488results about "Boron compound active ingredients" patented technology

Provided are a c-Myc protein inhibitor, and a preparation method therefor and use thereof. The c-Myc protein inhibitor selectively inhibits c-Myc protein. Therefore, the inhibitor can be used for prevention and treatment of diseases related to c-Myc protein disorders, such as cancers, cardiovascular and cerebrovascular diseases, diseases related to virus infection.

Disclosed are methods of treating a subject having high-risk multiple myeloma, methods of achieving negative minimal residual disease status in a subject having multiple myeloma, and methods of predicting a likelihood of, or decreasing a risk of, relapse and / or disease progression in a subject having multiple myeloma.

The tumor stroma, which accounts for a large portion of the tumor mass, is an attractive target for the delivery of diagnostic and therapeutic compounds. Here, we focus specifically on a subpopulation of stromal cells known as cancer-associated fibroblasts, which are present in over 90% of epithelial cancers, including pancreatic, colon, and breast cancers. Cancer-associated fibroblasts are characterized by high expression of FAPs, which are undetectable in adult normal tissues but are associated with poor prognosis in cancer patients. The present invention provides small molecule radiopharmaceuticals and imaging agents based on FAP-specific inhibitors.

The invention discloses application of 2-aminoethoxy diphenyl borate (2-APB) in preparation of a medicine for improving endometrial receptivity and treating diseases related to the endometrial receptivity, and belongs to the technical field of biological medicine. A large number of experiments prove that 2-APB specifically activates a TRPM6 channel, enhances calcium ion influx and activates a calcium-dependent CaM-CaMKII-Ecadherin signal axis, so that expression of receptivity markers (such as E-cadherin and ICAM-1) is up-regulated, and endometrial receptivity is improved. The problems of poor targeting property and high toxicity of the traditional calcium ion carrier are solved, and a safe and effective treatment strategy is provided for a patient suffering from repeated implantation failure (RIF).

The present invention relates to piperidine-containing heterocyclic compounds of formula (I), which inhibit / modulate complement factor B, thereby treating conditions and diseases associated with activation of the alternative complement pathway. [Formula 1] TIFF2023538844000270.tif33169

The present application relates to a substituted heterocyclic derivative, a preparation method therefor, and medicinal use of a pharmaceutical composition comprising the derivative or a deuterated derivative. Specifically, the present application relates to a substituted heterocyclic derivative represented by general formula (I), (I-A), or (I-B), a preparation method therefor, a pharmaceutically acceptable salt thereof, and use thereof as a voltage-gated channel Nav 1.8 antagonist in the prevention and / or treatment of a Nav 1.8-related disease, particularly in the field of pain. The definition of each substituent in general formula (I), (I-A), or (I-B) is the same as that in the specification.

Disclosed are methods of treating a subject having high-risk multiple myeloma, methods of achieving negative minimal residual disease status in a subject having multiple myeloma, and methods of predicting a likelihood of, or decreasing a risk of, relapse and / or disease progression in a subject having multiple myeloma.

Disclosed herein is a compound that is (R)-(2-(3-((((2-ethylbutanoyl)oxy)methoxy)carbonyl)-2-hydroxyphenyl)-1-propionamidoethyl)boronic acid citrate coordination complex, or a pharmaceutically acceptable salt or solvate thereof. Also disclosed herein are methods of treating a bacterial with a compound that is (R)-(2-(3-((((2-ethylbutanoyl)oxy)methoxy)carbonyl)-2-hydroxyphenyl)-1-propionamidoethyl)boronic acid citrate coordination complex, or a pharmaceutically acceptable salt or solvate thereof in combination with ceftibuten.

The invention relates to a substituted heterocyclic derivative, a preparation method thereof and application of a pharmaceutical composition containing the derivative or a deuterated derivative in medicine. Specifically, the invention relates to substituted heterocyclic derivatives as shown in general formulas (I), (I-A) and (I-B), a preparation method and medicinal salts thereof, and application of the substituted heterocyclic derivatives as voltage-gated channel Nav 1.8 antagonists in prevention and / or treatment of Nav 1.8 related diseases, especially in the field of pain. Wherein the definitions of substituent groups in the general formulas (I), (I-A) and (I-B) are the same as the definitions in the specification.

