Merck Patent Gmbh

Joerg Bomke

Hans-Peter Buchstaller

Markus Klein

Christina Esdar

Ulrich Emde

Hans Peter Buchstaller

Frank Zenke

Roland Kellner

The invention relates to a method for screening compounds, which inhibit MetAP2 activity, by providing a cellular system or a sample thereof being capable of expressing MetAP2 and/or EEF1A, incubating at least a portion of the system with compounds to be screened, and detecting MetAP2 inhibition by determining EEF1A with N-terminal methionine residue (MetEEF1A). Another object of the invention concerns a method for monitoring physiological and/or pathological conditions, which are caused, mediated and/or propagated by MetAP2 activity, by administering an effective amount of at least a single compound to a mammal in need of such treatment and determining MetEEF1A in a biological sample withdrawn from the mammal. The invention also relates to the use of EEF1A as biomarker.

Use of EEF1A as biomarker and a method of screening MetAP2 inhibitors

Compounds of the formula (I), in which X, X, L, Y, R, R, R, R, R, R, R, R, Rhave the meanings indicated in claim, are PI3K inhibitors and can be employed, inter alia, for the treatment of autoimmune diseases, inflammation, cardiovascular diseases, neurodegenerative diseases and tumors.

Pyridinylimidazolone derivatives for the inhibition of PI3 kinases

Compounds of the formula (I), in which X, Rand Rhave the meanings indicated in claim, are PI3K inhibitors and can be employed, inter alia, for the treatment of autoimmune diseases, inflammation, cardiovascular diseases, neurodegenerative diseases and tumors.

Pyrazolopyrimidine derivatives

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Heidelberg, Germany

Joerg Bomke