216 results about "Neoplastic disease" patented technology

A method based on a multi-task learning model comprises the following steps: acquiring and processing histopathological image data of gastritis through a data preparation and preprocessing step; feature extraction is performed by using a self-supervised learning pre-trained model, and image blocks are coded into high-dimensional feature vectors; and constructing a multi-task learning model, learning feature representation through a full connection layer module and an attention layer module, and outputting a classification result of each task. And carrying out model training and optimization by using an optimizer, adding multitask loss through a loss function, and dynamically adjusting the model performance. The trained model can automatically detect and grade gastritis, atrophy, acute activity, intestinal metaplasia and other pathological indexes, outputs a standardized evaluation result, and assists in pathological diagnosis. According to the method, a multi-task deep learning framework based on self-supervised learning pre-training is constructed, a traditional single-task modeling mode is broken through, deep learning framework design is driven through pathological index association, and accuracy and clinical practicability of non-neoplastic disease assessment of the stomach are remarkably improved.

The present application discloses substituted polycyclic heterocycles compound of Formula (I), pharmaceutically acceptable salt and / or solvate and pharmaceutical compositions thereof useful in the treatment of proliferative disease or condition characterized by a dysregulation of the RAS-ERK pathway such as neoplasm disease or disorder, inflammatory disease or immune system disorder.

The invention discloses a brain tumor disease treatment effect evaluation method, and belongs to the technical field of radiotherapy plan evaluation, and the method specifically comprises the steps: obtaining the brain multi-modal image data of a patient, and extracting a three-dimensional tumor region and a corresponding perfusion parameter; constructing a biological target region hierarchical structure containing a tumor overall region and an anoxic subregion; a relative hypoxia degree parameter is obtained by calculating the cerebral blood flow ratio of the hypoxia subregion to other regions of the tumor; historical treatment case data are deconstructed, and a dose-curative effect associated parameter set is established; training and outputting a dose adjustment strategy model for the hypoxia subregion; and generating a final radiotherapy dose planning scheme according to a dose adjustment value output by the model in combination with a clinical guide basic dose. Through a data-driven dose decision-making mechanism, the limitation of traditional uniform dose irradiation is overcome, so that an objective and reliable evaluation basis is provided for clinical selection and optimization of personalized treatment schemes.

Described is an antibody-drug conjugate (ADC) having the formula A-L, wherein A is an antibody or an antibody fragment and wherein L is a linker, said linker comprising: as a first payload a topoisomerase I inhibitor which is cell-permeable, e.g., a camptothecin cytotoxic molecule which is cell-permeable; as a second payload a topoisomerase I inhibitor which is not cell-permeable, e..g., a camptothecin cytotoxic molecule which is not cell-permeable; and as a as a third payload a toxin or a cytotoxin, e.g., an auristatin such asMMAE (Monomethyl auristatin E). Moreover, described is a pharmaceutical composition comprising said ADC and at least one pharmaceutically acceptable ingredient. Further, described method of treating a patient suffering from, being at risk of developing, and / or being diagnosed for a neoplastic disease.

The disclosure includes compounds of Formula (A):wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, and R12, j, k, m, n, Y, W, W1, W2, W3, V, L, Z1, Q1, Q2, Q3, and Q4, are defined herein. Also disclosed is a method for treating a neoplastic disease, an autoimmune disease, or a neorodegenerative disease with these compounds.

The use of a combination of a pyrido[2,3-d]pyrimidin-2(1H)-one derivative and an anti-PD-1 or anti-PD-L1 antibody and / or a chemotherapeutic drug in the preparation of a drug for preventing or treating a tumor disease.

The disclosure includes compounds of Formula (I) (1) wherein Q0, Q1, Q2, Q3, Q4, Z, W, i, j, m, n, Warhead, R0, R1, R3, R4, R5, R6, and R7, are defined herein. Also disclosed is a method for treating a neoplastic disease, autoimmune disease, and inflammatory disorder with these compounds.

