公开(公告)号：US20140275083A1

公开(公告)日：2014-09-18

申请号：US14208015

申请日：2014-03-13

申请人： 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

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： C07D413/04 ,  A61K31/5377 ,  C07D417/14 ,  C07D413/14 ,  A61K31/506

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：US20150306085A1

公开(公告)日：2015-10-29

申请号：US14754152

申请日：2015-06-29

申请人： Dylan DANIEL ,  Johanna JOYCE ,  James SUTTON

发明人： Dylan DANIEL ,  Johanna JOYCE ,  James SUTTON

IPC分类号： A61K31/4439 ,  A61K45/06 ,  C07D417/12

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.

摘要翻译： 本发明提供式I化合物; 其中R1是烷基吡唑或烷基甲酰胺，R2是羟基环烷基; 或其药学上可接受的盐，以及含有这些化合物的组合物，用于治疗脑肿瘤，特别是成胶质细胞瘤。 本发明提供对脑肿瘤的有效治疗，并且可以通过口服施用本文进一步描述的式I化合物来使用。 本发明还提供了治疗具有脑肿瘤如胶质母细胞瘤的受试者的方法，其中所述方法包括给予受试者有效量的式I化合物。还公开了使用这些方法与成功治疗相关的基因标记。

公开(公告)号：US20130101622A1

公开(公告)日：2013-04-25

申请号：US13466021

申请日：2012-05-07

申请人： James SUTTON ,  Feng Xu ,  Nicholas Valiante ,  Jiong Lan

发明人： James SUTTON ,  Feng Xu ,  Nicholas Valiante ,  Jiong Lan

IPC分类号： A61K31/4985 ,  A61K39/21 ,  A61K39/39 ,  C07D487/04

CPC分类号： A61K31/4985 ,  A61K39/21 ,  A61K39/39 ,  C07D487/04

摘要： The invention provides novel compositions comprising imidazoquinoxaline compounds of formula (I) and analogs thereof. Also provided are methods of administering the compositions in an effective amount to enhance the immune response of a subject. Further provided are novel compositions and methods of administering the compositions in combination with (an) other agent(s).

摘要翻译： 本发明提供了包含式（I）的咪唑并喹喔啉化合物及其类似物的新型组合物。 还提供了以有效量施用组合物以增强受试者的免疫应答的方法。 进一步提供了组合物与（一种或多种）其它试剂组合施用的新型组合物和方法。