86 results about "Receptor modulator" patented technology

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):

Abstract GPCR Receptor Agonists, Pharmaceutical Compositions Containing Them, and Methods of Use Thereof The application provides GLP-1 receptor modulator compounds, pharmaceutical compositions, methods of administration thereof, and methods of use thereof for treatment and / or diagnosis. 010-9319-5532 / 1 / AMERICAS 010-9319-5532 / 1 / AMERICAS 48513847.1 1

The present disclosure provides azocino[4,5,6-cd]indoles as serotonin receptor modulators. Uses of said compounds in the treatment of medical disorders, such as neurological or psychiatric disorders, and processes of synthesizing said compounds are also provided.

Described herein, inter alia, are modulators of the Nurr1 receptor and uses thereof. In one aspect, provided is a method for treating a disease associated with dysregulation and / or degeneration of dopaminergic neurons of the central nervous system in a subject in need thereof, the method comprising administering to the subject in need thereof a therapeutically effective amount of a compound described herein.

The present disclosure provides compounds, such as compounds of Formula I, and their use in the treatment of medical diseases or disorders, such as psychiatric and nervous system diseases. Pharmaceutical compositions and methods of making various benzisoxazole and benzisothiazole compounds are provided. These compounds are considered to be modulators of the serotonin 2A (5-HT2A) receptor.

The present disclosure provides compounds, such as compounds of Formula I, and their use in the treatment of medical diseases or disorders, such as psychiatric and nervous system diseases. Pharmaceutical compositions and methods of making various benzisoxazole and benzisothiazole compounds are provided. These compounds are considered to be modulators of the serotonin 2A (5-HT2A) receptor.

This invention discloses compounds of Formula I or pharmaceutically acceptable salts thereof. Compounds of Formula I exhibit excellent S1PR1 receptor modulatory activity and high selectivity, thereby effectively avoiding potential cardiovascular toxicity while exerting immunomodulatory effects. The compounds and pharmaceutical compositions of this invention lay a solid chemical and biological foundation for the development of next-generation drugs targeting autoimmune diseases and specific malignant tumors, demonstrating promising clinical application prospects, social benefits, and potential industrialization value.

The present invention relates to a steroid derivative regulator, in particular to a compound of formula (I), a salt and crystal form thereof, a preparation method therefor, a pharmaceutical composition containing a therapeutically effective amount of the crystal form, and an application thereof as a GABAA receptor regulator in treatment of depression, convulsions, Parkinsonism and nervous system diseases.

The present disclosure provides compounds, such as compounds of Formula I, and their use in the treatment of medical diseases or disorders, such as psychiatric and nervous system disorders. Pharmaceutical compositions and methods of making various tetrahydropyridine and piperidine compounds are provided. The compounds are expected to be modulators of the serotonin 2A (5-HT2A) receptor.

Disclosed herein are methods for treating an ocular surface disorder by administering a therapeutically effective amount of at least one lysophosphatidic acid receptor (LPAR) modulator to a subject.

The present invention provides compounds of formula (I) and / or salts thereof and / or biologically active metabolites thereof and / or prodrugs thereof and / or solvates thereof and / or hydrates thereof and / or polymorphs thereof having affinity and selectivity for the gamma-aminobutyric acid A receptor subunit alpha 5 and act as GABAA α5 positive allosteric modulators, thereby useful in the treatment or prevention of diseases related to the GABAA α5 receptor, process for the preparation and intermediates of the preparation process thereof, pharmaceutical compositions comprising them alone or in combination with one or more other active ingredients and their use as medicaments.

The present invention provides compounds of formula (I) and / or salt thereof and / or biologically active metabolite thereof and / or prodrug thereof and / or solvate thereof and / or hydrate thereof and / or polymorph thereof having affinity and selectivity for the gamma-aminobutyric acid A receptor subunit alpha 5 and act as GABAA α5 negative allosteric modulators, thereby useful in the treatment or prevention of diseases related to the GABAA α5 receptor, process for the preparation and intermediates of the preparation process thereof, pharmaceutical compositions comprising them alone or in combination with one or more other active ingredients and their use as medicaments.

The present disclosure relates to compounds useful as modulators of proton-activated G protein-coupled receptors, and pharmaceutical compositions comprising same. The present disclosure also relates to methods of using such compounds and pharmaceutical compositions for the treatment and / or prevention of diseases, disorders or conditions mediated by proton-activated G pro-tein-coupled receptors.

Processes for preparing (((3aR,6aS)-5-(4,6-dimethylpyrimidin-2-yl)hexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl)(2-fluoro-6-(2H-1,2,3-triazol-2-yl)phenyl)methanoneare described, which are useful for commercial manufacturing. Said compound is an orexin receptor modulator and may be useful in pharmaceutical compositions and methods for the treatment of diseased states, disorders, and conditions mediated by orexin activity, such as insomnia and depression.

