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公开(公告)号:US07868018B2
公开(公告)日:2011-01-11
申请号:US11997113
申请日:2006-08-09
申请人: Yongping Xie , Guobao Zhang , Xing Wang , Nathanael S. Gray , Yi Liu
发明人: Yongping Xie , Guobao Zhang , Xing Wang , Nathanael S. Gray , Yi Liu
IPC分类号: C07D471/04 , A61K31/4375 , A61P35/00 , A61P37/00 , A61P25/00 , A61K31/519 , C07D413/12 , A61K31/5355 , A61K31/4355 , C07D491/147
CPC分类号: C07D471/14 , C07D471/04 , C07D491/14
摘要: The invention provides compounds of Formula I: wherein R1-R6 are described in the Summary of the Invention; the 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, IKKα, IKKβ, JNK2α2, Lck, Met, MKK4, MKK6, MST2, NEK2, p70S6K, PDGFRβ, PKA, PKBα, PKD2, Rsk1, SAPK2α, SAPK2β, SAPK3, SGK, Tie2 and TrkB kinases.
摘要翻译: 本发明提供式I化合物:其中R 1 -R 6在发明概述中描述; 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,BMX,BTK,CHK2,b异常活化的疾病或病症 -RAF,c-RAF,CSK,c-SRC,Fes,FGFR3,Flt3,IKKα,IKK&bgr;JNK2α2,Lck,Met,MKK4,MKK6,MST2,NEK2,p70S6K,PDGFR&bgr; PKA,PKBα,PKD2,Rsk1 ,SAPK2α,SAPK2&bgr,SAPK3,SGK,Tie2和TrkB激酶。
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公开(公告)号:US20080300246A1
公开(公告)日:2008-12-04
申请号:US11997113
申请日:2006-08-09
申请人: Yongping Xie , Guobao Zhang , Xing Wang , Nathanael S. Gray , Yi Liu
发明人: Yongping Xie , Guobao Zhang , Xing Wang , Nathanael S. Gray , Yi Liu
IPC分类号: A61K31/5377 , C07D471/02 , A61K31/4375 , C07D471/12 , A61P35/00 , A61K31/519 , C07D413/14
CPC分类号: C07D471/14 , C07D471/04 , C07D491/14
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, BMX, BTK, CHK2, b-RAF, c-RAF, CSK, c-SRC, Fes, FGFR3, Flt3, IKKα, IKKβ, JNK2α 2, Lck, Met, MKK4, MKK6, MST2, NEK2, p70S6K, PDGFRβ, PKA, PKBα, 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,b-RAF,c-RAF,CSK,c-SRC,Fes,FGFR3,Flt3,IKKalpha,IKKbeta,JNK2alpha2,Lck,Met,MKK4,MKK6,MST2,NEK2,p70S6K,PDGFRbeta, PKA,PKBalpha,PKD2,Rsk1,SAPK2alpha,SAPK2beta,SAPK3,SGK,Tie2和TrkB激酶。
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公开(公告)号:US20090312321A1
公开(公告)日:2009-12-17
申请号:US12300088
申请日:2007-04-06
申请人: Pingda Ren , Guobao Zhang , Shuli You , Taebo Sim , Nathanael S. Gray , Yongping Xie , Xing Wang , Yun He
发明人: Pingda Ren , Guobao Zhang , Shuli You , Taebo Sim , Nathanael S. Gray , Yongping Xie , Xing Wang , Yun He
IPC分类号: A61K31/5377 , C07D471/04 , A61K31/4375 , C07D487/04 , A61K31/519
CPC分类号: C07D487/04 , C07D471/04
摘要: Described are compounds, pharmaceutical compositions comprising such compounds, and methods of using such compounds to treat or prevent disease or disordered associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activity of kinases such as Abl, ALK, AMPK, Aurora, Axl, Bcr-Abl, BIK, Bmx, BRK, BTK, c-Kit, CSK, cSrc, CDK1, CHK2, CK1, CK2, CaMKII, CaMKIV, DYRK2, EGFR, EphB1, FES, FGFR1, FGFR2, FGFR3, Flt1, Flt3, FMS, Fyn, GSK3β, IGF-1R, IKKα, IKKβ, IR, IRAK4, ITK, JAK2, JAK3, JNK1α1, JNK2α, KDR, Lck, LYN, MAPK1, MAPKAP-K2, MEK1, MET, MKK4, MKK6, MST2, NEK2, NLK, p70S6K, PAK2, PDGFR, PDGFRα, PDK1, Pim-2, Plk3, PKA, PKBα, PKCα, PKCtheta, PKD2, c-Raf, RET, ROCK-I, ROCK-II, Ron, Ros, Rsk1, SAPK2a, SAPK2b, SAPK3, SAPK4, SGK, SIK, Syk, Tie2, TrkB, WNK3, and ZAP-70.
