Gruenenthal Gmbh

Aeterna Zentaris Gmbh

Zentaris Gmbh

Centre National De La Recherche Scientifique

University of Montpellier I

University of Montpellier Ii

Ae Zentaris Gmbh

Grunenthal Gmbh

Æterna Zentaris Gmbh

Matthias Gerlach

Corinna Maul

Eckhard Guenther

Irene Seipelt

Utz-Peter Jagusch

Eckhard Claus

Silke Baasner

Bernd Sundermann

Werner Guenter Englberger

Hagen-Heinrich Hennies

Ruth Jostock

Melanie Reich

Corinna Sundermann

Beatrix Merla

Tilmann Schuster

Emmanuel Polymeropoulos

Peter Schmidt

Gilbert Mueller

Eckhard Günther

Michael Teifel

Klaus Paulini

Lars Blumenstein

Michael Haurand

Michael Przewosny

Petra Bloms-Funke

Claudia Katharina Puetz

Boris Chizh

Ronald Kühne

Elke Reissmueller

Arvid Söderhäll

Jean Martinez

Johannes Schneider

Jean-Alain Fehrentz

Adriaan Pieter Ijzerman

Heinz Uragg

Babette Aicher

Michael Czech

Stefan Oberbörsch

Anne-Laure Blayo

Pascal Marchand

Peter Ernig

Julien Defaux

Corrinna Sundermann

Martin Fuhr

Miriam Dissen-De Groote

Gero Gaube

D Enders

Gilbert MÜLLER

Claudia Katharina Pütz

The present invention provides new pyridopyrazine compounds of Formula (I) which are suitable for the treatment or prevention of physiological and/or pathophysiological states mediated and/or modulated by signal transduction pathways and/or enzymes in mammals and in particular in humans. 

Pyridopyrazine derivatives and their use

The invention provides new pyridopyrazine compounds according to formula (I) 

Pyridopyrazines as highly selective ras-Raf-Mek-Erk signal transduction pathway inhibitors

A method of modulating one or more of ras-Raf-Mek-Erk signal transduction pathway, PI3K-Akt signal transduction pathway and SAPK signal transduction pathway with 1-ethyl-3-[3-(1-methyl-1H-pyrazol-4-yl)-pyrido[2,3-b]pyrazine-6-yl]thiourea, its geometric isomer, or its tautomer.

Modulating signal transduction pathways with 1-ethyl-3-[3-(1-methyl-1H-pyrazol-4-yl)-pyrido[2.3-B]pyrazine-6-yl]thiourea

The present invention provides novel triazole derivatives with improved receptor activity and bioavailability properties as ghrelin analogue ligands of growth hormone secretagogue receptors according to formula (I) that are useful in the treatment or prophylaxis of physiological and/or pathophysiological conditions in mammals, preferably humans, that are mediated by GHS receptors. The present invention further provides GHS receptor antagonists and agonists that can be used for modulation of these receptors and are useful for treating above conditions, in particular alcohol disorder, drug abuse, growth retardation, cachexia, short-, medium-, and/or long term regulation of energy balance, short-, medium-, and/or long term regulation (stimulation and/or inhibition) of food intake, intake of rewarding food, adipogenesis, adiposity and/or obesity, body weight gain and/or reduction, diabetes, diabetes type I, diabetes type II, tumor cell proliferation, inflammation, inflammatory effects, gastric postoperative ileus, postoperative ileus and/or gastrectomy (ghrelin replacement therapy).

Triazole derivatives with improved receptor activity and bioavailability properties as ghrelin antagonists of growth hormone secretagogue receptors

Method of modulating ras-Raf-Mek-Erk signal transduction pathway, PI3K-Akt signal transduction pathway and/or SAPK signal transduction pathway with a pyrido[2,3-b]pyrazine of formula (Ia).

