Boehringer Ingelheim International Gmbh

Vitae Pharmaceuticals, Inc.

Boehringer Ingelheim Pharma Kg

Boehringer Ingelheim Pharma Gmbh & Co Kg

Klaus Fuchs

Cornelia Dorner-Ciossek

Niklas Heine

Christian Eickmeier

Riccardo Giovannini

Suresh B Singh

Lawrence Wayne Dillard

Jing Yuan

Zhenrong Xu

Yajun Zheng

Salvacion Cacatian

Lanqi Jia

Shankar Venkatraman

Angel Morales-Ramos

Gerhard Schaenzle

Dennis Fiegen

Thomas Fox

Holger Rosenbrock

Sandra Handschuh

Klaus Klinder

Yi Zhao

Yuri Bukhtiyarov

Deepak S Lala

David A Claremon

Katerina Leftheris

Jonathan Timothy Reeves

Stefan Hoerer

Georg Rast

Guosheng Wu

Zhongren Wu

Brian McKeever

Hans Briem

Stefan Peters

Martin Hendrix

Holger Wagner

Werner Stransky

Ruediger Streicher

Marcus Kostka

Daniela Berta

Katja Fechteler

Frank Himmelsbach

Matthias Grauert

Dieter Wolfgang Hamprecht

Ingo Konetzki

Herbert Nar

Helmut Ensinger

Wolfram Gaida

Thomas Trieselmann

Achim Sauer

Thomas Weiser

Adrian Carter

Klaus Bornemann

Ulrike Gross

Alessandro Mazzacani

Klaus Mendla

Cornelia Dornier-Ciossek

Helmut Michael Romig

Markus Kostka

Helmut Romig

Jonathan Reeves

Brian Mckeever

The present invention is directed to a compound represented by the following structural formula or a pharmaceutically acceptable salt thereof. Pharmaceutical compositions and method of use of the compounds are also described.

Inhibitors of beta-secretase

The present invention relates to spirocyclic acylguanidines and their use as inhibitors of the &#x3b2;-secretase enzyme (BACE1) activity, pharmaceutical compositions containing the same, and methods of using the same as therapeutic agents in the treatment of neurodegenerative disorders, disorders characterized by cognitive decline, cognitive impairment, dementia and diseases characterized by production of &#x3b2;-amyloid aggregates.

The present invention relates to spirocyclic acylguanidines and their use as inhibitors of the&#x3b2;-secretase enzyme (BACE1) activity, pharmaceutical compositions containing the same, and methods of using the same as therapeutic agents in the treatment of neurodegenerative disorders, disorders characterized by cognitive decline, cognitive impairment, dementia and diseases characterized by production of &#x3b2;-amyloid aggregates.

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 compounds defined by formula I wherein the variables R-Rare defined as in the description, possessing valuable pharmacological activity. Particularly, the compounds are inhibitors of cholesterol ester transfer protein (CETP) and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme.

Tricyclic pyridine derivatives, medicaments containing such compounds, their use and process for their preparation

Inhibitors of &#x3b2;-secretase

Compounds of formula (I) wherein the groups R1 to R8 have the meanings indicated in the description, the tautomers, the stereoisomers, the mixtures thereof and the salts thereof have valuable pharmacological properties, which make them useful for the treatment of cardiovascular and related disorders. 

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

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Mittelbiberach, Germany

Klaus Fuchs