Therapeutic Aryl-Amido-Aryl Compounds and Their Use

Abstract

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 α (RARα) 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 RARα, and in the treatment of diseases and conditions that are mediated by RARα, that are ameliorated by the activation of RARα, 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.

Description

RELATED APPLICATION[0001]This application is related to United Kingdom patent application number 0915196.0 filed 1 Sep. 2009, the contents of which are incorporated herein by reference in their entirety.TECHNICAL FIELD[0002]The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain aryl-amido-aryl compounds (for convenience, collectively referred to herein as “AAA compounds”), which, inter alia, are (selective) retinoic acid receptor α (RARα) 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 RARα, and in the treatment of diseases and conditions that are mediated by RARα, that are ameliorated by the activation of RARα, etc., including cognitive disorders, memory impairment, memory deficit, senile dementia, Alzheimer's disease, early stage Alzheimer's disease, intermediate stage ...

AI Technical Summary

Benefits of technology

The patent describes certain compounds, called AAA compounds, and their use in the treatment of various diseases and conditions. These compounds can activate a specific receptor called RARα, which is involved in the regulation of gene expression. The patent also describes methods for preparing and using these compounds, as well as methods for selectively activating RARα and down-regulating its expression in specific types of cells. The technical effects of the patent include the potential for improved treatment of diseases and conditions such as Alzheimer's disease and cognitive disorders, as well as the development of new pharmaceutical compositions and methods for manufacturing them.

Problems solved by technology

Most of the attempts to develop new treatments have focused on altering deposits of the amyloid protein in the brain, but despite more than a decade of intensive research this has still not yielded any new therapies in the clinic.

The only currently approved medications for the treatment of AD are two groups of drugs, acetylcholinesterase inhibitors (e.g., Aricept™) and non-competitive NMDA receptor blockers (e.g., Memantine™), which give significant symptomatic improvement but do not fundamentally prevent or alter disease progression.

However, despite considerable effort and research over more than a decade, these treatments have not yet translated into treatments in the clinic.

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