Methods of combatting bacterial infections in warm-blooded animal with cephalsporin R-sulfoxide
Granted: February 21, 1978
Patent Number:
4075337
R-sulfoxides of the formulae ##STR1## wherein ##STR2## represents an usual penicillin or cephalosporin amide group and X is selected from the group consisting of hydrogen, hydroxy, an alkanoyloxy and the residue of a nucleophilic agent and their salts and esters are prepared by oxidation of the corresponding penicillins and cephalosporins to convert the sulfur atom in the ring to a sulfoxide group and separating and isolating the penicillin- or cephalosporin R-sulfoxide so formed from…
Novel penicillanic acid
Granted: January 10, 1978
Patent Number:
4067986
Penicillanic acid derivatives of the formula ##STR1## wherein E is selected from the group consisting of hydrogen, a salt forming cation, and an ester forming residue which is known to improve the absorption characteristics of penicillanic compounds after oral administration to humans or animals, and Y is a group of the formula ##STR2## wherein Z.sub.1 and Z.sub.2 are individually selected from the group consisting of lower alkoxy, optionally substituted phenoxy, optionally substituted…
Dihydromocimycin antibiotics
Granted: December 13, 1977
Patent Number:
4062948
A new antibiotic (now called dihydromocimycin) being a yellow, salt-forming weak acid and its non-toxic, pharmaceutically acceptable salts produced by a novel microorganism called Streptomyces ramocissimus, a sample of which is deposited in the collection of "Centraal Bureau voor Schimmel-cultures" at Baarn, The Netherlands, under No. CBS 190.69, or mutants thereof, which antibiotic has antibacterial properties and has been found to be effective against Treponema dysentry, one of the…
18 OR 19 Hydroxy prostaglandins
Granted: October 18, 1977
Patent Number:
4054595
Novel 18 -, 19 - and 20 -hydroxy-prostaglandin derivatives of the formula I ##STR1## wherein the dotted line in the position 8-12 indicates the optional presence of a double bond, the waved lines in position 15 indicate that the hydroxyl group and the group R.sub.4 are either in .alpha.- or .beta.-position and Z represents a -- CH.sub.2 CH.sub.2 -- or a cis -- CH=CH -- group, and wherein R represents one of the groups: ##STR2## (wherein the waved lines indicate that the hydroxyl groups…
Aminoalkylethers; composition and method of use
Granted: September 20, 1977
Patent Number:
4049825
Diphenylmethoxyethylamines of the general formula ##STR1## in which R.sub.1 represents a fluorine, bromine or chlorine atom, R.sub.2 represents a hydrogen or fluorine atom and R.sub.3 represents a hydrogen, fluorine or chlorine atom, with the provisos that R.sub.3 is a hydrogen atom when R.sub.2 is a fluorine atom, R.sub.1 is a fluorine atom when R.sub.3 is a chlorine atom and R.sub.1 is a fluorine or bromine atom when R.sub.2 and R.sub.3 both are hydrogen atoms, and their non-toxic acid…
Process for preparing cephalosporin derivatives
Granted: September 6, 1977
Patent Number:
4046761
Novel azetidine derivatives of the formula ##STR1## wherein R.sub.1 is an acylamido group, R.sub.2 is selected from the group consisting of ##STR2## wherein R.sub.4, R.sub.5 and R.sub.6 are individually selected from the group consisting of hydrogen, lower alkyl and lower alkenyl, n is 2 or 3 and -- in the case when formula IIB is a phenyl -- this group may carry 1 to 4 substituents selected from the group consisting of halogen, lower alkyl, lower alkenyl and phenyl, and R.sub.3 is lower…
Preparation of 7-substituted amino-desacetoxycephalosporanic acid compounds
Granted: July 12, 1977
Patent Number:
4035352
Novel 6-substituted amino-penicillanic acid anhydrides useful in the process for the preparation of 7-substituted amino-desacetoxycephalosporanic derivatives comprising converting a 6-substituted amino-penicillanic acid sulfoxide into an anhydride of a 6-substituted amino-penicillanic acid sulfoxide, heating the said acid anhydride intermediate at a temperature up to at most 160.degree. C in a dry inert organic solvent with an anhydrous acid which is capable of causing ring expansion of…
Process for the preparation of heterocyclic compounds
Granted: May 17, 1977
Patent Number:
4024129
A process for the preparation of acylamido derivatives by reaction of a compound of the formula Z - N = C = O, wherein Z is an optionally substituted alkyl-, aryl- (preferably phenyl or naphthyl) or cycloalkyl or optionally substituted heterocyclic, preferably a penicillanic acid or a cephalosporanic acid nucleus, having carboxyl groups and an optionally present hydroxy group protected, with a carboxylic acid of the formula ##STR1## wherein Z.sup.1 is an optionally substituted…
Azetidine derivatives
Granted: February 8, 1977
Patent Number:
4007202
Novel azetidine derivatives of the formula ##STR1## wherein R.sub.1 is an acylamido group, R.sub.2 is selected from the group consisting of ##STR2## wherein R.sub.4, R.sub.5 and R.sub.6 are individually selected from the group consisting of hydrogen, lower alkyl and lower alkenyl, n is 2 or 3 and -- in the case when formula IIB is a phenyl - this group may carry one to four substituents selected from the group consisting of halogen, lower alkyl, lower alkenyl and phenyl, and R.sub.3 is…
Preparation of 7-substituted amino-desacetoxycephalosporanic acid compounds
Granted: January 18, 1977
Patent Number:
4003894
