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公开(公告)号:US09493441B2
公开(公告)日:2016-11-15
申请号:US14345977
申请日:2012-09-21
申请人: Jason Brubaker , Joshua T. Close , Joon Jung , Michelle Martinez , Catherine White , Kevin Wilson , Jonathan R. Young , Hongjun Zhang
发明人: Jason Brubaker , Joshua T. Close , Joon Jung , Michelle Martinez , Catherine White , Kevin Wilson , Jonathan R. Young , Hongjun Zhang
IPC分类号: C07D405/08 , C07D403/12 , C07D401/14 , C07D231/38 , C07D401/12 , C07D403/08 , C07D405/12 , C07D409/12 , C07D413/12 , C07D401/04 , C07D403/04 , C07D405/04 , C07D401/06 , C07D403/06 , C07D405/06 , C07D405/14 , C07D409/04 , C07D413/14 , C07D417/14
CPC分类号: C07D405/08 , C07D231/38 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/08 , C07D403/12 , C07D405/04 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/04 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/14
摘要: The instant invention provides compounds of formula I which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.
摘要翻译: 本发明提供了作为JAK抑制剂的式I化合物,因此可用于治疗JAK介导的疾病如类风湿性关节炎,哮喘,COPD和癌症。
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2.ACYCLIC CYANOETHYLPYRAZOLES AS JANUS KINASE INHIBITORS 有权
标题翻译: ACYCLIC CYANOETHYLZOLES作为JANUS KINASE INHIBITORS公开(公告)号:US20140228358A1
公开(公告)日:2014-08-14
申请号:US14345977
申请日:2012-09-21
申请人: Jason Brubaker , Joshua T. Close , Joon Jung , Michelle Martinez , Catherine White , Kevin Wilson , Jonathan R. Young , Hongjun Zhang
发明人: Jason Brubaker , Joshua T. Close , Joon Jung , Michelle Martinez , Catherine White , Kevin Wilson , Jonathan R. Young , Hongjun Zhang
IPC分类号: C07D231/38 , C07D403/06 , C07D401/14 , C07D405/06 , C07D401/12 , C07D401/06 , C07D403/12
CPC分类号: C07D405/08 , C07D231/38 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/08 , C07D403/12 , C07D405/04 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/04 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/14
摘要: The instant invention provides compounds of formula I which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.
摘要翻译: 本发明提供了作为JAK抑制剂的式I化合物,因此可用于治疗JAK介导的疾病如类风湿性关节炎,哮喘,COPD和癌症。
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公开(公告)号:US09328099B2
公开(公告)日:2016-05-03
申请号:US14345978
申请日:2012-09-21
申请人: Jason Brubaker , Matthew Lloyd Childers , Matthew Christopher , Joshua T. Close , Jason David Katz , Joon Jung , Scott Peterson , Phieng Siliphaivanh , Tony Siu , Graham Frank Smith , Luis E. Torres , Hyun Chong Woo , Jonathan R. Young , Hongjun Zhang
发明人: Jason Brubaker , Matthew Lloyd Childers , Matthew Christopher , Joshua T. Close , Jason David Katz , Joon Jung , Scott Peterson , Phieng Siliphaivanh , Tony Siu , Graham Frank Smith , Luis E. Torres , Hyun Chong Woo , Jonathan R. Young , Hongjun Zhang
IPC分类号: C07D231/38 , C07D405/04 , C07D401/14 , C07D401/04 , C07D403/04 , C07D405/08 , C07D403/12 , C07D401/12 , C07D403/08 , C07D405/12 , C07D409/12 , C07D413/12 , C07D401/06 , C07D403/06 , C07D405/06 , C07D405/14 , C07D409/04 , C07D413/14 , C07D417/14
CPC分类号: C07D405/08 , C07D231/38 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/08 , C07D403/12 , C07D405/04 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/04 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/14
摘要: The instant invention provides compounds of formula I which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.
