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1. 发明申请

US20170334924A1 Spirocyclic Heterocyclic Compounds Useful As HIV Integrase Inhibitors 审中-公开
公开(公告)号：US20170334924A1
公开(公告)日：2017-11-23
申请号：US15533169
申请日：2015-12-04
申请人： Mark W. Embrey , Thomas H. Graham , Izzat T. Raheem , John D. Schreier , Sherman T. Waddell , John S. Wai , Lihong Hu , Xuanjia Peng
发明人： Mark W. Embrey , Thomas H. Graham , Izzat T. Raheem , John D. Schreier , Sherman T. Waddell , John S. Wai , Lihong Hu , Xuanjia Peng
IPC分类号： C07D491/20 , C07D487/20 , A61K45/06 , A61K31/683 , A61K31/675 , C07F9/6561 , A61K31/499
CPC分类号： C07D491/20 , A61K31/499 , A61K31/675 , A61K31/683 , A61K45/06 , A61P31/18 , C07D487/20 , C07F9/6561 , A61K2300/00
摘要： The present invention relates to Spirocyclic Heterocycle Compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, B, X, Y, R1, R2 and R4 are as defined herein. The present invention also relates to compositions comprising at least one Spirocyclic Heterocycle Compound, and methods of using the Spirocyclic Heterocycle Compounds for treating or preventing HIV infection in a subject.

2. 发明申请

US20160317543A1 SPIROCYCLIC HETERCYCLE COMPOUNDS USEFUL AS HIV INTEGRASE INHIBITORS 有权
标题翻译：作为艾滋病毒整合抑制剂的螺旋体异构体化合物有用
公开(公告)号：US20160317543A1
公开(公告)日：2016-11-03
申请号：US15105376
申请日：2014-12-17
申请人： Thomas H. Graham , Wensheng Liu , Tao Yu , Yonglian Zhang , Sherman T. Waddell , John S. Wai , Paul J. Coleman , John M. Sanders , Mark W. Embrey , Abbas M. Walji , Ronald Dale Ferguson, II , Christine Ng Di Marco , Thomas G. Steele , Lihong Hu , Xuanjia Peng
发明人： Thomas H. Graham , Wensheng Liu , Tao Yu , Yonglian Zhang , Sherman T. Waddell , John S. Wai , Paul J. Coleman , John M. Sanders , Mark W. Embrey , Abbas M. Walji , Ronald Dale Ferguson, II , Christine Ng Di Marco , Thomas G. Steele , Lihong Hu , Xuanjia Peng
IPC分类号： A61K31/53 , A61K45/06 , C07D471/22 , A61K31/675 , C07D491/20 , A61K31/55 , A61K31/499 , C07F9/6561 , C07D471/20 , C07D495/20
CPC分类号： A61K31/53 , A61K31/427 , A61K31/499 , A61K31/513 , A61K31/52 , A61K31/55 , A61K31/675 , A61K45/06 , C07D471/20 , C07D471/22 , C07D475/10 , C07D491/10 , C07D491/20 , C07D495/10 , C07D495/20 , C07F9/65616 , A61K2300/00
摘要： The present invention relates to Spirocyclic Heterocycle Compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, B, X, Y, R1, R2 and R11 are as defined herein. The present invention also relates to compositions comprising at least one Spirocyclic Heterocycle Compound, and methods of using the Spirocyclic Heterocycle Compounds for treating or preventing HIV infection in a subject.
摘要翻译：本发明涉及式（I）的螺环杂环化合物及其药学上可接受的盐，其中A，B，X，Y，R 1，R 2和R 11如本文所定义。本发明还涉及包含至少一种螺环杂环化合物的组合物，以及使用螺环杂环化合物治疗或预防受试者中HIV感染的方法。

