59 results about "Solid Neoplasm" patented technology

Provided herein are methods of treating advanced solid tumors in a subject in need thereof, for example, when the subject has advanced head and neck squamous cell carcinoma, colorectal cancer, non-small cell lung cancer, and bladder transitional cell carcinoma. Also provided herein are methods of treating leukemia (e.g., acute myelogenous leukemia) in a subject in need thereof.

The invention discloses an RGD modified crocetin-paclitaxel co-drug-loaded compound liposome and a preparation method and application thereof, and belongs to the technical field of biological medicines.The RGD modified crocetin-paclitaxel co-drug-loaded compound liposome comprises the following components: an RGD modified liposome, paclitaxel and crocetin, wherein the RGD modified lipidosome is used as a drug carrier, paclitaxel and crocetin are delivered to prostate tumor cells in a targeted manner, and the RGD modified lipidosome is prepared through a film dispersion method or a reverse evaporation method. The prostate cancer targeted compound liposome prepared by the invention can increase the uptake of prostate cancer cells, improve the in-vitro cytotoxicity of the prostate cancer cells to the prostate cancer cell line RM-1, inhibit the growth of RM-1 ectopic solid tumors in mice, and do not cause obvious damage to other tissues.

Provided are an antibody-drug conjugate and a preparation method and a use thereof, which has a structure shown in the formula Ab-[M-L-E-D] x, the drug is selected from DNA topoisomerase inhibitors, the prepared antibody-drug conjugate has a relatively good drug-antibody conjugation ratio and has excellent targeted killing effects on solid tumors such as gastric cancer, breast cancer, lung cancer, and urothelium carcinoma.

The invention relates to a method and a system for constructing a traditional Chinese medicine lung cancer prevention and treatment system based on multi-source data fusion, belongs to the technical field of big data, integrates multi-source information such as global evidence-based literature, real world clinical data and expert decision support, constructs an AI-driven three-layer cognitive model, develops a clinical transformation platform, and provides a traditional Chinese medicine lung cancer prevention and treatment system. The method comprises the following steps: screening dominant treatment stages through an intelligent algorithm, optimizing a diagnosis and treatment scheme, establishing a quantitative correlation model of pathogenesis key elements and tumor metabolic activities, further constructing a syndrome-metabolism knowledge graph, forming a syndrome differentiation validity verification mechanism and a prescription linkage database, and finally designing a result transformation engine. New drug research and development and nosocomial preparation conversion are driven through an evidence chain, and evaluation standards are formulated in cooperation with traditional Chinese medicine syndrome improvement and western medicine solid tumor curative effect indexes. According to the method, the bottleneck problems of data splitting, dialectical staticizing and conversion in traditional research are solved, and full-chain innovation from cognitive modeling to clinical landing is achieved.

The invention discloses a conjugate with a targeting effect and a preparation method and application thereof, the conjugate has a structure shown in a formula Ab-[M-L-E-D] x, a drug is selected from a DNA topoisomerase inhibitor, and the prepared antibody drug conjugate has a better drug-antibody coupling ratio and has an excellent targeting killing effect on solid tumors such as gastric cancer, breast cancer, lung cancer and urothelial cancer.

The present disclosure is concerned with compounds and compositions for use in the prevention and treatment of cancer associated with FBOX21 mediated p85a ubiquitination such as, for example, cancer (e.g., sarcoma, a carcinoma, a hematological cancer, a solid tumor, breast cancer, cervical cancer, gastrointestinal cancer, colorectal cancer, brain cancer, skin cancer, prostate cancer, ovarian cancer, thyroid cancer, testicular cancer, pancreatic cancer, liver cancer, endometrial cancer, melanoma, a glioma, leukemia, lymphoma, chronic myeloproliferative disorder, myelodysplastic syndrome, myeloproliferative neoplasm, non-small cell lung carcinoma, renal cancer, lung cancer, colon cancer, cervical cancer, and plasma cell neoplasm (myeloma)). This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

The present disclosure is concerned with compounds and compositions for use in the prevention and treatment of cancer such as, for example, a primary or secondary tumor within a subject's brain, breast, kidney, pancreas, lung, colon, prostate, lymphatic system, liver, ovary, or cervix. Additional examples of cancers for which the disclosed compounds and compositions can be useful include, but are not limited to, sarcomas, carcinomas, hematological cancers, solid tumors, breast cancer, cervical cancer, gastrointestinal cancer, colorectal cancer, brain cancer, skin cancer, prostate cancer, ovarian cancer, thyroid cancer, testicular cancer, pancreatic cancer, liver cancer, endometrial cancer, melanomas, gliomas, leukemia, lymphoma, chronic myeloproliferative disorders, myelodysplastic syndrome, myeloproliferative neoplasm, non-small cell lung carcinomas, and plasma cell neoplasms (myelomas). This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

The invention relates to a compound with biological activity and a preparation method and application thereof, the compound has a structure shown in a formula M '-L-E-D. The compound can be used for preparing an antibody drug conjugate, and the conjugate has a better drug-antibody coupling ratio and has an excellent targeted killing effect on solid tumors such as gastric cancer, breast cancer, lung cancer and urothelial cancer.

