The present invention is directed to inhibitors of tyrosinase, pharmaceutical compositions comprising such tyrosinase inhibitors, and methods of making and using the same. Specifically, included in the present invention are compositions of matter comprised of at least one 2,4-dihydroxybenzene analog, which inhibit the activity of tyrosinase and which inhibit the overproduction of melanin.

The present invention is directed to inhibitors of tyrosinase, pharmaceutical compositions comprising such tyrosinase inhibitors, and methods of making and using the same. Specifically, included in the present invention are compositions of matter comprised of at least one 2,4-dihydroxybenzene analog, which inhibit the activity of tyrosinase and which inhibit the overproduction of melanin.

It is related to compounds used as autophagy modulators and a method for preparing and using the same, specifically providing a compound of general formula (I), or pharmaceutically acceptable salts thereof, which is a type of autophagy modulators, particularly mammalian ATG8 homologues modulators. ##STR00001##

Disclosed herein is an efficient, environment friendly and commercially viable process for preparation of chloromethylated compound of formula I in substantially pure form and high yield, from the compound of formula II. The process includes contacting the compound of formula II with a chloromethylating agent generated in-situ by reaction of a formaldehyde precursor and hydrogen chloride, in a suitable solvent/contacting medium and in the presence of a catalytic amount of a short chain/low molecular weight carboxylic acid of formula III. I II III wherein, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are as defined in the description. ##STR00001##

Disclosed herein is an efficient, environment friendly and commercially viable process for preparation of chloromethylated compound of formula I in substantially pure form and high yield, from the compound of formula II. The process includes contacting the compound of formula II with a chloromethylating agent generated in-situ by reaction of a formaldehyde precursor and hydrogen chloride, in a suitable solvent/contacting medium and in the presence of a catalytic amount of a short chain/low molecular weight carboxylic acid of formula III. I II III wherein, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are as defined in the description. ##STR00001##

Provided are compounds that can find use as nitrosation reagents. Provided are nitrosation methods that include reacting a substrate with one of the provided nitrosation reagents and thereby generating a nitrosation product. Provided are kits including a nitrosation reagent. Provided are compositions wherein the nitrosation reagent is enriched in the .sup.15N isotope.

Provided are a 1,3-di-substituted ketene compound having a structure as represented by formula (I) and an application thereof. Such a type of compound primarily activates peroxisome proliferator-activated receptor (PPAR) α, and also activates PPPAδ and PPPAγ. The compound may be used to treat various diseases associated with PPAR regulation and control abnormality, such as non-alcoholic fatty liver disease, and especially in treating non-alcoholic hepatitis, and may potentially be used in the treatment of diseases comprising diabetes, obesity, fibrotic diseases, cardiovascular diseases (comprising heart failure, atherosclerosis, and so on), kidney diseases (comprising chronic kidney disease, renal failure, and so on), and brain degenerative diseases (comprising Alzheimer's disease and so on), having great application value. ##STR00001##

Provided are a 1,3-di-substituted ketene compound having a structure as represented by formula (I) and an application thereof. Such a type of compound primarily activates peroxisome proliferator-activated receptor (PPAR) α, and also activates PPPAδ and PPPAγ. The compound may be used to treat various diseases associated with PPAR regulation and control abnormality, such as non-alcoholic fatty liver disease, and especially in treating non-alcoholic hepatitis, and may potentially be used in the treatment of diseases comprising diabetes, obesity, fibrotic diseases, cardiovascular diseases (comprising heart failure, atherosclerosis, and so on), kidney diseases (comprising chronic kidney disease, renal failure, and so on), and brain degenerative diseases (comprising Alzheimer's disease and so on), having great application value. ##STR00001##

The invention provides glucocorticoid receptor antagonists for treatment of infection, neoplasia, and fatty liver disease.

The invention provides glucocorticoid receptor antagonists for treatment of infection, neoplasia, and fatty liver disease.