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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：US09169201B2
公开(公告)日：2015-10-27
申请号：US14147457
申请日：2014-01-03
发明人： Jorge E. Gomez-Galeno , Raja K. Reddy , Paul D. van Poelje , Robert Huerta Lemus , Thanh Huu Nguyen , Matthew P. Grote , Qun Dang , Scott J. Hecker , Venkat Reddy Mali , Mingwei Chen , Zhili Sun , Serge Henri Boyer , Haiqing Li , William Craigo
IPC分类号： C07C307/02 , C07C309/11 , C07C309/15 , C07C317/44 , C07C323/62 , 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
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 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. The present invention also provides for processes of making the compounds of Formula I, including salts and co-crystals thereof, and pharmaceutical compositions comprising the same.
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其中指示一种或多种胰高血糖素受体拮抗剂的疾病或病症的发展或进展的风险的方法， 包括I型和II型糖尿病，胰岛素抵抗和高血糖。 本发明还提供制备式I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：US08563746B2
公开(公告)日：2013-10-22
申请号：US13125329
申请日：2009-10-19
申请人： Qun Dang , De Michael Chung , Tony S. Gibson , Hongjian Jiang , Daniel K. Cashion , Jianming Bao , Ping Lan , Huagang Lu , Gergely M. Makara , F. Anthony Romero , Iyassu Sebhat , Dariusz Wodka
发明人： Qun Dang , De Michael Chung , Tony S. Gibson , Hongjian Jiang , Daniel K. Cashion , Jianming Bao , Ping Lan , Huagang Lu , Gergely M. Makara , F. Anthony Romero , Iyassu Sebhat , Dariusz Wodka
IPC分类号： A61K31/4184 , A61K31/5377 , A61K31/497 , C07D235/26 , C07D235/28 , C07D401/10 , C07D401/06 , C07D409/04 , C07D403/10 , C07D413/10 , C07D413/14 , C07D417/04
CPC分类号： C07D235/28 , C07D235/26 , C07D401/04 , C07D401/06 , C07D403/04 , C07D403/10 , C07D405/04 , C07D409/04 , C07D409/06 , C07D417/04
摘要： Novel compounds of the structural formula (I) are activators of AMP-protein kinase and are useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention are useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension.
摘要翻译： 结构式（I）的新型化合物是AMP-蛋白激酶的活化剂，可用于治疗，预防和抑制AMPK活化蛋白激酶介导的疾病。 本发明的化合物可用于治疗2型糖尿病，高血糖症，代谢综合征，肥胖症，高胆固醇血症和高血压。
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公开(公告)号：US08410284B2
公开(公告)日：2013-04-02
申请号：US13124898
申请日：2009-10-12
申请人： Qun Dang , Tony S. Gibson , Hongjian Jiang , De Michael Chung , Jianming Bao , Jinlong Jiang , Andy Kassick , Ahmet Kekec , Ping Lan , Huagang Lu , Gergely M. Makara , F. Anthony Romero , Iyassu Sebhat , David Wilson , Dariusz Wodka , Brett C. Bookser
发明人： Qun Dang , Tony S. Gibson , Hongjian Jiang , De Michael Chung , Jianming Bao , Jinlong Jiang , Andy Kassick , Ahmet Kekec , Ping Lan , Huagang Lu , Gergely M. Makara , F. Anthony Romero , Iyassu Sebhat , David Wilson , Dariusz Wodka , Brett C. Bookser
IPC分类号： A61K31/675 , C07F9/00 , C07F9/6506
CPC分类号： C07F9/65068 , C07F9/65583 , C07F9/657181
摘要： Novel compounds of the structural formula (I) are activators of AMP-protein kinase and are useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention are useful in the treatment of Type 2 diabetes, hyperglycemia, Metabolic Syndrome, obesity, hypercholesterolemia, and hypertension.
