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公开(公告)号:US09227971B2
公开(公告)日:2016-01-05
申请号:US13520274
申请日:2011-01-18
申请人: M. Arshad Siddiqui , Yang Nan , Mehul F. Patel , Panduranga Adulla P. Reddy , Umar Faruk Mansoor , Zhaoyang Meng , Lalanthi Dilrukshi Vitharana , Lianyun Zhao , Amit K. Mandal , Duan Liu , Shuyi Tang , Andrew McRiner , David B. Belanger , Patrick J. Curran , Chaoyang Dai , Angie R. Angeles , Liping Yang , Matthew Hersh Daniels
发明人: M. Arshad Siddiqui , Yang Nan , Mehul F. Patel , Panduranga Adulla P. Reddy , Umar Faruk Mansoor , Zhaoyang Meng , Lalanthi Dilrukshi Vitharana , Lianyun Zhao , Amit K. Mandal , Duan Liu , Shuyi Tang , Andrew McRiner , David B. Belanger , Patrick J. Curran , Chaoyang Dai , Angie R. Angeles , Liping Yang , Matthew Hersh Daniels
IPC分类号: C07D487/04 , A61K31/519 , C07D471/08 , C07D498/08 , C07D491/147 , C07D487/08 , C07D513/08 , C07D519/00 , A61P35/00
CPC分类号: C07D471/08 , C07D487/04 , C07D487/08 , C07D491/147 , C07D498/08 , C07D513/08 , C07D519/00
摘要: The present invention provides Pyrazolopyrimidine Compounds of Formula (I): wherein L, T, Z, U, V, W, R3, R6, R7, R8, and m are as defined herein, and pharmaceutically acceptable salts of such Pyrazolopyrimidine Compounds. The Pyrazolopyrimidine Compounds are useful in the treatment of cancer and other diseases or disorders wherein mTOR is deregulated.
摘要翻译: 本发明提供式(I)的吡唑并嘧啶化合物:其中L,T,Z,U,V,W,R 3,R 6,R 7,R 8和m如本文所定义,以及这些吡唑并嘧啶化合物的药学上可接受的盐。 吡唑并嘧啶化合物可用于治疗其中mTOR失调的癌症和其它疾病或病症。
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公开(公告)号:US20120322791A1
公开(公告)日:2012-12-20
申请号:US13520274
申请日:2011-01-18
申请人: M. Arshad Siddiqui , Yang Nan , Mehul F. Patel , Panduranga Adulla P. Reddy , Umar Faruk Mansoor , Zhaoyang Meng , Lalanthi Dilrukshi Vitharana , Lianyun Zhao , Amit K. Mandal , Duan Liu , Shuyi Tang , Andrew McRiner , David B. Belanger , Patrick J. Curran , Chaoyang Dai , Angie R. Angeles , Liping Yang , Matthew Hersh Daniels
发明人: M. Arshad Siddiqui , Yang Nan , Mehul F. Patel , Panduranga Adulla P. Reddy , Umar Faruk Mansoor , Zhaoyang Meng , Lalanthi Dilrukshi Vitharana , Lianyun Zhao , Amit K. Mandal , Duan Liu , Shuyi Tang , Andrew McRiner , David B. Belanger , Patrick J. Curran , Chaoyang Dai , Angie R. Angeles , Liping Yang , Matthew Hersh Daniels
IPC分类号: A61K31/519 , A61K31/5377 , C07D487/08 , A61K31/55 , A61P35/00 , C07D498/08 , A61K31/5386 , C07D513/08 , A61K31/547 , C07D491/147 , C07D487/04 , C07D471/08
CPC分类号: C07D471/08 , C07D487/04 , C07D487/08 , C07D491/147 , C07D498/08 , C07D513/08 , C07D519/00
摘要: The present invention provides Pyrazolopyrimidine Compounds of Formula (I): wherein L, T, Z, U, V, W, R3, R6, R7, R8, and m are as defined herein, and pharmaceutically acceptable salts of such Pyrazolopyrimidine Compounds. The Pyrazolopyrimidine Compounds are useful in the treatment of cancer and other diseases or disorders wherein mTOR is deregulated.
