Abstract: Novel alkyloximes of 7-amino-thiazolyl-acetamidocephalosporanic acids of the formula ##STR1## wherein R is selected from the group consisting of alkyl of 1 to 5 carbon atoms, cycloalkyl of 3 to 5 carbon atoms and --CH.sub.2 --SR', R' is selected from the group consisting of acyl of an alkanoic acid of 2 to 4 carbon atoms, 1-methyl-tetrazolyl and 2-methyl-1,3,4-thiadiazolyl, R.sub.1 is selected from the group consisting of hydrogen and a group easily removeable by acid hydrolysis or hydrogenolysis, R.sub.2 is selected from the group consisting of alkyl of 1 to 4 carbon atoms and alkenyl and alkynyl of 2 to 4 carbon atoms, A is selected from the group consisting of hydrogen, an alkali metal cation, an equivalent of an alkaline earth metal or magnesium, an organic amine base cation and an ester group easily removeable by acid hydrolysis or hydrogenolysis with the proviso that when R.sub.1 is hydrogen, A is not an ester group easily removeable by hydrogenolysis or acid hydrolysis and the wavy line means that OR.
Abstract: Novel 7.alpha.-methoxy-cephalosporins and non-toxic salts thereof, which contain a di-oxo-piperazinyl-carbonylamino group in molecule. These compounds are valuable antibacterial compounds for use in mammals including man. This disclosure relates to such compounds and methods for producing the same.
Abstract: Lactone electron donative color-forming agents of quinoline-carboxylic acid are disclosed having the general formulae (I) and (II) ##STR1## wherein A and B represent a variety of chemical moieties, X represents halo- or nitro- and n.sup.1 is an integer of 0-4. The color-forming agents are useful in recording materials of the pressure-sensitive and heat-sensitive varieties, and the like.
Abstract: Cephalosporin compounds of the formula ##STR1## wherein R and R.sub.2 are hydrogen or protecting groups, R.sub.1 is hydrogen or methoxy, R.sub.3 is hydrogen or C.sub.1 -C.sub.4 alkyl and R.sub.4 is C.sub.1 -C.sub.4 alkyl, are broad spectrum antibiotics or intermediates thereto.
Abstract: A process for the preparation of alkaloids of the leurosine type having the formula I ##STR1## and the acid addition salts thereof. In the formula I R is hydrogen or methyl. The compounds prepared according to the invention are known compounds showing cytostatic activity.
May 19, 1978
Date of Patent:
April 22, 1980
Richter Gedeon Vegyeszeti Gyar Rt.
Csaba Szantay, Lajos Szabo, Katalin Honty, Katalin Nogradi, Karola Jovanovics, Eszter Dezseri, Lajos Dancsi, Csaba Lorincz, Bela Szarvady, Lajos Kovacs
Abstract: 7-[2-(2-aminothiazol-4-yl)-2-(syn)-methoxyiminoacetamido]cephalosporanic acid derivatives of the formula; ##STR1## wherein R.sup.1 NH is an amino group which may optionally be protected; COOR.sup.2 is a carboxyl group which may optionally be esterified; X is oxygen, sulfur or an imino group which may optionally be substituted; B is hydrogen or a hydroxyl, amino, thiol or hydrocarbon group which may optionally be substituted, or a salt thereof, are novel, .beta.-lactamase-resistant and low-toxicity compounds which display excellent activity against a broad spectrum of microorganisms including Gram-negative bacteria such as Escherichia coli, Serratia marcescens, Proteus rettgeri, Enterobacter cloacae, Citrobacter freundii. Thus, these compounds can be used for antibacterial agents in therapeutical purpose.
Abstract: 2-Hydroxyiminoacetamide compounds of the following formula and salts thereof: ##STR1## [wherein X is S, O or an imino group which may optionally be substituted; B is a hydrogen atom or a hydroxyl, amino, mercapto or hydrocarbon residue group which may optionally be substituted; and COOR is a carboxyl group which may optionally be esterified] and pharmaceutically acceptable salts thereof are novel and useful as antibacterial agents.
Abstract: New cephalosporin compounds of the formula: ##STR1## wherein R.sub.1 is hydrogen or hydroxy, R.sub.2 is a substituted alkanoyl group, R.sub.3 is hydrogen, carbamoyloxy, alkanoyloxy or a heterocyclic-thio group which may have suitable substituents, and R.sub.4 is carboxy or protected carboxy.
Abstract: A group of novel polynuclear heterocyclic compounds having a diazaphenalene skeleton. These compounds assume orange to reddish violet colors according to the types of substituents on the diazaphenalene skeleton, and have excellent thermal stability and weatherability and good dispersibility in polymeric materials. They are useful as orange to reddish violet pigments, especially for coloring polymeric materials.
Abstract: The present invention relates to new syn-isomer of 3,7-disubstituted-3-cephem-4-carboxylic acid compounds and pharmaceutically acceptable salts thereof. More particularly, it relates to new syn-isomer of 3,7-disubstituted-3-cephem-4-carboxylic acid compounds and pharmaceutically acceptable salts thereof which have antibacterial activities and to processes for the preparation thereof, to pharmaceutical composition comprising the same, and to a method of using the same therapeutically in the treatment of infectious diseases in human beings and animals.
Abstract: Novel .beta.-lactam antibiotics are compounds of the formula: ##STR1## wherein R is alkyl of up to 6 carbon atoms or, when A is oxygen, R is hydrogen; A is oxygen or --OCO--; Z is ##STR2## R.sup.1 is hydrogen, acetoxy or S-Het; Het is 1,2,3-triazol-5-yl, 1-methyltetrazol-5-yl, 1,3,4-thiadiazol-2-yl or 2-methyl-1,3,4-thiadiazol-5-yl; and n is an integer from 0 to 8; or a readily-cleavable ester or physiologically-acceptable salt thereof.
June 13, 1977
Date of Patent:
July 24, 1979
Merck Patent Gesellschaft mit beschrankter Haftung
Rudolf Gottschlich, Rolf Gericke, Horst Juraszyk, Jurgen Seubert, Wighard Strehlow, Helmut Wahlig, Rolf Bergmann, Elvira Dingeldein
Abstract: 3,4-Dihydro-4-oxo-quinazoline derivatives substituted in the 2-position by a substituted phenyl group are disclosed. The derivatives possess anti-allergy properties and can be used for the treatment of allergic conditions.
December 2, 1977
Date of Patent:
June 26, 1979
Carlo Erba S.p.A.
Gianfederico Doria, Ciriaco Romeo, Piernicola Giraldi, Francesco Lauria, Maria L. Corno, Piero Sberze, Marcello Tibolla