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公开(公告)号：US20140031344A1
公开(公告)日：2014-01-30
申请号：US14032629
申请日：2013-09-20
申请人： Argyrios G. Arvanitis , James D. Rodgers , Andrew P. Combs , Richard B. Sparks , Darius J. Robinson , Jordan S. Fridman , Krishna Vaddi
发明人： Argyrios G. Arvanitis , James D. Rodgers , Andrew P. Combs , Richard B. Sparks , Darius J. Robinson , Jordan S. Fridman , Krishna Vaddi
IPC分类号： C07D471/14 , C07D471/22
CPC分类号： C07D471/14 , C07D471/22 , C07D487/14 , C07D487/22
摘要： The present invention provides compounds that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases.
摘要翻译： 本发明提供调节Janus激酶活性的化合物，并且可用于治疗与Janus激酶活性相关的疾病，包括例如免疫相关疾病，皮肤病，骨髓增生性疾病，癌症和其它疾病。
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公开(公告)号：US20120329782A1
公开(公告)日：2012-12-27
申请号：US13479045
申请日：2012-05-23
申请人： Argyrios G. Arvanitis , James D. Rodgers , Andrew P. Combs , Richard B. Sparks , Darius J. Robinson , Jordan S. Fridman , Krishna Vaddi
发明人： Argyrios G. Arvanitis , James D. Rodgers , Andrew P. Combs , Richard B. Sparks , Darius J. Robinson , Jordan S. Fridman , Krishna Vaddi
IPC分类号： C07D487/22 , A61P37/00 , A61P17/00 , A61P19/02 , A61P35/02 , A61P37/02 , A61P1/04 , A61P37/08 , A61P31/12 , A61P35/04 , A61K31/55 , A61P3/10
CPC分类号： C07D471/14 , C07D471/22 , C07D487/14 , C07D487/22
摘要： The present invention provides compounds that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases.
摘要翻译： 本发明提供调节Janus激酶活性的化合物，并且可用于治疗与Janus激酶活性相关的疾病，包括例如免疫相关疾病，皮肤病，骨髓增生性疾病，癌症和其它疾病。
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![HETEROARYL SUBSTITUTED PYRROLO[2,3-b]PYRIDINES AND PYRROLO[2,3-b]PYRIMIDINES AS JANUS KINASE INHIBITORS](/abs-image/US/2011/09/15/US20110224157A1/abs.jpg.150x150.jpg)
3.发明申请HETEROARYL SUBSTITUTED PYRROLO[2,3-b]PYRIDINES AND PYRROLO[2,3-b]PYRIMIDINES AS JANUS KINASE INHIBITORS 有权异丙基取代的吡咯并[2,3-b]吡啶和吡咯并[2,3-b]吡嗪类作为甘薯激酶抑制剂公开(公告)号：US20110224157A1
公开(公告)日：2011-09-15
申请号：US13076176
申请日：2011-03-30
申请人： James D. Rodgers , Stacey Shepard , Thomas P. Maduskuie, JR. , Haisheng Wang , Nikoo Falahatpisheh , Maria Rafalski , Argyrios G. Arvanitis , Louis Storace , Ravi Kumar Jalluri , Jordan S. Fridman , Krishna Vaddi
发明人： James D. Rodgers , Stacey Shepard , Thomas P. Maduskuie, JR. , Haisheng Wang , Nikoo Falahatpisheh , Maria Rafalski , Argyrios G. Arvanitis , Louis Storace , Ravi Kumar Jalluri , Jordan S. Fridman , Krishna Vaddi
IPC分类号： A61K31/519 , A61K31/704 , A61K31/675 , A61K31/7048 , A61K31/573 , A61K31/69 , A61P35/00 , A61P43/00 , A61P35/02 , A61P9/00
CPC分类号： A61K31/519 , A61K9/0014 , A61K9/0053 , A61K9/20 , A61K31/573 , A61K45/06 , C07B59/002 , C07B2200/05 , C07D417/04 , C07D471/04 , C07D487/04
摘要： The present invention provides heteroaryl substituted pyrrolo[2,3-b]pyridines and heteroaryl substituted pyrrolo[2,3-b]pyrimidines that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases.
