199 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 invention relates to antibody conjugates which are particularly suitable for targeting CEA-expressing cells, in particular tumor cells. An antibody conjugate according to the present invention has the structure (1): AB-[(L6) b-{Z-L-D} x] y (1) wherein AB is an antibody capable of targeting a tumor expressing CEA; 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 hemiphyllum, a KSP inhibitor, a TLR agonist, an indolo-benzodiazepine # imgabs 0 # dimer or a pyrrolo-benzodiazepine # imgabs 1 # dimer (PBD), and analogs or prodrugs 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 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 invention discloses an application of DESs in extraction or in-situ separation of statins components in red yeast rice. The DESs are Btacc / Eg, Btacc / Gly, Btacc / Dim, Tebrc / La or Tebrc / Dim. According to the invention, the use of an organic solvent is avoided, operation units are reduced, and the method has great application potential; compared with a traditional organic solvent, the enzyme system is more compatible with cellulase and has higher enzyme catalysis efficiency; the strong solubility of DESs on a substrate can overcome the limitation of poor solubility of a traditional water-enzyme system; according to the present invention, the optimal process for extracting the effective components in the red yeast rice based on the BTAC / Eg (1: 2) DESs system is obtained, under the optimal extraction condition, the total extraction rate of the effective components is 9.209 mg / g, the extraction efficiency is higher than the extraction efficiency of the conventional solvent, and the extraction and the separation of the effective components in the red yeast rice are easily promoted.

The invention relates to a pharmaceutical composition for treating hyperlipidemia. The invention relates to the field of medicines, in particular to a pharmaceutical composition of probucol and statins, a pharmaceutical composition or a medicine box containing probucol and statins, and application of the pharmaceutical composition, the pharmaceutical composition or the medicine box in preparation of medicines for treating hyperlipidemia, in particular severe hypertriglyceridemia and severe hypercholesteremia, and application of the pharmaceutical composition, the pharmaceutical composition or the medicine box in preparation of medicines for treating hyperlipidemia, in particular severe hypertriglyceridemia and severe hypercholesteremia. The pharmaceutical composition, the pharmaceutical composition containing the probucol and the statins or the medicine box is characterized in that the pharmaceutical composition, the pharmaceutical composition containing the probucol and the statins or the medicine box containing the probucol and the statins contains a small dose of the probucol and the statins, and the probucol and the statins are configured to be in a form of simultaneous administration.

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.

Methods are disclosed for increasing retinal ganglion cell (RGC) survival and / or RGC axon regeneration and / or optic nerve survival and / or optic never regeneration in a subject in need thereof. These methods include locally administering to an eye of the subject a therapeutically effective amount of (a) isolated nanovesicles derived from an extracellular matrix and (b) a statin or a pharmaceutically acceptable salt thereof. Combination therapy is also disclosed for use in increasing RGC survival and / or RGC axon regeneration and / or or optic nerve survival and / or optic nerve regeneration in a subject. Disclosed is therapeutically effective amount of (a) isolated nanovesicles derived from an extracellular matrix and (b) a statin or a pharmaceutically acceptable salt thereof, for use in increasing RGC survival, RGC axon regeneration and / or optic nerve survival and / or optic never regeneration in a subject in need thereof in a subject, wherein the isolated nanovesicles and the statin are formulated for ophthalmic administration.

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 invention aims to provide a traditional Chinese medicine compound pill for treating femoral head necrosis and a preparation method thereof, and relates to the technical field of traditional Chinese medicine preparation. The traditional Chinese medicine compound pill for treating femoral head necrosis is prepared on the basis of ground beetles, leeches, pseudo-ginseng, rhizoma drynariae, eucommia ulmoides, herba epimedii, turmeric, red ginseng and exocarpium citri grandis. Long-term clinical practice and examination show that the traditional Chinese medicine compound pill has an obvious curative effect on ischemic necrosis of femoral head, especially has an obvious treatment effect on patients with early-stage femoral head necrosis, and avoids side effects such as jaw necrosis and diabetes induced by western medicines such as anticoagulants, statins and anti-osteoporosis medicines; the medicine is convenient to take, does not need to be decocted for a long time by using a professional vessel, and is not limited by time and space; operation treatment is avoided or delayed to a certain extent, and the advantages and effects of oral administration treatment of traditional Chinese medicine are fully exerted.

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 provides application of adrenochromic hydrazone in preparation of a medicine for treating subdural hematoma, and belongs to the technical field of medicines. The invention finds that the adrenochrome can improve the expression level of endothelial connexin of epidural blood vessels, enhance the resistance of blood capillaries to injury, reduce the permeability of the blood capillaries, reduce the bleeding amount of subdural hematoma, relieve inflammatory response caused by hematoma stimulation and accelerate the recovery of subdural hematoma for the first time. Therefore, the compound can be used for preparing medicines for treating subdural hematoma. The medicine can be administrated through oral administration, the risk existing in a traditional drilling drainage operation is avoided, and an alternative or auxiliary treatment scheme is provided for patients who are intolerant to statins or hormones and patients who are ineffective in treatment through combination of statins and hormones.

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.

Fungi are prolific producers of secondary metabolites and represent a rich and relatively untapped source for novel drug leads. Numerous successful therapeutics have derived from fungi, including penicillin, cephalosporin, statins, and cyclosporin. However, many promising classes of natural product are never developed into drugs because their chemical synthesis is complex or because the native organisms that naturally produce them, do so at impractically low levels. Pyridoxatins are a class of promising anti-fungal secondary metabolites produced by several naturally occurring strains filamentous fungi. The molecules have complex structures that impede straightforward chemical synthesis or analoging to increase efficacy. The disclosure herein details novel a novel use of pyridoxatin class molecules for the treatment of Candida auris and novel methods for the biosynthesis of pyridoxatins through fermentation of engineered microbes.

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.