公开(公告)号：EP1660458A1

公开(公告)日：2006-05-31

申请号：EP04764093.3

申请日：2004-08-13

申请人： Novartis AG ,  Novartis Pharma GmbH ,  IRM LLC

发明人： GARCIA-ECHEVERRIA, Carlos ,  KANAZAWA, Takanori ,  KAWAHARA, Eiji ,  MASUYA, Keiichi ,  MATSUURA, Naoko ,  MIYAKE, Takahiro ,  OHMORI, Osamu ,  UMEMURA, Ichiro ,  STEENSMA, Ruo ,  CHOPIUK, Greg ,  JIANG, Jiqing ,  WAN, Yongqin ,  DING, Qiang ,  ZHANG, Qiong ,  GRAY, Nathanael, Schiander ,  KARANEWSKY, Donald

IPC分类号： C07D239/48 ,  C07D405/12 ,  C07D403/12 ,  C07D401/12 ,  C07D401/14 ,  A61K31/506 ,  A61K35/00 ,  A61P37/00 ,  A61P29/00

CPC分类号： C07D239/48 ,  C04B35/632 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14

摘要： Novel pyrimidine derivatives of formula (I) Wherein R is selected from C16-10 aryl, C5-10heteroaryl, C3-12cycloalkyl and C3-10heterocycloalkyl; R0-R6 as described herein; and their use for the manufacture of a medicament for the treatment or prevention of a disease wich responds to inhibition of FAK and/or ALK and/or ZAP-70 and/or IGF-IR.

公开(公告)号：EP1660458B1

公开(公告)日：2012-01-25

申请号：EP04764093.3

申请日：2004-08-13

申请人： Novartis AG ,  IRM LLC

发明人： GARCIA-ECHEVERRIA, Carlos ,  KANAZAWA, Takanori ,  KAWAHARA, Eiji ,  MASUYA, Keiichi ,  MATSUURA, Naoko ,  MIYAKE, Takahiro ,  OHMORI, Osamu ,  UMEMURA, Ichiro ,  STEENSMA, Ruo ,  CHOPIUK, Greg ,  JIANG, Jiqing ,  WAN, Yongqin ,  DING, Qiang ,  ZHANG, Qiong ,  GRAY, Nathanael, Schiander ,  KARANEWSKY, Donald

IPC分类号： C07D239/48 ,  C07D405/12 ,  C07D403/12 ,  C07D401/12 ,  C07D401/14 ,  A61K31/506 ,  A61K35/00 ,  A61P37/00 ,  A61P29/00

CPC分类号： C07D239/48 ,  C04B35/632 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14

摘要： Novel pyrimidine derivatives of formula (I) Wherein R is selected from C16-10 aryl, C5-10heteroaryl, C3-12cycloalkyl and C3-10heterocycloalkyl; R0-R6 as described herein; and their use for the manufacture of a medicament for the treatment or prevention of a disease wich responds to inhibition of FAK and/or ALK and/or ZAP-70 and/or IGF-IR.

公开(公告)号：EP1761505B1

公开(公告)日：2011-08-17

申请号：EP05756693.7

申请日：2005-06-23

申请人： Novartis AG ,  IRM LLC

发明人： DING, Qiang ,  GRAY, Nathanael, Schiander ,  LI, Bing ,  LIU, Yi ,  SIM, Taebo ,  UNO, Tetsuo ,  ZHANG, Guobao ,  PISSOT SOLDERMANN, Carole ,  BREITENSTEIN, Werner ,  BOLD, Guido ,  CARAVATTI, Giorgio ,  FURET, Pascal ,  GUAGNANO, Vito ,  LANG, Marc ,  MANLEY, Paul, W. ,  SCHOEPFER, Joseph ,  SPANKA, Carsten

IPC分类号： C07D239/48 ,  C07D409/12 ,  C07D401/12 ,  C07D405/12 ,  C07D403/12 ,  A61K31/505 ,  A61K31/506 ,  C07D251/48 ,  A61P35/00

CPC分类号： C07D239/48 ,  C07D251/48 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12

摘要： The invention relates to compounds of formula (I) wherein the substituents X1, R1, R2, R3 and R4 have the meaning as set forth and explained in the description of the invention, to processes for the preparation of these compounds, pharmaceutical compositions containing same, the use thereof optionally in combination with one or more other pharmaceutically active compounds for the therapy of a disease which responds to an inhibition of protein kinase activity, and a method for the treatment of such a disease.

