AMID DERIVATIVES OF N-CARBAMIDE-SUBSTITUTED AMINO ACIDS AS MODULATORS OF FORMYLPEPTIDE RECEPTOR-1 (FPRL-1) Russian patent published in 2017 - IPC C07C275/30 C07C317/42 C07C317/50 C07C323/44 C07C323/60 C07D209/20 C07D233/64 C07K5/06 A61K31/17 A61K31/197 A61K31/216 A61K31/4045 A61K31/417 

Abstract RU 2629205 C2

FIELD: chemistry.

SUBSTANCE: invention relates to a compoundd represented by the formula

,

its enantiomers, diastereoisomers or pharmaceutically acceptable salts, which have modulatory activity against N-formylpeptide receptor-1 (FPRL-1). In formula II, a is 1, b is 0 or a is 1, b is 1; R1 is -OH; R2 is C1-8 Alkyl, optionally substituted by C6-10 aryl, amide or heterocycle, wherein the heterocycle is a 3 to 10-membered aromatic ring which contains at least one heteroatom selected from nitrogen, wherein one methylene group in the alkyl can be replaced by sulfur or sulphonyl; R3 is hydrogen or halogen; R4 is hydrogen; R5 is a halogen, -CF3 Or -S (O)nR14; N is 0, 1 or 2; R6 is hydrogen; R7 is hydrogen or halogen; R8 is hydrogen or C1-8 Alkyl; R9 is hydrogen, C1-8 Alkyl, Optionally substituted with a hydroxyl group, or C6-10 aryl; R10 is hydrogen, C1-8 alkyl optionally substituted with a hydroxyl group, or C6-10 aryl; R9a is hydrogen or C1-8 alkyl optionally substituted with a hydroxyl group; R10a is hydrogen or C1-8 alkyl optionally substituted with a hydroxyl group; R14 is CF3 or C1-8 alkyl.

EFFECT: increased activity of derivatives.

12 cl, 5 tbl, 4 ex

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RU 2 629 205 C2

Authors

Bird Richard L.

Duong Ten T.

Donello Dzhon E.

Visvanat Veena

Garst Majkl E.

Dates

2017-08-25Published

2012-10-23Filed