20 results about "P2X3 Receptor" patented technology

The invention discloses imidazopyridine derivatives and application thereof, a pharmaceutical composition and a pharmaceutical preparation, and belongs to the technical field of medical chemistry. The technical problems to be solved are that the existing P2X3 receptor inhibitor is poor in safety, low in P2X3 or P2X2 / 3 selectivity, poor in metabolic stability and the like. According to the key points of the technical scheme, the imidazopyridine derivative is selected from a compound as shown in a formula I or a racemate, a stereoisomer, a geometric isomer, a tautomer, a nitrogen oxide, a hydrate, an isotope label, a solvate, a polymorphic substance, a metabolite, an ester, a pharmaceutically acceptable salt or a prodrug thereof.

The application discloses an imidazopyridine derivative and application, a pharmaceutical composition and a pharmaceutical preparation, and belongs to the technical field of medicinal chemistry. The technical problems to be solved are that existing P2X3 receptor inhibitors have poor safety, low selectivity for P2X3 or P2X2 / 3 and poor metabolic stability. The technical solution is that an imidazopyridine derivative is selected from the compounds shown in the formula I or racemates, stereoisomers, geometric isomers, tautomers, nitroxides, hydrates, isotopically labeled compounds, solvates, polymorphs, metabolites, esters, pharmaceutically acceptable salts or prodrugs.

The invention discloses a crystal form of an N-formamido pyrazoline compound as well as a preparation method and application of the crystal form. The invention provides a crystal form of a compound as shown in a formula A. The crystal form is a crystal form I, a crystal form II, a crystal form III, a crystal form IV, a crystal form V, a crystal form VI or a crystal form VII, and discloses a preparation method, a composition and application of the crystal form in preparation of a P2X3 receptor antagonist. The invention also relates to application of the compound in preparation of drugs for treating respiratory system diseases, pains caused by various reasons, and skin diseases. The crystal form stability is good, the hygroscopicity is small, and the patent medicine prospect is good. # imgabs0 #

The application provides a preparation method of an imidazopyridine compound shown as formula IV and intermediates thereof shown as formula I or formula II. The imidazopyridine compound shown as formula IV can antagonize P2X3 receptors and has the effects of inhibiting cough and analgesia.

Pharmaceutical compositions comprising (i) a P2X3 receptor antagonist and (ii) a carbonic anhydrase inhibitor (CAI), and methods of treating sleep apnea and conditions associated with pharyngeal airway collapse are described herein.

The invention belongs to the technical field of oligopeptide pharmacology, and particularly discloses a Maged1 competitive oligopeptide and application thereof. The Maged1 competitive short peptide is a short peptide MP1 or a short peptide MP2, and the amino acid sequence of the Maged1 competitive short peptide is as shown in SEQ ID No. 1 or SEQ ID No. 2. Experiments prove that the Maged1 competitive oligopeptide and Maged1 can be competitively combined with a P2X3 receptor, so that activation of the Maged1 on the P2X3 receptor is inhibited, and the Maged1 competitive oligopeptide has a good clinical application prospect in treatment of chronic pain.

The present invention relates to compounds of Formula I (hereinafter referred to as P2X3 inhibitors) that inhibit P2X purinergic receptor 3; in particular, the present invention relates to compounds that are pyridopyrimidine derivatives, methods of making such compounds, pharmaceutical compositions containing them and therapeutic uses thereof. The compounds of the present invention are useful in the treatment of a number of disorders associated with P2X3 receptor mechanisms, such as respiratory diseases, including cough, asthma, idiopathic pulmonary fibrosis (IPF) and chronic obstructive pulmonary disease (COPD).

The present invention discloses a crystal form of a heterocyclic compound, a preparation method thereof and an application thereof. The present invention provides a crystal form of a compound represented by formula A: the crystal form is crystal form I, crystal form II, crystal form III, crystal form IV, crystal form V, crystal form VI, crystal form VII, crystal form VIII or crystal form IX, and discloses its preparation method, composition and its application in the preparation of P2X3 receptor antagonists, or in the preparation of drugs for preventing and / or treating pain, urinary tract diseases or respiratory diseases. It has high P2X3 antagonistic activity, good selectivity, low toxicity, good metabolic stability and little taste impact.

An N-formamidopyrazoline derivative is a compound having General Formula (I) or an enantiomer, a diastereomer, an epimer and a racemate thereof, or a pharmaceutically acceptable salt thereof. The compound is an antagonist of a ligand-gated non-selective cation channel receptor subtype P2X3, and can be used for treating or preventing various diseases mediated by the receptor P2X3.

The invention provides a heterocyclic compound as a P2X3 receptor inhibitor. The heterocyclic compound is a compound as shown in a formula (I), an isotope variant, a tautomer or a stereoisomer. The invention also provides a pharmaceutical composition containing the compound, and application of the pharmaceutical composition in treatment of diseases related to P2X3.

