C07D409/04

Fluorene Derivatives as Light Emitting Elements for Electroluminescent Devices

The present disclosure provides a composition comprising at least one compound selected from the group consisting of Compound 1, Compound 2, and combinations thereof, as shown below, and described herein: wherein, for Compound 1 and Compound 2, independently, R.sub.1 and R.sub.2 each independently is selected from the group consisting of hydrogen, a substituted alkyl, an unsubstituted alkyl, a substituted heteroalkyl, an unsubstituted heteroalkyl, a substituted aryl, an unsubstituted aryl, a substituted heteroaryl and an unsubstituted heteroaryl; wherein, for Compound 1 and Compound 2, independently, the Component A is selected from the group consisting of Group a) through Group h): wherein Group a) through Group h) are described herein.

TRICYCLIC SULFONES AS ROR GAMMA MODULATORS

There are described RORγ modulators of the formula (I),

##STR00001##

and formula (II)

##STR00002##

or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, wherein all substituents are defined herein. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for modulating RORγ activity in a cell and methods for treating a subject suffering from a disease or disorder in which the subject would therapeutically benefit from modulation of RORγ activity, for example, autoimmune and/or inflammatory disorders.

TRICYCLIC SULFONES AS ROR GAMMA MODULATORS

There are described RORγ modulators of the formula (I),

##STR00001##

and formula (II)

##STR00002##

or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, wherein all substituents are defined herein. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for modulating RORγ activity in a cell and methods for treating a subject suffering from a disease or disorder in which the subject would therapeutically benefit from modulation of RORγ activity, for example, autoimmune and/or inflammatory disorders.

TRICYCLIC SPIRO COMPOUND

A medicinal agent for the prevention and/or treatment of diseases caused by EP.sub.4 receptor activation. A compound having antagonistic activity against the EP.sub.4 receptor is contained as an active ingredient in the medicinal agent. The compound represented by the following general formula (I) as defined in the specification, a salt, an N-oxide, or a solvate thereof, or a prodrug of these is useful as a medicinal component having antagonistic activity against the EP.sub.4 receptor for the prevention and/or treatment of diseases caused by EP.sub.4 receptor activation.

##STR00001##

TRICYCLIC SPIRO COMPOUND

A medicinal agent for the prevention and/or treatment of diseases caused by EP.sub.4 receptor activation. A compound having antagonistic activity against the EP.sub.4 receptor is contained as an active ingredient in the medicinal agent. The compound represented by the following general formula (I) as defined in the specification, a salt, an N-oxide, or a solvate thereof, or a prodrug of these is useful as a medicinal component having antagonistic activity against the EP.sub.4 receptor for the prevention and/or treatment of diseases caused by EP.sub.4 receptor activation.

##STR00001##

COMPOUND FOR ORGANIC OPTOELECTRONIC DIODE, ORGANIC OPTOELECTRONIC DIODE COMPRISING SAME, AND DISPLAY DEVICE

The present invention relates to: a compound for an organic optoelectronic diode, represented by a combination of chemical formulas 1 and 2; an organic optoelectronic diode comprising the same; and a display device comprising the organic optoelectronic diode. The detailed contents of formulas 1 and 2 are the same as those defined in the specification.

METHOD FOR TREATING MACROPHAGE MIGRATION INHIBITORY FACTOR (MIF)-IMPLICATED DISEASES AND CONDITIONS WITH IODO PYRIMIDINE DERIVATIVES

Compounds useful for the inhibition of macrophage migration inhibitory factor (MIF) are provided herein, having the Formula I:

##STR00001##

wherein A is selected from the group consisting of aromatic or non-aromatic rings, bicyclic rings, polycyclic rings, alkenes or alkynes; B is H, OH, OR, SR, NH.sub.2, NHR, or alkyl; R is H or alkyl, and X and Y are independently N or CH, but one of X and Y must be N. Also provided are pharmaceutical compositions that contain a Formula I compound and methods for the treatment of MIF-implicated diseases or conditions that include administering a safe and effective amount of a Formula I compound.

METHOD FOR TREATING MACROPHAGE MIGRATION INHIBITORY FACTOR (MIF)-IMPLICATED DISEASES AND CONDITIONS WITH IODO PYRIMIDINE DERIVATIVES

Compounds useful for the inhibition of macrophage migration inhibitory factor (MIF) are provided herein, having the Formula I:

##STR00001##

wherein A is selected from the group consisting of aromatic or non-aromatic rings, bicyclic rings, polycyclic rings, alkenes or alkynes; B is H, OH, OR, SR, NH.sub.2, NHR, or alkyl; R is H or alkyl, and X and Y are independently N or CH, but one of X and Y must be N. Also provided are pharmaceutical compositions that contain a Formula I compound and methods for the treatment of MIF-implicated diseases or conditions that include administering a safe and effective amount of a Formula I compound.

Inhibitors of Beta-Hydroxylase for Treatment of Cancer
20180009798 · 2018-01-11 ·

The present invention relates to compounds which modulate (e.g., inhibit) the activity of beta-hydrolase (e.g., ASPH), including novel 2-aryl-5-amino-3(2H)-furanone and 2-heteroaryl-5-amino-3(2H)-furanone compounds, pharmaceutical compositions thereof, methods for their synthesis, and methods of using these compounds to modulate the activity of ASPH in an a cell-free sample, a cell-based assay, and in a subject. Other aspects of the invention relate to use of the compounds disclosed herein to ameliorate or treat cell proliferation disorders.

Inhibitors of Beta-Hydroxylase for Treatment of Cancer
20180009798 · 2018-01-11 ·

The present invention relates to compounds which modulate (e.g., inhibit) the activity of beta-hydrolase (e.g., ASPH), including novel 2-aryl-5-amino-3(2H)-furanone and 2-heteroaryl-5-amino-3(2H)-furanone compounds, pharmaceutical compositions thereof, methods for their synthesis, and methods of using these compounds to modulate the activity of ASPH in an a cell-free sample, a cell-based assay, and in a subject. Other aspects of the invention relate to use of the compounds disclosed herein to ameliorate or treat cell proliferation disorders.