http://rdf.ncbi.nlm.nih.gov/pubchem/patent/US-9422302-B2
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_1c8cbbf2290b3f3a9988da29598baa2c http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_86a533d313f31f6037d84e96156b0226 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D489-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D489-08 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-485 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D489-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D489-02 |
| filingDate | 2014-03-06-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| grantDate | 2016-08-23-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_dada438953532ee36174b4d3d146afb0 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_4d8b6ddf911bb51dd5532381b044b755 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_15b56fcceccd476bfaa6edbb590b3d00 |
| publicationDate | 2016-08-23-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | US-9422302-B2 |
| titleOfInvention | Mixed μ agonist/ δ antagonist opioid analgesics with reduced tolerance liabilities and uses thereof |
| abstract | An opioid narcotics used for the treatment of moderate-to-severe pain that primarily exert their analgesic effects through μ receptors. Although, traditional μ agonists can cause undesired side effects, including tolerance, addition of δ antagonists can attenuate said side effects. The present invention includes 4a,9-dihydroxy-7a-(hydroxymethyl)-3-methyl-2,3,4,4a,5,6-hexahydro-1H-4,12-methanobenzofuro[3,2-e]isoquinolin-7(7aH)-one (UMB 425) a 5,14-bridged morphinan-based orvinol precursor, along with analogs of morphine, dihydromorphine, hydromorphone, codeine, dihydrocodeine, hydrocodone and ethylmorphine. Although UMB 425 lacks δ-specific motifs, conformationally sampled pharmacophore models for μ and δ receptors predict it to have efficacy similar to morphine at μ receptors and similar to naltrexone at δ receptors, due to the compound sampling conformations in which the hydroxyl moiety interacts with the receptors similar to orvinols. UMB 425 exhibits a mixed μ agonist/δ antagonist profile as determined in receptor binding. UMB 425 has mixed μ agonist/δ antagonist properties in vitro that translate to reduced tolerance liabilities in vivo. |
| priorityDate | 2013-03-07-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 145.