43results about How to "Improve blood-brain barrier permeability" patented technology

Certain substances (e.g., large molecules) that ordinarily cannot traverse the blood brain barrier can be introduced into the brain by applying an alternating electric field to the brain for a period of time, wherein the frequency of the alternating electric field is selected so that application of the alternating electric field increases permeability of the blood brain barrier. In some embodiments, the frequency of the alternating electric field is less than 190 kHz (e.g., 100 kHz). Once the permeability of the blood brain barrier has been increased, the substance is able to cross the blood brain barrier.

The present invention includes methods of improving proteolytic stability of a polypeptide, comprising alkylating at least one selected from the group consisting of a N-terminus amino group, the NH group of the N-terminus first internal amide bond, another primary amino group, a thiol group and a thioether group within the polypeptide. The present invention further includes polypeptides incorporating such chemical modifications.

The present invention relates to a serine derivative compound having improved blood-brain barrier (BBB) permeability and the use thereof, and more particularly, to a novel serine derivative compound having improved blood-brain barrier permeability compared to L-serine, and a pharmaceutical composition for preventing, treating or alleviating nervous system diseases such as cognitive disorder, intellectual disability, microcephaly, epilepsy, neurodevelopmental disorder, dementia, autism spectrum disorder, Down's syndrome, Rett's syndrome, fragile X syndrome, Alzheimer's disease, Parkinson's disease, Huntington's disease, and amyotrophic lateral sclerosis, the pharmaceutical composition containing the compound as an active ingredient. The compound of Formula (I) or a pharmaceutically acceptable salt thereof as an active ingredient for the pharmaceutical composition for preventing or treating central nervous system diseases according to the present invention exhibits significantly improved blood-brain barrier permeability, activates neuronal cell proliferation, and exhibits a neuronal protective effect of inhibiting neuronal cell death resulting from mitochondrial membrane potential damage and / or endoplasmic reticulum stress caused by oxidative stress, and exhibits improved blood-brain barrier permeability. Therefore, the compound has an excellent effect on the prevention, treatment and alleviation of central nervous system diseases such as cognitive disorder, intellectual disability, microcephaly, epilepsy, neurodevelopmental disorder, dementia, autism spectrum disorder, Down's syndrome, Rett's syndrome, fragile X syndrome, Alzheimer's disease, Parkinson's disease, Huntington's disease, and amyotrophic lateral sclerosis, and thus is a highly useful invention in the pharmaceutical industry, the food industry and the livestock industry.

The invention discloses a croton acylated catapol derivative which is prepared by esterifying catalpol and crotonic anhydride. The invention provides a corresponding preparation method and application, and the preparation method comprises the following steps: 1) dissolving catalpol into triethylamine, adding a catalyst 4-dimethylaminopyridine, adding crotonic anhydride under protection of nitrogengas, reacting for 12-36 hours at a temperature of 30-90 DEG C, and drying triethylamine by distilling to obtain a product, wherein a molar ratio of crotonic anhydride to catalpol is (6-18) to 1, anda molar ratio of 4-dimethylaminopyridine to catalpol is 1 to (9.5-10.5); and 2) dissolving the product in the step 1) into dichloromethane, adding an alkaline agent, standing and layering, discardingan upper-layer water phase, drying an organic phase to remove water, drying dichloromethane by distilling, purifying and separating, evaporating-drying, and filtering to obtain the catapol derivative.The catapol derivative has good anti-ageing activity, improves blood-brain barrier permeability of catapol, and has an esterification rate of 99.16%.