Janssen Pharmaceutica Nv

Vistakon Pharmaceuticals, LLC

Tibotec Pharmaceuticals Ltd.

Janssen Pharmaceutica

Hanssen Pharmaceutica, N.v.

Janssen Pharmaceuitca N.v.

Janssen Pharmacatica, N.v.

Frans E Janssens

Joseph Elisabeth Leenaerts

Joseph L Torremans

Gaston S Diels

François Maria Sommen

Jozef F Hens

Francois M Sommen

Theophilus T Van Offenwert

Koenraad Jozef Lodewijk Marcel Andries

Jean Fernand Armand Lacrampe

Jérôme Emile Georges Guillemont

Kathleen Petrus Marie-José Meersman

Raymond A Stokbroekx

Yves Emiel Maria Van Roosbroeck

Dominique Louis Nestor Ghislaine Surleraux

Fran&ccedil;ois Maria Sommen

Benoît Christian Albert Ghislain De Boeck

Francisco Javier Fernández-Gadea

Antonio Gómez-Sánchez

Ludo E Kennis

Bruno Schoentjes

Alain Philippe Poncelet

Marcel G Luyckx

Sophie Philippe Coupa

Ludwig P Cooymans

Geert M Pille

Ann C Dierckx

Bernard R Boar

Marc Gaston Venet

José Manuel Bartolomé-Nebreda

Mark Barry Abelson

Manuel Jesús Alcázar-Vaca

Theo Frans Meert

Yvan René Ferdinand Simonnet

Pedro Martínez-Jiménez

Jean Fernand Lacrampe

Isabelle Noelle Pilatte

Koenraad Arthur Van Rossem

Anton Megens

Avner Ingerman

Jean-François Bonfanti

Jerôme Emile Georges Guillemont

Gaston Stanislas Marcella Diels

Frank Tegtmeier

Koenraad Jozef Lodewijk Andries

Jozeph L Torremans

Gasto S Diels

Jozef E Hens

Jerome Emile Geroges Guilemont

Gaston, S Diels

Dominique Louis Surleraux

Francedillaois Maria Sommen

Kathleen Petrus Marie-Jos&eacute; Meersman

Marcel J M Borgers

Willem Flameng

Paul Joannes Ludovicus Herijgers

Jos Van Reempts

Koenraads Jozef Lodewijk Marcell Andries

Jozef Leo Henri Van Reempts

Jagdish Parasrampuria

Compositions, kits and methods for the treatment or prevention of ocular allergies and inflammation and the symptoms thereof containing alcaftadine or a pharmaceutically acceptable salt thereof.

Ophthalmic compositions containing alcaftadine

Compositions, kits, and methods for the treatment or prevention of ocular allergies and inflammation and the symptoms thereof containing alcaftadine or a pharmaceutically acceptable salt thereof.

Ocular allergy treatments with alcaftadine

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 is concerned with novel compounds of formula (I) having fundic relaxating activity. The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use as a medicine of said compounds. 

2-piperazin-1-yl-3H-imidazo[4,5-b]pyridine derivatives

This invention concerns substituted I-piperidin-4-yl-4-pyrrolidin-3-yl-piperazine derivatives having neurokinin antagonistic activity, in particular 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 of schizophrenia, anxiety, depression, emesis and IBS. 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. In view of their capability to antagonize the actions of tachykinins by blocking the neurokinin receptors, and in particular antagonizing the actions of substance P and Neurokinin B by blocking the NK, NKand NKreceptors, the compounds according to the invention are useful as a medicine, in particular in the prophylactic and therapeutic treatment of tachykinin-mediated conditions, such as, for instance CNS disorders, in particular schizoaffective disorders, depression, anxiety disorders, stress-related disorders, sleep disorders, cognitive disorders, personality disorders, eating disorders, neurodegenerative diseases, addiction disorders, mood disorders, sexual dysfunction, pain and other CNS-related conditions; inflammation; allergic disorders; emesis; gastrointestinal disorders, in particular irritable bowel syndrome (IBS); skin disorders; vasospastic diseases; fibrosing and collagen diseases; disorders related to immune enhancement or suppression and rheumatic diseases and body weight control. 

