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公开(公告)号:US09023865B2
公开(公告)日:2015-05-05
申请号:US14353381
申请日:2012-10-25
申请人: Jongwon Lim , Elizabeth Helen Kelley , Joey L. Methot , Hua Zhou , Alessia Petrocchi , Umar Faruk Mansoor , Christian Fischer , Brendan O'Boyle , David Joseph Guerin , Corey E. Bienstock , Christopher W. Boyce , Matthew H. Daniels , Danielle Falcone , Ronald D. Ferguson , Salem Fevrier , Xianhai Huang , Kathryn Ann Lipford , David L. Sloman , Kevin Wilson , Wei Zhou , David Witter , Milana M. Maletic , Phieng Siliphaivanh
发明人: Jongwon Lim , Elizabeth Helen Kelley , Joey L. Methot , Hua Zhou , Alessia Petrocchi , Umar Faruk Mansoor , Christian Fischer , Brendan O'Boyle , David Joseph Guerin , Corey E. Bienstock , Christopher W. Boyce , Matthew H. Daniels , Danielle Falcone , Ronald D. Ferguson , Salem Fevrier , Xianhai Huang , Kathryn Ann Lipford , David L. Sloman , Kevin Wilson , Wei Zhou , David Witter , Milana M. Maletic , Phieng Siliphaivanh
IPC分类号: C07D401/14 , A61K31/437 , C07D471/04 , C07D519/00 , A61K31/444 , A61K31/4545 , A61K31/4709 , A61K31/496 , A61K31/501 , A61K31/506 , A61K31/5377 , A61K45/06
CPC分类号: C07D471/04 , A61K31/437 , A61K31/444 , A61K31/4545 , A61K31/4709 , A61K31/496 , A61K31/501 , A61K31/506 , A61K31/5377 , A61K45/06 , C07D519/00
摘要: Disclosed are the ERK inhibitors of formula (1): and the pharmaceutically acceptable salts thereof. Also disclosed are methods of treating cancer using the compounds of formula (1).
摘要翻译: 公开了式(1)的ERK抑制剂及其药学上可接受的盐。 还公开了使用式(1)的化合物治疗癌症的方法。
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公开(公告)号:US20150266895A1
公开(公告)日:2015-09-24
申请号:US14431462
申请日:2013-09-26
申请人: Kevin J. WILSON , David J. WITTER , Phieng SILIPHAIVANH , Kathryn KIPFORD , David SLOMAN , Danielle FALCONE , Brendan O'BOYLE , Umar Faruk MANSOOR , Jongwon LIM , Joey L. METHOT , Christopher BOYCE , Lei CHEN , Matthew H. DANIELS , Salem FEVRIER , Xianhai HUANG , Ravi KURUKULASURIYA , Ling TONG , Wei ZHOU , Joseph KOZLOWSKI , Milana M. MALETIC , Bidhan A. SHINKRE , Jayanth Thiruvellore THATAI , Raman Kumar BAKSHI , Ganesh Babu KARUNAKARAN , MERCK SHARP & DOHME CORP.
发明人: Kevin J. Wilson , David J. Witter , Phieng Siliphaivanh , Kathryn Lipford , David Sloman , Danielle Falcone , Brendan O'Boyle , Umar Faruk Mansoor , Jongwon Lim , Joey L. Methot , Christopher Boyce , Lei Chen , Matthew H. Daniels , Salem Fevrier , Xianhai Huang , Ravi Kurukulasuriya , Ling Tong , Wei Zhou , Joseph Kozlowski , Milana M. Maletic , Bidhan A. Shinkre , Jayanth Thiruvellore Thatai , Raman Kumar Bakshi , Ganesh Babu Karunakaran
IPC分类号: C07D498/18 , A61K31/437 , A61K31/5377 , A61K31/496 , A61K45/06 , A61K31/4375 , C07D498/14 , A61K31/553 , C07D519/00 , C07D471/04 , C07D471/14
CPC分类号: C07D498/18 , A61K31/437 , A61K31/4375 , A61K31/496 , A61K31/5377 , A61K31/553 , A61K45/06 , C07D471/04 , C07D471/14 , C07D471/16 , C07D498/14 , C07D498/16 , C07D519/00 , A61K2300/00
摘要: Disclosed are the ERK inhibitors of formula (1): and the pharmaceutically acceptable salts thereof. Also disclosed are methods of treating cancer using the compounds of formula (1).
