Other

Praecis Pharmaceuticals, Inc.

Takeda Pharmaceutical Company Limited

Millennium Pharmaceuticals Limited

Sonja A Komar

Phuong Nguyen

Raymond D Skwierczynski

Nobel T Truong

Michael J Kaufman

Eric L Elliott

Quentin J McCubbin

Vaithianathan Palaniappan

Csanad M Varga

Debra L Mazaik

Abu J Ferdous

Peter N Zawaneh

Malcolm L Gefter

Gary Fred Musso

Mark A Findeis

Christopher C Arico-Muendel

Ethan R Signer

Kathryn Phillips

James Wakefield

Michael Kelley

Susan Molineaux

Joseph Chin

Jung-Ja Lee

Neil J Hayward

Phoung M Nguyen

The present invention provides novel compounds useful as proteasome inhibitors. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.

Boronate ester compounds and pharmaceutical compositions thereof

Compounds that modulate natural &#x3b2; amyloid peptide aggregation are provided. The modulators of the invention comprise a peptide, preferably based on a &#x3b2; amyloid peptide, that is comprised entirely of D-amino acids. Preferably, the peptide comprises 3&#x2013;5 D-amino acid residues and includes at least two D-amino acid residues independently selected from the group consisting of D-leucine, D-phenylalanine and D-valine. In a particularly preferred embodiment, the peptide is a retro-inverso isomer of a &#x3b2; amyloid peptide, preferably a retro-inverso isomer of A&#x3b2;. In certain embodiments, the peptide is modified at the amino-terminus, the carboxy-terminus, or both. Preferred amino-terminal modifying groups include cyclic, heterocyclic, polycyclic and branched alkyl groups. Preferred carboxy-terminal modifying groups include an amide group, an alkyl amide group, an aryl amide group or a hydroxy group. Pharmaceutical compositions comprising the compounds of the invention, and diagnostic and treatment methods for amyloidogenic diseases using the compounds of the invention, are also disclosed.

Modulators of &#x3b2;-amyloid peptide aggregation comprising D-amino acids

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Belmont, MA, United States of America

Sonja A Komar