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192 results about "Allosteric modulator" patented technology

In pharmacology and biochemistry, allosteric modulators are a group of substances. Some of them, like benzodiazepines, are drugs. A modulator binds to a site in some receptor. This site (i.e., an allosteric site) is not the same one to which an endogenous activator of the receptor would bind (i.e., an orthosteric site). This natural activator could be a neurotransmitter. Receptor activators and inactivators are called agonists. Modulators are either positive, negative or neutral. Positive types increase and negative types lower the probability that an agonist will bind to a receptor (i.e. affinity) and/or its ability activate/inactivate the receptor (i.e. efficacy). Neutral types don't affect agonist activity, but can stop other modulators from binding to a receptor. Some modulators also works as allosteric agonists. Modulators and agonists can be called receptor ligands.

Deuterated 2-(azetidine-3-yl) ethanone compound as well as pharmaceutical composition and application thereof

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 #
Owner:YICHANG HUMANWELL PHARMA CO LTD

Azetukalner for use in the treatment of depression, anhedonia or a seizure disorder such as epilepsy in pediatric subjects

In certain embodiments, the present disclosure is directed to methods for treating disorders, including depressive disorders, seizure disorders, and anhedonia, in a pediatric subject, wherein the methods comprise orally administering a therapeutically effective amount of the voltage-gated potassium channel allosteric modulator, A-[4-(6-fluoro-3,4-dihydro-1H-isoquinolin-2-yl)-2,6- dimethylphenyl]-3,3-dimethylbutanamide (azetukalner), or a pharmaceutically acceptable salt thereof, to the pediatric subject, for example, under fed conditions.
Owner:XENON PHARMACEUTICALS INC

Allosteric agonists and positive allosteric modulators of glucagon-like peptide 1 receptor

The present disclosure relates to the discovery of small molecule compounds that act as GLP-1R agonists and / or as positive allosteric modulators (PAMs) of GLP-1R. Such compounds are useful to treat, ameliorate, and / or prevent insulin resistance and / or diabetes in a mammal.
Owner:SAINT JOSEPHS UNIV

Novel 6-membered ring heterocyclic compounds as gabab positive allosteric modulators

PCT designated stageWO2026068765A1Nervous disorderOrganic chemistryDiseaseReceptor
The present invention relates to novel compounds of Formula (I), wherein P, Q, A, B, m, n, R1, Z, J and L are defined as in Formula (I); which are gamma-(y)-aminobutyric acid type B receptor ("GABAB-R") positive allosteric modulators which are useful for the treatment or prevention of neurological and psychiatric disorders associated with GABA dysfunction and diseases in which the GABAB 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 in which GABAB-R is involved.
Owner:ADDEX PHARMACEUTICALS SA

Squaramide derivatives as cb1 allosteric modulators

Squaramide-based cannabinoid 1 receptor (CB1R) allosteric modulators are described. Exemplary analogs may provide improved potencies and pharmacokinetic properties. Methods of using the analogs to treat diseases mediated by CB1R, such as substance abuse and obesity, are described.
Owner:RES TRIANGLE INST

Thieno[2,3-c]pyridazine derivatives as positive allosteric modulators of cholinergic m4 receptors

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.
Owner:南京雷正医药科技有限公司

Indole allylamine amide derivative as well as preparation method and application thereof

The invention belongs to the field of medicinal chemistry, and relates to an indole allylamine amide derivative as well as a preparation method and application thereof. Functional activity screening of G protein dependent signaling pathways is carried out on all the synthesized compounds, and it is found that the new derivatives can be used for preparing beta2-adrenergic receptor allosteric antagonism regulator drugs. Trans-indole allylamine is used as a raw material, amide coupling is performed to obtain the novel indole allylamine amide derivative, and R1 is any one of phenyl, m-methylbenzene, m-methoxyphenyl, m-bromophenyl, m-chlorphenyl, m-fluorophenyl, o-methoxyphenyl, p-methoxyphenyl, naphthalene ring, oxazole, cyclohexyl, cyclopentyl, methyl, ethyl and isopropyl. A biological activity test result shows that the indole allylamine amide derivative disclosed by the invention has relatively good antagonistic activity on beta2AR and can be used for carrying out negative allosteric regulation on the functional activity of isoproterenol.
Owner:CHANGZHOU UNIV

