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公开(公告)号：US20170349516A1
公开(公告)日：2017-12-07
申请号：US15487623
申请日：2017-04-14
IPC分类号： C07C31/27 , C07F9/24 , A61K31/191 , A61K31/194 , C07F9/12 , C07F9/117 , C07F9/11 , C07F9/09 , C07D495/04 , C07D405/12 , C07D309/30 , C07D309/12 , C07D309/10 , C07D307/33 , C07D305/12 , C07D261/12 , C07D261/08 , C07D257/04 , C07D213/80 , C07C309/25 , C07C309/24 , C07C309/08 , C07C255/00 , C07C69/757 , C07C69/675 , C07C69/017 , C07C69/003 , C07C65/17 , C07C62/06 , C07C62/02 , C07C61/12 , C07C59/54 , C07C59/48 , C07C59/46 , C07C59/29 , C07C59/285 , C07C59/245 , C07C59/11 , C07C59/105 , C07C59/01 , C07C47/34 , C07C47/19 , C07C33/26 , C07C31/24 , C07C31/22 , C07C31/20 , A61K31/23 , A61K31/20 , C07F9/44 , C07C2601/02 , C07C2601/04 , C07C2601/08
CPC分类号： C07C31/27 , A61K31/191 , A61K31/194 , A61K31/20 , A61K31/23 , C07C31/20 , C07C31/22 , C07C31/24 , C07C33/26 , C07C47/19 , C07C47/34 , C07C59/01 , C07C59/105 , C07C59/11 , C07C59/245 , C07C59/285 , C07C59/29 , C07C59/46 , C07C59/48 , C07C59/54 , C07C61/12 , C07C62/02 , C07C62/06 , C07C65/17 , C07C69/003 , C07C69/017 , C07C69/675 , C07C69/757 , C07C255/00 , C07C309/08 , C07C309/24 , C07C309/25 , C07C2101/02 , C07C2101/04 , C07C2101/08 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07D213/80 , C07D257/04 , C07D261/08 , C07D261/12 , C07D305/12 , C07D307/33 , C07D309/10 , C07D309/12 , C07D309/30 , C07D405/12 , C07D495/04 , C07F9/093 , C07F9/094 , C07F9/11 , C07F9/117 , C07F9/12 , C07F9/2408 , C07F9/2416 , C07F9/242 , C07F9/2425 , C07F9/4423
摘要： The present invention relates to novel hydroxyl compounds, compositions comprising hydroxyl compounds, and methods useful for treating and preventing a variety of diseases and conditions such as, but not limited to aging, Alzheimer's Disease, cancer, cardiovascular disease, diabetic nephropathy, diabetic retinopathy, a disorder of glucose metabolism, dyslipidemia, dyslipoproteinemia, hypertension, impotence, inflammation, insulin resistance, lipid elimination in bile, obesity, oxysterol elimination in bile, pancreatitis, pancreatitius, Parkinson's disease, a peroxisome proliferator activated receptor-associated disorder, phospholipid elimination in bile, renal disease, septicemia, metabolic syndrome disorders (e.g., Syndrome X), thrombotic disorder. Compounds and methods of the invention can also be used to modulate C reactive protein or enhance bile production in a patient. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents.
