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公开(公告)号:US20090170882A1
公开(公告)日:2009-07-02
申请号:US11631138
申请日:2005-06-30
IPC分类号: A61K31/403 , C07D209/88 , A61K31/519 , A61P37/00 , A61P29/00 , A61P31/10 , A61P35/00 , C07D487/04
CPC分类号: C07D487/04 , C07D209/86 , C07D209/88
摘要: Compounds, compositions and methods relating to kinesin inhibition are described herein.
摘要翻译: 本文描述了与驱动蛋白抑制有关的化合物,组合物和方法。
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公开(公告)号:US08383635B2
公开(公告)日:2013-02-26
申请号:US13058251
申请日:2009-08-12
申请人: Francis Louis Atkinson , Jeffrey Michael Axten , Maria Cichy-Knight , Michael Lee Moore , Vipulkumar Kantibhai Patel , Xinrong Tian , Christopher Roland Wellaway , Allison K. Dunn
发明人: Francis Louis Atkinson , Jeffrey Michael Axten , Maria Cichy-Knight , Michael Lee Moore , Vipulkumar Kantibhai Patel , Xinrong Tian , Christopher Roland Wellaway , Allison K. Dunn
IPC分类号: A01N43/90 , A61K31/519 , C07D471/00
CPC分类号: C07D471/04
摘要: The invention is directed to pyrido[4,3-d]pyrimidin-5(6H)-one derivatives. Specifically, the invention is directed to compounds according to Formula I: wherein R1, R2, R3, and R4 are defined below. The compounds of the invention are inhibitors of PDK1 and can be useful in the treatment of disorders characterized by constitutively activated ACG kinases such as cancer and more specifically cancers of the breast, colon, and lung. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting PDK1 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
摘要翻译: 本发明涉及吡啶并[4,3-d]嘧啶-5(6H) - 酮衍生物。 具体地,本发明涉及式I化合物:其中R1,R2,R3和R4定义如下。 本发明的化合物是PDK1的抑制剂,可用于治疗特征在于组成型激活的ACG激酶(例如癌症,更特别是乳腺癌,结肠癌和肺癌)的病症。 因此,本发明进一步涉及包含本发明化合物的药物组合物。 本发明还涉及抑制PDK1活性的方法和使用本发明化合物或与本发明化合物组合的药物组合物治疗与之相关的病症的方法。
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公开(公告)号:US20090253908A1
公开(公告)日:2009-10-08
申请号:US10598743
申请日:2005-03-11
申请人: Brian W. Budzik , Anthony W. J. Cooper , David Francis Corbett , Jian Jin , Dramane I. Laine , Yonghui Wang , Michael Lee Moore , Ralph A. Rivero , Dongchuan Shi , Feng Wang , Haibo Xie , Chongjie Zhu
发明人: Brian W. Budzik , Anthony W. J. Cooper , David Francis Corbett , Jian Jin , Dramane I. Laine , Yonghui Wang , Michael Lee Moore , Ralph A. Rivero , Dongchuan Shi , Feng Wang , Haibo Xie , Chongjie Zhu
IPC分类号: C07F5/02 , C07D241/04
CPC分类号: C07D403/12 , C07D207/14 , C07D209/42 , C07D211/56 , C07D213/81 , C07D213/82 , C07D215/48 , C07D215/50 , C07D243/08 , C07D273/02 , C07D277/62 , C07D295/135 , C07D307/68 , C07D307/84 , C07D317/62 , C07D319/14 , C07D321/10 , C07D333/38 , C07D333/70 , C07D401/12 , C07D405/12 , C07D409/12 , C07D453/02 , C07D487/04
摘要: Muscarinic Acetylcholine receptor antagonists and methods of using them are provided.
