公开(公告)号：US20190263819A1

公开(公告)日：2019-08-29

申请号：US16093858

申请日：2017-04-18

Applicant: Cancer Research Technology Limited

Inventor： Allan Jordan ,  Rebecca Newton ,  Bohdan Waszkowycz ,  Jonathan Mark Sutton ,  George Hynd ,  Silvia Paoletta ,  Euan Alexander Fraser Fordyce

IPC: C07D487/04 ,  A61P35/00 ,  C07D471/04

Abstract: The present invention relates to compounds of formula I that function as inhibitors of RET (rearranged during transfection) kinase enzyme activity: wherein HET, X1, X2, X3, X4, integer a and R3 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 RET kinase activity is implicated.

公开(公告)号：US11352361B2

公开(公告)日：2022-06-07

申请号：US16604332

申请日：2018-04-13

Applicant: Cancer Research Technology Limited

Inventor： Allan Jordan ,  Rebecca Newton ,  George Hynd ,  Jonathan Mark Sutton ,  Bohdan Waszkowycz

IPC: C07D487/04

Abstract: 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, X1, X2, X3, X4, R2, and R3 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 RET kinase activity is implicated.

公开(公告)号：US20200157107A1

公开(公告)日：2020-05-21

申请号：US16604332

申请日：2018-04-13

Applicant: Cancer Research Technology Limited

Inventor： Allan Jordan ,  Rebecca Newton ,  George Hynd ,  Jonathan Mark Sutton ,  Bohdan Waszkowycz

IPC: C07D487/04

Abstract: 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, X1, X2, X3, X4, R2, and R3 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 RET kinase activity is implicated.

公开(公告)号：US20190106425A1

公开(公告)日：2019-04-11

申请号：US16093854

申请日：2017-04-18

Applicant: Cancer Research Technology Limited

Inventor： Allan Jordan ,  Rebecca Newton ,  Bohdan Waszkowycz ,  Jonathan Mark Sutton ,  George Hynd ,  Silvia Paoletta ,  Euan Alexander Fraser Fordyce

IPC: C07D487/04 ,  C07D519/00 ,  C07D495/04 ,  C07D471/04

Abstract: 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, X1, X2, X3, X4, R2, and R3 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 RET kinase activity is implicated.

公开(公告)号：US10239843B2

公开(公告)日：2019-03-26

申请号：US15533804

申请日：2015-12-11

Applicant: CANCER RESEARCH TECHNOLOGY LIMITED

Inventor： Alison E. McGonagle ,  Allan Jordan ,  Bohdan Waszkowycz ,  Colin Hutton ,  Ian Waddell ,  James R. Hitchin ,  Kate Mary Smith ,  Niall M. Hamilton

IPC: A61K31/517 ,  C07D239/96 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D215/227 ,  C07D217/22 ,  C07D217/24 ,  C07D401/06 ,  C07D403/06 ,  C07D403/14 ,  C07D405/06 ,  C07D409/14 ,  C07D239/88 ,  C07D239/90 ,  C07D239/91 ,  C07D413/06 ,  C07D417/06 ,  C07D241/44 ,  C07D417/14 ,  C07D237/32 ,  C07D471/04

Abstract: The present invention relates to compounds of formula I that function as inhibitors of PARG (Poly ADP-ribose glycohydrolase) enzyme activity wherein R1a, R1b, R1c, R1d, R1e, W, X1, X2, X3, X4, X5, X6, X7, 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.

公开(公告)号：US11453666B2

公开(公告)日：2022-09-27

申请号：US16826046

申请日：2020-03-20

Applicant: Cancer Research Technology Limited

Inventor： Martin Lee Stockley ,  Ellen Catherine Macdonald ,  Pritom Shah ,  Allan Jordan ,  James Hitchin ,  Niall Hamilton

IPC: A61P1/00 ,  A61P1/16 ,  A61P29/00 ,  A61P31/20 ,  A61P31/14 ,  A61P31/12 ,  A61P3/10 ,  A61P7/12 ,  A61P17/00 ,  A61P17/04 ,  A61P17/02 ,  A61P35/00 ,  A61P35/02 ,  A61P7/04 ,  A61P7/02 ,  A61P13/02 ,  A61P13/12 ,  A61P9/12 ,  A61P9/00 ,  A61P43/00 ,  A61P19/04 ,  A61K31/5025 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/5377 ,  A61K31/404 ,  A61K31/551 ,  A61K31/55 ,  A61K31/496 ,  A61K31/4184 ,  A61K45/06 ,  C07D235/02 ,  C07D471/04 ,  A61K31/437

Abstract: The present invention relates to compounds of formula I wherein A1, A2, A3, R1, R2, R3, R4, R5, R6, 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.

公开(公告)号：US20200283435A1

公开(公告)日：2020-09-10

申请号：US16826046

申请日：2020-03-20

Applicant: Cancer Research Technology Limited

Inventor： Martin Lee Stockley ,  Ellen Catherine Macdonald ,  Pritom Shah ,  Allan Jordan ,  James Hitchin ,  Niall Hamilton

IPC: C07D471/04 ,  C07D235/02 ,  A61K31/4184 ,  A61K31/5025 ,  A61K31/404 ,  A61K45/06 ,  A61K31/437 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/55 ,  A61K31/551

Abstract: The present invention relates to compounds of formula I wherein A1, A2, A3, R1, R2, R3, R4, R5, R6, 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.

公开(公告)号：US20240132504A1

公开(公告)日：2024-04-25

申请号：US18312069

申请日：2023-05-04

Applicant: Cancer Research Technology Limited

Inventor： Allan Jordan ,  Rebecca Newton ,  George Hynd ,  Jonathan Mark Sutton ,  Bohdan Waszkowycz

IPC: C07D487/04

CPC classification number: C07D487/04

Abstract: 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, X1, X2, X3, X4, R2, and R3 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 RET kinase activity is implicated.

公开(公告)号：US11680068B2

公开(公告)日：2023-06-20

申请号：US17738278

申请日：2022-05-06

Applicant: Cancer Research Technology Limited

Inventor： Allan Jordan ,  Rebecca Newton ,  George Hynd ,  Jonathan Mark Sutton ,  Bohdan Waszkowycz

IPC: C07D487/04

CPC classification number: C07D487/04

Abstract: 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, X1, X2, X3, X4, R2, and R3 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 RET kinase activity is implicated.

公开(公告)号：US20220348585A1

公开(公告)日：2022-11-03

申请号：US17738278

申请日：2022-05-06

Applicant: Cancer Research Technology Limited

Inventor： Allan Jordan ,  Rebecca Newton ,  George Hynd ,  Jonathan Mark Sutton ,  Bohdan Waszkowycz

IPC: C07D487/04

Abstract: 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, X1, X2, X3, X4, R2, and R3 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 RET kinase activity is implicated.