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：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.

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：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：US20200054617A1

公开(公告)日：2020-02-20

申请号：US16540091

申请日：2019-08-14

Applicant: Boehringer Ingelheim International GmbH

Inventor： Matthias ECKHARDT ,  Andreas GOLLNER ,  Elke LANGKOPF ,  Holger WAGNER ,  Dieter WIEDENMAYER

IPC: A61K31/4439 ,  C07D401/14 ,  C07D409/14 ,  C07D487/04 ,  A61K31/519 ,  A61K31/506 ,  C07D403/14 ,  C07D491/107 ,  C07D471/08 ,  C07D498/08 ,  C07D487/08 ,  A61K31/5386

Abstract: Heteroaromatic carboxamides of formula (I), wherein Y, R, and X are as defined herein, and pharmaceutically acceptable salts thereof. The compounds of formula (I) can be used in methods for the treatment of diseases which can be influenced by inhibition of plasma kallikrein.

公开(公告)号：US20210387963A1

公开(公告)日：2021-12-16

申请号：US17282789

申请日：2019-10-07

Applicant: Boehringer Ingelheim International GmbH

Inventor： Dieter WIEDENMAYER ,  Andreas GOLLNER ,  Iain LINGARD ,  Holger WAGNER

IPC: C07D401/14 ,  C07D487/04 ,  C07D491/107 ,  C07D498/08 ,  C07D487/08 ,  C07D471/08 ,  C07D491/048

Abstract: Disclosed are phenyltetrazole derivatives of formula (I), wherein A, R1, R2, X, R′, R″, and n are as defined herein, and pharmaceutically acceptable salts thereof. Also disclosed are methods of using the phenyltetrazole derivatives for the treatment of diseases which can be influenced by inhibition of plasma kallikrein.

公开(公告)号：US20170247394A1

公开(公告)日：2017-08-31

申请号：US15503754

申请日：2015-08-20

Applicant: Boehringer Ingelheim International GmbH

Inventor： Juergen RAMHARTER ,  Joachim BROEKER ,  Annika GILLE ,  Andreas GOLLNER ,  Manuel HENRY ,  Nina KERRES ,  Harald WEINSTABL

IPC: C07D498/20 ,  C07D471/22 ,  C07D487/10 ,  C07D498/22 ,  C08K3/18 ,  A61K31/553 ,  C07D487/20 ,  A61K45/06 ,  A61K31/438

CPC classification number: C07D498/20 ,  A61K31/438 ,  A61K31/5365 ,  A61K31/553 ,  A61K45/06 ,  C07D471/20 ,  C07D471/22 ,  C07D487/10 ,  C07D487/20 ,  C07D498/22 ,  C08K3/18

Abstract: The present invention encompasses compounds of formula (I) wherein the groups R1 to R7, A, V, W, X, Y, n, r and q are defined in claim 1, their use as inhibitors of MDM2-p53 interaction, pharmaceutical compositions which contain compounds of this kind, their use as medicaments, especially as agents for treatment and/or prevention of oncological diseases, and synthetic intermediates.