62 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.

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 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 invention discloses a substituted aromatic heterocyclic compound containing a spiro skeleton as well as a preparation method and application thereof, and relates to the field of medicinal chemistry, in particular to the substituted aromatic heterocyclic compound containing the spiro skeleton or pharmaceutically acceptable salt of the substituted aromatic heterocyclic compound, a necessary composition containing the compounds and medical application of the substituted aromatic heterocyclic compound. The invention relates to an application of a monoacylglyceridase inhibitor, in particular to application of the monoacylglyceridase inhibitor as a monoacylglyceridase (MAGL) inhibitor in preparation of drugs for preventing and / or treating MAGL-related diseases. Comprise depression, schizophrenia, bi-directional disorder, dyskinesia, traumatic brain injury, neuroinflammation, Parkinson's disease, Alzheimer's disease, multiple sclerosis, amyotrophic lateral sclerosis, anxiety disorder, pain, metabolic disorder, alcoholic fatty liver disease, non-alcoholic fatty liver disease, hepatic fibrosis, cholestasis, nephropathy and other related diseases.

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 present invention provides, inter alia, methods and compositions for treating complement-mediated diseases, particularly chronic diseases requiring preventive and / or maintenance therapy. In one aspect, a C1-INH fusion protein having a longer half-life than native plasma-derived C1-INH is provided. In some embodiments, the methods according to the present invention comprise administering an effective amount of a recombinant C1-INH fusion protein to an individual suffering from or susceptible to a complement-mediated disease, such that at least one symptom or feature of the complement-mediated disease is prevented and / or reduced in intensity, severity or frequency.

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.

The invention discloses a derivative with a high isoflavone-O-alkylamine structure and application thereof, the structural formula of the derivative is as follows: # imgabs0 #, and the derivative can be used as an acetylcholin esterase inhibitor and a beta-amyloid protein aggregation inhibitor for treating Alzheimer's disease and other nervous system diseases.

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 invention provides application of boxthorn leaf total alkaloids in preparation of an acetylcholin esterase inhibitor, and belongs to the technical field of traditional Chinese medicines. The invention proposes that the boxthorn leaf total alkaloid has an acetylcholin esterase inhibiting effect for the first time, and the boxthorn leaf total alkaloid can be developed into an acetylcholin esterase inhibitor for preventing and treating diseases related to abnormal rise of acetylcholin esterase. Meanwhile, compared with an existing boxthorn leaf total alkaloid preparation method in the field, the boxthorn leaf total alkaloid preparation method provided by the invention is simpler, and the boxthorn leaf total alkaloid can be obtained without extracting by using organic solvents such as ethyl acetate and the like which are mutually soluble with water.

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.

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

The invention discloses an application of a boxthorn leaf extract in preparation of an acetylcholin esterase inhibitor, and belongs to the technical field of traditional Chinese medicines. An in-vitro enzyme activity test experiment proves that the boxthorn leaf extract has an acetylcholin esterase inhibiting effect, can be developed into an acetylcholin esterase inhibitor and is used for treating diseases related to abnormal rise of acetylcholin esterase.

Described are human serum albumin (hSA) preparations prepared from human plasma and methods of preparing them. The preparations have an amount of C1 esterase (C1E) inhibitor activity and exhibit stability against serine protease activity.

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 invention discloses the application of caffeoyl butanediamine in preparation of the acetylcholin esterase inhibitor for the first time. Belongs to the technical field of biological medicine. In-vitro enzyme activity test experiments prove that caffeoylbutanediamine has an acetylcholin esterase inhibition effect and can be used for being developed into an acetylcholin esterase inhibitor to treat diseases related to abnormal rise of acetylcholin esterase.

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.

The use of a C6 to C24 mono- and polyunsaturated acids or their derivatives thereof enzyme inhibitors particularly as P450 and esterase inhibitors in pesticide formulations.

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.