251 results about "Nicotinic acetylcholine receptor" patented technology

The present invention relates to 3-substituted-2-(arylalkyl)-1-azabicycloalkanes, methods of preparing the compounds and methods of treatment using the compounds. The azabicycloalkanes generally are azabicycloheptanes, azabicyclooctanes, or azabicyclononanes. The aryl group in the arylalkyl moiety is a 5- or 6-membered ring heteroaromatic, preferably 3-pyridinyl and 5-pyrimidinyl moieties, and the alkyl group is typically a C1-4 alkyl. The substituent at the 3-position of the 1-azabicycloalkane is a carbonyl group-containing moiety, such as an amide, carbamate, urea, thioamide, thiocarbamate, thiourea or similar functionality. The compounds exhibit activity at nicotinic acetylcholine receptors (nAChRs), particularly the α7 nAChR subtype, and are useful towards modulating neurotransmission and the release of ligands involved in neurotransmission. Methods for preventing or treating conditions and disorders, including central nervous system (CNS) disorders, which are characterized by an alteration in normal neurotransmission, are also disclosed. Also disclosed are methods for treating inflammation, autoimmune disorders, pain and excess neovascularization, such as that associated with tumor growth.

The invention relates to insecticidal mixtures of spinosyns and agonists or antagonists of nicotinic acetylcholine receptors for protecting plants against attack by pests.

Tobacco products comprising smokeless tobacco products and active ingredients, including those that antagonize nicotinic acetylcholine receptors, the TRPV1 channel, and / or the TRPA1 channel are disclosed. Nicotine replacement therapies comprising active ingredients, including those that antagonize nicotinic acetylcholine receptors, the TRPV1 channel, and / or the TRPA1 channel. The active ingredient may reduce or eliminate sensory irritation arising due to use of the product. Analgesic compositions comprising active ingredients. Methods of reducing taste and sensory irritation by employing an active ingredient.

The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands for the nicotinic α7 receptor and may be useful for the treatment of various disorders of the central nervous system, especially affective and neurodegenerative disorders.

The present invention relates to compositions and methods to treat diseases or conditions with alpha-7 nicotinic acetylcholine receptor (AChR) full agonists by decreasing levels of tumor necrosis factor-alpha and / or by stimulating vascular angiogenesis.

The present invention relates conotoxin peptides that are analogs of the α-contoxin peptide RgIA. These conotoxin peptides block the α9α10 subtype of the nicotinic acetylcholine receptor (nAChR) and can be used for treating pain, such as neuropathic pain and inflammatory pain, inflammatory disorders, such as rheumatic diseases, and in the treatment of breast cancer.

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.

Disclosed are nicotine-related compounds that selectively inhibit cytochrome P-450 2A6 (CYP2A6), selectively inhibit cytochrome P-450 2A13 (CYP2A13), and / or selectively modulate a nicotinic acetylcholine receptor (nAChR). Also disclosed are pharmaceutical compositions comprising a compound of the invention, as well as methods of using the pharmaceutical compositions for treating or preventing a disease or disorder associated with nicotine-ingestion, or a disease or disorder amenable to treatment by selective modulation of nAChRs.

There is provided di-substituted iminoheterocyclic compounds of the following formula (I): in which,A is optionally substituted alkyl group, optionally substituted aryl group or optionally substituted heterocyclic group;X is oxygen atom, sulfur atom, carbon atom or nitrogen atom;the group —X—Y— represents optionally substituted alkylene or cyclic alkenylene bond; andB1 and B2 are, hydrogen atom, optionally substituted alkyl group, optionally substituted aryl group or optionally substituted heterocyclic group, independent from each other,or a pharmaceutically acceptable salt thereof.These compounds have good affinity for α4β2 nicotinic acetylcholine receptors and activate the same to thereby exert a preventive or therapeutic effect on cerebral dysfunction.

The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands for the nicotinic α7 receptor and may be useful for the treatment of various disorders of the central nervous system, especially affective and neurodegenerative disorders.

The present invention belongs to the field of insecticides, and relates to a pest-killing and mite-killing composition, which contains an active component A and an active component B, a weight part ratio of the component A to the component B is 1:99-99:1, the active component A is selected from a compound I represented by the following structural formula, the active component B is selected from an organic phosphorus pest / mite killing agent, a nicotine type acetylcholine receptor (nAChR) agonist pest / mite killing agent, an apastia pest / mite killing agent, a proton gradient interference and oxidative phosphorylation affecting uncoupling pest / mite killing agent, a nereistoxin analog pest / mite killing agent, a Ryania receptor regulating pest / mite killing agent, a voltage-dependent sodium ion channel blocking pest / mite killing agent, an ecdysone receptor stimulating pest / mite killing agent, an amino butyric acid (GABA) gated chloride channel antagonism pest / mite killing agent, a microorganism pest / mite killing agent or other pest / mite killing agents, and the active component A has the following structure. The composition of the present invention has advantages of significant synergy, resistance delaying and the like, and can be used for prevention and control of a variety of pests. The compound I is defined in the instruction.

