公开(公告)号：US20110053897A1

公开(公告)日：2011-03-03

申请号：US12843771

申请日：2010-07-26

Applicant: Jianwei CHE ,  Bei Chen ,  Qiang Ding ,  Xueshi Hao ,  Xiaohui He ,  Songchun Jiang ,  Qihui Jin ,  Yunho Jin ,  Hong Liu ,  Yahua Liu ,  Barun Okram ,  Tetsuo Uno ,  Xu Wu ,  Kunyong Yang ,  Xuefeng Zhu

Inventor： Jianwei CHE ,  Bei Chen ,  Qiang Ding ,  Xueshi Hao ,  Xiaohui He ,  Songchun Jiang ,  Qihui Jin ,  Yunho Jin ,  Hong Liu ,  Yahua Liu ,  Barun Okram ,  Tetsuo Uno ,  Xu Wu ,  Kunyong Yang ,  Xuefeng Zhu

IPC: A61K31/635 ,  C07D471/04 ,  A61K31/497 ,  A61K31/5377 ,  A61K31/506 ,  A61K31/444 ,  A61P11/06 ,  A61P19/02 ,  A61P35/00 ,  A61P7/06 ,  A61P25/00

CPC classification number: C07D471/04 ,  A61K31/4375

Abstract: 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.

Abstract translation: 本文提供了区域新颖的化合物类，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Syk激酶活性相关的疾病或病症的方法。

公开(公告)号：US20150094275A1

公开(公告)日：2015-04-02

申请号：US14540919

申请日：2014-11-13

Applicant: Nathanael S. GRAY ,  Jianming ZHANG ,  Barun OKRAM ,  Xianming DENG ,  Jae Won CHANG ,  Amy WOJCIECHOWSKI

Inventor： Nathanael S. GRAY ,  Jianming ZHANG ,  Barun OKRAM ,  Xianming DENG ,  Jae Won CHANG ,  Amy WOJCIECHOWSKI

IPC: C07D487/04 ,  A61K31/5377 ,  C07D495/04 ,  C07D239/94 ,  A61K31/517 ,  A61K45/06 ,  C07D471/04 ,  C07D403/04 ,  C07H19/16 ,  A61K31/7076 ,  C07D473/34 ,  A61K31/52 ,  A61K31/519 ,  C07D239/42

CPC classification number: C07D487/04 ,  A61K31/517 ,  A61K31/519 ,  A61K31/52 ,  A61K31/5377 ,  A61K31/7076 ,  A61K45/06 ,  C07D239/42 ,  C07D239/94 ,  C07D403/04 ,  C07D403/06 ,  C07D403/12 ,  C07D417/04 ,  C07D471/04 ,  C07D473/34 ,  C07D495/04 ,  C07H19/16 ,  Y02A50/401

Abstract: The present invention provides novel heteroaryl compounds having a pyrimidine-containing core that is linked to a 4-trifluoromethoxyphenyl group via an amine linker. Such compounds are useful for the treatment of cancers.

Abstract translation: 本发明提供了具有通过胺连接体与4-三氟甲氧基苯基连接的含嘧啶核心的新型杂芳基化合物。 这些化合物可用于治疗癌症。

公开(公告)号：US08546370B2

公开(公告)日：2013-10-01

申请号：US12865339

申请日：2009-01-27

Applicant: Barun Okram ,  Tetsuo Uno ,  Qiang Ding ,  Yahua Liu ,  Yunho Jin ,  Qihui Jin ,  Xu Wu ,  Jianwei Che ,  S. Frank Yan ,  Xueshi Hao

Inventor： Barun Okram ,  Tetsuo Uno ,  Qiang Ding ,  Yahua Liu ,  Yunho Jin ,  Qihui Jin ,  Xu Wu ,  Jianwei Che ,  S. Frank Yan ,  Xueshi Hao

IPC: A61K31/33

CPC classification number: C07D471/04

Abstract: The invention provides a novel class of 2,7-naphthyridin derivatives; 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-GR-1R, Alk, c-FMS, or combinations thereof.

