C07D221/10

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.

Substituted 2-pyridone tricyclic compounds, analogues thereof, and methods using same

The present invention includes in one aspect substituted 2-oxo-1,2,5,6-tetrahydrobenzo[h]quinoline-3-carboxylic acids, analogues thereof, and compositions comprising the same, which can be used to treat and/or prevent hepatitis B virus (HBV) infection and/or hepatitis D virus (HDV) in a patient. In certain embodiments, the invention provides a compound of formula (I), or a salt, solvate, geometric isomer, stereoisomer, tautomer, and any mixtures thereof: ##STR00001##

COMPOUND OR SALT THEREOF

The present invention relates to a compound represented by the following General Formula (1) or a salt thereof.

##STR00001##

In General Formula (1), R.sup.1, R.sup.2, R.sup.3 and R.sup.4 each independently represent a hydrogen atom, a linear or branched alkyl group which may have a substituent or the like. R.sup.1 and R.sup.2 may be bonded to each other to form a ring. R.sup.3 and R.sup.4 may be bonded to each other to form a ring. R.sup.1 and/or R.sup.2 may be bonded to a 6-membered ring to which —NR.sup.1R.sup.2 is bonded to form a ring. R.sup.3 and/or R.sup.4 may be bonded to a 6-membered ring to which —NR.sup.3R.sup.4 is bonded to form a ring. R.sup.5 represents —.sup.11CH.sub.3, a linear or branched alkyl group which may have a substituent or the like. R.sup.6 represents —F, —.sup.18F or the like. X, Y and Z each independently represent a carbon atom, an oxygen atom or the like. n is 0 or 1.

CHELATION DIRECTED C-H ACTIVATION REACTIONS CATALYZED BY SOLID-SUPPORTED PALLADIUM(II) CATALYSTS
20170362181 · 2017-12-21 ·

Chelation directed C—H activation reactions that are catalyzed by Pd(11) on Multi-Walled Carbon Nanotubes (MWCNT), Single-Walled Carbon Nanotubes (SWCNT), or graphene are provided. The reactions are used to directly and regioselectively or regiospecifically functionalize specific C—H bonds, e.g. to build complexity into small molecules. Features and advantages of the present invention will be set forth in the description of invention that follows, and in part will be apparent from the description or may be learned by practice of the invention. The invention will be realized and attained by the compositions and methods particularly pointed out in the written description and claims hereof.

CHELATION DIRECTED C-H ACTIVATION REACTIONS CATALYZED BY SOLID-SUPPORTED PALLADIUM(II) CATALYSTS
20170362181 · 2017-12-21 ·

Chelation directed C—H activation reactions that are catalyzed by Pd(11) on Multi-Walled Carbon Nanotubes (MWCNT), Single-Walled Carbon Nanotubes (SWCNT), or graphene are provided. The reactions are used to directly and regioselectively or regiospecifically functionalize specific C—H bonds, e.g. to build complexity into small molecules. Features and advantages of the present invention will be set forth in the description of invention that follows, and in part will be apparent from the description or may be learned by practice of the invention. The invention will be realized and attained by the compositions and methods particularly pointed out in the written description and claims hereof.

Anti-Cancer/Anti-Fibrosis Compounds

This invention provides, among other things, compounds useful for treating diseases such as fibrosis and/or cancer, pharmaceutical formulations containing such compounds, as well as combinations of these compounds with at least one additional therapeutic agent.

Anti-Cancer/Anti-Fibrosis Compounds

This invention provides, among other things, compounds useful for treating diseases such as fibrosis and/or cancer, pharmaceutical formulations containing such compounds, as well as combinations of these compounds with at least one additional therapeutic agent.

Inhibitors of paxillin function and related compositions and methods

This disclosure relates to small molecule inhibitors of paxillin and paxillin binding, and related compositions and methods of treatment.

Inhibitors of paxillin function and related compositions and methods

This disclosure relates to small molecule inhibitors of paxillin and paxillin binding, and related compositions and methods of treatment.