Gilead Sciences, Inc.

Inthera Bioscience Ag

Epitherapeutics Aps

Farman Ullah

Marc A Labelle

Ramkrishna Reddy Vakiti

Thomas Boesen

Mukund Mehrotra

Cyril Cook

Qasim Khan

Ying Yang

Neerja Saraswat

Jean-d'amour K Twibanire

Ulrich Kessler

Kevin R D Johnson

Matinder Kaur

Valentino Cattori

Marc Labelle

Utpal Sharma

Dastagiri Dudekula

Rui Zhang

Kevin RD Johnson

The present invention relates to novel compounds of formula (I) or formula (Ia) pharmaceutically-acceptable salts, hydrates, solvates, or stereoisomers thereof, and pharmaceutical compositions of these compounds which are useful for preventive and therapeutic use in human and veterinary medicine.

Oxopiperazine derivatives

The present application discloses compounds capable of modulating the activity of histone demethylases (HDMEs), which are useful for prevention and/or treatment of diseases in which genomic dysregulation is involved in the pathogenesis, such as e.g. cancer. The present application also discloses pharmaceutical compositions comprising said compounds and the use of such compounds as a medicament. The compounds take the form 

Inhibitors of histone demethylases

The present application relates to compounds being of Formula (I), (II), (III), (IV), (V), (VI), (IIIa), (IIIb), (IIIc), (IIId), (IIIe), (IIIf), and (IIIg). Compounds of Formula (I) have the structure: wherein Q, R, R, R, M, A and Y are as defined herein. The compounds of the application can modulate the activity of histone demethylases (HDMEs), and can be useful for the prevention and/or treatment of diseases in which genomic dysregulation is involved in the pathogenesis, e.g., cancer.

Compounds and methods for inhibiting histone demethylases

Compounds of the form In which Q is selected from &#x2014;CH&#x2550;NR, &#x2014;W, &#x2014;CHNHR, &#x2014;CH&#x2550;O and &#x2014;CH(OR)capable of modulating the activity of histone demethylases (HDMEs), which are useful for prevention and/or treatment of diseases in which genomic dysregulation is involved in the pathogenesis, such as e.g. cancer and formulations and methods of use of such compounds.

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Winnipeg, Canada

Farman Ullah