Abbvie Inc.

Abbvie Deutschland Gmbh and Co Kg

Abbott Laboratories Corporation

Abbott Gmbh & Co Kg

Yanbin Lao

Frauke Pohlki

Gisela Backfisch

Charles W Hutchins

Wilhelm Amberg

Udo Lange

Anil Vasudevan

Ying Wang

Jason T Brewer

Hongyu H Zhao

Huan-Qiu Li

Wilfried Hornberger

Andreas Kling

Helmut Mack

Katja Jantos

Marjoleen Nijsen

Philip R Kym

Valentino J Stella

Peter T Mayer

Eric A Voight

Xiaochun Lou

Ye Huang

Sean E Mackey

Achim Möller

Christopher P Miller

Brian P Enright

Liliane Unger

Andreas Haupt

Stevan Wakefield Djuric

Karla Drescher

Karsten M Wicke

Geoff G Zhang

Mark A Matulenko

Vincent S Chan

Justin D Dietrich

Ana-Lucia Relo

Min Zhang

Anton Bespalov

Zhi Wang

Barbara Vogg

Juergen Delzer

Irini Zanze

Russell C Klix

James Patrick Stambuli

Benoit Cardinal-David

Alexander D Huters

Scott W Krabbe

Rodger F Henry

Raimundo Ho

Kassibla E Dempah

James Stambuli

Jason Brewer

Justin Dietrich

Ying X Wang

The present disclosure relates to (a) carbidopa prodrugs, (b) pharmaceutical combinations and compositions comprising a carbidopa prodrug and/or an L-dopa prodrug, and (c) methods of treating Parkinson's disease and associated conditions comprising administering a carbidopa prodrug and an L-dopa prodrug to a subject with Parkinson's disease.

Methods of treating Parkinson's disease

Carbidopa and L-dopa prodrugs and methods of use

The present invention relates to pyrrolidine derivatives of the formula (I), or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such pyrrolidine derivatives, and the use of such pyrrolidine derivatives for therapeutic purposes. The pyrrolidine derivatives are GlyT1 inhibitors.

Pyrrolidine derivatives, pharmaceutical compositions containing them, and their use in therapy

The present invention relates to aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives, and the use of such aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives for therapeutic purposes. The aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives are GlyT1 inhibitors.

Aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives, pharmaceutical compositions containing them, and their use in therapy

The present invention relates to aminotetraline and aminoindane derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such aminotetraline and aminoindane derivatives, and the use of such aminotetraline and aminoindane derivatives for therapeutic purposes. The aminotetraline and aminoindane derivatives are GlyT1 inhibitors.

Aminotetraline and aminoindane derivatives, pharmaceutical compositions containing them, and their use in therapy

The present invention relates to 4,5-dihydropyrazole derivatives of the formula (I) and physiologically tolerated salts thereof which are GlyT1 inhibitors. The invention further relates to pharmaceutical compositions comprising such 4,5-dihydropyrazole derivatives, and the use of such 4,5-dihydropyrazole derivatives for therapeutic purposes.

4,5-dihydropyrazole derivatives, pharmaceutical compositions containing them, and their use in therapy

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 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 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. 

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Abbott Park, IL, United States of America

Yanbin Lao