Patent classifications
C07D515/14
BCL-2 INHIBITORS
The disclosure includes compounds of Formula (A), (A) wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8, R.sub.9, R.sub.10, and R.sub.11, h, j m, n, k, v, s, g, V, W, L, Z.sub.1, Q.sub.1, Q.sub.2, Q.sub.3, Q.sub.4, Q.sub.5, Q.sub.6 and Q.sub.7, are defined herein. Also disclosed is a method for treating a neoplastic disease, an autoimmune disease, or a nerodegenerative disease with these compounds.
##STR00001##
BCL-2 INHIBITORS
The disclosure includes compounds of Formula (A), (A) wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8, R.sub.9, R.sub.10, and R.sub.11, h, j m, n, k, v, s, g, V, W, L, Z.sub.1, Q.sub.1, Q.sub.2, Q.sub.3, Q.sub.4, Q.sub.5, Q.sub.6 and Q.sub.7, are defined herein. Also disclosed is a method for treating a neoplastic disease, an autoimmune disease, or a nerodegenerative disease with these compounds.
##STR00001##
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.
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.
BIARYL PYRAZOLES AS NRF2 REGULATORS
The present invention relates to biaryl pyrazole compounds of Formula (I)
##STR00001##
methods of making them, pharmaceutical compositions containing them and their use as NRF2 regulators.
BIARYL PYRAZOLES AS NRF2 REGULATORS
The present invention relates to biaryl pyrazole compounds of Formula (I)
##STR00001##
methods of making them, pharmaceutical compositions containing them and their use as NRF2 regulators.
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.1, 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.1, 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.