Pharmaceutical compositions of the invention include substituted riluzole prodrugs useful for the treatment of cancers including melanoma, breast cancer, brain cancer, and prostate cancer through the release of riluzole. Prodrugs of riluzole have enhanced stability to hepatic metabolism and are delivered into systemic circulation by oral administration, and then cleaved to release riluzole in the plasma via either an enzymatic or general biophysical release process.

This intention relates to a novel polymorph form of compound (R)-2-[2-amino-3-(indol-3-yl)propionylamino]-2-methylpropionic acid, a process for making the novel polymorph form of the compound, and uses thereof for making other polymorph forms of the compound. The invention further relates to composition comprising novel polymorph form of the compound and a pharmaceutically acceptable carrier or excipient.

The present invention provides a catalyst containing a Brønsted acid as a novel means capable of producing an amide compound by highly stereoselectively and/or highly efficiently causing an amidation reaction in a variety of substrates having a carboxylic ester group and an amino group.

The present invention relates to a peptide with amidated carboxy terminus having melanogenesis inhibitory activity and a composition comprising same, and more specifically, to a peptide with amidated (—NH.sub.2) carboxy terminus, composed of one amino acid sequence selected from the group consisting of SEQ ID NO: 3, SEQ ID NO: 5, SEQ ID NO: 9 to 18, and a pharmaceutical composition, cosmetic composition, and food composition for the treatment of pigmentation diseases comprising same as an active ingredient.

The present disclosure relates to prostate specific membrane antigen (PSMA) targeted compounds conjugated to near-infra red (NIR) dyes and methods for their therapeutic and diagnostic use. More specifically, this disclosure provides compounds and methods for diagnosing and treating diseases associated with cells and/or vasculature expressing prostate specific membrane antigen (PSMA), such as prostate cancer and related diseases. The disclosure further describes methods and compositions for making and using the compounds, methods incorporating the compounds, and kits incorporating the compounds.

Prodrugs of an NMDA antagonist, (S)-1-phenyl-2-(pyridin-2-yl)ethanamine, useful for the treatment of depression (particularly major depressive disorder) or pain; compositions comprising them, and methods of making them.

The present invention discloses compounds of Formula (I), and pharmaceutically acceptable salts, thereof:

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which inhibit coronavirus replication activity. The invention further relates to pharmaceutical compositions comprising a compound of Formula (I) or a pharmaceutically acceptable slat thereof, and methods of treating or preventing a coronavirus infection in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of a compound of Formula (I) or a pharmaceutically acceptable salt thereof.

N-terminally modified linear and branched polyamine conjugated peptidomimetics as antimicrobials agents. The invention relates to therapeutically viable antibacterial compositions based on ultra short mimetic of host defense cationic peptides (HDCPs). The invention relates to template based N-terminal modified di-peptidomimetics with or without modifications in polyamine backbone as new antibacterial agents. Most active peptidomimetics were bactericidal and caused a rapid decrease in viability of broad range of Gram-positive and Gram-negative bacterial strains in low micromolar concentration range including activity against clinically relevant pathogen methicillin resistant S. aureus (MRSA) andmethicillin resistant S. epidermidis(MRSE). Further the peptidomimetics were effective against MRSA biofilms (formation inhibition/killing of preformed biofilms) in vitro and were non toxic to human red blood cells and peripheral blood mononuclear cells. The molecules described in present invention do not develop resistance against MRSA under in vitro conditions and hence may be used as topical agents or in similar applications.

Provided are a tripeptide compound, a preparation method therefor, and an application thereof. The structure of the related compound is represented by formula (I). The provided compound has angiotensin converting enzyme inhibiting bioactivity, and the compound and a pharmaceutical composition thereof play a role in preventing and treating hypertension and other cardiocerebral vascular system diseases.

A compound of formula (I) and salts and solvates thereof, wherein R.sup.L is a linker for connection to a cell binding agent, which is formula (IIa) wherein Q is a tripeptide residue of formula (A), where x is 1 or 2, —C(═O)-Q.sup.x-NH— is a dipeptide residue; X is: formula (B), where a=0 to 5, b=0 to 16, c=0 or 1, d=0 to 5; and G.sup.L is a linker for connecting to a Ligand Unit.

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