, Colin Peter, Sambrook , THOMAS, Gerard, Hugh , KRULLE, Thomas, Martin , WANG, Jing
发明人： ARNOLD, Lee, D. , CHEN, Xin , DONG, Hanping , GARTON, Andrew , MULVIHILL, Mark, Joseph , SMITH, Colin Peter, Sambrook , THOMAS, Gerard, Hugh , KRULLE, Thomas, Martin , WANG, Jing
IPC分类号： C07D471/04 , A61K31/437 , A61P35/00
CPC分类号： C07D471/04
摘要： Compounds of the formula (I) and pharmaceutically acceptable salts thereof, wherein X 1 , X 2 , X 3 , X 4 , X 5 , X 6 , X 7 , R 1 , and Q 1 are defined herein, inhibit kinase enzymes and are useful for the treatment and/or prevention of hyperproliferative diseases such as cancer. The compounds are also useful in the treatment of inflammation, allergy, asthma, disease and conditions of the immune system, disease and conditions of the nervous system, cardiovascular diseases, disease and conditions of the eye, dermatological diseases, osteoporosis, diabetes, multiple sclerosis, and infections.
摘要翻译：式（I）化合物及其药学上可接受的盐，其中X 1，X 2，X 3，X 4， X 1，X 5，X 6，X 7，R 1和Q 1 本文定义抑制激酶，并且可用于治疗和/或预防过度增殖性疾病如癌症。该化合物还可用于治疗炎症，过敏，哮喘，免疫系统的疾病和状况，神经系统的疾病和状况，心血管疾病，眼睛疾病和病症，皮肤病，骨质疏松症，糖尿病，多发性硬化和感染。

6. 发明申请

WO2009152340A3 USE OF 2,3-SUBSTITUTED THIOPHENES FOR THE TREATMENT OF LUNG INFLAMMATION 审中-公开
标题翻译：使用2,3代替噻吩治疗肺炎
公开(公告)号：WO2009152340A3
公开(公告)日：2011-04-28
申请号：PCT/US2009047051
申请日：2009-06-11
申请人： OSI PHARM INC , GARTON ANDREW , GIBSON NEIL , GRIFFIN GRAEME
发明人： GARTON ANDREW , GIBSON NEIL , GRIFFIN GRAEME
IPC分类号： A61K31/381 , A61P11/06
CPC分类号： A61K31/381
摘要： Methods of treating inflammatory lung conditions comprising administering 2,3- substituted thiophenes of the formula (I).
摘要翻译：治疗炎症性肺病的方法包括给予式（I）的2,3-取代的噻吩。

7. 发明申请

WO2009073139A3 COMBINED TREATMENT WITH AN EGFR KINASE INHIBITOR AND AN INHIBITOR OF C-KIT 审中-公开
标题翻译：与EGFR激酶抑制剂和C-kit的抑制剂联合治疗
公开(公告)号：WO2009073139A3
公开(公告)日：2010-01-14
申请号：PCT/US2008013172
申请日：2008-11-26
申请人： OSI PHARM INC , GARTON ANDREW JOHN , FRANKLIN MARYLAND ROSENFELD
发明人： GARTON ANDREW JOHN , FRANKLIN MARYLAND ROSENFELD
IPC分类号： A61K39/395 , A61P35/00
CPC分类号： A61K31/517 , A61K31/4709 , A61K39/39541 , A61K45/06 , A61K2300/00
摘要： The present invention provides a composition and a method for treating tumors or tumor metastases in a patient, comprising administering to the patient simultaneously or sequentially a therapeutically effective amount of a combination of an EGFR kinase inhibitor and a KIT kinase inhibitors, with or without additional agents or treatments, such as other anti-cancer drugs or radiation therapy. A preferred example of an EGFR kinase inhibitor that can be used in practicing this invention is the compound erlotinib HCl (also known as TARCEV A®). A preferred example of a KIT kinase inhibitor that can be used in practicing this invention is OSI-930 and OSI-817.
摘要翻译：本发明提供了一种用于治疗患者的肿瘤或肿瘤转移的组合物和方法，其包括向所述患者同时或依次施用治疗有效量的EGFR激酶抑制剂和KIT激酶抑制剂的组合，或治疗，如其他抗癌药物或放射治疗。可用于实施本发明的EGFR激酶抑制剂的优选实例是化合物厄洛替尼HCl（也称为TARCEV A？）。可用于实施本发明的KIT激酶抑制剂的优选实例是OSI-930和OSI-817。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式