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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：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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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：US20190330239A1
公开(公告)日：2019-10-31
申请号：US16461902
申请日：2017-11-13
申请人： Dong-Ming Shen , Thomas H. Graham , Wensheng LIU , Clare TUDGE , Andreas VERRAS , Jinlong JIANG , Merck Sharp & Dohme Corp.
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：US08669252B2
公开(公告)日：2014-03-11
申请号：US13642584
申请日：2011-05-12
IPC分类号： A61K31/535 , A61K31/445 , A61K31/40 , A61K31/415 , C07D295/18 , C07D413/12 , C07D211/30 , C07D207/06 , C07D233/61 , C07D205/04
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：US20130143859A1
公开(公告)日：2013-06-06
申请号：US13702622
申请日：2011-06-03
IPC分类号： A61K31/5377 , A61K45/06 , C07D401/14 , A61K31/4545 , C07D401/04 , A61K31/454
CPC分类号： A61K31/5377 , A61K31/454 , A61K31/4545 , A61K45/06 , C07D401/04 , C07D401/14
摘要： Compounds of structural formulas I-1 and I-2 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-1和I-2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：US20190276443A1
公开(公告)日：2019-09-12
申请号：US16461880
申请日：2017-11-13
申请人： Dong-Ming SHEN , Thomas H. GRAHAM , Jinlong JIANG , Fa-Xiang DING , Clare TUDGE , Merck Sharp & Dohme Corp.
发明人： Dong-Ming Shen , Thomas H. Graham , Jinlong Jiang , Fa-Xiang Ding , Clare Tudge
IPC分类号： C07D409/12 , A61P1/16 , C07D209/08 , C07D401/12 , 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, 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：US08569299B2
公开(公告)日：2013-10-29
申请号：US13702622
申请日：2011-06-03
IPC分类号： A61K31/5377 , A61K31/454 , C07D413/14 , C07D401/02 , C07D401/14
CPC分类号： A61K31/5377 , A61K31/454 , A61K31/4545 , A61K45/06 , C07D401/04 , C07D401/14
摘要： Compounds of structural formulas I-1 and I-2 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-1和I-2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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