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

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.

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.

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.

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).

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).

A compound represented by the formula (I) or a pharmaceutically acceptable salt thereof: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).

A compound represented by the formula (I) or a pharmaceutically acceptable salt thereof: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).

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).

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.

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.

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.

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.

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.