Modulating signal transduction pathways with substituted pyridol [2,3-b] pyrazines

1-ethyl-3-[3-(1-methyl-1H-pyrazol-4-yl)-pyrido[2.3-b]pyrazine-6-yl]thiourea which HAS activity to the modulation of misdirected cellular signal transduction processes such as tyrosine kinases, serine/threonine kinases and/or lipid kinases.

Pyridopyrazine derivatives, process of manufacturing and uses thereof

The present invention relates to kinase modulators of the naphthyridine type and to the preparation and use thereof as medicaments for the modulation of misdirected cellular signal transduction processes, in particular for influencing the function of tyrosine and serine/threonine kinases and for the treatment of malignant or benign tumors and other disorders based on pathological cell proliferation, such as, for example, restenosis, psoriasis, arteriosclerosis and cirrhosis of the liver.

Naphthyridine derivatives and the use thereof as kinase inhibitors

The invention provides quinoxalines of the general formula I which are used as medicaments preferably for treating tumour disorders, in particular in cases of drug resistance to other active compounds and in cases of metastasic carcinoma. The possible applications are not limited to tumour disorders. 

Quinoxaline derivatives and their use for treating benign and malignant tumour disorders

The invention relates to pyrido[2,3-b]pyrazine compounds of formulae (Ia) and (Ib) which have activity to the modulation of misdirected cellular signal transduction processes such as tyrosine kinases, serine/threonine kinases and/or lipid kinases, their preparation and use as medicaments, especially for the treatment of malignant disorders and other disorders based on pathological cell proliferations: 

Substituted pyrido[2,3-b]pyrazine compounds as modulators of tyrosine kinases

The present invention provides novel tetrahydrocarbazole derivatives which have improved properties and which can be employed as inhibitors of GPCRs. This results in the possibility of using the novel compounds to treat pathological conditions whose severity depends on the pathobiochemical effect of GPCRs. The compounds of the invention act in particular via an antagonistic inhibition of the LHRH receptor. The invention further provides medicaments which comprise one or more of the novel compounds as active ingredient. The medicaments are suitable in particular to be employed in an oral dosage form for a mammal, in particular a human.

Tetrahydrocarbazole derivatives having improved biological action and improved solubility as ligands of G-protein coupled receptors (GPCPs)

Sulfonylguanidine compounds corresponding to the tautomeric formulas I and Ia, a method for producing them, pharmaceutical compositions containing them, and methods of using them to prepare medicaments and for treating various medical conditions. The sulfonylguanidine compounds have an affinity for the gabapentin binding site and can be used to treat conditions such as pain, epilepsy, migraine and others.

Sulfonylguanidine compounds and pharmaceutical uses thereof

Tetrahydrocarbazole derivatives having improved biological action and improved solubility as ligands of G-protein coupled receptors (GPCRs)

Substituted-dihydropyrido[1,2-a]pyrimidines of formula I and processes for the production thereof Also disclosed are substance libraries and pharmaceutical compositions containing the compound, and methods of treatment for pain, urinary incontinence, pruritus, tinnitus and/or diarrhoea using the pharmaceutical composition.

Substituted 3,4-dihydropyrido[1,2-a]pyrimidines

Substituted 3,4-dihydro-pyrimido[1,2a]pyrimidines and 3,4-dihydro-pyrazino[1,2a]pyrimidines of general formula I, the invention also relates to a method for the production thereof, substance libraries containing these compounds, medicaments which contain these compounds in the production of medicaments for treating pain, urinary incontinence, itching, tinnitus aurium and/or diarrhea and to pharmaceutical compositions containing these compounds.

Substituted 3,4-dihydro-pyrimido[1,2a]pyrimidines and 3,4-dihydro-pyrazino[1,2a]pyrimidines, and methods for their preparation and use

The invention relates to novel N-substituted indolyl-3-glyoxylamides of the general formula I, their preparation and use as medicaments, in particular for the treatment of tumors 

N-substituted indolyl-3-glyoxylamides, their use as medicaments and process for their preparation

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Matthias Gerlach