IMIDAZOLIDYLIC MACROLIDE OR ITS ISOMERS, OR ITS PHARMACEUTICALLY ACCEPTABLE SALT, METHODS OF ITS SYNTHESIS AND PHARMACEUTICAL COMPOSITION SHOWING IMMUNOSUPPRESSIVE ACTIVITY Russian patent published in 1998 - IPC

Abstract RU 2108338 C1

FIELD: organic chemistry, heterocyclic compounds. SUBSTANCE: product: imidazolidylic macrolide of the formula (I): where R1 - group where: G means NR6; R2 has values indicated for R1, H, (C1-C10)-alkyl; R3 - H, OH; R4 - H; R5 - methyl, ethyl or propyl; R6 - H, (C1-C6)-alkyl possibly substituted with phenyl that can be substituted with halogen; R7 and R8 are taken independently from H, (C1-C7)-alkyl, R14O(CH2)m- where R14- - H or (C1-C6)-alkyl; m = 0, 1, 2, 3; groups phenyl--(CH2)m- and phenyl group can be substituted with substituents X, Y, Z; A is taken from group involving: (C1-C10)-alkyl, group where s = 0-6, t = 0-6; Q - H; W - oxygen atom; X, Y and Z are taken independently from group involving: H, (C1-C10)-alkyl, halogen atom, trifluoromethyl, group R16O(CH2)m- where R16 - H, (C1-C6)-alkyl, hydroxy-(C2-C3)-alkyl, -CF3 and m = 0, 1, 2 or 3; or two of substituents X, Y and Z can be bound each with other and form five-membered saturated ring involving 2 oxygen atoms and 3 carbon atoms; n = 2. Invention proposes also two methods of synthesis of compounds (I) and pharmaceutical composition based on thereof. Synthesized compounds show IMMUNOSUPPRESSIVE activity. EFFECT: improved method of synthesis. 8 cl, 2 tbl

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RU 2 108 338 C1

Authors

Mark Goulet[Us]

Piter Dzh.Sinklejr[Us]

Frederik Vong[Us]

Mehtt'Ju Dzh.Vivratt[Us]

Dates

1998-04-10Published

1992-09-02Filed