The invention relates to methods for treating depression, anxiety, and other related diseases by administering a peptide NMDAR partial agonist.

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:

##STR00001##

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.

Processes are described for the preparation of tubulysins. The processes are useful for preparing predetermined mixtures of tubulysins, preparing single tubulysins from mixtures of tubulysins, and for converting one tubulysin into a different tubulysin. The tubulysins described herein are useful in treating diseases and disease states that include pathogenic cell populations.

A method of synthesing a compound of formula (I) from a compound of formula (III). ##STR00001##

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.

Some embodiments include compounds that can inhibit the growth of bacterial and/or inhibit or reduce microbial infections caused by one or more microorganisms (e.g., Pseudomonas aeruginosa and Cryptococcus neoformans) and methods of using these compounds to treat microbial infection and outbreaks and/or to reduce the formation of biofilms. Other embodiments include synthesis of the compounds that can inhibit the growth of one or more microorganisms and/or inhibit or reduce microbial infections.

The present disclosure provides compounds that are useful for inhibiting the STAT6 pathway. Also provided are related pharmaceutical compositions and methods of using the compounds. In some embodiments, the compounds may be used to treat a disease such as, e.g., an allergic lung disease, allergic rhinitis, chronic pulmonary obstructive disease, or a cancer.

Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases associated with the proteasome. The peptide-based compounds include an epoxide or aziridine, and functionalization at the N-terminus. Among other therapeutic utilities, the peptide-based compounds are expected to display anti-inflammatory properties and inhibition of cell proliferation. Oral administration of these peptide-based proteasome inhibitors is possible due to their bioavailability profiles.

The present invention relates to novel amide derivatives of N-urea substituted amino acids, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor like-1 (FPRL-1) receptor.