FIELD: chemistry.
SUBSTANCE: invention relates to a compound selected from formula I, or its stereoisomers, or pharmaceutically acceptable salts thereof, where R1 is optionally substituted C1-C3 alkyl; R2, R3 and R4 are independently selected from H, F, Cl; R5 is selected from (i) optionally substituted C6-C20 aryl, selected from phenyl; (ii) optionally substituted C5-C20 heteroaryl, selected from pyrazolyl, pyridinyl, pyrimidinyl, tetrahydroisoquinolinyl, 4,5,6,7-tetrahydropyrazolo[1,5-a]pyrazinyl, 6,7-dihydro-4H-pyrazolo[5,1-c][1,4]oxazinyl, 4,6,7-trihydropyrazolo[3,2-c][1,4]oxazinyl, 5,6,7,8-tetrahydro-1,6-naphthyridinyl, 2,3-dihydro-1H-isoindolyl, 4,5,6,7-tetrahydrothiazolo[5,4-c]pyridinyl; (iii) optionally substituted -(C6-C20 aryl)-(C3-C20 heterocyclyl), where heterocyclyl is selected from azetidinyl, piperidinyl, morpholino, piperazinyl; (iv) optionally substituted -(C5-C20 heteroaryl)-(C3-C20 heterocyclyl), where heteroaryl is selected from pyridinyl and pyridazinyl and heterocyclyl is selected from azetidinyl, pyrrolidinyl, piperidinyl, piperazinyl, 1,4-diazepanyl, 2,6-diazaspiro[3.3]heptanyl, 7,9-diazabicyclo[3.3.1]nonanyl, hexahydropyrrolo[3,4-c]pyrrolyl, morpholino; (v) optionally substituted -(C5-C20 heteroaryl)-(C1-C6 alkyl), where heteroaryl is selected from pirazolyl and pyridinyl; or (vi) optionally substituted -(C5-C20 heteroaryl)-C(=O)-(C3-C20 heterocyclyl), selected from (pyridinyl)-C(=O)-(morpholino); R6 represents H or C1-C3 alkyl; Y1 and Y2 are independently selected from CR6 and N; where C1-C3 alkyl, C3-C20 heterocyclyl, C6-C20 aryl and C5-C20 heteroaryl optionally substituted with one to three groups, independently selected from D, F, Cl, Br, I, -CH3, -CH2CH3, -CH2CH(CH3)2, -CH2OH, -CH2CH2OH, -C(CH3)2OH, -CH2F, -OC(O)CH3, -COCH3, -NHCH3, -N(CH3)2, =O, -OH, -OCH3, -OCH2CH2N(CH3)2, -OP(O)(OH)2, -CH2OCH3, cyclopropyl, azetidinyl, 1-(methylazetidin-3-yl)oxy, N-methyl-N-oxetan-3-ylamino, azetidin-1-ylmethyl, oxetanyl and morpholino; where group (a), formed Z1, Z2, Z3, Z4, Z5, X and NC(O), forms structure, given in claim, and wherein wavy line indicates bonding point. Invention relates to a pharmaceutical composition for treating a condition, mediated by Bruton's tyrosine kinase, containing a compound of formula (I) and a pharmaceutically acceptable carrier, lubricant, a diluent or filler. Compounds of formula (I) are intended for use as a drug for treating cancer, mediated by Bruton's tyrosine kinase.
EFFECT: pyridone and aza-pyridone compounds for treating disorders mediated by Bruton's tyrosine kinase (Btk).
20 cl, 9 dwg, 4 tbl, 907 ex
(а)
| Title | Year | Author | Number |
|---|---|---|---|
| BICYCLIC PIPERAZINE COMPOUNDS | 2012 |
|
RU2628616C2 |
| BRUTON'S TYROSINE KINASE INHIBITORS | 2010 |
|
RU2542585C2 |
| SERINE/THREONINE KINASE INHIBITORS | 2013 |
|
RU2650501C2 |
| HETEROYRYL PYRIDONES AND AZAPIRIDONS WITH ELECTROPHILIC FUNCTIONALITY | 2014 |
|
RU2646758C2 |
| NOVEL PYRIDINONES AND PYRIDAZINONES | 2009 |
|
RU2505538C2 |
| COMPOUND 8-FLUOROPHTHALAZINE-1(2H)-ONE AS INHIBITORS OF BRUTON TYROSINE KINASE | 2012 |
|
RU2622391C2 |
| PRIMARY CARBOXAMIDES AS BTK INHIBITORS | 2014 |
|
RU2708395C2 |
| TRANSGLUTAMINASE 2 (TG2) INHIBITORS | 2019 |
|
RU2781370C2 |
| CATECHOL-O-METHYL TRANSFERASE INHIBITORS AND USE THEREOF IN TREATING PSYCHOTIC DISORDERS | 2011 |
|
RU2586974C2 |
| SUBSTITUTED AMIDES, PHARMACEUTICAL COMPOSITION BASED THEREON, METHOD OF TREATING DISEASES SENSITIVE TO Btk, METHOD OF INCREASING SENSITIVITY OF CANCER CELLS TO CHEMOTHERAPY, METHOD OF REDUCING ERRORS WHEN TAKING MEDICINE AND IMPROVING OBSERVATION OF TREATMENT SCHEDULE, METHOD OF INHIBITING HYDROLYSIS OF ATP, METHOD OF DETERMINING PRESENCE OF Btk IN SAMPLE AND METHOD OF INHIBITING ACTIVITY OF B-CELLS | 2008 |
|
RU2470923C2 |
