97 results about "Muscarinics" patented technology

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):

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.

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.

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 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.

To regulate the number of peripheral regulatory T cells in the intestinal tract and to provide a new means for treating diseases associated with the cells.SOLUTION: A therapeutic agent for a disease, comprising a substance having an effect of regulating the amount of peripheral regulatory T cells in the intestinal tract, wherein the substance is a substance that activates or suppresses the hepatic vagal afferent pathway, a substance that activates or suppresses the left vagal efferent pathway, or an agonist or antagonist of a muscarinic acetylcholine receptor.SELECTED DRAWING: None

Disclosed herein are cyclopropylpiperidine compounds, which may be useful as antagonists of the muscarinic acetylcholine receptor M4 (niAChR M4). Also disclosed herein are methods of making the compounds, pharmaceutical compositions comprising the compounds, and methods of treating disorders using the compounds and compositions.

The present invention provides therapeutic methods, pharmaceutical compositions and unit dose formulations for the treatment of dyskinesia, such as the treatment of muscular dyskinesia using a muscarinic acetylcholine receptor inhibitor in combination with a muscarinic acetylcholine receptor activator.

Methods and compositions for the treatment of conditions associated with pharyngeal airway muscle collapse while the subject is in a non-fully conscious state, e.g., sleep apnea and snoring, comprising administration of a norepinephrine reuptake inhibitor (NRI) and a muscarinic receptor antagonist.

The present invention provides substituted tetrahydropyrrolo-pyridone compounds, pharmaceutical compositions and their use in the treatment of muscarinic acetylcholine receptor mediated conditions.

The present invention provides ophthalmic formulations comprising long-acting beta-adrenergic receptor agonist (LABA) compounds, long-acting muscarinic antagonists (LAMA), and combinations thereof. Also provided are methods of treating visual impairment with LABA, LAMA, and combinations thereof.

Disclosed herein are methods of treating cancers of the central nervous system (e.g. CNS tumors) in a subject involving providing to the subject a muscarinic acetylcholine receptor M1 and / or a muscarinic acetylcholine receptor M3 antagonist to the subject. Further disclosed herein are co-cultures comprising cholinergic neurons and glioma cells that may be used for therapy screening / testing, and methods of producing the same.

The present application relates to dihydropyrrolo heterocyclic compounds of formula (I) which can be used to modulate the muscarinic M4 receptor and thus can be used to prepare pharmaceutical compositions.

Compounds shown in Formula (I), pharmaceutical compositions, and methods of using related to muscarinic acetylcholine receptors. The compounds herein are typically muscarinic acetylcholine receptor antagonists, such as M3 antagonists, which can be used for treating a variety of disorders, conditions or diseases such as hyperhidrosis.

Deuterium-labeled 4-((2,3-dihydrobenzo[b][1,4]dioxin-6-yl)oxy)piperidines substituted with pyrrolo[3,4-b]pyridin-5-one, furo[3,4-b]pyridin-5(7H)-one, or [1,2,4]triazolo[4,3-a]pyrimidin-3(2H)-one are positive allosteric modulators of the muscarinic acetylcholine receptor M4 (mAChR M4) and may have use in treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction.

The invention provides a muscarinic acetylcholine M4 receptor positive allosteric modulator as well as a preparation method and a pharmaceutical composition thereof. The invention also relates to application of the compound or the pharmaceutical composition in preparation of drugs for preventing or treating muscarinic acetylcholine M4 receptor mediated related diseases, wherein the diseases comprise Alzheimer's disease, Parkinson's disease, schizophrenia, pain, addiction and sleep disorder.