81 results about "Statine" patented technology

According to the invention, the monooxygenase CYP102A1 from Bacillus megaterium is subjected to system modification and optimization, a series of monooxygenase mutants with improved activity and improved debenzylation selectivity are obtained, the activity of the mutant with the optimal effect is improved by 93.4 times compared with that of wild type monooxygenase CYP102A1, and the selectivity is improved to 99.5% from 33.2%. The monooxygenase mutant can be applied to catalytic synthesis of 3R, 5S-dihydroxy compounds, synthesis steps are simplified, reaction selectivity is improved, reaction conditions are mild, the monooxygenase mutant is environmentally friendly and efficient, and the overall efficiency of statin drug synthesis can be improved.

Described is an antibody-drug conjugate (ADC) having the formula A-L, wherein A is an antibody or an antibody fragment and wherein L is a linker, said linker comprising: as a first payload a topoisomerase I inhibitor which is cell-permeable, e.g., a camptothecin cytotoxic molecule which is cell-permeable; as a second payload a topoisomerase I inhibitor which is not cell-permeable, e..g., a camptothecin cytotoxic molecule which is not cell-permeable; and as a as a third payload a toxin or a cytotoxin, e.g., an auristatin such asMMAE (Monomethyl auristatin E). Moreover, described is a pharmaceutical composition comprising said ADC and at least one pharmaceutically acceptable ingredient. Further, described method of treating a patient suffering from, being at risk of developing, and / or being diagnosed for a neoplastic disease.

An antibody-drug conjugate as shown in formula I, a preparation method therefor, and a use thereof in prevention and / or treatment of diseases related to abnormal cell activity, including but not limited to a use in prevention and / or treatment of tumor diseases.

The present invention provides methods for treating patients suffering from familial hypercholesterolemia, including both HeFH and HoFH. The methods of the invention provide for lowering at least one lipid parameter in the patient by administering a therapeutically effective amount of an antibody or antigen-binding fragment thereof that specifically binds to ANGPTL3 in combination with a therapeutically effective amount of a statin, a first lipid lowering agent other than a statin, and a second lipid lowering agent other than a statin. The first non-statin lipid lowering agent is an agent that inhibits cholesterol uptake (e.g. ezetimibe) and the second non-statin lipid-lowering agent is an inhibitor of microsomal triglyceride transfer protein (e.g. lomitapide). The combination therapy is useful in treating hypercholesterolemia, as well as hyperlipidemia, hyperlipoproteinemia and dyslipidemia, including hypertriglyceridemia, chylomicronemia, and to prevent or treat diseases or disorders, for which abnormal lipid metabolism is a risk factor, such as cardiovascular diseases.

The invention discloses application of a polyketone natural product enterocin in preparation of a lipid-lowering medicine, and relates to the technical field of medicine preparation. Research finds that the compound enterocin can regulate a cell ASGR1 target spot and promote cholesterol to flow out of cells, and is different from the action mechanism of statins; the polyketone enterocin can reduce the levels of lipid, TC, TG, LDL-C and the like in an animal body, improve the HDL-C content and promote excretion of TC and TG, part of indexes are equivalent to that of a clinical medicine atorvastatin calcium, part of indexes have remarkable advantages, and the polyketone enterocin has a good application prospect in preparation of the lipid-lowering medicine, and the application proposes that the polyketone natural product enterocin is applied to the lipid-lowering medicine for the first time, so that the application prospect of the polyketone enterocin is wide. A new development direction is provided for the source of the lipid-lowering medicine.

The application discloses an inhibitor for inhibiting KRAS phase separation to play an anti-tumor role and application, and relates to the fields of tumor molecular biology and targeted therapy.The application aims at solving the problems of limited effect, strong drug resistance and limited application range of KRAS tumor treatment methods, and the inhibitor is a statin.The KRAS protein can form a liquid condensate in cells, and the application discloses the mechanism of the KRAS protein in promoting KRAS protein processing, transportation and downstream signal activation, and further provides a technical scheme for inhibiting tumor growth and enhancing the therapeutic effect of a KRAS inhibitor by inhibiting the formation of KRAS condensates, so as to provide a new target and intervention approach for tumor treatment.

This invention relates to the field of ovarian tissue in vitro culture technology, and discloses a formulation for activating and increasing follicles and its application. The formulation consists of a PI3K / Akt / mTOR pathway activator and / or a PTEN inhibitor SF1670. The PI3K / Akt / mTOR pathway activator is a 5-15 μM statin, and the PTEN inhibitor is a 20-50 μM SF1670. Using this formulation can achieve the follicle activation and increase effect of existing technologies, contributing to the development and selection of in vitro follicle activators in clinical practice. Furthermore, the use of this formulation opens up a new technological application area for statins.

