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208 results about "Anti neoplastic" patented technology

Aza base [3,2-b] indole derivatives, processes for their preparation and use

This invention belongs to the field of organic synthesis and relates to a nitrogen-containing [3,2-b]indole derivative, its preparation method, and its application. The nitrogen-containing [3,2-b]indole derivative is a compound, optical isomer, or pharmaceutically acceptable salt thereof, as shown in the following structure: ; wherein R1, R2, R3, and R4 are independently selected from hydrogen atoms, halogens, cyano groups, C1-C8 alkyl groups, and C1-C8 alkoxy groups; R5, R6, R7, and R8 are independently selected from hydrogen atoms, halogens, and C1-C8 alkyl groups; R9 is selected from C1-C8 alkyl groups; when R1, R2, R3, R4, R5, R6, R7, and R8 are all hydrogen atoms, R9 is selected from C1-C2 alkyl groups. The compound exhibits antitumor activity, particularly against HeLa cervical cancer, showing a significant inhibitory effect on its proliferation.
Owner:CHANGSHA MEDICAL UNIV

Antitumor drug compositions based on immune checkpoint blockade and their applications

The present invention discloses an antitumor pharmaceutical composition based on immune checkpoint blockade and its application, which comprises paroxetine hydrochloride and a T cell enhancer, which is at least one of vitamin E and thymosin. Through a series of in vitro and in vivo experiments, the present invention has first discovered that cannabidiol and paroxetine hydrochloride can effectively reduce the expression of PD-L1 on the surface of tumor cells, block the PD-1 / PD-L1 signaling pathway, and enhance the tumor cell killing effect of T cells. Based on this, the addition of a T cell enhancer can further increase the number and activity of T cells, significantly enhancing the killing ability of T cells after immunosuppression is released, thereby significantly enhancing the antitumor effect of the drug. The components of the pharmaceutical composition of the present invention, cannabidiol, paroxetine hydrochloride, vitamin E, and thymosin, exert a synergistic effect, improving the antitumor effect.
Owner:SHANGHAI HUI TIAN JIN ZE BIOTECH CO LTD

3-(5-(aminomethyl)-1-oxoisoindolin-2-yl)piperidine-2,6-dione derivatives, process for their synthesis, use

PendingCN122444688Aprevent proliferationSmall toxicityOncologyMalignancy
The application discloses a 3-(5-(aminomethyl)-1-oxoisoindoline-2-yl)piperidine-2,6-dione derivative and a synthesis method and application thereof, and relates to a 3-(5-(aminomethyl)-1-oxoisoindoline-2-yl)piperidine-2,6-dione derivative which is a compound with the following general formula (I): wherein R1 is selected from,,,,,,,,, and R2 is selected from,,, and. The compound can significantly inhibit the proliferation of leukemia, multiple myeloma, lymphoma, breast cancer, liver cancer and the like at a low dose (nanomole), can effectively degrade IKZF1, IKZF3, BRD4, GSPT1 and CK1 alpha, and has the prospect of being developed into an anti-tumor drug. The application solves the problem that the existing malignant hematological disease treatment drugs have a high safety risk.
Owner:NANTONG QUNDING PHARMACEUTICAL TECHNOLOGY CO LTD +1

A pharmaceutical composition for treating tumor and use thereof

This invention relates to a pharmaceutical composition for tumor treatment and its application. Specifically, this invention relates to a composition containing a fluorouracil drug and pyrimidine nucleosides and their derivatives. Fluorouracil drugs and pyrimidine nucleotides and their derivatives have a synergistic antitumor effect; combined use can reduce the concentration of single drugs and achieve better antitumor efficacy, while reducing toxic side effects.
Owner:WUXI XISHAN NJU INSTITUTE OF APPLIED BIOTECHNOLOGY

Lyta-c-gem complex for enhancing anti-tumor effect of gemcitabine and application thereof

