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公开(公告)号：US08680116B2
公开(公告)日：2014-03-25
申请号：US13384946
申请日：2010-07-19
IPC分类号： A61K31/04 , C07D215/38
CPC分类号： A61K31/47 , C07D215/22 , C07D215/227 , C07D401/14 , C07D409/04 , C07D409/14
摘要： The present invention is directed to quinolinone compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 2 (PDE2). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
摘要翻译： 本发明涉及可用作治疗与磷酸二酯酶2（PDE2）相关的中枢神经系统疾病的治疗剂的喹啉酮化合物。 本发明还涉及这些化合物用于治疗神经和精神疾病如精神分裂症，精神病或亨廷顿病以及与纹状体功能减退或基底神经节功能障碍相关的疾病的用途。
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公开(公告)号：US20120115885A1
公开(公告)日：2012-05-10
申请号：US13384946
申请日：2010-07-19
IPC分类号： A61K31/4709 , C07D409/04 , C07D215/22 , A61K31/4704 , A61P25/18 , C07D401/12 , A61P25/22 , A61P25/00 , A61P25/16 , C07D409/14 , A61K31/506
CPC分类号： A61K31/47 , C07D215/22 , C07D215/227 , C07D401/14 , C07D409/04 , C07D409/14
摘要： The present invention is directed to quinolinone compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 2 (PDE2). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
摘要翻译： 本发明涉及可用作治疗与磷酸二酯酶2（PDE2）相关的中枢神经系统疾病的治疗剂的喹啉酮化合物。 本发明还涉及这些化合物用于治疗神经和精神疾病如精神分裂症，精神病或亨廷顿病以及与纹状体功能减退或基底神经节功能障碍相关的疾病的用途。
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公开(公告)号：US20090306071A1
公开(公告)日：2009-12-10
申请号：US12227959
申请日：2007-06-05
IPC分类号： A61K31/5377 , A61K31/497 , A61K31/4745 , C07D471/04
CPC分类号： C07D471/04
摘要： The instant invention provides for compounds that inhibit the four known mammalian JAK kinases (JAK1, JAK2, JAK3 and TYK2) and PDK1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting the activity of JAK1, JAK2, JAK3 TYK2 and PDK1 by administering the compound to a patient in need of treatment for myeloproliferative disorders or cancer.
摘要翻译： 本发明提供抑制四种已知的哺乳动物JAK激酶（JAK1，JAK2，JAK3和TYK2）和PDK1的化合物。 本发明还提供了包含这种抑制化合物的组合物和通过向需要治疗骨髓增生性疾病或癌症的患者施用化合物来抑制JAK1，JAK2，JAK3 TYK2和PDK1的活性的方法。
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公开(公告)号：US08344144B2
公开(公告)日：2013-01-01
申请号：US12999342
申请日：2009-06-08
申请人： Michelle Machacek , Gabriela de Almeida , Jonathan B. Grimm , Rachel N. MacCoss , Eric Romeo , Tony Siu , Catherine White , Kevin Wilson
发明人： Michelle Machacek , Gabriela de Almeida , Jonathan B. Grimm , Rachel N. MacCoss , Eric Romeo , Tony Siu , Catherine White , Kevin Wilson
IPC分类号： C07D471/02 , A61K31/395
CPC分类号： C07D513/04 , C07D471/04 , C07D487/04 , C07D498/04
摘要： The instant invention provides for compounds that inhibit the four known mammalian JAK kinases (JAK1, JAK2, JAK3 and TYK2) and PDK1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting the activity of JAK1, JAK2, JAK3, TYK2 and PDK1 by administering the compound to a patient in need of treatment for myeloproliferative disorders or cancer.
摘要翻译： 本发明提供抑制四种已知的哺乳动物JAK激酶（JAK1，JAK2，JAK3和TYK2）和PDK1的化合物。 本发明还提供了包含这种抑制化合物的组合物和通过将该化合物施用于需要治疗骨髓增生性疾病或癌症的患者的JAK1，JAK2，JAK3，TYK2和PDK1的活性的方法。
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公开(公告)号：US20100256097A1
公开(公告)日：2010-10-07
申请号：US12665045
申请日：2008-06-16
申请人： Michael Altman , Matthew Christopher , Jonathan B. Grimm , Andrew Haidle , Kaleen Konrad , Jongwon Lim , Rachel N. MacCoss , Michelle Machacek , Ekundayo Osimboni , Ryan D. Otte , Tony Siu , Kerrie Spencer , Brandon Taoka , Paul Tempest , Kevin Wilson , Hyan Chong Woo , Jonathan Young , Anna Zabierek
发明人： Michael Altman , Matthew Christopher , Jonathan B. Grimm , Andrew Haidle , Kaleen Konrad , Jongwon Lim , Rachel N. MacCoss , Michelle Machacek , Ekundayo Osimboni , Ryan D. Otte , Tony Siu , Kerrie Spencer , Brandon Taoka , Paul Tempest , Kevin Wilson , Hyan Chong Woo , Jonathan Young , Anna Zabierek
IPC分类号： A61K31/675 , C07D409/14 , A61K31/4439 , A61K31/4436 , C07D413/14 , A61K31/5377 , C07D409/12 , A61K31/501 , C07F9/28 , C07D417/14 , A61K31/541
CPC分类号： C07D409/12 , C07D409/14 , C07D413/14 , C07D417/14 , C07D498/10 , C07F9/65586 , C07F9/65685
摘要： The instant invention provides for compounds that inhibit the four known mammalian JAK kinases (JAK1, JAK2, JAK3 and TYK2) and PDK1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting the activity of JAK1, JAK2, JAK3 TYK2 and PDK1 by administering the compound to a patient in need of treatment for myeloproliferative disorders or cancer.
