Janssen Pharmaceuticals, Inc.

Arzneimittelwerk Dresden Gmbh

Boehringer Ingelheim Vetmedica Gmbh

Boehringer Ingelheim International Gmbh

Arzneitmittelwerk Dresden G.m.b.h.

Hans-Joachim Lankau

Rita Dost

Klaus Unverferth

Barbara Langen

Ute Egerland

Norbert Höfgen

Chris Rundfeldt

Rudolf Schindler

Simon Ward

Christian Grunwald

Angelika Rostock

Wolfgang Loscher

Andrea Tipold

Thomas Arnold

Manfred Menzer

Reni Bartsch

Christine Tober

Hans Stange

Thorsten Hage

Riccardo Giovannini

Sara Frattini

Barbara Bertani

Vladimir G Granik

Giustino Di Antonio

Sofia Grizik

Norbert Hoefgen

Abgelika Rostock

Harry Schafer, Deceased

Ure Egerland

Karl Gewald

Wolfgang Loescher

Vladimir Granik

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 (1,2,4)triazolo[4,3-a]quinoxaline derivatives which are inhibitors of phosphodiesterase 2 and/or 10, useful in treating central nervous system diseases.

(1,2,4)triazolo[4,3-A]quinoxaline derivatives as inhibitors of phosphodiesterases

The present invention relates to the use of substituted dihydroimidazolones, particularly [1-(4-Chlorophenyl)-4-(4-morpholinyl)-2,5-dihydro-1H-imidazol-2-one] (AWD 131-138) or a physiologically acceptable salt thereof for the treatment of epilepsy in dogs.

Use of dihydroimidazolones for the treatment of dogs

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 1,5-dihydropyrrol-2-ones of Formula 1 which contain an aryl radical in the 1-position and a secondary amine radical in the 4-position, to a process for making and for a process to treat various forms of epilepsies and of states of anxiety and tension.

4-amino-1-aryl-1,5-dihydropyrrol-2-ones and process for making

Antiepileptic compounds of the formula ##STR1## wherein X is hydrogen, a C.sub.1-4 alkyl, C.sub.1-4 alkoxy, trifluoromethyl, trifluoromethoxy or halogen residue, A is an amino, C.sub.1-4 alkylamino, C.sub.1-4 dialkylamino, morpholino, piperidino or pyrrolidino residue, and n is a cardinal number from 0 to 5, and process for preparing the foregoing compounds and for their use as anticonvulsives.

4-amino-1-arylpyridin-2-ones and process for making

The invention relates to pyrazolo[3,4d]pyrimidin-4(5H)-ones and pyrazolo[3,4-d]pyrimidine-4(5H)-thiones and their tautomers and pharmaceutically acceptable salts, which contain a benzyl radical in the 2-position, processes for their preparation and their use as medicaments, in particular for the treatment of epilepsies of various forms and of allergic/asthmatic diseases.

Anticonvulsive and antiallergic/antiasthmatic

Compounds having anticonsulive activity, of the formula 1 ##STR1## in which X is hydrogen, a C.sub.1-4 -alkyl, C.sub.1-4 alkoxy, trifluoromethyl, or halogen residue, R.sup.1 and R.sup.2 are independently of each other C.sub.1-4 -alkyl, C.sub.2-4 hydroxyalkyl, cycloalkyl or heteroalkyl, or R.sup.1 and R.sup.2 are together a C.sub.2-6 alkylene reside in which a--CH.sub.2 --group is optionally replaced by oxygen, nitrogen or sulfur, m is 0 or 1, and n is 0 or a cardinal number from 1 to 5, and their pharmaceutically acceptable salts. The application also relates to a process for making the compound of formula (I).

Anticonvulsive 1-ar(alk)ylimidazolin-2-ones and process for making

Anticonvulsive compounds and compositions, of the formula ##STR1## in which X is a C.sub.1-4 -alkyl, trifluoromethyl, or halogen residue, Y is hydrogen or halogen, n is 0 or 1, and m is 0 or a cardinal number from 1 to 4, and its pharmacologically acceptable acid addition salts.

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Weinböhla, Germany

Hans-Joachim Lankau