Boehringer Ingelheim International Gmbh

Boehringer Ingelheim Pharma Gmbh & Co Kg

Vitae Pharmaceuticals, Inc.

Annette Schuler-Metz

Henning Priepke

Herbert Nar

Wolfgang Wienen

Kai Gerlach

Roland Pfau

Georg Dahmann

Sandra Handschuh

Norbert Hauel

Iris Kauffmann-Hefner

Henri Doods

Ingo Konetzki

Angelo Ceci

Rainer Walter

Matthias Eckhardt

Elke Langkopf

Holger Wagner

Alexander Pautsch

Ruediger Streicher

Corinna Schoelch

Frank Himmelsbach

Matthias Hoffmann

Andreas Schnapp

Dennis Fiegen

Juergen Mack

Heiner Ebel

Bradford S Hamilton

Silke Hobbie

Takeshi Kono

Yayoi Sato

Linghang Zhuang

Armin Heckel

Stefan Peters

Joerg Kley

Thorsten Lehmann-Lintz

Dieter Wiedenmayer

Enzo Cereda

James Gillard

Eckhart Bauer

Matthias Zentgraf

Peter Kuehn

Rüdiger Streicher

The present invention relates to new substituted glycinamides of general formula (I) wherein D, M, R, Rand Rare defined as in the specification, the tautomers, enantiomers, diastereomers, mixtures and salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties.

Substituted glycinamides, process for their manufacture and use thereof as medicaments

The invention relates to new substituted naphthyridines of formula 1, as well as pharmacologically acceptable salts, diastereomers, enantiomers, racemates, hydrates or solvates thereof, wherein

4-dimethylamino-phenyl-substituted naphthyridines, and use thereof as medicaments

The present invention relates to compounds of general formula I wherein n, R, R, R, R, R, R, Rand Rare defined as stated hereinafter, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with organic or inorganic acids or bases, which have valuable properties, the preparation thereof, the pharmaceutical compositions containing the pharmacologically effective compounds, the preparation thereof and the use thereof.

Bradykinin B1-antagonists

Disclosed are compounds of the formula I wherein A, Y, R, R, R, Rand Rare defined, suitable for treating diseases and symptoms of diseases caused at least to some extent by stimulation of bradykinin-B1 receptors, the preparation thereof and the use thereof.

B1-antagonists

The present invention relates to compounds defined by formula I wherein the groups Rto R, X, m, n and o are defined as in claim, possessing valuable pharmacological activity. Particularly the compounds are inhibitors of 11&#x3b2;-hydroxysteroid dehydrogenase (HSD) 1 and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme, such as metabolic diseases, in particular diabetes type 2, obesity and dyslipidemia.

Aryl- and heteroarylcarbonyl derivatives of benzomorphanes and related scaffolds, medicaments containing such compounds and their use

This invention relates to novel compounds of the Formula (I), (Ia), (Ib), (Ic), (Id), (Ie) pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11&#x3b2;-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of cortisol in a cell or the inhibition of the conversion of cortisone to cortisol in a cell. 

Inhibitors of 11beta-hydroxysteroid dehydrogenase 1

The present invention relates to new substituted carboxylic acid amides of general formula wherein A, B and Rto Rare defined as in claim, the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties.

Carboxylic acid amides, the preparation thereof and their use as medicaments

The present invention relates to new substituted prolinamides of general formula (I) wherein D, Y, A, B, R, Rand Rare defined as in the specification, the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties. 

Substituted amides, manufacturing and use thereof as medicaments

The invention relates to novel substituted naphthyridines of formula 1 as well as pharmacologically acceptable salts, diastereomers, enantiomers, racemates, hydrates, or solvates thereof. In formula 1, Rcan represent a group A selected from among the group comprising &#x2014;O&#x2014;R, &#x2014;NRR, &#x2014;CRRR, -(ethyne)-R, &#x2014;S&#x2014;R, &#x2014;SO&#x2014;R, and SO&#x2014;R, or Rrepresents a group B selected from among the group comprising: &#x2014;C-aryl; &#x2014;a five-membered to ten-membered, monocyclic or bicyclic heteroaryl containing 1 to 3 heteroatoms independently selected from among the group comprising N, O, and S, wherein said heteroaryl is linked to the structure according to formula 1 via a C atom or an N atom; &#x2014;a three-membered to ten-membered, monocyclic or bicyclic, saturated or partially saturated heterocycle containing 1 to 3 heteroatoms independently selected from among the group comprising N, O, and S, wherein said heterocycle is linked to the structure according to formula 1 via a C atom or an N atom; and &#x2014;a 5-membered to 11-membered spiro group which can optionally contain 1, 2, or 3 heteroatoms independently selected from among the group comprising N, O, and S, wherein said spiro group is linked to the structure according to formula 1 via a C atom or an N atom, wherein said group B can be optionally substituted as described in claims, and R, R, R, R, and m can have the meanings indicated in claim. The invention also relates to pharmaceutical compositions containing said compounds. 

Novel compounds which are useful for treating acute pain, visceral pain, neuropathic pain, inflammatory/pain receptor-mediated pain, tumor pain and headache diseases. The following is exemplary: 

Bradykinin B1-receptor antagonists

Novel compounds of which the following is exemplary: 

Compounds

Compounds of the formula I wherein n, R, R, R, R, R, R, R, R, R, R, Rand X are defined as described in the specification, which are bradykinin B1 antagonists, and their use as medicaments.

Compounds as bradykinin B1 antagonists

The present invention relates to substituted arylsulphonylaminomethyl-phosphonic acid derivatives of general formula wherein R, X, Y and Z are defined as in claim, the tautomers, enantiomers, diastereomers, mixtures thereof and salts thereof which have valuable pharmacological properties, particularly the suppression of the interaction of glycogen phosphorylase a with the Gsubunit of glycogen-associated protein phosphatase 1 (PP1), and their use as pharmaceutical compositions.

Substituted arylsulfonylaminomethylphosphonic acid derivatives, their preparation and their use in the treatment of type I and II diabetes mellitus

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Ulm, Germany

Annette Schuler-Metz