4-AMINOMETHYLBENZOIC ACID DERIVATIVES Russian patent published in 2018 - IPC C07C229/38 C07C229/46 C07D277/34 C07D333/16 C07D333/20 C07D333/56 A61K31/197 A61K31/275 A61K31/381 A61K31/426 A61P9/10 A61P9/12 A61P11/00 A61P43/00 

Abstract RU 2673245 C2

FIELD: chemistry.

SUBSTANCE: invention relates to a novel compound of formula (1) and a pharmaceutically acceptable salt thereof. Disclosed is a medicament containing a compound represented by general formula (1), a pharmaceutically acceptable salt thereof, or a solvate thereof. Compounds have the properties of the activation effect of soluble guanylate cyclase (sGC) and can be used to treat diseases such as heart failure, hypertension, pulmonary hypertension and coronary heart disease. In formula (1)

Ar represents a phenyl group or a 5-membered heteroaryl group containing a sulphur atom; Y represents a hydrogen atom, C1-C6 alkyl group, halogen C1-C4 alkyl group, a cyano group or a halogen atom; A represents a C1-C3 alkylene chain which may be substituted wit two C1-C2 alkyl groups, where are two C1-C2 alkyl groups may be substituents on the same carbon atom of the C1-C3 alkylene chain and also two C1-C2 alkyl groups taken together can form a C3-C5 saturated hydrocarbon ring containing one carbon atom of the C1-C3 alkylene chain; X represents a hydrogen atom or a halogen atom; V represents an oxygen atom or a methylene chain; R is a group selected from the following formulae

,

where R1, R2 and R3 each independently represents a hydrogen atom, a halogen atom, C1-C6 alkyl group that may have a substitute C3-C6 cycloalkyl group, C1-C6 alkoxy, C3-C6 cycloalkyl group, C3-C6 cycloalkoxy, halogen C1-C4 alkyl group, a phenyl group which may have a substituent group on the phenyl ring, a phenoxy group which may have a substituent group on the phenyl ring, where the substituent group is a halogen atom, cyano group or C1-C6 alkyl group, a benzyl group that may have a substituent group on the benzene ring, a phenethyl group which may have a substituent group on the benzene ring, or a benzyloxy group which may have a substituent group on the benzene ring, where the substituent group is a halogen atom or halogen C1-C6 alkyl group; W represents =CH- or a nitrogen atom, n is an integer from 1 to 3, and if n is 2 or more, the values of n for R1 may differ from each other.

EFFECT: disclosed are 4-aminomethylbenzoic acid derivatives.

8 cl, 61 tbl, 60 ex

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RU 2 673 245 C2

Authors

Uemoto Kadzukhiro

Sato Josimiti

Okada Naoki

Iimori Emiko

Kageyama Masayuki

Dates

2018-11-23Published

2014-10-14Filed