14 results about "Memantine" patented technology

The invention belongs to the technical field of medicine synthesis, and particularly relates to a memantine derivative and a synthesis method and application thereof. The memantine derivative comprises an intermediate structural formula I, an intermediate structural formula II, an intermediate structural formula III and a structural general formula, Linker is substituted or unsubstituted C6-C10 aroyl, R1 is hydrogen or C1-C6 alkyl, R2 is hydrogen, C1-C6 alkyl or a nitrogen-containing or nitrogen-free structural fragment, or the integral structure of R1 and R2 is N-substituted heterocyclic pentyl or heterocyclic cyclohexyl. According to the memantine derivative provided by the invention, a memantine group is combined with an OAB-14 partial structure to change a parent nucleus structure, so that the drug activity is improved. The invention also provides a synthesis method of the compound, and the obtained compound is used for treating Alzheimer's disease and Parkinson's disease.

The disclosure provides new and improved combination therapies using lisinopril and memantine.

The invention relates to compositions comprising a synergistic combination of memantine and vitamin D, to the method for preparing same and to the use thereof in the prevention and treatment of neurodegenerative diseases, in particular Alzheimer's disease.

At least one pharmaceutical composition for use in a method of prophylaxis or treatment of COVID wherein the at least one pharmaceutical composition comprises donepezil, rivastigmine or galantamine or one of donepezil, rivastigmine or galantamine combined with one of: Artemether and Lumefantrine; Atazanavir Sulfate; Efavirenz; Fosamprenavir Calcium; Saquinavir; Remdesivir (GS-5734); Digoxin; Memantine; Rivastigmine; Galantamine; Valsartan; Teriflunomide and wherein the method of prophylaxis or treatment of COVID or COVID-19 comprises: providing a subject in need of said prophylaxis or treatment; providing the at least one pharmaceutical composition as defined supra; wherein said components are provided together or separately; wherein said components are administered together or separately; and wherein said components are provided in a pharmaceutically acceptable diluent, adjuvant and / or excipient; and administering a pharmaceutically effective amount of said at least one pharmaceutical composition to said subject; and wherein, in the method, said subject is provided prophylaxis or treatment of COVID and COVID relates to a human coronavirus, mouse hepatitis virus (MHV), or recombinant mouse-adapted SARS-CoV (SARS-CoV MAI 5).

The disclosure provides new and improved combination therapies using lisinopril and memantine.

Methods and compositions are disclosed for rapidly relieving symptoms in subjects with depressive, stressor and substance abuse conditions, e.g., major depression, treatment-resistant depression, post-partum depression, bipolar depression, post-traumatic stress disorder, substance use disorders, negative and cognitive symptoms of schizophrenia, as well as for slowing progression of mild cognitive impairment and dementia, using an intermittent dosing regimen of memantine or amantadine or a structural analogue or pharmaceutically acceptable salt of memantine or amantadine (optionally no more frequently than every 2 days) at a dose sufficient to activate Set A brain structures, in combination with a second drug at a dose which activates Set B brain structures but which does not appreciably evoke brain activity linked to hallucinogenic and other psychotomimetic perceptions. In some instances the second drug is either 1) a low dose psilocybin or low dose of other psychedelic and stimulant molecules capable of activating Set B of brain structures which is administered at a dose low enough such that it does not appreciably evoke brain activity linked to hallucinogenic and other psychotomimetic perceptions, or is 2) mianserin (S isomer, R isomer, or a racemate comprising both isomers or structural analog or pharmaceutically acceptable salt thereof) or another standard of care antidepressant capable of activating Set B brain structures, or 3) lumateperone or another antipsychotic capable of activating Set B brain structures.

The present disclosure is directed to methods for treating a neuropsychiatric disorder associated with expression of autoantibodies to ionotropic glutamate receptor, NMD A 2A (GiuN2A), expression of anti-double-stranded (ds) DNA antibodies that cross react with one or more subunits of the NMD A receptor, or a mutation in the ionotropic glutamate receptor NMD A type subunit 2A (GRIN2A) gene. The methods involve administering a memantine, or a pharmaceutically acceptable salt thereof, to a subject suffering from a neuropsychiatric disorder associated with expression of GluN2A or a mutation in the GRIN2A gene.