The application discloses a LYTAG-Gem compound for enhancing the anti-tumor effect of gemcitabine and application thereof, relates to the technical field of biological medicine, and particularly relates to a gemcitabine (Gem) targeted delivery system based on a lysosome targeting chimera (LYTAC) and application thereof in enhancing the anti-tumor process. 2+ The system is assembled from heavy chain ferritin, Ni 2+ , NTA-PEG5000-DBCO and a targeting ligand TPP-1-N3 in a specific mass percentage, can efficiently load Gem and form a nano compound with a particle size of about 59-79 nm, the system targets tumor cells through heavy chain ferritin, and realizes site-specific release of Gem in cells by means of an endocytosis-lysosome pathway mediated by the LYTAC structure, in-vivo pharmacodynamic experiments show that the LYTAC-Gem compound can significantly inhibit the tumor growth of a KPC pancreatic cancer mouse model, molecular mechanism research further reveals that the LYTAC-Gem compound can down-regulate the expression of PD-L1 protein in tumor tissues, and it is indicated that the LYTAC-Gem compound has the potential to activate an anti-tumor immune response, and the application provides a novel targeted delivery strategy for overcoming the toxic side effects and tumor drug resistance of gemcitabine.
Owner:THE AFFILIATED SIR RUN RUN SHAW HOSPITAL OF SCHOOL OF MEDICINE ZHEJIANG UNIV +1

AuNRs@l / d-ag2s qds complex, preparation method and application thereof

PendingCN122321162AChiral selectivityPolystyrene
The application belongs to the technical field of antitumor drugs, and particularly relates to an AuNRs@L / D-Ag2S QDs complex, a preparation method and application thereof. Sodium polystyrene sulfonate is electrostatically adsorbed on AuNRs to obtain 1-PSS-AuNRs; polyallylamine hydrochloride is electrostatically adsorbed on 1-PSS-AuNRs to obtain 2-PAH-AuNRs; polyallylamine hydrochloride is electrostatically adsorbed on 2-PAH-AuNRs to obtain a non-chiral nanomaterial; and the non-chiral nanomaterial is covalently crosslinked with L / D-Ag2S QDs to obtain the AuNRs@L / D-Ag2S QDs complex. The application combines the efficient photo-thermal conversion characteristics of AuNRs with the chiral-dependent targeting and potential fluorescence imaging ability of chiral Ag2S quantum dots by constructing a complex structure, so that a novel nanodiagnostic and therapeutic agent with efficient photo-thermal performance and chiral selectivity is obtained.
Owner:YANAN UNIV

Application of Uncaria rhynchophylla neutral polysaccharide URP-W in the preparation of anti-glioma drugs

ActiveCN121005799Bachieve separationSolve the technical problems of extraction and separationOrganic active ingredientsNervous disorderCelluloseMonosaccharide composition
This invention discloses the application of Uncaria rhynchophylla neutral polysaccharide URP-W in the preparation of anti-glioma drugs, belonging to the field of anti-tumor technology of medicinal plant polysaccharides. The invention obtains a crude polysaccharide extract from Uncaria rhynchophylla through hot water extraction and ethanol precipitation, followed by purification using a DEAE cellulose column and G200 dextran gel to obtain Uncaria rhynchophylla neutral polysaccharide URP-W. The monosaccharide composition of URP-W includes arabinose, rhamnose, galactose, glucose, xylose, mannose, galacturonic acid, and mannuronic acid in a molar ratio of 17.99:6.32:21.71:27.17:2.56:7.57:16.20:0.49. Experiments have shown that URP-W can inhibit the proliferation of gliomas and induce apoptosis, exhibiting significant anti-tumor activity against glioma cells, providing a new drug raw material and treatment method for the clinical treatment of gliomas.
Owner:CHANGCHUN UNIV OF CHINESE MEDICINE

