N-(carbacyclyl)-indolocarbazoles, such as I [R = substituted or unsubstituted 5 or 6 membered carbacyclyl; R3, R4 = H, halogen, alkyl, carboxy, carboxamide, amino, alkoxy, etc.], were prepd. as protein kinase inhibitors which are useful for the treatment of non-insulin dependent diabetes mellitus, acute stroke and other neurotraumatic injuries, malignant diseases, and neurodegenerative diseases, such as Alzheimer's disease. Thus, NAD 006 (II) was prepd. via a multistep synthetic sequence starting from cyclopentadiene, 1H-indole-3-acetonitrile and 2-indolone. The prepd. staurosporine analogs were assayed for inhibition of extracellular signal regulated kinase 2, protein kinase A, protein kinase C and glycogen synthase kinase 3β.
Preparation of N-carbacycle monosubstituted indolocarbazoles for therapeutic use as protein kinase inhibitors / H. Sahagun-Krause, O. Thillaye Du Boullay, V. Thillaye Du Boullay, L. Casiraghi, P. Seneci, H. Klafki, T. Braxmeier, S. Mueller, W. Froehner, B. Monse, S. Gordon, H. Roder.
Titolo: | Preparation of N-carbacycle monosubstituted indolocarbazoles for therapeutic use as protein kinase inhibitors |
Autori: | |
Enti collegati: | NAD AG, MUNICH, GERMANY |
Codice di pubblicazione: | C07D487-14 |
Data di pubblicazione: | 2003 |
Parole Chiave: | INDOLOCARBAZOLES ; kinases ; alzheimer's disease |
Settore Scientifico Disciplinare: | Settore CHIM/06 - Chimica Organica Settore CHIM/08 - Chimica Farmaceutica Settore BIO/13 - Biologia Applicata |
Citazione: | Preparation of N-carbacycle monosubstituted indolocarbazoles for therapeutic use as protein kinase inhibitors / H. Sahagun-Krause, O. Thillaye Du Boullay, V. Thillaye Du Boullay, L. Casiraghi, P. Seneci, H. Klafki, T. Braxmeier, S. Mueller, W. Froehner, B. Monse, S. Gordon, H. Roder. |
Numero di deposito: | WO 2003051887 |
Appare nelle tipologie: | 09 - Brevetto, privativa o norma |