167 results about "Muscarinics" patented technology

The invention belongs to the technical field of synthetic chemistry, and provides a muscarinic acetylcholine receptor 3 fluorescent probe as well as a preparation method and application thereof. The chemical structural formula of the fluorescent probe is shown in the specification, and the fluorescent probe can be used for M3 receptor tracing in cells or organisms. The probe provided by the invention has a good fluorescent property and can be influenced by the polarity and viscosity of an external environment; and the probe has good biocompatibility, and the IC50 of the probe is 43 times of the concentration of a working solution, so that the probe can meet the requirements of cell fluorescence imaging. In the aspect of cell fluorescence imaging, the probe can realize selective fluorescence labeling of the M3 receptor in the cell, washing is not needed in the dyeing process, and the operation is simple and convenient, so that visual research on positioning of the M3 receptor in the cell is realized.

A topical ophthalmological composition includes a muscarinic receptor antagonist as an active pharmaceutical ingredient; and medium chain triglycerides (MCTs) or light liquid paraffin oil as liquid vehicle. The topical ophthalmological composition treats an ocular disease.

The invention belongs to the technical field of pharmaceutical composition pellet preparations, and particularly relates to a double-drug co-loaded oral pellet preparation with a multilayer core-shell structure as well as a preparation method and application of the double-drug co-loaded oral pellet preparation. According to the double-drug co-loaded oral pellet preparation provided by the invention, through the design of a multi-layer core-shell structure, the oral pellet preparation has microenvironment regulation and time difference release synergy, namely the peripheral antagonist trospium chloride on the outermost layer is preferentially released and acts on a peripheral muscarinic receptor (M1 / M4); the xanomeline of the pellet core is subjected to post-release or pulse release and acts on a peripheral receptor (M2 / M3), so that the curative effect and side effect inhibition of the two drugs form time difference synergy, peripheral adverse reactions caused by xanomeline can be reduced, and the problem of synergy in combined administration of xanomeline and an antagonist trospium chloride is solved.

The invention provides therapeutic methods, pharmaceutical compositions, and unit dose formulations for treating movement disorders, such as using a muscarinic acetylcholine receptor inhibitor in combination with a muscarinic acetylcholine receptor activator to treat dystonia. In some aspects, the invention provides a method of treating a movement disorder in a patient, where the method comprises administering to a patient in need thereof (i) a muscarinic acetylcholine receptor inhibitor in an amount effective to treat the movement disorder and (ii) a muscarinic acetylcholine receptor activator in an amount effective to reduce the frequency and / or magnitude of at least one side effect of the muscarinic acetylcholine receptor inhibitor, to thereby treat the movement disorder.

The invention discloses a deuterated 2-(azetidine-3-yl) ethanone compound as well as a pharmaceutical composition and application of the deuterated 2-(azetidine-3-yl) ethanone compound. The deuterated 2-(azetidine-3-yl) ethanone compound has the structural characteristics of a formula (I), and the definition of each group in the formula (I) is shown in the specification. The compound shown in the formula (I) can be used as a muscarinic M4 receptor positive allosteric modulator, and compared with Emraclidine (CV-231), the compound shown in the formula (I) has better pharmacokinetic characteristics and higher safety. # imgabs0 #

The invention relates to a CHRM4 receptor agonist and application thereof. The invention discloses a compound shown as a formula (I), or a stereoisomer, a deuterated compound, a solvate, a co-crystal or a pharmaceutically acceptable salt of the compound, a pharmaceutical composition of the stereoisomer, the deuterated compound, the solvate, the co-crystal or the pharmaceutically acceptable salt, and application of the stereoisomer, the deuterated compound, the solvate, the co-crystal or the pharmaceutically acceptable salt in preparation of drugs for treating / preventing CHRM4-mediated diseases, and all groups in the formula (I) are defined as in the specification.

The present application relates to a kind of thieno [2, 3-c] pyridazine derivatives, and its isotope form, stereoisomer, tautomer, cis-trans isomer, pharmaceutically acceptable salt, pharmaceutically acceptable solvate, hydrate, prodrug and polymorph, these compounds can be used as cholinergic M4 receptor positive allosteric modulator, it has good application prospect in preparation for preventing and / or treating the drug for the disease related to abnormal muscarinic acetylcholine receptor.

