http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-042532-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_966a6c1f382ec9bcb5e3839dfd73e5b8 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D471-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P43-00 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D471-04 |
| filingDate | 2003-12-18-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 2005-06-22-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-042532-A1 |
| titleOfInvention | COMPOUNDS OF 5,8-DIHIDRO-6H-PIRIDO [2,3-D] PIRIMIDIN-7-ONA |
| abstract | The present discloses compounds that are selective inhibitors of both KDR and FGFR kinase. These compounds, as well as their pharmaceutically acceptable salts, are antiproliferative agents useful in the treatment or control of solid tumors, especially breast, colon, lung and prostate tumors. Pharmaceutical compositions containing these compounds and their preparation are also described. Claim 1: The compounds of the formula (1) or pharmaceutically acceptable salts thereof, in which Ar and Ar 'are independently selected from the group consisting of aryl, substituted aryl, heteroaryl and substituted heteroaryl, with the condition that that, in the case of Ar, the heteroaryl is not 2-pyridyl and the substituted heteroaryl is not 2-pyridyl; R1 is selected from the group consisting of H, C1-10 alkyl, C1-10 alkyl independently substituted with up to three groups selected from aryl, heteroaryl, heterocycle, cycloalkyl, NR8R9, OR10, SR10, halogen, COR11, CO2R11, CONR11R12, SO2NR11R12, SOR11, SO2R11, CN and NO2, where each of the aryl, heteroaryl, heterocycle and cycloalkyl groups can be independently substituted with up to three groups selected from NR8R9, OR10, SR10, halogen, COR11, CO2R11, CONR11R12, SO2NR11R12, SOR11 , SO2R11, CN and NO2, aryl; aryl independently substituted with up to three groups selected from lower alkyl, NR8R9, OR10, SR10, halogen, COR11, CO2R11, CONR11R12, SO2NR11R12, SOR11, SO2R11, CN and NO2, heteroaryl; heteroaryl independently substituted with up to three groups selected from lower alkyl, NR8R9, OR10, SR10, halogen, COR11, CO2R11, CONR11R12, SO2NR11R12, SOR11, SO2R11, CN and NO2, heterocycle; heterocycle independently substituted with up to three groups selected from lower alkyl, NR8R9, OR10, SR10, halogen, COR11, CO2R11, CONR11R12, SO2NR11R12, SOR11, SO2R11, CN and NO2, C3-10 cycloalkyl; C3-10 cycloalkyl independently substituted with up to three groups selected from lower alkyl, substituted lower alkyl, NR8R9, OR10, SR10, halogen, COR11, CO2R11, CONR11R12, SO2NR11R12, SOR11, SO2R11, CN and NO2, C2-10 alkenyl; C2-10 alkenyl independently substituted with up to three groups selected cycloalkyl, substituted cycloalkyl, heterocyclyl, substituted heterocycloalkyl, NR8R9, OR10, SR10, halogen, COR11, CO2R11, CONR11R12, SO2NR11R12, SOR11, SO2R11, CN and NO2, C2-10 alkynyl C2-10 alkynyl independently substituted with up to three groups selected from NR8R9, OR10, SR10, halogen, COR11, CO2R11, CONR11R12, SO2NR11R12, SOR11, SO2R11, CN and NO2; R8, R9 and R10 are independently H or lower alkyl; R11 and R12 are independently selected from the group consisting of H, unsubstituted lower alkyl, hydroxy substituted lower alkyl, alkoxy or NR21R22; unsubstituted cycloalkyl, hydroxy, alkoxy, lower alkyl or NR21R22 substituted cycloalkyl; unsubstituted heterocycle, hydroxy substituted heterocycle, alkoxy, lower alkyl or NR21R22; or, on the other hand, NR11R12 forms a ring with 3 to 7 atoms, a ring that does not have or at least has an additional heteroatom, with the proviso that if the heteroatom is N, the heteroatom may be substituted with one or more substituents selected from the group consisting of lower alkyl, OR13, COR14, CO2R14, CONR14R15, SO2R14, and SO2NR14R15; R13 is selected from the group consisting of H, COR14, CONR14R15, unsubstituted lower alkyl, hydroxy substituted lower alkyl, alkoxy or NR21R22; unsubstituted cycloalkyl, hydroxy, alkoxy, lower alkyl or NR21R22 substituted cycloalkyl; unsubstituted heterocycle and heterocycle substituted with hydroxy, alkoxy, lower alkyl or NR21R22; R14 and R15 are independently selected from the group consisting of H; lower alkyl unsubstituted, lower alkyl substituted with hydroxy, alkoxy or NR21R22; unsubstituted cycloalkyl, hydroxy, alkoxy, lower alkyl or NR21R22 substituted cycloalkyl; unsubstituted heterocycle; heterocycle substituted with hydroxy, alkoxy, lower alkyl or NR21R22; or, on the other hand, NR14R15 forms a ring with 3 to 7 atoms, a ring that does not have or at least has an additional heteroatom, with the proviso that if the heteroatom is N, the heteroatom may be substituted with one or more substituents selected from the group consisting of lower alkyl, OR23, COR23, CO2R23, CONR23R24, SO2R23 and SO2NR23R24; R21 is selected from the group consisting of H, lower alkyl, COR23 or CO2R23; R22, R23 and R24 are independently selected from the group consisting of H or lower alkyl; or, on the other hand, NR21R22 or NR23R24 forms a ring with 3 to 7 atoms, a ring that does not have or at least has an additional heteroatom selected from the group consisting of N, O or S, with the proviso that, if the heteroatom is N, the heteroatom can be in the form of -NH or NR25 and if the heteroatom is S, it can be in the form of S (O) m where m = 0.1 or 2 and R25 is lower alkyl. |
| priorityDate | 2002-12-20-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
| Predicate | Subject |
|---|---|
| isDiscussedBy | http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID457493163 http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID458397310 |
Total number of triples: 15.