The invention discloses a compound of a Galectin-3 and EGFR (Epidermal Growth Factor Receptor) double-target inhibitor in the technical field of biological medicines, and the compound disclosed by the invention not only shows a relatively strong Galectin-3 and EGFR binding effect, but also has certain in-vitro anti-hepatic fibrosis activity, and can be applied to Galectin-3 and EGFR target related tumor diseases. As a double-target anti-hepatic fibrosis candidate compound based on Galectin-3 and EGFR, which is reported for the first time, the compound has further values of research and development and research of original new drugs based on double targets of Galectin-3 and EGFR.

The application provides use of a compound A or a pharmaceutically acceptable salt thereof as a Bruton's tyrosine kinase (BTK) inhibitor in preparation of a drug for treating a BTK-related tumor disease. In vitro and in vivo test results show that the compound A has good inhibitory activity on BTK kinase, good inhibitory activity on human B-cell lymphoma cells with high BTK expression, and good in vivo anti-tumor activity. In addition, the compound A has good pharmacokinetic properties and metabolic stability, and can be used for developing a drug preparation for treating a BTK-related tumor disease, and has important clinical application value.

The invention belongs to the field of natural medicines and medicinal chemistry, and discloses a thiotriptolide derivative and a preparation method, a pharmaceutical composition and application thereof. Specifically, the invention discloses a thiotriptolide derivative shown as a general formula I and a general formula II. The derivatives are prepared in an artificial synthesis mode, pharmaceutical compositions containing the derivatives, and uses of the derivatives in preparation of drugs for treating tumor diseases.

In one aspect, the disclosure relates to immunogenic compositions comprising a semisynthetic saponin adjuvant (VSA) including, but not limited to, VSA-1 and VSA-2, derived from a Momordica saponin and at least one antigen. In a further aspect, the immunogenic compositions can include other known adjuvants, emulsifiers, and / or surface-active agents and can be formulated as liposomes, micelles, emulsions, and the like. Also disclosed are methods of eliciting effective immune responses to viral, bacterial, protozoal, and neoplastic diseases using the disclosed immunogenic compositions.

The invention relates to organic chemistry, pharmacology and medicine and concerns novel peptides characterized in that they exhibit antitumour activity, which can be used, in particular, for the prophylaxis and treatment of neoplastic diseases in a subject. In addition, the present invention also includes the use of the claimed peptides for the treatment of neoplastic diseases, as well as pharmaceutical compositions for the treatment of neoplastic diseases which contain the claimed peptides.

The invention belongs to the field of molecular fluorescent probes, and particularly discloses a near-infrared fluorescent probe of quinone oxidoreductase 1 (NAD (P) H: quinone oxidoreductase 1, NQO1) with an in-situ covalent anchoring function and a preparation method of the near-infrared fluorescent probe. According to the probe, dicyanoisophorone is used as a core fluorophore, an aldehyde group is used as an NQO1 covalent anchoring group, and 3-methyl-3-(2, 4, 5-trimethyl-3, 6-dioxocyclohex-1, 4-diene-1-yl) butyrate is used as a recognition group of NQO1. The invention also provides an application of the near-infrared fluorescent probe with the in-situ covalent anchoring NQO1. Compared with other probes, the probe is simple in synthesis method and suitable for industrial production, and has high sensitivity, high selectivity and good biocompatibility in NQO1 detection. The fluorescent probe disclosed by the invention can realize covalent labeling and in-situ imaging functions after target NQO1 recognition response. Long-time in-situ tracking and imaging can be carried out on tumor cells and tissues by monitoring the NQO1 level, and a simple and effective method is provided for accurate detection of tumor disease related protease.

Various embodiments of the invention provide binding agents for glypican-3 (GPC3), including antibodies or antigen-binding fragments thereof that bind to GPC3 and antigen recognizing receptors (e.g., CARs) that target GPC3 including cells that express GPC3. Embodiments of the i n vention also provide cells comprising such binding agents such as CAR T-cells, therapeutic compositions comprising such cells and methods of using one or more of the binding agents, cells or therapeutic compositions for the treatment of diseases or disorders associated with GPC3 expression such as various neoplastic diseases or disorders (e.g., hepatocellular carcinoma). Various embodiments of the invention also provide methods and systems for treati ng hepatocellular carcinoma (HCC) utilizing a combi nation of radiofrequency (RF) ablation and GPC3-targeted cell therapy. In certain embodiments, immune modulators, such as checkpoint inhibitors, may be co-administered to potentiate immune responses. Additionally, compositions and kits comprising RF ablation devices and GPC3-targeted cell therapy formulations are provided.

