N''-SUBSTITUTED 9a-N-(N'-CARBAMOYL- γ -AMINOPROPYL) AND 9a-N-(N'-THIOCARBAMOYL- γ -AMINOPROPYL) DERIVATIVES OF 9-DESOXO-9-DIHYDRO-9a-A3A-9a-HOMOERYTHROMYCINE A OR 5-O-DESOSAMINYL-9-DESOXO-9-DIHYDRO-9a-A3A-9a-HOMOERYTHRONOLIDE A Russian patent published in 2008 - IPC C07H17/00 A61K31/7048 A61K31/7052 A61P31/04 

Abstract RU 2328503 C2

FIELD: chemistry.

SUBSTANCE: invention relates to the N" -substituted 9a-N-(N'- carbamoyl-γ-aminopropyl) and 9a-M-(M'-thiocarbamoyl-γ-aminopropyl)) derivatives of 9-desoxo-9-dihydro-9a-ase-9a-homoerythromycine A or 5-O-desosaminyl-9-desoxo-9-dihydro-9a-ase-9a-homoerythronolide A, novel semisynthetic macrolide antibiotics from the group of azalides with the common formula 1, where R means H or cladinosyl fragment, R means H, R means the isopropyl group, 1-naphtyl, 2-naphtyl, benzene, 2-(trifluoromethyl)phenyl, 3-phenylpropyl, (3-phenylethyl, ehtoxicarbonylmethyl, 1-(1-naphtyl)ethyl, 3,4,5-trimethoxiphenyl and 2,4-dichlorphenyl, and X means O or S, or to their pharmaceutically compliant additive salts with the inorganic or organic acids and to the method of their production. The invention also relates to the pharmaceutical composition with the antibacterial activity and to the application of the compounds with the common formula 1 or their pharmaceutically compliant salts, in producing the said composition.

EFFECT: antibacterial activity.

16 cl, 26 ex, 1 tbl

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RU 2 328 503 C2

Authors

Kujundzhich Nedel'Ko

Bukvich Krajachich Mirjana

Brajsa Karmen

Dates

2008-07-10Published

2003-12-10Filed