专利号:US-7399773-B2 优先权日:2001-01-09 标 题 :Process for the synthesis of 5-(4-fluorophenyl)-1-[2-((2R,4R)-4-hydroxy-6-oxo-tetrahydro-pyran-2-yl)-ethyl]-2-isopropyl-4-phenyl-1H-pyrrole-3-carboxylic acid and phenylamide 发明人:NELSON JADE DOUGLAS; PAMMENT MICHAEL GERARD 权利人:WARNER LAMBERT CO 摘要:An improved process for the preparation of 5-(4-fluorophenyl)-1-[2-((2R,4R)-4-hydroxy-6-oxo-tetrahydro-pyran-2-yl)-ethyl]-2-isopropyl-4-phenyl-1H-pyrrole-3-carboxylic acid phenylamide by a novel synthesis is described where methyl cyanoacetate is converted in eight operations or fewer to the desired product, as well as other valuable intermediates used in the process.
专利号:WO-2008075165-A1 优先权日:2006-12-19 标 题 :Novel process for the synthesis of [r-(r*, r*)]-2-(4-fluorophenyl)-beta, delta-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1h-pyrrole-1-heptanoic acid or a pharmaceutically acceptable salt thereof 发明人:CHOPRA TIMOTHY JAY; O'NEILL PADRAIG MARY; WILKES PHILIPPA BRENDA 权利人:PFIZER PROD INC; CHOPRA TIMOTHY JAY; O'NEILL PADRAIG MARY; WILKES PHILIPPA BRENDA 摘要:An improved synthesis for the preparation of [R-(R*, R*)]-2-(4-fluorophenyl)- β, δ-dihydroxy-5-(1- methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1 H-pyrrole-1-heptanoic acid or a pharmaceutically acceptable salt thereof, as well as other valuable intermediates used in the process, are described. The compounds prepared by a process of the invention are useful in treating hyperlipidemia, hypercholesterolemia, osteoporosis, benign prostatic hyperplasia, or Alzheimer's disease.
专利号:EP-2719288-A1 优先权日:2012-10-12 标 题:Composition for the treatment or prevention of dyslipidaemias 发明人:FULGA ION GIGEL; VASILE DANUT 权利人:FULGA ION GIGEL; VASILE DANUT 摘要:The invention is a composition consisting of a combination of a compound which decreases the synthesis of endogenous cholesterol with a compound that reduces cholesterol absorption, a compound that increases HDL and a compound that enhances cholesterol degradation, the ratio of the four compounds being 0.5...1: 0.5...1: 0.015: 1.5...2, expressed in parts by weight. Preferably, the composition according to the invention contains a combination of red rice yeast (or red rice extract) with niacin, sitostanol and taurine in oral pharmaceutical preparations to be used as food supplement or as medicine for the treatment or prevention of dyslipidaemias, for improving or preventing disturbances in the serum lipid profile.
专利号:US-2006122240-A1 优先权日:2002-11-05 标题 :Benzotriazoles and methods of prophylaxis or treatment of metabolic-related disorders thereof 发明人:SEMPLE GRAEME; SKINNER PHILIP J; CHERRIER MARTIN C; WEBB PETER; TAMURA SUSAN Y 权利人:ARENA PHARM INC 摘要:The present invention relates to certain benzotriazole carboxylic acid or ester derivatives of Formula (I), pharmaceutically acceptable salts and solvates thereof, which exhibit useful pharmaceutical properties, for example, as agonists for the GPCR referred to as hRUP38. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the prophylaxis or treatment of metabolic-related disorders, including dyslipidemia, atherosclerosis, coronary heart disease, insulin resistance, type 2 diabetes, Syndrome-X and the like. In addition, the present invention also provides for the use of the compounds of the invention in combination with other active agents such as those belonging to the class of -glucosidase inhibitors, aldose reductase inhibitors, biguanides, HMG-CoA reductase inhibitors, squalene synthesis inhibitors, fibrates, LDL catabolism enhancers, angiotensin converting enzyme (ACE) inhibitors, insulin secretion enhancers and the like.
专利号:US-2008227846-A1 优先权日:2007-03-13 标 题:Methods of treating juvenile type 1 diabetes mellitus 发明人:SINGH INDERJIT; KEY LYNDON 权利人:MUSC FOUND FOR RES DEV; UNIV SOUTH CAROLINA 摘要:The present disclosure describes methods for treating or preventing Type 1 diabetes mellitus in juveniles, particularly in juveniles newly diagnosed with Type 1 diabetes. This prevention or treatment of Type 1 diabetes is achieved by administering one or more therapeutic agents to a juvenile in need, wherein the therapeutic agent is, for example, a competitive inhibitor of mevalonate synthesis, a competitive inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase, or an inducer of AMP protein kinase (AMPK) activity. In certain embodiments, juveniles with Type 1 diabetes are treated with an HMG-CoA reductase inhibitor such as a statin, thereby decreasing the destruction of islet cells, or maintaining endogenous insulin production, in the juvenile.
专利号:US-2008275104-A1 优先权日:1997-11-25 标 题 :Methods of treating juvenile type 1 diabetes mellitus 发明人:SINGH INDERJIT; KEY LYNDON 权利人:MUSC FOUND FOR RES DEV 摘要:The present disclosure describes methods for treating Type 1 diabetes mellitus in juveniles. This treatment of Type 1 diabetes is achieved by administering one or more therapeutic agents to a juvenile in need, wherein the therapeutic agent is, for example, a competitive inhibitor of mevalonate synthesis, a competitive inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase, or an inducer of AMP protein kinase (AMPK) activity. In certain embodiments, juveniles with Type 1 diabetes are treated with an HMG-CoA reductase inhibitor such as a statin.
1: Yadav M, Dhami A, Ahsan U, Nadeem L, Raja F, Raif M, Mushtaq H, Ali SM, Butt SB, Kolanu ND. Efficacy of High-Dose Atorvastatin Loading in Patients With ST- Elevation Myocardial Infarction (STEMI) Undergoing Percutaneous Coronary Intervention: A Systematic Review of Randomized Controlled Trials. Cureus. 2025 Aug 23;17(8):e90817. doi: 10.7759/cureus.90817. 2: Haque SM. Comparative Studies of GAC Metric Tools AGREE, Analytical Eco- Scale, BAGI and WAC RGB Model to Determine Atorvastatin in Pharmaceuticals. Crit Rev Anal Chem. 2025 May 24:1-15. doi: 10.1080/10408347.2025.2507759. Epub ahead of print.