公开(公告)号：WO2018013867A8

公开(公告)日：2018-01-18

申请号：PCT/US2017/042017

申请日：2017-07-13

申请人： MARINEAU, Jason, J. ,  ZAHLER, Robert ,  CIBLAT, Stephane ,  WINTER, Dana, K. ,  KABRO, Anzhelika ,  ROY, Stephanie ,  SCHMIDT, Darby ,  CHUAQUI, Claudio ,  MALOJCIC, Goran ,  PIRAS, Henri ,  WHITMORE, Kenneth, Matthew ,  LUND, Kate-Iyn ,  SINKO, Bill ,  SPROTT, Kevin

发明人： MARINEAU, Jason, J. ,  ZAHLER, Robert ,  CIBLAT, Stephane ,  WINTER, Dana, K. ,  KABRO, Anzhelika ,  ROY, Stephanie ,  SCHMIDT, Darby ,  CHUAQUI, Claudio ,  MALOJCIC, Goran ,  PIRAS, Henri ,  WHITMORE, Kenneth, Matthew ,  LUND, Kate-Iyn ,  SINKO, Bill ,  SPROTT, Kevin

IPC分类号： C07D401/14 ,  A61P35/00 ,  A61K31/506

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 cyclin-dependent kinase 7 (CDK7), and therefore, induce cellular apoptosis and/or inhibit transcription in the subject.

公开(公告)号：WO2018013867A1

公开(公告)日：2018-01-18

申请号：PCT/US2017/042017

申请日：2017-07-13

申请人： MARINEAU, Jason, J. ,  ZAHLER, Robert ,  CIBLAT, Stephane ,  WINTER, Dana, K. ,  KABRO, Anzhelika ,  ROY, Stephanie ,  SCHMIDT, Darby ,  CHUAQUI, Claudio ,  MALOJCIC, Goran ,  PIRAS, Henri ,  WHITMORE, Kenneth, Matthew ,  LUND, Kate-Iyn ,  SINKO, Bill ,  SPROTT, Kevin

发明人： MARINEAU, Jason, J. ,  ZAHLER, Robert ,  CIBLAT, Stephane ,  WINTER, Dana, K. ,  KABRO, Anzhelika ,  ROY, Stephanie ,  SCHMIDT, Darby ,  CHUAQUI, Claudio ,  MALOJCIC, Goran ,  PIRAS, Henri ,  WHITMORE, Kenneth, Matthew ,  LUND, Kate-Iyn ,  SINKO, Bill ,  SPROTT, Kevin

IPC分类号： C07D401/14 ,  A61P35/00 ,  A61K31/506

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 cyclin-dependent kinase 7 (CDK7), and therefore, induce cellular apoptosis and/or inhibit transcription in the subject.

摘要翻译： 本发明提供了新的式（I）化合物及其药学上可接受的盐，溶剂化物，水合物，互变异构体，立体异构体，同位素标记的衍生物和组合物。 还提供涉及用于在受试者中治疗或预防增殖性疾病（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，炎症性疾病，自身炎症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患有增殖性疾病的受试者可抑制细胞周期蛋白依赖性激酶7（CDK7）的异常活性，并因此诱导细胞凋亡和/或抑制受试者中的转录。