摘要翻译: 本发明提供了作为JAK抑制剂的式I化合物,因此可用于治疗JAK介导的疾病如类风湿性关节炎,哮喘,COPD和癌症。
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4.CYCLOALKYL-FUSED TETRAHYDROQUINOLINES AS CRTH2 RECEPTOR MODULATORS 审中-公开
标题翻译: 作为CRTH2受体调节剂的环丙基二烯丙基四氢喹啉公开(公告)号:US20140128367A1
公开(公告)日:2014-05-08
申请号:US14126579
申请日:2012-06-14
申请人: Xianhai Huang , Jason Brubaker , Scott L. Peterson , John W. Butcher , Joshua T. Close , Michelle Martinez , Rachel Nicola MacCoss , Joon O. Jung , Phieng Siliphaivanh , Hongjun Zhang , Robert G. Aslanian , Purakkattle Johny Biju , Li Dong , Ying Huang , Kevin D. McCormick , Anandan Palani , Ning Shao , Wei Zhou
发明人: Xianhai Huang , Jason Brubaker , Scott L. Peterson , John W. Butcher , Joshua T. Close , Michelle Martinez , Rachel Nicola MacCoss , Joon O. Jung , Phieng Siliphaivanh , Hongjun Zhang , Robert G. Aslanian , Purakkattle Johny Biju , Li Dong , Ying Huang , Kevin D. McCormick , Anandan Palani , Ning Shao , Wei Zhou
IPC分类号: C07D221/16 , A61K31/5377 , C07D401/12 , A61K31/506 , A61K31/501 , A61K31/473 , C07D401/10
CPC分类号: C07D221/16 , A61K31/473 , A61K31/501 , A61K31/506 , A61K31/5377 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/12 , C07D405/06 , C07D405/12 , C07D409/12 , C07D413/04 , C07D413/12 , C07D417/10 , C07D417/12
摘要: The invention provides certain cycloalkyl-fused tetrahydroquinolines of the Formula (I), and their pharmaceutically acceptable salts and esters, wherein R1, R2, R7, R8a, E, Y, Z, n, u, and t are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions associated with uncontrolled or inappropriate stimulation of CRTH2 function.
摘要翻译: 本发明提供一些式(I)的环烷基稠合的四氢喹啉及其药学上可接受的盐和酯,其中R1,R2,R7,R8a,E,Y,Z,n,u和t如本文所定义。 本发明还提供包含这些化合物的药物组合物,以及使用该化合物治疗与不受控制或不适当刺激CRTH2功能相关的疾病或病症的方法。
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5.CYCLOALKYL-FUSED TETRAHYDROQUINOLINES AS CRTH2 RECEPTOR MODULATORS 有权
标题翻译: 作为CRTH2受体调节剂的环丙基二烯丙基四氢喹啉公开(公告)号:US20120329743A1
公开(公告)日:2012-12-27
申请号:US13523354
申请日:2012-06-14
申请人: Xianhai Huang , Jason Brubaker , Scott L. Peterson , John W. Butcher , Joshua T. Close , Michelle Martinez , Rachel Nicola MacCoss , Joon O. Jung , Phieng Siliphaivanh , Hongjun Zhang , Robert G. Aslanian , Purakkattle Johny Biju , Li Dong , Ying Huang , Kevin D. McCormick , Anandan Palani , Ning Shao , Wei Zhou
发明人: Xianhai Huang , Jason Brubaker , Scott L. Peterson , John W. Butcher , Joshua T. Close , Michelle Martinez , Rachel Nicola MacCoss , Joon O. Jung , Phieng Siliphaivanh , Hongjun Zhang , Robert G. Aslanian , Purakkattle Johny Biju , Li Dong , Ying Huang , Kevin D. McCormick , Anandan Palani , Ning Shao , Wei Zhou
IPC分类号: C07D221/16 , C07D413/10 , A61K31/5377 , C07D401/10 , A61P11/00 , A61K31/501 , C07H15/26 , A61K31/706 , A61P11/06 , A61P37/08 , A61K31/473 , A61K31/506
CPC分类号: C07D221/16 , A61K31/473 , A61K31/501 , A61K31/506 , A61K31/5377 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/12 , C07D405/06 , C07D405/12 , C07D409/12 , C07D413/04 , C07D413/12 , C07D417/10 , C07D417/12
摘要: The invention provides certain cycloalkyl-fused tetrahydroquinolines of the Formula (I), and their pharmaceutically acceptable salts and esters, wherein R1, R2, R7, R8, R8a, E, Y, Z, n, u, and t are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions associated with uncontrolled or inappropriate stimulation of CRTH2 function.