摘要翻译： 本发明提供调节Janus激酶活性的杂芳基取代的吡咯并[2,3-b]吡啶和杂芳基取代的吡咯并[2,3-b]嘧啶，可用于治疗与Janus激酶活性有关的疾病， 例如免疫相关疾病，皮肤病，骨髓增生性疾病，癌症和其它疾病。
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![HETEROARYL SUBSTITUTED PYRROLO[2,3-b]PYRIDINES AND PYRROLO[2,3-b]PYRIMIDINES AS JANUS KINASE INHIBITORS](/abs-image/US/2009/07/16/US20090181959A1/abs.jpg.150x150.jpg)
4.发明申请HETEROARYL SUBSTITUTED PYRROLO[2,3-b]PYRIDINES AND PYRROLO[2,3-b]PYRIMIDINES AS JANUS KINASE INHIBITORS 有权异丙基取代的吡咯并[2,3-b]吡啶和吡咯并[2,3-b]吡嗪类作为甘薯激酶抑制剂公开(公告)号：US20090181959A1
公开(公告)日：2009-07-16
申请号：US12138082
申请日：2008-06-12
申请人： James D. Rodgers , Stacey Shepard , Thomas P. Maduskuie, JR. , Haisheng Wang , Nikoo Falahatpisheh , Maria Rafalski , Argyrios G. Arvanitis , Louis Storace , Ravi Kumar Jalluri , Jordan S. Fridman , Krishna Vaddi
发明人： James D. Rodgers , Stacey Shepard , Thomas P. Maduskuie, JR. , Haisheng Wang , Nikoo Falahatpisheh , Maria Rafalski , Argyrios G. Arvanitis , Louis Storace , Ravi Kumar Jalluri , Jordan S. Fridman , Krishna Vaddi
IPC分类号： A61K31/519 , A61P37/06 , A61P17/00 , A61P31/12 , A61P29/00 , A61P11/00 , A61K31/437 , C07D471/04 , C07D487/04 , A61K31/541 , A61K31/5377 , A61K31/496
CPC分类号： A61K31/519 , A61K9/0014 , A61K9/0053 , A61K9/20 , A61K31/573 , A61K45/06 , C07B59/002 , C07B2200/05 , C07D417/04 , C07D471/04 , C07D487/04
摘要： The present invention provides heteroaryl substituted pyrrolo[2,3-b]pyridines and heteroaryl substituted pyrrolo[2,3-b]pyrimidines that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases.
摘要翻译： 本发明提供调节Janus激酶活性的杂芳基取代的吡咯并[2,3-b]吡啶和杂芳基取代的吡咯并[2,3-b]嘧啶，并且可用于治疗与Janus激酶活性有关的疾病， 例如免疫相关疾病，皮肤病，骨髓增生性疾病，癌症和其它疾病。
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公开(公告)号：US09345677B2
公开(公告)日：2016-05-24
申请号：US13336587
申请日：2011-12-23
IPC分类号： A61K31/19 , A61K31/395
CPC分类号： A61K31/19 , A61K31/395
摘要： The present invention relates to compositions, methods and kits based on the ADAM-mediated cleavage of Her-2. The present invention also relates to treatments for cancer, and in particular, breast cancer, by modulating the ADAM-mediated cleavage of Her-2. Further, the invention relates to compositions, methods and kits based on the surprising synergistic effect between inhibition of Her-2 cleavage by an ADAM and certain cytostatic (e.g., Herceptin) and cytotoxic (e.g., Taxol) compounds in, among other things, inhibiting tumor cell proliferation and inducing cell death. Additionally, the invention relates to novel variants of ADAM15, designated ADAM15 variant 1 and ADAM15 variant 2, now identified and isolated.