A method for treating cancer comprises the combined use of a therapeutically effective amount of elzovtinib or an elzovtinib analog, a derivative thereof, or a pharmaceutically acceptable salt, and a therapeutically effective amount of bortezomib, ibrutinib, or an analog, derivative, or pharmaceutically acceptable salt thereof. The composition and kit are included herein. The cancer may be refractory to bortezomib and / or ibrutinib.

The invention discloses a preparation method and application of bioactive lipid and lipid nanoparticles thereof. The bioactive lipid molecule is formed by bonding long-chain fatty acid (LCFA) with different chain lengths with two functional small molecules, namely phenylboronic acid pinacol ester (PBAP) and Tempol (Tpl) respectively, so that two types of lipid molecules, namely PBAP-LCFA and Tpl-LCFA, with anti-inflammatory activity are constructed. The lipids are used as functional components, and the anti-inflammatory lipid nanoparticles with good biocompatibility, including PLP, TLP and TPLP, can be prepared through a film dispersion method. The lipidoid and the lipid nanoparticles are simple and convenient in preparation process, controllable in structure and function and easy for large-scale production, and have treatment potential in various acute and chronic inflammatory diseases. In an animal model, the lipid nanoparticles have remarkable curative effects on acute peritonitis, acute lung injury, acute hepatic failure, asthma and other diseases. Besides, the lipid bilayer structure of the TPLP can efficiently entrap hydrophilic / hydrophobic drugs, can synergistically deliver treatment drugs while exerting the anti-inflammatory effect of the TPLP, and realizes a synergistic combined treatment strategy for chronic lung inflammation and other diseases.

The present invention describes novel boron containing pyrazole compounds, or their pharmaceutically acceptable salts, pharmaceutical compositions containing them, and their medical uses. The compounds of the invention have activity as Janus kinase (JAK) inhibitors and are useful in the in the treatment or control of inflammation, auto-immune diseases, cancer, and other disorders and indications where modulation of JAK would be desirable. Also described are methods of treating inflammation, auto-immune diseases, cancer, and other conditions that are susceptible to the inhibition of a Janus kinase by administering a compound herein described.

Disclosed are compounds according to Formula (1) and Formula (2) which inhibit LONP1, and pharmaceutical compositions comprising compounds of the disclosure. Compounds and pharmaceutical compositions of the disclosure may be useful for the treatment of diseases and disorders associated with LONP1, including oncologic diseases and disorders, such as cancer, and diseases and disorders related to mitochondrial dysfunction, such as neurodegenerative disorders, metabolic disorders, and diseases associated with the aging process. The disclosure also relates to methods of using such compounds and compositions for the treatment of such diseases and disorders.

A pyridine amide compound-containing composition and a pharmaceutical composition, a preparation method therefor and a use thereof. The composition comprises an active ingredient and at least one matrix material, wherein the active ingredient is a compound represented by formula I or a pharmaceutically acceptable salt, a stereoisomer, a solvate, an isotopically labeled compound, a polymorph, a metabolite or a prodrug thereof. The composition has a high drug loading capacity, improves drug solubility, and has good stability. The in vivo bioavailability of the composition can reach the same level of bioavailability as that of a clear drug solution.

The present application provides a compound represented by Formula 0, a pharmaceutical composition containing the same, and a method for synthesizing and using the same. The compound of the present application significantly suppresses the cellular integrated stress response (ISR), activates eIF2B activity, and normalizes intracellular protein synthesis, providing more potential drugs for integrated stress response (ISR) pathway-mediated diseases or conditions, eIF2B-related diseases, and / or diseases associated with modulation of eIF2B activity or levels, the eIF2 pathway, or the ISR pathway activity or levels. TIFF2025539152000388.tif40108

The present disclosure provides methods of treating diseases or disorders responsive to inhibiting or blocking B-cell maturation antigen (BMCA) by administering one or more BCMA antagonists.

