http://rdf.ncbi.nlm.nih.gov/pubchem/patent/EP-1768965-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_c76ecadad74a1a35270b3e3a34d60f37 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P19-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P19-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P17-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P29-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P37-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D253-075 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D253-07 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-53 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D253-065 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P29-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D253-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-53 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P19-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D253-075 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D253-06 |
| filingDate | 2005-06-17-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_fe931f98453594d1eb7d6df5dd94a5ee http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_47f414623b8b6ad71a20ba5beb50d9fd http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_3d7062d621bb569387b5af1f1e005def http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_900e00b2a0252d79d5c2653dcd711e28 |
| publicationDate | 2007-04-04-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | EP-1768965-A1 |
| titleOfInvention | Method for preparing 5-¬4-(2-hydroxy-ethyl)-3,5-dioxo-4,5-dihydro-3h-¬1,2,4|-triazin-2-yl|benzamide derivatives with p2x7 inhibiting activity by reaction of the derivative unsubstituted in 4-position of the triazine with an oxiran in the presence of a lewis acid |
| abstract | The present invention relates to methods of preparing compounds of formula (I), R7 is -CH2-C(R10R11)-OH, wherein R10 and R11 are independently selected from the group consisting of: hydrogen, phenyl, and (C1-C6)alkyl optionally substituted with one to three halos, hydroxy, -CN, (C1-C6)alkoxy-,((C1-C6)alkyl)n-N-,(C1-C6)alkyl-(C=O)-,(C3-C8)cycloalkyl-(C=O)-, 5 or 6-membered heterocycloalkyl-(C=O)-,phenyl-(C=O)-,naphthyl-(C=O)-,5- or 6-membered heteroaryl-(C=O)-,(C1-C6)alkyl-(C=O)O-,(C1-C6)alkyl-O(C=O)-,(C3-C8)cycloalkyl, phenyl, naphthyl, 5 or 6-membered heterocycloalkyl, and 5- or 6-membered heteroaryl; or a pharmaceutically acceptable salt thereof, wherein R1, R2 and R4 have any of the values as defined in the specification. Wherein said method comprises reacting a compound of formula (II) with a compound of formula (VIII) in the presence of at least one Lewis acid. The compounds are useful as agents in the treatment of diseases, including inflammatory diseases such as rheumatoid arthritis. Also provided are compositions of crystalline 2-Chloro-N-(1-hydroxy-cycloheptylmethyl)-5-[4-(2R-hydroxy-3-methoxy-propyl)-3,5-dioxo-4,5-dihydro-3H-[1,2,4]triazin-2-yl]-benzamide comprising less than 2.5% residual organic solvent, and methods for preparing said compositions. Further provided are methods for crystallizing 2-Chloro-N-(1-hydroxy-cycloheptylmethyl)-5-[4-(2R-hydroxy-3-methoxy-propyl)-3,5-dioxo-4,5-dihydro-3H-[1,2,4]triazin-2-yl]-benzamide. |
| priorityDate | 2004-06-29-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
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