The present invention provides compounds for inhibiting matriptase 2, or a mutant thereof, and compositions and methods of use thereof.

The present invention provides compounds for inhibiting matriptase 2, or a mutant thereof, and compositions and methods of use thereof.

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.

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.

The present invention provides compositions and formulations of compounds having formula (I) and pharmaceutically acceptable derivatives thereof, wherein p, R.sup.1, R.sup.2 and B are as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of any of a number of injuries, conditions or diseases in which HGF/SF or the activities thereof, or agonists or antagonists thereof have a therapeutically useful role. In addition, methods are provided for treating such diseases or diseases starting at a time after the onset of the injury, condition or disease.

##STR00001##

The present invention provides compositions and formulations of compounds having formula (I) and pharmaceutically acceptable derivatives thereof, wherein p, R.sup.1, R.sup.2 and B are as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of any of a number of injuries, conditions or diseases in which HGF/SF or the activities thereof, or agonists or antagonists thereof have a therapeutically useful role. In addition, methods are provided for treating such diseases or diseases starting at a time after the onset of the injury, condition or disease.

##STR00001##

Embodiments of bridged tetrahydroisoquinolines and methods for their use in selectively inhibiting nicotinamide adenine dinucleotide phosphate (NADPH) oxidase 2 are disclosed. The disclosed compounds have a structure according to general formula I or a pharmaceutically acceptable salt thereof:

##STR00001##

wherein “” represents a single or double bond, R.sup.1 is hydrogen, halogen, lower aliphatic, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; R.sup.a is hydrogen, —CH.sub.2R.sup.2, R.sup.3, or —SO.sub.2R.sup.4; R.sup.2 is lower aliphatic, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; R.sup.3 is substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; R.sup.4 is lower aliphatic, or substituted or unsubstituted aryl; and R.sup.5 is hydrogen, halogen, or lower aliphatic.

Embodiments of bridged tetrahydroisoquinolines and methods for their use in selectively inhibiting nicotinamide adenine dinucleotide phosphate (NADPH) oxidase 2 are disclosed. The disclosed compounds have a structure according to general formula I or a pharmaceutically acceptable salt thereof:

##STR00001##

wherein “” represents a single or double bond, R.sup.1 is hydrogen, halogen, lower aliphatic, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; R.sup.a is hydrogen, —CH.sub.2R.sup.2, R.sup.3, or —SO.sub.2R.sup.4; R.sup.2 is lower aliphatic, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; R.sup.3 is substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; R.sup.4 is lower aliphatic, or substituted or unsubstituted aryl; and R.sup.5 is hydrogen, halogen, or lower aliphatic.

An object of the present invention is to provide a novel compound useful for manufacturing salacinol, a method for manufacturing the compound, a method for manufacturing salacinol, methods for protecting and deprotecting a diol group, and a protective agent for a diol group. A compound represented by Formula (1) is a compound useful for manufacturing salacinol.

##STR00001##

(In the formula, each of R.sup.1a and R.sup.1b is a hydrogen atom or a hydroxy protective group; R.sup.2 is a hydroxy group or the like; and R.sup.3 is a hydroxy group or the like.)

An object of the present invention is to provide a novel compound useful for manufacturing salacinol, a method for manufacturing the compound, a method for manufacturing salacinol, methods for protecting and deprotecting a diol group, and a protective agent for a diol group. A compound represented by Formula (1) is a compound useful for manufacturing salacinol.

##STR00001##

(In the formula, each of R.sup.1a and R.sup.1b is a hydrogen atom or a hydroxy protective group; R.sup.2 is a hydroxy group or the like; and R.sup.3 is a hydroxy group or the like.)