http://rdf.ncbi.nlm.nih.gov/pubchem/patent/US-8105570-B2

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filingDate 2004-06-01-04:00^^<http://www.w3.org/2001/XMLSchema#date>
grantDate 2012-01-31-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_97702ba298695a932bbbdad2019995b9
publicationDate 2012-01-31-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber US-8105570-B2
titleOfInvention Methods and compositions for controlled release of drugs
abstract This invention provides a method and compositions for the controlled release of drugs that have been attached by means of a covalent bond to a polymer or other moiety that blocks activity of the drug until it has been released. A two-stage process is provided in which an unmasking reaction results in the formation of a chemical group that can then undergo a second reaction to release the drug. In a preferred embodiment, the narcotic analgesic fentanyl covalently attached to an inert polymer by way of its nitrogen through the formation of a quaternary vinylammonium salt, and then released by a sequence involving hydrolysis of an acetal that exposes an alcohol that may then undergo an intramolecular nucleophilic substitution reaction involving displacement of the nitrogen of oxycodone. The rate of this process may be controlled by controlling either or both of the rates of the acetal hydrolysis or the intramolecular substitution reaction, but is preferably controlled by the latter through varying the number of atoms in the chain connecting the alcohol group and the vinylic carbon, as well as by the addition of substituents on that chain. The drug-delivery molecules of this invention are useful for release of amine, alcohol and thiol drugs, including a number of narcotic analgesics, tricyclic amine antidepressants, and many others.
priorityDate 2001-12-14-04:00^^<http://www.w3.org/2001/XMLSchema#date>
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http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID235276464
http://rdf.ncbi.nlm.nih.gov/pubchem/protein/ACCP01259
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID127551320
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID226414168
http://rdf.ncbi.nlm.nih.gov/pubchem/protein/ACCP69048
http://rdf.ncbi.nlm.nih.gov/pubchem/compound/CID227
http://rdf.ncbi.nlm.nih.gov/pubchem/compound/CID70091
http://rdf.ncbi.nlm.nih.gov/pubchem/compound/CID7044
http://rdf.ncbi.nlm.nih.gov/pubchem/protein/ACCP01258
http://rdf.ncbi.nlm.nih.gov/pubchem/protein/ACCP69047
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID128558711
http://rdf.ncbi.nlm.nih.gov/pubchem/protein/ACCP01257
http://rdf.ncbi.nlm.nih.gov/pubchem/gene/GID436744
http://rdf.ncbi.nlm.nih.gov/pubchem/compound/CID62258
http://rdf.ncbi.nlm.nih.gov/pubchem/protein/ACCP69046
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID128588482
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID226395164
http://rdf.ncbi.nlm.nih.gov/pubchem/protein/ACCP69045
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID226395163
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID129163637
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID127958259
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID226395472
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID226812759
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID128586172
http://rdf.ncbi.nlm.nih.gov/pubchem/gene/GID24241
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID226813121
http://rdf.ncbi.nlm.nih.gov/pubchem/gene/GID463609
http://rdf.ncbi.nlm.nih.gov/pubchem/compound/CID21872039
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID227552772
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID129318501
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID452356878
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID226405538
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID128423620
http://rdf.ncbi.nlm.nih.gov/pubchem/compound/CID11582
http://rdf.ncbi.nlm.nih.gov/pubchem/compound/CID3337
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID226393239
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID226396655
http://rdf.ncbi.nlm.nih.gov/pubchem/compound/CID59979859
http://rdf.ncbi.nlm.nih.gov/pubchem/compound/CID12296
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID226396654
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID226588475
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID129298073
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID226588474
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID129327354
http://rdf.ncbi.nlm.nih.gov/pubchem/protein/ACCP01262
http://rdf.ncbi.nlm.nih.gov/pubchem/compound/CID542372
http://rdf.ncbi.nlm.nih.gov/pubchem/compound/CID21963684
http://rdf.ncbi.nlm.nih.gov/pubchem/gene/GID13856
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID127394794
http://rdf.ncbi.nlm.nih.gov/pubchem/protein/ACCB5UBG1
http://rdf.ncbi.nlm.nih.gov/pubchem/protein/ACCP01261
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID129149658
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID226399670
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID127394659
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID454383257
http://rdf.ncbi.nlm.nih.gov/pubchem/compound/CID7859
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID226395216
http://rdf.ncbi.nlm.nih.gov/pubchem/compound/CID11594
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID127833068
http://rdf.ncbi.nlm.nih.gov/pubchem/compound/CID3661
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID325881072
http://rdf.ncbi.nlm.nih.gov/pubchem/compound/CID4723
http://rdf.ncbi.nlm.nih.gov/pubchem/compound/CID443939
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID226428425
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID226610000
http://rdf.ncbi.nlm.nih.gov/pubchem/compound/CID138
http://rdf.ncbi.nlm.nih.gov/pubchem/compound/CID3345
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID467842649
http://rdf.ncbi.nlm.nih.gov/pubchem/compound/CID5284371
http://rdf.ncbi.nlm.nih.gov/pubchem/compound/CID19493
http://rdf.ncbi.nlm.nih.gov/pubchem/compound/CID7745

Total number of triples: 1008.