公开(公告)号：US12060367B2

公开(公告)日：2024-08-13

申请号：US18314445

申请日：2023-05-09

申请人： BOEHRINGER INGELHEIM INTERNATIONAL GMBH ,  VANDERBILT UNIVERSITY

发明人： Joachim Broeker ,  Jason Abbott ,  Jianwen Cui ,  Stephen W. Fesik ,  Julian Fuchs ,  Andreas Gollner ,  Lorenz Herdeis ,  Tim Hodges ,  Andrew Little ,  Andreas Mantoulidis ,  Jason Phan ,  Juergen Ramharter ,  Dhruba Sarkar ,  Christian Alan Paul Smethurst ,  Kevin Sokol ,  Heinz Stadtmueller ,  Qi Sun ,  Matthias Treu ,  Alex Waterson ,  Birgit Wilding ,  Tobias Wunberg

IPC分类号： C07D498/10 ,  A61P1/00 ,  A61P1/18 ,  A61P11/00 ,  A61P17/00 ,  A61P35/00 ,  C07D519/00

CPC分类号： C07D498/10 ,  A61P1/00 ,  A61P1/18 ,  A61P11/00 ,  A61P17/00 ,  A61P35/00 ,  C07D519/00

摘要： The present invention encompasses compounds of formula (I)






wherein R1a, R1b, R2a, R2b, Z, R3 to R5, A, p, U, V and W have the meanings given in the claims and specification, their use as inhibitors of KRAS, pharmaceutical compositions and preparations containing such compounds and their use as medicaments/medical uses, especially as agents for treatment and/or prevention of oncological diseases.

公开(公告)号：US11945812B2

公开(公告)日：2024-04-02

申请号：US17335620

申请日：2021-06-01

申请人： Boehringer Ingelheim International GmbH ,  Vanderbilt University

发明人： Jason Abbott ,  Joachim Broeker ,  Jianwen Cui ,  Steve W. Fesik ,  Andreas Gollner ,  Tim Hodges ,  Jale Karolyi-Oezguer ,  Andrew Little ,  Andreas Mantoulidis ,  Jason Phan ,  Dhruba Sarkar ,  Christian Alan Paul Smethurst ,  Qi Sun ,  Matthias Treu ,  Alex Waterson

IPC分类号： C07D521/00 ,  A61K31/381 ,  A61K31/506 ,  A61P35/00 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D471/10 ,  C07D487/04 ,  C07D487/08 ,  C07D487/10

CPC分类号： C07D413/14 ,  A61K31/506 ,  A61P35/00 ,  C07D409/14 ,  C07D417/14 ,  C07D471/04 ,  C07D471/10 ,  C07D487/04 ,  C07D487/08 ,  C07D487/10

摘要： The present invention encompasses compounds of formula (I)




wherein R1a, R1b, R2a, R2b, Z, R3 to R5, A, p, U, V, W, L and E have the meanings given in the claims and specification, their use as inhibitors of mutant Ras family proteins, pharmaceutical compositions and preparations containing such compounds and their use as medicaments/medical uses, especially as agents for treatment and/or prevention of oncological diseases.

公开(公告)号：US11318137B2

公开(公告)日：2022-05-03

申请号：US16500369

申请日：2017-05-17

申请人： VANDERBILT UNIVERSITY

发明人： Alex G. Waterson ,  Jason R. Abbott ,  J. Phillip Kennedy ,  Stephen W. Fesik ,  Qi Sun ,  Jason Phan ,  Michael C. Burns ,  Pratiq Patel

IPC分类号： C07D239/95 ,  A61K31/517 ,  A61K31/5377 ,  C07D401/10 ,  C07D401/14 ,  C07D403/10 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/10 ,  C07D413/14

摘要： The present invention relates to quinazoline compounds and compositions that modulate Ras signaling. Compounds and compositions of the present invention are useful in the treatment of cancers and other disease states associated with Ras dysfunction (e.g., Ras-associated autoimmune leukoproliferative disorder, or certain types of mitochondrial dysfunction) in a subject, for example a mammal or a human.

公开(公告)号：US20200253974A1

公开(公告)日：2020-08-13

申请号：US16500369

申请日：2017-05-17

申请人： VANDERBILT UNIVERSITY

发明人： Alex G. Waterson ,  Jason R. Abbott ,  J. Phillip Kennedy ,  Stephen W. Fesik ,  Qi Sun ,  Jason Phan ,  Michael C. Burns ,  Pratiq Patel

IPC分类号： A61K31/517 ,  C07D239/95 ,  C07D405/12 ,  C07D409/12 ,  C07D405/14 ,  C07D403/12 ,  C07D401/10 ,  C07D403/10 ,  C07D401/14 ,  C07D413/14 ,  A61K31/5377 ,  C07D413/10

摘要： The present invention relates to quinazoline compounds and compositions that modulate Ras signaling. Compounds and compositions of the present invention are useful in the treatment of cancers and other disease states associated with Ras dysfunction (e.g., Ras-associated autoimmune leukoproliferative disorder, or certain types of mitochondrial dysfunction) in a subject, for example a mammal or a human.