65 results about "Cholinergic" patented technology

The invention relates to a pharmaceutical composition comprising benzgalantamine and uses and methods for the preparation thereof. The present invention provides a pharmaceutical composition in the form of a tablet, said tablet comprising a tablet core, wherein said core comprises benzgalantamine (ALPHA-1062) or salt thereof, and an enteric coating, wherein said enteric coating is configured for dissolution at pH 5.5 and above. The pharmaceutical composition could be used in the treatment of a brain disease associated with cognitive impairment and / or with a cholinergic deficit. The invention further provides a method for preparing the pharmaceutical composition.

Methods, formulations, and kits comprising an antioxidant compound for treatment of seizures, viral infections, encephalitis, exposure to chemical warfare agents, and / or exposure to a pesticide. An antioxidant such as N-acetyl cysteine (NAC) or a pharmaceutically acceptable salt is delivered by administration to a subject in need of treatment. Methods, formulations and kits may also comprise a cholinergic muscarinic antagonist, a cholinesterase reactivator, or both, and / or an inhibitor of a purinergic receptor, and / or a benzodiazepam. Kits for treating the subject comprising (a) at least one antioxidant compound or a pharmaceutically acceptable salt thereof, (b) an intranasal delivery device, and (c) an intramuscular delivery device. The pharmaceutical formulations can be pre-formulated into vials or cartridges that can be loaded into the intranasal delivery device or intramuscular delivery device.

Described herein are systems and methods for applying extremely low duty-cycle stimulation sufficient to treat chronic inflammation using feedback to adjust the off times between stimulations. In particular, the feedback include an assessment of the level of inflammation by the patient or the healthcare provider, or by measure the level of an inflammatory analyte or biomarker, or by detecting nerve activity correlated with inflammation.

The invention belongs to the technical field of food nutrition and health, and particularly discloses protein powder for assisting in improving Alzheimer's disease and a preparation method of the protein powder according to the concept of dietary therapy in China, and the protein powder is prepared from the following components in percentage by weight: 35-45% of egg white protein peptide powder and 55-65% of core function compound powder. According to the invention, egg white protein peptide is used as a high-quality matrix, and nine specific medicinal materials including hippocampus, egg yolk phospholipid, egg membrane peptide, walnut, fructus alpiniae oxyphyllae, gastrodia elata, mulberry, sargassum fusiforme, wolfberry, ginkgo leaf, fructus evodiae and dandelion are cooperatively compatible; aiming at seven core pathological links of Alzheimer's disease, such as A beta deposition, Tauopathy, neuroinflammation, oxidative stress, cholinergic deficiency, neurodystrophy and cerebral circulation disorder, a multi-target synergistic effect network is constructed, comprehensive neuroprotection is realized, and tests prove that the space learning and memory ability and the autonomous activity ability can be effectively improved.

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.

The present invention relates to a topical formulation comprising at least one anticholinergic compound for use in treating patients suffering from severe hyperhidrosis, wherein administration of the formulation to the patient comprises: a) an initial phase with a topical administration of a predetermined amount of the formulation 5 to 7 times per week for a total time period of less than six months: followed by b) a maintenance phase with a topical administration of the same amount of the formulation 1 to less than 5 times per week.

Described herein are systems and methods for applying extremely low duty-cycle stimulation sufficient to treat chronic inflammation using feedback to adjust the off times between stimulations. In particular, the feedback include an assessment of the level of inflammation by the patient or the healthcare provider, or by measure the level of an inflammatory analyte or biomarker, or by detecting nerve activity correlated with inflammation.

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.

In one aspect, the invention relates to an amorphous solid form of Alpha-1062 gluconate. In another aspect, the invention relates to methods of preparing an amorphous solid form of Alpha-1062 gluconate. Also disclosed are methods for treating a brain disease associated with cognitive impairment and / or with a cholinergic deficit in a subject, including administering the amorphous form of Alpha-1062 gluconate to a subject in need thereof.

The invention belongs to the technical field of medicinal chemistry, and relates to a benzazepine compound or pharmaceutically acceptable salt thereof as well as a preparation method and application of the benzazepine compound, in particular to a compound with a structural general formula as shown in a formula (I). The benzoazepine compound disclosed by the invention has a remarkable curative effect on treating brain organic lesion diseases, including vascular lesion and degenerative lesion, especially vascular dementia, Alzheimer's disease and cholinergic deficiency related diseases. Formula (I).

Topical formulations comprising soft glycopyrrolates are useful for treating excessive sweating conditions in subjects, such as humans suffering from hyperhidrosis. Preferably, at least one soft anticholinergic agent is provided in an effective amount or concentration in an anhydrous formulation that can inhibit excessive perspiration resulting from a condition such as hyperhidrosis.

