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1. 发明申请

US20170073354A1 PIPERAZINE DERIVATIVES AS HIV PROTEASE INHIBITORS 审中-公开
标题翻译：作为HIV蛋白酶抑制剂的哌嗪衍生物
公开(公告)号：US20170073354A1
公开(公告)日：2017-03-16
申请号：US15124635
申请日：2015-03-06
申请人： Jurgen SCHULZ , Peter D. WILLIAMS , John A. MCCAULEY , Christopher J. BUNGARD , David Jonathan BENNETT , Sherman T. WADDELL , Gregori J. MORRIELLO , Lehua CHANG , Michael P. DWYER , Katharine M. HOLLOWAY , Alejandro CRESPO , Xin-Jie CHU , Catherine WISCOUNT , Marie H. LOUGHRAN , Jesse J. MANIKOWSKI , Kartik M. KEERTIKAR , Bin HU , Bin ZHONG , Tao JI , Merck Sharp & Dohme Corp. , MSD R&D (China) Co., Ltd.
发明人： Peter D. Williams , John A. McCauley , Christopher J. Bungard , David Jonathan Bennett , Sherman T. Waddell , Gregori J. Morriello , Lehua Chang , Michael P. Dwyer , M. Katharine Holloway , Alejandro Crespo , Xin-Jie Chu , Catherine Wiscount , H. Marie Loughran , Jesse J. Manikowski , Jurgen Schulz , Kartik M. Keertikar , Bin Hu , Bin Zhong , Tao Ji
IPC分类号： C07D513/08 , A61K31/554 , A61K45/06
CPC分类号： C07D513/08 , A61K31/554 , A61K45/06
摘要： The present invention is directed to compounds of Formula I pharmaceutical compositions comprising the same, and their use in the inhibition of HIV protease, the inhibition of HIV replication, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS.
摘要翻译：本发明涉及含有该化合物的式I药物组合物的化合物及其在抑制HIV蛋白酶，抑制HIV复制，预防HIV感染，HIV感染治疗和预防，治疗和延迟艾滋病的发病或进展。

2. 发明申请

US20140378416A1 SILYL-CONTAINING HETEROCYCLIC COMPOUNDS AND METHODS OF USE THEREOF FOR THE TREATMENT OF VIRAL DISEASES 审中-公开
标题翻译：含有SILYL的杂环化合物及其用于治疗病毒性疾病的方法
公开(公告)号：US20140378416A1
公开(公告)日：2014-12-25
申请号：US14345114
申请日：2012-09-11
申请人： Michael P. Dwyer , Kartik M. Keertikar , Qingbei Zeng , Robert D. Mazzola, JR. , Wensheng Yu , Haiqun Tang , Seong Heon Kim , Ling Tong , Stuart B. Rosenblum , Joseph A. Kozlowski , Anilkumar Gopinadhan Nair
发明人： Michael P. Dwyer , Kartik M. Keertikar , Qingbei Zeng , Robert D. Mazzola, JR. , Wensheng Yu , Haiqun Tang , Seong Heon Kim , Ling Tong , Stuart B. Rosenblum , Joseph A. Kozlowski , Anilkumar Gopinadhan Nair
IPC分类号： C07F7/10 , A61K45/06 , A61K31/695
CPC分类号： C07F7/10 , A61K31/695 , A61K45/06 , A61K2201/094 , A61K2300/00 , C07F7/0816
摘要： The present invention relates to novel Silyl-Containing Heterocyclic Compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, B, C, D, E, F and L are as defined herein. The present invention also relates to compositions comprising at least one Silyl-Containing Heterocyclic Compound, and methods of using the Silyl-Containing Heterocyclic Compounds for treating or preventing HCV infection in a patient.
摘要翻译：本发明涉及式（I）的新的含甲硅烷基的杂环化合物及其药学上可接受的盐，其中A，B，C，D，E，F和L如本文所定义。本发明还涉及包含至少一种含甲硅烷基的杂环化合物的组合物，以及使用含有甲硅烷基的杂环化合物治疗或预防患者HCV感染的方法。

