29 results about "GABAA receptor" patented technology

The present invention relates to a novel compound useful in the treatment of central nervous system diseases and disorders which are responsive to modulation of the GABAA receptor complex.

This invention relates to a cinnabar-2-oxide compound, its preparation method, and its uses. The cinnabar-2-oxide compound is shown in formula (I). By oxidizing a nitrogen atom to an N-oxide and then combining it with a heteroaryl group, the above-mentioned cinnabar-2-oxide compound achieves good α2-GABAA receptor affinity and positive regulatory activity. Simultaneously, it has the potential to significantly reduce PXR (pregnane X receptor) activation, thereby reducing drug-drug interactions and improving drug efficacy or safety.

This invention relates to a crystal form, preparation method, and application of a GABAA receptor modulator. Specifically, it provides the crystal form, preparation method, and application of the compound of formula (I) in the preparation of a GABAA receptor modulator drug.

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 invention relates to the field of compounds, and discloses a steroidal compound with a structure of a general formula I, application and a preparation method thereof and a pharmaceutical composition containing the steroidal compound, the steroidal compound has a relatively strong positive regulation effect on a GABAA receptor, can be used for preparing oral medicines for resisting severe depression and postpartum depression, and has the characteristic of high efficiency.

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.

Provided are an imidazopyridazine derivative, and a preparation method therefor, a pharmaceutical composition thereof and the use thereof. Specifically provided are a compound as shown in formula (1), and a stereoisomer, tautomer, prodrug, pharmaceutically acceptable salt, amorphous substance, isotopologue, polymorph or solvate thereof, a pharmaceutical composition containing the compound and the use of the compound as a GABAA receptor modulator.

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 discloses a traditional Chinese medicine composition for treating prostatic hypertrophy and a preparation method thereof, and the traditional Chinese medicine composition for treating prostatic hypertrophy comprises the following components: 12-18 parts of spina date seed, 10-14 parts of salvia miltiorrhiza, 8-12 parts of lily, 6-10 parts of poria cocos, 5-7 parts of polygala tenuifolia, 4-6 parts of valerian root, 3-5 parts of liquorice and 1-3 parts of cinnamon. The cinnamon can relax the smooth muscle of the prostate, reduce the number of times of night urination and directly improve the urination symptom of prostatic hyperplasia; the valerian root directly excites a GABAA receptor, quickly induces sleep and solves the sleep disorder of a patient, and the valerian root and the valerian root have a synergistic effect, so that local symptoms of prostate can be relieved, and related problems of a nervous system can be improved.

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.

To provide a method for treating epileptic conditions in a subject.SOLUTION: A method for treating epileptic conditions in a subject by administering a GABAA receptor modulator or a composition comprising a GABAA receptor modulator is provided.SELECTED DRAWING: Figure 14-1

The invention provides a steroid compound containing a 3-methyl allopregnenolone mother nucleus structure as well as a preparation method, a pharmaceutical composition and application of the steroid compound, and belongs to the technical field of medicines. The invention provides a steroid compound containing a 3-methyl pregnenolone mother nucleus structure, and pharmaceutically acceptable salts, stereoisomers, tautomers, prodrugs, solvates or isotope compounds of the steroid compound. The steroid compound containing the 3-methyl pregnenolone mother nucleus structure has a structure as shown in a formula I. The invention further provides a preparation method of the steroid compound containing the 3-methyl pregnenolone mother nucleus structure. The steroid compound containing the 3-methyl allopregnenolone mother nucleus structure has a strong positive regulation effect on a GABAA receptor, and has potential application to treatment of central nervous system related diseases.

Described herein are uses of 2 ', 6-difluoro-5'-(3-(2-hydroxypropyl-2-yl) imidazo [1, 2-b] [1, 2, 4] triazine-7-yl)-[1, 1 '-biphenyl]-2-formonitrile or a salt thereof, and also described herein are compositions (e.g., dosage forms) of 2', 6-difluoro-5 '-(3-(2-hydroxypropyl-2-yl) imidazo [1, 2-b] [1, 2, 4] triazine-7-yl)-[1, 1'-biphenyl]-2-formonitrile or a salt thereof, and uses thereof.

The purpose of the present invention is to provide a crystal form of a steroid compound, a pharmaceutical composition and the use thereof in the preparation of a drug for diseases related to a GABAA receptor. Compared with the prior art, the crystal form provided in the present invention has one or more improved properties, and has great significance in further development of the drug.

The invention relates to a pharmaceutical preparation of a GABAA receptor enhancer and a preparation method of the pharmaceutical preparation. The GABAA receptor enhancer is represented by a formula (I) or a stereoisomer, a pharmaceutically acceptable salt or a prodrug thereof.

Provided herein are alpha5-containing GABAA receptor agonists and pharmaceutical compositions and methods of treatment of cognitive and mood symptoms in neurodegenerative and neuropsychiatric disorders using them.

