Glaxo Group Limited

Smithkline Beecham Corporation

Glaxo Wellcome Spa

Neurocrine Biosciences, Inc.

Leo-pharma A/s

Smithkline Beecham (cork) Ltd

Glaxogrouplimited

Sb Pharmco Puerto Rico Inc.

Chronos Therapeutics Limited

Neurocrine, Inc.

Sb Pharmaco Puerto Rico Inc.

Giaxo Group Limited

Smithkline Beecham Croporation

Glaxosmithkline LLC

Nerre Therapeutics Limited

Romano Di Fabio

Fabrizio Micheli

Giuseppe Alvaro

Yves St-Denis

Silvia Terreni

Alessandra Pasquarello

Riccardo Giovannini

Luca Tarsi

Antonella Ursini

Barbara Bertani

Gabriella Gentile

Giuseppe Guercio

Anna Maria Capelli

Dieter Hamprecht

Maria Elvira Tranquillini

Luca Arista

Federica Damiani

Alfonso Pozzan

Jakob Felding

Karl Richard Gibson

Sandro Belvedere

Giorgio Bonanomi

Giovanna Tedesco

Alfredo Cugola

Giorgio Pentassuglia

Simone Spada

Anna Checchia

Chiara Marchionni

Yves St Denis

Michael Schwaebe

Morten Dahl Sørensen

Daniele Andreotti

Susanna Cremonesi

Teresa Semeraro

Collin Regan

Alessandro Falchi

David Amantini

Aldo Feriani

Mauro Corsi

Elettra Fazzolari

Emiliano Castiglioni

Marsia Tampieri

Fabio Maria Sabbatini

Maria Pia Catalani

Paolo Maragni

Bendetta Perini

Benedetta Perini

Sergio Melotto

Luca Raveglia

Timothy Jon Luker

Riccardo Zanaletti

Simone Giacobbe

Nadia Conti

Elisabetta De Magistris

Haakon Bladh

Francesca Pavone

Morten Dahl SØRENSEN

There is provided a compound of formula (I), wherein Lto L', Rto R, X, A and B have meanings given in the description, and pharmaceutically acceptable salts, solvates and prodrugs thereof, which compounds are useful as antagonists of the orexin-1 and orexin-2 receptors or as selective antagonists of the orexin-1 receptor, and thus, in particular, in the treatment or prevention of inter alia substance dependence, addiction, anxiety disorders, panic disorders, binge eating, compulsive disorders, impulse control disorders, cognitive impairment and Alzheimer's disease.

Substituted 2-azabicyclo[3.1.1]heptane and 2-azabicyclo[3.2.1]octane derivatives as orexin receptor antagonists

The present invention relates to a compound according to formula (A) wherein n is 1 or 2; R1 and R2 are independently hydrogen, Calkyl, Chaloalkyl, Calkoxy, CD3 or halogen; R3 is hydrogen, C(&#x2550;O)OR7 or Calkyl optionally substituted with hydroxy or NR8R9; R4 is hydrogen or oxo; R5 and R6 are independently hydrogen, hydroxy, NR8R9, C(&#x2550;O)R7, C(&#x2550;O)OR7, C(&#x2550;O)NR8R9, Calkyl, wherein said Calkyl is optionally substituted with hydroxy, NR8R9 or a 5- or 6-membered heterocyclic ring, wherein said 5- or 6-membered heterocyclic ring is optionally substituted with Calkyl or C(&#x2550;O)R7; or R5 and R6, together with the carbon atom to which they are attached, form &#x2550;CHor a 5- or 6-membered heterocycloalkyl, wherein said heterocycloalkyl is optionally substituted with Calkyl; R7 is hydrogen or Calkyl; R8 and R9 are independently hydrogen or Calkyl, or R8 and R9, together with the nitrogen atom to which they are attached, form a 5- or 6-membered heterocyclic ring, or a pharmaceutically acceptable salt or solvate thereof. The invention relates further to intermediates for the preparation of said compounds, to said compounds for use in therapy, to pharmaceutical compositions comprising said compounds, to methods of treating or ameliorating pruritic dermal diseases or conditions with said compounds, and to the use of said compounds in the manufacture of medicaments. 

