Elbion Ag

Janssen Pharmaceuticals, Inc.

Biotie Therapies Corporation

Elbion Gmbh

Boehringer Ingelheim International Gmbh

Wyeth

Norbert Höfgen

Ute Egerland

Rudolf Schindler

Barbara Langen

Hans-Joachim Lankau

Hildegard Kuss

Emmanuel Polymeropoulos

Thomas Kronbach

Degenhard Marx

Rita Dost

Hans Stange

Simon Ward

Chris Rundfeldt

Stefan Szelenyi

Christian Grunwald

Helge Hartenhauer

Thorsten Hage

Michael Sotirios Malamas

Riccardo Giovannini

Sara Frattini

Hildegard Poppe

Sabine Heer

James Joseph Erdei

Barbara Bertani

Hans-Joachim Jänsch

Karin Steinike

Matthias Olbrich

Jürgen Schäfer

Yike Ni

Thomas Pfeifer

Antje Gasparic

Giustino Di Antonio

Stefan Szelényi

The invention relates to pyrazole derivatives which are NMDA NR2B receptor inhibitors, useful in treating central nervous system diseases.

Pyrazoles

Provided here in are compounds of Formula I having the structure: Also provided herein are compositions comprising compounds of Formula I and methods of using compounds of Formula I for the treatment of disorders, diseases or conditions mediated by GluN2B receptors.

Triazoles as NR2B receptor inhibitors

The invention relates to pyrazole derivatives which are NMDA NR2B receptor inhibitors, useful in treating central nervous system diseases. 

Provided here in are compounds of Formula I having the structure: Also provided herein are compositions comprising compounds of Formula I and methods of using compounds of Formula I for the treatment of disorders, diseases or conditions mediated by GluN2B receptors. 

The compounds are of the class of pyrido[3,2-e][1,2,4]-tiazolo[4,3-a]pyrazines, useful in the treatment of central nervous system disorders. A species illustrative of members of the class is the following: 

Substituted pyrido[3,2-E][1,2,4]-triazolo[4,3-A]pyrazines for the treatment of central nervous system disorders

The invention relates to substituted 7-azaindoles, process for their preparation, pharmaceutical preparations which comprise these compounds, and the pharmaceutical use of these compounds, which are inhibitors of phosphodiesterase 4, as active ingredients for the treatment of disorders which can be influenced by inhibition of phosphodiesterase 4 activity in particular in immunocompetent cells (e.g. macrophages and lymphocytes) by the compounds of the invention.

7-azaindoles and the use thereof as therapeutic agents

The invention relates to imidazo[1,5-a]quinoxaline derivatives having Formula IIa: to processes for preparing them, to pharmaceutical preparations which comprise these compounds and to the pharmaceutical use of these compounds, which are inhibitors of phosphodiesterase 10 (PDE10), as active compounds for treating central nervous system diseases of mammals, including humans.

Substituted imidazo[1,5-a]quinoxalines useful as inhibitors of phosphodiesterase 10 for the treatment of neurological and other disorders

7-azaindoles inhibit phosphodiesterase 4 (PDE4). Methods for preparing these compounds and methods of treating arthritis and other conditions with the compounds are also provided.

7-azaindoles, their use as inhibitors of phosphodiesterase 4, and a method for synthesizing them

The invention relates to pyrido[3,2-e]pyrazines, to processes for preparing them, to pharmaceutical preparations which comprise these compounds and to the pharmaceutical use of these compounds, which are inhibitors of phosphodiesterase 10, as active compounds for treating diseases of mammals including a human which can be influenced by using the compounds according to the invention to inhibit phosphodiesterase 10 activity in the central nervous system. More particularly, the invention relates to the treatment of neurologic and psychiatric disorders, for example psychosis and disorders comprising cognitive deficits as symptoms.

Pyrido[3,2-e]pyrazines, their use as inhibitors of phosphodiesterase 10, and processes for preparing them

7-azaindoles inhibit phosphodiesterase 4 (PDE4). Methods for preparing these compounds are also provided.

The invention relates to new 7-azaindoles, their use as inhibitors of phosphodiesterase 4 and to methods for their synthesis.

7-azaindoles, use thereof as phosphodiesterase 4 inhibitors and method for producing the same

The invention relates to substituted 4- or/and 7-hydroxyindoles, to processes for preparing them, to pharmaceutical preparations which comprise these compounds and to the pharmaceutical use of these compounds, which are inhibitors of phosphodiesterase 4, as active compounds for treating diseases which can be influenced by using the compounds according to the invention to inhibit phosphodiesterase 4 activity in immunocompetent cells (e.g. macrophages and lymphocytes).

Hydroxyindoles, their use as inhibitors of phosphodiesterase 4, and processes for preparing them

The invention relates to new hydroxyindoles of the Formula, their use as inhibitors of phosphodiesterase 4 and processes for their preparation.

Hydroxyindoles, their use as inhibitors of phosphodiesterase 4 and processes for their preparation

The invention relates to a process for preparing hydroxyindolylglyoxylamides in high yields and particularly pure form.

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Ottendorf-Okrilla, Germany

Norbert Höfgen