Glaxo Group Limited

Indivior UK Limited

Chronos Therapeutics Limited

Glaxo Wellcome Spa

Glaxogrouplimited

Yale University

Neurocrine Biosciences, Inc.

Sb Pharmco Puerto Rico Inc.

Giaxo Group Limited

Fabrizio Micheli

Luca Tarsi

Romano Di Fabio

Dieter Hamprecht

Silvia Terreni

Alessandra Pasquarello

Susanna Cremonesi

Teresa Semeraro

Giorgio Bonanomi

Barbara Bertani

Giovanna Tedesco

Gabriella Gentile

Anna Maria Capelli

Anna Checchia

Yves St-Denis

Luca Arista

Federica Damiani

Elettra Fazzolari

Chiara Marchionni

Tim Luker

Karl Richard Gibson

Giovanni Gaviraghi

Jonathan A Ellman

Michael Schwaebe

Daniele Andreotti

Colin Philip Leslie

Paolo Dambruoso

Alfredo Cugola

Tadataka Yamada

Collin Regan

Alfonso Pozzan

Francesca Cardullo

Yves St Denis

Claudia Beato

Adolfo Prandi

Bendetta Perini

Benedetta Perini

Sergio Melotto

Luca Raveglia

Susana Cremonesi

Timothy Jon Luker

Riccardo Zanaletti

Teresa Semerano

Simone Giacobbe

Song Chen

Ya Ha

Caroline Chandra Tjin

Agostino Cianciulli

Paola Marzorati

Catia Seri

Caterina Mazzoni

Christian Heidbreder

Colin Leslie

Dieter Wolfgang Hamprecht

The present-disclosure relates to the discovery of novel 2-amino-dihydropteridinone compounds and analogues thereof, which are capable of inhibiting phosphatidylinositol phosphate kinases. In certain embodiments, the compounds of the present disclosure can be used to treat p53-null cancer in a subject. In other embodiments, the compounds of the present disclosure can be used to treat metabolic disorders in a subject, including but not limited to type 2 diabetes and/or obesity.

Small-molecule PI5P4K alpha/beta inhibitors and methods of treatment using same

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 disclosure is directed to novel dopamine D3 receptor antagonists, processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, including treating drug dependency and psychosis.

Dopamine Dreceptor antagonist compounds

The disclosure provides compounds having formula (I), where the substituents are as defined herein. The compounds are useful for modulating the dopamine D3 receptor and for treating conditions associated therewith, such as addictions, drug dependency, and psychiatric conditions.

Substituted 3,6-diazabicyclo[3.2.0]heptanes

The disclosure provides compounds of formula (I) or pharmaceutically acceptable salts thereof: The disclosure also provides processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them, and their use as modulators of dopamine Dreceptors, such as treating substance abuse or psychiatric diseases. 

Dopamine D3 receptor antagonists having a morpholine moiety

The disclosure provides compounds having formula (I), wherein the substituents are as defined herein. The compounds are useful for modulating the dopamine Dreceptor and for treating conditions associated therewith, such as addictions, drug dependency, and psychiatric conditions. 

Substituted hexahydropyrrolo[3,4-b]pyrroles and hexahydrocyclopenta[c]pyrroles as dopamine receptor modulators

Dopamine D3 receptor antagonists

Dopamine D3 receptor antagonist compounds

The present invention provides compounds of formula (I): compositions comprising such compounds; the use of such compounds in therapy (for example in the treatment or prevention of a disease, disorder or condition ameliorated by inhibition of a dopamine transporter); and methods of treating patients with such compounds; wherein R, R, R, R, R, R, R, R, R, R, m, n, A, L and B are as defined herein. 

N-(hetero)aryl-substituted heteroyclic derivatives useful for the treatment of diseases or conditions related to the central nervous system

The present invention provides compounds of formula (I): compositions comprising such compounds; the use of such compounds in therapy (for example in the treatment or prevention of a disease, disorder or condition ameliorated by inhibition of a dopamine transporter); and methods of treating patients with such compounds; wherein R, R, R, R, R, R, R, R, Q, X, Y, Z, A, L, B, m, n and p are as defined herein. 

Spirocyclic derivatives

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.

The present invention relates to novel compounds of formula (I) or a salt thereof: wherein Ris a 5-membered heteroaryl group, optionally fused with a 6-membered hetero or carbocycle; such 5 or 11-membered system, may be optionally substituted by 1, 2, 3 or 4 substituents selected from the group consisting of: halogen, cyano, Calkyl, haloCalkyl, Calkoxy, Calkanoyl, haloCalkoxy and SF; and n is 1 or 2; their use in therapy, as modulators of dopamine Dreceptors, e.g. to treat drug dependency, as antipsychotic agents, to treat obsessive compulsive spectrum disorders, or premature ejaculation.

Azabicyclo [3. 1. O] hexyl derivatives as modulators of dopamine D3 receptors

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

Azabicyclo [3.1.0] hexane derivatives as modulators of dopamine D3 receptors

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

Growing community of inventors

Verona, Italy

Fabrizio Micheli