Abb Vie Deutschland Gmbh & Co. Kg

Abbvie Inc.

Abbott Gmbh & Co Kg

Abbott Laboratories Corporation

Abbvie Deutschland Gmbh and Co Kg

Katja Jantos

Wilfried Hornberger

Andreas Kling

Hervé Geneste

Helmut Mack

Charles W Hutchins

Marcel Van Gaalen

Achim Moeller

Loic Laplanche

Wilfried Martin Braje

Karla Drescher

Berthold Behl

Michael Ochse

Gisela Backfisch

Yanbin Lao

Marjoleen Nijsen

Jürgen Dinges

Clarissa Jakob

Achim Möller

Jayne Froggett

Liliane Unger

Sean Colm Turner

Lawrence A Black

Herve Geneste

Mario Mezler

Margaretha Henrica Maria Bakker

Silke Weber

Wilfred Braje

Claudia Krack

The present invention relates to novel carboxamide compounds, pharmaceutical compositions containing them, and their use in therapy. The compounds possess valuable therapeutic properties and are particularly suitable for treating or controlling medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders.

Inhibitor compounds of phosphodiesterase type 10A

The present invention relates to novel substituted oxindole derivatives of formula (I) wherein the variables are as defined in the claims and description; to pharmaceutical compositions comprising them, and to their use for the treatment of vasopressin-related disorders. 

Oxindole derivatives carrying an amine-substituted piperidyl-acetidinyl substituent and use thereof for treating vasopressine-related diseases

The present invention relates to novel substituted oxindole derivatives of formula (I) wherein the variables are as defined in the claims and description; to pharmaceutical compositions comprising them, and to their use for treatment of vasopressin-related disorders. 

Oxindole derivatives carrying a piperidyl-substituted azetidinyl substituent and use thereof for treating vasopressine-related diseases

The present invention relates to compounds which are inhibitors of phosphodiesterase type 10A and to their use for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders.

The present invention relates to novel substituted oxindole derivatives of the formula I wherein A is a ring selected from phenyl and 6-membered hetaryl containing 1 or 2 nitrogen atoms as ring members, where ring A carries one substituent Rand optionally one substituent R; B is a ring selected from phenyl and a monocyclic or bicyclic heteroaromatic ring containing 1, 2 or 3 heteroatoms selected from O, N and S as ring members, where ring B may carry 1, 2 or 3 substituents R; X, X, Xand X, independently of each other, are selected from &#x2014;CH&#x2014;, &#x2014;O&#x2014;, &#x2014;S(O)&#x2014;, &#x2014;NH&#x2014;, &#x2014;C(O)&#x2014;, &#x2014;CHCH&#x2014;, &#x2014;CHO&#x2014;, &#x2014;OCH&#x2014;, &#x2014;S(O)CH&#x2014;, &#x2014;CHS(O)&#x2014;, CHNH&#x2014;, &#x2014;NHCH&#x2014;, &#x2014;CHC(O)&#x2014; and C(O)CH&#x2014;; The present invention also relates to pharmaceutical compositions comprising the novel substituted oxindole derivatives of the formula I, and to their use for the treatment of vasopressin-related disorders.

Oxindole compounds carrying a nitrogen-bound spiro substituent and use thereof for treating vasopressin-related diseases

The present invention relates to novel substituted oxindole derivatives of formula (I), pharmaceutical compositions comprising them, and their use for the treatment of vasopressin-related disorders. 

Oxindole derivatives carrying an oxetane substituent and use thereof for treating vassopressin-related diseases

The present invention relates to novel compounds of the formula I which are inhibitors of phosphodiesterase type 10A and to their use for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders.  

Substituted furo[3,2-c]pyridines, thieno[3,2-c]pyridines, thieno[2,3-d]pyridazines and pyrido[3,4-d]pyridazines as phosphodiesterase type 10A inhibitors

The present invention relates to novel fused heterocyclic or carbocyclic compounds of formula I wherein the variables are as defined in the claims and the description. The invention further relates to pharmaceutical compositions comprising these compounds, and to their use for the treatment of vasopressin-related disorders.

Fused heterocyclic or carbocyclic compounds carrying a substituted cycloaliphatic radical and use thereof for treating vasopressin-related diseases

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 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.

The present invention relates to novel substituted oxindole derivatives of formula I wherein the variables are as defined in the claims and the description. The invention further relates to pharmaceutical compositions comprising compounds I and their use for the treatment of vasopressin-related disorders.

Oxindole compounds carrying a CO-bound spiro substituent and use thereof for treating vasopressin-related diseases

The present invention relates to novel substituted oxindole derivatives of formula (I), pharmaceutical compositions comprising them, and their use for the treatment of vasopressin-related disorders 

Oxindole derivatives carrying an oxetane substituent and use thereof for treating vasopressine-related diseases

The present invention relates to compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof:  In formula I the variables X1 is CH or N, X2 is O or S and where R1, R2, R3, R4 and Q are as defined in the claims. The compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof are inhibitors of phosphodiesterase type 10A. Thus, the invention also relates to the use of the compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders.

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. 

Growing community of inventors

Ludwigshafen, Germany

Katja Jantos