Abb Vie Deutschland Gmbh & Co. Kg

Abbvie Inc.

Abbott Gmbh & Co Kg

Basf Aktiengesellschaft

Abbott Laboratories Corporation

Abbvie Deutschland Gmbh and Co Kg

Helmut Mack

Wilfried Hornberger

Andreas Kling

Werner Seitz

Achim Moeller

Katja Jantos

Thomas Pfeiffer

Thomas Zierke

Gisela Backfisch

Margaretha Henrica Maria Bakker

Andreas Haupt

Charles W Hutchins

Udo Lange

Anil Vasudevan

Stefan Koser

Wilfried Martin Braje

Karla Drescher

Ana Lucia Relo

Viktor Lakics

Carolin Hoft

Wilfried Lubisch

Sean Colm Turner

Adrian Hobson

Nicole Teusch

Yanbin Lao

Volker Nimmrich

Marjoleen Nijsen

Hans Wolfgang H&ouml;ffken

Hannes Koolman

Dorit Baucke

Dietmar Seemann

Achim Möller

Hans-Joachim Bohm

Steven Lewis Swann, Jr

Thomas Dale Penning

Stevan Wakefield Djuric

Julie M Miyashiro

Bryan K Sorensen

Todd M Hansen

Michael Michaelides

Kevin R Woller

Alan Frank Gasiecki

Keith W Woods

Jyoti R Patel

Marina Pliushchev

Daryl Richard Sauer

Qi Shuai

Irini Akritopoulou-Zanze

Ramzi Farah Sweis

Ryan G Keddy

Martin Schmidt

Kathy A Sarris

Howard Robin Heyman

Douglas M Kalvin

Biqin C Li

Marcel Van Gaalen

Lu Wang

Dawn M George

Brian D Wakefield

Melissa J Michmerhuizen

Dominique Bonafoux

Vijaya J Gracias

Omar J Shah

Andrew J Long

Chris Tse

Michael F Jarvis

Margaretha Bakker

Eric F Johnson

Peter J Kovar

Günter Blaich

Thomas Erhard

Anna Linsenmeier

Hans-Joachim B&ouml;hm

George A Doherty

Gerd Steiner

Andrew O Stewart

Hervé Geneste

Karsten M Wicke

Richard F Clark

Thomas Subkowski

Heinz Hillen

Irene I Drizin

Pramila A Bhatia

Richard J Perner

Bernhard K Mueller

Michael L Curtin

Reinhold Mueller

Friedhelm Balkenhohl

Hans Wolfgang Höffken

Hans Wolfgang Hoeffken

Arnulf Lauterbach

Volker Laux

Barbara Vogg

Juergen Delzer

Uta Holzenkamp

Armin Beyerbach

Johann-Christian Zechel

Claudia Isabella Graef

Jens Sadowski

Qingwei Zhang

The present invention relates to tricyclic quinoline and quinoxaline derivatives, to a pharmaceutical composition containing such compounds, to their use as modulators, especially agonists or partial agonists, of the 5-HTreceptor, their use for preparing a medicament for the prevention or treatment of conditions and disorders which respond to the modulation of 5-HTreceptor, and to a method for preventing or treating conditions and disorders which respond to the modulation of 5-HTreceptor.

Tricyclic quinoline and quinoxaline derivatives

Disclosed are isoindoline carboxamide, dihydropyrrolopyridine carboxamide, and dihydropyrrolopyrimidine carboxamide compounds which inhibit the activity of NAMPT, compositions containing the compounds and methods of treating diseases during which NAMPT is expressed. Disclosed are isoindoline carboxamide, dihydropyrrolopyridine carboxamide, and dihydropyrrolopyrimidine carboxamide compounds which inhibit the activity of ROCK, compositions containing the compounds and methods of treating diseases during which ROCK is expressed.

NAMPT and ROCK inhibitors

The present invention relates to compound of formula (I) as tricyclic hexahydrodiazepinoquinolines carrying a cyclic substituent, useful for modulating the 5-HTreceptor and preventing and/or treating conditions and disorders that respond to the modulation of the 5-HTreceptor. The present invention also relates to methods for producing compounds of formula (I), pharmaceutical compositions containing such compounds, and methods for preventing or treating conditions and disorders that respond to the modulation of the 5-HTreceptor by administering compounds of formula (1) or pharmaceutical compositions thereof.

Substituted [1,4]diazepino[6,7,1-ij]quinolines as serotonin 5-HT2C receptor modulators

The present invention relates to novel carboxamide compounds and their use as a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity and to a method for the therapeutic and/or prophylactic treatment by administering an effective amount of at least one of these carboxamide compounds. The carboxamide compounds are compounds of the general formula I in whichW&#x2014;Ris selected from and R, R, R, R, Y, Y, Y, Y, X, Q, m, k, Rand Rhave the meanings mentioned in the claims, the tautomers thereof and the pharmaceutically suitable salts thereof. Of these compounds those are preferred wherein Y, Y, Yand Yare CR, or one or two of the variables Yto Yare a nitrogen atom and the remaining variables are CR, wherein the radicals Rmay be identical or different and have the meanings mentioned in the claims.

