Glaxo Group Limited

King's College London

Glaxo S.p.a.

Smithkline Beecham Corporation

Alan D Borthwick

Andrew McMurtrie Mason

John Liddle

Deirdre Mary Bernadette Hickey

Giovanni Gaviraghi

Claudio Semeraro

Dino Micheli

Daniele Pieraccioli

Jane Theresa Brown

Jonathan Patrick Thomas Corcoran

Maria Beatriz De Castro Vasconcelos Goncalves

Sarkis Barret Kalindjian

Nigel Stephen Watson

Mark Trevor Mills

Paul Graham Wyatt

Anna Katrin Szardenings

Henry Anderson Kelly

Robert John Young

Neil Derek Miller

Savvas Kleanthous

Steven Leslie Sollis

David George Hubert Livermore

Richard Jonathan Hatley

Fabrizio Nerozzi

Keith Biggadike

Chuen Chan

Edwin Aret

Ronnie Maxwell Lawrence

Richard Storer

Peter C Cherry

Sarkis Barrett Kalindjian

Andrew J Crame

John Kitchin

Adrian J Pipe

John David Harling

David Michel Adrien Taddei

Nigel Paul King

Matthew Campbell

Stefan Senger

Jason John Shiers

Paul William Smith

Niall G Weir

Richard J Coles

Anthony D Baxter

Barrie E Kirk

Chi L Mo

David Reginald Adams

Wendy Rebecca Irving

Ian L Paternoster

Derek Burn

The present invention pertains generally to the field of therapeutic compounds, and more specifically to crystalline forms of 4-(5-(4,7-dimethylbenzofuran-2-yl)-1,2,4-oxadiazol-3-yl)benzoic acid (referred to herein as 'BHBA-001'), which, inter alia, is a (selective) retinoic acid receptor beta (RAR&#x3b2;) (e.g., RAR&#x3b2;2) agonist. The present invention also pertains to pharmaceutical compositions comprising such crystalline forms, and the use of such crystalline forms and compositions, both in vitro and in vivo, to (selectively) activate RAR&#x3b2; (e.g., RAR&#x3b2;2), to cause or promote neurite development, neurite outgrowth, and/or neurite regeneration, and in the treatment of diseases and conditions that are mediated by RAR&#x3b2; (e.g., RAR&#x3b2;2), that are ameliorated by the activation of RAR&#x3b2; (e.g., RAR&#x3b2;2), etc., including, e.g., neurological injuries such as spinal cord injuries.

Crystalline forms of 4-(5-(4,7-dimethylbenzofuran-2-yl)-1,2,4-oxadiazol-3-yl)benzoic acid and processes for their preparation

The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain bicycloheteroaryl-heteroaryl-benzoic acid compounds of the following formula (for convenience, collectively referred to herein as 'BHBA compounds'), which, inter alia, are (selective) retinoic acid receptor beta (RAR&#x3b2;) (e.g., RAR&#x3b2;2) agonists. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to (selectively) activate RAR&#x3b2; (e.g., RAR&#x3b2;2), to cause or promote neurite development, neurite outgrowth, and/or neurite regeneration, and in the treatment of diseases and conditions that are mediated by RAR&#x3b2; (e.g., RAR&#x3b2;2), that are ameliorated by the activation of RAR&#x3b2; (e.g., RAR&#x3b2;2), etc., including, e.g., neurological injuries such as spinal cord injuries. 

Bicycloheteroaryl-heteroaryl-benzoic acid compounds as retinoic acid receptor beta (RAR&#x3b2;) agonists

The present invention pertains generally to the field of therapeutic compounds, and more specifically to crystalline forms of 4-(5-(4,7-dimethylbenzofuran-2-yl)-1,2,4-oxadiazol-3-yl)benzoic acid (referred to herein as 'BHBA-001'), which, inter alia, is a (selective) retinoic acid receptor beta (RAR&#x3b2;) (e.g., RAR&#x3b2;2) agonist. The present invention also pertains to pharmaceutical compositions comprising such crystalline forms, and the use of such crystalline forms and compositions, both in vitro and in vivo, to (selectively) activate RAR&#x3b2; (e.g., RAR&#x3b2;2), to cause or promote neurite development, neurite outgrowth, and/or neurite regeneration, and in the treatment of diseases and conditions that are mediated by RAR&#x3b2;(e.g., RAR&#x3b2;2), that are ameliorated by the activation of RAR&#x3b2; (e.g., RAR&#x3b2;2), etc., including, e.g., neurological injuries such as spinal cord injuries. 