3. 发明申请

US20110183933A1 NOVEL MODULATORS OF CELL CYCLE CHECKPOINTS AND THEIR USE IN COMBINATION WITH CHECKPOINT KINASE INHIBITORS 有权
标题翻译：细胞周期调节因子的新型调节因子及其与检查点激酶抑制剂的组合使用
公开(公告)号：US20110183933A1
公开(公告)日：2011-07-28
申请号：US12744021
申请日：2008-11-05
申请人： Timothy J. Guzi , David A. Parry , Marc A. Labroli , Michael P. Dwyer , Kamil Paruch
发明人： Timothy J. Guzi , David A. Parry , Marc A. Labroli , Michael P. Dwyer , Kamil Paruch
IPC分类号： A61K31/7072 , C07H19/06 , A61K31/7068 , A61P35/00 , A61P35/02
CPC分类号： C07H19/067 , C07H19/073
摘要： In its many embodiments, the present invention provides a novel class of pyrimidine analogs of formula (V) as targeted mechanism-based modulators of cell cycle checkpoints. Cancers and/or malignancies can be treated by administration of a cell cycle checkpoint modulator of the invention. Also discussed are suitable combinations of the cell cycle checkpoint modulator with a checkpoint kinase inhibitor to produce synergistic apoptosis in cancer cells. The invention includes methods of treating cancers by administering the combination of the cell cycle checkpoint modulator and the checkpoint kinase inhibitor, pharmaceutical compositions comprising the activator as well as the combination and pharmaceutical kits.
摘要翻译：在其许多实施方案中，本发明提供了一类新颖的式（V）嘧啶类似物作为细胞周期检查点的靶向基于机制的调节剂。可以通过施用本发明的细胞周期检查点调节剂来治疗癌症和/或恶性肿瘤。还讨论了细胞周期检查点调节剂与检查点激酶抑制剂的合适组合，以在癌细胞中产生协同凋亡。本发明包括通过施用细胞周期检查点调节剂和检查点激酶抑制剂的组合，包含活化剂的药物组合物以及组合药物试剂盒来治疗癌症的方法。

4. 发明申请

US20100125068A1 METHODS FOR INHIBITING PROTEIN KINASES 有权
标题翻译：抑制蛋白激酶的方法
公开(公告)号：US20100125068A1
公开(公告)日：2010-05-20
申请号：US12688664
申请日：2010-01-15
申请人： Timothy J. Guzi , Kamil Paruch , Michael P. Dwyer , David A. Parry
发明人： Timothy J. Guzi , Kamil Paruch , Michael P. Dwyer , David A. Parry
IPC分类号： A61K31/54 , C07D487/04 , C07D279/12 , C07D413/14 , A61K31/519 , A61K31/5377 , A61P35/00
CPC分类号： A61K31/519 , A61K31/5377 , A61K45/06 , A61K2300/00
摘要： The present invention provides methods for inhibiting protein kinases selected from the group consisting of AKT, Checkpoint kinase, Aurora kinase, Pim kinases, and tyrosine kinase using pyrazolo[1,5-a]pyrimidine compounds and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with protein kinases using such compounds.
摘要翻译：本发明提供使用吡唑并[1,5-a]嘧啶化合物抑制选自AKT，检查点激酶，极光激酶，Pim激酶和酪氨酸激酶的蛋白激酶的方法，以及治疗，预防，抑制或使用这种化合物改善与蛋白激酶相关的一种或多种疾病。

