144 results about "Receptor modulator" patented technology

The present invention relates to compounds of formula (I), their synthesis and their use as CCR6 receptor modulators for the treatment or prevention of various diseases, conditions or disorders. [Formula 1] TIFF2023523300000191.tif51156

The present disclosure relates to compounds useful as proton activated G protein coupled receptor modulators and pharmaceutical compositions comprising the compounds. The present disclosure also relates to methods of using such compounds and pharmaceutical compositions to treat and / or prevent diseases, disorders or conditions mediated by proton activated G protein coupled receptors.

Alkoxy-substituted N-benzyl-2-phenylacetamide compounds and derivatives are G-protein coupled receptor (GPR) 88 modulators for use in the treatment of a disease mediated by GPR88. Indications include Tourette's Syndrome, Huntington's Disease (HD), Addiction, Parkinson's Disease (PD), Schizophrenia, and Attention Deficit Hyperactivity Disorder (ADHD), choreiform movements, speech delay, learning disabilities, depression, hyperkinetic movement disorders characterised by chorea and / or dystonia, psychosis, cognitive deficits in schizophrenia, affective disorders, bipolar disorder, Alzheimer's disease and basal ganglia disorders.

A compound for use in the treatment of itch is provided, wherein the compound comprises the general formula (1a), general formula (1b) or general formula (1c). The compounds of the invention are positive allosteric α2 and / or α3 GABAA receptor modulators.

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 invention relates to an insecticidal and acaricidal composition. The composition contains active component A and active component B, wherein the active component A is selected from compound I; the active component B is selected from one or more of bionic juvenile hormones, chitin biosynthesis inhibitors affecting CHS1, type-1 chitin biosynthesis inhibitors, ecdysone receptor agonists, nicotinic acetylcholine receptor competitive modulators, ryanodine receptor modulators, nicotinic acetylcholine receptor allosteric modulators, glutamate-gated chloride channel allosteric modulators, sodium channel modulators, voltage-dependent sodium channel blockers, inhibitors, trifluoroethyl sulfide acaricides, other insecticides and acaricides, etc.; and the active component A has a structure as follows. The composition of the present invention has advantages such as obvious synergistic effects and delayed resistance development, and can be used for controlling a variety of pests.

Compounds are provided having the structure of Formula (I): or a pharmaceutically acceptable salt, homolog, hydrate or solvate thereof, wherein R is as defined herein. Such compounds serve as modulators of the sphingosine-1-phosphate receptor, and have utility for treatment of a malcondition for which activation of this receptor is medically indicated.

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.

Provided herein are GLP-1 receptor modulator compounds, pharmaceutical compositions, methods of their preparation, and methods of their use in treatment, and / or diagnosis.

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 invention relates to a steroidal compound as well as a preparation method and application thereof. Specifically, the invention provides a compound shown as a general formula (I), a stereoisomer or pharmaceutically acceptable salt of the compound, a preparation method of the compound, a pharmaceutical composition containing the compound and application of the compound as a GABAa receptor modulator to treatment of CNS-related diseases.

The present invention relates to the preparation of a SIP receptor modulator tauzimod ((R)-5-(2, 5-dichloro-4-(5-(8-chloro-6-(trifluoromethyl) imidazo [1, 2-a] pyridin-2-yl)-1, 2, 4-oxadiazol-3-yl) phenoxy) piperidin-2-one), and chemical intermediates used in the synthesis process of the SIP receptor modulator tauzimod ((R)-5-(2, 5-dichloro-4-(5-(8-chloro-6-(trifluoromethyl) imidazo [1, 2-a] pyridin-2-yl)-1, 2, 4-oxadiazol-3-yl) phenoxy) piperidin-2-one).

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.

Disclosed herein are GABA receptor antagonists for the treatment of epileptic conditions. A Receptor Modulators and GABA A Also disclosed herein are compositions comprising the GABA receptor modulators described herein. A A method of treating an epileptic condition in a subject by administering a receptor modulator or composition.

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.

To provide: compounds useful in treating central nervous system diseases and other diseases; pharmaceutical compositions; and processes for the manufacture of the same.SOLUTION: The present invention relates to: difluoromethyl-pyridin-2-yl triazoles of general formula (I), which are modulators of GABAA receptors containing the α5 subunit; pharmaceutical compositions containing the compounds; and processes for the manufacture of the compounds.SELECTED DRAWING: None

The invention provides a method of assessing the appropriate therapeutic dose of 1-{4-[1-(4-cyclohexyl-3-trifluoromethyl-benzyloxyimino)-ethyl]-2-ethyl-benzyl}-azetidine-3-carboxylic acid to administer to a patient in need thereof, comprising the steps of:(i) testing whether or not the patient has the poor metabolizer genotype; and(ii) if the patient does not have the poor metaboliser genotype, administering 1-{4-[1-(4-cyclohexyl-3-trifluoromethyl-benzyloxyimino)-ethyl]-2-ethyl-benzyl}-azetidine-3-carboxylic acid, or a pharmaceutically acceptable salt thereof, to the patient at the standard therapeutic dose; and(iii) if the patient does have the poor metaboliser genotype, either(a) administering 1-{4-[1-(4-cyclohexyl-3-trifluoromethyl-benzyloxyimino)-ethyl]-2-ethyl-benzyl}-azetidine-3-carboxylic acid, or a pharmaceutically acceptable salt thereof, to the patient at a therapeutic dose below that of the standard therapeutic dose; or(b) not administering 1-{4-[1-(4-cyclohexyl-3-trifluoromethyl-benzyloxyimino)-ethyl]-2-ethyl-benzyl}-azetidine-3-carboxylic acid, or a pharmaceutically acceptable salt thereof, to the patient.

The invention relates to imidazopyridazine derivatives as well as a preparation method, a pharmaceutical composition and application thereof. The invention provides a compound as shown in a formula (1), and a stereoisomer, a tautomer, a prodrug, a pharmaceutically acceptable salt, an amorphous substance, an isotopic body, a polymorphic substance or a solvate thereof. The present invention relates to compounds of general formula (I) wherein R1, R2 and R3 are as defined in the specification, pharmaceutical compositions containing the compounds and the use of the compounds as GABAA receptor modulators.

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.

Disclosed herein are small molecule follicle stimulating hormone (FSH) receptor modulators, methods of making the same, and methods of treatment using the same.