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公开(公告)号：US10034891B2
公开(公告)日：2018-07-31
申请号：US15151740
申请日：2016-05-11
发明人： K. Raja Reddy , Jeff Stebbins , Serge H. Boyer , Mark D. Erion , Scott J. Hecker , Nicholas Brian Raffaele , Brett C. Bookser , Venkat Reddy Mali
IPC分类号： A01N43/82 , A61K31/41 , A61K31/675 , A61K31/542 , A61K31/52 , A61K31/662 , A61K31/665 , A61K45/06 , C07D473/16 , C07D473/34 , C07D473/40 , C07F9/30 , C07F9/32 , C07F9/653 , C07F9/6561 , C07F9/6574 , C07F9/48 , C07F9/655 , A61K31/683 , A61K31/688 , C07F9/40
CPC分类号： A61K31/675 , A61K31/52 , A61K31/542 , A61K31/662 , A61K31/665 , A61K31/683 , A61K31/688 , A61K45/06 , A61P3/04 , A61P3/10 , C07D473/16 , C07D473/34 , C07D473/40 , C07F9/303 , C07F9/3229 , C07F9/40 , C07F9/48 , C07F9/65312 , C07F9/6552 , C07F9/6561 , C07F9/65616 , C07F9/65742 , A61K2300/00
摘要： The invention pertains to the use of compounds represented by the formula, Q-G1-G2-G3-G4-Z, where Q is The compounds can be used as diacylglycerol O-acyltransferase 1 (DGAT-1) inhibitors to treat hyperlipidiemias and various diseases and disorders associated therewith. Other conditions also can be ameliorated or avoided, such as high postprandial triglycerides or diet-related hypertriglyceridemia, cardiovascular risk associated with excessive triglycerides, and insulin resistance/glucose intolerance in overweight patients, those with diabetes or other glucose metabolic disorders such as Syndrome X and/or polycystic ovary disease.
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公开(公告)号：US10174062B2
公开(公告)日：2019-01-08
申请号：US15384226
申请日：2016-12-19
发明人： Feng Tian , Qun Dang , G. Sridhar Prasad , Wenyu Li , Brett C. Bookser , Nicholas Brian Raffaele , Mark D. Erion
IPC分类号： C07D213/81 , A61K31/44 , C07F9/6558 , C07F9/58 , C07F9/653 , C07F9/6539 , C07F9/6571 , C07F9/6512 , C07F9/6561 , C07F9/6509 , C07F9/6541
摘要： The present invention provides for novel compounds of Formulas I and II and pharmaceutically acceptable salts and co-crystals thereof which have glucokinsae activator activity. The present invention further provides for pharmaceutical compositions comprising the same as well as methods of treating, preventing, delaying the time to onset or reducing the risk for the development or progression of a disease or condition for which one or more glucokinase activator is indicated, including Type 1 and 2 diabetes, impaired glucose tolerance, insulin resistance and hyperglycemia. The present invention also provides for processes of making the compounds of Formulas I and II, including salts and co-crystals thereof, and pharmaceutical compositions comprising the same.
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公开(公告)号：US10005805B2
公开(公告)日：2018-06-26
申请号：US15384226
申请日：2016-12-19
发明人： Feng Tian , Qun Dang , G. Sridhar Prasad , Wenyu Li , Brett C. Bookser , Nicholas Brian Raffaele , Mark D. Erion
IPC分类号： C07D213/81 , A61K31/44 , C07F9/6558 , C07F9/6539 , C07F9/58 , C07F9/6509 , C07F9/6541 , C07F9/6561 , C07F9/653 , C07F9/6512 , C07F9/6571
摘要： The present invention provides for novel compounds of Formulas I and II and pharmaceutically acceptable salts and co-crystals thereof which have glucokinsae activator activity. The present invention further provides for pharmaceutical compositions comprising the same as well as methods of treating, preventing, delaying the time to onset or reducing the risk for the development or progression of a disease or condition for which one or more glucokinase activator is indicated, including Type 1 and 2 diabetes, impaired glucose tolerance, insulin resistance and hyperglycemia. The present invention also provides for processes of making the compounds of Formulas I and II, including salts and co-crystals thereof, and pharmaceutical compositions comprising the same.