A reducing triterpenoid compound and use thereof

PendingCN122325476AWater methanolGradient elution
The application relates to the technical field of natural medicinal chemistry, and specifically discloses a triterpenoid compound and application, and a preparation method of the compound. The preparation method comprises the following steps: drying and crushing schisandra chinensis roots to obtain dried and crushed schisandra chinensis roots, extracting the dried and crushed schisandra chinensis roots by using 70% ethanol water solution under negative pressure cavitation, combining and concentrating the extract to obtain a crude extract, separating the crude extract by using a D101 macroporous adsorption resin, eluting the crude extract by using water, 30% ethanol, 70% ethanol and 90% ethanol in sequence, collecting a 70% ethanol elution part, performing MCI column chromatography on the 70% ethanol elution part, performing gradient elution on the 70% ethanol elution part by using methanol-water, collecting a depigmentation sample, performing ODS column chromatography on the depigmentation sample, performing gradient elution on the depigmentation sample by using water-methanol, collecting a target component, and purifying the target component by using a preparative high performance liquid chromatograph to obtain the target compound. The application separates a novel triterpenoid compound from schisandra chinensis roots for the first time, expands the development range of medicinal resources of schisandra chinensis plants, simultaneously provides a novel structure mother nucleus and a candidate active molecule for anticancer drug research and development, and enriches the research and development reserves of antitumor natural medicines.
Owner:QILU SCHOOL OF MEDICINE

Combination of pla2g7 inhibitor and chemotherapy drugs and its use in triple-negative breast cancer

PendingCN122342825ACancer cellPhosphorylation
The application provides a combination drug of a PLA2G7 inhibitor and a chemotherapeutic drug and its use in resisting triple-negative breast cancer, and belongs to the technical field of medicines. The combination drug is a PLA2G7 inhibitor and a chemotherapeutic drug in the same or different specifications of unit preparations for simultaneous or separate administration, and a pharmaceutically acceptable carrier. The application first discovers and proves that the PLA2G7 inhibitor Darapladib can significantly enhance the anti-tumor activity of paclitaxel, 5-fluorouracil or cisplatin on triple-negative breast cancer, and meanwhile, the combination of the PLA2G7 inhibitor and paclitaxel has a synergistic effect in down-regulating the phosphorylation level of STAT3 protein in cancer cells and inhibiting the growth and proliferation of cancer cells; the combination of the PLA2G7 inhibitor and 5-fluorouracil also shows a synergistic effect in inhibiting the growth and proliferation of cancer cells. The application provides a new and effective combination drug strategy for improving the treatment effect of the chemotherapeutic drug on triple-negative breast cancer.
Owner:CHENGDU UNIV OF TRADITIONAL CHINESE MEDICINE

A method for preparing an anti-tumor composition for pets

PendingCN122376657AYolkGreen Tea Polyphenols
This application belongs to the field of biomedicine, specifically relating to a method for preparing an antitumor composition for pets, aiming to solve the technical problems of low bioavailability, poor stability, and poor drug administration compliance of poorly soluble active ingredients in antitumor drugs for pets. The method includes: a raw material pretreatment step, in which curcumin, resveratrol, quercetin, green tea polyphenols, and astragalus polysaccharides are pulverized and sieved separately; an organic phase preparation step, in which egg yolk lecithin and solid lipids are dissolved in an ethanol-acetone mixed solvent, and curcumin and resveratrol are added and dissolved by stirring in a water bath; an aqueous phase preparation step, in which poloxamer F68 is dissolved in purified water and dissolved in a water bath; a high-pressure homogenization step, in which a nanoemulsion containing a solid lipid core is prepared; a moderately polar component encapsulation step, in which quercetin and green tea polyphenols are ultrasonically dispersed and then added dropwise to the nanoemulsion; a freeze-drying step, in which a nano-lyophilized powder is obtained; and an outer hydrophilic component coating step, in which astragalus polysaccharides are sprayed or adsorbed onto the surface of the freeze-dried powder. The composition obtained by this method is a core-shell multilayer nanoparticle with a core consisting of curcumin and resveratrol encapsulated by solid lipids, a middle shell adsorbing quercetin and green tea polyphenols, and an outer shell coated with astragalus polysaccharides. This application utilizes the above-mentioned layered encapsulation technology to achieve stable co-encapsulation of multiple antitumor active ingredients, improve the bioavailability of poorly soluble components, optimize drug stability, and enhance antitumor effects through multi-target synergistic effects. Simultaneously, it endows the composition with immunomodulatory functions and sustained-release properties. The composition can be formulated into a nano-lyophilized powder form, making it easy to add to pet food or formulate into a paste for administration, improving pet drug compliance. Figure 2 is a schematic diagram of the three-layer core-shell nanoparticle structure of the composition of this invention.

