18 results about "Histamine receptor" patented technology

The present invention discloses a series of phenylurea derivative compounds, specifically relating to the compounds as free base, or isomer, or solvate, or pharmaceutically acceptable salt forms; methods of preparing medicaments; compounds composition, and therapeutic uses thereof. The present invention has developed a series of structurally novel compounds based on histamine H3 receptor ligands, and a series of relevant biological tests have been performed on the compounds. The results of the tests all indicate that the compounds have significant H3 receptor antagonistic activity and can be used as lead compounds for the prevention or treatment of H3 receptor-related diseases.

The present invention relates to novel heterocyclic compounds useful in the preparation of medicaments for the treatment of diseases associated with various functions of the histamine 4 receptor.In particular, said drugs are useful for treating inflammatory diseases, allergy, pain, nasal polyps, rhinitis, chronic sinusitis, nasal congestion, nasal itching, asthma, chronic obstructive pulmonary disease, rheumatoid arthritis, atopic dermatitis, psoriasis, eczema, pruritus, itchy skin, urticaria, idiopathic chronic urticaria, scleroderma, conjunctivitis, keratoconjunctivitis, ocular inflammation, dry eye, cardiac dysfunction, arrhythmia, atherosclerosis, multiple sclerosis, inflammatory bowel disease (including colitis, Crohn's disease, ulcerative colitis), inflammatory pain, neuropathic pain, osteoarthritis pain, autoimmune disease, thyroid, immune-mediated (also known as type I) diabetes, lupus, post-surgical adhesions, vestibular disorders and cancer.

The invention provides sinomenine in preparation of a medicine for treating chronic pain of rheumatoid arthritis and application of the sinomenine in preparation of the medicine for treating the chronic pain of the rheumatoid arthritis, and aims at solving the problems that an existing medicine for resisting the rheumatoid arthritis is limited in action target spot and poor in treatment effect. The sinomenine takes a histamine receptor H1R on a nervous system dorsal root ganglion M1 type macrophage as the action target spot; the target spot is intervened to regulate and control polarization of macrophages, reduce expression of histamine H1R in M1 type macrophages and inhibit infiltration of the macrophages, so that chronic pain, including crymodynia, mechanical pain, heat pain and the like, of rheumatoid arthritis is effectively relieved; the sinomenine combined action target can improve pain and arthritis symptoms of a model mouse, reduce the level of inflammatory factors and inhibit LPS-induced macrophage migration and H1R expression, and the sinomenine pharmaceutical composition has various dosage forms, has unique action target and mechanism, has a remarkable treatment effect, and can be used for preparing medicines for treating chronic infectious diseases. The compound is expected to become a novel non-opioid anti-rheumatoid arthritis chronic pain medicine.

The invention discloses a traditional Chinese medicine composition for relieving itching. The traditional Chinese medicine composition is prepared from the following raw materials in parts by weight: 6-50g of radix scutellariae, 6-50g of fructus gardeniae, 6-50g of fructus forsythiae, 6-50g of flos lonicerae and 6-50g of radix geutianae. According to the invention, the radix scutellariae for inhibiting histamine release, the fructus forsythiae for antagonizing histamine receptors and the felwort for blocking itching signal transduction are subjected to multi-way action to cover the whole link of itching-inducing medium generation-receptor combination-signal transmission, so that rapid itching relieving is realized; the cape jasmine for promoting prothrombin activation, the baical skullcap root for enhancing platelet aggregation and the honeysuckle flower for contracting blood vessels act together, so that the blood coagulation time is shortened, and the effect fluctuation of a single hemostasis mechanism is avoided; the five medicines jointly inhibit the release of inflammatory factors, enhance the local antibacterial ability, relieve inflammatory pruritus, prevent wound infection, avoid vicious circle of itching-grasping-infection-aggravated itching, and reduce the infection risk after bleeding.

The invention relates to compounds of formula (I):or pharmaceutically acceptable salts or solvates thereof, to pharmaceutical compositions comprising them and to their use in the treatment and / or prevention of diseases or disorders mediated by histamine H4 receptor.

