Janssen Pharmaceutica Nv

Alain Philippe Poncelet

Bruno Schoentjes

Sophie Philippe Coupa

Lieven Meerpoel

Frans E Janssens

Jean Fernand Armand Lacrampe

Christophe Meyer

Joannes Theodorus Maria Linders

Julien Georges Pierre-Olivier Doyon

Luc Van Hijfte

Luc August Laurentius Ver Donck

Yvan René Ferdinand Simonnet

Bruno Giethlen

Dominique Jean-Pierre Mabire

Camille Georges Wermuth

Anne Simone Josephine Lesage

Jean-Marie Contreras

Muriel Joubert

Marc Gaston Venet

Pierre-Henri Storck

Virginie Sophie Poncelet

Carina Leys

Delphine Yvonne Raymonde Lardeau

Marc Venet Gaston

Frans Eduard Jenssens

The present invention relates to a compound of formula (I) including any stereochemically isomeric form thereof, wherein the substituents are as defined in the specification and the claims; a N-oxide thereof, a pharmaceutically acceptable salt thereof or a solvate thereof; or a pharmaceutically acceptable salt thereof. The claimed compounds are useful for the treatment of a disease, the treatment of which is affected, mediated or facilitated by activating the GHS1A-r receptor. The invention also relates to pharmaceutical compositions thereof and processes for the preparation thereof.

Benzocycloheptane and benzoxepine derivatives

The present invention provides compounds of formula (I), their use as an inhibitor of a p53-MDM2 interaction as well as pharmaceutical compositions comprising said compounds of formula (I). 

Substituted phenylenediamines as inhibitors of the interaction between MDM2 and P53

The present invention relates to a compound of formula (I) including any stereochemically isomeric form thereof, wherein the substituents are as defined in the specification and the claims; a N-oxide thereof, a pharmaceutically acceptable salt thereof or a solvate thereof;  The claimed compounds are useful for the treatment of a disease, the treatment of which is affected, mediated or facilitated by activating the GHS1A-r receptor. The invention also relates to pharmaceutical compositions thereof and processes for the preparation thereof.

This invention concerns substituted diaza-spiro-[4.4]-nonane derivatives having neurokinin antagonistic activity, in particular NK1 antagonistic activity, their preparation, compositions comprising them and their use as a medicine, in particular for the treatment and/or prophylaxis of schizophrenia, emesis, anxiety and depression, irritable bowel syndrome (IBS), circadian rhythm disturbances, pre-eclampsia, nociception, pain, in particular visceral and neuropathic pain, pancreatitis, neurogenic inflammation, asthma, chronic obstructive pulmonary disease (COPD) and micturition disorders such as urinary incontinence. The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in claim. 

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The present invention provides compounds of formula (I), their use as an inhibitor of a p53-MDM2 interaction as well as pharmaceutical compositions comprising said compounds of formula (I) wherein n, m, p, t, R, R, R, R, R, R, R, Q, Y and Z have defined meanings.

Cyclic-alkylamine derivatives as inhibitors of the interaction between MDM2 and P53

The present invention relates to a compound of formula (I) including any stereochemically isomeric form thereof, wherein the substituents are as defined in the specification and the claims; a N-oxide thereof, a pharmaceutically acceptable salt thereof or a solvate thereof;provided that the compound is other than or a pharmaceutically acceptable salt thereof. The claimed compounds are useful for the treatment of a disease, the treatment of which is affected, mediated or facilitated by activating the GHS1A-r receptor. The invention also relates to pharmaceutical compositions thereof and processes for the preparation thereof.

The present invention provides compounds of formula (I), their use as an inhibitor of a p53-MDM2 interaction as well as pharmaceutical compositions comprising said compounds of formula (I) wherein n, m, p, s, t, R, R, A and Z have defined meanings.

Inhibitors of the interaction between MDM2 and P53

This invention concerns substituted oxa-diaza-spiro-[5.5]-undecanone derivatives having neurokinin antagonistic activity, in particular an NKantagonistic activity, an NKantagonistic activity, a combined NK/NKantagonistic activity and a combined NK/NK/NKantagonistic activity, their preparation, compositions comprising them and their use as a medicine, in particular for the treatment and/or prophylaxis of schizophrenia, emesis, anxiety and depression, irritable bowel syndrome (IBS), circadian rhythm disturbances, pre-eclampsia, nociception, pain, in particular visceral and neuropathic pain, pancreatitis, neurogenic inflammation, asthma, chronic obstructive pulmonary disease (COPD) and micturition disorders such as urinary incontinence. The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in Claim. 