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公开(公告)号：US10709718B2
公开(公告)日：2020-07-14
申请号：US16025199
申请日：2018-07-02
发明人： K. Raja Reddy , Jeff Stebbins , Serge H. Boyer , Mark D. Erion , Scott J. Hecker , Nicholas Brian Raffaele , Brett C. Bookser , Venkat Reddy Mali
IPC分类号： A61K31/675 , A61K31/542 , A61K31/52 , A61K31/662 , A61K31/665 , A61K45/06 , C07D473/16 , C07D473/34 , C07D473/40 , C07F9/30 , C07F9/32 , C07F9/653 , C07F9/6561 , C07F9/6574 , A61P3/04 , A61P3/10 , C07F9/48 , C07F9/655 , A61K31/683 , A61K31/688 , C07F9/40
摘要： This invention pertains to the use of fused bicycle heterocyclic adducts of thiohydroxy pyridines or pyrimidines as diacylglycerol O-acyltransferase 1 (DGAT-1) inhibitors to treat hyperlipidiemias and various diseases and disorders associated therewith. Other conditions also be ameliorated or avoided, such as high postprandial triglycerides or diet-related hypertriglyceridemia, cardiovascular risk associated with excessive triglycerides, and insulin resistance/glucose intolerance in overweight patients, those with diabetes or other glucose metabolic disorders such as Syndrome X and/or polycystic ovary disease.
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公开(公告)号：US20150119365A1
公开(公告)日：2015-04-30
申请号：US14585073
申请日：2014-12-29
发明人： Feng Tian , Qun Dang , G. Sridhar Prasad , Wenyu Li , Brett C. Bookser , Nicholas Brian Raffaele , Mark D. Erion
IPC分类号： C07F9/6539 , C07F9/58 , C07F9/6512 , C07F9/6558 , C07F9/6509
CPC分类号： C07F9/65586 , A61K31/44 , C07C233/11 , C07D213/81 , C07F9/3834 , C07F9/4021 , C07F9/58 , C07F9/65031 , C07F9/650952 , C07F9/6512 , C07F9/653 , C07F9/6539 , C07F9/65392 , C07F9/65395 , C07F9/65397 , C07F9/6541 , C07F9/655345 , C07F9/65583 , C07F9/6561 , C07F9/65616 , C07F9/657181
摘要： The present invention provides for novel compounds of Formulas I and II and pharmaceutically acceptable salts and co-crystals thereof which have glucokinsae activator activity. The present invention further provides for pharmaceutical compositions comprising the same as well as methods of treating, preventing, delaying the time to onset or reducing the risk for the development or progression of a disease or condition for which one or more glucokinase activator is indicated, including Type 1 and 2 diabetes, impaired glucose tolerance, insulin resistance and hyperglycemia. The present invention also provides for processes of making the compounds of Formulas I and II, including salts and co-crystals thereof, and pharmaceutical compositions comprising the same.
