http://rdf.ncbi.nlm.nih.gov/pubchem/patent/EP-4043447-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_a160054f76336c1a428663b1fd206a46 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07J53-004 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-58 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07J17-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-341 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D307-04 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P9-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D307-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-341 |
| filingDate | 2020-09-03-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_0bfe1ba213f2041fdfeab3436062751e http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_53f8fd885b83b2c4ccbf33fb81a06f39 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_a76912e958eea23505c9bc2ec75664a7 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_9ab48e46ea6aee0209eba71d88a5368c |
| publicationDate | 2022-08-17-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | EP-4043447-A1 |
| titleOfInvention | Halogenated tetracyclic triterpene derivative, preparation and application thereof |
| abstract | The invention provides a series of halogenated tetracyclic triterpene derivatives and their preparation and application. It is represented by the following general structural formula:wherein R<sub>1</sub> is halogen, R<sub>2</sub> is H, and the halogen is selected from fluorine, chlorine, bromine or iodine; or R<sub>1</sub> and R<sub>2</sub> are each fluorine, and R<sub>3</sub> is an amine, alcohol, amino acid, peptide or phosphate linked to oxygen through an acyl group.The derivatives of the present invention are relatively stable in rat whole blood through pharmacokinetic studies. The absolute bioavailability after a single intragastric administration for male and female rats was 15.6% and 28.4% respectively. The mean bioavailability was 22%. The derivatives of the present invention showed better in vivo activities compared with the existing standard drugs enalapril and sacubitril valsartan sodium. Meanwhile, hydrophilic prodrugs of the tetracyclic triterpenoid derivatives in the present invention were prepared, which improved the solubility and had better drug-likeness properties. The derivatives of the present invention can be used for preparing cardiovascular medicines and have great application value. |
| priorityDate | 2019-09-06-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 258.