| Predicate |
Object |
| assignee |
http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_f95e45fd68a57404ee589cb5f9283ecf
http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_fd5e5cf13b3b87b366a8d558bf8c17a0
http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_2a819eda0adf22936a52362eeebb9fb4
http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_f0addd7bd30ed6d7d6b9c4f5d9c6cc57 |
| classificationCPCAdditional |
http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07B2200-07 |
| classificationCPCInventive |
http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P29-00
http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07C235-74
http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07C237-22
http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-22 |
| classificationIPCInventive |
http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07C229-24
http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-22
http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-195
http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P29-00 |
| filingDate |
2010-04-19-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor |
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_bdb9bafb86f27b35089eec9f6e00025c
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_bbe281cfc99e56c9a1a54a1e39a0e877
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_9c2e9e20c0c630a62942035a417c3554 |
| publicationDate |
2012-04-19-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber |
US-2012095096-A1 |
| titleOfInvention |
2-oxamide inhibitors of phospholipase a2 activity and cellular arachidonate release based on dipeptides and pseudopeptides |
| abstract |
The disclosure provides a series of 2-oxoamides based on dipeptides and pseudodipeptides, which were synthesized and their activities toward two human intracellular phospholipases A2 (GIVA CPLA 2 and GVIA 1PLA 2 ) and one human secretory phospholipase A2 (GVsPLA 2 ) were evaluated. Derivatives containing a free carboxyl group are selective GIVA cPLA 2 inhibitors. A derivative based on the ethyl ester of an ether pseudodipeptide is the first 2-oxoamide, which preferentially inhibits GVIA iPLA 2 . The effect of 2-oxoamides on the generation of arachidonic acid from RAW 264.7 macrophages was also studied. It was found that selective GIVA cPLA 2 inhibitors preferentially inhibited cellular arachidonic acid release; in which one pseudodipeptide gave an IC50 value of 2 μM. |
| priorityDate |
2009-04-20-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type |
http://data.epo.org/linked-data/def/patent/Publication |