22029 results about "Pharmaceutical Substances" patented technology

The invention belongs to the technical field of microbial fermentation, and particularly relates to lactobacillus rhamnosus capable of maintaining bone health and improving local joint inflammation and a metagen and application of the lactobacillus rhamnosus. According to the invention, the probiotic NKU ML1-2 is subjected to fermentation culture, such that a post-generation product is prepared. Results of embodiments prove that the metagen product can enhance the oxidation resistance of cartilage and osteoblasts and promote the synthesis of anti-inflammatory factors and cartilage matrixes (type II collagen and proteoglycan), and has the potential of relieving oxidative stress and inflammatory response of local joints, relieving joint inflammation and delaying cartilage destruction. The prepared metagen product is high in safety and good in stability, and can be applied to preparation of medicines for preventing and / or treating osteoarthritis; the metagen product can also be used for promoting bone health, enhancing the antioxidant capacity of osteoblasts and / or chondrocytes, promoting osteoblast activity and / or promoting calcium absorption and fixation, and a new solution is provided for joint health management.

The invention relates to application of a targeted inhibition circPDK1 reagent in preparation of an anti-esophageal cancer drug, and belongs to the field of biological medicines. The reagent for targeted inhibition of circPDK1 expression provided by the invention is shRNA or siRNA, and in-vivo and in-vitro experiments prove that the reagent can significantly inhibit circPDK1 expression and inhibit growth and migration of esophageal cancer tumor cells; after siRNA of targeted annular circPDK1 is packaged into efficient and low-toxicity LNP-siRNA, circPDK1 expression is specifically silenced, proliferation and migration of esophageal cancer tumors can be remarkably inhibited, and a basis is provided for clinical treatment and scientific research of esophageal cancer related circRNA.

Pharmaceutical formulations of novel indole compounds and psilocybin analogs are manufactured, provided in novel oral, transdermal, and nasal pharmaceutical compositions for use to treat neurological, mood or abuse diseases and disorders.

The application discloses a compound and application thereof, and belongs to the technical field of biological pharmacy. The compound has a structure shown in formula (I), or a deuterium compound thereof, or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof. The compound has good PDE3 and / or PDE4 inhibiting effect, and is of great significance to the preparation of a medicine for PDE3 and / or PDE4 related diseases.

This invention relates to pharmaceutically acceptable tryptamine analogues and salts thereof. In particular, though not exclusively, the invention relates to formulations and uses of the same as a medicament.

The invention relates to the field of medicinal chemistry, and particularly discloses a piperidine derivative as well as a pharmaceutical composition, application and a preparation method thereof. The piperidine derivative has the following general formula. The piperidine derivative can be effectively used for treating or preventing multiple sclerosis, and shows an unexpected synergistic effect in an animal model: the piperidine derivative not only can significantly improve neurological function impairment and promote recovery, but also can deeply reduce the levels of key proinflammatory cytokines IFN-gamma and IL-17 at the same time. The invention provides a novel small molecule candidate drug with central permeability, neuroprotection and comprehensive immune regulation functions for treatment of multiple sclerosis.

The invention discloses a 3-sterone-delta1-dehydrogenase mutant and application of the 3-sterone-delta1-dehydrogenase mutant in preparation of a steroid drug intermediate. The mutant is obtained by performing single mutation or multiple mutation on 551, 468, 48 and 157 sites of an amino acid sequence of 3-sterone-delta1-dehydrogenase as shown in SEQ ID NO: 1. The 3-ketosterone-delta1-dehydrogenase is subjected to molecular modification through directed evolution and semi-rational design, the mutant with improved enzyme activity is screened in a high-throughput mode, the mutant can effectively improve the conversion rate of a substrate 11alpha, 17alpha-dihydroxyprogesterone, and the substrate conversion rate of the mutant ISM-2 is improved to 92.4% compared with 36.7% before mutation.

