2323 results about "Anti neoplastic" patented technology

The invention relates to the technical field of medicines, and provides a use of a heterocyclic anti-tumor compound, in particular a use of the heterocyclic anti-tumor compound in the preparation of a medicine for preventing and / or treating tumors or cancers. The compound has a tri-heterocyclic structure (for example, a structure as shown in formula (B)), has a novel structure, and provides a new direction for the development of SOS1 inhibitor drugs.

The invention relates to the field of medicinal chemistry, in particular to a substituted quinolinone compound targeting KRASG12D and application of the substituted quinolinone compound. Pharmacological tests prove that the affinity effect of the synthesized compound on a KRASG12D mutant is superior to that of a lead compound KAL-21404358. The compounds WY1-014 and WY1-062 have ideal inhibition effects on cells of human lung cancer (A549), human melanoma (A375) and human colon cancer (LOVO). The compound WY1-062 has excellent anti-tumor activity, and the activity of the compound WY1-062 is superior to that of cis-platinum.

A PI3Kα inhibitor and the use thereof. The inhibitor has a structure as shown in formula (I), has a good selective inhibitory activity on mutant PI3Kα, and can be used for preparing anti-tumor drugs.

The invention relates to the field of antitumor drugs, in particular to a pharmaceutical composition of a KRAS G12C inhibitor and Ly2090314 and application of the pharmaceutical composition. According to the invention, the Ly2090314 and the KRAS G12C inhibitor are combined to play a synergistic effect, a DNA damage repair pathway is inhibited, a better inhibition effect is generated on tumor cells containing KRAS G12C mutation, the dosage required for achieving the same anti-tumor effect is greatly reduced, and the medication safety is improved.

The invention provides application of an SRC inhibitor combined with a KRAS-G12C inhibitor to preparation of a medicine for treating KRAS-G12C mutant lung cancer and a medicine composition, and relates to the technical field of biological medicine, compared with independent use of the KRAS-G12C inhibitor, the scheme of the SRC inhibitor combined with the KRAS-G12C inhibitor can effectively inhibit proliferation and survival of KRAS-G12C mutant lung cancer cells, and the application of the SRC inhibitor combined with the KRAS-G12C inhibitor to preparation of the medicine for treating the KRAS-G12C mutant lung cancer can be used for preparing the medicine for treating the KRAS-G12C mutant lung cancer. The compound can effectively inhibit the activation of a KRAS-MARK pathway and an SRC-FAK pathway, the combination of the compound and the compound has a synergistic anti-tumor effect, and the compound and the compound can be directly combined for medication, can also be prepared into a combined preparation for treating KRAS mutant lung cancer, and have a good clinical transformation prospect.

The invention discloses an anti-tumor treatment adverse reaction risk early warning method and system, and relates to the technical field of medical information processing, and the method comprises the steps: obtaining the physiological index data of a patient, and obtaining a short-term risk prediction result based on the time sequence change characteristics of the physiological index data of a deep neural network; obtaining clinical feature data of the patient, constructing a susceptibility assessment model, and analyzing correlation features of the clinical feature data through the susceptibility assessment model to obtain a baseline risk assessment result; and according to the short-term risk prediction result and the baseline risk assessment result, calculating a comprehensive risk score, and when the comprehensive risk score exceeds an early warning threshold of the corresponding adverse reaction type, triggering an early warning signal. According to the method, a double-layer risk assessment system is constructed by combining instant physiological index changes and clinical features of patients, the technical problems that an existing early warning method is insufficient in consideration of individual differences of the patients and poor in early warning timeliness are solved, and the accuracy and timeliness of early warning of adverse reactions of anti-tumor treatment are improved.

Provided is an antibody-drug conjugate for use in the treatment of cancer in which one or more KRAS mutants, particularly a KRAS G12V mutant, a KRAS G12D mutant, and a KRAS G12C mutant, are expressed. Also provided are a drug and a drug-linker conjugate for use in the antibody-drug conjugate.　The present inventors have produced an antibody-drug conjugate with which a heterocyclic compound represented by formula (II) and having an activity of inducing the decomposition of KRAS mutant proteins can be delivered to cancer in which EGFRs are expressed, the production being achieved by linking the compound to an anti-EGFR antibody. The present inventors have also discovered a drug-linker conjugate for use in the antibody-drug conjugate or a salt thereof. In cancer in which EGFRs are expressed, the antibody-drug conjugate induces the decomposition of one or more KRAS mutants, particularly a KRAS G12V mutant protein, a KRAS G12D mutant protein, and a KRAS G12C mutant protein, thereby inhibiting the KRAS mutants and exhibiting an anti-tumor effect.

