发明名称 9-[(Substituted glycyl)amido)]-6-demethyl-6-deoxytetracykline compounds, processes and intermediates for their preparation and pharmaceutical preparations based thereon
摘要 In the present invention there are disclosed 9-[(substituted glycyl)amido)]-6-demethyl-6-deoxytetracykline compounds of the general formula I, in which R represents hydrogen; Re1 represents hydrogen or alkyl containing 1 to 3 carbon atoms; W represents an amino group, being optionally substituted with one group being selected from a group comprising alkyl having 1 to 8 carbon atoms, cycloalkylmethyl containing 3 to 6 carbon atoms in the cycloalkyl moiety, phenylmethyl, pyridylmethyl and thienylmethyl or with two alkyl groups having 1 to 3 carbon atoms; N-pyrrolidinyl or N-piperidyl, whereby each of the later groups can be optionally substituted with one methyl; and their pharmacologically acceptable salts with organic or inorganic acids. The compounds of the general formula III, in which Y represents bromine, chlorine, iodine or fluorine and R and Re1 are as specified above and their salts with organic and inorganic acids as intermediates for preparing the compounds of the general formula I. A process for preparing the compounds of the general formula I by reacting the compound of the general formula III with nucleophilic compound of the general formula WH, wherein W is as specified above in a polar aprotic solvent and in inert atmosphere. A process for preparing the compounds of the general formula I by reacting the compound of the general formula 1, wherein R represents hydrogen with a chloride of the compound of the general formula (R,Re1,W)C-C(=O)X, in which R and Re1 and W are as specified above and X represents bromine, chlorine, iodine or fluorine, in an inert solvent and in polar aprotic solvent in the presence of a base. In the present invention there are also claimed pharmaceutical and veterinary preparations based on the compounds of the general formula I. The compounds of the general formula I are antibacterial agents.
申请公布号 CZ288174(B6) 申请公布日期 2001.05.16
申请号 CZ19930001574 申请日期 1993.08.04
申请人 AMERICAN CYANAMID COMPANY 发明人 SUM PHAIK-ENG;LEE VING J.;TESTA RAYMOND T.
分类号 A61K31/65;A61P31/00;A61P31/04;C07C;C07C237/26;C07C239/18;C07C239/20;C07C255/50;C07C271/22;C07C323/29;C07D207/06;C07D207/14;C07D207/16;C07D207/30;C07D209/02;C07D211/14;C07D211/56;C07D213/40;C07D213/74;C07D221/22;C07D231/12;C07D231/14;C07D241/04;C07D241/14;C07D249/02;C07D249/04;C07D249/08;C07D265/28;C07D279/04;C07D295/14;C07D295/15;C07D295/215;C07D295/24;C07D307/33;C07D333/20;C07D333/36;C07F15/00;(IPC1-7):C07C237/26 主分类号 A61K31/65
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