Gary H. Posner - Baltimore MD, US Lindsey C. Hess - Pflugerville TX, US Alvin S. Kalinda - Bloomington IN, US Rachel D. Slack - Baltimore MD, US Uttam Saha - Thornhill, CA P. Martin Petkovich - Kingston, CA
Assignee:
JOHNS HOPKINS UNIVERSITY - Baltimore MD CYTOCHROMA INC. - Markham ON
International Classification:
A61K 45/06 A61K 31/593 C07C 401/00
US Classification:
514167, 552653
Abstract:
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.
Meta-Diamide Compounds For Controlling Invertebrate Pests
- Bethesda MD, US JoLynn Barbara GIANCOLA - Boardman OH, US Rachel D. SLACK - Baltimore MD, US
International Classification:
C07D 471/10 C07D 211/58 C07D 241/04
Abstract:
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.
- Baltimore MD, US - Grand Cayman, KY Alvin S. Kalinda - Bloomington IN, US Rachel D. Slack - Baltimore MD, US Uttam Saha - Thornhill, CA P. Martin Petkovich - Kingston, CA
International Classification:
A61K 45/06 C07C 401/00 A61K 31/593
Abstract:
This present disclosure is directed to novel prodrugs of activated vitamin Dcompounds. 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.
- Baltimore MD, US Alvin S. Kalinda - Bloomington IN, US Rachel D. Slack - Baltimore MD, US Uttam Saha - Thornhill, CA P. Martin Petkovich - Kingston, CA
International Classification:
A61K 45/06 C07C 401/00 A61K 31/593
Abstract:
This present disclosure is directed to novel prodrugs of activated vitamin Dcompounds. 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.
Gary H. Posner - Baltimore MD, US Rachel D. Slack - Baltimore MD, US
Assignee:
THE JOHNS HOPKINS UNIVERSITY - BALTIMORE MD
International Classification:
C07D 493/18 A61K 45/06 A61K 31/357
Abstract:
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.
Trioxane Thioacetal Monomers And Dimers And Methods Of Use Thereof
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.