Abstract: The invention relates to novel 7-acylamino-3-vinylcephalosporanic acid derivatives of antimicrobial activity, and to methods of preparation thereof from novel intermediate compounds of the formula: ##STR1## in which R.sub.C is amino or a group of the formula: ##STR2## wherein R.sup.8 is aryl,A.sup.12 is lower alkylene having a group of the formula: .dbd.N.about.OR.sup.4, wherein R.sup.4 is hydrogen, cyclo(lower) alkenyl, lower alkynyl, lower alkenyl, lower alkenyl substituted by carboxy or a protected carboxy group, lower alkyl, or lower alkyl substituted by one or more substituent(s) selected from carboxy, a protected carboxy group, amino, a protected amino group, cyano, phosphono, a protected phosphono group and a heterocyclic group which may have suitable substituent(s),R.sup.a is a protected amino group,R.sup.b is a protected carboxy group,R.sup.c and R.sup.d are combined to form oxo or a protected oxo group, and X.sup.1 is halogen, andR.sup.
Abstract: A compound of the formula: ##STR1## wherein R.sup.1 represents hydrogen or an alkyl group, X represents oxygen or sulfur or a group of formula --NR.sup.2 (where R.sup.2 is hydrogen or an alkyl group and in the case of alkyl, it may form a ring jointed with R.sup.1), and Y represents acetoxy group or a group of formula --SR.sup.3 (where R.sup.3 is a nitrogen-containing heterocyclic group), or a pharmaceutically acceptable salt thereof, is found to have a broad antimicrobial spectrum and, in particular, effective against gram-negative bacteria including Escherichia coli, Klebsiella pneumoniae, Proteus vulgaris, Proteus morganii, as well as gram positive ones. Thus, these compounds may be used for antimicrobial agents in therapeutical purposes.
Abstract: An improvement in the production of methotrexate as set out in Ellard U.S. Pat. No. 4,080,325. It has been found that magnesium oxide facilitates the coupling reaction by acting as an acid acceptor. The dense grade of magnesium oxide is preferred in molar proportions of 2 to 4 moles of magnesium oxide per mole of 2,4-diamino-6-hydroxymethylpteridine. Further, the triphenylphosphine oxide which is generated by hydrolysis of the protecting groups is removed from the reaction stream by utilization of toluene or BTX-type solvents.
Type:
Grant
Filed:
December 11, 1981
Date of Patent:
December 20, 1983
Assignee:
The United States of America as represented by the Secretary of the Department of Health and Human Services
Abstract: Novel syn isomers of oximes of 3-azidomethyl-7-amino-thiazolyl-cephalosporanic acids of the formula ##STR1## wherein R is selected from the group consisting of hydrogen, alkyl of 1 to 4 carbon atoms, unsaturated alkyl of 2 to 4 carbon atoms, benzoyl and --(CH.sub.2).sub.n --R.sub.1, n is an integer from 1 to 4, R.sub.1 is selected from the group consisting of NH.sub.2 and --COOA' and A' and A are selected from the group consisting of hydrogen, alkali metal, alkaline earth metal, magnesium, --NH.sub.4, an easily cleavable ester group and a non-toxic, pharmaceutically acceptable organic amine and their non-toxic, pharmaceutically acceptable acid addition salts having antibiotic activity and a novel process and novel intermediates for their preparation.
Abstract: Novel tricyclic imidyl derivatives, for example those of the formula ##STR1## [n=1 or 2, Y=a bridge member and X=a functional group] are described. The novel tricyclic imidyl derivatives are suitable for the preparation of photocrosslinkable polymers by incorporation into existing polymer chains or by building up the polymer chain from tricyclic imidyl derivatives, according to the definition, with suitable functional groups X by polymerization or polycondensation. The photocrosslinkable polymers obtained by this means can be used, for example, to produce printing plates for the offset printing process and especially as photoresists.