摘要翻译： 本发明涉及基于ADAM介导的Her-2切割的组合物，方法和试剂盒。 本发明还涉及通过调节ADAM介导的Her-2切割来治疗癌症，特别是乳腺癌。 此外，本发明涉及基于由ADAM抑制Her-2切割和某些细胞抑制（例如赫赛汀）和细胞毒性（例如紫杉醇）化合物之间令人惊讶的协同效应的组合物，方法和试剂盒，其中包括抑制 肿瘤细胞增殖和诱导细胞死亡。 另外，本发明涉及现在鉴定和分离的ADAM15的新型变体，称为ADAM15变体1和ADAM15变体2。
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![Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as Janus kinase inhibitors](/abs-image/US/2015/02/03/US08946245B2/abs.jpg.150x150.jpg)
6.发明授权Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as Janus kinase inhibitors 有权杂芳基取代的吡咯并[2,3-b]吡啶和吡咯并[2,3-b]嘧啶作为Janus激酶抑制剂公开(公告)号：US08946245B2
公开(公告)日：2015-02-03
申请号：US13076176
申请日：2011-03-30
IPC分类号： A61K31/519 , C07D471/04 , A61K45/06 , C07D487/04
CPC分类号： A61K31/519 , A61K9/0014 , A61K9/0053 , A61K9/20 , A61K31/573 , A61K45/06 , C07B59/002 , C07B2200/05 , C07D417/04 , C07D471/04 , C07D487/04
摘要： The present invention provides heteroaryl substituted pyrrolo[2,3-b]pyridines and heteroaryl substituted pyrrolo[2,3-b]pyrimidines that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases.
摘要翻译： 本发明提供调节Janus激酶活性的杂芳基取代的吡咯并[2,3-b]吡啶和杂芳基取代的吡咯并[2,3-b]嘧啶，可用于治疗与Janus激酶活性有关的疾病， 例如免疫相关疾病，皮肤病，骨髓增生性疾病，癌症和其它疾病。
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![Heteroaryl Substituted Pyrrolo[2,3-B]Pyridines And Pyrrolo[2,3-B]Pyrimidines As Janus Kinase Inhibitors](/abs-image/US/2014/01/16/US20140018374A1/abs.jpg.150x150.jpg)
7.发明申请Heteroaryl Substituted Pyrrolo[2,3-B]Pyridines And Pyrrolo[2,3-B]Pyrimidines As Janus Kinase Inhibitors 有权杂芳基取代的吡咯并[2,3-B]吡啶和吡咯并[2,3-B]嘧啶作为Janus激酶抑制剂公开(公告)号：US20140018374A1
公开(公告)日：2014-01-16
申请号：US14033039
申请日：2013-09-20
IPC分类号： C07D487/04 , A61K31/519 , A61K45/06
CPC分类号： A61K31/519 , A61K9/0014 , A61K9/0053 , A61K9/20 , A61K31/573 , A61K45/06 , C07B59/002 , C07B2200/05 , C07D417/04 , C07D471/04 , C07D487/04
摘要： The present invention provides heteroaryl substituted pyrrolo[2,3-b]pyridines and heteroaryl substituted pyrrolo[2,3-b]pyrimidines that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases.
摘要翻译： 本发明提供调节Janus激酶活性的杂芳基取代的吡咯并[2,3-b]吡啶和杂芳基取代的吡咯并[2,3-b]嘧啶，可用于治疗与Janus激酶活性有关的疾病， 例如免疫相关疾病，皮肤病，骨髓增生性疾病，癌症和其它疾病。
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公开(公告)号：US20120263676A1
公开(公告)日：2012-10-18
申请号：US13336587
申请日：2011-12-23
申请人： Steven M. Friedman , Peggy A. Scherle , Xiangdong Liu , Timothy C. Burn , Reid Huber , Phillip C.C. Liu , Gregory F. Hollis , Krishna Vaddi , Jordan S. Fridman
发明人： Steven M. Friedman , Peggy A. Scherle , Xiangdong Liu , Timothy C. Burn , Reid Huber , Phillip C.C. Liu , Gregory F. Hollis , Krishna Vaddi , Jordan S. Fridman
IPC分类号： A61K31/496 , A61K38/20 , A61K38/21 , A61K31/495 , A61P35/00 , A61K31/541 , A61K31/444 , A61K31/713 , A61P35/04 , A61K39/395 , A61K31/472
CPC分类号： A61K31/19 , A61K31/395
摘要： The present invention relates to compositions, methods and kits based on the ADAM-mediated cleavage of Her-2. The present invention also relates to treatments for cancer, and in particular, breast cancer, by modulating the ADAM-mediated cleavage of Her-2. Further, the invention relates to compositions, methods and kits based on the surprising synergistic effect between inhibition of Her-2 cleavage by an ADAM and certain cytostatic (e.g., Herceptin) and cytotoxic (e.g., Taxol) compounds in, among other things, inhibiting tumor cell proliferation and inducing cell death. Additionally, the invention relates to novel variants of ADAM15, designated ADAM15 variant 1 and ADAM15 variant 2, now identified and isolated.
