413624-71-2Relevant academic research and scientific papers
Long hydrocarbon chain keto diols and diacids that favorably alter lipid disorders in vivo
Mueller, Ralf,Yang, Jing,Duan, Caiming,Pop, Emil,Geoffroy, Otto J.,Zhang, Lian Hao,Huang, Tian-Bao,Denisenko, Sergey,McCosar, Bruce H.,Oniciu, Daniela C.,Bisgaier, Charles L.,Pape, Michael E.,Freiman, Catherine Delaney,Goetz, Brian,Cramer, Clay T.,Hopson, Krista L.,Dasseux, Jean-Louis H.
, p. 6082 - 6099 (2004)
Keto-substituted hydrocarbons with 11-19 methylene and bis-terminal hydroxyl and carboxyl groups have been synthesized and evaluated in both in vivo and in vitro assays for their potential to favorably alter lipid disorders including metabolic syndrome. Compounds were assessed for their effects on the de novo incorporation of radiolabeled acetate into lipids in primary cultures of rat hepatocytes as well as for their effects on lipid and glycemic variables in obese female Zucker fatty rats [Crl:(ZUC)-faBR] following 1 and 2 weeks of oral administration. The most active compounds were found to be symmetrical with four to five methylene groups separating the central ketone functionality and the gem dimethyl or methyl/aryl substituents. Furthermore, biological activity was found to be greatest in both in vivo and in vitro assays for the tetramethyl-substituted keto diacids and diols (e.g., 10c, 10g, 14c), and the least active were shown to be the bis(arylmethyl) derivatives (e.g., 10e, 10f, 14f). Compound 14c dose-dependently elevated HDL-cholesterol, reduced triglycerides, and reduced NEFA, with a minimum effective dose of 30 mg/kg/day. Compound 10g dose-dependently modified non-HDL-cholesterol, triglycerides, and nonesterified fatty acids, with a minimum effective dose of 10 mg/kg/day. At this dose, compound 10g elevated HDL-cholesterol levels 2-3 times higher than pretreatment levels, and a dose-dependent reduction of fasting insulin and glucose levels was observed.
PROCESS FOR PREPARATION OF BEMPEDOIC ACID
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Page/Page column 17, (2020/10/17)
Aspect of the present application provides cost effective and commercially viable process for preparation of Bempedoic acid. The process involves the reduction of compound formula I to obtain compound formula II which is hydrolyzed to get Bempedoic acid. The present application also provides the process for preparation of Bempedoic acid using compound of formula II without purification.
Substituted pentadecanedioic acid compound and pharmaceutical composition and application thereof
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Paragraph 0161; 0164; 0167; 0168, (2019/08/07)
The invention provides a substituted pentadecanedioic acid compound, a pharmaceutical composition comprising the substituted pentadecanedioic acid compound and application of the substituted pentadecanedioic acid compound and the pharmaceutical composition. The compound refers to a compound shown as a formula (I), or a pharmaceutically acceptable salt of the compound, a prodrug, a hydrate or a solvate, a crystal form, a stereoisomer or an isotope variant. The compound can be used for treatment or prevention of cardiovascular diseases or dyslipidemia and has excellent pharmacokinetic properties.
HYDROXYL COMPOUNDS AND COMPOSITIONS FOR CHOLESTEROL MANAGEMENT AND RELATED USES
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Page 263, (2008/06/13)
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.
