公开(公告)号：EP3953351A1

公开(公告)日：2022-02-16

申请号：EP20722870.1

申请日：2020-04-08

申请人： Plexxikon Inc.

发明人： SPEVAK, Wayne ,  BUELL, John ,  GUO, Zuojun ,  INAGAKI, Hiroaki ,  JIN, Yongil ,  PHAM, Phuongly ,  SHI, Songyuan ,  WALLESHAUSER, Jack ,  WU, Jeffrey ,  WU, Guoxian ,  ZHANG, Chao ,  ZHANG, Jiazhong ,  ZHANG, Ying

IPC分类号： C07D471/04 ,  A61K31/437 ,  A61P35/00

公开(公告)号：EP3004060B1

公开(公告)日：2019-11-27

申请号：EP14733877.6

申请日：2014-05-29

申请人： PLEXXIKON INC.

发明人： ZHANG, Chao ,  HIRTH, Klaus-Peter ,  IBRAHIM, Prabha N. ,  NESPI, Marika ,  SHI, Songyuan ,  SPEVAK, Wayne ,  HABETS, Gaston G. ,  BURTON, Elizabeth, A.

IPC分类号： C07D213/75 ,  C07D417/04 ,  C07D471/04 ,  C07D487/04 ,  A61K31/519

公开(公告)号：EP2516438A2

公开(公告)日：2012-10-31

申请号：EP10840075.5

申请日：2010-12-21

申请人： Plexxikon, Inc.

发明人： IBRAHIM, Prabha N. ,  WU, Guoxian ,  LIN, Jack ,  SPEVAK, Wayne ,  CHO, Hanna ,  EWING, Todd ,  ZHANG, Chao

IPC分类号： C07D471/04 ,  A61K31/437 ,  A61P35/00

CPC分类号： C07D471/04 ,  A61K31/437 ,  A61K31/497 ,  A61K31/498 ,  A61K31/506 ,  A61K31/519 ,  C07D519/00

摘要： Compounds and salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof and uses thereof are described. In certain aspects and embodiments, the described compounds or salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof are active on each of B-Raf, B-Raf V600E and c-Raf-1 protein kinase. In certain aspects and embodiments, the described compounds are active in inhibiting proliferation of a Ras mutant cell line. Also described are methods of use thereof to treat diseases and conditions, including melanoma, glioma, glioblastoma, pilocytic astrocytoma, liver cancer, biliary tract cancer, cholangiocarcinoma, colorectal cancer, lung cancer, bladder cancer, gallbladder cancer, breast cancer, pancreatic cancer, thyroid cancer, kidney cancer, ovarian cancer, adrenocortical cancer, prostate cancer, gastrointestinal stromal tumors, medullary thyroid cancer, tumor angiogenesis, acute myeloid leukemia, chronic myelomonocytic leukemia, childhood acute lymphoblastic leukemia, plasma cell leukemia, and multiple myeloma.

公开(公告)号：EP1943245A2

公开(公告)日：2008-07-16

申请号：EP06803059.2

申请日：2006-09-06

申请人： PLEXXIKON, INC.

发明人： LIN, Jack ,  WOMACK, Patrick ,  LEE, Byunghun ,  SHI, Shenghua ,  ZHANG, Chao ,  ZUCKERMAN, Rebecca ,  ARTIS, Dean R. ,  IBRAHIM, Prabha N. ,  WANG, Weiru

IPC分类号： C07D409/14 ,  C07D413/14 ,  A61K31/405 ,  A61P3/10

CPC分类号： C07D409/14 ,  C07D209/18 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/04 ,  C07D409/12 ,  C07D413/06 ,  C07D413/12 ,  C07D413/14 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14 ,  C07D491/04

摘要： Compounds are described that are active on PPARs, including pan-active compounds and compounds selective for any one or any two of PPARα, PPARϜ and PPARδ. Also describe are methods of use of the compounds in treating various diseases.

公开(公告)号：EP1885723A2

公开(公告)日：2008-02-13

申请号：EP06813186.1

申请日：2006-05-16

申请人： PLEXXIKON, INC.

发明人： ZHANG, Chao ,  ZHANG, Jiazhong ,  IBRAHIM, Prabha, N. ,  HURT, Clarence, R. ,  ZUCKERMAN, Rebecca ,  ARTIS, Dean, R. ,  BREMER, Ryan ,  SPEVAK, Wayne ,  WU, Guoxian ,  ZHU, Hongyao

IPC分类号： C07D471/04 ,  A61K31/435 ,  A61P35/00

CPC分类号： C07D471/04

摘要： Compounds active on the receptor protein tyrosine kinases c-kit and c-fms are provided herewith. Also provided herewith are compositions useful for treatment of c-kit mediated diseases or condition and c-fms-mediated diseases or condition, and methods for the use thereof.

公开(公告)号：EP1742627A2

公开(公告)日：2007-01-17

申请号：EP05856703.3

申请日：2005-05-06

申请人： PLEXXIKON, INC.

