Predicate |
Object |
assignee |
http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_9dd1cf56ed8d12cc30ad6a693968ce27 |
classificationCPCInventive |
http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K45-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K47-545 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D307-68 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-423 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-28 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-341 |
classificationIPCInventive |
http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D307-68 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-341 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P25-28 |
filingDate |
2016-06-15-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
inventor |
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_2c9096cb32dfbe9dbd6bdac4e603df9f http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_ae3601d4ede82480d078951f05aa4c2d http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_760d406c999b0e61b783b1c9d53b8099 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_509914cabbcdb0fbfd18f3ff411274d1 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_a6e6a7a150f51c750972e74e4ade80f2 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_357cdb8d51cdbc3771d305ea5ae97bcb |
publicationDate |
2016-12-22-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationNumber |
WO-2016203402-A1 |
titleOfInvention |
Bis-furan derivatives as transthyretin (ttr) stabilizers and amyloid inhibitors for the treatment of familial amyloid polyneuropathy (fap) |
abstract |
The design and synthesis of a novel bis-furan scaffold tailored for high efficiency at inhibiting transthyretin amyloid formation is reported. In vitro results show that the discovered compounds are more efficient inhibitors of amyloid formation than tafamidis, a drug currently used in the treatment of familial amyloid polyneuropathy (FAP), despite their lower molecular weight and lipophilicity. Moreover, ex vivo experiments with the strongest inhibitor in the series, conducted in human blood plasma from normal and FAP Val30Met-transthyretin carriers, disclose remarkable affinity and selectivity profiles. The promises and challenges facing further development of this compound are discussed under the light of increasing evidence implicating transthyretin stability as a key factor not only in transthyretin amyloidoses and several associated co-morbidities, but also in Alzheimer's disease. |
isCitedBy |
http://rdf.ncbi.nlm.nih.gov/pubchem/patent/WO-2020205683-A1 |
priorityDate |
2015-06-15-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
type |
http://data.epo.org/linked-data/def/patent/Publication |