Abstract translation: 本发明提供了一类新的2,7-萘啶衍生物; 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激酶活性相关的疾病或病症的方法，特别是Syk，ZAP70，KDR，FMS，FLT3，c-Kit，RET，TrkA，TrkB，TrkC-GR -1R，Alk，c-FMS或其组合。

公开(公告)号：US08722692B2

公开(公告)日：2014-05-13

申请号：US13386645

申请日：2010-07-30

Applicant: Jianwei Che ,  Qiang Ding ,  Xiaohui He ,  Hong Liu ,  Yahua Liu ,  Pierre-Yves Michellys ,  Barun Okram ,  Xu Wu ,  Kunyong Yang ,  Xuefeng Zhu

Inventor： Jianwei Che ,  Qiang Ding ,  Xiaohui He ,  Hong Liu ,  Yahua Liu ,  Pierre-Yves Michellys ,  Barun Okram ,  Xu Wu ,  Kunyong Yang ,  Xuefeng Zhu

IPC: A01N43/90 ,  A61K31/519 ,  C07D471/00 ,  C07D487/00

CPC classification number: C07D471/04

Abstract: Provided herein are a novel 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 Syk kinase activity.

Abstract translation: 本文提供了一类新的式（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Syk激酶活性相关的疾病或病症的方法。

公开(公告)号：US20120184526A1

公开(公告)日：2012-07-19

申请号：US13386645

申请日：2010-07-30

Applicant: Jianwei Che ,  Qiang Ding ,  Xiaohui He ,  Hong Liu ,  Yahua Liu ,  Pierre-Yves Michellys ,  Barun Okram ,  Xu Wu ,  Kunyong Yang ,  Xuefeng Zhu

Inventor： Jianwei Che ,  Qiang Ding ,  Xiaohui He ,  Hong Liu ,  Yahua Liu ,  Pierre-Yves Michellys ,  Barun Okram ,  Xu Wu ,  Kunyong Yang ,  Xuefeng Zhu

IPC: A61K31/5377 ,  A61K31/519 ,  A61P35/00 ,  A61P37/08 ,  A61P29/00 ,  A61P19/02 ,  C07D471/04 ,  A61K31/496

CPC classification number: C07D471/04

Abstract: Provided herein are 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 Syk kinase activity.

Abstract translation: 本文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Syk激酶活性相关的疾病或病症的方法。

公开(公告)号：US20080287432A1

公开(公告)日：2008-11-20

申请号：US12063550

申请日：2006-08-15

Applicant: Barun Okram ,  Pingda Ren ,  Nathanael S. Gray

Inventor： Barun Okram ,  Pingda Ren ,  Nathanael S. Gray

IPC: A61K31/5377 ,  C07D495/14 ,  A61K31/4365 ,  A61K31/496 ,  C07D413/12

CPC classification number: C07D471/14 ,  C07D495/14

Abstract: The invention provides a novel 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 diseases or disorders that involve abnormal activation of the AbI, Bcr-AbI, Aurora-A, SGK, Tie-2, Trk-B, FGFR3, c-kit, b-RAF, c-RAF, DYRK2, Fms, Fyn and PDGFRalpha and PDGFR&bgr; kinases.

Abstract translation: 本发明提供了一类新颖的式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AbI异常活化的疾病或病症， Bcr-AbI，Aurora-A，SGK，Tie-2，Trk-B，FGFR3，c-kit，b-RAF，c-RAF，DYRK2，Fms，Fyn和PDGFRα和PDGFRβ激酶。

公开(公告)号：US20190084990A1

公开(公告)日：2019-03-21

申请号：US16170921

申请日：2018-10-25

Applicant: Nathanael S. Gray ,  Jianming Zhang ,  Barun Okram ,  Xianming Deng ,  Jae Won Chang ,  Amy Wojciechowski

Inventor： Nathanael S. Gray ,  Jianming Zhang ,  Barun Okram ,  Xianming Deng ,  Jae Won Chang ,  Amy Wojciechowski

