University of California

Michigan State University

Other

University of Central Florida Research Foundation Inc

The United States Government as Represented by the Department of Veterans Affairs

Memorial Sloan Kettering Cancer Center

The Broad Institute, Inc.

James H McKerrow

Fred Ehrenkranz Cohen

Muraleedharan G Nair

George Lommel Kenyon

Zhe Li

Robert H Cichewicz

Khanitha Pudhom

Philip Jon Rosenthal

Gabriel Navarro

Rongshi Li

Baoqing Gong

Xiaowu Chen

Xiaohui Du

Chun Guo

Christine Sun Ring

Derek Shieh Tan

Sivaraman Dandapani

Debopam Chakrabarti

Roger G Linington

Corinne N Foley

Rahul Edwankar

Alyssa Verano

Bracken Roberts

Gustavo Moura-Letts

William E Keene

Roger R Linington

The present disclosure provides compounds of Formula (I'), Formula (II), and Formula (III). The compounds described herein may useful in treating and/or preventing protozoan infections in a subject in need thereof, treating and/or preventing trypanosomal infections (e.g.,() orinfections) and/or plasmodial infections in a subject in need thereof, treating and/or preventing diseases in a subject in need thereof (e.g., Chagas disease, malaria, and/or sleeping sickness), and may be useful in treating and/or preventing infectious diseases in a subject in need thereof. Also provided in the present disclosure are pharmaceutical compositions, kits, methods, and uses including a compound described herein. 

Anti-parasitic compounds and uses thereof

Small molecule therapeutics for the treatment of parasitic diseases, in particular, semi-synthetic derivatives of the fungally-derived natural product merulin A for the treatment of African Sleeping Sickness.

Methods for making and using novel semi-synthetic small molecules for the treatment parasitic disease

Small molecule therapeutics for the treatment of parasitic diseases, in particular, semi-synthetic derivatives of the fugally-derived natural product merulin A for the treatment of African Sleeping Sickness.

Semi-synthetic small molecules for the treatment parasitic disease

The present invention relates to thio semicarbazone and semicarbazone inhibitors of cysteine proteases and methods of using such compounds to prevent and treat protozoan infections such as trypanosomiasis, malaria and leishmaniasis. The compounds also find use in inhibiting cysteine proteases associated with carcinogenesis, including cathepsins B and L.

Thio semicarbazone and semicarbozone inhibitors of cysteine proteases and methods of their use

Anthraquinones are described which are antihelminthic and in particular, are useful in compositions for inhibitingsp. in vitro or in vivo. The preferred anthraquinones have the formula: wherein R, R, R, and Rare each hydrogen, hydroxy, halogen, alkyl, substituted alkyl, alkene, substituted alkene, alkyne, aryl, substituted aryl, cyclic, substituted cyclic, acid group, carbohydrate, or combination thereof, R is a group containing 1 to 12 carbons such as methyl, alkyl, substituted alkyl, aldehyde, hydroxy, hydroxymethyl, acid group, carbohydrate, or combination thereof, and the halogen is I, F, Br, or Cl.

Antihelminthic anthraquinones and method of use thereof

Anthraquinones are described which are antihelminthic and in particular, are useful in compositions for inhibitingsp. in vitro or in vivo. The preferred anthraquinones have the formula:wherein R, R, R, and Rare each hydrogen, hydroxy, halogen, alkyl, substituted alkyl, alkene, substituted alkene, alkyne, aryl, substituted aryl, cyclic, substituted cyclic, acid group, carbohydrate, or combination thereof, R is a group containing 1 to 12 carbons such as methyl, alkyl, substituted alkyl, aldehyde, hydroxy, hydroxymethyl, acid group, carbohydrate, or combination thereof, and the halogen is I, F, Br, or Cl.

Thio semicarbazone and semicarbazone inhibitors of cysteine proteases and methods of their use

Inhibitors of metazoan parasite proteases

Compositions and methods are disclosed for treating a patient infected with a metazoan parasite by inhibiting the enzymatic action of the metazoan parasite protease, wherein there is employed at least one compound of formula I

The invention relates to synthetic tetrapeptides that contain a peptide blocking group at the amino terminus and an enzyme inhibitor at the carboxy terminus, and their use in the prevention of schistosome parasite infection.

Synthetic tetrapeptides for the prevention of schistosome parasite

The present invention is a composition of matter composed essentially of a purified homogeneous thiol proteinase secreted by Entamoeba histolytica trophozoites. In purified homogeneous form the neutral thiol proteinase has a subunit molecular weight of about 56,000.+-.4,000, a neutral pH optimum, and an isoelectric point of about 6. The purified neutral thiol proteinase of the present invention can be obtained by using anion exchange and chromatofocusing Fast Protein Liquid Chromatography (FPLC) to purify the major neutral proteinase from secretions of axenically cultured Entamoeba histolytica trophozoites. The homogeneous neutral thiol proteinase of the present invention is immunogenic. It is useful as a serodiagnostic reagent for identifying the presence of antibodies in the sera of individuals exposed to Entamoeba histolytica trophozoites. The purified homogeneous enzyme can be used in ELISA assays or in other standard immunoassays.

Serodiagnostic reagent for entamoeba histolytica

Growing community of inventors

San Francisco, CA, United States of America

James H McKerrow