Boehringer Ingelheim International Gmbh

Boehringer Ingelheim Pharma Gmbh & Co Kg

Dennis Fiegen

Thomas Fox

Christoph Hoenke

Gerhard Schaenzle

Peter Nickolaus

Pascale Pouzet

Rolf Goeggel

Riccardo Giovannini

Matthias Hoffmann

Niklas Heine

Christian Eickmeier

Klaus Fuchs

Holger Rosenbrock

Andreas Schnapp

Sandra Handschuh

Cornelia Dorner-Ciossek

Klaus Klinder

Georg Dahmann

Horst Dollinger

Jasna Klicic

Birgit Jung

Ralf Anderskewitz

Domnic Martyres

Christian Gnamm

Thorsten K Oost

Guenter Linz

Martin Hendrix

Annette Schuler-Metz

Edward Walker

Stephen East

Michael Philip Mazanetz

Silke Hobbie

Takeshi Kono

Robert John Scott

Yayoi Sato

Stefan Peters

Gerald Juergen Roth

Martin Thomas Fleck

John Scott

David James Lamb

Spencer Charles R Napier

Stephen Peter East

Cornelia Dornier-Ciossek

Stephen P East

This invention relates to substituted 4-pyridones of formula 1 and their use as inhibitors of neutrophil elastase activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of pulmonary, gastrointestinal and genitourinary diseases, inflammatory diseases of the skin and the eye and other auto-immune and allergic disorders, allograft rejection, and oncological diseases.

Substituted 4-pyridones and their use as inhibitors of neutrophil elastase activity

The invention relates to new substituted naphthyridines of formula 1, as well as pharmacologically acceptable salts, diastereomers, enantiomers, racemates, hydrates or solvates thereof, wherein wherein n is either 0 or 1,

Substituted naphthyridines and their use as medicaments

Dihydrothienopyrimidinesulphoxides of formula 1 wherein X is SO or SO, Ris H or C-alkyl, Ris H or an organic group as disclosed herein, and Ris an optionally substituted, mono- or bicyclic, unsaturated, partially saturated or saturated heterocycle or an optionally substituted, mono- or bicyclic heteroaryl, and the pharmacologically acceptable salts thereof, as well as pharmaceutical compositions which contain these compounds. These dihydrothienopyrimidinesulphoxides are suitable for the treatment 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.

Heterocycle-substituted piperazino-dihydrothienopyrimidines

The invention relates to novel 1,6-disubstituted pyrazolopyrimidinones of formula (I), in which Hc is a tetrahydropyranyl-group and Ris the group V&#x2014;W&#x2014;*, whereby V and W independently of each other may be an aryl group or an heteroaryl group, which independently of each other may optionally be substituted. According to one aspect of the invention the new compounds are for use as medicaments or for the manufacture of medicaments, in particular medicaments for the treatment of conditions concerning deficits in perception, concentration, learning or memory. The new compounds are also for the manufacture of medicaments and/or for use in the treatment of e.g. Alzheimer's disease, in particular for cognitive impairment associated with Alzheimer's disease.

Compounds for the treatment of CNS disorders

The invention relates to novel 1,6-disubstituted pyrazolopyrimidinones, wherein i.) the nitrogen atom of the pyrazolo-group that is next to the pyrimidino-group is attached to a non-aromatic, organic heterocycle having at least one ring hetero atom selected from O, N and S and ii.) to the C-atom between the two nitrogen atoms of the pyrimidinone-ring a second substituent is bound via an optionally substituted methylene-bridge. According to one aspect of the invention the new compounds are for the manufacture of medicaments, in particular medicaments for the treatment of conditions concerning deficits in perception, concentration, learning or memory. The new compounds are also for the manufacture of medicaments for the treatment of Alzheimer's disease.

1-heterocyclyl-1,5-dihydro-pyrazolo[3,4-D] pyrimidin-4-one derivatives and their use as PDE9A modulators

The invention relates to new amino-indole-substituted imidazolyl-pyrimidines of formula 1 whereinR, R, R, Rand Rare defined as in claimand pharmaceutically acceptable salts thereof and the use of these compounds for the preparation of a medicament for treating a disease selected from asthma, COPD, rheumatoid arthritis, specific lymphomas and specific diseases of the nervous system.

Amino-indolyl-substituted imidazolyl-pyrimidines and their use as medicaments

A method for treating diseases associated with the inhibition of phosphodiesterase 4 (PDE4) enzyme in a patient comprising administering to the patient in need thereof a therapeutically effective amount of a dihydrothienopyrimidinesulphoxide of formula 1, as well as pharmacologically acceptable salts, diastereomers, enantiomers, racemates, hydrates or solvates thereof 

Piperazino-dihydrothienopyrimidine derivatives

The invention relates to novel cycloalkyl- or cycloalkenyl-substituted pyrazolopyrimidinones of formula (I). wherein A, R-Rand x are as defined herein, and their use as medicaments for improving perception, concentration, learning and/or memory in patients in need thereof.

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 invention relates to new dihydrothienopyrimidine of formula 1, as well as pharmacologically acceptable salts, diastereomers, enantiomers, racemates, hydrates or solvates thereof, wherein X is SO or SO, but preferably SO, and wherein R, Rand Rhave the meanings given in the description,and which are suitable for the treatment 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.

6,7-dihydrothieno[3,2-d]pyrimidine for the treatment of inflammatory diseases

The invention relates to new substituted pyridinyl-pyrimidines of formula 

Substituted pyridinyl-pyrimidines and their use as medicaments

Piperidinodihydrothienopyrimidines of formula 1 wherein X is SO or SO(preferably SO), and R, R, R, and Rmay have the meanings given in the disclosure and claims, pharmacologically acceptable salts thereof, and pharmaceutical compositions containing these compounds. These piperidinodihydrothienopyrimidines are suitable for the treatment 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.

Substituted piperazino-dihydrothienopyrimidines

The invention relates to novel substituted pyrazolopyrimidines. Chemically, the compounds are characterized by general Formula (I): with Rbeing phenyl or pyridyl, any of which is substituted with 1 to 4, preferably 1 to 3 substituents X; X independently of each other being selected from C-C-alkyor Ci-C-alkoxy, where C-C-alkyl and C-C-alkoxy are at least dihalogenated up to perhalogenated. preferably with 2 to 6 halogen substituents, and the halogen atoms being selected from the group of fluoro, chloro and bromo, preferably fluoro; Rbeing phenyl or heteroaryl, where phenyl is substituted by 1 to 3 radicals and heteroaryl is optionally substituted by 1 to 3 radicals in each case independently of one another selected from the group of C-C-alkyl, C-C-alkoxy, hydroxycarbonyl, cyano, trifluoromethyl, amino, nitro, hydroxy, C-C-alkylamino, halogen, C-C-arylcarbonylamino, C-C-alkylcarbonylamino, C-C-alkylaminocarbonyl. C-C-alkoxycarbonyl, C-C-arylaminocarbonyl, heteroarylaminocarbonyl. heteroarylcarbonylamino, C-C-alkylsulphonyl-amino, C-C-alkylsulphonyl and C-C-alkylthio; The new compounds shall be used for the manufacture of medicaments, in particular medicaments for improving, perception, concentration, learning and/or memory in patients in need thereof. 

1, 5-dihydro-pyrazolo (3, 4-D) pyrimidin-4-one derivatives and their use as PDE9A mudulators for the treatment of CNS disorders

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Biberach, Germany

Dennis Fiegen