公开(公告)号：EP1797072A2

公开(公告)日：2007-06-20

申请号：EP05796701.0

申请日：2005-09-15

申请人： Exelixis, Inc.

发明人： BAIK, Tae-Gon ,  BUHR, Chris, A. ,  MA, Sunghoon ,  NUSS, John, M. ,  TESFAI, Zerom ,  WANG, Longcheng ,  YEUNG, Bryan, K.S. Novartis Inst. for Tropical Diseases

IPC分类号： C07D401/14

CPC分类号： C07D403/04 ,  C07D231/12 ,  C07D401/04 ,  C07D405/04 ,  C07D409/04

摘要： The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferationm, differentiation, programmed cell death, migration and chemoinvasion. Compounds of the invention inhibit, regulate and/0r modulate kinases. Methods of using the compounds and pharmaceutical compositions thereof to treat kinase-dependent diseases and conditions are also an aspect of the invention.

摘要翻译： 本发明提供了调节蛋白激酶酶活性以调节细胞活性如增殖，分化，程序性细胞死亡，迁移和化学侵袭的化合物。 本发明化合物抑制，调节和/或调节激酶。 使用该化合物及其药物组合物治疗激酶依赖性疾病和病症的方法也是本发明的一个方面。

公开(公告)号：EP1931645B1

公开(公告)日：2014-07-16

申请号：EP06836252.4

申请日：2006-10-09

申请人： Exelixis, Inc.

发明人： BAJJALIEH, William ,  CANNE BANNEN, Lynne ,  BROWN, S., David ,  KEARNEY, Patrick ,  MAC, Morrison, B. ,  MARLOWE, Charles, K. ,  NUSS, John, M. ,  TESFAI, Zerom ,  WANG, Yong ,  XU, Wei

IPC分类号： C07D241/44 ,  C07D401/12 ,  C07D403/12 ,  C07D407/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  A61K31/498 ,  A61K31/4985 ,  A61P35/00

CPC分类号： C07D401/12 ,  C07D241/44 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  Y02P20/55

公开(公告)号：EP1501514B1

公开(公告)日：2012-12-19

申请号：EP03728690.3

申请日：2003-05-02

申请人： Exelixis, Inc.

发明人： BUHR, Chris, A. ,  BAIK, Tae-Gon ,  MA, Sunghoon ,  TESFAI, Zerom ,  WANG, Longcheng ,  CO, Erick, Wang ,  EPSHTEYN, Sergey ,  KENNEDY, Abigail, R. ,  CHEN, Baili ,  DUBENKO, Larisa ,  ANAND, Neel Kumar ,  TSANG, Tsze, H. ,  NUSS, John, M. ,  PETO, Csaba, J. ,  RICE, Kenneth, D. ,  IBRAHIM, Mohamed, Abdulkader ,  SCHNEPP, Kevin, Luke ,  SHI, Xian ,  LEAHY, James, William ,  CHEN, Jeff ,  DALRYMPLE, Lisa Esther ,  FORSYTH, Thimothy Patrick ,  HUYNH, Tai Phat ,  MANN, Grace ,  MANN, Lary Wayne ,  TAKEUCHI, Craig Stacy

IPC分类号： C07D241/26 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/10 ,  C07D403/12 ,  C07D405/12 ,  C07D413/04 ,  C07D413/12 ,  C07D413/14

CPC分类号： C07D401/04 ,  C07D241/26 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/10 ,  C07D403/12 ,  C07D405/12 ,  C07D413/04 ,  C07D413/12 ,  C07D413/14

公开(公告)号：EP2134695A1

公开(公告)日：2009-12-23

申请号：EP08732145.1

申请日：2008-03-13

申请人： Exelixis, Inc.

发明人： BAHCECI, Suleyman ,  BAJJALIEH, William ,  CHEN, Jeff ,  EPSHTEYN, Sergey ,  FORSYTH, Timothy Patrick ,  HUYNH, Tai Phat ,  KIM, Byung Gyu ,  LEAHY, James W. ,  LEE, Matthew Sangyup ,  LEWIS, Gary L. ,  MAC, Morrison B. ,  MANN, Grace ,  MARLOWE, Charles K. ,  RIDGWAY, Brian Hugh ,  SANGALANG, Joan C. ,  SHI, Xian ,  TAKEUCHI, Craig Stacy ,  WANG, Yong ,  TESFAI, Zerom

IPC分类号： C07D239/42 ,  C07D401/04 ,  C07D403/12

CPC分类号： C07D239/42 ,  C07D239/70 ,  C07D239/84 ,  C07D239/95 ,  C07D401/04 ,  C07D403/12

摘要： The present invention is directed to a compound of Formula (I) or a single isomer thereof; where the compound is optionally as a pharmaceutically acceptable salt, hydrate, solvate or combination thereof, in addition to methods of preparing a Compound of Formula I, and methods of using a Compound of Formula (I) to treat cancer.

公开(公告)号：EP1931645A2

公开(公告)日：2008-06-18

申请号：EP06836252.4

申请日：2006-10-09

申请人： Exelixis, Inc.

