C07D515/14

BCL-2 INHIBITORS
20210332065 · 2021-10-28 ·

The disclosure includes compounds of Formula (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 neorodegenerative disease with these compounds.

##STR00001##

BCL-2 INHIBITORS
20210315904 · 2021-10-14 ·

The disclosure includes compounds of Formula (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 neorodegenerative disease with these compounds.

##STR00001##

CHROMENOPYRIDINE DERIVATIVES AS PHOSPHATIDYLINOSITOL PHOSPHATE KINASE INHIBITORS

The invention relates to inhibitors of PI5P4K inhibitors useful in the treatment of cancers, neurodegenerative diseases, inflammatory disorders, and metabolic diseases, having the Formula:

##STR00001##

where A1, A2, G, R1, R2, R3, R4, and W are described herein.

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.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.

RECEPTORS AND SPACERS FOR A FLUORESCENCE-BASED LEAD ION CHEMOSENSOR
20210190695 · 2021-06-24 ·

Provided are chemosensor compounds of formula (I) useful for detecting an ion, such as Pb.sup.2+ in an aqueous sample. Also provided are chemosensor device including such compounds, and methods of use thereof.

RECEPTORS AND SPACERS FOR A FLUORESCENCE-BASED LEAD ION CHEMOSENSOR
20210190695 · 2021-06-24 ·

Provided are chemosensor compounds of formula (I) useful for detecting an ion, such as Pb.sup.2+ in an aqueous sample. Also provided are chemosensor device including such compounds, and methods of use thereof.

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.