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公开(公告)号：US20060293358A1
公开(公告)日：2006-12-28
申请号：US11473273
申请日：2006-06-22
申请人： Christopher Dinsmore , Ana Gabarda Ortega , David Guerin , James Jewell , Jason Katz , Jongwon Lim , Michelle Machacek , Ryan Otte , Jonathan Young
发明人： Christopher Dinsmore , Ana Gabarda Ortega , David Guerin , James Jewell , Jason Katz , Jongwon Lim , Michelle Machacek , Ryan Otte , Jonathan Young
IPC分类号： A61K31/473 , C07D221/02
CPC分类号： C07D471/04 , C07D221/16 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/04 , C07D405/12 , C07D405/14 , C07D409/04 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/14 , C07D487/04 , C07D491/10 , C07D491/113 , C07F7/1804
摘要： The present invention relates to 5H-benzo[4,5]cyclohepta[1,2-b]pyridine compounds, that are useful for treating cellular proliferative diseases, for treating disorders associated with MET activity, and for inhibiting the receptor tyrosine kinase MET. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.
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公开(公告)号：US20210309688A1
公开(公告)日：2021-10-07
申请号：US17266507
申请日：2019-08-05
申请人： Jongwon Lim , Michelle Machacek , Michael H. Reutershan , Sebastian Schneider , Merck Sharp & Dohme Corp.
IPC分类号： C07H19/167 , C07D473/34 , C07D471/04
摘要： The present invention provides a compound of Formula (I) or the pharmaceutically acceptable salts thereof, which are PRMT5 inhibitors.
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公开(公告)号：US07763634B2
公开(公告)日：2010-07-27
申请号：US12227959
申请日：2007-06-05
IPC分类号： A61K31/4745 , C07D471/02
CPC分类号： C07D471/04
摘要： The instant invention provides for tetracyclic compounds that inhibit the four known mammalian JAK kinases (JAK1, JAK2, JAK3 and TYK2) and PDK1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting the activity of JAK1, JAK2, JAK3 TYK2 and PDK1 by administering the compound to a patient in need of treatment for myeloproliferative disorders or cancer.
摘要翻译： 本发明提供抑制四种已知的哺乳动物JAK激酶（JAK1，JAK2，JAK3和TYK2）和PDK1的四环化合物。 本发明还提供了包含这种抑制化合物的组合物和通过向需要治疗骨髓增生性疾病或癌症的患者施用化合物来抑制JAK1，JAK2，JAK3 TYK2和PDK1的活性的方法。
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公开(公告)号：US20210309687A1
公开(公告)日：2021-10-07
申请号：US17266515
申请日：2019-08-05
申请人： Michelle MACHACEK , David WITTER , Chunhui HUANG , Shuhei KAWAMURA , Sebastian SCHNEIDER , Mrray WAN , Merck Sharp & Dohme Corp.
发明人： Michelle Machacek , David Witter , Chunhui Huang , Shuhei Kawamura , Sebastian Schneider , Murray Wan
摘要： The present invention provides a compound of formula (I) Formula (I) and the pharmaceutically acceptable salts, esters, and prodrugs thereof, are PRMT5 inhibitors. Also provided are methods of making compounds of formula (I), pharmaceutical compositions comprising compounds of formula (I), and methods of using these compounds to treat cancer, sickle cell, and hereditary persistence of foetal hemoglobin (HPFH) mutations.
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公开(公告)号：US20150368247A1
公开(公告)日：2015-12-24
申请号：US14764616
申请日：2014-02-04
申请人： Matthew P. CHRISTOPHER , Francesc Xavier FRADERA LLINAS , Michelle MACHACEK , Michelle MARTINEZ , Michael Hale REUTERSHAN , Manami SHIZUKA , Binyuan SUN , Christopher Francis THOMPSON , Wesley B. TROTTER , Matthew E. VOSS , Liping YANG , Merck Sharp & Dohme Corp.
发明人： Matthew P. Christopher , Francesc Xavier Fradera Llinas , Michelle Machacek , Michelle Martinez , Michael Hale Reutershan , Manami Shizuka , Binyuan Sun , Christopher Francis Thompson , B. Wesley Trotter , Matthew E. Voss , Liping Yang
IPC分类号： C07D473/34 , C07D473/00 , C07D473/30
CPC分类号： C07D473/34 , C07D473/00 , C07D473/30
摘要： The present invention provides 2,6,7 substituted purines as described herein or a pharmaceutically acceptable salt thereof. The representative compounds are useful as inhibitors of the HDM2 protein. Also disclosed are pharmaceutical compositions comprising the above compounds and potential methods of treating cancer using the same.
摘要翻译： 本发明提供2,6,7本文所述的取代嘌呤或其药学上可接受的盐。 代表性化合物可用作HDM2蛋白的抑制剂。 还公开了包含上述化合物的药物组合物和使用其治疗癌症的潜在方法。
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