The present invention relates to a composition for preventing, alleviating or treating metabolic diseases, the composition comprising a rosuvastatin and ursodeoxycholic acid conjugate or a pharmaceutically acceptable salt thereof, in which the statin conjugates to an ursodeoxycholic acid transporter and has the effects of function inhibition, cholesterol level reduction, antilipid toxicity, body weight reduction, blood lipid reduction, fatty liver alleviation, inflammation alleviation, and kidney damage alleviation. The composition, in the form of a single formulation, has the characteristics of maintaining the therapeutic effects of rosuvastatin and ursodeoxycholic acid while reducing the side effects of existing statins, and thus can be widely used as a substitute for complex formulations in the treatment of metabolic diseases.

Provided herein are compositions, systems, and methods for treating wounds with the combination of statins and cholesterol to help prevent and reduce scar formation.

The invention relates to the technical field of biological medicine. The invention provides a PCSK9-targeted PROTAC oral drug as well as a preparation method and application thereof. The drug comprises the following structures: a PCSK9 binding peptide, an E3 ubiquitin ligase ligand, a cell penetrating peptide and a flexible linker. The medicine provided by the invention can be used for preparing products for treating lipid metabolism disorder diseases such as hypercholesteremia and atherosclerosis. In addition, the medicine disclosed by the invention can also be combined with statins to synergistically enhance the lipid-lowering curative effect.

Described herein are formulations for the controlled release of statin therapies and methods related thereto.

A preparation method of a tumor microparticle encapsulating a metabolic inhibitor includes following steps. A tumor cell is cultivated, and a statin drug is added to a culture medium after the tumor cell grows stably. Then, the tumor cell is irradiated with an ultraviolet, and then the tumor cell is incubated in a cell incubator for 22˜26 hours. After the incubation, cell supernatant is collected and the tumor microparticle encapsulating the metabolic inhibitor is obtained through a gradient centrifugation. The preparation method uses tumor cell-derived microparticles as drug delivery platforms, with a simple preparation process that preserves functions such as biosafety, biocompatibility, targeting, and intercellular communication. The preparation method discovers new uses of a statin drug, which can inhibit tumor growths with the statin drug, regulate tumors metabolism and improve a tumor microenvironment, and have a potential to enhance a chemotherapy efficacy and delay a chemotherapy resistance.

The invention relates to the technical field of medicines, and relates to an auristatin drug and a conjugate thereof. In particular, the present invention relates to a ligand-drug conjugate or a pharmaceutically acceptable salt or solvate thereof, a preparation method and use thereof. The invention also relates to a linker-drug compound or an isomer, a meso-form, a raceme, an enantiomer thereof or a mixture thereof, or a pharmaceutically acceptable salt or solvate thereof, a method for the production thereof and the use thereof.

Disclosed herein are therapeutics compositions including one or more active agents, for instance a statin, cyclodextrin, or combination thereof. The compositions are useful in the treatment of tissue injuries, including wounds, as well as skin inflammation and infections.

The invention discloses an efficient composite immobilized enzyme for preparing ethyl R (-)-4-cyano-3-hydroxybutyrate and a preparation method of the efficient composite immobilized enzyme, and relates to the technical field of biological catalysis. The composite immobilized enzyme comprises an active enzyme component, a Nicoordination modified mesoporous silica-chitosan composite carrier, and a sodium alginate auxiliary embedding-glutaraldehyde covalent cross-linking composite immobilization mode. The preparation method comprises the following steps: preparing a modified carrier, preparing an active enzyme mixed solution, carrying out an embedding-crosslinking reaction, collecting and drying. The compound immobilized enzyme can catalytically prepare ethyl R (-)-4-cyano-3-hydroxybutyrate, the substrate conversion rate is still kept at an extremely high level after the compound immobilized enzyme is repeatedly used for more than 15 times, and the compound immobilized enzyme is stable in enzyme activity, low in cost and suitable for industrial green production of statin drug intermediates.

The present invention relates to a pharmaceutical combination comprising 6α-ethyl-3α, 7 a-dihydroxy-24-nor-5 β-cholan-23-ol or a pharmaceutically acceptable salt thereof and a statin and to a combination comprising 6α-ethyl-3α, 7α-dihydroxy-24-nor-5β-cholan-23-ol and ursodesoxycholic acid and the use thereof for the treatment of non-alcoholic liver steatosis and non-alcoholic steatohepatitis.