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2.发明申请CYCLOALKYL-HYDROXYL COMPOUNDS AND COMPOSITIONS FOR CHOLESTEROL MANAGEMENT AND RELATED USES 有权环烷基羟基化合物及其组合物用于胆固醇管理及相关用途公开(公告)号：US20150344389A1
公开(公告)日：2015-12-03
申请号：US14674025
申请日：2015-03-31
IPC分类号： C07C31/27 , C07C47/34 , C07C69/757 , C07C309/25 , C07F9/11 , C07D495/04 , C07C59/11 , C07C59/29 , C07C255/00 , C07F9/24 , C07D257/04 , C07D261/12 , C07D309/12 , C07D305/12 , C07D307/33 , C07D309/30 , C07C61/12
CPC分类号： C07C31/27 , A61K31/191 , A61K31/194 , A61K31/20 , A61K31/23 , C07C31/20 , C07C31/22 , C07C31/24 , C07C33/26 , C07C47/19 , C07C47/34 , C07C59/01 , C07C59/105 , C07C59/11 , C07C59/245 , C07C59/285 , C07C59/29 , C07C59/46 , C07C59/48 , C07C59/54 , C07C61/12 , C07C62/02 , C07C62/06 , C07C65/17 , C07C69/003 , C07C69/017 , C07C69/675 , C07C69/757 , C07C255/00 , C07C309/08 , C07C309/24 , C07C309/25 , C07C2101/02 , C07C2101/04 , C07C2101/08 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07D213/80 , C07D257/04 , C07D261/08 , C07D261/12 , C07D305/12 , C07D307/33 , C07D309/10 , C07D309/12 , C07D309/30 , C07D405/12 , C07D495/04 , C07F9/093 , C07F9/094 , C07F9/11 , C07F9/117 , C07F9/12 , C07F9/2408 , C07F9/2416 , C07F9/242 , C07F9/2425 , C07F9/4423
摘要： The present invention relates to novel cycloalkyl-hydroxyl compounds, compositions comprising hydroxyl compounds, and methods useful for treating and preventing a variety of diseases and conditions such as, but not limited to aging, Alzheimer's Disease, cancer, cardiovascular disease, diabetic nephropathy, diabetic retinopathy, a disorder of glucose metabolism, dyslipidemia, dyslipoproteinemia, hypertension, impotence, inflammation, insulin resistance, lipid elimination in bile, obesity, oxysterol elimination in bile, pancreatitis, Parkinson's disease, a peroxisome proliferator activated receptor-associated disorder, phospholipid elimination in bile, renal disease, septicemia, Syndrome X, thrombotic disorder. Compounds and methods of the invention can also be used to modulate C reactive protein or enhance bile production in a patient. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents.
摘要翻译： 本发明涉及新的环烷基 - 羟基化合物，包含羟基化合物的组合物和可用于治疗和预防各种疾病和病症例如但不限于老化，阿尔茨海默氏病，癌症，心血管疾病，糖尿病性肾病，糖尿病 视网膜病变，葡萄糖代谢紊乱，血脂异常，脂蛋白血症，高血压，阳ence，炎症，胰岛素抵抗，胆汁中的脂质消除，肥胖，胆汁中的氧固醇消除，胰腺炎，帕金森病，过氧化物酶体增殖物激活受体相关病症，磷脂消除 胆汁，肾脏疾病，败血症，X综合征，血栓形成障碍。 本发明的化合物和方法也可用于调节C反应蛋白或增强患者的胆汁产生。 在某些实施方案中，本发明的化合物，组合物和方法可用于与其它治疗剂如降胆固醇和降血糖药物组合治疗。
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公开(公告)号：US5389659A
公开(公告)日：1995-02-14
申请号：US666746
申请日：1991-03-08
IPC分类号： A61K31/415 , A61P5/38 , A61P9/00 , A61P9/08 , A61P9/10 , A61P9/12 , A61P27/02 , A61P43/00 , C07C45/45 , C07C49/175 , C07C49/213 , C07C49/255 , C07C59/29 , C07C63/331 , C07C65/30 , C07C205/45 , C07C271/06 , C07C311/08 , C07D231/12 , C07D231/14 , C07D257/04 , C07D403/10 , A61K31/41
CPC分类号： C07D231/12 , C07C205/45 , C07C45/455 , C07C49/175 , C07C49/255 , C07D231/14 , C07D403/10
摘要： The invention provides compounds of the general formula (I): ##STR1## or a physiologically acceptable salt, solvate (e.g. hydrate) or a metabolically labile ester thereof.The compounds may be used in the treatment or prophylaxis of hypertension and diseases associated with cognitive disorders.
