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1. 发明申请

WO2016149405A1 FIXED DOSE COMBINATIONS COMPRISING ETC1002 AND ONE OR MORE STATINS FOR TREATING OR REDUCING CARDIOVASCULAR RISK 审中-公开
标题翻译：包含ETC1002的固定剂量组合和一种或多种用于治疗或减少心血管风险的统计数据
公开(公告)号：WO2016149405A1
公开(公告)日：2016-09-22
申请号：PCT/US2016/022694
申请日：2016-03-16
申请人： ESPERION THERAPEUTICS, INC.
发明人： NEWTON, Roger, Schofield , ROSENBERG, Noah, Laban , MCDOUGALL, Diane, Elaine
IPC分类号： A61K31/194 , A61P9/10 , A61P3/06
CPC分类号： A61K31/20 , A61K31/22 , A61K31/366 , A61K31/40 , A61K31/405 , A61K31/47 , A61K31/505 , A61K2300/00
摘要： Disclosed herein are compositions comprising fixed doses of ETC-1002 and one or more statins. Also disclosed herein are methods for using fixed doses of ETC-1002 and one or more statins. Uses include methods of treating cardiovascular disease or reducing the risk of cardiovascular disease in a subject. Uses also include methods of treating hypercholesterolemia in a subject.
摘要翻译：本文公开了包含固定剂量的ETC-1002和一种或多种他汀类的组合物。本文还公开了使用固定剂量的ETC-1002和一种或多种他汀类药物的方法。用途包括治疗心血管疾病或降低受试者心血管疾病风险的方法。用途还包括在受试者中治疗高胆固醇血症的方法。

2. 发明申请

WO2005068420A1 UREA AND THIOUREA COMPOUNDS AND COMPOSITIONS FOR CHOLESTEROL MANAGEMENT AND RELATED USES 审中-公开
标题翻译：尿素和硫脲化合物和组合物用于胆固醇管理和相关用途
公开(公告)号：WO2005068420A1
公开(公告)日：2005-07-28
申请号：PCT/US2003/041789
申请日：2003-12-23
申请人： ESPERION THERAPEUTICS, INC.
发明人： DASSEUX, Jean-Louis, Henri , ONICIU, Daniela, Carmen
IPC分类号： C07C335/08
CPC分类号： C07D257/04 , C07C275/06 , C07C275/24 , C07C335/08 , C07C335/12 , C07D233/72 , C07D233/84 , C07D261/12 , C07D305/12 , C07D307/33 , C07D309/12 , C07D309/28 , C07D309/30 , C07D495/04 , C07F9/091 , C07F9/2408
摘要： The present invention relates to novel urea and thiourea compounds, compositions comprising urea or thiourea compounds, and methods useful for treating and preventing aging, Alzheimer’s Disease, cancer, cardiovascular disease, diabetic nephropathy, diabetic retinopathy, a disorder of glucose metabolism, dyslipidemia, dyslipoproteinemia, enhancing bile production, enhancing reverse lipid transport, hypertension, impotence, inflammation, insulin resistance, lipid elimination in bile, modulating C reactive protein, obesity, oxysterol elimination in bile, pancreatitis, Parkinson’s disease, a peroxisome proliferator activated receptor-associated disorder, phospholipid elimination in bile, renal disease, septicemia, metabolic syndrome disorders ( e.g ., Syndrome X), a thrombotic disorder, gastrointestinal disease , irritable bowel syndrome (IBS), inflammatory bowel disease ( e.g ., Crohn’s Disease, ulcerative colitis), arthritis ( e.g ., rheumatoid arthritis, osteoarthritis), autoimmune disease ( e.g ., systemic lupus erythematosus), scleroderma, ankylosing spondylitis, gout and pseudogout, muscle painö polymyositis/polymyogia rheumatica/bifrositis; infection and arthritis, juvenile rheumatoid arthritis, tendonitis, bursitis and other soft tissue rheumatism. 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：本发明涉及新型尿素和硫脲化合物，包含尿素或硫脲化合物的组合物，以及用于治疗和预防衰老，阿尔茨海默病，癌症，心血管疾病，糖尿病性肾病，糖尿病性视网膜病变，葡萄糖代谢障碍，血脂异常，血脂异常增加胆汁产生，增强胆汁产生，增加逆转脂质运输，高血压，阳ence，炎症，胰岛素抵抗，胆汁中的脂质消除，调节C反应蛋白，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疾病，胆汁中的磷脂消除，肾脏疾病，败血症，代谢综合症（例如，X综合症），血栓形成障碍，胃肠道疾病，肠易激综合征（IBS），炎性肠病（例如克罗恩病，溃疡性结肠炎），关节炎，类风湿性关节炎，骨关节炎），自身免疫性疾病（例如，系统性红斑狼疮），硬皮病，强直性脊柱炎，痛风和假阴性，肌肉多肌炎/多粘液性风湿性/双性炎; 感染和关节炎，青少年类风湿关节炎，腱炎，滑囊炎等软组织风湿病。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。

