156 results about "Statin" patented technology

The invention provides a carbonyl reductase mutant. The carbonyl reductase mutant is obtained by performing single-point mutation or multi-point combined mutation on the 17th site, the 40th site and the 64th site of an amino acid sequence as shown in SEQ ID NO.1. The invention also provides a coding gene, a recombinant vector containing the coding gene, a co-expression engineering bacterium and an application of the co-expression engineering bacterium. Compared with a wild type enzyme, the carbonyl reductase mutant has high activity and high stereoselectivity, the enzyme activity can reach more than two times that of the wild type enzyme, the catalytic efficiency on a substrate precursor ketone is remarkably improved, the yield of a statin drug intermediate and chiral alcohol synthesized by an enzyme method of the carbonyl reductase mutant is remarkably improved, and the yield of a rosuvastatin intermediate (3R, 3R, 3R, 3R, 3R, 3R, 3R, 3R, 3R, 3R, 3R, 3R, 3R, 3R, 3R, 3R, 3R, 3R, 3R, 3R, 3R) is remarkably improved. The highest yields of the (3R, 5R)-6-chloro-3, 5-dihydroxyhexanoic acid tert-butyl ester and the atorvastatin intermediate (3R, 5R)-6-cyano-3, 5-dihydroxyhexanoic acid tert-butyl ester reach 99% and 97.6% respectively, e.e. Is larger than 99%, and the method has high industrial application value.

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.

The invention relates to the technical field of biology, and discloses nucleic acid targeting statin subunit betaE and application of the nucleic acid. The nucleic acid provided by the invention can effectively inhibit the expression of INH [beta] E, so that diseases related to the increase of the expression of INH [beta] E can be treated and / or prevented.

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 discloses a traditional Chinese medicine composition with an effect of improving artery blood vessel plaque and a preparation method and application thereof, and belongs to the technical field of traditional Chinese medicine. The technical problem to be solved is to provide a traditional Chinese medicine composition capable of improving vascular plaques such as carotid artery, aortic arch, brachial trunk, subclavian artery and the like aiming at the current situation that adverse reactions exist when statin lipid-lowering drugs and antiplatelet drugs are taken for a long time to treat artery vascular plaques. According to the technical scheme, the traditional Chinese medicine composition with the effect of improving the artery blood vessel plaque is characterized by comprising radix puerariae, red yeast rice, folium cortex eucommiae, hippophae rhamnoides leaves and natto.

It relates to statins or their pharmaceutically acceptable salts for use in the prevention and / or treatment of splanchnic vascular dysfunctions in a patient which is a mammal wherein the prevention and / or treatment comprises inhibiting and / or reverting endothelial-to-mesenchymal transition of endothelial cells.

The present invention relates to antibody conjugates which are particularly suitable for targeting cells expressing PTK7, in particular tumor cells. An antibody conjugate according to the present invention has structure (1): AB-[(L6) b-{Z-L-D} x] y (1) wherein AB is an antibody capable of targeting a tumor expressing PTK7; l is a joint connecting Z to D; z is a linking group; l6 is-GlcNAc (Fuc) w-(G) j-S-(L7) w '-wherein G is a monosaccharide, j is an integer in the range of 0 to 10, S is a sugar or a sugar derivative, GlcNAc is N-acetylglucosamine, and Fuc is fucose, w is 0 or 1, w' is 0, 1 or 2, and L7 is-N (H) C (O) CH2-,-N (H) C (O) CF2-or-CH2-; d is selected from the group consisting of an anthracycline, a camptothecin, a tubulysin, an endiyne, an amanitine, a duocarmycin, a maytansinoid, an aurestatin, eribulin, a BCL-XL inhibitor, a miscanthus semiaquilaria, a KSP inhibitor, a TLR agonist, an indolo-benzodiazepine dimer or a pyrrolo-benzodiazepine dimer (PBD), and an analog or prodrug thereof; b is 0 or 1; x is 1 or 2; and y is 1, 2, 3 or 4. The invention further relates to a method for preparing said antibody conjugate of structure (1) and to the use of said antibody conjugate of structure (1).

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.

Described herein is a method of treating biliary tract cancer (BTC) comprising administering to a subject a bispecific antigen-binding construct targeting HER2 or a bispecific antigen-binding construct (ADC) targeting HER2 linked to an auristatin analog.

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 present invention relates to the field of food and medicine, and in particular to a red apple and cherry plum composition with anti-atherosclerotic efficacy, wherein the weight ratio of the red apple and cherry plum is 1:10-10:1. Mouse animal experiments show that the red apple and cherry plum composition has a synergistic effect in anti-atherosclerotic efficacy, and the efficacy of the composition in preventing or treating atherosclerosis is better than that of using red apple or cherry plum alone. The product forms of the red apple and cherry plum composition include juice, jam, fruit powder, oral liquid products, capsules, tablets, etc. The red apple and cherry plum composition also has a certain synergistic effect when used in combination with statins and other drugs.

The invention provides a culture medium for improving Klotho protein secreted by mesenchymal stem cells and application of the culture medium, and particularly, the culture medium comprises a basic culture medium, statins and a ROCK inhibitor. The culture medium can effectively improve the Klotho protein secretion level of the mesenchymal stem cells, does not affect the biological activity of the mesenchymal stem cells, and ensures the biological function integrity of the mesenchymal stem cells; meanwhile, operation is easy, cost is low, and good clinical application value is achieved.

