Hoffmann-la Roche Inc.

Arrowhead Madison, Inc.

Arrowhead Pharmaceuticals, Inc.

F. Hoffmann-la Roche Ag

Arrowhead Research Corporation

Torsten Hoffmann

Patrick Schnider

Heinz Stadler

Thierry Godel

Peter Mohr

David B Rozema

Guido Galley

Philipp Hadwiger

David L Lewis

Eric Argirios Kitas

Walter Hunkeler

Michael B&ouml;s

Ingo Roehl

Darren H Wakefield

Andrew Sleight

Hans Martin Mueller

Kerstin Jahn-Hofmann

Guenther Ott

Sonia Maria Poli

Jon Asher Wolff

Roger David Norcross

Roland Jakob-Roetne

Andrei V Blokhin

Jeffrey Carlson

Cornelia Hertel

Jonathan D Benson

Andreas Koblet

Linda Valis

Jens-Uwe Peters

Stephan Roever

Quirico Branca

Matthias Heinrich Nettekoven

Hasane Ratni

Henner Knust

Uwe Grether

Sabine Kolczewski

Philippe Pflieger

Paul Hebeisen

Caterina Bissantz

Holger Kuehne

Annick Goergler

Urs Schwitter

Eric Joseph Niesor

Pius Waldmeier

Fabienne Hoffmann-Emery

Xihan Wu

Philippe Jablonski

Wilma Thuer

Theresa Maria Ballard

Ingo Röhl

Günther Ott

Kerstin Jahn-Hoffmann

Christoph Funk

Sonja Nick

Linda Christine Valis

Eric A Kitas

Michael Boes

The invention provides novel compounds and conjugates of these compounds useful for the delivery of biologically active substances. Further novel design criteria for chemically stabilized siRNA particular useful when covalently attached to a delivery polymer to achieve in vivo mRNA knock down are disclosed therein.

Small molecule conjugates for intracellular delivery of biologically active compounds

The present invention is directed compositions for targeted delivery of RNA interference (RNAi) polynucleotides to cell in vivo. The pharmacokinetic modulator improve in vivo targeting compared to the targeting ligand alone. Targeting ligand-pharmacokinetic modulator targeting moiety targeted RNAi polynucleotides can be administered in vivo alone or together with co-targeted delivery polymers.

Galactose cluster-pharmacokinetic modulator targeting moiety for siRNA

The invention provides use of novel compounds for delivery of nucleic acids, and conjugates of these compounds with nucleic acids. Further novel design criteria for chemically stabilized siRNA particular useful when covalently attached to said compounds and co-administered with a delivery polymer to achieve mRNA knock down in vivo are disclosed therein.

Small molecule conjugates for intracellular delivery of nucleic acids

The present invention is directed compositions for targeted delivery of RNA interference (RNAi) polynucleotides to hepatocytes in vivo. Targeted RNAi polynucleotides are administered together with co-targeted melittin delivery peptides. Delivery peptides provide membrane penetration function for movement of the RNAi polynucleotides from outside the cell to inside the cell. Reversible modification provides physiological responsiveness to the delivery peptides.

Peptide-based in vivo siRNA delivery system

The present invention is directed compositions for targeted delivery of RNA interference (RNAi) polynucleotides to hepatocytes in vivo. Targeted RNAi polynucleotides are administered together with co-targeted delivery polymers. Delivery polymers provide membrane penetration function for movement of the RNAi polynucleotides from outside the cell to inside the cell. Reversible modification provides physiological responsiveness to the delivery polymers.

Compositions for targeted delivery of siRNA

The present invention is directed compositions for delivery of RNA interference (RNAi) polynucleotides to cells in vivo. The compositions comprise amphipathic membrane active polyamines reversibly modified with enzyme cleavable dipeptide-amidobenzyl-carbonate masking agents. Modification masks membrane activity of the polymer while reversibility provides physiological responsiveness. The reversibly modified polyamines (dynamic polyconjugate or DPC) are further covalently linked to an RNAi polynucleotide or co-administered with a targeted RNAi polynucleotide-targeting molecule conjugate.

In vivo polynucleotide delivery conjugates having enzyme sensitive linkages

The present invention relates to compounds of formula I, wherein A, Rto Rare defined in the description, and to pharmaceutically acceptable salts thereof. The present invention also relates to the manufacture of such compounds or their pharmaceutically acceptable salts, pharmaceutical compositions containing them and their use as medicaments for the treatment and/or prophylaxis of diseases which can be treated with HDL-cholesterol raising agents, such as dyslipidemia, atherosclerosis and cardiovascular diseases.

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The present invention provides a method for the treatment of schizophrenia which comprises administering a compound of formula 

Dual NK1/NK3 receptor antagonists

The invention is concerned with compounds of formula I: wherein R, R, and Q are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds are useful as inhibitors of cholesteryl ester transfer protein (CETP).

Compounds

The invention relates to pyrrolidine derivatives of formula wherein

Pyrrolidine derivatives as dual NK1/NK3 receptor antagonists

Growing community of inventors

Weil am Rhein, Germany

Torsten Hoffmann