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1. 发明申请

WO2002100351A2 A METHOD FOR TREATING INFLAMMATORY DISEASES BY ADMINISTERING A PPAR-DELTA AGONIST 审中-公开
标题翻译：通过管理PPAR-DELTA AGONIST治疗炎症疾病的方法
公开(公告)号：WO2002100351A2
公开(公告)日：2002-12-19
申请号：PCT/US2002/020974
申请日：2002-06-07
申请人： MERCK & CO., INC. , FORREST, Michael, J. , BERGER, Joel, P. , MOLLER, David, E. , WRIGHT, Samuel
发明人： FORREST, Michael, J. , BERGER, Joel, P. , MOLLER, David, E. , WRIGHT, Samuel
IPC分类号： A61K
CPC分类号： A61K45/06
摘要： A method for treating, controlling, preventing or reducing the risk of contracting an inflammatory disease or condition in a mammalian patient, comprises the steps of (1) selecting a patient in need thereof, and (2) treating the patient with a therapeutically effective amount of a composition comprising a PPAR-δ agonist. Inflammatory diseases that may be treated by this method include but are not limited to rheumatoid arthritis, juvenile rheumatoid arthritis, systemic lupus erythematosus, osteoarthritis, degenerative joint disease, one or more connective tissue diseases, ankylosing spondylitis, and bursitis.
摘要翻译：一种用于治疗，控制，预防或降低在哺乳动物患者中发生炎性疾病或病症的风险的方法，包括以下步骤：（1）选择有需要的患者，和（2）以治疗有效量治疗患者包含PPAR-δ激动剂的组合物。可以通过该方法治疗的炎性疾病包括但不限于类风湿性关节炎，幼年类风湿性关节炎，系统性红斑狼疮，骨关节炎，退行性关节疾病，一种或多种结缔组织疾病，强直性脊柱炎和滑囊炎。

2. 发明申请

WO2003000301A1 COMBINATION OF A PPAR-ALPHA LIGAND AND GLUCOCORTICOID FOR THE TREATMENT OR PREVENTION OF INFLAMMATION 审中-公开
标题翻译：用于治疗或预防感染的PPAR-ALPHA配体和葡萄糖激素的组合
公开(公告)号：WO2003000301A1
公开(公告)日：2003-01-03
申请号：PCT/US2002/019520
申请日：2002-06-19
申请人： MERCK & CO., INC. , WRIGHT, Samuel, D.
发明人： WRIGHT, Samuel, D.
IPC分类号： A61L9/04
CPC分类号： A61K45/06 , A61K31/573 , A61K2300/00
摘要： The present invention relates to a method for treating or preventing an inflammatory disease or condition in a patient in need thereof comprising concomitantly administering to said patient a PPARα agonist and a glucocorticoid in amounts that are effective to treat or prevent the inflammatory disease or condition. Pharmaceutical compositions for treating or preventing an inflammatory disease or condition are also encompassed.
摘要翻译：本发明涉及一种治疗或预防有需要的患者的炎性疾病或病症的方法，其包括对所述患者同时施用PPAR和α; 激动剂和糖皮质激素，其用量可以有效治疗或预防炎性疾病或病症。也包括用于治疗或预防炎性疾病或病症的药物组合物。

3. 发明申请

WO2002085123A1 PPAR-ALPHA-GAMMA LIGANDS OR AGONISTS FOR THE TREATMENT OF INFLAMMATION 审中-公开
标题翻译：用于治疗感染的PPAR-ALPHA-GAMMA配偶或激素
公开(公告)号：WO2002085123A1
公开(公告)日：2002-10-31
申请号：PCT/US2002/011990
申请日：2002-04-12
申请人： MERCK & CO., INC. , WRIGHT, Samuel, D. , CAI, Tian-Quan
发明人： WRIGHT, Samuel, D. , CAI, Tian-Quan
IPC分类号： A01N61/00
CPC分类号： A61K45/06 , A61K31/00 , A61K2300/00
摘要： The invention encompasses a method for treating or preventing an inflammatory disease or condition in a mammalian patient in need of such treatment or prevention comprising administering to said patient a compound that is capable of simultaneously binding PPARα and PPARγ or concomitantly administering a compound that selectively binds PPARα with a compound that selectively binds PPARγ in an amount that is effective to treat or prevent the inflammatory disease or condition. The invention also encompasses a method for treating or preventing an inflammatory disease or condition in a mammalian patient in need of such treatment or prevention comprising administering to said patient a compound that is capable of simultaneously binding and activating PPARα and PPARγ or concomitantly administering a compound that selectively binds and activates PPARα with a compound that selectively binds and activates PPARγ in an amount that is effective to treat or prevent the inflammatory disease or condition.
摘要翻译：本发明包括在需要这种治疗或预防的哺乳动物患者中治疗或预防炎症性疾病或病症的方法，包括向所述患者施用能够同时结合PPARα和PPARγ的化合物或伴随施用选择性的化合物将PPARα与选择性结合PPARγ的化合物结合，其量可有效治疗或预防炎性疾病或病症。本发明还包括在需要这种治疗或预防的哺乳动物患者中治疗或预防炎性疾病或病症的方法，其包括向所述患者施用能够同时结合和激活PPARα和PPARγ或伴随施用选择性地结合并激活PPARα的化合物，其选择性结合并激活PPARγ的量，其有效治疗或预防炎性疾病或病症。