Embodiments of the present invention provide a pharmaceutical intervention in the neonatal pig that inhibits and delays development and activation of the HPG axis, growth of the boar testis and inhibits testicular production of testosterone and androstenone, which prevents the development of aggressive behavior in the maturing boars and the presence of boar taint in the meat. The invention comprises treatment with a combination of an androgen and an estrogen in the newborn male piglet using extended drug delivery methods, with a defined duration of no more than 12 weeks, for the purpose of inhibiting the production of testosterone and androstenone and the accumulation of the boar taint-inducing molecules androstenone and skatole in the fat.

The invention provides a novel anti-human DKK-1 monoclonal antibody, aiming at solving the problems that osteoporosis antibody drugs developed in China at present are biosimilar drugs, and the existing antibody drugs also have certain defects, for example, Romosozumab is easy to cause cardiovascular adverse reactions, and DKK-1 antibody drugs aiming at osteoporosis do not appear on the market globally. According to the present invention, the rarely researched DKK-1 is adopted as the target spot to research the humanized DKK-1 antibody, such that the foundation is laid for the clinic and the effectiveness of the DKK-1 antibody, the treatment approach with the excellent effect is provided for the patient, and the problem of the lack of the innovation of the domestic antibody drug for treating osteoporosis can be hopefully solved.

The present invention relates to a pharmaceutical composition comprising a weak acid drug, with the use of a bicarbonate salt to achieve a high incorporation of the drug into the liposome and a better therapeutic efficacy. Also disclosed is a method for treating a respiratory disease using the pharmaceutical composition disclosed herein.

To provide a pharmaceutical composition for treating a cancer patient having a tumor having a total passenger gene mutation amount larger than the background mutation amount of the tumor.SOLUTION: A pharmaceutical composition for treating a subject having a tumor with a total passenger gene mutation load that is greater than the background mutation load of the tumor, wherein the background mutation load has been determined based on randomly selected genes of the tumor, comprising antibodies that bind to PD1 as an active ingredient. Antibodies that bind PD1 comprise a heavy chain variable region (HCVR) comprising the amino acid sequence of SEQ ID NO: 21 and / or comprise a light chain variable region (LCVR) comprising the amino acid sequence of SEQ ID NO: 22.SELECTED DRAWING: Figure 1

The invention provides a benzofuranone compound as well as a pharmaceutical composition and application thereof, and relates to the technical field of medicines. The benzofuranone compound is a compound as shown in a formula I, a stereoisomer thereof, a tautomer thereof, a crystalline hydrate thereof, a solvate thereof, a prodrug thereof or a pharmaceutically acceptable salt thereof. The benzofuranone compound and the pharmaceutical composition and the pharmaceutical preparation prepared from the benzofuranone compound can prevent or treat organ injury diseases, and have good treatment effects in kidney injury, liver injury, lung injury, brain injury and heart injury.

Disclosed is an oral apparatus for injection administration in the digestive tract, comprising a housing, a trigger assembly, and an administration assembly. The housing comprises a top cover at the upper part thereof, a middle housing placed in the middle, and a base located at the bottom. The material density of the middle housing is less than the material density of the base, so that the apparatus is in the shape of a roly-poly toy. The trigger assembly comprises a soluble fixing member, an elastic member, and a transmission member. The administration assembly comprises a microneedle and a drug. The apparatus provided by the present invention, by means of an arranged liquid storage bag, greatly increases the drug loading capacity and can theoretically achieve a drug loading capacity of 50 mg, which is a significant improvement over the prior art.

The invention belongs to the field of biological pharmacy, and discloses a GPCR-based ultramicro drug screening method and application thereof in screening of antipruritic traditional Chinese medicines. According to the invention, an Echo ultrasonic pipetting system is combined with a GPCR function experiment (beta-arrest recruitment) to establish the ultramicro screening method for screening the GPCR ligand. The Echo 550 system utilizes ultrasonic waves to beat liquid into 2.5 nL liquid drops and then transfer the liquid drops into a 384 or 1536 pore plate, rapid and accurate sample adding of at least 2.5 nL (1 / 400 mu L) can be achieved, ultra-micro screening and high-throughput screening can be achieved at the same time, and the method is particularly suitable for screening of itching relieving drugs.