We report a method of treating an epileptic seizure in a patient, comprising: detecting said epileptic seizure, based on body data from said patient; and reducing a flow of blood to a brain of said patient in response to said detected seizure; wherein said reducing is effected by: increasing the parasympathetic input to said patient's heart, such as by electrically stimulating a parasympathetic nervous structure, applying cooling energy to a sympathetic nervous structure, or administering a cholinergic or a sympatho-blocking agent to said patient. We also report a medical device system configured to implement the method. We also report a non-transitory computer readable program storage unit encoded with instructions that, when executed by a computer, perform the method.

The present invention relates to a crystalline microparticle form of 6,7-dihydro-4-hydroxy-7-isopropyl-6-oxo-N-(3-(piperidin-1-yl)propyl)thieno[2,3-b]pyridine-5-carboxamide potassium salt (PRX-3140) (I) for a particle delivery system (PDS) having good bioavailability and stability for the treatment of Alzheimer's disease (AD) and other dementias including post-traumatic stress disorder (PTSD) that affect the cholinergic and / or serotonergic systems. In other aspects, the present invention relates to an oral dosage form, a method of synthesizing the crystalline microparticle form, the preparation of a particle delivery system (PDS), and a final dosage form (FDF). JPEG2025518713000025.jpg49169

The invention provides an application of choline in preparation of a drug for preventing or / and treating broad-spectrum virus infection. The broad-spectrum virus is a DNA (deoxyribonucleic acid) mode virus HSV-1 and an RNA (ribonucleic acid) mode virus VSV of infected people. Choline can inhibit replication and expression of a DNA mode virus HSV-1 and an RNA mode virus VSV, and an effective new way is provided for prevention or / and treatment of broad-spectrum virus infection; the choline can activate PI3K-AKT signals and promote transcription of type I interferon, and a new potential drug is provided for prevention and treatment of broad-spectrum virus infection.

The invention relates to an inhalation dry powder preparation containing a salmeterol and tiotropium salt composition and a preparation method of the inhalation dry powder preparation, and belongs to the technical field of pharmaceutical preparations. The preparation comprises a long-acting beta-2 adrenergic receptor agonist (LABA) salmeterol and a long-acting anticholinergic drug (LAMA) tiotropium salt, and the efficient synergistic effect of the two drugs is achieved by optimizing a drug micronization process, a carrier particle design, a carrier material and a preparation process. The medicine can penetrate into a lung target region, so that precise treatment is realized. A powder mist inhalation device CN219423486U disclosed by Nanchang large pharmaceutical industry limited company is adopted as a delivery device, and the lung deposition rate and delivery efficiency of the medicine are remarkably improved by controlling the particle size of the medicine, the particle property of a carrier and the uniformity of the preparation. In addition, the invention further provides a preparation method of the preparation, the preparation method comprises the processes of medicine micronization, mixing homogenization and packaging, and the stability and dosage accuracy of the preparation are ensured. Experiments show that in an accelerated stability investigation period as long as 6 months, the drug content, impurity level and fine particle fraction in the preparation are kept stable and do not change significantly, and it is proved that the preparation has good physical and chemical stability and storage performance. The preparation has quick-acting and long-acting bronchiectasia effects, is suitable for long-term management of moderate and severe asthma and chronic obstructive pulmonary disease (COPD), and can significantly improve the medication convenience and treatment compliance of patients.

Intra-oral formulations comprising soft anticholinergic alkyl esters are useful for treating excessive drooling conditions in subjects, such as humans, suffering from sialorrhea. Preferably, at least one soft anticholinergic ester is provided in an effective amount or concentration in an anhydrous intra-oral formulation that can inhibit excessive drooling resulting from a condition known as sialorrhea.

The present invention discloses the use of Xinshubao tablets in preparing a drug for preventing and / or treating senile dementia. The present invention uses an AD animal model experiment constructed with scopolamine to determine that Xinshubao tablets improve the spatial learning and memory function of senile dementia mice by improving cortical and hippocampal tissue pathological damage, hippocampal neuron ultrastructure damage, and the cholinergic nervous system in the brain, and improving the neurotrophic state and synaptic function in the brain. The application of Xinshubao tablets in preventing and treating senile dementia has broad application prospects.