摘要翻译： 本发明提供了通式（I）的化合物：其中（I）或其生理学上可接受的盐，溶剂合物（例如水合物）或其代谢不稳定的酯。 该化合物可用于治疗或预防与认知障碍相关的高血压和疾病。
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4.发明授权Hydroxyl compounds and compositions for cholesterol management and related uses 有权用于胆固醇管理和相关用途的羟基化合物和组合物公开(公告)号：US09000041B2
公开(公告)日：2015-04-07
申请号：US13925818
申请日：2013-06-24
IPC分类号： A61K31/20 , C07C59/245 , C07C31/20 , C07C31/22 , C07C31/24 , C07C59/11 , C07C59/285 , C07C59/29 , C07C59/46 , C07C59/48 , C07C59/54 , C07C62/02 , C07C62/06 , C07C65/17 , C07C69/757 , C07D213/80 , C07D309/10 , C07D309/12 , C07D405/12 , C07F9/09 , C07F9/117 , C07F9/24 , C07F9/44
CPC分类号： C07C31/27 , A61K31/191 , A61K31/194 , A61K31/20 , A61K31/23 , C07C31/20 , C07C31/22 , C07C31/24 , C07C33/26 , C07C47/19 , C07C47/34 , C07C59/01 , C07C59/105 , C07C59/11 , C07C59/245 , C07C59/285 , C07C59/29 , C07C59/46 , C07C59/48 , C07C59/54 , C07C61/12 , C07C62/02 , C07C62/06 , C07C65/17 , C07C69/003 , C07C69/017 , C07C69/675 , C07C69/757 , C07C255/00 , C07C309/08 , C07C309/24 , C07C309/25 , C07C2101/02 , C07C2101/04 , C07C2101/08 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07D213/80 , C07D257/04 , C07D261/08 , C07D261/12 , C07D305/12 , C07D307/33 , C07D309/10 , C07D309/12 , C07D309/30 , C07D405/12 , C07D495/04 , C07F9/093 , C07F9/094 , C07F9/11 , C07F9/117 , C07F9/12 , C07F9/2408 , C07F9/2416 , C07F9/242 , C07F9/2425 , C07F9/4423
摘要： The present invention relates to novel hydroxyl compounds, compositions comprising hydroxyl compounds, and methods useful for treating and preventing a variety of diseases and conditions such as, but not limited to aging, Alzheimer's Disease, cancer, cardiovascular disease, diabetic nephropathy, diabetic retinopathy, a disorder of glucose metabolism, dyslipidemia, dyslipoproteinemia, hypertension, impotence, inflammation, insulin resistance, lipid elimination in bile, obesity, oxysterol elimination in bile, pancreatitis, pancreatitius, Parkinson's disease, a peroxisome proliferator activated receptor-associated disorder, phospholipid elimination in bile, renal disease, septicemia, metabolic syndrome disorders (e.g., Syndrome X), thrombotic disorder. Compounds and methods of the invention can also be used to modulate C reactive protein or enhance bile production in a patient. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents.
