Patent classifications
C07D515/14
Hybrid cyclic libraries and screens thereof
Provided are novel types of hybrid cyclic libraries that contain a known protein binding domain of a natural product. Also provided are synthetic methods to make such libraries and methods for the deconvolution of hits using partially split-pooled library compounds. Such methods are applicable for use with the entire human proteome to screen such libraries that bind and for the identification of hits.
NOVEL PYRIMIDINE DERIVATIVE COMPOUND, PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, PREPARATION PROCESS THEREOF, AND PHARMACEUTICAL COMPOSITION USING THE SAME
The present invention is related to a novel pyrimidine derivative compound or a pharmaceutically acceptable salt thereof, a process for preparing the same, and a pharmaceutical composition using the same.
NOVEL PYRIMIDINE DERIVATIVE COMPOUND, PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, PREPARATION PROCESS THEREOF, AND PHARMACEUTICAL COMPOSITION USING THE SAME
The present invention is related to a novel pyrimidine derivative compound or a pharmaceutically acceptable salt thereof, a process for preparing the same, and a pharmaceutical composition using the same.
MODULATORS OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR
- Jason McCartney ,
- Alexander Russell Abela ,
- Sunny Abraham ,
- Corey Don ANDERSON ,
- Vijayalaksmi Arumugam ,
- Jaclyn CHAU ,
- Jeremy CLEMENS ,
- Thomas Cleveland ,
- Timothy Richard Coon ,
- Andrew DINH ,
- Timothy A. DWIGHT ,
- Lev Tyler Dewey Fanning ,
- Bryan A. Frieman ,
- Peter Grootenhuis ,
- Sara Sabina Hadida Ruah ,
- Yoshihiro ISHIHARA ,
- Paul KRENITSKY ,
- Mark Thomas MILLER ,
- Fabrice Pierre ,
- Alina SILINA ,
- Joe A. TRAN ,
- Lino Valdez ,
- Jinglan Zhou
This disclosure provides modulators of Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) having core structure (I), pharmaceutical compositions containing at least one such modulator, methods of treatment of CFTR mediated diseases, including cystic fibrosis, using such modulators and pharmaceutical compositions, combination pharmaceutical compositions and combination therapies, and processes and intermediates for making such modulators.
##STR00001##
MODULATORS OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR
- Jason McCartney ,
- Alexander Russell Abela ,
- Sunny Abraham ,
- Corey Don ANDERSON ,
- Vijayalaksmi Arumugam ,
- Jaclyn CHAU ,
- Jeremy CLEMENS ,
- Thomas Cleveland ,
- Timothy Richard Coon ,
- Andrew DINH ,
- Timothy A. DWIGHT ,
- Lev Tyler Dewey Fanning ,
- Bryan A. Frieman ,
- Peter Grootenhuis ,
- Sara Sabina Hadida Ruah ,
- Yoshihiro ISHIHARA ,
- Paul KRENITSKY ,
- Mark Thomas MILLER ,
- Fabrice Pierre ,
- Alina SILINA ,
- Joe A. TRAN ,
- Lino Valdez ,
- Jinglan Zhou
This disclosure provides modulators of Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) having core structure (I), pharmaceutical compositions containing at least one such modulator, methods of treatment of CFTR mediated diseases, including cystic fibrosis, using such modulators and pharmaceutical compositions, combination pharmaceutical compositions and combination therapies, and processes and intermediates for making such modulators.
##STR00001##
INHIBITORS OF KEAP1-Nrf2 PROTEIN-PROTEIN INTERACTION
Sultam compounds, pharmaceutical compositions containing them, methods of making them, and methods of using them including methods for treating disease states, disorders, and conditions associated with the KEAP1-Nrf2 interaction, such as inflammatory bowel disease, including Crohn's disease and ulcerative colitis.
HYBRID CYCLIC LIBRARIES AND SCREENS THEREOF
Provided are novel types of hybrid cyclic libraries that contain a known protein binding domain of a natural product. Also provided are synthetic methods to make such libraries and methods for the deconvolution of hits using partially split-pooled library compounds. Such methods are applicable for use with the entire human proteome to screen such libraries that bind and for the identification of hits.
HYBRID CYCLIC LIBRARIES AND SCREENS THEREOF
Provided are novel types of hybrid cyclic libraries that contain a known protein binding domain of a natural product. Also provided are synthetic methods to make such libraries and methods for the deconvolution of hits using partially split-pooled library compounds. Such methods are applicable for use with the entire human proteome to screen such libraries that bind and for the identification of hits.
Tricyclic heteroaryl-substituted quinoline and azaquinoline compounds as PAR4 inhibitors
Disclosed are compounds of Formula (I) to (VIII): ##STR00001##
or a stereoisomer, tautomer, pharmaceutically acceptable salt, solvate or prodrug thereof, wherein R.sub.3 is a tricyclic heteroaryl group substituted with R.sub.3a and zero to 2 R.sub.3b; and R.sub.i, R.sub.2, R.sub.3a, R.sub.3b, R.sub.4, and n are defined herein. Also disclosed are methods of using such compounds as PAR4 inhibitors, and pharmaceutical compositions comprising such compounds. These compounds are useful in inhibiting or preventing platelet aggregation, and are useful for the treatment of a thromboembolic disorder or the primary prophylaxis of a thromboembolic disorder.
Tricyclic heteroaryl-substituted quinoline and azaquinoline compounds as PAR4 inhibitors
Disclosed are compounds of Formula (I) to (VIII): ##STR00001##
or a stereoisomer, tautomer, pharmaceutically acceptable salt, solvate or prodrug thereof, wherein R.sub.3 is a tricyclic heteroaryl group substituted with R.sub.3a and zero to 2 R.sub.3b; and R.sub.i, R.sub.2, R.sub.3a, R.sub.3b, R.sub.4, and n are defined herein. Also disclosed are methods of using such compounds as PAR4 inhibitors, and pharmaceutical compositions comprising such compounds. These compounds are useful in inhibiting or preventing platelet aggregation, and are useful for the treatment of a thromboembolic disorder or the primary prophylaxis of a thromboembolic disorder.