http://rdf.ncbi.nlm.nih.gov/pubchem/patent/US-11084794-B2
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_fb5d44e15e402abbf25c43eb3f714e9c |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D241-08 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D241-08 |
| filingDate | 2019-10-30-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| grantDate | 2021-08-10-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_db22bdecd518c626aee64e7c54fc9cb7 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_b88d9f1b5cb6254389135554840f4f3a http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_45de8cf0b492560b9d43e1a3903a6bc3 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_f488ff8d2df008140c72ee2e9f65cd3a http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_9589e2e6d6df16aa1dc6c5a46697d833 |
| publicationDate | 2021-08-10-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | US-11084794-B2 |
| titleOfInvention | Controlled cyclization of peptoids to form chiral diketopiperazines |
| abstract | The present disclosure provides improved methods for controlled cyclization of peptoid dimers to form N,N′-2,5-diketopiperazines (N,N′-2,5-DKPs) with significant selectivity. In at least some examples, selectivity is based on a serendipitous conglomeration of slow exchange of amide rotamers, steric repulsion from the degree of α-substitution, and the geometric bulk of an amine nucleophile. By varying reaction conditions, the selectivity of the reaction and formation of a particular N,N′-2,5-DKP can be switched. The cyclization works in the presence of a variety of protection groups and diverse functionalities. The teachings herein provide techniques for synthesizing N,N′-2,5-DKPs that can be readily docked with drug candidates for shuttling across the blood brain barrier. This method provides a facile way to produce substituted DKPs containing groups ready for post-modification to include docking drug candidates. |
| priorityDate | 2018-10-30-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 392.