IPC: C07D487/04 ,  A61K31/519 ,  C07D495/04 ,  C07D473/34 ,  C07D417/04 ,  C07D403/12 ,  C07D403/06 ,  C07D403/04 ,  C07D239/94 ,  C07D239/42 ,  A61K31/52 ,  A61K31/5377 ,  A61K31/7076 ,  A61K45/06 ,  C07D471/04 ,  A61K31/517 ,  C07H19/16

Abstract: The present invention provides novel heteroaryl compounds of formula (I) having a pyrimidine-containing core that is linked to a 4-trifluoromethoxyphenyl group via an amine linker. Such compounds are useful for the treatment of cancers.

公开(公告)号：US09670214B2

公开(公告)日：2017-06-06

申请号：US14540919

申请日：2014-11-13

Applicant: Nathanael S. Gray ,  Jianming Zhang ,  Barun Okram ,  Xianming Deng

Inventor： Nathanael S. Gray ,  Jianming Zhang ,  Barun Okram ,  Xianming Deng

IPC: C07D487/04 ,  A61K31/519 ,  C07D471/04 ,  C07D239/42 ,  C07D239/94 ,  C07D403/04 ,  C07D403/06 ,  C07D403/12 ,  C07D495/04 ,  C07D417/04 ,  C07D473/34 ,  A61K31/517 ,  A61K31/52 ,  A61K31/5377 ,  A61K31/7076 ,  A61K45/06 ,  C07H19/16

CPC classification number: C07D487/04 ,  A61K31/517 ,  A61K31/519 ,  A61K31/52 ,  A61K31/5377 ,  A61K31/7076 ,  A61K45/06 ,  C07D239/42 ,  C07D239/94 ,  C07D403/04 ,  C07D403/06 ,  C07D403/12 ,  C07D417/04 ,  C07D471/04 ,  C07D473/34 ,  C07D495/04 ,  C07H19/16 ,  Y02A50/401

Abstract: The present invention provides novel heteroaryl compounds of formula (I) having a pyrimidine-containing core that is linked to a 4-trifluoromethoxyphenyl group via an amine linker. Such compounds are useful for the treatment of cancers.

公开(公告)号：US20100048552A1

公开(公告)日：2010-02-25

申请号：US12299687

申请日：2007-05-11

Applicant: Pingda Ren ,  Baogen Wu ,  Guobao Zhang ,  Yongping Xie ,  Barun Okram ,  Victor Nikulin ,  Xia Wang ,  Ha-Soon Choi

Inventor： Pingda Ren ,  Baogen Wu ,  Guobao Zhang ,  Yongping Xie ,  Barun Okram ,  Victor Nikulin ,  Xia Wang ,  Ha-Soon Choi

IPC: A61K31/4375 ,  C07D471/14 ,  A61K31/5377 ,  A61P43/00

CPC classification number: C07D471/14

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US07589101B2

公开(公告)日：2009-09-15

申请号：US12063550

申请日：2006-08-15

Applicant: Barun Okram ,  Pingda Ren ,  Nathanael S. Gray

Inventor： Barun Okram ,  Pingda Ren ,  Nathanael S. Gray

IPC: A61K31/407 ,  A61K31/4162 ,  A61K31/437 ,  C07D471/14

CPC classification number: C07D471/14 ,  C07D495/14

Abstract: The invention provides a novel 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 diseases or disorders that involve abnormal activation of the AbI, Bcr-AbI, Aurora-A, SGK, Tie-2, Trk-B, FGFR3, c-kit, b-RAF, c-RAF, DYRK2, Fms, Fyn and PDGFRalpha and PDGFR&bgr; kinases.

Abstract translation: 本发明提供了一类新颖的式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AbI异常活化的疾病或病症， Bcr-AbI，Aurora-A，SGK，Tie-2，Trk-B，FGFR3，c-kit，b-RAF，c-RAF，DYRK2，Fms，Fyn和PDGFRα和PDGFRβ激酶。