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1. 发明申请

WO2017164887A8 PULSE DOSING REGIMEN AND METHODS FOR TREATMENT 审中-公开
标题翻译：脉冲给药方案和治疗方法
公开(公告)号：WO2017164887A8
公开(公告)日：2017-09-28
申请号：PCT/US2016/024232
申请日：2016-03-25
申请人： OSI PHARMACEUTICALS, LLC
发明人： GILL, Stanley, C. , IWATA, Kenneth, K. , RIELY, Gregory, J. , WU, Jun , YU, Helena
IPC分类号： A61K31/517 , C07D239/94
摘要： A novel dosing regimen for erlotinib or a pharmaceutically acceptable salt thereof is described herein. The dosing regimen demonstrates impressive control of central nervous system disease, which is better than that reported with standard dose erlotinib. The use of the novel dosing regimen for treating patients in need thereof, including for controlling formation of metastatic brain, leptomeninges, or CNS lesions in a patient with non-small cell lung cancer (NSCLC) that harbors epidermal growth factor receptor (EGFR) mutation with or without pre-existing brain metastases, is also described herein.
摘要翻译：本文描述了厄洛替尼或其药学上可接受的盐的新剂量方案。给药方案显示出令人印象深刻的中枢神经系统疾病控制，这优于标准剂量厄洛替尼报道的。新型给药方案用于治疗有此需要的患者，包括用于控制具有表皮生长因子受体（EGFR）突变的非小细胞肺癌（NSCLC）患者中转移性脑，柔脑膜炎或中枢神经系统损伤的形成有或没有预先存在的脑转移瘤，也在本文中描述。

2. 发明申请

WO2013152252A1 COMBINATION ANTI-CANCER THERAPY 审中-公开
标题翻译：组合抗癌治疗
公开(公告)号：WO2013152252A1
公开(公告)日：2013-10-10
申请号：PCT/US2013/035358
申请日：2013-04-05
申请人： OSI PHARMACEUTICALS, LLC
发明人： BUCK, Elizabeth, A. , HALEY, John, D. , THOMSON, Stuart , MULVIHILL, Mark, J. , EPSTEIN, David, M. , MIGLARESE, Mark, R.
IPC分类号： A61K38/00 , A61K39/00 , A61K45/06 , A61K31/404 , A61K31/4985 , A61K31/517 , A61K31/713 , A61P35/00 , A61P35/04 , A61K31/53
CPC分类号： A61K31/404 , A61K31/4985 , A61K31/517 , A61K31/53 , A61K31/713 , A61K45/06 , A61K2300/00
摘要： The present invention provides a method for treating tumors or tumor metastases in a patient, comprising administering to said patient simultaneously or sequentially a therapeutically effective amount of a combination of an inhibitor of MET kinase signaling (e.g. a small molecule MET kinase inhibitor, an anti-MET antibody, or an HGF binding protein) and an inhibitor of IGF-1R signaling (e.g. a small molecule IGF-1R kinase inhibitor (e.g. OSI-906), an anti-IGF-1R antibody, or one or more IGF binding proteins (e.g. IGFBP3)). The present invention also provides a pharmaceutical composition comprising a combination of an inhibitor of MET kinase signaling and an inhibitor of IGF-1R signaling, with a pharmaceutically acceptable carrier. The present invention also provides such methods or compositions where the inhibitory activities of MET kinase signaling and IGF-1R kinase signaling reside in the same molecule.
摘要翻译：本发明提供了一种治疗患者肿瘤或肿瘤转移的方法，其包括向所述患者同时或依次施用治疗有效量的MET激酶信号传导抑制剂（例如小分子MET激酶抑制剂， MET抗体或HGF结合蛋白）和IGF-1R信号传导抑制剂（例如小分子IGF-1R激酶抑制剂（例如OSI-906），抗IGF-1R抗体或一种或多种IGF结合蛋白（例如IGFBP3））。本发明还提供了包含MET激酶信号传导抑制剂和IGF-1R信号传导抑制剂的组合的药物组合物与药学上可接受的载体。本发明还提供了这样的方法或组合物，其中MET激酶信号传导和IGF-1R激酶信号传导的抑制活性位于同一分子中。

