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42results about How to "Inhibition of neurotoxic effects" patented technology

3-Substituted-4-pyrimidone derivatives

A pyrimidone derivative represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof having inhibitory activity against tau protein kinase 1:wherein R1 represents a C1-C12 alkyl group which may be substituted;R represents, for example, a group represented by the following formula (II):wherein R2 and R3 independently represent a hydrogen atom or a C1-C8 alkyl group;R4 represents a benzene ring which may be substituted, a naphthalene ring which may be substituted, an indan ring which may be substituted, a tetrahydronaphthalene ring which may be substituted, or an optionally substituted heterocyclic ring having 1 to 4 hetero atoms selected from the group consisting of oxygen atom, sulfur atom and nitrogen atom, and having 5 to 10 ring-constituting atoms in total.
Owner:MITSUBISHI TANABE PHARMA CORP

3-Substituted-4-pyrimidone derivatives

A pyrimidone derivative represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof having inhibitory activity against tau protein kinase 1: wherein R1 represents a C1-C12 alkyl group which may be substituted; R represents, for example, a group represented by the following formula (II): wherein R2 and R3 independently represent a hydrogen atom or a C1-C8 alkyl group; R4 represents a benzene ring which may be substituted, a naphthalene ring which may be substituted, an indan ring which may be substituted, a tetrahydronaphthalene ring which may be substituted, or an optionally substituted heterocyclic ring having 1 to 4 hetero atoms selected from the group consisting of oxygen atom, sulfur atom and nitrogen atom, and having 5 to 10 ring-constituting atoms in total.
Owner:MITSUBISHI TANABE PHARMA CORP

3-substituted-4-pyrimidone derivatives

A pyrimidone derivative represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof having inhibitory activity against tau protein kinase 1: wherein R1 represents a C1-C12 alkyl group which may be substituted; R represents, for example, a group represented by the following formula (II): wherein R2 and R3 independently represent a hydrogen atom or a C1-C8 alkyl group; R4 represents a benzene ring which may be substituted, a naphthalene ring which may be substituted, an indan ring which may be substituted, a tetrahydronaphthalene ring which may be substituted, or an optionally substituted heterocyclic ring having 1 to 4 hetero atoms selected from the group consisting of oxygen atom, sulfur atom and nitrogen atom, and having 5 to 10 ring-constituting atoms in total.
Owner:SANOFI AVENTIS SA +1

3-Substituted-4-pyrimidone derivatives

a pyrimidone derivative represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof having inhibitory activity against tau protein kinase 1: wherein R1 represents a C1-C12 alkyl group which may be substituted; R represents, for example, a group represented by the following formula (II): wherein R2 and R3 independently represent a hydrogen atom or a C1-C8 alkyl group; R4 represents a benzene ring which may be substituted, a naphthalene ring which may be substituted, an indan ring which may be substituted, a tetrahydronaphthalene ring which may be substituted, or an optionally substituted heterocyclic ring having 1 to 4 heteno atoms selected from the group consisting of oxygen atom, sulfur atom and nitrogen atom, and having 5 to 10 ring-constituting atoms in total.
Owner:SANOFI AVENTIS SA +1

2,3,6-Trisubstituted-4-pyrimidone derivatives

A pyrimidone derivative having tau protein kinase 1 inhibitory activity which is represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof; useful for prventive and / or therapeutic treatment of diseass such as neurodegenerative diseases (e.g. Alzheimer disease); wherein Q represents CH or nitrogen atom; R represents a C1-C12 alkyl group; the ring of Formula (I): represents piperazine ring or piperidine ring; each X independently represents a C1-C8 alkyl group, an optionally partially hydrogenated C6-C10 aryl ring, an indan ring or the like; m represents an integer of 1 to 3; each independently represents a halogen atom, a hydroxy group, a cyano group, a C1-C6 alkyl group or the like; n represents an integer of 0 to 8; when X and Y or two Y groups are attached on the same carbon atom, they may combine to each other to form a C2-C6 alkylene group.
Owner:SANOFI SA +1

