http://rdf.ncbi.nlm.nih.gov/pubchem/patent/EA-201700586-A1
Outgoing Links
| Predicate | Object |
|---|---|
| classificationCPCAdditional | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/Y02P20-55 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-4245 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-4523 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P3-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-4427 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D413-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D271-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D413-04 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D413-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D413-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-4523 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P9-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P3-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-4427 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D271-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-4245 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P25-00 |
| filingDate | 2017-12-21-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 2019-06-28-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | EA-201700586-A1 |
| titleOfInvention | SUBSTITUTED 1,2,4-OXADIAZOLES AS MODULATORS OF RECEPTOR 1 ASSOCIATED WITH NEDED AMINES (TAAR1) |
| abstract | The invention relates to 3,5-disubstituted 1,2,4-oxadiazoles of general formula 1 and their pharmaceutically acceptable salts, which are modulators of receptor 1 associated with trace amines (TAAR1). The compounds can be used to treat diseases that are related to the TAAR1 receptor, such as mental disorders, cognitive and neurodegenerative disorders, schizophrenia, depression, bipolar disorder, attention deficit hyperactivity disorder (ADHD), obsessive-compulsive disorder, Parkinson's disease, Alzheimer's disease , epilepsy, migraine, high blood pressure (hypertension), alcohol or drug abuse, nicotine addiction, obesity, diabetes, metabolic disorder oh, a disorder associated with the consumption of energy and assimilation, a disorder associated with impaired homeostasis of body temperature, sleep disorders and circadian rhythms, as well as cardiovascular disorders. 3,5-Disubstituted 1,2,4-oxadiazoles correspond to the general formula 1 where a single or double bond represents a carbon-oxygen or carbon-nitrogen bond; n and m independently take the values 0, 1, 2, 3; X and Y are atoms of nitrogen and oxygen or oxygen and nitrogen, respectively; R represents a hydrogen atom, C 1 -C 6 alkyl, optionally substituted with C 1 -C 5 cycloalkyl; C-C-cycloalkyl; aryl, optionally substituted with halogen, C 1 -C 6 -alkyl, C 1 -C 5 -alkoxy, CF, ester or carboxamide group; 5 or 6 membered hetaryl containing one nitrogen, oxygen or sulfur atom in the ring; and a hydroxymethyl and 2-hydroxyethyl substituent substituted by the oxygen atom groups listed above; as well as primary, secondary or tertiary carboxamide group; R 'and R "represent, independently of one another, a hydrogen atom, CC-alkyl, CC-cycloalkyl, and also alkyl substituted by a CC-cycloalkyl group; optionally substituted aryl; R" "represents CC-alkyl, CC-cycloalkyl as well as alkyl substituted with a CC cycloalkyl group; optionally substituted aryl, wherein R 'and / or R "may form part of a nitrogen-containing heterocycle. The invention also relates to a method for producing compounds of general formula 1. The method consists of four stages: a) reacting a nitrile with hydroxylamine to form amidoxime; b) acylation amidoxime carboxylic acid; c) cyclodehydration of the product of the previous stage in 1,2,4-oxadiazole and d) removal of the tert-butoxycarbonyl protecting group from the nitrogen atom of the product of the previous stage. |
| priorityDate | 2017-12-12-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
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