699results about "Boron compound active ingredients" patented technology

Disclosed are methods of performing iterative N-C and C-C bond formation, methods of making compounds which enable iterative N-C and C-C bond formation, and compounds which enable iterative N-C and C-C bond formation.

The present invention relates to a boron-containing drug and a method for preparing the same, which can be obtained by polymerization of dopamine or its derivatives with a boron-containing compound. The boron-containing drug has a high tumor concentration of 70 μg / g, significantly improves the tumor / blood concentration ratio of boron, reaching 70:1, and is rapidly removed from the blood and normal organs, significantly reducing the drug dosage and side effects, and significantly improving the tumor treatment effect.

Provided are an anti-CLDN18.2 antibody or an antigen-binding fragment thereof, a derivative comprising said antibody or antigen-binding fragment thereof, a pharmaceutical composition, and related use of said antibody or antigen-binding fragment thereof for treating, diagnosing and detecting cancers.

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.

The present invention relates to the pharmaceutical field, and provides a boric acid β-lactamase inhibitor or a use thereof. The boric acid β-lactamase inhibitor is a compound shown in formula (I), or an optical isomer or a pharmaceutically acceptable salt thereof: formula (I). The ultra-broad-spectrum boric acid β-lactamase inhibitor of the present invention has an inhibition effect on A, B, C, and D enzymes, and carbapenem drug-resistant bacteria such as Klebsiella pneumoniae, Escherichia coli, Enterobacter cloacae, Acinetobacter baumannii, and Pseudomonas aeruginosa.

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 invention discloses supramolecular hydrogel and microneedle patch for treating oral mucositis and a preparation method and application thereof, and belongs to the technical field of biological medicine, and the supramolecular hydrogel for treating oral mucositis comprises the following raw materials: guanosine, a potassium hydroxide solution containing metal ion soluble salt and phenylboronic acid lactone drugs. The raw material of the microneedle patch further comprises a water-soluble backing solution. The supramolecular hydrogel or microneedle patch for treating oral mucositis integrates antibacterial, anti-inflammatory, antioxidant and angiogenesis promoting functions, and has a remarkable effect of promoting healing of chemotherapeutic oral mucosal lesion.

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.

Methods and corresponding uses are provided for treating disease in patients involving the use of sodium trans-[tetrachloridobis(1H-indazole)ruthenate(III)] to improve drug resistance, including resistance to proteasome inhibitors and immunomodulatory imide drugs. The disease may be, for example, relapsed / refractory multiple myeloma.

The present invention relates to antibodies, such as full-length antibodies or antigen-binding fragments thereof, that specifically bind to BCMA (B-cell maturation antigen) and CD3 (cluster of differentiation 3). The present invention also relates to antibody conjugates (e.g., antigen-drug-conjugates) comprising BCMA antibodies, compositions comprising BCMA antibodies, and methods of using BCMA antibodies and their conjugates to treat disease conditions associated with cells expressing BCMA (e.g., cancer or autoimmune diseases). The present invention further relates to heteromultimeric antibodies that specifically bind to CD3 and tumor cell antigens (e.g., bispecific antibodies that specifically bind to CD3 and BCMA). Compositions comprising such heteromultimeric antibodies, methods for preparing and purifying such heterodimeric antibodies, and their use in diagnosis and treatment are also provided.

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.

The invention relates to the technical field of medicines, and particularly discloses an application of 4-chloro-2, 5-dimethoxy-N-[(2-methoxyphenyl) methyl] phenylethylamine (25C-NBOMe) in preparation of a medicine for inhibiting addiction, and a preparation method of the 4-chloro-2, 5-dimethoxy-N-[(2-methoxyphenyl) methyl] phenylethylamine (25C-NBOMe). As a selective 5-HT2A receptor agonist, the compound can regulate a neural circuit from the prefrontal cortex to the marginal system and indirectly influence dopamine release, so that active drug foraging, relapse and preference behaviors of addicted individuals are inhibited. The invention further covers pharmaceutical salt forms and structural analogues of the compound and application of the compound in pharmaceutical compositions, and administration can be achieved through multiple dosage forms such as sustained-release implants and nasal spray. Compared with the existing drug for treating addiction, the invention has the advantages of independence, definite target spot, obvious curative effect, high safety and the like, is suitable for intervention of various addiction substances, and provides a new strategy for prevention and treatment of addiction behaviors.

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.

Disclosed herein are crystalline forms of ((2-Ethylbutanoyl)oxy)methyl (R)-2-hydroxy-3-propionamido-3,4-dihydro-2H-benzo[e][1,2]oxaborinine-8-carboxylate. Also disclosed herein are methods of treating a bacterial with a crystalline form of ((2-Ethylbutanoyl)oxy)methyl (R)-2-hydroxy-3-propionamido-3,4-dihydro-2H-benzo[e][1,2]oxaborinine-8-carboxylate.

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

To provide various uses of compositions and methods of cancer therapy in which various pharmaceutical compositions are administered to the patient to revert tumor cells or tissue from the escape phase back to the equilibrium or even elimination phase.SOLUTION: Disclosed is a method of providing a coordinated treatment regimen for treating a tumor, comprising: reverting an escape phase of the tumor by administering at least a first pharmaceutical composition that reduces immune suppression in a tumor microenvironment; inducing an elimination phase of the tumor by administering at least a second pharmaceutical composition that enhances at least one of an adaptive immune response and an innate immune response; and maintaining an equilibrium phase of the tumor by administering at least a third pharmaceutical composition that biases the adaptive immune response towards a TH1 response.SELECTED DRAWING: Figure 2