2,3,6-Trisubstituted-4-pyrimidone derivatives

A pyrimidone derivative having tau protein kinase 1 inhibitory activity which is represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof; useful for prventive and / or therapeutic treatment of diseass such as neurodegenerative diseases (e.g. Alzheimer disease); wherein Q represents CH or nitrogen atom; R represents a C1-C12 alkyl group; the ring of Formula (I): represents piperazine ring or piperidine ring; each X independently represents a C1-C8 alkyl group, an optionally partially hydrogenated C6-C10 aryl ring, an indan ring or the like; m represents an integer of 1 to 3; each independently represents a halogen atom, a hydroxy group, a cyano group, a C1-C6 alkyl group or the like; n represents an integer of 0 to 8; when X and Y or two Y groups are attached on the same carbon atom, they may combine to each other to form a C2-C6 alkylene group.
Owner:SANOFI SA +1

2-morpholino-4-pyrimidone compound

A compound represented by the formula (I), an optically active isomer thereof, or a pharmaceutical acceptable salt thereof: wherein X represents CH or N; represents a C1-C12 alkyl; R2 represents a hydrogen atom, or the like; R′ represents a C1-C6 alkyl or the like; q represents 0 or an integer of 1 to 7; Y represents a C1-C6 alkyl or the like; p represents 0 or an integer of 1 to 5; R represents a 2,3-dihydroindolyl or the like, which is used for preventive and / or therapeutic treatment of a disease caused by tau protein kinase 1 hyperactivity such as a neurodegenerative diseases (e.g. Alzheimer disease).
Owner:MITSUBISHI TANABE PHARMA CORP +1

Pyrimidone derivatives

A pyrimidone derivative represented by the formula (I) or a salts thereof:wherein R1 represents an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group, an aryl group and the like; R2 represents a hydrogen atom, hydroxyl group, an alkyl group, an alkenyl group and the like, R3 represents a pyridyl group, and a medicament comprising said derivative or a salt thereof as an active ingredient which is used for preventive and / or therapeutic treatment of a disease caused by tau protein kinase 1 hyperactivity such as Alzheimer disease.
Owner:MITSUBISHI CHEM CORP

2-substituted-6-heterocyclic pyrimidone derivatives as tau protein kinase 1 inhibitors

InactiveUS20100113775A1Improves neutrophilImproves megakaryocyte recoveryOrganic active ingredientsSenses disorderArylHydrogen atom
A compound represented by the formula (I), an optically active isomer thereof, or a pharmaceutical acceptable salt thereof: wherein each R1 represents hydrogen atom or the like; X represents oxygen atom or the like; A represents a C3-C7 cycloalkyl group, a C6-C10 aryl group or a heterocyclic group; R6 represents a halogen atom or the like; s represents 0 or an integer of 1 to 5; Q represents a pyridine ring which may be substituted or pyrimidine ring; and R2 represents hydrogen atom or the like, which is used for preventive and / or therapeutic treatment of a disease caused by abnormal activity of tau protein kinase 1 such as a neurodegenerative diseases (e.g. Alzheimer disease).
Owner:MITSUBISHI TANABE PHARMA CORP +1

6-(pyridinyl)-4-pyrimidone derivates as tau protein kinase 1 inhibitors

A compound represented by the formula (I), an optically active isomer thereof, or a pharmaceutical acceptable salt thereof:wherein R1 represents a C1-C12 alkyl; R2 represents a hydrogen atom or the like; R3 represents a halogen or the like; q represents an integer of 1 to 7; R4 represents a halogen or the like; p represents 0 or an integer of 1 to 5; R5 represents a C6-C10 aryl, a heterocycle or the like; and X represents oxygen, NH, or the like, which is used for preventive and / or therapeutic treatment of a disease caused by tau protein kinase 1 hyperactivity such as a neurodegenerative diseases (e.g. Alzheimer disease).
Owner:MITSUBISHI TANABE PHARMA CORP +1

Visual stimuli maze test for detecting visual abnormalities in prodromal alzheimer's disease and in alzheimer's disease