摘要翻译: 公开了式(1)的ERK抑制剂及其药学上可接受的盐。 还公开了使用式(1)的化合物治疗癌症的方法。
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公开(公告)号:US20150258074A1
公开(公告)日:2015-09-17
申请号:US14431485
申请日:2013-09-26
申请人: Kevin J. WILSON , David J. WITTER , Matthew H. DANIELS , Angie R. ANGELES , Phieng SILIPHAIVANH , David L. SLOMAN , Brendan O'BOYLE , Danielle FALCONE , Catherine WHITE , Ron FERGUSON , Wei ZHOU , Kathryn LIPFORD , Umar Faruk MANSOOR , Salem FEVRIRE , Xianhai HUANG , Ravi KURUKULASURIYA , Judson E. RICHARD , Shuyi TANG , Christopher BOYCE , Joseph KOZLOWSKI , Raman Kumar BAKSHI , Ganesh Babu UNAKARAN , Merck Sharp & Dohme Corp.
发明人: Kevin J. Wilson , David J. Witter , Matthew H. Daniels , Angie R. Angeles , Phieng Siliphaivanh , David Sloman , Brendan O'Boyle , Danielle Falcone , Catherine White , Ron Ferguson , Wei Zhou , Kathryn Lipford , Umar Faruk Mansoor , Salem Fevrier , Xianhai Huang , Ravi Kurukulasuriya , Judson E. Richard , Shuyi Tang , Christopher Boyce , Joseph Kozlowski , Raman Kumar Bakshi , Ganesh Babu Karunakaran
IPC分类号: A61K31/437 , A61K45/06 , A61K31/4545 , C07D471/04
CPC分类号: A61K31/437 , A61K31/4545 , A61K45/06 , C07D471/04
摘要: Disclosed are the ERK inhibitors of formula (1.0), having a pyrazolopyridine base structure, and the pharmaceutically acceptable salts thereof. Also disclosed are methods of treating cancer using the compounds of formula (1.0).
摘要翻译: 公开了具有吡唑并吡啶基结构的式(1.0)的ERK抑制剂及其药学上可接受的盐。 还公开了使用式(1.0)化合物治疗癌症的方法。
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公开(公告)号:US20160068532A1
公开(公告)日:2016-03-10
申请号:US14787280
申请日:2014-04-25
申请人: Jongwon LIM , Xianhai HUANG , Ronald D. FERGUSON , Wei ZHOU , Christopher W. BOYCE , Phieng SILIPHAIVANH , David J. WITTER , Milana M. MALETIC , Joseph A. KOZLOWSKI , Kevin J. WILSON , MERCK SHARP & DOHME CORP.
发明人: Jongwon Lim , Xianhai Huang , Ronald D. Ferguson , Wei Zhou , Christopher W. Boyce , Phieng Siliphaivanh , David J. Witter , Milana M. Maletic , Joseph A. Kozlowski , Kevin J. Wilson
IPC分类号: C07D487/04 , C07D471/14 , C07D471/04
CPC分类号: C07D487/04 , C07D471/04 , C07D471/14 , C07D519/00
摘要: Disclosed are the ERK inhibitors of formula (I) and the pharmaceutically acceptable salts thereof. Also disclosed are methods of treating cancer using the compounds of formula (I). This invention also provides a pharmaceutical composition comprising an effective amount of at least one compound of formula (I) and a pharmaceutically acceptable carrier. This invention also provides a pharmaceutical composition comprising an effective amount of at least one compound of formula (I) and an effective amount of at least one other pharmaceutically active ingredient (such as, for example, a chemotherapeutic agent), and a pharmaceutically acceptable carrier. This invention also provides a method of inhibiting ERK (i.e., inhibiting the activity of ERK2) in a patient in need of such treatment comprising administering to said patient an effective amount of at least one compound of formula (I).