GD2 specific chimeric antigen receptor effector cells for the treatment of solid tumors, possibly in combination with an enhancer of a Zeste homolog 2 (EZH2) inhibitor. The invention relates to a GD2-specific chimeric antigen receptor (GD2. CAR) effector cell for use in the treatment of solid tumors, in particular in the treatment of extracranial GD2 + tumors, such as soft tissue sarcoma and osteosarcoma, neuroblastoma, melanoma, lung cancer, bladder cancer and retinoblastoma, and brain tumors. In addition, the present invention also relates to the use of the GD2. CAR genetically modified effector cell in combination with an enhancer of a Zeste homolog 2 (EZH2) inhibitor for the treatment of solid tumors.

The invention discloses a compound with an anti-tumor effect and a preparation method and application thereof, the compound has a structure as shown in a formula M '-L-E-D. The compound can be used for preparing an antibody drug conjugate, and the conjugate has a better drug-antibody coupling ratio and has an excellent targeted killing effect on solid tumors such as gastric cancer, breast cancer, lung cancer and urothelial cancer.

Disclosed is an mIDH1 / NAMPT dual-target inhibitor, which is selected from a compound having a structure as shown in formula (I) or formula (II), or a pharmaceutically acceptable salt, racemate, stereoisomer, prodrug, or solvent compound thereof. The dual-target inhibitor of the present invention can effectively overcome the shortcomings of a single mIDH1 inhibitor and single NAMPT inhibitor having poor efficacy against solid tumors. Said inhibitor can inhibit the malignant proliferation of tumors, has a good therapeutic effect, has low toxicity, and can penetrate the blood-brain barrier, and it is not easy to acquire drug resistance to said inhibitor. Moreover, the inhibitor can be used to prepare a medicament for treating cancer or tumor-related diseases, the cancer or tumor-related diseases comprising multiple myeloma, leukemia, breast cancer, prostate cancer, lung cancer, liver cancer, gastric cancer, bone cancer, brain cancer, head and neck cancer, intestinal cancer, pancreatic cancer, bladder cancer, testicular cancer, ovarian cancer, and endometrial cancer.

This invention discloses an engineered CAR-T cell targeting HIF-1α and its application in tumor immunotherapy. The CAR-T cell expresses a chimeric antigen receptor regulated by the hypoxia-responsive element HRE promoter, with its extracellular domain specifically binding to HIF-1α and its intracellular domain employing the 4-1BB+CD3ζ signaling module. Simultaneously, through immune checkpoint knockout and cytokine / chemokine modification, it achieves hypoxia-dependent activation, anti-exhaustion, high infiltration, and strong killing effects. The CAR-T cells of this invention significantly improve the adaptability to the solid tumor microenvironment and therapeutic efficacy, reduce off-target toxicity, and can be used to prepare drugs for treating malignant tumors such as lung cancer, liver cancer, pancreatic cancer, colorectal cancer, and glioblastoma, possessing significant clinical translational value.

The present disclosure provides a group of aromatic (e.g., pyridinyl, pyrimidinyl, pyrazinyl, or phenyl) diamidine analogs and pharmaceutically acceptable salts that are useful for treating a proliferative disease. The proliferative disease may include solid cancer or blood cancer. Compositions, methods of synthesizing the same and methods for treating various cancer using the analogs are disclosed herein. The present disclosure also provides pharmaceutical formulations comprising at least one of the compounds with a pharmaceutically acceptable carrier, diluent or excipient therefor.

This invention discloses a class of 2-(2-(quinolin-4-yloxy)ethyl)pyridazine-3(2H)-one compounds, their preparation methods, and applications. The structure of these compounds is shown in general formula (I). This invention also discloses that the above compounds have a significant inhibitory effect on interleukin-1 receptor-associated kinase 1 (IRAK1). These compounds can inhibit the proliferation of various tumor cells, including liver cancer, lung cancer, pancreatic cancer, gastric cancer, kidney cancer, colon cancer, esophageal cancer, glioblastoma, leukemia, multiple myeloma, and other solid tumors and hematological malignancies. This invention provides a new option for tumor treatment.

