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公开(公告)号：US20120264735A1
公开(公告)日：2012-10-18
申请号：US13517321
申请日：2010-12-14
申请人： Jonathan Young , Barbara Czako , Michael Altman , David Guerin , Michelle Martinez , Alexey Rivkin , Kevin Wilson , Kathryn Lipford , Catherine White , Laura Surdi , Stephanie Chichetti , Matthew H. Daniels , Sean P. Ahearn , Danielle Falcone , Ekundayo Osimboni
发明人： Jonathan Young , Barbara Czako , Michael Altman , David Guerin , Michelle Martinez , Alexey Rivkin , Kevin Wilson , Kathryn Lipford , Catherine White , Laura Surdi , Stephanie Chichetti , Matthew H. Daniels , Sean P. Ahearn , Danielle Falcone , Ekundayo Osimboni
IPC分类号： A61K31/501 , A61K31/506 , C07D413/12 , A61P35/00 , C07D413/14 , C07D417/14 , A61K31/541 , C07D403/04 , A61K31/5377
CPC分类号： C07D403/04 , C07D237/14 , C07D401/14 , C07D403/10 , C07D403/14 , C07D405/14 , C07D413/14 , C07D417/10 , C07D417/14 , C07D471/04
摘要： The present invention relates to pyridazin-4(1H)-one derivatives, that are useful for treating cellular proliferative diseases, for treating disorders associated with MET activity, and for inhibiting the receptor tyrosine kinase MET. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.
摘要翻译： 本发明涉及哒嗪-4（1H） - 酮衍生物，其可用于治疗细胞增殖性疾病，用于治疗与MET活性相关的疾病，以及用于抑制受体酪氨酸激酶MET。 本发明还涉及包含这些化合物的组合物，以及使用它们治疗哺乳动物癌症的方法。
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公开(公告)号：US20150258074A1
公开(公告)日：2015-09-17
申请号：US14431485
申请日：2013-09-26
申请人： Kevin J. WILSON , David J. WITTER , Matthew H. DANIELS , Angie R. ANGELES , Phieng SILIPHAIVANH , David L. SLOMAN , Brendan O'BOYLE , Danielle FALCONE , Catherine WHITE , Ron FERGUSON , Wei ZHOU , Kathryn LIPFORD , Umar Faruk MANSOOR , Salem FEVRIRE , Xianhai HUANG , Ravi KURUKULASURIYA , Judson E. RICHARD , Shuyi TANG , Christopher BOYCE , Joseph KOZLOWSKI , Raman Kumar BAKSHI , Ganesh Babu UNAKARAN , Merck Sharp & Dohme Corp.
发明人： Kevin J. Wilson , David J. Witter , Matthew H. Daniels , Angie R. Angeles , Phieng Siliphaivanh , David Sloman , Brendan O'Boyle , Danielle Falcone , Catherine White , Ron Ferguson , Wei Zhou , Kathryn Lipford , Umar Faruk Mansoor , Salem Fevrier , Xianhai Huang , Ravi Kurukulasuriya , Judson E. Richard , Shuyi Tang , Christopher Boyce , Joseph Kozlowski , Raman Kumar Bakshi , Ganesh Babu Karunakaran
IPC分类号： A61K31/437 , A61K45/06 , A61K31/4545 , C07D471/04
CPC分类号： A61K31/437 , A61K31/4545 , A61K45/06 , C07D471/04
摘要： Disclosed are the ERK inhibitors of formula (1.0), having a pyrazolopyridine base structure, and the pharmaceutically acceptable salts thereof. Also disclosed are methods of treating cancer using the compounds of formula (1.0).
摘要翻译： 公开了具有吡唑并吡啶基结构的式（1.0）的ERK抑制剂及其药学上可接受的盐。 还公开了使用式（1.0）化合物治疗癌症的方法。
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公开(公告)号：US20130116231A1
公开(公告)日：2013-05-09
申请号：US13809436
申请日：2011-07-07
IPC分类号： C07D411/14 , C07D403/14 , C07D403/04 , C07D401/14 , C07D401/12
CPC分类号： C07D411/14 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D417/14
摘要： The present invention relates to 1,4-dihydropyridazinone derivatives, that are useful for treating cellular proliferative diseases, for treating disorders associated with MET activity, and for inhibiting the receptor tyrosine kinase MET. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.
摘要翻译： 本发明涉及1,4-二氢哒嗪酮衍生物，其可用于治疗细胞增殖性疾病，用于治疗与MET活性相关的疾病，以及用于抑制受体酪氨酸激酶MET。 本发明还涉及包含这些化合物的组合物，以及使用它们治疗哺乳动物癌症的方法。
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公开(公告)号：US09493441B2
公开(公告)日：2016-11-15
申请号：US14345977
申请日：2012-09-21
申请人： Jason Brubaker , Joshua T. Close , Joon Jung , Michelle Martinez , Catherine White , Kevin Wilson , Jonathan R. Young , Hongjun Zhang
发明人： Jason Brubaker , Joshua T. Close , Joon Jung , Michelle Martinez , Catherine White , Kevin Wilson , Jonathan R. Young , Hongjun Zhang
IPC分类号： C07D405/08 , C07D403/12 , C07D401/14 , C07D231/38 , C07D401/12 , C07D403/08 , C07D405/12 , C07D409/12 , C07D413/12 , C07D401/04 , C07D403/04 , C07D405/04 , C07D401/06 , C07D403/06 , C07D405/06 , C07D405/14 , C07D409/04 , C07D413/14 , C07D417/14
CPC分类号： C07D405/08 , C07D231/38 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/08 , C07D403/12 , C07D405/04 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/04 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/14
摘要： The instant invention provides compounds of formula I which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.
