Patent classifications
C07D267/20
Tricyclic Modulators of PP2A
Chemical modulators of PP2A, comprising tricyclic sulfonimidamides are disclosed. The compounds are useful in preventing or treating cancer, diabetes, autoimmune disease, solid organ transplant rejection, graft vs host disease, chronic obstructive pulmonary disease (COPD), non-alcoholic fatty liver disease, abdominal aortic aneurysm, chronic liver disease, heart failure, neurodegenerative disease and cardiac hypertrophy. The compounds are of formula (I)
##STR00001##
HEPATITIS B CORE PROTEIN MODULATORS
The present disclosure provides, in part, compounds having allosteric effector properties against Hepatitis B virus Cp. Also provided herein are methods of treating viral infections, such as hepatitis B, comprising administering to a patient in need thereof a disclosed compound.
HEPATITIS B CORE PROTEIN MODULATORS
The present disclosure provides, in part, compounds having allosteric effector properties against Hepatitis B virus Cp. Also provided herein are methods of treating viral infections, such as hepatitis B, comprising administering to a patient in need thereof a disclosed compound.
HECT E3 LIGASE INHIBITORS AND USES THEREOF
The present invention relates to tricyclic derivatives of formula (I), which are useful as inhibitors of HECT-domain-containing E3 ligases, in particular NEDD4. The present invention also refers to pharmaceutical compositions comprising compounds of formula (I), to their medical use and to their process of preparation.
##STR00001##
HECT E3 LIGASE INHIBITORS AND USES THEREOF
The present invention relates to tricyclic derivatives of formula (I), which are useful as inhibitors of HECT-domain-containing E3 ligases, in particular NEDD4. The present invention also refers to pharmaceutical compositions comprising compounds of formula (I), to their medical use and to their process of preparation.
##STR00001##
MCL-1 INHIBITORS
- Hang Chu ,
- Juan A. Guerrero ,
- Anna E. Hurtley ,
- Tae H. Hwang ,
- Lan Jiang ,
- Darryl Kato ,
- Tetsuya Kobayashi ,
- John E. Knox ,
- Scott E. Lazerwith ,
- Xiaofen LI ,
- David W. Lin ,
- Jonathan W. Medley ,
- Michael L. Mitchell ,
- Devan Naduthambi ,
- Zachary Newby ,
- Neil H. Squires ,
- Vickie H. Tsui ,
- Chandrasekar Venkataramani ,
- William J. Watkins ,
- Hong Yang
The present disclosure generally relates to compounds and pharmaceutical compositions that may be used in methods of treating cancer.
MCL-1 INHIBITORS
- Hang Chu ,
- Juan A. Guerrero ,
- Anna E. Hurtley ,
- Tae H. Hwang ,
- Lan Jiang ,
- Darryl Kato ,
- Tetsuya Kobayashi ,
- John E. Knox ,
- Scott E. Lazerwith ,
- Xiaofen LI ,
- David W. Lin ,
- Jonathan W. Medley ,
- Michael L. Mitchell ,
- Devan Naduthambi ,
- Zachary Newby ,
- Neil H. Squires ,
- Vickie H. Tsui ,
- Chandrasekar Venkataramani ,
- William J. Watkins ,
- Hong Yang
The present disclosure generally relates to compounds and pharmaceutical compositions that may be used in methods of treating cancer.
C-Abl tyrosine kinase inhibitory compound embodiments and methods of making and using the same
Disclosed herein are embodiments of a compound that inhibits c-Abl tyrosine kinase (also referred to herein as “c-Abl”). The compound embodiments described herein are novel c-Abl inhibitors that can bind to c-Abl at an allosteric site and inhibit its activity in various pathways. The compound embodiments also are capable of crossing the blood brain barrier and therefore are useful in inhibiting c-Abl activity as it affects pathways and/or proteins in the brain. The compound embodiments described herein are effective therapeutic agents for treating diseases involving c-Abl, such as cancers, motor neuron diseases, and neurodegenerative diseases. Also disclosed herein are embodiments of methods for making and using the c-Abl inhibitory compound embodiments.
C-Abl tyrosine kinase inhibitory compound embodiments and methods of making and using the same
Disclosed herein are embodiments of a compound that inhibits c-Abl tyrosine kinase (also referred to herein as “c-Abl”). The compound embodiments described herein are novel c-Abl inhibitors that can bind to c-Abl at an allosteric site and inhibit its activity in various pathways. The compound embodiments also are capable of crossing the blood brain barrier and therefore are useful in inhibiting c-Abl activity as it affects pathways and/or proteins in the brain. The compound embodiments described herein are effective therapeutic agents for treating diseases involving c-Abl, such as cancers, motor neuron diseases, and neurodegenerative diseases. Also disclosed herein are embodiments of methods for making and using the c-Abl inhibitory compound embodiments.
MCL-1 inhibitors
- Hang Chu ,
- Juan A. Guerrero ,
- Anna E. Hurtley ,
- Tae H. Hwang ,
- Lan Jiang ,
- Darryl Kato ,
- Tetsuya Kobayashi ,
- John E. Knox ,
- Scott E. Lazerwith ,
- Xiaofen LI ,
- David W. Lin ,
- Jonathan W. Medley ,
- Michael L. Mitchell ,
- Devan Naduthambi ,
- Zachary Newby ,
- Neil H. Squires ,
- Vickie H. Tsui ,
- Chandrasekar Venkataramani ,
- William J. Watkins ,
- Hong Yang
The present disclosure generally relates to compounds and pharmaceutical compositions that may be used in methods of treating cancer.