27 results about "Esterase inhibitor" patented technology

The invention provides a method for detecting an anti-C1 esterase inhibitor neutralizing antibody in a biological sample, and the method mainly utilizes the characteristic that protein A resin is combined with an Fc segment of the antibody to capture the antibody (containing the anti-C1 esterase inhibitor neutralizing antibody), so that the C1 esterase inhibitor and complement component 1s (C1s) in the biological sample after thermal inactivation are removed; furthermore, an antibody (containing a neutralizing antibody) or an anti-C1 esterase inhibitor compound on the protein A resin is subjected to acid dissociation through an acidolysis solution, so that not only can the anti-C1 esterase inhibitor neutralizing antibody existing in a free form in a biological sample be detected, but also the anti-C1 esterase inhibitor neutralizing antibody existing in a combined form in the biological sample can be detected.

The present disclosure relates generally to processes for providing compounds that can be used as inhibitors of ectonucleotide pyrophosphatase / phosphodiesterase 1 (ENPP1), which inhibitors can be useful in treating or preventing soft bone diseases, such as hypophosphatasia (HPP).

The invention discloses a cascade targeted drug delivery system as well as a preparation method and application thereof, and belongs to the technical field of biological medicines. The invention designs a drug delivery system with a cascade targeting function, and the drug delivery system is used for delivering a phosphodiesterase 4 inhibitor A5. Through polypeptide modification and exosome fusion, phagocytosis and ingestion of cells to a drug delivery system are promoted, and the bioavailability of the drug is significantly improved. The drug delivery system shows excellent in-vivo lung targeting, can effectively inhibit the aggravation of inflammatory infiltration in the lung, and plays a role in treating acute lung injury. The invention provides a new strategy for improving the targeting property and the utilization rate of the medicine, provides a new medicine for treating the acute lung injury, and has a wide application prospect and an extremely high application value.

This specification describes methods for treating cancer using small molecule ectonucleotide pyrophosphatase / phosphodiesterase 1 (ENPP1) inhibitors and additional agents.

The application discloses a steroid-indole alkaloid hybrid dimer compound, a preparation method thereof and application of the compound in preparation of an antitumor chemotherapy drug sensitizer, and first prepares the steroid-indole diketopiperazine alkaloid hybrid compound from a fungus Aspergillus sp. EGF15-0-3 rice culture medium. The compound is a new skeleton compound first discovered in nature. It is first discovered that the hybrid compound has Tdp1 inhibitory activity and can be applied as a tyrosine-DNA phosphodiesterase 1 (Tdp1) inhibitor. It is first discovered that the hybrid compound has chemotherapy sensitization activity on a tumor chemotherapy drug topotecan TPT, which provides a drug source molecule and data support for development of a new natural antitumor combination inhibitor, and has important significance for development and utilization of marine Aspergillus sp. fungus resources.

This invention generally relates to veterinary use of an ectonucleotide pyrophosphatase / phosphodiesterase 1 (ENPP1) inhibitor, e.g., for modulating (e.g., inhibiting) ENPP1 activity and / or signaling, for example, for the treatment or prophylaxis of periodontal disease or bone disorder, such as periodontitis.

A device for detecting and / or quantifying functional C1-esterase inhibitor (fC1-INH), the device comprising: (i) a conjugate pad comprising a first zone and a second zone, on which a first agent and a second agent are immobilized, respectively, and (ii) a membrane, which is in communication with the conjugate pad, wherein the membrane comprises a third zone, on which a third agent is immobilized. The conjugate pad may further comprise a fourth zone for placing a biological sample, which flows through the device in the order of the first zone, the second zone, and the third zone.

The present invention provides combinations of inhibitors of Ectonucleotide Pyrophosphatase / Phosphodiesterase (ENPP1) with a radiation therapy or a radioligand for the purposes of treating cancer. The invention includes both methods of treatment of cancer with the provided combinations and pharmaceutical compositions comprising such combinations. A preferred ENPP1 inhibitor is SR-8541A; and a preferred radioligand is PluvictoTM.

The present application provides a novel medium composition for use in inducing differentiation of somatic cells into brown adipocytes. As the present application, for example, there can be mentioned a medium composition for use in inducing differentiation of somatic cells into brown adipocytes, which is characterized by comprising seven components of a thyroid hormone receptor agonist, a glucocorticoid receptor agonist, a phosphodiesterase inhibitor, insulin, an ascorbic acid derivative, albumin, and an antibiotic. According to the present application, differentiation induction of somatic cells into brown adipocytes can be effectively performed. In addition, according to the present application, brown adipocytes can be effectively maintained.