The present invention concerns methods for treating or preventing neurological disorders characterized by dysfunction of nicotine acetylcholine receptors by co-administration of metanicotine and at least one compound which exhibits antagonist activity, or both agonistic and antagonist activity, toward one or more nicotinic acetylcholine receptor subtypes. The subject invention, in another aspect, pertains to pharmaceutical compositions containing metanicotine and at least one compound which exhibits antagonistic activity, or both agonistic and antagonistic activity, toward one or more nicotinic acetylcholine receptor subtypes.

N-n-Alkylation of nicotine converts nicotine from an agonist into an antagonist specifically for neuronal nicotinic acetylcholine receptor subtypes mediating nicotine-evoked dopamine release. Conformationally restricted analogs exhibit both high affinity and selectivity at this site, and are able to access the brain due to their ability to act as substrates for the blood-brain barrier choline transporter.

The present invention relates to compounds useful in therapy, to compositions comprising said compounds, and to methods of treating diseases comprising administration of said compounds. The compounds referred to are positive allosteric modulators (PAMs) of the nicotinic acetylcholine α7 receptor.

Provided are bis-quaternary ammonium compounds which are modulators of nicotinic acetylcholine receptors. Also provided are methods of using the compounds for modulating the function of a nicotinic acetylcholine receptor, and for the prevention and / or treatment of central nervous system disorders, substance use and / or abuse, and or gastrointestinal tract disorders.

One aspect of the present invention relates to heterocyclic compounds that are ligands for nicotinic acetylcholine receptors. A second aspect of the invention relates to the use of a compound of the invention for modulation of a mammalian nicotinic acetylcholine receptor. The present invention also relates to the use of a compound of the invention for treating a mammal suffering from Alzheimer's disease, Parkinson's disease, dyskinesias, Tourette's syndrome, schizophrenia, attention deficit disorder, anxiety, pain, depression, obsessive compulsive disorder, chemical substance abuse, alcoholism, memory deficit, pseudodementia, Ganser's syndrome, migraine pain, bulimia, obesity, premenstrual syndrome or late luteal phase syndrome, tobacco abuse, post-traumatic syndrome, social phobia, chronic fatigue syndrome, premature ejaculation, erectile difficulty, anorexia nervosa, disorders of sleep, autism, mutism or trichtillomania.

A computer readable medium holding data of a molecular model of a ligand-gated ion channel receptor and / or a computer system for modeling said receptor are provided by the instant invention. The molecular model can be used to design novel compounds having activity as non-competitive inhibitors of the ion channel. A preferred embodiment of the invention relates to nicotinic acetylcholine receptors. Compounds having activity as non-competitive inhibitors of ligand-gated ion channel receptors and methods for inhibiting the receptor and treating diseases or disorders mediated by function of the receptor are also disclosed.

One aspect of the present invention relates to heterocyclic compounds that are ligands for nicotinic acetylcholine receptors. A second aspect of the invention relates to the use of a compound of the invention for modulation of a mammalian nicotinic acetylcholine receptor. The present invention also relates to the use of a compound of the invention for treating a mammal suffering from Alzheimer's disease, Parkinson's disease, dyskinesias, Tourette's syndrome, schizophrenia, attention deficit disorder, anxiety, pain, depression, obsessive compulsive disorder, chemical substance abuse, alcoholism, memory deficit, pseudodementia, Ganser's syndrome, migraine pain, bulimia, obesity, premenstrual syndrome or late luteal phase syndrome, tobacco abuse, post-traumatic syndrome, social phobia, chronic fatigue syndrome, premature ejaculation, erectile difficulty, anorexia nervosa, disorders of sleep, autism, mutism or trichtillomania.

The present invention relates to 1-alkyl-3-aniline-5-aryl-pyrazole derivatives and pharmaceutically acceptable salts thereof, processes for preparing them, pharmaceutical compositions containing them and their use in therapy, according to Formula (I).The invention particularly relates to positive allosteric modulators of nicotinic acetylcholine receptors, such positive allosteric modulator having the capability to increase the efficacy of nicotinic receptor agonists.