A nanoliposome suspension for soft aerosol spray and its preparation method are disclosed. The active ingredient of the nanoliposome suspension is selected from the following combinations: inhaled glucocorticoids, long / short-acting β2 receptor agonists and long / short-acting anticholinergic drugs (LAMA / SAMA), inhaled glucocorticoids, long / short-acting β2 receptor agonists and long / short-acting anticholinergic drugs, inhaled glucocorticoids and long / short-acting β2 receptor agonists, inhaled glucocorticoids and long / short-acting anticholinergic drugs; the active ingredient is encapsulated in nanoliposomes, which are prepared using cholesterol and phospholipids.

This invention provides an application and method of lysophosphatidylcholine (LPC) in promoting early development of reconstructed embryos, belonging to the field of embryo engineering technology. The invention first prepares reconstructed embryos, then adds lysophosphatidylcholine to the culture system for culturing. Lysophosphatidylcholine effectively promotes early development of the reconstructed embryos; at an optimal concentration of 5 μM, the blastocyst development rate increases to 24.56%, providing a novel and operable biochemical intervention target to solve the problem of low reconstructed embryo culture efficiency. This invention not only fills the gap in our understanding of the mechanism of action of LPC in this field, but also achieves controllability and reproducibility of the technical solution through precise definition of the optimal concentration. It provides key parameters for establishing standardized culture procedures and provides a more solid foundation for downstream applications such as developmental biology research and disease model construction that rely on high-quality reconstructed embryos, significantly accelerating the process of related scientific discovery and application development.

The application provides a lactobacillus gasseri strain A21120 with antioxidant, anti-inflammatory and antitumor functions, and a probiotic agent and application thereof, and belongs to the technical field of functional microorganisms. The strain A21120 is obtained by screening from intestinal feces of a centenarian healthy old person, and is identified by morphology and molecules and belongs to lactobacillus gasseri. The strain has good resistance to gastrointestinal fluid and bovine choline capacity, and has the potential to colonize the intestinal tract. The lactobacillus gasseri strain A21120 provided by the application has bacteriostatic, anti-inflammatory, antioxidant and antitumor activities, and provides a new way for the treatment of clinical related diseases, the development of drugs and the preparation of in vitro preparations or daily necessities.

Compounds shown in Formula (I), pharmaceutical compositions, and methods of using related to muscarinic acetylcholine receptors. The compounds herein are typically muscarinic acetylcholine receptor antagonists, such as M3 antagonists, which can be used for treating a variety of disorders, conditions or diseases such as hyperhidrosis.

The present invention relates to a composition for preventing, alleviating or treating Alzheimer's disease, comprising a Gongjindan composition as an active ingredient. The Gongjindan composition enhances memory or cognitive function, alleviates cholinergic dysfunction, strengthens neurotrophic factors, and has antioxidant and anti-inflammatory effects.

The application discloses application of triacetylandrographolide and a composition thereof in preparation of a medicine for relaxing airway smooth muscle, and belongs to the technical field of medicines. In view of the problems of obvious side effects and narrow treatment window of existing medicines, the application finds that triacetylandrographolide (3, 14, 19-Triacetylandrographolide, TAA) and the composition thereof have tracheal relaxation activity, and the triacetylandrographolide and the composition thereof play a relaxation role through non-competitive antagonism of a downstream signal path of a cholinergic receptor. The new mechanism provides a new idea for developing a new bronchial dilator for overcoming drug resistance of existing medicines. The TAA after preparation optimization can be used for treating or preventing airway obstructive diseases such as asthma, chronic obstructive pulmonary disease, bronchitis and acute lung injury.

The present invention provides a compound having a cholinergic muscarinic M1 receptor positive allosteric modulator activity and useful as an agent for the prophylaxis or treatment of Alzheimer's disease, schizophrenia, pain, sleep disorder, Parkinson's disease dementia, dementia with Lewy bodies, and the like.The present invention relates to a compound represented by the formula (I) or a salt thereof.wherein each symbol is as described in the specification, or a salt thereof.

The invention relates to a composition for inducing reprogramming of mesenchymal stem cells and application of the composition, and belongs to the technical field of biological medicine. According to the present invention, it is firstly found that the composition of CHIR99021, Y27632, SB431542 and purmorphamine can induce the reprogramming of mesenchymal stem cells into cholinergic motor neurons and glutamic acid energy interneurons, the cholinergic motor neurons are mainly adopted, and the induction efficiency of the composition is the highest; and inoculating the mesenchymal stem cells onto the silk fibroin scaffold, adding CYSP for induced culture, and finding that the induced neuron-like cells wrap the periphery of silk fibroin fibers to form a transplantable neuron network. When the neural network is transplanted into a spinal cord injury rat model, the deposition of collagen in a spinal cord injury cavity of a rat transplanted with the neural network is reduced, host neurons are saved, nerve fiber regeneration is promoted, and the injured spinal cord is repaired.

