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公开(公告)号:US08927562B2
公开(公告)日:2015-01-06
申请号:US13876192
申请日:2011-09-26
IPC分类号: A61K31/519 , C07D487/14 , C07D495/14 , C07D487/04
CPC分类号: C07D495/14 , A61K31/519 , C07D487/04 , C07D487/14
摘要: This invention relates to novel fused tricyclic compounds that are inhibitors of mammalian Target of Rapamycin (mTOR) kinase, which is also known as FRAP, RAFT, RAPT or SEP, and are useful in the treatment of cellular proliferative diseases, for example cancer and other proliferative disorders.
摘要翻译: 本发明涉及新的融合三环化合物,其是哺乳动物雷帕霉素靶标(mTOR)激酶的抑制剂,其也称为FRAP,RAFT,RAPT或SEP,并且可用于治疗细胞增殖性疾病,例如癌症和其它 增生性疾病
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公开(公告)号:US20140171456A1
公开(公告)日:2014-06-19
申请号:US14234837
申请日:2012-07-20
IPC分类号: C07D487/14 , A61K31/519
CPC分类号: C07D487/14 , A61K31/519 , C07D519/00
摘要: The present invention relates to certain pyrazolo[1,5-a]pyrrolo[3,2-e]pyrimidine and dipyrazolopyrimidine 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]pyrrolo[3,2-e]pyrimidine or dipyrazolopyrimidine compounds.
摘要翻译: 本发明涉及式(I)的某些吡唑并[1,5-a]吡咯并[3,2-e]嘧啶和二吡唑并嘧啶化合物作为哺乳动物雷帕霉素靶标(mTOR)激酶的抑制剂,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]吡咯并[3,2-e]嘧啶或二吡唑并嘧啶化合物的药物组合物。
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公开(公告)号:US20120114739A1
公开(公告)日:2012-05-10
申请号:US13263193
申请日:2010-04-08
申请人: Yongqi Deng , Binyuan Sun , Hongbo Zeng , Matthew Richards , Gerald W. Shipps, JR. , Cliff C. Cheng , Yinyan Zhao , Andrew McRiner , Zhaoyang Meng , Yang Nan , Mehul F. Patel , Iwona E. Wrona , Panduranga Adulla Reddy , Brian M. Eklov , Shuyi Tang , Duan Liu , Amit K. Mandal , Lianyun Zhao , M. Asshad Siddiqui
发明人: Yongqi Deng , Binyuan Sun , Hongbo Zeng , Matthew Richards , Gerald W. Shipps, JR. , Cliff C. Cheng , Yinyan Zhao , Andrew McRiner , Zhaoyang Meng , Yang Nan , Mehul F. Patel , Iwona E. Wrona , Panduranga Adulla Reddy , Brian M. Eklov , Shuyi Tang , Duan Liu , Amit K. Mandal , Lianyun Zhao , M. Asshad Siddiqui
IPC分类号: A61K9/127 , A61K31/519 , A61K31/5377 , C07D491/048 , C07D495/04 , A61K31/538 , A61K31/551 , A61K31/553 , A61K31/541 , A61K31/554 , C07D498/04 , C12N9/99 , A61K31/704 , A61K39/395 , A61K33/36 , A61K38/50 , A61K33/24 , A61P29/00 , A61P37/08 , A61P11/00 , A61P37/06 , A61P35/00 , A61P35/02 , C07D487/04
CPC分类号: C07D487/04 , C07D519/00
摘要: The present invention provides methods for inhibiting mTOR using pyrazolo[1,5-a]pyrimidine compounds and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with mTOR using such compounds.
摘要翻译: 本发明提供使用吡唑并[1,5-a]嘧啶化合物抑制mTOR的方法以及使用这些化合物治疗,预防,抑制或改善与mTOR相关的一种或多种疾病的方法。
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公开(公告)号:US10894775B2
公开(公告)日:2021-01-19
申请号:US16341591
申请日:2017-10-09
申请人: Merck Sharp & Dohme Corp. , Michael T. Rudd , Zhaoyang Meng , Jenny Wai , David Jonathan Bennett , Edward J. Brnardic , Nigel J. Liverton , Shawn J. Stachel , Yongxin Han , Paul Tempest , Jiuxiang Zhu , Xuewang Xu , Bin Zhu , Chuanman Huang
发明人: Michael T. Rudd , Zhaoyang Meng , Jenny Wai , David Jonathan Bennett , Edward J. Brnardic , Nigel J. Liverton , Shawn J. Stachel , Yongxin Han , Paul Tempest , Jiuxiang Zhu , Xuewang Xu , Bin Zhu , Chuanman Huang
IPC分类号: C07D221/20 , C07D211/16 , C07D211/96
摘要: In its many embodiments, the present invention provides certain piperidine compounds of the Formula (I): and pharmaceutically acceptable salts thereof, wherein X, Y, R1, R2, R3, L, R4, L1, Q, and R5 are as defined herein. The novel compounds of the invention, and pharmaceutically acceptable compositions comprising a compound thereof, are useful as Liver X-β receptor (LXRβ) agonists, and may be useful for treating or preventing pathologies related thereto. Such pathologies include, but are not limited to, inflammatory diseases and diseases characterized by defects in cholesterol and lipid metabolism, such as Alzheimer's disease.