3. 发明申请

WO2004067489A8 HYDROXYL COMPOUNDS AND COMPOSITIONS FOR CHOLESTEROL MANAGEMENT AND RELATED USES 审中-公开
标题翻译：羟丙基化合物和组合物用于胆固醇管理和相关用途
公开(公告)号：WO2004067489A8
公开(公告)日：2005-02-17
申请号：PCT/US0341411
申请日：2003-12-23
申请人： ESPERION THERAPEUTICS INC , DASSEUX JEAN-LOUIS HENRI , ONICIU DANIELA CARMEN
发明人： DASSEUX JEAN-LOUIS HENRI , ONICIU DANIELA CARMEN
IPC分类号： A61P3/10 , 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 , C07F9/24 , C07F9/44 , A61K31/047 , C07C59/105 , C07C261/04 , C07C311/24 , C07D207/44 , C07D233/02 , C07D257/04 , C07D261/12 , C07D309/38 , C07F9/06 , C07F9/22
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，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。

4. 发明申请

WO2003097696A1 METHODS AND COPOSITIONS FOR THE TREATMENT OF ISCHEMIC REPERFUSION 审中-公开
标题翻译：用于治疗间歇性再灌注的方法和联合
公开(公告)号：WO2003097696A1
公开(公告)日：2003-11-27
申请号：PCT/US2003/015469
申请日：2003-05-16
申请人： ESPERION THERAPEUTICS, INC.
发明人： BISGAIER, Charles, L.
IPC分类号： C07K16/00
CPC分类号： A61K31/727 , A61K9/1275 , A61K31/4365 , A61K31/60 , A61K38/1709 , A61K38/49 , A61K2300/00
摘要： The invention provides methods and compositions for treating or preventing ischemic reperfusion injury. The methods of the instant invention comprise the administration of compositions comprising apolipoproteins, lecithin cholesterol acyltransferase or paraoxo nase to treat, reduce or prevent ischemic reperfusion injury.
摘要翻译：本发明提供了治疗或预防缺血再灌注损伤的方法和组合物。本发明的方法包括给予包含载脂蛋白，卵磷脂胆固醇酰基转移酶或对氧磷酸酶的组合物以治疗，减少或预防缺血再灌注损伤。

5. 发明申请

WO2003026588A3 METHODS AND APPARATUS FOR EXTRUSION OF VESICLES AT HIGH PRESSURE 审中-公开
公开(公告)号：WO2003026588A3
公开(公告)日：2003-04-03
申请号：PCT/US2002/031019
申请日：2002-09-27
申请人： ESPERION THERAPEUTICS, INC.
发明人： HILL, Knut, R. , RODRIGUEZA, Wendi , SY, Gavin, A.
IPC分类号： A61K3/127
摘要： This invention discloses devices and general methods to produce vesicles, including micelles, and particularly liposomes, by extruding solutions comprising materials capable of forming vesicles through a screen membrane at high pressure (Figure 1).

