16 results about "Fibrosarcoma" patented technology

The invention discloses a PET (positron emission tomography) imaging agent, a precursor and a probe for targeting an EphA2 receptor as well as a preparation method and application of the PET imaging agent, the precursor and the probe, and a radioactive probe which is formed by labeling a chelating agent (such as DOTA and NOTA) and a radionuclide (such as 68Ga) by taking bicyclic peptide as a targeting group is specifically combined with the EphA2 receptor highly expressed on the surface of a tumor cell. According to the invention, a conformation limitation strategy is adopted for transforming the peptide probe targeting EphA2 for the first time, the bicyclic peptide radioactive probe with excellent targeting performance and in-vivo imaging effect is obtained, the tumor uptake value is high, and tumor and non-tumor imaging is clear; and successful imaging in a fibrosarcoma model. According to the EphA2 receptor-targeted PET imaging agent provided by the invention, the precursor, namely the probe, has the advantages of simplicity in preparation, good targeting property, excellent imaging effect and the like, can be used for PET imaging diagnosis, prognosis evaluation and targeted therapy guidance of EphA2 positive tumors, and has good clinical value.

To provide compounds that find utility as modulators of RapidlyAcceleratedFibrosarcoma (RAF, such as c-RAF, A-RAF and / or B-RAF; target proteins).SOLUTION: The present invention is directed to bifunctional compounds that contain a von Hippel-Lindau, cereblon, Inhibitorsof Apoptosis Proteins, or mousedouble-RAF ligand that binds to the respective E3 ubiquitin ligase at one end and a moiety that binds to the target proteins RAF at the other end, such that the target proteins are placed in proximity to the ubiquitin ligase to effect degradation (and minutehomolog2) of the target proteins. The present disclosure presents a wide range of pharmacological activities related to degradation / inhibition of target proteins.SELECTED DRAWING: None

The application provides a lipid peroxidation detection probe based on a perylene imide-triphenyl phosphine structure and a preparation method and application thereof, and belongs to the technical field of design and synthesis of lipid peroxidation fluorescent probes and visual imaging technology.The structural formula of the lipid peroxidation detection probe is: the lipid peroxidation detection probe is based on structure optimization of a perylene imide-triphenyl phosphine compound Liperfluo, and the stability of the lipid peroxidation detection probe is greatly improved.The lipid peroxidation detection probe has good sensitivity and selectivity to the iron death marker lipid hydroperoxide, and the pretreatment of a test sample is simple.The lipid peroxidation detection probe can be used for detecting endogenous and exogenous iron death in fibrosarcoma cells, and can be used for studying specific regulation mechanisms and biological functions of iron death related metabolic diseases.The lipid peroxidation detection probe is a solid powder, is convenient to store and use, and has a simple synthesis method, high yield, low cost and good market application prospect.

The present invention relates to a heterocyclic compound, a preparation method therefor and a pharmaceutical use thereof. Specifically, the present invention relates to a compound as shown in general formula (I), a preparation method therefor, a pharmaceutical composition comprising the compound, and a use thereof as a PRMT5 inhibitor. The compound and the pharmaceutical composition comprising the compound can be used for treating and / or preventing PRMT5 activity-related diseases, such as non-small cell lung cancer, tumor of mesothelial tissue, neurofibrosarcoma, pancreatic cancer, and solid tumors. The definition of each group in general formula (I) is the same as that in the description.

The invention discloses a transmembrane protein 16F and application of a gene coded by the transmembrane protein 16F as a target spot in preparation of a medicine for regulating and controlling tumor ferroptosis. The tumor is any one of lymphoma, melanoma, colon cancer, cervical cancer, fibrosarcoma and ovarian epithelial cancer. The invention finds that TMEM16F is a ferroptosis inhibiting factor which does not change a cell lipid peroxidation process, and shows that the spatial distribution of oxPLs can regulate ferroptosis. In the ferroptosis process, the TMEM16F-mediated phospholipid overturning process is activated, and the effect of regulating and controlling phospholipid redistribution is achieved. In addition, the combination of TMEM16F defect and anti-PD-1 treatment shows a synergistic anti-tumor effect, and initiates a strong tumor immunological rejection reaction. The ivermectin has the biological activity of inhibiting the overturning function of TMEM16F phospholipid, and the inhibition effect of the ivermectin on TMEM16F effectively enhances the reactivity of anti-PD-1 treatment.

