http://rdf.ncbi.nlm.nih.gov/pubchem/patent/ES-2355797-T7
Outgoing Links
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| filingDate | 2004-11-18-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| grantDate | 2013-04-01-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_d33fd4fd9ad8e45cdcb2eefb78cee0c8 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_972c5560ba9721956b37b2cf9c2dccc1 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_0c65865ff2addf79a261bc96deb074f1 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_71de793a5a5fbe8c7c8ed002842e9197 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_adf5175283850043cadc948e51f1d996 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_0795239a206e1a00e7cb28e1e8861ff7 |
| publicationDate | 2013-04-01-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | ES-2355797-T7 |
| titleOfInvention | MEK heterocyclic inhibitors |
| abstract | A compound that includes resolved enantiomers, diastereomers and pharmaceutically acceptable salts thereof, said compound has the formula: where X is N or CR 10; R 1, R 2, R 8, R 9 and R 10 are independently hydrogen, halogen, cyano, nitro, trifluoromethyl, difluoromethyl, fluoromethyl, fluoromethoxy, difluoromethoxy, trifluoromethoxy, azido, -SR 11, -OR 3, -C (O ) R 3, -C (O) OR 3, -NR 4 C (O) OR 6, - OC (O) R 3, -NR 4 SO2R 6, -SO2NR 3 R 4, -NR 4 C (O) R 3, -C (O) NR 3 R 4, -NR 5 C (O) NR 3 R 4, -NR 5 C (NCN) NR 3 R 4, -NR 3 R 4, C1-C10 alkyl, C2 alkenyl C10, C2-C10 alkynyl, C3-C10 cycloalkyl, C3-C10 cycloalkylalkyl, -S (O) j (C1-C6 alkyl), -S (O) j (CR 4 R 5) m-aryl, aryl, arylalkyl , heteroaryl, heteroarylalkyl, heterocyclyl, heterocyclylalkyl, - O (CR 4 R 5) m-aryl, -NR 4 (CR 4 R 5) m-aryl, -O (CR 4 R 5) m-heteroaryl, -NR 4 ( CR 4 R 5) m-heteroaryl, -O (CR 4 R 5) m-heterocyclyl or -NR 4 (CR 4 R 5) m-heterocyclyl, wherein any of said parts alkyl, alkenyl, alkynyl, cycloalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, heterocyclyl and heterocyclylalkyl are optionally substituted with one or more independently selected groups of oxo (with the proviso that it is not substituted in an aryl or heteroaryl), halogen, cyano, nitro, trifluoromethyl, difluoromethoxy, trifluoromethoxy, azido, -NR 4 SO2R 6, -SO2NR 3 R 4, -C (O) R 3, -C (O) OR 3, -OC (O) R 3, -NR 4 C (O) OR 6, - NR 4 C (O) R 3, -C (O) NR 3 R 4, -NR 3 R 4, -NR 5 C (O) NR 3 R 4, - NR 5 C (NCN) NR 3 R 4, -OR 3, aryl, heteroaryl, arylalkyl, heteroarylalkyl, heterocyclyl and heterocyclylalkyl, and wherein said aryl, heteroaryl, arylalkyl, heteroarylalkyl, heterocyclyl or heterocyclylalkyl rings may be further substituted with one or more groups selected from halogen, hydroxy, cyano, nitro, azido, fluoromethyl, difluoromethyl, trifluoromethyl, C1-C4 alkyl, C2 alkenyl -C4, C2-C4 alkynyl, C3-C6 cycloalkyl, C3-C6 heterocycloalkyl, NR 3 R 4 and OR 3; R 7 is hydrogen, trifluoromethyl, C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, C3-C10 cycloalkyl, C3-C10 cycloalkylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, heterocyclyl or heterocyclyl alkyl parts of any part