摘要翻译: 公开了式(I)的ERK抑制剂及其药学上可接受的盐。 还公开了使用式(I)化合物治疗癌症的方法。 本发明还提供了包含有效量的至少一种式(I)化合物和药学上可接受的载体的药物组合物。 本发明还提供一种药物组合物,其包含有效量的至少一种式(I)化合物和有效量的至少一种其它药学活性成分(例如化学治疗剂)和药学上可接受的载体 。 本发明还提供了在需要这种治疗的患者中抑制ERK(即,抑制ERK2的活性)的方法,包括向所述患者施用有效量的至少一种式(I)化合物。
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5.
公开(公告)号:US20130303517A1
公开(公告)日:2013-11-14
申请号:US13996361
申请日:2011-12-19
申请人: Christopher W. Boyce , Sylvia Joanna Degrado , Xiao Chen , Jun Qin , Robert D. Mazzola, JR. , Younong Yu , Kevin D. McCormick , Anandan Palani , Dong Xiao , Robert George Aslanian , Jie Wu , Ashwin Umesh Rao , Phieng Siliphaivanh , Joey L. Methot , Hongjun Zhang , Elizabeth Helen Kelley , William Colby Brown , Qin Jiang , Jolicia Polivina Gauuan , Andrew J. Leyhane , Purakkattle Johny Biju , Pawan K. Dhondi , Li Dong , Salem Fevrier , Xianhai Huang , Henry M. Vaccaro
发明人: Christopher W. Boyce , Sylvia Joanna Degrado , Xiao Chen , Jun Qin , Robert D. Mazzola, JR. , Younong Yu , Kevin D. McCormick , Anandan Palani , Dong Xiao , Robert George Aslanian , Jie Wu , Ashwin Umesh Rao , Phieng Siliphaivanh , Joey L. Methot , Hongjun Zhang , Elizabeth Helen Kelley , William Colby Brown , Qin Jiang , Jolicia Polivina Gauuan , Andrew J. Leyhane , Purakkattle Johny Biju , Pawan K. Dhondi , Li Dong , Salem Fevrier , Xianhai Huang , Henry M. Vaccaro
IPC分类号: C07D241/42 , C07D401/12 , C07D403/06 , C07D471/04 , A61K31/4985 , C07D471/10 , C07D405/12 , C07D401/14 , A61K31/506 , A61K31/55 , C07D417/12 , C07D498/04 , C07D491/107 , A61K45/06 , A61K31/498
CPC分类号: C07D241/42 , A61K31/498 , A61K31/4985 , A61K31/506 , A61K31/55 , A61K45/06 , C07D241/38 , C07D241/44 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/12 , C07D403/14 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D451/02 , C07D471/04 , C07D471/08 , C07D471/10 , C07D487/04 , C07D487/08 , C07D491/048 , C07D491/107 , C07D498/04 , C07D498/10
摘要: The invention provides certain quinoxalines and aza-quinoxalines of the Formula (I), and their pharmaceutically acceptable salts, wherein J1, J2, R1, R2, R3, R22, Ra, Rb, Rc, Rd, X, Y, b, n, and q 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: 本发明提供了式(I)的某些喹喔啉和氮杂 - 喹喔啉及其药学上可接受的盐,其中J1,J2,R1,R2,R3,R22,Ra,Rb,Rc,Rd,X,Y,b,n ,和q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:US09469615B2
公开(公告)日:2016-10-18
申请号:US13996361
申请日:2011-12-19
申请人: Christopher W. Boyce , Sylvia Joanna Degrado , Xiao Chen , Jun Qin , Robert D. Mazzola, Jr. , Younong Yu , Kevin D. McCormick , Anandan Palani , Dong Xiao , Robert George Aslanian , Jie Wu , Ashwin Umesh Rao , Phieng Siliphaivanh , Joey L. Methot , Hongjun Zhang , Elizabeth Helen Kelley , William Colby Brown , Qin Jiang , Jolicia Polivina Gauuan , Andrew J. Leyhane , Purakkattle Johny Biju , Pawan K. Dhondi , Li Dong , Salem Fevrier , Xianhai Huang , Henry M. Vaccaro
