Patent classifications
C07D498/10
BIFUNCTIONAL COMPOUNDS FOR THE TREATMENT OF CANCER
The invention provides bifunctional compounds of formula (I) or a pharmaceutically acceptable salt thereof. Formula (I). The compounds cause the degradation of SMARCA2 via the targeted ubiquination of SMARCA2 protein and subsequent proteasomal degradation and are thus useful for the treatment of cancer. The targeting ligand is of formula (TL).
##STR00001##
BIFUNCTIONAL COMPOUNDS FOR DEGRADING BTK VIA UBIQUITIN PROTEOSOME PATHWAY
The present invention relates to compounds useful for degrading BTK via a ubiquitin proteolytic pathway. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
BIFUNCTIONAL COMPOUNDS FOR DEGRADING BTK VIA UBIQUITIN PROTEOSOME PATHWAY
The present invention relates to compounds useful for degrading BTK via a ubiquitin proteolytic pathway. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
BIFUNCTIONAL COMPOUNDS FOR DEGRADING BTK VIA UBIQUITIN PROTEOSOME PATHWAY
This disclosure relates to compounds useful for degrading BTK via a ubiquitin proteolytic pathway. The description also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
BIFUNCTIONAL COMPOUNDS FOR DEGRADING BTK VIA UBIQUITIN PROTEOSOME PATHWAY
This disclosure relates to compounds useful for degrading BTK via a ubiquitin proteolytic pathway. The description also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
Compounds and compositions for the treatment of cancer
The present disclosure provides compounds, pharmaceutical compositions, and methods for the treatment of cancer and fibrosis. The disclosed pharmaceutical compositions may include one or more pyrazolyl-containing compounds, or a derivative thereof.
ANNULATED 2-AMINO-3-CYANO THIOPHENES AND DERIVATIVES FOR THE TREATMENT OF CANCER
- 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
The present invention encompasses compounds of formula (I)
##STR00001##
wherein R.sup.1a, R.sup.1b, R.sup.2a, R.sup.2b, Z, R.sup.3 to R.sup.5, 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.
ANNULATED 2-AMINO-3-CYANO THIOPHENES AND DERIVATIVES FOR THE TREATMENT OF CANCER
- 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
The present invention encompasses compounds of formula (I)
##STR00001##
wherein R.sup.1a, R.sup.1b, R.sup.2a, R.sup.2b, Z, R.sup.3 to R.sup.5, 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.
RIP1K INHIBITORS
Disclosed herein are kinase inhibitory compounds, such as a receptor-interacting protein-1 (RIP1) kinase inhibitor compounds, as well as pharmaceutical compositions and combinations comprising such inhibitory compounds. The disclosed compounds, pharmaceutical compositions, and/or combinations may be used to treat or prevent a kinase-associated disease or condition, particularly a RIP1-associated disease or condition.
SOS1 inhibitors
The present invention relates to compounds that inhibit Son of sevenless homolog 1 (SOS1) activity. In particular, the present invention relates to compounds, pharmaceutical compositions and methods of use, such as methods of treating cancer using the compounds and pharmaceutical compositions of the present invention.