Harvard College

Lion Bioscience Ag

Ludwig Institute for Cancer Research Limited

Kalypsys, Inc.

Timothy Gahman

Randall W King

Daniel J Finley

Byung-Hoon Lee

Min Jae Lee

Beverly E Girten

Hengyuan Lang

Andrew Shiau

Michael C Griffith

Kevin Ross Holme

Sandra R Slivka

Karen J Watson-Straughan

Michael J Green

John S Kiely

Yazhong Pei

Stewart Alwyn Noble

Ronald R Tuttle

Mark R Herbert

Russell Donovan Cousins

Christian Andreus Hassig

Andrew K Shiau

Amaresh Basu

Christa Hamashin

Ming Qi

Curtis C Hecht

Richard Kolodner

Angelina M Thayer

Douglas L Hitchin

Hui Zhuang

Kevin C Dines

Christopher R Santos

Xiaohong Chen

James E Macdonald

Described inter alia are compounds according to formula (I): or a pharmaceutically acceptable salt thereof, and uses in methods for the modulation of flap endonuclease 1 (FEN1), Xeroderma Pigmentosum Complementation Group G protein (XPG), Exonuclease 1 (EXO1) and/or GEN1. 

3-hydroxy-quinazoline-2,4-dione derivatives and their use as nuclease modulators

Provided herein, inter alia, are compounds and methods for inhibiting PLK4 and for treating cancer in a subject in need thereof.

PLK4 inhibitors

Proteinopathies result from the proteasome not acting efficiently enough to eliminate harmful proteins and prevent the formation of the pathogenic aggregates. As described herein, inhibition of proteasome-associated deubiquitinase Usp14 results in increased proteasome efficiency. The present invention therefore provides novel compositions and methods for inhibition of Usp14, enhancement of proteasome activity and treatment of proteinopathies.

Compositions and methods for enhancing proteasome activity

Tricyclic proteasome activity enhancing compounds

The present invention relates to compounds and methods useful as inhibitors of nitric oxide synthase. Certain compounds of the subject invention have the following structural formula: wherein T, X, and Y are independently selected from the group consisting of CR, N, NR, S, and O; U is selected from the group consisting of CRand N; V is selected from the group consisting of CRand N; W and W' are independently selected from the group consisting of CH, CRR, NR, O, N(O), S(O)and C(O); n, m and p are independently an integer from 0 to 5; q is 0, 1, or 2; and other substituents are as defined herein. Other compounds of the subject invention have structural formulas as defined herein. Also disclosed herein are pharmaceutical compositions comprising the compounds of the subject invention.

Inducible nitric oxide synthase dimerization inhibitors

Triamine derivative melanocortin receptor ligands and methods of using same

Methods for treating erectile dysfunction using tetrahydroisoquinoline aromatic amines that function as melanocortin receptor ligands.

Treatment of erectile dysfunction using isoquinoline compound melanocortin receptor ligands

Methods for treating sexual dysfunction, such as erectile dysfunction or sexual arousal disorder, with a compound having the generic formula X &mdash;X -(D)Phe-Arg-(D)Trp-X . A particularly useful compound is HP-228, which has the formula Ac-Nle-Gln-His-(D)Phe-Arg-(D)Trp-Gly-NH . The invention also provides methods for selecting melanocortin receptor-3 ligands by determining whether a compound modulates the activity of MC-3 as an agonist or antagonist. These methods can be used to screen compound libraries for ligands to treat MC-3-associated conditions. Such conditions include sexual dysfunction, including erectile dysfunction and sexual arousal disorder.

Melanocortin receptor-3 ligands to treat sexual dysfunction

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Encinitas, CA, United States of America

Timothy Gahman