Purino[1,2-a]carbazolin derivatives, their preparation methods and applications

This application discloses a purino[1,2-a]carbazolin derivative, its preparation method, and its application. Specifically, it discloses a compound having the structure shown in Formula I, or its stereoisomers, solvates, metabolites, pharmaceutically acceptable salts, cocrystals, or prodrugs: ; wherein R1 and R2 are each independently selected from hydrogen, hydroxyl, carboxyl, substituted or unsubstituted C1-C6 alkyl, -CONH-R3, and -COO-R4; wherein R3 is a substituted or unsubstituted C1-C5 alkyl, and the substituent can be any of cyano, halogen, alkylC1-C5 alkoxy, C1-C5 alkylsulfonyl, di(C1-C5 alkyl)amino, nitrogen-containing heterocyclic, aryl, and C1-C5 heteroaryl; R4 is selected from any of substituted or unsubstituted aryl C1-C5 alkyl and nitrogen-containing saturated heterocyclic C1-C5 alkyl. This compound can be used as a TDP1 inhibitor for antitumor therapy.
Owner:JIAYING UNIV

Stress granule targeting degraders, methods of making and using the same

ActiveCN119751442BUbiquitin ligaseNeuro-degenerative disease
This invention relates to the field of pharmaceutical technology, and discloses a stress particle targeted degrader, its preparation method, and its applications. The compounds provided by this invention include ternary complexes composed of stress particle protein, a linker group, and an E3 ubiquitin ligand, or ternary complexes composed of stress particle protein, a linker group, and a ribonuclease L ligand. Compounds with different ligands exhibit good targeting and degradation effects on stress particles and can be used as stress particle targeted degraders in the preparation of antitumor drugs and anti-neurodegenerative disease drugs, showing promising application prospects in treating stress particle-induced tumor drug resistance and neurodegenerative diseases.
Owner:SUN YAT SEN UNIV

A tumor-resistant formononetin derivative, a preparation method and application thereof

The present application relates to the chemical medicine field, specifically, it relates to a kind of anti-tumor calophyllol derivative, preparation method and application, the calophyllol derivative has good inhibitory effect on thioredoxin reductase activity, and it is found that the molecule inhibits the activity of thioredoxin reductase by inhibiting the selenium cysteine of thioredoxin reductase carbon end, and then kills tumor cell, and then obtain the anti-tumor candidate drug with higher activity and better pharmacokinetic characteristics.
Owner:AFFILIATED HOSPITAL OF GANSU UNIV OF TRADITIONAL CHINESE MEDICINE

125 I. Nanoparticles, their preparation methods, and applications

ActiveCN119185537BEfficient use ofImprove utilization efficiencyPowder deliveryPhotodynamic therapySinglet oxygenBrachytherapy
This invention relates to the fields of brachytherapy and radiosensitization, specifically providing a... 125 I-nano implantable particles, their preparation methods, and applications. 125 The 1-nanometer implanted particles have a core-shell structure, consisting of a particle core and particles adsorbed on the outer surface of the particle core. 125 I and the particles encapsulated in the nucleus and 125 The outer shell of the I-type photosensitizer is a covalent organic framework. This invention... 125 The core of the I-nanometer implanted particle is used to enhance the energy deposition of gamma rays and X-rays, generating more hydroxyl radicals; the shell containing a type I photosensitizer is used to absorb the energy of Auger electrons and internal conversion electrons and excite the photosensitizer to generate singlet oxygen, effectively improving the response to... 125 The efficiency of I decay energy utilization. 125 I-nano implanted particles, combined with internal radiation therapy and radiodynamic therapy, destroy tumor cell DNA and cell membranes, enhance tumor killing and induce immunogenic cell death, thereby activating anti-tumor immunity and inducing remote effects.
Owner:PEKING UNIV

