wherein R 1 is amino or a protected amino group, R 2 is hydrogen or an organic group, R 3 is hydrogen, lower alkyl, hydrory(lower)alkyl, protected hydroxy(lower)alkyl, amino(lower)alkyl, protected amino(lower)alkyl, carbamoyl-(lower)alkyl, N,N-di(lower)alkylcarbamoyl(lower)alkyl or an imino protective group, R 4 is hydrogen, lower alkyl, carboxy, protected carboxy, amino,protected amino or carbamoyl, and Z is N or CH, and a pharmaceutically acceptable salt thereof, processes for their preparation and pharmaceutical compositions comprising them as an active ingredient in admixture with pharmaceutically acceptable carriers. The invention also relates to intermediates of the formula and processes for their preparation.
R' is amino or protected amino, R 2 is hydrogen, hydroxy protective group, lower alkyl, dihalogenated lower alkyl, cyclo(lower)alkenyl, thietanyl, carboxy(lower)alkyl or protected carboxy(lower)alkyl, R 3 is lower alkyl, R 4 and R 5 are each hydrogen, lower alkyl, hydroxy (lower)alkyl, lower alkoxy, amino or protected amino, R 6 is COO e , carboxy or protected carboxy, X ⊖ is an anion, and n is 0 or 1, with certain provisions, processes for their preparation and pharmaceutical compositions containing them. The invention relates also to compounds of the formula and of the formula in which Z is an acid residue.
R' is amino or protected amino, R' is aryl which may have suitable substituent(s), a heterocyclic group which may have suitable substituent(s), cyano, hydrogen or tri(lower)alkylsilyl, R' is carboxy or protected carboxy, and A is -CH=CH- or -C≡C-, and pharmaceutically acceptable saltthereof, processes for their preparation and pharmaceutical compositions containing them in association with a pharmaceutically acceptable, substantially non-toxic carrier or excipient. The invention also relates to intermediates of the formula and processes for their preparation.
R 1 is amino or acylamino, R 2 is 2,2-dihalovinyl or ethynyl, and R 3 is carboxy or protected carboxy,
and pharmaceutically acceptable salts thereof, processes for their preparations and pharmaceutical compositions comprising an effective amount of them or pharmaceutical acceptable salt thereof in association with a pharmaceutically acceptable, substantially non-toxic carrier or excipient. The invention also relates to the 1-oxides of such compounds and salts thereof.
摘要:
7-acylamino-3-vinylcephalosporanic acid derivatives of the formula: in which R 1 is amino-substituted-heterocyclic group which may have halogen, protected amino-substituted-heterocyclic groug which may have halogen, or a group of the formula: wherein R 3 is lower alkyl, R 2 is carboxy or a protected carboxy group, A is lower alkylene which may have certain substituents and pharmaceutically acceptable salt thereof and processes fortheir preparation and also a pharmaceutically composition comprising, as an effective ingredient, the above compound in association with pharmaceutically acceptable carriers. The invention also relates to the starting compounds and other starting compounds and their preparation.
摘要:
7-acylamino-3-substituted cephalosporanic acid derivatives of the formula: in which R 1 is a group of the formula: wherein R 4 is lower alkyl and
R 5 is amino or a protected amino group, R 2 is lower alkoxymethyl, lower alkylthiomethyl or lower alkenylthiomethyl, R 3 is carboxy or a protected carboxy group, and A is lower alkylene which may have certain substituents
and pharmaceutically acceptable salt thereof and processes for their preparation and also a pharmaceutically composition comprising, as an effective ingredient, the above compound in association with pharmaceutically acceptable carriers. The invention also relates to the starting compounds and their preparation.
R¹ is amino or protected amino, R² is lower alkyl substituted with 1 to 6 halogen, R³ is hydroxy(lower)alkyl, protected hydroxy(lower)alkyl or halo(lower)alkyl and R⁴ is hydrogen, or R³ and R⁴ are linked together to form lower alkylene, and R⁵ is hydrogen or an amino protective group, and a pharmaceutically acceptable salt thereof, processes for their preparation and pharmaceutical compositions comprising them. The invention also relates to intermediate products of the formula
摘要:
A compound of the formula : wherein R 1 is amino or a protected amino group, R 2 is an organic group, R 3 is hydrogen, lower alkyl, hydroxy(lower)alkyl, protected hydroxy(lower)alkyl, amino(lower)alkyl, protected amino(lower)alkyl or an imino protective group, R 4 is hydrogen, lower alkyl or lower alkylthio, A is lower alkylene which may be substituted with suitable substituent(s) and Z is N or CH, and a pharmaceutically acceptable salt thereof, processes for its preparation and pharmaceutical compositions comprising them or a pharmaceutically acceptable salt thereof in admixture with pharmaceutically acceptable carriers.