COMPOUND BASED ON PYRROLAMIDOPYRIDONE, METHOD OF ITS PREPARATION AND USE Russian patent published in 2023 - IPC C07D471/04 A61K31/437 A61K31/4545 A61K31/538 A61P29/00 A61P35/00 

Abstract RU 2809596 C2

FIELD: medicinal chemistry.

SUBSTANCE: invention relates to the compound based on acylaminopyrrolopyridone represented by general formula I, or a pharmaceutically acceptable salt thereof, wherein R1 is independently selected from C1-C8 alkyl, 3-8 membered cycloalkyl, C1-C8 alkyl substituted with 3-8 membered cycloalkyl, and; wherein C1-C8alkyl, 3-8-membered cycloalkyl, C1-C8alkyl substituted with 3-8-membered cycloalkyl, and optionally substituted with one or more substituents, the substituents being independently selected from halogen, cyano, C1-C6alkyl, C1-C6alkyl-O- and C1-C6alkyl-(SO2)-; if there are several substituents, they are the same or different; L1 is -(C1-C8alkyl)-, -(C2-C6alkynyl)- or -(C1-C6alkyl)-(CH2OCH2)m1 -(C1-C6alkyl)-; m1 equals 1, 2, 3 or 4; L2 represents the connecting link, , or; W represents either -CH2 - or -C(O)-; R2 represents hydrogen; X1 represents CH; X2 represents NH; R3 and R5 are each independently hydrogen; R4 represents, R6 and R7 are independently selected from hydrogen and -LR10 ; L represents -O-; R10 is independently selected from C1-C6 alkyl, 6-10 membered aryl and 6-10 membered aryl substituted with one or more substituents; wherein the substituents in the 6-10 membered aryl substituted with one or more substituents are independently halogen or C1-C6 alkyl; if there are several substituents, they are the same or different; or R4 is a C1-C6 alkylsulfone or a C1-C6 alkyl sulfoxide, R6 and R7 form a 6-membered heterocycloalkyl or a 6-membered heterocycloalkyl substituted with one or more substituents, wherein the heteroatoms in the 6-membered heterocycloalkyl are selected from N and O, and the number of heteroatoms is 2; wherein the substituent is independently C1-C6alkyl or =O; if there are several substituents, they are either the same or different. Besides, the invention relates to a method of producing a compound represented by formula I, a pharmaceutical composition based thereon, the use of this compound and a pharmaceutical composition containing it in the preparation of a medicinal product, as well as an intermediate compound represented by formula D, formula C, formula A or formula A', where Ra represents C1-C6alkyl.

EFFECT: provision of a new type of inhibitor of the BRD and/or c-Myc enzyme which can be used to obtain a medicinal product for the treatment of tumors or inflammatory diseases.

18 cl, 3 tbl, 27 ex

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RU 2 809 596 C2

Authors

Wan, Huixin

Pan, Jianfeng

Ma, Jingui

Dates

2023-12-13Published

2020-03-12Filed