摘要翻译: 本发明提供式(I)的吡唑并嘧啶化合物:其中L,T,Z,U,V,W,R 3,R 6,R 7,R 8和m如本文所定义,以及这些吡唑并嘧啶化合物的药学上可接受的盐。 吡唑并嘧啶化合物可用于治疗其中mTOR失调的癌症和其它疾病或病症。
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公开(公告)号:US20130150362A1
公开(公告)日:2013-06-13
申请号:US13818177
申请日:2011-08-22
申请人: Lianyun Zhao , Duan Liu , Shuyi Tang , Amit K. Mandal , Umar Faruk Mansoor , Lalanthi Dilrukshi Vitharana , Panduranga Adulla P. Reddy , M. Arshad Siddiqui
发明人: Lianyun Zhao , Duan Liu , Shuyi Tang , Amit K. Mandal , Umar Faruk Mansoor , Lalanthi Dilrukshi Vitharana , Panduranga Adulla P. Reddy , M. Arshad Siddiqui
IPC分类号: C07D487/04 , A61K31/519 , A61K31/5377 , A61K45/06
CPC分类号: C07D487/04 , A61K31/519 , A61K31/5377 , A61K45/06
摘要: The present invention relates to certain pyrazolo[1,5-a]pyrimidine compounds of Formula (I) as inhibitors of mammalian Target Of Rapamycin (mTOR) kinase, which is also known as FRAP, RAFT, RAPT or SEP. The compounds may be used in the treatment of cancer and other disorders where mTOR is deregulated. The present invention further provides pharmaceutical compositions comprising the pyrazolo[1,5-a]pyrimidine compounds.
摘要翻译: 本发明涉及作为哺乳动物雷帕霉素靶标(mTOR)激酶的抑制剂的式(I)的吡唑并[1,5-a]嘧啶化合物,其也称为FRAP,RAFT,RAPT或SEP。 所述化合物可用于治疗其中mTOR失调的癌症和其它病症。 本发明还提供包含吡唑并[1,5-a]嘧啶化合物的药物组合物。
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公开(公告)号:US08883801B2
公开(公告)日:2014-11-11
申请号:US13818177
申请日:2011-08-22
申请人: Lianyun Zhao , Duan Liu , Shuyi Tang , Amit K. Mandal , Umar Faruk Mansoor , Lalanthi Dilrukshi Vitharana , Panduranga Adulla P. Reddy , M. Arshad Siddiqui
发明人: Lianyun Zhao , Duan Liu , Shuyi Tang , Amit K. Mandal , Umar Faruk Mansoor , Lalanthi Dilrukshi Vitharana , Panduranga Adulla P. Reddy , M. Arshad Siddiqui
IPC分类号: A61K31/519 , C07D239/70 , A61K31/5377 , C07D487/04 , A61K45/06
CPC分类号: C07D487/04 , A61K31/519 , A61K31/5377 , A61K45/06
摘要: The present invention relates to certain pyrazolo[1,5-a]pyrimidine compounds of Formula (I) as inhibitors of mammalian Target Of Rapamycin (mTOR) kinase, which is also known as FRAP, RAFT, RAPT or SEP. The compounds may be used in the treatment of cancer and other disorders where mTOR is deregulated. The present invention further provides pharmaceutical compositions comprising the pyrazolo[1,5-a]pyrimidine compounds.
摘要翻译: 本发明涉及作为哺乳动物雷帕霉素靶标(mTOR)激酶的抑制剂的式(I)的吡唑并[1,5-a]嘧啶化合物,其也称为FRAP,RAFT,RAPT或SEP。 所述化合物可用于治疗其中mTOR失调的癌症和其它病症。 本发明还提供包含吡唑并[1,5-a]嘧啶化合物的药物组合物。
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公开(公告)号:US08278337B2
公开(公告)日:2012-10-02
申请号:US12519731
申请日:2007-12-17
申请人: David B. Belanger , M. Arshad Siddiqui , Patrick J. Curran , Blake Hamann , Lianyun Zhao , Panduranga Adulla P. Reddy , Praveen K. Tadikonda , Gerald W. Shipps, Jr. , Umar Faruk Mansoor
发明人: David B. Belanger , M. Arshad Siddiqui , Patrick J. Curran , Blake Hamann , Lianyun Zhao , Panduranga Adulla P. Reddy , Praveen K. Tadikonda , Gerald W. Shipps, Jr. , Umar Faruk Mansoor
IPC分类号: A61K31/44
CPC分类号: C07D417/12 , C07D213/81 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/04 , C07D405/12 , C07D409/04 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04
摘要: Disclosed are compounds of the formula (I) wherein X is N or CH, and Y is N or CR5. Also disclosed are methods of treating JNK and ERK mediated diseases using the compounds of formula 1.0.