摘要翻译： 本发明提供具有葡糖多糖激活剂活性的新颖的式I和II化合物及其药学上可接受的盐和共结晶。 本发明进一步提供包含其的药物组合物以及治疗，预防，延迟发病时间或降低其中指示出一种或多种葡萄糖激酶激活剂的疾病或病症的发展或进展的风险的方法，包括 1型和2型糖尿病，糖耐量异常，胰岛素抵抗和高血糖。 本发明还提供了制备式I和II化合物的方法，包括其盐和共结晶，以及包含其的药物组合物。
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公开(公告)号：US20180303856A1
公开(公告)日：2018-10-25
申请号：US16025199
申请日：2018-07-02
发明人： K. Raja Reddy , Jeff Stebbins , Serge H. Boyer , Mark D. Erion , Scott J. Hecker , Nicholas Brian Raffaele , Brett C. Bookser , Venkat Reddy Mali
IPC分类号： A61K31/675 , A61K31/542 , A61K31/52 , A61K31/688 , A61K31/683 , A61P3/10 , C07F9/40 , C07F9/655 , C07F9/48 , A61P3/04 , A61K31/662 , A61K31/665 , A61K45/06 , C07D473/16 , C07D473/34 , C07D473/40 , C07F9/30 , C07F9/6574 , C07F9/6561 , C07F9/653 , C07F9/32
CPC分类号： A61K31/675 , A61K31/52 , A61K31/542 , A61K31/662 , A61K31/665 , A61K31/683 , A61K31/688 , A61K45/06 , A61P3/04 , A61P3/10 , C07D473/16 , C07D473/34 , C07D473/40 , C07F9/303 , C07F9/3229 , C07F9/40 , C07F9/48 , C07F9/65312 , C07F9/6552 , C07F9/6561 , C07F9/65616 , C07F9/65742 , A61K2300/00
摘要： This invention pertains to the use of fused bicycle heterocyclic adducts of thiohydroxy pyridines or pyrimidines as diacylglycerol O-acyltransferase 1 (DGAT-1) inhibitors to treat hyperlipidiemias and various diseases and disorders associated therewith. Other conditions also be ameliorated or avoided, such as high postprandial triglycerides or diet-related hypertriglyceridemia, cardiovascular risk associated with excessive triglycerides, and insulin resistance/glucose intolerance in overweight patients, those with diabetes or other glucose metabolic disorders such as Syndrome X and/or polycystic ovary disease.
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公开(公告)号：US20170096440A1
公开(公告)日：2017-04-06
申请号：US15384226
申请日：2016-12-19
发明人： Feng Tian , Qun Dang , G. Sridhar Prasad , Wenyu Li , Brett C. Bookser , Nicholas Brian Raffaele , Mark D. Erion
IPC分类号： C07F9/6558 , C07F9/58 , C07F9/6509 , C07F9/6571 , C07F9/6561 , C07F9/653 , C07F9/6512 , C07F9/6539 , C07F9/6541
CPC分类号： C07F9/65586 , A61K31/44 , C07C233/11 , C07D213/81 , C07F9/3834 , C07F9/4021 , C07F9/58 , C07F9/65031 , C07F9/650952 , C07F9/6512 , C07F9/653 , C07F9/6539 , C07F9/65392 , C07F9/65395 , C07F9/65397 , C07F9/6541 , C07F9/655345 , C07F9/65583 , C07F9/6561 , C07F9/65616 , C07F9/657181
摘要： The present invention provides for novel compounds of Formulas I and II and pharmaceutically acceptable salts and co-crystals thereof which have glucokinsae activator activity. The present invention further provides for pharmaceutical compositions comprising the same as well as methods of treating, preventing, delaying the time to onset or reducing the risk for the development or progression of a disease or condition for which one or more glucokinase activator is indicated, including Type 1 and 2 diabetes, impaired glucose tolerance, insulin resistance and hyperglycemia. The present invention also provides for processes of making the compounds of Formulas I and II, including salts and co-crystals thereof, and pharmaceutical compositions comprising the same.
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公开(公告)号：US09522926B2
公开(公告)日：2016-12-20
申请号：US14585073
申请日：2014-12-29
发明人： Feng Tian , Qun Dang , G. Sridhar Prasad , Wenyu Li , Brett C. Bookser , Nicholas Brian Raffaele , Mark D. Erion
IPC分类号： C07C233/11 , C07F9/28 , C07F9/40 , C07F9/58 , C07F9/6503 , C07F9/6509 , C07F9/653 , C07F9/6539 , C07F9/6553 , C07F9/6561 , C07F9/6571 , C07F9/38 , C07F9/6512 , C07F9/6558 , A61K31/166 , A61K31/08 , A61K31/10 , A61K31/04 , A61P3/00 , A61P3/10
CPC分类号： C07F9/65586 , A61K31/44 , C07C233/11 , C07D213/81 , C07F9/3834 , C07F9/4021 , C07F9/58 , C07F9/65031 , C07F9/650952 , C07F9/6512 , C07F9/653 , C07F9/6539 , C07F9/65392 , C07F9/65395 , C07F9/65397 , C07F9/6541 , C07F9/655345 , C07F9/65583 , C07F9/6561 , C07F9/65616 , C07F9/657181
摘要： The present invention provides for novel compounds of Formulas I and II and pharmaceutically acceptable salts and co-crystals thereof which have glucokinsae activator activity. The present invention further provides for pharmaceutical compositions comprising the same as well as methods of treating, preventing, delaying the time to onset or reducing the risk for the development or progression of a disease or condition for which one or more glucokinase activator is indicated, including Type 1 and 2 diabetes, impaired glucose tolerance, insulin resistance and hyperglycemia. The present invention also provides for processes of making the compounds of Formulas I and II, including salts and co-crystals thereof, and pharmaceutical compositions comprising the same.