Carboxamide compounds and their use as calpain inhibitors

The present invention relates to novel heterocyclic compounds of formula I wherein the variables are as defined in the claims or the description, which are useful for inhibiting glycogen synthase kinase 3 (GSK-3), compositions containing the compounds, their use for preparing a medicament for the treatment of a medical disorder susceptible to the treatment with a compound that modulates, preferably inhibits, the activity of glycogen synthase kinase 3&#x3b2;, and methods of treatment of medical disorders susceptible to treatment with a compound that modulates glycogen synthase kinase 3&#x3b2; activity using the compounds.

Heterocyclic compounds and their use as glycogen synthase kinase-3 inhibitors

The present invention relates to tricyclic hexahydrodiazepinoquinolines, such as compounds of formula (I), carrying a substituted alkyl radical, to a method for producing them, to a pharmaceutical composition containing such compounds, to their use as modulators, especially agonists or partial agonists, of the 5-HTreceptor, their use for preparing a medicament for the prevention or treatment of conditions and disorders which respond to the modulation of 5-HTreceptor, to a method for preventing or treating conditions and disorders which respond to the modulation of 5-HTreceptor, and processes for preparing such compounds and compositions. 

Hexahydrodiazepinoquinolines carrying a substituted alkyl radical

The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity. The carboxamide compounds are compounds of the general formula I in which R, R, R, R, R, Q, Y, A and X have the meanings mentioned in the claims and the description, the tautomers thereof and the pharmaceutically suitable salts thereof. In particular, the compounds have the general formula Ia and Ib in which R, r, R, R, R, R, Y and X have the meanings mentioned in the claims, including the tautomers thereof and the pharmaceutically suitable salts thereof. Of these compounds those are preferred wherein Y is a moiety CH&#x2014;CH, CH&#x2014;CH&#x2014;CH, N(R)&#x2014;CH, N(R)&#x2014;CH&#x2014;CHor CH&#x2550;CH&#x2014;CH&#x2550;, each optionally having 1 or 2H-atoms replaced with identical or different radicals R, wherein Rand Rhave the meanings mentioned in the claims.

Disclosed are 1,3-dihydro-2H-isoindole compounds which inhibit the activity of NAMPT, compositions containing the compounds and methods of using the compounds to treat diseases during which NAMPT is expressed, e.g., cancer, metabolic disorders, and inflammatory disorders. Disclosed are 1,3-dihydro-2H-isoindole compounds which inhibit the activity of ROCK, compositions containing the compounds and methods of using the compounds to treat diseases during which ROCK is expressed, e.g., cancer, cardiovascular disorders, and inflammatory disorders.

NAMPT and rock inhibitors

The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein A, R, R, Rand m, are defined in the description. The present invention relates also to methods of making said compounds, and compositions containing said compounds which are useful for inhibiting kinases such as Glycogen Synthase kinase 3 (GSK-3), Rho kinase (ROCK), Janus Kinases (JAK), Cdc7, AKT, PAK4, PLK, CK2, KDR, MK2, JNK1, aurora, pim 1 and nek 2.

5-substituted indazoles as kinase inhibitors

The present invention relates to novel carboxamide compounds of the formula I and their use for the manufacture of a medicament. The carboxamide compounds are prodrugs of inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity.  

The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity. The carboxamide compounds are compounds of the general formula (I) in which R, Rand n have the meanings mentioned in the claims and the description, Y is a radical of the formulae (Y1) or (Y2) where # indicates the point of attachment of Y to the pyridine ring, R, R, R, Rand m have the meanings mentioned in the claims and the description, A is (CH)with p being 1, 2, 3 or 4, where one or two hydrogen atoms may be replaced by a radical R, where A is attached to the 3- or 4-position of the pyrazole radical and Rhas the meaning mentioned in the claims and the description; Ais (CH)q with q being 0, 1, 2 or 3, where one or two hydrogen atoms may be replaced by halogen or C-C-alkyl; and Ais (CH)r with r being 0, 1, 2 or 3, where one or two hydrogen atoms may be replaced by halogen or C-C-alkyl, provided that that r+q is 2, 3, 4, 5 or 6; their tautomers, the hydrates thereof, the pharmaceutically suitable salts of the carbox-amide compounds (I), the prodrugs of (I) and the pharmaceutically suitable salts of the prodrugs, tautomers or hydrates of (I). 

Carboxamide compounds and their use as calpain inhibitors V

The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity. The carboxamide compounds are compounds of the general formula I in which R, R, R, R, W, Y and X have the meanings mentioned in the claims and the description, the tautomers thereof and the pharmaceutically suitable salts thereof. In particular, the compounds have the general formula I-A.a' and I-A.a&#x2033; in which m, E, R, R, R, R, R, Rand Rhave the meanings mentioned in the claims, n is 0, 1 or 2, the tautomers thereof and the pharmaceutically suitable salts thereof.

The present invention relates to novel heterocyclic compounds of formula I wherein the variables are as defined in the claims or the description,which are useful for inhibiting glycogen synthase kinase 3 (GSK-3), compositions containing the compounds, their use for preparing a medicament for the treatment of a medical disorder susceptible to the treatment with a compound that modulates, preferably inhibits, the activity of glycogen synthase kinase 3&#x3b2;, and methods of treatment of medical disorders susceptible to treatment with a compound that modulates glycogen synthase kinase 3&#x3b2; activity using the compounds.

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Ludwigshafen, Germany

Helmut Mack