Abbott Gmbh & Co Kg

Abbvie Deutschland Gmbh and Co Kg

Abbott Laboratories Corporation

Abbvie Inc.

Gisela Backfisch

Andreas Haupt

Karla Drescher

Helmut Mack

Liliane Unger

Wilfried Hornberger

Yanbin Lao

Andreas Kling

Wilfried Martin Braje

Barbara Vogg

Juergen Delzer

Karsten M Wicke

Frauke Pohlki

Katja Jantos

Ana-Lucia Relo

Min Zhang

Marjoleen Nijsen

Anton Bespalov

Armin Beyerbach

Sean Colm Turner

Achim Möller

Wilfried Lubisch

Roland Grandel

Margaretha Henrica Maria Bakker

Ana Lucia Relo

Christophe Henry

Viktor Lakics

Günter Blaich

Thomas Erhard

Anna Linsenmeier

Raimund Peter

Werner Seitz

Achim Moeller

Hannes Koolman

Dorit Baucke

Xiaona Zhao

Jincheng Wang

Lynette Smyth

Jürgen Delzer

John Darbyshire

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 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 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.  

Carboxamide compounds and their use as calpain inhibitors

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, X, m and n have the meanings mentioned in the claims and the description, the tautomers thereof, the hydrates thereof and the pharmaceutically suitable salts thereof. Of these compounds those are preferred wherein Ris optionally substituted benzyl or hetaryl-methyl, X is a single bond or an oxygen atom, Ris C-C-alkyl, C-C-haloalkyl, C-C-alkenyl, C-C-cycloalkyl, C-C-cycloalkyl-C-C-alkyl, C-C-heterocycloalkyl-C-C-alkyl, phenyl, phenyl-C-C-alkyl, pyridin-2-yl-C-C-alkyl or CH&#x2014;C(O)OCH, Rand Rindependently of one another are halogen, CN, CF, CHF, CHF, C-C-alkyl or C-C-alkoxy, and m and n independently of one another are 0 or 1. 

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, RR, R, m and n have the meanings mentioned in the claims and the description, the tautomers thereof, the hydrates thereof and the pharmaceutically suitable salts thereof. Of these compounds those are preferred wherein Ris optionally substituted phenyl-C-C-alkyl or hetaryl-C-C-alkyl, Ris optionally substituted aryl, hetaryl, aryl-C-C-alkyl, aryl-C-C-alkenyl or hetaryl-C-C-alkyl, Ris C-C-alkyl, C-C-haloalkyl, C-C-alkenyl, C-C-cycloalkyl, C-C-cycloalkyl-C-C-alkyl, or phenyl-C-C-alkyl, Rand Rindependently of one another are halogen, CF, CHF, CHF, C-C-alkyl or C-C-alkoxy, and m and n independently of one another are 0 or 1.

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, RR, R, m and n have the meanings mentioned in the claims and the description, the tautomers thereof, the hydrates thereof and the pharmaceutically suitable salts thereof. Of these compounds those are preferred wherein Ris optionally substituted phenyl-C-C-alkyl or hetaryl-C-C-alkyl, Ris optionally substituted aryl, hetaryl, aryl-C-C-alkyl, aryl-C-C-alkenyl or hetaryl-C-C-alkyl, Ris C-C-alkyl, C-C-haloalkyl, C-C-alkenyl, C-C-cycloalkyl, C-C-cycloalkyl-C-C-alkyl, C-C-heterocycloalkyl-C-C-alkyl, phenyl-C-C-alkyl, pyridin-2-yl-C-C-alkyl or 1,3-benzoxazol-2-yl-methyl, Rand Rindependently of one another are halogen, CF, CHF, CHF, C-C-alkyl or C-C-alkoxy, and m and n independently of one another are 0 or 1.