alkyl, alkenyl, alkynyl, cycloalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, heterocyclyl and heterocyclylalkyl are optionally substituted with one or more independently selected groups of oxo (with the proviso that it is not substituted in an aryl or heteroaryl), halogen, cyano , nitro, trifluoromethyl, difluoromethyl, fluoromethyl, difluoromethoxy, trifluoromethoxy, azido, -NR 11 SO2R 14, -SO2NR 11 R 12, - C (O) R 11, C (O) OR 11, -OC (O) R 11, -NR 11 C (O) OR 14, -NR 11 C (O) R 12, -C (O) NR 11 R 12, -SR 11, -S (O) R 14, -SO2R 14, - NR 11 R 12, -NR 11 C (O) NR 12 R 13, -NR 11 C (NCN) NR 12 R 13, -OR 11, C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, C3-C10 cycloalkyl, aryl, heteroaryl , arylalkyl, heteroarylalkyl, heterocyclyl and heterocyclylalkyl and wherein said aryl, heteroaryl, arylalkyl, heteroarylalkyl, heterocyclyl or heterocyclylalkyl rings may also be substituted with one or more groups selected from halogen, hydroxy, cyano, nitro, difluoromethyl, fluoromethyl , C1-C4 alkyl, C2-C4 alkenyl, C2-C4 alkynyl, C3-C6 cycloalkyl, C3-C6 heterocycloalkyl, NR 3 R 4 and OR 3; R 3 is hydrogen, trifluoromethyl, C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, C3-C10 cycloalkyl, C3-C10 cycloalkylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, heterocyclyl, heterocyclyl, alkyl amino acid phosphate , wherein any of said alkyl, alkenyl, alkynyl, cycloalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, heterocyclyl and heterocyclylalkyl parts are optionally substituted with one or more independently selected groups of oxo (with the proviso that it is not substituted in an aryl or heteroaryl), halogen, cyano, nitro, trifluoromethyl, difluoromethoxy, trifluoromethoxy, azido, -NR 11 SO2R 14, - SO2NR 11 R 12, -C (O) R 11, C (O) OR 11, -OC (O) R 11, -NR 11 C (O) OR 14, -NR 11 C (O) R 12, -C (O) NR 11 R 12, -SR 11, -S (O) R 14, - SO2R 14, - NR 11 R 12, -NR 11 C (O) NR 12 R 13, -NR 11 C (NCN) NR 12 R 13, -OR 11, aryl, heteroaryl, arylalkyl, heteroarylalkyl, heterocyclyl and heterocyclylalkyl lo, or R 3 and R 4 together with the atom to which they are attached form a 4- to 10-membered carbocyclic, heteroaryl or heterocyclic ring, wherein any of said carbocyclic, heteroaryl or heterocyclic rings are optionally substituted with one or more groups independently selected from halogen, cyano, nitro, trifluoromethyl, difluoromethoxy, trifluoromethoxy, azido, -NR 11 SO2R 14, -SO2NR 11 R 12, -C (O) R 11, C (O) OR 11, -OC (O) R 11 , - NR 11 C (O) OR 14, -NR 11 C (O) R 12, -C (O) NR 11 R 12, -SR 11, -S (O) R 14, -SO2R 14, -NR 11 R 12, -NR 11 C (O) NR 12 R 13, - NR 11 C (NCN) NR 12 R 13, -OR 11, aryl, heteroaryl, arylalkyl, heteroarylalkyl, heterocyclyl and heterocyclylalkyl; R 4 and R 5 are independently hydrogen or C1-C6 alkyl, or R 4 and R 5 together with the atom to which they are attached form a 4 to 10 membered carbocyclic, heteroaryl or heterocyclic ring, wherein said alkyl or any of said carbocyclic, heteroaryl and heterocyclic rings are optionally substituted with one or more groups independently selected from