http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-051794-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_da54f7ebbd2d9d8a82f92aca4d1b4e48 |
| 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/C07D213-85 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P17-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P3-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P17-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P29-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P15-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P13-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P27-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P13-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-28 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-16 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D471-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P21-04 |
| filingDate | 2005-12-14-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_75cabb16dcd5176de37f4cd0c27673fb http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_813cdc3c9af9fc947eaf82f6158938b6 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_edab82ae6c83f11c4319873ad285aff5 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_43ae825901d939d8d54711cf556cb695 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_66a6fc4b24bc915e3b31b4d62629bf68 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_a9d10c30e36a9796d5c224b24b0912ba http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_c7f7c2b8a482b4c2d4eb16af2f2cfae5 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_49fc0b132fd502488d6aa274519e8824 |
| publicationDate | 2007-02-07-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-051794-A1 |
| titleOfInvention | 3-AMINO-PIRAZOL [3,4B] PYRIDINS AS INHIBITORS OF PROTEINTIROSINQUINASAS, ITS PREPARATION AND USE AS A MEDICINAL PRODUCT |
| abstract | The use of the compounds of the general formula (1) as protein-tyrosine kinase inhibitors to treat different diseases, such as those where angiogenesis, lymphangiogenesis or vasculogenesis, hyperproliferation vasodilation of body cells or neurodegenerative diseases participate. Claim 1: Compounds of the general formula (1), characterized in that: R 1 represents C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, C 3-10 cycloalkyl, C 3-10 heterocycloalkyl, aryl or heteroaryl, optionally substituted with one or more same or different K groups, where C3-10-heterocycloalkyl and / or heteroaryl is interrupted by at least one of the following ring atoms: nitrogen, oxygen and / or sulfur, and the C3-10-heterocycloalkyl and / or heteroaryl may be attached to pyrazolpyridine only through a carbon atom of the ring, and C3-10-cycloalkyl and / or C3-10-heterocycloalkyl may be interrupted by one or more groups - (CO) -, -SO- or -SO2- same or different in the ring, and optionally may contain one or more double bonds in the ring, or C3-10-cycloalkyl, aryl, C3-10-heterocycloalkyl or substituted heteroaryl with the group -O- (CH2) nO-, where the terminal oxygen atom of the group -O- (CH2) nO- is directly linked to an equal group or to a carbon atom of a C3-10-cycloalkyl ring, aryl ring, C3-10-heterocycloalkyl ring or attached heteroaryl ring group; K represents halogen, hydroxyl or the group -OR3, COR4 or -NR5R6, or represents -C3-10-cycloalkyl, C3-10-heterocycloalkyl, aryl or heteroaryl, optionally substituted with one or more same or different L groups, where C3 -10-heterocycloalkyl and / or heteroaryl is interrupted by at least one of the following ring atoms: nitrogen, oxygen and / or sulfur, and C3-10-cycloalkyl and / or C3-10-heterocycloalkyl may be interrupted optionally in the ring by one or more groups -C (O) -, -SO- or -SO2- same or different, and optionally it may contain one or more double bonds in the ring; L represents C1-6-alkyl or the groups -COR4, -OR3 or -NR5R6; R2 represents C1-6-alkyl, C3-10-cycloalkyl, aryl or heteroaryl, optionally substituted with one or more same or different M groups; R3 represents C1-6-alkyl, aryl or - (CH2) n-aryl optionally substituted with one or more same or different -NR5R6 groups; R4 represents hydrogen, hydroxyl, C1-6-alkyl or C1-6-alkoxy; M represents amino, cyano, halogen, hydroxyl, nitro or C1-6-alkyl optionally substituted with one or more amino, cyano, halogen, hydroxyl, nitro, C1-6-alkoxy groups the same or different, C2-6-alkenyl, C2 -6-alkynyl or groups - O-R3, -COR4 or -CO-N-R7; R5 and R6, independently of each other, represent hydrogen, C1-6-alkyl or the group -COR4; and R7 represents hydrogen or NH2; n has a value between 1 and 4; taking into account that when: R1 represents methyl, R2 cannot simultaneously be methyl, -CH2-O-CH3, phenyl, chlorophenyl, benzofuranyl substituted with hydroxyl and / or methoxy, -CF3 or furanyl, or when R1 represents -CH2-O -CH3, R2 cannot simultaneously be methyl, or when R1 represents -CH = CH-phenyl, R2 cannot simultaneously be phenyl, or when R1 represents -CH = CH-chlorophenyl, R2 cannot simultaneously be phenyl or chlorophenyl, or when R1 represents -CH = CH-methoxyphenyl, R2 cannot simultaneously be phenyl or methoxyphenyl, or when R1 represents phenyl, R2 cannot be simultaneously -CF3, methyl, methoxyphenyl or phenyl, or when R1 represents methoxyphenyl, R2 cannot be simultaneously - CF3, when: R1 represents methylphenyl, R2 cannot be simultaneously -CF3, or when R1 represents chlorophenyl, R2 cannot simultaneously be chlorophenyl or -CF3, or when R1 represents dichlorophenyl, R2 cannot simultaneously be trimethoxyphenyl, or when R1 represents Bromophenyl, R2 cannot simultaneously be trimethoxyphenyl, or when R1 represents alkyl, alkenyl, aryl, aralkyl, cycloalkyl, a alkyl substituted with phenyl or p-methoxyphenyl, R2 cannot be simultaneously alkyl, alkenyl, aryl, aralkyl, cyano, a residue heterocyclic or cycloalkyl, or when R1 represents a lower alkyl, alkoxy or aryloxy radical, R2 cannot simultaneously be a lower alkyl radical, or when R1 represents hydroxyphenyl, R2 cannot simultaneously be heterocyclyl or heterocycloalkyl substituted with -COO-tert-butyl, or when R1 represents benzyloxyphenyl, R2 cannot simultaneously be heterocycloalkyl substituted with -COO-tert-butyl, solvates, hydrates, stereoisomers, diastereomers, enantiomers and salts thereof. Claim 15: Compounds of the general formulas (2) and / or (3), characterized in that: X represents halogen or -O-SOz-CmF2m + 1; m has a value between 1 and 4; and R1a and R2a have the same meaning as that having R1 and R2 according to one of claims 1 to 8, wherein K can additionally represent the groups -COR4 and R3, and can also represent the trimethylsilyl (TMS) groups, ter -butyl dimethylsilyl (TBDMS), tert-butyl diphenylsilyl (TBDPS), triethylsilyl (TES), C1-2-alkyl, C3-6-allyl, benzyl or the group -COR4a, solvates, hydrates, stereoisomers, diastereomers, enantiomers and salts thereof, as intermediates for the preparation of compounds of the formula (1). |
| priorityDate | 2004-12-14-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 65.