The present application relates to a benzidine compound and an application thereof, the benzidine compound having the structure as shown in formula I below. Further provided in the present application are a pharmaceutically acceptable salt, isomer, racemate, prodrug co-crystal complex, hydrate, and solvate of the compound, as well as an application thereof in the preparation of a drug for the treatment or prevention of RORγ-regulated diseases; more importantly, such a compound can also be used in the preparation of a drug for the treatment of inflammation, immune diseases, cancer and neurological diseases.

The present application relates to a benzidine compound and an application thereof, the benzidine compound having the structure as shown in formula I below. Further provided in the present application are a pharmaceutically acceptable salt, isomer, racemate, prodrug co-crystal complex, hydrate, and solvate of the compound, as well as an application thereof in the preparation of a drug for the treatment or prevention of RORγ-regulated diseases; more importantly, such a compound can also be used in the preparation of a drug for the treatment of inflammation, immune diseases, cancer and neurological diseases.

Disclosed herein are dihydroceramide desaturase 1 (Des1) inhibitor compounds and compositions, which are useful in the treatment of diseases, such as metabolic, cardiovascular, fibrotic, autoimmune/chronic inflammatory diseases, cystic fibrosis, various cancers, neurodegenerative diseases, lipid storage disorders, and ischemia/reperfusion injury, where inhibition of Des1 is expected to be therapeutic to a patient. Methods of inhibition of Des1 activity in a human or animal subject are also provided.

The present disclosure relates to a novel anticancer pharmaceutical composition. The present disclosure achieves an anticancer effect using a compound effective in inhibiting the expression of ANO1 (TMEM16A). In addition, the present disclosure provides an ANO1 (TMEM16A) antagonist using the compound inhibiting the expression of ANO1 (TMEM16A).

The present disclosure relates to a novel anticancer pharmaceutical composition. The present disclosure achieves an anticancer effect using a compound effective in inhibiting the expression of ANO1 (TMEM16A). In addition, the present disclosure provides an ANO1 (TMEM16A) antagonist using the compound inhibiting the expression of ANO1 (TMEM16A).

The present invention relates to a compound of formula I, or an isotopic form, stereoisomer, a tautomer, a pharmaceutically acceptable salt, a solvate, a polymorph, a prodrug, N-oxide or S-oxide thereof; and processes for their preparation. The invention further relates to pharmaceutical compositions containing the compounds and their use in the treatment of diseases or disorders mediated by RORγ.

The present invention relates to a compound of formula I, or an isotopic form, stereoisomer, a tautomer, a pharmaceutically acceptable salt, a solvate, a polymorph, a prodrug, N-oxide or S-oxide thereof; and processes for their preparation. The invention further relates to pharmaceutical compositions containing the compounds and their use in the treatment of diseases or disorders mediated by RORγ.

The present disclosure provides compounds useful as anesthetics, such as topical anesthetics, of general formula (VIIIk):

##STR00001##

wherein: R.sub.2═H or Me; R.sub.3═H or Me; R.sub.4=Alkyl; R.sub.5═O-Alkyl; and Alkyl=aliphatic C.sub.1-C.sub.4 alkyl.

The present disclosure further provides methods of making compounds of general formula (VIIIk), compositions comprising a therapeutically effective amount of a compound of general formula (VIIIk), and methods of treating or preventing pain in a subject by administering (e.g., topically applying) compositions comprising an effective amount of a compound of general formula (VIIIk) to the subject.

The present disclosure provides compounds useful as anesthetics, such as topical anesthetics, of general formula (VIIIk):

##STR00001##

wherein: R.sub.2═H or Me; R.sub.3═H or Me; R.sub.4=Alkyl; R.sub.5═O-Alkyl; and Alkyl=aliphatic C.sub.1-C.sub.4 alkyl.

The present disclosure further provides methods of making compounds of general formula (VIIIk), compositions comprising a therapeutically effective amount of a compound of general formula (VIIIk), and methods of treating or preventing pain in a subject by administering (e.g., topically applying) compositions comprising an effective amount of a compound of general formula (VIIIk) to the subject.

The present disclosure provides compositions comprising one or more compounds of general formula (I):

##STR00001##

wherein: R.sub.1 is H, —OMe, Me, or one or more electron withdrawing groups; R.sub.2 and R.sub.3 are each independently H or alkyl or, taken together, form a 4- to 8-membered heterocyclic ring with the adjacent nitrogen atom; R.sub.4 is H or alkyl; R.sub.5 is H or one or more electron donating groups; and n is 1 to 4.