公开(公告)号：US20180134716A1

公开(公告)日：2018-05-17

申请号：US15707484

申请日：2017-09-18

申请人： Millennium Pharmaceuticals, Inc.

发明人： Christopher F. Claiborne ,  Lloyd J. Payne ,  Richard J. Boyce ,  Todd B. Sells ,  Stephen G. Stroud ,  Stuart Travers ,  Tricia J. Vos ,  Gabriel S. Weatherhead

IPC分类号： C07D487/04 ,  C07D487/14 ,  C07D491/14 ,  C07D495/14 ,  C07D513/14

CPC分类号： C07D487/04 ,  C07D487/14 ,  C07D491/14 ,  C07D495/14 ,  C07D513/14

摘要： This invention relates to compounds and methods for the treatment of cancer. In particular, the invention provides compounds that inhibit Aurora kinase, pharmaceutical compositions comprising the compounds, and methods of using the compounds for the treatment of cancer.

公开(公告)号：US09850214B2

公开(公告)日：2017-12-26

申请号：US14326051

申请日：2014-07-08

申请人： Millennium Pharmaceuticals, Inc.

发明人： Ashley Sue McCarron ,  Todd B. Sells ,  Matthew Stirling ,  Stephen G. Stroud

IPC分类号： A61K31/505 ,  C07D239/02 ,  C07D239/47 ,  C07D239/46 ,  C07D473/02

CPC分类号： C07D239/47 ,  C07D239/46 ,  C07D473/02

摘要： Disclosed are chemical entities which are inhibitors of Nedd8-activating enzyme (NAE), namely, the compound {(1S,2S,4R)-4-[(6-{[(1R,2S)-5-chloro-2-methoxy-2,3-dihydro-1H-inden-1-yl]amino}pyrimidin-4-yl)oxy]-2-hydroxycyclopentyl}methyl sulfamate and pharmaceutically acceptable salts thereof; solid state forms thereof; and prodrugs thereof. Also disclosed are methods of using the chemical entities to treat disorders such as cancer.

公开(公告)号：US20140046055A1

公开(公告)日：2014-02-13

申请号：US13644216

申请日：2012-10-03

申请人： MILLENNIUM PHARMACEUTICALS, INC.

发明人： Christopher F. Claiborne ,  Lloyd J. Payne ,  Richard J. Boyce ,  Todd B. Sells ,  Stephen G. Stroud ,  Stuart Travers ,  Tricia J. Vos ,  Gabriel S. Weatherhead

IPC分类号： C07D487/04

CPC分类号： C07D487/04 ,  C07D487/14 ,  C07D491/14 ,  C07D495/14 ,  C07D513/14

摘要： This invention relates to compounds and methods for the treatment of cancer. In particular, the invention provides compounds that inhibit Aurora kinase, pharmaceutical compositions comprising the compounds, and methods of using the compounds for the treatment of cancer.

摘要翻译： 本发明涉及治疗癌症的化合物和方法。 特别地，本发明提供抑制极光激酶的化合物，包含该化合物的药物组合物，以及使用该化合物治疗癌症的方法。

公开(公告)号：US20200247810A1

公开(公告)日：2020-08-06

申请号：US16569809

申请日：2019-09-13

申请人： Millennium Pharmaceuticals, Inc.

发明人： Christopher F. Claiborne ,  Lloyd J. Payne ,  Richard J. Boyce ,  Todd B. Sells ,  Stephen G. Stroud ,  Stuart Travers ,  Tricia J. Vos ,  Gabriel S. Weatherhead

IPC分类号： C07D487/04 ,  C07D513/14 ,  C07D495/14 ,  C07D491/14 ,  C07D487/14

摘要： This invention relates to compounds and methods for the treatment of cancer. In particular, the invention provides compounds that inhibit Aurora kinase, pharmaceutical compositions comprising the compounds, and methods of using the compounds for the treatment of cancer.

公开(公告)号：US20150011572A1

公开(公告)日：2015-01-08

申请号：US14326051

申请日：2014-07-08

申请人： Millennium Pharmaceuticals, Inc.

发明人： Ashley Sue McCarron ,  Todd B. Sells ,  Matthew Stirling ,  Stephen G. Stroud

IPC分类号： C07D239/47

CPC分类号： C07D239/47 ,  C07D239/46 ,  C07D473/02

摘要： Disclosed are chemical entities which are inhibitors of Nedd8-activating enzyme (NAE), namely, the compound {(1S,2S,4R)-4-[(6-{[(1R,2S)-5-chloro-2-methoxy-2,3-dihydro-1H-inden-1-yl]amino}pyrimidin-4-yl)oxy]-2-hydroxycyclopentyl}methyl sulfamate and pharmaceutically acceptable salts thereof; solid state forms thereof; and prodrugs thereof. Also disclosed are methods of using the chemical entities to treat disorders such as cancer.

摘要翻译： 公开了作为Nedd8活化酶（NAE）抑制剂的化学实体，即化合物{（1S，2S，4R）-4 - [（6 - {[（1R，2S）-5-氯-2-甲氧基 -2,3-二氢-1H-茚-1-基]氨基}嘧啶-4-基）氧基] -2-羟基环戊基}甲基氨基磺酸酯及其药学上可接受的盐; 其固态形式; 及其前体药物。 还公开了使用化学实体来治疗诸如癌症的疾病的方法。

公开(公告)号：US11014928B2

公开(公告)日：2021-05-25

申请号：US16569809

申请日：2019-09-13

申请人： Millennium Pharmaceuticals, Inc.

