BENZENE DERIVATIVE Russian patent published in 2024 - IPC C07C311/21 C07C311/14 C07C59/64 C07D209/08 C07D209/44 C07D213/71 C07D215/58 C07D217/08 C07D277/24 C07D295/185 C07D305/06 C07D307/14 C07D333/62 A61K31/192 A61P25/00 

Abstract RU 2811803 C2

FIELD: pharmaceuticals.

SUBSTANCE: invention relates to a compound represented by general formula (I), or a pharmaceutically acceptable salt thereof, which can be used for the treatment and/or prevention of peripheral neuropathy and/or central neuropathy:

[Formula 1]

where: R1 is (1) -R11-COOR12, (2) -R13-CONR14R15, (3) -R17-CN, (4) -R18-CONHS(O)2-R19, (5) -R20-CycD, or

[Formula 2]

(where: ring 1 represents morpholine and n represents the integer 0); R2 represents (1) a halogen atom or (2) a C1-4 alkyl group, and p is an integer from 0 or 1; X represents either (1) CH2 or (2) an oxygen atom; L1 represents (1) a linear C3-7 alkylene group, which may be substituted by 1-2 RL1a, or (4) (a linear C1-3 alkylene group)-O-(a linear C1-3 alkylene group); R3 represents either (1) a hydrogen atom, (2) a halogen atom, or (4) a C1-2 alkyl group, and q represents an integer from 0 to 2, wherein: when

[Formula 4]

represents a single bond and q is 2, the set of R3 may be the same or different from each other; and when at least one of R3 is a methyl group, the methyl group can form cyclopropane in combination with a carbon atom in adjacent L1 ; CycA is (1) a C6 monocyclic carbocyclic ring or (2) a 5–10 membered monocyclic or bicyclic heterocyclic ring containing a heteroatom selected from an oxygen atom, a nitrogen atom and a sulfur atom; R4 represents (1) a halogen atom, (2) a hydroxyl group, (3) a C1-4 alkyl group, (4) a C1-4 haloalkyl group; (7) a cyano group or (8) a -SO2-C1-2 alkyl group, and r is an integer from 0 to 3, wherein when r is 2 or more, the plurality of R4 may be the same or different from each other; L2 represents -R31-L3-R32-; CycB is (1) a C5-6 monocyclic ring or (2) a 5–10 membered monocyclic or bicyclic heterocyclic ring containing a heteroatom selected from an oxygen atom, a nitrogen atom and a sulfur atom; and R5 represents either (1) a halogen atom, (2) a C1-6 alkyl group, (5) a C1-6 haloalkyl group, or (8) a C1-6 alkoxy group, and t represents the integer 0 or 1, and R11–R20, R31, R32, L3, CycD have the meanings specified in the claims.

EFFECT: production of a compound having neuroprotective and/or neurorestorative activity.

20 cl, 1 dwg, 2 tbl, 273 ex

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RU 2 811 803 C2

Authors

Nojima, Shoji

Sasaki, Kenji

Kambe, Tohru

Konemura, Takashi

Goto, Yoshikazu

Dates

2024-01-17Published

2019-07-30Filed