Janssen Pharmaceuticals, Inc.

Arzneimittelwerk Dresden Gmbh

Elbion Gmbh

Wyeth

Biotie Therapies Corporation

Elbion Ag

Rudolf Schindler

Ute Egerland

Norbert Höfgen

Barbara Langen

Hans-Joachim Lankau

Rita Dost

Simon Ward

Kay Brune

Chris Rundfeldt

Hildegard Poppe

Hildegard Kuss

Hans Stange

Christian Grunwald

Karin Steinike

Thorsten Hage

Norbert Hofgen

Matthias Olbrich

Michael Sotirios Malamas

Istvan Szelenyi

Ilona Fleischhauer

James Joseph Erdei

Norbert H&ouml;fgen

Nobert Höfgen

Yike Ni

Thomas Pfeifer

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 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

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

The invention relates to 1,2,5-trisubstituted 1,2-dihydroindazol-3-ones of formula (I)

1,2,5-trisubstituted 1,2-dihydroindazol-3-ones having anti-asthmatic, anti-allergic, anti-inflammatory, immunomodulating and neuroprotective action, process for their preparation and their use as medicaments

The invention relates to 1,5- and 3-O-substituted 1H-indazoles of formula (I) ##STR1##

1,5- and 3-O-substituted 1H-indazoles having anti-asthmatic,

1,3,5-trisubstituted indazole derivatives of the formula ##STR1## wherein R1 is H, (b) a C.sub.1-6 straight or branched, substituted or unsubstituted alkyl residue, (c) a C.sub.3-7 cycloalkyl residue, (d) an unsustituted or substituted phenyl, naphthyl, anthranyl, or fluorenyl residue, (e) a quinolin-2-ylmethoxy, or pyridin-2-ylmethoxy residue; X is O, or a --NH, --NH--(C.dbd.O)--NH--, --NH--(C.dbd.O)--O--, --NH--(C.dbd.O)--, or --NH--CH.sub.2 --(C.dbd.O)-- residue; Y is O, or S; R.sub.2 is H; Z is a SO, SO.sub.2, --(CH.sub.2).sub.p --, --(CH.sub.2).sub.p --O--, --O--(CH.sub.2).sub.p --, --(CH.sub.2).sub.p --(C.dbd.O)--, --(C.dbd.O)--(CH.sub.2).sub.p --, --(CH.sub.2).sub.p --(C.dbd.O)--NH--, --NH--(C.dbd.O)--(CH.sub.2).sub.p --, --(CH.sub.2).sub.p --CHOH--, --CHOH--(CH.sub.2).sub.p --, --(CH.sub.2).sub.p --CH.dbd.CH--, or --CH.dbd.CH--(CH.sub.2).sub.p -- residue, wherein p is between 1 and 6; A is a phenyl, naphthyl, anthranyl, fluorenyl, thiophenyl, pyridinyl, isoxazolyl, benzimidazolyl, benz�1,3!dioxolyl, pyrimidyl, pyrimidine-2,4-dionyl, quinolinyl, quinoxazolinyl, morpholinyl, or pyrrolidinyl residue; and, R.sub.3, R.sub.4, and R.sub.5, the same or different, are defined in the specification; and pharmaceutically acceptable salts, stereoisomers, racemates, racemic modifications, and enantiomers thereof. The invention also relates to specific compounds, processes for preparing and for treating an allergic, asthmatic, inflamed condition of a host, or for modulating the immune system of a host.

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Dresden, Germany

Rudolf Schindler