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434 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.

Muscarinic receptor antagonists

Disclosed are multibinding compounds which are muscarinic receptor antagonists. The multibinding compounds of this invention containing from 2 to 10 ligands covalently attached to one or more linkers. Each ligand is, independently of each other, a muscarinic receptor antagonist or an allosteric modulator provided that at least one of said ligand is a muscarinic receptor antagonist. The multibinding compounds of this invention are useful in the treatment and prevention of diseases such as chronic obstructive pulmonary disease, chronic bronchitis, irritable bowel syndrome, urinary incontinence, and the like.
Owner:THERAVANCE BIOPHARMA R&D IP LLC

Novel Thieno-Pyridine and Thieno-Pyrimidine Derivatives and Their Use as Positive Allosteric Modulators of Mglur2-Receptors

The present invention relates to novel compounds, in particular novel thieno-pyridine and thieno-pyrimidine derivatives according to Formula (I), wherein all radicals are defined in the application. The compounds according to the invention are positive allosteric modulators of metabotropic receptors-subtype 2 ("mGluR2") which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. In particular, such diseases are central nervous system disorders selected from the group of anxiety, schizophrenia, migraine, depression, and epilepsy. The invention is also directed to pharmaceutical compositions and processes to prepare such compounds and compositions, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR2 is involved.
Owner:ORTHO MCNEIL JANSSEN PHARMA

Methods for treating idiopathic hyperhidrosis and associated conditions

InactiveUS20040192754A1Reduced activityAlleviate and treat symptomBiocideAnimal repellantsAllosteric modulatorMianserin Hydrochloride
The subject invention provides methods for treating symptoms and / or conditions associated with idiopathic hyperhidrosis by using compounds that decrease the activity of serotonin 5-HT2C receptors. Compounds that can ameliorate symptoms of idiopathic hyperhidrosis and associated conditions include 5-HT2C receptor antagonists (i.e., ketanserin, ritanserin, mianserin, mesulergine, cyproheptadine, fluoxetine, mirtazapine, olanzapine, and ziprasidone) as well as 5-HT2C receptor modulators (i.e., inverse agonists, partial agonists, and allosteric modulators).
Owner:SHAPIRA NATHAN ANDREW +2

BENZAMIDE mGluR5 POSITIVE ALLOSTERIC MODULATORS AND METHODS OF MAKING AND USING SAME

InactiveUS20090042855A1Increase awarenessPotentiate metabotropic glutamate receptor activityBiocideNervous disorderAllosteric modulatorMetabotropic glutamate receptor
In one aspect, the invention relates to compounds, including phenylethynylbenzamide derivatives, cycloalkylethynylbenzamide derivatives, styrylbenzamide derivatives, 4-(3-phenyl-1,2,4-oxadiazol-5-yl)benzamide derivatives, 4-(pyridinylethynyl)benzamide derivatives, and N1-phenylterephthalamide derivatives, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
Owner:VANDERBILT UNIV

GLP-1 receptor agonist and allosteric modulator monoclonal antibodies and uses thereof

InactiveUS20060275288A1Induction of insulin secretionSuppression of glucagon releaseImmunoglobulins against cell receptors/antigens/surface-determinantsAntibody ingredientsDiabetes mellitusAllosteric modulator
The subject invention relates to monoclonal antibodies that have the ability to bolster the function of the GLP-1 receptor and may therefore have utility in the treatment of mammalian metabolic disorders such as, for example, diabetes. In particular, the invention describes the generation of fully human monoclonal antibodies made against extracellular domains of the human GLP-1 receptor which are capable of binding the intact receptor and activating it in a manner similar to the native ligand. Additionally, the invention describes methods used to generate and develop allosteric modulator antibodies of the human GLP-1 receptor with potential therapeutic uses.
Owner:ABBOTT LAB INC

Substituted benzaldehyde compounds and methods for their use in increasing tissue oxygenation

Provided are substituted benzaldehydes and derivatives thereof that act as allosteric modulators of hemoglobin, methods and intermediates for their preparation, pharmaceutical compositions comprising the modulators, and methods for their use in treating disorders mediate by hemoglobin and disorders that would benefit from increased tissue oxygenation.
Owner:RGT UNIV OF CALIFORNIA +1

Apj receptor compounds

The invention relates generally to compounds which are allosteric modulators (e.g., negative and positive allosteric modulators, allosteric agonists, and ago-allosteric modulators) of the G protein coupled receptor apelin, also known as the APJ receptor. The APJ receptor compounds are derived from the intracellular loops and domains of the the APJ receptor. The invention also relates to the use of these APJ receptor compounds and pharmaceutical compositions comprising the APJ receptor compounds in the treatment of diseases and conditions associated with APJ receptor modulation, such as heart diseases (e.g., hypertension and tension and heart failure, such as congestive heart failure), cancer, diabetes, stem cell trafficking, fluid homeostasis, cell proliferation, immune function, obesity, metastatic disease, and HIV infection.
Owner:ANCHOR THERAPEUTICS

