54 results about "3-hydroxy-3-methylglutaryl-CoA lyase" patented technology

A method of lipid therapy, comprising providing a subject group having a baseline triglyceride level of 200 to 499 mg / dl and being at or near its low-density lipoprotein cholesterol (LDL-C) level goal, and reducing the triglyceride level and the non-high-density lipoprotein cholesterol (non-HDL-C) level of the subject group as compared to treatment with a 3-hydroxy-3-methyl glutaryl coenzyme A (HMG CoA) inhibitor alone, by administering to the subject group an effective amount of an HMG CoA inhibitor and a composition comprising omega-3 fatty acids.

A highly safe and effective prophylactic / ameliorating or therapeutic agent for NACH and the method for using the same are provided.A prophylactic / ameliorating or therapeutic agent for NASH containing a combination of at least one first ingredient selected from the group consisting of an ω3PUFA and pharmaceutically acceptable salts and esters thereof and at least one second ingredient selected from the group consisting of (a) a biguanide hypoglycemic agent, (b) a nonsteroidal anti-inflammatory drug, (c) a 3-hydroxy-3-methyl glutaryl coenzyme A reductase inhibitor, and (d) an angiotensin II receptor blocker as the active ingredients; and its method of use.

A method of lipid therapy, comprising providing a subject group having a baseline triglyceride level of 200 to 499 mg / dl and being at or near its low-density lipoprotein cholesterol (LDL-C) level goal, and reducing the triglyceride level and the non-high-density lipoprotein cholesterol (non-HDL-C) level of the subject group as compared to treatment with a 3-hydroxy-3-methyl glutaryl coenzyme A (HMG CoA) inhibitor alone, by administering to the subject group an effective amount of an HMG CoA inhibitor and a composition comprising omega-3 fatty acids.

Novel 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase inhibitors are useful as antihypercholesterolemic agents and are represented by the following general structural formula (II):

The present invention describes novel nitrosated and / or nitrosylated cyclooxygenase 2 (COX-2) inhibitors and novel compositions comprising at least one nitrosated and / or nitrosylated cyclooxygenase 2 (COX-2) inhibitor, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and / or optionally, at least one therapeutic agent, such as, steroids, nonsteroidal antiinflammatory compounds (NSAID), 5-lipoxygenase (5-LO) inhibitors, leukotriene B4 (LTB4) receptor antagonists, leukotriene A4 (LTA4) hydrolase inhibitors, 5-HT agonists, 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) inhibitors, H2antagonists, antineoplastic agents, antiplatelet agents, decongestants, diuretics, sedating or non-sedating anti-histamines, inducible nitric oxide synthase inhibitors, opioids, analgesics, Helicobacter pylori inhibitors, proton pump inhibitors, isoprostane inhibitors, and mixtures thereof. The present invention also provides novel compositions comprising at least one parent COX-2 inhibitor and at least one nitric oxide donor, and, optionally, at least one therapeutic agent. The present invention also provides kits and methods for treating inflammation, pain and fever; for treating and / or improving the gastrointestinal properties of COX-2 inhibitors; for facilitating wound healing; for treating and / or preventing renal toxicity; and for treating and / or preventing other disorders resulting from elevated levels of cyclooxygenase-2.

A method for treating age related macular degeneration (AMD) using an insulin preparation applied topically to the conjunctival sac of the affected eye. Another aspect of this invention is using antiangiogenic adjuvant therapeutic agents such as bevacizumab, ranibizumab, pegaptanib, etanercept, instilled in to the afflicted eye conjunctival sac with insulin to prevent further formation of new blood vessels, and shrink the existing pathologically formed blood vessels and reduce the edema in wet AMD. This method incorporates putting the patients on low fat diet, aerobic exercise, ketamine-a NMDA blocker, reducing the blood cholesterol using adjuvant therapeutic agents selected from Statins, that are inhibitors of 3-hydroxy-3-methylglutaryl coenzyme A, (i.e. HMG-Co A) reductase which in turn reduce drusen formation that leads to AMD, combined with insulin ophthalmic drops.

Novel compounds and pharmaceutical compositions useful as hypocholesterolemic and hypolipidemic agents are described. More specifically, potent inhibitors of the enzyme 3-hydroxy-3-methylglutaryl-coenzyme A reductase (“HMG CoA reductase”) are described. Methods of using such compounds and compositions to treat subjects, including humans, suffering from hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, atherosclerosis, Alzheimer's Disease, benign prostatic hypertrophy (BPH), diabetes and osteoporosis are also described.