Disclosed herein is a rodent and human behavioral test for evaluating visual dysfunctions associated with the retinal changes in Alzheimer disease progression. In one example, the inventors developed a maze that tests rodent's ability to identify (1) specific contrasts, (2) specific colors, (3) certain items in the visual field, and (4) other ‘non-typical’ peripheral and night vision functions associated with AD. For instance, the inventors developed a maze the tests the rodents ability to avoid certain colors or contrasts gradients. The maze may include certain rooms with specific visual markers (e.g., colors, contrasts, objects or other visual features) that also contain shock plates.
Owner:CEDARS SINAI MEDICAL CENT

3-Substituted-4-pyrimidone derivatives

A pyrimidone derivative represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof useful as a tau protein kinase 1 inhibitor:wherein X represents CH or nitrogen atom; R1 represents a C?1#191-C?12#191 alkyl group which may be substituted; R2 represents a C?1#191-C?8#191 alkyl group which may be substituted, a benzene ring which may be substituted, a naphthalene ring which may be substituted, an indan ring which may be substituted, a tetrahydronaphthalene ring which may be substituted, or an optionally substituted heterocyclic ring having 1 to 4 hetero atoms selected from the group consisting of oxygen atom, sulfur atom, and nitrogen atom, and having 5 to 10 ring-constituting atoms in total.
Owner:SANOFI SA +1

A nanocomposite with therapeutic effect on Alzheimer's disease, and preparation method and application thereof

The invention discloses a nanocomposite with therapeutic effect on Alzheimer's disease and a preparation method thereof. The nanocomposite comprises a liposome synthesized from lecithin, cholesterol,distearoyl phosphatidylethanolamine and phosphatidic acid and a medicine with the effect of treating Alzheimer's disease contained in the liposome, wherein the liposome is modified with polyethylene glycol and transferrin. The invention utilizes Pep63 to inhibit the neurotoxic effect of ADDLs in the brain of early Alzheimer's disease patients, and simultaneously combines the affinity effect of phosphatidic acid on A beta to play a double coordinating therapeutic effect according to different pathological processes of Alzheimer's disease; At that same time, the surface of the liposome is modifywith transferrin, so that the multifunctional nanocomposite has the brain targeting ability, and can enter the brain through the blood-brain barrier or play a therapeutic role in the periphery; And has the advantages of high safety, biocompatibility and small side effects.
Owner:XUZHOU MEDICAL UNIV

Pyrimidone compounds

A pyrimidone derivative represented by general formula (I) or a pharmaceutically acceptable salt thereof:wherein X represents hydrogen atom and Y represents hydroxyl group, or X represents fluorine atom and Y represents hydrogen atom; R1 represents a C1-6 alkyl group; R2 represents a morpholin-4-yl group which may be substituted, or the like, which is used for preventive and / or therapeutic treatment of a disease caused by tau protein kinase 1 hyperactivity such as a neurodegenerative diseases (e.g. Alzheimer disease).
Owner:MITSUBISHI TANABE PHARMA CORP

2-(cyclic amino)-pyrimidone derivatives

A compound represented by the formula (I), an optically active isomer thereof, or a pharmaceutical acceptable salt thereof:wherein R2 represents a hydrogen or the like; R3 represents methyl group or the like; R20 represents a halogen atom or the like; q represents an integer of 0 to 3; Z represent nitrogen atom, CH, or the like; R4 represents hydrogen or the like; R5 represents hydrogen or the like; R6 represents a substituted alkyloxy and the like; p represents an integer of 0 to 3; X represents bond, CH2, oxygen atom, NH, or the like; any one or more of R5 and R6, R5 and R4, R6 and R4, X and R5, X and R4, X and R6, and R6 and R6 may combine to each other to form a ring, which is used for preventive and / or therapeutic treatment of a disease caused by tau protein kinase 1 hyperactivity such as a neurodegenerative diseases (e.g. Alzheimer disease).
Owner:SANOFI SA +1

Ferulic acid derivatives, preparation and application of ferulic acid derivatives