4. 发明申请

WO1995034289A1 COMPOSITIONS FOR NEUTRALIZATION OF LIPOPOLYSACCHARIDES 审中-公开
标题翻译：用于中性脂多糖的组合物
公开(公告)号：WO1995034289A1
公开(公告)日：1995-12-21
申请号：PCT/US1995007903
申请日：1995-06-07
申请人： THE ROCKEFELLER UNIVERSITY , WRIGHT, Samuel, D. , WURFEL, Mark, M. , HAILMAN, Peter, Eric
发明人： THE ROCKEFELLER UNIVERSITY
IPC分类号： A61K09/127
CPC分类号： C07K14/47 , A61K9/127 , A61K9/1275 , G01N33/92 , G01N2333/5412 , G01N2400/50 , Y10S436/811
摘要： The present invention relates to compositions and methods for neutralizing lipopolysaccharide, and treatment of gram-negative sepsis based thereon. Accordingly, the invention is directed to a composition of homogeneous particles comprising phospholipids and a lipid exchange protein, such as phospholipid transfer protein or LPS binding protein. The lipid exchange protein is characterized by being capable of faciliting an exchange of lipopolysaccharide into the particles. In a specific embodiment, exemplified herein, the lipid particles are high density lipoprotein particles comprising apolipoprotein A-I (apo A-I), a phospholipid, and cholesterol or a lipid bilayer binding derivative thereof. In a specific example, the phospholipid is phosphatidylcholine (PC). In a specific example, the ratio of phosphatidylcholine: cholesterol: apolipoprotein A-I is approximately 80:4:1. The level of LPS exchange protein activity in a sample from a patient provides a diagnostic, monitoring, or prognostic indicator for a subject with endotoxemia, gram-negative sepsis, or septic shock.
摘要翻译：本发明涉及中和脂多糖的组合物和方法，以及基于其的革兰氏阴性败血症的治疗。因此，本发明涉及包含磷脂和脂质交换蛋白如磷脂转移蛋白或LPS结合蛋白的均匀颗粒的组合物。脂质交换蛋白的特征在于能够促进脂多糖进入颗粒的交换。在本文示例的具体实施方案中，脂质颗粒是包含载脂蛋白A-1（载脂蛋白A-I），磷脂和胆固醇或其脂双层结合衍生物的高密度脂蛋白颗粒。在具体实例中，磷脂是磷脂酰胆碱（PC）。在一个具体实例中，磷脂酰胆碱：胆固醇：载脂蛋白A-I的比率为约80:4:1。来自患者的样品中LPS交换蛋白活性的水平为内毒素血症，革兰氏阴性脓毒症或败血性休克的受试者提供诊断，监测或预后指标。

5. 发明申请

WO2012000048A1 A RECONSTITUTED HIGH DENSITY LIPOPROTEIN FORMULATION AND PRODUCTION METHOD THEREOF 审中-公开
标题翻译：重建高密度脂蛋白制剂及其制备方法
公开(公告)号：WO2012000048A1
公开(公告)日：2012-01-05
申请号：PCT/AU2011/000819
申请日：2011-06-30
申请人： CSL LIMITED , WRIGHT, Samuel , IMBODEN, Martin , BOLLI, Reinhard , WALCHLI, Marcel
发明人： WRIGHT, Samuel , IMBODEN, Martin , BOLLI, Reinhard , WALCHLI, Marcel
IPC分类号： A61K31/56 , A61K31/685 , A61P3/06 , A61P9/10
CPC分类号： A61K38/1709 , A61K9/0019 , A61K9/1275 , A61K31/56 , A61K31/575 , A61K31/685 , A61K45/06 , A61K2300/00
摘要： A reconstituted high density lipoprotein formulation having relatively low toxicity comprises an apolipoprotein such as ApoAI or fragment thereof, a lipid and a detergent at a level which is about 5-50% of that which would normally cause liver toxicity upon administration to a human. The lipid is optimally phosphatidylcholine at about 30-50g/L and the molar ratio of apolipoprotein:lipid is optimally in the range 1:40 to 1:75. The formulation is useful for treating diseases or conditions such as cardiovascular disease, hypercholesterolaemia and hypocholesterolaemia inclusive of acute coronary syndrome (ACS), atherosclerosis and myocardial infarction.
摘要翻译：具有相对低毒性的重构高密度脂蛋白制剂包含载脂蛋白，例如ApoAI或其片段，脂质和洗涤剂，其含量约为施用于人时通常引起肝毒性的约5-50％。脂质是最好的磷脂酰胆碱约30-50g / L，载脂蛋白：脂质的摩尔比在1:40至1:75范围内最佳。该制剂可用于治疗诸如心血管疾病，高胆固醇血症和低胆固醇血症（包括急性冠状动脉综合征（ACS）），动脉粥样硬化和心肌梗死的疾病或病症。

