http://rdf.ncbi.nlm.nih.gov/pubchem/patent/RU-2505534-C2

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filingDate 2009-06-30-04:00^^<http://www.w3.org/2001/XMLSchema#date>
grantDate 2014-01-27-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_709ec797422b9f9ff6389603ca631688
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_bc16414f9f2d1cc545998122e2f732ea
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publicationDate 2014-01-27-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber RU-2505534-C2
titleOfInvention Quinazoline derivatives inhibiting egfr activity
abstract FIELD: chemistry. n SUBSTANCE: invention relates to novel quinazoline derivatives of formula , where each of R 1 , R 2 and R 5 , independently, represents H; one of R 3 and R 4 represents where n - 1 or 2; each R a represents H, C 1-10 alkyl, optionally substituted with substituent, selected from group, including C 1-10 alkoxy, C 1-10 alkansulfonyl carboxy-group, 5-6-membered monocyclic heterocycloalkyl, which has one or several heteroatoms, selected from O and N, where N atom can be substituted with C 1-10 alkyl, phenyl, optionally substituted with halogen, 5-6-membered monocyclic heteroaryl, which has one or several heteroatoms, selected from N and S, 7-membered bicyclic heterocycloalkyl, which has 2 N atoms; C 2-10 alkenyl; C 2-10 alkinyl; cycloalkyl, representing saturated cyclic group, containing 3-6 carbon atoms; each of R b and R c , independently, represents H or C 1-10 alkyl, optionally substituted C 1-10 alkoxy, or R b and R c , together with atom of nitrogen, with which they are bound, form bicyclic ring of the following formula: , where each of m 1 , m 2 , m 3 , and m 4 is 0, 1 or 2; A is CH; B is NR, where R is H or C 1-10 alkyl; and each of R i , R ii , R iii , R iV , R v , R vi , R vii and R viii is H; or 6-7-membered monocyclic heterocycloalkyl, containing 1-2 N atoms, optionally substituted with substituent, selected from group, including hydroxy, C 1-10 alkyl, optionally substituted C 1-10 alkoxy, C 1-10 alkyl, optionally substituted with C 3-6 cycloalkyl; and each of R d , R e , independently represents H, C 2-10 alkenyl; C 2-10 alkinyl; or C 1-10 alkyl, optionally substituted with substituent, selected from group, including C 1-10 alkyloxy, hydroxy, CN, 5-6-membered monocyclic heterocycloalkyl, which has 1 or 2 N atoms, optionally substituted with C 1-10 alkyl, halogen or 5-6-membered heterocycloalkyl, which has 1 N atom, phenyl, optionally substituted with halogen, cycloalkyl, representing saturated cyclic group, containing 3-6 carbon atoms, 5-6-membered monocyclic heteroaryl, which has one or 2 N atoms; or R d and R e , together with nitrogen atom, with which they are bound, form 5-6-membered saturated heterocycloalkyl, which has 1-2 heteroatoms, selected from N and O, optionally substituted with substituent, selected from group, including C 1-10 alkyl (which is optionally substituted with C 3-6 cicloalkyl, C 1-10 alkoxy, halogen), 5-membered heterocycloalkyl, which has one N atom, halogen, C 1-10 alkansulfonyl, C 1-10 alkylcarbonyl, optionally substituted with halogen, or R d and R e , together with nitrogen, with which they are bound, form 7-10-membered, saturated, bicyclic heterocycloalkyl, containing 1-2 heteroatoms, selected from N and O, optionally substituted with C 1-10 alkyl; and the other of R 3 and R 4 represents H, halogen or C 1-10 alkoxy; X represents NR f , where R f represents phenyl, substituted with C 2-4 alkinyl; and Z represents N. Invention also relates to particular quinazoline derivatives, based on it pharmaceutical composition, and to method of cancer treatment. n EFFECT: novel quinazoline derivatives, inhibiting EGFR activity are obtained. n 11 cl, 171 ex
priorityDate 2008-06-30-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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