公开(公告)号：EP2018167A2

公开(公告)日：2009-01-28

申请号：EP07755084.6

申请日：2007-04-06

申请人： IRM LLC

发明人： REN, Pingda ,  ZHANG, Guobao ,  YOU, Shuli ,  SIM, Taebo ,  GRAY, Nathanael ,  XIE, Yongping ,  WANG, Xing ,  HE, Yun

IPC分类号： A61K31/519

CPC分类号： C07D487/04 ,  C07D471/04

摘要： Described are compounds, pharmaceutical compositions comprising such compounds, and methods of using such compounds to treat or prevent disease or disordered associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activity of kinases such as AbI, ALK, AMPK, Aurora, AxI, Bcr-Abl, BIK, Bmx, BRK, BTK, c-Kit, CSK, cSrc, CDKl, CHK2, CKl, CK2, CaMKII, CaMKIV, DYRK2, EGFR, EphBl, FES, FGFRl, FGFR2, FGFR3, Fltl, FlO, FMS, Fyn, GSK3β, IGF lR, IKKα DCKβ, IR, IRAK4, ITK, JAK2, JAK3, JNKlαl, JNK2α, KDR, Lck, LYN, MAPKl, MAPKAP-K2, MEKl, MET, MKK4, MKK6, MST2, NEK2, NLK, p70S6K, PAK2, PDGFR, PDGFRα, PDKl, Pim-2, Plk3, PKA, PKBα, PKCα PKCtheta, PKD2, c-Raf, RET, ROCK-I1 ROCK-II, Ron, Ros, Rskl, SAPK2a, SAPK2b, SAPK3, SAPK4, SGK, SIK, Syk, Tie2, TrkB, WNK3, and ZAP-70.

公开(公告)号：EP1758892A1

公开(公告)日：2007-03-07

申请号：EP05759571.2

申请日：2005-06-09

申请人： IRM LLC

发明人： REN, Pingda ,  WANG, Xia ,  ZHANG, Guobao ,  DING, Qiang ,  YOU, Shuli ,  ZHANG, Qiong ,  CHOPIUK, Greg ,  ALBAUGH, Pamela A. ,  SIM, Taebo ,  GRAY, Nathanael Schiander

IPC分类号： C07D403/04 ,  A61K31/4178

CPC分类号： C07D403/04 ,  C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  C07D417/14

摘要： The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the Abl, BCR-Abl, PDGF-R, trkB, c-SRC, BMX, FGFR3, b-RAF, SGK, Tie2, Lck, JNK2 2, MKK4, c-RAF, MKK6, SAPK2 and SAPK2 kinases.

公开(公告)号：EP2190825B1

公开(公告)日：2014-04-09

申请号：EP08798168.4

申请日：2008-08-19

申请人： IRM LLC

发明人： MOLTENI, Valentina ,  LI, Xiaolin ,  LIU, Xiaodong ,  CHIANELLI, Donatella ,  NABAKKA, Juliet ,  LOREN, Jon ,  YOU, Shuli

IPC分类号： C07D239/42 ,  C07D401/12 ,  C07D403/12 ,  C07D413/12 ,  A61K31/505 ,  A61K31/506 ,  A61P1/00 ,  A61P7/04 ,  A61P11/06

CPC分类号： C07D239/42 ,  C07D401/12 ,  C07D403/12 ,  C07D413/12

公开(公告)号：EP1891066B1

公开(公告)日：2010-12-22

申请号：EP06752481.9

申请日：2006-05-10

申请人： IRM, LLC

发明人： NAGLE, Advait ,  GRAY, Nathanael, Schiander ,  LIU, Yi ,  REN, Pingda ,  SIM, Taebo ,  YOU, Shuli

IPC分类号： C07D471/04 ,  A61K31/519 ,  A61P29/00 ,  A61P35/00

CPC分类号： C07D471/04

摘要： The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of Abl, Bcr-Abl, Bmx, BTK, b-RAF, c RAF, CSK, cSRC, Fes, FGFR3, Flt3, IKKα, IKKβ, JNK1α1, JNK2α2, Lck, Met, MKK4, MKK6, p70S6K, PAK2, PDGFRα, PKA, PKCα, PKD2, ROCK-II, Ros, Rsk1, SAPK2α, SAPK2β, SAPK3, SAPK4, SGK, Syk, Tie2 and TrkB kinases.

公开(公告)号：EP1928236A2

公开(公告)日：2008-06-11

申请号：EP06815653.8

申请日：2006-09-26

申请人： IRM, LLC ,  Novartis AG

发明人： MOLTENI, Valentina ,  LI, Xiaolin ,  CHIANELLI, Donatella ,  LOREN, Jon ,  LIU, Yi ,  KARANEWSKY, Donald, S. ,  FURET, Pascal ,  GUAGNANO, Vito ,  YOU, Shuli ,  NABAKKA, Juliet ,  LIU, Xiaodong ,  PAN, Shifeng

IPC分类号： A01N43/42 ,  A61K31/44

CPC分类号： C07D403/04 ,  C07D239/42 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/04 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D491/10

摘要： Described herein are compounds that include a diarylamine structural feature. Also described herein are methods for making such compounds, methods for using such compounds to modulate the activity of c-kit receptors, and pharmaceutical compositions and medicaments comprising such compounds. Also described herein are methods of using such compounds, pharmaceutical compositions and medicaments to treat and/or prevent and/or inhibit and/or ameliorate the pathology and/or symptomology diseases or conditions associated with the activity of c-kit receptors.

