发明名称 CYCLIC BORONIC ACID ESTER DERIVATIVES AND THERAPEUTIC USE THEREOF
摘要 FIELD: chemistry.SUBSTANCE: invention relates to a compound of formula I:or a pharmaceutically acceptable salt thereof. Values of radicals are as follows: Y is a 1-4 atom alkylene or 2-4 atoms alkenylene linker; Ris selected from a group consisting of -C-alkyl,-C-alkenyl, -C-alkynyl, -NRR, -C-alkyl-R, -C-alkenyl-R, -C-alkynyl-R, -carboxylic radical-R, -CH(OH)C-alkyl-R, -CH(OH)C-alkenyl-R, -CH(OH)C-alkynyl-R, -CH(OH)-carboxylic radical-R, -C(=O)R, -C(=O)C-alkyl-R, -C(=O)C-alkenyl-R, -C(=O)C-alkynyl-R, -C(=O)C-carboxylic radical-R, -C(=O)NRR, -N(R)C(=O)R, -N(R)C(=O)NRR, -N(R)C(=O)OR, -N(R)C(=O)C(=NR)R, -N(R)C(=O)C(=CRR)R, -N(R)C(=O)C-alkyl-N(R)C(=O)R, -N(R)C(=NR)R, -C(=NR)NRR, -N=C(R)NRR, -N(R)SOR, -N(R)SONRR, -N=CHR, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted carboxylic radical and substituted or unsubstituted heterocyclic radical; Ris hydrogen; Ris hydrogen; Ris hydrogen; each Ris independently selected from a group consisting of H, -C-alkyl, C-alkenyl, -C-alkynyl, carboxylic radical, -C-alkyl-R, -C-alkenyl-R, -C-alkynyl-R, -carboxylic radical-R, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted carboxylic radical and substituted or unsubstituted heterocyclic radical; each Ris independently selected from a group consisting of H, -C-alkyl, -OR, -CH (=NH), -C (=O)OR, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted carboxylic radical and substituted or unsubstituted heterocyclic radical; each Ris independently selected from a group consisting of substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted carboxylic radical and substituted or unsubstituted heterocyclic radical; X is -COR; Ris selected from a group consisting of H, C-alkyl, -(CH)-R, -C(R)OC(O)C-alkyl, -C(R)OC(O)R, -C(R)OC(O)OC-alkyl and -C(R)OC(O)OR; each Ris independently selected from a group consisting of H and C-alkyl; and m independently denotes zero or a whole number, selected from 1-2. Invention also discloses a pharmaceutical composition, a method of increasing sensitivity to bacterial infection of β-lactam antibacterial agent, use of compounds for preparing a drug, a sterile container, a method of preparing a pharmaceutical composition and method for administering a solution.EFFECT: compound of formula I is used as therapeutic agents, especially in treating bacterial infections.64 cl, 4 dwg, 16 tbl, 17 ex
申请公布号 RU2599791(C2) 申请公布日期 2016.10.20
申请号 RU20130104951 申请日期 2011.08.08
申请人 REMPEX PHARMACEUTICALS, INC. 发明人 HIRST Gavin;REDDY Raja;HECKER Scott;TOTROV Maxim;GRIFFITH David C.;RODNV Olga;DUDLEV Michael N.;BOVER Serge
分类号 C07F5/02;A61K31/69;A61P31/04 主分类号 C07F5/02
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