Substituted 1-piperidin-4-yl-4-pyrrolidin-3-yl-piperazine derivatives and their use as neurokinin antagonists

The invention concerns a novel histamine receptor antagonist and the use of an histamine receptor antagonist for the reduction of intracranial pressure (ICP), in particular for the prevention and treatment of elevated intracranial pressure and/or secondary ischaemida, in particular caused by brain injury, more in particular caused by traumatic (TBI) and non-traumatic brain injury. The novel compounds comprise compounds according to the general Formula (I) the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof and the N-oxide form thereof. In particular, the preferred compound is 3-[2-[4-(11,12-dihydro-6H-benzimidazo[2,1-b][3]benzazepin-6-yl)-2-(phenyl-methyl)-1-piperidinyl]ethyl]-2,10-dimethyl pyrimido[1,2-&#x3b1;]benzimidazol-4(10H)-one, the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof and the N-oxide form thereof. Also claimed is the novel use of commercially available histamine H1-and H2-receptor antagonists for the reduction of intracranial pressure (ICP). 

Use of anti-histaminics for acute reduction of elevated intracranial pressure

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 1-piperidin-3-yl-4-piperidin-4-yl-piperazine derivatives having neurokinin antagonistic activity, in particular 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 of schizophrenia, emesis, anxiety and depression, irritable bowel syndrom (IBS), circadian rhythm disturbances, visceral pain, neurogenic inflammation, asthma, micturition disorders such as urinary incontinence and nociception. 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 1. In view of their capability to antagonize the actions of tachykinins by blocking the neurokinin receptors, and in particular antagonizing the actions of substance P, Neurokinin A and Neurokinin B by blocking the NK, NKand NKreceptors, the compounds according to the invention are useful as a medicine, in particular in the prophylactic and therapeutic treatment of tachykinin-mediated conditions, such as, for instance CNS disorders, in particular schizoaffective disorders, depression, anxiety disorders, stress-related disorders, sleep disorders, cognitive disorders, personality disorders, eating disorders, neurodegenerative diseases, addiction disorders, mood disorders, sexual dysfunction, pain and other CNS-related conditions; inflammation; allergic disorders; emesis; gastrointestinal disorders, in particular irritable bowel syndrome (IBS); skin disorders; vasospastic diseases; fibrosing and collagen diseases; disorders related to immune enhancement or suppression and rheumatic diseases and body weight control.

Substituted 1-piperidin-3-yl-4-piperidin-4-yl-piperazine 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

This invention concerns compounds of formula (I)  prodrugs, addition salts, or stereochemically isomeric forms thereof for use as, inter alia, respiratory syncytial virus replication inhibitors; their preparation, compositions containing them and methods of their use in treating respiratory syncytial viral infections.

Respiratory syncytial virus replication inhibitors

The invention concerns substituted 4-(4-piperidin-4-yl-piperazin-1-yl)-azepane derivatives having neurokinin antagonistic activity, in particular NK&#x2dc;antagonistic activity, their preparation, compositions comprising them and their use as a medicine, in particular for the treatment of pain, emesis, anxiety, depression and IBS.

Substituted 4-(4-piperidin-4-yl-piperazin-1-yl)-azepane derivatives and their use as neurokinin antagonists

The invention concerns novel substituted tetracyclic imidazole derivatives useful for the treatment of elevated intracranial pressure (ICP) and/or secondary ischaemia, in particular caused by brain injury, more in particular caused by traumatic (TBI) and non-traumatic brain injury, processes for their preparation, pharmaceutical compositions comprising them and their use as a medicine. The novel compounds comprise compounds according to the general Formula (I), the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof and the N-oxide form thereof. In particular, the preferred compound is 3-[2-[4-(11,12-dihydro-6H-benzimidazo[2,1-b][3]benzazepin-6-yl)-2-(phenyl-l-methyl)-1-piperidinyl]ethyl]-2,10-dimethyl pyrimido[1,2-&#x3b1;]benzimidazol-4(10H)-one, the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof and the N-oxide form thereof. 

