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：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：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：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。

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：EP1943233A2

公开(公告)日：2008-07-16

申请号：EP06844262.3

申请日：2006-11-03

申请人： IRM, LLC

发明人： ZHANG, Qiong ,  GRAY, Nathanael, S. ,  LIU, Yi ,  DING, Qiang ,  UNO, Tetsuo

IPC分类号： C07D239/42 ,  C07D239/48 ,  C07D239/52 ,  C07D239/47 ,  C07D213/74 ,  A61K31/44 ,  A61K31/505 ,  A61P35/00

CPC分类号： C07D239/48 ,  C07D213/74 ,  C07D239/42 ,  C07D239/47 ,  C07D239/52

摘要： The invention provides disubtituted pyrimidine or pyridine 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 Lck, IR, IGF-IR, JNKl , Flt3, Fes, EFGR (Her-1, erbB-1) , cSRC, CDKl/cyclinB, c-RAF, BTK, Bmx, AxI, Aurora-A, AbI, BCR-AbI, TrkB, Tie2, Syk, SGK, SAPK2a, Rskl and Met kinases.

公开(公告)号：EP1578722A2

公开(公告)日：2005-09-28

申请号：EP02776216.0

申请日：2002-10-12

申请人： IRM LLC ,  THE SCRIPPS RESEARCH INSTITUTE

发明人： DING, Sheng ,  DING, Qiang ,  GRAY, Nathanael, S.

IPC分类号： C07D201/00

CPC分类号： C07D239/42 ,  C07D239/94 ,  C07D241/20 ,  C07D241/44 ,  C07D473/16 ,  C07D473/18 ,  C07D473/34

摘要： General methods for the solution phase as well as solid phase synthesis of various substituted heteroaryls has been demonstrated. These substituted heteroaryls can be further elaborated by aromatic substitution with amines at elevated temperature or by anilines, boronic acids and phenols via palladium catalyzed cross-coupling reactions.