A fused-ring compound, a preparation method therefor, and use thereof. The fused-ring compound has a structure represented by the formula D-E-L-M' and can be used for preparing an antibody-drug conjugate. The prepared antibody-drug conjugate has a relatively good drug-to-antibody conjugation ratio and has excellent targeted killing effects on solid tumors such as gastric cancer, breast cancer, lung cancer, and urothelial carcinoma.

Disclosed in the present invention are a PIM kinase inhibitor as shown in general formula II, a pharmaceutical composition thereof, a preparation method therefor and the use thereof in the preparation of a drug for preventing and / or treating indications related to a PIM signaling pathway. The compound of the present invention is an ideal PIM kinase inhibitor with a high activity, which can be used for treating and / or preventing diseases including autoimmune diseases and tumors, e.g., inflammatory bowel disease, hematologic malignancies such as acute myeloid leukemia, myelofibrosis and chronic lymphocytic leukemia, and solid tumors such as gastric cancer and prostate cancer.

The invention discloses a fused ring compound as well as a preparation method and application thereof. The fused ring compound has an excellent treatment effect on solid tumors such as gastric cancer, breast cancer, lung cancer or urothelial cancer or malignant tumors of a blood system.

The present application relates to the technical field of biological medicine, and particularly relates to application of fullerenol in preparation of tumor prevention or treatment drugs for inducing trained immunity. The present application finds that fullerenol can induce formation of trained immunity, activate immune reprogramming of bone marrow hematopoietic stem cells, produce long-term pro-inflammatory phenotype, form persistent immune memory, and further enhance functions of innate immune cells. It is verified by experiments that fullerenol can significantly inhibit tumor growth in an animal model without obvious systemic toxicity; epigenetic remodeling of bone marrow hematopoietic stem cells can be sustained for several weeks to several months, and has long-acting anti-recurrence potential. In addition, trained immunity induced by fullerenol can be used for immune regulation of various solid tumors, and fullerenol is simple in synthesis, can be produced on a large scale, has excellent biocompatibility and stability. Therefore, the present application has wide application prospect.

Several embodiments of the methods and compositions disclosed herein relate to immune cells engineered to express cytotoxic chimeric receptors and various dosing regimens for administering such cells. In several embodiments, the immune cell expresses a chimeric receptor that targets a ligand of NKG2D on a tumor cell. In several embodiments, the cancer is a leukemia, e.g., acute myelogenous leukemia (e.g., recurrent / refractory acute myelogenous leukemia) or myelodysplastic syndrome. In several embodiments, the tumor is a solid tumor, such as breast cancer, cervical cancer, colorectal cancer, gastric cancer, head and neck cancer, hepatocellular cancer, lung cancer, melanoma, intrahepatic cholangiocarcinoma, or other liver tumor, such as a secondary metastatic tumor from colorectal cancer. In several embodiments, the immune cells are administered in combination with a therapeutic agent, such as an additional anti-cancer agent.

Provided is a means to predict the anticancer therapeutic efficacy of 1-((5-(1R)-1-fluoroethyl)-1,3,4-oxadiazol-yl)methyl)-6-(4-methoxypyrrolo[2,1-f][1,2,4]triazin-5-yl)-2-methyl-1H-imidazo[4,5-b]pyridine or a derivative thereof in solid cancer and thereby specifying a subject who will be the most benefitted from treatment with the compound and treatment with the compound in combination with another drug and / or another therapy. As a biomarker for predicting therapeutic response to the compound, a genetic character predicted to impart sensitivity to CLK inhibition is used.

The invention provides a conjugate with a targeting effect and a preparation method and application thereof, the conjugate has a structure as shown in a formula Ab-[M-L-E-D] x, a drug is selected from a DNA topoisomerase inhibitor, and the prepared antibody drug conjugate has a better drug-antibody coupling ratio and can be used for preparing a drug-antibody conjugate. The compound has an excellent targeted killing effect on solid tumors such as gastric cancer, breast cancer, lung cancer and urothelial carcinoma.

The invention provides a macrocyclic drug conjugate as well as a preparation method and application thereof. The macrocyclic drug conjugate has a structure as shown in a formula Ab-[M-L-E-D] x, the macrocyclic drug conjugate has an excellent targeted killing effect on solid tumors such as gastric cancer, breast cancer, lung cancer and urothelial cancer.