The present invention provides a composition for preventing or treating neurodegenerative diseases, the composition containing a phosphodiesterase 5 inhibitor (PDE5 inhibitor) and an N-methyl-D-aspartate-receptor (NMDA-receptor) antagonist, and a method of using the same, wherein the PDE5 inhibitor is mironafil, sildenafil, vardenafil, tadalafil, udenafil, dabigatafil, avanafil, a pharmaceutically acceptable salt, a solvate, a hydrate or a mixture thereof; and the NMDA-receptor antagonist is selected from the group consisting of memantine, amantadine, ketamine, trasolodipine, Lanisidine, lispiranet, pethidine, levonorfen, methadone, dextroproxen, tramadol, ktormitone, dextromethorphan (DXM), phencyclidine (PCP), and methoxyximine (MXE), pharmaceutically acceptable salts, solvates, hydrates, and mixtures thereof; and pharmaceutically acceptable salts, solvates, hydrates, and mixtures thereof, as well as pharmaceutically acceptable salts, solvates, hydrates, and mixtures thereof, as well as pharmaceutically acceptable salts, solvates, hydrates, and mixtures thereof, or pharmaceutically acceptable salts, solvates, hydrates, and mixtures thereof; and the neurodegenerative disease is dementia, Parkinson's disease (PD), dementia with Lewy bodies (DLB), Alzheimer's disease (AD), Huntington's disease (HD), multiple sclerosis (MS), vascular dementia (VaD), amyotrophic lateral sclerosis (ALS), frontotemporal dementia or a mixed cause thereof.

The present application provides a derivative of memantine, wherein at least one hydrogen atom on the amino group of memantine is replaced by a peptide chain containing 5-10 amino acids, and the peptide chain at least contains the sequence of Arg-Glu-Arg-Met-Ser. The derivative of memantine modified by the RERMS pentapeptide has lower cytotoxicity, higher neurotrophic activity, and can promote the expression of Bcl-2 protein, compared with memantine.

The invention provides sustained release microspheres containing memantine or salt derivatives thereof and a preparation method of the sustained release microspheres. The preparation method comprises the following steps: preparing an external water phase W2, dissolving a surfactant and an osmotic pressure regulator in ultrapure water, and regulating the pH value to a target pH value by using a pH regulator; preparing an oil phase O, dissolving memantine or a salt derivative thereof and a biocompatible polymer in an organic solvent, and carrying out vortex to dissolve the memantine or the salt derivative thereof and the biocompatible polymer; mixing the external water phase W2 with the oil phase O, and adding the mixture into a rapid membrane emulsifier to prepare an emulsion; and stirring, curing, washing and freeze-drying the emulsion to obtain the sustained-release microspheres containing memantine or the salt derivatives thereof. According to the invention, the medication compliance of the Alzheimer's disease patient can be effectively improved, the medication frequency of the patient is greatly reduced, and the repeated or worsened condition caused by the fluctuation of the blood concentration due to wrong taking and missed taking can be effectively avoided; meanwhile, the sustained-release microspheres for injection can effectively avoid adverse reaction of gastrointestinal tracts caused by oral administration, and have obvious clinical advantages.

The present disclosure relates to a method of treating or ameliorating symptoms of a motor neurone disease and improving motor neuron survival in a subject, more specifically treating or ameliorating symptoms of amyotrophic lateral sclerosis (ALS) and related neurodegenerative disorders. The treatment method comprises administering a Janus kinase (JAK) inhibitor in combination with one or more compounds selected from a glutamate antagonist and an N-methyl-D-aspartate (NMDA) receptor antagonist, in particular baricitinib in combination with riluzole and / or memantine, and compositions and kits thereof for same.

The present invention provides a composition for preventing or treating a neurodegenerative disease containing a phosphodiesterase 5 inhibitor (PDE5 inhibitor) and an N-methyl-D-aspartate-receptor (NMDA-receptor) antagonist and a method using thereof, wherein the PDE5 inhibitor is mirodenafil, sildenafil, vardenafil, tadalafil, udenafil, dasantafil, avanafil, pharmaceutically acceptable salts, solvates, hydrates, or a mixture thereof; and the NMDA-receptor antagonist is selected from among memantine, amantadine, ketamine, traxoprodil, lanicemine, rislenemdaz, pethidine, levorphanol, methadone, dextropropoxyphene, tramadol, ketobemidone, dextromethorphan (DXM), phencyclidine (PCP), and methoxetamine (MXE), pharmaceutically acceptable salts, solvates, hydrates and a mixture thereof; and the neurodegenerative disease is dementia, Parkinson's disease (PD), Dementia with Lewy body (DLB), Alzheimer's disease (AD), Huntington's disease (HD), Multiple sclerosis (MS), Vascular Dementia (VaD), Amyotrophic Lateral Sclerosis (ALS), frontotemporal dementia, or a mixed etiologies thereof.

This invention relates to the field of pharmaceutical technology, providing memantine derivatives, their preparation methods, and their application in the preparation of drugs for treating soluble cyclooxygenase-mediated diseases. The memantine derivatives provided by this invention have typical urea or amide structures. The urea and amide structures serve as the primary pharmacophores of sEH (hydrophobic epoxide hemoglobin). The memantine moiety, as a hydrophobic segment, interacts with the receptor hydrophobically. Molecular docking shows that the memantine moiety, as a hydrophobic segment, interacts with the receptor hydrophobically, particularly when both R1 and R2 are methyl groups, which enhances the van der Waals forces. Therefore, the memantine derivatives provided by this invention exhibit high inhibitory activity against human (HsEH) and murine sEH (MsEH), and can be used as sEH inhibitors in the preparation of drugs for treating soluble cyclooxygenase-mediated diseases, showing broad application prospects.