3. 发明授权

US10233193B2 Fused tricyclic heterocyclic compounds useful for treating HIV infection 有权
公开(公告)号：US10233193B2
公开(公告)日：2019-03-19
申请号：US15575433
申请日：2016-05-20
申请人： MERCK SHARP & DOHME CORP. , Tao Yu , Thomas H. Graham , Sherman T. Waddell , John A. McCauley , Andrew W. Stamford , John M. Sanders , Lihong Hu , Jiaqiang Cai , Lianyun Zhao
发明人： Tao Yu , Thomas H. Graham , Sherman T. Waddell , John A. McCauley , Andrew W. Stamford , John M. Sanders , Lihong Hu , Jiaqiang Cai , Lianyun Zhao
IPC分类号： A61K31/4375 , C07D491/147 , A61K31/4355 , A61K31/437 , C07D471/14 , A61K31/427 , A61K31/4402 , A61K31/505 , A61K31/513 , A61K31/52 , A61K31/635 , A61K31/675 , A61P31/18
摘要： The present invention relates to Fused Tricyclic Heterocycle Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, B, X, Y, m, R1, R2, R3, R3, R3, R4, R5 and R9 are as defined herein. The present invention also relates to compositions comprising at least one Fused Tricyclic Heterocycle Derivative, and methods of using the Fused Tricyclic Heterocycle Derivatives for treating or preventing HIV infection in a subject.

4. 发明申请

US20170190701A1 FUSED TRICYCLIC HETEROCYCLIC COMPOUNDS AS HIV INTEGRASE INHIBITORS 审中-公开
公开(公告)号：US20170190701A1
公开(公告)日：2017-07-06
申请号：US15387732
申请日：2016-12-22
申请人： Tao Yu , Sherman T. Waddell , Thomas H. Graham , Yonglian Zhang , John A. McCauley , Andrew W. Stamford , Jiaqiang Cai , Zhiqi Qi
发明人： Tao Yu , Sherman T. Waddell , Thomas H. Graham , Yonglian Zhang , John A. McCauley , Andrew W. Stamford , Jiaqiang Cai , Zhiqi Qi
IPC分类号： C07D471/16 , A61K31/683 , A61K31/52 , A61K31/4402 , A61K31/5365 , A61K31/513 , A61K31/505 , A61K31/427 , A61K31/4985 , A61K31/635
CPC分类号： C07D471/16 , A61K31/427 , A61K31/4402 , A61K31/4985 , A61K31/505 , A61K31/513 , A61K31/52 , A61K31/5365 , A61K31/635 , A61K31/683
摘要： The present invention relates to Fused Tricyclic Heterocyclic Compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2 and R3 are as defined herein. The present invention also relates to compositions comprising at least one Fused Tricyclic Heterocyclic Compound, and methods of using the Fused Tricyclic Heterocyclic Compounds for treating or preventing HIV infection in a subject.

5. 发明授权

US11104690B2 Indazole derivatives useful as inhibitors of diacylglyceride O-acyltransferase 2 有权
公开(公告)号：US11104690B2
公开(公告)日：2021-08-31
申请号：US16461902
申请日：2017-11-13
申请人： Merck Sharp & Dohme Corp. , Dong-Ming Shen , Thomas H. Graham , Wensheng Liu , Clare Tudge , Andreas Verras , Jinlong Jiang
发明人： Dong-Ming Shen , Thomas H. Graham , Wensheng Liu , Clare Tudge , Andreas Verras , Jinlong Jiang
IPC分类号： C07D515/08 , C07D409/12 , C07D401/12 , C07D403/12 , C07D231/56 , C07D405/12 , C07D487/04 , C07D417/12 , C07D413/12 , C07D409/14
摘要： The present invention relates to a compound represented by formula I′: and pharmaceutically acceptable salts thereof. The compounds of formula I are inhibitors of diacylglyceride O-acyltransferase 2 (“DGAT2”) and may be useful in the treatment, prevention and suppression of diseases mediated by DGAT2. The compounds of the present invention may be useful in the treatment of hepatic steatosis, diabetes mellitus, obesity, hyperlipidemia, hypercholesterolemia, atherosclerosis, cardiorenal diseases such as chronic kidney diseases and heart failure and related diseases and conditions.

