C07D335/02

Ketone ligands for modulating the expression of exogenous genes via an ecdysone receptor complex

This invention relates to a method to modulate exogenous gene expression in which an ecdysone receptor complex comprising: a DNA binding domain; a ligand binding domain; a transactivation domain; and a ligand is contacted with a DNA construct comprising: the exogenous gene and a response element; wherein the exogenous gene is under the control of the response element and binding of the DNA binding domain to the response element in the presence of the ligand results in activation or suppression of the gene. The ligands comprise a class of ketones.

SULFINYLAMINOBENZAMIDE AND SULFONYLAMINOBENZAMIDE DERIVATIVES

Provided is a compound of Formula (I):

##STR00001## wherein the variable groups are defined herein.

SULFINYLAMINOBENZAMIDE AND SULFONYLAMINOBENZAMIDE DERIVATIVES

Provided is a compound of Formula (I):

##STR00001## wherein the variable groups are defined herein.

STAT3 inhibitors and their anticancer use

In one aspect, the invention relates to substituted 6-amino-5,8-dioxo-5,8-dihydronaphthalene-1-sulfonamide analogs and derivatives thereof, substituted 4-amino-5H-naphtho[1,8-cd]isothiazol-5-one 1,1-dioxide analogs and derivatives thereof, and related compounds, which are useful as inhibitors of STAT protein activity; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating disorders of uncontrolled cellular proliferation associated with a STAT protein activity dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

Compounds and uses thereof for the modulation of hemoglobin
09776960 · 2017-10-03 · ·

Provide herein are compounds and pharmaceutical compositions suitable as modulators of hemoglobin, methods and intermediates for their preparation, and methods for their use in treating disorders mediated by hemoglobin and disorders that would benefit from tissue and/or cellular oxygenation.

Compounds and uses thereof for the modulation of hemoglobin
09776960 · 2017-10-03 · ·

Provide herein are compounds and pharmaceutical compositions suitable as modulators of hemoglobin, methods and intermediates for their preparation, and methods for their use in treating disorders mediated by hemoglobin and disorders that would benefit from tissue and/or cellular oxygenation.

Method for the synthesis of 4-(heterocycloalkyl)-benzene-1,3,-diol compounds
09745281 · 2017-08-29 · ·

A method is described for the synthesis of 4-(heterocycloalkyl)-benzene-1,3-diol compounds of general formulae (I) and (II): ##STR00001##
wherein X can be an oxygen atom or a sulphur atom. Also described, is a method for the synthesis of the reactive intermediates of general formula (7a) or (7b) ##STR00002##
Novel compounds as synthesis intermediates are also described.

Method for the synthesis of 4-(heterocycloalkyl)-benzene-1,3,-diol compounds
09745281 · 2017-08-29 · ·

A method is described for the synthesis of 4-(heterocycloalkyl)-benzene-1,3-diol compounds of general formulae (I) and (II): ##STR00001##
wherein X can be an oxygen atom or a sulphur atom. Also described, is a method for the synthesis of the reactive intermediates of general formula (7a) or (7b) ##STR00002##
Novel compounds as synthesis intermediates are also described.

IDO INHIBITORS

There are disclosed compounds that modulate or inhibit the enzymatic activity of indoleamine 2,3-dioxygenase (IDO), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders, such as cancer, viral infections and/or inflammatory disorders utilizing the compounds of the invention.

AGONISTS OF ROR GAMMAt

The present invention is directed to compounds of the formula (I) wherein all substituents are defined herein, as well as pharmaceutically acceptable compositions comprising compounds of the invention and methods of using said compositions in the treatment of various disorders.

##STR00001##