发明人: Christopher W. Boyce , Sylvia Joanna Degrado , Xiao Chen , Jun Qin , Robert D. Mazzola, Jr. , Younong Yu , Kevin D. McCormick , Anandan Palani , Dong Xiao , Robert George Aslanian , Jie Wu , Ashwin Umesh Rao , Phieng Siliphaivanh , Joey L. Methot , Hongjun Zhang , Elizabeth Helen Kelley , William Colby Brown , Qin Jiang , Jolicia Polivina Gauuan , Andrew J. Leyhane , Purakkattle Johny Biju , Pawan K. Dhondi , Li Dong , Salem Fevrier , Xianhai Huang , Henry M. Vaccaro
IPC分类号: C07D241/38 , C07D241/42 , A61K31/498 , A61K31/506 , A61K31/4985 , A61K31/55 , A61K45/06 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D451/02 , C07D471/08 , C07D487/04 , C07D487/08 , C07D403/06 , C07D471/04 , C07D471/10 , C07D491/107 , C07D498/04 , C07D403/12 , C07D401/06 , C07D403/14 , C07D409/14 , C07D413/06 , C07D241/44 , C07D417/14 , C07D491/048 , C07D498/10
CPC分类号: C07D241/42 , A61K31/498 , A61K31/4985 , A61K31/506 , A61K31/55 , A61K45/06 , C07D241/38 , C07D241/44 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/12 , C07D403/14 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D451/02 , C07D471/04 , C07D471/08 , C07D471/10 , C07D487/04 , C07D487/08 , C07D491/048 , C07D491/107 , C07D498/04 , C07D498/10
摘要: The invention provides certain quinoxalines and aza-quinoxalines of the Formula (I), and their pharmaceutically acceptable salts, wherein J1, J2, R1, R2, R3, R22, Ra, Rb, Rc, Rd, X, Y, b, n, and q 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.
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公开(公告)号:US08927559B2
公开(公告)日:2015-01-06
申请号:US13878654
申请日:2011-10-06
申请人: Robert G. Aslanian , Christopher W. Boyce , Robert D. Mazzola, Jr. , Brian A. McKittrick , Kevin D. McCormick , Anandan Palani , Jun Qin , Haiqun Tang , Dong Xiao , Younong Yu , John P. Caldwell , Elizabeth Helen Kelley , Hongjun Zhang , Phieng Siliphaivanh , Rachel N. MacCoss , Joey L. Methot , Jolicia Polivina Gauuan , Qin Jiang , Andrew J. Leyhane , Purakkattle Johny Biju , Li Dong , Xianhai Huang , Ning Shao , Wei Zhou , Pawan K. Dhondi , Ashwin U. Rao
发明人: Robert G. Aslanian , Christopher W. Boyce , Robert D. Mazzola, Jr. , Brian A. McKittrick , Kevin D. McCormick , Anandan Palani , Jun Qin , Haiqun Tang , Dong Xiao , Younong Yu , John P. Caldwell , Elizabeth Helen Kelley , Hongjun Zhang , Phieng Siliphaivanh , Rachel N. MacCoss , Joey L. Methot , Jolicia Polivina Gauuan , Qin Jiang , Andrew J. Leyhane , Purakkattle Johny Biju , Li Dong , Xianhai Huang , Ning Shao , Wei Zhou , Pawan K. Dhondi , Ashwin U. Rao
IPC分类号: A01N43/54 , A61K31/517 , C07D239/72 , C07D401/00
CPC分类号: C07D239/91 , A61K31/517 , A61K31/5395 , A61K31/55 , A61K45/06 , C07D401/10 , C07D401/14 , C07D403/04 , C07D403/10 , C07D403/14 , C07D405/10 , C07D413/04 , C07D413/10 , C07D413/14 , C07D417/04 , C07D417/10 , C07D471/04 , C07D498/10
摘要: This application provides for compounds of the formula Formula I or a pharmaceutically acceptable salt thereof, wherein the individual variables are defined herein, as well as processes to prepare these compounds, pharmaceutical compositions comprising the same and their use in treating disease state associated with the CRTH2 receptor.
