Neuromed Pharmaceuticals Ltd.

Neuromed Technologies, Inc.

Zalicus Pharmaceuticals, Ltd.

Francesco Belardetti

Terrance P Snutch

Hassan Pajouhesh

Hossein Pajouhesh

Gerald Werner Zamponi

Yanbing Ding

Richard James Holland

Ramesh Kaul

Jason Tan

David Parker

Mike Grimwood

Navjot Chahal

Diana Janke

Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted T-type calcium channel activity are disclosed. Specifically, a series of compounds containing thienopyrimidine or oxoquinazoline derivatives are disclosed of the general formula (1) or formula (2) where X is a linker and Y is an aromatic moiety or N(R5)(R6). 

Bicyclic pyrimidine derivatives as calcium channel blockers

Aromatic derivatives of aliphatic diamines are effective in ameliorating conditions characterized by unwanted calcium ion channel activity, especially T-type and N-type channels. These conditions include, for example, stroke and pain.

Diamine calcium channel blockers

A fluorescence based assay for compounds that modulate T-type calcium ion channels and that can be adapted to high throughput screening formats. Modulators of T-type channels are useful to correct functional abnormalities. These abnormalities are associated with epilepsy, pain, schizophrenia, depression, anxiety, cardiac arrhythmia, hypertension, certain types of cancer, diabetes, infertility, sexual dysfunction and other undesirable conditions.

Fluorescence based T-type channel assay

Certain piperazine substituted compounds are described which are useful in altering calcium channel activity.

Preferentially substituted calcium channel blockers

Calcium channel blockers comprising two benzhydril moieties

Calcium channel inhibitors comprising benzhydril spaced from piperazine

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Vancouver, Canada

Francesco Belardetti