摘要翻译: 提供毒蕈碱性乙酰胆碱受体拮抗剂及其使用方法。
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公开(公告)号:US09096605B2
公开(公告)日:2015-08-04
申请号:US14233896
申请日:2012-06-29
申请人: Hong Lin , Juan Ignacio Luengo , Michael Lee Moore , Junya Qu , Ralph A. Rivero , Rosanna Tedesco , Hongyi Yu
发明人: Hong Lin , Juan Ignacio Luengo , Michael Lee Moore , Junya Qu , Ralph A. Rivero , Rosanna Tedesco , Hongyi Yu
IPC分类号: C07D413/04 , C07D487/04
CPC分类号: C07D487/04 , C07D413/04
摘要: PI3Kβ selective compounds having the structure
摘要翻译: PI3K&bgr 具有结构的选择性化合物
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公开(公告)号:US20140194415A1
公开(公告)日:2014-07-10
申请号:US14238418
申请日:2012-08-16
申请人: Jonathan Michael Ghergurovich , Michael Lee Moore , Cynthia Ann Parrish , Lance Howard Ridgers , Hongyi Lu
发明人: Jonathan Michael Ghergurovich , Michael Lee Moore , Cynthia Ann Parrish , Lance Howard Ridgers , Hongyi Lu
IPC分类号: A61K31/5386 , A61K45/06 , C07D498/10
CPC分类号: A61K31/5386 , A61K45/06 , C07D498/10 , A61K2300/00
摘要: This invention relates to spirocyclic piperidines according to Formula (I) and the use of spirocyclic piperidines for the modulation, notably the inhibition of the activity or function of fatty acid synthase (FAS). Suitably, the present invention relates to the use of spirocyclic piperidines in the treatment of cancer.
摘要翻译: 本发明涉及式(I)的螺环哌啶和螺环哌啶用于调节,特别是抑制脂肪酸合成酶(FAS)活性或功能的用途。 合适地,本发明涉及螺环哌啶在治疗癌症中的用途。
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公开(公告)号:US06194544B1
公开(公告)日:2001-02-27
申请号:US08571869
申请日:1996-01-05
IPC分类号: C07K764
摘要: Cyclic penta- and hexa-peptide libraries containing one or more known amino acids, one or more randomized amino acids and a conformationally constraining element are disclosed. These peptide libraries may be used for screening for new bioactive peptides and for elucidating structural information pertinent to drug design.
摘要翻译: 公开了含有一种或多种已知氨基酸,一种或多种随机氨基酸和构象约束元件的环状五肽和六肽文库。 这些肽文库可用于筛选新的生物活性肽和用于阐明与药物设计有关的结构信息。
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公开(公告)号:US09084794B2
公开(公告)日:2015-07-21
申请号:US14238418
申请日:2012-08-16
申请人: Jonathan Michael Ghergurovich , Michael Lee Moore , Cynthia Ann Parrish , Lance Howard Ridgers , Hongyi Lu
发明人: Jonathan Michael Ghergurovich , Michael Lee Moore , Cynthia Ann Parrish , Lance Howard Ridgers , Hongyi Lu
IPC分类号: C07D498/10 , A61K31/5386 , A61K45/06
CPC分类号: A61K31/5386 , A61K45/06 , C07D498/10 , A61K2300/00
摘要: This invention relates to spirocyclic piperidines according to Formula (I) and the use of spirocyclic piperidines for the modulation, notably the inhibition of the activity or function of fatty acid synthase (FAS). Suitably, the present invention relates to the use of spirocyclic piperidines in the treatment of cancer.
摘要翻译: 本发明涉及式(I)的螺环哌啶和螺环哌啶用于调节,特别是抑制脂肪酸合成酶(FAS)活性或功能的用途。 合适地,本发明涉及螺环哌啶在治疗癌症中的用途。
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公开(公告)号:US20120208827A1
公开(公告)日:2012-08-16
申请号:US13504547
申请日:2010-10-27
申请人: Steven Dock , Jason Hallman , Christopher Laudeman , Ronggang Liu , Aaron Miller , Michael Lee Moore , David Musso , Cynthia Parrish
发明人: Steven Dock , Jason Hallman , Christopher Laudeman , Ronggang Liu , Aaron Miller , Michael Lee Moore , David Musso , Cynthia Parrish
IPC分类号: A61K31/496 , A61K31/437 , A61K31/4725 , A61K31/428 , A61K31/423 , A61K31/4184 , C07D471/04 , C07D401/14 , C07D417/14 , C07D413/14 , C07D403/14 , C07D405/14 , A61P35/00 , C07D403/06 , A61K31/517
CPC分类号: C07D403/14 , C07D403/06 , C07D405/14 , C07D413/14 , C07D417/14 , C07D471/04
摘要: This invention relates to the use of benzimidazole derivatives for the modulation, notably the inhibition of the activity or function of fatty acid synthase (FAS). Suitably, the present invention relates to the use of benzimidazoles in the treatment of cancer.
