AZALACTAM COMPOUNDS AS INHIBITORS OF HPK1 Russian patent published in 2024 - IPC C07D471/04 C07D487/04 C07D519/00 A61K31/4375 A61P35/00 

Abstract RU 2819642 C1

FIELD: organic chemistry.

SUBSTANCE: group of inventions includes a compound of formula I, pharmaceutically acceptable salts, stereoisomers, individual compounds specified in the claim, a pharmaceutical composition containing them, and methods of treatment. In formula I R1 is (C1-C6)alkyl, -N(R5)(R6), or (C3-C6)cycloalkyl, where said (C3-C6)cycloalkyl is substituted with 0 or 1 a substituent which is (C1-C6)alkyl or (C1-C6)alkoxy; R5 and R6 each independently represent hydrogen or (C1-C6)alkyl, or R5 and R6 together with nitrogen to which they are attached form (4–8-membered) heterocycloalkyl, which is substituted with 0, 1 or 2 substitutes independently selected from the group consisting of (C1-C6)alkyl, halogen(C1-C6)alkyl and (C1-C6)alkoxy; R2 is N(R7)(R8), each of R7 and R8 is independently hydrogen or (C1-C6)alkyl, which is substituted with 0 or 1 substituent, which is halogen, (C1-C6)alkoxy, cyano or hydroxy; R3a is hydrogen or (C1-C3)alkyl substituted with 0 or 1 substituent, which is hydroxy or (C1-C3)alkoxy; R3b is hydrogen or (C1-C3)alkyl, provided that R3a and R3b are not both H when R4 is (R4-i); R4 is (R4-i) or (R4-ii); R4N is (C1-C6)alkyl, halogen(C1-C6)alkyl or (C3-C6)cycloalkyl; R4C is hydrogen, (C1-C6)alkyl, halogen(C1-C6)alkyl or (C1-C6)alkoxy; R4D is hydrogen, (C1-C6)alkyl, halogen(C1-C6)alkyl, halogen(C1-C6)alkoxy or (C3-C6)cycloalkyl, where said (C1-C6)alkyl and halogen(C1-C6)alkyl are substituted with 0 or 1 substituent, which is hydroxy or (C1-C6)alkoxy; R4E is hydrogen or (C1-C6)alkyl; R4F is hydrogen, halogen, (C1-C6)alkyl or halogen(C1-C6)alkyl, where said (C1-C6)alkyl and halogen(C1-C6)alkyl are substituted with 0 or 1 substitute, which is hydroxy, cyano or (C1-C6)alkoxy.

EFFECT: proposed are 2-(pyridin-2-yl)-2,3-dihydro-1H-pyrrolo[3,4-c]pyridin-1-one derivatives of formula I, having inhibitory activity on HPK1 kinase.

21 cl, 8 tbl, 300 ex

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RU 2 819 642 C1

Authors

Barber, Dzhojenn

Cho-Shultts, Sudzhin

Del Bel, Mettyu L.

Gallego, Rebekka Enn

Khe, Mining

Dzhalej, Mekhran

Kania, Robert Stiven

Maktig, Mishel Enn

Nair, Sadzhiv Krishnan

Shmitt, Anne-Mari Dechert

Tattl, Dzhejmison Brajs

Chzhou, Dakhuej

Chzhou, Ru

Dates

2024-05-22Published

2021-04-28Filed