The present invention relates to substituted pyrrole derivatives, which can be used as 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase inhibitors. Compounds disclosed herein can function as cholesterol lowering agents and can be used for the treatment of cholesterol-related diseases and related symptoms. Processes for the preparation of disclosed compounds are provided, as well as pharmaceutical compositions containing the disclosed compounds, and methods of treating cholesterol-related diseases and related symptoms.

The invention discloses an inonotus obliquus 3-hydroxy-3-methylglutaryl CoA reductase gene, protein of a code thereof and an application thereof. A squalene synthase gene provided in the inonotus obliquus 3-hydroxy-3-methylglutaryl CoA reductase gene has nucleotide sequences indicated by SEQ ID NO. 1 or homologous sequences for adding, replacing, inserting or missing one or a plurality of nucleotides or nucleotide sequences derived by an allele of the nucleotide and the nucleotide. The protein of the code of the gene has amino acid sequences indicated by SEQ ID NO.2 or homologous sequences for adding, replacing, inserting or missing one or a plurality of amino acids. The inonotus obliquus 3-hydroxy-3-methylglutaryl CoA reductase gene can improve the content of inonotus alcohol in inonotusobliquus by utilizing the gene engineering technology and also can be used in the research of improving the content of the inonotus alcohol in the inonotus obliquus by utilizing the transgenic technology and the industrialization. A plurality of secondary metabolites have huge application value clinically and help to protect the healthy growth of people. Therefore, the inonotus obliquus 3-hydroxy-3-methylglutaryl CoA reductase gene, the protein of the code thereof and the application thereof have huge application prospect.

A solid amorphous dispersion comprises a cholesteryl ester transfer protein (CETP) inhibitor, an inhibitor of 3-hydroxy-3-methylglutaryl-conenzyme A reductase (HMG-CoA reductase inhibitor), and a concentration enhancing polymer. At least a major portion of the CETP inhibitor in the dispersion is amorphous. The solid amorphous dispersion provides concentration-enhancement of the CETP inhibitor when administered to an aqueous use environment.

Disclosed herein are novel compounds of formula (I), and uses thereof. The compounds of Formula (I) are inhibitors of histone deacetylases (HDACs) and 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase (HMGR). Also provided are methods of using the compounds of Formula (I) for inhibiting the activity of HDACs and HMGR, treating diseases associated with HDACs or HMGR (e.g., cancer, hypercholesterolemia, an acute or chronic inflammatory disease, autoimmune disease, allergic disease, pathogen infection, neurodegenerative disease, or a disease associated with oxidative stress,

The invention relates to alisma 3-hydroxy-3-methyl glutaric acyl coenzyme A reductase coded by genes of an amino acid sequence in a sequence table SEQ ID No.2 or a base sequence in a sequence table SEQ ID No.1. The invention further relates to a prokaryotic expression of the alisma 3-hydroxy-3-methyl glutaric acyl coenzyme A reductase, a method for obtaining purified albumen and a preparation method of a polyclonal antibody. The alisma 3-hydroxy-3-methyl glutaric acyl coenzyme A reductase is obtained, the polyclonal antibody of the albumen is prepared, an ELISA detection method and a Western blot detection method of the albumen are obtained, a basis is laid for further AoHMGR functional analysis development, and an important basis is provided for original terpane type triterpenoid bioengineering application.

Novel compounds and pharmaceutical compositions useful as hypocholesterolemic and hypolipidemic agents are described. More specifically, potent inhibitors of the enzyme 3-hydroxy-3-methylglutaryl-coenzyme A reductase (“HMG CoA reductase”) are described. Methods of using such compounds and compositions to treat subjects, including humans, suffering from hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, atherosclerosis, Alzheimer's Disease, benign prostatic hypertrophy (BPH), diabetes and osteoporosis are also described.

Novel compounds and pharmaceutical compositions useful as hypocholesterolemic and hypolipidemic agents are described. More specifically, potent inhibitors of the enzyme 3-hydroxy-3-methylglutaryl-coenzyme A reductase (“HMG CoA reductase”) are described. Methods of using such compounds and compositions to treat subjects, including humans, suffering from hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, atherosclerosis, Alzheimer's Disease, benign prostatic hypertrophy (BPH), diabetes and osteoporosis are also described.

