COMPOUNDING, WHICH INHIBITES ACTIVITY OF BTK AND/OR JAK3 KINASES Russian patent published in 2018 - IPC C07D487/04 C07D491/48 C07D495/04 A61K31/53 A61K31/519 A61K31/5377 A61P37/02 A61P29/00 A61P7/02 A61P35/00 A61P19/02 A61P11/00 A61P17/06 A61P1/00 

Abstract RU 2650512 C2

FIELD: chemistry.

SUBSTANCE: present invention refers to the new compound of formula I, or to the stereoisomer thereof, or to the pharmaceutically acceptable salt, which has the properties of Bruton tyrosine kinase (BTK) activity inhibitor and/or Janus kinase 3 (JAK3). In the formula I (I) R is C3-8cycloalkyl substituted with the -NR2W group; 4-10 membered saturated N-heterocyclic group, which contains only one nitrogen atom in its ring and this nitrogen atom is replaced by W; or C1-4alkyl substituted with the 4-10 membered saturated N-heterocyclic group, which contains only one nitrogen atom in its ring and this nitrogen atom is replaced by W; W denotes or ; V denotes C or N; X denotes NR4 or O; Y denotes CH, S or O; Z is CH, S, O or NR5; R1 is phenyl or 5-9 membered heteroaryl, which contains 1-2 heteroatoms that are selected from nitrogen, oxygen and sulfur, optionally substituted by one or two R6; R2 is hydrogen or C1-8alkyl; R3a, R3b and R3c denote hydrogen; R4 is hydrogen or C1-8alkyl; R5 is hydrogen or C1-8alkyl; each R6 is independently selected from the group, which consists of halogen, heterocyclyl, C1-8alkyl, C1-C8cycloalkyl, C1-8haloalkyl, heterocyclyl-C1-8alkyl, hydroxy-C1-8alkyl, C1-8alkyloxy-C1-8alkyl, amino-C1-8alkyl, C1-8alkylamino-C1-8alkyl, di(C1-8alkyl) amino-C1-8alkyl, C1-8alkyloxy, heterocyclyloxy, heterocyclyl-C1-8alkyloxy, hydroxy-C1-8alkyloxy, C1-8alkyloxy-C1-8alkyloxy, C1-8alkylamino, di(C1-8alkyl) amino, C3-C8cycloalkylamino, heterocyclylamino, C1-8alkylamino-C1-8alkylamino, di(C1-8alkyl) amino-C1-8alkylamino, C1-8alkylcarbonyl, heterocyclylcarbonyl, C1-8alkylaminoacyl, di(C1-8alkyl) aminoacyl and heterocyclylaminoacyl, where in the given C1-8alkylaminoacyl, di(C1-8alkyl) aminoacyl and heterocyclylaminoacyl acyl denote the group -C(=O)-; and heterocyclyl as an independent group or as part of other group(s) is the saturated 6-membered heterocyclic group, which contains one or two heteroatoms that are selected from the group, which consists of N and O; optionally, each heterocyclyl is independently substituted with one or two substituents that are selected from the group, which consists of C1-8alkyl, hydroxy, C1-8alkyloxy and C1-8alkylcarbonyl.

EFFECT: compound can be used during the treatment of diseases such as rheumatoid arthritis, osteoarthritis, juvenile arthritis, systemic lupus erythematosus, psoriasis and psoriatic arthritis, the cancer that is selected from the group, which consists of B-cell chronic lymphocytic leukemia, acute lymphocytic leukemia, non-Hodgkin's lymphoma, Hodgkin's lymphoma, diffuse large-cell B-cell lymphoma, lymphoma of mantle cells and small-cell lymphocytic lymphoma.

24 cl, 3 dwg, 11 tbl, 145 ex

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RU 2 650 512 C2

Authors

Liu Jinming

Cha Mi Young

Li Gong

Li Zhanmei

Qiu Hongjuan

Kim Maengsup

Dates

2018-04-16Published

2014-09-18Filed