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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.
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2.发明申请公开(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。
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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.
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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.
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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.
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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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公开(公告)号：US20130217660A1
公开(公告)日：2013-08-22
申请号：US13642584
申请日：2011-05-12
IPC分类号： C07C237/24 , C07D295/155 , A61K31/165 , C07D213/40 , A61K31/5377 , C07D241/12 , C07D239/26 , A61K31/397 , C07D205/04 , A61K31/4453 , A61K31/40 , C07D233/61 , A61K31/4164 , A61K45/06 , C07C271/24 , C07D213/61 , A61K31/5375
CPC分类号： C07C237/24 , A61K31/165 , A61K31/397 , A61K31/40 , A61K31/4164 , A61K31/4453 , A61K31/5375 , A61K31/5377 , A61K45/06 , C07C271/24 , C07C2601/02 , C07C2601/14 , C07D205/04 , C07D213/40 , C07D213/61 , C07D213/64 , C07D213/85 , C07D233/56 , C07D233/61 , C07D239/26 , C07D241/12 , C07D295/15 , C07D295/155
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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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.
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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.
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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。
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