6. 发明申请

WO0230882A9 SULFOXIDE AND BIS-SULFOXIDE COMPOUNDS AND COMPOSITIONS FOR CHOLESTEROL MANAGEMENT AND RELATED USES 审中-公开
标题翻译：硫代脂肪酸和双硫代磷脂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：WO0230882A9
公开(公告)日：2003-02-20
申请号：PCT/US0131871
申请日：2001-10-11
申请人： ESPERION THERAPEUTICS INC
发明人： DASSEUX JEAN-LOUIS H , ONICIU CARMEN DANIELA
IPC分类号： A61P1/18 , A61K31/10 , A61P3/00 , A61P3/04 , A61P3/06 , A61P3/08 , A61P7/02 , A61P9/00 , A61P9/12 , A61P13/12 , A61P15/10 , A61P25/28 , A61P29/00 , A61P31/04 , A61P35/00 , C07C59/347 , C07C317/04 , C07C317/10 , C07C317/14 , C07C317/18 , C07C317/22 , C07C317/24 , C07C317/44 , C07C323/60 , C07D233/76 , C07D233/86 , C07D257/04 , C07D261/12 , C07D305/12 , C07D307/32 , C07D307/33 , C07D309/12 , C07D309/30 , C07D309/38 , C07D333/48 , C07D335/02 , C07F9/09 , C07F9/24 , C07F9/44 , C07D233/40 , C07D233/42 , C07D249/04 , C07D309/40 , C07D495/04
CPC分类号： C07F9/2408 , C07C59/347 , C07C317/04 , C07C317/14 , C07C317/18 , C07C317/24 , C07C317/44 , C07D233/76 , C07D233/86 , C07D257/04 , C07D261/12 , C07D305/12 , C07D307/32 , C07D307/33 , C07D309/12 , C07D309/30 , C07D309/38 , C07D333/48 , C07D335/02 , C07F9/091 , C07F9/094 , C07F9/4407
摘要： The present invention relates to novel sulfoxide and bis-sulfoxide compounds, compositions comprising sulfoxide and bis-sulfoxide compounds, and methods useful for treating and preventing caridovascular diseases, dyslipidemias, dysproteinemias, and glucose metabolism disorders comprising administering a composition comprising an ether compound. The compounds, compositions, and methods of the invention are also useful for treating and preventing Alzheimer's Disease, Syndrome X, peroxisome proliferator activated receptor-related disorders, septicemia, thrombotic disorders, obesity, pancreatitis, hypertension, renal disease, cancer inflammation, and impotence. 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：本发明涉及新的亚砜和双亚砜化合物，包含亚砜和双亚砜化合物的组合物，以及可用于治疗和预防血管内疾病，血脂异常，dysproteinemias和葡萄糖代谢紊乱的方法，包括施用包含醚化合物的组合物。本发明的化合物，组合物和方法也可用于治疗和预防阿尔茨海默病，综合征X，过氧化物酶体增殖物激活受体相关病症，败血症，血栓形成障碍，肥胖症，胰腺炎，高血压，肾脏疾病，癌症发炎和阳ence 。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。

7. 发明申请

WO2002030860A3 KETONE COMPOUNDS AND COMPOSITIONS FOR CHOLESTEROL MANAGEMENT AND RELATED USES 审中-公开
公开(公告)号：WO2002030860A3
公开(公告)日：2002-04-18
申请号：PCT/US2001/031872
申请日：2001-10-11
申请人： ESPERION THERAPEUTICS, INC.
发明人： DASSEUX, Jean-Louis, H. , ONICIU, Carmen, Daniela
IPC分类号： C07C49/17
摘要： The present invention relates to novel ketone compounds, compositions comprising ketone compounds, and methods useful for treating and preventing cardiovascular diseases, dyslipidemias, dysproteinemias, and glucose metabolism disorders comprising administering a composition comprising a ketone compound. The compounds, compositions, and methods of the invention are also useful for treating and preventing Alzheimer's Disease, Syndrome X, peroxisome proliferator activated receptor-related disorders, septicemia, thrombotic disorders, obesity, pancreatitis, hypertension, renal disease, cancer, inflammation, and impotence. 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.

8. 发明申请

WO2011143362A1 DIMERIC OXIDATION-RESISTANT APOLIPOPROTEIN A1 VARIANTS 审中-公开
标题翻译：二氧化硫抗氧化蛋白A1变体
公开(公告)号：WO2011143362A1
公开(公告)日：2011-11-17
申请号：PCT/US2011/036144
申请日：2011-05-11
申请人： ESPERION THERAPEUTICS, INC. , NEWTON, Roger, S. , SRIVASTAVA, Ajit, K. , HURLEY, Tim , CRAMER, Clay , FILIPPOV, Sergey, V. , PINKOSKY, Stephen, L.
发明人： NEWTON, Roger, S. , SRIVASTAVA, Ajit, K. , HURLEY, Tim , CRAMER, Clay , FILIPPOV, Sergey, V. , PINKOSKY, Stephen, L.
IPC分类号： A61K38/17 , C07K14/775
CPC分类号： C07K14/775 , A61K38/00
摘要： An isolated oxidation-resistant ApoA1 variant dimer includes a first oxidation-resistant ApoA1 variant polypeptide monomer and a second oxidation-resistant ApoA1 variant polypeptide monomer, wherein at least one of the first and the second monomers comprises at least one amino acid substitution of a tryptophan residue for an oxidation resistant amino acid, or a functional fragment or variant thereof. Methods for treating a disease or disorder comprises administering to a subject in need thereof, a therapeutically effective amount of an isolated oxidation-resistant ApoA1 variant dimer, an oxidation-resistant ApoA1 variant monomer, an oxidation-resistant ApoA1 monomer -lipid complex, a lipid complexed oxidation-resistant ApoA1 variant monomer, a lipid complexed oxidation-resistant ApoA1 variant dimer, or combinations thereof to the subject to enhance cholesterol efflux activity in the presence of an oxidant.
摘要翻译：分离的抗氧化ApoA1变体二聚体包括第一抗氧化ApoA1变体多肽单体和第二抗氧化ApoA1变体多肽单体，其中第一和第二单体中的至少一个包含至少一个色氨酸的氨基酸取代用于抗氧化氨基酸的残基或其功能片段或变体。用于治疗疾病或病症的方法包括向有需要的受试者施用治疗有效量的分离的抗氧化ApoA1变体二聚体，抗氧化ApoA1变体单体，抗氧化ApoA1单体脂质复合物，脂质复合抗氧化ApoA1变体单体，脂质复合抗氧化ApoA1变体二聚体或其组合，以增强氧化剂存在下的胆固醇流出活性。

