http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CN-108047207-A
Outgoing Links
Predicate | Object |
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assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_be2c55a9de09e08e3404c0a5a1ae4dc7 |
classificationCPCAdditional | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07B2200-05 |
classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D403-04 |
classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-506 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P35-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D403-04 |
filingDate | 2018-01-30-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_f6819f068b37ac6f1171bd973c7ba697 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_3500c2cc2e65c1e6daab0e93025827aa http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_40b500137a9a6010b3d54555ea74252b |
publicationDate | 2018-05-18-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationNumber | CN-108047207-A |
titleOfInvention | N-[5-(pyrimidine-2-amino)-2,4-disubstituted phenyl]-2-fluoroacrylamide deuterated product and its application |
abstract | The present invention provides a kind of N-[5-(pyrimidine-2-amino)-2,4-disubstituted phenyl]-2-fluoroacrylamide deuterated substance, such as the compound shown in formula (I), its pharmaceutical acceptable salts or prodrugs thereof. Compared with the prior art, the present invention replaces the hydrogen atom on the acrylamide group with the fluorine atom, and the deuterium atom replaces the hydrogen atom in other parts, and the compound is not easy to be recognized by the active substance in the body after entering the body; at the same time, due to the C-F bond and The C-D bond is stable and not easy to break, and the redox stability of the compound is enhanced, making it difficult to be metabolically degraded in vivo; in addition, the introduction of fluorine-containing deuterium-containing groups into organic molecules improves the penetration ability of membranes and tissues, and enhances its bioavailability Therefore, compounds containing both fluorine-carbon bonds and deuterium-carbon bonds are used as EGFR tuners to treat or prevent cancer, slow down the degradation rate in vivo, prolong the half-life of the drug, increase the blood drug concentration, and expand the administration time interval . |
isCitedBy | http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CN-113387935-B http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CN-113387935-A http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CN-108675993-A http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CN-113582976-A |
priorityDate | 2018-01-30-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 26.