Disclosed herein are certain thiadiazolyl derivatives Formula (I):that inhibit DNA Polymerase Theta (Polθ) activity, in particular inhibit Polθ activity by inhibiting ATP dependent helicase domain activity of Polθ. Also, disclosed are pharmaceutical compositions comprising such compounds and methods of treating and / or preventing diseases treatable by inhibition of Polθ such as cancer, including homologous recombination (HR) deficient cancers.

The invention relates to a curcumin-loaded MMP response type melittin nano-pellicle vesicle as well as a preparation method and application thereof, and belongs to the technical field of pharmaceutical preparations. The preparation method comprises the following steps: firstly, preparing curcumin entrapped lipidosome; then carrying out culture amplification on engineering bacteria carrying melittin recombinant plasmids, extracting cell membranes after removing cell walls, and carrying out ultrasonic treatment and membrane extrusion to obtain melittin cell membrane nano-vesicles; fusing the curcumin lipidosome and the cell membrane nano-vesicles in an ultrasonic extrusion mode to obtain fused vesicles; and finally, carrying out surface calcium phosphate mineralization treatment on the fused vesicles to obtain the curcumin-loaded MMP response type melittin nano pellicle vesicles. The nano mycofilm vesicle prepared by the invention can be used for preparing antitumor drugs, and the biocompatibility and in-vivo stability of nanoparticles are improved by introducing a calcium phosphate coating; through combined delivery of melittin and curcumin, the anti-tumor effect is enhanced, so that the growth and proliferation of tumor cells are inhibited.

The invention discloses a hexapeptide with a hypoglycemic effect as well as a preparation method and application thereof, and belongs to the technical field of biological medicines. The amino acid sequence of the hexapeptide is Ile-Trp-Asp-Pro-His-Phe, and the amino acid sequence of the hexapeptide is as shown in the specification. The novel hexapeptide IWDPHF with prominent DPP-IV inhibition ability is successfully identified from mulberry leaf proteolysis products through liquid chromatography-mass spectrometry and a virtual screening method, the hexapeptide IWDPHF shows the blood glucose reducing effect superior to that of part of known peptides in an in-vitro enzyme activity inhibition experiment and a zebra fish hyperglycemia model, and no obvious side effect exists; the compound has a good potential of being developed into a hypoglycemic functional product or a drug lead compound. The invention further provides the mulberry leaf peptide with the peptide fragment IWDPHF, and the mulberry leaf peptide can be applied to preparation of drugs or food for reducing blood sugar. The invention provides a new scheme and theoretical basis for treatment of diabetes, and has good market prospect and application potential.

The present invention relates to a compound having a structure represented by formula (I) and having GLP-1 receptor agonistic activity; and the use of said compound and a pharmaceutically acceptable salt, stereoisomer, solvate, or hydrate thereof in the preparation of a GLP-1 receptor agonist and in the preparation of a drug for treating and / or preventing metabolic diseases.

The present disclosure relates to compounds that function as degraders or inhibitors of BTK. The present disclosure further relates to pharmaceutical compositions comprising them, and to their use in the treatment of diseases mediated by BTK, such as cancer.

The invention relates to ultra-small prussian blue nano-particles (T-USPB-C) carrying tirofian, a preparation method of the nano-particles and application of the nano-particles in preparation of drugs for reducing MVO and MIRI. According to the preparation method, the T-USPB-C is prepared by three steps. The T-USPB-C provided by the invention can carry tirofiban, and has catalase and superoxide dismutase simulated nano-enzyme activity. Moreover, the size of the nano-scale drug is required to reach a nano-scale size, and the drug can be efficiently cleared through kidney excretion, so that the potential long-term toxicity problem is minimized. The ultra-small prussian blue nanoparticle carrying the tirofian has an excellent active oxygen scavenging capability. Microvascular perfusion can be rapidly improved through the antithrombotic effect, then the protection effect is continuously achieved through the anti-oxidation and anti-inflammatory mechanism, and microvascular injury and MIRI are effectively prevented.

