The present invention is directed to novel compounds of Formula (I), pharmaceutically acceptable salts or solvates thereof, and their use.

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Disclosed herein are structures, compositions and syntheses of pharmaceutically relevant compounds inspired by thiostrepton, as well as methods of treating cancer with such compounds.

Disclosed herein are structures, compositions and syntheses of pharmaceutically relevant compounds inspired by thiostrepton, as well as methods of treating cancer with such compounds.

A compound of formula (I)

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or a pharmaceutically acceptable salt or solvate thereof, and a pharmaceutical composition comprising the compound. The compound is useful for the treatment a disease resulting from pathologic inflammation, such as inflammatory bowel disease, psoriasis or rheumatoid arthritis.

The identification of a direct kinase of eukaryotic initiation factor 2 alpha (eIF2), microtubule affinity-regulating kinase 2 (MARK2), which phosphorylates eIF2 in response to proteotoxic stress, is provided. Inhibitors of MARK2 and their use in treating neurodegenerative disease, including Alzheimer's disease, Parkinson disease, Creutzfeldt-Jakob disease, Huntington's disease, frontotemporal dementia (FTD), and amyotrophic lateral sclerosis (ALS), also are disclosed.

The identification of a direct kinase of eukaryotic initiation factor 2 alpha (eIF2), microtubule affinity-regulating kinase 2 (MARK2), which phosphorylates eIF2 in response to proteotoxic stress, is provided. Inhibitors of MARK2 and their use in treating neurodegenerative disease, including Alzheimer's disease, Parkinson disease, Creutzfeldt-Jakob disease, Huntington's disease, frontotemporal dementia (FTD), and amyotrophic lateral sclerosis (ALS), also are disclosed.

Disclosed are a dual modulator of mGluR5 and 5-HT2AR (5-HT2A receptor), and use thereof. More specifically, disclosed are a compound which acts as modulator of mGluR5 and an antagonist of 5-HT2AR at the same time, and use thereof as therapeutic agent for pain.

Disclosed are a dual modulator of mGluR5 and 5-HT2AR (5-HT2A receptor), and use thereof. More specifically, disclosed are a compound which acts as modulator of mGluR5 and an antagonist of 5-HT2AR at the same time, and use thereof as therapeutic agent for pain.

The disclosure relates to compounds that act as irreversible inactivators that target ARAF/MEK complexes; pharmaceutical compositions comprising the compounds; and methods of treating or preventing kinase-mediated disorders, including cancer and other proliferation diseases.

The disclosure relates to compounds that act as irreversible inactivators that target ARAF/MEK complexes; pharmaceutical compositions comprising the compounds; and methods of treating or preventing kinase-mediated disorders, including cancer and other proliferation diseases.