Abstract: A process for etherifying the hydroxymethyl group in position 3 of a cephalosporin by reaction of a 3-hydroxymethyl cephalosporin with an dioxycarbenium-tetrafluoroborate.
Abstract: A cephalosporin intermediate of the formula ##STR1## where R.sub.3 is carboxyl, carboxylate, or a carboxylic acid ester group and,R.sub.8 and R.sub.9 are each independently hydrogen, halogen,(C.sub.1-4) alkyl, hydroxy, carboxamido,(C.sub.1-4) alkoxycarbonyl, amino,mono- (C.sub.1-4) alkylamino, di- (C.sub.1-4) alkylamino, ortogether are a 5 or 6-membered carbocyclic ring or an alkali metal, alkaline earth metal, or acid addition salt thereof. Valuable cephalosporin antibiotics can be produced from the cephalosporin intermediate products of formula I.
Type:
Grant
Filed:
June 6, 1995
Date of Patent:
December 17, 1996
Assignee:
Biochemie Gesellschaft m.b.h.
Inventors:
Gerd Ascher, Hubert Sturm, Heinrich Thaler, Werner Veit
Abstract: Complexes and pharmaceutical preparations containing complexes of the pleuromutilin derivative of formula I ##STR1## in free base or in acid addition or quaternary salt form and cyclodextrin are described.They can be prepared by complexing the above pleuromutilin compound with an appropriate cyclodextrin.They are indicated for use as pharmaceuticals, e.g. as antibiotics, especially in veterinary medicine, e.g. as feed additives.
Abstract: The invention relates to a new process for the production of the disodium salt hemiheptahydrate of ceftriaxone by reacting 7-amino-3-{[(2,5-dihydro-6-hydroxy-2-methyl-5-oxo-1,2,4-triazin-3-yl)thio] methyl}-3-cephem-4-carboxylic acid with 2-(2-aminothiazol-4-yl)-2-syn-methoximinoacetic acid-(2-benzthiazolyl)thiolester in the presence of a base, characterized in that the reaction and the crystallization of the disodium salt hemiheptahydrate of ceftriaxone are carried out in aqueous acetone.
Type:
Grant
Filed:
February 19, 1993
Date of Patent:
November 12, 1996
Assignee:
BIOCHEMIE Gesellschaft m.b.H.
Inventors:
Johann Danklmaier, Ingolf Macher, Bernhard Prager
Abstract: A compound of formula (I), in which each of R.sub.1 and R.sub.2 is independently hydrogen, alkyi or, together with the carbon atom to which it is bonded, a cycloalkyl; and each of R.sub.3 and R.sub.4 is independently hydrogen, alkyl or substituted alkyl. The compounds are useful intermediates and prodrugs.
Abstract: Compound of formula IVe ##STR1## where Het is 2-pyridyl or 2-benzothiazolyl, are useful as acylating agents in preparing 7-[2-(2-amino-4-thiazol)-2-oxoacetyl]-cephalosporin intermediates.
Type:
Grant
Filed:
April 30, 1993
Date of Patent:
January 16, 1996
Assignee:
Biochemie Gesellschaft m.b.H.
Inventors:
Hubert Sturm, Heinrich Thaler, Werner Veit
Abstract: Compounds of formula I ##STR1## wherein R.sub.1 and R.sub.2 are the same or different and each represent hydrogen, alkyl, alkenyl, cycloalkyl, aryl or aralkyl are produced by a new environmentally acceptable process.
Abstract: Compounds of formula I ##STR1## wherein R.sub.1 and R.sub.2 are the same or different and each represent hydrogen, alkyl, alkenyl, cycloalkyl, aryl or aralkyl are produced by a new environmentally acceptable process.
Abstract: The invention provides crystallilne (6R, 7R)-7-[[2 ( 2-Amino-4-thiazolyl)-(Z)-2-(1-diphenylmethoxycarbonyl-1-methylethoxy)imino ]acetamido]-3-(1--pyridiniummethyl)-3-cephem-4-carboxylate and a process for its production.
Abstract: The invention provides crystalline (6R, 7R)-7-[[2-(2-Amino-4-thiazolyl)-(Z)-2-(1-diphenylmethoxycarbonyl-1-methyle thoxy)imino ]acetamido]-3-(1-pyridiniummethyl)-3-cephem-4-carboxylate and a process for its production.
Abstract: De-acylation of Penicillins and Cephalosporins to obtain the corresponding 6-aminopenicillanic acid or 7-aminocephalosporanic acid by the imino halide/imino ether process using long chain bases.
Type:
Grant
Filed:
August 3, 1983
Date of Patent:
December 31, 1985
Assignee:
Biochemie Gesellschaft m.b.H.
Inventors:
Bernhard C. Prager, Peter Punk, Heinrich Thaler
Abstract: The invention provides a method of facilitating vegetation with the aid of a fungal mycelium biomass in admixture with a polybutadiene and application forms comprising such components.
Abstract: A pleuromutilin derivative which is 14-desoxy-14-thiocyanatoacetoxy-mutilin is useful as an animal feed additive to increase meat production and also finds application in veterinary medicine as an antibiotic.
Abstract: The present invention concerns novel pleuromutilin derivatives of the formula: ##SPC1##Wherein X, Y and Z are as defined in any one of the following groups:I. X is --CO--CH.sub.2 --R.sub.1 wherein R.sub.1 is hydrogen, chlorine, bromine, iodine, thiocyanato, azido, dithiocarbonic acid-O-alkyl(C.sub.1 to C.sub.5), (N,N-tetramethylene-thiocarbamoyl)-mercapto, --S-phenyl, --S-phenyl substituted by carboxyl or by one or two hydroxyl radicals, --S--pyridyl, --S--alkyl(C.sub.1 to C.sub.5), or --S--alkyl(C.sub.1 to C.sub.5) substituted by one or more amino hydroxyl or carboxyl radicals, Y is vinyl, and Z is hydrogen,Ii. X is --CO--CO--OH, Y is vinyl, and Z is hydrogen,Iii. X is --CO--CH.sub.3, Y is vinyl, and Z and hydrogen,Iv. X is --CO--CH.sub.2 --NH.sub.2, Y is ethyl, and Z is hydrogen,V. X is ##EQU1## Y is ethyl, and Z is hydrogen, VI. X is hydrogen, Y is vinyl, and Z is acetyl, orVii. X is --COR.sub.2, wherein R.sub.2 is alkyl of 1 to 5 carbon atoms, Y is vinyl, and Z is hydrogen.