Substituted pyrrolo[1,2-a]piperazines and pyrrolo[1,2-a][1,4]diazepines as neurokinin 1 receptor antagonists

The present invention relates to novel compounds of formula (I) or a pharmaceutically acceptable salt thereof: wherein

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The present invention relates to certain azabicyclo compounds of formula (I)': wherein the various groups are defined herein and that are modulators of dopamine Dreceptors, e.g. to treat drug dependency, as antipsychotic agents, to treat obsessive compulsive spectrum disorders, or premature ejaculation.

Disclosed are N-{[(1S,4S,6S)-3-(2-pyridinylcarbonyl)-3-azabicyclo[4.1.0]hept-4-yl]methyl}-2-heteroarylamine derivatives having the following formula: wherein m, n, Het, R, Rand Rare as defined herein, and their use as orexin antagonists.

Heteroaryl derivatives of N-{[(1S,4S,6S)-3-(2-pyridinylcarbonyl)-3-azabicyclo[4.1.0]hept-4-yl]methyl}-2-amine

The present invention relates to compounds of formula (I) or salts thereof wherein A, X, R, Rand n are defined herein, processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as modulators of dopamine Dreceptors, e.g., to treat drug dependency, as antipsychotic agents, to treat obsessive compulsive spectrum disorders, premature ejaculation or to enhance cognition.

Spirocompounds useful as modulators for dopamine D3 receptors

The present invention relates to novel compounds of formula (I) or a pharmaceutically acceptable salt thereof: 

The present invention relates to novel compounds of formula (I) or a salt thereof: wherein:

Triazole derivatives as modulators of dopamine D3 receptors

The present invention relates to novel compounds of formula (I)' or a salt thereof: wherein and the other groups are define in herein.

Azabicyclo[3.1.0]hex-3-yl}alkyl)pyrimidinedione

The present invention relates to (1S,6R)-6-(3,4-dichlorophenyl)-1-[(methyloxy)methyl]-3-azabicyclo[4.1.0]heptane, pharmaceutically acceptable salts, prodrugs or solvates thereof; processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as serotonin (5-HT), dopamine (DA) and norepinephrine (NE), re-uptake inhibitors.

Chemical compounds

The present invention relates to piperidine derivatives of formula (I) specifically 2-(R)-(4-Fluoro-2-methyl-phenyl)-4-(S)-((8aS)-6-oxo-hexahydro-pyrrolo[1,2-a]-pyrazin-2-yl)-piperidine-1-carboxylic acid [1-(R)-(3,5-bis-trifluoromethyl-phenyl)-ethyl]-methylamide maleate and pharmaceutical compositions thereof, useful in the treatment of conditions mediated by tachykinins.

The invention relates to methods for the treatment of a sleep disorder in a mammal comprising administering to said mammal an effective amount of a compound of formula (I): wherein all variables are as defined herein.

Methods for the treatment of sleep disorders

The present invention provides compounds of formula (I) including stereoisomers, prodrugs and pharmaceutically acceptable salts or solvates thereof wherein

Pyrrolo[2, 3-d] pyrimidine derivatives as corticotropin releasing factor antagonists

CRF receptor antagonists are disclosed which have utility in the treatment of a variety of disorders, including the treatment of disorders manifesting hypersecretion of CRF in a warm-blooded animals, such as stroke. The CRF receptor antagonists of this invention have the following structure: including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof, R, R, R, R, R, A, X, and Y are as defined herein. Compositions containing a CRF receptor antagonist in combination with a pharmaceutically acceptable carrier are also disclosed, as well as methods for use of the same.

Tri-and tetraaza-acenaphthylen derivatives as CRF receptor antagonists

The present invention provides compounds of formula (I) including stereoisomers, prodrugs and pharmaceutically acceptable salts or solvates thereof to processes for their preparation, to pharmaceutical compositions containing them and to their use in the treatment of conditions mediated by corticotrophin-releasing factor (CRF).

Condensed N-heterocyclic compounds and their use as CRF receptor antagonists

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Verona, Italy

Romano Di Fabio