5. 发明授权

US07511049B2 Pyrazolopyrimidines as cyclin dependent kinase inhibitors 失效
标题翻译：吡唑并嘧啶类作为细胞周期蛋白依赖性激酶抑制剂
公开(公告)号：US07511049B2
公开(公告)日：2009-03-31
申请号：US11779050
申请日：2007-07-17
申请人： Timothy J. Guzi , Kamil Paruch , Michael P. Dwyer , Ronald J. Doll , Viyyoor M. Girijavallabhan , Lawrence W. Dillard , Vinh D. Tran , Zhenmin He , Ray Anthony James , Haengsoon Park
发明人： Timothy J. Guzi , Kamil Paruch , Michael P. Dwyer , Ronald J. Doll , Viyyoor M. Girijavallabhan , Lawrence W. Dillard , Vinh D. Tran , Zhenmin He , Ray Anthony James , Haengsoon Park
IPC分类号： A61K31/519 , A61P35/00 , C07D487/04
CPC分类号： C07D487/04 , A61K31/519 , A61K31/52 , A61K31/704 , A61K31/7072 , A61K45/06 , A61K2300/00
摘要： In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases, 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 diseases associated with the CDKs 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吡唑并[1,5-a]嘧啶化合物作为细胞周期蛋白依赖性激酶的抑制剂，制备此类化合物的方法，含有一种或多种此类化合物的药物组合物，制备药物制剂的方法包括一种或多种这样的化合物，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CDK相关的一种或多种疾病的方法。

6. 发明授权

US07449488B2 Pyrazolopyrimidines as protein kinase inhibitors 有权
标题翻译：吡唑并嘧啶作为蛋白激酶抑制剂
公开(公告)号：US07449488B2
公开(公告)日：2008-11-11
申请号：US11244628
申请日：2005-10-06
申请人： Kamil Paruch , Timothy J. Guzi , Michael P. Dwyer , Gerald W. Shipps, Jr.
发明人： Kamil Paruch , Timothy J. Guzi , Michael P. Dwyer , Gerald W. Shipps, Jr.
IPC分类号： C07D231/00 , C07D231/54 , A61K31/415 , A01N43/56
CPC分类号： C07D487/04
摘要： In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of protein and/or checkpoint kinases, methods of preparing such compounds, pharmaceutical compositions including one or more such compounds, methods of preparing pharmaceutical formulations including one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the protein or checkpoint kinases using such compounds or pharmaceutical compositions. The invention also relates to the inhibition of hepatitis C virus (HCV) replication. In particular, embodiments of the invention provide compounds and methods for inhibiting HCV RNA-dependent RNA polymerase enzymatic activity. The invention also provides compositions and methods for the prophylaxis and treatment of HCV infection.
摘要翻译：在其许多实施方案中，本发明提供了一类新颖的吡唑并[1,5-a]嘧啶化合物作为蛋白质和/或检查点激酶的抑制剂，制备此类化合物的方法，包含一种或多种这类化合物的药物组合物，制备包括一种或多种这样的化合物的药物制剂，以及使用这些化合物或药物组合物治疗，预防，抑制或改善与蛋白质或检查点激酶相关的一种或多种疾病的方法。本发明还涉及丙型肝炎病毒（HCV）复制的抑制。特别地，本发明的实施方案提供了用于抑制HCV RNA依赖性RNA聚合酶酶活性的化合物和方法。本发明还提供了预防和治疗HCV感染的组合物和方法。

7. 发明授权

US07309705B2 Pyrazolopyrimidines as cyclin dependent kinase inhibitors 失效
公开(公告)号：US07309705B2
公开(公告)日：2007-12-18
申请号：US11395824
申请日：2006-03-31
申请人： Timothy J. Guzi , Kamil Paruch , Michael P. Dwyer , Ronald J. Doll , Viyyoor M. Girijavallabhan , Lawrence W. Dillard , Vinh D. Tran , Zhen Min He , Ray Anthony James , Haengsoon Park
发明人： Timothy J. Guzi , Kamil Paruch , Michael P. Dwyer , Ronald J. Doll , Viyyoor M. Girijavallabhan , Lawrence W. Dillard , Vinh D. Tran , Zhen Min He , Ray Anthony James , Haengsoon Park
IPC分类号： A61K31/519 , A61P35/00 , C07D484/04
CPC分类号： C07D487/04 , A61K31/519 , A61K31/52 , A61K31/704 , A61K31/7072 , A61K45/06 , A61K2300/00
摘要： In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases, 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 diseases associated with the CDKs using such compounds or pharmaceutical compositions.

