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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: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:US07642255B2
公开(公告)日:2010-01-05
申请号:US12099708
申请日:2008-04-08
申请人: Taebo Sim , Hyun Soo Lee , Pingda Ren , Qiang Ding , Yi Liu , Bing Li , Lintong Li , Xia Wang , Tetsuo Uno , Guobao Zhang , Nathanael Schiander Gray , Shuli You
发明人: Taebo Sim , Hyun Soo Lee , Pingda Ren , Qiang Ding , Yi Liu , Bing Li , Lintong Li , Xia Wang , Tetsuo Uno , Guobao Zhang , Nathanael Schiander Gray , Shuli You
IPC分类号: C07D413/14 , C07D471/04 , C07D487/04 , A61K31/535 , A61K31/497 , A61K31/519 , C07D251/12 , A61K31/53 , A61P35/00
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,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。
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公开(公告)号:US20090137804A1
公开(公告)日:2009-05-28
申请号:US11570983
申请日:2005-06-23
申请人: Qiang Ding , Nathanael Schiander Gray , Bing Li , Yi Liu , Taebo Sim , Tetsuo Uno , Guobao Zhang , Carole Pissot Soldermann , Werner Breitenstein , Guido Bold , Giorgio Caravatti , Pascal Furet , Vito Guagnano , Marc Lang , Paul W. Manley , Joseph Schoepfer , Carsten Spanka
发明人: Qiang Ding , Nathanael Schiander Gray , Bing Li , Yi Liu , Taebo Sim , Tetsuo Uno , Guobao Zhang , Carole Pissot Soldermann , Werner Breitenstein , Guido Bold , Giorgio Caravatti , Pascal Furet , Vito Guagnano , Marc Lang , Paul W. Manley , Joseph Schoepfer , Carsten Spanka
IPC分类号: A61K31/50 , C07D239/12 , 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.
摘要翻译: 本发明涉及式(I)化合物,其中取代基X1,R1,R2,R3和R4具有本发明说明书中阐述和解释的含义,制备这些化合物的方法,含有它们的药物组合物 ,其任选与一种或多种其它药学活性化合物组合用于治疗对蛋白激酶活性的抑制作出反应的疾病的用途,以及治疗这种疾病的方法。
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公开(公告)号:US08552002B2
公开(公告)日:2013-10-08
申请号:US11570983
申请日:2005-06-23
申请人: Qiang Ding , Nathanael Schiander Gray , Bing Li , Yi Liu , Taebo Sim , Tetsuo Uno , Guobao Zhang , Carole Pissot Soldermann , Werner Breitenstein , Guido Bold , Giorgio Caravatti , Pascal Furet , Vito Guagnano , Marc Lang , Paul William Manley , Joseph Schoepfer , Carsten Spanka
发明人: Qiang Ding , Nathanael Schiander Gray , Bing Li , Yi Liu , Taebo Sim , Tetsuo Uno , Guobao Zhang , Carole Pissot Soldermann , Werner Breitenstein , Guido Bold , Giorgio Caravatti , Pascal Furet , Vito Guagnano , Marc Lang , Paul William Manley , Joseph Schoepfer , Carsten Spanka
IPC分类号: A01N43/54 , C07D239/02
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.
摘要翻译: 本发明涉及式(I)化合物,其中取代基X1,R1,R2,R3和R4具有本发明说明书中阐述和解释的含义,制备这些化合物的方法,含有它们的药物组合物 ,其任选与一种或多种其它药学活性化合物组合用于治疗对蛋白激酶活性的抑制作出反应的疾病的用途,以及治疗这种疾病的方法。
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公开(公告)号:US07745437B2
公开(公告)日:2010-06-29
申请号:US11628881
申请日:2005-06-09
申请人: Pingda Ren , Xia Wang , Guobao Zhang , Qiang Ding , Shuli You , Qiong Zhang , Greg Chopiuk , Pamela A. Albaugh , Taebo Sim , Nathanael Schiander Gray
发明人: Pingda Ren , Xia Wang , Guobao Zhang , Qiang Ding , Shuli You , Qiong Zhang , Greg Chopiuk , Pamela A. Albaugh , Taebo Sim , Nathanael Schiander Gray
IPC分类号: C07D403/04 , A61K31/4178
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, ΣΓK, Tιε2, Λχκ, θNK2α2, MKK4, c-RAF, MKK6, SAPK2α 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 ,PDGF-R,trkB,c-SRC,BMX,FGFR3,b-RAF,& Ggr; K,Tι&egr; 2,Λχ&kgr;; thetas;NK2α2,MKK4,c-RAF,MKK6,SAPK2α和SAPK2& 激酶。
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公开(公告)号:US20080221098A1
公开(公告)日:2008-09-11
申请号:US12099708
申请日:2008-04-08
申请人: Taebo Sim , Hyun Soo Lee , Pingda Ren , Qiang Ding , Yi Liu , Bing Li , Lintong Li , Xia Wang , Tetsuo Uno , Guobao Zhang , Nathanael Schiander Gray , Shuli You
发明人: Taebo Sim , Hyun Soo Lee , Pingda Ren , Qiang Ding , Yi Liu , Bing Li , Lintong Li , Xia Wang , Tetsuo Uno , Guobao Zhang , Nathanael Schiander Gray , Shuli You
IPC分类号: A61K31/5377 , C07D487/04 , A61K31/519 , A61K31/496
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,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。
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公开(公告)号:US07371750B2
公开(公告)日:2008-05-13
申请号:US10909227
申请日:2004-07-29
申请人: Taebo Sim , Hyun Soo Lee , Pingda Ren , Qiang Ding , Guobao Zhang , Yi Liu , Xia Wang , Tetsuo Uno , Bing Li , Lintong Li , Nathanael Schiander Gray , Shuli You
发明人: Taebo Sim , Hyun Soo Lee , Pingda Ren , Qiang Ding , Guobao Zhang , Yi Liu , Xia Wang , Tetsuo Uno , Bing Li , Lintong Li , Nathanael Schiander Gray , Shuli You
IPC分类号: A61K31/5355 , A61K31/53 , A61K31/497 , A61K31/513 , C07D413/12 , C07D253/065 , C07D487/04 , C07D413/14 , A61P35/00 , C07D471/04
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,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。
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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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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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