Warner-lambert Company

Isis Pharmaceuticals, Inc.

Trega Biosciences, Inc.

Other

Lion Bioscience Ag

Phenex Pharmaceuticals Ag

Pfizer Corporation

Otsuka Pharmaceutical Company, Limited

Mitokor, Inc.

Phenix Pharmaceuticals Ag

John S Kiely

Mel C Schroeder

Michael R Pavia

Sheila H DeWitt

Charles J Stankovic

David T Connor

Jagadish C Sircar

John Michael Domagala

Paul C Unangst

Charles F Schwender

Roderick J Sorenson

Mary E Carethers

Robert F Bruns

Elizabeth A Johnson

Michael C Griffith

Wiaczeslaw A Cetenko

Kelly G Sprankle

Phillip Dan Cook

John C Hodges

Marland P Hutt, Jr

David J Ecker

Jacqueline R Wyatt

Michael Egholm

Peter Eigil Nielsen

Oscar L Acevedo

Ole Buchardt

Claus Kremoser

Ronnie C Hanecak

Normand Hebert

Peter W Davis

Elena Dneprovskaia

Ulrich Deuschle

Kerstin Otte

Carlton Sage

Manish Sud

Ulrike Bauer

Zach Cheruvallath

Thomas K Hayes

Tim Gahman

Kristina Giegrich

Normand Hébert

Ingo Kober

Manfred Kögl

Harald Kranz

Matthew Lee

Bruce D Roth

James M Coull

Walter H Moos

Sylvester R Klutchko

Susan E Hagen

Beverly E Girten

Leif Hoejslet Christensen

Donna Reynolds Cody

Amaresh Basu

Sandra R Slivka

Suchin Huang

C John Blankley

Curtis C Hecht

Kim L Dueholm

Yazhong Pei

Muthiah Manoharan

Robert E Davis

Soumitra S Ghosh

Mark J Suto

Christopher Franklin Bigge

Jesper Lohse

Shelly Ann Glase

Mark Robert Barvian

Corinne E Augelli-Szafran

Timothy Gahman

Tomoyuki Yasunaga

Yingjie Lai

Takenori Kimura

Behrouz Bruce Forood

Steven Ware

Lawrence E Lesheski

Shunichiro Hachiya

Annette Theresa Sakkab

Larry Craswell Walker

Nian Zhuang

Michael Kell

Soren Holst Sonnechsen

Wiaczeslaw A Centenko

Behrouz Forood

Timothy C Gahman

A novel class of peptide nucleic acids are described which include a conjugate attached thereto. The peptide nucleic acids generally comprise ligands such as naturally occurring DNA bases attached to a peptide backbone through a suitable linker.

Peptide nucleic acid conjugates

The invention provides compounds according to the general formula () which bind to the NRHreceptor and act as agonists, antagonists or mixed agonists/antagonists of the NRHreceptor. The invention further provides methods of treating diseases and/or conditions through binding of the nuclear receptor by the compounds and the production of medicaments using the compounds.

FXR NR1H4 nuclear receptor binding compounds

The present invention relates to compounds according to the general formula (I) which bind to the nuclear receptor, NR1H4, and act as agonists and antagonists of the NR1H4 receptor. The invention further relates to the treatment of diseases and/or conditions through binding of the nuclear receptor by the compounds.

NR1H4 nuclear receptor binding compounds

The present invention relates to compounds according to the general formula (I) which bind to the NR1H4 receptor and act as agonists of the NR1H4 receptor. The invention further relates to the treatment of diseases and/or conditions through binding of the nuclear receptor by the compounds and the production of medicaments using the compounds.

The present invention provides a method of treating Alzheimer's disease using a compound of Formula (I). Also provided is a method of inhibiting the aggregation of amyloid proteins using a compound of the Formula (I) and a method of imaging amyloid deposits, as well as new compounds of Formula (I).

Method of inhibiting amyloid protein aggregation and imaging amyloid deposits

The present invention relates to genetic mutations in mitochondrial cytochrome c oxidase genes that segregate with Alzheimer's disease (AD). The invention provides methods for detecting such mutations, as a diagnostic for Alzheimer's Disease, either before or after the onset of clinical symptoms. The invention further provides treatment of cytochrome c oxidase dysfunction.

Method of targeting conjugate molecules to mitochondria

New sub-monomer synthetic methods for the preparation of peptide nucleic acid oligomeric structures are disclosed that provide for the synthesis of both predefined sequence peptide nucleic acid oligomers as well as random sequence peptide nucleic acid oligomers. Further these methods also provide for the incorporation of peptide nucleic acid units or strings of such units with amino acids or strings of amino acids in chimeric peptide nucleic acid-amino acid compounds. Further disclosed are method of making random libraries of peptide nucleic acids using the fully preformed monomers. Chimeric oligomers and libraries of the same are also disclosed.

Peptide nucleic acid combinatorial libraries and improved methods of synthesis

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

Chemical reaction apparatus, materials and methods are provided for the automatable, efficient synthesis of chemical species and libraries. In accordance with preferred embodiments, chemical droplet generation and direction techniques are employed to prepare oligomers and libraries of chemical species. Reaction assemblies adapted for efficient synthetic employment and for improved collection are also disclosed.

Chemical reaction apparatus and methods

Novel peptide nucleic acids and novel linked peptide nucleic acids, form triple stranded structures with nucleic acids. The peptide nucleic acids include ligands such as naturally occurring nucleobases attached to a peptide backbone through a suitable linker. Other nucleobases including C-pyrimidines and iso-pyrimidines can be used as the ligands in Hoogsteen strands to increase binding affinity. Two peptide nucleic acid strands are joined together with a linker to form a bis-peptide nucleic acid. The individual strands of the peptide nucleic acids in the bis compounds can be orientated either parallel or antiparallel to each other.

Peptide nucleic acids

Novel peptide nucleic acids and novel linked peptide nucleic acids, form triple stranded structures with nucleic acids. The peptide nucleic acids include ligands such as naturally occurring nucleobases attached to the peptide backbone through a suitable linker. Other nucleobases including C-pyrimidines and iso-pyrimidines can be used as the ligands in Hoogsteen strands to increase binding affinity. Two peptide nucleic acid strands are joined together with a linker to form a bis-peptide nucleic acid. The individual strands of the peptide nucleic acids in the bis compounds can be oriented either parallel or antiparallel to each other.

Linked peptide nucleic acids

4-substituted-quinoline derivatives and 4-substituted-quinoline combinatorial libraries

Chemical synthesis apparatus employing a droplet generator

The present invention relates to novel 4-substituted quinoline compounds of the following formula, libraries containing such compounds, and to the generation of such combinatorial libraries composed of such compounds:

4-Substituted-quinoline derivatives and 4-substituted-quinoline combinatorial libraries

New sub-monomer synthetic methods for the preparation of peptide nucleic acid oligomeric structures are disclosed that provide for the synthesis of both predefined sequence peptide nucleic acid oligomers as well as random sequence peptide nucleic acid oligomers. Further these methods also provide for the incorporation of peptide nucleic acid units or strings of such units with amino acids or strings of amino acids in chimeric peptide nucleic acid-amino acid compounds. Further disclosed are methods of making random libraries of peptide nucleic acids using the fully preformed monomers.

PNA combinatorial libraries and improved methods of synthesis

Growing community of inventors

Ann Arbor, MI, United States of America

John S Kiely