University of Notre Dame Du Lac

Klinikum Der Universitat Munchen

Leibnizinstitut Für Naturstoff-Forschung Und Infektionsbiologie E. V. -Hans-Knöll-Institut

Leibniz-institut Fuer Naturstoff-forschung Und Infektionsbiologie

Leibniz-institut Für Naturstoff-forschung Und Infektionsbiologie E.v. -hans-knöll-institut- (hki)

Leibniz-Institut Für Naturstoff-Forschung Und Infektionsbiologie

Florian Kloss

Christian Hertweck

Marvin J Miller

Hans-Martin Dahse

Axel Brakhage

Ute Möllmann

Martin Roth

Sebastian Schieferdecker

Julia Dreisbach

Kamil Philip Wojtas

Swantje Behnken

Keishi Ishida

Thorger Lincke

Toni Neuwirth

Veit Haensch

The present invention relates to a method for the metal-free preparation of a biaryl compound by a photosplicing reaction and its use in the preparation of chemical compounds, preferably of active ingredients e.g. in the fields of pharmaceuticals and agrochemicals. In particular, it refers to a method for the regiocontrolled preparation of a biaryl compound of formula (I): Ar&#x2014;Ar' by photochemically reacting a precursor compound of formula (II): Ar&#x2014;L&#x2014;Ar&#x2032; to form a biaryl compound of general formula: Ar&#x2014;L&#x2014;Ar&#x2032;(II)&#x2192;Ar&#x2014;Ar&#x2032; (I) wherein Ar and Ar&#x2032;, independently of each other, represent an unsubstituted or substituted C6-C20 aryl group or a heteroaryl group with 5-20 ring atoms selected from carbon, nitrogen, oxygen and sulfur, and L represents a group &#x2014;X&#x2014;Y&#x2014;Z&#x2014; as defined herein. The biaryl compounds are generally suitable as intermediates or key building blocks in a very broad spectrum of organic chemical syntheses and their respective utilities. Their use within the field of synthesis of active ingredients is an aspect of the invention, and their use in the preparation of pharmaceutically active ingredients is particularly preferred.

Method for the metal-free preparation of a biaryl by a photosplicing reaction and their uses

The present invention relates to the general field of treatment of infectious diseases of mammals (humans and animals) caused by bacteria, in particular to the treatment of diseases like tuberculosis (TB), Buruli ulcer and leprosy caused by mycobacteria. The invention aims at the generation of a new series of benzothiazinone compounds having the potential to overcome the above mentioned problems. In a preferred embodiment the invention is concerned with compounds of the general formula (I) whereinRrepresents NO,Rrepresents CF,at least one of the substituents Rand Ris OH, SR, NHR, CN, N, a saturated or unsaturated, optionally halogenated, linear or branched aliphatic radical having 1-4 carbon atoms, linear or branched C-Calkoxy, C-Cacyl, and the other of Rand Rmay in addition be hydrogen,Rrepresents a 2-methyl-1,4-dioxa-8-azaspiro[4.5]decan-8-yl or a 4-(cyclo-hexylmethyl)piperazin-1-yl group andRand Rindependently of each other are hydrogen or a C-Calkyl group and/or a pharmaceutically acceptable salt thereof.

Antimicrobial compounds, their use for the treatment of mammalian infections and a new metabolic mechanism

This invention relates to the field of biologically active compounds and specifically to closthioamides, pharmaceutical compositions comprising these compounds, and their use as antibiotic, antifungal, and/or cytotoxic agent.

Closthioamides, compositions, and methods for treating bacterial or fungal infections or cancer

Growing community of inventors

Jena, Germany

Florian Kloss