Described herein are methods for reducing or preventing blood flow in a neurovascular blood vessel of a subject. The method involves injecting a composition composed of water, one or more polycationic polyelectrolytes and anionic counterions, one or more one polyanionic polyelectrolytes and cationic counterions, and a statin, an anti-cancer agent, or a combination thereof, wherein the composition has an ion concentration that is (i) sufficient to prevent association of the polycationic polyelectrolytes and the polyanionic polyelectrolytes in water and (ii) greater than the concentration of ions in the subject. Upon introduction of the composition into a subject, a solid is produced in situ. The injectable compositions have unique distal penetration properties, which make the injectable compositions described herein very useful as embolics for neurovascular blood vessels.

Described herein are formulations for the controlled release of statin therapies and methods related thereto.

The invention belongs to the technical field of traditional Chinese medicines, and particularly relates to a traditional Chinese medicine composition for treating atherosclerosis and a preparation method thereof. The traditional Chinese medicine composition for treating atherosclerosis is prepared from the following raw materials in parts by weight: 20 to 40 parts of radix astragali seu hedysari, 7 to 10 parts of radix notoginseng, 10 to 20 parts of poria cocos, 5 to 15 parts of lotus leaves, 10 to 15 parts of raw fructus crataegi, 10 to 20 parts of radix salviae miltiorrhizae, 10 to 15 parts of radix angelicae sinensis and 2 to 10 parts of ramulus cinnamomi. The traditional Chinese medicine composition can intervene in the atherosclerosis process through multiple ways of adjusting the blood fat level, improving aorta pathological injury, inhibiting inflammatory response, increasing intestinal flora diversity and the like, and the comprehensive treatment effect of the traditional Chinese medicine composition is equivalent to that of clinical conventional medicine statins.

The present disclosure provides pharmaceutic compositions for oral delivery comprising an antisense oligonucleotide (e.g., CIVI 008) and an oral delivery agent such as 5-CNAC. In some aspects, the disclosure provides a capsule comprising a dry blend of CIVI 008 and 5-CNAC, and optionally a statin.

The present invention relates to a pharmaceutical composition comprising a combination of an FXR agonist and at least one lipid lowering agent (e.g., PPAR-alpha agonist, PPAR-delta agonist, PPAR-alpha and delta dual agonist, and / or statin). Also disclosed is use of the combination for the treatment or prevention of a FXR mediated disease or condition, such as primary biliary cirrhosis (PBC), primary sclerosing cholangitis (PSC), portal hypertension, bile acid diarrhea, NAFLD (nonalcoholic fatty liver disease), NASH (non-alcohol-induced steatohepatitis), and other chronic liver diseases. The combination of the present invention is useful for the treatment or prevention of conditions related to elevated lipid and liver enzyme levels. The present invention also relates to packs or kits including the pharmaceutical combination.

The application provides a method for improving 2-deoxy-D-ribose-5-phosphate aldolase (DERA) activity through immobilization. The method can significantly activate the aldolase activity of DERA, and is simple, mild, simple and easy to operate, and can be applied to preparation of chiral side chains of statins.

The present invention relates to a pharmaceutical composition for treating hyperlipidemia. In particular, the present invention relates to a pharmaceutical combination of probucol with a statin drug / monascus, a pharmaceutical composition or kit containing probucol and a statin drug / monascus, and use of the pharmaceutical combination or the pharmaceutical composition or kit in preparing a medicament for treating hyperlipidemia, especially severe hypertriglyceridemia, severe hypercholesterolemia, and statin-refractory or statin-resistant hypercholesterolemia. The present invention is characterized in that the pharmaceutical combination or the pharmaceutical composition or kit containing probucol and the statin drug contain reduced doses of probucol and the statin drug / monascus, and the probucol and the statin / monascus are configured for simultaneous administration.

The present invention relates to a self-assembling selenopeptide targeting vascular cell adhesion molecule-1 (VCAM-1), a selenopeptide nanomedicine, and a preparation method and application thereof. The self-assembling selenopeptide targeting vascular cell adhesion molecule-1 includes an oxidation response unit and a vascular cell adhesion molecule-1 targeting unit sequentially connected from the N-terminus to the C-terminus; the oxidation response unit contains a selenocysteine substituted with a fatty chain. The self-assembling selenopeptide has the ability to sensitively respond and eliminate reactive oxygen species, and can target vascular cell adhesion factor-1 overexpressed in plaque tissue, with excellent active targeting. It can be used alone as a drug for treating atherosclerosis or as a carrier to effectively deliver drugs such as statins to plaque tissue, thereby jointly improving the inflammatory microenvironment of plaque tissue. In addition, the self-assembling selenopeptide as a nanocarrier also significantly improves the enrichment of statins in the liver and increases the bioavailability of statins.