Preparation and application of spaced disulfide bridge-linked dimer prodrugs and their self-assembled nanoparticles

ActiveCN118439985BDisulfide bondingDimer
The preparation and application of spaced double disulfide bond bridged dimer prodrug and self-assembled nanoparticles thereof belong to the technical field of medicine, and relate to the synthesis of the connection of the spaced double disulfide bond bridged dimer prodrug shown in structural general formula (I) and the construction of the spaced double disulfide bond bridged dimer prodrug shown in structural general formula (II) and self-assembled nanoparticles thereof, and the application thereof in drug delivery. The preparation method is simple and easy to implement, the spaced double disulfide bond bridged dimer prodrug can be self-assembled to form nanoparticles, and has the ability of redox dual response drug release, so that the intelligent response activation of the prodrug in tumor cells can be realized, and the anti-tumor effect and safety of the prodrug are ensured. The anti-tumor effect, pharmacokinetic parameters and safety thereof are superior to those of the prodrug nanoparticles bridged by a single disulfide bond. The present application provides a new strategy for developing a high-efficiency low-toxicity drug delivery system, and meets the urgent needs of high-end chemotherapy preparations in clinical practice.
Owner:SHENYANG PHARMA UNIV

Preparation method and application of a sarcosine-based pH-responsive polyamino acid drug-loaded nanoparticle

This application provides a method for preparing pH-responsive polyamino acid drug-loaded nanoparticles based on sarcosine and their application. Sar-NNCA, L-lysine-NCA, and L-phenylalanine-NCA are dissolved in anhydrous DMF and polymerized under argon protection with a hexamethyldisilazine initiator to obtain a polyamino acid block copolymer Sar-NNCA. 80 -Lys(Cbz) n -Phe 10 The crude product was deprotected under HBr / acetic acid and loaded with DOX to obtain Sar. 80 -Lys n -Phe 10 -DOX. This application describes the preparation of a pH-responsive polymer nanoplatform, Sar, by encapsulating doxorubicin in polysarcosine-polylysine-polyphenylalanine nanoparticles via Schiff base bonds. 80 -Lys n -Phe 10 -DOX is used for tumor treatment. These polyamino acid nanoparticles are spherical with an average particle size of approximately 200 nanometers, exhibiting pH-responsive properties, excellent cellular uptake capacity, and anti-tumor effects. In vitro experiments show that Sar... 80 -Lys n -Phe 10 The carrier material exhibits excellent biocompatibility. The newly synthesized Sar... 80 -Lys n -Phe 10 -DOX nanomicelles show promise as a drug delivery system for cancer treatment.
Owner:NINGDE NORMAL UNIV

A method for synthesizing a functionalized phthalide lactone compound

PendingCN122444675AOrganic synthesisPhthalide
Phthalide lactones, as an important class of benzopentolactone skeleton, are widely distributed in natural products, medicinal plants and bioactive molecules, and have significant pharmacological activities and synthetic application potential. This kind of structure not only shows various biological activities such as antibacterial, anti-inflammatory, antitumor, antioxidant, but also is an indispensable core structural unit in many drug molecules and lead compounds. At the same time, cyano is a very valuable functional group in the field of organic synthesis and medicinal chemistry, with strong electron-withdrawing properties, strong structural stability and other advantages, which can effectively improve the electronic distribution, lipid solubility and drug performance of the molecule. In view of the important significance of phthalide lactones and cyano in organic synthesis and drug research and development, the present invention develops a synthetic method for efficiently constructing cyano-containing alkyl chain substituted phthalide lactone compounds. It has important value in medicinal chemistry and organic synthesis.
Owner:CHUZHOU UNIV