A pharmaceutical composition for inhibiting inflammation, comprising (a) hyaluronic acid, (b) a 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase inhibitor, and (c) a pharmaceutically acceptable carrier, is provided. Also provided is a method for inhibiting inflammation in a mammal, comprising administrating to the mammal an effective amount of a composition comprising (a) hyaluronic acid and (b) an HMG-CoA reductase inhibitor.

A novel solid oral dosage form comprising a therapeutically effective amount of hydrophobic pharmacological active ingredient and at least one particle separating agent preferably selected from a class of wetting agents, prepared without or with minimum amount of a disintegrating agent. The hydrophobic pharmacological active ingredient active ingredient belongs to the class of angiotensin receptor blocking agents preferably is valsartan optionally in combination with hydrochlorothiazide. The active ingredient may also be a class of 3-hydroxy-3-methylglutaryl coenzyme A (HMG CoA) reductase inhibitors preferably atorvastatin. The ratio of hydrophobic active ingredient to particle separating agent is about 20:1 to about 1:20. The process for the preparation of the novel solid oral dosage form comprises treating a hydrophobic active ingredient with at least one particle separating agent, and incorporating the treated hydrophobic active ingredient into a solid dosage form.

Inhibitors of 3-hydroxy-3-methylglutaryl-coenzyme A reductase (statins) are prescribed to lower serum cholesterol levels and reduce the risk of CVD. Despite the success of statins, many patients abandon treatment owing to neuromuscular adverse drug reactions (ADRs). Genome-wide association studies have identified the single-nucleotide polymorphism (SNP) rs4149056 in the SLCO1B1 gene as being associated with an increased risk for statin-induced ADRs.By studying slow-channel syndrome transgenic mouse models, this invention determined that statins trigger ADRs in mice expressing the mutant allele of the rs137852808 SNP in the nicotinic acetylcholine receptor (nAChR) α-subunit gene CHRNA1. Mice expressing this allele show a remarkable contamination of end-plates with caveolin-1 and develop early signs of neuromuscular degeneration upon statin treatment. The invention demonstrates that genes coding for nAChR subunits may contain variants associated with statin-induced ADRs.

The present invention discloses statins (3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitors) consistently and significantly increased endothelial cell thrombomodulin protein and functional activity. Statins also abrogated the downregulation of thrombomodulin that occurs in response to radiation injury. These results indicate that preserving or restoring endothelial thrombomodulin expression and function by statins may be useful in a variety of disorders associated with widespread endothelial dysfunction such as sepsis, adult respiratory distress syndrome, and normal tissue radiation injury.

The invention belongs to the technical field of bioengineering and discloses a recombinant eukaryotic strain for generating amorphadiene and a method for preparing the amorphadiene with the recombinant eukaryotic strain. Expression genes of 3-hydroxyl-3-methylglutaryl coenzyme A, FPP (farnesylpyrophosphate) synthase and amorphadiene synthase are integrated in a genome of the eukaryotic strain and integrated at a multi-copy locus of the genome of the eukaryotic strain. The recombinant eukaryotic strain for generating the amorphadiene is an integrated eukaryotic strain, greatly increases yield of the amorphadiene and is beneficial to amorphadiene production.

The invention belongs to the field of molecular biology, and relates to an isolation and cloning, gene site-specific mutagenesis, zymoprotein prokaryotic expression, zymoprotein separation and purification, and enzymatic activity detection technology for a first key enzyme gene participating in isoprenoid substance synthesis in wheat mevalonic acid metabolic pathways. Important technical reserves are provided for further carrying out gene modification and augmentation, constructing eukaryotic genetic expression vectors of 3-hydroxy-3-methylglutaryl-coenzyme A reductase (HMGR) genes and converting corresponding products, and are particularly provided for obtaining plants with the high commercial value through secondary metabolism, discussing the relationship between overexpression of the HMGR genes in the receiver plants and important economical characters such as secondary metabolism products, the crop grain size and the grain weight, then increasing the crop yield, analyzing the structures of introns, exons and promoters of the HMGR genes, researching the functions of the promoters and developing related molecular markers.

