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1. 发明申请

WO2005080393A1 COMPOUNDS AND COMPOSITIONS AS PROTEIN KINASE INHIBITORS 审中-公开
标题翻译：作为蛋白激酶抑制剂的化合物和组合物
公开(公告)号：WO2005080393A1
公开(公告)日：2005-09-01
申请号：PCT/US2005/004630
申请日：2005-02-14
申请人： IRM LLC , CHOI, Ha-Soon , WANG, Zhicheng , GRAY, Nathanael Schiander , GU, Xiang-ju , HE, Xiaohui , HE, Yun , JIANG, Tao , LIU, YI , RICHMOND, Wendy , SIM, Taebo , YANG, Kunyong
发明人： CHOI, Ha-Soon , WANG, Zhicheng , GRAY, Nathanael Schiander , GU, Xiang-ju , HE, Xiaohui , HE, Yun , JIANG, Tao , LIU, YI , RICHMOND, Wendy , SIM, Taebo , YANG, Kunyong
IPC分类号： C07D471/04
CPC分类号： C07D471/04 , C07D487/04
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 the FAK, Abl, BCR-Abl, PDGF-R, c-Kit, NPM-ALK, Flt-3, JAK2 and c-Met 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FAK异常活化的疾病或病症，Abl，BCR -AbI，PDGF-R，c-Kit，NPM-ALK，Flt-3，JAK2和c-Met激酶。

2. 发明申请

WO2008157575A1 PROTEIN KINASE INHIBITORS AND METHODS FOR USING THEREOF 审中-公开
标题翻译：蛋白激酶抑制剂及其使用方法
公开(公告)号：WO2008157575A1
公开(公告)日：2008-12-24
申请号：PCT/US2008/067290
申请日：2008-06-18
申请人： IRM LLC , SIM, Taebo , NGUYEN, Truc Ngoc , WU, Baogen , HE, Yun , XIE, Yongping , WANG, Xing , ZHANG, Guobao , GRAY, Nathanael S.
发明人： SIM, Taebo , NGUYEN, Truc Ngoc , WU, Baogen , HE, Yun , XIE, Yongping , WANG, Xing , ZHANG, Guobao , GRAY, Nathanael S.
IPC分类号： C07D239/88 , C07D239/94 , C07D401/12 , C07D403/12 , C07D403/14 , C07D413/12 , C07D413/14 , C07D417/12 , A61K31/33 , A61P35/00 , A61P37/00
CPC分类号： C07D239/94 , C07D239/88 , C07D401/12 , C07D403/12 , C07D403/14 , C07D413/12 , C07D413/14 , C07D417/12
摘要： The invention provides compounds and pharmaceutical compositions thereof, which are useful as protein kinase inhibitors, and 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 AIk, AbI, Aurora- A, B-Raf, C- Raf, Bcr-Abl, BRK, BIk, Bmx, BTK, C-Kit, C-Raf, C-Src, EphB1, EphB2, EphB4, FGFR1, FGFR2, FGFR3, FLT1, Fms, Flt3, Fyn, FRK3, JAK2, KDR, Lck, Lyn, PDGFRα, PDGFRβ, PKCα, p38, Src, SIK, Syk, Tie2 and TrkB kinases.
摘要翻译：本发明提供了可用作蛋白激酶抑制剂的化合物及其药物组合物，以及使用这些化合物治疗，改善或预防与异常或失调的激酶活性相关的病症的方法。在一些实施方案中，本发明提供了使用这些化合物治疗，改善或预防涉及AIk，AbI，Aurora-A，B-Raf，C-Raf，Bcr-Abl，BRK，BIk等的异常活化的疾病或病症的方法。 BGFR，BK，BK，BKX，BTK，C-Kit，C-Raf，C-Src，EphB1，EphB2，EphB4，FGFR1，FGFR2，FGFR3，FLT1，Fms，Flt3，Fyn，FRK3，JAK2，KDR，Lck，Lyn， PKCa，p38，Src，SIK，Syk，Tie2和TrkB激酶。