A multidrug linker, an antibody-drug conjugate comprising the multidrug linker, a preparation method for the antibody-drug conjugate, and uses of the multidrug linker and the antibody-drug conjugate in disease treatment. A specific structure can effectively reduce the aggregation of a multi-payload drug-antibody conjugate, thereby facilitating process scale-up. In addition, payload drugs can achieve a significant synergistic effect, thereby achieving a synergistic anti-tumor effect, effectively overcoming the resistance to drugs, and improving the therapeutic window of drugs.

The invention relates to the field of natural products, in particular to a dimer compound of guaiane type sesquiterpenes and uric acid as well as an extraction and separation method and application of the dimer compound. According to the invention, a new dimer compound of guaiane type sesquiterpene and uric acid is extracted and separated from carpesium abrotanoides in Guizhou, and it is found that the dimer compound has relatively strong anti-tumor activity. The compound has strong inhibitory activity on breast cancer, prostate cancer, nasopharynx cancer, liver cancer, lung cancer, leukemia, pancreatic cancer, glioma, osteosarcoma, skin cancer, cervical cancer, ovarian cancer, kidney cancer and esophageal cancer, and provides an optional scheme for broad-spectrum anti-cancer drugs. Moreover, in human prostate cancer cells PC3, human cervical cancer cells Hela, human liver cancer cells HepG2 and human glioma cells U87 which are resistant to paclitaxel, the compound also shows strong anti-cancer activity, which indicates that the compound has the potential of treating patients resistant to paclitaxel.

The invention provides a compound DOTA-HX2-DZ and application thereof, and belongs to the technical field of biological medicine. According to the invention, the molecular structure of DZ-HX2-DOTA is optimized, and a special connexon is designed and adopted, so that the problem of limited anti-tumor curative effect caused by poorer stability, fat solubility, tumor residence time and other properties of a radiolabeled drug in the prior art is solved. The compound provided by the invention can significantly reduce the risk of label removal of radioactive metal ions in an in-vivo environment, and ensures that the compound stably plays a role at a targeted part; the compound has excellent molecular lipid solubility, can penetrate cell membranes and vascular barriers more easily, improves the bioavailability of drugs, prolongs the in-vivo circulation time, prolongs the tumor residence time, and further improves the treatment efficiency. The DZ-HX2-DOTA disclosed by the invention has broad-spectrum tumor targeting property, and can be used for diagnosing and treating various types of malignant tumors.

The invention discloses application of camellia nitidissima exosome-like nano-vesicles in preparation of antitumor drugs, and belongs to the technical field of biological medicines. The exosome-like nano-vesicles are extracted from golden camellia for the first time, and the exosome-like nano-vesicles are proved to have remarkable anti-tumor activity.

The invention relates to an anti-CD3 nano antibody, an anti-CD38 antibody and a bispecific antibody containing the anti-CD3 nano antibody and the anti-CD38 antibody. According to the invention, an anti-CD3 nano antibody and an anti-CD38 monoclonal antibody are excavated and prepared, humanized design is carried out to obtain antibodies with high affinity and specificity, and different configurations of bispecific T cell conjugation antibodies targeting CD3 and CD38 are further designed, so that the CD3 and CD38 dual-specificity T cell conjugation antibodies are obtained. The antigen binding activity, the T cell-mediated tumor cell killing effect and the T cell proliferation and activation function of the antibody are systematically evaluated in vitro, and experimental results show that the T cell conjugation antibody can effectively recruit and activate T cells and has a remarkable killing effect on CD38 positive tumor cells, and it is further verified that the antibody has remarkable in-vivo anti-tumor activity and has a good application prospect. Therefore, the polypeptide has high affinity, good pharmacological characteristics and development potential.