摘要翻译: 描述的是化合物,包含这些化合物的药物组合物,以及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紊乱的方法,特别是涉及激酶例如Abl,ALK,AMPK,Aurora的异常活性的疾病或病症 ,Ax1,Bcr-Abl,BIK,Bmx,BRK,BTK,c-Kit,CSK,cSrc,CDK1,CHK2,CK1,CK2,CaMKII,CaMKIV,DYRK2,EGFR,EphB1,FES,FGFR1,FGFR2,FGFR3,Flt1 ,Flt3,FMS,Fyn,GSK3beta,IGF-1R,IKKalpha,IKKbeta,IR,IRAK4,ITK,JAK2,JAK3,JNK1alpha1,JNK2alpha,KDR,Lck,LYN,MAPK1,MAPKAP-K2,MEK1,MET,MKK4,MKK6 ,MST2,NEK2,NLK,p70S6K,PAK2,PDGFR,PDGFRalpha,PDK1,Pim-2,Plk3,PKA,PKBalpha,PKCalpha,PKCθ,PKD2,c-Raf,RET,ROCK-1,ROCK-II,Ron, ,Rsk1,SAPK2a,SAPK2b,SAPK3,SAPK4,SGK,SIK,Syk,Tie2,TrkB,WNK3和ZAP-70。
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公开(公告)号:US07449582B2
公开(公告)日:2008-11-11
申请号:US10961646
申请日:2004-10-08
申请人: Qiang Ding , Yongping Xie , Nathanael S. Gray , Shuli You , Greg Chopiuk , Jiqing Jiang , Yi Liu , Ruo Steensma , Xing Wang , Taebo Sim
发明人: Qiang Ding , Yongping Xie , Nathanael S. Gray , Shuli You , Greg Chopiuk , Jiqing Jiang , Yi Liu , Ruo Steensma , Xing Wang , Taebo Sim
IPC分类号: C07D215/38 , C07D471/02 , C07D251/38
CPC分类号: 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, CSK, JNK1, JNK2, PDGF-R, p38, p70S6K, TGFβ, SRC, EGFR, c-Kit, trkB, FGFR3, Fes, Lck, Syk, RAF, MKK4, MKK6 and SAPK2β 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 ,CSK,JNK1,JNK2,PDGF-R,p38,p70S6K,TGFbeta,SRC,EGFR,c-Kit,trkB,FGFR3,Fes,Lck,Syk,RAF,MKK4,MKK6和SAPK2β激酶。
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公开(公告)号:US08202876B2
公开(公告)日:2012-06-19
申请号:US12444129
申请日:2007-09-24
申请人: Pamela Albaugh , Gregory B. Chopiuk , Qiang Ding , Shenlin Huang , Zuosheng Liu , Shifeng Pan , Pingda Ren , Xia Wang , Xing Wang , Yongping Xie , Chengzhi Zhang , Qiong Zhang , Guobao Zhang , Daniel Poon , Paul Renhowe , Martin Sendzik
发明人: Pamela Albaugh , Gregory B. Chopiuk , Qiang Ding , Shenlin Huang , Zuosheng Liu , Shifeng Pan , Pingda Ren , Xia Wang , Xing Wang , Yongping Xie , Chengzhi Zhang , Qiong Zhang , Guobao Zhang , Daniel Poon , Paul Renhowe , Martin Sendzik
IPC分类号: C07D401/00 , C07D403/00 , C07D405/00 , C07D409/00 , C07D411/00 , C07D413/00 , C07D417/00 , C07D419/00 , C07D231/00 , C07D403/02 , A01N43/56 , A61K31/415
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。
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公开(公告)号:US20100184765A1
