Isis Pharmaceuticals, Inc.

Ambit Biosciences Corporation

Other

Ambit Bioscience Corporation

Kelly G Sprankle

Phillip Dan Cook

Shripad S Bhagwat

Qi Chao

John S Kiely

Bruce S Ross

Martin W Rowbottom

Mark W Holladay

Eduardo Setti

Andiliy Gokching Lai

Brian T Campbell

Sunny Abraham

Raffaella Faraoni

Yogesh S Sanghvi

Robert H Springer

Rich H Griffey

Hitesh K Patel

Robert M Grotzfeld

Eric E Swayze

Muthiah Manoharan

Michael Egholm

Peter Eigil Nielsen

Jesper Lohse

Ole Buchardt

Peter W Davis

Michael C Griffith

Soren Holst Sonnechsen

Robert Jay Tinder

Shripad Bhagwat

Compounds, compositions and methods are provided for modulating the activity of RAF kinases, including BRAF kinase and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder mediated by RAF kinases.

RAF kinase modulator compounds and methods of use thereof

Compositions of 1-(3-((6,7-dimethoxyquinazolin-4-yl)oxy)phenyl)-3-(5-(1,1,1, -trifluoro-2-methylpropan-2-yl)isoxazol-3-yl)urea are provided for modulating the activity of RAF kinases, including BRAF kinase and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder mediated by RAF kinases.

Compounds according to formula (I), compositions and methods are provided for modulating the activity of RAF kinases, including BRAF kinase and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder mediated by RAF kinases. Formula (I): or a pharmaceutically acceptable salt, solvate, clathrate of hydrate thereof, wherein X is O or S(O); Ris O or S. 

Compounds, compositions and methods are provided for modulating the activity of receptor kinases and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder mediated by receptor kinases.

Imidazolothiazole compounds for the treatment of disease

Method of using imidazolothiazole compounds for the treatment of disease

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

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

The present invention provides monocyclic, bicyclic and oligomeric amine compounds with at least two sites of diversity. These compounds are formed from monocyclic scaffolds which can be cyclized to form bicyclic amine scaffolds. These can then be reacted with building blocks to form the amine compounds of the invention. This invention further provides libraries or monocyclic, bicyclic and oligomeric amine compounds. Also provided are methods for preparing monocyclic, bicyclic and oligomeric amine compounds and libraries thereof. The present invention also provides pharmaceutical compositions of the monocyclic, bicyclic and oligomeric amine compounds.

Amine compounds and combinatorial libraries comprising same

Oligonucleotide analogs are disclosed having pyrimidine monomeric sub-units therein that are modified at the 2&prime; and 5&prime; positions. Monomeric sub-units having these modifications may be further modified at the 2&prime; position. Improved processes for the synthesis of 2&prime;-O-substituted pyrimidine nucleosides are also provided. The processes feature alkylation of a 2,2&prime;-anhydropyrimidine nucleoside or a 2S,2&prime;-anhydropyrimidine nucleoside with a weak nucleophile in the presence of a Lewis acid.

Process for the synthesis of 2&prime;-O-substituted pyrimidines and oligomeric compounds therefrom

Oligonucleotide analogs are disclosed having pyrimidine monomeric sub-units therein that are modified at the 2&prime; and 5 positions. Monomeric sub-units having these modifications may be further modified at the 2 position. Improved processes for the synthesis of 2&prime;-O-substituted pyrimidine nucleosides are also provided. The processes feature alkylation of a 2,2&prime;-anhydropyrimidine nucleoside or a 2S,2&prime;-anhydropyrimidine nucleoside with a weak nucleophile in the presence of a Lewis acid.

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

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Vista, CA, United States of America

Kelly G Sprankle