SODIUM CHANNEL MODULATORS FOR THE TREATMENT OF PAIN Russian patent published in 2018 - IPC C07D277/52 C07D285/08 C07D417/12 C07D487/04 A61K31/18 A61K31/433 A61P29/00 

Abstract RU 2669367 C2

FIELD: chemistry.

SUBSTANCE: invention relates to compounds of formula (I):

Formula (I) or a pharmaceutically acceptable salt thereof, where: Z is -O- or -S-; Y is - (CH2)3-NR9R10; R1 is a partially unsaturated or aromatic 5- or 6-membered heterocycle; R2 independently in each case is -F, -Cl, -Br, -CH3 or -CN; R3 independently in each case is -H,- F, -Cl, -Br, -CF3, -OCF3, -CN, (C1-C12)alkyl or (C1-C12)alkoxy; R9 represents (C1-C6)alkyl, (C3-C8)cycloalkyl, pyrazolyl or pyridinyl; here R9 optionally is further substituted with 1 or 2 substituents selected from the group consisting of -COOH, -COOR11, -CONR11R12, -SO2R11, -SO2NR11R12, -OH, -CN, -OR11 and -NR11R12; where R11 and R12 can form a 6-membered heterocycloalkyl ring; R10 is R11, -COR11, -COOR11, -SO2R11, 5-methyl-2-oxo-1,3-dioxol-4-yl, , -COO-CH(CH3)OCOCH(CH3)2; or R9 and R10 together form a piperazinone or 4-8-membered heterocycloalkyl ring, wherein said heterocycloalkyl ring is substituted with 1 or 2 substituents selected from the group consisting of -COOH, -COOR11, -CH2-COOR11, -OH, -NH2, -CN and (C1-C8)alkoxy; R11 and R12 are independently H or (C1-C6)alkyl optionally substituted with 4-8-membered heterocycloalkyl ring; and m and n are each independently 1, 2, 3 or 4 modulating the sodium channels, in particular modulating NaV1.7.

EFFECT: modulators of the sodium channel for the treatment of pain are proposed.

40 cl, 33 ex, 2 tbl

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RU 2 669 367 C2

Authors

Babich Olga

Luo Robert Z.

Van-Fisher Yanlin

Polling Devid Dzh.

Venkatakhalan Srinivasan P.

Dates

2018-10-11Published

2014-03-13Filed