http://rdf.ncbi.nlm.nih.gov/pubchem/patent/RU-2283311-C2
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_0a910d33c239980f3a705e312c5bad6a |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D403-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D409-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D417-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D417-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-505 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-517 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-517 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/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D413-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D417-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D417-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D403-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D409-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D409-12 |
| filingDate | 2001-06-21-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| grantDate | 2006-09-10-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_4aff9a3c1ae62016f225c88fee8163fa http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_814fa03bad2d560c768b46d27823b2a3 |
| publicationDate | 2006-09-10-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | RU-2283311-C2 |
| titleOfInvention | Quinazoline substituted derivatives and their using as inhibitors |
| abstract | FIELD: organic chemistry, biochemistry, medicine, pharmacy. n SUBSTANCE: invention relates to compound of the formula (IA) wherein X means -NH; R 5a represents optionally substituted 5-membered heteroaromatic ring chosen from the group of the following formulae: (a) (b) (c) (d) (e) (f) (g) (h) (i) or (j) wherein * means the addition position to the group X in the formula (IA); R 60 and R 61 from group of the formula (k) wherein p and q mean independently 0 or 1; R 1 ' and R 1 '' represent independently hydrogen atom, hydroxy-group wherein T represents C=O, sulfur atom (S), -C(=NOR)CO, -C(O)C(O) wherein R represents hydrogen atom, (C 1 -C 6 )-alkyl and phenyl; V represents independently hydrogen atom, hydroxyl, (C 1 -C 6 )-alkyl, (C 1 -C 6 )-alkoxy-, (C 2 -C 6 )-alkenyloxy-group, trifluoromethyl, phenyl optionally substituted with (C 1 -C 6 )-alkoxy- or (C 1 -C 6 )-alkanoyloxy-group or (C 3 -C 7 )-cycloalkyl; or V represents -N(R 63 )R 64 wherein one of R 63 and R 64 is chosen independently from hydrogen atom, (C 1 -C 10 )-alkyl optionally substituted with hydroxy-group, (C 1 -C 6 )-alkoxycarbonyl and (C 1 -C 6 )-alkoxyl; and (C 2 -C 6 )-alkenyl and another represents (C 1 -C 6 )-alkyl optionally substituted 1 or 2 with (C 1 -C 4 )-alkoxyl, cyano-group, (C 1 -C 4 )-alkoxycarbonyl, (C 2 -C 4 )-alkanoyloxy- or hydroxy-group; heteroaryl-(C 1 -C 6 )-alkyl wherein heteroaryl represents 5-6-membered ring comprising 1-2 heteroatoms chosen from oxygen (O), sulfur (S) and nitrogen (N) atoms and optionally substituted with (C 1 -C 6 )-alkyl; phenyl or phenyl-(C 1 -C 6 )-alkyl optionally substituted with 1, 2 or 3 groups chosen from halogen atom, N,N-di-(C 1 -C 6 )-alkyl)-amino-, N-(C 1 -C 6 )-alkyl)-amino-, (C 1 -C 6 )-alkoxy-group, (C 2 -C 6 )-alkanoyl, trifluoromethyl, cyano-group, (C 1 -C 6 )-alkyl optionally substituted with hydroxy- or cyano-group, carbamoyl, hydroxy-, trifluoromethoxy-, nitro-, (C 1 -C 6 )-alkylthio-, amino-group, -O-(C 1 -C 3 )-alkyl-O- and (C 1 -C 6 )-alkylcarbonyl; heteroaryl chosen from pyridyl, furanyl and indolyl optionally substituted with 1 or 2 hydroxy-groups, halogen atom, (C 1 -C 6 )-alkyl or (C 1 -C 6 )-alkoxy-group; (C 3 -C 7 )-cycloalkyl or (C 3 -C 7 )-cycloalkyl-(C 1 -C 6 )-alkyl optionally substituted with hydroxy-group; or R 63 and R 64 in common with nitrogen atom to which they are bound form 5-6-membered ring that can comprise additionally heteroatom N or O and can be optionally substituted with (C 1 -C 6 )-alkyl, hydroxy-group, hydroxy-(C 1 -C 6 )-alkyl or carbamoyl; R 62 represents hydrogen atom, (C 1 -C 6 )-alkyl, (C 1 -C 6 )-alkoxycarbonyl or carbamoyl; R 1' represents hydrogen atom; R 2' represents (C 1 -C 5 )-alkoxy-group; R 3' represents -X 1 R 9 wherein X 1 represents -O- and R 9 is chosen from the following groups: (1) (C 1 -C 5 )-alkyl; (2) (C 1 -C 5 )-alkyl-X 3 R 20 wherein X 3 represents -NR 25 - wherein R 25 represents hydrogen atom or (C 1 -C 3 )-alkyl; R 20 represents (C 1 -C 3 )-alkyl, cyclopentyl and (C 1 -C 3 )-alkyl group can comprise 1 or 2 substitutes chosen from oxo-, hydroxy-group, halogen atom and (C 1 -C 4 )-alkoxy-group; (3) represents (C 1 -C 5 )-X 4 -(C 1 -C 5 )-alkyl-X 5 R 26 wherein each among X 4 and X 5 represents -NR 31 - wherein R 31 represents hydrogen atom or (C 1 -C 3 )-alkyl; R 26 represents hydrogen atom or (C 1 -C 3 )-alkyl; (4) (C 1 -C 5 )-alkyl-R 32 wherein R 32 represents 5-6-membered saturated heterocyclic group bound through carbon or nitrogen atom with 1-2 heteroatoms chosen independently from O and N and wherein heterocyclic group can comprise 1 or 2 substitutes chosen from hydroxy-group, (C 1 -C 4 )-alkyl and (C 1 -C 4 )-hydroxyalkyl; (5) (C 1 -C 3 )-alkyl-X 9 -(C 1 -C 3 )-alkyl-R 32 wherein X 9 represents -NR 57 - wherein R 57 represents hydrogen atom or (C 1 -C 3 )-alkyl and R 32 is given above; R 4' represents hydrogen atom; or to its pharmaceutically acceptable salts. Compounds are inhibitors of kinase aurora 2 and can be used for preparing a medicinal agent used in treatment of proliferative diseases, in particular, in cancer treatment. Except for, invention relates to a pharmaceutical composition possessing the abovementioned activity and a method for preparing compounds of the formula (IA). n EFFECT: valuable medicinal properties of compounds and pharmaceutical composition. n 14 cl, 30 tbl, 477 ex |
| priorityDate | 2000-06-28-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 954.