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：US20190062324A1

公开(公告)日：2019-02-28

申请号：US16171236

申请日：2018-10-25

Applicant: CANCER RESEARCH TECHNOLOGY LIMITED

Inventor： Francesca Blum ,  James Lindsay Carr ,  Pritom Shah ,  Maria Del Mar Jimenez Quesada ,  Irene Farre Gutierrez

IPC: C07D417/14 ,  A61K31/5377 ,  A61K31/551 ,  A61K31/501 ,  A61K31/433 ,  A61K45/06 ,  A61K31/553 ,  C07D413/12 ,  C07D405/14 ,  C07D491/107 ,  C07D403/12 ,  C07D401/14 ,  A61K31/454 ,  A61K31/496 ,  C07D417/12 ,  C07D413/14 ,  A61K31/55

CPC classification number: C07D417/14 ,  A61K31/433 ,  A61K31/454 ,  A61K31/496 ,  A61K31/501 ,  A61K31/5377 ,  A61K31/55 ,  A61K31/551 ,  A61K31/553 ,  A61K45/06 ,  C07D401/14 ,  C07D403/12 ,  C07D405/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D491/107

Abstract: The present invention relates to compounds of formula I wherein R1, R2, R3, R4a, R4b, R4c, R4d, L, A, Q, W and HET 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：US10428061B2

公开(公告)日：2019-10-01

申请号：US16171236

申请日：2018-10-25

Applicant: CANCER RESEARCH TECHNOLOGY LIMITED

Inventor： Francesca Blum ,  James Lindsay Carr ,  Pritom Shah ,  Maria Del Mar Jimenez Quesada ,  Irene Farre Gutierrez

IPC: C07D417/14 ,  C07D403/12 ,  C07D405/14 ,  C07D413/12 ,  C07D417/12 ,  C07D491/107 ,  C07D401/14 ,  C07D413/14 ,  A61K31/433 ,  A61K31/454 ,  A61K31/496 ,  A61K31/501 ,  A61K31/5377 ,  A61K31/55 ,  A61K31/551 ,  A61K31/553 ,  A61K45/06

Abstract: The present invention relates to compounds of formula I wherein R1, R2, R3, R4a, R4b, R4c, R4d, L, A, Q, W and HET 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：US10138230B2

公开(公告)日：2018-11-27

申请号：US15547776

申请日：2016-02-04

Applicant: CANCER RESEARCH TECHNOLOGY LIMITED

Inventor： Francesca Blum ,  James Lindsay Carr ,  Pritom Shah ,  Maria Del Mar Jimenez Quesada ,  Irene Farre Gutierrez

IPC: C07D417/14 ,  C07D413/14 ,  C07D401/14 ,  C07D403/12 ,  C07D417/12 ,  C07D413/12 ,  C07D405/14 ,  A61K31/454 ,  A61K31/5377 ,  A61K31/433 ,  A61K31/496 ,  A61K31/551 ,  A61K31/55 ,  A61K31/553 ,  A61K31/501 ,  A61K45/06

Abstract: The present invention relates to compounds of formula (I): wherein R1, R2, R3, R4a, R4b, R4C, R4d, L, A, Q, W and HET 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：US10654846B2

公开(公告)日：2020-05-19

申请号：US15548079

申请日：2016-02-04

Applicant: CANCER RESEARCH TECHNOLOGY LIMITED

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

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

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.