9. 发明申请

WO2005041866A3 PHARMACEUTICAL FORMULATIONS, METHODS AND DOSING REGIMENS FOR THE TREATMENT AND PREVENTION OF ACUTE CORONARY SYNDROMES 审中-公开
标题翻译：用于治疗和预防急性冠状动脉综合征的药物制剂，方法和剂量方案
公开(公告)号：WO2005041866A3
公开(公告)日：2006-05-18
申请号：PCT/US2004034800
申请日：2004-10-19
申请人： ESPERION THERAPEUTICS INC , BISGAIER CHARLES L , RODRIGUEZA WENDI V , LALWANI NARENDRA D , HARTMAN DANIEL , JOHANSSON JAN
发明人： BISGAIER CHARLES L , RODRIGUEZA WENDI V , LALWANI NARENDRA D , HARTMAN DANIEL , JOHANSSON JAN
IPC分类号： A01N37/18 , A61K20060101 , A61K9/00 , A61K9/127 , A61K38/00 , A61K38/17
CPC分类号： A61K9/0019 , A61K9/127 , A61K38/1709 , A61K47/26 , A61K47/544
摘要： The invention provides methods and formulations for treating and preventing acute coronary syndromes. The methods of the instant invention provide safe and effective doses of an Apolipoprotein A-I Milano: phospholipid complex to reduce and stabilize atherosclerotic plaque. Pharmaceutical fomrulations of the Apo A-I Milano: phospholipid complexes are also provided.
摘要翻译：本发明提供治疗和预防急性冠状动脉综合征的方法和制剂。本发明的方法提供安全有效的剂量的载脂蛋白A-1 Milano：磷脂复合物，以减少和稳定动脉粥样硬化斑块。还提供Apo A-I Milano的药物制剂：磷脂复合物。

10. 发明申请

WO2005047236A1 SULFOXIDE AND BIS-SULFOXIDE COMPOUNDS AND COMPOSITIONS FOR CHOLESTEROL MANAGEMENT AND RELATED USES 审中-公开
标题翻译：硫代脂肪酸和双硫代磷脂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：WO2005047236A1
公开(公告)日：2005-05-26
申请号：PCT/US2003/041614
申请日：2003-12-24
申请人： ESPERION THERAPEUTICS, INC. , DASSEUX, Jean-Louis , ONICIU, Carmen, Daniela
发明人： DASSEUX, Jean-Louis , ONICIU, Carmen, Daniela
IPC分类号： C07C317/18
CPC分类号： C07C317/04 , C07C59/347 , C07C317/10 , C07C317/14 , C07C317/18 , C07C317/24 , C07C317/44 , C07D233/76 , C07D233/86 , C07D257/04 , C07D261/12 , C07D305/12 , C07D307/32 , C07D307/33 , C07D309/12 , C07D309/30 , C07D309/38 , C07D333/48 , C07D335/02 , C07F9/091 , C07F9/094 , C07F9/2408 , C07F9/4407
摘要： The present invention relates to sulfoxide and bis-sulfoxide compounds of formula (I), formula (II), or formula (III), compositions comprising sulfoxide and bis-sulfoxide compounds, and methods useful for treating and preventing cardiovascular diseases, dyslipidemias, dysproteinemias, and glucose metabolism disorders comprising administering a composition comprising an ether compound. The compounds, compositions, and methods of the invention are also useful for treating and preventing Alzheimer's Disease, Syndrome X, peroxisome proliferator activated receptor-related disorders, septicemia, thrombotic disorders, obesity, pancreatitis, hypertension, renal disease, cancer, inflammation, and impotence. 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：本发明涉及式（I），式（II）或式（III）的亚砜和双亚砜化合物，包含亚砜和双亚砜化合物的组合物，以及可用于治疗和预防心血管疾病，血脂异常，dysproteinemias 和葡萄糖代谢紊乱，包括施用包含醚化合物的组合物。本发明的化合物，组合物和方法还可用于治疗和预防阿尔茨海默病，综合征X，过氧化物酶体增殖物激活受体相关病症，败血症，血栓形成障碍，肥胖症，胰腺炎，高血压，肾脏疾病，癌症，炎症和阳痿。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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