8. 发明授权

US07161003B1 Pyrazolopyrimidines as cyclin dependent kinase inhibitors 有权
标题翻译：吡唑并嘧啶类作为细胞周期蛋白依赖性激酶抑制剂
公开(公告)号：US07161003B1
公开(公告)日：2007-01-09
申请号：US10654546
申请日：2003-09-03
申请人： Timothy J. Guzi , Kamil Paruch , Michael P. Dwyer , Ronald J. Doll , Viyyoor M. Girijavallabhan , Alan Mallams , Carmen S. Alvarez , Kartik M. Keertikar , Jocelyn Rivera , Tin-Yau Chan , Vincent Madison , Thierry O. Fischmann , Lawrence W. Dillard , Vinh D. Tran , Zhen Min He , Ray Anthony James , Haengsoon Park , Vidyadhar M. Paradkar , Douglas Walsh Hobbs
发明人： Timothy J. Guzi , Kamil Paruch , Michael P. Dwyer , Ronald J. Doll , Viyyoor M. Girijavallabhan , Alan Mallams , Carmen S. Alvarez , Kartik M. Keertikar , Jocelyn Rivera , Tin-Yau Chan , Vincent Madison , Thierry O. Fischmann , Lawrence W. Dillard , Vinh D. Tran , Zhen Min He , Ray Anthony James , Haengsoon Park , Vidyadhar M. Paradkar , Douglas Walsh Hobbs
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases, 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 diseases associated with the CDKs 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吡唑并[1,5-a]嘧啶化合物作为细胞周期蛋白依赖性激酶的抑制剂，制备此类化合物的方法，含有一种或多种此类化合物的药物组合物，制备药物制剂的方法包括一种或多种这样的化合物，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CDK相关的一种或多种疾病的方法。

9. 发明授权

US06312573B1 Corner insert for edge strips used with modified electrodes for electrolytic processes 失效
标题翻译：与用于电解过程的改性电极一起使用的边缘条的角插入件
公开(公告)号：US06312573B1
公开(公告)日：2001-11-06
申请号：US09579653
申请日：2000-05-26
申请人： Michael P. Dwyer , Manuel G. Santoyo , David Watson
发明人： Michael P. Dwyer , Manuel G. Santoyo , David Watson
IPC分类号： C25B900
CPC分类号： C25C7/02
摘要： A nonconductive insert is provided to fill the void resulting from the removal of mother-plate corners wrapped within the abutting ends of side and bottom edge strips. The insert includes at least one anchor, adapted to frictionally engage the end of a strip mounted along the edge of the mother plate. The insert and its anchors are designed to completely fill the void left by the missing mother-plate corner, thereby preventing penetration of electrolyte and accumulation of deposits. According to other embodiments of the invention, the insert may be incorporated into the edge-strip end as an integral component of the strip.
摘要翻译：提供非导电插入物以填充由于去除包裹在侧边缘和下边缘条带的邻接端之间的母板拐角而产生的空隙。插入件包括至少一个锚固件，其适于摩擦地接合沿着母板的边缘安装的条带的端部。插入物及其锚固件被设计成完全填充缺失的母板角落留下的空隙，从而防止电解质渗透和沉积物积聚。根据本发明的其它实施例，插入件可以作为带的整体部件结合到边缘带端部中。

10. 发明授权

US10647727B2 Substituted pyrazolo/imidazolo bicyclic compounds as PDE2 inhibitors 有权
公开(公告)号：US10647727B2
公开(公告)日：2020-05-12
申请号：US15579115
申请日：2016-06-20
申请人： Merck Sharp & Dohme Corp. , Gregori J. Morriello , Michael P. Dwyer , Lehua Chang , Yili Chen , Ming Wang , Ashley Forster , Richard Berger , Kausik K. Nanda , Jamie L. Bunda , William D. Shipe
发明人： Gregori J. Morriello , Lehua Chang , Ashley Forster , Richard Berger , Kausik K. Nanda , William D. Shipe
IPC分类号： C07D487/04 , C07D498/04 , C07D473/34 , A61P25/06 , A61P25/28 , A61P25/18 , A61P25/16
摘要： The present invention is directed to pyrimidine carboxamide compounds of formula I 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, Parkinson's disease, Parkinson's disease dementia (PDD), or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.

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