Boehringer Ingelheim Gmbh

Boehringer Ingelheim Kg

Dr. Karl Thomae Gmbh

C. H. Boehringer Sohn

Gojko Muacevic

Herbert Koppe

Werner Kummer

Helmut Stahle

Albrecht Harreus

Gerhard Walther

Karl-Heinz Weber

Kurt Schromm

Ernst-Otto Renth

Anton Mentrup

Werner Traunecker

Wolfgang Hoefke

Jorge Casals-Stenzel

Armin Heckel

Johannes M Weisenberger

Werner Stransky

Wolfgang Eisert

Thomas Muller

Wolf-Dietrich Bechtel

Rainer Soyka

Wolfgang Troger

Josef Nickl, Deceased

Christopher Meade

Jorge C Stenzel

Hubert Heuer

Bernd Zierenberg

Armin Fugner

Karl H Weber

The invention relates to micronized biodegradable particles, processes for preparing them and use thereof.

Micronized biodegradable particles, process for preparing them and use

The invention relates to new arylsulphonamides of the formula ##STR1## (wherein A, B and R.sub.1 to R.sub.6 are as defined in claim 1, the enantiomers, the cis- and trans-isomers thereof where R.sub.4 and R.sub.5 together represent a carbon-carbon bond, and the addition salts thereof, more particularly for pharmaceutical use the physiologically acceptable addition salts thereof with inorganic or organic bases, if R.sub.6 represents a hydroxy group) which have useful pharmacological properties, particularly antithrombotic activities and thromboxane-mediating activities. Furthermore, the new compounds are also thromboxane antagonists (TRA) and thromboxane synthesis inhibitors (TSH). They also have an effect on PGE.sub.2 production.

Arylsulphonamides, pharmaceutical compositions containing these

The invention relates to new hetrazepines of general formula ##STR1## wherein A, Z, n, X, Y, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 have the meanings given in the specification.

Hetrazepine compounds which have useful pharmaceutical utility

Arylsulphonamides, pharmaceutical compositions containing these compounds

The invention relates to new arylsulphonamides of the formula ##STR1## (wherein A, B and R.sub.1 to R.sub.6 are as defined in claim 1, the enantiomers, the cis- and trans-isomers thereof where R.sub.4 and R.sub.5 together represent a carbon-carbon bond, and the addition salts thereof, more particularly for pharmaceutical use the physiologically acceptable addition salts thereof with inorganic or organic bases, if R.sub.6 represents a hydroxy group) which have useful pharmacological properties, particularly antithrombotic activities and thromboxane-mediating activities. Furthermore, the new compounds are also thromboxane antagonists (TRA) and thromboxane synthesis inhibitors (TSH) They also have an effect on PGE.sub.2 production.

Arylsulphonamides pharmaceutical compositions containing these compounds

The invention relates to new thieno-triazolo-1,4-diazepino-2-carboxylic acid amides of formula I ##STR1## wherein R.sub.1 represents hydrogen, a C.sub.1 -C.sub.4 straight-chained or branched alkyl which can optionally be substituted by halogen, preferably Cl or Br, or by hydroxy, cyclopropyl, C.sub.1 -C.sub.3 alkoxy, preferably methoxy, or halogen, preferably chlorine or bromine;

Methods of using new thieno-triazole-1,4-diazepino-2-carboxylic acid

The invention relates to new 1,4-diazepines of the general formula ##STR1## in which R.sub.1, R.sub.2 R.sub.3, X and A have the meaning indicated in the specification. The new compounds are intended for use for the treatment of pathological states and diseases in which PAF (platelet activating factor) is involved.

Substituted-1,4-diazepines

The invention relates to new thieno-triazolo-1,4-diazepino-2-carboxylic acid amides of formula I ##STR1## wherein R.sub.1 represents hydrogen, a C.sub.1-C.sub.4 straight-chained or branched alkyl which can optionally be substituted by halogen, preferably C1 or Br, or by hydroxy, cyclopropyl, C.sub.1 -C.sub.3 alkoxy, preferably methoxy, or halogen, preferably chlorine or bromine;

Thieno-triazolo-1,4-diazepino-2-carboxylic acid amides

The invention relates to new thieno-traizolo-1,4-diazepino-2-carboxylic acid amides of formula I ##STR1## wherein R.sub.1 represents hydrogen, a C.sub.1 -C.sub.4 straight-chained or branched alkyl which can optionally be substituted by halogen, preferably Cl or Br, or by hydroxy, cyclopropyl, C.sub.1 -C.sub.3 alkoxy, preferably methoxy, or halogen, preferably chlorine or bromine;

Thieno-traizolo-1,4-diazepino-2-carboxylic acid amides

The invention relates to new thieno-1,4-diazepines of general formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.degree., R', Z, X, Y and n have the meanings given in the specification. The new compounds are intended to be used in the treatment of pathological conditions and diseases in which PAF (platelet activating factor) is implicated.

Thieno-1,4-diazepines

The invention discloses a method of treating an individual having a disorder responsive to PAF-antagonist activity by treating the individual with a compound of formula I. ##STR1## wherein A is an anellated and optionally substituted benzene or 5- or 6- membered heterocyclic ring; R.sub.5 and Z are each independently hydrogen or an optionally substituted C.sub.1 -C.sub.8 alkyl, alkenyl or alkynyl; R.sub.6 is an optionally substituted phenyl, or is thienyl or .alpha.-pyridyl; Y is ##STR2## and nontoxic, pharmaceutically acceptable acid addition salts thereof.

PAF-antagonistic diazepines, methods of use

The invention discloses a method of treating an individual having a disorder responsive to PAF-antagonist activity by treating the individual with a compound of formula I or II ##STR1## wherein A is an anellated and optionally substituted benzene or 5- or 6-membered heterocyclic ring; R.sub.5 and Z are each independently hydrogen or an optionally substituted C.sub.1 -C.sub.8 alkyl, alkenyl or alkynyl; R.sub.6 is an optionally substituted phenyl, or is thienyl or is .alpha.-pyridyl; Y is CO, CS or CH.sub.2 ; and nontoxic, pharmaceutically acceptable acid addition salts thereof.

Methods of using PAF-antagonistic diazepines

The invention discloses a method of treating an individual having a disorder responsive to PAF-antagonist activity by treating the individual with a compound of formula I or II: ##STR1## wherein A is an annealed and optionally substituted benzene or 5- or 6-membered heterocyclic ring; B is an optionally substituted 5-membered heterocyclic ring; R.sub.5 and R.sub.7 are each independently hydrogen or an optionally substituted C.sub.1 -C.sub.8 alkyl, alkenyl or alkynyl; R.sub.6 is an optionally substituted phenyl, or is thienyl or .alpha.-pyridyl; and non-toxic, pharmaceutically acceptable acid addition salts thereof.

PAF-antagonistic diazepines

The invention relates to a compound of the formula ##STR1## wherein R.sub.1 is a linear or branched alkyl of 4 to 20 carbon atoms;

1-(Alkanoylamino-aryloxy)-2-hydroxy-3-(alkinyl-amino)-propanes and salts

Compounds of the formula ##STR1## wherein n is 1 or 2, R.sub.1 is hydrogen, --CO--R.sub.2 or --SO.sub.2 R.sub.3,

Growing community of inventors

Ingelheim am Rhein, Germany

Gojko Muacevic