A composition for enhancing tumor immunogenicity and use thereof

PendingCN122097453AAntineoplastic agentsPlant ingredientsSide effectRadix Astragali seu Hedysari
The application belongs to the technical field of tumor immunotherapy, and particularly relates to a composition for enhancing tumor immunogenicity and application thereof. The composition for enhancing tumor immunogenicity comprises, in terms of mass fraction, 10-15 parts of radix stephaniae tetrandrae, 10-20 parts of radix astragali, 3-9 parts of glycyrrhiza uralensis, and 3-12 parts of atractylodes macrocephala. The composition for enhancing tumor immunogenicity provided by the application is a natural traditional Chinese medicine prescription, has good biocompatibility, low toxicity and side effects, and is suitable for long-term treatment. The composition enhances immunogenicity by up-regulating MHC-I expression of tumor cells, activates CD8 + T cell-mediated anti-tumor effect, realizes autologous immunotherapy, and can avoid related side effects of exogenous immunotherapy. The composition can also be used in combination with a PD-1 blocker to synergistically improve anti-tumor efficacy and prolong patient survival.
Owner:GUANGZHOU UNIVERSITY OF CHINESE MEDICINE

Use of thieno[2,3-c]pyrazole compounds in the preparation of antitumor drugs

The application discloses a kind of thieno [2, 3-c] pyrazole compounds in preparation antitumor drug purposes, belong to pharmaceutical chemistry technical field.The application provides a kind of small molecule skeleton thieno [2, 3-c] pyrazole compound I and II, compound I is 2-oxo benzo [d] [1, 3] oxathiole-6-yl 1-(3-fluorophenyl)-3-methyl-1H-thieno [2, 3-c] pyrazole-5-carboxylate.Compound II is 1-(4-chlorophenyl)-N-[4-((4-ethylpiperazine-1-yl)methyl)phenyl]-3-methyl-1H-thieno [2, 3-c] pyrazole-5-formyl.Both have strong antitumor activity.Compound II has strong inhibition to a variety of human tumor cells, such as bone sarcoma MG63, breast cancer HCC1806, liver cancer LM3, lung cancer A549, colorectal cancer HCT-8 and the like, provides new candidate compounds for broad-spectrum antitumor drugs.
Owner:KUNMING MEDICAL UNIVERSITY

Highly active 8-hydroxyquinoline rhodium complex in vitro and in vivo, and synthesis method and application thereof

PendingCN122444791ADimerCancer cell
The application discloses a high-activity 8-hydroxyquinoline rhodium complex in vivo and in vitro and a synthesis method and application thereof. The 5,7-dichloro-8-hydroxy-2-methylquinoline, dichloro (pentamethylcyclopentadienyl) rhodium (III) dimer, methanol, dimethyl sulfoxide and triethylamine are taken, and under a closed condition, the reaction is carried out at 80 DEG C for 3 days; after being cooled to 37 DEG C, filtration and drying are carried out, and the 5-chloro-8-hydroxyquinoline rhodium complex is obtained. The 5-chloro-8-hydroxyquinoline rhodium complex has obvious inhibiting effect on SK-OV-3 and SK-OV-3 / DDP cancer cells, shows superior antitumor activity, and has small toxicity to normal HL-7702 cells; the 5-chloro-8-hydroxyquinoline rhodium complex has potential medicinal value and is expected to be used for preparation of various antitumor drugs.
Owner:YULIN NORMAL UNIVERSITY

A highly safe tumor treatment preparation based on a prodrug-enzyme-neutralizing antibody three-system and a preparation method and application thereof

The application discloses a high-safety tumor treatment preparation based on a prodrug-enzyme-neutralizing antibody three-system, and a preparation method and application thereof. The preparation comprises three core components: (a) a prodrug, which is coupled by an anti-tumor drug (such as doxorubicin) and cephalosporin; (b) an activating enzyme, such as beta-lactamase, which is specifically expressed in the tumor by phage, catalyzes the hydrolysis of the prodrug, and releases the active drug; and (c) a neutralizing antibody, such as an anti-doxorubicin monoclonal antibody, which can specifically bind and neutralize the active drug overflowing into the blood circulation. The application first integrates the precise killing strategy of "prodrug-local activation" and the safety strategy of "neutralizing antibody-systematic protection" into a complete treatment closed loop, utilizes the "differential neutralization" characteristics of the anti-doxorubicin antibody, effectively protects normal tissues from toxic damage under the premise of not affecting the local efficacy of the tumor, and significantly improves the therapeutic index of the chemotherapy drug, reduces the side effects such as cardiotoxicity and bone marrow suppression, and provides a new paradigm with high efficiency and safety for tumor treatment.
Owner:GUANGZHOU XINGLIN NO 1 BIOTECHNOLOGY CO LTD