发明人： Christopher F. Claiborne ,  Lloyd J. Payne ,  Richard J. Boyce ,  Todd B. Sells ,  Stephen G. Stroud ,  Stuart Travers ,  Tricia J. Vos ,  Gabriel S. Weatherhead

IPC分类号： C07D239/42 ,  C07D403/04 ,  C07D403/12 ,  C07D403/14 ,  C07D405/04 ,  C07D405/12 ,  C07D409/04 ,  C07D413/12 ,  C07D417/04 ,  C07D487/04 ,  C07D487/14 ,  C07D491/14 ,  C07D495/14 ,  C07D513/14

摘要： This invention relates to compounds and methods for the treatment of cancer. In particular, the invention provides compounds that inhibit Aurora kinase, pharmaceutical compositions comprising the compounds, and methods of using the compounds for the treatment of cancer.

公开(公告)号：US09765078B2

公开(公告)日：2017-09-19

申请号：US14810225

申请日：2015-07-27

申请人： Millennium Pharmaceuticals, Inc.

发明人： Christopher F. Claiborne ,  Lloyd J. Payne ,  Richard J. Boyce ,  Todd B. Sells ,  Stephen G. Stroud ,  Stuart Travers ,  Tricia J. Vos ,  Gabriel S. Weatherhead

IPC分类号： A61K31/55 ,  C07D471/12 ,  C07D487/04 ,  C07D487/12 ,  C07D487/14 ,  C07D491/14 ,  C07D495/14 ,  C07D513/14

CPC分类号： C07D487/04 ,  C07D487/14 ,  C07D491/14 ,  C07D495/14 ,  C07D513/14

摘要： This invention relates to compounds and methods for the treatment of cancer. In particular, the invention provides compounds that inhibit Aurora kinase, pharmaceutical compositions comprising the compounds, and methods of using the compounds for the treatment of cancer.

公开(公告)号：US09102678B2

公开(公告)日：2015-08-11

申请号：US13644216

申请日：2012-10-03

申请人： Millennium Pharmaceuticals, Inc.

发明人： Christopher F. Claiborne ,  Lloyd J. Payne ,  Richard J. Boyce ,  Todd B. Sells ,  Stephen G. Stroud ,  Stuart Travers ,  Tricia J. Vos ,  Gabriel S. Weatherhead

IPC分类号： A61K31/55 ,  C07D487/04 ,  C07D487/14 ,  C07D491/14 ,  C07D495/14 ,  C07D513/14

CPC分类号： C07D487/04 ,  C07D487/14 ,  C07D491/14 ,  C07D495/14 ,  C07D513/14

摘要： This invention relates to compounds and methods for the treatment of cancer. In particular, the invention provides compounds that inhibit Aurora kinase, pharmaceutical compositions comprising the compounds, and methods of using the compounds for the treatment of cancer.

公开(公告)号：US20190031662A1

公开(公告)日：2019-01-31

申请号：US15996166

申请日：2018-06-01

申请人： Millennium Pharmaceuticals, Inc.

发明人： Christopher F. Claiborne ,  Todd B. Sells ,  Stephen G. Stroud

IPC分类号： C07D487/04

摘要： The present invention relates to compounds and methods for the treatment of cancer. In particular, the invention provides potent inhibitors of Aurora A kinase, pharmaceutical compositions comprising the compounds, and methods of using the compounds for the treatment of cancer.

公开(公告)号：US20150175563A1

公开(公告)日：2015-06-25

申请号：US14445376

申请日：2014-07-29

申请人： Millennium Pharmaceuticals, Inc.

发明人： Brian S. Freeze ,  Masaaki Hirose ,  Yongbo Hu ,  Todd B. Sells ,  Zhan Shi ,  Stepan Vyskocil ,  Tianlin Xu

IPC分类号： C07D277/56 ,  C07D409/14 ,  C07D417/14 ,  C07D417/04 ,  C07D333/38 ,  C07D409/04

CPC分类号： C07D277/56 ,  A61K31/4155 ,  A61K31/425 ,  A61K31/437 ,  A61K31/4375 ,  A61K31/4439 ,  A61K31/4725 ,  A61K31/495 ,  A61K31/496 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  A61K45/06 ,  C07D277/64 ,  C07D293/06 ,  C07D333/38 ,  C07D333/54 ,  C07D409/04 ,  C07D409/06 ,  C07D409/14 ,  C07D413/14 ,  C07D417/04 ,  C07D417/06 ,  C07D417/14 ,  C07D471/04 ,  C07D491/107 ,  C07D495/04

摘要： This invention provides compounds of formula IA-i-a or IB-i-a and subsets thereof: wherein Z, HY, R1, R2, R3, G1, W, n, and A and subsets thereof are as described in the specification. The compounds are inhibitors of PI3K and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.

摘要翻译： 本发明提供式IA-i-a或IB-i-a及其子集的化合物：其中Z，HY，R1，R2，R3，G1，W，n和A及其子集如说明书中所述。 这些化合物是PI3K的抑制剂，因此可用于治疗增殖性，炎性或心血管疾病。