摘要翻译: 本发明提供一些式(I)的环烷基稠合的四氢喹啉及其药学上可接受的盐和酯,其中R1,R2,R7,R8,R8a,E,Y,Z,n,u和t如本文所定义 。 本发明还提供包含这些化合物的药物组合物,以及使用该化合物治疗与不受控制或不适当刺激CRTH2功能相关的疾病或病症的方法。
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6.
公开(公告)号:US08592383B2
公开(公告)日:2013-11-26
申请号:US13523354
申请日:2012-06-14
申请人: Xianhai Huang , Jason Brubaker , Scott L. Peterson , John W. Butcher , Joshua T. Close , Michelle Martinez , Rachel Nicola MacCoss , Joon O. Jung , Phieng Siliphaivanh , Hongjun Zhang , Robert G. Aslanian , Purakkattle Johny Biju , Li Dong , Ying Huang , Kevin D. McCormick , Anandan Palani , Ning Shao , Wei Zhou
发明人: Xianhai Huang , Jason Brubaker , Scott L. Peterson , John W. Butcher , Joshua T. Close , Michelle Martinez , Rachel Nicola MacCoss , Joon O. Jung , Phieng Siliphaivanh , Hongjun Zhang , Robert G. Aslanian , Purakkattle Johny Biju , Li Dong , Ying Huang , Kevin D. McCormick , Anandan Palani , Ning Shao , Wei Zhou
IPC分类号: C07D221/16 , C07D401/10 , C07D413/10 , A61K31/473 , A61K31/501 , A61K31/506 , A61K31/5377 , A61K31/706 , A61P11/00 , A61P11/06 , A61P37/08 , C07H15/26
CPC分类号: C07D221/16 , A61K31/473 , A61K31/501 , A61K31/506 , A61K31/5377 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/12 , C07D405/06 , C07D405/12 , C07D409/12 , C07D413/04 , C07D413/12 , C07D417/10 , C07D417/12
摘要: The invention provides certain cycloalkyl-fused tetrahydroquinolines of the Formula (I), and their pharmaceutically acceptable salts and esters, wherein R1, R2, R7, R8, R8a, E, Y, Z, n, u, and t are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions associated with uncontrolled or inappropriate stimulation of CRTH2 function.
摘要翻译: 本发明提供一些式(I)的环烷基稠合的四氢喹啉及其药学上可接受的盐和酯,其中R1,R2,R7,R8,R8a,E,Y,Z,n,u和t如本文所定义 。 本发明还提供包含这些化合物的药物组合物,以及使用该化合物治疗与不受控制或不适当刺激CRTH2功能相关的疾病或病症的方法。
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7.
公开(公告)号:US08962608B2
公开(公告)日:2015-02-24
申请号:US14345976
申请日:2012-09-21
申请人: Jason Brubaker , Christopher Dinsmore , Dawn Marie Hoffman , Joon Jung , Duan Liu , Scott Peterson , Tony Siu , Luis E. Torres , Hongjun Zhang , Zhongyong Wei , Feng Shi
发明人: Jason Brubaker , Christopher Dinsmore , Dawn Marie Hoffman , Joon Jung , Duan Liu , Scott Peterson , Tony Siu , Luis E. Torres , Hongjun Zhang , Zhongyong Wei , Feng Shi
IPC分类号: A61K31/397 , A61K31/5377 , A61K31/501 , A61K31/497 , A61K31/415 , C07D231/38 , C07D403/08 , C07D403/12 , C07D405/08 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12 , C07D413/12 , C07D401/04 , C07D403/04 , C07D405/04 , C07D401/06 , C07D403/06 , C07D405/06 , C07D405/14 , C07D409/04 , C07D413/14 , C07D417/14
CPC分类号: C07D405/08 , C07D231/38 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/08 , C07D403/12 , C07D405/04 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/04 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/14
摘要: The instant invention provides compounds of formula I which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.
摘要翻译: 本发明提供了作为JAK抑制剂的式I化合物,因此可用于治疗JAK介导的疾病如类风湿性关节炎,哮喘,COPD和癌症。
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8.CYCLOALKYL NITRILE PYRAZOLO PYRIDONES AS JANUS KINASE INHIBITORS 有权
标题翻译: 甘氨酸激酶抑制剂CYCLOALKYL NITRILE PYRAZOLO PYRIDONES公开(公告)号:US20160280704A1
公开(公告)日:2016-09-29
申请号:US14778019
申请日:2014-03-19
申请人: Matthew Lloyd Childers , Christopher Dinsmore , Peter Fuller , David Guerin , Jason David Katz , Qinglin Pu , Mark E. Scott , Christopher F. Thompson , Hongjun Zhang , Danielle Falcone , Luis Torres , Jason Brubaker , Hongbo Zeng , Jiaqiang Cai , Xiaoxing Du , Chonggang Wang , Yunfeng Bai , Norman Kong , Yumei Liu , Zhixiang Zheng , Merck Sharp & Dohme Corp.