The present invention relates to a galantamine analog having a cholinesterase inhibitory activity, and a preparation method therefor and the use thereof. The galantamine analog has a general structural formula as shown in formula (IA), (IB) or (IC). In formula (IA), R1 is selected from hydrogen, o-fluoro, m-fluoro, p-fluoro, 2,4-difluoro, m-trifluoromethyl, p-methyl, 3,5-dimethoxy, p-chloro, p-nitro, p-cyano or p-trifluoromethoxy. In formula (IB), R2 is selected from phenyl, o-fluorophenyl, m-fluorophenyl, p-fluorophenyl, 2,4-difluorophenyl, 3,5-difluorophenyl, o-methylphenyl, p-methylphenyl, p-methoxyphenyl, indole, p-cyanophenyl, p-trifluoromethylphenyl, p-trifluoromethoxyphenyl, p-nitrophenyl or naphthalene ring. In formula (IC), R3 is selected from hydrogen, o-fluoro, m-fluoro, p-fluoro, m-chloro, p-chloro, p-methyl, o-methoxy, m-methoxy or p-methoxy. The galantamine analog of the present invention has a cholinesterase inhibitory activity superior to that of galantamine, and is expected to be used for treating diseases associated with cholinergic dysfunction.

The present invention provides the use of an Iris fruit extract in preparing a product for preventing and / or treating nerve cell damage. The present invention establishes an AD model, and after treatment with the Iris fruit extract, the activities of SOD and GSH can be significantly increased, and the increase in MDA levels can be inhibited, and the AchE content can also be inhibited. This indicates that the Iris fruit extract can effectively improve the oxidative stress response in the pathological process of AD and improve the cholinergic nerve damage of AD.

This invention relates to a galantamine analogue with cholinesterase-inhibiting activity, its preparation method, and its application. The general structural formula is shown in formula (IA), (IB), or (IC). In formula (IA), R1 is selected from hydrogen, o-fluorine, m-fluorine, p-fluorine, 2,4-difluoro, m-trifluoromethyl, p-methyl, 3,5-dimethoxy, p-chloro, p-nitro, p-cyano, or p-trifluoromethoxy. In formula (IB), R2 is selected from phenyl, o-fluorophenyl, m-fluorophenyl, p-fluorophenyl, 2,4-difluorophenyl, 3,5-difluorophenyl, o-methylphenyl, p-methylphenyl, p-methoxyphenyl, indole, p-cyanophenyl, p-trifluoromethylphenyl, p-trifluoromethoxyphenyl, p-nitrophenyl, or a naphthalene ring. In formula (IC), R3 is selected from hydrogen, o-fluorine, m-fluorine, p-fluorine, m-chloro, p-chloro, p-methyl, o-methoxy, m-methoxy, or p-methoxy. The galantamine analogue of this invention exhibits superior inhibitory activity against cholinesterase compared to galantamine, and holds promise for the treatment of cholinergic dysfunction-related diseases.

The invention provides a dry powder composition for relaxing an airway, a dry powder inhalation preparation and a preparation method thereof, and relates to the technical field of medicines, the dry powder composition comprises a carrier and a micronized drug active ingredient dispersed in the carrier, and the mass ratio of the micronized drug active ingredient to the carrier is 1: (11-21); the carrier comprises a coarse powder carrier and a micronized fine powder carrier; the pharmaceutical active component is composed of JKN2304 and glucocorticoid, a JKN2304-glucocorticoid duplex dry powder composition with inhaled glucocorticoid (ICS) and a beta2 receptor agonist effect and a cholinergic M receptor antagonist effect is constructed, the effects of relaxing the airway and inhibiting inflammation are achieved at the same time, the problem that a single powder inhalation is single in effect is solved, and the pharmaceutical composition is suitable for clinical application. The possibility of drug interaction is reduced. The dosage of fine particles is increased; the coarse powder carrier improves the fluidity and the total delivery amount, and a dispersion-delivery synergistic mechanism is formed.

Topical formulations comprising soft glycopyrrolates are useful for treating excessive sweating conditions in subjects, such as humans suffering from hyperhidrosis. Preferably, at least one soft anticholinergic agent is provided in an effective amount or concentration in an anhydrous formulation that can inhibit excessive perspiration resulting from a condition such as hyperhidrosis. 20 24 22 77 14 29 O ct 2 02 4 A B S T R A C T 2 0 2 4 2 2 7 7 1 4 2 9 O c t 2 0 2 4