Predicate |
Object |
assignee |
http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_dc62792656aa2e858252e97e5ffaca79 http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_61f88efcda59d7062a4252ecf6886f58 |
classificationCPCInventive |
http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-675 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-683 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/A61P9-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07F9-65616 |
classificationIPCInventive |
http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-675 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07F9-6561 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P9-10 |
filingDate |
2011-02-22-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
inventor |
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_de8b9356c77d610291aa2c6f3fa0e999 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_9cbbfe028bbdff71d058985310fc52f1 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_7500a6be9137ac139b7553c8cc518d0a http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_0b8ef24b97a8ad4eba7126f0b764cd22 |
publicationDate |
2013-01-02-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationNumber |
EP-2539352-A2 |
titleOfInvention |
Amp derivatives for treating cardiac diseases |
abstract |
Phosphonate and phosphinate N-methanocarba derivatives of AMP including their prodrug analogs are described. MRS2339, a 2-chloro-AMP derivative containing a (N)- methanocarba (bicyclo[3.1.0]hexane) ring system in place of ribose, activates P2X receptors, ligand-gated ion channels. Phosphonate analogues of MRS2339 were synthesized using Michaelis-Arbuzov and Wittig reactions, based on the expectation of increased half-life in vivo due to the stability of the C-P bond. When administered to calsequestrin-overexpressing mice (a genetic model of heart failure) via a mini-osmotic pump (Alzet), some analogues significantly increased intact heart contractile function in vivo, as assessed by echocardiography-derived fractional shortening (FS) as compared to vehicle-infused mice. The range of carbocyclic nucleotide analogues for treatment of heart failure has been expanded. |
priorityDate |
2010-02-22-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
type |
http://data.epo.org/linked-data/def/patent/Publication |