CEPHALOSPORIN DERIVATIVES, ANTIBACTERIAL COMPOSITION CONTAINING THEREOF, DERIVATIVES OF 2-AMINOTHIAZOLES AS INTERMEDIATES, AND METHOD OF PREPARATION THEREOF Russian patent published in 2001 - IPC

FIELD: pharmaceutical chemistry. SUBSTANCE: invention provides novel cephalosporin derivatives of general formulas I and II: (I) and (II), wherein R¹ is selected from group including -NHC(O)ZR³ and -NR⁴R⁵, Z denotes -CH₂(X)_m or -C(NOR⁶), X sulfur atom, m= 0-1; R³ denotes thiazolyl group substituted by chlorine atom or amino group or (CH₂)T, in which n=1-6, T is guanidine group; R⁴ and R⁵ each denotes hydrogen atom; R⁶ hydrogen atom or group forming with adjacent oxygen atom protected hydroxyl group; R² hydrogen atom; each of G, H, L, and M denotes carbon atom; J nitrogen atm; rings A, B, D, and E are selected from group including thiazolyl and thiadiazolyl; R¹¹ denotes hydrogen atom; alk₁ is C1-C6-alkyl; alk₂ is C1-C6-alkyl optionally substituted by hydroxyl, amino, or carboxamido group; p= 0-1; R⁹⁹ is sulfur atom or SO₂ group; q=1; r=1-3; R¹² denotes group NR¹³R¹⁴, group a: (a), or group b: (b); R¹³-R¹⁷ each denotes hydrogen atom; or their pharmacologically acceptable salts. Antibacterial composition possessing activity against methicillinum-, vancomycin-, and ampicillinum- resistant bacteria includes pharmaceutically acceptable vehicle and effective amount of compound of formula I or II or its salt. Aminothiazole of general formula III: (III), in which Pg₁ is hydrogen atom or triphenylmethyl and Pg₂ is triphenylmethyl is prepared by reaction of compound IIIa: (IIIa) with chlorination agent in organic solvent. EFFECT: enlarged choice of cephalosporin derivatives. 25 cl, 5 dwg, 2 tbl, 140 ex