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公开(公告)号：EP3366686A3
公开(公告)日：2018-10-24
申请号：EP18150958.9
申请日：2010-03-19
发明人： REDDY, K. Raja , STEBBINS, Jeff , BOYER, Serge, H. , ERION, Mark, D. , HECKER, Scott, J. , RAFFAELE, Nicholas, Brian , BOOKSER, Brett, C. , REDDY, Mali, Venkat
IPC分类号： C07D473/16 , C07D473/34 , C07D473/40 , C07F9/30 , C07F9/32 , C07F9/653 , C07F9/6561 , C07F9/6574 , A61K31/52 , A61K31/662 , A61K31/665 , A61K31/675 , A61P3/10 , A61P3/04 , A61K45/06
摘要： The invention pertains to use of DGAT-1 inhibitors to treat and/or prevent overweight, obesity 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. Compounds and compositions suitable for use in the disclosed methods are also provided. The DGAT-1 inhibiting composition comprises a DGAT-1 inhibitor, the DGAT-1 inhibitor including a compound of Formula (I), pharmaceutically acceptable salts or stereoisomers thereof,
wherein Q is:
and
Z is Z 1 ; and
Z 1 is-
2.发明授权
公开(公告)号：EP2408774B1
公开(公告)日：2014-11-26
申请号：EP10710137.0
申请日：2010-03-19
发明人： REDDY, K., Raja , STEBBINS, Jeff , BOYER, Serge, H. , ERION, Mark, D. , HECKER, Scott, J. , RAFFAELE, Nicholas, Brian , BOOKSER, Brett, C. , REDDY, Mali, Venkat
IPC分类号： C07D473/16 , C07D473/34 , C07D473/40 , C07F9/30 , C07F9/32 , C07F9/653 , C07F9/6561 , C07F9/6574 , A61K31/52 , A61K31/662 , A61K31/665 , A61K31/675 , A61P3/10 , A61P3/04 , A61K45/06
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 use of DGAT-1 inhibitors to treat and/or prevent overweight, obesity 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. Compounds and compositions suitable for use in the disclosed methods are also provided.
摘要翻译： 本发明涉及使用DGAT-1抑制剂治疗和/或预防超重，肥胖以及与之相关的各种疾病和病症。 其他条件也可以被改善或避免，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综合症患者和胰岛素抵抗/葡萄糖不耐受 /或多囊卵巢疾病。 还提供适用于所公开方法的化合物和组合物。
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公开(公告)号：EP2326618B1
公开(公告)日：2014-10-15
申请号：EP09791510.2
申请日：2009-08-13
发明人： GOMEZ-GALENO, Jorge, E. , HECKER, Scott, J. , DANG, Qun , REDDY, Mali Venkat , SUN, Zhili , GROTE, Matthew, P. , NGUYEN, Thanh Huu , LEMUS, Robert, Huerta , LI, Haiqing
IPC分类号： C07C309/15 , C07D263/57 , A61K31/167 , A61K31/423 , A61P3/10
CPC分类号： C07C309/15 , A61K31/185 , A61K31/423 , A61K45/06 , C07B2200/07 , C07C2601/14 , C07C2601/16 , C07D263/57
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公开(公告)号：EP2326618A1
公开(公告)日：2011-06-01
申请号：EP09791510.2
申请日：2009-08-13
发明人： GOMEZ-GALENO, Jorge, E. , HECKER, Scott, J. , DANG, Qun , REDDY, Mali Venkat , SUN, Zhili , GROTE, Matthew, P. , NGUYEN, Thanh Huu , LEMUS, Robert, Huerta , LI, Haiqing
IPC分类号： C07C309/15 , C07D263/57 , A61K31/167 , A61K31/423 , A61P3/10
CPC分类号： C07C309/15 , A61K31/185 , A61K31/423 , A61K45/06 , C07B2200/07 , C07C2601/14 , C07C2601/16 , C07D263/57
摘要： Provided herein are compounds, including enantiomerically pure forms thereof, and pharmaceutically acceptable salts or co-crystals and prodrugs thereof which have glucagon receptor antagonist or inverse agonist activity. Further, provided herein are 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 glucagon receptor antagonist is indicated, including Type I and II diabetes, insulin resistance and hyperglycemia. Moreover, provided herein are methods of making or manufacturing compounds disclosed herein, including enantiomerically pure forms thereof, and pharmaceutically acceptable salts or Co- crystals and prodrugs thereof. Formula I
摘要翻译： 本文提供了具有胰高血糖素受体拮抗剂或反向激动剂活性的化合物，包括其对映体纯的形式，及其药学上可接受的盐或共晶体和前药。 此外，本文提供了包含其的药物组合物以及治疗，预防，延迟发病时间或降低发生或进展一种或多种胰高血糖素受体拮抗剂的疾病或病症的风险的方法，包括 I型和II型糖尿病，胰岛素抵抗和高血糖。 此外，本文提供了制备或制备本文公开的化合物的方法，包括其对映体纯的形式，及其药学上可接受的盐或共结晶和前药。
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公开(公告)号：EP2129654A1
公开(公告)日：2009-12-09
申请号：EP08729528.3
申请日：2008-02-11