In one aspect, the present application provides azabicyclo and diazepine derivatives useful as muscarinic receptor modulators. In another aspect, the present application provides pharmaceutical compositions for the treatment of ocular diseases, the compositions comprising at least one muscarinic receptor modulator. Formulas (I) and (II):

To provide compounds which are useful as antagonists of the muscarinic acetylcholine receptor M1 (mAChR M1), and methods for preparing the compounds.SOLUTION: The present invention provides a compound having the structure of formula (IA) or (IB), or a pharmaceutically acceptable salt or solvate thereof.SELECTED DRAWING: None

The application provides a preparation method and application of a sterile inhalation suspension containing a PDE-4 or PDE-3 / 4 inhibitor. The preparation method comprises dispersing the PDE-4 or PDE-3 / 4 inhibitor in injection water containing an excipient, high-pressure wet heat sterilization to obtain a PDE-4 or PDE-3 / 4 inhibitor dispersion; further comprising dissolving a long-acting beta2-receptor agonist and / or a long-acting muscarinic receptor antagonist, sterile filtration to obtain a mixed solution; mixing the PDE-4 or PDE-3 / 4 inhibitor dispersion with the mixed solution, dispersing and sterilely filling. The pharmaceutical preparation prepared by the application is a sterile inhalation suspension, the sterile inhalation suspension containing the PDE-4 or PDE-3 / 4 inhibitor has high bioavailability, good patient medication compliance and good preparation stability.

Disclosed in the present invention are nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof, a preparation method therefor, and the use thereof. Provided in the present invention are compounds represented by formula I or pharmaceutically acceptable salts thereof. The compounds of the present invention can be used as positive allosteric modulators of muscarinic receptors. The compounds of the present invention can be used for treatment of M receptor-mediated (or M receptor-related) diseases.

5, 6, 7, 8-tetrahydro-1, 6-naphthyridines and derivatives thereof, which are substituted in the 6 position with 6, 7-dihydro-5H-pyrrolo [3, 4-b] pyridin-5-one, furo [3, 4-b] pyridin-5 (7H)-one, 6, 7-dihydro-5H-cyclopenta [b] pyridin-5-one, or [1, 2, 4] triazolo [4, 3-a] pyrimidine-3 (2H)-one, are positive allosteric modulators of muscarinic acetylcholine receptor M4 (mAChR M4), and can be used for treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction.

Disclosed are compounds of formula (I) wherein G1 is as antagonists of the muscarinic acetylcholine receptor M4 (mAChR M4) for use in the treatment of e.g. a neurodegenerative disorder, a movement disorder, or a brain disorder, such as e.g. Parkinson's disease, drug-induced Parkinsonism, dystonia, Tourette's syndrome, dyskinesias, schizophrenia, cognitive deficits associated with schizophrenia, excessive daytime sleepiness, attention deficit hyperactivity disorder (ADHD), Huntington's disease, chorea, cerebral palsy, and progressive supranuclear palsy. An exemplary compound is e.g. (2,5-difluoro-4-(6-(((3aR,5s,6aS)-2-((tetrahydro-2H-pyran-4-yl)methyl)octahydrocyclopenta[c]pyrrol-5-yl)amino)pyridazin-3-yl)phenyl)(imino)(methyl)-λ6-sulfanone (e.g. example 12; compound no. 7) Pharmacological data on the activity of the compounds in an mAChR M4 cell-based assay are provided (e.g. table 2).TABLE 2Human M4Cpd. No.IC50 (nM)Emin (%)*113.44239.62318.5345846575.4361883746.0385607918.43101.821186.231243.42138.63*% ACh maximum at 30 μM.

The present invention relates to novel compounds of Formula (I'), wherein P, Q, A, B, m, n, R1, R2, R9, R10, R11 and R12 are defined as in Formula (I'). These compounds may be useful as muscarinic M4 receptor subtype ("M4-mAChR") positive allosteric modulators which are useful for the treatment or prevention of neurological and psychiatric disorders associated with muscarinic M4 receptor dysfunction and diseases in which the M4 receptor is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes of preparing such compounds and such compositions, and to the use of such compounds for the prevention or treatment of neurological and psychiatric disorders and diseases such as for example, cognitive decline, both positive and negative symptoms in schizophrenia as well as other disorders modulated by M4 muscarinic receptors.

In general, the invention relates to pharmaceutical compositions comprising a norepinephrine reuptake inhibitor (NRI), muscarinic receptor antagonist, and carbonic anhydrase inhibitor and methods of treating Sleep Apnea comprising the administration of these pharmaceutical compositions.

6, 7-dihydrothiazolo [5, 4-c] pyridines substituted in position 5 by a heterocyclic ring are positive allosteric modulators of muscarinic acetylcholine receptor M4 (mAChR M4) and are useful in the treatment of neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction.

Provided herein are compounds of the following Formula (I): or a pharmaceutically acceptable salt thereof. Methods for treating a diseases, disorders, or symptom by antagonizing muscarinic receptors, including specifically antagonizing muscarinic receptor 4 (M4), are also provided.