A quinazoline compound and application thereof

The application belongs to the technical field of chemical medicine raw materials, and particularly relates to a quinazoline compound and application thereof, a structure of the compound is shown as formula I. It is verified through experiments that the compound provided in the application has good in-vitro anti-tumor activity, and lays a foundation for further development of anti-tumor drugs. Formula I.
Owner:HEBEI MEDICAL UNIVERSITY +1

Use of raspberry ketone in immune combination therapy for pancreatic cancer

The application of raspberry ketone in the immunotherapy of pancreatic cancer belongs to the technical field of biological medicine, and provides the application of raspberry ketone in the immunotherapy of pancreatic cancer. The application discloses that raspberry ketone can specifically and widely up-regulate the expression of MHC-I molecules on the surface of pancreatic cancer cells, and significantly enhances the infiltration and function of anti-tumor effector T cells in the tumor immune microenvironment. In-vivo and in-vitro experiments prove that raspberry ketone can reverse tumor immune escape by up-regulating MHC-I, and after being combined with a PD-1 immune checkpoint inhibitor, the raspberry ketone can produce a significant synergistic anti-tumor effect, significantly inhibit the growth of pancreatic cancer and prolong the survival period of tumor-bearing mice. The application provides a new strategy of combining a natural small molecule immunomodulator with an existing immunotherapy, and provides an innovative solution and a drug candidate for overcoming the difficulty of pancreatic cancer tolerance to immunotherapy.
Owner:HARBIN INST OF TECH +1

Cancer treatment comprising 3,5-disubstituted phenylalkynyl compounds and immune checkpoint inhibitors

The present invention aims to solve the problem of providing a novel combination therapy with excellent antitumor effects. The present invention provides an antitumor agent (excluding pembrolizumab as an active ingredient) which includes as an active ingredient, fobamintib or a pharmaceutically acceptable salt thereof, to be administered in combination with an immune checkpoint inhibitor (excluding a CD155 / TIGIT pathway antagonist) and at least one or more other antitumor agents to a cancer patient.
Owner:TAIHO PHARMA CO LTD

Use of novel antigen esr1-derived ctl epitope peptide in preparation of drugs for treating tumors

PendingCN122351466ACtl epitopeAntigen receptors
This invention belongs to the field of biomedical technology, specifically disclosing the application of a CTL epitope peptide derived from the neoantigen ESR1 or its encoded nucleic acid in the preparation of a drug for treating tumors. Through analysis of the COSMIC database, epitope prediction, and in vitro and in vivo immunomodulatory activity experiments, this invention identified an HLA-A2-restricted CTL epitope peptide derived from the neoantigen ESR1. This mutant epitope peptide originates from a high-frequency mutation of ESR1 and can effectively stimulate and induce the production of neotope-specific cytotoxic T lymphocytes, specifically distinguishing between wild-type and mutant sequences, and killing tumor cells expressing the mutant epitope, exhibiting good anti-tumor effects. The resulting drug for treating tumors may contain the CTL epitope peptide derived from the neoantigen ESR1 or its encoded nucleic acid, or may contain a T-cell receptor, chimeric antigen receptor, or its encoded nucleic acid that specifically recognizes the mutant epitope peptide, demonstrating good therapeutic potential and clinical application prospects.
Owner:ZHENGZHOU UNIV

A cell preparation targeting bone metastatic tumor cells, its preparation method and application