公开(公告)日:2010-07-22
申请号:US12664765
申请日:2008-06-10
申请人: Shenlin Huang , Zuosheng Liu , Pamela A. Albaugh , Xing Wang , Shifeng Pan , Yongping Xie , Guobao Zhang
发明人: Shenlin Huang , Zuosheng Liu , Pamela A. Albaugh , Xing Wang , Shifeng Pan , Yongping Xie , Guobao Zhang
IPC分类号: A61K31/5377 , C07D401/04 , C07D241/02 , C07D413/04 , A61K31/497 , A61P35/00
CPC分类号: C07D401/14 , C07D403/04
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 Alk, Abl, Aurora-A, B-Raf, C-Raf, Bcr-Abl, BRK, Blk, Bmx, BTK, C-Kit, CSK, C-Src, EphB1, EphB2, EphB4, FLT1, Fms, Flt3, Fyn, FRK3, JAK2, KDR, Lck, Lyn, PDGFRα, PDGFRβ, PKCα, SAPK2α, 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Alk,Abl,Aurora-A,B-Raf,C-Raf,Bcr-Abl,BRK,Blk等异常活化的疾病或病症的方法。 Bcl,Rb,C-Kit,CSK,C-Src,EphB1,EphB2,EphB4,FLT1,Fms,Flt3,Fyn,FRK3,JAK2,KDR,Lck,Lyn,PDGFRα,PDGFR&bgr;PKCα,SAPK2α,Src,SIK ,Syk,Tie2和TrkB激酶。
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公开(公告)号:US20110053932A1
公开(公告)日:2011-03-03
申请号:US12665894
申请日:2008-06-18
申请人: Taebo Sim , Truc Ngoc Nguyen , Baogen Wu , Yun He , Yongping Xie , Xing Wang , Guobao Zhang , Nathanael Schiander Gray
发明人: Taebo Sim , Truc Ngoc Nguyen , Baogen Wu , Yun He , Yongping Xie , Xing Wang , Guobao Zhang , Nathanael Schiander Gray
IPC分类号: A61K31/5377 , C07D239/94 , A61K31/517 , C12N5/00 , A61P35/00 , A61P35/04 , A61P19/02 , A61P17/06 , A61P37/00 , C07D239/88 , C07D413/14 , C07D413/12
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 Alk, Abl, Aurora-A, B-Raf, C-Raf, Bcr-Abl, BRK, Blk, 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Alk,Abl,Aurora-A,B-Raf,C-Raf,Bcr-Abl,BRK,Blk等异常活化的疾病或病症的方法。 BGFR,BK,BTK,C-Kit,C-Raf,C-Src,EphB1,EphB2,EphB4,FGFR1,FGFR2,FGFR3,FLT1,Fms,Flt3,Fyn,FRK3,JAK2,KDR,Lck,Lyn,PDGFRα,PDGFR& ,PKCα,p38,Src,SIK,Syk,Tie2和TrkB激酶。
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公开(公告)号:US20050187230A1
公开(公告)日:2005-08-25
申请号:US10961646
申请日:2004-10-08
申请人: Qiang Ding , Yongping Xie , Nathanael Gray , Shuli You , Greg Chopiuk , Jiqing Jiang , Yi Liu , Ruo Steensma , Xing Wang , Taebo Sim
发明人: Qiang Ding , Yongping Xie , Nathanael Gray , Shuli You , Greg Chopiuk , Jiqing Jiang , Yi Liu , Ruo Steensma , Xing Wang , Taebo Sim
