Cancer Research Technology Limited

Cellcentric Limited

Silvia Paoletta

George Hynd

Jonathan Mark Sutton

Allan Michael Jordan

Euan Alexander Fraser Fordyce

Bohdan Waszkowycz

Rebecca Newton

Jonathan Shannon

David Michel Adrien Taddei

Gareth Harbottle

Neil Anthony Pegg

Stuart Thomas Onions

Richard James Brown

Don Smyth

Ting Qin

The present invention relates to compounds of formula I that function as inhibitors of RET (rearranged during transfection) kinase enzyme activity: wherein HET, X, X, X, X, integer a and Rare 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 RET kinase activity is implicated. 

Heterocyclic compounds as RET kinase inhibitors

The present invention relates to compounds of Formula I that function as inhibitors of RET (rearranged during transfection) kinase enzyme activity: wherein HET, bonds a, b, c and d, X, X, X, X, R, and Rare 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 RET kinase activity is implicated. 

A compound which is an arylimidazolyl isoxazole of formula (I): (Formula (I)) or a pharmaceutically acceptable salt thereof. The compound has activity in modulating the activity of p300 and/or CBP and is used to treat cancer, particularly prostate cancer. 

Pharmaceutical compounds

The present invention relates to compounds of Formula I that function as inhibitors of RET (rearranged during transfection) kinase enzyme activity: wherein HET, bonds a, b, c and d, X, X, X, X, R, and Rare 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 RET kinase activity is implicated.

Heterocyclic compounds as ret kinase inhibitors

The present invention relates to compounds of formula I that function as inhibitors of RET (rearranged during transfection) kinase enzyme activity: wherein HET, X, X, X, X, integer a and Rare 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 RET kinase activity is implicated.

A compound which is a benzimidazole of formula (I): wherein X is a 5-membered heteroaryl group selected from the following: or a pharmaceutically acceptable salt thereof. The compound has activity in modulating the activity of p300 and/or CBP and is used to treat cancer, particularly prostate cancer. 

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Nottingham, United Kingdom

Silvia Paoletta