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Pro-drugs of NSAIAs With Very High Skin and Membranes Penetration Rates and Their New Medicinal Uses
专利权人:
테크필즈 인크;위, 충시
发明人:
위, 충시,쉬, 리나
申请号:
KR1020197021994
公开号:
KR1020190091378A
申请日:
2007.06.04
申请国别(地区):
KR
年份:
2019
代理人:
摘要:
New positively charged NSAIA drug precursors of structure (1, 2a, 2b, 2c, or 2d) structures 1, 2a, 2b, 2c or 2d were designed and synthesized. Structure 1 The above general formula (1, 2a, 2b, 2c, or 2d) "structure 1, 2a, 2b, 2c, or 2d" compounds are prepared by reaction with metal salts, organic base or immobilized base salts of NSAIA and suitable halide compounds. Can be. Positively charged amino groups greatly increase the water solubility of the drug. The positive charge of these drug precursor amino groups will be combined with the negative conversion of the phosphate head group of the membrane. Thus, the local concentration outside the membrane or skin is so high that these drug precursors will easily pass from the high concentration region to the low concentration region. This binding will slightly disrupt the membrane and create some space for the lipophilic portion of the drug precursor. When membrane molecules move, the membrane is weakly cracked by drug precursor binding. The drug precursor is then inserted into the membrane. At pH 7.4, only about 99% of the amino groups are protonated. When the amino group is not protonated, the bond between the amino group of the drug precursor and the phosphate head group of the membrane will break and the drug precursor will enter the membrane completely. The amino group of the drug precursor enters the other side of the membrane and is thus protonated, after which the drug is drawn into the cytoplasm, which is a semi-liquid concentrated aqueous solution or suspension. These drug precursors include diabetes (type I and / or II), abnormal blood glucose and blood lipid levels, stroke, myocardial infarction, and other cardiovascular diseases, Alzheimer''s disease, Parkinson''s disease, and other neurodegenerative diseases, psoriasis, disc erythema Lupus, systemic lupus erythematosus (SLE), autoimmune hepatitis, scleroderma, Sjogren''s syndrome, rheumatoid arthritis, polymyositis, scleroderma, Hashimoto''s thyroiditis, ju
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