The invention belongs to the technical field of medicines, and discloses parthenolide derivatives (general formula I), pharmaceutically acceptable salts thereof, a preparation method thereof, a pharmaceutical composition thereof and an application thereof, especially an application of the parthenolide derivatives in preparation of anti-tumor and immunotherapy medicines. # imgabs0 #

The invention provides a tumor cell exosome, an anti-tumor immune drug delivery system and a preparation method and application of the anti-tumor immune drug delivery system, the tumor cell exosome is derived from starved and stimulated tumor cells, the tumor cell exosome is coated with nano drug particles for delivery, and the exosome has the effects of enhancing immune cell infiltration and remodeling an immune microenvironment; due to the homing effect of the exosome, the medicine and the exosome are more easily accumulated in the tumor, and the targeting property is improved; due to coating and camouflage of the biological membrane of the exosome membrane, the exosome membrane is prevented from being recognized, attacked and removed by an organism, and the biological safety is improved, so that the exosome and the nano-drug act on the tumor together to achieve a synergistic effect.

The invention belongs to the technical field of genetic engineering and biological medicine, and particularly discloses a cascade response type nano-particle with a microenvironment remodeling function and a preparation method and application of the cascade response type nano-particle. The nanoparticle provided by the invention adopts a bionic hybrid membrane engineering strategy: an inner core is formed by loading an exosome inhibitor on a nano material, and the surface is covalently coupled with M2 type macrophage specific targeting peptide; the outer layer coats a macrophage membrane and active oxygen response type liposome composite membrane layer through a co-extrusion technology, and is loaded with a TLR agonist. Animal experiments show that after being injected through caudal vein, the nano-particles are enriched at a tumor site in a targeted manner through homing receptors such as membrane surface integrin alpha4beta1 and the like, and outer membrane cracking is triggered in a high-ROS tumor microenvironment, so that space-time controlled release of a TLR agonist and targeted phagocytosis of an exosome inhibitor by macrophages guided by a targeted peptide are realized. The anti-tumor synergistic effect is achieved through multiple regulation and control mechanisms, and an effective treatment strategy is provided for tumor immunotherapy.

The present disclosure relates to compounds of formula (I) and their anti-tumor uses, and their intermediates of formula (III), intermediates of formula (IV), and uses of the intermediates. The compound of formula (I) has a degrading effect on a specific target protein, which is mainly composed of three parts. The first part is a small molecule compound (SMBP, Small Molecules Binding Protein) that can bind to a protein, the second part LIN is a linker, and the three-part ULM is a ubiquitin ligand (ULM, Ubiquitin Ligase Binding Moiety), wherein SMBP is covalently bound to LIN, and LIN is covalently bound to ULM. A series of compounds designed and synthesized in the present disclosure have a wide range of pharmacological activities, including the functions of degrading specific proteins and / or inhibiting activities of specific proteins, and thus can be used in related tumor treatments.

To provide an antitumor drug having an excellent therapeutic effect, which is excellent in terms of antitumor effect and safety. Provided is an anti-cadherin 17 antibody comprising a heavy chain variable region and a light chain variable region, a drug conjugate thereof, and a composition containing the anti-cadherin 17 antibody or the drug conjugate thereof, and an application thereof as a drug.

The invention belongs to the technical field of medicine synthesis, and particularly relates to an inhibitor compound, application and a medicine for treating cancer. The invention provides an inhibitor compound or a pharmaceutically acceptable salt, which can be used for preparing an EGFR kinase inhibitor and preparing a medicine for treating or preventing cancers. The present invention also provides medicaments for the treatment of cancer comprising the inhibitor compound or a pharmaceutically acceptable salt. The compound or the medicine provided by the invention is efficient and low in toxicity, not only has higher anti-tumor activity and can effectively inhibit the growth of cancer cells, but also keeps higher brain permeability, and has wide application prospects.

The preparation method comprises the following steps: synthesizing gold nanostars (GNS) by using a seed growth method, coating mesoporous cerium dioxide (mCeO2) by using a template method, and loading a photosensitizer indocyanine green (ICG), so as to form a nano enzyme diagnosis and treatment system with chemical activity, photoactivity and photothermal effects. In the system, the gold nanostars have a good photo-thermal effect due to the multi-branched structure of the gold nanostars; on one hand, the mesoporous cerium dioxide coated on the outer layer has a chemical effect due to the nano-enzyme effect, and on the other hand, the mesoporous structure of the mesoporous cerium dioxide can better load the photosensitizer indocyanine green. All the components have good stability and biological safety, also have peroxidase simulation activity and a drug loading function, can improve the level of reactive oxygen species (ROS) in a tumor microenvironment and load photosensitizer drugs, and have an excellent anti-tumor effect and small side effects.

