Helmholtz Zentrum Munchen Deutsches Forschungszentrum Fur Gesundheit Und Umwelt

Technische Universitat Munchen

Ludwig-Maximilians-Universitat München

Helmholtz Zentrum München Deutsches Forschungszentrum Für Gesundheit Und Umweld (Gmbh)

Helmholtz Zentrum Munchen

Daniel Krappmann

Daniel Nagel

Robert Alan Chrusciel

Dolores Schendel

Stefani Spranger

Karl-Peter Hopfner

Katja Lammens

Andrea Eitelhuber

Dale L Kling

Steven Verhelst

Florian Schlauderer

The present invention provides means and methods for selectively detecting activated MALT1 in a sample. Moreover, the present invention provides a method for diagnosing diseases, which are characterized by an increased MALT1 activity. Finally, the present invention provides methods for identifying patients which are amenable to treatment with a therapeutic agent capable of inhibiting MALT1 activity.

Means and methods for detecting activated MALT1

The present invention relates to the (S)-enantiomer of mepazine, its applicability in therapy, a pharmacological composition comprising (S)-mepazine, and processes for the preparation of (S)-mepazine and one of its intermediates.

(S)-enantiomer of mepazine

The invention relates to a compound for use in treating a cancer, wherein the cancer depends on the proteolytic activity of the MALT1 protease, and wherein the compound has the general formula (I) wherein X is N or C; Y is S, O, SO, SO, NH, CO, CH, CH&#x2550;CH, or CH&#x2014;CH; ( )is a C-Clinear or branched alkyl chain; A is NRR, or OR, or HET; Rand Rin each occurrence are independently selected from &#x2014;H, &#x2014;CH, &#x2014;OH, &#x2014;OCH, &#x2014;SCH, &#x2014;F, &#x2014;Cl, &#x2014;CF, &#x2014;NH, and &#x2014;COOH; R, R, and Rare H, or C-Clinear or branched alkyl groups, and HET is a heterocyclic ring of 5, 6, or 7 members, wherein the ring atoms can be C, O, N, or S, the ring can be saturated or aromatic, and the ring can be substituted with H or C-Clinear or branched alkyl groups; or a pharmaceutically acceptable salt, prodrug, enantiomer, diastereomer, racemic mixture, crystalline form, amorphous form, unsolvated form or solvate of said compound. The compound of the invention may further be used in the treatment of MALT1-dependent immune diseases.

Selective inhibition of MALT1 protease by phenothiazine derivatives

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Munich, Germany

Daniel Krappmann