Abstract: Crystalline cephem acid addition salts of the general formula II ##STR1## pharmaceutical preparations effective against bacterial infections which contain such cephem derivatives, processes for the preparation of the cephem derivatives and the pharmaceutical preparations, and the use of the cephem derivatives for combating bacterial infections.
Type:
Grant
Filed:
August 21, 1992
Date of Patent:
April 25, 1995
Assignee:
Hoechst Aktiengesellschaft
Inventors:
Friedhelm Adam, Walter Durckheimer, Burkhard Mencke, Dieter Isert
Abstract: A compound of the formula: ##STR1## wherein R.sup.1 is an amino group which may be protected, R.sup.3 is a hydrogen atom or an optionally substituted hydrocarbon residue; Z is S, S.fwdarw.O, O or CH.sub.2, R.sup.4 is a hydrogen atom, methoxy group or formamido group, R.sup.13 is a hydrogen atom, methyl group, hydroxyl group or halogen atom and A.sup..sym. is an optionally substituted imidazolium-1-yl group forming a condensed ring at the 2,3- or 3,4-position or a pharmaceutically acceptable salt or ester thereof is novel and has excellent antibacterial activity.
Abstract: New monoquaternary and diquaternary 5-alpha-hydroxy-3,16-diaminoandrostane salts are disclosed with curare-like muscle relaxant activity. The new salts are characterized by a surprisingly rapid onset time.
Type:
Grant
Filed:
June 27, 1986
Date of Patent:
April 25, 1995
Assignee:
Richter Gedeon Vegyeszeti Gyar Rt.
Inventors:
Zoltan Tuba, Judit Horvath, Maria Lovas nee Marsai, Miklos Riesz, deceased, Katalin Biro, Laszle Szporny, Egon Karpati
Abstract: R-(-)-1-(5-Hydroxyhexyl)-3-methyl-7-propylxanthine, a process for its preparation, and pharmaceuticals which contain this compound and which are suitable, in particular, for the prophylaxis and treatment of cerebral vascular disorders.
Type:
Grant
Filed:
December 21, 1990
Date of Patent:
April 18, 1995
Assignee:
Hoechst Aktiengesellschaft
Inventors:
Harald Furrer, Ulrich Gebert, Karl Rudolphi
Abstract: 7.beta.-[(Z)-2-(2-Amino-4-thiazolyl)-2-hydroxyiminoacetamido]-3-(1,2,3-tria zol-4-yl)thiomethylthio-3-cephem-4-carboxylic acid hydrochloride and its crystalline hydrate, have a potent antibiotic activity, low toxicity and are pharmaceutically stable. They are useful as an active ingredient for clinically useful antibiotic formulations. Methods are disclosed for their production.
Abstract: The present invention relates to a compound represented by the structural formula I: ##STR1## its pharmaceutically acceptable salt or ester, or its crystalline, which is a novel optically active compound useful as a curing agent for bacterial infections, a process for production thereof and a use thereof.
Abstract: New compounds are disclosed having the general formulas (1) and (2): ##STR1## Also described is a process for preparing the compounds of formulas (1) and (2). Further described is a process for preparing a cephalosporin derivative having formula (5): ##STR2## by converting the compound of formula (1) to the compound of formula (2) and then converting the compound of formula (2) to the compound of formula (5).
Abstract: The present invention relates to a compound represented by the structural formula: ##STR1## or its pharmaceutically acceptable salt or ester, which is a novel optically active compound useful as a curing agent for bacterial infections, a process for production thereof and a use thereof.
Abstract: Zinc salts of Cephalosporin C are dissolved in a solution of halides of univalent metals at a temperature of 0.degree.-25.degree. C. and the pH is adjusted to 1-2 prior to being ion exchanged with a sodium form cation-exchange resin packed in a column and being eluted with a water miscible solvent. The column can be further eluted with a solution of halides of univalent metals.
Type:
Grant
Filed:
September 27, 1993
Date of Patent:
April 4, 1995
Assignee:
Industrial Technology Research Institute
Abstract: Cephem compounds of the formula: ##STR1## wherein R.sup.1 is amino or a protected amino group,Z is N or CH,R.sup.2 is lower alkyl, mono(or di or tri)halo(lower)alkyl, lower alkenyl, lower alkynyl, phenyl, naphthyl, phenyl(lower)alkyl, carboxy(lower)alkyl or protected carboxy(lower)alkyl, andR is a group of the formula: ##STR2## in which R.sup.3 and R.sup.4 are each lower alkyl,A is lower alkylene, andR.sup.5 is hydroxy or a protected hydroxy group; or pharmaceutically acceptable salts thereof show antimicrobial activities and are useful in the treatment of microbial infections.
Abstract: The present invention provides physical admixtures of a new crystalline dihydrochloride dihydrate salt of the cephalosporin antibiotic, cefepime with a pharmaceutically acceptable non-toxic organic or inorganic base. In particular, this invention provides physical admixtures having a temperature and moisture stable crystalline dihydrochloride dihydrate form of cefepime having a specific X-ray powder diffraction pattern as described herein.