The invention provides a whole-process targeting polypeptide, a drug compound thereof, a drug delivery system and application of the whole-process targeting polypeptide. The whole-process targeting polypeptide comprises pHA and VAP which are covalently connected through a bridging structure; the VAP is LVAP, a reverse sequence polypeptide of the LVAP, DVAP or SVAP; wherein the amino acid sequence of the LVAP is as shown in SEQ ID NO: 1; the SVAP is a D-configuration polypeptide of the LVAP; the DVAP is a D-configuration polypeptide of the LVAP inverted sequence polypeptide; the bridging structure is amino-monoethylene glycol-carboxylic acid or a derivative thereof. The whole-process targeting polypeptide not only can cross a blood-brain barrier, target tumor neovascularization, cross a blood-tumor barrier, target tumor mimicry vessels, tumor cells and stem cells thereof, but also has better tumor cell affinity, anti-tumor treatment and in-vivo safety effects. Meanwhile, the drug compound or the drug delivery system has a synergistic effect after being combined with a chemotherapeutic drug, and the anti-tumor drug effect can be remarkably improved.

The present invention relates to the field of cancer immunotherapy. Specifically, the present invention relates to the effect of an intestinal-specific strain Anaerostipes caccae ibiome007 on anti-tumor immunity, and provides a method for improving the tumor immunotherapy response rate of patients.

The application describes the first-in-human study on using a anti-KLK2xCD3 bispecific antibody and another anti-cancer drug, in particular, in particular a taxane chemotherapy or Androgen Receptor Pathway Inhibitor (ARPI), to provide enhanced antitumor efficacy with a deeper and more durable clinical response.

The invention provides a gamma delta T cell preparation as well as a preparation method and application thereof, and belongs to the technical field of T cells. The liposome is prepared from the following raw materials in parts by weight: 15-20 parts of modified gamma delta T cell liposome, 1-3 parts of cell stimulating factors and 4-7 parts of culture medium freeze-dried powder, the modified gamma delta T cell lipidosome is prepared by embedding gamma delta T cells through lipidosome, coupling with acetylenic bond modified chitosan, and further mixing with MFAP4 protein and b4GALT1 protein. The culture medium freeze-dried powder is prepared by freeze-drying the culture medium in the engineering culture process of gamma delta T cells, and the cell stimulating factors are resveratrol and quercitrin. According to the gamma delta T cell preparation prepared by the invention, the survival ability and resistance of gamma delta T cells are improved, the anti-tumor activity of the gamma delta T cells is improved, and the gamma delta T cell preparation has relatively good antioxidant and anti-inflammatory effects, reduces the inhibition of inflammation on an immune system and has a very good treatment effect on pancreatic ductal adenocarcinoma.

The invention discloses a preparation method of a doxorubicin-loaded ginseng selenium polysaccharide nano-carrier with immunoregulation and liver cancer cell inhibition functions, and aims to solve the problems of toxic injury of tissues and organs and inhibition of an immune system caused by an antitumor drug doxorubicin. According to the invention, deoxycholic acid is grafted on the ginseng selenium polysaccharide, so that the ginseng selenium polysaccharide is hydrophobized and forms an amphiphilic polysaccharide polymer, and the limitations of large molecular weight, low bioavailability and the like of the ginseng selenium polysaccharide are overcome. The self-assembled ginseng selenium polysaccharide nanoparticles are used as carriers for delivering antitumor drugs, so that the self-assembled ginseng selenium polysaccharide nanoparticles have an immunoregulation effect and can effectively improve side effects such as immunosuppression caused by the antitumor drugs; and the carrier also has a pH sensitive response release characteristic, so that the targeting effect of the medicine in a tumor area is enhanced, and the innovative carrier has a good clinical application prospect.