The invention discloses an engineered exosome for immunotherapy of lung cancer and a preparation method of the engineered exosome, particularly relates to a method for delivering synNotch-CAR mRNA (messenger Ribonucleic Acid) into a body through the exosome for in-situ modification of macrophages, and provides the engineered exosome capable of immunotherapy of lung cancer. The exosome derived from the M1 macrophages is used for engineering transformation, and targeted delivery of drugs to the macrophages is realized. The synNotch-CAR-TAMs in-vivo transformation strategy provided by the invention has high controllability, tissue specificity and durability, is expected to be expanded to various solid tumor types in the future, and provides a precise treatment scheme with higher clinical transformation value for cancer patients. The exosome is subjected to a series of engineering modification, so that the treatment effect of the exosome on lung cancer is improved.

To provide safe and effective, non-toxic pentamidine analogs that exhibit increased organ targeting that may allow for oncological clinical development designed for specific types of cancer.SOLUTION: The present disclosure provides a group of aromatic (e.g., pyridinyl, pyrimidinyl, pyrazinyl, or phenyl) diamidine analogs and pharmaceutically acceptable salts that are useful for treating a proliferative disease. The proliferative disease may include solid cancer or blood cancer. Compositions, methods of synthesizing the same and methods for treating various cancer using the analogs are disclosed herein. The present disclosure also provides pharmaceutical formulations comprising at least one of the compounds with a pharmaceutically acceptable carrier, diluent or excipient therefor.SELECTED DRAWING: Figure 1

The invention provides a macrocyclic drug conjugate as well as a preparation method and application thereof. The macrocyclic drug conjugate has a structure as shown in a formula Ab-[M-L-E-D] x. The antibody drug conjugate has an excellent targeted killing effect on solid tumors such as gastric cancer, breast cancer, lung cancer and urothelial cancer.

The invention relates to application of HDAC (histone deacetylase) inhibitor and Cathepsin B inhibitor combined medicine in lung cancer treatment, and belongs to the technical field of biological medicine. Research finds that histone deacetylase inhibitors (HDAC inhibitors, HDACIs) can promote invasion and migration of tumor cells by inducing epithelial-mesenchymal transition while inhibiting tumor growth, and side effects are generated. Therefore, in order to inhibit the side effect and enable the HDAC inhibitor to effectively exert the curative effect clinically, the invention provides a novel medicine combination mode, the HDAC inhibitor and the Cathepsin B inhibitor are combined for use, so that the antitumor activity of the HDAC inhibitor is retained, the tumor invasion and migration capability induced by the HDAC inhibitor is effectively inhibited, and the curative effect of the HDAC inhibitor is effectively exerted clinically. A new strategy is provided for precise treatment of solid tumors, and the method is verified in treatment of lung cancer.

The present disclosure relates to compounds, pharmaceutical compositions, and methods of using the compounds and compositions to restore activity of von Hippel Lindau tumor suppressor protein (pVHL). Such compounds and compositions can be useful in, for example, the treatment of cancer (e.g.. a sarcoma, a carcinoma, a head-and-neck cancer, hematological cancer, a solid tumor, breast cancer, cervical cancer, gastrointestinal cancer, colorectal cancer, brain cancer, skin cancer, prostate cancer, ovarian cancer, thyroid cancer, testicular cancer, pancreatic cancer, liver cancer, endometrial cancer, melanoma, a glioma, leukemia, lymphoma, chronic myeloproliferative disorder, myelodysplastic syndrome, myeloproliferative neoplasm, non-small cell lung carcinoma, small cell lung carcinoma, renal cancer, lung cancer, colon cancer, cervical cancer, and plasma cell neoplasm (myeloma)) and von Hippel-Lindau disease (VHLD). This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

Provided herein are small molecule inhibitors of NSD1, NSD2 and / or NSD3 activity, and methods of use thereof for the treatment of disease, including leukemia, breast cancer, osteosarcoma, lung and prostate cancers and other solid tumors as well as other diseases dependent on the activity of NSD1, NSD2 and / or NSD3.

The present invention relates to therapeutic treatment of cancer, particularly solid and hematological tumors, with combination therapy using Compound IA and a topoisomerase I inhibitor.

Disclosed herein are crystalline polymorphs of indotecan (LMP400) that can be used in the treatment of cancers associated with dysregulation of Topl and / or MYC activity, such as, for example, a sarcoma, (e.g., Ewing's sarcoma), a carcinoma, a hematological cancer, a solid tumor, breast cancer, cervical cancer, gastrointestinal cancer, colorectal cancer, brain cancer, skin cancer, prostate cancer, ovarian cancer, non-small cell lung carcinoma, thyroid cancer, testicular cancer, pancreatic cancer, liver cancer, endometrial cancer, a melanoma, a. glioma, leukemia, a lymphoma, chronic myeloproliferative disorder, myelodysplastic syndrome, myeloproliferative neoplasm, and plasma cell neoplasm (myeloma). This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.