摘要翻译： 本发明提供了作为JAK抑制剂的式I化合物，因此可用于治疗JAK介导的疾病如类风湿性关节炎，哮喘，COPD和癌症。
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5.发明申请ACYCLIC CYANOETHYLPYRAZOLES AS JANUS KINASE INHIBITORS 有权ACYCLIC CYANOETHYLZOLES作为JANUS KINASE INHIBITORS公开(公告)号：US20140228358A1
公开(公告)日：2014-08-14
申请号：US14345977
申请日：2012-09-21
申请人： Jason Brubaker , Joshua T. Close , Joon Jung , Michelle Martinez , Catherine White , Kevin Wilson , Jonathan R. Young , Hongjun Zhang
发明人： Jason Brubaker , Joshua T. Close , Joon Jung , Michelle Martinez , Catherine White , Kevin Wilson , Jonathan R. Young , Hongjun Zhang
IPC分类号： C07D231/38 , C07D403/06 , C07D401/14 , C07D405/06 , C07D401/12 , C07D401/06 , C07D403/12
CPC分类号： C07D405/08 , C07D231/38 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/08 , C07D403/12 , C07D405/04 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/04 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/14
摘要： The instant invention provides compounds of formula I which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.
摘要翻译： 本发明提供了作为JAK抑制剂的式I化合物，因此可用于治疗JAK介导的疾病如类风湿性关节炎，哮喘，COPD和癌症。
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公开(公告)号：US08344144B2
公开(公告)日：2013-01-01
申请号：US12999342
申请日：2009-06-08
申请人： Michelle Machacek , Gabriela de Almeida , Jonathan B. Grimm , Rachel N. MacCoss , Eric Romeo , Tony Siu , Catherine White , Kevin Wilson
发明人： Michelle Machacek , Gabriela de Almeida , Jonathan B. Grimm , Rachel N. MacCoss , Eric Romeo , Tony Siu , Catherine White , Kevin Wilson
IPC分类号： C07D471/02 , A61K31/395
CPC分类号： C07D513/04 , C07D471/04 , C07D487/04 , C07D498/04
摘要： The instant invention provides for compounds that inhibit the four known mammalian JAK kinases (JAK1, JAK2, JAK3 and TYK2) and PDK1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting the activity of JAK1, JAK2, JAK3, TYK2 and PDK1 by administering the compound to a patient in need of treatment for myeloproliferative disorders or cancer.
摘要翻译： 本发明提供抑制四种已知的哺乳动物JAK激酶（JAK1，JAK2，JAK3和TYK2）和PDK1的化合物。 本发明还提供了包含这种抑制化合物的组合物和通过将该化合物施用于需要治疗骨髓增生性疾病或癌症的患者的JAK1，JAK2，JAK3，TYK2和PDK1的活性的方法。
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公开(公告)号：US20110082136A1
公开(公告)日：2011-04-07
申请号：US12999342
申请日：2009-06-08
申请人： Michelle Machacek , Gabriela de Almeida , Jonathan B. Grimm , Rachel N. MacCoss , Eric Romeo , Tony Siu , Catherine White , Kevin Wilson
发明人： Michelle Machacek , Gabriela de Almeida , Jonathan B. Grimm , Rachel N. MacCoss , Eric Romeo , Tony Siu , Catherine White , Kevin Wilson
IPC分类号： A61K31/5377 , A61K31/502 , A61K31/495 , A61K31/519 , A61K31/4375 , A61K31/437 , C07D487/04 , C07D513/04 , C07D498/04 , C07D471/04
CPC分类号： C07D513/04 , C07D471/04 , C07D487/04 , C07D498/04
摘要： The instant invention provides for compounds that inhibit the four known mammalian JAK kinases (JAK1, JAK2, JAK3 and TYK2) and PDK1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting the activity of JAK1, JAK2, JAK3, TYK2 and PDK1 by administering the compound to a patient in need of treatment for myeloproliferative disorders or cancer.
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公开(公告)号：USD709908S1
公开(公告)日：2014-07-29
申请号：US29418884
申请日：2012-04-23
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公开(公告)号：US20120329128A1
公开(公告)日：2012-12-27
申请号：US13488324
申请日：2012-06-04
IPC分类号： C12N9/96
CPC分类号： A61K38/482 , A61K9/0019 , A61K9/08 , A61K9/19 , A61K47/26 , C12N9/6454 , C12Y304/21075
摘要： The present application provides stabilized formulations of furin (e.g., rfurin) containing a sugar, sugar alcohol, and/or non-ionic surfactant. As compared to non-stabilized compositions, the furin formulations disclosed herein retain greater amounts of furin activity and monomeric furin content, while reducing furin aggregation when stored and/or subjected to mechanical stress. Also provided are methods for stably diluting furin (e.g., rfurin) compositions.
摘要翻译： 本申请提供了含有糖，糖醇和/或非离子表面活性剂的弗林蛋白酶（例如，富马林）的稳定制剂。 与未稳定的组合物相比，本文公开的弗林蛋白酶制剂保留更大量的弗林蛋白酶活性和单一弗林素含量，同时在储存和/或经受机械应力时减少弗林蛋白聚糖。 还提供了用于稳定稀释弗林蛋白酶（例如rfurin）组合物的方法。
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公开(公告)号：USD667455S1
公开(公告)日：2012-09-18
申请号：US29401423
申请日：2011-09-12
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