Type:
Grant
Filed:
February 16, 1982
Date of Patent:
November 29, 1983
Assignee:
Ciba-Geigy Corporation
Inventors:
Hans Zweifel, Walter Schilling, Angelo Storni, Daniel Bellus
Abstract: Novel tricyclic imidyl derivatives, for example those of the formula ##STR1## [n=1 or 2, Y=a bridge member and X=a functional group] are described. The novel tricyclic imidyl derivatives are suitable for the preparation of photocrosslinkable polymers by incorporation into existing polymer chains or by building up the polymer chain from tricyclic imidyl derivatives, according to the definition, with suitable functional groups X by polymerization or polycondensation. The photocrosslinkable polymers obtained by this means can be used, for example, to produce printing plates for the offset printing process and especially as photoresists.
Type:
Grant
Filed:
February 16, 1982
Date of Patent:
November 22, 1983
Assignee:
Ciba-Geigy Corporation
Inventors:
Hans Zweifel, Walter Schilling, Angelo Storni, Daniel Bellus
Abstract: New cephalosporins of the general formula: ##STR1## in which R is alkyl, L-2-amino-2-carboxyethyl, phenyl or various heterocyclic rings, R' is a hydrogen atom or a radical of the general formula: ##STR2## and R.degree. is hydrogen, alkyl, vinyl, cyanomethyl or a carboxyalkyl radical of the general formula: ##STR3## and also their salts, their preparation and the pharmaceutical compositions in which they are present.
Type:
Grant
Filed:
November 19, 1981
Date of Patent:
November 15, 1983
Assignee:
Rhone-Poulenc Industries
Inventors:
Daniel Farge, Pierre L. Roy, Claude Moutonnier, Jean-Francois Peyronel
Abstract: The invention provides new cephalosporins of the general formula: ##STR1## in which n=0 or 1, R.sub.4 is an amine-protecting radical, R.sup.a.sub.5 and R.sup.b.sub.5, which are identical or different, are hydrogen atoms or alkyl radicals, or form an alkylene radical of 2 or 3 carbon atoms, R.sup.c.sub.5 is a hydrogen atom or an acid-protecting radical and R.sub.2 is an acid-protecting radical or a radical which can easily be removed by an enzymatic method. The compounds of formula (I) are in the form of a 3-oxoethyl-bicyclooct-2-ene or -bicyclooct-3-ene or a 3-oxoethylidenebicyclooctane if n=0, and in the form of a 3-oxoethylbicyclooct-2-ene or a 3-oxoethylidenebicyclooctane if n=1. They are useful as intermediates for the preparation of pharmaceutically active cephalosporins.
Type:
Grant
Filed:
November 19, 1981
Date of Patent:
November 15, 1983
Assignee:
Rhone-Poulenc Industries
Inventors:
Daniel Farge, Pierre L. Roy, Claude Moutonnier, Jean-Francois Peyronel
Abstract: Heterocyclic carbamates are disclosed which have potent gastric secretion inhibitory properties. The heterocyclic substituent is a pyridyl group or a 6-membered heterocycle with two nitrogen heteroatoms, which may be optionally substituted. Further substituents on the carbamate nitrogen and oxygen atoms are also disclosed. The compounds have profound effects on the inhibition of gastric secretions in the gastro-intestinal tract, and compositions for such uses are also disclosed.
Abstract: Cephapirin acetylcysteinate having antibacterial activity. Said salt is obtained by reacting an aqueous solution of cephapirin with an aqueous solution of acetylcysteine. To isolate the salt, the aqueous solution is submitted to lyophilization.
Abstract: There are disclosed tetrahydrofuran compounds and analogs thereof of the formula: ##STR1## and pharmaceutically acceptable acid addition salts thereof, wherein X is oxygen or sulfur, R.sup.1 and R.sup.2 are each hydrogen, halogen, lower alkyl or lower alkoxy, and Am is a group of the formula: ##STR2## wherein Z is oxygen or sulfur, R.sup.3 is hydrogen or halogen, R.sup.4 is hydrogen, lower alkyl or phenyl which may be substituted by 1 to 3 substituents at any position(s) on the phenyl nucleus, each substituent being independently selected from halogen, lower alkyl and lower alkoxy, and R.sup.5 is hydrogen or lower alkyl. Such compounds are useful as neuroleptics.