The invention provides ferulic acid derivatives adopting a structure shown in formula I or formula II. Starting from the mechanism of various mechanisms causing brain injury after cerebral stroke and the action of ferulic acid in treatment of the cerebral stroke, alkane is taken as a joint arm, ADT-OH (5-(4-hydroxyphenyl)-3H-1,2-dithiole-3-thione) and ferulic acid are connected through ether linkage and ester linkage, and the ferulic acid derivatives are obtained. The invention further provides the application of the ferulic acid derivatives in preparation of drugs for preventing and / or treating cerebral stroke diseases.
Owner:江苏冠瑜生物科技有限公司

3-[1,4]oxazepane-4-pyrimidone derivatives

A compound represented by the formula (I) or a pharmaceutically acceptable salt thereof:wherein Z represents nitrogen atom, C—F or the like; R1 represents a C1-C3 alkyl group; Y represents oxygen atom or N—R7; R2, R3, R4, R5, R6 and R7 each independently represents hydrogen atom, a C1-C6 alkyl group, or a group represented by the formula (II):which is used for preventive and / or therapeutic treatment of a disease caused by tau protein kinase 1 hyperactivity such as a neurodegenerative diseases (e.g. Alzheimer disease).
Owner:MITSUBISHI TANABE PHARMA CORP

Antrodia camphorata mycelium active substance and composition for protecting nerve cells

The invention discloses an antrodia camphorata mycelium active substance and a composition for protecting nerve cells. Under the noncytotoxic concentrations, i.e., 50 [mu]M, the antrodia camphorata mycelium active substance can inhibit the cytotoxicity caused by 10 [mu]M of amyloid protein (beta-amyloid (25-35)), and also can inhibit the cell apoptosis due to the mitochondrion breakage caused by 1-methyl-4-phenylpyridine (MPP<+>), and therefore, the antrodia camphorata mycelium active substance has the potential of preventing neurodegenerative diseases.
Owner:GRAPE KING

Diarylmethylene disulfide compound as well as preparation method and application thereof

The invention relates to the technical field of medicines and in particular relates to a diarylmethylene disulfide compound as well as a preparation method and application thereof. An experiment result shows that on a cell model, the diarylmethylene disulfide compound provided by the invention has an effect of inhibiting neurotoxicity caused by excessive glutamic acid and an effect of inhibiting neurotoxicity caused by hydrogen peroxide; the diarylmethylene disulfide compound also has a platelet aggregation resisting effect and can be used for reducing a cerebral infarct area in a mouse MCAO (Middle Cerebral Artery Occlusion) model. The results show that the diarylmethylene disulfide compound provided by the invention can have prevention and / or treatment effects on cerebral stroke.
Owner:SUZHOU UNIV

Polypeptide and gene vaccine used for treating alzheimer disease

InactiveCN103450347APrevent oligomerizationBlock hydrophobic interactionsNervous disorderGenetic material ingredientsAntigenAβ oligomers
The invention discloses a polypeptide used for treating alzheimer disease (AD). The amino acid sequence of the polypeptide is Ile-Ile-Gly-Leu-Met-Val-Gly-Gly-Val-Val-Ile-Ala. The polypeptide is smart in concept, an Abeta1-42 carboxyl terminal polypeptide Abeta31-42 is taken as an antigen, Th1 immune cell mediated self immunity inflammatory reactions, induced by Abeta16-30, are avoided, an organism can also be effectively induced to produce an antibody for identifying an Abeta1-42 carboxyl terminal, Abeta oligomerization is prevented, neurovirulence of an Abeta oligomer is effectively inhibited, and the aim of treating AD is achieved.
Owner:SICHUAN BAILI PHARM CO LTD

Brain-targeting functional nucleic acid and use thereof

InactiveUS20140051637A1Excellent in brain migrationImprove stabilityOrganic active ingredientsNervous disorderDiseaseMedicine
The purpose of the invention is to provide a novel therapeutic agent for Alzheimer's disease and use thereof. Provided is a therapeutic agent for Alzheimer's disease, which contains a CpG oligodeoxynucleotide structure having a brain migration and improved stability or a salt thereof as an active ingredient.
Owner:NAGOYA UNIVERSITY

