摘要:
A compound of formula (I) wherein R and R2 together with the nitrogen atom to which they are attached form pyrrolidinyl or piperidinyl, R1 is a group of formula (II) R3 and R'3 are hydrogen, deuterium or halogen, R4, R5 and R10 are independently of each other hydrogen or alkyl, R6, R7 and R8 are hydrogen or deuterium; R9 is amino, alkyl, aryl, heterocyclyl or mercapto; and, if X is oxygen, R9 is additionally hydrogen; R'10 is alkyl, X is sulphur, oxygen, NR10, or N+(R'10)2; Y is sulphur or oxygen, and m is 0, 1 or 2; with the proviso that, when R and R2 together with the nitrogen atom to which they are attached form piperidinyl, m is O, Y is S and Y is attached in position 3 of said piperidine ring, that group of formula (I) which is attached to the piperidine ring via the residue Y is either in the (S)-configuration or in the (R)-configuration, preferably in the (S) -configuration which is e.g. useful as antimicrobial, antibacterial.
摘要:
Crystalline 2-(aminothiazol-4-yl)-2-(tert.butoxycarbonylmethoxyimino)acetic acid-S-mercapto-benzo-thiazolylester in form of an N,N-dimethylacetamide solvate; a crystalline salt of a 7-[2-(aminothiazol-4-yl)-2-(carboxymethoxyimino)acetamido]-3-vinyl-3-cephem-4-carboxylic acid with an amine of formula N(R1)(R2)(R3), wherein R1, R2, and R3 have various meanings, a crystalline sulphuric acid addition salt of a 7-[2-(2-aminothiazol-4-yl)-2-carboxymethoxyimino)acetamido]-3-vinyl-3-cephem-4-carboxylic acid; and the use of these salts in the production of cefixime, e.g. in form of a trihydrate.
摘要:
A composition comprising itraconazole and an organic acid and the use of such composition in the production of pharmaceutical compositions comprising itryconazole as an active ingredient.
摘要:
Auxiliary-free agglomerates of a β-lactam antibiotic; a mixture of agglomerates of an active β-lactam antibiotic and a second pharmaceutically active agent, with or without auxiliaries; a tablet comprising compressed agglomerates of a β-lactam antibiotic optionally in mixture with pharmaceutically acceptable auxiliaries; and a tablet comprising compressed agglomerates of a β-lactam antibiotic in mixture with a second pharmaceutically active agent and with or without pharmaceutically acceptable auxiliaries.
摘要:
A compound of formula wherein Ac, R 1 and R 2 have various meanings, a process for a preparation thereof and its use as a pharmaceutical, i.e. as antibacterial agent
摘要:
The invention relates to a new process for the production of pharmaceutically active cephalosporines by depletion of 7-amino-3-[(E)-1-propen-1-yl]-3- cephem-4-carboxylic acid in mixtures of 7-amino-3-[(Z)-1-propen-1-yl]-3- cephem-4-carboxylic acid and 7-amino-3-[(E)-1-propen-1-yl]-3-cephem-4-carboxylic acid, by means of a metal or amine salt of 7-amino-3-[(Z/E)-1-propen-1-yl]-3-cephem-4-carboxylic acid.
摘要:
A process for the purification of cefixime via a novel tert.octylamine salt of a cefixime intermediate which may be crystalline and which may be produced in a one pot reaction from 7-amino-3-vinyl-ceph-3-em-4-carboxylic acid.