Abstract: The invention relates to a new, economical and simple process for the production of 3-vinylcephalosporin compounds of formula ##STR1## wherein R.sub.1 and R.sub.2 may be the same or different and denote hydrogen or an organic radical.
Type:
Grant
Filed:
May 28, 1993
Date of Patent:
March 28, 1995
Assignee:
Sandoz Ltd.
Inventors:
Gerd Ascher, Johannes Ludescher, Hubert Sturm
Abstract: A simplified method for making the chloromethyl ester of sulbactam in which the tetraalkylammonium sulbactam salt is not dried and isolated prior to alkylation. The method comprises reacting a tetraalkylammonium salt and a sulbactam salt in an aqueous solution to form an aqueous solution of tetraalkylammonium sulbactam. The tetraalkylammonium sulbactam is extracted into bromochloromethane or iodochloromethane, and water is removed from the organic layer to enhance the formation of the chloromethyl ester of sulbactam. The tetraalkylammonium sulbactam is reacted with bromochloromethane or iodochloromethane in the organic layer to form the chloromethyl ester of sulbactam.
Abstract: The invention is directed to the crystalline isopropyl alcohol solvate of loracarbef, and also is directed to a process for the preparation of the crystalline monohydrate form of the compound of formula (I) ##STR1## which includes exposing the crystalline isopropyl solvate form of the compound of formula (I) to a temperature of between about 50.degree. and 90.degree. C. and a relative humidity of between about 60 to about 100%.
Abstract: The invention relates to a process for recovering caffeine from caffeine-loaded activated carbon and which is characterized in that the caffeine destroying activity of the activated carbon is reduced before or after loading with caffeine. The activated carbon can to that end be treated with acids, buffers, complexing agents, redox substances, caffeine and other xanthine derivatives. The caffeine recovery yield can be considerably increased by this means.
Type:
Grant
Filed:
July 15, 1993
Date of Patent:
March 21, 1995
Assignee:
Jacobs Suchard AG
Inventors:
Stefan Sipos, Gabriel von Lengyel-Konopi
Abstract: There is provided a process for preparing a compound of formula (I) ##STR1## wherein R is H or a hydroxy protecting group, R.sub.2 is an organic residue and R.sub.3 is H or a nitrogen protecting group, which process comprises reacting together a compound of formula (II) ##STR2## wherein R.sub.1 is a C.sub.1 -C.sub.4 alkyl or a phenyl group, R and R.sub.3 are as defined above, a compound of formula (III) ##STR3## wherein R.sub.2 is as defined above and X is a cation or a silicon-containing residue, and a salt of a group IIa, IIb or transition element. The compounds of formula (I) are intermediates in the synthesis of penem antibiotics.
Type:
Grant
Filed:
April 30, 1993
Date of Patent:
March 21, 1995
Assignee:
Farmitalia Carlo Erba S.r.l.
Inventors:
Walter Cabri, Ilaria Candiani, Franco Zarini, Angelo Bedeschi
Abstract: A compound selected from the group consisting of a syn isomer of a compound of the formula ##STR1## in the R or S form or in the form of an R, S mixture wherein R.sub.1, Rc, Rb, A and A' are defined as in the following specification and their non-toxic, pharmaceutically acceptable acid addition salts having anti-bacterial activity.
Type:
Grant
Filed:
December 7, 1992
Date of Patent:
March 14, 1995
Assignee:
Roussel-Uclaf
Inventors:
Jozsef Aszodi, Jean-Francois Chantot, Solange G. D'Ambrieres
Abstract: A method for preparing 2-amino-.beta.-lactams which are substituted by readily-removed protecting groups is provided. According to this invention, an acyl-2-amino-.beta.-lactam is further acylated with a different acyl group and is subsequently treated with base to provide a protected 2-amino .beta.-lactam with a more desirable protecting group.
Type:
Grant
Filed:
February 24, 1993
Date of Patent:
February 28, 1995
Assignee:
Eli Lilly and Company
Inventors:
Larry C. Blaszczak, John E. Munroe, Douglas O. Spry
Abstract: The present invention relates to a new crystalline dihydrochloride dihydrate salt of the cephalosporin antibiotic, cefepime. In particular, this invention provides a temperature and moisture stable crystalline dihydrochloride dihydrate form of cefepime having enhanced stability and a specific x-ray powder diffraction pattern as described herein.
Type:
Grant
Filed:
May 28, 1993
Date of Patent:
February 21, 1995
Assignee:
Bristol-Myers Squibb Company
Inventors:
Elizabeth A. Garofalo, Gary M. F. Lim, Murray A. Kaplan
Abstract: Cephemcarboxylic acid esters of the general formula ##STR1## pharmaceutical preparations which are active against bacterial infections, which contain such cephem derivatives, a process for the preparation of the cephem derivatives and the pharmaceutical preparations, and also the use of the cephem derivatives for combating bacterial infections.
Type:
Grant
Filed:
November 19, 1992
Date of Patent:
February 21, 1995
Assignee:
Hoechst Aktiengesellschaft
Inventors:
Friedhelm Adam, Jurgen Blumbach, Walter Durckheimer, Gerd Fischer, Burghard Mencke, Dieter Isert, Gerhard Seibert