Astrazeneca Ab

Anna Minidis

Ulf G Larsson

Adrian Clark

Elfyn Jones

Carl-Johan Aurell

Lanna Li

Eva-Lotte Lindstedt Alstermark

Anna Christina Olsson

Jenny Viklund

Esmail Yousefi-Salakdeh

Fredrik Rahm

Mikael Ulf Johan Dahlström

Beta-secretase inhibitors, of formula (I) as described in the specification, pharmaceutical compositions comprising them and therapeutic methods using them for the treatment and/or prevention of A&#x3b2;-related pathologies such as Down's syndrome, &#x3b2;-amyloid angiopathy such as but not limited to cerebral amyloid angiopathy or hereditary cerebral hemorrhage, disorders associated with cognitive impairment such as but not limited to MCI ('mild cognitive impairment'), Alzheimer's Disease, memory loss, attention deficit symptoms associated with Alzheimer's disease, neurodegeneration associated with diseases such as Alzheimer's disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration. 

Mono-fluoro beta-secretase inhibitors

The invention relates to a novel process for the preparation of certain cyclopropyl carboxylic acid esters and other cyclopropyl carboxylic acid derivatives; a novel process for the preparation of dimethylsulfoxonium methylide and dimethylsulfonium methylide; to the use of certain cyclopropyl carboxylic acid esters in a process for the preparation of intermediates that can be used in the synthesis of pharmaceutically active entities; and to certain intermediates provided by these processes.

Process for the preparation of cyclopropyl carboxylic acid esters and derivatives

The compounds trans-(1R,2R)-2-(3,4-difluorophenyl)cyclopropanecarbonyl azide and trans-(1R,2S)-2-(3,4-difluorophenyl)cyclopropanaminium (2R)-2-hydroxy-2-phenylethanoate.

The present invention provides the S enantiomer of a compound of formula I wherein Rrepresents chloro, trifluoromethyl or trifluoromethoxy, Rrepresents H or fluoro and Rrepresents a Calkyl group as well as pharmaceutically acceptable salts, solvates and prodrugs thereof, to processes for preparing such compounds, to their the utility in treating clinical conditions including lipid disorders (dyslipidemias) whether or not associated with insulin resistance, to methods for their therapeutic use and to pharmaceutical compositions containing them.

Therapeutic agents

Growing community of inventors

Södertälje, Sweden

Anna Minidis