12 results about "Mast cell activation" patented technology

The disclosure relates to pharmaceutical formulations and method of using chymase inhibitors for the prevention and treatment of mast cell-related disease states in which chymase is involved. More particularly the present disclosure is in the field of treating or preventing or reducing the symptoms of mast cell-related diseases, including atopic dermatitis (AD), chronic urticaria (CU), Eosinophilic Gastrointestinal Disorders (EGIDs), and prurigo nodularis (PN), using a chymase inhibitor, including a chymase inhibitor that prevents cleavage of stem cell factor (SCF) and its interaction with receptor tyrosine kinase (c-kit), thereby reducing mast cell activation and proliferation.

This invention provides a small molecule inhibitor targeting the FcεRIγ subunit and its application. It discovers that erythrophenol can act as a small molecule inhibitor targeting the FcεRIγ subunit, thereby inhibiting the occurrence of allergic reactions. This invention confirms the direct binding interaction between erythrophenol and the FcεRIγ subunit using SPR and CETSA techniques, revealing that erythrophenol can target and inhibit the FcεRIγ subunit. Furthermore, this invention finds that erythrophenol can significantly inhibit the release of IgE signal-induced β-aminoglycosidase in mast cells, exhibiting a significant ability to inhibit IgE signal-mediated mast cell degranulation and suppress mast cell activation-mediated allergic reactions. This fully demonstrates that erythrophenol, as an inhibitor targeting the FcεRIγ subunit, holds promise as the first inhibitor to induce FcεRIγ subunit degradation in anti-type I allergic diseases, and has broad application prospects for further use in anti-allergy treatment.

The application discloses application of a CGRP receptor small molecule antagonist in preparation of a medicine for treating chronic rhinosinusitis with nasal polyps. The medicine preparation is composed of an effective amount of the CGRP receptor small molecule antagonist and pharmaceutically acceptable adjuvants, and the dosage form is a nasal spray / drop / irrigation agent, and the administration route is simple and easy to operate, and is convenient for patients to use. The application can significantly reduce eosinophilic inflammation by inhibiting CGRP-mediated mast cell activation, and has a clear treatment advantage for eosinophilic nasal polyps. Compared with a biological preparation targeting type 2 cytokines, a small molecule compound is safer and simpler to obtain, can significantly reduce the treatment cost of patients, and provides a new efficient and economical choice for nasal polyp treatment.

Therapeutic methods and ophthalmic compositions for reducing ocular mast cell degranulation and / or ocular mast cell cytokine production in a human subject, inhibiting ocular mast cell activation in a human subject, treating dry eye disease (DED) or allergic conjunctivitis (AC) in a human subject, inhibiting mast cell activation in a human subject, and reducing or alleviating a sign or symptom of dry eye disease in a human subject using a BTK inhibitor are described. The disclosure also includes therapeutic methods and ophthalmic compositions for reducing or alleviating a sign or symptom of allergic conjunctivitis in a human subject and treating allergic conjunctivitis in a human subject using a BTK inhibitor.

Inhibiting mast cell activation by binding sialic acid-binding immunoglobulin-like lectin-9 (Siglec-9) is described. Inhibiting mast cell activation by binding Siglec-9 can be used to treat mast-cell associated inflammatory disorders, such as allergic diseases, rheumatoid arthritis, and mastocytosis.

This invention discloses a fusion peptide with synergistic anti-allergic effects, an anti-LTB4 monoclonal antibody, and an anti-allergic drug composition thereof. The fusion peptide is composed of peptide A, which inhibits histamine release, and peptide B, which blocks mast cell activation signals, covalently linked by a linker peptide, which can synergistically inhibit mast cell activation. The anti-LTB4 monoclonal antibody can specifically bind to LTB4, blocking its mediated inflammatory response. Combining the fusion peptide, the anti-LTB4 monoclonal antibody, and myricetin, which has antioxidant activity, forms a multi-target drug composition that can synergistically inhibit allergic reactions from multiple aspects, such as inhibiting mast cell degranulation, blocking the action of inflammatory mediators, and clearing oxidative stress products. In vitro cell experiments and OVA-induced allergic asthma mouse models have demonstrated that the anti-allergic effect of this composition is significantly better than that of a single component, and it has no obvious toxicity, providing a new candidate drug for the efficient treatment of allergic diseases.

