Disclosed herein are new compounds and compositions and their application as pharmaceuticals for the treatment of diseases. Methods of inhibition of KDMIA, methods of increasing gamma globin gene expression, and methods to induce differentiation of cancer cells in a human or animal subject are also provided for the treatment of diseases such as acute myelogenous leukemia.

There are disclosed compounds that modulate or inhibit the enzymatic activity of indoleamine 2,3-dioxygenase (IDO), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders, such as cancer, viral infections and/or inflammatory disorders utilizing the compounds of the disclosure.

Disclosed is a compound of Formula I, including N-oxides, and salts thereof, wherein R.sup.1, R.sup.2 and R.sup.3 are defined as set forth in the disclosure. Also disclosed is a process for preparing a compound of Formula I. A compound of Formula I can also be used as a synthetic intermediate to prepare pyridazinone-based herbicides.

##STR00001##

Disclosed is a compound of Formula I, including N-oxides, and salts thereof, wherein R.sup.1, R.sup.2 and R.sup.3 are defined as set forth in the disclosure. Also disclosed is a process for preparing a compound of Formula I. A compound of Formula I can also be used as a synthetic intermediate to prepare pyridazinone-based herbicides.

##STR00001##

Novel bromodomain and extraterminal domain (BET) inhibitors contanining substituted 2-pyridones and therapeutic methods of treating conditions and diseases using these novel BET inhibitors are provided.

Novel bromodomain and extraterminal domain (BET) inhibitors contanining substituted 2-pyridones and therapeutic methods of treating conditions and diseases using these novel BET inhibitors are provided.

Specifically, the present invention relates to the 6-oxo-1,6-dihydropyridazine prodrug derivative shown in general formula (I), a preparation method therefor, a pharmaceutical composition containing the derivative, a use thereof as a NaV inhibitor, and a use thereof in the preparation of a drug for the treatment and/or prevention of pain and pain-related diseases.

##STR00001##

Specifically, the present invention relates to the 6-oxo-1,6-dihydropyridazine prodrug derivative shown in general formula (I), a preparation method therefor, a pharmaceutical composition containing the derivative, a use thereof as a NaV inhibitor, and a use thereof in the preparation of a drug for the treatment and/or prevention of pain and pain-related diseases.

##STR00001##

Compounds provided herein function as thyromimetics and have utility for treating diseases such as neurodegenerative disorders and fibrotic diseases. Pharmaceutical compositions containing such compounds are also provided, as are methods of their preparation.

The present invention discloses a compound as a sodium channel regulator, and this type of compound can effectively inhibit and block the activity of Nav1.8 ion channel, a subtype of voltage-gated sodium channels, and can be used as a specific Nav1.8 inhibitor and to prepare drugs for the treatment of pain diseases mediated by Nav1.8 such as of intestinal pain, neuropathic pain, musculoskeletal pain, acute pain, inflammatory pain, cancer pain, primary pain, multiple sclerosis, Charcot-Marie-Tooth syndrome, incontinence, and cardiac arrhythmia, with broad application prospects.