To provide a method and a computing device that allow for more effective determination regarding which patients will experience drug efficacy, and which patients will experience adverse drug events, and that provide personalized recommendations for patients regarding dose, the frequency of drug administration, and drug choice.SOLUTION: A method for identifying patients diagnosed with treatment resistant or refractory depression, pain or other clinical indications, who are eligible to receive N-methyl-D-aspartate receptor antagonist, glycine receptor beta modulator, or α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor-based therapies.SELECTED DRAWING: None

The present invention relates to compounds of formula (I), their synthesis and use as modulators of the CCR6 receptor for the prevention or treatment of, for example, inflammatory / autoimmune diseases / disorders and cancer.

Disclosed in the present invention is a compound having significant Apelin receptor modulation activity, and specifically disclosed is a compound represented by the following formula (I), or a pharmaceutically acceptable salt, solvate, hydrate, isotopologue, or isomer thereof.

This invention discloses substituted pyrazolopyridine as a GluN2B receptor ligand. Such compounds can be used in pharmaceutical compositions and methods for treating disease states, disorders, and conditions mediated by GluN2B receptor activity, including those involving GluN2B receptor modulation and neutralization.

The present disclosure relates to oral compositions that include at least two agents selected from: agents that increase the concentration of glutamate; agents that increase dopamine production; agents that increase the concentration of brain-derived neurotrophic factor (BDNF); NMDA and / or AMPA receptor modulators; and acetylcholinesterase inhibitors. In son embodiments, a composition as provided herein includes D-glutamine present in an amount of about 20% to about 30% w / w of the composition; ginkgolide B present in an amount of about 0.1% to about 0.4% w / w of the composition; phosphatidylserine present in an amount of about 65% to about 80% w / w of the composition; and ascorbic acid present in an amount of about 0.5% to about 2.5% w / w of the composition. Such compositions are useful for improving memory and / or focus.

The present invention relates to compounds of Formula (I), their synthesis and use as CCR6 receptor modulators for the treatment or prevention of various diseases, conditions or disorders.

This application relates generally to toll like receptor modulator compounds and pharmaceutical compositions which, among other things, modulate toll-like receptors (e.g. TLR8), and methods of making and using them.

The present disclosure provides compounds, such as compounds of Formula I, and their use in the treatment of medical diseases or disorders, such as psychiatric and nervous system disorders. Pharmaceutical compositions and methods of making various piperidine compounds are also provided. These compounds are expected to be modulators of the serotonin 2A (5-HT2A) receptor.

This specification discloses small molecule follicular-stimulating hormone (FSH) receptor modifiers, methods for producing them, and therapeutic methods using them.

Provided herein are compositions relating to psychedelics and serotonin receptor modulators. Further provided herein are methods of suppressing or halting hallucinogenic effects of a psychedelic and methods of treating a disease or disorder (e.g., depression or diseases or disorders related to depression) comprising administering psychedelics and serotonin receptor modulators.

The present invention provides a method for the treatment of GABAergic steroids having affinity and selectivity for the gamma-aminobutyric acid A receptor subunit alpha 5. A Acts as a positive allosteric regulator of α5, thereby increasing the GABA A Provided are compounds of formula (I), and / or salts thereof, and / or biologically active metabolites thereof, and / or prodrugs thereof, and / or solvates thereof, and / or hydrates thereof, and / or polymorphs thereof, processes for their preparation and intermediates in the preparation processes, pharmaceutical compositions containing them alone or in combination with one or more other active ingredients, and their use as medicaments, which are useful in the treatment or prevention of diseases associated with the α5 receptor. [Formula 1] TIFF2023520647000122.tif46170

Disclosed herein, inter alia, methods of synthesis of trans isomeric forms of G protein-coupled receptor modulators of high trans isomeric purity.

Provided herein are compositions and methods for treating a disease or disorder using a therapeutically effective amount of an N-methyl-D-aspartate (NMDA) receptor modulator and a therapeutically effective amount of a target of rapamycin (mTOR) inhibitor.

The present application discloses the use of SUR2 receptor modulators. In the present application, SUR2 receptor modulators (e.g. MLC1) can be combined with skeletal muscle cell K ATP SUR2 specific binding on potassium ion channel, thus enhancing intracellular calcium signal, increasing glucose uptake of skeletal muscle cell and reducing blood glucose, and thus can be used as a therapeutic drug for diabetes; SUR2 receptor modulators selectively bind to SUR2 through a non-islet β cell dependent mechanism, and have no inhibitory effect on islet β cell SUR1 receptor, and thus can effectively avoid hypoglycemia while reducing blood glucose, and have small side effects.

This disclosure relates to serotonin receptor modulators, including conformationally constrained serotonin receptor agonists, and methods of making and using the same are disclosed herein.