The present invention discloses biphenyloxadiazole ether derivatives as immune checkpoint inhibitors capable of blocking the PD-1 / PD-L1 signaling pathway, as well as their preparation methods and uses. These compounds, as shown in Formula I below, can modulate the PD-1 / PD-L1 signaling pathway to treat a variety of related tumor diseases through tumor immunotherapy, demonstrating potential drug development. The biphenyloxadiazole ether derivatives of the present invention, or their pharmaceutically acceptable salts, racemates, optical isomers, or solvates, are also disclosed. #imgabs0#

The invention provides compounds of formula (IA) and compounds of formula (IB) and pharmaceutically acceptable salts thereof; wherein A is selected from group (A1) and group (A2): wherein #1 is attached to the carbon atom forming the oxime moiety and wherein group (A1) is optionally substituted by one or two R10 and group (A2) is optionally substituted by one R10, and wherein R1, X, R2 and R10 are as defined in the claims, as well as methods of using the compounds to treat neoplastic diseases, in particular cancer.

The invention belongs to the technical field of biomedicine, and particularly relates to a polypeptide, an immunogen, a polyclonal antibody for detecting hnRNPK protein K163 site lactylation and a preparation method and application of the polyclonal antibody. The invention provides an hnRNPK protein K163 site lactylated polypeptide, the polypeptide is used for preparing an immunogen to further prepare a lactylated antibody aiming at the hnRNPK protein K163 site, the lactylated antibody can be used for tumor diagnosis, curative effect judgment or prognosis judgment products, and research on the application of the lactylated modification of the hnRNPK protein in tumor diseases, tumors, tumors and the like is facilitated. The invention has the effect of inhibiting glioma, especially in the occurrence and development process of children glioma, and provides a potential action target for diagnosis or treatment of clinical tumor diseases.

The present invention relates to a device for intravascular drug delivery, preferably an implant for intravascular drug delivery. The invention also relates to a device for a method for preventing or treating neurological diseases, neoplastic diseases, cardiac diseases, vascular diseases, immune diseases, carcinoids, infectious diseases and / or edema.

The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof or a stereoisomer thereof or a mixture of stereoisomers thereof, wherein n is an integer from 0 to 10; R1 is a divalent radical selected from CH2, O, NH and S; and R2 is (C3-C 15 ) alkyl. The present invention also provides a pharmaceutical composition comprising the compound of formula (I), and the use of the compound and the pharmaceutical composition as a medicament, more specifically for the treatment or prevention of tumor diseases such as pancreatic cancer.

Bacterial strains are provided having at least one of a reduced size, a sialic acid coat, inducibly altered surface antigens, and expression of PD-L1 or CTLA-4 antagonists and / or tryptophanase. The bacteria may have improved serum half-life, increased penetration into tumors, increased tumor targeting and increased antitumor activity. The bacteria are useful for delivery of therapeutic agents that treat neoplastic diseases including solid tumors and lymphomas.

The present invention provides a computer implemented method for the prediction of clinical outcomes in patients with cancer or pre-neoplastic conditions through the integration of genomic evolutionary, genomic and clinical. More specifically, the invention provides systems and algorithms that generate prognostic and predictive models based on the combined analysis of molecular features, inferred evolutionary routes, and clinical parameters, enabling patient risk stratification and individualized outcome estimation.

The invention relates to application of an active component in preparation of a medicine for treating tumor diseases. Specifically, it is found for the first time that small-molecule isovaleric acid and the prodrug thereof can inhibit DNA homologous recombination so as to efficiently inhibit tumor growth, and isovaleric acid and the prodrug thereof can be combined with chemotherapeutic drugs for radiotherapy, DNA damage induction or DNA synthesis inhibition to generate a synergistic tumor treatment effect.

