Cancer Research Technology Limited

Astrazeneca Ab

Mark David Charles

Maurice Raymond Verschoyle Finlay

Johannes Wilhelmus Maria Nissink

Chukuemeka Tennyson Ekwuru

Gregory R Ott

Emma Louise Carswell

Katherine M Fowler

Jonathan R Roffey

Maurice Raymond Finlay

Piotr Antoni Raubo

Jonathan James Gordon Winter

Joanna L Brookfield

Mathew L Calder

Frederic Elustondo

Daniel James Ford

Johannes Wilhelmus Nissink

Benjamin J Dugan

Nathaniel J T Monck

Neil Tremayne

Matt Wood

Anne Cochi

Fred Elustondo

Frederic Georges Marie Leroux

Gurwinder Sidhu

Emma L Carswell

Nathaniel JT Monck

Frédéric Elustondo

James Matthew Wood

Nathaniel Jt Monck

Jonathan James Winter

The present invention relates to compounds of formula I as defined herein, and salts and solvates thereof, that function as inhibitors of cell division cycle 7 (Cdc7) kinase enzyme activity. The present invention also relates to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative disorders, such as cancer, as well as other diseases or conditions in which Cdc7 kinase activity is implicated.

Pyrimidinone derivatives as CDC7 inhibitors

A compound of Formula (I): or a pharmaceutically acceptable salt thereof, where: Q can be 1,2,4-triazin-3-yl, pyridazin-3-yl, 6-methylpyridazin-3-yl, or 6-fluoropyridazin-3-yl; Rcan be hydrogen, methoxy, trifluoromethoxy, oxetan-3-yl, 3-fluoroazetidin-1-yl, 3-methoxyazetidin-1-yl, or 3,3-difluoroazetidin-1-yl; Rcan be hydrogen or fluoro; Rcan be hydrogen or methoxy; and Rcan be methoxy, ethoxy, or methoxymethyl; provided that when Ris hydrogen, methoxy or trifluoromethoxy, then Ris not hydrogen, and/or Ris methoxymethyl. The compound of formula (I) can inhibit glutaminase, e.g., GLS1.

1,3,4-thiadiazole compounds and their use in treating cancer

The present invention relates to compounds of formula I as defined herein, and salts and solvates thereof, that function as inhibitors of cell division cycle 7 (Cdc7) kinase enzyme activity. The present invention also relates to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative disorders, such as cancer, as well as other diseases or conditions in which Cdc7 kinase activity is implicated. 

Pyrimidinone derivatives as Cdc7 inhibitors

The present invention relates to compounds of formula (I), and salts and solvates thereof, that function as inhibitors of cell division cycle 7 (Cdc7) kinase enzyme activity: wherein X, R, R, and n are each as defined herein. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative disorders, such as cancer, as well as other diseases or conditions in which Cdc7 kinase activity is implicated.

Preparation and uses of pyrimidinone derivatives

The specification relates to compounds of Formula (I): and pharmaceutically acceptable salts thereof, where Q, R, Rand Rhave any of the meanings defined herein. The specification also relates to the use of such compounds and salts thereof to treat or prevent GLS1 mediated disease, including cancer. The specification further relates to crystalline forms of compounds of Formula (I) and pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising such compounds and salts; kits comprising such compounds and salts; methods of manufacture of such compounds and salts; intermediates useful in the manufacture of such compounds and salts; and to methods of treating GLS1 kinase mediated disease, including cancer, using such compounds and salts.

1, 3, 4-thiadiazole compounds and their use in treating cancer

The specification relates to compounds of Formula (I), and pharmaceutically acceptable salts thereof, where Q, R, Rand Rhave any of the meanings defined herein. The specification also relates to the use of such compounds and salts thereof to treat or prevent GLS1 mediated disease, including cancer. The specification further relates to crystalline forms of compounds of Formula (I) and pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising such compounds and salts; kits comprising such compounds and salts; methods of manufacture of such compounds and salts; intermediates useful in the manufacture of such compounds and salts; and to methods of treating GLS1 kinase mediated disease, including cancer, using such compounds and salts. 

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Cambridge, United Kingdom

Mark David Charles