公开(公告)号：EP1761505A1

公开(公告)日：2007-03-14

申请号：EP05756693.7

申请日：2005-06-23

申请人： Novartis AG ,  NOVARTIS-PHARMA GMBH ,  IRM LLC

发明人： DING, Qiang ,  GRAY, Nathanael, Schiander ,  LI, Bing ,  LIU, Yi ,  SIM, Taebo ,  UNO, Tetsuo ,  ZHANG, Guobao ,  PISSOT SOLDERMANN, Carole ,  BREITENSTEIN, Werner ,  BOLD, Guido ,  CARAVATTI, Giorgio ,  FURET, Pascal ,  GUAGNANO, Vito ,  LANG, Marc ,  MANLEY, Paul, W. ,  SCHOEPFER, Joseph ,  SPANKA, Carsten

IPC分类号： C07D239/48 ,  C07D409/12 ,  C07D401/12 ,  C07D405/12 ,  C07D403/12 ,  A61K31/505 ,  A61K31/506 ,  C07D251/48 ,  A61P35/00

CPC分类号： C07D239/48 ,  C07D251/48 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12

摘要： The invention relates to compounds of formula (I) wherein the substituents X1, R1, R2, R3 and R4 have the meaning as set forth and explained in the description of the invention, to processes for the preparation of these compounds, pharmaceutical compositions containing same, the use thereof optionally in combination with one or more other pharmaceutically active compounds for the therapy of a disease which responds to an inhibition of protein kinase activity, and a method for the treatment of such a disease.

公开(公告)号：EP2057146A1

公开(公告)日：2009-05-13

申请号：EP07814982.0

申请日：2007-09-24

申请人： IRM LLC ,  NOVARTIS AG

发明人： ALBAUGH, Pamela ,  CHOPIUK, Gregory S. ,  DING, Qiang ,  HUANG, Shenlin ,  LIU, Zuosheng ,  PAN, Shifeng ,  REN, Pingda ,  WANG, Xia ,  WANG, Xing ,  XIE, Yongping ,  ZHANG, Chengzhi ,  ZHANG, Qiong ,  ZHANG, Guobao ,  POON, Daniel ,  RENHOWE, Paul ,  SENDZIK, Martin

IPC分类号： C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D417/14 ,  A61K31/506 ,  A61P35/00

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, ARG, BCR-Abl, BRK, EphB, Fms, Fyn, KDR, c-Kit, LCK, PDGF-R, b-Raf, c-Raf, SAPK2, Src, Tie2 and TrkB kinases.

摘要翻译： 本发明提供了一类新颖的化合物，包含这些化合物的药物组合物和使用这些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的方法，特别是涉及Abl，ARG，BCR异常活化的疾病或病症 -Abl，BRK，EphB，Fms，Fyn，KDR，c-Kit，LCK，PDGF-R，b-Raf，c-Raf，SAPK2，Src，Tie2和TrkB激酶。

公开(公告)号：EP1656378A2

公开(公告)日：2006-05-17

申请号：EP04781114.6

申请日：2004-08-13

申请人： IRM LLC

发明人： CHENG, Dai ,  DING, Qiang ,  HAN, Dong ,  GRAY, Nathanael Schiander ,  ZHANG, Guobao

IPC分类号： C07D473/40 ,  C07D473/34 ,  C07D473/18 ,  C07D473/16 ,  A61K31/52 ,  A61K31/522 ,  A61P35/02 ,  A61P35/00 ,  A61P9/10 ,  A61P17/06 ,  A61P11/06

CPC分类号： C07D473/16 ,  C07D473/18 ,  C07D473/34 ,  C07D473/40

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 cSRC, Lck, FGFR3, Flt3, TrkB, Bmx, and/or PFGFRα kinase activity.