摘要翻译: 公开了式(I)的化合物,其中X是N或CH,Y是N或CR 5。 还公开了使用式1.0化合物治疗JNK和ERK介导的疾病的方法。
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公开(公告)号:US20100179141A1
公开(公告)日:2010-07-15
申请号:US12519731
申请日:2007-12-17
申请人: David B. Belanger , M. Arshad Siddiqui , Patrick J. Curran , Blake Hamann , Lianyun Zhao , Panduranga Adulla P. Reddy , Praveen K. Tadikonda , Gerald W. Shipps, JR. , Umar Faruk Mansoor
发明人: David B. Belanger , M. Arshad Siddiqui , Patrick J. Curran , Blake Hamann , Lianyun Zhao , Panduranga Adulla P. Reddy , Praveen K. Tadikonda , Gerald W. Shipps, JR. , Umar Faruk Mansoor
IPC分类号: A61K31/5377 , C07D417/12 , A61K31/4439 , A61K31/4545 , C07D417/14 , C07D401/12 , C07D413/14 , C07D405/12 , A61K31/444 , A61K31/502 , A61K31/497 , C07D213/81 , A61K31/44 , C07D401/14 , A61K31/506 , C07D513/04 , A61K31/517 , C07D471/04 , A61K31/496 , A61P19/02 , A61P29/00 , A61P11/06 , A61P25/28 , A61P1/00 , A61P3/10 , A61P17/06
CPC分类号: C07D417/12 , C07D213/81 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/04 , C07D405/12 , C07D409/04 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04
摘要: Disclosed are compounds of the formula (I) wherein X is N or CH, and Y is N or CR5. Also disclosed are methods of treating JNK and ERK mediated diseases using the compounds of formula 1.0.
摘要翻译: 公开了式(I)的化合物,其中X是N或CH,Y是N或CR 5。 还公开了使用式1.0化合物治疗JNK和ERK介导的疾病的方法。
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公开(公告)号:US20100298314A1
公开(公告)日:2010-11-25
申请号:US12519733
申请日:2007-12-17
申请人: Panduranga Adulla P. Reddy , M. Arshad Siddiqui , Praveen K. Tadikonda , Umar Faruk Mansoor , Gerald W. Shipps, JR. , David B. Belanger , Lianyun Zhao
发明人: Panduranga Adulla P. Reddy , M. Arshad Siddiqui , Praveen K. Tadikonda , Umar Faruk Mansoor , Gerald W. Shipps, JR. , David B. Belanger , Lianyun Zhao
IPC分类号: A61K31/5377 , C07D471/04 , A61K31/437 , A61K31/496 , A61K31/497 , A61K31/519 , A61K31/4985 , A61P29/00 , A61P19/02 , A61P11/06 , A61P17/06 , A61P3/10 , A61P9/00 , A61P37/00
CPC分类号: C07D471/04 , C07D487/04
摘要: Disclosed are substituted imidazo[1,2-a]pyridines, imidazo[1,2-a]pyrazines, imidazo[1,2-c]pyrimidines and imidazo[1,2-d]triazines compounds of the formula: (1.0) Also disclosed are methods for treating JNK1 and ERK mediated diseases using the compounds of formula 1.0.
摘要翻译: 公开了下式的取代咪唑并[1,2-a]吡啶,咪唑并[1,2-a]吡嗪,咪唑并[1,2-c]嘧啶和咪唑并[1,2-d]三嗪化合物:(1.0) 还公开了使用式1.0化合物治疗JNK1和ERK介导的疾病的方法。
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公开(公告)号:US20110123435A1
公开(公告)日:2011-05-26
申请号:US12738537
申请日:2008-10-16
申请人: M. Arshad Siddiqui , Chaoyang Dai , Umar Faruk Mansoor , Liping Yang , Lalalnthi Dilrukshi Vitharana , Angie R. Angeles
发明人: M. Arshad Siddiqui , Chaoyang Dai , Umar Faruk Mansoor , Liping Yang , Lalalnthi Dilrukshi Vitharana , Angie R. Angeles
IPC分类号: A61K31/433 , C07D285/14 , C07D513/10 , C07D513/16 , C07D513/20 , A61K31/4747 , A61K31/438 , A61K31/454 , A61K31/5377 , A61K31/7105 , A61K31/711 , A61K39/395 , A61K51/00 , A61K38/21 , A61P35/00 , A61P35/02 , A61P29/00 , A61P37/02 , A61P9/00 , A61P37/06 , A61P31/10 , A61P19/02 , A61P1/00
CPC分类号: C07D211/14 , C07D285/14 , C07D471/04 , C07D515/10 , C07D515/20