This invention discloses a cell preparation targeting bone metastatic tumor cells, its preparation method, and its application, belonging to the field of biomedical technology. The cell preparation comprises senescent neutrophils and drug-loaded cationic liposomes internalized within them. The cationic liposomes encapsulate a STING agonist and a pan-photokinase inhibitor. The preparation method includes: preparing drug-loaded liposomes using a thin-film dispersion-ultrasound method; obtaining senescent neutrophils through in vitro culture of extracted neutrophils; and preparing a senescent neutrophil preparation loaded with liposomes. This invention utilizes the natural bone marrow homing ability of senescent neutrophils to achieve precise targeting of bone metastatic tumor cells, and co-delivers two drugs through liposomes, simultaneously activating anti-tumor immunity and inducing tumor cell apoptosis / autophagy, synergistically treating bone metastases. This system has high drug loading capacity, good encapsulation efficiency, and sustained-release effect, and the preparation process is simple and controllable, providing a new strategy for the treatment of cancer bone metastases.
Owner:SICHUAN UNIV

Preparation method of fucoidan from Sargassum hemifolia and its application in the preparation of anti-hepatocellular carcinoma drugs

ActiveCN118047883BMitochondrial pathwayApoptosis
This invention discloses a method for preparing fucoidan from *Sargassum hemifolia* and its application in the preparation of anti-hepatocellular carcinoma drugs. Experimental results show that *Sargassum hemifolia* fucoidan Fb has a strong inhibitory effect on HepG2 hepatocellular carcinoma cells, significantly stronger than the inhibitory effects of *Sargassum henryi* polysaccharide Fh and *Sargassum fusiforme* polysaccharide SFPS on HepG2 hepatocellular carcinoma cells. After treatment of HepG2 hepatocellular carcinoma cells with *Sargassum hemifolia* fucoidan DF1 and DF2, apoptosis is ultimately induced through the interaction and cooperation of exogenous (death receptor pathway) and endogenous (mitochondrial pathway). *Sargassum hemifolia* fucoidan possesses strong antitumor activity and therefore can be used to prepare anti-hepatocellular carcinoma drugs.
Owner:GUANGDONG OCEAN UNIVERSITY

Thymosin alpha 1 mutant polypeptides and uses thereof

PendingCN122302030ADiseaseMutant
This invention relates to the field of biomedicine, specifically providing a mutant thymosin α1 polypeptide and its applications. The mutant differs from natural thymosin α1 by substituting at least one amino acid at positions 15, 21, and 27, with preferred mutations including D15M, E21W, and E27R. Amino acid substitutions at these sites significantly improve the structural stability and in vivo pharmacokinetic properties of thymosin α1. Experimental results show that, while maintaining the main secondary structural features and overall thermal stability without significant degradation, the mutant improves serum stability and in vivo pharmacokinetic properties, exhibiting superior in vivo half-life and antitumor activity. This invention also provides nucleic acid molecules encoding the mutant, expression vectors, host cells, and pharmaceutical compositions containing the mutant, which can be used for the treatment of tumors, viral infections, and immune-related diseases.
Owner:XIANGYA HOSPITAL CENT SOUTH UNIV

Application of polydextral lactic acid and polydextral lactic acid-glycolic acid copolymer in constructing micro / nanocarriers for antitumor drugs

PendingCN122297697ANanocarriersImmunotherapeutic agent
The application of poly(D-lactic acid) and poly(D-lactic acid-glycolic acid) copolymers in constructing micro / nanocarriers for antitumor drugs belongs to the field of biomedical polymer materials and nanomedicine. The antitumor drugs are small-molecule chemotherapeutic agents, small-molecule photosensitizers, small-molecule immunotherapeutic agents, and small-molecule radiosensitizers. The particle size of the poly(D-lactic acid) and poly(D-lactic acid-glycolic acid) copolymers is 10–5000 nm. The effective concentration of the poly(D-lactic acid) and poly(D-lactic acid-glycolic acid) copolymers is 1–500 mg / kg. The antitumor mechanism of the poly(D-lactic acid) and poly(D-lactic acid-glycolic acid) copolymers includes increasing the activity of effector T cells in the tumor microenvironment and increasing the concentration of cytokines such as IFN-γ at the tumor site. In the field of tumor therapy, PLA and PLGA materials composed of D-lactic acid have shown good effects in inhibiting tumor growth, prolonging the survival period of tumor-bearing mice, and activating antitumor immune responses.
Owner:HARBIN INST OF TECH +1