摘要翻译： 本发明涉及新的羟基化合物，包含羟基化合物的组合物和可用于治疗和预防各种疾病和病症例如但不限于老化，阿尔茨海默氏病，癌症，心血管疾病，糖尿病性肾病，糖尿病性视网膜病变， 葡萄糖代谢异常，血脂异常，脂蛋白血症，高血压，阳ence，炎症，胰岛素抵抗，胆汁中的脂质清除，肥胖，胆汁中的氧固醇消除，胰腺炎，胰腺炎，帕金森病，过氧化物酶体增殖物激活受体相关病症，磷脂消除 胆汁，肾脏疾病，败血症，代谢综合症（如X综合症），血栓形成障碍。 本发明的化合物和方法也可用于调节C反应蛋白或增强患者的胆汁产生。 在某些实施方案中，本发明的化合物，组合物和方法可用于与其它治疗剂如降胆固醇和降血糖药物组合治疗。
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5.发明授权Process for the preparation of the lactone of 1R, cis 2,2-dimethyl-3-formyl-cyclopropane-1-carboxylic acid 失效制备1R，顺式2,2-二甲基-3-甲酰基 - 环丙烷-1-羧酸的内酯的方法
公开(公告)号：US5276167A
公开(公告)日：1994-01-04
申请号：US964500
申请日：1992-10-21
IPC分类号： C07D307/32 , C07C27/02 , C07C51/09 , C07C59/29 , C07C62/02 , C07D307/93 , C07D307/00
CPC分类号： C07D307/93
摘要： A process for preparation of a compound of the formula ##STR1##
摘要翻译： 制备式（Ⅰ）化合物的方法
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公开(公告)号：US4645858A
公开(公告)日：1987-02-24
申请号：US786027
申请日：1985-10-10
申请人： Harman S. Lowrie , John S. Baran
发明人： Harman S. Lowrie , John S. Baran
CPC分类号： C07C59/31 , C07C33/20 , C07C57/26 , C07C59/245 , C07C59/29 , C07F9/5407
摘要： Compounds of formula I are described which are useful to inhibit the formation of serum cholesterol by virtue of their ability to inhibit .beta.-hydroxy-.beta.-methylglutaryl-CoA(HMG CoA), the rate-controlling substance in the synthesis of serum cholesterol.
摘要翻译： 描述了通式I的化合物，其可用于通过抑制β-羟基-β-甲基戊二酰辅酶A（HMG CoA）（合成血清胆固醇中的速率控制物质）的能力来抑制血清胆固醇的形成。
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公开(公告)号：US10118881B2
公开(公告)日：2018-11-06
申请号：US15487623
申请日：2017-04-14
IPC分类号： A61K31/20 , C07C31/27 , C07C61/12 , C07C47/34 , C07C309/25 , C07F9/24 , C07D261/12 , C07C59/105 , C07C33/26 , C07C47/19 , C07C69/675 , C07C69/003 , C07C69/017 , C07C309/08 , C07C309/24 , C07F9/12 , C07D261/08 , C07C59/01 , A61K31/194 , A61K31/23 , A61K31/191 , C07C31/20 , C07C31/22 , C07C31/24 , C07C59/11 , C07C59/245 , C07C59/285 , C07C59/29 , C07C59/46 , C07C59/48 , C07C59/54 , C07C62/02 , C07C62/06 , C07C65/17 , C07C69/757 , C07D213/80 , C07D309/10 , C07D309/12 , C07D405/12 , C07F9/09 , C07F9/117 , C07F9/44
摘要： The present invention relates to novel hydroxyl compounds, compositions comprising hydroxyl compounds, and methods useful for treating and preventing a variety of diseases and conditions such as, but not limited to aging, Alzheimer's Disease, cancer, cardiovascular disease, diabetic nephropathy, diabetic retinopathy, a disorder of glucose metabolism, dyslipidemia, dyslipoproteinemia, hypertension, impotence, inflammation, insulin resistance, lipid elimination in bile, obesity, oxysterol elimination in bile, pancreatitis, pancreatitius, Parkinson's disease, a peroxisome proliferator activated receptor-associated disorder, phospholipid elimination in bile, renal disease, septicemia, metabolic syndrome disorders (e.g., Syndrome X), thrombotic disorder. Compounds and methods of the invention can also be used to modulate C reactive protein or enhance bile production in a patient. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents.
