41 results about "Esterase inhibitor" patented technology

The invention belongs to the technical field of biological information, and relates to an acetylcholin esterase inhibitor prediction method based on Stacking ensemble learning and molecular feature fusion, which comprises the steps of data collection and preparation, data annotation and optimization, feature extraction and analysis, construction of a Stacking model, result verification and feedback and construction of a prediction platform. The molecular fingerprints and the property descriptors are used as features, and an acetylcholin esterase inhibitor classifier is successfully constructed by adopting a Stacking algorithm. According to the method, the problems that the efficiency of finding the acetylcholin esterase inhibitor by a traditional experimental method is low, and a common quantitative structure-function relationship method is high in complexity and poor in generalization ability can be solved, the new drug finding speed is increased, experimental candidates are accurately positioned, and resource waste is reduced.

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 invention relates to a compound of formula (I) or a pharmaceutically acceptable salt and / or solvate thereof. The invention also relates to the use of the compounds of formula (I) as a medicament, in particular for the prevention or treatment of obsessive-compulsive disorder and related behaviors, including addiction, obsessive-compulsive disorder and dietary disorder, and neurodegenerative diseases, such as Parkinson's disease or Alzheimer's disease.

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.

The disclosure relates to the use of phosphodiesterase 1 (PDE1) inhibitors for preventing or treating chemobrain, e.g., inhibiting or mitigating one or more symptoms of chemobrain, e.g., feeling of mental fogginess, deficit in attention, disorganized behavior or thinking, confusion, impaired concentration, difficulty finding the right word, difficulty learning new skills, difficulty multitasking, memory impairment (e.g., short-term memory problems, long-term memory problems, impaired verbal memory, impaired visual memory), and / or fatigue.

The invention relates to the technical field of medicines, in particular to a novel medical application of a phosphodiesterase 4B inhibitor namiklast, and particularly relates to an application of namiklast in preparation of a medicine for treating intervertebral disc fibrosis through targeted inhibition of macrophage-myofibroblast transformation.

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 invention provides an acetylcholin esterase inhibitor screening method based on a neural network. The method comprises the steps of 1, constructing a multi-species data set; step 2, data set preprocessing and sample labeling; step 3, constructing graph structure data representation; step 4, multi-scale feature extraction; 5, feature fusion and binding affinity prediction; step 6, model training and verification; and 7, screening and verifying the acetylcholin esterase inhibitor. According to the method, the problems of single species limitation and low precision in the existing method can be solved, the screening efficiency is improved by several times compared with that of the traditional method, the high-affinity AChE inhibitor can be rapidly identified, and a key tool is provided for research and development of Alzheimer disease treatment drugs through a differential feature extraction and alternating fusion mechanism.

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 disclosure provides certain quinazoline compounds that inhibit ectonucleotide pyrophosphatase / phosphodiesterase 1 (ENPP1) enzymatic activity and are therefore useful for the treatment of diseases and conditions modulated at least in part by ENPP1. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.

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.

Please add the following heading and paragraph on a separate sheet, after the claims: The disclosure relates to the use of phosphodiesterase 1 (PDE1) inhibitors for the treatment of cancers and tumors, including for inhibiting tumor recruitment of macrophages and other cells to the tumor or cancer, for complementing and enhancing checkpoint inhibitor therapies, and for mitigating the side effects (i.e., inflammatory-related adverse events) associated with checkpoint inhibitor therapies.

The present disclosure provides certain bicyclic heteroaryl sulfanediimine compounds that inhibit ectonucleotide pyrophosphatase / phosphodiesterase 1 (ENPP1) enzymatic activity and are therefore useful for the treatment of diseases treatable by inhibition of ENPP1. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.

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.

The invention discloses a trachinotus ovatus sourced acetylcholin esterase inhibitory peptide as well as a preparation method and application thereof, and belongs to the technical field of bioactive peptides. The acetylcholin esterase inhibitory peptide is any one of polypeptides with amino acid sequences as shown in SEQ ID NO. 1 to SEQ ID NO. 4. According to the invention, trachinotus ovatus is taken as a raw material, heptapeptides DLTDYLM, QGPIGPR, hexapeptide APDPFR and pentapeptide WGDAG with acetylcholin esterase inhibitory activity, antioxidant activity and Ca < 2 + > binding activity are obtained through enzymolysis and immobilized calcium ion affinity chromatography separation, and the action mechanism of chelating with acetylcholin esterase and Keap1 is defined. The polypeptide from trachinotus ovatus can be applied to preparation of acetylcholin esterase inhibitors, antioxidants and calcium supplements, and has a good application prospect.

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.

The invention discloses a method for detecting rabbit DNA residual quantity in a rabbit-derived biological product, and belongs to the field of DNA detection. The rabbit DNA in the recombinant human C1 esterase inhibitor expressed by a transgenic rabbit breast bioreactor platform can be effectively detected through the combination of specific primer sequences and probe sequences, and the rabbit DNA detection kit has good specificity, a large linear range and high accuracy, precision and sensitivity, and can be used for detecting the rabbit DNA in the recombinant human C1 esterase inhibitor expressed by the transgenic rabbit breast bioreactor platform. The method can be applied to detection of DNA residues in rabbit-derived biological products and related biological products, and has a good application prospect.

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

To discover an ingredient having anti-obesity action, a cyclic AMP phosphodiesterase activity inhibitory action, a dipeptidyl peptidase IV activity inhibitory action, anti-aging action, hair-growing action, antiandrogen action, skin-whitening action or anti-inflammatory action from compounds derived from a natural product and to provide an anti-obesity agent, a cyclic AMP phosphodiesterase activity inhibitor, a dipeptidyl peptidase IV activity inhibitor, an anti-aging agent, a hair-growing agent, an antiandrogen agent, a skin whitening agent or an anti-inflammatory agent, which uses the ingredient as an active ingredient.SOLUTION: Dihydroferulic acid is used as an active ingredient of an anti-obesity agent, a cyclic AMP phosphodiesterase activity inhibitor, a dipeptidyl peptidase IV activity inhibitor, an anti-aging agent, a hair-growing agent, an anti-androgen agent, a skin-whitening agent and an anti-inflammatory agent. Further, dihydroferulic acid is blended in a skin cosmetic, a hair cosmetic and a food or drink.SELECTED DRAWING: None

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 present disclosure provides certain bicyclic heteroaryl compounds that inhibit the exonucleotide pyrophosphatase / phosphodiesterase 1 (ENPP1) enzyme activity, and thus are useful in the treatment of diseases and conditions modulated at least by the ENPP1 moiety. In some embodiments, the bicyclic heteroaryl compounds include those having formula (I): Also provided herein are pharmaceutical compositions containing such compounds and methods for preparing such compounds.