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1. 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.

2. 发明申请

WO2007005673A1 PYRIMIDINE-SUBSTITUTED BENZIMIDAZOLE DERIVATIVES AS PROTEIN KINASE INHIBITORS 审中-公开
标题翻译：作为蛋白激酶抑制剂的吡嗪基取代苯并咪唑衍生物
公开(公告)号：WO2007005673A1
公开(公告)日：2007-01-11
申请号：PCT/US2006/025706
申请日：2006-06-30
申请人： IRM LLC , ZHANG, Guobao , REN, Pingda , WANG, Xia , GRAY, Nathanael, S. , SIM, Taebo
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.
摘要翻译：本发明提供了式（I）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Alk，Abl异常激活的疾病或病症， BRK，Blk，BMX，CSK，c-Src，c-Raf，EGFR，Fes，FGFR3，Fms，Fyn，IGF-IR，IR，IKKa，IKKβ，JAK2，JAK3，KDR，Lck，Met，p70S6k， Rskl，SAPK2a，SAPK2β，SAPK3，SIK，Tie2，TrkB和/或WNK3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. 发明申请

WO2008144253A1 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：WO2008144253A1
公开(公告)日：2008-11-27
申请号：PCT/US2008/063187
申请日：2008-05-09
申请人： IRM LLC , REN, Pingda , WANG, Xia , JIANG, Songchun , NAGLE, Advait , OKRAM, Barun , HE, Yun , XIE, Yongping , WANG, Xing , HUANG, Shenlin , WANG, Xiaodong , LIU, Yi , ALBAUGH, Pamela, A. , GRAY, Nathanael, S. , ZHANG, Guobao
发明人： REN, Pingda , WANG, Xia , JIANG, Songchun , NAGLE, Advait , OKRAM, Barun , HE, Yun , XIE, Yongping , WANG, Xing , HUANG, Shenlin , WANG, Xiaodong , LIU, Yi , ALBAUGH, Pamela, A. , GRAY, Nathanael, S. , ZHANG, Guobao
IPC分类号： C07D471/04 , C07D487/04 , A61K31/519 , A61P35/00
CPC分类号： C07D471/04 , C07D487/04
摘要： The invention provides compounds of formula (l) 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, CSK, c-SRC, EphBl, EphB2, EphB4, FLTl, Fms, Flt3, Fyn, FRK3, JAK2, KDR, Lck, Lyn, PDGFRalpha, PDGFRbeta, PKCalpha, SAPK2alpha, 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式（I）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。 Bcl，Bcl，BK，BK，BK，BK，BK，BKX，BTK，c-Kit，c-RAF，CSK，c-SRC，EphB1，EphB2，EphB4，FLT1，Fms，Flt3，Fyn，FRK3，JAK2，KDR，Lck，Lyn，PDGFRalpha，PDGFRbeta，PKCalpha，SAPK2alpha， Src，SIK，Syk，Tie2和TrkB激酶。

5. 发明申请

WO2005011597A2 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：WO2005011597A2
公开(公告)日：2005-02-10
申请号：PCT/US2004/024764
申请日：2004-07-29
申请人： IRM LLC , SIM, Taebo , LEE, Hyun, Soo , REN, Pingda , DING, Qiang , WANG, Xia , UNO, Tetsuo , ZHANG, Guobao , LIU, Yi , LI, Bing , LI, Lintong , GRAY, Nathaniel , YOU, Shuli
发明人： SIM, Taebo , LEE, Hyun, Soo , REN, Pingda , DING, Qiang , WANG, Xia , UNO, Tetsuo , ZHANG, Guobao , LIU, Yi , LI, Bing , LI, Lintong , GRAY, Nathaniel , YOU, Shuli
IPC分类号： A61K
CPC分类号： C07D487/04 , 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 the Abl, BCR-Abl, Bmx, c-Raf, Csk, Fes, FGFR, Flt3, Ikk, IR, JNK, Lck, Mkk, PKC, PKD, Rsk, SAPK, Syk, Trk, BTK, Src, EGFR, IGF, Mek, Ros and Tie2 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，特别是涉及异常的疾病或病症的方法激活Abl，BCR-Abl，Bmx，c-Raf，Csk，Fes，FGFR，Flt3，Ikk，IR，JNK，Lck，Mkk，PKC，PKD，Rsk，SAPK，Syk，Trk，BTK，Src，EGFR ，IGF，Mek，Ros和Tie2激酶。