The invention provides a steroid compound as well as a preparation method, a pharmaceutical composition and application thereof, and belongs to the technical field of medicines. The invention provides a steroid compound, a pharmaceutically acceptable salt, a stereoisomer, a tautomer, a prodrug, a solvate or an isotope compound thereof. The steroid compound has a structure as shown in a formula I in the specification. The compound provided by the invention has a strong positive regulation effect on a GABAA receptor, and has potential application in treatment of central nervous system related diseases. # imgabs0 #

Described herein are salts (e.g., fumarate salts) of 3-(2,5-difluorophenyl)-7-[1,1-di(methyl-d 3 )ethyl-2,2,2-d 3 ]-6-[(1-methyl-1H-1,2,4-triazol-5-yl)methoxy]-1,2,4-triazolo[4,3-b]pyridazine and particles comprising 3-(2,5-difluorophenyl)-7-[1,1-di(methyl-d 3 )ethyl-2,2,2-d 3 ]-6-[(1-methyl-1H-1,2,4-triazol-5-yl)methoxy]-1,2,4-triazolo[4,3-b]pyridazine or a salt thereof, and uses thereof.

The present invention relates to difluoromethyl-pyridin-2-yl triazoles of general formula (I), which are modulators of the GABAA receptor containing the alpha5 subunit, useful in the treatment of central nervous system diseases and other diseases. In addition, the invention relates to a method for preparing a pharmaceutical composition and to a method for producing the compounds according to the invention.

To provide compounds for use in methods of treating a disease or disorder associated with α2 / α3 GABAA receptor.SOLUTION: Provided herein are crystalline polymorphs or co-crystals of 2',6-difluoro-5'-[3-(1-hydroxy-1-methylethyl)-imidazo[1,2-b][1,2,4]triazin-7-yl]biphenyl-2-carbonitrile with phosphoric acid.SELECTED DRAWING: Figure 19

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 relates to a cinnoline-2-oxide compound as well as a preparation method and application thereof. The cinnoline-2-oxide compound is shown as a formula (I) in the specification. According to the cinnoline-2-oxide compound, a nitrogen atom is oxidized into N-oxide to be matched with heteroaryl, good alpha2-GABAA receptor affinity activity and positive regulation activity can be achieved, meanwhile, the cinnoline-2-oxide compound has the potential of remarkably reducing and activating a PXR (pregnane X receptor), then the drug-drug interaction can be reduced, and the clinical application prospect is broad. The medicine curative effect or safety is improved. # imgabs0 #

The invention provides methods and related compositions for preventing neurocognitive decline associated with chronic stress, age, and neurodegenerative diseases. The methods described here are based upon the use of alpha5-GABAA receptor agonists to slow or prevent deleterious morphological changes in dendrites of the hippocampus and prefrontal cortex, which eventually manifest in functional decline and the neurocognitive deficits.

Provided in the present invention are a fused ring compound, and an intermediate thereof and the use thereof. Specifically, the present invention relates to a compound as shown in general formula (I), a cis-trans isomer thereof, an enantiomer thereof, a diastereomer thereof, a racemate thereof, a solvate thereof, a hydrate thereof, or a pharmaceutically acceptable salt thereof, or a prodrug thereof. The compound of the present invention has a good modulatory effect on an α5-GABAA receptor, and has good pharmaceutical application prospects.

The invention aims to provide a crystal form of a steroid compound, a pharmaceutical composition and application of the crystal form in preparation of a medicine for treating GABAA receptor related diseases. Compared with the prior art, the crystal form provided by the invention has one or more improved properties, and is of great significance to further development of the medicine.

The present disclosure concerns the novel compounds 3α-ethyl-3β-hydroxy-5α-androstan-17-one and 3α-ethyl-3β-hydroxy-5α-androstan-17-one, the medical use thereof and in particular use in the treatment of diseases and disorders associated with an α3 subtype of the GABAA receptor, for example 5 treatment of obesity, hyperphagia disorder, Prader-Willi's syndrome, polycystic ovarian syndrome, and / or diabetes. Said disclosure is also concerned with reducing and / or preventing overweight. Additionally, related pharmaceutical and cosmetic compositions are disclosed as well as treatment against alcoholism and substance abuse.

Disclosed are compositions and methods for treating benzodiazepine misuse and / or use disorder. A method of treating benzodiazepine misuse and / or use disorder includes administering to a subject in need thereof of an effective amount of a compound that provides both partial modulator and antagonist effects at GABAA receptors.

Described herein are salts (e.g., fumarates) of 3-(2, 5-difluorophenyl)-7-[1, 1-bis (methyl-d3) ethyl-2, 2, 2-d3]-6-[(1-methyl-1H-1, 2, 4-triazol-5-yl) methoxy]-1, 2, 4-triazolo [4, 3-b] pyridazine and salts (e.g., fumarates) of 3-(2, 5-difluorophenyl)-7-[1, 1-bis (methyl-d3) ethyl-2, 2, 2-d3]-6-[(1-methyl-1H-1, 2, 4-triazol-5-yl) methoxy]-1, 2, 4-triazolo [4, 3-b] pyridazine and salts (e.g., fumarates) The present invention relates to particles of [1, 3-b] pyridazine or a salt thereof and uses thereof.

The invention relates to an isoxazole-heterocyclic derivative, a pharmaceutical composition and use, and specifically provides a compound represented by formula (I) or a pharmaceutically acceptable salt, a stereoisomer, a tautomer, a prodrug, an amorphous form, an isotopologue, a polymorph or a solvate thereof, a pharmaceutical composition comprising the compound and use of the compound as α5-GABAA receptor regulator.