The invention discloses an antibacterial peptide fragment intercepted from chitinase IDGF4 protein and application of the antibacterial peptide fragment in preparation of antibacterial drugs. According to the invention, short peptide fragments in chitinase IDGF4 protein are screened, three candidate peptides are obtained through chemical synthesis, the antibacterial performance of the candidate peptides is systematically evaluated, and the evaluation result shows that the peptide fragment with the amino acid sequence as shown in SEQ ID No.2 can effectively inhibit the growth of salmonella and staphylococcus aureus under the concentration of 1mg / mL; the antibacterial effect of the compound is confirmed in inhibition zone experiments, enzyme-labeled turbidimetry and growth curve monitoring, and the compound shows stable and remarkable antibacterial activity and can be used as a novel antibacterial molecule; the invention provides a new candidate sequence for developing the antibacterial peptide with high efficiency and low drug resistance risk, and has application potential in the aspect of preparing clinical antibacterial drugs.

The disclosure relates to an audible indicator in combination with a drug delivery device having a resilient force member capable of resting in either of two states. In a biased state, the resilient force member is biased and stores energy and in a relaxed state, the resilient force member is relaxed. The resilient force member releases the stored energy when changing from the biased state into the relaxed state, thereby generating an audible signal, wherein the resilient force member is supported by a retaining element in the biased state in order to prevent transition into the relaxed state.

The invention provides a sustained-release microneedle for treating ill-conditioned pregnancy and a preparation method and application thereof, and relates to the technical field of biological medicines.The sustained-release microneedle for treating ill-conditioned pregnancy comprises a base and a needle tip on the base, the needle tip part of the gel microneedle is made of heparin medicine, and the needle tip part of the gel microneedle is made of gelatin. The heparin medicine comprises heparin, heparin sodium, low-molecular heparin, low-molecular heparin sodium or low-molecular heparin calcium; the needle point part comprises a heparin photo-crosslinking monomer, and the base comprises a biocompatible polymer matrix. The sustained-release microneedle for treating pathological pregnancy provided by the embodiment of the invention has good mechanical strength, skin permeability and anticoagulant activity, can reduce skin bruises caused by subcutaneous injection of heparin, improves abortion caused by infection and inflammation and abortion caused by APS (anti-phospholipid antibody syndrome), can realize sustained release of drugs and increase of drug loading capacity, and has good application prospects. Sustainable drug delivery is achieved, and frequent injection is avoided.

The invention discloses a preparation method of artemisia apiacea extracellular vesicles, which comprises the following steps: step 1, pre-treating artemisia apiacea, carrying out primary centrifugal treatment, removing large plant tissues and cell debris, carrying out secondary centrifugal treatment, filtering by a needle filter, and collecting; step 2, transferring the filtered suspension to a sucrose density gradient solution, then carrying out third centrifugal treatment, collecting the solution with the concentration of 30% in the layer, and carrying out fourth centrifugal treatment to obtain artemisia apiacea extracellular vesicles; the invention further discloses an artemisia apiacea extracellular vesicle, a pharmaceutical composition for treating cerebral apoplexy, a medicine and application of the artemisia apiacea extracellular vesicle in preparation of the medicine for treating cerebral apoplexy. The naturally-sourced vesicle delivery system provided by the invention is expected to have higher safety and lower toxic and side effects, and the enrichment concentration of the therapeutic component at the focus part of cerebral apoplexy is improved, so that the bioavailability and the treatment efficiency of the medicine are remarkably improved.

The invention relates to a composite hydroxypropyl methylcellulose skeleton sustained-release material and a preparation method thereof, and belongs to the technical field of drug sustained release. The sustained-release material is prepared from 70 to 90 parts of hydroxypropyl methylcellulose (HPMC), 10 to 20 parts of sodium alginate, 8 to 15 parts of chitosan, 0.1 to 0.2 part of Omega-3 fatty acid, 0.05 to 0.06 part of vitamin D, 2.5 to 5 parts of soluble calcium salt-zinc salt composite cross-linking agent, 0.5 to 1.5 parts of hydrolyzable cross-linking agent, 3 to 10 parts of enzyme sensitive auxiliary material, 1 to 5 parts of pore-foaming agent and 2 to 8 parts of hydrophobic blocking agent. The preparation method comprises the steps of raw material pretreatment and dry mixing, active component dispersion liquid preparation, wet granulation and primary cross-linking, secondary cross-linking and drying, vacuum drying and size stabilization, curing and packaging and the like. The sustained-release material provided by the invention has the advantages of controllable drug release rate, good mechanical strength and biodegradability, is suitable for sustained-release delivery of Omega-3 fatty acid, vitamin D and other active components, and can improve the bioavailability and stability of drugs.