The application belongs to the technical field of short peptide medicine, and specifically discloses a Maged1 competitive short peptide and application thereof.The Maged1 competitive short peptide is short peptide MP1 or short peptide MP2, and the amino acid sequence is shown as SEQ ID No.1 or SEQ ID No.2.Experiments prove that the Maged1 competitive short peptide can compete with Maged1 to combine with P2X3 receptors, thereby inhibiting the activation of Maged1 on P2X3 receptors, and has a good clinical application prospect in the treatment of chronic pain.

The present application provides a new compound which effectively antagonizes P2X3 receptor, which is a compound shown in formula I, a tautomer, a stereoisomer, a hydrate, a solvate, a pharmaceutically acceptable salt or a prodrug thereof, a preparation method thereof, and a use thereof in the preparation of a medicine

A class of arylcarboxamide compounds, their preparation methods, and pharmaceutical uses. Specifically, the present invention relates to compounds represented by general formula (I), their preparation methods, and pharmaceutical compositions containing the compounds, as well as their use as P2X3 receptor antagonists, and for treating and / or preventing diseases associated with P2X3 receptor activity, such as chronic cough, pain, endometriosis, and overactive bladder. The definitions of the substituents in general formula (I) are the same as those in the specification.

The invention provides the solid dispersion containing the P2X3 receptor antagonist compound shown in the formula I. The solid dispersion can remarkably improve the solubility of the compound shown in the formula I, greatly improve the dissolution rate and bioavailability of the medicine and ensure the treatment effect of the medicine. Meanwhile, the solid dispersion disclosed by the invention is good in stability, does not generate crystal form transformation in a storage process, does not generate obvious growth of related substances, and improves the safety of clinical application of the medicine.

The present invention relates to a combination of selective blockers of TASK-1 and TASK-3 channels, in particular substituted imidazo[1,2-a]pyrimidine and substituted imidazo[1,2-a]pyridine derivatives of formula (I) and P2X3 receptor antagonists for the treatment and / or prophylaxis of sleep-related breathing disorders, preferably obstructive and central sleep apneas and snoring.

The present application provides a new compound which effectively antagonizes P2X3 receptor, which is a compound shown in formula I, a tautomer, a stereoisomer, a pharmaceutically acceptable salt thereof, a preparation method thereof, and a use thereof in the preparation of a medicine.

The invention discloses imidazopyridine derivatives as well as a preparation method, a pharmaceutical composition and application thereof, and belongs to the technical field of pharmaceutical synthesis. The technical problem to be solved is to provide a P2X3 receptor antagonist of an imidazopyridine derivative with a new structure, and the compound has good P2X3 selectivity, low toxicity, good metabolic stability and small taste influence, and has good prospects in treatment of P2X3 receptor dysfunction diseases, especially in treatment of neurogenic diseases. According to the key point of the technical scheme, the imidazopyridine derivative is selected from a compound as shown in a formula I or a racemate, a stereoisomer, a geometric isomer, a tautomer, nitrogen oxide, hydrate, an isotope label, a solvate, a polymorphic substance, a metabolite, ester, pharmaceutically acceptable salt or prodrug of the compound, wherein the formula I is shown in the specification.

The invention provides a heterocyclic compound as a P2X3 receptor inhibitor. The heterocyclic compound is a compound as shown in a formula (I), an isotope variant, a tautomer or a stereoisomer. The invention also provides a pharmaceutical composition containing the compound, and application of the pharmaceutical composition in treatment of diseases related to P2X3.

Provided is a solid dispersion containing a P2X3 receptor antagonist compound shown in formula I, which can increase the solubility of the compound shown in formula I, and improve the dissolution rate and bioavailability of the drug, ensuring the therapeutic effect of the drug. Meanwhile, the solid dispersion has good stability. During the storage process, the solid dispersion does not experience crystal form transformation and does not exhibit a significant increase in related substances, which improves the safety of the clinical use of the drug.

This invention, entitled "Imidazolopyridine Derivatives, Preparation Methods, Pharmaceutical Compositions, and Applications thereof," belongs to the field of pharmaceutical synthesis technology. The technical problem to be solved is to provide a novel imidazopyridine derivative P2X3 receptor antagonist. These compounds exhibit good P2X3 selectivity, low toxicity, good metabolic stability, and minimal impact on taste, showing great promise in treating P2X3 receptor dysfunction diseases, particularly neurogenic diseases. The key technical solution is an imidazopyridine derivative selected from compounds represented by Formula I or their racemic, stereoisomer, geometric isomer, tautomer, nitride, hydrate, isotope-labeled, solvate, polymorph, metabolite, ester, pharmaceutically acceptable salt, or prodrug: Formula I.