发明名称 DERIVATIVES OF 7-, 8-, 9-(SUBSTITUTED)-6-DEMETHYL-6-DEHYDROXY-TETRACYCLINES, METHODS OF THEIR SYNTHESIS, INTERMEDIATE COMPOUNDS AND A PHARMACEUTICAL COMPOSITION
摘要 FIELD: organic chemistry, antibiotics. SUBSTANCE: invention relates to derivatives of 7-, 8-, 9-(substituted)-6-demethyl-6-dehydroxy- tetracyclines of the formula (I) <EMI ID=0.530 HE=27 WI=54 TI=CHI> where X - halogen; R and R are similar or distinct and mean H, NH<SB>2</SB>, halogen, NR<SP>2</SP>R and when R and R is NR<SP>2</SP>R and R is H then R - methyl, ethyl, n-propyl, 1-methylethyl, n-butyl, 1-methylpropyl, 2-methyl- propyl, 1,1-dimethylethyl; when R - methyl, ethyl then R is methyl, ethyl, n-propyl, 1-methylethyl, n-butyl, 1-methyl- propyl, 2-methylpropyl; when R is n-propyl then R is n-propyl, 1-methylethyl, n-butyl, 1-methylpropyl, 2-methyl- -propyl; when R is 1-methylethyl then R is n-butyl, 1-methylpropyl, 2-methylpropyl; when R is n-butyl then R is n-butyl, 1-methylpropyl, 2-methylpropyl; when R is 1-methylpropyl then R is 2-methylpropyl; when R and R are NR<SP>2</SP>R and R - H then R is -CO-R where R - H, NH<SB>2</SB>, mono-(C<SB>1</SB>-C<SB>6</SB>)-alkylamino-groups, diastereoisomers and enantiomers of mono - (C<SB>1</SB>-C<SB>6</SB>) - alkylamino - group; or R is di-(C<SB>1</SB>-C<SB>6</SB>)-alkylamino-group. Compounds are used as a pharmaceutical composition showing antibacterial activity. EFFECT: improved method of synthesis, enhanced effectiveness. 7 cl, 3 dwg, 3 tbl, 49 ex
申请公布号 RU2127255(C1) 申请公布日期 1999.03.10
申请号 RU19930048636 申请日期 1993.08.12
申请人 AMERIKAN TSIANAMID KOMPANI 发明人 FAJK-ENG SAM;VING DZH.LI;DZHOZEF DZH. KHLAVKA;REHJMOND T.TESTA
分类号 A61K31/65;A61P31/00;A61P31/04;C07C;C07C237/26;C07C239/18;C07C243/20;C07C245/20;C07C247/18;C07C255/41;C07C271/24;C07C271/60;C07C309/39;C07C309/65;C07C317/28;C07C323/59;C07D205/04;C07D207/16;C07D209/52;C07D221/22;C07D231/14;C07D233/61;C07D233/96;C07D241/12;C07D249/04;C07D249/08;C07D249/10;C07D249/16;C07D257/04;C07D261/08;C07D265/30;C07D265/36;C07D279/12;C07D295/08;C07D295/14;C07D295/20;C07D295/22;C07D307/18;C07D333/06;C07D333/36;C07D453/06;C07D471/08;C07D487/08;(IPC1-7):C07C237/26 主分类号 A61K31/65
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