摘要翻译： 结构式（I）的新型化合物是AMP-蛋白激酶的活化剂，可用于治疗，预防和抑制AMPK活化蛋白激酶介导的疾病。 本发明的化合物可用于治疗2型糖尿病，高血糖症，代谢综合征，肥胖，高胆固醇血症和高血压。
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公开(公告)号：US20120214769A1
公开(公告)日：2012-08-23
申请号：US13083321
申请日：2011-04-08
申请人： Jorge E. Gomez-Galeno , K. Raja Reddy , Paul D. van Poelje , Robert Huerta Lemus , Thanh Huu Nguyen , Matthew P. Grote , Qun Dang , Scott J. Hecker , Venkat Reddy Mali , Mingwei Chen , Zhili Sun , Serge Henri Boyer , Haiqing Li , William Craigo
发明人： Jorge E. Gomez-Galeno , K. Raja Reddy , Paul D. van Poelje , Robert Huerta Lemus , Thanh Huu Nguyen , Matthew P. Grote , Qun Dang , Scott J. Hecker , Venkat Reddy Mali , Mingwei Chen , Zhili Sun , Serge Henri Boyer , Haiqing Li , William Craigo
IPC分类号： A61K31/675 , A61K31/185 , C07D307/81 , A61K31/343 , C07D295/185 , A61K31/4965 , C07D213/75 , A61K31/4418 , C07D405/04 , A61K31/443 , C07D235/30 , A61K31/4184 , C07F9/655 , A61K31/665 , C07D471/04 , A61K31/437 , C07F9/40 , A61K31/662 , C07D295/135 , A61K31/5375 , C07D261/08 , A61K31/42 , C07F9/653 , A61P3/10 , A61P3/08 , A61P1/16 , A61P3/06 , A61P9/10 , A61P3/04 , A61P3/00 , C07C309/15
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 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. The present invention also provides for processes of making the compounds of Formula I, including salts and co-crystals thereof, and pharmaceutical compositions comprising the same.
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其中指示一种或多种胰高血糖素受体拮抗剂的疾病或病症的发展或进展的风险的方法， 包括I型和II型糖尿病，胰岛素抵抗和高血糖。 本发明还提供制备式I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：US07816345B2
公开(公告)日：2010-10-19
申请号：US11779689
申请日：2007-07-18
申请人： Mark D. Erion , K. Raja Reddy , Serge H. Boyer
发明人： Mark D. Erion , K. Raja Reddy , Serge H. Boyer
CPC分类号： C07F9/65846 , C07F9/65848 , C07H19/10 , C07H19/20
摘要： Novel cyclic phosphoramidate prodrugs of drugs of formula I their use in delivery of drugs to the liver, their use in enhancing oral bioavailability, and their method of preparation are described.
摘要翻译： 描述了式I药物的新型环状氨基磷酸酯前药，其用于将药物递送至肝脏，其用于提高口服生物利用度的用途及其制备方法。
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公开(公告)号：US07582758B2
公开(公告)日：2009-09-01
申请号：US11144348
申请日：2005-06-03
申请人： Kevin V. Martin
发明人： Kevin V. Martin
IPC分类号： C07D473/00
CPC分类号： C07F9/657181
摘要： Methods for the synthesis of cyclic phosphonic acid diesters from 1,3-diols are described, whereby cyclic phosphonic acid diesters are produced by reacting a chiral 1,3-diol and an activated phosphonic acid in the presence of a Lewis acid.
摘要翻译： 描述了从1,3-二醇合成环状膦酸二酯的方法，由此在路易斯酸存在下使手性1,3-二醇和活化的膦酸反应来制备环状膦酸二酯。
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8.发明授权Combination of FBPase inhibitors and antidiabetic agents useful for the treatment of diabetes 有权用于治疗糖尿病的FBP酶抑制剂和抗糖尿病药物的组合公开(公告)号：US07563774B2
公开(公告)日：2009-07-21
申请号：US09900364
申请日：2001-07-05
CPC分类号： A61K31/175 , A61K31/426 , A61K45/06
摘要： A combination therapy of at least one FBPase inhibitor and at least one other antidiabetic agent is disclosed.
摘要翻译： 公开了至少一种FBPase抑制剂和至少一种其它抗糖尿病药物的组合疗法。
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公开(公告)号：US20080070868A1
公开(公告)日：2008-03-20
申请号：US11841840
申请日：2007-08-20
申请人： Qun Dang , Joseph Kopcho , Scott Hecker , Bheemarao Ugarkar
发明人： Qun Dang , Joseph Kopcho , Scott Hecker , Bheemarao Ugarkar
IPC分类号： A61K31/675 , A61P3/08 , C07F9/02
CPC分类号： C07F9/65586 , C12N9/99
摘要： Compounds of Formula I, their prodrugs and salts, their preparation and their uses are described.
摘要翻译： 描述了式I化合物，其前体药物和盐，其制备方法及用途。
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公开(公告)号：US07205404B1
公开(公告)日：2007-04-17
申请号：US09518501
申请日：2000-03-03
申请人： Mark D. Erion , K. Raja Reddy , Serge H. Boyer
发明人： Mark D. Erion , K. Raja Reddy , Serge H. Boyer
IPC分类号： C07F9/6584 , C07F9/6527 , C07F9/02
CPC分类号： C07F9/65846 , C07F9/65848 , C07H19/10 , C07H19/20
摘要： Novel cyclic phosphoramidate prodrugs of drugs of formula I in their use in delivery of drugs to the liver, their use in enhancing oral bioavailability, and their method of preparation are described.
摘要翻译： 式I药物的新型环状氨基磷酸酯前体药物
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