FIELD: chemistry.
SUBSTANCE: invention concerns new derivatives of 1,3,4-triazaphenalene and 1,3,4,6-tetraazaphenalene of formula I and their pharmaceutically acceptable salts with inhibition effect on epidermal growth factor receptor (EGFR) of tyrosinekynase and with antiproliferation activity. E.g. compounds can be applied in treatment and prevention of cancer, particularly solid tumours. In formula I 
, Z is C or N; R1 and R2 are independently selected out of H, lower alkyl; R3 and R4 are independently selected out of H, F, Cl or Br; R5 is selected out of H, oxo group, thione, C1-C3alkyl. Invention also concerns pharmaceutical compositions containing the claimed compounds.
EFFECT: obtaining compounds with inhibition effect on EGFR of tyrosinekynase and with antiproliferation activity.
22 cl, 5 dwg, 23 ex
| Title | Year | Author | Number |
|---|---|---|---|
| SUBSTITUTED 4-(SELENOPHEN-2(OR 3)-YLAMINO) PYRIMIDINE COMPOUNDS AND METHODS OF USE THEREOF | 2011 |
|
RU2597609C2 |
| DERIVATIVES OF QUINAZOLINE OR THEIR PHARMACEUTICALLY ACCEPTABLE SALTS, A METHOD OF THEIR SYNTHESIS AND A PHARMACEUTICAL COMPOSITION BASED ON SAID | 1993 |
|
RU2127263C1 |
| 4-HETEROCYCLYL-SUBSTITUTED DERIVATIVE OF QUINAZOLINE, PHARMACEUTICAL COMPOSITION | 1995 |
|
RU2137762C1 |
| QUINAZOLINE DERIVATIVES AND THEIR USE AS INHIBITORS OF VESSEL ENDOTHELIUM GROWTH FACTOR | 1997 |
|
RU2196137C2 |
| METHOD OF PRODUCING QUINAZOLINONE DERIVATIVES | 2009 |
|
RU2520098C2 |
| 3-HYDROXYQUINAZOLINE-4(3H)-ONE DERIVATIVES AS HISTONE DEACETYLASE INHIBITORS AND A METHOD FOR PRODUCTION THEREOF | 2020 |
|
RU2740503C1 |
| PHENOXYPYRIDINYLAMIDE DERIVATIVES, AND THEIR USE IN TREATMENT OF PDE4-MEDIATED DISEASE STATES | 2009 |
|
RU2509077C2 |
| DERIVATIVES OF PIPERAZINE AND PIPERIDINE AND METHOD OF THEIR SYNTHESIS | 1997 |
|
RU2178414C2 |
| 5-OXA-2-AZASPIRO[3.4]OCTANE DERIVATIVES AS M4 AGONISTS | 2020 |
|
RU2820477C1 |
| PYRAZOLOPYRIMIDINE DERIVATIVES AS CYCLIN-DEPENDENT KINASE INHIBITORS | 2005 |
|
RU2414472C9 |