摘要翻译: 本申请提供式I化合物或其药学上可接受的盐,其中各个变量在本文中定义,以及制备这些化合物的方法,包含其的药物组合物及其用于治疗与CRTH2相关的疾病状态 受体。
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公开(公告)号:US20170267695A1
公开(公告)日:2017-09-21
申请号:US15531771
申请日:2015-12-10
申请人: Phieng Siliphaivanh , David L. Sloman , David Witter , Umar Faruk Mansoor , Joseph Kozlowski , Ziping Liu , Jianmin Fu , Zhilong Wan , Wei Liu , Yimin Qian , Xianhai Huang
发明人: Phieng Siliphaivanh , David L. Sloman , David Witter , Umar Faruk Mansoor , Joseph Kozlowski , Ziping Liu , Jianmin Fu , Zhilong Wan , Wei Liu , Yimin Qian , Xianhai Huang
IPC分类号: C07D498/18 , C07D471/22 , C07D471/18
CPC分类号: C07D498/18 , A61K31/437 , A61K31/444 , C07D471/18 , C07D471/22
摘要: The present invention provides a compound of Formula (I) or the pharmaceutically acceptable salts, esters, and prodrugs thereof, which are ERK2 inhibitors. The invention also provides a method of inhibiting ERK2 in a patient in need of such treatment comprising administering to said patient an effective amount of at least one compound of Formula (I). The invention also provides a method for treating cancer in a patient in need of such treatment, said method comprising administering to said patient an effective amount of at least one compound of Formula (I).
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9.BIARYL-SPIROAMINOOXAZOLINE ANALOGUES AS ALPHA 2C ADRENERGIC RECEPTOR MODULATORS 失效
标题翻译: 作为ALPHA 2C ADRENERGIC受体调节剂的BIARYL-SPIROAMINOOXAZOLINE ANALOGUES公开(公告)号:US20110251207A1
公开(公告)日:2011-10-13
申请号:US13122679
申请日:2009-10-06
申请人: Kevin D. McCormick , Li Dong , Christopher W. Boyce , Manuel de Lera Ruiz , Salem Fevrier , Jie Wu , Junying Zheng , Younong Yu , Jianhua Chao , Walter S. Won , Ashwin U. Rao , Rongze Kuang , Pauline C. Ting , Xianhai Huang , Ning Shao , Adandan Palani , Michael Y. Berlin , Robert G. Aslanian
发明人: Kevin D. McCormick , Li Dong , Christopher W. Boyce , Manuel de Lera Ruiz , Salem Fevrier , Jie Wu , Junying Zheng , Younong Yu , Jianhua Chao , Walter S. Won , Ashwin U. Rao , Rongze Kuang , Pauline C. Ting , Xianhai Huang , Ning Shao , Adandan Palani , Michael Y. Berlin , Robert G. Aslanian
IPC分类号: A61K31/501 , A61K31/506 , A61K31/4439 , A61K31/427 , A61K31/497 , C07D263/52 , A61K31/423 , C07D235/02 , A61K31/4184 , C07D405/10 , C07D409/10 , A61K31/422 , C07D403/10 , A61P27/06 , A61P25/22 , A61P21/02 , A61P9/00 , A61P25/18 , A61P25/06 , A61P25/28 , A61P3/10 , A61P11/02 , C07D413/10
CPC分类号: A61K31/5377 , A61K31/437 , A61K31/501 , A61K31/506 , A61K31/537 , C07D235/02 , C07D263/52 , C07D401/10 , C07D403/10 , C07D405/10 , C07D409/10 , C07D413/10 , C07D413/14 , C07D417/10 , C07D471/04 , C07D498/10 , C07D519/00
摘要: In its many embodiments, the present invention provides a novel class of biaryi spiroaminooxazoline analogues as modulators of α2C adrenergic receptor agonists, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the α2C adrenergic receptors using such compounds or pharmaceutical compositions.
