Johns Hopkins University

The United States of America, as Represented by the Secretary, Department of Health and Human Services

Opko Ireland Global Holdings, Limited

Rachel D Slack

Gary H Posner

P Martin Petkovich

Amy Hauck Newman

Uttam Saha

Lindsey C Hess

JoLynn Barbara Giancola

Jennifer R Mazzone

Alvin S Kalinda

Alexander M Jacobine

Disclosed herein are a series of modafinil analogue compounds that bind with moderate to high affinity to the dopamine (DA) transporter (DAT) and several analogues also having affinity for the serotonin (5-HT) transporter (SERT) and/or sigma-1 receptor. Employing aminopiperidine, piperidineamino, spirobicyclodiaza, or substituted piperazine functional groups, desired dopamine transporter affinity has been retained along with improved metabolic stability over unsubstituted piperazine ring analogues. Importantly, these compounds have no predicted addictive liability. Also disclosed are methods for treating substance use disorders as well as other neuropsychiatric disorders such as ADHD, depression, narcolepsy, and cognitive impairment.

Atypical inhibitors of monoamine transporters; method of making; and use thereof

This present disclosure is directed to novel prodrugs of activated vitamin D3 compounds. The prodrugs can be designed to have one or more beneficial properties, such as selective inhibition of the enzyme CYP24, low calcemic activity, and anti-proliferative activity. Specifically, these prodrugs are 1-deoxy prohormones of active Vitamin D analogs, e.g. analogs of calcitriol. This disclosure is also directed to pharmaceutical and diagnostic compositions containing the prodrugs of the invention, and to their medical use, particularly as prodrugs in the treatment and/or prevention of diseases.

1-deoxy analogs of 1,25-dihydroxyvitamin D3 compounds

Monomeric and dimeric trioxane thioacetals and methods of their use for treating subjects infected with malaria or other parasitic infectious diseases including, but not limited to, toxoplasmic infection; subjects afflicted with psychiatric conditions associated with toxoplasmic infection; and subjects afflicted with cancer.

Trioxane thioacetal monomers and dimers and methods of use thereof

Anilide derivatives of the natural trioxane artemisinin were prepared and evaluated for antimalarial efficacy in-infected mice. Selected anilides derivatives administered orally as one single-digit dose combined with mefloquine hydrochloride were completely curative, i.e., all 5 of the mice in the particular treatment group had no detectable parasitemia on day 30 post infection, gained as much weight by day 30 post infection as the control mice (no infection), and behaved normally.

Monomeric trioxane amide sulfur compounds

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Baltimore, MD, United States of America

Rachel D Slack