Vivolux Ab

Stig Linder

Rolf Larsson

Mårten Fryknäs

Padraig D'Arcy

Slavica Brnjic

The invention provides well-defined and stable pharmaceutical compositions comprising indole derivatives of general formula 1, a process for the preparation of di-hydrochloride salts comprising a high content of the pharmacologically active isomer suitable for industrial production, and use of these in pharmaceutical compositions. The invention further provides a method for use of said compounds for the treatment of cancer. The invention also provides methods to use these compounds in conjunction with other therapies commonly used for treating cancer diseases. 

Pharmaceutical composition comprising indole derivatives, process for preparation and use thereof

A cell permeable iron chelator, optionally in combination with an autophagy inhibiting agent, is used for treating a solid cancer tumor in a person. A preferred chelator is an alkyl substituted N-(1-pyridine-2-yl-methylidene)-N-(9H-1,3,4,9-tetraaza-fluoren-2-yl)-hydrazine. A preferred autophagy inhibiting agent is chloroquine. Also disclosed is a pharmaceutical composition comprising iron chelator, pharmaceutically acceptable carrier and, optionally, autophagy inhibiting agent; and a method of treating cancer by administering cancer combating-effective amount(s) of the iron chelator or the combination of iron chelator and autophagy inhibiting agent.

Treatment of solid tumours

A method for screening a compound to determine whether the compound is a proteasome deubiquitinating inhibitor of high specificity comprises contacting the compound with human 19S regulatory particles (19S RP) of 26S proteasome and determining whether the compound inhibits activity of deubiquitinating (DUB) enzymes UCHL5 and USP14; inhibition of UCHL5 and USCP14 activities indicates that the compound is a proteasome deubiquitinating inhibitor of high specificity.

Protease deubiquitinating inhibitor screening

In a cytotoxic compound of the general formula (I) R is H or methyl or methylene substituted by C-Cstraight or branched alkyl, Ris selected from the group consisting of H, C-Cstraight or branched alkyl, methoxy, methoxy substituted by from one to three fluorine, halogen; Ris H or C-Cstraight or branched alkyl; X is CH or N; Y is CH or N. 

Means and method for treating solid tumors

Compounds of the general structure S-1, wherein X and R-Rare defined in the specification, are capable of abrogating the deubiquitinating (DUB) activity of the 19S RP DUBs and are useful in methods and compositions for treating cancer, in particular, cancer tumors refractory to treatment by state-of-the-art chemotherapy. 

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Bromma, Sweden

Stig Linder