Selvita S.a.

Krzysztof Brzózka

Wojciech Czardybon

Michal Galezowski

Aleksandra Sabiniarz

Tomasz Rzymski

Raymond Horvath

Katarzyna Wiklik

Mariusz Milik

Renata Windak

Wieslaw Marek Cholody

Ewelina Wincza

Marta Prokop

Pawel Guzik

Magdalena Zawadzka

Adrian Zarebski

Agnieszka Dreas

Karolina Osowska

Katarzyna Kucwaj

Joanna Fogt

Marek Cholody

Mariusz Millik

Nicolas Beuzen

The present invention relates to derivatives of benzimidazoles of formula (I) as disclosed herein as well as pharmaceutical compositions comprising said derivatives. The derivates according to the present invention are serine/threonine and tyrosine kinase-inhibitors, particularly of PIM1-3- and DYRK1A-kinases and may particularly be used in the treatment of diseases linked to these kinases, such as e.g. leukemias, lymphomas, solid tumors and autoimmune disorders.

Benzimidazole derivatives as kinase inhibitors

Disclosed are substituted tricyclic benzimidazoles compounds as defined herein in formula (I) or pharmaceutically acceptable salts thereof. The compounds of the invention selectively inhibit CDK8 and are therefore useful for treating diseases related to this kinase, especially colorectal and melanoma cancers and other solid and hemathological malignancies, autoimmune diseases and inflammatory diseases. Also disclosed are processes for preparing these compounds. 

Substituted tricyclic benzimidazoles as kinase inhibitors

Benzimidazole derivatives as Kinase Inhibitors

A compound, a process for its preparation, a pharmaceutical composition, use of a compound, a method for modulating or regulating serine/threonine and tyrosine kinases and a serine/threonine and tyrosine kinases modulating agent. Novel small-molecule compounds with kinase inhibitory activity, having superior properties as pharmaceutical agents, production method thereof and uses thereof. In particular, new derivatives of tetrahalogenated benzimidazole with serine/threonine and tyrosine kinases inhibitory properties, preferably selected from the group of PIM, HIPK, DYRK, CLK, CDK, FLT, PKG, Haspin, MER, TAO, MNK, TRK kinases which exhibit superior pharmacological actions, and can be useful for the treatment of disease conditions, especially cancers depending on serine/threonine and tyrosine kinases, such as but not limited to leukemias and solid tumors.

Compound, a process for its preparation, a pharmaceutical composition, use of a compound, a method for modulating or regulating serine/threonine kinases and a serine/threonine kinases modulating agent

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Kraków, Poland

Krzysztof Brzózka