Boehringer Ingelheim International Gmbh

Boehringer Ingelheim Pharma Gmbh & Co Kg

Boehringer Ingelheim Pharma Kg

Boehringer Ingelheim Kg

Hydra Biosciences, Inc.

Christian Eickmeier

Niklas Heine

Klaus Fuchs

Cornelia Dorner-Ciossek

Riccardo Giovannini

Gerhard Schaenzle

Holger Rosenbrock

Matthias Grauert

Kai Gerlach

Dennis Fiegen

Thomas Fox

Sandra Handschuh

Martin Steegmaier

Steffen Breitfelder

Gisela Schnapp

Matthias Hoffmann

Flavio Solca

Klaus Rudolf

Stefan Peters

Martin Hendrix

Otto Roos

Trixi Brandl

Klaus Klinder

Anke Baum

Norbert Redemann

Bernhard Schmid

Stefan Hoerer

Florian Colbatzky

Jens Juergen Quant

Lothar Kussmaul

Jan Magnus Kriegl

Marcus Kostka

Alexander Weber

Matthias Hoffman

Jens Jurgen Quant

Ulrike Gross

Erich Buerger

Bertrand Leo Chenard

Georg Speck

Peter Sieger

Herbert Nar

Thorsten Lehmann-Lintz

Michael Paul Pieper

Marco Ferrara

Werner Stransky

Werner Rall

Gerald Pohl

Achim Sauer

Stefan Matthias Blech

Sabine Pestel

Eckhart Bauer

Claudia Heine

Sabine Germeyer

Stefan Just

Rolf Herter

Marco Ferrera

Cornelia Dornier-Ciossek

Volkmar Koerner

Volkmar Körner

The present invention describes compounds modulating the function of mitochondrial complex I (NADH-quinone oxidoreductase) having formula (I)

Modulators of complex I

The present invention relates to triazolo pyridines of formula (II) and their use as modulators of #-secretase. In particular, the present invention relates to compounds which interfere with #-secretase and/or its substrate and therefore modulate the formation of A&#x3b2; peptides. Accordingly these compounds can be used for the treatment of A&#x3b2;-related pathologies, e.g. Alzheimer's disease. 

Triazolo pyridines as modulators of gamma-secretase

The present invention relates to substituted xanthine derivatives, pharmaceutical compositions containing them and their use in therapy, particularly in the treatment of conditions having an association with TRPC5 containing ion channels.

Substituted xanthine derivatives

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

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 dihydropteridinones, their use as modulators of &#x3b3;-secretase and to pharmaceutical compositions containing said compounds. In particular, the present invention relates to compounds which interfere with &#x3b3;-secretase and/or its substrate and therefore modulate the formation of A&#x3b2; peptides.

Dihydropteridinones I

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 spiroheterocycl-dihydropyrimidines, their use as modulators of &#x3b3;-secretase and to pharmaceutical compositions containing said compounds. In particular, the present invention relates to compounds which interfere with &#x3b3;-secretase and/or its substrate and therefore modulate the formation of A&#x3b2; peptides.

Dihydropteridinones II

The present invention relates to substituted amino-quinazolinones of general formula (I) wherein the groups Rto Rand A, are defined as in the specification and claims and the use thereof for the treatment of Alzheimer's disease (AD) and similar diseases. 

Substituted amino-quinazolinones, medicaments comprising said compound, their use and their method of manufacture

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 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

The invention relates to novel 1,6-disubstituted pyrazolopyrimidinones of formula (I), in which Hc is a tetrahydropyranyl-group and Ris the group V&#x2212;W&#x2212;*, 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.

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Mittelbiberach, Germany

Christian Eickmeier