Allosteric modulators of inhibitory immune receptor complexes

This disclosure relates to an immunoglobulin single variable domain (ISVD)-containing modulator that allosterically binds to a three-dimensional (3D) epitope of a protein complex comprising at least one inhibitory immune receptor and at least one corresponding ligand. The modulator regulates cooperativity within such complexes, thereby affecting the binding affinity and downstream signaling pathways. Specifically, the allosteric modulator of this invention induces positive cooperativity in immunoinhibitory receptor-ligand complexes, thus suppressing immune responses in a spatiotemporally restricted manner. Accordingly, these allosteric modulators are useful as therapeutic agents for inflammatory diseases, such as autoimmune diseases, allergic diseases, or graft-versus-host disease (GVHD). Moreover, this disclosure pertains to methods for identifying, selecting, and producing said allosteric modulators.
Owner:VLAAMS INTERUNIVERSITAIR INST VOOR BIOTECHNOLOGIE VZW +1

Human beta-glucocerebrosidase binders and uses thereof

This application relates to polypeptide agents and compositions specifically binding human beta-glucocerebrosidase (GCase, GBA1). Particularly, immunoglobulin single variable domains (ISVDs) are described which allosterically bind human GCase, thereby positively modulating GCase in its stability and / or catalytic activity. The invention relates further to vectors and nucleic acids encoding such ISVD-based modulators. Also encompassed are compositions, in particular pharmaceutical compositions, containing such ISVD modulators. The GCase-specific allosteric modulators, specifically the ISVDs and compositions described herein, may be used for prevention and / or treatment of GCase-related diseases, including Gaucher disease (GD) and Parkinson's disease (PD).
Owner:VLAAMS INTERUNIVERSITAIR INST VOOR BIOTECHNOLOGIE VZW +2

Negative allosteric modulators of metabotropic glutamate receptor 2

PCT designated stage expiredWO2024182692A8Nervous disorderOrganic chemistryMetabotropic glutamate receptor 2Compulsive disorders
Described are 6-aryl isoindolin-1-ones as negative allosteric modulators of metabotropic glutamate receptor 2 (mGlu2), pharmaceutical compositions including the compounds, and methods of using the compounds and compositions for treating depression, anxiety, obsessive-compulsive disorder, cognitive disorders, Alzheimer's disease, or autism spectrum disorders in a subject.
Owner:VANDERBILT UNIV

Insecticidal and acaricidal composition

PCT designated stageWO2025209606A1BiocideAnimal repellantsRyanodine receptorSKELETAL MUSCLE RYANODINE RECEPTOR
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.
Owner:SHANDONG MEIYANG BIO-TECHNOLOGY CO LTD

Azapeptide compounds derived from melanocyte-stimulating hormone release-inhibiting factor-1 and a method to obtain the same

PCT designated stageWO2026133155A1Nervous disorderPeptide/protein ingredientsMelanocyteMelanophore-dispersing hormone
The present application relates to azapeptide compounds of formula (I) derived from melanocyte-stimulating hormone release-inhibiting factor-1. A method to obtain compounds of formula (I) is also described herein. The compounds of formula (I) have been shown to be suitable for the treatment of dopamine-related disorders of the central nervous system. These compounds showed enhanced potency as positive allosteric modulators of the dopamine D2 receptors in comparison with the melanocyte-stimulating hormone release- inhibiting factor-1 and, in general, do not exhibit meaningful cytotoxicity.
Owner:UNIVERSIDADE DO PORTO +3

MGluR5 micromolecule allosteric modulator and application thereof in inhibition of neuroinflammation

The invention discloses an mGluR5 small-molecule allosteric modulator and application thereof in inhibition of neuroinflammation, and belongs to the technical field of neuropharmacology and anti-inflammatory drug research, two mGluR5 small-molecule allosteric modulators are obtained by virtual screening through an allosteric pocket targeting mGluR5, the structural formulas of the two mGluR5 small-molecule allosteric modulators are shown in the specification, and the structural formula of the mGluR5 small-molecule allosteric modulators is shown in the specification. The mGluR5 micromolecule allosteric modulator can be used for inhibiting microglial cell inflammation, and can effectively relieve LPS-induced microglial cell NO release.
Owner:MACAO POLYTECHNIC INST

