Hoechst Aktiengesellschaft

Roussel Uclaf

Dieter Bormann

Wulf Merkel

Roman Muschaweck

Elmar Schrinner

Walter Durckheimer

Rene Heymes

Eberhard Ehlers

Dieter Mania

Bernd Knabe

Manfred Worm

Jean Jolly

Manfred Schorr

Wilfried Schmitt

Merkel Wulf

Gaston Amiard

Walter Duerckheimer

Cephem derivatives of the general formula ##STR1## in which the R.sub.2 O group is in the syn-position, a process for their manufacture and pharmaceutical formulations which are active against bacterial infections and contain these compounds.

Cephem derivatives and processes for their manufacture

Cephem derivatives

What are disclosed are pyrrolidinylsulfamoylbenzoic acid compounds of the formula ##STR1## in which R.sup.1 and R.sup.2 denote C.sub.1 -C.sub.4 alkyl and one of the radicals R.sup.1 or R.sup.2 may be hydrogen, R.sup.3 and R.sup.3' denote hydrogen or C.sub.1 -C.sub.4 alkyl or together denote a C--C linkage, R.sup.4 and R.sup.4' denote hydrogen, halogen, CF.sub.3, alkyl or C.sub.1 -C.sub.2 alkoxy, hydroxy, amino or dimethylamino in the various positions of the aryl nucleus, or together denote 3,4-methylenedioxy, R.sup.5 and R.sup.6 denote hydrogen, C.sub.1 -C.sub.4 alkyl or benzyl, Ar denotes phenyl or a 5-membered or 6-membered heteroaromatic ring containing a O, S or N atom and X is omitted or denotes oxygen, sulfur, NH, or CH.sub.2, and their pharmaceutically acceptable salts with bases or acids. The compounds and salts have a salidiuretic action and can be used for the treatment of edematous diseases.

Substituted pyrrolidinyl-benzoic acid derivatives and a process for

The invention provides thienylbenzoic acid derivatives of the formula I ##STR1## in which R.sup.1 is an alkyl radical having from 1 to 3 carbon atoms, a phenyl, thienyl or furyl radical optionally substituted by halogen, CF.sub.3, CH.sub.3 or OCH.sub.3 ; R.sup.2 is hydrogen, halogen or CH.sub.3 ; R.sup.3 is hydrogen or alkyl having from 1 to 4 carbon atoms or benzyl; and n is 1 or 2; and the pharmaceutically tolerable salts thereof with acids or bases.

Thienylbenzoic acid derivatives

What is disclosed are cephalosporin compounds of the formula ##STR1## pharmaceutical preparations having an action against bacterial infections and containing such cephem compounds, a process for the manufacture of the cephem compounds and of pharmaceutical preparations containing the same, and the use of the cephem compounds to combat bacterial infections.

Cephem derivative

Novel stable crystalline hydrate of D form of the syn isomer of sodium 3-acetoxymethyl-7-[2-(2-amino-4-thiazolyl)-2-methoxyimino-acetamido]-ceph- 3-eme-4-carboxylate having the formula ##STR1## which has excellent antibiotic activity against both gram negative and gram positive bacteria and a process for its preparation.

Sodium

Cephem derivatives of the formula ##STR1## in which R.sup.1 denotes hydrogen or low-molecular alkoxy, R.sup.2 denotes hydrogen, optionally substituted alkyl, phthalide or a cation, X denotes sulfur, oxygen or CH.sub.2 and A denotes hydrogen, alkoxy, halogen or a group --CH.sub.2 Y, in which Y represents hydrogen, acyloxy, alkoxy, optionally substituted carbamoyloxy or a group --SR.sup.3, in which R.sup.3 can represent acyl, alkyl or an optionally substituted 5-membered or 6-membered heterocyclic structure are disclosed as valuable antibiotics which are well suited for combating Gram-positive and in particular Gram-negative infections and also have an unexpectedly good action against penicillinase-forming staphylococci.

7[(2-Amino-thiazol-4-yl)glyoxylamido]-cephem derivatives and processes

Salidiuretically-active 3-pyrrolo-5-sulfamoylbenzoic acids having a methylphenoxy or chlorophenoxy group substituted in the 4-position, and alkyl esters thereof, are disclosed, as are methods of making and using the same.

Process for preparing pyrrolo-benzoic acid derivatives

5-Sulfamoylbenzoic acids substituted in 4-position by various substituents and in 3-position by a cyclic amino group having sali-diuretic properties.

Diuretic and saluretic 5-sulfamoylbenzoic acid derivatives carrying a

A process is disclosed for preparing 5-sulfamoylbenzoic acid derivatives substituted in 4-position by various substituents and in 3-position by a cyclic amino group and having sali-diuretic properties. Novel intermediate compounds are also disclosed.

Derivatives of 5-aminobenzoic acid having a heterocyclic substituent in

A process is disclosed for preparing 5-sulfamoylbenzoic acids substituted in 4-position by various substituents and in 3-position by a cyclic amino group having sali-diuretic properties. Novel intermediate compounds are also disclosed.

5-Sulfamoylbenzoic acid derivatives carrying a heterocyclic substituent

Acylamino-cephem-carboxylic acids of the formula I ##STR1## in which R.sup.1, R.sup.2 and R.sup.3 represent hydrogen or alkyl, R.sup.1 and R.sup.2 or R.sup.2 and R.sup.3 together may form an alkylene radical which may be substituted, X represents a single bond or NH, A represents a phenylene or thienylene radical which may be substituted, Y represents a single bond or oxygen and Z represents a 5- or 6-membered ring which may be substituted and which may be bound to an anellated ring system, and their physiologically tolerated salts and esters, a process for preparing these compounds and preparations containing them.

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Kelkheim, Germany

Dieter Bormann