Provided herein are methods of determining a treatment for a subject having a neoplastic disease, said method comprising assaying a sample obtained from the subject for (a) SAC activity, (b) ploidy, (c) WGD, (d) APC / C activity, or (e) a combination thereof. In exemplary embodiments, the treatment determined for the subject comprises, consists essentially of, or consists of a KIF18A inhibitor, when the sample is positive for (a) increased SAC activity, (b) high ploidy, (c) WGD, (d) low APC / C activity, (d) or a combination thereof.

The invention discloses a fusion protein and application thereof. The fusion protein comprises an anti-VEGFR2 (vascular endothelial growth factor receptor 2) antibody and an IL-10 monomer; wherein the IL-10 monomer is connected with the anti-VEGFR2 (vascular endothelial growth factor receptor 2) antibody. The fusion protein provided by the invention has the advantages of strong targeting property, small side effect, good drug effect and the like. The fusion protein can be used for preparing pharmaceutical compositions or drugs, and can be used for treating or preventing tumor diseases.

Provided are a human NBS1 protein antigen lactylated at lysine 388, an antibody, a preparation method therefor, and a use thereof, relating to the technical field of biomedicine. A human NBS1 protein antigen peptide lactylated at lysine 388 is provided, and is used to prepare an antibody targeting lactylation at lysine 388 of human NBS1 protein. The antibody targeting lactylation at lysine 388 of human NBS1 protein can detect expression differences among normal cells, tumor cells, and drug-treated tumor cells, thereby helping to study the role of lactylation modification of human NBS1 protein in the occurrence and development of tumor diseases, and providing potential therapeutic targets for clinical diagnosis or treatment of tumor diseases. The antibody targeting lactylation at lysine 388 of human NBS1 protein can be used to detect the lactylation level of human NBS1 protein, and to investigate its relationship with tumor diagnosis and resistance to radiotherapy and chemotherapy, thereby offering broad clinical application prospects in disease diagnosis, treatment, and prognosis evaluation.

The invention relates to a use of combinations of PD-1 inhibitor therapy with certain kinase inhibitors, in particular inhibitors of protein kinases including the SIK-family, CSF1R, ABL / BCR-ABL, SRC, HCK, PDGFR, KIT and / or their mutants, to overcome resistance to PD-1 / PDL1 inhibitor therapy in tumours. A preferred tumour disease treatable in accordance with the invention is a squamous cell lung cancer with a PD-1 inhibitor therapy resistance phenotype.

The present invention relates to a multifunctional cascade reactive nano - scale ultrasound contrast agent and its preparation method and application. The contrast agent (GHB - NPs) has a core of chitosan loaded with Basigin - siRNA and modified with hyaluronidase, and a shell membrane of phospholipid - polyethylene glycol - 2GSH. Perfluoropentane is encapsulated inside the shell membrane, and the particle size is 106 - 295 nm. For the GHB - NPs prepared by the present invention, DSPE - PEG2k - 2GSH on its surface can react with highly expressed γ - GGT on the surface of tumor cells, resulting in electrostatic repulsion to expose hyaluronidase, enabling GHB - NPs to penetrate deep into tumor tissues, and having targeting and high efficiency for the treatment of tumors. And it can be used in combination with UTMD. By inhibiting the β - catenin / c - Myc pathway, it down - regulates glycolysis - related proteins and reduces the production of lactic acid and ATP, which is beneficial to the treatment of tumor diseases. And the present invention has experimentally proved that GHB - NPs + UTMD has an obvious therapeutic effect on melanoma model mice, and can be used for the preparation of anti - tumor drugs to achieve the integration of tumor diagnosis and treatment.

The invention provides a compound as shown in a formula (I) and a racemate, a stereoisomer, a tautomer, a nitrogen oxide, a solvate, a polymorphic substance, a metabolite, an ester, a prodrug or a pharmaceutically acceptable salt thereof, and the compound has a good p53-Y220C mutant activation effect and can be used for treating tumor diseases containing p53-Y220C mutant protein. And preparation of medicaments for such conditions or diseases.

The invention relates to a compound, which has good H3K27me3 demethylation inhibition activity at a cellular level, can effectively inhibit KDM6A / B activity, and can effectively treat inflammation and tumor diseases. The compound is shown in the formula.