Boehringer Mannheim Gmbh

Hoffmann-la Roche Inc.

Roche Diagnostics Gmbh

Herbert Leinert

Christos Tsaklakidis

Alfred Mertens

Harald Zilch

Frank Grams

Wolfgang Kampe

Ernesto Menta

Wolfgang Von Der Saal

Hans-Willi Krell

Klaus Strein

Gerd Zimmermann

Bernd Muller-Beckmann

Gisbert Sponer

Wolfgang Bartsch

Karlheinz Stegmeier

Dieter Herrmann

Jens-Peter Holck

Peter Freund

Erwin Bohm

Ralf Kucznierz

Walter-Gunar Friebe

Joachim Dickhaut

Kurt Stach

Karl Dietmann

Hans Seidel

Bernhard Konig

Ulrike Leser

Rainer Haag

Alfred Popelak

Reinhard Heck

Christiane Kehr

Dagmar Geppert

Richard Neidlein

Barbituric acid derivatives

3-aryl-succinamido-hydroxamic acids, methods for producing said acids and medicaments containing the same

Pyrimidine-2,4,6-trione derivatives, processes for their production and pharmaceutical agents containing these compounds

The invention provides novel azulene derivatives of general formula I ##STR1## wherein R.sub.1 to R.sub.6 have the significance given in the description, as well as their tautomers, enantiomers, diastereomers, racemates and physiologically compatible salts or esters and substances which are hydrolyzed or metabolized in vivo to compounds of formula I. The invention is also concerned with a process and intermediates for the manufacture of the above compounds, pharmaceutical compositions which contain such compounds as well as the use of these compounds in the treatment of inflammatory conditions.

Azulene derivatives

Phosphonates, process for preparing the same and medicaments

Phosphanoxides--preparation and use

4-aminopyridazines, method of preparing them and drugs containing these

Compounds of the formula I ##STR1## in which R.sub.1 and R.sub.2 represent a possibly substituted C.sub.8 -C.sub.15 -alkyl chain, n the number 0, 1 or 2 and A the residue of a nucleoside, processes for their preparation, as well as antiviral medicaments which contain these compounds.

Phospholipid derivatives of nucleosides and their use as anti-viral

Liponucleotides containing an ether linkage in the 2-position and a thioether, sulfoxide, or sulfone linkage in the 3-position. The nucleoside component of said liponucleotide is AZT or 3'-deoxy-3'-fluorothymidine. These compounds exhibit antiviral activity.

Phospholipid derivatives of nucleosides

Tricyclic thiazole and oxazole derivatives and pharmaceutical agents

Use of thiazoloisoindolinone derivatives as antiviral medicaments

A process for the preparation of S- or R-carbazole derivatives of the general formula: ##STR1## in which R is an unsubstituted or substituted amino radical and pharmacologically acceptable salts, by either reacting R-(-)-epichlorohydrin (for the S-carbozole derivative); or reacting an S-epoxide derivative of the general formula: ##STR2## in which R.sub.1 is the residue of a substituted sulphonic acid derivative (for the R-carbazole derivative); with 4-hydroxycarbazole and then with ammonia or a substituted amine of the general formula RH, and recovering the compound or converting it to a pharmacologically acceptable salt. The new R-(+)- and S(-)-carbazole derivatives provided by the inventive process have unexpected beta blocking and vasodilatory properties and are useful in pharmaceutical compositions. R-(+)-carbazole derivatives are also useful for the treatment of glaucoma.