摘要翻译： 本发明提供具有葡糖多糖激活剂活性的新颖的式I和II化合物及其药学上可接受的盐和共结晶。 本发明进一步提供包含其的药物组合物以及治疗，预防，延迟发病时间或降低其中指示出一种或多种葡萄糖激酶激活剂的疾病或病症的发展或进展的风险的方法，包括 1型和2型糖尿病，糖耐量异常，胰岛素抵抗和高血糖。 本发明还提供了制备式I和II化合物的方法，包括其盐和共结晶，以及包含其的药物组合物。
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9.发明授权Inhibitors of diacylglycerol O-acyltransferase 1 (DGAT-1) and uses thereof 有权二酰基甘油O-酰基转移酶1（DGAT-1）的抑制剂及其用途公开(公告)号：US09340566B2
公开(公告)日：2016-05-17
申请号：US14628373
申请日：2015-02-23
发明人： K. Raja Reddy , Jeff Stebbins , Serge H. Boyer , Mark D. Erion , Scott J. Hecker , Nicholas Brian Raffaele , Brett C. Bookser , Venkat Reddy Mali
IPC分类号： A61K31/54 , C07F9/655 , A61K31/542 , A61K31/52 , A61K31/662 , A61K31/665 , A61K31/675 , A61K45/06 , C07D473/16 , C07D473/34 , C07D473/40 , C07F9/30 , C07F9/32 , C07F9/653 , C07F9/6561 , C07F9/6574 , C07F9/48
CPC分类号： A61K31/675 , A61K31/52 , A61K31/542 , A61K31/662 , A61K31/665 , A61K31/683 , A61K31/688 , A61K45/06 , A61P3/04 , A61P3/10 , C07D473/16 , C07D473/34 , C07D473/40 , C07F9/303 , C07F9/3229 , C07F9/40 , C07F9/48 , C07F9/65312 , C07F9/6552 , C07F9/6561 , C07F9/65616 , C07F9/65742 , A61K2300/00
摘要： The invention pertains to the use of fused bicyclo heterocyclic adducts of thiohydroxy pyridines or pyrimidines as diacylglycerol O-acyltransferase 1 (DGAT-1) inhibitors to treat hyperlipidiemias and various diseases and disorders associated therewith. Other conditions also can be ameliorated or avoided, such as high postprandial triglycerides or diet-related hypertriglyceridemia, cardiovascular risk associated with excessive triglycerides, and insulin resistance/glucose intolerance in overweight patients, those with diabetes or other glucose metabolic disorders such as Syndrome X and/or polycystic ovary disease.
摘要翻译： 本发明涉及硫代羟基吡啶或嘧啶的稠合双环杂环加合物作为二酰基甘油O-酰基转移酶1（DGAT-1）抑制剂用于治疗高脂血症和与其相关的各种疾病和病症的用途。 其他条件也可以被改善或避免，例如高餐后甘油三酸酯或饮食相关的高甘油三酯血症，与过量甘油三酯相关的心血管风险，以及超重患者，糖尿病患者或其他葡萄糖代谢紊乱如X综合征和胰岛素抵抗/葡萄糖不耐受 /或多囊卵巢疾病。
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