Carboxamide compounds and their use as calpain inhibitors IV

The invention relates to compounds of the formula (I) wherein n is 0, 1 or 2; G is CHor CHR; Ris H, C,-C-alkyl, C,-C-alkyl substituted by C-C-cycloalkyl, C-C-hydroxyalkyl, fluorinated C,-C-alkyl, C-C-cycloalkyl, fluorinated C-C-cycloalkyl, C-Calkenyl, fluorinated C-C-alkenyl, formyl, acetyl or propionyl; R, Rand Rare, independently of each other, H, methyl, fluoromethyl, difluoromethyl, or trifluoromethyl; A is phenylene, pyridylene, pyrimidylene, pyrazinylene, pyridazinylene or thiophenylene, which can be substituted by one or more substituents selected from halogen, methyl, methoxy and CF; E is NRor CH, wherein Ris H or C-C-alkyl; Ar is a cyclic radical selected from the group consisting of phenyl, a 5- or 6-membered heteroaromatic radical comprising as ring members 1, 2 or 3 heteroatoms selected from N, O and S and a phenyl ring fused to a saturated or unsaturated 5- or 6-membered carbocyclic or heterocyclic ring, where the heterocyclic ring comprises as ring members 1, 2 or 3 heteroatoms selected from N, O and S and/or 1, 2 or 3 heteroatom-containing groups each independently selected from NR, where Ris H, C-C-alkyl, fluorinated C-C-alkyl, C-Calkylcarbonyl or fluorinated C-C-alkylcarbonyl, and where the cyclic radical Ar may carry 1, 2 or 3 substituents R, wherein the variable Rhas the meanings given in the claims and in the description; and physiologically tolerated acid addition salts thereof. The invention also relates to the use of a compound of the formula I or a pharmaceutically acceptable salt thereof for preparing a pharmaceutical composition for the treatment of a medical disorder susceptible to treatment with a dopamine D3 receptor ligand. 

Heterocyclic compounds suitable for treating disorders that respond to modulation of the dopamine D3 receptor

The present invention relates to novel benzenesulfonanilide compounds of the formulae I and I' and physiologically tolerated acid addition salts and the N-oxides thereof. The compounds possess valuable therapeutic properties and are particularly suitable, for treating diseases that respond to modulation of the serotonin 5-HTreceptor. 

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The present invention relates to N-phenyl-(piperazinyl or homopiperazinyl)-benzenesulfonamide or benzenesulfonyl-phenyl-(piperazine or homopiperazine) compounds, pharmaceutical compositions containing them, and their use in therapy. The compounds possess valuable therapeutic properties and are particularly suitable for treating diseases that respond to modulation of the serotonin 5-HTreceptor.

N-phenyl-(piperazinyl or homopiperazinyl)-benzenesulfonamide or benzenesulfonyl-phenyl-(piperazine or homopiperazine) compounds suitable for treating disorders that respond to modulation of the serotonin 5-HT6 receptor

The invention relates to compounds of the formula I: wherein The invention also relates to a pharmaceutical composition that comprises at least one triazole compound of the formula I and/or at least one physiologically tolerated acid addition salt thereof, and further to a method for treating disorders that respond beneficially to dopamine Dreceptor antagonists or dopamine Dagonists, said method comprising administering an effective amount of at least one triazole compound or physiologically tolerated acid addition salt of the formula I to a subject in need thereof.

The present invention relates to N-phenyl-(piperazinyl or homopiperazinyl)-benzenesulfonamide or benzenesulfonyl-phenyl-(piperazine or homopiperazine) compounds, pharmaceutical compositions containing them, and their use in therapy. The compounds possess valuable therapeutic properties and are particularly suitable for treating diseases that respond to modulation of the serotonin 5-HTreceptor. 

The invention relates to compounds of the formula (I). The invention also relates to the use of a compound of the formula I or a pharmaceutically acceptable salt thereof for preparing a pharmaceutical composition for the treatment of a medical disorder susceptible to treatment with a dopamine D3 receptor ligand. The invention also relates to the use of a compound of the formula I or a pharmaceutically acceptable salt thereof for preparing a pharmaceutical composition for the treatment of a medical disorder susceptible to treatment with a dopamine D3 receptor ligand.

The present invention relates to prodrugs of pharmacologically active five-membered heterocyclic amidines from which are produced in vivo compounds which are competitive inhibitors of trypsin-like serine proteases, in particular thrombin and kininogenases such as kallikrein, to the preparation thereof and to the use thereof as medicines. The invention also relates to pharmaceutical compositions which comprise the prodrugs of the active compounds as ingredients, and to the use of the compounds as thrombin inhibitors, anticoagulants and as antiinflammatory agents.

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Ludwigshafen, Germany

Gisela Backfisch