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Bioorganic & Medicinal Chemistry Letters | 1998

Highly efficient and versatile synthesis of libraries of constrained β-strand mimetics

Cyprian O. Ogbu; Maher Qabar; P. Douglas Boatman; Jan Urban; Joseph Patrick Meara; Mark D. Ferguson; John Tulinsky; Chris Lum; Suresh Babu; Mark A. T. Blaskovich; Hiroshi Nakanishi; Fuqiang Ruan; Bolong Cao; Ryan Minarik; Thomas Little; Sherry Nelson; Minh T. Nguyen; Anna Gall; Michael Kann

The general approach of using a bicyclic template to produce inhibitors of the protease superfamily of enzymes has been investigated. The Diels-Alder cycloaddition reaction on solid support has been found to be highly efficient for the synthesis of libraries of compounds that mimic the β-strand secondary structure of proteins. Several potent and selective inhibitors of proteases have been discovered.


Synthetic Communications | 2002

EFFICIENT SYNTHESIS OF NOVEL 4-SUBSTITUTED URAZOLES

Thomas Little; Joseph Patrick Meara; Fuqiang Ruan; Minh T. Nguyen; Maher Qabar

ABSTRACT The efficient synthesis of several new and novel 4-substituted triazolidindiones (urazoles) starting from isocyanates, amines, anilines and carboxylic acids is reported.


Bioorganic & Medicinal Chemistry Letters | 2003

Sulphonamide-based small molecule VLA-4 antagonists

Marcin Stasiak; Christopher Mehlin; Erica Boni; Tomas Vaisar; Thomas Little; Hwa Ok Kim; Maher Qabar

The discovery of a sulphonamide by-product with VLA-4 antagonistic activity led to a series of potent, small molecule VLA-4 antagonists. Synthesis, SAR and in vivo evaluation of the selected compound will be presented.


Archive | 2011

PDE10 inhibitors and related compositions and methods

Neil S. Cutshall; Jennifer Lynn Gage; Thomas Neil Wheeler; Thomas Little


Archive | 2008

Amine derivative compounds for treating ophthalmic diseases and disorders

Ian L. Scott; Vladimir Kuksa; Mark W. Orme; Feng Hong; Thomas Little; Ryo Kubota


Archive | 2005

Protein tyrosine phosphatase inhibitors and methods of use thereof

Mark A. T. Blaskovich; Ted Baughman; Thomas Little; William Patt; Maher Qabar; Lauri Schultz; Feng Hong; Gangadhar Nagula; Jennifer Gage; James Jeffrey Howbert


Archive | 2011

Alkoxy compounds for disease treatment

Ian L. Scott; Vladimir Kuksa; Mark W. Orme; Thomas Little; Anna Gall; Feng Hong


Archive | 2008

Alkynyl phenyl derivative compounds for treating ophthalmic diseases and disorders

Ian L. Scott; Vladimir Kuksa; Mark W. Orme; Thomas Little; Anna Gall; Jennifer Gage; Feng Hong


Archive | 2008

Styrenyl derivative compounds for treating ophthalmic diseases and disorders

Ian L. Scott; Vladimir Aleksandrovich Kuska; Anna Gall; Mark W. Orme; Jennifer Gage; Thomas Little; Qin Jiang; Lana Michele Rossiter; Kevin F Mcgee; Ryo Kubota


Archive | 2015

PROCESSES AND INTERMEDIATES FOR THE PREPARATION OF A PDE10 INHIBITOR

Neil S. Cutshall; Jennifer Lynn Gage; Thomas Little; Wayne Douglas Luke; Elisabeth C.A. Brot; Marco Jonas; Michael James Mcdermott; Karl Reineke

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