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107 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.

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

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

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

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

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

3-cyclopropylpyrazole derivatives as positive allosteric modulators of the muscarinic acetylcholine receptor

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.
Owner:NEUROSTERIX PHARMA SÀRL

Naphthyridine and pyrido[3,4-c]pyridazine derivatives as GABAA α5 receptor modulators

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.
Owner:RICHTER GEDEON NYRT

1,3-dihydro-2H-pyrrolo[3,4-c]pyridine derivatives as GABAA α5 receptor modulators

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.
Owner:RICHTER GEDEON NYRT

Novel uracil derivatives as gabab positive allosteric modulators

PCT designated stageWO2026068756A1Nervous disorderOrganic chemistryDiseaseReceptor
The present invention relates to novel compounds of Formula (I), (I), wherein P, Q, A, B, m, n, R1 and R2 are defined as in Formula (I); which are gamma-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

GABAA positive allosteric modulator compounds, methods of making and uses thereof

The invention relates to GABAA positive allosteric modulator compounds, methods of preparation and uses thereof. Described herein are polymorphs comprising 2 ', 6-difluoro-5'-[3-(1-hydroxy-1-methylethyl)-imidazo [1, 2-b] [1, 2, 4] triazin-7-yl] biphenyl-2-carbonitrile (TPA023B) or a salt thereof. In one aspect, crystalline polymorphic salts or co-crystals of TPA023B with phosphoric acid are disclosed herein, Methods of making and using the same are also described herein.
Owner:NEUROCYCLE THERAPEUTICS INC

Indazole compounds as mglur4 allosteric potentiators, compositions, and methods of treating neurological dysfunction

Indazole compounds which are useful as allosteric potentiators / positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds, for example, in treating neurological and psychiatric disorders or other disease states associated with glutamate dysfunction.
Owner:VANDERBILT UNIV

Treatment for depression with a positive allosteric modulator of ampa

Described herein are methods for treating depression and / or preventing a relapse in depression in a patient, comprising: administering to the patient a first dose comprising 9-[4- (Cyclohexyloxy)phenyi]-7-methyl-3,4-dihydropyrazino[2, 1-c][l,2,4]thiadiazine 2,2-dioxide ("COMPOUND A" or "CMPD A") or a salt thereof; and administering to the patient at least one daily maintenance dose comprising COMPOUND A or a salt thereof, wherein the at least one daily maintenance dose is less than the first dose.
Owner:TAKEDA PHARMA CO LTD

New GABA b modulators

The present invention relates to novel compounds of Formula (I), wherein Z, P, Q, A, B, m, n, R1 and R2 are defined as in Formula (I); which are gamma-(γ)-aminobutyric acid type B receptor ("GABAB-R") positive allosteric modulators which are useful for the treatment or prevention of central and peripheral nervous system 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 disorders and diseases in which GABAB-R is involved.
Owner:ADDEX PHARMACEUTICALS SA

Use of oxime-based cholic acid analogs as allosteric agonists for TGR5

PCT designated stageWO2026000802A1Organic active ingredientsMetabolism disorderCholic acidChenodeoxycholic acid
The present invention relates to the field of medicinal chemistry. Specifically disclosed is a use of oxime-based cholic acid (CA) analogs as allosteric agonists for TGR5. In the present invention, CA used as a raw material undergoes a series of reactions to obtain CA intermediates each having an oxime at either or both of positions 7 and 12, and a series of modifications are then carried out on positions 24 and the oximes of these intermediates to obtain CA analogs as represented by formula 1, formula 2, or formula 3. The present invention uses a GloSensor cAMP accumulation assay to test the functional activity and allosteric mechanism of all target compounds on TGR5. Pharmacological results have shown that all synthesized target compounds have relatively good agonistic activity on TGR5 and can positively allosterically regulate the functional activity of chenodeoxycholic acid (CDCA) or lithocholic acid (LCA), that is, the target compounds are all positive allosteric modulators or allosteric agonists for TGR5.
Owner:CHANGZHOU UNIV

N-methyl-D-aspartic acid receptor modulators

ActiveUS12544363B2Organic active ingredientsOrganic chemistryAspartic acid receptorsNR1 NMDA receptor
A series of subunit selective allosteric modulators of NMDA receptor function according to Formula (I) is provided herein. Also provided is a method of treating neurological disorders such as Alzheimer's disease Parkinson's disease, schizophrenia, depression, stroke, psychosis and the like using compounds of Formula (I), optionally in combination with one or more further active agent. Pharmaceutical compositions containing a compound of Formula (I) and optionally one or more active agent for treating such disorders may be provided in the form of a tablet, capsule, pill, gel, granules, aerosol, aqueous buffer or a nanoparticle formulation, emulsion, liposome, etc.
Owner:EMORY UNIVERSITY