The invention discloses an enantiokaurane compound with antitumor activity as well as a preparation method and application of the enantiokaurane compound. According to the present invention, chemical components of Western African plant I.trichantha tubers are deeply studied, and a variety of chromatographic separation methods such as macroporous resin, silica gel resin, medium pressure preparation-MCI column, gel normal pressure column and semi-preparative high performance liquid chromatography are combined to separate to obtain one enantiokaurane new compound Trichanthone B; experiments show that the compound obtained through separation has a good inhibition effect on an MIA PaCa-2 pancreatic cancer cell line and an A549 lung cancer cell line, and IC50 of the compound on the MIA PaCa-2 pancreatic cancer cell line reaches a nanomole level; the effect of the compound is stronger than that of positive drugs 5-fluorouracil and carboplatin, and the compound has the potential of being developed into new drugs for resisting pancreatic cancer and lung cancer.

The invention discloses an N-phenylbenzenesulfonamide compound as well as a preparation method and application thereof. The compound disclosed by the invention is shown as a formula (I). The compound is an LDHA enzyme inhibitor, is a sulfonamide compound with anti-tumor activity, shows good anti-tumor activity at the cellular level, has good safety and can be used for preparing anti-tumor drugs. # imgabs0 #

The invention relates to the technical field of ferula asafoetida endophytic fungi separation and purification, in particular to alkaloid compounds in ferula asafoetida endophytic fungi as well as a preparation method and application of the alkaloid compounds in the ferula asafoetida endophytic fungi. And extracting with dichloromethane to obtain dichloromethane part extract, and purifying and separating the dichloromethane part extract by adopting silica gel column chromatography and high performance liquid chromatography to obtain the alkaloid compounds in the endophytic fungi of ferula sinkiangensis. The alkaloid compound in the ferula sinkiangensis endophytic fungi is disclosed for the first time, the compound is subjected to an in-vitro anti-tumor pharmacodynamic experiment, and according to the experiment result, the alkaloid compound has a certain inhibition effect on MCF-7 cells; therefore, the alkaloid compound can be used for preparing the medicine for preventing and treating the breast cancer, and a new medicine is provided for preventing and treating the breast cancer.

The invention relates to the technical field of medicines, and provides mitoxantrone-loaded ZIF-8 nanoparticles, a preparation method thereof and an application of the mitoxantrone-loaded ZIF-8 nanoparticles in tumor chemical-immunotherapy. Aiming at the defects of combined chemotherapy and immunotherapy clinically at the present stage, MIT ZIF-8 synthesized by a normal-temperature full-water-phase one-pot method is used as a novel chemical-immunotherapy scheme, and the capability of inducing cell immunogenic death of a chemotherapeutic drug mitoxantrone is enhanced by utilizing pyroptosis; the anti-tumor immune activation capability is enhanced while tumor cells are killed through chemotherapy, effective chemical-immune therapy is achieved, and the responsiveness of tumors to immune checkpoint inhibitor therapy is enhanced.

Drug delivery nanoparticle compositions and methods for the treatment of a cancer are provided that can be used individually or in combination. These compositions and methods include: (1) exogenous vaccination using neoantigens or tumor-associated antigens to potentiate an anti-tumor immune response; (2) nanoparticle-based drug delivery targeting the liver, aimed at reprogramming the hepatic immune environment to reduce or eliminate tumor antigen tolerance, thereby enhancing the immune system's ability to combat metastatic cancer; and (3) expansion of the liver metastasis treatment platform to target tumor-associated lymphoid structures, supporting the immune response at the primary tumor site. Any of these methods may be optionally combined with chemo-immunotherapy for enhanced efficacy.

The invention discloses an anti-tumor drug tablet stability prediction method based on multi-source data fusion, and particularly relates to the field of pharmaceutical preparation stability prediction, and the method comprises the following steps: S1, data acquisition; s2, extracting multi-dimensional characteristic parameters; s3, constructing a stability prediction reference model; s4, calculating a real-time attenuation index; s5, determining a deviation threshold range; s6, analyzing a stability deviation index; s7, dynamically updating a prediction result; according to the method, accurate prediction of content attenuation, related substance growth and disintegration time limit change indexes is realized through integration of multi-source data, construction of a stability prediction reference model, simple trend analysis not limited to a single factor, key influence factor marking, critical threshold setting and theoretical attenuation curve fitting; the accuracy and timeliness of stability prediction of antitumor drug tablets are effectively improved, and a scientific basis is provided for drug validity period evaluation and quality risk management and control.