发明人： CHO, Hanna ,  ENGLAND, Bruce ,  GILLETTE, Sam ,  IBRAHIM, Prabha, L. ,  ARTIS, Dean, R. ,  ZUCKERMAN, Rebecca, L. ,  ZHANG, Chao

IPC分类号： A61K31/4025 ,  A61K31/401 ,  A61K31/381 ,  A61K31/34 ,  C07D409/02 ,  C07D403/02

CPC分类号： C07C311/48 ,  C07D215/36 ,  C07D215/40 ,  C07D231/12 ,  C07D239/18 ,  C07D239/46 ,  C07D275/04 ,  C07D277/42 ,  C07D277/62 ,  C07D333/36 ,  C07D333/38 ,  C07D333/40 ,  C07D401/12 ,  C07D405/06 ,  C07D405/14 ,  C07D409/04 ,  C07D409/06 ,  C07D409/12 ,  C07D409/14 ,  C07D413/06 ,  C07D413/12 ,  C07D413/14 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04

摘要： Compounds active on phosphodiesterase PDE4B are provided. Also provided herewith are compositions useful for treatment of PDE4B-mediated diseases or conditions, and methods for the use thereof.

公开(公告)号：EP1696920B1

公开(公告)日：2014-10-29

申请号：EP04814626.0

申请日：2004-12-17

申请人： PLEXXIKON INC.

发明人： IBRAHIM, Prabha ,  WEST, Brian ,  KUMAR, Abhinav ,  KRUPKA, Helke ,  ZUCKERMAN, Rebecca ,  ZHU, Yong ,  ZHANG, Jiazhong ,  ZHANG, Chao ,  NESPI, Marika ,  MAMO, Shumeye ,  HURT, Clarence, R. ,  HABETS, Gaston ,  BREMER, Ryan ,  ARTIS, Richard, Dean

IPC分类号： A61K31/44 ,  C07D471/04

CPC分类号： C07D471/04

公开(公告)号：EP2170830B1

公开(公告)日：2014-10-15

申请号：EP08781880.3

申请日：2008-07-16

申请人： PLEXXIKON, INC.

发明人： WU, Guoxian ,  ZHANG, Jiazhong ,  ZHU, Yong-Liang ,  ZHANG, Chao ,  IBRAHIM, Prabha, N. ,  SHI, Songyuan ,  SPEVAK, Wayne ,  ARTIS, Dean, R. ,  TSAI, James

IPC分类号： C07D213/75 ,  C07D215/12 ,  C07D215/20 ,  C07D239/48 ,  C07D263/48 ,  C07D417/12 ,  C07D215/38 ,  C07D471/04 ,  C07D213/82 ,  A61P35/00

CPC分类号： A61K31/44 ,  A61K31/415 ,  A61K31/42 ,  A61K31/433 ,  A61K31/437 ,  A61K31/4436 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/47 ,  A61K31/505 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/549 ,  A61K45/06 ,  C07D213/74 ,  C07D213/75 ,  C07D213/76 ,  C07D213/82 ,  C07D215/12 ,  C07D215/14 ,  C07D215/20 ,  C07D215/38 ,  C07D231/40 ,  C07D239/48 ,  C07D239/49 ,  C07D261/14 ,  C07D263/48 ,  C07D285/135 ,  C07D285/16 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/04 ,  C07D417/12 ,  C07D471/04 ,  A61K31/4427 ,  A61K2300/00

摘要： Compounds of formula I active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases. Formula (I) wherein Ar is optionally substituted heteroaryl; R2 is hydrogen, lower alkyl or halogen; U is selected from the group consisting of —S(O)2—, —C(X)—, —C(X)—N(R10)—, and —S(O)2—N(R10)—; R3 is optionally substituted lower alkyl, optionally substituted C3.6 cycloalkyl, optionally substituted heterocycloalkyl, optionally substituted aryl or optionally substituted heteroaryl; and wherein R1, R3, R4, m, L1, X R10 are as described herein.

公开(公告)号：EP1648867B1

公开(公告)日：2013-09-04

申请号：EP04778641.3

申请日：2004-07-16

申请人： PLEXXIKON INC.

发明人： ARNOLD, James ,  ARTIS, Dean, R. ,  HURT, Clarence ,  IBRAHIM, Prabha, N. ,  KRUPKA, Heike ,  LIN, Jack ,  MILBURN, Michael, V. ,  WANG, Weiru ,  ZHANG, Chao

IPC分类号： C07D209/08 ,  C07D209/12 ,  C07D209/18 ,  C07D209/22 ,  C07D209/26 ,  C04B35/632 ,  C07D231/56 ,  C07D401/04 ,  C07D401/12 ,  C07D405/12 ,  C07D409/04 ,  C07D409/12 ,  C07D471/04 ,  C07D487/04

CPC分类号： C07D471/04 ,  C04B35/632 ,  C07D209/08 ,  C07D209/12 ,  C07D209/18 ,  C07D209/22 ,  C07D209/26 ,  C07D231/56 ,  C07D401/04 ,  C07D401/12 ,  C07D405/12 ,  C07D409/04 ,  C07D409/12 ,  C07D487/04

摘要： Compounds are described that are active on PPARs, including pan-active compounds. Also described are methods for developing or identifying compounds having a desired selectivity profile.

公开(公告)号：EP2094701A2

公开(公告)日：2009-09-02

申请号：EP07871726.1

申请日：2007-12-20

申请人： PLEXXIKON, INC.

发明人： IBRAHIM, Prabha N. ,  BREMER, Ryan ,  ZHANG, Chao ,  ZHANG, Jiazhong ,  HIRTH, Klaus-Peter ,  WU, Guoxian ,  ZHU, Hongyao

IPC分类号： C07D471/04 ,  A61K31/437 ,  A61P25/00 ,  A61P29/00 ,  A61P35/00

CPC分类号： C07D471/04

摘要： Compounds according to formulae IIa, IIIa, IIIc and IVb active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases.