发明名称 IMIDAZOLIDYLIC MACROLIDE OR ITS ISOMERS, OR ITS PHARMACEUTICALLY ACCEPTABLE SALT, METHODS OF ITS SYNTHESIS AND PHARMACEUTICAL COMPOSITION SHOWING IMMUNOSUPPRESSIVE ACTIVITY
摘要 FIELD: organic chemistry, heterocyclic compounds. SUBSTANCE: product: imidazolidylic macrolide of the formula (I): <EMI ID=0.281 HE=78 WI=54 TI=CHI> where R - group <EMI ID=0.282 HE=21 WI=27 TI=CHI> where: G means NR ; R has values indicated for R , H, (C<SB>1</SB>-C<SB>10</SB>)-alkyl; R - H, OH; R - H; R - methyl, ethyl or propyl; R - H, (C<SB>1</SB>-C<SB>6</SB>)-alkyl possibly substituted with phenyl that can be substituted with halogen; R and R are taken independently from H, (C<SB>1</SB>-C<SB>7</SB>)-alkyl, R<SP>14</SP>O(CH<SB>2</SB>)<SB>m</SB>- where R<SP>14</SP>- - H or (C<SB>1</SB>-C<SB>6</SB>)-alkyl; m = 0, 1, 2, 3; groups phenyl--(CH<SB>2</SB>)<SB>m</SB>- and phenyl group can be substituted with substituents X, Y, Z; A is taken from group involving: (C<SB>1</SB>-C<SB>10</SB>)-alkyl, group <EMI ID=0.283 HE=15 WI=57 TI=CHI> where s = 0-6, t = 0-6; Q - H; W - oxygen atom; X, Y and Z are taken independently from group involving: H, (C<SB>1</SB>-C<SB>10</SB>)-alkyl, halogen atom, trifluoromethyl, group R<SP>16</SP>O(CH<SB>2</SB>)<SB>m</SB>- where R - H, (C<SB>1</SB>-C<SB>6</SB>)-alkyl, hydroxy-(C<SB>2</SB>-C<SB>3</SB>)-alkyl, -CF<SB>3</SB> 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) <EMI ID=0.284 HE=78 WI=54 TI=CHI> and pharmaceutical composition based on thereof. Synthesized compounds show IMMUNOSUPPRESSIVE activity. EFFECT: improved method of synthesis. 8 cl, 2 tbl+
申请公布号 RU2108338(C1) 申请公布日期 1998.04.10
申请号 RU19940020407 申请日期 1992.09.02
申请人 MERK EHND KO., INK. 发明人 MARK GOULET;PITER DZH.SINKLEJR;FREDERIK VONG;MEHTT'JU DZH.VIVRATT;MARK GOULET;PITER DZH.SINKLEJR;FREDERIK VONG;MEHTT'JU DZH.VIVRATT
分类号 C07H19/01;A61K;A61K31/395;A61K31/4178;A61K31/4184;A61K31/422;A61K31/423;A61K31/427;A61K31/428;A61K31/435;A61K31/436;A61K31/70;A61K31/7056;A61P37/06;C07D;C07D498/12;C07D498/18;C07H7/06;C07H15/04;C07H19/02;(IPC1-7):C07H19/01 主分类号 C07H19/01
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