Crystalline forms of 4-(5-(4,7-dimethylbenzofuran-2-yl)-l,2,4-oxadiazol-3-yl)benzoic acid and processes for their preparation

The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain bicycloheteroaryl-heteroaryl-benzoic acid compounds of the following formula (for convenience, collectively referred to herein as 'BHBA compounds'), which, inter alia, are (selective) retinoic acid receptor beta (RAR&#x3b2;) (e.g., RAR&#x3b2;2) agonists. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to (selectively) activate RAR&#x3b2; (e.g., RARP&#x3b2;2), to cause or promote neurite development, neurite outgrowth, and/or neurite regeneration, and in the treatment of diseases and conditions that are mediated by RAR&#x3b2; (e.g., RAR&#x3b2;2), that are ameliorated by the activation of RAR&#x3b2; (e.g., RAR&#x3b2;2), etc., including, e.g., neurological injuries such as spinal cord injuries. 

The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain aryl-amido-aryl compounds of the following formula (for convenience, collectively referred to herein as 'AAA compounds'), which, inter alia, are (selective) retinoic acid receptor &#x3b1; (RAR&#x3b1;) agonists. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to (selectively) activate RAR&#x3b1;, and in the treatment of diseases and conditions that are mediated by RAR&#x3b1;, that are ameliorated by the activation of RAR&#x3b1;, etc., including cognitive disorders, memory impairment, memory deficit, senile dementia, Alzheimer's disease, early stage Alzheimer's disease, intermediate stage Alzheimer's disease, late stage Alzheimer's disease, cognitive impairment, and mild cognitive impairment. 

Therapeutic aryl-amido-aryl compounds and their use

Compounds of formula (I) wherein Ris 2-indanyl, Ris 1-methylpropyl, Ris a group selected from 2,6-dimethyl-3-pyridyl or 4,6-dimethyl-3-pyridyl, Rrepresents methyl and Rrepresents hydrogen or methyl or, Rand Rtogether with the nitrogen atom to which they are attached represent morpholino and pharmaceutically acceptable derivatives thereof are described, as are processes for their preparation, pharmaceutical compositions containing them and their use in medicine, particularly their use as oxytocin antagonists.

Compounds

A method of treating or preventing diseases or conditions mediated through the action of oxytocin which comprises administering to a human in need thereof of an effective amount of a compound of the formula (I) or a pharmaceutically acceptable salt thereof.

Substituted diketopiperazines as oxytocin antagonists

A method of treating or preventing diseases or conditions mediated through the action of oxytocin which comprises administering to a human in need thereof of an effective amount of a compound of formula (I) or a pharmaceutically acceptable salt thereof.

Compounds of formula (I) wherein Ris 2-indanyl, Ris 1-methylpropyl, Ris a group selected from 2,6-dimethyl-3-pyridyl or 4,6-dimethyl-3-pyridyl, Rrepresents methyl and Rrepresents hydrogen or methyl or, Rand Rtogether with the nitrogen atom to which they are attached represent morpholino and pharmaceutically acceptable derivatives thereof are described, as are for their preparation, pharmaceutical compositions containing them and their use in medicine, particularly their use as oxytocin antagonists.

Piperazinediones as oxytocin receptor antagonists

A method of treating or preventing diseases or conditions mediated through the action of oxytocin which comprises administering to a mammal in need thereof of an effective amount of a compound of the formula (I) and/or a physiologically acceptable derivative thereof, wherein the substituents have the meaning given in the description. Disclosed are also novel compounds of formula (I) and processes for their preparation.

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London, United Kingdom

Alan D Borthwick