Solvay Pharmaceuticals, B.v.

Abbott Healthcare Products B.v.

Pieter Smid

Cornelis G Kruse

Josephus H M Lange

Roelof Van Hes

Michael Mlinaric

Konrad Koehler

Martinus Th M Tulp

Sara Nuñez Garcia

Elmar Wegener

This invention concerns spiro azepane-ox-azolidinones as voltage gated Kv1.3 potassium channel blockers, pharmaceutical compositions containing these compounds, methods for preparing the compounds, methods for preparing novel intermediates useful for their synthesis, and methods for preparing compositions. The invention also relates to the uses of such compounds and compositions, particularly their use in administering them to patients to achieve a therapeutic effect in the treatment of diabetes, psoriasis, obesity, transplant rejection and inflammatory neuropathies, including T-cell mediated autoimmune diseases such as rheumatoid arthritis and multiple sclerosis. The compounds have formula (1): wherein R, R, (R), and (R)have the meanings given in the specification.

Spiro azepane-oxazolidinones as Kv1.3 potassium channel blockers

The present invention relates to a group of novel tetrahydropyridin-4-yl indoles with a dual mode of action: serotonin reuptake inhibition and affinity for dopamine-Dreceptors, to methods for the preparation of these compounds and to novel intermediates useful for the synthesis of said tetrahydropyridin-4-yl indoles. The invention also relates to the use of a compound disclosed herein for the manufacture of a medicament giving a beneficial effect. The invention relates to novel tetrahydropyridin-4-yl indoles of the formula. and tautomers, stereoisomers, prodrugs, N-oxides, pharmacologically acceptable salts, hydrates and solvates thereof,wherein:

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Weesp, Netherlands

Pieter Smid