Process for the preparation of optically-active carbazole derivatives,

The present invention provides compounds of the general formula ##STR1## wherein R.sub.1 is a hydrogen atom, a straight-chained or branched C.sub.1 -C.sub.12 -alkyl radical, a C.sub.3 -C.sub.7 -cycloalkyl radical, a straight-chained or branched C.sub.2 -C.sub.12 -alkenyl radical or an unsubstituted or substituted C.sub.3 -C.sub.7 -mono- or bicycloalkenyl radical, an unsubstituted or singly or multiple substituted monocyclic aromatic or heteroaromatic radical, R.sub.2 and R.sub.3, which can be the same or different, are straight-chained, branched, saturated or unsaturated C.sub.1 -C.sub.6 -aliphatic radicals or, together with the nitrogen atom to which they are attached, form a saturated or unsaturated ring which can contain further heteroatoms and can optionally be substituted by a lower alkyl radical, a lower alkoxy radical or an oxygen atom, R.sub.4 is an unsubstituted or singly or multiple substituted monocyclic aromatic radical, an unsubstituted or substituted five- or six-membered heteroaromatic ring, R.sub.5 is a hydrogen atom, a cyano radical, a --CO--OR.sub.7 radical, an unsubstituted or a singly or multiple substituted monocyclic aromatic radical or an unsubstituted or substituted five- or six-membered ring, R.sub.6 is a hydrogen atom, a cyano group or a --CO--OR.sub.7, ##STR2## or --CH.sub.2 --O--R.sub.10 radical, R.sub.7 is a hydrogen atom, a C.sub.1 -C.sub.12 -alkyl radical or an N-dialkylamino-C.sub.1 -C.sub.6 -alkyl radical, R.sub.8 and R.sub.9, which can be the same or different, are hydrogen atoms or straight-chained, branched, saturated or unsaturated aliphatic C.sub.1 -C.sub.12 -aliphatic radicals or, together with the nitrogen atom to which they are attached, form a saturated or unsaturated ring with 2 to 6 carbon atoms, R.sub.10 is a hydrogen atom, a straight-chained or branched C.sub.1 -C.sub.6 -alkyl or C.sub.2 -C.sub.6 -alkenyl radical, an aralkyl radical or an acyl radical, X is a valency bond or a methylene radical, Y is a valency bond or a straight-chained, branched, saturated or unsaturated hydrocarbon radical containing up to 6 carbon atoms and Z is a valency bond, or oxygen atom or a carbonyl group; as well as the pharmacologically acceptable salts and optical isomers thereof. The present invention also provides processes for the preparation of these compounds, as well as pharmaceutical compositions containing them for the treatment of heart and circulatory diseases.

Trisubstituted amines, pharmacologically acceptable salts thereof and

A process for the preparation of S- or R-carbazole derivatives of the general formula: ##STR1## in which R is an unsubstituted or substituted amino radical and pharmacologically acceptable salts, by either reacting R-(-)-epichlorohydrin (for the S-carbazole derivative); or reacting an S-epoxide derivative of the general formula: ##STR2## in which R.sub.1 is the residue of a substituted sulphonic acid derivative (for the R-carbazole derivative); with 4-hydroxycarbazole and then with ammonia or a substituted amine of the general formula RH, and recovering the compound or converting it to a pharmacologically acceptable salt. The new R-(+)- and S(-)-carbazole derivatives provided by the inventive process have unexpected beta blocking and vasodilatory properties and are useful in pharmaceutical compositions. R-(+)-carbazole derivatives are also useful for the treatment of glaucoma.

The present invention provides compounds of the general formula: ##STR1## wherein R.sub.1 is a straight-chained or branched C.sub.1 -C.sub.12 -alkyl radical which can be substituted by a phenyl, naphthyl or C.sub.3 -C.sub.7 -cycloalkyl radical, a straight-chained or branched C.sub.2 -C.sub.12 -alkenyl radical which can be substituted by a C.sub.3 -C.sub.7 -cycloalkyl, phenyl or naphthyl radical, a C.sub.3 -C.sub.7 -cycloalkyl radical or an unsubstituted or mono- or polysubstituted mono- or bicyclic aromatic radical, in which the substituents can be halogen atoms, carboxyl groups or C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy or C.sub.1 -C.sub.4 -alkoxycarbonyl radicals, R.sub.2 and R.sub.3, which can be the same or different, are straight-chained, branched, saturated or unsaturated C.sub.1 -C.sub.6 -alkyl radicals or, together with the nitrogen atom to which they are attached, form a saturated or unsaturated ring which can contain further heteroatoms and can possibly be substituted by a C.sub.1 -C.sub.6 -alkyl radical, one or more C.sub.1 -C.sub.6 -alkoxy radicals, one or more hydroxyl groups or by an oxygen atom, X is a methylene radical, an oxygen or sulphur atom, a sulphoxide or sulphonyl group or an .dbd.NR.sub.6 group, in which R.sub.6 is a hydrogen atom or a C.sub.1 -C.sub.4 -alkyl or aralkyl radical, n is 0, 1 or 2, k is 0, 1, 2 or 3, R.sub.4 is a halogen atom, a hydroxyl group or a C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -alkoxy or aralkoxy radical or, when k is 2, is a C.sub.1 -C.sub.2 -alkylenedioxy radical on two adjacent carbon atoms, m is 0, 1, 2 or 3 and R.sub.5 is a halogen atom, a hydroxyl group or a C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.6 -alkoxy or aralkoxy radical or, when m is 2, is a C.sub.1 -C.sub.2 -alkylenedioxy radical on two adjacent carbon atoms; as well as the pharmacologically acceptable salts thereof. The present invention also provides processes for the preparation of these compounds and pharmaceutical compositions containing them.

Substituted heterocyclic compounds and the pharmacologically acceptable

Growing community of inventors

Heppenheim, Germany

Herbert Leinert