FIELD: pharmacology.
SUBSTANCE: in formula I , one of X and X' is N, and the other X and X' is C; one of the dashed lines in formula I is a single bond, and the other dashed line in formula I is a double bond; R1 is phenyl which may be substituted with 1 to 2 substituents selected from halogen atoms, S(O)2R, where R is a 5-6-member cycloalkyl in which one CH2 group is optionally replaced by an oxygen atom; NRaRb, -CH2NRaRb, 1,1-cyclopropyl-NRaRb, S(O)2NRaRb, wherein each Ra and Rb are hydrogen or both Ra and Rb are 4-6-member heterocycloalkyl which may further contain NH, N-CH3, O (oxygen) as a heteroatom and may be substituted by halogen atoms; R2 is -R5'R6, where R5' is a covalent bond or C1-C3alkyl, and R6 is C6cycloalkyl, and wherein R6 is optionally substituted one to two times with independently selected polar groups selected from amino or hydroxy; R3 is -NR7R8, where one of R7 and R8 is selected from H, C1-C6alkyl, and the other R7 and R8 is selected from C1-C6alkyl, C3-C6thcycloalkyl-C1-C6alkyl, each of which is optionally substituted once with a polar group selected from hydroxy; or R2 and R3 together form a linking group, wherein the linking group is -NH-(CH2)4-C(=O)-NH-(CH2)3-, R4 is H and R5 is H or a pharmaceutically acceptable salt thereof. The compounds are selected from IA or IB structure, where R1-R5 have the values indicated in paragraph 1.
EFFECT: possibility to use for treatment of a malignant tumour selected from the group consisting of myeloid leukemia, lymphoblastic leukemia, melanoma, malignant breast, lung, colon, liver, stomach, kidney, ovary, uterus and brain.
14 cl, 3 tbl, 5 ex
Title | Year | Author | Number |
---|---|---|---|
BICYCLIC HETEROCYCLIC COMPOUNDS AND THEIR APPLICATIONS | 2020 |
|
RU2811612C2 |
INFLUENZA VIRUS REPLICATION INHIBITORS, METHODS OF APPLICATION AND USING | 2016 |
|
RU2737190C2 |
NEW BICYCLIC DERIVATIVES, METHOD FOR THEIR PRODUCTION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM | 2016 |
|
RU2760554C1 |
PYRAZOLOPYRIMIDONE OR PYRROLOTRIAZONE DERIVATIVES, METHOD OF PREPARING SAME AND PHARMACEUTICAL APPLICATIONS THEREOF | 2014 |
|
RU2674977C2 |
PHARMACEUTICAL AGENT CONTAINING INHIBITOR OF SODIUM-DEPENDENT PHOSPHATE CARRIER | 2015 |
|
RU2740008C2 |
PHARMACEUTICAL PRODUCT CONTAINING INHIBITOR OF SODIUM DEPENDENT PHOSPHATE CARRIER | 2015 |
|
RU2811864C1 |
MACROCYCLIC COMPOUNDS AS TRK KINASE INHIBITORS | 2019 |
|
RU2778294C2 |
DERIVATIVES OF PYRROLOPYRIMIDINE USEFUL AS JAK-KINASES INHIBITORS | 2012 |
|
RU2618673C2 |
THIENO[2,3-d]PYRIMIDINES AS ANTIMICROBIAL AGENTS | 2018 |
|
RU2803136C2 |
SERINE/THREONINE KINASE INHIBITORS | 2013 |
|
RU2650501C2 |
Authors
Dates
2017-09-26—Published
2012-10-01—Filed