Boehringer Ingelheim International Gmbh

Vitae Pharmaceuticals, Inc.

Boehringer Ingelheim Vetmedica Gmbh

Boehringer Ingelheim Pharmaceuticals, Inc.

Boehringer Ingelheim Pharma Gmbh & Co Kg

Ablynx N.v.

Cornelia Dorner-Ciossek

Klaus Fuchs

Niklas Heine

Riccardo Giovannini

Christian Eickmeier

Klaus Klinder

Stefan Hoerer

Gerhard Schaenzle

Sandra Handschuh

Dennis Fiegen

Thomas Fox

Holger Rosenbrock

Suresh B Singh

Lawrence Wayne Dillard

Jing Yuan

Yajun Zheng

Zhenrong Xu

Salvacion Cacatian

Lanqi Jia

Roland Pfau

Dieter Wiedenmayer

Shankar Venkatraman

Angelo Ceci

Angel Morales-Ramos

Yi Zhao

Lothar Kussmaul

Yuri Bukhtiyarov

Marcus Kostka

Deepak S Lala

Toon Laeremans

Gerald Beste

John Edward Park

Martin Lenter

Jonathan Timothy Reeves

Jo Vercammen

Georg Rast

Klaus Bornemann

Stefan Peters

Martin Hendrix

Guenter Trummlitz

Bernd Beck

Frank Sams-Dodd

Dagmar Kugler

Katharina Zimmermann

Pascal Merchiers

Frank Himmelsbach

Georg Dahmann

Hans Briem

Herbert Nar

Werner Stransky

Achim Sauer

Edward S Lazer

Pascal Gerard Merchiers

Clara K Miao

Ulrike Gross

Katja Fechteler

Katharina Zimmerman

Markus Kostka

Jonathan Reeves

Disclosed are 4-pyrazin-2-ylmethyl-morpholines of formula A and pharmaceutically acceptable salts thereof, wherein Rand Rare defined herein. Also disclosed are processes for their preparation, pharmaceutical compositions containing the compounds, and their use in therapy, particularly in the treatment or prevention of conditions having an association with NR2B negative allosteric modulating properties.

4-pyrazin-2-ylmethyl-morpholine derivatives and the use thereof as medicament

Disclosed are 4-pyridinylmethyl-morpholines of formula A and pharmaceutically acceptable salts thereof, wherein Rand Rare defined herein. Also disclosed are processes for their preparation, pharmaceutical compositions containing the compounds, and their use in therapy, particularly in the treatment or prevention of conditions having an association with NR2B negative allosteric modulating properties.

4-pyridinylmethyl-morpholine derivatives and the use thereof as medicament

Disclosed are 4-pyrimidin-5-ylmethyl-morpholines of formula A and pharmaceutically acceptable salts thereof, wherein Rand Rare defined herein. Also disclosed are processes for their preparation, pharmaceutical compositions containing the compounds, and their use in therapy, particularly in the treatment or prevention of conditions having an association with NR2B negative allosteric modulating properties.

4-pyrimidin-5-ylmethyl-morpholine derivatives and the use thereof as medicament

The present invention relates to imidazopyridines of formula A processes for their preparation, pharmaceutical compositions containing them and their use in therapy, particularly in the treatment or prevention of conditions having an association with NR2B negative allosteric modulating properties.

Imidazopyridine derivatives and the use thereof as medicament

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.

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 invention relates to biparatopic A-beta binding polypeptides and, more specifically, to biparatopic A-beta binding polypeptides comprising at least two immunoglobulin single variable domains binding to different epitopes of A-beta. The invention also relates to specific sequences of such polypeptides, methods of their production, and methods of using them, including methods of treatment of diseases such as Alzheimer's Disease.

A-beta binding polypeptides

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.

Compounds for the treatment of CNS disorders

Inhibitors of &#x3b2;-secretase

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.

Growing community of inventors

Warthausen, Germany

Cornelia Dorner-Ciossek