公开(公告)号：EP2349997B1

公开(公告)日：2015-08-12

申请号：EP09737501.8

申请日：2009-10-07

申请人： Exelixis, Inc. ,  Daiichi Sankyo Company, Limited

发明人： NUSS, John ,  WILLIAMS, Matthew ,  MOHAN, Raju ,  MARTIN, Richard ,  WANG, Tie-Lin ,  AOKI, Kazumasa ,  TSURUOKA, Hiroyuki ,  HAYASHI, Noriyuki ,  HOMMA, Tsuyoshi

IPC分类号： C07D207/34 ,  A61K31/40 ,  A61P9/00

CPC分类号： C07D207/34

公开(公告)号：EP2349997A1

公开(公告)日：2011-08-03

申请号：EP09737501.8

申请日：2009-10-07

申请人： Exelixis, Inc. ,  Daiichi Sankyo Company, Limited

发明人： NUSS, John ,  WILLIAMS, Matthew ,  MOHAN, Raju ,  MARTIN, Richard ,  WANG, Tie-Lin ,  AOKI, Kazumasa ,  TSURUOKA, Hiroyuki ,  HAYASHI, Noriyuki ,  HOMMA, Tsuyoshi

IPC分类号： C07D207/34 ,  A61K31/40 ,  A61P9/00

CPC分类号： C07D207/34

摘要： The present invention comprises a compound for the prevention and/or treatment of cardiovascular diseases. The compound is an atropisomer of a compound represented by the following general formula (I ) : wherein R
1 represents a C1-C3 alkyl group; R
2 represents a 2-hydroxy- C4-C6 alkyl group; R
3 represents a halogeno group, a halogeno-C1-C3 alkyl group and the like; R
4 represents a hydrogen atom, a halogeno group and the like; R
5 represents a C1-C3 alkyl group; and R
6 represents a hydrogen atom, a halogeno group and the like] or atropisomers thereof.

公开(公告)号：EP1773768A2

公开(公告)日：2007-04-18

申请号：EP05803281.4

申请日：2005-07-30

申请人： Exelixis, Inc.

发明人： CANNE BANNEN, Lynne ,  CHEN, Jeff ,  DALRYMPLE, Lisa, Esther ,  FLATT, Brenton, T. ,  FORSYTH, Timothy, Patrick ,  GU, Xiao-Hu ,  MAC, Morrison, B. ,  MANN, Larry, W. ,  MANN, Grace ,  MARTIN, Richard ,  MOHAN, Raju ,  MURPHY, Brett ,  NYMAN, Michael, Charles ,  STEVENS, William, C., Jr. ,  WANG, Tie-Lin ,  WANG, Yong ,  WU, Jason, H.

IPC分类号： C07D207/325 ,  A61K31/40

CPC分类号： C07D207/416 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12

摘要： Compounds, compositions and methods for modulating the activity of receptors are provided. In particular compounds and compositions are provided for modulating the activity of receptors and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder directly or indirectly related to the activity of the receptors.

公开(公告)号：EP1773768B8

公开(公告)日：2018-12-26

申请号：EP05803281.4

申请日：2005-07-30

申请人： Exelixis, Inc.

发明人： CANNE BANNEN, Lynne ,  CHEN, Jeff ,  DALRYMPLE, Lisa, Esther ,  FLATT, Brenton, T. ,  FORSYTH, Timothy, Patrick ,  GU, Xiao-Hui ,  MAC, Morrison, B. ,  MANN, Larry, W. ,  MANN, Grace ,  MARTIN, Richard ,  MOHAN, Raju ,  MURPHY, Brett ,  NYMAN, Michael, Charles ,  STEVENS, William, C., Jr. ,  WANG, Tie-Lin ,  WANG, Yong ,  WU, Jason, H.

IPC分类号： C07D207/416 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12 ,  A61K31/40 ,  A61K31/4025 ,  A61K31/415 ,  A61K31/426 ,  A61K31/428 ,  A61K31/433 ,  A61K31/4439 ,  A61P3/00 ,  A61P15/08 ,  A61P19/00 ,  A61P35/00

CPC分类号： C07D207/416 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12

摘要： Compounds, compositions and methods for modulating the activity of receptors are provided. In particular compounds and compositions are provided for modulating the activity of receptors and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder directly or indirectly related to the activity of the receptors.

公开(公告)号：EP1773768B1

公开(公告)日：2018-08-22

申请号：EP05803281.4

申请日：2005-07-30

申请人： Exelixis, Inc.

发明人： CANNE BANNEN, Lynne ,  CHEN, Jeff ,  DALRYMPLE, Lisa, Esther ,  FLATT, Brenton, T. ,  FORSYTH, Timothy, Patrick ,  GU, Xiao-Hui ,  MAC, Morrison, B. ,  MANN, Larry, W. ,  MANN, Grace ,  MARTIN, Richard ,  MOHAN, Raju ,  MURPHY, Brett ,  NYMAN, Michael, Charles ,  STEVENS, William, C., Jr. ,  WANG, Tie-Lin ,  WANG, Yong ,  WU, Jason, H.

