公开(公告)号：US20250002485A1

公开(公告)日：2025-01-02

申请号：US18441380

申请日：2024-02-14

Applicant: Boehringer Ingelheim International GmbH ,  Vanderbilt University

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

Abstract: 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：US20250019385A1

公开(公告)日：2025-01-16

申请号：US18676758

申请日：2024-05-29

Applicant: Boehringer Ingelheim International GmbH ,  VANDERBILT UNIVERSITY

Inventor： Joachim BROEKER ,  Jason ABBOTT ,  Jianwen CUI ,  Stephen W. FESIK ,  Andreas GOLLNER ,  Lorenz HERDEIS ,  Tim HODGES ,  Andrew LITTLE ,  Andreas MANTOULIDIS ,  Juergen RAMHARTER ,  Dhruba SARKAR ,  Kevin SOKOL ,  Alex WATERSON ,  Tobias WUNBERG

IPC: C07D519/00 ,  A61K31/52 ,  A61K31/527 ,  A61K31/5386 ,  A61P35/00

Abstract: The present invention encompasses compounds of formula (I) wherein R1a, R1b, R2a, R2b, Z, R3 to R5, ring A, ring B, p, q, 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：US20240174690A1

公开(公告)日：2024-05-30

申请号：US18314445

申请日：2023-05-09

Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH ,  VANDERBILT UNIVERSITY

Inventor： 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: C07D498/10 ,  A61P1/00 ,  A61P1/18 ,  A61P11/00 ,  A61P17/00 ,  A61P35/00 ,  C07D519/00

CPC classification number: C07D498/10 ,  A61P1/00 ,  A61P1/18 ,  A61P11/00 ,  A61P17/00 ,  A61P35/00 ,  C07D519/00

Abstract: 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：US20230212164A1

公开(公告)日：2023-07-06

申请号：US18000442

申请日：2021-06-01

Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH ,  VANDERBILT UNIVERSITY

Inventor： Jason ABBOTT ,  Joachim BROEKER ,  Jianwen CUI ,  Stephen 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: C07D413/14 ,  C07D487/04 ,  C07D487/08 ,  C07D471/10 ,  C07D487/10 ,  C07D471/04

CPC classification number: C07D413/14 ,  C07D487/04 ,  C07D487/08 ,  C07D471/10 ,  C07D487/10 ,  C07D471/04

Abstract: The present invention encompasses compounds of formula (I), wherein R1a, R1b, R2a, R2b, Z, R3, R5, A, 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：US20250002504A1

公开(公告)日：2025-01-02

申请号：US18755002

申请日：2024-06-26

Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH ,  VANDERBILT UNIVERSITY

Inventor： 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: C07D498/10 ,  A61P1/00 ,  A61P1/18 ,  A61P11/00 ,  A61P17/00 ,  A61P35/00 ,  C07D519/00

Abstract: 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：US20230227470A1

公开(公告)日：2023-07-20

申请号：US18060053

申请日：2022-11-30

Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH ,  VANDERBILT UNIVERSITY

Inventor： 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: C07D498/10 ,  C07D519/00 ,  A61P35/00 ,  A61P11/00 ,  A61P1/18 ,  A61P1/00 ,  A61P17/00

CPC classification number: C07D498/10 ,  C07D519/00 ,  A61P35/00 ,  A61P11/00 ,  A61P1/18 ,  A61P1/00 ,  A61P17/00

Abstract: 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：US20210380574A1

公开(公告)日：2021-12-09

申请号：US17335620

申请日：2021-06-01

Applicant: Boehringer Ingelheim International GmbH ,  Vanderbilt University

Inventor： 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: C07D413/14 ,  A61K31/506 ,  C07D417/14 ,  C07D409/14 ,  A61P35/00

Abstract: 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.