发明人： GOMEZ-GALENO, Jorge, E. , REDDY, Raja, K. , VAN POELJE, Paul, D. , LEMUS, Robert, Huerta , NGUYEN, Thanh, Huu , GROTE, Matthew, P. , DANG, Qun , HECKER, Scott, J. , MALI, Venkat, Reddy , CHEN, Mingwei , SUN, Zhili , BOYER, Serge, Henri , LI, Haiqing , CRAIGO, William
IPC分类号： C07C311/08 , C07C233/29 , C07C235/56
CPC分类号： C07C309/15 , C07C307/02 , C07C309/11 , C07C317/44 , C07C323/62 , C07C2601/02 , C07C2601/14 , C07C2601/16 , C07C2602/08 , C07C2602/10 , C07C2603/74 , C07D209/20 , C07D213/53 , C07D213/75 , C07D235/30 , C07D261/08 , C07D263/56 , C07D277/66 , C07D307/68 , C07D307/81 , C07D317/66 , C07D333/38 , C07D405/04 , C07D409/12 , C07D413/04 , C07D471/04 , C07D498/04
摘要： The present invention provides for novel compounds of Formula I and pharmaceutically acceptable salts and co-crystals thereof which have glucagon receptor antagonist or inverse agonist activity. The present invention further provides for pharmaceutical compositions comprising the same as well as their use in 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 glucagon receptor antagonist is indicated, including Type I and II diabetes, insulin resistence and hyperglycemia.
摘要翻译： 本发明提供具有胰高血糖素受体拮抗剂或反向激动剂活性的新颖的式I化合物及其药学上可接受的盐和共晶体。 本发明进一步提供包含其的药物组合物以及它们在治疗，预防，延迟发病时间或降低发生或进展一种或多种胰高血糖素受体拮抗剂的疾病或病症的风险的方法中的用途 被指出，包括I型和II型糖尿病，胰岛素抵抗和高血糖。
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公开(公告)号：EP3366686B1
公开(公告)日：2020-09-09
申请号：EP18150958.9
申请日：2010-03-19
发明人： REDDY, K. Raja , STEBBINS, Jeff , BOYER, Serge, H. , ERION, Mark, D. , HECKER, Scott, J. , RAFFAELE, Nicholas, Brian , BOOKSER, Brett, C. , REDDY, Mali, Venkat
IPC分类号： C07D473/16 , C07D473/34 , C07D473/40 , C07F9/30 , C07F9/32 , C07F9/653 , C07F9/6561 , C07F9/6574 , A61K31/52 , A61K31/662 , A61K31/665 , A61K31/675 , A61P3/10 , A61P3/04 , A61K45/06
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公开(公告)号：EP3366686A2
公开(公告)日：2018-08-29
申请号：EP18150958.9
申请日：2010-03-19
发明人： REDDY, K. Raja , STEBBINS, Jeff , BOYER, Serge, H. , ERION, Mark, D. , HECKER, Scott, J. , RAFFAELE, Nicholas, Brian , BOOKSER, Brett, C. , REDDY, Mali, Venkat
IPC分类号： C07D473/16 , C07D473/34 , C07D473/40 , C07F9/30 , C07F9/32 , C07F9/653 , C07F9/6561 , C07F9/6574 , A61K31/52 , A61K31/662 , A61K31/665 , A61K31/675 , A61P3/10 , A61P3/04 , A61K45/06
摘要： The invention pertains to use of DGAT-1 inhibitors to treat and/or prevent overweight, obesity 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. Compounds and compositions suitable for use in the disclosed methods are also provided. The DGAT-1 inhibiting composition comprises a DGAT-1 inhibitor, the DGAT-1 inhibitor including a compound of Formula (I), pharmaceutically acceptable salts or stereoisomers thereof,
wherein Q is:
and
Z is Z 1 ; and
Z 1 is-
公开(公告)号：EP3153501A1
公开(公告)日：2017-04-12
申请号：EP16198552.8
申请日：2009-08-13
发明人： GOMEZ-GALENO, Jorge, E. , HECKER, Scott, J. , DANG, Qun , REDDY, Mali Venkat , SUN, Zhili , GROTE, Matthew, P. , NGUYEN, Thanh Huu , LEMUS, Robert, Huerta , LI, Haiqing
IPC分类号： C07C309/15 , C07D263/57 , A61K31/185 , A61K31/423 , A61P3/10
CPC分类号： C07C309/15 , A61K31/185 , A61K31/423 , A61K45/06 , C07B2200/07 , C07C2601/14 , C07C2601/16 , C07D263/57
摘要： Provided herein are compounds of Formula I, where the variables are as defined herein, and pharmaceutically acceptable salts, solvates or prodrugs thereof having an optical purity of at least 95% of the R enantiomer which have glucagon receptor antagonist or inverse agonist activity. Further, provided herein are pharmaceutical compositions comprising the same as well the the same for use in methods of treating, preventing or ameliorating a condition, disorder or disease for which one or more glucagon receptor antagonist is indicated, including Type I and II diabetes, insulin resistance and hyperglycemia.
