公开(公告)号：EP3057955B1

公开(公告)日：2018-04-11

申请号：EP14799918.9

申请日：2014-10-17

申请人： Syros Pharmaceuticals, Inc. ,  Dana-Farber Cancer Institute, Inc.

发明人： CIBLAT, Stephane ,  DEROY, Patrick ,  GRAY, Nathanael ,  LEBLANC, Melissa ,  MARINEAU, Jason, J. ,  MOORE, Joel ,  SPROTT, Kevin ,  ZHANG, Tinghu ,  SIDDIQUI, M., Arshad ,  KABRO, Anzhelika ,  LEGER, Serge ,  MILLER, Tom ,  ROY, Stephanie ,  SCHMIDT, Darby ,  WINTER, Dana, K. ,  BRADLEY, Michael

IPC分类号： C07D401/14 ,  A61K31/506 ,  A61P35/02

CPC分类号： C07D401/14 ,  A61K31/506 ,  A61K45/06

摘要： The present invention provides novel compounds of Formula (I), and pharmaceutically acceptable salts, solvates, hydrates, tautomers, stereoisomers, isotopically labeled derivatives, and compositions thereof. Also provided are methods and kits involving the compounds or compositions for treating or preventing proliferative diseases (e.g., cancers (e.g., leukemia, melanoma, multiple myeloma), benign neoplasms, angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases) in a subject. Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity of a kinase, such as a cyclin-dependent kinase (CDK) (e.g., cyclin-dependent kinase 7 (CDK7)), and therefore, induce cellular apoptosis and/or inhibit transcription in the subject.

公开(公告)号：EP3057956A1

公开(公告)日：2016-08-24

申请号：EP14799580.7

申请日：2014-10-17

申请人： Dana-Farber Cancer Institute, Inc.

发明人： GRAY, Nathanael ,  ZHANG, Tinghu ,  CIBLAT, Stephane ,  LEBLANC, Melissa ,  SPROTT, Kevin ,  MOORE, Joel ,  MARINEAU, Jason J. ,  KABRO, Anzhelika ,  MILLER, Tom ,  ROY, Stephanie ,  SIDDIQUI, M. Arshad ,  SCHMIDT, Darby ,  WINTER, Dana K. ,  BRADLEY, Michael

IPC分类号： C07D403/04 ,  C07D401/04 ,  C07D471/04 ,  C07D417/04 ,  C07D413/04 ,  C07F7/08 ,  A61K31/506 ,  A61P35/00

CPC分类号： C07D403/04 ,  C07D401/04 ,  C07D413/04 ,  C07D417/04 ,  C07D471/04 ,  C07F7/0812

摘要： The present invention provides novel compounds of Formula (I), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, prodrugs, and compositions thereof. Also provided are methods and kits involving the inventive compounds or compositions for treating or preventing proliferative diseases (e.g., cancers (e.g., leukemia, lymphoma, melanoma, multiple myeloma, breast cancer, Ewing' s sarcoma, osteosarcoma, brain cancer, neuroblastoma, lung cancer), benign neoplasms, angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases) in a subject. Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity of a kinase, such as a cyclin-dependent kinase (CDK) (e.g., cyclin-dependent kinase 7 (CDK7), cyclin-dependent kinase 12 (CDK12), or cyclin-dependent kinase 13 (CDK13)), and therefore, induce cellular apoptosis and/or inhibit transcription in the subject.

公开(公告)号：EP3057955A1

公开(公告)日：2016-08-24

申请号：EP14799918.9

申请日：2014-10-17

申请人： Syros Pharmaceuticals, Inc. ,  Dana-Farber Cancer Institute, Inc.

发明人： CIBLAT, Stephane ,  DEROY, Patrick ,  GRAY, Nathanael ,  LEBLANC, Melissa ,  MARINEAU, Jason, J. ,  MOORE, Joel ,  SPROTT, Kevin ,  ZHANG, Tinghu ,  SIDDIQUI, M., Arshad ,  KABRO, Anzhelika ,  LEGER, Serge ,  MILLER, Tom ,  ROY, Stephanie ,  SCHMIDT, Darby ,  WINTER, Dana, K. ,  BRADLEY, Michael

IPC分类号： C07D401/14 ,  A61K31/506 ,  A61P35/02

CPC分类号： C07D401/14 ,  A61K31/506 ,  A61K45/06

摘要： The present invention provides novel compounds of Formula (I), and pharmaceutically acceptable salts, solvates, hydrates, tautomers, stereoisomers, isotopically labeled derivatives, and compositions thereof. Also provided are methods and kits involving the compounds or compositions for treating or preventing proliferative diseases (e.g., cancers (e.g., leukemia, melanoma, multiple myeloma), benign neoplasms, angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases) in a subject. Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity of a kinase, such as a cyclin-dependent kinase (CDK) (e.g., cyclin-dependent kinase 7 (CDK7)), and therefore, induce cellular apoptosis and/or inhibit transcription in the subject.

摘要翻译： 本发明提供新的式（I）化合物及其药学上可接受的盐，溶剂合物，水合物，互变异构体，立体异构体，同位素标记的衍生物及其组合物。 还提供了涉及用于治疗或预防受试者的增殖性疾病（例如，癌症（例如白血病，黑素瘤，多发性骨髓瘤），良性肿瘤，血管生成，炎性疾病，自身炎性疾病和自身免疫性疾病）的化合物或组合物的方法和试剂盒 。 使用本发明的化合物或组合物治疗具有增殖性疾病的受试者可以抑制激酶例如细胞周期蛋白依赖性激酶（CDK）（例如，细胞周期蛋白依赖性激酶7（CDK7））的异常活性，因此 ，诱导受试者的细胞凋亡和/或抑制转录。