公开(公告)号：US10954241B2

公开(公告)日：2021-03-23

申请号：US16093854

申请日：2017-04-18

Applicant: Cancer Research Technology Limited

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

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

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：US20240116938A1

公开(公告)日：2024-04-11

申请号：US18302313

申请日：2023-04-18

Applicant: Cancer Research Technology Limited

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

IPC: C07D487/04 ,  A61P35/00 ,  C07D471/04 ,  C07D519/00

CPC classification number: C07D487/04 ,  A61P35/00 ,  C07D471/04 ,  C07D519/00

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：US20210155628A1

公开(公告)日：2021-05-27

申请号：US17165151

申请日：2021-02-02

Applicant: Cancer Research Technology Limited

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

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

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：US20210047334A1

公开(公告)日：2021-02-18

申请号：US17075004

申请日：2020-10-20

Applicant: Cancer Research Technology Limited

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

IPC: C07D487/04 ,  A61P35/00 ,  C07D471/04 ,  C07D519/00

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：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：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.

公开(公告)号：US20230339954A1

公开(公告)日：2023-10-26

申请号：US17992049

申请日：2022-11-22

Applicant: Cancer Research Technology Limited

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

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

CPC classification number: C07D487/04 ,  C07D471/04 ,  C07D495/04 ,  C07D519/00

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：US11661423B2

公开(公告)日：2023-05-30

申请号：US17075004

申请日：2020-10-20

Applicant: Cancer Research Technology Limited

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

IPC: C07D487/04 ,  A61P35/00 ,  C07D471/04 ,  C07D519/00

CPC classification number: C07D487/04 ,  A61P35/00 ,  C07D471/04 ,  C07D519/00

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.