6. 发明申请

WO03000182A3 PPAR-ALPHA LIGANDS FOR THE TREATMENT OR PREVENTION OF CACHEXIA 审中-公开
标题翻译：用于治疗或预防CACHEXIA的PPAR-ALPHA配体
公开(公告)号：WO03000182A3
公开(公告)日：2003-05-08
申请号：PCT/US0219464
申请日：2002-06-19
申请人： MERCK & CO INC , WRIGHT SAMUEL D
发明人： WRIGHT SAMUEL D
IPC分类号： A61K31/00 , A61K31/573 , A61K31/235 , A61K31/19 , A61K31/423
CPC分类号： A61K31/573 , A61K31/00
摘要： The present invention relates to a method for treating or preventing cachexia in a patient in need thereof comprising administering to said patient a PPAR alpha agonist in an amount that is effective to treat or prevent cachexia. Combination therapies and pharmaceutical compositions for treating or preventing cachexia are also encompassed.
摘要翻译：本发明涉及用于治疗或预防有此需要的患者的恶病质的方法，包括以有效治疗或预防恶病质的量向所述患者施用PPARα激动剂。还包括用于治疗或预防恶病质的组合疗法和药物组合物。

7. 发明申请

WO2003000182A2 PPAR-ALPHA LIGANDS FOR THE TREATMENT OR PREVENTION OF CACHEXIA 审中-公开
标题翻译：用于治疗或预防CACHEXIA的PPAR-ALPHA配体
公开(公告)号：WO2003000182A2
公开(公告)日：2003-01-03
申请号：PCT/US2002/019464
申请日：2002-06-19
申请人： MERCK & CO., INC. , WRIGHT, Samuel, D.
发明人： WRIGHT, Samuel, D.
IPC分类号： A61K
CPC分类号： A61K31/573 , A61K31/00
摘要： The present invention relates to a method for treating or preventing cachexia in a patient in need thereof comprising administering to said patient a PPARα agonist in an amount that is effective to treat or prevent cachexia. Combination therapies and pharmaceutical compositions for treating or preventing cachexia are also encompassed.
摘要翻译：本发明涉及治疗或预防有此需要的患者的恶病质的方法，其包括以有效治疗或预防恶病质的量向所述患者施用PPARα激动剂。还包括用于治疗或预防恶病质的组合疗法和药物组合物。

8. 发明申请

WO1991011464A1 LIPOPOLYSACCHARIDE BINDING OPSONIN AND METHODS OF USE THEREOF 审中-公开
标题翻译： LOPOPOLYSACCHARIDE BINDING OPSONIN及其使用方法
公开(公告)号：WO1991011464A1
公开(公告)日：1991-08-08
申请号：PCT/US1991000696
申请日：1991-02-01
申请人： THE ROCKEFELLER UNIVERSITY , WRIGHT, Samuel, D.
发明人： THE ROCKEFELLER UNIVERSITY
IPC分类号： C07K15/06
CPC分类号： C07K16/40 , A61K38/00 , C07K14/47 , C07K14/8121 , C12N9/6421
摘要： An opsonin is disclosed which has been isolated from human serum and which is present at high levels in normal serum in distinction to the acute phase protein LBP. The opsonin comprises a protein in purified form that is capable of binding to lipopolysaccharide to form a complex that is recognized by a receptor on monocytes, macrophage cells and polymorphonuclear cells, and that possesses an apparent molecular weight of about 90 kD as determined by SDS-PAGE analysis. The opsonin has been further characterized and appears to be a complex of a protease and a substrate for such protease. The substrate appears to possess some structural similarity to protein C inhibitor, and the opsonin is believed to be derived from a protease cascade leading to its availability for interaction with LPS. Diagnostic and therapeutic utilities are proposed, and testing procedures, materials in kit form, recombinant materials and procedures, and pharmaceutical compositions are likewise set forth.
摘要翻译：公开了一种从人血清中分离出的调理素，其与正常血清中以高水平存在，与急性期蛋白LBP不同。调理素包括纯化形式的蛋白质，其能够结合脂多糖以形成被单核细胞，巨噬细胞和多形核细胞上的受体识别的复合物，并且具有通过SDS-PAGE测定的约90kD的表观分子量， PAGE分析。调理素被进一步表征，似乎是这种蛋白酶的蛋白酶和底物的复合物。底物似乎具有与蛋白C抑制剂的一些结构相似性，并且认为调理素来自蛋白酶级联，导致其与LPS相互作用的可用性。提出了诊断和治疗用途，同样阐述了测试程序，试剂盒形式的材料，重组材料和程序以及药物组合物。