The invention discloses a drug relocation model construction method for simultaneously predicting drug-target interaction and drug-disease incidence relation, and belongs to the field of drug research and development, and the method comprises the following steps: integrating heterogeneous networks and attribute characteristics of drugs, targets and diseases, learning multi-relation node embedding by using RGCN, and constructing a drug relocation model for simultaneously predicting drug-target interaction and drug-disease incidence relation; a Gelato algorithm is combined to enhance a network structure, an auto-covariance is introduced to calculate a potential association score, and drug-target interaction and drug-disease association are synchronously predicted; the weighted cross entropy and N-pair loss joint optimization is adopted, unbiased training is realized, the problems of class imbalance and network sparseness are solved, and the model generalization ability and prediction precision are improved.

Provided in the present invention are compounds as VAV1 degradation agents and the use thereof. Specifically provided are compounds represented by formula (II), and tautomers, stereoisomers, pharmaceutically acceptable salts or prodrugs thereof. The compounds provided by the present invention have good efficacy, and can be used for preparing drugs for treating or preventing VAV1-related diseases.

The invention relates to a crystal form of a compound tigoran, a preparation method of the crystal form, a pharmaceutical composition containing the crystal form, and application of the crystal form in preparation of drugs for treating related diseases needing to control the pH value of gastric juice, such as gastroesophageal reflux disease and erosive esophagitis. The new crystal form DCVI of the compound tigorasone, provided by the invention, has an important value for the development of the medicine in the future.

Disclosed are novel pharmaceutical, animal feed compositions and methods of treating non-human animals comprising at least one component selected from the extract(s), fraction(s), active compound(s) and phytochemical(s), or mixtures thereof, derived from non-woody plants of the genus Hesperaloe. Animal feed compositions may comprise a basal animal feed and water soluble solids extracted from Hesperaloe and comprising at least one saponin. The water soluble solids may comprise from about 5 to about 30 wt % saponin. The compositions of the present invention can be used for the treatment of non-human animals, such as poultry and more particularly for preventing and treating coccidiosis. An embodiment provides an immunological composition useful for inducing the production of antibodies to an antigen in a non-human animal comprising an antigen, preferably a coccidia, and a saponin composition extracted from Hesperaloe. The saponins extracted from Hesperaloe biomass may comprise 25(27)-dehydrofucreastatin, 5(6),25(27)-disdehydroyuccaloiside C, 5(6)-disdehydroyuccaloiside C, furcreastatin and yuccaloiside C.

The invention discloses an application of an antibacterial peptide and an application of the antibacterial peptide in preparation of antibacterial drugs for treating carbapenem-resistant pseudomonas aeruginosa, klebsiella pneumoniae (ATCC700603), escherichia coli (ATCC25922), staphylococcus aureus and methicillin-resistant staphylococcus aureus, the antibacterial peptide is characterized in that the sequence is w-r-r-w-k-r-w-w-r-r, and the sequence is shown in the description. All amino acids are D-type amino acids; the antibacterial peptide can be used as an antibacterial substance in wash supplies, food preservative additives, medical consumable antibacterial agents and cosmetics, can be synthesized through an Fmoc solid-phase chemical method, and is low in synthesis difficulty and good in in-vivo antibacterial activity. Particularly, the antibacterial peptide has broad-spectrum killing activity against carbapenem pseudomonas aeruginosa, klebsiella pneumoniae (ATCC700603), escherichia coli (ATCC25922), staphylococcus aureus and methicillin-resistant staphylococcus aureus, the cell survival rate of the antibacterial peptide within the range of medium and low concentration (2 mu g / mL-32 mu g / mL) reaches half or more, the toxicity is small, the toxicity is almost avoided, the operability is high, and the antibacterial peptide can be widely applied to the field of medical application. The cost is low.