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assay prodrugs, process for preparing them, their use, therapeutic systems for transdermal application and composition comprising them
专利权人:
TECHFIELDS INC.;CHONGXI YU
发明人:
CHONGXI YU,LINA XU
申请号:
BRPI0721709
公开号:
BRPI0721709A2
申请日:
2007.06.04
申请国别(地区):
BR
年份:
2013
代理人:
摘要:
TEST PRE-PHARMACEUTICALS, PROCESS FOR THE PREPARATION OF THEMSELVES, THEIR USE, THERAPEUTIC TRANSDERMAL APPLICATION SYSTEMS AND COMPOSITION UNDERSTANDING THEM. The present invention relates to novel positively charged NSAIA prodrugs in the general formulas (1, 2a, 2b, 2c or 2d). Structure 1, 2a, 2b, 2c or 2d has been designed and synthesized. The compounds of the general formulas (1, 2a, 2b, 2c, or 2d) 'Structure 1, 2a, 2b, 2c or 2d' above may be prepared from metal salts, organic base salts, or base salts. NSAIAs with appropriate halide compounds. The positively charged amino groups on the prodrugs in this invention greatly increase the solubility of the drugs in water and will be linked to the negative charge of the membrane major phosphate group. Thus, the local concentration of the outer membrane or skin will be very high and will facilitate the passage of these prodrugs from a high concentration region to a low concentration region. This binding will slightly affect the membrane and may make room for the lipophilic portion of the prodrug. When membrane molecules move, the membrane may 'break' somewhat due to the binding of the prodrug. This will allow the prodrug to penetrate the membrane. At a pH of 7.4, only about 99% of the amino group will be protonated. When the amino group is not protonated, the bond between the prodrug amino group and the main membrane phosphate group will be disassociated, and the prodrug will penetrate the membrane completely. When the prodrug amino group passes across the membrane and becomes protonated, the prodrug is pushed into the cytosol, a concentrated semi-liquid aqueous solution or suspension. These prodrugs may be used to treat and prevent diabetes (types I and / or uncle II), abnormal blood glucose and lipid levels, stroke, heart attack, and other heart and vascular diseases, Alzheimer's disease, Parkinson's disease, and others. neurodegenerative diseases, psoriasis, discoid lupus erythematosus, systemic lupus erythematosus
来源网站:
中国工程科技知识中心
来源网址:
http://www.ckcest.cn/home/

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