The invention relates to inhibitors of the NHR2 tetramerization and their use as tumor therapeutics (e.g. against acute myeloid leukemia (AML)), cytostatics, and diagnostic agents.

A series of novel amides showing broad pharmaceutical activity. Compounds described herein are effective as anticonvulsants, chemical countermeasures, and analgesics. Such compounds also show, neuroprotective/neuroreparative effects and activity against spinal muscular atrophy. Such pharmaceutically active compounds show utility in the treatment of central nervous system (CNS) diseases and disorders, such as anxiety, depression, insomnia, migraine headaches, schizophrenia, neurodegenerative diseases (e.g., Parkinson's disease, Alzheimer's, ALS, and Huntington's disease) spasticity, and bipolar disorder. Furthermore, such compounds may additionally find utility as analgesics (e.g., for the treatment of chronic or neuropathic pain) and as neuroprotective agents useful in the treatment of stroke(s), and/or traumatic brain and/or spinal cord injuries.

A series of novel amides showing broad pharmaceutical activity. Compounds described herein are effective as anticonvulsants, chemical countermeasures, and analgesics. Such compounds also show, neuroprotective/neuroreparative effects and activity against spinal muscular atrophy. Such pharmaceutically active compounds show utility in the treatment of central nervous system (CNS) diseases and disorders, such as anxiety, depression, insomnia, migraine headaches, schizophrenia, neurodegenerative diseases (e.g., Parkinson's disease, Alzheimer's, ALS, and Huntington's disease) spasticity, and bipolar disorder. Furthermore, such compounds may additionally find utility as analgesics (e.g., for the treatment of chronic or neuropathic pain) and as neuroprotective agents useful in the treatment of stroke(s), and/or traumatic brain and/or spinal cord injuries.

A chemoselective and reactive Mn(CF.sub.3-PDP) catalyst system that enables for the first time the strategic advantages of late-stage aliphatic CH hydroxylation to be leveraged in aromatic compounds. This discovery will benefit small molecule therapeutics by enabling the rapid diversification of aromatic drugs and natural products and identification of their metabolites.

A chemoselective and reactive Mn(CF.sub.3-PDP) catalyst system that enables for the first time the strategic advantages of late-stage aliphatic CH hydroxylation to be leveraged in aromatic compounds. This discovery will benefit small molecule therapeutics by enabling the rapid diversification of aromatic drugs and natural products and identification of their metabolites.

Provided herein are compounds that inhibit IDO1 and methods of use thereof. Also provided are pharmaceutical compositions and medicaments that include the compounds described herein as well as methods of treating sarcopenia or age-related muscle loss.

Provided herein are compounds that inhibit IDO1 and methods of use thereof. Also provided are pharmaceutical compositions and medicaments that include the compounds described herein as well as methods of treating sarcopenia or age-related muscle loss.

Disclosed is an application of substituted cinnamamide derivatives in the preparation of anti-anxiety medications, the substituted cinnammide derivatives are compounds having the structure of formula (I) or pharmaceutically acceptable salts thereof, wherein, R.sub.1 is H, OH, F, Cl, Br, I, OCH.sub.3, OCF.sub.3, OCHF.sub.2, OCH.sub.2F, CF.sub.3, CHF.sub.2, CH.sub.2F, CH.sub.3, CH.sub.3CH.sub.2, CF.sub.3CH.sub.2, CN, NO.sub.2, NH.sub.2 or COOR.sub.5; R.sub.2 is H, C.sub.1-C.sub.10 linear alkyl, C.sub.3-C.sub.10 branched alkyl, C.sub.3-C.sub.10 cyclic alkyl, C.sub.1-C.sub.10 hydroxyalkyl or a N-substituted piperazine-derived group; or R.sub.2 is a group forming with adjacent Y a tetrahydropyrrolyl group, a piperidyl group or a cyclohexanimido group. ##STR00001##

Disclosed is an application of substituted cinnamamide derivatives in the preparation of anti-anxiety medications, the substituted cinnammide derivatives are compounds having the structure of formula (I) or pharmaceutically acceptable salts thereof, wherein, R.sub.1 is H, OH, F, Cl, Br, I, OCH.sub.3, OCF.sub.3, OCHF.sub.2, OCH.sub.2F, CF.sub.3, CHF.sub.2, CH.sub.2F, CH.sub.3, CH.sub.3CH.sub.2, CF.sub.3CH.sub.2, CN, NO.sub.2, NH.sub.2 or COOR.sub.5; R.sub.2 is H, C.sub.1-C.sub.10 linear alkyl, C.sub.3-C.sub.10 branched alkyl, C.sub.3-C.sub.10 cyclic alkyl, C.sub.1-C.sub.10 hydroxyalkyl or a N-substituted piperazine-derived group; or R.sub.2 is a group forming with adjacent Y a tetrahydropyrrolyl group, a piperidyl group or a cyclohexanimido group. ##STR00001##

The present invention provides processes for the preparation of Tezacaftor, as well as intermediates useful in the preparation thereof. In particular, processes are provided for the preparation of a compound of Formula (3), and its conversion to Tezacaftor (1). ##STR00001##