A one-pot process for the manufacture of 5-chloro-7-methylindoline-2,3-dione starting from 2-hydroxyimino-N-(2-methylphenyl)acetamide via tandem cyclization in sulfuric acid and acetic acid, followed by in-situ chlorination with sulfur dioxide and chlorine gas in high regioselectivity and yield.

The present invention provides e.g. N-{[2-(piperidin-1-yl)phenyl](phenyl)methyl}-2-(3-oxo-3,4-dihydro-2H-1,4-benzoxazin-7-yl)acetamide derivatives and related compounds as ROR-gamma modulators for treating e.g. autoimmune diseases, autoimmune-related diseases, inflammatory diseases, metabolic diseases, fibrotic diseases or cholestatic diseases, such as e.g. arthitis and asthma.

Indoline derivative compounds that act as EWS-FLI1 transcription factor inhibitors are provided. Also provided are pharmaceutical compositions of the indoline derivatives, methods of synthesizing the same, methods of treating using same, and assays for identifying the inhibitors of EWS-FLI1 oncoprotein.

Indoline derivative compounds that act as EWS-FLI1 transcription factor inhibitors are provided. Also provided are pharmaceutical compositions of the indoline derivatives, methods of synthesizing the same, methods of treating using same, and assays for identifying the inhibitors of EWS-FLI1 oncoprotein.

A novel type of water-soluble isatin derivatives, and manufacturing method and application thereof. An isatin derivative comprising a phenolic hydroxy group is used as the substrates. A dimethylaminomethylene group is introduced to an ortho position of the phenolic hydroxy group to significantly improve the water solubility of a class of compounds provided by the invention. An antitumor activity study showed that the activity of the class of compounds was not reduced, and even improved. The class of compounds has great prospects for applications in developing an antitumor pharmaceutical product.

A novel type of water-soluble isatin derivatives, and manufacturing method and application thereof. An isatin derivative comprising a phenolic hydroxy group is used as the substrates. A dimethylaminomethylene group is introduced to an ortho position of the phenolic hydroxy group to significantly improve the water solubility of a class of compounds provided by the invention. An antitumor activity study showed that the activity of the class of compounds was not reduced, and even improved. The class of compounds has great prospects for applications in developing an antitumor pharmaceutical product.

The present invention relates to compounds of formula (I). The compounds may be used to modulate the Stimulator of Interferon Genes (STING) protein and thereby treat diseases such as cancer and microbial infections. (I)

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The present invention relates to 3-hydroxyoxindole derivatives which have antagonistic activities against CRHR2, and which are useful in the treatment or prevention of disorders and diseases in which CRHR2 is involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CRHR2 is involved.

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The present invention relates to 3-hydroxyoxindole derivatives which have antagonistic activities against CRHR2, and which are useful in the treatment or prevention of disorders and diseases in which CRHR2 is involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CRHR2 is involved.

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The present invention provides an SSAO inhibitor and an application thereof in preparing a drug for treating a disease related to SSAO. In particular, the present invention provides a compound shown in formula (IV) and a pharmaceutically acceptable salt thereof.

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