http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-038259-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_c902faf6ae746c51fc8010672fc22894 |
| classificationCPCAdditional | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/G01N2333-5751 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/G01N2500-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/Y10S206-828 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D241-26 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D241-20 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D241-18 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D409-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/G01N33-74 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D405-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D491-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D403-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-12 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D409-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D403-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D405-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D241-18 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D241-26 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D241-20 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D401-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D401-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D491-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D401-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/G01N33-74 |
| filingDate | 2002-11-19-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 2005-01-12-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-038259-A1 |
| titleOfInvention | SUBSTITUTED DERIVATIVES OF ARIL-1,4-PIRAZINA, PHARMACEUTICAL COMPOSITIONS THAT CONTAIN THEM, ITS USE FOR THE PREPARATION OF MEDICINES, MANUFACTURING ARTICLE THAT UNDERSTANDS THEM, METHOD FOR INHIBITING THE CRF UNION TO THE RECEIVER OF CRF1, METHOD FOR CLASSIFYING CLASSIFYING OF CRF AND METHOD P |
| abstract | A compound comprising a substituted aryl-1,4-pyrazine derivative of formula (1) or a stereoisomer of said formula, a pharmaceutically acceptable salt of said formula, or a prodrug of said formula, wherein in formula (1) : X is selected from NR3R4, -OR3, -CR3R5R5, -C (O) R3, -S (O) mR3, -NR3C (O) R4, -NR3S (O) mR4, m is 0, 1 or 2; Ar is selected from aryl, substituted aryl, heteroaryl, substituted heteroaryl; R1, R2 and R5 are independently selected from halogen, -NO2, -CN, -Ra, -ORa, -S (O) mRa, -NRaRa, -C (O) NRaRa, -C (S) NRaRa-S (O ) mNRaRa, -NRaS (O) mRa, -NRaC (O) ORa, -OC (O) NRaRa, -NRaC (O) NRaRa, -NRaC (S) NRaRa, -C (O) ORa, -C (S) ORa, and -OC (O) ORa; R3 and R4 are independently selected from Ra, heterocycloalkyl, substituted heterocycloalkyl, substituted heteroaryl, substituted aryl, aryl-cycloalkyl, substituted aryl-cycloalkyl, heteroaryl-cycloalkyl, substituted heteroaryl-cycloalkyl, aryl-heterocycloalkyl, aryl-heterocycloalkyl substituted , or substituted heteroaryl-heterocycloalkyl provided that at least one of R3 or R4 is heteroaryl, substituted heteroaryl, aryl-cycloalkyl, substituted aryl-cycloalkyl, heteroaryl-cycloalkyl, substituted heteroaryl-cycloalkyl, aryl-heterocycloalkyl, substituted aryl-heterocycloalkyl, -heterocycloalkyl, substituted heteroaryl-heterocycloalkyl, heterocycloalkyl or substituted heterocycloalkyl; each Ra is selected from H, alkyl, cycloalkyl, haloalkyl, aryl, heteroaryl, or heterocycloalkyl optionally substituted with 1 to 5 of Rt, -ORt, -S (O) mRt, NRtRt, oxo (= O), thione (= S ), phenyl, heteroaryl, or heterocycloalkyl wherein phenyl, heteroaryl, and heterocycloalkyl are optionally substituted with 1 to 5 groups independently selected from Rt; and each Rt is selected from H, halogen, -NO2, -NH2, -OH, -SH, -CN, -C (O) NH2, -C (O) -NH alkyl, -C (O) N alkylalkyl, - Or alkyl, NH alkyl, Nalkylalkyl, -S (O) malkyl, SO2NH2, SO2NHalkyl and SO2N alkylalkyl, alkyl, cycloalkyl, haloalkyl, phenyl, benzyl, heteroaryl, or heterocycloalkyl wherein phenyl, benzyl heteroaryl and heterocycloalkyl may optionally be substituted with alkyl or halogen, provided that the compound is not: 2,5-dimethyl-3- (2,4-dichlorophenyl) -6 - [(1-methylpiperidin-4-yl) oxy] pyrazine; 2,5-dimethyl-3- (2,4-dichlorophenyl) -6- (tetrahydrofuran-3-yl) oxy] pyrazine; 2,5-dimethyl-3- (2,4-dichlorophenyl) -6- (tetrahydro-2H-pyran-4-yloxy) pyrazine, 2,5-dimethyl-3- (2,4-dichlorophenyl) -6- [ (1-methylpiperidin-3-yl) oxy] pyrazine, 2,5-dimethyl-3- (2,4-dichlorophenyl) -6- [1-ethylpiperdin-3-yl) oxy] pyrazine, 2,5-dimethyl- 3- (2,4-Dichlorophenyl) -6- (1-piperidin-4-yl) oxy] pyrazine, 2,5-dimethyl-3- (2,4-dichlorophenyl) -6-piperidin-3-yl) oxy ] pyrazine, 2,5-dimethyl-3- (2,4-dichlorophenyl) -6 - [(1-ethylpyrrolidin-3-yl) oxy] pyrazine, 2,5-dimethyl-3- (2,4-dichlorophenyl) -6 - [(1-methylpyrrolidin-3-yl) oxy] pyrazine, 2,5-dimethyl-3- (2,4-dichlorophenyl) -6 - [(pyrrolidin-3-yl) oxy] pyrazine, 2.5 -dimethyl-3- (2,4-dichlorophenyl) -6 - [(pyridin-4-yl) oxy] pyrazine. Pharmaceutical compositions containing them, their use for the manufacture of medicaments, manufacturing article comprising them, method for inhibiting the binding of CRF to the CRF1 receptor, method for classifying ligands of CRF receptors and method for detecting receptors are also disclosed. of tissue CRF. These compounds are useful for the preparation of useful medications for the treatment of anxiety disorders, depression and stress-related disorders. |
| priorityDate | 2001-11-21-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
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