3. 发明申请

WO2007092531A3 COMPOUNDS AND COMPOSITIONS AS PROTEIN KINASE INHIBITORS 审中-公开
公开(公告)号：WO2007092531A3
公开(公告)日：2007-08-16
申请号：PCT/US2007/003319
申请日：2007-02-06
申请人： IRM LLC , DING, Qiang , REN, Pingda , ZHANG, Qiong , WANG, Xia , SIM, Taebo , ALBAUGH, Pamela A. , GRAY, Nathanael S.
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
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: R 1 is selected from -NR 6 R 7 and -NR 6 C(O)R 8 ; wherein R 6 is selected from hydrogen and C 1-6 alkyl; R 7 is selected from hydrogen, C 1-6 alkyl. -NR 9 R 10 , C 6-10 aryl-C 0-4 alkyl, C 1-10 heteroaryl-C 0-4 alkyl, C 3-12 cycloalkyl-C 0-4 alkyl and C 3-8 heterocycloalkyl-C 0-4 alkyl; wherein any aryl, heteroaryl, cycloalkyl or heterocycloalkyl of R 7 can be optionally substituted by 1 to 3 radicals independently selected from C 1-6 alkyl, C 1-6 alkoxy, -QNR 9 R 10 and C 3-8 heterocycloalkyl-C 0-4 alkyl; wherein Q is selected from a bond and C 1-4 alkylene; R 8 is selected from hydrogen and C 1-4 alkyl; R 9 and R 10 are independently selected from hydrogen and C 1-6 alkyl; R 2 is selected from hydrogen and C 1-6 alkyl; R 3 is selected from hydrogen and C 1-6 alkyl; R 4 is selected from hydrogen, halo, C 1-6 alkyl, C 1-6 alkoxy, halosubstituted-C 1-6 alkyl and halosubsb'tuted-C 1-6 alkoxy; R 5 is selected from -C(O)NHR 11 and -NHC(O)R 11 ; wherein R 11 is selected from C 6-10 aryl and C 1-10 heteroaryl; wherein any aryl or heteroaryl of R 11 is optionally substituted with 1 to 3 radicals independently selected from halo, C 1-6 alkyl, C 1-6 alkoxy, halosubstituted-C 1-6 alkyl, halosubstituted-C 1-6 alkoxy, di-C 1-4 alkyl-amino-C 1-6 alkoxy, di-C 1-4 alkyl-amino-C 1-4 alkyl(C 1-4 alkyl)amino, C 1-10 heteroaiyl-C 0-4 alkyl, C 3-8 heterocycIoalkyl-C 0-4 alkyl and C 3-8 heterocycloalkyl-oxy; wherein any heteroaryl or heterocycloalkyl substituent of R 11 is further optionally substituted by 1 to 2 radicals independently selected from C 1-6 alkyl and hydroxy-C 1-6 alkyl; X and Y are independently selected from N and CH; and the pharmaceutically acceptable salts, hydrates, solvates and isomers thereof.

4. 发明授权

EP1899329B1 PYRIMIDINE-SUBSTITUTED BENZIMIDAZOLE DERIVATIVES AS PROTEIN KINASE INHIBITORS 有权
标题翻译：嘧啶取代的苯并咪唑衍生物作为蛋白激酶抑制剂
公开(公告)号：EP1899329B1
公开(公告)日：2011-10-05
申请号：EP06774386.4
申请日：2006-06-30
申请人： IRM LLC
发明人： ZHANG, Guobao , REN, Pingda , WANG, Xia , GRAY, Nathanael S. , SIM, Taebo
IPC分类号： C07D403/14 , C07D403/04 , C07D401/14 , C07D409/14 , C07D413/14 , A61K31/495 , A61P35/00
CPC分类号： C07D413/14 , C07D401/14 , C07D403/04 , C07D403/14 , C07D409/14
摘要： The invention provides, 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 diseases or disorders that involve abnormal activation of Alk, Abl, BRK, Blk, BMX, CSK, c-Src, c-Raf, EGFR, Fes, FGFR3, Fms, Fyn, IGF-IR, IR, IKKα, IKKβ, JAK2, JAK3, KDR, Lck, Met, p70S6k, Ros, Rskl, SAPK2α, SAPK2β, SAPK3, SIK, Tie2, TrkB and/or WNK3 kinases.