3. 发明申请

WO2012129145A1 NSCLE COMBINATION THERAPY 审中-公开
标题翻译： NSCLE组合治疗
公开(公告)号：WO2012129145A1
公开(公告)日：2012-09-27
申请号：PCT/US2012029598
申请日：2012-03-19
申请人： OSI PHARMACEUTICALS LLC , THOMSON STUART , BROWN ERIC N , CHAU ANDREW , FRANKLIN MARYLAND , IWATA KENNETH K
发明人： THOMSON STUART , BROWN ERIC N , CHAU ANDREW , FRANKLIN MARYLAND , IWATA KENNETH K
IPC分类号： A61K31/4985 , A61K31/517 , A61K45/06 , A61P35/00
CPC分类号： A61K31/4985 , A61K31/517 , A61K45/06 , A61K2300/00
摘要： A method of treating NSCLC comprising in some aspects administering OSI-906 and an EGFR inhibitor to a patient having NSCLC having an activating EGFR mutation, as disclosed herein.
摘要翻译：本文公开的治疗NSCLC的方法，其包括在某些方面对具有激活性EGFR突变的NSCLC的患者施用OSI-906和EGFR抑制剂。

4. 发明申请

WO2011143645A1 FUSED BICYCLIC KINASE INHIBITORS 审中-公开
标题翻译：熔融双相激酶抑制剂
公开(公告)号：WO2011143645A1
公开(公告)日：2011-11-17
申请号：PCT/US2011/036572
申请日：2011-05-16
申请人： OSI PHARMACEUTICALS, LLC , MULVIHILL, Mark, J. , STEINIG, Arno, G. , CREW, Andrew, Philip , JIN, Meizhong , KLEINBERG, Andrew , LI, An-Hu , WANG, Jing
发明人： MULVIHILL, Mark, J. , STEINIG, Arno, G. , CREW, Andrew, Philip , JIN, Meizhong , KLEINBERG, Andrew , LI, An-Hu , WANG, Jing
IPC分类号： C07D471/04 , A61K31/437 , A61P35/00
CPC分类号： C07D471/04
摘要： Compounds of Formula I, as shown below and defined herein: (I) pharmaceutically acceptable salts thereof, synthesis, intermediates, formulations, and methods of disease treatment therewith, including treatment of cancers, such as tumors driven at least in part by at least one of RON, MET or ALK. This Abstract is not limiting of the invention.
摘要翻译：式I化合物，如下文所示和定义：（I）其药学上可接受的盐，合成，中间体，制剂及其治疗方法，包括治疗癌症，例如至少部分由至少一种的RON，MET或ALK。本发明不限于本发明。

5. 发明申请

WO2013078138A1 PROTON NMR SPECTROSCOPY FOR BIOCHEMICAL SCREENING 审中-公开
标题翻译：用于生物化学筛选的原核NMR光谱
公开(公告)号：WO2013078138A1
公开(公告)日：2013-05-30
申请号：PCT/US2012/065893
申请日：2012-11-19
申请人： OSI PHARMACEUTICALS, LLC
发明人： LI, Yingjie , MA, Lifu , MULVIHILL, Mark, J.
IPC分类号： C12Q1/00 , C12Q1/30 , C12Q1/48
CPC分类号： C12Q1/30 , C12Q1/008 , C12Q1/48
摘要： High-Throughput Screening (HTS) of large compound libraries is the method of choice for discovery of lead compounds for drug development. The present invention provides novel, sensitive and broadly applicable NMR screening methods in which the H8 signal of a purine-containing substrate or product, or the H6 signal of a pyrimidine-containing substrate or product, is used to monitor enzymic reactions that utilize such substrates. Experiments can be performed in real time or in an endpoint assay format using protein and substrate concentrations comparable to the ones used by other HTS techniques. Application of the NMR method to the assay of the enzymes creatine kinase and phosphodiesterase 2A is presented. The methods are applicable to any of a multitude of enzymes that utilize purine nucleoside substrates (e.g. ATP, GTP) or pyrimidine nucleoside substrates (e.g. CTP, UDP-GlcNac), including protein kinases, GTPases, and lipid kinases.
摘要翻译：大型化合物库的高通量筛选（HTS）是用于发现药物开发的铅化合物的首选方法。本发明提供新颖，灵敏和广泛应用的NMR筛选方法，其中含嘌呤的底物或产物的H8信号或含嘧啶的底物或产物的H6信号用于监测利用这种底物的酶反应。实验可以使用与其他HTS技术使用的蛋白质和底物浓度相当的实时或终点分析格式进行。提出了NMR方法对酶肌酸激酶和磷酸二酯酶2A的测定的应用。该方法适用于使用嘌呤核苷底物（例如ATP，GTP）或嘧啶核苷底物（例如CTP，UDP-GlcNac）（包括蛋白激酶，GTP酶和脂质激酶）的任何多种酶。