halogen, cyano, nitro, trifluoromethyl, difluoromethoxy, trifluoromethoxy, azido, -NR 11 SO2R 14, -SO2NR 11 R 12, -C (O) R 11 , C (O) OR 11, -OC (O) R 11, -NR 11 C (O) OR 14, -NR 11 C (O) R 12, -C (O) NR 11 R 12, -SR 11, -S (O) R 14, -SO2R 14, -NR 11 R 12, -NR 11 C (O) NR 12 R 13, - NR 11 C (NCN) NR 12 R 13, -OR 11, aryl, heteroaryl, arylalkyl, heteroarylalkyl, heterocyclyl and heterocyclylalkyl; R 6 is trifluoromethyl, C1-C10 alkyl, C3-C10 cycloalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, heterocyclyl or heterocyclylalkyl, wherein any of said alkyl, cycloalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, heterocyclyl are optionally heterocyclyl groups substituted with one or more independently selected groups of oxo (with the proviso that it is not substituted in an aryl or heteroaryl), halogen, cyano, nitro, trifluoromethyl, difluoromethoxy, trifluoromethoxy, azido, -NR 11 SO2R 14, - SO2NR 11 R 12, -C (O) R 11, C (O) OR 11, -OC (O) R 11, -NR 11 C (O) OR 14, -NR 11 C (O) R 12, -C (O) NR 11 R 12, -SR 11, -S (O) R 14, - SO2R 14, -NR 11 R 12, -NR 11 C (O) NR 12 R 13, -NR 11 C (NCN) NR 12 R 13 , -OR 11, aryl, heteroaryl, arylalkyl, heteroarylalkyl, heterocyclyl and heterocyclylalkyl, R 11, R 12 and R 13 are independently hydrogen, C1-C10 alkyl, C2-C10 alkenyl, aryl and arylalkyl, and R 14 is C1 alkyl -C10, C1-C10 alkenyl, aryl and arylalkyl; or any two of R 11, R 12, R 13 or R 14 together with the atom to which they are attached form a 4 to 10 membered carbocyclic, heteroaryl or heterocyclic ring, wherein any of said alkyl, alkenyl, aryl, arylalkyl, carbocyclic rings, heteroaryl rings or heterocyclic rings are optionally substituted with one or more groups independently selected from halogen, cyano, nitro, trifluoromethyl, difluoromethoxy, trifluoromethoxy, azido, aryl, heteroaryl, arylalkyl, heteroarylalkyl, heterocyclyl and heterocyclyl; W is heteroaryl, heterocyclyl, -C (O) OR 3, -C (O) NR 3 R 4, -C (O) NR 4 OR 3, -C (O) R 4 OR 3, -C (O) NR 4 SO2R 3, - C (O) (C3-C10 cycloalkyl), -C (O) (C1-C10 alkyl), -C (O) (aryl), -C (O) (heteroaryl), -C (O ) (heterocyclyl) or CR 3 OR 3, wherein any of said heteroaryl, heterocyclyl, -C (O) OR 3, -C (O) NR 3 R 4, -C (O) NR 4 OR 3, -C ( O) R 4 OR 3, - C (O) NR 4 SO2R 3, -C (O) (C3-C10 cycloalkyl), -C (O) (C1-C10 alkyl), -C (O) (aryl), -C (O) (heteroaryl), - C (O) (heterocyclyl) or CR 3 OR 3, are optionally substituted with one or more groups independently selected from halogen, cyano, nitro, azido, -NR 3 R 4, -OR 3, C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, cycloalkyl and heterocycloalkyl, wherein any of said C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, cycloalkyl and heterocycloalkyl are optionally substituted with one or more groups independently selected from -NR 3 R 4 and -OR 3; with the proviso that when X is CH, W cannot be C (O) aryl or C (O) heteroaryl, and also with the proviso that when X is CH, W is C (O) OR 3 and R 9 is F, R 7 cannot be H; m is 0, 1, 2, 3, 4 or 5; and j is 0, 1 or 2. |
| priorityDate | 2003-11-19-04:00^^<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: 1276.