IPC分类号： C07D207/416 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12 ,  A61K31/40 ,  A61K31/4025 ,  A61K31/415 ,  A61K31/426 ,  A61K31/428 ,  A61K31/433 ,  A61K31/4439 ,  A61P3/00 ,  A61P15/08 ,  A61P19/00 ,  A61P35/00

CPC分类号： C07D207/416 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12

摘要： Compounds, compositions and methods for modulating the activity of receptors are provided. In particular compounds and compositions are provided for modulating the activity of receptors and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder directly or indirectly related to the activity of the receptors.

公开(公告)号：EP1910308A1

公开(公告)日：2008-04-16

申请号：EP06785562.7

申请日：2006-06-26

申请人： Exelixis, Inc.

发明人： BUSCH, Brett B. ,  FLATT, Brenton T. ,  GU, Xiao-Hui ,  LU, Shao-Po ,  MARTIN, Richard ,  MOHAN, Raju ,  NYMAN, Michael Charles ,  SCHWEIGER, Edwin ,  STEVENS, William C., Jr. ,  WANG, Tie-Lin ,  XIE, Yinong

IPC分类号： C07D233/54 ,  C07D409/04 ,  C07D401/04 ,  A61K31/4164 ,  A61P3/10

CPC分类号： C07D233/64 ,  C07D231/12 ,  C07D231/22 ,  C07D233/90 ,  C07D401/04 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/10 ,  C07D403/12 ,  C07D403/14 ,  C07D405/10 ,  C07D405/12 ,  C07D405/14 ,  C07D409/04 ,  C07D409/10 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/10 ,  C07D417/12 ,  C07D417/14 ,  C07D487/08

摘要： Compounds of the invention, such as compounds of Formulae IIa, IIb, IIc or IId, and pharmaceutically acceptable salts, isomers, and prodrugs thereof, are useful as modulators of the activity of liver X receptors, where R1, R2, R21, R3 and G are defined herein. Pharmaceutical compositions containing the compounds and methods of using the compounds are also disclosed.

公开(公告)号：EP1844020A1

公开(公告)日：2007-10-17

申请号：EP06717506.7

申请日：2006-01-06

申请人： Exelixis, Inc.

发明人： FLATT, Brenton ,  GU, Xiao-Hui ,  MARTIN, Richard ,  MOHAN, Raju ,  MURPHY, Brett ,  NYMAN, Michael, C. ,  STEVENS, William, C. Jr. ,  WANG, Tie-Lin

IPC分类号： C07D233/90 ,  C07D231/14 ,  C07D333/38 ,  C07D307/68 ,  A61K31/4164 ,  A61K31/415 ,  A61K31/381 ,  A61K31/341 ,  A61P35/00

CPC分类号： C07D231/14 ,  C07D233/90 ,  C07D307/68 ,  C07D333/38

摘要： Heterocyclic carboxamide compounds are described herein as being useful in modulating the activity of steroid nuclear receptors. Pharmaceutical compositions containing the compounds, methods of using the compounds and processes for making the compounds are also described.

摘要翻译： 杂环羧酰胺化合物在本文中被描述为可用于调节类固醇核受体的活性。 还描述了含有化合物的药物组合物，使用该化合物的方法和制备该化合物的方法。

公开(公告)号：EP1844020B1

公开(公告)日：2017-09-06

申请号：EP06717506.7

申请日：2006-01-06

申请人： Exelixis, Inc.

发明人： FLATT, Brenton ,  GU, Xiao-Hui ,  MARTIN, Richard ,  MOHAN, Raju ,  MURPHY, Brett ,  NYMAN, Michael, C. ,  STEVENS, William, C. Jr. ,  WANG, Tie-Lin

IPC分类号： C07D233/90 ,  C07D231/14 ,  C07D333/38 ,  C07D307/68 ,  A61K31/4164 ,  A61K31/415 ,  A61K31/381 ,  A61K31/341 ,  A61P35/00

CPC分类号： C07D231/14 ,  C07D233/90 ,  C07D307/68 ,  C07D333/38

公开(公告)号：EP1532153B8

公开(公告)日：2012-04-11

申请号：EP03755523.2

申请日：2003-05-27

申请人： Exelixis, Inc.

发明人： MARTIN, Richard ,  WANG, Tie-Lin ,  FLATT, Brenton, Todd ,  GU, Xiao-Hui ,  GRIFFITH, Ronald

IPC分类号： C07D487/04 ,  C07D471/04 ,  A61K31/435 ,  A61P31/04 ,  A61P31/10 ,  A61K31/55 ,  C07D223/00 ,  C07D209/00 ,  C07D221/00

CPC分类号： C07D471/04 ,  C07D487/10 ,  C07D491/04

摘要： The present invention is directed to compounds of formula (I) and formula (II): formula (I) and (II), wherein R1-R8, A and n are as described in the description. These compounds are used in pharmaceutical compositions and methods for modulating the activity of orphan nuclear receptors.