1466results about "Boron compound active ingredients" patented technology

The present invention relates to methods of treatment of light chain amyloidosis and other CD38-positive hematological malignancies with anti-CD38 antibodies.

Disclosed are compounds of formula (Ia) or a pharmaceutically acceptable salt thereof pharmaceutical compositions comprising compounds of formula (Ia) and methods of using the same for treating cancer or a respiratory inflammatory disease and inhibiting arginase:whereinR1 is —NHR1a;R1a is —H or —C(O)CH(R1b)NHR1c; andR1b is selected from —H, —(C1-C4) alkyl and CH2OR1d and R1c is —H; orR1b and R1c, together with the atom to which they are attached, form a 5-membered heterocyclic ring; andR1d is H or —CH3.

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.

The invention relates to the technical field of radiopharmaceuticals, and in particular relates to a bicyclo [1.1. 1] pentane compound for targeting and combining fibrocyte activating protein and application of the bicyclo [1.1. 1] pentane compound. The structure of the compound as shown in the formula (I) is # imgabs0 # (I); according to the invention, the structure of the FAP combined compound is modified, so that the compound with longer residence time in in-vivo tumors is obtained.

The invention relates to the technical field of radiopharmaceuticals, in particular to a targeted binding fibrocyte-activated protein polymer compound and application thereof. The structure of the compound as shown in the formula (I) is # imgabs0 # (I); according to the invention, the structure of the FAP combined compound is modified, so that the compound with longer residence time in in-vivo tumors is obtained.

Disclosed herein are antimicrobial compounds, polymorphic forms, compositions, pharmaceutical compositions, the method of use and preparation thereof. Some embodiments relate to boronic acid derivatives and their use as therapeutic agents, for example, β-lactamase inhibitors (BLIs).

Disclosed herein are antimicrobial compounds compositions, pharmaceutical compositions, the method of use and preparation thereof. Some embodiments relate to boronic acid derivatives and their use as therapeutic agents, for example, β-lactamase inhibitors (BLIs).

The invention relates to the field of biological medicine, in particular to a compound and a preparation method and application thereof. Particularly, the invention relates to a compound shown in a formula (I) or pharmaceutically acceptable salt, stereoisomer, solvate, isotope labeled compound or polymorphic substance thereof, a preparation method thereof, a pharmaceutical composition containing the compound and application thereof, the compound can be used as a sodion channel inhibitor, has an analgesic effect, and can be used for preparing a sodion channel inhibitor. The compounds of the present application also have a variety of excellent properties. # imgabs0 #

The present disclosure provides compounds of the formulae herein (e.g., Formula (I)), and pharmaceutically acceptable salts thereof, which are useful for modulating protein synthesis (e.g., modulating synthesis of BCL-2, MYC, CCND1, MCL-1, ALK, KRAS-G12D). The present disclosure also provides pharmaceutical compositions and kits comprising the compounds, or pharmaceutically acceptable salts thereof, and methods of treating or preventing diseases or disorders (e.g., diseases or disorders associated with BCL-2, MYC, CCND1, MCL-1, ALK, KRAS-G12D) by administering to a subject in need thereof the compounds, or pharmaceutically acceptable salts thereof, or pharmaceutical compositions thereof.

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 #

The invention discloses a nano-carrier based on charge crosslinking, a preparation method of the nano-carrier and application of the nano-carrier as a tumor chemotherapy drug. Wherein the nano-carrier is formed by assembling two polymer chains with positive and negative charges through electrostatic interaction, a precursor ligand on a polymer chain B releases an organic ligand under exogenous or endogenous stimulation, and competes for metal ions on a polymer chain A with positive charges to generate a metal complex in situ, and meanwhile, the electrostatic interaction of the nano-carrier is weakened, so that the metal complex is formed. The dissociation of the nano-carrier is caused, a macromolecular chain B containing an organic ligand is released, and the effect of tumor chemotherapy or immunoregulation is achieved. The method is simple to operate, short in time consumption and mild in reaction condition; the material is good in biocompatibility and high in safety degree. Pharmacodynamic experiments in some embodiments show that the nano-carrier can effectively kill the breast cancer and trigger cellular immunogenic death, meanwhile, tumor cell metastasis is inhibited, and a new thought and means are provided for the clinical problem of breast cancer lung metastasis urgently needing to be solved at present.

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 chemiluminescent probe of a targeted A beta oligomer as well as a preparation method and application of the chemiluminescent probe. The structural general formula of the chemiluminescent probe of the targeted A beta oligomer is shown as I in the specification. According to the present invention, the chemiluminescence probe capable of specifically targeting the A beta oligomer is successfully constructed for the first time so as to achieve the early diagnosis and treatment of AD; an additional light source is not needed, and background signals caused by exciting light can be effectively reduced, so that the detection sensitivity is higher. The chemiluminescent probe targeting the A beta oligomer can promote selective oxygenation of beta amyloid protein through chemical excitation and neutralize toxicity of the A beta oligomer, has certain treatment potential and is expected to be developed into an effective method for treating amyloidosis. # imgabs0 #

There is provided a method of at least partially inhibiting the function of Klebsiella pneumoniae carbapenemase-2 (KPC-2) or a variant thereof, the method comprising reacting said KPC-2 with a compound selected from the group consisting of 5-chloro-1, 3-dihydro-1-hydroxy-2, 1-benzoxaborolane, 5-fluoro-1, 3-dihydro-1-hydroxy-2, 1-benzoxaborolane, 5-fluoro-1, 3-dihydro-1-hydroxy-2, 1-benzoxaborolane, 5-fluoro-1, 3-dihydro-1-hydroxy-2, 1-benzoxaborolane, 5-chloro-1, 3-dihydro-1-hydroxy-2, 1-benzoxaborolane, 5-chloro-1, 3-dihydro-1-hydroxy-2, 1- The present invention relates to a method for contacting a beta-lactam antibiotic-resistant bacterium with a benzoxaborolane selected from the group consisting of 1, 1-benzoxaborolane and mixtures thereof, which can be used to treat an infection with a beta-lactam antibiotic-resistant bacterium in a subject.

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.

The invention provides a preparation method and application of a suspension containing a PDE-4 or PDE-3 / 4 inhibitor for sterile inhalation. The preparation method comprises the following steps: dispersing a PDE-4 or PDE-3 / 4 inhibitor in injection water containing an excipient, and carrying out high-pressure moist heat sterilization to obtain a PDE-4 or PDE-3 / 4 inhibitor dispersion liquid; dissolving the long-acting beta2-receptor stimulant and / or the long-acting muscarinic receptor antagonist, sterilizing and filtering to obtain a mixed solution; and mixing the PDE-4 or PDE-3 / 4 inhibitor dispersion liquid with the mixed solution, dispersing, and carrying out sterile filling. The medicinal preparation prepared by the invention is a sterile inhalation suspension, and the sterile inhalation suspension containing the PDE-4 or PDE-3 / 4 inhibitor is high in bioavailability, good in patient medication compliance and good in preparation stability.

Method of at least partially inhibiting the function of Klebsiella pneumoniae carbapenemase-2 (KPC-2) or a variant thereof, the method including contacting the KPC-2 with a benzoxaborole selected from the group consisting of 5-chloro-1,3-dihydro-1-hydroxy-2,1-benzoxaborole, 5-fluoro-1,3-dihydro-1-hydroxy-2,1-benzoxaborole, and mixtures thereof useful in the treatment of beta-lactam antibiotic resistant bacteria infections in a subject.

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.