公开(公告)号：US10537561B2

公开(公告)日：2020-01-21

申请号：US15996945

申请日：2018-06-04

申请人： Novartis AG ,  Sloan-Kettering Institute for Cancer Research

发明人： Dylan Daniel ,  Johanna Joyce ,  James Sutton

IPC分类号： A61K31/4439 ,  A61K31/175 ,  A61K31/4545 ,  A61K31/675 ,  A61K45/06 ,  C07D417/12 ,  C07D417/14 ,  A61K39/395

摘要： The present invention provides a compound of formula I; wherein R1 is an alkyl pyrazole or an alkyl carboxamide, and R2 is a hydroxycycloalkyl; or a pharmaceutically acceptable salt thereof, and compositions containing these compounds, for use to treat a brain tumor, particularly glioblastoma. The invention provides effective treatment of a brain tumor and can be used by oral administration of a compound of Formula I as further described herein. The invention also provides a method to treat a subject having a brain tumor such as glioblastoma, wherein the method comprises administering to the subject an effective amount of a compound of Formula I. Gene signatures correlated with successful treatment using these methods are also disclosed.

公开(公告)号：US20130172354A1

公开(公告)日：2013-07-04

申请号：US13773052

申请日：2013-02-21

申请人： Novartis AG

发明人： Paul A. Barsanti ,  Cheng Hu ,  Jeff Jin ,  Robert Keyes ,  Robert Kucejko ,  Xiaodong Lin ,  Yue Pan ,  Keith B. Pfister ,  Martin Sendzik ,  James Sutton ,  Lifeng Wan

IPC分类号： C07D401/04 ,  C07D409/14 ,  C07D413/14 ,  C07D401/14 ,  C07D405/14

CPC分类号： A61K31/497 ,  C07D213/74 ,  C07D241/20 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14

摘要： The present invention provides a compound of formula (I): and pharmaceutically acceptable salts, enantiomers, stereoisomers, rotamers, tautomers, diastereomers, or racemates thereof. Also provided is a method of treating a disease or condition mediated by CDK9.

摘要翻译： 本发明提供式（I）化合物及其药学上可接受的盐，对映体，立体异构体，旋转异构体，互变异构体，非对映体或其外消旋物。 还提供了治疗由CDK9介导的疾病或病症的方法。

公开(公告)号：US20150152093A1

公开(公告)日：2015-06-04

申请号：US14408418

申请日：2014-03-12

申请人： NOVARTIS AG

发明人： Thomas Raymond Caferro ,  Zhuoliang Chen ,  Young Shin Cho ,  Abran Q. Costales ,  Julian Roy Levell ,  Gang Liu ,  James R. Manning ,  Martin Sendzik ,  Cynthia Shafer ,  Michael David Shultz ,  James Sutton ,  Yaping Wang ,  Qian Zhao

IPC分类号： C07D413/14 ,  C07D413/04 ,  A61K31/5377 ,  A61K31/506 ,  C07D417/14

CPC分类号： C07D413/14 ,  A61K31/506 ,  A61K31/5377 ,  A61K45/06 ,  C07D413/04 ,  C07D417/14

摘要： The invention is directed to a formula (I): or a pharmaceutically acceptable salt thereof, wherein R1, R2a, R2b and R3-R7 are herein. The invention is also directed to compositions containing a compound of formula (I) and to the use of such compounds in the inhibition of mutant IDH proteins having a neomorphic activity. The invention is further directed to the use of a compound of formula (I) in the treatment of diseases or disorders associated with such mutant IDH proteins including, but not limited to, cell-proliferation disorders, such as cancer.

摘要翻译： 本发明涉及式（I）：或其药学上可接受的盐，其中R1，R2a，R2b和R3-R7为本文。 本发明还涉及含有式（I）化合物的组合物以及这些化合物在抑制具有新形态活性的突变体IDH蛋白质中的用途。 本发明还涉及式（I）化合物在治疗与这种突变体IDH蛋白相关的疾病或病症中的用途，包括但不限于细胞增殖病症如癌症。

公开(公告)号：US08778951B2

公开(公告)日：2014-07-15

申请号：US13773052

申请日：2013-02-21

申请人： Novartis AG

发明人： Paul A. Barsanti ,  Cheng Hu ,  Jeff Jin ,  Robert Keyes ,  Robert Kucejko ,  Xiaodong Lin ,  Yue Pan ,  Keith B. Pfister ,  Martin Sendzik ,  James Sutton ,  Lifeng Wan

IPC分类号： A61K31/50 ,  A61K31/501 ,  A61K31/497 ,  C07D241/20

CPC分类号： A61K31/497 ,  C07D213/74 ,  C07D241/20 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14

摘要： The present invention provides a compound of formula (I): and pharmaceutically acceptable salts, enantiomers, stereoisomers, rotamers, tautomers, diastereomers, or racemates thereof. Also provided is a method of treating a disease or condition mediated by CDK9.

摘要翻译： 本发明提供式（I）化合物及其药学上可接受的盐，对映体，立体异构体，旋转异构体，互变异构体，非对映体或其外消旋物。 还提供了治疗由CDK9介导的疾病或病症的方法。

公开(公告)号：US20190030013A1

公开(公告)日：2019-01-31

申请号：US15996945

申请日：2018-06-04

申请人： Novartis AG ,  Sloan-Kettering Institute for Cancer Research

发明人： Dylan Daniel ,  Johanna Joyce ,  James Sutton

IPC分类号： A61K31/4439 ,  A61K39/395 ,  A61K31/675 ,  A61K31/4545 ,  C07D417/14 ,  C07D417/12 ,  A61K45/06 ,  A61K31/175

CPC分类号： A61K31/4439 ,  A61K31/175 ,  A61K31/4545 ,  A61K31/675 ,  A61K39/3955 ,  A61K45/06 ,  C07D417/12 ,  C07D417/14

摘要： The present invention provides a compound of formula I; wherein R1 is an alkyl pyrazole or an alkyl carboxamide, and R2 is a hydroxycycloalkyl; or a pharmaceutically acceptable salt thereof, and compositions containing these compounds, for use to treat a brain tumor, particularly glioblastoma. The invention provides effective treatment of a brain tumor and can be used by oral administration of a compound of Formula I as further described herein. The invention also provides a method to treat a subject having a brain tumor such as glioblastoma, wherein the method comprises administering to the subject an effective amount of a compound of Formula I. Gene signatures correlated with successful treatment using these methods are also disclosed.