The invention relates to the field of biological technology and discloses a method of increasing the content of tanshinone. According to the method, the 3-hydroxy-3-methylglutaryl coenzyme A reductase gene SmHMGR and the 1-deoxy-D-xylosone-5-phosphate reductase gene SmDXR of salvia miltiorrhiza bunge are used to construct a recombinant vector, and genetic transformation is carried out on leaves of salvia miltiorrhiza bunge so as to obtain hairy roots of salvia miltiorrhiza bunge with transgenic SmHMGR and SmDXR genes. The content of tanshinone in the obtained transgenic hairy roots of salvia miltiorrhiza bunge in the invention substantially increases, and total tanshinone content in a line (HD34) of cotransformed SmHMGR and SmDXR double genes is 5.30 times of that of a comparison hairy root of salvia miltiorrhiza bunge. The invention provides the method for increasing content of tanshinone in the hairy roots of salvia miltiorrhiza bunge, providing a novel high-quality drug source for producing tanshinone in critical clinical demand and having a positive promotion effect in alleviating shortage of drug sources for tanshinone.

The invention discloses a 3-hydroxy-3-methylglutaryl-CoA reductase and a coding gene and application of the 3-hydroxy-3-methylglutaryl-CoA reductase. An amino acid sequence of the 3-hydroxy-3-methylglutaryl-CoA reductase is shown as SEQ ID NO.6. A complete 3669bp gene sequence is obtained by that total RNA (ribose nucleic acid) of grifola frondosa sporophores is extracted and synthesized into cDNA (complementary deoxyribonucleic acid) by reverse transcription and a 3-hydroxy-3-methylglutaryl-CoA reductase gene (Gfhg) is cloned according to RT-PCR (reverse transcription-polymerase chain reaction) technologies. A eukaryotic expression vector pCAMBIA1302-Gfhg-hyg is constructed, and functional verification of pCAMBIA1302-Gfhg-hyg obtained by cloning is realized by application of an antrodia cinnamomea mycelium system. By the 3-hydroxy-3-methylglutaryl-CoA reductase gene (Gfhg) of grifola frondosa, content of antrodia cinnamomea triterpenes in antrodia cinnamomea sporophores and secondary metabolites can be increased, and content of triterpenes generated by plants is increased so as to improve disease resistance of the plants.

Disclosed herein are compositions and methods for decreasing vascular permeability in a blood vessel and treating or preventing conditions associated with defects or injuries of vascular endothelium. For example, the disclosed compositions and methods can be used to treat a vascular dysplasia such as cerebral cavernous malformation (CCM). These methods relate generally to the use of compositions that inhibit RhoA GTPase levels or activity, such as inhibitors of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase.

The invention relates to a medicament containing theophylines and statins. In the invention, the theophylines and 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitor form a compound to obtain excellent synergistic effect. The medicament compound greatly reduces the toxic and side effect of aminophylline when used alone, and the pharmacy security is improved.

Chemical syntheses and medical uses of novel modulators of 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase and diastereomeric mixtures of isomers, individual diastereomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, the chemical synthesis thereof, and the medical use of such compounds for the treatment and / or management of hypercholesterolemia, dyslipidemia, coronary artery disease, atherosclerosis, metabolic syndrome, a hyperproliferative disease such as colorectal cancer, prostate cancer, and melanoma, a neurodegenerative disease such as cerebral ischemia, Alzheimer's disease, and Parkinson's disease are described.

The invention relates to processes for the preparation of atorvastatin. Atorvastatin is known by the chemical name [R—(R*,R*)]-2-(4-fluorophenyl)-β,δ-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid. The hemi-calcium salt of atorvastatin is useful as an inhibitor of the enzyme 3-hydroxy-3-methylglutaryl-coenzyme A reductase (HMG-CoA reductase). The invention also relates to pharmaceutical compositions that include the atorvastatin or a pharmaceutically acceptable salt thereof and to use of said compositions for treating hypolipidemia, hypocholesterolemia and atherosclerosis.

A solid amorphous dispersion comprises a cholesteryl ester transfer protein (CETP) inhibitor, an inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme A reductase (HMG-CoA reductase inhibitor), and a concentration enhancing polymer. At least a major portion of the CETP inhibitor in the dispersion is amorphous. The solid amorphous dispersion provides concentration-enhancement of the CETP inhibitor when administered to an aqueous use environment.