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5.
公开(公告)号:US20180354901A1
公开(公告)日:2018-12-13
申请号:US15780289
申请日:2016-11-29
申请人: Michael T. Rudd , David Jonathan Bennett , Jenny Wai , Zhaoyang Meng , Merck Sharp & Dohme Corp.
IPC分类号: C07D211/16 , C07D401/14 , C07D211/44 , C07D409/14 , C07D401/06 , C07D487/08 , C07D413/14 , C07D417/14 , C07D451/02
摘要: In its many embodiments, the present invention provides certain substituted bispiperidinyl compounds of the Formula (I): and pharmaceutically acceptable salts thereof, wherein ring A, ring B, R1, R2, R3, L, R4, X, Z, Li, Q and R5 are as defined herein. The novel compounds of the invention, and pharmaceutically acceptable compositions comprising a compound thereof, are useful as Liver X-β receptor (LXRβ) agonists, and may be useful for treating or preventing pathologies related thereto. Such pathologies include, but are not limited to, inflammatory diseases and diseases characterized by defects in cholesterol and lipid metabolism, such as Alzheimer's disease.
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6.
公开(公告)号:US20200247754A1
公开(公告)日:2020-08-06
申请号:US16341595
申请日:2017-10-09
申请人: Michael T. RUDD , Zhaoyang MENG , Jenny WAI , David Jonathan BENNETT , Edward J. BRNARDIC , Nigel J. LIVERTON , Shawn J. STACHEL , Yongxin HAN , Paul TEMPEST , Jiuxiang ZHU , Xuewang XU , Bin ZHU , Merck Sharp & Dohme Corp.
发明人: Michael T. Rudd , Zhaoyang Meng , Jenny Wai , David Jonathan Bennett , Edward J. Brnardic , Nigel J. Liverton , Shawn J. Stachel , Yongxin Han , Paul Tempest , Jiuxiang Zhu , Xuewang Xu , Bin Zhu
IPC分类号: C07D221/20 , C07D401/12 , C07D417/12 , C07D405/12 , C07D211/22 , C07D401/14 , C07D417/14
摘要: In its many embodiments, the present invention provides certain substituted aryl and heteroaryl ether compounds of the Formula (I): and pharmaceutically acceptable salts thereof, wherein X, R1, R2, R3, L, R4, L1, Q, and R5 are as defined herein. The novel compounds of the invention, and pharmaceutically acceptable compositions comprising a compound thereof, are useful as Liver X-β receptor (LXRβ) agonists, and may be useful for treating or preventing pathologies related thereto. Such pathologies include, but are not limited to, inflammatory diseases and diseases characterized by defects in cholesterol and lipid metabolism, such as Alzheimer's disease.
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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:US20130281474A1
公开(公告)日:2013-10-24
申请号:US13876192
申请日:2011-09-26
IPC分类号: C07D495/14 , C07D487/04 , C07D487/14
CPC分类号: C07D495/14 , A61K31/519 , C07D487/04 , C07D487/14
摘要: This invention relates to novel fused tricyclic compounds that are inhibitors of mammalian Target of Rapamycin (mTOR) kinase, which is also known as FRAP, RAFT, RAPT or SEP, and are useful in the treatment of cellular proliferative diseases, for example cancer and other proliferative disorders.
摘要翻译: 本发明涉及新的融合三环化合物,其是哺乳动物雷帕霉素靶标(mTOR)激酶的抑制剂,其也称为FRAP,RAFT,RAPT或SEP,并且可用于治疗细胞增殖性疾病,例如癌症和其它 增生性疾病
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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:US20090131498A1
公开(公告)日:2009-05-21
申请号:US11795705
申请日:2006-01-18
IPC分类号: A61K31/365 , C07D493/02 , C07D491/02 , C07C69/757 , C07C49/573 , A61P25/00 , C07D303/02 , C07D307/93 , C07D409/02 , A61K31/407
CPC分类号: C07D493/18 , C07C45/515 , C07C49/733 , C07C67/343 , C07C69/732 , C07C69/757 , C07C2602/42 , C07D303/00 , C07D307/93 , C07D409/04
摘要: This invention provides a method of synthesizing enantioenriched merrilactone A and enantiopure merrilactone A, as well as an improved method of synthesizing racemic merrilactone. This invention also provides intermediate compounds and methods of treating peripheral neuropathies
摘要翻译: 本发明提供了一种合成富含烯雌醇的内酯A和对映体育内酯A的方法,以及合成外消旋内酯的改进方法。 本发明还提供中间体化合物和治疗周围神经病的方法
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