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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：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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公开(公告)号：US20080125605A1
公开(公告)日：2008-05-29
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
IPC分类号： C07F9/6584
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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4.发明申请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：US20120270842A1
公开(公告)日：2012-10-25
申请号：US13458452
申请日：2012-04-27
申请人： K. RAJA REDDY , Jeff Stebbins , Serge H. Boyer , Mark D. Erion , Scott J. Hecker , Nicholas Brian Raffaele , Brett C. Bookser , Venkat Reddy Mali
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： A61K31/66 , A61K31/675 , C07F9/02 , C07F9/30 , A61P3/06 , A61K31/661 , C07D473/32 , A61K31/52 , A61P3/04 , C07D498/04 , C07F9/06
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，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。 还提供适用于所公开方法的化合物和组合物。
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5.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：US08962618B2
公开(公告)日：2015-02-24
申请号：US13458452
申请日：2012-04-27
申请人： K. Raja Reddy , Jeff Stebbins , Serge H. Boyer , Mark D. Erion , Scott J. Hecker , Nicholas Brian Raffaele , Brett C. Bookser , Venkat Reddy Mali
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 , A61K31/535 , C07D513/00 , C07D265/36 , C07D498/02 , C07F9/6561 , A61K31/52 , A61K31/662 , A61K31/665 , A61K31/675 , A61K45/06 , C07D473/16 , C07D473/34 , C07D473/40 , C07F9/30 , C07F9/32 , C07F9/653 , C07F9/6574
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 thiohdroxy pridines or primidines 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： 本发明涉及硫代二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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公开(公告)号：US08664195B2
公开(公告)日：2014-03-04
申请号：US13329753
申请日：2011-12-19
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：US08080536B2
公开(公告)日：2011-12-20
申请号：US12889889
申请日：2010-09-24
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：US20110009356A1
公开(公告)日：2011-01-13
申请号：US12889889
申请日：2010-09-24
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： A61K31/7076 , C07F9/02 , A61K31/675 , C07H19/16 , A61K31/7072 , A61P31/12 , A61P35/00 , A61P33/00 , A61P3/06 , A61P3/10 , A61P3/04
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：US20090028925A1
公开(公告)日：2009-01-29
申请号：US11814819
申请日：2006-05-26
申请人： Mark D. Erion , Hongjian Jiang , Serge H. Boyer
发明人： Mark D. Erion , Hongjian Jiang , Serge H. Boyer
IPC分类号： A61K31/662 , C07F9/30 , C07F9/32 , C07F9/36 , A61K31/675 , A61K9/70 , A61K9/48 , A61K31/665 , A61P5/14 , C07F9/655 , C07F9/572
CPC分类号： C07F9/4808 , C07F9/301 , C07F9/306 , C07F9/3264 , C07F9/3282 , C07F9/3288 , C07F9/36 , C07F9/4056 , C07F9/4084 , C07F9/4087 , C07F9/5728 , C07F9/65515 , C07F9/65517 , C07F9/657172
摘要： The present invention relates to compounds of phosphonic acid-containing T3 mimetics and monoesters thereof, stereoisomers, pharmaceutically acceptable salts, co-crystals, and prodrugs thereof and pharmaceutically acceptable salts and co-crystals of the prodrugs, as well as their preparation and uses for preventing and/or treating metabolic diseases such as obesity, NASH, hypercholesterolemia and hyperlipidemia, as well as associated conditions such as atherosclerosis, coronary heart disease, impaired glucose tolerance, metabolic syndrome x and diabetes.
摘要翻译： 本发明涉及含膦酸的T3模拟物及其单酯的化合物，其立体异构体，药学上可接受的盐，共晶体和前药以及其药学上可接受的盐和共结晶，以及它们的制备和用途 预防和/或治疗诸如肥胖，NASH，高胆固醇血症和高脂血症的代谢疾病，以及相关病症如动脉粥样硬化，冠心病，葡萄糖耐量降低，代谢综合症x和糖尿病。
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公开(公告)号：US20090118236A1
公开(公告)日：2009-05-07
申请号：US10580134
申请日：2004-11-19
申请人： Mark D. Erion , Hongjian Jiang , Serge H. Boyer
发明人： Mark D. Erion , Hongjian Jiang , Serge H. Boyer
IPC分类号： A61K31/675 , C07F9/6571 , A61K31/662 , C07F9/59 , A61P5/14 , A61P3/00 , G01N33/566 , C07F9/58 , C07F9/38
CPC分类号： C07F9/4056 , C07F9/301 , C07F9/306 , C07F9/3808 , C07F9/3882 , C07F9/4006 , C07F9/4075 , C07F9/4407 , C07F9/4465 , C07F9/5728 , C07F9/58 , C07F9/65517 , C07F9/657181
摘要： The present invention relates to compounds of phosphonic acid containing T3 mimetics, stereoisomers, pharmaceutically acceptable salts, co-crystals, and prodrugs thereof and pharmaceutically acceptable salts and co-crystals of the prodrugs, as well as their preparation and uses for preventing and/or treating metabolic diseases such as obesity, NASH, hypercholesterolemia and hyperlipidemia, as well as associated conditions such as atherosclerosis, coronary heart disease, impaired glucose tolerance, metabolic syndromex and diabetes.
摘要翻译： 本发明涉及含有T3模拟物的膦酸化合物，其立体异构体，药学上可接受的盐，共晶体和前体药物以及前体药学上可接受的盐和共晶体，以及它们的制备和用途，用于预防和/或 治疗代谢疾病如肥胖，NASH，高胆固醇血症和高脂血症，以及相关病症如动脉粥样硬化，冠心病，糖耐量异常，代谢综合征和糖尿病。
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