This invention relates to a cyclic polypeptide molecular probe targeting neurocilia protein-1 (NRP-1), its preparation method, and its applications. The cyclic polypeptide molecular probe comprises the structure shown in Formula I or Formula II, where R1 is the structure shown in Formula III or Formula IV; and R2 is a radiolabeled nuclide or a radiolabeled nuclide including a bifunctional chelating group. The technical solution of this invention exhibits excellent targeting specificity and high sensitivity for NRP-1 protein, enabling visualization of NRP-1-highly expressing tumors (such as fibrosarcoma, lung cancer, pancreatic cancer, or breast cancer) and NRP-1-positive lesions (such as metabolic diseases, sclerotic lesions, or autoimmune diseases) on positron emission tomography (PET). It shows great promise in the early diagnosis of NRP-1-highly expressing malignant tumors and in guiding clinical NRP-1 monoclonal antibody treatment regimens.

The present disclosure relates to bifunctional compounds, which find utility as modulators of Rapidly Accelerated Fibrosarcoma (RAF, such as c-RAF, A-RAF and / or B-RAF; the target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a Von Hippel-Lindau, cereblon, Inhibitors of Apotosis Proteins or mouse double-minute homolog 2 ligand which binds to the respective E3 ubiquitin ligase and on the other end a moiety which binds the target protein RAF, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation / inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein, or the constitutive activation of the target protein, are treated or prevented with compounds and compositions of the present disclosure.

The present disclosure relates to a novel benzotriazine dioxide and a pharmaceutical composition thereof. The benzotriazine dioxide has a structure of formula (I). The benzotriazine dioxide can be used alone or in combination with other drugs to treat or alleviate benign and malignant tumor disorders in the liver, bile duct, pancreas, stomach, esophagus, kidney, colon, lung, brain (glioma), malignant glioma, breast, ovary, cervical, head and neck, skin, melanoma, prostate, fibrosarcoma, sarcoma, thyroid gland, etc.

The present invention provides a compound of Formula I, a salt thereof, or a solvate thereof, as described herein, the composition is used for treating MYC positive cancers including lung cancer, leukemia, breast cancer, myeloproliferative diseases, colorectal cancer, medulloblastoma, kidney cancer, hepatocellular cancer, melanoma, ovarian cancer, prostate cancer, esophageal adenocarcinoma, liposarcoma, esophageal squamous carcinoma, gastrointestinal stromal tumor, glioma, mucus fibrosarcoma, smooth muscle sarcoma, neuroblastoma, synovial sarcoma, mesothelioma, and the like. Gastric cancer, thyroid cancer, lymphoma, osteosarcoma, rhabdomyosarcoma, fibrosarcoma, epithelial cancer and neurological cancer.

The present invention belongs to the technical fields of lipid peroxidation fluorescent probe design synthesis and visualization imaging. Provided are a lipid peroxidation detection probe based on a perylene imide-triphenylphosphine structure, a preparation method therefor and the use thereof. The structural formula of the lipid peroxidation detection probe is shown as formula (I). The lipid peroxidation detection probe is based on structural optimization of perylene imide-triphenylphosphine compound Liperfluo, thereby greatly improving the stability thereof. The present invention has good sensitivity and selectivity to a ferroptosis marker lipid hydroperoxides, involves simple pretreatment of test samples, can be used for detecting ferroptosis endogenously and exogenously caused by fibrosarcoma cells, and can be used for studying specific regulation mechanisms and biological functions for ferroptosis-related metabolic diseases. The detection probe is a solid powder, is easy to store and use, involves a simple synthesis method, has a high yield and a low cost, and has good prospects in market application.

