Disclosed are immune cell-selective small molecule IMPDH inhibitor compounds and methods of their synthesis and use to treat proliferative disorders.

The present invention provides a method of industrially and safely producing lacosamide high in diastereomeric excess at a high yield and a low cost. Adopting a particular isomerization-crystallization condition makes it possible to a method of industrially and safely producing lacosamide high in diastereomeric excess at a high yield and a low cost. Additionally, an intermediate efficacious for producing lacosamide is provided.

The present invention regards specific IBAT inhibitors useful in the prophylaxis and/or treatment of a liver disease. It also relates to compositions comprising these IBAT inhibitors, a method for treatment of the disorders and a kit comprising the substances or the compositions.

The present application is directed to cargo delivery complexes for intracellular delivery of a cargo molecule comprising: a first peptide comprising a cell-penetrating peptide (CPP), a second peptide comprising a cell-penetrating peptide, and a cargo molecule. The second peptide comprises a polyethylene glycol (PEG) moiety linked to the second CPP, and the first peptide does not have a PEG moiety. The present application is also directed to a cargo delivery complex comprising a CPP and a cargo molecule wherein the CPP is a retro-inverso peptide. The present application is also directed to a cargo delivery complex comprising a CPP and a cargo molecule wherein the peptide further comprises a targeting sequence selected from the group consisting of GYVSK, GYVS, YIGS and YIGSR. Methods of making and using the cargo delivery complexes are also disclosed.

This invention is in the field of medicinal pharmacology. In particular, the present invention relates to pharmaceutical agents which function as inhibitors of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) viral replication and/or SARS-CoV-2 related viral 3CL protease (M.sup.pro) activity. The invention further relates to methods of treating and/or ameliorating symptoms related to conditions caused by the SARS-CoV-2 virus (e.g., COVID-19), comprising administering to a subject (e.g., a human patient) a composition comprising one or more pharmaceutical agents which function as inhibitors of SARS-CoV-2 viral replication and/or inhibitors of SARS-CoV-2 related M.sup.pro activity.

The present invention provides a compound represented by the formula (1) or a salt thereof, or a complex of the compound or the salt with a metal, in the formula (1), A.sup.1 represents a chelate group; R.sup.1 represents a hydrogen atom or the like; R.sup.2 represents a hydrogen atom or the like; and Z.sup.1, Z.sup.2, Z.sup.3, Z.sup.4, and Z.sup.5 are the same or different and each represent a nitrogen atom or CR.sup.3 or the like wherein R.sup.3 represents a hydrogen atom or an optionally substituted C.sub.1-6 alkyl group or the like; L.sup.1 represents a group represented by the formula (3) wherein R.sup.13, R.sup.14, R.sup.15, and R.sup.16 are the same or different and each represent a hydrogen atom or the like; L.sup.2 represents an optionally substituted C.sub.1-6 alkylene group; and L.sup.3 represents as optionally substituted C.sub.1-6 alkylene group.

##STR00001##

The present invention discloses a tripeptide propylene oxide derivative or a pharmaceutically acceptable salt thereof, and a preparation method and application thereof. The structure of the tripeptide propylene oxide derivative is shown in formula I. Compared with the prior art, the present invention provides tripeptide epoxy ketone compounds with a novel structure and a function of inhibiting proteasome. As 20S proteasome inhibitors, the tripeptide epoxy ketone compounds can block tumor cell proliferation and induce tumor cell apoptosis, so the tripeptide epoxy ketone compounds can be used for the treatment and prevention of a plurality of human and animal diseases such as malignant tumors, and the effect is significantly better.

The invention disclosed herein concerns a novel class of compounds suitable for the treatment of neurodegenerative diseases, such as Parkinson’s Disease.

Methods for the use of glutathione trisulfide (GSSSG) in neuroprotection, e.g., in neurodegenerative diseases and to reduce the risk of ischemic injury. The methods can be used, e.g., to reduce risk of injury to brain, spinal cord, and peripheral nerves from ischemia or low blood flow states possibly caused by surgery, trauma, and other conditions that decrease/impair blood flow and or oxygen delivery to the nervous system.

The present invention regards specific IBAT inhibitors useful in the prophylaxis and/or treatment of a liver disease. It also relates to compositions comprising these IBAT inhibitors, a method for treatment of the disorders and a kit comprising the substances or the compositions.