发明人: Matthew Lloyd Childers , Christopher Dinsmore , Peter Fuller , David Guerin , Jason David Katz , Qinglin Pu , Mark E. Scott , Christopher F. Thompson , Hongjun Zhang , Danielle Falcone , Luis Torres , Jason Brubaker , Hongbo Zeng , Jiaqiang Cai , Xiaoxing Du , Chonggang Wang , Yunfeng Bai , Norman Kong , Yumei Liu , Zhixiang Zheng
IPC分类号: C07D471/04 , C07D519/00
CPC分类号: C07D471/04 , C07D519/00
摘要: Compounds of formula I are provided, which are JAK inhibitors and are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.
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公开(公告)号:US10442819B2
公开(公告)日:2019-10-15
申请号:US15532549
申请日:2015-12-01
申请人: Christian Fischer , Stephane L. Bogen , Matthew L. Childers , Francesc Xavier Fradera Llinas , J. Michael Ellis , Sara Esposite , Qingmei Hong , Chunhui Huang , Alexander J. Kim , John W. Lampe , Michelle R. Machacek , Daniel R. McMasters , Ryan D. Otte , Dann L. Parker, Jr. , Michael Reutershan , Nunzio Sciammetta , Pengcheng P. Shao , David L. Sloman , Feroze Ujjainwalla , Catherine White , Zhicai Wu , Yang Yu , Kake Zhao , Craig Gibeau , Tesfaye Biftu , Purakkattle Biju , Lei Chen , Joshua Close , Peter H. Fuller , Xianhai Huang , Min K. Park , Valdimir Simov , David J. Witter , Hongjun Zhang
发明人: Christian Fischer , Stephane L. Bogen , Matthew L. Childers , Francesc Xavier Fradera Llinas , J. Michael Ellis , Sara Esposite , Qingmei Hong , Chunhui Huang , Alexander J. Kim , John W. Lampe , Michelle R. Machacek , Daniel R. McMasters , Ryan D. Otte , Dann L. Parker, Jr. , Michael Reutershan , Nunzio Sciammetta , Pengcheng P. Shao , David L. Sloman , Feroze Ujjainwalla , Catherine White , Zhicai Wu , Yang Yu , Kake Zhao , Craig Gibeau , Tesfaye Biftu , Purakkattle Biju , Lei Chen , Joshua Close , Peter H. Fuller , Xianhai Huang , Min K. Park , Valdimir Simov , David J. Witter , Hongjun Zhang
IPC分类号: A61K31/351 , A61K31/4353 , A61K31/5355 , A61K31/551 , C07D471/04 , C07D471/14 , C07D498/08 , C07D471/08 , C07D498/04 , C07D498/10 , A01N43/00
摘要: The present invention is directed to tricyclic compounds of formula (I) which are inhibitors of one or more mutant IDH enzymes: (I). The present invention is also directed to uses of the tricyclic compounds described herein in the potential treatment or prevention of cancers in which one or more mutant IDH enzymes are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such cancers.
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10.
公开(公告)号:US20220235028A1
公开(公告)日:2022-07-28
申请号:US17615718
申请日:2020-06-08
申请人: Yongxin HAN , Yongqi DENG , Hua ZHOU , Meredeth A. MCGOWAN , Hongjun ZHANG , Wensheng YU , Brett A. HOPKINS , Xavier FRADERA , Nunzio SCIAMMETTA , Merck Sharp & Dohme Corp.
发明人: Yongxin Han , Yongqi Deng , Hua Zhou , Meredeth A. McGowan , Hongjun Zhang , Wensheng Yu , Brett A. Hopkins , Xavier Fradera , Nunzio Sciammetta
IPC分类号: C07D401/06 , C07D401/08 , C07D471/04 , C07D519/00
摘要: Disclosed herein is a compound of formula (I), or a pharmaceutically acceptable salt thereof: Also disclosed herein are uses of the compounds disclosed herein in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising a compound disclosed herein. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder.
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