The present application relates to heterocyclic compounds, and preparation methods and medical uses thereof. Specifically, the present application relates to compounds represented by general formula (I), preparation methods thereof, and pharmaceutical compositions containing the compounds, and uses thereof as PRMT5 inhibitors. The compounds and the pharmaceutical compositions containing the compounds can be used for treating and / or preventing diseases related to PRMT5 activity, such as non-small cell lung cancer, mesothelial tissue tumor, neurofibrosarcoma, pancreatic cancer, and solid tumor, etc. Wherein the definitions of the groups in general formula (I) are the same as the definitions in the specification.

Provided herein are compounds, pharmaceutical compositions comprising the compounds, methods of preparing the compounds, and methods of using the compounds and compositions, for example, in treating inflammatory dermatitis diseases, proliferative diseases, and cancer, including, but not limited to breast cancer, ovarian cancer, colon cancer, prostate cancer, melanoma, and fibrosarcoma.

The invention discloses application of Bafetinib as an NLRP3 inflammasome activator and in preparation of a medicine for preventing and treating fibrosarcoma, and belongs to the technical field of biological medicine. The application of the Bafetinib in preparation of the medicine for preventing and treating fibrosarcoma further comprises combination of the Bafetinib and a PD-1 antibody. The application has the beneficial effect that the invention provides a new application of the Bafetinib in treating fibrosarcoma and activating NLRP3 inflammasomes. By establishing a fibrosarcoma subcutaneous tumor disease model, it is found that Bafetinib has very good effects of promoting NLRP3 inflammasome activation, enhancing lymphocyte infiltration and treating fibrosarcoma in vivo. The effect of the Bafetinib on activation of the NLRP3 inflammasome is clarified to be a key direction for promoting anti-fibrosarcoma immunotherapy, and the Bafetinib has important clinical significance. A new medical effect is explored, and a new application field is opened up.

The application discloses siRNA for inhibiting expression of a CREPT gene, wherein a positive sense chain nucleotide sequence of the siRNA is shown in any one of SEQ ID No. 1-3. The siRNA can inhibit the CREPT. Some siRNAs can inhibit growth of mouse colon cancer cells and growth of NIH3T3 fibrosarcoma cells. The liposome delivery drug of the si-CREPT through a delivery system can treat mouse liver cancer, and significantly reduce tumor load of the mouse liver cancer.

The invention discloses a marker for prognosis layering of mucus fibrosarcoma and application of the marker, and belongs to the technical field of biological medicine. The MDM2 protein or the number 12 chromosome polysome has obvious correlation with the prognostic stratification of the mucus fibrosarcoma, the MDM2 protein or the number 12 chromosome polysome is used as the marker for the prognostic stratification of the mucus fibrosarcoma, and a reagent for preparing and detecting the two markers can be applied to judging the prognostic stratification of the mucus fibrosarcoma. The marker disclosed by the invention is abnormal in protein level or specific chromosome structure, and compared with a gene-level marker, the marker disclosed by the invention is easier to carry out standardized detection and interpretation through conventional technologies such as immunohistochemistry and the like, and is suitable for developing related prognosis detection reagents.

This invention relates to tricyclic heterocyclic compounds, their preparation methods, and pharmaceutical uses. In particular, this invention relates to compounds of general formula (I), their preparation methods, pharmaceutical compositions containing such compounds, and their use as PRMT5 inhibitors. These compounds and pharmaceutical compositions containing such compounds can be used to treat and / or prevent diseases associated with PRMT5 activity, such as non-small cell lung cancer, mesothelial carcinoma, neurofibrosarcoma, pancreatic cancer, and solid tumors. The definitions of the groups in general formula (I) are the same as those in the specification.