http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-052307-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/C07D253-075 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P17-06 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 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P29-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P37-02 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D253-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D253-075 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-53 |
| filingDate | 2005-06-27-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 2007-03-14-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-052307-A1 |
| titleOfInvention | PROCEDURES FOR THE PREPARATION OF P2X7 INHIBITORS, PHARMACEUTICAL COMPOSITION AND A PREPARATION METHOD |
| abstract | The compounds are useful as agents in the treatment of diseases, including inflammatory diseases such as arthritis (of various types), Crohn's disease, emphysema, osteoporosis and others. Claim 1: A process for preparing a compound of formula (1) or a pharmaceutically acceptable salt thereof, wherein R 1 is C 1-6 alkyl, optionally substituted with C 3-8 cycloalkyl, phenyl, naphthyl, heterocycloalkyl of 5 or 6 members, or a 5- or 6-membered heteroaryl, wherein each of said C 1-6 alkyl, C 3-8 cycloalkyl, phenyl, naphthyl, 5- or 6-membered heterocycloalkyl, or 5- or 6-membered heteroaryl are optionally substituted with one to three moieties independently selected from the group consisting of hydroxy, halo, CN, C1-6 alkyl, HO-C1-6 alkyl, C1-6 alkyl-NH- (C = O) -, NH2 (C = O) -, C1-6 alkoxy, or C3-8 cycloalkyl; R2 is H, halo, -CN or C1-6 alkyl, wherein said C1-6 alkyl is optionally substituted with one to three moieties independently selected from the group consisting of halo, hydroxy, amino, -CN, C1- alkyl 6, C1-6 alkoxy, -CF3, CF3O-, C1-6-NH- alkyl, [C1-6 alkyl] 2-N-, C1-6-S- alkyl, C1-6- alkyl (S = O) -, C1-6- (SO2) alkyl -, C1-6-O- (C = O) -, formyl, C1-6- (C = O) alkyl - and C3-6 cycloalkyl; wherein R4 is independently selected from the group consisting of H, halo, hydroxy, -CN, HO-C1-6 alkyl, C1-6 alkyl, optionally substituted with 1 to 3 fluoro, C1-6 alkoxy optionally substituted with one to three fluoro, HO2C-C1-6-O-alkyl (C = O) -, R5R6N (O2S) -, C1-6- (O2S) -NH- alkyl, C1-6-O2S alkyl [C1-6-N alkyl ] -, R5R6N (C = O) -, R5R6N (CH2) m-, phenyl, naphthyl, C3-8 cycloalkyl, 5 or 6 membered heteroaryl, 5 or 6 membered heterocycloalkyl, phenyl-O-, naphthyl-O- , C3-8-O- cycloalkyl, 5- or 6-membered heteroaryloxy and 5- or 6-membered heterocycloalkyl-O-; and R7 is -CH2-C (R10R11) -OH, wherein R10 and R11 are independently selected from the group consisting of: H, phenyl and C1-6 alkyl optionally substituted with one to three halo, hydroxy, -CN, C1 alkoxy -6, (C1-6 alkyl) nN-, C1-6 alkyl- (C = O) -, C3-8 cycloalkyl- (C = O) -, 5- or 6-membered heterocycloalkyl- (C = O), phenyl - (C = O) -, naphthyl- (C = O), heteroaryl- (C = O) - 5 or 6 members, C1-6 alkyl- (C = O) O-, C1-6-O alkyl ( C = O) -, C3-8 cycloalkyl, phenyl, naphthyl, 5 or 6 membered heterocycloalkyl and 5 or 6 membered heteroaryl; R5 and R6 are each independently selected from the group consisting of H, C1-6 alkyl, HO-C2-6 alkyl, and C3-8 cycloalkyl, or R5 and R6 can optionally be taken together with the N atom to which they are joined to form a 5- or 6-membered heterocycloalkyl; n is 1 or 2; m is 1 or 2; wherein said process comprises reacting a compound of formula (2) with a compound of formula (7) in the presence of at least one Lewis acid. |
| 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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Total number of triples: 26.