This disclosure features chemical entities (e.g., a compound or a pharmaceutically acceptable salt, and/or hydrate, and/or cocrystal, and/or drug combination of the compound) that inhibit (e.g., antagonize) Stimulator of Interferon Genes (STING). Said chemical entities are useful, e.g., for treating a condition, disease or disorder in which increased (e.g., excessive) STING activation (e.g., STING signaling) contributes to the pathology and/or symptoms and/or progression of the condition, disease or disorder (e.g., cancer) in a subject (e.g., a human). This disclosure also features compositions containing the same as well as methods of using and making the same.

The present application relates to a nitrogen-containing compound. The structural formula of the nitrogen-containing compound is as shown in a Formula 1, in which a ring A and a ring B are each independently selected from a benzene ring or a fused aromatic ring with 10 to 14 ring-forming carbon atoms, and at least one of the ring A and the ring B is selected from the fused aromatic ring with 10 to 14 ring-forming carbon atoms; L is selected from a single bond, a substituted or unsubstituted arylene group with 6 to 30 carbon atoms, and a substituted or unsubstituted heteroarylene group with 3 to 30 carbon atoms; and Het is a substituted or unsubstituted nitrogen-containing heteroaryl group with 3 to 30 carbon atoms. The nitrogen-containing compound of the present application can improve the luminous efficiency of an organic electroluminescent device and the conversion efficiency of a photoelectric conversion device using the nitrogen-containing compound.

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The present application relates to a nitrogen-containing compound. The structural formula of the nitrogen-containing compound is as shown in a Formula 1, in which a ring A and a ring B are each independently selected from a benzene ring or a fused aromatic ring with 10 to 14 ring-forming carbon atoms, and at least one of the ring A and the ring B is selected from the fused aromatic ring with 10 to 14 ring-forming carbon atoms; L is selected from a single bond, a substituted or unsubstituted arylene group with 6 to 30 carbon atoms, and a substituted or unsubstituted heteroarylene group with 3 to 30 carbon atoms; and Het is a substituted or unsubstituted nitrogen-containing heteroaryl group with 3 to 30 carbon atoms. The nitrogen-containing compound of the present application can improve the luminous efficiency of an organic electroluminescent device and the conversion efficiency of a photoelectric conversion device using the nitrogen-containing compound.

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The present invention relates to the field of medicine. More specifically, the present invention relates to compounds that are sigma-1 receptor agonists and their use for the treatment of central nervous system disorders, including cognitive or neurodegenerative disorders, such as Alzheimer's disease, Parkinson's disease, Huntington's disease, Amyotrophic lateral sclerosis, and multiple sclerosis.

The present invention relates to the field of medicine. More specifically, the present invention relates to compounds that are sigma-1 receptor agonists and their use for the treatment of central nervous system disorders, including cognitive or neurodegenerative disorders, such as Alzheimer's disease, Parkinson's disease, Huntington's disease, Amyotrophic lateral sclerosis, and multiple sclerosis.

This disclosure relates to new phthalimide and isoindolinone derivatives and other PFKFB3 inhibitors for use in the treatment of diseases. The invention further relates to pharmaceutical compositions containing such PFKFB3 inhibitors, methods of preparation thereof, methods for their use as therapeutic agents, and methods of preparation of a medicament for use in therapy, as well as kits and other inventions comprising such PFKFB3 inhibitors. These PFKFB3 inhibitors are useful for the treatment and prophylaxis of cancer, neurodegenerative diseases, autoimmune diseases, inflammatory disorders, multiple sclerosis, metabolic diseases, inhibition of angiogenesis and other diseases and conditions, where the modulation of PFKFB3 and/or PFKFB4 has beneficial effect as well as neuroprotection.

This disclosure relates to new phthalimide and isoindolinone derivatives and other PFKFB3 inhibitors for use in the treatment of diseases. The invention further relates to pharmaceutical compositions containing such PFKFB3 inhibitors, methods of preparation thereof, methods for their use as therapeutic agents, and methods of preparation of a medicament for use in therapy, as well as kits and other inventions comprising such PFKFB3 inhibitors. These PFKFB3 inhibitors are useful for the treatment and prophylaxis of cancer, neurodegenerative diseases, autoimmune diseases, inflammatory disorders, multiple sclerosis, metabolic diseases, inhibition of angiogenesis and other diseases and conditions, where the modulation of PFKFB3 and/or PFKFB4 has beneficial effect as well as neuroprotection.

A process and intermediates for making the compound of Formula (I).

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A process and intermediates for making the compound of Formula (I).

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The compound represented by formula (I), and racemates, stereoisomers, tautomers, isotopic markers, nitrogen oxides, solvates, polymorphs, metabolites, esters, pharmaceutically acceptable salts, or prodrugs thereof have ROCK inhibitory activity. The compound represented by formula (1) has good safety, good metabolic stability, and a low risk of potential hepatotoxicity. Further, the compound represented by formula (I) has a simple preparation method and is easy to purify, and therefore has good application prospects.

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