6. 发明申请

WO2012158658A1 FUSED BICYCLIC KINASE INHIBITORS 审中-公开
标题翻译：熔融双相激酶抑制剂
公开(公告)号：WO2012158658A1
公开(公告)日：2012-11-22
申请号：PCT/US2012/037866
申请日：2012-05-15
申请人： OSI PHARMACEUTICALS, LLC , JIN, Meizhong , MULVIHILL, Mark, J. , STEINIG, Arno, G. , WANG, Jing
发明人： JIN, Meizhong , MULVIHILL, Mark, J. , STEINIG, Arno, G. , WANG, Jing
IPC分类号： C07D471/04 , C07D487/04 , A61K31/437 , A61K31/4985 , A61P35/00
CPC分类号： C07D471/04 , C07D487/04
摘要： Compounds of Formula (I), pharmaceutically acceptable salts thereof, synthesis, intermediates, formulations, and methods of disease treatment therewith, including treatment of cancers, such as tumors driven at least in part by at least one of MET, RON, ALK, IR, or IGF-1R. This Abstract is not limiting of the invention.
摘要翻译：式（I）的化合物，其药学上可接受的盐，合成，中间体，制剂及其治疗方法，包括治疗癌症，例如至少部分地由至少一种MET，RON，ALK，IR ，或IGF-1R。本发明并不限于本发明。

7. 发明申请

WO2012129145A8 NSCLC COMBINATION THERAPY 审中-公开
公开(公告)号：WO2012129145A8
公开(公告)日：2012-09-27
申请号：PCT/US2012/029598
申请日：2012-03-19
申请人： OSI PHARMACEUTICALS, LLC , THOMSON, Stuart , BROWN, Eric, N. , CHAU, Andrew , FRANKLIN, Maryland , IWATA, Kenneth, K.
发明人： THOMSON, Stuart , BROWN, Eric, N. , CHAU, Andrew , FRANKLIN, Maryland , IWATA, Kenneth, K.
IPC分类号： A61K31/4985 , A61K31/517 , A61K45/06 , A61P35/00
摘要： A method of treating NSCLC comprising in some aspects administering OSI-906 and an EGFR inhibitor to a patient having NSCLC having an activating EGFR mutation, as disclosed herein.

