Boehringer Ingelheim International Gmbh

Boehringer Ingelheim Pharma Gmbh & Co Kg

Thomas Fox

Dennis Fiegen

Christoph Hoenke

Peter Nickolaus

Pascale Pouzet

Rolf Goeggel

Riccardo Giovannini

Niklas Heine

Gerhard Schaenzle

Christian Eickmeier

Klaus Fuchs

Holger Rosenbrock

Cornelia Dorner-Ciossek

Klaus Klinder

Birgit Jung

Horst Dollinger

Ralf Anderskewitz

Domnic Martyres

Martin Hendrix

Matthias Grauert

Thorsten Lehmann-Lintz

Peter Eickelmann

Steffen Breitfelder

Marc Grundl

Frank Buettner

Wolfgang Rist

Remko Alexander Bakker

Cornelia Dornier-Ciossek

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

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 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 present invention relates to pyridazinone derivatives of general formula I, wherein the groups A, G and Rare as defined in the application, the tautomers thereof, stereoisomers thereof, the mixtures thereof and the salts thereof, which have valuable pharmacological properties, and in particular bind to the GPR119 receptor and modulate its activity. 

Benzoxazole- and tetrahydrobenzoxazole-substituted pyridazinones as GPR119 agonists

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

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.

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.

Dihydrothienopyrimidines for the treatment of inflammatory diseases

The invention relates to the novel dihydrothienopyrimidine sulfoxides of formula (I) and to the pharmacologically acceptable salts thereof, wherein X represents SO or SO, preferably however SO, and wherein R, R, R, R, Rand Rare defined as in claim. The invention also relates to pharmaceutical compositions containing said compounds. The novel dihydrothienopyrimidine sulfoxides are suitable for use in the treatment of respiratory or gastrointestinal disorders or diseases, inflammatory diseases of the joints, the skin or the eyes, diseases of the peripheral or central nervous system or cancers. 

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Biberach, Germany

Thomas Fox