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2 315 041

(13)

(51)

IPC

C07D215/14(2006-01-01)

C07C309/65(2006-01-01)

C07D215/36(2006-01-01)

C07C229/40(2006-01-01)

C07D215/22(2006-01-01)

C07D401/06(2006-01-01)

C07D401/12(2006-01-01)

C07C205/49(2006-01-01)

C07C237/36(2006-01-01)

C07C43/205(2006-01-01)

A61K31/47(2006-01-01)

A61P19/02(2006-01-01)

A61P29/00(2006-01-01)

A61P37/08(2006-01-01)

(21) (22)

Application

2004135304/04, 2003-04-15

(24)

Start date

2003-04-15

(22)

Actual filing date

2003-04-15

(45)

Published

2008-01-20

(72)

Inventor

Lassua Mari-AgnesKner LoranDemod T'ErriDe Lavelej FransuazKozhezh T'ErriRut'E Sil'VehnGijomet Zheral'D

(73)

Holder

Jusibi, S.A.

DERIVATIVES OF 2,6-QUINOLINYL AND 2,6-NAPHTHYL, PHARMACEUTICAL COMPOSITIONS BASED ON THEREOF, THEIR USING AS VLA-4 INHIBITORS AND INTERMEDIATE COMPOUNDS Russian patent published in 2008 - IPC C07D215/14 C07C309/65 C07D215/36 C07C229/40 C07D215/22 C07D401/06 C07D401/12 C07C205/49 C07C237/36 C07C43/205 A61K31/47 A61P19/02 A61P29/00 A61P37/08

Abstract RU 2315041 C2

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to novel compounds of the formula (I): wherein X represents nitrogen atom (N) or -CH; R¹ represents cycloalkyl, aryl, heterocycle, aralkyl, heterocyclic alkyl or oxy-derivative, or group of the formula: ; R² represents -NR⁴R⁵, -OR⁴; R³ represents tetrazole, -CN, -CH₂OH or -CO-R⁷; R⁴ represents hydrogen atom (H), -G₁-R⁸ or group of the formula: or wherein G₁ represents -CO, -CH₂, -SO₂; R⁵ represents H, (C₁-C₄)-alkyl; R⁷ represents hydroxy-, amino-, hydroxylamino- or oxy-derivative or amino-derivative; R⁸ represents aryl, heterocycle, cycloalkyl, aralkyl. Also, invention describes a pharmaceutical composition designated for treatment of VLA-4-dependent inflammatory diseases based on proposed compounds. Also, invention considers using these compounds for treatment and preparing an agent for treatment of VLA-4-dependent inflammatory diseases. Invention provides synthesis of novel compounds possessing useful biological properties.

EFFECT: improved and valuable medicinal properties of compounds and pharmaceutical composition.

26 cl, 9 tbl, 5 ex

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RU 2 315 041 C2

Authors

Lassua Mari-Agnes

Kner Loran

Demod T'Erri

De Lavelej Fransuaz

Kozhezh T'Erri

Rut'E Sil'Vehn

Gijomet Zheral'D

Dates

2008-01-20—Published

2003-04-15—Filed