Helmholtz Zentrum Munchen Deutsches Forschungszentrum Fur Gesundheit Und Umwelt

Ludwig-Maximilians-Universitat München

Daniel Nagel

Daniel Krappmann

Robert Alan Chrusciel

Dolores Schendel

Stefani Spranger

Karl-Peter Hopfner

Florian Schlauderer

Katja Lammens

Dale L Kling

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 Nagel