6. 发明授权

US10947222B2 Indole derivatives useful as inhibitors of diacylglyceride O-acyltransferase 2 有权
公开(公告)号：US10947222B2
公开(公告)日：2021-03-16
申请号：US16461880
申请日：2017-11-13
申请人： Merck Sharp & Dohme Corp. , Dong-Ming Shen , Thomas H. Graham , Jinlong Jiang , Fa-Xiang Ding , Clare Tudge
发明人： Dong-Ming Shen , Thomas H. Graham , Jinlong Jiang , Fa-Xiang Ding , Clare Tudge
IPC分类号： C07D401/12 , C07D409/12 , A61P1/16 , C07D209/08 , C07D409/14 , C07D413/12 , A61K31/506 , A61K45/06 , C07D413/14 , A61K31/404 , A61K31/4439 , C07D209/10
摘要： The present invention relates to a compound represented by formula I: and pharmaceutically acceptable salts thereof. The compounds of formula I are inhibitors of diacylglyceride O-acyltransferase 2 (“DGAT2”) and may be useful in the treatment, prevention and suppression of diseases mediated by DGAT2. The compounds of the present invention may be useful in the treatment of hepatic steatosis, diabetes mellitus, obesity, hyperlipidemia, hypercholesterolemia, atherosclerosis, nonalcoholic steatohepatitis (NASH), cardiorenal diseases such as chronic kidney diseases and heart failure and related diseases and conditions.

7. 发明申请

US20130030019A1 NOVEL PROLYLCARBOXYPEPTIDASE INHIBITORS 有权
标题翻译：新型丙烯酰胆碱酯酶抑制剂
公开(公告)号：US20130030019A1
公开(公告)日：2013-01-31
申请号：US13638991
申请日：2011-04-21
申请人： Thomas H. Graham , Dong-Ming Shen , Min Shu
发明人： Thomas H. Graham , Dong-Ming Shen , Min Shu
IPC分类号： C07D401/04 , A61K31/4545 , A61K31/454 , A61P3/00 , A61K31/4155 , A61P3/04 , A61P3/10 , C07D401/14 , C07D403/04
CPC分类号： C07D401/04 , A61K9/4858 , C07D401/14 , C07D403/04
摘要： Compounds of structural formula (I) are inhibitors of prolylcarboxypeptidase (PrCP). The compounds of the present invention are useful for the prevention and treatment of conditions related to the enzymatic activity of PrCP such as abnormal metabolism, including obesity; diabetes; metabolic syndrome; obesity related disorders; and diabetes related disorders.
摘要翻译：结构式（I）的化合物是脯氨酰羧肽酶（PrCP）的抑制剂。本发明的化合物可用于预防和治疗与PrCP的酶活性相关的病症，例如异常代谢，包括肥胖症; 糖尿病; 代谢综合征; 肥胖相关疾病; 和糖尿病相关疾病。

8. 发明授权

US5517747A Method and apparatus for the interconnection of radio frequency (RF) monolithic microwave integrated circuits 失效
标题翻译：用于射频（RF）单片微波集成电路互连的方法和装置
公开(公告)号：US5517747A
公开(公告)日：1996-05-21
申请号：US365676
申请日：1994-12-29
申请人： John A. Pierro , Thomas H. Graham , Scott M. Weiner , Paul Heller , Joseph L. Merenda
发明人： John A. Pierro , Thomas H. Graham , Scott M. Weiner , Paul Heller , Joseph L. Merenda
IPC分类号： H01P3/02 , H01P5/08 , H01P11/00 , H01R13/646 , H05K1/02
CPC分类号： H01P5/085 , H01P11/00 , H01L2224/48091 , H01L2224/48227 , H01L2224/49175 , H05K1/0237 , Y10T29/49016 , Y10T29/49162
摘要： A coaxial-to-coplanar waveguide connector is used for interconnecting stripline compatible devices utilizing coaxial cable. The connector is formed at the end of a length of coaxial cable embedded within a circuit board. The connector generally has a substantially semi-circular connection section. The connection section includes a conductor partly surrounded by an electrically insulative dielectric which is partly surrounded by a shield. An electrically conductive sheet is used to couple the shield to a ground plane of the circuit board. Electrically conductive ribbon is connect the conductor to a stripline compatible device. The coaxial-to-coplanar waveguide connector may be fabricated by coating a dielectric board with an adhesive material and then routing a length of miniature coaxial cable in the adhesive. Conductive material and dielectric material are consecutively laid upon the dielectric cable board. A portion of the board including a section of miniature coaxial cable is milled so as to remove a top portion of the cable. An electrically conductive material is coupled to the coaxial shield in order to connect the shield to a ground plane of the circuit board and the stripline compatible device. Furthermore, an additional electrically conductive ribbon is operatively connected from the conductor to the stripline compatible device.
摘要翻译：同轴对共面波导连接器用于使用同轴电缆互连带状线兼容设备。连接器形成在嵌入电路板的同轴电缆长度的端部。连接器通常具有基本上半圆形的连接部分。连接部分包括部分被电绝缘电介质包围的导体，该电绝缘电介质被屏蔽部分地包围。导电片用于将屏蔽件耦合到电路板的接地平面。导电带将导体连接到带状线兼容设备。同轴对共面波导连接器可以通过用粘合剂材料涂覆介电板并且然后将一定数量的微型同轴电缆布置在粘合剂中来制造。导电材料和电介质材料连续铺设在电介质电缆板上。包括一段微型同轴电缆的板的一部分被铣削以去除电缆的顶部。导电材料耦合到同轴屏蔽，以将屏蔽件连接到电路板和带状线兼容装置的接地平面。此外，附加的导电带从导体可操作地连接到带状线兼容装置。

