Cancer Research Technology Limited

Vernalis &r&d) Ltd.

Other

The Institute of Cancer Research

Glaxosmithkline Intellectual Property Development Limited

Vernalis (cambridge) Limited

Allan Michael Jordan

Bohdan Waszkowycz

George Hynd

Jonathan Mark Sutton

Simon Bedford

James R Hitchin

Niall M Hamilton

Karine Poullennec

Ian Yule

Rebecca Newton

Klenke Burkhard

Euan Alexander Fraser Fordyce

Silvia Paoletta

Kate Mary Smith

Alison E McGonagle

Colin P Hutton

Ian D Waddell

Martin Stockley

Brian William Dymock

Martin James Drysdale

Pritom Shah

Xavier Barril-Alonso

Ellen Catherine MacDonald

Christofe Fromont

William Henry Miller

Juan I Luengo

Stephen Martin Brown

Roger John Gillespie

Stuart Paul Romeril

Nicholas D Adams

Dick De Vos

Bryan Wayne King

Richard Simon Todd

Andrew B Benowitz

Gemma Caroline Stratton

Stanley J Schmidt

David T Fosbenner

Alexander Joseph Reif

Mei Li

Karen Anderson Evans

Roger J Butlin

María Lourdes Rueda Benede

Kristin M Goldberg

Christopher S Kershaw

Bodhan Waszkowycz

Ali Raoof

Nicholas J Lawrence

Alan Th McGown

Alison E Mcgonagle

Nicholas David Adams

Juan Ignacio Luengo

The present invention relates to compounds of formula I that function as inhibitors of PARG (Poly ADP-ribose glycohydrolase) enzyme activity: wherein R, R, R, R, W, X, X, X, X, X, X, X, c 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 PARG activity is implicated.

PARG inhibitory 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.

Compounds useful as RET 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. 

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. 

The present invention relates to compounds of formula I wherein A, A, A, R, R, R, R, R, R, L, Ar and Q are each as defined herein. The compounds of the present invention are inhibitors of autotaxin (ATX) enzyme activity. 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 (e.g. fibrosis) in which ATX activity is implicated.

Autotaxin inhibitory compounds

Compounds of formula (I) are Areceptor antagonists: Wherein Ris optionally substituted aryl or an optionally substituted 5- or 6-membered heteroaryl ring; Rand Rare independently selected from hydrogen, C-Calkyl, C-Ccycloalkyl, C-Ccycloalkyl-(C-C)-alkyl, aryl-(C-C)-alkyl optionally substituted in the ring part thereof, a 5- or 6-membered monocyclic heterocyclic group optionally linked via a C-Calkylene chain and optionally substituted in the ring part thereof, benzimidazol-2-yl-methyl, pyrid-3-yl-carbonyl, or (1-methyl-piperidin-4-yl)-carbonyl-methyl; or Rand Rtaken together with the nitrogen atom to which they are attached form an optionally substituted 5- or 6-membered ring; Ris C-Calkyl, C-Calkenyl, &#x2014;N(&#x2014;R)&#x2014;R, or optionally substituted heteroarylmethylamino; and Rand Rare independently selected from hydrogen or C-Calkyl; or Rand Rtaken together with the nitrogen atom to which they are attached form an optionally substituted 4- to 6-membered saturated ring.

Thienopyrimidine compounds

The present invention relates to compounds of formula I that function as inhibitors of PARG (Poly ADP-ribose glycohydrolase) enzyme activity: wherein R, R, R, R, R, W, X, X, X, X, X, X, X, c 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 PARG activity is implicated. 

The invention is directed to substituted pyridine derivatives. Specifically, the invention is directed to compounds according to Formula (Iar): wherein Y, X, X, R, R, R, Rand Rare as defined herein; or a pharmaceutically acceptable salt or prodrug thereof. The compounds of the invention are selective inhibitors of DNMT1 and can be useful in the treatment of cancer, pre-cancerous syndromes, beta hemoglobinopathy disorders, sickle cell disease, sickle cell anemia, and beta thalassemia, and diseases associated with DNMT1 inhibition. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting DNMT1 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.

Substituted pyridines as inhibitors of DNMT1

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.

The present invention relates to compounds of formula I, wherein A, A, A, R, R, R, R, R, R, L, Ar and Q are each as defined herein. The compounds of the present invention are inhibitors of autotaxin (ATX) enzyme activity. 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 (e.g. fibrosis) in which ATX activity is implicated. 

The present invention relates to compounds of formula I that function as inhibitors of PARG (Poly ADP-ribose glycohydrolase) enzyme activity wherein R, R, R, R, R, W, X, X, X, X, X, X, X, c 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 PARG activity is implicated. 

2,4-dioxo-quinazoline-6-sulfonamide derivatives as inhibitors of PARG

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Manchester, United Kingdom

Allan Michael Jordan