22 results about "Muscarinics" patented technology

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):

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 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.

N-Biarylmethylene substituted pyrrolopyridinone, pyrrolopyrazinone, pyrrolopyrimidinone, and isoindolin-1-one compounds having a tertiary alcohol-containing group substituted on the biarylmethylene are positive allosteric modulators of the muscarinic acetylcholine receptor M1 (mAChRM1). The compounds and pharmaceutical compositions may be used in treating neurological disorders, psychiatric disorders, or a combination thereof.

This invention relates to compounds that are agonists of the muscarinic M1 and / or M4 receptors useful in the treatment of diseases mediated by the muscarinic M1 and / or M4 receptors. Also provided are pharmaceutical compositions containing the compounds and the therapeutic applications of the compounds. Specifically, the present disclosure is related to compounds that are useful in treating pain, schizophrenia, Parkinson's disease, Alzheimer's disease, and other neuropsychiatric and neurodegenerative diseases.

The present application provides a new crystal form of the pamoate salt of zanomeline represented by formula (I) and a preparation method thereof, and the crystal form can be used for preparing a medicine for preventing and / or treating diseases improved by activating muscarinic receptors. (I)

A pharmaceutical composition comprises a muscarinic agonist and a pharmacokinetic (PK) modifier that changes the metabolic profile the muscarinic agonist. The pharmaceutical composition may be used for the treatment of a neurological disorder or condition in a subject.

6,7-dihydrothiazolo[5,4-c]pyridine, substituted at position 5 with 6,7-dihydro-5H-pyrrolo[3,4-b]pyridine-5-one or flu[3,4-b]pyridine-5(7H)-one, is a positive allosteric modulator of the muscarinic acetylcholine receptor M4 (mAChR M4) and may be used to treat neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction.

Crystalline forms of a muscarinic M4 receptor activator, Compound A, pharmaceutical compositions and combinations comprising those crystalline forms, their use in treating diseases or disorders and methods of producing the crystalline forms. Also provided are pharmaceutical compositions comprising a core comprising Compound A or a pharmaceutically acceptable salt or hydrate thereof, and a coating comprising an opacifier.

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.

Provided are a tetrahydropyridine derivative or a pharmaceutically acceptable salt thereof, a pharmaceutical composition containing same, a use thereof as a muscarinic receptor agonist, and a use thereof in the preparation of drugs for treating pains, central nervous system disorders, or diseases related to the pains and the central psychiatric disorders. The provided compound has the advantages of high selectivity for muscarinic receptors, no gender differences in pharmacokinetic parameters, minimal gastrointestinal adverse reactions, a wide therapeutic window, high drug safety, and a lower clinical dosage.

The present invention relates to methods of treating depression using a muscarinic acetylcholine receptor M1 antagonist.

The present disclosure provides methods and kits for treating or preventing brain atrophy in a subject. The methods involve administering a sigma-1 receptor agonist and / or a dual modulator of sigma-1 receptor and muscarinic receptor. The brain atrophy can be associated with or related to a neurological disorder.

This invention relates to CHRM4 receptor agonists and their uses. The present invention discloses compounds represented by formula (I), or their stereoisomers, deuterides, solvates, cocrystals or pharmaceutically acceptable salts, and pharmaceutical compositions thereof, as well as their uses in the manufacture of drugs for the treatment / prevention of CHRM4-mediated diseases, where each group in formula (I) is as defined in the specification. [C1] TIFF2026521193000480.tif19156

Provided in the present invention are a new crystal form of xanomeline pamoate represented by formula (I) and a preparation method therefor. The crystal form can be used for preparing a drug for preventing and / or treating diseases that are ameliorated by activating a muscarinic receptor.

The invention provides substituted tetrahydropyrrolo-pyridinone compounds, pharmaceutical compositions, and their use in treating muscarinic acetylcholine receptor mediated disorders.

The present invention provides ophthalmic acceptable formulations of atropine and other muscarinic acetylcholine receptor antagonists, which can be heat sterilized without significant degradation of the muscarinic acetylcholine receptor antagonists. The formulations are less acidic than previous muscarinic acetylcholine receptor antagonist ocular formulations, making them more comfortable when administered to the eye.

Disclosed are (pyrrolidin-3-yl)methyl)pyridazin-3-amine and (pyrrolidin-3-yl)methyl)pyridin-3-amine compounds substituted on the pyrrolidine nitrogen and the 6-position of the pyridazine or pyridine. The compounds are useful as antagonists of the muscarinic acetylcholine receptor M4 (mAChR M4). Also disclosed are methods of making the compounds, pharmaceutical compositions comprising the compounds, and methods of treating disorders using the compounds and compositions.