Therapeutic formulations and uses thereof

This invention relates to formulations of compound (I) (BNC2IO), an allosteric modulator of the a7-nicotinic receptor with non-sedative anxiolytic effects; specifically, solid dispersions, methods of manufacture thereof, and therapeutic methods and uses in the treatment of diseases of the central nervous system thereof.
Owner:BONOMICS LTD

Method for measuring alpha value of muscarinic M1 receptor positive allosteric modulators

The present invention provides a useful and efficient screening method for finding a cholinergic muscarinic M1 receptor positive allosteric modulator (M1PAM) with reduced cholinergic side effects. The present invention also provides a method for treating Alzheimer's disease and the like, a method for reducing cholinergic side effects, and the like which use M1PAM selected by the screening method and having a low α value, or the M1PAM and an acetylcholinesterase inhibitor.
Owner:TAKEDA PHARMA CO LTD

A benzimidazole amine derivative, a preparation method thereof and use thereof as a beta2-adrenergic receptor allosteric modulator

The application belongs to the field of pharmaceutical chemistry, and specifically discloses a benzimidazole amine derivative, a preparation method thereof and application of the benzimidazole amine derivative as a beta2-adrenergic receptor allosteric antagonist. In the benzimidazole amine derivative, R1 is a hydrogen atom or a bromine atom; and R2 is a substituted benzoyl group or a substituted benzyl group. Pharmacological results show that the benzimidazole amine derivative has good antagonistic activity on beta2AR and can negatively allosterically regulate the functional activity of isoprenaline (ISO).
Owner:CHANGZHOU UNIV

Allosteric sting modulators and methods of use

Provided are various Stimulator of Interferon Genes (STING) allosteric modulators as well as methods of making and use thereof. Specifically provided herein are highly active STING inhibitors (antagonists) and activators (agonists). The compounds provide herein may be prepared as pharmaceutical compositions and used in methods of treating conditions related to disrupted or defective STING signaling.
Owner:BOARD OF RGT THE UNIV OF TEXAS SYST

Uptake mechanism of essential lysophospholipids into the brain and inhibition by endogenous-retroviral envelope protein

The disclosure provides the structure of an MFSD2A-SYNC2 complex together with functional data that revealed important molecular aspects of MFSD2A transport cycle, receptor-mediated cell-cell fusion, and pharmacology and resulted in the identification of two novel allosteric modulators of MFSD2A, which are two soluble fragments of SYNC2, namely SYNC2su-co and SYNC2su-co-2, representing first-in-class molecules to inhibit MFSD2A LPCs uptake and increase transcytosis rate.
Owner:INST PASTEUR

Combinations for use in restoring cognitive and behavioural deficits and improving memory deficits in individuals born preterm

PCT designated stage expiredWO2025158274A1Organic active ingredientsNervous disorderAllosteric modulatorExtrasynaptic receptors
The present invention relates to a pharmaceutical combination comprising a positive allosteric modulator ( PAM) of the α5 subunit of the extra-synaptic GABAA receptor and a positive allosteric modulator of the δ subunit of the extra-synaptic GABAA receptor for use in restoring behavioural deficits and improving memory deficits in individuals born preterm.
Owner:FOND INST ITAL DI TECH +1

SK channel positive allosteric modulators

A compound according to Formula (I) or a pharmaceutically acceptable salt thereof:is provided. X1 is N or C—Y; Y is H, halogen, NH2, OH, SH, alkyl, aryl, alkoxy, or aryloxy; A is O, NH, S, Se, or CH2,B isX2 is N or CH; and Z is NH, CH2, S, O, or Se.
Owner:CHAPMAN UNIVERSITY +2

Nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof, preparation method therefor, and the use thereof

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.
Owner:NEUSHEN THERAPEUTICS (SHANGHAI) CO LTD