The invention relates to compounds of chemical formula (1) or pharmaceutically acceptable salts or solvates thereof, to pharmaceutical compositions containing them and to their use in the treatment and / or prevention of diseases or disorders mediated by the histamine-H4 receptor.

The present invention provides histamine H1 receptor antagonism-based uses for various uses (histamine H1 receptor antagonism uses, uses to improve sleep quality and / or modulate balance of the autonomic nervous system, and uses to improve sleep quality and / or modulate balance of the autonomic nervous system. And a use for preventing the onset of autonomic nervous system dysfunction or a symptom caused thereby or for improving autonomic nervous system dysfunction or a symptom caused thereby). The present invention relates to: a composition comprising, as an active ingredient, at least one substance selected from the group consisting of indole-3-lactic acid, alpha-Asp-Phe, Val-Arg, Asp-Gly-Glu, and salts thereof, or a lactic acid bacteria culture supernatant (not containing lactic acid bacteria cells) of a lactic acid bacteria belonging to any genus selected from the group consisting of the genus Lactobacillus, the genus Lactobacillus, and the genus Lactobacillus; the liquid supernatant contains at least one substance selected from the group consisting of indole-3-lactic acid, alpha-Asp-Phe, Val-Arg, Asp-Gly-Glu, and salts thereof. The liquid supernatant contains at least one substance selected from the group consisting of indole-3-lactic acid, alpha-Asp-Phe, Val-Arg, Asp-Gly-Glu.

This invention relates to the field of pharmaceutical technology for myocardial fibrosis. Specifically, it provides the application of histamine H1 receptor antagonists in the preparation of drugs for treating myocardial fibrosis. This invention utilizes a stress overload mouse model constructed via TAC surgery to simulate the in vivo process of myocardial fibrosis, and a TGF-β1-induced fibrotic cell model. Combined with network pharmacology analysis and histamine H1 receptor gene knockout mice, the anti-myocardial fibrosis effects and mechanisms of action of the histamine H1 receptor antagonists brompheniramine maleate (BHM) and desloratadine (DLT) were investigated at both the systemic and cellular levels, providing a theoretical and experimental basis for the development of new anti-myocardial fibrosis drugs.

The invention discloses an antihistamine component modified nano delivery system as well as a preparation method and application thereof. The nano delivery system comprises a nano capsule modified by an antihistamine component. The nanocapsule comprises nanoparticles formed by an acrylic acid derivative polymeric monomer, a cross-linking agent and an initiator. Specific binding of the antihistamine component and a histamine receptor in a brain area is utilized, and specific receptor mediated cross-blood brain barrier drug delivery is achieved.

The application provides a compound with histamine H3 receptor protein degradation activity and a preparation method and application thereof, and belongs to the field of medicines. The application provides a compound shown in formula I, the compound has obvious degradation effect on HRH3 protein, the compound can be used for preparing a histamine H3 receptor degrading agent, and is used for treating diseases related to the activity of HRH3 protein. The application further proves through experiments that the compound has the effects of significantly improving cognition, learning and memory and attention, and has a wide application prospect. A-L-B formula I.

The invention discloses a nucleic acid composition, an anti-allergic drug associated diagnosis detection kit and a micro-fluidic chip, and relates to the field of allergy detection. The nucleic acid composition disclosed by the invention realizes multi-target cooperative detection through three-section design: the histamine receptor aptamer specifically recognizes the histamine receptor and triggers the change of a stem-loop structure, and the leukotriene receptor response type DNA skeleton enhances the binding stability with the leukotriene receptor through a repetitive sequence; and the drug-triggered auxiliary chain promotes the formation of the complex by prolonging the tail of the poly (adenylic acid). The three components form a cascade reaction, the inflammatory mediator level and the drug responsiveness can be synchronously detected, the detection is more comprehensive than single target detection, and the structural parametric design ensures the suitability and repeatability.

