Boehringer Ingelheim International Gmbh

Boehringer Ingelheim Pharma Gmbh & Co Kg

Gerhard Schaenzle

Klaus Rudolf

Henri Doods

Stephan Georg Mueller

Dirk Stenkamp

Kirsten Arndt

Philipp Lustenberger

Marco Santagostino

Fabio Paleari

Georg Dahmann

Riccardo Giovannini

Niklas Heine

Christian Eickmeier

Dennis Fiegen

Holger Rosenbrock

Dirk Gottschling

Annekatrin Charlotte Heimann

Klaus Fuchs

Thomas Fox

Alexander Dreyer

Cornelia Dorner-Ciossek

Matthias Hoffmann

Jasna Klicic

Stephen East

Guenter Linz

Martin Hendrix

Andreas Schnapp

Sandra Handschuh

Edward Walker

John Scott

Daniel Bischoff

Clive Mccarthy

Michael Philip Mazanetz

Stefan Ludwig Michael Wollin

Serge Convers-Reignier

Robert John Scott

Frederic Jacques Marlin

Matthias Grauert

Christoph Hoenke

Stefan Peters

Kai Gerlach

Thierry Bouyssou

Alexander Pautsch

Marco Ferrara

Steffen Breitfelder

Trixi Brandl

Eckhart Bauer

Frank Buettner

Udo Maier

Stephen Peter East

Frank Kalkbrenner

Marco Ferrera

Cornelia Dornier-Ciossek

Anne Joergensen

Frank Büttner

Rudlof Klaus

Stephen P East

Serge Gaston Convers-Reignier

Stefan Ludwig Wollin

The invention relates to novel 6-Cycloalkyl-pyrazolopyrimidinones according to formula (I). wherein Ris a 5 or 6 membered aromatic heteroaryl-group, Ris an optional substituent, D is optionally substituted cyclopentyl, cyclohexyl, tetrahydrofuranyl, tetrahydropyranyl or 2-, 3- or 4-pyridyl, m=1 or 2 and n is 0, 1 or 2. The new compounds are for use as the active entity of medicaments or for the manufacture of medicaments respectively, in particular medicaments for the treatment of conditions concerning deficits in perception, concentration, learning or memory. Such conditions may for example be associated with Alzheimer's disease, schizophrenia and other diseases. The new compounds are also for example for the manufacture of medicaments and/or for use in the treatment of these diseases, in particular for cognitive impairment associated with such disease. The compounds of the invention show PDE9 inhibiting properties.

6-cycloalkyl-pyrazolopyrimidinones for the treatment of CNS disorders

Disclosed are substituted quinolines of formula 1 whereinRand Rare defined herein, the processing of making and using the same.

Substituted quinolines and their use 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 wherein n is either 0 or 1,

Substituted naphthyridines and their use as medicaments

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 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 present invention relates to the new compounds of general formula I wherein A, U, V, X, Y, R, Rand Rare defined as stated hereinafter, the tautomers, the isomers thereof, the diastereomers, the enantiomers, the hydrates, the mixtures and the salts thereof as well as the hydrates of the salts, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, medicaments containing these compounds, their use and processes for preparing them.

Pyrimidine derivatives which are CGRP&#x2014;antagonists

The invention relates to novel 6-cycloalkyl-pyrazolopyrimidinones according to formula (I) wherein R, R, D, m and n are as defined herein. The invention also relates to medicaments comprising these compounds and methods of using these compounds in the treatment of diseases and conditions, particularly diseases or conditions concerning deficits in perception, concentration, learning or memory.

The present invention relates to new CGRP-antagonists of general formula I wherein U, V, X, Y, R, R, Rand Rare defined as mentioned in the description, the tautomers thereof, the isomers thereof, the diastereomers thereof, the enantiomers thereof, the hydrates thereof, the mixtures thereof and the salts thereof as well as the hydrates of the salts, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, medicaments containing these compounds, the use thereof and processes for the preparation thereof.

Compounds

The present invention relates to new CGRP-antagonists of general formula I wherein R, R, R, R, R, R, X, Y and Z are defined as mentioned hereinafter, the individual diastereomers, the individual enantiomers and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, medicaments containing these compounds, the use thereof and processes for the preparation thereof.

Substituted piperazines as CGRP antagonists

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

The present invention relates to new CGRP-antagonists of general formula I wherein U, V, X, Y, R, Rand Rare defined as stated hereinafter, the tautomers, the isomers, the diastereomers, the enantiomers, the hydrates, the mixtures thereof and the salts thereof and the hydrates of the salts, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, pharmaceutical compositions containing these compounds, their use and processes for preparing them.

CGRP antagonists

The invention relates to novel 1,6-disubstituted pyrazolopyrimidinones, Formula (I) with is a mono-, bi- or tri-cyclic heterocyclyl group, the ring members of which are carbon atoms and at least 1, preferably 1, 2 or 3, heteroatom(s), which are selected from the group of nitrogen, oxygen and sulphur, which is in the form of &#x2014;S(O)&#x2014; with r being 0, 1 or 2, and&#x2014;said heterocyclyl group is or comprises 1 non-aromatic, saturated, or partly unsaturated monocyclic ring which comprises at least 1 heteroatom as ring member and&#x2014;said heterocyclyl group is bound to the scaffold by said 1 non-aromatic, saturated, or partly unsaturated monocyclic ring which comprises at least 1 heteroatom as ring member. 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 derivates and their use as PDE9A modulators

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Biberach, Germany

Gerhard Schaenzle