1057results about "Boron compound active ingredients" patented technology

The disclosure provides compounds useful for treating alpha-1 antitrypsin deficiency (AATD), according to formula (I):tautomers thereof, pharmaceutically acceptable salts of the compounds, pharmaceutically acceptable salts of the tautomers, deuterated derivatives of the compounds, deuterated derivatives of the tautomers, and deuterated derivatives of the salts, solid forms of those compounds and processes for making those compounds.

A boron carrying agent, a preparation method therefor, and a pharmaceutical formulation. The boron carrying agent contains compound 1, N-4-carboxyphenylboronic acid amide-threonine-phenylalanine-phenylalanine-tyrosine-glycine-glycine-serine-arginine-glycine-lysine-arginine-aspartic acid-aspartic acid-phenylalanine-lysine-threonine-glutamic acid-glutamic acid-tyrosine-cysteine, having a molecular formula of C114H158BN30O35S1 and a molecular weight of 2552.4, and further contains compound 2, N-4-carboxyphenylboronic acid amide-arginine-lysine-lysine-lysine-arginine-arginine-glutamine-arginine-arginine-arginine, and / or compound 3, N-4-carboxyphenylboronic acid amide-methionine-alanine-serine-methionine-threonine-glycine-glycine-glutamine-glutamine-methionine-glycine. Compounds 1-3 can serve as a targeted medicament for boron neutron capture therapy used for treating a cerebral glioma and a head and neck tumor.

The invention discloses a novel isoxazolopyrimidine derivative with anti-new coronavirus activity as well as a preparation method and application of the novel isoxazolopyrimidine derivative. The isoxazolopyrimidine compound provided by the invention has a good inhibition effect on SARS-CoV-2, and relates to the compound shown in the general formula (I), and pharmaceutically acceptable salts and solvent compounds thereof have a good inhibition effect on new coronavirus, and can be used for preparing antiviral drugs related to the new coronavirus for prevention, treatment or adjuvant treatment. # imgabs0 #

A drug combination of purinostat mesylate and an analog thereof for preventing and treating multiple myeloma, and the use thereof. Specifically, provided is a three-drug or four-drug combination of purinostat mesylate and an analog thereof, dexamethasone and other drug, which drug combination has significantly enhanced synergistic anti-tumor activity in vitro and in vivo, synergistically inhibits the expression of the key survival protein in multiple myeloma, is superior to existing clinical combination regimens, and has no significant toxic side effects. In addition, the drug combination significantly down-regulates the expression of CDK6, and overcomes the drug resistance to an immunomodulator. In particular, the three-drug combination of puisostat mesylate, a glucocorticoid and an immunomodulator has an excellent prevention and treatment effect on multiple myeloma, especially relapsed / refractory multiple myeloma.

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.

Methods for treating itch in human patients with atopic dermatitis (AD) and / or prurigo nodularis (PN) comprising administering a therapeutically effective amount of at least one compound chosen from (R)-2-[3-[4-amino-3-(2-fluoro-4-phenoxyphenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4-methyl-4-[4-(oxetan-3- yl)piperazin-1-yl]pent-2-enenitrile (rilzabrutinib) and pharmaceutically acceptable salts thereof are disclosed.

The compound shown in formula I, its stereoisomers or pharmaceutically acceptable salts, or a pharmaceutical composition containing them, and their use in the manufacture of a therapeutic agent for treating related diseases as a PDE4B inhibitor, wherein each group shown in formula (I) is as defined in the specification. [Chemical formula 1] TIFF2025518257000169.tif37156

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.

The invention relates to the field of biological medicine, in particular to a prodrug structure with ROS signal response performance and a preparation method and application thereof. The prodrug molecule with ROS signal response performance developed by the invention can quickly release living active molecules in a disease signal ROS-enriched environment, and plays a role in targeted therapy. The method has good universality, prodrug modification can be carried out on multiple molecules, four kinds of drug molecules approved to appear on the market are included, and it is verified that the solubility and biocompatibility of drugs can be improved, cytotoxicity can be reduced, and the effect of targeted therapy can be improved. Based on the structural characteristics of the molecules, the molecules can also be complexed with PVA hydrogel, and responsive controllable release of the medicine is further achieved.

The invention discloses a crisaborole Pickering emulsion as well as a preparation method and application of the crisaborole Pickering emulsion. The crisaborole Pickering emulsion prepared by the invention solves the problem of poor water solubility of crisaborole, improves the drug solubility, and has the characteristics of small particle size, high centrifugal stability, good long-term stability and the like. Compared with the traditional nanoemulsion, the Pickering emulsion disclosed by the invention shows certain advantages in the aspects of biocompatibility, cumulative transdermal amount and cutin retention, improves the curative effect of a local preparation and reduces skin toxicity, and can be used as an ideal local preparation for treating atopic dermatitis and other diseases.

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.

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.

The invention relates to a small molecular boron-10 carrying agent, a preparation method and application. The structural formula of the small molecule boron-10 carrying agent is shown as a formula (I). The invention also provides a preparation method of the small molecular boron-10 carrying agent, which comprises the following steps: carrying out condensation connection on a phenylboronic acid derivative and N-(2-aminoethyl) maleimide hydrochloride, and covalently coupling a boron drug to obtain a first intermediate; n < 2 >-(((9H-fluorene-9-yl) methoxy) carbonyl)-N < 6 >-(tert-butoxycarbonyl)-L-lysine, N-(2-aminoethyl) maleimide hydrochloride and a phenylboronic acid derivative are subjected to condensation connection, and a second intermediate is obtained; carrying out esterification connection on a selenium-containing compound and a DNA repair inhibiting compound to obtain a third intermediate; and carrying out condensation connection on the second intermediate and the third intermediate, and connecting the first intermediate to obtain the small molecule boron-10 carrying agent. The invention solves the problems of limited treatment effect and difficulty in inhibiting DNA damage repair in the existing BNCT. # imgabs0 # (I)

The present invention provides compounds that inhibit matriptase 2 or its mutant forms, as well as compositions and methods of use thereof.

The disclosure relates to synthetic peptides that are capable of modulating metabolism and find uses e.g. in treating metabolic diseases or disorders.

Provided herein are methods and uses for treating multiple myeloma (such as Newly Diagnosed Multiple Myeloma) in a patient in need thereof. The methods comprise administering to the patient an anti-CD38 antibody, bortezomib, lenalidomide, and dexamethasone.

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 embodiments are directed to methods of using a glycine transporter inhibitor, e.g., a GlyT1 inhibitor, or a pharmaceutically acceptable salt, hydrate, or prodrug thereof, or a pharmaceutical composition thereof, to prevent or treat erythropoietic protoporphyria (EPP), X-linked protoporphyria (XLPP), and / or congenital erythropoietic porphyria (CEP), and their associated syndromes. The present application provides a method of treating erythropoietic protoporphyria (EPP), X-linked protoporphyria (XLPP), or congenital erythropoietic porphyria (CEP) in a subject, the method comprising administering to the subject a pharmaceutical composition comprising one or more glycine transporter 1 (GlyT1) inhibitors or pharmaceutically acceptable salts thereof, or one or more prodrugs of GlyT1 inhibitors or salts thereof.

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.