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8.发明授权公开(公告)号：US10047028B2
公开(公告)日：2018-08-14
申请号：US15274436
申请日：2016-09-23
IPC分类号： C07C31/27 , C07C61/12 , C07C47/34 , C07C309/25 , C07F9/24 , C07D261/12 , C07C59/105 , C07C33/26 , C07C47/19 , C07C69/675 , C07C69/003 , C07C69/017 , C07C309/08 , C07C309/24 , C07F9/12 , C07D261/08 , C07C59/01 , A61K31/194 , A61K31/23 , A61K31/20 , A61K31/191 , C07C31/20 , C07C31/22 , C07C31/24 , C07C59/11 , C07C59/245 , C07C59/285 , C07C59/29 , C07C59/46 , C07C59/48 , C07C59/54 , C07C62/02 , C07C62/06 , C07C65/17 , C07C69/757 , C07D213/80 , C07D309/10 , C07D309/12 , C07D405/12 , C07F9/09 , C07F9/117 , C07F9/44
摘要： The present invention relates to novel cycloalkyl-hydroxyl compounds, compositions comprising hydroxyl compounds, and methods useful for treating and preventing a variety of diseases and conditions such as, but not limited to aging, Alzheimer's Disease, cancer, cardiovascular disease, diabetic nephropathy, diabetic retinopathy, a disorder of glucose metabolism, dyslipidemia, dyslipoproteinemia, hypertension, impotence, inflammation, insulin resistance, lipid elimination in bile, obesity, oxysterol elimination in bile, pancreatitis, Parkinson's disease, a peroxisome proliferator activated receptor-associated disorder, phospholipid elimination in bile, renal disease, septicemia, Syndrome X, thrombotic disorder. Compounds and methods of the invention can also be used to modulate C reactive protein or enhance bile production in a patient. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents.
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9.发明申请CYCLOALKYL-HYDROXYL COMPOUNDS AND COMPOSITIONS FOR CHOLESTEROL MANAGEMENT AND RELATED USES 审中-公开环烷基羟基化合物及其组合物用于胆固醇管理及相关用途公开(公告)号：US20170073286A1
公开(公告)日：2017-03-16
申请号：US15274436
申请日：2016-09-23
IPC分类号： C07C31/27 , C07C69/757 , C07C47/34 , C07C309/25 , C07F9/11 , C07C59/11 , C07C59/29 , C07D495/04 , C07C255/00 , C07F9/24 , C07D257/04 , C07D261/12 , C07D309/12 , C07D305/12 , C07D307/33 , C07D309/30 , C07C61/12
CPC分类号： C07C31/27 , A61K31/191 , A61K31/194 , A61K31/20 , A61K31/23 , C07C31/20 , C07C31/22 , C07C31/24 , C07C33/26 , C07C47/19 , C07C47/34 , C07C59/01 , C07C59/105 , C07C59/11 , C07C59/245 , C07C59/285 , C07C59/29 , C07C59/46 , C07C59/48 , C07C59/54 , C07C61/12 , C07C62/02 , C07C62/06 , C07C65/17 , C07C69/003 , C07C69/017 , C07C69/675 , C07C69/757 , C07C255/00 , C07C309/08 , C07C309/24 , C07C309/25 , C07C2101/02 , C07C2101/04 , C07C2101/08 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07D213/80 , C07D257/04 , C07D261/08 , C07D261/12 , C07D305/12 , C07D307/33 , C07D309/10 , C07D309/12 , C07D309/30 , C07D405/12 , C07D495/04 , C07F9/093 , C07F9/094 , C07F9/11 , C07F9/117 , C07F9/12 , C07F9/2408 , C07F9/2416 , C07F9/242 , C07F9/2425 , C07F9/4423
摘要： The present invention relates to novel cycloalkyl-hydroxyl compounds, compositions comprising hydroxyl compounds, and methods useful for treating and preventing a variety of diseases and conditions such as, but not limited to aging, Alzheimer's Disease, cancer, cardiovascular disease, diabetic nephropathy, diabetic retinopathy, a disorder of glucose metabolism, dyslipidemia, dyslipoproteinemia, hypertension, impotence, inflammation, insulin resistance, lipid elimination in bile, obesity, oxysterol elimination in bile, pancreatitis, Parkinson's disease, a peroxisome proliferator activated receptor-associated disorder, phospholipid elimination in bile, renal disease, septicemia, Syndrome X, thrombotic disorder. Compounds and methods of the invention can also be used to modulate C reactive protein or enhance bile production in a patient. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents.
