http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CN-101676291-B

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filingDate 2008-09-18-04:00^^<http://www.w3.org/2001/XMLSchema#date>
grantDate 2012-05-09-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_05d8eb41e60efc608b75e37a0649d16c
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publicationDate 2012-05-09-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber CN-101676291-B
titleOfInvention A kind of rapamycin carbonate analogue, its pharmaceutical composition and its preparation method and application
abstract The invention belongs to the field of medicinal chemistry, and discloses a rapamycin carbonate analog shown in structural formula I or a pharmaceutically acceptable salt thereof, a pharmaceutical composition thereof, a preparation method and application thereof. Compared with rapamycin, the rapamycin carbonate analog of the present invention enhances its water solubility by introducing water-soluble and polar groups such as hydroxyl groups, and its pharmacological and pharmacokinetic properties are improved. Biological tests on different tumor strains show that its antitumor activity is superior to that of rapamycin; compared with rapamycin and the marketed rapamycin analogue CCI-779, this type of compound has better pharmacokinetics The drug is more easily absorbed and distributed in tumor tissue; systematic immunosuppressive biological activity experiments show that this type of compound has higher immunosuppressive activity than rapamycin. The preparation method of the rapamycin carbonate analogue provided by the invention is simple, strong in operability, high in yield, and has good prospects for drug development.
priorityDate 2008-09-18-04:00^^<http://www.w3.org/2001/XMLSchema#date>
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