Process for the preparation of 7-substituted amino-desacetoxycephalosporanic derivatives comprising converting a 6-substituted amino-penicillanic acid sulfoxide into an anhydride of a 6-substituted amino-penicillanic acid sulfoxide, heating the said acid anhydride intermediate at a temperature up to at most 160.degree. C in a dry inert organic solvent with an anhydrous acid which is capable of causing ring expansion of the penam ring to a .DELTA..sup.3 -cephem ring, in the presence of a…
Aminoalkylethers
Granted: January 18, 1977
Patent Number:
4003932
Diphenylmethoxyethylamines of the general formula ##STR1## in which R.sub.1 represents a fluorine, bromine or chlorine atom, R.sub.2 represents a hydrogen or fluorine atom and R.sub.3 represents a hydrogen, fluorine or chlorine atom, with the provisos that R.sub.3 is a hydrogen atom when R.sub.2 is a fluorine atom, R.sub.1 is a fluorine atom when R.sub.3 is a chlorine atom and R.sub.1 is a fluorine or bromine atom when R.sub.2 and R.sub.3 both are hydrogen atoms, and their non-toxic acid…
Alkaline protease produced by a bacillus
Granted: January 11, 1977
Patent Number:
4002572
A novel enzyme having a high proteolytic activity in alkaline media and being suitable for inclusion in washing compositions and which is produced by a novel Bacillus strain designated "PB 92", or its proteolytic enzyme producing mutants or variants. A culture of the Bacillus is deposited with the Laboratory for Microbiology of the Technical University of Delft, The Netherlands, where it has been given number OR-60.
Phenylene di-ethers
Granted: December 21, 1976
Patent Number:
3998874
Substituted phenylene di-ethers of the formula; ##STR1## wherein R represents an isopropyl or tertiary butyl group and X represents hydrogen or lower alkyl, and acid addition salts thereof.The compounds are useful anti-arrhythmic agents and also show local anaesthetic activity in mammals. Their methods of preparation are disclosed and also pharmacological preparations containing the same.
4-Amino-pyrimidine derivatives
Granted: September 14, 1976
Patent Number:
3980650
A process is described for the preparation of pyrimidine derivatives having therapeutic properties. They have the general formula: ##SPC1##Wherein A represents an alkylene or alkenylene grouping which together with the carbon atoms of the pyrimidine nucleus to which it is attached forms a homocyclic ring containing five to seven carbon atoms, which homocyclic ring may carry one or more halogen, lower alkyl and/or lower alkoxy substituents and R represents an amino, lower alkylamino or…
Azetidine derivatives
Granted: June 29, 1976
Patent Number:
3966738
New azetidine derivatives of the formula: ##EQU1## wherein R.sub.1 represents a penicillin- or cephalosporin-amido group, R.sub.2 represents one of the groups of the following formulae: ##EQU2## wherein R.sub.4, R.sub.5 and R.sub.6 are the same or different and each represents a hydrogen atom or a lower alkyl or alkenyl group, n represents 2 or 3 and - in case formula IIB represents a phenyl group - this group may carry one to four further substituents selected from the group consisting…
Acetidine derivatives
Granted: June 8, 1976
Patent Number:
3962277
A new azetidine derivative of the formula: ##EQU1## wherein R.sub.1 represents a penicillin- or cephalosporin-amido group, R.sub.2 represents one of the groups of the following formulae: ##EQU2## wherein R.sub.4, R.sub.5 and R.sub.6 are the same or different and each represents a hydrogen atom or a lower alkyl or alkenyl group, n represents 2 or 3 and - in case formula IIB represents a phenyl group - this group may carry one to four further substituents selected from the group consisting…
Novel acid compounds
Granted: March 23, 1976
Patent Number:
3945994
Novel therapeutically useful and disinfecting penicillanic and cephalosporanic acid derivatives of the formula: ##SPC1##Wherein W represents a penicillanic or cephalosporanic acid residue or derivatives thereof and wherein Y represents a carbonamido group N-substituted by a phosphorous or sulfur containing residue or Y represents a phosphorous or sulfur containing substituent, and pharmaceutical and disinfecting compositions containing them and their use and process for the preparation…
Method for determination of the presence of antibiotics
Granted: March 2, 1976
Patent Number:
3941658
A method for the rapid determination of the presence or absence of residues of antibiotic such as penicillin, in liquids, for example milk, and meat comprising introducing spores of a microorganism which possesses a high sensitivity for the antibiotic to be determined into an agar medium so that the spores are prevented from starting to germ due to lack of nutrients, but stay alive, and being sufficiently heavily inoculated that after addition of nutrients and incubation at or near…
Viscosimeter
Granted: January 6, 1976
Patent Number:
3930402
Viscosimeter comprising a flow system for the liquid to be tested, having a narrow zone, zones for determining the pressure of the liquid to be tested located before and after the narrow zone, said zones for determining the pressure of the liquid to be tested being surrounded by tubes of a thin-walled material adapted to transfer the pressure of the liquid within the tubes to pressure transduction liquids outside each of the tubes, each of said pressure transduction liquids being in…