公开(公告)号：EP1928236B1

公开(公告)日：2011-11-23

申请号：EP06815653.8

申请日：2006-09-26

申请人： IRM LLC ,  Novartis AG

发明人： MOLTENI, Valentina ,  LI, Xiaolin ,  CHIANELLI, Donatella ,  LOREN, Jon ,  LIU, Yi ,  KARANEWSKY, Donald, S. ,  FURET, Pascal ,  GUAGNANO, Vito ,  YOU, Shuli ,  NABAKKA, Juliet ,  LIU, Xiaodong ,  PAN, Shifeng

IPC分类号： A01N43/42 ,  A61K31/44

CPC分类号： C07D403/04 ,  C07D239/42 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/04 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D491/10

摘要： Described herein are compounds that include a diarylamine structural feature. Also described herein are methods for making such compounds, methods for using such compounds to modulate the activity of c-kit receptors, and pharmaceutical compositions and medicaments comprising such compounds. Also described herein are methods of using such compounds, pharmaceutical compositions and medicaments to treat and/or prevent and/or inhibit and/or ameliorate the pathology and/or symptomology diseases or conditions associated with the activity of c-kit receptors.

公开(公告)号：EP2076513A1

公开(公告)日：2009-07-08

申请号：EP07844322.3

申请日：2007-10-16

申请人： IRM LLC

发明人： CHIANELLI, Donatella ,  COW, Christopher ,  HE, Yun ,  JIANG, Songchun ,  LI, Xiaolin ,  LIU, Xiaodong ,  LIU, Zuosheng ,  LOREN, Jon ,  MOLTENI, Valentina ,  NABAKKA, Juliet ,  REN, Pingda ,  SIM, Taebo ,  WANG, Xiaodong ,  YOU, Shuli

IPC分类号： C07D471/04

CPC分类号： C07D471/04

摘要： The invention provides compounds and pharmaceutical compositions thereof, which are useful as protein kinase inhibitors, as well as methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated kinase activity. In some embodiments, the invention provides methods for using such compounds to treat, ameliorate or prevent diseases or disorders that involve abnormal activation of c-kit, PDGFR , PDGFR , CSF1R, Abl, BCR-Abl, CSK, JNK1, JNK2, p38, p70S6K, TGF , SRC, EGFR, trkB, FGFR3, FLT3, Fes, Lck, Syk, RAF, MKK4, MKK6, SAPK2 , BRK, KDR, c-raf or b-raf kinase, or mutant forms thereof.

公开(公告)号：EP1891066A2

公开(公告)日：2008-02-27

申请号：EP06752481.9

申请日：2006-05-10

申请人： IRM, LLC

发明人： NAGLE, Advait ,  GRAY, Nathanael, Schiander ,  LIU, Yi ,  REN, Pingda ,  SIM, Taebo ,  YOU, Shuli

IPC分类号： C07D471/04 ,  A61K31/519 ,  A61P29/00 ,  A61P35/00

CPC分类号： C07D471/04

摘要： The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of Abl, Bcr-Abl, Bmx, BTK, b-RAF, c RAF, CSK, cSRC, Fes, FGFR3, Flt3, IKKα, IKKβ, JNK1α1, JNK2α2, Lck, Met, MKK4, MKK6, p70S6K, PAK2, PDGFRα, PKA, PKCα, PKD2, ROCK-II, Ros, Rsk1, SAPK2α, SAPK2β, SAPK3, SAPK4, SGK, Syk, Tie2 and TrkB kinases.

摘要翻译： 本发明提供了一类新化合物，包含此类化合物的药物组合物以及使用此类化合物治疗或预防与异常或失调的激酶活性相关的疾病或病症，特别是涉及Abl，Bcr-Abl， Bmx，BTK，b-RAF，c RAF，CSK，cSRC，Fes，FGFR3，Flt3，IKKα，IKKβ，JNK1α1，JNK2α2，Lck，Met，MKK4，MKK6，p70S6K，PAK2，PDGFRα，PKA，PKCα，PKD2，ROCK -II，Ros，Rsk1，SAPK2α，SAPK2β，SAPK3，SAPK4，SGK，Syk，Tie2和TrkB激酶。

公开(公告)号：EP1841431A2

公开(公告)日：2007-10-10

申请号：EP06733803.8

申请日：2006-01-19

申请人： IRM, LLC

发明人： SIM, Taebo ,  GRAY, Nathanael Schiander ,  LEE, Hyun Soo ,  LIU, Yi ,  REN, Pingda ,  YOU, Shuli ,  ZHANG, Qiong ,  DING, Qiang ,  WANG, Xia ,  JIANG, Songchun ,  ALBAUGH, Pamela A.

IPC分类号： A61K31/5377

CPC分类号： C07D277/56 ,  C07D417/12 ,  C07D417/14

摘要： The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the Abl, Bcr-Abl, FGFR3, PDGFRβ and b-Raf kinases.

摘要翻译： 本发明提供了一类新化合物，包含此类化合物的药物组合物以及使用此类化合物治疗或预防与异常或失调的激酶活性有关的疾病或病症，特别是涉及Abl，Bcr-Abl异常活化的疾病或病症的方法 ，FGFR3，PDGFRβ和b-Raf激酶。

公开(公告)号：EP1758892B1

公开(公告)日：2012-10-17

申请号：EP05759571.2

申请日：2005-06-09

申请人： IRM LLC

发明人： REN, Pingda ,  WANG, Xia ,  ZHANG, Guobao ,  DING, Qiang ,  YOU, Shuli ,  ZHANG, Qiong ,  CHOPIUK, Greg ,  ALBAUGH, Pamela A. ,  SIM, Taebo ,  GRAY, Nathanael Schiander

IPC分类号： C07D403/04 ,  A61K31/4178

CPC分类号： C07D403/04 ,  C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  C07D417/14