摘要翻译: 在其许多实施方案中,本发明提供了一类新颖的作为α2C肾上腺素能受体激动剂的调节剂的生物二螺吡喃恶唑啉类似物,制备这些化合物的方法,含有一种或多种这类化合物的药物组合物,制备包含一种或多种这类化合物的药物制剂的方法 以及使用这些化合物或药物组合物治疗,预防,抑制或改善与α2C肾上腺素能受体相关的一种或多种病症的方法。
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10.Biaryl-spiroaminooxazoline analogues as alpha 2C adrenergic receptor modulators 失效
标题翻译: 双芳基 - 螺氨基恶唑啉类似物作为α2C肾上腺素能受体调节剂公开(公告)号:US08324213B2
公开(公告)日:2012-12-04
申请号:US13122679
申请日:2009-10-06
申请人: Kevin D. McCormick , Li Dong , Christopher W. Boyce , Manuel de Lera Ruiz , Salem Fevrier , Jie Wu , Junying Zheng , Youngong Yu , Jianhua Chao , Walter S. Won , Ashwin U. Rao , Rongze Kuang , Pauline C. Ting , Xianhai Huang , Ning Shao , Anandan Palani , Michael Y. Berlin , Robert G. Aslanian
发明人: Kevin D. McCormick , Li Dong , Christopher W. Boyce , Manuel de Lera Ruiz , Salem Fevrier , Jie Wu , Junying Zheng , Youngong Yu , Jianhua Chao , Walter S. Won , Ashwin U. Rao , Rongze Kuang , Pauline C. Ting , Xianhai Huang , Ning Shao , Anandan Palani , Michael Y. Berlin , Robert G. Aslanian
IPC分类号: A61K31/501 , A61K31/497 , A61K31/506 , A61K31/4439 , A61K31/427 , A61K31/423 , C07D235/02 , C07D405/02 , C07D409/02 , C07D413/02 , C07D263/52
CPC分类号: A61K31/5377 , A61K31/437 , A61K31/501 , A61K31/506 , A61K31/537 , C07D235/02 , C07D263/52 , C07D401/10 , C07D403/10 , C07D405/10 , C07D409/10 , C07D413/10 , C07D413/14 , C07D417/10 , C07D471/04 , C07D498/10 , C07D519/00
摘要: In its many embodiments, the present invention provides a novel class of biaryi spiroaminooxazoline analogues as modulators of α2C adrenergic receptor agonists, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the α2C adrenergic receptors using such compounds or pharmaceutical compositions.
摘要翻译: 在其许多实施方案中,本发明提供了一类新颖的作为α2C肾上腺素能受体激动剂的调节剂的生物二螺吡喃恶唑啉类似物,制备这些化合物的方法,含有一种或多种这类化合物的药物组合物,制备包含一种或多种这类化合物的药物制剂的方法 以及使用这些化合物或药物组合物治疗,预防,抑制或改善与α2C肾上腺素能受体相关的一种或多种病症的方法。
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