8. 发明申请

WO2011100502A8 7-AMINOFUROPYRIDINE DERIVATIVES 审中-公开
标题翻译： 7-氨基脲衍生物
公开(公告)号：WO2011100502A8
公开(公告)日：2011-09-22
申请号：PCT/US2011024449
申请日：2011-02-11
申请人： OSI PHARMACEUTICALS LLC , HORNBERGER KEITH R , BERGER DAN M , CHEN XIN , CREW ANDREW P , DONG HANQING , KLEINBERG ANDREW , LI AN-HU , MA LIFU , MULVIHILL MARK J , PANICKER BIJOY , SIU KAM W , STEINIG ARNO G , TARRANT JAMES G , WANG JING , WENG QINGHUA , SANGEM RAJARAM , GUPTA RAMESH C
发明人： HORNBERGER KEITH R , BERGER DAN M , CHEN XIN , CREW ANDREW P , DONG HANQING , KLEINBERG ANDREW , LI AN-HU , MA LIFU , MULVIHILL MARK J , PANICKER BIJOY , SIU KAM W , STEINIG ARNO G , TARRANT JAMES G , WANG JING , WENG QINGHUA , SANGEM RAJARAM , GUPTA RAMESH C
IPC分类号： C07D491/048 , A61K31/4355 , A61P35/00
CPC分类号： C07D491/048
摘要： Compounds of Formula (1), as shown below and defined herein: pharmaceutically acceptable salts thereof, synthesis, intermediates, formulations, and methods of disease treatment therewith, including treatment of cancers, such as tumors driven at least in part by TAK1 or for which an appropriate TAK1 inhibitor is effective. This Abstract is not limiting of the invention.
摘要翻译：式（1）的化合物，如下文所定义：其药学上可接受的盐，合成，中间体，制剂及其治疗方法，包括治疗癌症，例如至少部分由TAK1驱动的肿瘤，或其中适当的TAK1抑制剂是有效的。本发明并不限于本发明。

9. 发明申请

WO2011112666A1 COMBINATION ANTI-CANCER THERAPY 审中-公开
标题翻译：组合抗癌治疗
公开(公告)号：WO2011112666A1
公开(公告)日：2011-09-15
申请号：PCT/US2011/027673
申请日：2011-03-09
申请人： OSI PHARMACEUTICALS, LLC , BARR, Sharon , BUCK, Elizabeth, A. , EPSTEIN, David, M. , GOKHALE, Prafulla, C. , MIGLARESE, Mark, R.
发明人： BARR, Sharon , BUCK, Elizabeth, A. , EPSTEIN, David, M. , GOKHALE, Prafulla, C. , MIGLARESE, Mark, R.
IPC分类号： A61K31/00 , A61K31/4985 , A61K31/53 , A61P35/00
CPC分类号： A61K31/00 , A61K31/4985 , A61K31/53 , A61K45/06 , A61K2300/00
摘要： Methods and compositions for treating cancer comprising administering to a patient inhibitors of mT0RC1/C2, IGF-1 R, and IR. In some aspects, a combination of an mT0RC1/C2 inhibitor and an IGF-1 R/IR inhibitor is employed. Other aspects are described herein.
摘要翻译：用于治疗癌症的方法和组合物包括向患者施用mT0RC1 / C2，IGF-1R和IR的抑制剂。在一些方面，使用mT0RC1 / C2抑制剂和IGF-1R / IR抑制剂的组合。本文描述了其它方面。

10. 发明申请

WO2011109593A1 SUBSTITUTED-5-AMINOPYRROLO/PYRAZOLOPYRIDINES 审中-公开
标题翻译：取代的-5-氨基吡咯并/吡唑并吡啶
公开(公告)号：WO2011109593A1
公开(公告)日：2011-09-09
申请号：PCT/US2011/026984
申请日：2011-03-03
申请人： OSI PHARMACEUTICALS, LLC , AN-HU, Li , GUPTA, Ramesh, C. , MULVIHILL, Mark, J. , RAI, Anand, Narain , WANG, Jing
发明人： AN-HU, Li , GUPTA, Ramesh, C. , MULVIHILL, Mark, J. , RAI, Anand, Narain , WANG, Jing
IPC分类号： C07D471/04 , A61K31/437 , A61P35/00
CPC分类号： C07D471/04
摘要： Compounds of Formula I, as shown below and defined herein: pharmaceutically acceptable salts, synthesis, intermediates, formulations, and methods of disease treatment therewith, including cancers mediated at least in part by RON and/or MET.
摘要翻译：式I的化合物，如下文所示和本文定义：药学上可接受的盐，合成，中间体，制剂及其治疗方法，包括至少部分由RON和/或MET介导的癌症。

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