LEDOUSSAL BENOIT,GOURDEL MARIE EDITH,RENAUD EMILIE,PIERRES CAMILLE,KEBSI ADEL
申请号：
IN2633/DELNP/2011
公开号：
IN2011DN02633A
申请日:
2011.04.08
申请国别(地区):
IN
年份:
2013
代理人:
摘要：
Nitrogenous Heterocyclic Compounds, Preparation thereof, and Use thereof as Antibacterial Agents The invention relates to nitrogenous heterocyclic compounds of formula (I): in which: R1 represents hydrogen, -{CH2)m-NH2, - (CH2)M-NH (C1-C6) alk, -(CH2)m-N{C1-C6)alk2, -(CH2)m-NH-C(NH)NH2 or - {CH2)m-NH-CH=NH, m is equal to 1"or 2 R2 and R3 together form a nitrogenous heterocycle of aromatic character with 5 vertices containing 1, 2 or 3 nitrogen atoms, substituted on a nitrogen atom by R4 R4 represents hydrogen, Ci-C6)alk or a chain of formula: - (A) n- (NH) o- (CH2) p- (CHR ) q R" A represents C=0, C=NH or SO2 R represents hydrogen or carboxy R represents hydrogen or NH2, NH (C1-C6) alk, N (C1-C6) alk2, CONH2, CONH (C1-C6) alk, CON (C1-C6) alk2, or a saturated heterocycle with 5 or 6 vertices containing 1 or 2 nitrogen atoms and, if appropriate, an oxygen or sulphur atom, fixed to the cha in by a nitrogen or by a carbon and optionally substituted by (C1-C6) alk n, o and q represent 0 or 1 and p represents an integer from 0 to 4 R5 represents OSO3H, OCFCO2H or OCF2CO2H - R1 being different from hydrogen, -(CH2)m-NH2, - (CH2)m-NH (C1-C6)alk or - (CH2)m-N (C1-C6) alk2 when R4 is hydrogen, -{C1-C6)alk, -{C=0)n-(CH2) (o-5)-NH2, -(C=0)n-(CH2) (0-5) "NH {C1-C6) alk or -{C=0)n-(CH2) {o-5)~N(C1-C6) alk2 and R5 is an OSO3H group, or when R4 has all of the values of R above except for the heterocycle, - and n, o, p and q cannot all be equal to 0 except when R is hydrogen or a CONH2, CONH (C1-C6) alk, CON {C1-C6) alk2 group, or a heterocycle in the free .form and in the form of zwitterions and salts with pharmaceutically acceptable bases and mineral or organic acids, their preparation and their use as antibacterial medicaments.