The present invention provides compositions used for the treatment and / or prevention of protein aggregation disorders. [Solution] Proteopathy encompasses a wide range of ailments, including neurodegenerative diseases (e.g., polyglutamine diseases such as huntingtin in Alzheimer's disease, Parkinson's disease, and Huntington's disease, and prion diseases); amyloidosis of other non-neuronal proteins (especially I1-antitrypsin, immunoglobulin light and heavy chains, lactadherin, apolipoprotein, gelzolin, lysozyme, fibrinogen, atrial natriuretic factor, keratin, lactoferrin, and β-2 microglobulin, etc.); sickle cell disease; cataracts; cystic fibrosis; retinitis pigmentosa; and nephrogenic diabetes insipidus. Administration of sulfatase inhibitors is generally suitable for treating and / or preventing protein toxicity associated with proteopathy. Therefore, the present invention provides compositions comprising sulfatase inhibitors for the treatment of proteopathy.

The present application provides a phosphodiesterase inhibitor compound and a preparation method and application thereof, in particular, the present application provides a compound with structural formula (I) or a pharmaceutically acceptable form thereof, wherein each substituent is defined in the description. The compound of the present application or the pharmaceutically acceptable form thereof can be used as a phosphodiesterase inhibitor and has high activity.

The present disclosure provides certain bicyclic heteroaryl phosphonate and boronate compounds that inhibit ectonucleotide pyrophosphatase / phosphodiesterase 1 (ENPP1) enzymatic activity for the treatment of certain diseases mediated by upregulation of ENPP1 such as cancers, inflammatory diseases, and viral infections. Also provided are pharmaceutical compositions containing such compounds.

This invention relates to a phosphodiesterase 4 (PDE4) inhibitor composition, belonging to the field of pharmaceutical formulations. The composition comprises a PDE4 inhibitor, a suspending agent, and other pharmaceutically acceptable excipients. The PDE4 inhibitor composition prepared by this invention has advantages such as good taste, convenient administration, high patient acceptance, and greater flexibility in clinical application.

A method for treating hypophosphatasia (HPP) is provided herein, comprising administering a therapeutically effective dose of an ectonucleotide pyrophosphatase / phosphodiesterase 1 (ENPP1) inhibitor. A method for using an ENPP1 inhibitor to treat or prevent cartilage disease is disclosed herein. In some embodiments, the cartilage disease is hypophosphatasia. Ectonucleotide pyrophosphatase / phosphodiesterase 1 (ENPP1) is an extracellular enzyme that hydrolyzes ATP to PPi and AMP in the extracellular space.

A method of producing a perfusion solution comprising combining pre-weighed amounts of a nutrient, a colloid, a hormone, a steroid, a buffer, magnesium sulfate anhydrate, and at least one of a phosphodiesterase inhibitor and a nitrate to form a solution for perfusing a lung at near physiologic conditions.

To provide a novel assay and / or platform for measuring functional C1-INH involved in HAE disease pathology.SOLUTION: A device and a lateral flow assay (LFA) method performed using such device is a device for detecting and / or quantifying functional C1-esterase inhibitor (fC1-INH), including: (i) a conjugate pad comprising a first zone and a second zone in which a first agent and a second agent are immobilized, respectively; and (ii) a membrane in communication with the conjugate pad, in which the membrane includes a third zone in which a third agent is immobilized.SELECTED DRAWING: Figure 4

Solid state forms of small molecule exonucleotide pyrophosphatase-phosphodiesterase 1 (ENPP1) inhibitors and pharmaceutical compositions comprising the solid state forms are described herein. The solid state forms and pharmaceutical compositions are useful for the treatment of diseases or disorders associated with ENPP1.