5. 发明公开

EP1899329A1 PYRIMIDINE-SUBSTITUTED BENZIMIDAZOLE DERIVATIVES AS PROTEIN KINASE INHIBITORS 有权
标题翻译：嘧啶取代的苯并咪唑衍生物作为蛋白激酶抑制剂
公开(公告)号：EP1899329A1
公开(公告)日：2008-03-19
申请号：EP06774386.4
申请日：2006-06-30
申请人： IRM LLC A Delware Limited Liability Company
发明人： ZHANG, Guobao , REN, Pingda , WANG, Xia , GRAY, Nathanael S. , SIM, Taebo
IPC分类号： C07D403/14 , C07D403/04 , C07D401/14 , C07D409/14 , C07D413/14 , A61K31/495 , A61P35/00
CPC分类号： C07D413/14 , C07D401/14 , C07D403/04 , C07D403/14 , C07D409/14
摘要： The invention provides, 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 diseases or disorders that involve abnormal activation of Alk, Abl, BRK, Blk, BMX, CSK, c-Src, c-Raf, EGFR, Fes, FGFR3, Fms, Fyn, IGF-IR, IR, IKKα, IKKβ, JAK2, JAK3, KDR, Lck, Met, p70S6k, Ros, Rskl, SAPK2α, SAPK2β, SAPK3, SIK, Tie2, TrkB and/or WNK3 kinases.

6. 发明申请

WO2006124731A3 COMPOUNDS AND COMPOSITIONS AS PROTEIN KINASE INHIBITORS 审中-公开
公开(公告)号：WO2006124731A3
公开(公告)日：2006-11-23
申请号：PCT/US2006/018644
申请日：2006-05-12
申请人： IRM LLC , REN, Pingda , GRAY, Nathanael S. , WANG, Xia , ZHANG, Guobao , SIM, Taebo , JIANG, Songchun
发明人： REN, Pingda , GRAY, Nathanael S. , WANG, Xia , ZHANG, Guobao , SIM, Taebo , JIANG, Songchun
IPC分类号： C07D471/14 , A61K31/4985 , A61P29/00 , A61P35/00
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, BMX, BTK, CHK2, b-RAF, c-RAF, CSK, c-SRC, Fes, FGFR3, Flt3, IKK , IKK , JNK2 2, Lck, Met, MKK4, MKK6, MST2, NEK2, p70S6K, PDGFR , PKA, PKB , PKD2, Rsk1, SAPK2 , SAPK2 , SAPK3, SGK, Tie2 and TrkB kinases.

7. 发明申请

WO2006081172A3 COMPOUNDS AND COMPOSITIONS AS PROTEIN KINASE INHIBITORS 审中-公开
公开(公告)号：WO2006081172A3
公开(公告)日：2006-08-03
申请号：PCT/US2006/002266
申请日：2006-01-19
申请人： IRM LLC , 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.
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： A61K31/426 , A61K31/427 , C07D277/56
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.

8. 发明申请

WO2005123719A1 COMPOUNDS AND COMPOSITIONS AS PROTEIN KINASE INHIBITORS 审中-公开
标题翻译：作为蛋白激酶抑制剂的化合物和组合物
公开(公告)号：WO2005123719A1
公开(公告)日：2005-12-29
申请号：PCT/US2005/020371
申请日：2005-06-09
申请人： IRM LLC , REN, Pingda , WANG, Xia , ZHANG, Guobao , DING, Qiang , YOU, Shuli , ZHANG, Qiong , CHOPIUK, Greg , ALBAUGH, Pamela, A. , SIM, Taebo , GRAY, Nathanael, Schiander
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
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.
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，BCR-Abl异常活化的疾病或病症，PDGF-R，trkB，c-SRC，BMX，FGFR3，b-RAF，SGK，Tie2，Lck，JNK2 2，MKK4，c-RAF，MKK6，SAPK2和SAPK2激酶。

9. 发明公开

EP2076513A1 COMPOSITIONS AND METHODS FOR MODULATING C-KIT AND PDGFR RECEPTORS 审中-公开
标题翻译：组合物和方法调制的c-kit和PDGFR受体
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.

10. 发明公开

EP1981870A2 COMPOUNDS AND COMPOSITIONS AS PROTEIN KINASE INHIBITORS 审中-公开
标题翻译：化合物和组合物作为蛋白激酶抑制剂
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.

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