Dsm IP Assets B.v.

Università Degli Studi Di Roma "la Sapienza"

Universita′ Degli Studi Di Milano

Universitá Degli Studi Di Pavia

Fondazione Ieo

Andrea Mattevi

Saverio Minucci

Antonello Mai

Werner Bonrath

Nicholas Turner

Martin Schürmann

Jose Ruben Casstellanos

Michele Tavanti

Fabio Parmeggiani

The present invention relates to novel process for the production of ketoisophorone via biocatalytic conversion of isophorone, in particular a one-pot biocatalytic system for conversion of α-isophorone in a two-step oxidation process, with a first oxidation being catalyzed by a heme containing oxidoreductase such as a cytochrome P450 monooxygenase followed by another oxidation which can be either a chemical reaction or a biocatalytic reaction, in particular wherein the oxidation is catalyzed by an NAD(P) or NADP(H)-dependent oxidoreductase. The invention further provides polypeptides and nucleic acid sequences coding for cytochrome P450 monooxygenase with modified (higher) substrate selectivity, total turnover numbers and/or (re)activity compared to the wild-type enzyme. Ketoisophorone is useful as building block in the synthesis of vitamins and carotenoids.

Regioselective hydroxylation of isophorone

Tranylcypromine derivatives useful as therapeutic agents, particularly for the prevention and/or treatment of diseases and conditions associated with the activity of histone demethylases LSD1 and LSD2, such as the diseases characterized by deregulation of gene transcription, cell differentiation and proliferation, e.g. tumors, viral infections, are herein described. These compounds belong to the structural formula (I) wherein A and Rare as defined in the specification. The invention also relates to the preparation of these compounds, as well as to compositions containing them and to therapeutic use thereof. 

Tranylcypromine derivatives as inhibitors of histone demethylases LSD1 and/or LSD2

Growing community of inventors

Pavia, Italy

Andrea Mattevi