Sirna Therapeutics, Inc.

Merck + Co., Inc.

Jennifer R Davis

Matthew G Stanton

Steven L Colletti

Brian W Budzik

Darla Danile Seifried

Ivory Hills

Weimin Wang

Lu Tian

Mark Cameron

Andrea R Geiser

Vladislav V Telyatnikov

Harold G Selnick

Linghang Zhuang

Craig Alan Coburn

James C Barrow

Shawn J Stachel

Shaun R Stauffer

Philippe G Nantermet

The instant invention provides for novel cationic lipids that can be used in combination with other lipid components such as cholesterol and PEG-lipids to form lipid nanoparticles with siRNA, to facilitate the cellular uptake and endosomal escape, and to knockdown target mRNA both in vitro and in vivo.

Cationic lipids with various head groups for oligonucleotide delivery

The instant invention provides for novel cationic lipids that can be used in combination with other lipid components such as cholesterol and PEG-lipids to form lipid nanoparticles with oligonucleotides. It is an object of the instant invention to provide a cationic lipid scaffold that demonstrates enhanced efficacy along with lower liver toxicity as a result of lower lipid levels in the liver. The present invention employs low molecular weight cationic lipids with one short lipid chain to enhance the efficiency and tolerability of in vivo delivery of siRNA.

Low molecular weight cationic lipids for oligonucleotide delivery

The present invention is directed to phenylamide and pyridylamide derivative compounds of which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.

Phenylamide and pyridylamide beta-secretase inhibitors for the treatment of Alzheimer's disease

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Richboro, PA, United States of America

Jennifer R Davis