The present invention relates to a combination of a specific binding molecule that binds to human ANXA1 and a second active agent for use in the treatment of cancer. The second active agent includes thymidylate synthase inhibitors, nucleobase analogs, checkpoint inhibitors, proteasome inhibitors, taxanes, platinum-based chemotherapy agents, and nucleoside analogs. Suitable cancers for treatment include pancreatic cancer, colon cancer, breast cancer, lung cancer, myeloma, and mantle cell lymphoma. Also provided are related kits, products, and uses.

The present application relates to a compound represented by formula 1, a pharmaceutically acceptable salt thereof or an isomer thereof, and a pharmaceutical composition comprising the same as an active ingredient and for treating or preventing a proteasome-mediated disease.

The present invention relates to an heparanase-binding and heparanase-neutralizing monoclonal antibody (IgG-1 mAb A54), including its epitope (HBD-II) and mode of interaction with heparanase, pharmaceutical composition comprising same, and uses thereof e.g. for inhibiting or treating a disease or disorder associated with heparanase activity, including but not limited to cancer, inflammation, viral infection, diabetes and related complications. The present invention further provides combinatorial cancer therapies, comprising the heparanase-neutralizing mAb and an additional anti-cancer treatment such as chemotherapy or radiation.

Boronic acid and ester substituted estrogen receptor beta selective phenyl-2H-indazole compounds and hydroxy derivatives have immunomodulatory properties and increase oligodendrocyte survival, differentiation, and remyelination. The compounds, compositions, and kits are useful in the treatment of multiple sclerosis and endometriosis.

A new class of boronic acid compounds. Specifically disclosed are compounds represented by Formula (II) or (II′), pharmaceutically acceptable salts thereof or stereoisomers thereof, and the application thereof in the preparation of a medicament for treating diseases associated with bacterial infection.

The present invention provides an organic boron compound of formula I or a salt thereof, a pharmaceutical composition thereof, and uses of the organic boron compound and the pharmaceutical composition in the treatment of non-tuberculous mycobacterial infections. [Chemical 1] TIFF2025520237000027.tif49159

Compounds, compositions, and methods for inhibiting ENPP1 are provided. Embodiments of the subject methods include contacting a sample with an ENPP1 inhibitor compound to inhibit the cGAMP hydrolysis activity of ENPP1. In some cases, the ENPP1 inhibitor compound is cell-impermeable. The ENPP1 inhibitor compound can act extracellularly and block the degradation of cGAMP. Similarly, pharmaceutical compositions and methods for treating cancer are provided. Embodiments of the method include administering a therapeutically effective amount of an ENPP1 inhibitor to a subject to treat the cancer in the subject. In certain cases, the cancer is a solid tumor cancer. Similarly, methods are provided in which radiation therapy is administered to a subject in conjunction with administering an ENPP1 inhibitor to the subject. In the subject methods, radiation therapy can be administered at a dosage and / or frequency effective to reduce radiation damage to the subject while still eliciting an immune response.

The present invention relates to a heparanase-binding and heparanase-neutralizing monoclonal antibody (IgG-1 mAb A54), including its epitope (HBD-II) and mode of interaction with heparanase, to pharmaceutical compositions comprising same, and to its use for inhibiting or treating diseases or disorders associated with heparanase activity, including, but not limited to, cancer, inflammation, viral infection, diabetes, and related complications. The present invention further provides combination cancer treatments comprising a heparanase-neutralizing mAb and an additional anti-cancer treatment, such as chemotherapy or radiation.

Use of an anti-HER2 antibody-drug conjugate in the preparation of a drug for treating HER2 low-expression breast cancer. The structure of the antibody-drug conjugate is represented by formula (I).

This invention relates to, among other items, treating non-tuberculosis Mycobacteria-associated disease in a human with epetraborole.