Substituted tetracyclic imidazole derivatives, processes for their preparation, pharmaceutical compositions comprising them and their use as a medicine

The invention concerns substituted 1-piperidin-4-yl-4-azetidin-3-yl-piperazine having neurokinin antagonistic activity, in particular NKand NK/NK-antagonistic activity, their preparation, compositions comprising them and their use as a medicine, in particular for the treatment of schizophrenia, emesis, anxiety, depression, irritable bowel syndrome (IBS), circadian rhythm disturbances, pain, neurogenic inflammation, asthma, micturition disorders such as urinary incontinence and nociception. 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 In view of their capability to antagonize the actions of tachykinins by blocking the neurokinin receptors, and in particular antagonizing the actions of substance P by blocking the NK receptors, the compounds according to the invention are useful as a medicine, in particular in the prophylactic and therapeutic treatment of tachykinin-mediated conditions, such as, for instance CNS disorders, in particular depression, anxiety disorders, stress-related disorders, sleep disorders, cognitive disorders, personality disorders, schizoaffective disorders, eating disorders, neurodegenerative diseases, addiction disorders, mood disorders, sexual dysfunction, pain and other CNS-related conditions; inflammation; allergic disorders; emesis; gastrointestinal disorders, in particular irritable bowel syndrome (IBS); skin disorders; vasospastic diseases; fibrosing and collagen diseases; disorders related to immune enhancement or suppression and rheumatic diseases and body weight control.

Substituted 1-piperidin-4-yl-4-azetidin-3-yl-piperazine derivatives and their use as neurokinin antagonists

The invention concerns substituted 1,4-di-piperidin-4-yl-piperazine derivatives having neurokinin antagonistic activity, in particular NKantagonistic activity, their preparation, compositions comprising them and their use as a medicine, in particular for the treatment of emesis, anxiety, depression, pain, pancreatitis and IBS.

Substituted 1,4,-di-piperidin-4-yl-piperazine derivatives and their use as neurokinin antagonists

The present invention concerns compounds of formula (I), prodrugs, N-oxides, addition salts, quaternary amines, metal complexes and stereochemically isomeric forms thereof wherein -a=a-a=a- represents a radical of formula &#x2014;CH&#x2550;CH&#x2014;CH&#x2550;CH&#x2014;; &#x2014;N&#x2550;CH&#x2014;CH&#x2550;CH&#x2014;; &#x2014;CH&#x2550;N&#x2014;CH&#x2550;CH&#x2014;; &#x2014;CH&#x2550;CH&#x2014;N&#x2550;CH&#x2014;; CH&#x2550;CH&#x2014;CH&#x2550;N&#x2014;; wherein each hydrogen atom may optionally be substituted; Q is a radical of formulae (b-1), (b-2), (b-3), (b-4), (b-5), (b-6), (b-7) and (b-8), wherein Alk is Calkanediyl; Yis a bivalent radical of formula &#x2014;NR&#x2014; or &#x2014;CH(NRR); Xis NR, S, S(&#x2550;O), S(&#x2550;O), O, CH, C(&#x2550;O), CH(&#x2550;CH), CH(OH), CH(CH), CH(OCH), CH(SCH), CH(NRR), CH&#x2014;NRor NR&#x2014;CH; Xis a direct bond, CH, C(&#x2550;O), NR, Calkyl-NR, NR&#x2014;Calkyl, t is 2 to 5; u is 1 to 5; v is 2 or 3; and whereby each hydrogen in Alk and in (b-3), (b-4), (b-5), (b-6), (b-7) and (b-8), may optionally be replaced by R; provided that when Ris hydroxy or Calkyloxy, then Rcannot replace a hydrogen atom in the &#x3b1; position relative to a nitrogen atom; G is a direct bond or optionally substituted Calkanediyl; Ris an optionally substituted bicyclic heterocycle; Ris hydrogen, formyl, Calkylcarbonyl, Hetcarbonyl, pyrrolidinyl, piperidinyl, homopiperidinyl, Ccycloalkyl or Calkyl substituted with N(R)and optionally with another substituent; Ris hydrogen, hydroxy, Calkyl, Calkyloxy, arylCalkyl or arylCalkyloxy, Ris hydrogen, Calkyl or arylCalkyl; R, R, Rand Rare hydrogen or Calkyl; or Rand R, or Rand Rtaken together from a bivalent radical of formula &#x2014;(CH)&#x2014; wherein S is 4 or 5; Ris hydrogen, Calkyl, formyl, hydroxyCalkyl, Calkylcarbonyl or Calkyloxycarbonyl; aryl is optionally substituted phenyl; Het is pyridyl, pyrimidinyl, pyryzinyl, pyridazinyl; as respiratory syncytial virus replication inhibitors; their preparation, compositions containing them and their use as a medicine.

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Bonheiden, Belgium

Frans E Janssens