The present invention relates to a compound of formula (I) wherein R1 and R2 are as defined herein, a pharmaceutical composition comprising such compound for treatment of a PGD2-mediated disorder including, to, allergic disease (such as allergic rhinitis, allergic conjunctivitis, atopic dermatitis, bronchial asthma and food allergy), systemic mastocytosis, disorders accompanied by systemic mast cell activation, anaphylaxis shock, bronchoconstriction, bronchitis, urticaria, eczema, diseases accompanied by itch (such as atopic dermatitis and urticaria), diseases (such as cataract, retinal detachment, inflammation, infection and sleeping disorders) which are generated secondarily as a result of behavior accompanied by itch (such as scratching and beating), inflammation, chronic obstructive pulmonary diseases, ischemic reperfusion injury, cerebrovascular accident, chronic rheumatoid arthritis, pleurisy, ulcerative colitis and the like.

The invention discloses an application of a CGRP receptor small molecule antagonist in preparation of a medicine for treating eosinophilic chronic sinusitis with nasal polyp. The pharmaceutical preparation is composed of an effective amount of a CGRP receptor small molecule antagonist and pharmaceutically acceptable auxiliary materials, the dosage form is nasal spray / nose drop / irrigation, and the pharmaceutical preparation is simple and convenient in administration route, easy to operate and convenient for patients to use. According to the invention, by inhibiting CGRP-mediated mast cell activation, eosinophilic granulocyte inflammation is significantly relieved, and especially, the traditional Chinese medicine composition has a definite treatment advantage on eosinophilic granulocyte nasal polyp; and compared with a biological agent of a targeted type 2 cytokine, the small molecule compound is safer, simpler and more convenient to obtain, the treatment cost of a patient can be remarkably reduced, and a new efficient and economic choice is provided for nasal polyp treatment.

The present application belongs to the field of biomedical detection technology, and particularly relates to a reaction solution for detecting trypsin-like transpeptidase activity and application thereof. The present application uses BAPNA as a specific substrate, which can produce a detectable signal change in the transpeptidation reaction, and a high-concentration amino group-glycine amide is added as a receptor molecule to enhance the transpeptidation reaction efficiency. Therefore, the present application solves the technical problem that the enzyme activity cannot be detected by the immunization method, has high reaction efficiency, stable and reliable detection process, shortened operation time (within 15 minutes), simple operation, strong practicability, can be used for evaluating the severity of acute allergic reaction, providing scientific guidance for the diagnosis of mast cell-related airway inflammation and mast cell activation syndrome, monitoring the effect of allergic treatment, and has clinical value in airway inflammation typing, differential diagnosis and efficacy monitoring through induced sputum or BAL fluid trypsin activity determination.

Compounds that have antiallergic and / or anti-inflammatory properties and methods of making thereof are disclosed. These compounds can block MMRGPRX2 and prevent or reduce mast cells activation. Pharmaceutical formulations in a unit dosage form suitable for the delivery of the compounds to a subject in need thereof are disclosed. The pharmaceutical formulations may include one or more active agents in addition to the compounds, such as one or more additional antiallergic and / or anti-inflammatory agents. The pharmaceutical formulation can be administered by oral administration, parenteral administration, inhalation, mucosal administration, or a combination thereof. Methods for preventing or treating pseudo allergic reactions, pseudo allergic diseases, and / or pseudo inflammatory diseases, or treating or ameliorating one or more symptoms associated with a pseudo allergic reaction, a pseudo allergic disease, and / or a pseudo inflammatory disease in a subject are also disclosed.

Inhibiting mast cell activation by binding sialic acid-binding immunoglobulin-like lectin-9 (Siglec-9) is described. Inhibiting mast cell activation by binding Siglec-9 can be used to treat mast-cell associated inflammatory disorders, such as allergic diseases, rheumatoid arthritis, and mastocytosis.

The invention belongs to the technical field of biomedical detection, and particularly relates to reaction liquid for detecting trypsin transpeptidase activity and application of the reaction liquid. BAPNA is adopted as a specific substrate, detectable signal change can be generated in the transpeptidation reaction, then high-concentration amino group-glycinamide is added as an acceptor molecule, and the transpeptidation reaction efficiency is enhanced. Therefore, the technical problem that the enzyme activity cannot be detected by an immunoassay is solved, the reaction efficiency is high, the detection process is stable and reliable, the operation time is shortened to be within 15 minutes, the operation is simple and convenient, and the practicability is high; the kit can be used for evaluating the severity of acute anaphylaxis, provides scientific guidance for diagnosis of mast cell related airway inflammation and mast cell activation syndrome, monitors the anaphylaxis treatment effect, and has clinical value in the aspects of airway inflammation typing, differential diagnosis and curative effect monitoring by inducing phlegm or BAL liquid trypsin activity determination.