Formula I摘要翻译： 本文提供式I化合物，其中变量如本文所定义，以及其具有至少95％的具有胰高血糖素受体拮抗剂或反向激动剂活性的R对映异构体的光学纯度的药学上可接受的盐，溶剂合物或前药。 此外，本文提供的药物组合物包含与用于治疗，预防或改善指示一种或多种胰高血糖素受体拮抗剂的病症，障碍或疾病相关的药物组合物，包括I型和II型糖尿病，胰岛素 抵抗和高血糖。 一级方程式
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公开(公告)号：EP2129654B1
公开(公告)日：2014-05-28
申请号：EP08729528.3
申请日：2008-02-11
发明人： GOMEZ-GALENO, Jorge, E. , REDDY, Raja, K. , VAN POELJE, Paul, D. , LEMUS, Robert, Huerta , NGUYEN, Thanh, Huu , GROTE, Matthew, P. , DANG, Qun , HECKER, Scott, J. , MALI, Venkat, Reddy , CHEN, Mingwei , SUN, Zhili , BOYER, Serge, Henri , LI, Haiqing , CRAIGO, William
IPC分类号： C07C307/02 , C07C309/11 , C07C309/15 , C07C317/44 , C07C323/62 , C07D213/75 , C07D235/30 , C07D261/08 , C07D263/56 , C07D307/68 , C07D317/66 , C07D333/38 , A61K31/185 , A61P3/06 , A61P3/10
CPC分类号： C07C309/15 , C07C307/02 , C07C309/11 , C07C317/44 , C07C323/62 , C07C2601/02 , C07C2601/14 , C07C2601/16 , C07C2602/08 , C07C2602/10 , C07C2603/74 , C07D209/20 , C07D213/53 , C07D213/75 , C07D235/30 , C07D261/08 , C07D263/56 , C07D277/66 , C07D307/68 , C07D307/81 , C07D317/66 , C07D333/38 , C07D405/04 , C07D409/12 , C07D413/04 , C07D471/04 , C07D498/04
摘要： The present invention provides for novel compounds of Formula I and pharmaceutically acceptable salts and co-crystals thereof which have glucagon receptor antagonist or inverse agonist activity. The present invention further provides for pharmaceutical compositions comprising the same as well as their use in 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 glucagon receptor antagonist is indicated, including Type I and II diabetes, insulin resistence and hyperglycemia.
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公开(公告)号：EP2786985B1
公开(公告)日：2018-11-28
申请号：EP14162609.3
申请日：2008-02-11
发明人： GOMEZ-GALENO, Jorge, E. , REDDY, Raja, K. , VAN POLJE, Paul, D. , LEMUS, Robert, Huerta , NGUYEN, Thanh, Huu , GROTE, Matthew, P. , DANG, Qun , HECKER, Scott, J. , REDDY, Mali, Venkat , CHEN, Mingwei , SUN, Zhili , BOYER, Serge, Henri , LI, Haiqing , CRAIGO, William
IPC分类号： C07C307/02 , C07C309/11 , C07C309/15 , C07C317/44 , C07C323/62 , C07D209/20 , C07D213/75 , C07D261/08 , C07D333/38 , C07D405/04 , C07D498/04 , A61K31/185 , A61P3/06 , A61P3/10
CPC分类号： C07C309/15 , C07C307/02 , C07C309/11 , C07C317/44 , C07C323/62 , C07C2601/02 , C07C2601/14 , C07C2601/16 , C07C2602/08 , C07C2602/10 , C07C2603/74 , C07D209/20 , C07D213/53 , C07D213/75 , C07D235/30 , C07D261/08 , C07D263/56 , C07D277/66 , C07D307/68 , C07D307/81 , C07D317/66 , C07D333/38 , C07D405/04 , C07D409/12 , C07D413/04 , C07D471/04 , C07D498/04
摘要： The present invention provides for novel compounds of Formula I and pharmaceutically acceptable salts and co-crystals thereof which have glucagon receptor antagonist or inverse agonist activity. The present invention further provides for pharmaceutical compositions comprising the same as well as their use in 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 glucagon receptor antagonist is indicated, including Type I and II diabetes, insulin resistence and hyperglycemia.
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