Oslo University Hospital Hf

Forschungsverbund Berlin E.v.

Oslo Universitetssykehus Hf

University of Oulu

Stefan Krauss

Jo Waaler

Daniel Dale Holsworth

Ondrej Machon

Andrey Edward Voronkov

Anita Wegert

Ruben Gerardus George Leenders

Marc Nazare

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

The present invention relates to compounds of formula I, to processes for their preparation, to pharmaceutical formulations containing such compounds and to their use in therapy:  Such compounds find particular use in the treatment and/or prevention of conditions or diseases which are affected by over-activation of signaling in the Wnt pathway and increased presence of nuclear &#x3b2;-catenin. For example, these may be used in preventing and/or retarding proliferation of tumor cells and metastasis, for example carcinomas such as colon carcinomas.

Triazole derivatives as Wnt signaling pathway inhibitors

The present invention relates to compounds of formula (I), to processes for their preparation, to pharmaceutical formulations containing such compounds and to their use in therapy: Such compounds find particular use in the treatment and/or prevention of conditions or diseases which are affected by over-activation of signaling in the Wnt pathway and increased presence of nuclear &#x3b2;-catenin. For example, these may be used in preventing and/or retarding proliferation of tumor cells and metastasis, for example carcinomas such as colon carcinomas. 

The present invention relates to new compounds of formula I, to processes for their preparation, to pharmaceutical formulations containing such compounds and to their use in therapy. Such compounds find particular use in the treatment and/or prevention of conditions or diseases which are affected by over-activation of signaling in the Wnt pathway. For example, these may be used in preventing and/or retarding proliferation of tumor cells, for example carcinomas such as colon carcinomas. 

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Eidsvoll Verk, Norway

Stefan Krauss