Boehringer Ingelheim International Gmbh

Centrexion Therapeutics Corporation

Iain Lingard

Riccardo Giovannini

Marco Ferrara

Rocco Mazzaferro

Klaus Rudolf

Dieter Wolfgang Hamprecht

Sara Frattini

Henri Doods

Raimund Kuelzer

Yunhai Cui

Stefan Just

Holger Wagner

Bernd Wellenzohn

Remko Alexander Bakker

Matthias Eckhardt

Elke Langkopf

Stefan Peters

Alexander Pautsch

Dieter Wiedenmayer

Andreas Gollner

Barbara Kistler

Dieter Hamprecht

Frank Himmelsbach

Holger Rosenbrock

Joerg P Hehn

Giacomo Fossati

Barbara Bertani

Disclosed are phenyltetrazole derivatives of formula (I), wherein A, R, R, X, R', R″, and n are as defined herein, and pharmaceutically acceptable salts thereof. Also disclosed are methods of using the phenyltetrazole derivatives for the treatment of diseases which can be influenced by inhibition of plasma kallikrein.

Phenyltetrazole derivatives as plasma kallikrein inhibitors

3-aza-bicyclo[3.1.0]hexane-6-carboxylic acid amide derivatives which are agonists of somatostatin receptor subtype 4 (SSTR4), useful for preventing or treating medical disorders related to SSTR4.

Somatostatin receptor subtype 4 (SSTR4) agonists

The present invention relates to compounds of general formula (I), wherein Dto D, -A-, n, R, R, Y, L andare defined as in claim, which have valuable pharmacological properties, in particular are inhibitors of plasma kallikrein. The compounds are suitable for treatment and prevention of diseases which can be influenced by inhibition of plasma kallikrein, such as diabetic complications, particularly in the treatment of retinal vascular permeability associated with diabetic retinopathy and diabetic macular edema. 

Heteroarylcarboxamide derivatives as plasma kallikrein inhibitors

The invention relates to morpholine and 1,4-oxazepane amide derivatives of general formula (I), which are agonists of somatostatin receptor subtype 4 (SSTR4), useful for preventing or treating medical disorders related to SSTR4. In addition, the invention relates to processes for preparing pharmaceutical compositions as well as processes for manufacture of the compounds according to the invention.

Morpholine and 1,4-oxazepane amides as somatostatin receptor subtype 4 (SSTR4) agonists

Disclosed are heteroarylcarboxamides of formula (I), and pharmaceutically acceptable salts thereof, wherein A, T, R, Rand Rare as defined herein. Also disclosed are methods of using these compounds for the treatment of diseases which can be influenced by inhibition of plasma kallikrein.

The present invention relates to compounds of general formula I, wherein Dto D, A, R, R, Y and n are defined as in claim, which have valuable pharmacological properties, in particular are inhibitors of plasma kallikrein. The compounds are suitable for treatment and prevention of diseases which can be influenced by influenced by inhibition of plasma kallikrein, such as diabetic complications, particularly in the treatment of retinal vascular permeability associated with diabetic retinopathy and diabetic macular edema. 

The invention relates to aryl and heteroaryl-fused tetrahydro-1,4-oxazepine amide derivatives of general formula (1), which are agonists of somatostatin receptor subtype 4 (SSTR4), useful for preventing or treating medical disorders related to SSTR4. In addition, the invention relates processes for manufacture of the compounds according to the invention. 

Aryl and heteroaryl-fused tetrahydro-1,4-oxazepine amides as somatostatin receptor subtype 4 (SSTR4) agonists

The invention relates to morpholine and 1,4-oxazepane amide derivatives of general formula (I), which are agonists of somatostatin receptor subtype 4 (SSTR4), useful for preventing or treating medical disorders related to SSTR4. In addition, the invention relates to processes for preparing pharmaceutical compositions as well as processes for manufacture of the compounds according to the invention. 

A compound of formula I, wherein the groups R, R, R, X, m, and n are defined as in claim, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2. Furthermore, the invention relates to novel intermediates, useful for the synthesis of compounds of formula I.

Indanyloxyphenylcyclopropanecarboxylic acids

Substituted phenyl-3-aza-bicyclo[3.1.0]hex-3-yl-methanones which are glycine transporter-1 (GlyT1) inhibitors. These are useful for the treatment of schizophrenia, Alzheimer's Disease and other neurological and psychiatric disorders.

Phenyl-3-aza-bicyclo[3.1.0]hex-3-yl-methanones and the use thereof as medicament

This invention relates to bicyclic ring system substituted amide functionalized phenols of general formula 1, their use as inhibitors of CXCR2 activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of respiratory or gastrointestinal complaints or diseases, inflammatory diseases of the joints, skin, or eyes, diseases of the peripheral or central nervous system or cancers, as well as pharmaceutical compositions which contain these compounds.

Bicyclic ring system substituted amide functionalised phenols as medicaments

This invention relates to bicyclic ring system substituted sulfonamide functionalized phenols of general formula 1, their use as inhibitors of CXCR2 activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of respiratory or gastrointestinal complaints or diseases, inflammatory diseases of the joints, skin, or eyes, diseases of the peripheral or central nervous system or cancers, as well as pharmaceutical compositions which contain these compounds.

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Monza, Italy

Iain Lingard