The disclosure relates to an aqueous ophthalmic pharmaceutical composition including: a) at least 0.4% w / v of bilastine, of formulaor a pharmaceutically acceptable salt or solvate thereof, wherein the bilastine salt or solvate thereof is completely dissolved in the pharmaceutical composition; b) at least one β-cyclodextrin; and c) at least one pharmaceutically acceptable water-soluble gelling agent; and wherein the pH is comprised between 4 and 9. Use of the composition is described for the treatment and / or prevention of conditions mediated by H1 histamine receptor, such as allergic disorders or diseases. The treatment and / or prevention of allergic conjunctivitis is described.

Disclosed herein are formulations of histamine and histamine receptor agonists for treating a cancer or a tumor. Also disclosed are methods of using myeloid derived suppressor cell (MDSC) detection assays to select cancer patients for treatment with the formulations as disclosed herein. Also disclosed are methods of restoring the immune response against tumors in cancer patients who are incomplete responders to immune checkpoint inhibitor (ICI) therapy.

Provided herein is a pharmaceutical composition comprising two or more compounds, wherein each compound is independently a phosphodiesterase inhibitor, an adenosine receptor antagonist, a calcium channel blocker, a histamine H1-receptor agonist, a histamine H2-receptor agonist, a histamine H3-receptor antagonist, or a β2-adrenoreceptor agonist. Also provided herein is a method of treating, preventing, or ameliorating a cardiovascular disease in a subject, comprising administering to the subject in need thereof two or more compounds, wherein each compound is independently a phosphodiesterase inhibitor, an adenosine receptor antagonist, a calcium channel blocker, a histamine H1-receptor agonist, a histamine H2-receptor agonist, a histamine H3-receptor antagonist, or a β2-adrenoreceptor agonist.

A compound of formula (I) or a pharmaceutically acceptable salt or ester thereof. The compounds have activity against multiple histamine receptor subtypes, including for example histamine H1 and H4.

The invention relates to the technical field of antiepileptic drugs, in particular to a sulfur-containing piperidine ether aryl derivative as well as a preparation method and application thereof, and the structural general formula of the sulfur-containing piperidine ether aryl derivative is as shown in formula (I), in the formula (I), R is selected from H, 2-Cl, 3-Cl and 4-Cl; n = 1 or 2. The sulfur-containing piperidine ether aryl derivative provided by the invention has remarkable histamine H3 receptor antagonistic activity and shows an anti-convulsion characteristic, so that the sulfur-containing piperidine ether aryl derivative can be used as an anti-epileptic compound.

This application relates to the field of medicinal chemistry, specifically to a derivative of ligustilide-7-aminocarbamate-4'-substituted aminopropyl ether, its preparation method, and its application. Addressing the shortcomings of ligustilide in AD treatment, this application utilizes previous studies to demonstrate strong eeAChE and huACh inhibitory activity, strong inhibition of self-induction, and Cu... 2+ Induced Aβ 1‑42 Aggregation activity, significantly reduced Aβ 25‑35 The lead compound, scutellarin aglycone-4′-L-amino acid carbamate, which induces tau hyperphosphorylation and significantly improves learning and memory impairment in scopolamine-induced AD model mice, is used to introduce histamine H at the 7-position of its structure. 3 By using the key structural fragment (3-methylpiperidinyl) or cycloheptane group of the receptor antagonist, a cholinesterase inhibitor and histamine H2 receptor antagonist can be obtained. 3 Multi-targeted ligand derivatives with better anti-AD properties through receptor antagonistic synergistic mechanism.

The application discloses an amino thiazole compound and use thereof as a brain-permeable histamine H2 receptor agonist, and belongs to the field of medicines. The amino thiazole compound provided by the application has a structural general formula as shown in formula (I) and includes pharmaceutically acceptable salts. The amino thiazole compound has histamine H2 receptor agonistic activity and excellent blood-brain barrier permeability. Therefore, the amino thiazole compound can be applied to preparation of a medicine for treating diseases such as schizophrenia, mania, attention deficit hyperactivity disorder, binge eating or bulimia nervosa, autism, Parkinson's disease, ischemic brain injury and the like.