Bionomics Inc.

Genentech, Inc.

The Walter and Eliza Hall Institute of Medical Research

Abbott Laboratories Corporation

Abbvie Inc.

Merck Sharp + Dohme Corp.

The Walter and Eliza Hall Medical Research Institute

Brad E Sleebs

Jonathan Bayldon Baell

Chinh Thien Bui

Bernard Luke Flynn

Nurul Quazi

Ian Phillip Street

John A Flygare

Wayne J Fairbrother

Guillaume Laurent Lessene

Andrew J Souers

Keith G Watson

Steven Elmore

Chudi Obioma Ndubaku

Andrew M Petros

Danette Dudley

Brian John Smith

Peter Colman

Peter Edward Czabotar

George Nikolakopoulos

Carl Steven Rye

Ian Philip Street

Jared N Cumming

Xilu Wang

Le Wang

Zhi-Fu Tao

David Brian Olsen

Lisa A Hasvold

Andrew John Harvey

Dharam Paul

Damian Wojciech Grobelny

Tanweer A Khan

Michael F T Koehler

Kurt Deshayes

Alan F Cowman

Justin A Boddey

Sue O'Connor

The present invention provides methods of treating malaria comprising administration of an N3-substituted iminopyrimidinone of Formula (I) or a pharmaceutically acceptable salt thereof, to a subject in need thereof, wherein the variables R, R, R, R, R, A, B, L, m, and n are as defined herein. The invention also provides uses of the compounds of Formula (I), as defined herein, for inhibiting plasmepsin V activity, for treating ainfection, and for treating malaria. Also provided are methods of treatment further comprising administration of one or more additional anti-malarial compounds.

N3-substituted iminopyrimidinones as antimalarial agents

The present invention relates to chemical compounds of general formula (I): which may possess useful therapeutic activity in a range of central nervous system disorders, and in particular, anxiety disorders.

Anxiolytic compounds

The present invention relates to chemical compounds of general formula (I) which may possess useful therapeutic activity in a range of central nervous system disorders, and in particular, anxiety disorders.

In one aspect, the present invention provides for a compound of Formula I in which in Formula I, the variables X, X, X, X, R, B, L, E, A and the subscript n are as defined herein. In another aspect, the present invention provides for pharmaceutical compositions comprising compounds of Formula I as well as methods for using compounds of Formula I for the treatment of diseases and conditions (e.g., cancer, thrombocythemia, etc) characterized by the expression or over-expression of Bcl-2 anti-apoptotic proteins, e.g., of anti-apoptotic Bcl-xproteins.

Compounds and methods of use

The present invention provides compounds of formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful in treating central nervous system disorders, such as anxiety disorders or depression. 

Small-molecules as therapeutics

In one aspect, the present invention provides for a compound of Formula I in which the variable X, X, X, X, Q, A, R, B, L, E, and the subscripts m and n have the meanings as described herein. In another aspect, the present invention provides for pharmaceutical compositions comprising compounds of Formula I as well as methods for using compounds of Formula I for the treatment of diseases and conditions (e.g., cancer, thrombocythemia, etc) characterized by the expression or over-expression of Bcl-2 anti-apoptotic proteins, e.g., of anti-apoptotic Bcl-xproteins.

Heterocyclic compounds and methods of use

The invention relates generally to small molecules that mimic the biological activity of certain peptides and proteins, to compositions containing them and to their use. In particular, the invention relates to compounds of the general formula (I) that mimic the biological activity of BH3-only proteins and are capable of binding to and neutralizing pro-survival Bcl-2 proteins: wherein A, A, B, B, B, X, Z, R, R, Rand t are as described herein. The invention also relates to processes of preparing the benzenesulfonamide compounds that mimic portions of peptides and proteins, and to the use of such compounds in the regulation of cell death and the treatment and/or prophylaxis of diseases or conditions associated with the deregulation of cell death.

Arylsulfonamide compounds

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Victoria, Australia

Brad E Sleebs