Substituted oxa-diaza-spiro-[5.5]-undecanone derivatives and their use as neurokinin antagonists

The present invention provides compounds of formula (I), their use as an inhibitor of a p53-MDM2 interaction as well as pharmaceutical compositions comprising said compounds of formula (I) wherein n, m, p, t, R, R, R, R, R, R, R, Q, Y and Z have defined meanings. 

Cyclic-alkylamine derivatives as inhibitors of the interaction between MDM2 and p53

The present invention concerns compounds of formula. In a preferable embodiment, X represents O; Rrepresents Calkyl; cycloCalkyl or (cycloCalkyl)Calkyl, wherein one or more hydrogen atoms in a Calkyl-moiety or in a cycloCalkyl-moiety optionally may be replaced by Calkyloxy, aryl, halo or thienyl; Rrepresents hydrogen; halo; Calkyl or amino; Rand Reach independently represent hydrogen or Calkyl; or Rand Rmay be taken together to form &#x2014;R&#x2014;R&#x2014;, which represents a bivalent radical of formula -Z-CH&#x2014;CH&#x2014;CH&#x2014; or -Z-CH&#x2014;CH&#x2014; with Zbeing O or NRwherein Ris Calkyl; and wherein each bivalent radical is optionally substituted with Calkyl; or Rand Rmay be taken together to form a bivalent radical of formula &#x2014;CH&#x2014;CH&#x2014;CH&#x2014;CH&#x2014;; Rrepresents hydrogen; Y represents O; and aryl represents phenyl optionally substituted with halo. The invention also relates to the use of a compound according to the invention as a medicament and in the manufacture of a medicament for treating or preventing glutamate-induced diseases of the central nervous system, as well as formulations comprising such a compound and processes for preparing such a compound.

Metabotropic glutamate receptor antagonists

This invention concerns substituted diaza-spiro-[4.5]-decane derivatives having neurokinin antagonistic activity, in particular NKantagonistic activity, a combined NK/NKantagonistic activity, a combined NK/NKantagonistic activity and a combined NK/NK/NKantagonistic activity, their preparation, compositions comprising them and their use as a medicine, in particular for the treatment and/or prophylaxis of schizophrenia, emesis, anxiety and depression, irritable bowel syndrome (IBS), circadian rhythm disturbances, pre-eclampsia, nociception, pain, in particular visceral and neuropathic pain, pancreatitis, neurogenic inflammation, asthma, chronic obstructive pulmonary disease (COPD) and micturition disorders such as urinary incontinence. The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in Claim

Substituted diaza-spiro-[4.5]-decane derivatives and their use as neurokinin antagonists

This invention concerns substituted diaza-spiro-[5.5]-undecane derivatives having neurokinin antagonistic activity, in particular NKantagonistic activity, a combined NK/NKantagonistic activity, a combined NK/NKantagonistic activity and a combined NK/NK/NKantagonistic activity, their preparation, compositions comprising them and their use as a medicine, in particular for the treatment and/or prophylaxis of schizophrenia, emesis, anxiety and depression, irritable bowel syndrome (IBS), circadian rhythm disturbances, pre-eclampsia, nociception, pain, in particular visceral and neuropathic pain, pancreatitis, neurogenic inflammation, asthma, COPD and micturition disorders such as urinary incontinence. The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in Claim

Substituted diaza-spiro-[5.5]-undecane derivatives and their use as neurokinin antagonists

The present invention concerns compounds of formula. In a preferable embodiment, X represents O; Rrepresents Calkyl; cycloCalkyl or (cycloCalkyl)Calkyl, wherein one or more hydrogen atoms in a Calkyl-moiety or in a cycloCalkyl-moiety optionally may be replaced by Calkyloxy, aryl, halo or thienyl; Rrepresents hydrogen; halo; Calkyl or amino; Rand Reach independently represent hydrogen or Calkyl; or Rand Rmay be taken together to form &#x2014;R&#x2014;R&#x2014;, which represents a bivalent radical of formula &#x2014;Z&#x2014;CH&#x2014;CH&#x2014;CH&#x2014; or &#x2014;Z&#x2014;CH&#x2014;CH&#x2014; with Zbeing O or NRwherein Ris Calkyl; and wherein each bivalent radical is optionally substituted with Calkyl; or Rand Rmay be taken together to form a bivalent radical of formula &#x2014;CH&#x2014;CH&#x2014;CH&#x2014;CH&#x2014;; Rrepresents hydrogen; Y represents O; and aryl represents phenyl optionally substituted with halo. The invention also relates to the use of a compound according to the invention as a medicament and in the manufacture of a medicament for treating or preventing glutamate-induced diseases of the central nervous system, as well as formulations comprising such a compound and processes for preparing such a compound.

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Le Manoir sur Seine, France

Alain Philippe Poncelet