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Neue heterozyklische Stickstoffverbindungen, ihre Herstellung und ihre Verwendung als antibakterielle Medikamente
专利权人:
ASTRA ZENECA HOLDING FRANCE
发明人:
申请号:
EP14192364.9
公开号:
EP2853534A1
申请日:
2009.07.29
申请国别(地区):
EP
年份:
2015
代理人:
摘要:
NOVEL HETEROCYCLIC NITROGEN COMPOUNDS, THEIR PREPARATION AND THEIR USE AS ANTIBACTERIAL MEDICAMENTS The invention relates to nitrogenous heterocyclic compounds of formula (I):in which :R 1 represents - (CH 2) m -NH 2, - (CH 2) m -NH (C 1 -C 6) alk, - (CH 2) m -N (C 1 -C 6) alk 2, - ( CH 2) m -NH-C (NH) NH 2 or - (CH 2) m -NH-CH = NH, m is 1 or 2;R 2 and R 3 together form a nitrogenous heterocyclic ring with 5-membered aromatic atoms containing 1, 2 or 3 nitrogen atoms, substituted on a nitrogen atom by R 4;R 4 represents hydrogen, (C 1 -C 6) alk or a chain of formula:€ ƒ € ƒ € ƒ € ƒ € ƒ € ƒ € ƒ - (A) n - (NH) o - (CH 2) p - (CHR ') q R ";A represents C = O, C = NH or SO 2;R 'is hydrogen or carboxy;R "is hydrogen, NH 2, NH (C 1 -C 6) alk, N (C 1 -C 6) alC 2, CONH 2, CONH (C 1 -C 6) alk, CON (C 1 -C 6) alc 2, or a saturated heterocycle with 5 or 6 vertices containing 1 or 2 nitrogens and optionally an oxygen or a sulfur, attached to the chain by a nitrogen or a carbon and optionally substituted by (C 1 -C 6) alc ;n, o and q represent 0 or 1 and p represents an integer of 0 to 4;R 5 represents OSO 3 H, OCFCO 2 H or OCF 2 CO 2 H;- R 1 being different - (CH 2) m -NH 2, - (CH 2) m -NH (C 1 -C 6) alc or - (CH 2) m -N (C 1 -C 6) alc 2 when R 4 is hydrogen, - (C 1 -C 6) alk, - (C = O) n - (CH 2) (O-5) -NH 2, - (C = O) n - (CH 2) (0 -5) -NH (C 1 -C 6) alk or - (C = O) n - (CH 2) (O-5) -N (C 1 -C 6) alk 2 and R 5 is a group OSO 3 H, or when R 4 has all the values of R "above with the exception of heterocycle,and n, o, p and q can not all be 0 except when R "is hydrogen or CONH 2, CONH (C 1 -C 6) alk, CON (C 1 -C 6) alk 2 or heterocycle;in free form and in the form of zwitterions and salts with pharmaceutically acceptable inorganic or organic bases and acids, their preparation and their use as antibacterial drugs.NOUVEAUX COMPOSES HETEROCYCLIQUES AZOTES, LEUR PREPARATION ET LEUR UTILISATION COMME MEDICAMENTS ANTIBACTERIENSL'invention concerne des compo
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