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：EP2079729A1

公开(公告)日：2009-07-22

申请号：EP07844851.1

申请日：2007-11-02

申请人： IRM LLC ,  NOVARTIS AG

发明人： CHIANELLI, Donatella ,  LI, Xiaolin ,  LIU, Xiaodong ,  LOREN, Jon ,  MOLTENI, Valentina ,  NABAKKA, Juliet ,  REVESZ, Laszlo ,  PEREZ, Lawrence B. ,  BROOKS, Clinton ,  WRONA, Wojciech ,  MANLEY, Paul W. ,  BREITENSTEIN, Werner

IPC分类号： C07D401/14 ,  C07D403/12 ,  C07D405/14 ,  C07D407/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  A61K31/506 ,  A61P33/06 ,  A61P25/00 ,  A61P35/00

CPC分类号： C07D401/14 ,  C07D401/04 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14

摘要： The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to beat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of c-kit, PDGFRα and PDGFRβ kinases. Formula (I).

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这些化合物来击败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c-kit，PDGFRα和PDGFRα异常活化的疾病或病症 PDGFRβ激酶。 公式（I）。

公开(公告)号：EP2152688A1

公开(公告)日：2010-02-17

申请号：EP08747596.8

申请日：2008-05-02

申请人： IRM LLC ,  Novartis AG ,  Li, Xiaolin ,  Liu, Xiaodong ,  Molteni, Valentina ,  Chianelli, Donatella ,  Loren, Jon ,  Nabakka, Juliet

发明人： LI, Xiaolin ,  LIU, Xiaodong ,  MOLTENI, Valentina ,  CHIANELLI, Donatella ,  LOREN, Jon ,  NABAKKA, Juliet ,  RAMSEY, Timothy ,  BREITENSTEIN, Werner

IPC分类号： C07D401/04 ,  C07D417/14 ,  A61K31/506 ,  A61P35/00 ,  A61P37/00

CPC分类号： C07D401/04 ,  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 c-kit, PDGFR and PDGFR 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c-kit，PDGFR和PDGFR异常活化的疾病或病症的方法 PDGFR激酶。

公开(公告)号：EP1948636A2

公开(公告)日：2008-07-30

申请号：EP06849884.9

申请日：2006-11-14

申请人： IRM LLC ,  Novartis AG

发明人： MOLTENI, Valentina ,  ELLIS, David A. ,  NABAKKA, Juliet ,  CHIANELLI, Donatella ,  SAEZ, Enrique ,  LI, Xiaolin ,  CHAMOIN, Sylvie ,  ROTH, Hans-Jorg

IPC分类号： C07D401/10 ,  A61K31/4545 ,  A61P9/00 ,  A61P29/00 ,  A61P3/10

CPC分类号： C07D401/10

摘要： The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of liver X receptors (LXRs).

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：EP2252612B1

公开(公告)日：2012-03-28

申请号：EP09711557.0

申请日：2009-02-20

申请人： IRM LLC

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

IPC分类号： C07D471/04 ,  A61K31/4375 ,  A61P29/00 ,  A61P35/00 ,  A61P37/00 ,  A61P25/00 ,  A61P9/00

CPC分类号： C07D471/04

摘要： The invention provides a novel class of compounds of Formula I: (I) pharmaceutical compositions comprising 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 c-kit, PDGFRα and PDGFRβ kinases.

公开(公告)号：EP2655370A1

公开(公告)日：2013-10-30

申请号：EP11796872.7

申请日：2011-11-30

申请人： IRM LLC

发明人： TULLY, David C. ,  RUCKER, Paul Vincent ,  ALPER, Phillip B. ,  MUTNICK, Daniel ,  CHIANELLI, Donatella

IPC分类号： C07D451/06 ,  A61K31/46 ,  A61P3/00 ,  C07D471/04 ,  C07D487/04

CPC分类号： A61K31/46 ,  A61K31/4709 ,  A61K31/497 ,  A61K31/501 ,  A61K31/5025 ,  A61K31/506 ,  A61K31/706 ,  A61K45/06 ,  C07D451/06 ,  C07D471/04 ,  C07D487/04 ,  C07D519/00 ,  C07H17/00

摘要： The present invention relates to compounds of Formula (I), a stereoisomer, enantiomer, a pharmaceutically acceptable salt or an amino acid conjugate thereof; wherein variables are as defined herein; and their pharmaceutical compositions, which are useful as modulators of the activity of Farnesiod X receptors (FXR).

摘要翻译： 本发明涉及式（I）的化合物，其立体异构体，对映异构体，其药学上可接受的盐或氨基酸缀合物; 其中变量如本文所定义; 及其药物组合物，其可用作Farnesiod X受体（FXR）活性的调节剂。

公开(公告)号：EP2655369A1

公开(公告)日：2013-10-30

申请号：EP11796873.5

申请日：2011-11-30

申请人： IRM LLC

发明人： TULLY, David C. ,  CHIANELLI, Donatella

IPC分类号： C07D413/12 ,  C07D413/14 ,  A61K31/422

CPC分类号： C07D413/14 ,  A61K31/454 ,  A61K31/4545 ,  A61K45/06 ,  C07D413/12

摘要： The present invention relates to compounds of Formula I, a stereoisomer, enantiomer, a pharmaceutically acceptable salt or an amino acid conjugate thereof; wherein variables are as defined herein; and their pharmaceutical compositions, which are useful as modulators of the activity of Farnesiod X receptors (FXR).

公开(公告)号：EP1979355B1

公开(公告)日：2010-08-18

申请号：EP07717085.0

申请日：2007-01-25

申请人： IRM LLC

发明人： EPPLE, Robert ,  RUSSO, Ross ,  AZIMIOARA, Mihai ,  COW, Christopher ,  MOLTENI, Valentina ,  LI, Xiaolin ,  CHIANELLI, Donatella

IPC分类号： C07D471/10 ,  A61K31/435 ,  A61P3/00 ,  A61P9/00 ,  A61P11/00

CPC分类号： C07D471/10

摘要： The invention provides compounds (Ia), (Ib) and (Ic), pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of the Peroxisome Proliferator-Activated Receptor (PPAR) families.

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.