The application discloses a kind of compound oral muscarine antipsychotic drug compositions and preparation method thereof, belong to pharmaceutical composition technical field, its technical scheme main point is a kind of compound oral muscarine antipsychotic drug compositions, the pharmaceutical composition is the composition containing two active ingredients, the composition containing two active ingredients is the combination of xanthomelin tartrate microtablet and trospium chloride microtablet, after two active ingredients are made into microtablet respectively, while guaranteeing that product can be released faster, can also increase the time of drug retention in stomach, significantly increase the penetration absorption of drug in body, reduce the fluctuation of blood drug concentration caused by the inconsistent drug release absorption behavior after each administration, so as to better play a role in body, in addition, the technical scheme in the application does not use complex production process, reduces the process development threshold, significantly increases the process reproducibility and stability.

The invention relates to a CHRM4 receptor agonist and application thereof. The invention discloses a compound shown as a formula (I), or a stereoisomer or a pharmaceutically acceptable salt thereof, a pharmaceutical composition of the compound and the stereoisomer or the pharmaceutically acceptable salt, and application of the compound and the pharmaceutical composition in preparation of drugs for treating / preventing CHRM4-mediated diseases, and all groups in the formula (I) are defined as in the specification.

The invention belongs to the field of pharmaceutics, particularly relates to a composition containing levosalbutamol hydrochloride and ipratropium bromide as well as a preparation method and application of the composition, and overcomes the defects of a stabilizer disodium ethylene diamine tetraacetate adopted in the prior art. The invention provides a levosalbutamol hydrochloride and ipratropium bromide composition which is simpler in prescription and better in safety, can be used for treating reversible bronchospasm related to airway obstructive diseases, can jointly act on muscarinic acid and beta2 adrenergic receptors in the lung, can enhance the bronchiectasia effect, takes effect quickly, and is free of toxic and side effects. The clinical application value is very high.

The present invention provides an ocular drug delivery method comprising the method step of topically administering to the skin of the eyelids of a subject a therapeutically effective amount of a pharmaceutical composition, wherein the pharmaceutical composition comprises: (a) a therapeutically active agent comprising a muscarinic acetylcholine receptor (mAChRs) modulator; and (b) a pharmaceutically acceptable carrier.

The present invention relates to an (aminomethyl)cyclohexane derivative useful as a medicine, a pharmaceutically acceptable salt thereof, a pharmaceutical composition containing the same as an active ingredient, or a therapeutic and / or prophylactic agent for a disease mediated by antagonism of the muscarinic M4 receptor.

The invention relates to a combination of sabcomeline, or a pharmaceutically acceptable salt thereof, and a non-Central Nervous System penetrant muscarinic antagonist, wherein the daily dose provided by the combination of the non-Central Nervous System penetrant muscarinic antagonist is no more than 20 mg. The invention further relates to pharmaceutical compositions comprising the combination of sabcomeline, or a pharmaceutically acceptable salt thereof, and a non-Central Nervous System penetrant muscarinic antagonist and uses thereof.

The invention discloses an application of a compound Darifenacin hydrobromide in preparation of a medicine for resisting influenza A (H1N1) virus, and belongs to the technical field of medicines. The invention discloses for the first time that Darifenacin hydrobromide can significantly inhibit replication of H1N1-PR8 virus, reduce virus titer and reduce cytopathic effect (CPE) in an in-vitro cell model, the EC50 value of Darifenacin hydrobromide is 2.5 [mu] M, and the selection index (SI) is gt; and 10, the compound has good antiviral activity and safety. The compound Darifenacin hydrobromide is a high-selectivity M3 muscarinic acetylcholine receptor antagonist and is approved to be used for treating overactive bladder at present, the invention discloses that the compound can inhibit replication and release of H1N1-PR8 virus for the first time, and the compound has a wide prospect of being developed into a medicine for treating human influenza virus infection.

The present invention relates to compounds of formula (Ia), pharmaceutically acceptable salts of compounds of formula (Ia), and pharmaceutical compositions thereof that modulate the activity of the muscarinic acetylcholine receptor M4. The compounds, pharmaceutical salts of compounds, and pharmaceutical compositions of the present invention are directed to methods useful in the treatment or prophylaxis of a neurological disease, disorder, or symptom, and conditions related thereto.

Provided herein, inter alia, are compounds which are useful as antagonists of the muscarinic acetylcholine receptor M1 (mAChR M1); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions.

The present invention relates to a plurality of engineered variants based on muscarinic toxin MT3 which specifically bind to muscarinic acetylcholine receptor M4 or adrenergic receptor alpha 2A, preferably human muscarinic acetylcholine receptor M4 or human adrenergic receptor alpha 2A.