King's College London

Jonathan Patrick Thomas Corcoran

Alan D Borthwick

Jane Theresa Brown

Maria Beatriz De Castro Vasconcelos Goncalves

Sarkis Barret Kalindjian

Mark Trevor Mills

Edwin Aret

Ronnie Maxwell Lawrence

Sarkis Barrett Kalindjian

David Michel Adrien Taddei

Jason John Shiers

David Reginald Adams

Alan David Borthwick

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. 

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London, United Kingdom

Jonathan Patrick Thomas Corcoran