摘要翻译： 本发明涉及基于ADAM介导的Her-2切割的组合物，方法和试剂盒。 本发明还涉及通过调节ADAM介导的Her-2切割来治疗癌症，特别是乳腺癌。 此外，本发明涉及基于由ADAM抑制Her-2切割和某些细胞抑制（例如赫赛汀）和细胞毒性（例如紫杉醇）化合物之间令人惊讶的协同效应的组合物，方法和试剂盒，其中包括抑制 肿瘤细胞增殖和诱导细胞死亡。 另外，本发明涉及现在鉴定和分离的ADAM15的新型变体，称为ADAM15变体1和ADAM15变体2。
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公开(公告)号：US08088737B2
公开(公告)日：2012-01-03
申请号：US10817718
申请日：2004-04-02
申请人： Steven M. Friedman , Peggy A. Scherle , Xiangdong Liu , Timothy C. Burn , Reid Huber , Phillip C. C. Liu , Gregory F. Hollis , Krishna Vaddi , Jordan S. Fridman
发明人： Steven M. Friedman , Peggy A. Scherle , Xiangdong Liu , Timothy C. Burn , Reid Huber , Phillip C. C. Liu , Gregory F. Hollis , Krishna Vaddi , Jordan S. Fridman
IPC分类号： A01N61/00 , A61K31/00 , A61K38/00 , A61K39/395 , G01N33/48
CPC分类号： A61K31/19 , A61K31/395
摘要： The present invention relates to compositions, methods and kits based on the ADAM-mediated cleavage of Her-2. The present invention also relates to treatments for cancer, and in particular, breast cancer, by modulating the ADAM-mediated cleavage of Her-2. Further, the invention relates to compositions, methods and kits based on the surprising synergistic effect between inhibition of Her-2 cleavage by an ADAM and certain cytostatic (e.g., Herceptin) and cytotoxic (e.g., Taxol) compounds in, among other things, inhibiting tumor cell proliferation and inducing cell death. Additionally, the invention relates to novel variants of ADAM15, designated ADAM15 variant 1 and ADAM15 variant 2, now identified and isolated.
摘要翻译： 本发明涉及基于ADAM介导的Her-2切割的组合物，方法和试剂盒。 本发明还涉及通过调节ADAM介导的Her-2切割来治疗癌症，特别是乳腺癌。 此外，本发明涉及基于由ADAM抑制Her-2切割和某些细胞抑制（例如赫赛汀）和细胞毒性（例如紫杉醇）化合物之间令人惊讶的协同效应的组合物，方法和试剂盒，其中包括抑制 肿瘤细胞增殖和诱导细胞死亡。 另外，本发明涉及现在鉴定和分离的ADAM15的新型变体，称为ADAM15变体1和ADAM15变体2。
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![HETEROARYL SUBSTITUTED PYRROLO[2,3-b]PYRIDINES AND PYRROLO[2,3-b]PYRIMIDINES AS JANUS KINASE INHIBITORS](/abs-image/US/2011/09/15/US20110223210A1/abs.jpg.150x150.jpg)
10.发明申请公开(公告)号：US20110223210A1
公开(公告)日：2011-09-15
申请号：US13076220
申请日：2011-03-30
申请人： James D. Rodgers , Stacey Shepard , Thomas P. Maduskuie, JR. , Haisheng Wang , Nikoo Falahatpisheh , Maria Rafalski , Argyrios G. Arvanitis , Louis Storace , Ravikumar Jalluri , Jordan S. Fridman , Krishna Vaddi
发明人： James D. Rodgers , Stacey Shepard , Thomas P. Maduskuie, JR. , Haisheng Wang , Nikoo Falahatpisheh , Maria Rafalski , Argyrios G. Arvanitis , Louis Storace , Ravikumar Jalluri , Jordan S. Fridman , Krishna Vaddi
CPC分类号： A61K31/519 , A61K9/0014 , A61K9/0053 , A61K9/20 , A61K31/573 , A61K45/06 , C07B59/002 , C07B2200/05 , C07D417/04 , C07D471/04 , C07D487/04
摘要： The present invention provides heteroaryl substituted pyrrolo[2,3-b]pyridines and heteroaryl substituted pyrrolo[2,3-b]pyrimidines that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases.
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