The invention relates to the technical field of medicines, relates to a phenazine statin compound as well as a preparation method and application thereof, and in particular relates to a phenazine statin compound as well as a preparation method and application thereof. The invention provides a phenazine statin compound as shown in a general formula I, II or III or pharmaceutically acceptable salt thereof, and R1, R2, R3 and R4 are described in the claims and the specification. The compound provided by the invention has obvious anti-tumor or antibacterial activity. # imgabs0 #

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.

A combination preparation is provided according to exemplary embodiments. The combination preparation comprises statin and cilostazol, wherein the sustained release index of cilostazol, as calculated by mathematical formula 1, is 16.652% to 28.400%.

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.

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.

In some aspects, the present invention provides cell-reactive compstatin analogs and compositions comprising cell-reactive compstatin analogs. In some aspects, the invention further provides methods of using cell-reactive compstatin analogs, e.g., treat a complement-mediated disorder, e.g., to inhibit complement-mediated damage to a cell, tissue, or organ. In some aspects, the invention provides long-acting compstatin analogs and compositions comprising long-acting compstatin analogs. In some aspects, the invention further provides methods of using long-acting compstatin analogs, e.g., to treat a complement-mediated disorder, e.g., to inhibit complement-mediated damage to a cell, tissue, or organ. In some aspects, the invention provides targeted compstatin analogs and compositions comprising targeted compstatin analogs. In some aspects, the invention further provides methods of using targeted compstatin analogs, e.g., to treat a complement-mediated disorder, e.g., to inhibit complement-mediated damage to a cell, tissue, or organ.

Described herein is a method of treating biliary tract cancer (BTC) comprising administering a bispecific antigen-binding construct targeting HER2 or a bispecific antigen-binding construct targeting HER2 linked to an auristatin analogue (ADC) to a subject.

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

Described herein is a method of treating biliary tract cancer (BTC) comprising administering to a subject a bispecific antigen binding construct targeting HER2 or a bispecific antigen binding construct targeting HER2 (ADC) linked to an auristatin analogue.

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 present invention is directed to oral pharmaceutical compositions comprising at least one statin and at least one antiseptic and / or antibacterial agent. Likewise, it is aimed at their use to prevent and / or treat diseases of the soft tissues present in the oral cavity, such as periodontal disease. A method is also described for preventing and / or treating diseases of the soft and hard tissues surrounding the tooth present in the oral cavity that comprises administering said pharmaceutical composition.

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 belongs to the technical field of medicine. The invention particularly relates to application of statin combined with a KRAS inhibitor in preparation of a medicine for treating colorectal cancer. The invention provides a new effective strategy for treatment of the KRAS inhibitor drug-resistant colorectal cancer, namely a medication scheme of statin combined with the KRAS inhibitor, can significantly improve the treatment effect of the drug-resistant colorectal cancer, effectively inhibit the growth of tumor cells, inhibit the proliferation of tumors, and improve the treatment effect of the KRAS inhibitor drug-resistant colorectal cancer. The KRAS mutant colorectal cancer has an excellent treatment effect on the KRAS mutant colorectal cancer generating drug resistance to a first-line chemotherapy regimen, overcomes the clinical treatment difficulty caused by KRAS mutation, and has a very good application prospect.

The invention belongs to the technical field of chromatographic detection, and provides a simvastatin detection method and application thereof. According to the detection method disclosed by the invention, qualitative and quantitative detection of simvastatin in a sample can be realized by adopting a high performance liquid chromatography-tandem mass spectrometry mode. In the high performance liquid chromatography detection, the simvastatin possibly existing in the red yeast rice powder and the product thereof can be detected by combining a pentafluorophenyl propyl chromatographic column and a formic acid methanol mobile phase. The detection method provided by the invention can effectively distinguish the statins and simvastatin naturally existing in the red yeast rice powder, and can effectively avoid the false positive result of simvastatin detection; the method can also be applied to detection of various products including capsules, tablets, oral liquid and the like containing the red yeast rice powder, and various quality monitoring scenes can be considered.

The present invention concerns antibody-conjugate having general structure (2):wherein AB is an antibody capable of targeting Trop-2-expressing tumours and D is selected from the group consisting of taxanes, anthracyclines, camptothecins, epothilones, mytomycins, combretastatins, vinca alkaloids, maytansinoids, enediynes such as calicheamicins, duocarmycins, tubulysins, amatoxins, bleomycins, dolastatins and auristatins, pyrrolobenzodiazepine dimers, indolinobenzodiazepine dimers, radioisotopes, therapeutic proteins and peptides (or fragments thereof), kinase inhibitors, MEK inhibitors, KSP inhibitors, and analogues or prodrugs thereof. These antibody-conjugates exhibit an improved therapeutic index. The invention further concerns a process for preparing the antibody-conjugate according to the invention, a method for targeting Trop-2-expressing cells, medical uses of the antibody-conjugates according to the invention.

In some aspects, the present invention provides cell-reactive compstatin analogs and compositions comprising cell-reactive compstatin analogs. In some aspects, the invention further provides methods of using cell-reactive compstatin analogs, e.g., treat a complement-mediated disorder, e.g., to inhibit complement-mediated damage to a cell, tissue, or organ. In some aspects, the invention provides long-acting compstatin analogs and compositions comprising long-acting compstatin analogs. In some aspects, the invention further provides methods of using long-acting compstatin analogs, e.g., to treat a complement-mediated disorder, e.g., to inhibit complement-mediated damage to a cell, tissue, or organ. In some aspects, the invention provides targeted compstatin analogs and compositions comprising targeted compstatin analogs. In some aspects, the invention further provides methods of using targeted compstatin analogs, e.g., to treat a complement-mediated disorder, e.g., to inhibit complement-mediated damage to a cell, tissue, or organ.

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.