BENZAMIDE COMPOUNDS Russian patent published in 2023 - IPC C07D471/04 C07D211/46 C07D295/155 C07D471/14 C07D491/107 A61K31/496 A61K31/5377 A61P35/00 

Abstract RU 2801647 C2

FIELD: pharmaceuticals.

SUBSTANCE: invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof. In formula (I): R1 is selected from the group consisting of hydrogen, halogen, unsubstituted C1-C6 alkyl, and unsubstituted C1-C6 haloalkyl; each R2 is independently unsubstituted C1-C6 alkyl; or, when m is 2, each R2 is independently unsubstituted C1-C6 alkyl, or two R2 groups taken together with the atom(s) to which they are attached form an unsubstituted C3-C6 cycloalkyl; R3 is X-R3A; R3A is an unsubstituted 5–10-membered heteroaryl such as ; R4 is NO2; R5 is -X1-(Alk1)n-R7; Alk1 is selected from unsubstituted C1-C4 alkylene and C1-C4 alkylene substituted with 1, 2 or 3 substituents independently selected from fluorine, chlorine, unsubstituted C1-C3 alkyl and unsubstituted C1-C3 haloalkyl; R7 is selected from substituted or unsubstituted C3-C10 cycloalkyl and substituted or unsubstituted 3–10-membered heterocyclyl containing 1–2 heteroatoms selected from nitrogen and oxygen; m is either 0, 1 or 2; n is selected from 0 and 1; X1 is -NH-; and X is -O-. Also the following is provided: a pharmaceutical composition, a method of treating cancer or a tumor, a method of inhibiting the replication of a malignant formation or tumor, a method of inhibiting Bcl-2 activity, and using a compound of formula (I) or a pharmaceutical composition for the manufacture of a medicinal product.

EFFECT: proposed compounds, as well as their pharmaceutically acceptable salts and compositions are used to treat diseases or conditions mediated by Bcl-2 including conditions characterized by excessive cell proliferation, such as cancer and tumors.

35 cl, 7 dwg, 3 tbl, 77 ex

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RU 2 801 647 C2

Authors

Pinchman, Dzhozef Robert

Khuan, Piter Tsinkhua

Banker, Kevin Duejn

Sit, Rakesh Kumar

Samatar, Akhmed Abdi

Dates

2023-08-11Published

2019-01-08Filed