公开(公告)号：US20230183197A1

公开(公告)日：2023-06-15

申请号：US17925493

申请日：2020-06-01

申请人： NeoPhore Limited

发明人： Julian Blagg ,  Jon Roffey ,  Martin Drysdale ,  Paul Winship ,  David Clark

IPC分类号： C07D295/16 ,  C07D239/26 ,  C07D209/44 ,  C07D207/12 ,  C07D211/42 ,  C07D213/16 ,  C07D471/04 ,  C07D231/12 ,  C07D249/04 ,  C07D401/12 ,  C07D217/04 ,  C07D217/16 ,  C07D265/36 ,  C07D209/08 ,  C07D215/08 ,  C07D405/12 ,  C07D401/04 ,  C07D403/12 ,  C07D403/04 ,  A61K45/06

CPC分类号： C07D295/16 ,  C07D239/26 ,  C07D209/44 ,  C07D207/12 ,  C07D211/42 ,  C07D213/16 ,  C07D471/04 ,  C07D231/12 ,  C07D249/04 ,  C07D401/12 ,  C07D217/04 ,  C07D217/16 ,  C07D265/36 ,  C07D209/08 ,  C07D215/08 ,  C07D405/12 ,  C07D401/04 ,  C07D403/12 ,  C07D403/04 ,  A61K45/06

摘要： The present invention relates to compounds of Formula (I) that target the MLH1 and/or PMS2 proteins that are components of the DNA Mismatch Repair (MMR) process:




wherein R1, R2, R3, R4, R6 and R10 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 MLH1 and/or PMS2 activity is implicated.

公开(公告)号：US20240293392A1

公开(公告)日：2024-09-05

申请号：US18570244

申请日：2022-07-18

申请人： NeoPhore Limited

发明人： Julian Blagg ,  Martin Drysdale ,  David Clark ,  Paul Winship

IPC分类号： A61K31/4725 ,  A61K31/4035 ,  A61K31/4375 ,  A61K31/496 ,  A61K31/501 ,  C07D209/44 ,  C07D217/06 ,  C07D401/12 ,  C07D405/14 ,  C07D471/04

CPC分类号： A61K31/4725 ,  A61K31/4035 ,  A61K31/4375 ,  A61K31/496 ,  A61K31/501 ,  C07D209/44 ,  C07D217/06 ,  C07D401/12 ,  C07D405/14 ,  C07D471/04

摘要： The present invention relates to compounds of Formula (I) that target the MLH1 or MLH1 and PMS2 proteins that are components of the DNA Mismatch Repair (MMR) process: Formula (I) wherein R6, Y1, Y2, A1, A2, A3, A4, R11, R12, R13 and R14 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 MLH1 or MLH1 and PMS2 activity is implicated.

公开(公告)号：US20230061002A1

公开(公告)日：2023-03-02

申请号：US17793912

申请日：2021-01-20

申请人： NeoPhore Limited

发明人： Julian Blagg ,  Jonathon Richard Anthony Roffey ,  Paul Colin Michael Winship ,  Gareth William Langley

IPC分类号： G01N33/573 ,  C07D209/44 ,  G01N33/68

摘要： The present invention relates to novel probe compounds of formulae I and II defined herein. The present invention also relates to methods of synthesising these novel probe compounds and to their use in assays and screens for determining the binding of a test molecule to the ATP-binding site of a target protein, such as, for example, the Mismatch Repair (MMR) component proteins PMS2 and MLH1, or for determining the location and/or quantity of such target proteins in a biological sample.