9. 发明申请

WO2003088962A1 COMBINATION THERAPY USING A PPAR ALPHA/GAMMA AGONIST 审中-公开
标题翻译：使用PPAR ALPHA / GAMMA AGONIST的组合治疗
公开(公告)号：WO2003088962A1
公开(公告)日：2003-10-30
申请号：PCT/US2003/011896
申请日：2003-04-15
申请人： MERCK & CO., INC. , MOLLER, David, E. , WRIGHT, Samuel, D.
发明人： MOLLER, David, E. , WRIGHT, Samuel, D.
IPC分类号： A61K31/426
CPC分类号： A61K45/06 , A61K31/216 , A61K31/22 , A61K31/397 , A61K31/426 , A61K2300/00
摘要： The present invention relates to pharmaceutical compositions comprising a combination of a first drug which is a PPARα/γ dual agonist and a second drug which is selected from the group consisting of (1) a cholesterol absorption inhibitor, (2) an HMG-CoA reductase inhibitor, (3) a bile acid sequestrant, (4) nicotinyl alcohol, nicotinic acid or a salt thereof, (5) a PPARα agonist, (6) a phenolic anti-oxidant, (7) an ACAT inhibitor, and (8) a CTEP inhibitor, including pharmaceutically acceptable salts of one or more of the active ingredients, and a pharmaceutically acceptable carrier. Such combinations are useful for treating hyperglycemia, lipid disorders, and obesity in patients who have type 2 diabetes, metabolic syndrome, insulin resistance, and impaired glucose tolerance.
摘要翻译：本发明涉及药物组合物，其包含作为PPARα/γ双重激动剂的第一药物和选自（1）胆固醇吸收抑制剂，（2）HMG-CoA还原酶抑制剂，（3）胆汁酸螯合剂，（4）烟酰醇，烟酸或其盐，（5）PPARα激动剂，（6）酚类抗氧化剂，（7）ACAT抑制剂，和（8） CTEP抑制剂，包括一种或多种活性成分的药学上可接受的盐和药学上可接受的载体。这些组合可用于治疗患有2型糖尿病，代谢综合征，胰岛素抵抗和葡萄糖耐量异常的患者的高血糖症，脂质紊乱和肥胖。

10. 发明申请

WO0215845A3 ANTI-HYPERCHOLESTEROLEMIC DRUG COMBINATION 审中-公开
标题翻译：抗高血压药物组合
公开(公告)号：WO0215845A3
公开(公告)日：2003-01-09
申请号：PCT/US0125815
申请日：2001-08-17
申请人： MERCK & CO INC , CHENG KANG , WRIGHT SAMUEL D , WU TSUEI-JU
发明人： CHENG KANG , WRIGHT SAMUEL D , WU TSUEI-JU
IPC分类号： A61K31/192 , A61K31/197 , A61K31/198 , A61K31/216 , A61K45/06 , A61P9/10 , A61K31/24
CPC分类号： A61K45/06 , A61K31/192 , A61K31/197 , A61K31/198 , A61K31/216 , A61K2300/00
摘要： This invention provides a drug combination comprised of a thyroid hormone receptor beta agonist with a fibrate in therapeutically effective amounts, which is useful for reducing cholesterol synthesis, lowering plasma cholesterol levels and lowering plasma triglyceride levels.
摘要翻译：本发明提供由治疗有效量的甲状腺激素受体β激动剂与贝特类药物组合的药物组合，其可用于降低胆固醇合成，降低血浆胆固醇水平和降低血浆甘油三酯水平。

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