9. 发明申请

US20230054411A1 7-, 8-, and 10-SUBSTITUTED AMINO TRIAZOLO QUINAZOLINE DERIVATIVES AS ADENOSINE RECEPTOR ANTAGONISTS, PHARMACEUTICAL COMPOSITIONS AND THEIR USE 有权
公开(公告)号：US20230054411A1
公开(公告)日：2023-02-23
申请号：US17294836
申请日：2019-11-26
申请人： Yonglian ZHANG , Amjad ALI , Jared CUMMING , Duane DEMONG , Qiaolin DENG , Thomas H. GRAHAM , Elisabeth HENNESSY , Matthew A. LARSEN , Kun LIU , Ping LIU , Umar Faruk MANSOOR , Jianping PAN , Christopher W. PLUMMER , Aaron SATHER , Uma SWAMINATHAN , Huijun WANG , Merck Sharp & Dohme Corp.
发明人： Yonglian Zhang , Amjad Ali , Jared Cumming , Duane DeMong , Qiaolin Deng , Thomas H. Graham , Elisabeth Hennessy , Matthew A. Larsen , Kun Liu , Ping Liu , Umar Faruk Mansoor , Jianping Pan , Christopher W. Plummer , Aaron Sather , Uma Swaminathan , Huijun Wang
IPC分类号： A61K31/519 , A61K39/395 , C07D471/04 , C07D519/00 , A61K31/55
摘要： In its many embodiments, the present invention provides certain 7-, 8-, and 10-substituted amino triazolo quinazoline derivatives of Formula (I): or a pharmaceutically acceptable salt thereof, wherein ring A, R1, R2, and R4 are as defined herein, pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other therapeutic agents), and methods for their preparation and use, alone and in combination with other therapeutic agents, as antagonists of A2a and/or A2b receptors, and their use in the treatment of a variety of diseases, conditions, or disorders that are mediated, at least in part, by the adenosine A2a receptor and/or the adenosine A2b receptor.

10. 发明授权

US08921394B2 Prolylcarboxypeptidase inhibitors 有权
标题翻译：脯氨酰羧肽酶抑制剂
公开(公告)号：US08921394B2
公开(公告)日：2014-12-30
申请号：US13638991
申请日：2011-04-21
申请人： Thomas H. Graham , Dong-Ming Shen , Min Shu
发明人： Thomas H. Graham , Dong-Ming Shen , Min Shu
IPC分类号： A01N43/00 , A61K31/33 , A01N43/40 , A61K31/435 , A61K31/445 , A61K9/48 , C07D403/04 , C07D401/14 , C07D401/04
CPC分类号： C07D401/04 , A61K9/4858 , C07D401/14 , C07D403/04
摘要： Compounds of structural formula (I) are inhibitors of prolylcarboxypeptidase (PrCP). The compounds of the present invention are useful for the prevention and treatment of conditions related to the enzymatic activity of PrCP such as abnormal metabolism, including obesity; diabetes; metabolic syndrome; obesity related disorders; and diabetes related disorders.
摘要翻译：结构式（I）的化合物是脯氨酰羧肽酶（PrCP）的抑制剂。本发明的化合物可用于预防和治疗与PrCP的酶活性相关的病症，例如异常代谢，包括肥胖症; 糖尿病; 代谢综合征; 肥胖相关疾病; 和糖尿病相关疾病。

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