Novartis Ag

U.S. Department of Energy

Cameron Lee

Tanzina Fazal

Jeremy Baryza

Laura West

Junping Zhao

Keith Bowman

Andrew John Geall

Chandra Vargeese

Jun Liu

Jean M J Frechet

Keith A Bowman

Dirk Behnke

Jeremy Lee Baryza

Timothy Z Hoffman

Juergen Klaus Maibaum

Qihui Jin

Yefen Zou

Yun Feng Xie

Jianfeng Pan

Laura Ellen West

Rachna Jain

Xueshi Hao

Arnaud Lacoste

Tingting Mo

Xin Qu

Shanshan Yan

Jan Tchorz

Yahu Liu

Frada Berenshteyn

Stephany M Standley

Tanzina Labonte

Timothy Hoffman

The present invention is related to 6-6 Fused Bicyclic Heteroaryl Compounds of the Formula A2 or A1 and their Use as LATS Inhibitors, or a salt, stereoisomer or pharmaceutical composition thereof; wherein the variables are as defined herein. The present invention further relates to a method of LATS inhibition in a cell population using a compound of Formula A1, or a salt, stereoisomer or pharmaceutical composition thereof. The present invention further provides a method for manufacturing compounds of the invention, and its therapeutic uses. The invention further provides methods to their preparation, to their medical use, their use in the treatment and management of diseases or disorders.

6-6 fused bicyclic heteroaryl compounds and their use as LATS inhibitors

Disclosed are formulation and optimization protocols for delivery of therapeutically effective amounts of biologically active agents to liver, tumors, and/or other cells or tissues. Also provided are compositions and uses for cationic lipid compounds of formula (I). The invention also relates to compositions and uses for stealth lipids of formula (XI). Also provided are processes for making such compounds, compositions, and formulations, plus methods and uses of such compounds, compositions, and formulations to deliver biologically active agents to cells and/or tissues.

Lipids, lipid compositions, and methods of using them

Novel main chain acid degradable polymer backbones and drug delivery systems comprised of materials capable of delivering bioactive materials to cells for use as vaccines or other therapeutic agents are described. The polymers are synthesized using monomers that contain acid-degradable linkages cleavable under mild acidic conditions. The main chain of the resulting polymers readily degrade into many small molecules at low pH, but remain relatively stable and intact at physiological pH. The new materials have the common characteristic of being able to degrade by acid hydrolysis under conditions commonly found within the endosomal or lysosomal compartments of cells thereby releasing their payload within the cell. The materials can also be used for the delivery of therapeutics to the acidic regions of tumors and other sites of inflammation.

Main chain acid-degradable polymers for the delivery of bioactive materials

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Cambridge, MA, United States of America

Cameron Lee