Forschungsverbund Berlin E.v.

Oslo Universitetssykehus Hf

Max-delbruck-centrum Fur Molekulare Medizin in Der Helmholtz-gemeinschaft

University of Oulu

Marc Nazare

Jens-Peter Von Kries

Edgar Specker

Anita Wegert

Ruben Gerardus George Leenders

Gerd Krause

Stefan Krauss

Jo Waaler

Michael Willenbrock

Wen-Ting Lo

Murat Kucukdisli

Hassane Belabed

Volker Haucke

Martin Neuenschwander

Patrick Marcinkowski

Jens Furkert

Inna Hoyer

Silke Radetzki

Peter Lindemann

Claus Scheidereit

Jens Peter Von Kries

Murat KÜCÜKDISLI

Compounds of the following formula: having defined substituents. The compounds can inhibit class II phosphoinositide 3-kinase (PI3K) signaling and are useful for the treatment of a medical condition associated with defective PI3K signaling, such as myopathy, cancer, diabetes, thrombosis or cardiovascular disease.

Heterocyclic compounds as class II phosphoinositide 3-kinase inhibitors

The present invention relates to compounds of formula (I), tautomers, stereoisomers, pharmaceutically acceptable salts and pro-drugs thereof, to processes for their preparation, to pharmaceutical compositions containing such compounds and to their use in therapy wherein a dashed line indicates an optional bond; X represents: a 5- or 6-membered, unsaturated heterocyclic group optionally substituted by one or more (e.g. 1, 2 or 3) substituents independently selected from halogen (i.e. F, Cl, Br, I), Calkyl (e.g. Calkyl), Chaloalkyl (e.g. Chaloalkyl), Calkoxy (e.g. Calkoxy), —CN, —NO, —N(R)2, and —SOR (where each R is independently H or Calkyl, e.g. H or Calkyl); a Ccycloalkyl group optionally substituted by one or more (e.g. 1 or 2) substituents independently selected from Calkyl (preferably Calkyl), Chaloalkyl (e.g. Chaloalkyl), and Calkoxy (e.g. Calkoxy); or an aryl group optionally substituted by one or more (e.g. 1, 2 or 3) substituents independently selected from halogen (i.e. F, Cl, Br, I), Calkyl (e.g Calkyl), Chaloalkyl (e.g. Chaloalkyl), and Calkoxy (e.g. Calkoxy); Y represents: an aryl or heteroaryl group optionally substituted by one or more (e.g. 1, 2 or 3) substituents independently selected from halogen (i.e. F, Cl, Br, I), Calkyl (e.g Calkyl), Chaloalkyl (e.g. Chaloalkyl), and Calkoxy (e.g. Calkoxy); a 5- or 6-membered, saturated heterocyclic group optionally substituted by one or more (e.g. 1, 2 or 3) substituents independently selected from Calkyl (preferably Calkyl), Chaloalkyl (e.g. Chaloalkyl), and Calkoxy (e.g. Calkoxy); or a Ccycloalkyl group optionally substituted by one or more (e.g. 1 or 2) substituents independently selected from Calkyl (preferably Calkyl), Chaloalkyl (e.g. Chaloalkyl), and Calkoxy (e.g. Calkoxy); and Z represents: an aryl group optionally substituted by one or more (e.g. 1, 2 or 3) substituents independently selected from halogen (i.e. F, Cl, Br, I), Calkyl (e.g. Calkyl), Chaloalkyl (e.g. Chaloalkyl), Calkoxy (e.g. Calkoxy), —CN, —NO, —N(R), and —SOR (where each R is independently H or Calkyl, e.g. H or Calkyl); or an unsaturated, 5- to 10-membered mono- or bicyclic heterocyclic group optionally substituted by one or more (e.g. 1, 2 or 3) substituents independently selected from halogen (i.e. F, Cl, Br, I), Calkyl (e.g. Calkyl), Chaloalkyl (e.g. Chaloalkyl), Calkoxy (e.g. Calkoxy), —CN, —NO, —N(R), and —SOR (where each R is independently H or Calkyl, e.g. H or Calkyl). These compounds find particular use in the treatment and/or prevention of a disease or disorder responsive to inhibition of tankyrase 1 and/or 2, for example a disorder which is mediated by tankyrase 1 and/or 2 such as cancer.

1,2,4-triazole derivatives as tankyrase inhibitors

A method is for treatment of a disease associated with genotoxic stress-induced inhibitor of nuclear factor-&#x3ba;B kinase/nuclear factor kappa-light chain enhancer of activated B cells (IKK/NF-&#x3ba;B) signaling. The method can include administering a compound to a subject having a cancer exhibiting genotoxic stress induced IKK/NF-&#x3ba;B activation.

Selective inhibitors of gentotoxic steress-induced IKK/NF-&#x3ba;B pathways

Chemical compounds are useful in the treatment of a subject afflicted by a thyroid disease. The compounds exhibit activity as thyroid-stimulating hormone receptor (TSHR) antagonists and can be used in the treatment of hyperthyroidism, Graves' disease, Graves' Ophthalmopathy and thyroid cancer.

Antagonists of the thyroid-stimulating hormone receptor (TSHR)

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Berlin, Germany

Marc Nazare