http://rdf.ncbi.nlm.nih.gov/pubchem/patent/EP-1648896-B1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_a8f70c5b59b293a0220e30a752bb017f |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D487-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-22 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-20 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P21-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-00 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P25-22 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D487-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-519 |
| filingDate | 2004-07-22^^<http://www.w3.org/2001/XMLSchema#date> |
| grantDate | 2008-02-13^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_42416ebc7391ebb0d306fdbd836616f9 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_98b55cd43db2bd969adbbf14fc8c5094 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_9d08f1812f4d495661d732722d284830 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_2a0d52e4e1b8179cde641237f8971643 |
| publicationDate | 2008-02-13^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | EP-1648896-B1 |
| titleOfInvention | 7-substituted 3-nitro-pyrazolo [1,5-a] pyrimidines |
| abstract | 7-Substituted 3-nitropyrazolo[1,5-a]pyrimidine derivatives (I) are new. 7-Substituted 3-nitropyrazolo[1,5-a]pyrimidine derivatives of formula (I) and their salts are new. [Image] R1phenyl, pyridyl, pyrimidinyl, triazinyl, pyridyl-N-oxide, thienyl, furyl, thiazolyl or oxazolyl (all optionally substituted by R2); R21-6C alkyl, 3-6C cycloalkyl, 2-6C alkenyl, 2-6C alkynyl, 1-6C alkoxy, CF3, CN, SO2R3, NO2, NHR3, NR3R4, C(O)R5, C(O)NHR5, C(O)OR5, NR5C(X)R6, NR5SO2R6 or a substituted heterocycle of formula (a) or (b); R3, R41-6C alkyl, 3-6C cycloalkyl, aryl or heteroaryl; R5H, 1-6C alkyl, 2-6C alkenyl, 2-6C alkynyl or 3-6C cycloalkyl; R61-6C alkyl, 3-6C cycloalkyl, 1-6C alkoxy, 1-6C alkylamino, di(1-6C alkyl)amino, 1-6C alkoxy(1-6C alkyl), 1-6C alkylamino(1-6C alkyl), di(1-6C alkyl)amino(1-6C alkyl), optionally monosubstituted phenyl, furyl, thienyl, thiazolyl or pyridyl; R7H, 1-6C alkyl, 3-6C cycloalkyl, aryl or optionally substituted heteroaryl; R8H, 1-6C alkyl, CF3, CN, CO-R9 or SO2R9; R9H, 1-6C alkyl, optionally substituted phenyl or optionally substituted heteroaryl; X : O, S or NR8; and n : 1-3. [Image] An independent claim is also included for the preparation of (I). - ACTIVITY : Tranquilizer; Anticonvulsant; Hypnotic; Sedative; Anesthetic; Muscular-Gen. - MECHANISM OF ACTION : alpha 1 Gamma-aminobutyric acid (GABA-A) receptor modulator; alpha 2 Gamma-aminobutyric acid receptor modulator. (I) were tested for alpha 1 GABA-A receptor modulatory activity using biological assays. The results showed that the inhibition constant of N-ethyl-N-[3-(3-nitropyrazolo[1,5-a]pyrimidin-7-yl)phenyl]methanesulf onamide was 11.1 nM. - |
| priorityDate | 2003-07-24^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
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