4-AMINOQUINOLINE-3-CARBOXYLIC ACID DERIVATIVES AND COMPOSITIONS CONTAINING THEM FOR ENHANCING SWEET TASTE Russian patent published in 2017 - IPC C07D215/42 C07D403/12 C07D405/12 C07D413/12 A61K31/4725 A23L2/60 A23L27/30 A61P1/00 

FIELD: chemistry.

SUBSTANCE: invention relates to a new derivative of quinoline of formula (I)

(I)

or its salt suitable for internal use, where R¹ and R² represents hydrogen; L represents a C1-C7 alkylene, C3-C6 cycloalkylene or -(CH₂)_1-3-(C3-C6) cycloalkylene; M represents -NR⁴-C(O)- or -C(O)-NR⁴-; when M represents -NR⁴-C(O)-, R⁴ represents hydrogen; or alternatively R⁴ represents a C1-C3 alkilinity linker, where the specified alkilinity linker and from 2 to 5 atoms of L, together with the nitrogen to which they are attached, form a 5-8-membered monocyclic, bicyclic or bridged heterocyclic ring that is optionally substituted and contains one hetero-atom representing a nitrogen atom; and R³ represents a C1-C6 alkyl, a substituted C1-C3 alkyl, a C3-C6 cycloalkyl, a substituted C3-C6 cycloalkyl, a 6-membered heterocyclyl containing one oxygen atom, or a substituted 6-membered heterocyclyl containing one nitrogen atom; when M represents -C(O)-NR⁴-, R⁴ represents hydrogen; or alternatively R⁴ and R³ together with the nitrogen to which they are attached form a 5-6-membered monocyclic heterocyclic ring which contains one nitrogen atom; where in the group indicated as substituted, one substituent is selected from the group consisting of the following substituents: -NH₂, a hydroxyl, a C_1-6 alkoxy, a C_1-6 alkyl, a 6-membered heterocyclyl containing one or two atoms selected from N and O, a C_3-4 cycloalkyl, and C(=O)NR^aR^a, where each R^a independently means hydrogen or a C_3-6 cycloalkyl; provided that the compounds of the formula (I) cannot represent compounds mentioned in claim 1. The invention also relates to a composition based on a compound of the formula (I) and methods for enhancing the sweet taste.

EFFECT: new quinoline derivatives useful as sweet taste modifiers are obtained.

31 cl, 24 tbl, 24 ex