Atisane compounds and use thereof

The present invention provides a novel compound exhibiting an excellent suppressing effect to cell injury caused by radicals and neurotoxicity induced by excitatory nuerotransmitters such as glutamate. Specifically, it provides a compound represented by the following formula, a salt thereof or a hydrate of them.Wherein Z represents a bivalent organic group and the like of from 2 to 3 carbon atom(s) which may have a substituent; and R3 represents a carboxyl group and the like.
Owner:EISIA R&D MANAGEMENT CO LTD

Application of compound in antagonization of accumulation of beta amyloid proteins

The invention discloses application of Hispolon in the antagonization of the accumulation of beta amyloid proteins 1-42. Alzheimer's disease (AD) is a neurodegenerative disease with nerve cell fiber entanglement, beta amyloid protein (Abeta) plaque deposition and cognitive function decline as pathological features, wherein Abeta protein extracellular toxicity accumulation is known as one of main pathogenetic links of the AD. The application finds that Hispolon is capable of inhibiting the formation of a beta folding structure of an Abeta monomer, the formation of oligomers and fiber structures by the Abeta monomer and the oligomer mediated nerve cell toxicity injury formed by the accumulation of Abeta proteins, namely that Hispolon can be applied to the inhibition of the accumulation effect of the beta amyloid proteins 1-42.
Owner:NORTHEAST NORMAL UNIVERSITY

Application of matrine in preparing drug for preventing and treating alzheimer disease

The invention belongs to field of drug research and particularly relates to a new application of matrine in preparing a drug for preventing and treating an alzheimer disease. Found by long term study, the matrine has the effect of significantly inhibiting or neutralizing cytotoxicity of A beta 42 monomer or A beta 42 oligomer; found by further detection, the matrine can inhibit the cytotoxicity of A beta 42 through inhibiting the aggregation of the A beta 42 monomer or the A beta 42 oligomer; therefore, the new application of the matrine in preparing the drug for preventing and treating the alzheimer disease is confirmed and a new drug selection for clinic treatment of the alzheimer disease is provided.
Owner:JILIN UNIV

Application of (1,2,3-trimethoxybenzene)-propenone in the preparation of drugs for improving neurotoxicity caused by glutamic acid

The application of (1,2,3-trimethoxybenzene)-propenone in the preparation of drugs for improving the neurotoxicity caused by glutamate, by increasing the mitochondrial membrane potential and mitochondrial aerobic metabolism, enhancing mitochondrial function, and activating biphasic Enzyme system, up-regulate the expression of biphasic enzyme genes, scavenge mitochondrial reactive oxygen species, (1,2,3-trimethoxyphenyl)-propenone, as an antioxidant targeting mitochondria, can regulate PI3K / Akt signaling pathway, restore Mitochondrial function damage and oxidative stress caused by glutamate, exert anti-oxidation and protect mitochondrial function, restore oxidative stress and mitochondrial damage caused by glutamate, thereby preventing acute neurotoxicity caused by glutamate Onset and progression of chronic brain injury.
Owner:XI AN JIAOTONG UNIV

Neutralizing monoclonal antibodies against B type botulinum neurotoxin, preparation method and use thereof

The invention discloses a neutrality monoclonal antibody against botulinum neurotoxin type B and also discloses a humanized modifier of the antibody. The antibody is prepared through the following method: firstly, the CDR region, variable region, IgG part or full gene of the antibody is prepared through molecular biological methods or other methods and is expressed in prokaryotic cells such as colibacillus, eukaryote cells such as yeast, or insect cells, vegetable cells or mammal cells such as CHO; and the antibody is obtained through purification. The antibody is characterized by strong specific neutralization activity and high affinity. In addition, the humanized antibody is characterized by low side and toxic effect. The neutrality monoclonal antibody and the humanized modifier of the antibody are suitable for the first aid treatment of botulinum neurotoxin type B intoxication and also for the detection of botulinum neurotoxin type B. Therefore, the antibody and the humanized modifier thereof have good application prospect.
Owner:MICROBE EPIDEMIC DISEASE INST OF PLA MILITARY MEDICAL ACAD OF SCI
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