Substituted heteroaryl aldehyde compounds and methods for their use in increasing tissue oxygenation

Provided are substituted heteroaryl aldehydes and derivatives thereof that act as allosteric modulators of hemoglobin, methods and intermediates for their preparation, pharmaceutical compositions comprising the modulators, and methods for their use in treating disorders mediate by hemoglobin and disorders that would benefit from increased tissue oxygenation.
Owner:GLOBAL BLOOD THERAPEUTICS +1

Pthr1 receptor compounds

The invention relates generally to compounds which are allosteric modulators (e.g., negative and positive allosteric modulators, allosteric agonists, and ago-allosteric modulators) of the G protein coupled receptor PTHR1, also known as parathyroid hormone / parathyroid hormone related protein receptor. The PTHR1 compounds are derived from the intracellular loops and domains of the PTHR1 receptor. The invention also relates to the use of these PTHR1 receptor compounds and pharmaceutical compositions comprising the PTHR1 receptor compounds in the treatment of diseases and conditions associated with PTHR1 receptor modulation, such as osteoporosis; humoral hypercalcemia of malignancy; osteolytic and osteoblastic metastasis to bone; primary and secondary hyperparathyroidism associated increase in bone absorption; vascular calcification; psychiatric disorders and cognitive disorders associated with hyperparathyroidism; dermatological disorders; and excess hair growth.
Owner:REN YONG +2

Cxcr5 receptor compounds

The invention relates generally to compounds which are allosteric modulators (e.g., negative and positive allosteric modulators, allosteric agonists, and ago-allosteric modulators) of the G protein coupled receptor CXCR5. The CXCR5 receptor compounds are derived from the intracellular loops and domains of the CXCR5 receptor. The invention also relates to the use of these CXCR5 receptor compounds and pharmaceutical compositions comprising the CXCR5 receptor compounds in the treatment of diseases and conditions associated with CXCR5 receptor modulation such as autoimmune diseases including lupus, HIV and rheumatoid arthritis, Primary Sjogren's Syndrome, chronic lymphocytic leukemia, Burkitt Lymphoma, colon and breast cancer tumor metastasis, Multiple Sclerosis and compromised immune function.
Owner:ANCHOR THERAPEUTICS

Substituted benzaldehyde compounds and methods for their use in increasing tissue oxygenation

Provided are substituted benzaldehydes and derivatives thereof that act as allosteric modulators of hemoglobin, methods and intermediates for their preparation, pharmaceutical compositions comprising the modulators, and methods for their use in treating disorders mediate by hemoglobin and disorders that would benefit from increased tissue oxygenation.
Owner:RGT UNIV OF CALIFORNIA +1

Novel Heterocyclic Compounds as Positive Allosteric Modulators of Metabotropic Glutamate Receptors

The present invention relates to new compounds which are Heterocyclic derivatives of formula (I) wherein A, B, P, X, Y, Q, W, R1 and R2 are defined in the description. Invention compounds are useful for treating central or peripheral nervous system disorders and other disorders which are affected by the neuromodulatory effect of mGluR5 positive allosteric modulators such as cognitive decline and also to treat both positive and negative symptoms in schizophrenia.
Owner:ADDEX PHARM SA

Novel Tetrazole Derivatives as Positive Allosteric Modulators of Metabotropic Glutamate

The present invention relates to new tetrazole compounds of formula I wherein B, P, Q, W, R1 and R2 are defined in the description: invention compounds are useful for the treatment or prevention of central nervous system disorders as well as other disorders modulated by mGluR5 receptors.
Owner:ADDEX PHARM SA

Indole and benzoxazine derivatives as modulators of metabotropic glutamate receptors

The present invention relates to novel indole and benzoxazine derivatives which are positive allosteric modulators of the metabotropic glutamate receptor subtype 2 (“mGluR2”) and which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes to prepare such compounds and compositions, and to the use of such compounds for the prevention or treatment of neurological and psychiatric disorders and diseases in which mGluR2 is involved.
Owner:JANSSEN PHARMA INC +1

1,3,5-trisubstituted triazole derivative

The present invention relates to 2-[3-(2,2-Difluoro-benzo[1,3]dioxol-5-ylamino)-5-(2,6-dimethyl-pyridin-4-yl)-[1,2,4]triazol-1-yl]-N-ethyl-acetamide and analogues or pharmaceutically acceptable salts thereof, processes for preparing them, pharmaceutical compositions containing them and their use in therapy.The invention particularly relates to a potent positive allosteric modulator of nicotinic acetylcholine receptors which have the capability of increasing the efficacy of nicotinic receptor agonists.
Owner:JANSSEN PHARMA NV
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