摘要: The present invention relates to compounds of Formula (I), below, (wherein X, R1, R2, R3, p, E, ring A, and ring B are as defined herein). The present invention also relates to compositions (including pharmaceutically acceptable compositions) comprising these compounds, alone and in combination with one or more additional therapeutic agents, and to methods for their use in inhibiting KSP kinesin activity, and for treating cellular proliferative diseases or disorders associated with KSP kinesin activity. Formula I
摘要翻译: 本发明涉及下式(I)的化合物(其中X,R 1,R 2,R 3,p,E,环A和环B如本文所定义)。 本发明还涉及包含这些化合物的组合物(包括药学上可接受的组合物),其单独并与一种或多种另外的治疗剂组合,以及其用于抑制KSP驱动蛋白活性的方法,以及用于治疗相关的细胞增殖性疾病或病症 与KSP驱动组织活动。 一级方程式
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公开(公告)号:US08796460B2
公开(公告)日:2014-08-05
申请号:US12738537
申请日:2008-10-16
申请人: M. Arshad Siddiqui , Chaoyang Dai , Umar Faruk Mansoor , Liping Yang , Lalalnthi Dilrukshi Vitharana , Angie R. Angeles
发明人: M. Arshad Siddiqui , Chaoyang Dai , Umar Faruk Mansoor , Liping Yang , Lalalnthi Dilrukshi Vitharana , Angie R. Angeles
IPC分类号: C07D211/26 , A61K31/397 , C07D211/14 , C07D471/04
CPC分类号: C07D211/14 , C07D285/14 , C07D471/04 , C07D515/10 , C07D515/20
摘要: The present invention relates to compounds of Formula (I), below, (wherein X, R1, R2, R3, p, E, ring A, and ring B are as defined herein). The present invention also relates to compositions (including pharmaceutically acceptable compositions) comprising these compounds, alone and in combination with one or more additional therapeutic agents, and to methods for their use in inhibiting KSP kinesin activity, and for treating cellular proliferative diseases or disorders associated with KSP kinesin activity. Formula I
摘要翻译: 本发明涉及下式(I)的化合物(其中X,R 1,R 2,R 3,p,E,环A和环B如本文所定义)。 本发明还涉及包含这些化合物的组合物(包括药学上可接受的组合物),其单独并与一种或多种另外的治疗剂组合,以及其用于抑制KSP驱动蛋白活性的方法,以及用于治疗相关的细胞增殖性疾病或病症 与KSP驱动组织活动。 一级方程式
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公开(公告)号:US20110150757A1
公开(公告)日:2011-06-23
申请号:US12738529
申请日:2008-10-16
申请人: M. Arshad Siddiqui , Chaoyang Dai , Umar Faruk Mansoor , Liping Yang , Lalalnthi Dilrukshi Vitharana , Angie R. Angeles
发明人: M. Arshad Siddiqui , Chaoyang Dai , Umar Faruk Mansoor , Liping Yang , Lalalnthi Dilrukshi Vitharana , Angie R. Angeles
IPC分类号: A61K31/403 , C07D209/96 , C07D491/107 , C07D401/12 , C07D471/10 , A61K31/407 , A61K31/454 , A61K31/438 , A61K31/7105 , A61K31/711 , A61K51/00 , A61K39/395 , A61K38/21 , A61P35/00 , A61P9/00 , A61P37/06 , A61P31/10 , A61P19/02 , A61P1/00 , A61P29/00 , A61P37/02 , A61P35/02
CPC分类号: C07D209/96 , C07D401/12 , C07D471/10 , C07D491/107
摘要: The present invention relates to compounds of Formula (I), below, (wherein R1, R2, R3, R27, R28, R29, p, E, ring A, and ring B are as defined herein). The present invention also relates to compositions (including pharmaceutically acceptable compositions) comprising these compounds, alone and in combination with one or more additional therapeutic agents, and to methods for their use in inhibiting KSP kinesin activity, and for treating cellular proliferative diseases or disorders associated with KSP kinesin activity.
摘要翻译: 本发明涉及下式(I)的化合物(其中R 1,R 2,R 3,R 27,R 28,R 29,p,E,环A和环B如本文所定义)。 本发明还涉及包含这些化合物的组合物(包括药学上可接受的组合物),其单独并与一种或多种另外的治疗剂组合,以及其用于抑制KSP驱动蛋白活性的方法,以及用于治疗相关的细胞增殖性疾病或病症 与KSP驱动组织活动。
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