http://rdf.ncbi.nlm.nih.gov/pubchem/patent/US-5624936-A

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classificationCPCAdditional http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K38-00
classificationCPCInventive http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07K5-06139
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classificationIPCInventive http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07K5-078
filingDate 1996-02-13-04:00^^<http://www.w3.org/2001/XMLSchema#date>
grantDate 1997-04-29-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_767c94ee590fcadc766aa9acdebdbcea
publicationDate 1997-04-29-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber US-5624936-A
titleOfInvention Inhibitors of farnesyl-protein transferase
abstract The present invention comprises analogs of the CA1A2X motif of the protein Ras that is modified by farnesylation in vivo. These CA1A2X analogs inhibit the farnesyl-protein transferase and the farnesylation of certain proteins. Furthermore, these CA1A2X analogs differ from those previously described as inhibitors of farnesyl-protein transferase in that they do not have a thiol moiety. The lack of the thiol offers unique advantages in terms of improved pharmacokinetic behavior in animals, prevention of thiol-dependent chemical reactions, such as rapid autoxidation and disulfide formation with endogenous thiols, and reduced systemic toxicity. The compounds of the instant invention also incorporate a cyclic amine moiety in the A2 position of the motif. Further contained in this invention are chemotherapeutic compositions containing these farnesyl transferase inhibitors and methods for their production.
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Total number of triples: 415.