摘要翻译: 本发明涉及苯并咪唑衍生物用于调节,特别是抑制脂肪酸合成酶(FAS)的活性或功能的用途。 合适地,本发明涉及苯并咪唑在治疗癌症中的用途。
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公开(公告)号:US20110136838A1
公开(公告)日:2011-06-09
申请号:US13058251
申请日:2009-08-12
申请人: Francis Louis Atkinson , Jeffrey Michael Axten , Maria Cichy-Knight , Michael Lee Moore , Vipulkumar Kantibhai Patel , Xinrong Tian , Christopher Roland Wellaway , Allison K. Dunn
发明人: Francis Louis Atkinson , Jeffrey Michael Axten , Maria Cichy-Knight , Michael Lee Moore , Vipulkumar Kantibhai Patel , Xinrong Tian , Christopher Roland Wellaway , Allison K. Dunn
IPC分类号: A61K31/519 , C07D471/04 , A61P35/00
CPC分类号: C07D471/04
摘要: The invention is directed to pyrido[4,3-d]pyrimidin-5(6H)-one derivatives. Specifically, the invention is directed to compounds according to Formula I: wherein R1, R2, R3, and R4 are defined below.The compounds of the invention are inhibitors of PDK1 and can be useful in the treatment of disorders characterized by constitutively activated ACG kinases such as cancer and more specifically cancers of the breast, colon, and lung. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting PDK1 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
摘要翻译: 本发明涉及吡啶并〔4,3-d〕嘧啶-5(6H) - 酮衍生物。 具体地,本发明涉及式I化合物:其中R1,R2,R3和R4定义如下。 本发明的化合物是PDK1的抑制剂,可用于治疗特征在于组成型激活的ACG激酶(例如癌症,更特别是乳腺癌,结肠癌和肺癌)的病症。 因此,本发明进一步涉及包含本发明化合物的药物组合物。 本发明还涉及抑制PDK1活性的方法和使用本发明化合物或与本发明化合物组合的药物组合物治疗与之相关的病症的方法。
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公开(公告)号:US06224832B1
公开(公告)日:2001-05-01
申请号:US09194212
申请日:1998-11-20
IPC分类号: C08F200
CPC分类号: B01J19/0046
摘要: Solid phase combinatorial synthesis is carried out in a multi-reactor synthesizer comprising an array of separate reactor cells (1-9) containing a solid reaction support medium (26). Subsets of the reactor cells (1-9) are interconnected with one another in a desired pattern, and, in a first reaction step, reagents (A, B, C) are circulated through the subsets. After the first reaction step is completed, the reactor cells (1-9) are rearranged into a new configuration of the subsets, and the same, or other, reagents (A, B, C) are circulated through the new subsets. The process can be repeated to produce large numbers of compounds differing from one another.
摘要翻译: 在多反应器合成器中进行固相组合合成,该反应器合成器包括含有固体反应支持介质(26)的分离的反应器单元阵列(1-9)。 反应器单元(1-9)的子集以所需的模式彼此互连,并且在第一反应步骤中,试剂(A,B,C)循环通过子集。 在第一反应步骤完成之后,将反应器电池(1-9)重新排列成子组的新配置,并且相同或其它试剂(A,B,C)循环通过新的子集。 可以重复该过程以产生大量彼此不同的化合物。
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