http://rdf.ncbi.nlm.nih.gov/pubchem/patent/ES-2338545-T3
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_c76ecadad74a1a35270b3e3a34d60f37 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D513-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D403-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D403-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D417-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D413-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D409-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D405-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-00 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D513-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-505 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D409-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D403-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D403-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D405-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D413-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D417-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D401-14 |
| filingDate | 2003-12-08-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| grantDate | 2010-05-10-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_2a0ad96b57435808128aa3ec4899150e http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_4d9b880408c85d46597d8409a7880027 |
| publicationDate | 2010-05-10-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | ES-2338545-T3 |
| titleOfInvention | PIRIMIDINE DERIVATIVES FOR THE TREATMENT OF ABNORMAL CELLULAR GROWTH. |
| abstract | A compound of the formula 1 ** (See formula) ** or a pharmaceutically acceptable salt, solvate, hydrate or prodrug thereof, wherein n is an integer from 1 to 3; each R1 is a substituent independently selected from the group consisting of hydrogen, hydroxy, -C1-C6 alkyl, cycloalkyl (C3-C7), -heterocyclyl (C2-C9), -O-alkyl (C1-C6), - O-cycloalkyl (C3-C7), -O-heterocyclyl (C2-C9), -NR5R6, -SR7, -SOR7, -SO2R7, -CO2R5, -CONR5R6, -SO2NR5R6, -NHCOR5, -NR5CONR5R6, and -NN5; with the proviso that a heteroatom of said substituents R1 cannot be attached to a sp3 carbon atom attached to another heteroatom; and said R1 substituents, -C1-C6-alkyl, -C3-C7-alkyl, -C-C2-C-alkyl, -O-C1-C6-alkyl, -O-C3-C7-alkyl groups, -O-heterocyclyl (C2-C9), -NR5R6, -SR7, -SOR7, -SO2R7, -CO2R5, -CONR5R6, -SO2NR5R6, -NHCOR5, -NR5CONR5R6, and -NR5SO2R7 are optionally substituted with one to three moieties independently selected with one to three moieties from the group consisting of hydrogen, halogen, hydroxy, -CF3, -CN, -C1-C6 alkyl, -NR5R6, -OR5, -cycloalkyl (C3-C7), -heterocyclyl (C2-C9), -CO2R5, - CONR5R6 and -CONR5R8; with the proviso that a heteroatom of said optional moieties R1 cannot be attached to a sp3 carbon atom attached to another heteroatom; each R2 is a substituent independently selected from the group consisting of hydrogen, -alkyl (C1-C6), -alkenyl (C2-C6), -alkynyl (C2-C6), -cycloalkyl (C3-C7), -heterocyclyl (C2- C9), -CO2R5, and -CONR5R6; with the proviso that a heteroatom of any of said R2 substituents cannot be attached to a sp3 carbon atom that is linked to another heteroatom; and said substituents R2, -C1-C6-alkyl, -C2-C6-alkenyl, -C2-C6-alkynyl, -C3-C7-cycloalkyl, -C2-C9-heterocyclyl, -CO2R5, and - CONR5R6, are optionally substituted with one to three moieties independently selected from the group consisting of hydrogen, halogen, hydroxy, -CF3, -NO2, -CN, -alkyl (C1-C6), -alkenyl (C2-C6), -alkynyl ( C2-C6), -C = N-OH, -C = NO ((C1-C6) alkyl), -NR5R6, -OR5, -cycloalkyl (C3-C7), -heterocyclyl (C2-C9), -CO2R5, -CONR5R6, -CONR5R8, -SR7, -SOR7, -SO2R7, -SO2NR5R6, -NHCOR5, -NR5CONR5R6, and -NR5SO2R7, where said radicals R2-alkenyl (C2-C6) and -alkynyl (C2-C6), can be optionally substituted with one to three R5 groups; and with the proviso that a heteroatom of the aforementioned optional radicals R2 cannot be attached to a sp3 carbon atom attached to another heteroatom; R1 and R2 may be taken together with the atom (s) to which they are attached to form a (C3-C10) or -heterocyclyl (C2-C9) alkyl; R3 is a substituent selected from the group consisting of: (a) hydrogen; (b) -C6-C10 -aryl or -C1-C9 heteroaryl, optionally substituted with one to three moieties independently selected from the group consisting of halogen, hydroxy, -C1-C6 alkyl, -C1-C6 alkyl ) -P (O) (O-(C1-C6) alkyl) 2, -C3-C10 cycloalkyl, -C6-C10 -aryl, -C2-C9-heterocyclyl, (C1-C9) heteroaryl, -NR5R6, -NHSO2-alkyl (C1-C6), -NHSO2-cycloalkyl (C3-C6), -N (alkyl (C1-C6)) (SO2-alkyl (C1-C6)), -N (alkyl (C1 -C6)) (SO2-C3-C6 cycloalkyl), -O-C1-C6 alkyl, -O-SO2-C1-C6 alkyl, - (CO) C1-C6 alkyl, - ( CO) CF3, - (CO) cycloalkyl (C3-C10), - (CO) aryl (C6-C10), - (CO) heterocyclyl (C2-C9), - (CO) heteroaryl (C1-C9), - ( CO) O (C1-C6) alkyl, - (CO) O-cycloalkyl (C3-C10), - (CO) O-aryl (C6-C10), - (CO) O-heterocyclyl (C2-C9), - (CO) O-heteroaryl (C1-C9), - (CO) -alkyl (C1-C6) -O-alkyl (C1-C6), -SO2-alkyl (C1-C6), -SO2-cycloalkyl (C3 -C6), SO2CF3, SO2NH2, -SO2NH-alkyl (C1-C6), -SO2NH-cycloalkyl (C3-C6), -SO2N (alkyl (C1-C6)) 2, -SO2N (cycloalkyl (C3-C6)) 2, SO2NR5R6, and -SO2N-(C1-C6) alkyl-C6-C10 alkyl; where said -aryl (C6-C10) or -heteroaryl (C1-C9), are optionally interrupted with one to three elements selected from the group consisting of - (C = O), -SO2, -S-, -O-, - N-, -NH- and -NR5; and R5 and R6 of said NR5R6 group can be taken together with the atoms to which they are attached to form a (C2-C9) heterocyclyl; (c) -C3-C10-cycloalkyl, -heterocyclyl (C2-C9), and -alkyl (C1-C6) -heterocyclyl (C2-C9) optionally substituted with one to three moieties independently selected from the group consisting of halogen, hydroxy, -C1-C6-alkyl, -C1-C6-alkyl-P (O) (O-C1-C6-alkyl) 2, -C3-C10-alkyl, aryl (C6-C10), heterocyclyl (C2-C9), -heteroaryl (C1-C9), -NR5R6, -NHSO2-alkyl (C1-C6), -NHSO2-cycloalkyl (C3-C6), -N (alkyl (C1-C6)) (SO2- (C1-C6) alkyl, -N ((C1-C6) alkyl) (SO2-C3-C6 cycloalkyl), -O-(C1-C6) alkyl, -O-SO2-(C1-C6) alkyl, - (CO) (C1-C6) alkyl, - (CO) CF3, - (CO) cycloalkyl (C3-C10), - (CO) aryl (C6-C10), - (CO) -heterocyclyl (C2-C9) , - (CO) C1-C9 heteroaryl, - (CO) O-C1-C6 alkyl, - (CO) O-cycloalkyl (C3-C10), - (CO) O-aryl (C6-C10) , - (CO) O-heterocyclyl (C2-C9), - (CO) O-heteroaryl (C1-C9), - (CO) (C1-C6) alkyl -O-(C1-C6) alkyl, -SO2- (C1-C6) alkyl, -SO2-cycloalkyl (C3-C6), SO2CF3, SO2NH2, -SO2NH-alkyl (C1-C6), -SO2NH-cycloalkyl (C3-C6), -SO2N ((C1-) alkyl C6)) 2, -SO2N (cycloalkyl (C3-C6)) 2, SO2NR5R6, and -SO2N-alkyl (C1-C6) -aryl (C6-C10); wherein said -cyclo (C3-C10) alkyl, -heterocyclyl (C2-C9) and -alkyl (C1-C6) -heterocyclyl (C2-C9), are optionally interrupted with one to three elements selected from the group consisting of - (C = O), -SO2, -S-, -O-, -N-, -NH- and -NR5; and R5 and R6 of said NR5R6 group can be taken together with the atoms to which they are attached to form a (C2-C9) heterocyclyl; (d) -C1-C6 alkyl optionally substituted with one to three moieties selected from the group consisting of halogen, hydroxy, -C1-C6 alkyl, -C1-C6 alkyl-P (O) (O-alkyl) (C1-C6)) 2, -C3-C10 cycloalkyl, aryl (C6-C10), heterocyclyl (C2-C9), -heteroaryl (C1-C9), -NR5R6, -NHSO2-alkyl (C1-C6) , -NHSO2-C3-C6 cycloalkyl, -N (C1-C6 alkyl) (SO2-C1-C6 alkyl), -N (C1-C6 alkyl) (SO2-C3-C6 alkyl) )), -O-(C1-C6) alkyl, -O-SO2-(C1-C6) alkyl, - (CO) (C1-C6) alkyl, - (CO) CF3, - (CO) cycloalkyl (C3-) C10), - (CO) aryl (C6-C10), - (CO) heterocyclyl (C2-C9), - (CO) heteroaryl (C1-C9), - (CO) O-alkyl (C1-C6), - (CO) O-C3-C10 cycloalkyl, - (CO) O-aryl (C6-C10), - (CO) O-heterocyclyl (C2-C9), - (CO) O-heteroaryl (C1-C9) , - (CO) (C1-C6) alkyl -O-(C1-C6) alkyl, -SO2-(C1-C6) alkyl, -SO2-cycloalkyl (C3-C6), SO2CF3, SO2NH2, -SO2NH-alkyl ( C1-C6), -SO2NH-cycloalkyl (C3-C6), -SO2N (alkyl (C1-C6)) 2, -SO2N (cycloalkyl (C3-C6)) 2, SO2NR5R6, and -SO2N-alkyl (C1-C6) ) -aryl (C6-C10); where said -alkyl (C1-C6), is optionally interrupted with one to three elements selected from the group consisting of - (C = O), -SO2, -S-, -O-, -N-, -NH- and - NR5; and R5 and R6 of said NR5R6 group can be taken together with the atoms to which they are attached to form a (C2-C9) heterocyclyl; and wherein each substituent, residue or element R3 (b) - (d) is optionally substituted with one to three radicals independently selected from the group consisting of hydrogen, halogen, hydroxy, -CF3, -NO2, -CN, -C1 -alkyl C6), -alkyl (C2-C6), -alkynyl (C2-C6), -cycloalkyl (C3-C7), -heterocyclyl (C2-C9), -aryl (C6-C10), -heteroaryl (C1-C9) , -O-C1-C6 alkyl, -O-cycloalkyl (C3-C7), O-heterocyclyl (C2-C9), -C = N-OH, -C = NO ((C1-C6) alkyl), -NR5R6, -SR7, -SOR7, -SO2R7, -CO2R5, -CONR5R6, -SO2NR5R6, -NHCOR5, -NR5CONR5R6, and -NR5SO2R7; with the proviso that a heteroatom of said substituents, moieties, elements or radicals R3 (b) - (d), cannot be attached to a sp3 carbon atom attached to another heteroatom; and where R5 and R6 of said groups -NR5R6, -CONR5R6, -SO2NR5R6, and -NR5CONR5R6, can be taken together with the atoms to which they are attached to form a -heterocyclyl (C2-C9); R4 is a substituent selected from the group consisting of hydrogen, -C1-C6 alkyl, cycloalkyl (C3-C7) and -heterocyclyl (C2-C9); wherein said substituents R4-(C1-C6) alkyl, -cycloalkyl (C3-C7) and -heterocyclyl (C2-C9), are optionally substituted with one to three moieties independently selected from the group consisting of hydrogen, halogen, -alkyl (C1 -C6), -CN, NR52, -OR5, -cycloalkyl (C3-C7), -heterocyclyl (C2-C9), -CO2R5, and -CONR5R8; with the proviso that a heteroatom of said R4 substituents cannot be attached to a sp3 carbon atom attached to another heteroatom; and where R5 and R8 of said group-CONR5R8 can be taken together with the atoms to which they are attached to form a -cycloalkyl (C3-C10) or a -heterocyclyl (C2-C9); R5 and R6 are each substituents independently selected from the group consisting of hydrogen, -alkyl (C1-C6), -cycloalkyl (C3-C7), -heterocyclyl (C2-C9), -aryl (C6-C10), and -heteroaryl (C1-C9); wherein said substituents R5 or R6-(C1-C6) alkyl, -cyclo (C3-C7) alkyl, -heterocyclyl (C2-C9), -aryl (C6-C10), and -heteroaryl (C1-C9), are optionally substituted with one to three moieties independently selected from the group consisting of hydrogen, halogen, -CF3, -CN, -C1-C6 alkyl, -NH-C1-C6 alkyl, -NH-C3-C7 cycloalkyl, - NH-heterocyclyl (C2-C9), -NH-aryl (C6-C10), -NH-heteroaryl (C1-C9), -N ((C1-C6) alkyl) 2, -N (cycloalkyl (C3-C7) ) 2, -N (heterocyclyl (C2-C9)) 2, -N (aryl (C6-C10)) 2, -N (heteroaryl (C1-C9)) 2, -O-alkyl (C1-C6), - O-cycloalkyl (C3-C7), O-heterocyclyl (C2-C9), -O-aryl (C6-C10), -O-heteroaryl (C1-C9), -cycloalkyl (C3-C7), -heterocyclyl (C2 -C9), -CO2R7, -CONH2, -CONHR7 and -CONR7R8; with the proviso that a heteroatom of said substituents or moieties R5 or R6 cannot be attached to a sp3 carbon atom attached to other heteroatoms; and where R7 and R8 of said group -CONR7R8 can be taken together with the atoms to which they are attached to form a (C1-C9) heteroaryl; R5 and R6 can be taken together with the atom (s) to which they are attached to form a (C3-C10) cycloalkyl or (C2-C9) heterocyclyl; R7 is an s |
| priorityDate | 2002-12-20-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
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