公开(公告)号：EP2459558A2

公开(公告)日：2012-06-06

申请号：EP10747541.0

申请日：2010-07-30

申请人： IRM LLC

发明人： CHE, Jianwei ,  DING, Qiang ,  HE, Xiaohui ,  LIU, Hong ,  LIU, Yahua ,  MICHELLYS, Pierre-Yves ,  OKRAM, Barun ,  WU, Xu ,  YANG, Kunyong ,  ZHU, Xuefeng

IPC分类号： C07D471/04

CPC分类号： C07D471/04

摘要： Provided herein area 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 Syk kinase activity.

公开(公告)号：EP2250169A1

公开(公告)日：2010-11-17

申请号：EP09708389.3

申请日：2009-01-27

申请人： IRM LLC

发明人： DING, Qiang ,  LIU, Yahua ,  WU, Xu ,  JIN, Qihui ,  CHE, Jianwei ,  YAN, S. Frank

IPC分类号： C07D471/04 ,  A61K31/519

CPC分类号： C07D471/04

摘要： The invention provides a class of compounds of Formula (I), 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 Syk, ZAP70, KDR, FMS, FLT3, c-Kit, RET, TrkA, TrkB, TrkC, IGR-IR, AIk, c-FMS, or combinations thereof.

公开(公告)号：EP1981870A2

公开(公告)日：2008-10-22

申请号：EP07717222.9

申请日：2007-02-06

申请人： IRM LLC

发明人： DING, Qiang ,  REN, Pingda ,  ZHANG, Qiong ,  WANG, Xia ,  SIM, Taebo ,  ALBAUGH, Pamela A. ,  GRAY, Nathanael S.

IPC分类号： C07D401/04 ,  C07D401/14 ,  C07D413/14 ,  A61K31/4427 ,  A61K31/444 ,  A61K31/4468

CPC分类号： C07D239/42 ,  C07D401/04 ,  C07D401/14 ,  C07D403/14 ,  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 treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particulary diseases or disorders that involve abnormal activation of the Abl.Bcr-Abl, Bmx, b-RAF, c-RAFI c-SRC,KDR,CSKlFGFR3,JAK2ILck,Met,PKCalpha,SAPK2alpha)Tie2,TrkB and P70S6K kinases. These compounds have the following structure: (Formula I); in which: R1 is selected from -NR6R7 and -NR6C(O)R8; wherein R6 is selected from hydrogen and C1-6alkyl; R7 is selected from hydrogen, C1-6alkyl. -NR9R10, C6-10aryl-C0-4alkyl, C1-10heteroaryl-C0-4alkyl, C3-12cycloalkyl-C0-4alkyl and C3-8heterocycloalkyl-C0-4alkyl; wherein any aryl, heteroaryl, cycloalkyl or heterocycloalkyl of R7 can be optionally substituted by 1 to 3 radicals independently selected from C1-6alkyl, C1-6alkoxy, -QNR9R10 and C3-8heterocycloalkyl-C0-4alkyl; wherein Q is selected from a bond and C1-4alkylene; R8 is selected from hydrogen and C1-4alkyl; R9 and R10 are independently selected from hydrogen and C1-6alkyl; R2 is selected from hydrogen and C1-6alkyl; R3 is selected from hydrogen and C1-6alkyl; R4 is selected from hydrogen, halo, C1-6alkyl, C1-6alkoxy, halosubstituted-C1-6alkyl and halosubsb'tuted-C1-6alkoxy; R5 is selected from -C(O)NHR11 and -NHC(O)R11; wherein R11 is selected from C6-10aryl and C1-10heteroaryl; wherein any aryl or heteroaryl of R11 is optionally substituted with 1 to 3 radicals independently selected from halo, C1-6alkyl, C1-6alkoxy, halosubstituted-C1-6alkyl, halosubstituted-C1-6alkoxy, di-C1-4alkyl-amino-C1-6alkoxy, di-C1-4alkyl-amino-C1-4alkyl(C1-4alkyl)amino, C1-10heteroaiyl-C0-4alkyl, C3-8heterocycIoalkyl-C0-4alkyl and C3-8heterocycloalkyl-oxy; wherein any heteroaryl or heterocycloalkyl substituent of R11 is further optionally substituted by 1 to 2 radicals independently selected from C1-6alkyl and hydroxy-C1-6alkyl; X and Y are independently selected from N and CH; and the pharmaceutically acceptable salts, hydrates, solvates and isomers thereof.

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。