There is provided a method for controlling flies, that live in or come flying to livestock pens or poultry houses, by using a compound or salt thereof with an affinity for a nicotinic acetylcholine receptor of insects. Since having a very high activity against flies, the compound or salt thereof helps quickly and efficiently to control flies that live in or come flying to livestock pens or poultry houses. Also, since having an excellent control effect on flies that are resistant to conventional chemicals including a organo-phosphoric pesticide and a pyrethroid, the compound or salt thereof helps to prevent propagation, caused by flies, of various diseases to livestock, poultry and humans, and reduce discomfort of workers engaged in the livestock and poultry farming and a community. Still, it is possible with the present invention to keep livestock pens or poultry houses in a hygienic condition, which may greatly contribute to the development of the livestock and poultry farming.

The present invention relates to 3-substituted-2-(arylalkyl)-1-azabicycloalkanes, methods of preparing the compounds and methods of treatment using the compounds. The azabicycloalkanes generally are azabicycloheptanes, azabicyclooctanes, or azabicyclononanes. The aryl group in the arylalkyl moiety is a 5- or 6-membered ring heteroaromatic, preferably 3-pyridinyl and 5-pyrimidinyl moieties, and the alkyl group is typically a C1-4 alkyl. The substituent at the 3-position of the 1 -azabicycloalkane is a carbonyl group-containing moiety, such as an amide, carbamate, urea, thioamide, thiocarbamate, thiourea or similar functionality. The compounds exhibit activity at nicotinic acetylcholine receptors (nAChRs), particularly the α7 nAChR subtype, and are useful towards modulating neurotransmission and the release of ligands involved in neurotransmission. Methods for preventing or treating conditions and disorders, including central nervous system (CNS) disorders, which are characterized by an alteration in normal neurotransmission, are also disclosed. Also disclosed are methods for treating inflammation, autoimmune disorders, pain and excess neovascularization, such as that associated with tumor growth.

The present invention relates to methods and compositions which act as nicotinic acetylcholine receptor antagonist in living organisms. More particularly, the present invention relates to methods and compositions which act as nicotinic acetylcholine receptor antagonist using processed Morinda citrifolia L. plant products.

The present invention relates to the use of compounds that block the α9α10 subtype of the nicotinic acetylcholine receptor (nAChR) for treating pain, such as neuropathic pain and inflammatory pain, and inflammatory disorders, such as arthritis. The present invention also relates to screening compounds to identify analgesic agents that block the α9α10 subtype of the nAChR.

The invention belongs to the fields of biochemistry and molecular biology, relates to a new conopeptide, and a medicinal composition, a preparation method and uses thereof, also relates to a nucleic acid construct, an expression vector of the nucleic acid construct, a converted cell of the expression vector and a fusion protein of the conopeptide, and further relates to a method for blocking out an acetylcholine receptor, and pharmaceutical uses of the conopeptide. The new conopeptide K41JM and analogs thereof can specifically block out the acetylcholine receptor (nAChRs) (such as alpha9alpha10nAChR), have can treat neuralgia, cancer chemotherapy, breast cancer, lung cancer, wound healing, encephalomyelitis, epilepsy and ischaemia, and have good application prospects in the preparation of pain easing medicines, anticancer medicines and neuroscience tool medicines.

The invention relates to the field of polypeptide drugs, in particular to a conotoxin polypeptide, a preparation method and an application thereof, and especially relates to the conotoxin polypeptide acting on muscle-type nicotinic acetylcholine receptors. The amino acid sequence of the conotoxin polypeptide is HPA. The experimental results indicates that the conotoxin polypeptide HPA can act on the muscle-type nicotinic acetylcholine receptors to effectively inhibit the acetylcholine receptors, and can serve as antagonists of the muscle-type nicotinic acetylcholine receptors. The conotoxin polypeptide HPA can be used for preparing anti-wrinkle cosmetics, is broadly used and has good economic and social effects.

The présent invention relates to a method for manufacturing an analysis device including torpédo membrane fragments immobilized at the surface thereof, to the resulting analysis device, and to the use of said device for detecting, purifying, and characterizing molécules acting on nicotinic acetylcholine receptors. The présent invention is useful in the field of monitoring seafood, monitoring neurotoxic phytoplankton for the shellfish industry, monitoring the quality of bathing waters along tourist beaches, the field of monitoring fresh water reserves, the field of médical research, the field of the biological analysis and characterization of molécules, e.g., non-radioactive assays of the movement of the ligand-receptor bond on an ELISA-type microplate, thereby enabling compétitive agonists and antagonists of targets to be detected, e.g., of highly sensitive receptors.

The present invention relates to compounds useful in therapy, to compositions comprising said compounds, and to methods of treating diseases comprising administration of said compounds. The compounds referred to are positive allosteric modulators (PAMs) of the nicotinic acetylcholine α7 receptor.