公开(公告)号：US20220226279A1

公开(公告)日：2022-07-21

申请号：US17605818

申请日：2020-04-20

申请人： Bayer Aktiengesellschaft ,  The Broad Institute, Inc.

发明人： Léa Aurelie Bouché ,  Daniel Korr ,  Antonius ter Laak ,  Ernesto Amaury Fernandez-Montalvan ,  Naomi Barak ,  Roman Hillig ,  Roland Neuhaus ,  Matyas Gorjanacz ,  Vera Pütter ,  Stefan Niklaus Gradl ,  Simon Anthony Herbert ,  Steven James Ferrara ,  Craig Strathdee ,  Jacob Jaffe

IPC分类号： A61K31/343 ,  C07D307/85 ,  C07D405/12 ,  C07D407/12 ,  C07D405/04 ,  C07D333/70 ,  C07D487/04 ,  C07D413/12 ,  A61K31/4709 ,  A61K31/443 ,  A61K31/351 ,  A61K31/4025 ,  A61K31/4525 ,  A61K31/381 ,  A61K31/4155 ,  A61K31/5025 ,  A61K31/4035 ,  A61K31/357 ,  A61K31/4245 ,  A61P35/00

摘要： The present invention provides acyl sulfonamide compounds of general formula (I): in which X, R1, R2, R3, R4, R5, R6′ Ra and Rb are as described and defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds, and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of hyperproliferative disorders, as a sole agent or in combination with other active ingredients as well as methods of treating and/or prophylaxing diseases, particularly cancer, more particularly cancer in which KAT6A and/or KAT6B is focally amplified, said method comprising administering an effective amount of at least one compound of formula (I) to a subject in need thereof.

公开(公告)号：US20240279207A1

公开(公告)日：2024-08-22

申请号：US18032067

申请日：2021-10-14

申请人： The Broad Institute, Inc. ,  Bayer Aktiengesellschaft

发明人： Léa Bouché ,  Daniel Korr ,  Antonius ter Laak ,  Michael Kröber ,  Naomi Barak ,  Roman Hillig ,  Roland Neuhaus ,  Stefan Gradl ,  Jörg Wichard ,  Ernesto Amaury Fernamdez-Montalvan ,  Matyas Gorjanacz ,  Vera Pütter ,  Andreas Stutter ,  Steven James Ferrara

IPC分类号： C07D405/04 ,  A61K31/397 ,  A61K31/4025 ,  A61K31/404 ,  A61K31/4155 ,  A61K31/4192 ,  A61K31/422 ,  A61K31/4245 ,  A61K31/427 ,  A61K31/433 ,  A61K31/437 ,  A61K31/443 ,  A61K31/4525 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/498 ,  A61K31/5025 ,  A61K31/5365 ,  A61K31/5377 ,  A61K31/539 ,  A61P35/00 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/107 ,  C07D498/04

CPC分类号： C07D405/04 ,  A61K31/397 ,  A61K31/4025 ,  A61K31/404 ,  A61K31/4155 ,  A61K31/4192 ,  A61K31/422 ,  A61K31/4245 ,  A61K31/427 ,  A61K31/433 ,  A61K31/437 ,  A61K31/443 ,  A61K31/4525 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/498 ,  A61K31/5025 ,  A61K31/5365 ,  A61K31/5377 ,  A61K31/539 ,  A61P35/00 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/107 ,  C07D498/04

摘要： The present invention provides acyl sulfonamide compounds of general formula (I):






in which R1, R2, R3, R4, R5, R6, Ra and Rb are as described and defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds, and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of hyperproliferative disorders, as a sole agent or in combination with other active ingredients as well as methods of treatment and/or prophylaxis of diseases, particularly cancer, more particularly cancer in which KAT6A and/or KAT6B is focally amplified, said method comprising administering an effective amount of at least one compound of formula (I) to a subject in need thereof.

公开(公告)号：US20240287048A1

公开(公告)日：2024-08-29

申请号：US18032096

申请日：2021-10-14

申请人： The Broad Institute, Inc. ,  Bayer Aktiengesellschaft

发明人： Léa Bouché ,  Daniel Korr ,  Antonius ter Laak ,  Simon Herbert ,  Naomi Barak ,  Roman Hillig ,  Roland Neuhaus ,  Stefan Gradl ,  Jörg Wichard ,  Ernesto Amaury Fernandez-Montalvan ,  Matyas Gorjanacz ,  Vera Pütter ,  Robin Meier ,  Andreas Sutter ,  Steven James Ferrara

IPC分类号： C07D405/12 ,  A61K31/343 ,  A61K31/4155 ,  A61K31/443 ,  A61K31/4709 ,  A61P35/00 ,  C07D307/85 ,  C07D405/04

CPC分类号： C07D405/12 ,  A61K31/343 ,  A61K31/4155 ,  A61K31/443 ,  A61K31/4709 ,  A61P35/00 ,  C07D307/85 ,  C07D405/04

摘要： The present invention provides acyl sulfonamide compounds of general formula (I):






in which R1, R2, R3, R4, R5 and R6 are as described and defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds, and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of hyperproliferative disorders, as a sole agent or in combination with other active ingredients as well as methods of treatment and/or prophylaxis of diseases, particularly cancer, more particularly cancer in which KAT6A and/or KAT6B is focally amplified, said method comprising administering an effective amount of at least one compound of formula (I) to a subject in need thereof.