A method of treating a wound may include topically administering a statin composition including a statin selected from atorvastatin, fluvastatin, lovastatin, pitavastatin, pravastatin, rosuvastatin, simvastatin, or combination thereof. The statin composition may be administered in an ointment, powder, or liquid format. The method may also include topically administering one or more antimicrobial drugs and / or naltrexone.

The invention discloses a pharmaceutical composition for treating chronic kidney disease, belongs to the field of pharmaceutical preparations in the technical field of medicines, and aims to solve the clinical requirements of patients with chronic kidney disease on dyslipidemia, especially hypertriglyceridemia, and the problem that lipid deposition is aggravated due to long-term use of existing statins. The invention provides a solution taking puerarin as a core active component. The weight content of puerarin in the pharmaceutical composition is 5.2%-100%, and the preparation method comprises the following steps: puerarin and an excipient are mixed in proportion and then are subjected to a wet granulation process to form particles, the wet granulation process adopts a hydroxypropyl methylcellulose aqueous solution with the concentration of 2%-5% as an adhesive, and the granulation time is 10-15 minutes; the pharmaceutical composition is suitable for treating chronic nephropathy and improving dyslipidemia of patients by regulating and controlling the synergistic effect of puerarin content and preparation process parameters, and is especially suitable for cases with reduction of glomerular filtration rate along with increase of triglyceride.

The present disclosure provides pharmaceutic compositions for oral delivery comprising an antisense oligonucleotide (e.g., CIVI 008) and an oral delivery agent such as 5-CNAC. In some aspects, the disclosure provides a capsule comprising a dry blend of CIVI 008 and 5-CNAC, and optionally a statin.

The invention belongs to the technical field of biological medicines, and particularly relates to application of a blood fat reducing medicine in preparation of a medicine for treating pemphigus. According to the application disclosed by the invention, the hypolipidemic drug is found to be used for treating pemphigus for the first time, and by analyzing the blood fat of a PV patient, the hypolipidemic metabolism of the patient is found to be abnormal, and the oxidative stress level is related to the classical biomarker level of PV. Lipid-induced oxidative stress was confirmed by in vitro experiments using HaCaT cells treated with serum of PV patients, and it was found that it results in STAT3 activation and mitochondrial dependent apoptosis. ATO intervention can effectively reverse the pathological process: by correcting lipid metabolism disorder, ATO significantly reduces the oxidative stress level, inhibits STAT3 phosphorylation, and reduces the occurrence of mitochondrial dependent apoptosis. The invention discloses an important relationship among lipid disorder, oxidative stress, apoptosis and STAT3 activation in PV, and prompts that statins may become a potential treatment strategy for PV.

This disclosure provides medicaments and methods for treating envenomation using small molecule inhibitors of secretory phospholipase A2 (sPLA2). The sPLA2 inhibitor AZD2716 and related compounds can be used as monotherapy. Alternatively, the sPLA2 inhibitor varespladib and / or methyl varespladib can be used in combination with a statin. When a subject has been envenomed (for example, by a snake bite or bee sting), the medicaments can be administered to prevent lethal effects or tissues damage cause by the venom: for example, acute kidney injury, mast cell degranulation, or cerebral edema. The medicaments may be contained in an automatic injection device or an injection pen to deliver an effective dose as soon as possible following envenomation.

Described is an antibody-drug conjugate (ADC) having the formula A-L, wherein A is an antibody or an antibody fragment and wherein L is a linker, said linker comprising: as a first payload a topoisomerase I inhibitor which is cell-permeable, e.g., a camptothecin cytotoxic molecule which is cell-permeable; as a second payload a topoisomerase I inhibitor which is not cell-permeable, e.g., a camptothecin cytotoxic molecule which is not cell-permeable; and as a as a third payload a toxin or a cytotoxin, e.g., an auristatin such as MMAE (Monomethyl auristatin E). Moreover, described is a pharmaceutical composition comprising said ADC and at least one pharmaceutically acceptable ingredient. Further, described method of treating a patient suffering from, being at risk of developing, and / or being diagnosed for a neoplastic disease.