The invention belongs to the technical field of medicine analysis, and particularly relates to a method for analyzing a phosphodiesterase 4 inhibitor and impurities thereof. According to the analysis method for the phosphodiesterase 4 inhibitor and the impurities thereof, the dipotassium phosphate aqueous solution is used as a mobile phase A, acetonitrile is used as a mobile phase B, and gradient elution parameters and chromatographic parameters such as the flowing speed of the mobile phase, the column temperature, the sample size and the detection wavelength are improved, so that the purity of the phosphodiesterase 4 inhibitor is improved. The method can be used for simultaneously detecting and analyzing (E)-1-(3-(tetrahydrothiophene-3-yl) oxy-4-methoxystyryl)-2, 6-dimethyl pyridine-4-(1H)-ketone and seven impurities thereof, and solves the problem that in the prior art, the (E)-1-(3-(tetrahydrothiophene-3-yl) oxy-4-methoxystyryl)-2, 6-dimethyl pyridine-4-(1H)-ketone and seven impurities thereof are lacked. The invention aims to solve the technical problems in the prior art in a conventional method for detecting and analyzing 2, 6-dimethyl pyridine-4-(1H)-ketone and impurities thereof.

The invention discloses an isoaurone compound as well as a preparation method, a pharmaceutical composition and application thereof, and the preparation method comprises the following steps: carrying out Perkin reaction on substituted o-bromophenylacetic acid and substituted benzaldehyde under the action of acetic anhydride and alkali to obtain an intermediate A; and heating the intermediate A or an ammoniation product intermediate B thereof in a solvent in a nitrogen atmosphere under the action of a copper catalyst and alkali, and carrying out intramolecular C-O or C-N coupling to obtain the isoaurone compound. The isoaurone compound, the hydride thereof, the isomer thereof, and the application of the pharmaceutically acceptable salt or solvate thereof are used for preparing a phosphodiesterase inhibitor. The synthesis route is simple, the atom economy is high, the cost is low, large-scale implementation is facilitated, and the compound can be combined with various drug carriers for use and is convenient to take.

The disclosure relates to the use of phosphodiesterase 1 (PDE1) inhibitors in combination with a Compound of Formula VIII or a Compound of Formula IX, as described herein, or in combination with an antiemetic agent, such as an antipsychotic agent, e.g., olanzapine, for preventing or treating nausea and / or vomiting, e.g., CINV (chemotherapy-induced nausea and vomiting). In some embodiments, the Compound of Formula VIII or the Compound of Formula IX is used as mono-therapy (i.e., without a PDE1 inhibitor).

The invention relates to a pharmaceutical formulation to be administered by pressurized metered dose inhalers (pMDIs), comprising: (a) the (-) enantiomer of 3-cyclopropylmethoxy-4methanesulfonylaminobenzoic acid 1 -(3 -cyclopropylmethoxy-4difluoromethoxyphenyl)-2-(3 , 5 -dichloro- 1 oxypyrid in-4-yl)ethyl ester; a propellant; a co-solvent; and a surfactant selected from the group consisting of a PEG surfactant, a PVP surfactant, and a mixture thereof. may be used for the treatment of inflammatory or obstructive airway diseases.

This invention generally relates to formulations comprising an ectonucleotide pyrophosphatase / phosphodiesterase 1 (ENPP1) inhibitor, kit comprising the same and methods of use comprising an ENPP1 inhibitor or a formulation comprising the same.

The present invention relates to a method for preparing C1-esterase inhibitor (C1-INH) comprising the following steps: a) obtaining a starting fraction selected from plasma fractions; b) purifying said obtained starting fraction by affinity chromatography, said affinity chromatography comprising an elution step with an elution buffer having a pH of between 4.0 and 8.0; and c) recovering the eluate after chromatography step b), said eluate corresponding to the fraction comprising C1-INH.

Process for Preparing a C1-Esterase Inhibitor. The present invention relates to a process for preparing a C1-esterase inhibitor (C1-INH) comprising the following steps: a) obtaining a starting fraction selected from plasma fractions; b) purifying said starting fraction obtained by affinity chromatography, said affinity chromatography comprising an elution step with an elution buffer having a pH between 4.0 and 8.0; and c) recovering the eluate after chromatography b), and this eluate corresponds to the fraction comprising the C1-INH. Figure for abstract: none

Described herein are methods of treating cancer using small molecule exonucleotide pyrophosphatase / phosphodiesterase 1 (ENPP1) inhibitors and additional active agents.

To provide a technology that suppresses the compatibility changes between phosphodiesterase 5 inhibitors and vitamin B12. [Solution] A packaged composition comprising a composition containing a phosphodiesterase 5 inhibitor and vitamin B12, contained in an airtight package.

To provide a composition with good quality stability in which solidification of garlic processed products is suppressed during high-temperature storage, or discoloration of gamma-oryzanol is suppressed. [Solution] A composition containing a phosphodiesterase 5 inhibitor and one or more selected from the group consisting of garlic processed products and gamma-oryzanol.