Cephalon, Inc.

Kyowa Hakko Kogyo Co., Ltd.

Kyowa Hakko Kogyo

Marcie A Glicksman

Chikara Murakata

Nicola T Neff

Hiromitsu Saito

James C Kauer

Michael E Lewis

Yuzuru Matsuda

Jill M Roberts-Lewis

Fumihiko Kanai

Masami Kaneko

David P Rotella

Robert L Hudkins

The invention features novel derivatives of K-252a, as well as novel bis-N-substituted derivatives of staurosporine. The invention also features a method for treating diseased neuronal cells involving the administration of either the novel staurosporine derivatives or specified functional derivatives of K-252a.

Protein kinase inhibitors for treatment of neurological disorders

Protein kinase inhibitors for treatmen of neurological disorders

K-252a derivatives for treatment of neurological disorders

Disclosed are derivatives of the indolocarbazole alkaloid K-252a of the Formulae I-VI, useful for enhancing neurotrophin-induced activity of neurotrophin responsive cells. A particularly preferred neurotrophin is NT-3, and a particularly preferred neurotrophin responsive cell is one which comprises a trk receptor. The enhanced neurotrophin-induced activity occasioned by the disclosed K-252a derivatives may be determined by the following assays: ChAT activity; DRG neuronal survival; or cell division (mitogenesis).

K-252 derivatives which enhance neurotrophin-induced activity

Functional K-252a derivatives are used to enhance trk phosphorylation and to potentiate the activity of neurotrophin-3 (NT-3). These compounds can be used to treat neurological disorders, alone or in combination with NT-3.

K-252a functional derivatives potentiate neurotrophin-3 for the

The invention features novel derivatives of K-252a, as well as novel bis-N-substituted derivatives of staurosporine. Also, a method for treating diseased neuronal cells involving the administration of either the novel staurosporine derivatives or specified functional derivatives of K-252a.

Selected protein kinase inhibitors for the treatment of neurological

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Swarthmore, PA, United States of America

Marcie A Glicksman