http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-036375-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_cf32b60391b469c41e86c353437f5751 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P29-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P11-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P1-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P21-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P19-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P19-08 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/A61P37-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D239-42 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D403-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P33-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P33-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P33-00 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D239-42 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P11-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D403-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P9-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P19-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P19-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P19-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P19-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P21-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P33-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P33-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P29-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D401-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-505 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P1-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P37-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P33-12 |
| filingDate | 2002-08-28-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 2004-09-01-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-036375-A1 |
| titleOfInvention | PIRROLO [2,3-D] PIRIMIDINE -2- CARBONITRILE COMPOUNDS, A PROCESS FOR THEIR PREPARATION, A PHARMACEUTICAL COMPOSITION AND THE USE OF SUCH COMPOUNDS FOR THE PREPARATION OF MEDICINES |
| abstract | A pyrrolo [2,3-d] pyrimidine-2-carbonitrile compound of the formula (1), or a pharmaceutically acceptable salt or ester thereof, wherein: R is H, -R4, -OR4 or NR3R4; where R3 is H, lower alkyl or C3-10 cycloalkyl; R4 is lower alkyl or C3-10 cycloalkyl; and where R3 and R4 are independently substituted, optionally by halo, hydroxy, lower alkoxy, CN, NO2, or optionally substituted mono- or bi-lower alkyl amino; R1 is -CO-NR5R6, -NH-CO-R5, -CH2-NH-C (O) -R5, -CO-R5, -S (O) R5, -S (O) 2-R5, -CH2- CO-R5 or -CH2-NR5R6, where R5 is aryl, aryl-lower alkyl, C3-10 cycloalkyl, C3-10 cycloalkyl-lower alkyl, heterocycloalkyl or heterocycloalkyl-lower alkyl; R6 is H, aryl, aryl-lower alkyl, aryl-lower alkenyl, C3-10 cycloalkyl, C3-10 cycloalkyl-lower alkyl, heterocyclyl or heterocyclyl-lower alkyl; or where R5 and R6 together with the nitrogen atom to which they form form an N-heterocycle group, where N-heterocycle denotes a saturated, partially unsaturated or aromatic nitrogen containing a heterocyclic moiety linked through a nitrogen atom of it has 3 to 8 ring atoms that optionally contain 1, 2 or 3 additional heteroatoms selected from N, NR7, O, S, S (O) or S (O) 2 where R7 is H or optionally substituted (alkyl lower, carboxy, acyl (including both lower alkyl acyl, for example, formyl, acetyl or propionyl, or aryl acyl, for example, benzoyl), amido, aryl S (O) or S (O) 2), and where the N-heterocyclyl is optionally fused in a bicyclic structure, for example, with a benzene or pyridine ring, and where the N-heterocyclyl is optionally linked in a spiral structure with an integrated 3 to 8 membered heterocyclic or cycloalkyl ring in which the heterocyclic ring has 3 to 10 ring members and contains 1 to 3 heteroatoms selected from N, NR6, O, S; S (O), or S (O) 2, where R6 is as defined above), and where heterocyclyl denotes a ring that has 3 to 10 ring members and that contains 1 to 3 heteroatoms selected from N, NR7 , O, S, S (O) or S (O) 2 where R7 is as defined above), and where R5 and R6 are independently substituted, optionally by one or more groups, for example, 1-3 groups, selected from halo, hydroxy, oxo, lower alkoxy, CN or NO2, or optionally substituted (optionally amino substituted with mono- or bi-lower alkyl, lower alkoxy, aryl, lower alkyl with aryl, N-heterocyclyl, or N-heterocyclyl- lower alkyl (where the optional substitution comprises 1 to 3 substituents selected from halo, hydroxy, lower alkoxy, lower alkoxy-lower alkyl, lower alkoxy-carbonyl, CN, NO2, optionally mono- or bi-lower alkyl substituted amino, N -heterocyclyl or N-heterocyclyl-lower alkyl, or optionally amino substituted with mon o- or bi-lower alkyl; R2 is H independently, or optionally substituted (lower alkyl, aryl, aryl-lower alkyl, C3-10 cycloalkyl, C3-10 cycloalkyl-lower alkyl, heterocyclyl, or heterocyclyl-lower alkyl), and where R2 is optionally substituted by halo, hydroxy, oxo, lower alkoxy, CN, NO2, or optionally substituted mono- or bi-lower alkyl amino, a process for its preparation, a pharmaceutical composition and the use of said compounds for the preparation of medicaments, which are inhibitors of cathepsin K and find pharmaceutical use for the treatment of diseases and medical conditions in which cathepsin K is involved, for example, various conditions that include inflammation, rheumatoid arthritis, osteoarthritis, osteoporosis and tumors. |
| priorityDate | 2001-08-30-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
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