摘要翻译： 本发明涉及新的环烷基 - 羟基化合物，包含羟基化合物的组合物和可用于治疗和预防各种疾病和病症例如但不限于老化，阿尔茨海默氏病，癌症，心血管疾病，糖尿病性肾病，糖尿病 视网膜病变，葡萄糖代谢紊乱，血脂异常，脂蛋白血症，高血压，阳ence，炎症，胰岛素抵抗，胆汁中的脂质消除，肥胖，胆汁中的氧固醇消除，胰腺炎，帕金森病，过氧化物酶体增殖物激活受体相关病症，磷脂消除 胆汁，肾脏疾病，败血症，X综合征，血栓形成障碍。 本发明的化合物和方法也可用于调节C反应蛋白或增强患者的胆汁产生。 在某些实施方案中，本发明的化合物，组合物和方法可用于与其它治疗剂如降胆固醇和降血糖药物组合治疗。
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10.发明授权公开(公告)号：US09452964B2
公开(公告)日：2016-09-27
申请号：US14674025
申请日：2015-03-31
IPC分类号： C07C31/27 , C07C61/12 , C07C47/34 , C07C309/25 , C07F9/24 , C07D261/12 , C07C59/105 , C07C33/26 , C07C47/19 , C07C69/675 , C07C69/003 , C07C69/017 , C07C309/08 , C07F9/11 , C07C309/24 , C07F9/12 , C07D495/04 , C07C255/00 , C07D257/04 , C07D261/08 , C07D305/12 , C07D307/33 , C07C59/01 , C07D309/30 , C07C31/20 , C07C31/22 , C07C31/24 , C07C59/11 , C07C59/245 , C07C59/285 , C07C59/29 , C07C59/46 , C07C59/48 , C07C59/54 , C07C62/02 , C07C62/06 , C07C65/17 , C07C69/757 , C07D213/80 , C07D309/10 , C07D309/12 , C07D405/12 , C07F9/09 , C07F9/117 , C07F9/44
CPC分类号： C07C31/27 , A61K31/191 , A61K31/194 , A61K31/20 , A61K31/23 , C07C31/20 , C07C31/22 , C07C31/24 , C07C33/26 , C07C47/19 , C07C47/34 , C07C59/01 , C07C59/105 , C07C59/11 , C07C59/245 , C07C59/285 , C07C59/29 , C07C59/46 , C07C59/48 , C07C59/54 , C07C61/12 , C07C62/02 , C07C62/06 , C07C65/17 , C07C69/003 , C07C69/017 , C07C69/675 , C07C69/757 , C07C255/00 , C07C309/08 , C07C309/24 , C07C309/25 , C07C2101/02 , C07C2101/04 , C07C2101/08 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07D213/80 , C07D257/04 , C07D261/08 , C07D261/12 , C07D305/12 , C07D307/33 , C07D309/10 , C07D309/12 , C07D309/30 , C07D405/12 , C07D495/04 , C07F9/093 , C07F9/094 , C07F9/11 , C07F9/117 , C07F9/12 , C07F9/2408 , C07F9/2416 , C07F9/242 , C07F9/2425 , C07F9/4423
摘要： The present invention relates to novel cycloalkyl-hydroxyl compounds, compositions comprising hydroxyl compounds, and methods useful for treating and preventing a variety of diseases and conditions such as, but not limited to aging, Alzheimer's Disease, cancer, cardiovascular disease, diabetic nephropathy, diabetic retinopathy, a disorder of glucose metabolism, dyslipidemia, dyslipoproteinemia, hypertension, impotence, inflammation, insulin resistance, lipid elimination in bile, obesity, oxysterol elimination in bile, pancreatitis, Parkinson's disease, a peroxisome proliferator activated receptor-associated disorder, phospholipid elimination in bile, renal disease, septicemia, Syndrome X, thrombotic disorder. Compounds and methods of the invention can also be used to modulate C reactive protein or enhance bile production in a patient. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents.
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