IPC分类号: A61K20060101 , A61K31/44 , A61K31/47 , A61K31/4706 , A61K31/4745 , A61K31/519 , C07D215/16 , C07D471/00 , C07D471/02
CPC分类号: 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, CSK, JNK1, JNK2, PDGF-R, p38, p70S6K, TGFβ, SRC, EGFR, c-Kit, trkB, FGFR3, Fes, Lck, Syk, RAF, MKK4, MKK6 and SAPK2β 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 ,CSK,JNK1,JNK2,PDGF-R,p38,p70S6K,TGFbeta,SRC,EGFR,c-Kit,trkB,FGFR3,Fes,Lck,Syk,RAF,MKK4,MKK6和SAPK2β激酶。
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公开(公告)号:US20100048552A1
公开(公告)日:2010-02-25
申请号:US12299687
申请日:2007-05-11
申请人: Pingda Ren , Baogen Wu , Guobao Zhang , Yongping Xie , Barun Okram , Victor Nikulin , Xia Wang , Ha-Soon Choi
发明人: Pingda Ren , Baogen Wu , Guobao Zhang , Yongping Xie , Barun Okram , Victor Nikulin , Xia Wang , Ha-Soon Choi
IPC分类号: A61K31/4375 , C07D471/14 , A61K31/5377 , A61P43/00
CPC分类号: C07D471/14
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, Bcr-Abl(T315I), ALK, BLK, BMX, BRK, C-kit, c-RAF, CSK, c-SRC, EGFR, Fes, FGFR3, Flt3, Fms, Fyn, IGF-1R, IR, JAK(2), JAK(3), KDR, Lck, NLK, p70S6K, PDGFRα, Ros, SAPK2α, SGK, SIK, Syk, 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 ,Bcr-Abl(T315I),ALK,BLK,BMX,BRK,C-kit,c-RAF,CSK,c-SRC,EGFR,Fes,FGFR3,Flt3,Fms,Fyn,IGF-1R,IR,JAK( 2),JAK(3),KDR,Lck,NLK,p70S6K,PDGFRα,Ros,SAPK2α,SGK,SIK,Syk,Tie2和TrkB激酶。
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公开(公告)号:US07846923B2
公开(公告)日:2010-12-07
申请号:US12299687
申请日:2007-05-11
申请人: Pingda Ren , Baogen Wu , Guobao Zhang , Yongping Xie , Barun Okram , Victor Nikulin , Xia Wang , Ha-Soon Choi
发明人: Pingda Ren , Baogen Wu , Guobao Zhang , Yongping Xie , Barun Okram , Victor Nikulin , Xia Wang , Ha-Soon Choi
IPC分类号: C07D471/00 , A61K31/54
CPC分类号: C07D471/14
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, Bcr-Abl(T315I), ALK, BLK, BMX, BRK, C-kit, c-RAF, CSK, c-SRC, EGFR, Fes, FGFR3, Flt3, Fms, Fyn, IGF-1R, IR, JAK(2), JAK(3), KDR, Lck, NLK, p70S6K, PDGFRα, Ros, SAPK2α, SGK, SIK, Syk, 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 ,Bcr-Abl(T315I),ALK,BLK,BMX,BRK,C-kit,c-RAF,CSK,c-SRC,EGFR,Fes,FGFR3,Flt3,Fms,Fyn,IGF-1R,IR,JAK( 2),JAK(3),KDR,Lck,NLK,p70S6K,PDGFRα,Ros,SAPK2α,SGK,SIK,Syk,Tie2和TrkB激酶。
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