Abstract: Novel tricyclic imidyl derivatives, for example those of the formula ##STR1## [n=1 or 2, Y=a bridge member and X=a functional group] are described. The novel tricyclic imidyl derivatives are suitable for the preparation of photocrosslinkable polymers by incorporation into existing polymer chains or by building up the polymer chain from tricyclic imidyl derivatives, according to the definition, with suitable functional groups X by polymerization or polycondensation. The photocrosslinkable polymers obtained by this means can be used, for example, to produce printing plates for the offset printing process and especially as pohtoresists.
Type:
Grant
Filed:
February 16, 1982
Date of Patent:
November 8, 1983
Assignee:
Ciba-Geigy Corporation
Inventors:
Hans Zweifel, Walter Schilling, Angelo Storni, Daniel Bellus
Abstract: A 3,7-disubstituted-3-cephem-4-carboxylic acid of the general formula: ##STR1## having antibacterial activity, processes for preparing same, and pharmaceutical compositions thereof for treating infectious diseases in humans and animals.
Abstract: There is presented compounds of the formula ##STR1## wherein X represents the 1,2,5,6-tetrahydro-2-methyl- 5,6-dioxo-as-triazin-3-yl group or its corresponding tautomeric form, the 2,5-dihydro-6-hydroxy-2-methyl-5-oxo-as-triazin-3-yl group, and the readily hydrolyzable esters, readily hydrolyzable ethers and salts of the compounds and hydrates of the compounds of formula I or of their esters, ethers and salts. Also provided is a method of their manufacture and intermediates therefor as well as corresponding pharmaceutical preparations.
Abstract: Novel 1-substituted pyrimidinediones and thiopyrimidineones, synthesis thereof and intermediates therefor, useful as control agents for pests.
Type:
Grant
Filed:
May 27, 1982
Date of Patent:
October 25, 1983
Assignee:
Zoecon Corporation
Inventors:
George R. Lindahl, III, Clive A. Henrick
Abstract: Fused [1,2,4]oxadiazolylidenebenzenesulfonamides such as 2-chloro-N-(5,7-dimethyl-2H-[1,2,4]oxadiazolo-[2,3-a]pyrimidin-2-ylidene)b enzenesulfonamide and 2-chloro-N-(7-methoxy-5-methyl-2H-[1,2,4]oxadiazolo-[2,3-a][1,3,5]triazin- 2-ylidene)benzenesulfonamide are general and selective pre- or post-emergence herbicides and can be useful in regulating plant growth.
Abstract: The invention relates to the novel crystalline hydrochloride and the crystalline hydrobromide of 7.beta.-[2-(2-amino-4-thiazolyl)-2-methoxyiminoacetamido]-3-cephem-4-carbo xylic acid pivaloyloxymethyl ester, a process for the production thereof, and pharmaceutical preparations that contain these compounds.
Abstract: Novel penicillins and cephalosporins and non-toxic salts thereof, which contain a mono- or di-oxo- or thioxo-piperazino(thio)carbonylamino group in molecule. These compounds are valuable antibacterial compounds for use in mammals including man. This disclosure relates to such compounds and a process for the preparation thereof.
Abstract: The invention relates to new cephem compounds, of high antimicrobial activity of the formula: ##STR1## wherein R.sup.1 is amino or protected amino,R.sup.2 is carboxy(lower)alkyl or protected carboxy(lower)alkyl,R.sup.3 is halogen or lower alkoxy, andR.sup.4 is carboxy or protected carboxy,and a pharmaceutically acceptable salt thereof.