发明人： BAJJALIEH, William ,  CANNE BANNEN, Lynne ,  BROWN, S., David ,  KEARNEY, Patrick ,  MAC, Morrison, B. ,  MARLOWE, Charles, K. ,  NUSS, John, M. ,  TESFAI, Zerom ,  WANG, Yong ,  XU, Wei

IPC分类号： C07D241/44 ,  C07D401/12 ,  C07D403/12 ,  C07D407/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  A61K31/498 ,  A61K31/4985 ,  A61P35/00

CPC分类号： C07D401/12 ,  C07D241/44 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  Y02P20/55

摘要： The present invention comprises small molecule inhibitors of phosphatidylinositol 3-kinase (PI3K), which is associated with a number of malignancies such as ovarian cancer, cervical cancer, breast cancer, colon cancer, rectal cancer, and glioblastomas, among others. Accordingly, the compounds of the present invention are useful for treating, preventing, and/or inhibiting these diseases.

公开(公告)号：EP1501514A2

公开(公告)日：2005-02-02

申请号：EP03728690.3

申请日：2003-05-02

申请人： Exelixis, Inc.

发明人： BUHR, Chris, A. ,  BAIK, Tae-Gon ,  MA, Sunghoon ,  TESFAI, Zerom ,  WANG, Longcheng ,  CO, Erick, Wang ,  EPSHTEYN, Sergey ,  KENNEDY, Abigail, R. ,  CHEN, Baili ,  DUBENKO, Larisa ,  ANAND, Neel Kumar ,  TSANG, Tsze, H. ,  NUSS, John, M. ,  PETO, Csaba, J. ,  RICE, Kenneth, D. ,  IBRAHIM, Mohamed, Abdulkader ,  SCHNEPP, Kevin, Luke ,  SHI, Xian ,  LEAHY, James, William ,  CHEN, Jeff ,  DALRYMPLE, Lisa Esther ,  FORSYTH, Thimothy Patrick ,  HUYNH, Tai Phat ,  MANN, Grace ,  MANN, Lary Wayne ,  TAKEUCHI, Craig Stacy

IPC分类号： A61K31/4965 ,  A61K31/497 ,  A61K31/55 ,  C07D241/28 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D405/04 ,  C07D413/04 ,  C07D413/14

CPC分类号： C07D401/04 ,  C07D241/26 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/10 ,  C07D403/12 ,  C07D405/12 ,  C07D413/04 ,  C07D413/12 ,  C07D413/14

摘要： This invention relates to compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion, and to pharmaceutical compositions containing such compounds. Even more specifically, the invention relates to compounds that inhibit, regulate and/or modulate kinases, particularly Checkpoint Kinases, even more particularly Checkpoint Kinase 1, or Chk1. Methods of therapeutically or prophylactically using the compounds and compositions to treat kinase-dependent diseases and conditions are also an aspect of the invention, and include methods of treating cancer, as well as other disease states associated with unwanted angiogenesis and/or cellular proliferation, by administering effective amounts of such compounds.

公开(公告)号：EP2702043A1

公开(公告)日：2014-03-05

申请号：EP12725560.2

申请日：2012-04-30

申请人： Exelixis, Inc.

发明人： TSUHAKO, Amy, Lew ,  MARLOWE, Charles, K. ,  ZAHARIA, Christiana, A. ,  KABIGTING, Lori ,  BAJJALIEH, William ,  TESFAI, Zerom ,  HUANG, Ping ,  MOON, Kim ,  AAY, Naing ,  TAMBO-ONG, Arlyn ,  NUSS, John, M. ,  XU, Wei ,  KEARNEY, Patrick

IPC分类号： C07D239/42 ,  C07D401/04 ,  C07D403/04 ,  C07D403/12 ,  C07D405/04 ,  C07D405/12 ,  C07D405/14 ,  C07D409/04 ,  C07D413/04 ,  C07D417/04 ,  C07D417/14 ,  A61K31/506 ,  A61P35/00

CPC分类号： C07D239/42 ,  C07D401/04 ,  C07D403/04 ,  C07D403/12 ,  C07D405/04 ,  C07D405/12 ,  C07D405/14 ,  C07D409/04 ,  C07D413/04 ,  C07D417/04 ,  C07D417/14

摘要： The invention is directed to inhibitors of inducible form of 6-phosphofructose-2-kinase of formula I, as well as to pharmaceutically acceptable salts of formula I, and pharmaceutical compositions comprising a compound of formula I. The compounds can be used to treat cancer.

公开(公告)号：EP2616443A1

公开(公告)日：2013-07-24

申请号：EP11764895.6

申请日：2011-09-13

申请人： Exelixis, Inc.

发明人： ANAND, Neel, Kumar ,  BROWN, S., David ,  TESFAI, Zerom ,  ZAHARIA, Cristiana, A.

IPC分类号： C07D217/22 ,  C07D237/34 ,  C07D403/10 ,  C07D405/04 ,  C07D409/04 ,  C07D417/10 ,  C07D471/04 ,  A61K31/4985 ,  A61P35/00

CPC分类号： C07D409/04 ,  C07D217/22 ,  C07D237/34 ,  C07D403/10 ,  C07D405/04 ,  C07D417/10 ,  C07D471/04

摘要： JAK1 inhibitors of structural formula (I), wherein Ar
1 , Ar
2 , Q, W, X, Y, and Z are defined in the specification, pharmaceutically acceptable salts thereof, compositions thereof, and use of the compounds and compositions for treating diseases. The invention also comprises use of the compounds in and for the manufacture of medicaments, particularly for treating diseases.

摘要翻译： 结构式（I）的JAK1抑制剂，其中Ar 1，Ar 2，Q，W，X，Y和Z如说明书中所定义，其药学上可接受的盐，其组合物以及该化合物和组合物用于治疗疾病 。 本发明还包括化合物在和用于制造药物中的用途，特别是用于治疗疾病。