6. 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。

7. 发明申请

WO2006101783A2 COMPOUNDS AND COMPOSITIONS AS PROTEIN KINASE INHBITORS 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：WO2006101783A2
公开(公告)日：2006-09-28
申请号：PCT/US2006/008719
申请日：2006-03-10
申请人： IRM LLC , REN, Pingda , GRAY, Nathanael, S. , WANG, Xia , ZHANG, Gubao
发明人： REN, Pingda , GRAY, Nathanael, S. , WANG, Xia , ZHANG, Gubao
IPC分类号： A61K31/519
CPC分类号： C07D487/04 , A61K31/519 , A61K31/52
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, c-RAF, CSK, c-SRC, Fes, FGFR3, Flt3, IKKα , IKKβ, JNK2α 2, Lck, Met, MKK4, MKK6, MST2, NEK2, p70S6K, PDGFRβ , PKA, PKB β, PKD2, Rsk1, SAPK2α , SAPK2β , SAPK3, SGK, 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，Bcr-Abl异常活化的疾病或病症，BMX，BTK，CHK2，c-RAF，CSK，c-SRC，Fes，FGFR3，Flt3，IKKa，IKKβ，JNK2a2，Lck，Met，MKK4，MKK6，MST2，NEK2，p70S6K，PDGFRβ，PKA，PKB ，PKD2，Rsk1，SAPK2a，SAPK2β，SAPK3，SGK，Tie2和TrkB激酶。

8. 发明申请

WO2004078682A2 CYCLIC 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循环化合物和组合物
公开(公告)号：WO2004078682A2
公开(公告)日：2004-09-16
申请号：PCT/US2004/006947
申请日：2004-03-05
申请人： IRM LLC , REN, Pingda , ADRIAN, Francisco , GRAY, Nathanael S. , WANG, Xia
发明人： REN, Pingda , ADRIAN, Francisco , GRAY, Nathanael S. , WANG, Xia
IPC分类号： C07C
CPC分类号： C07D471/18 , C07D498/18 , C07D513/18
摘要： The invention provides a novel class of cyclic compounds, pharmaceutical compositions comprising such cyclic compounds and methods of using such compounds to treat or prevent diseases and disorders associated with cyclin-dependent kinases (CDKs) activity, particularly diseases associated with the activity of CDK2 and CDK5.
摘要翻译：本发明提供了一类新颖的环状化合物，包含这种环状化合物的药物组合物和使用这些化合物治疗或预防与细胞周期蛋白依赖性激酶（CDK）活性相关的疾病和病症的方法，特别是与CDK2和CDK5的活性相关的疾病。

9. 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.

10. 发明申请

WO2006002367A1 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：WO2006002367A1
公开(公告)日：2006-01-05
申请号：PCT/US2005/022463
申请日：2005-06-23
申请人： IRM LLC , REN, Pingda , WANG, Xia , GRAY, Nathanael, Schiander , LIU, Yi , SIM, Taebo
发明人： REN, Pingda , WANG, Xia , GRAY, Nathanael, Schiander , LIU, Yi , SIM, Taebo
IPC分类号： C07D475/00
CPC分类号： C07D475/00
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, c-RAF, CSK, Fes, FGFR3, Flt3, GSK3β , IR, JNK1α 1, JNK2α 2, Lck, MKK4, MKK6, p70S6K, PDGFRα , Rsk1, SAPK2α , SAPK2β , Syk and Trkβ 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的异常活化的疾病或病症，Bmx，c-RAF，CSK，Fes，FGFR3，Flt3，GSK3β，IR，JNK1a1，JNK2a2，Lck，MKK4，MKK6，p70S6K，PDGFRa，Rsk1，SAPK2a，SAPK2β，Syk和Trkβ激酶。

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