Abstract: The present invention relates to a novel solid support template of Formula (I) and methods for producing novel highly functionalized imidazoles, pyrazinones and benzodiazepinones through a plurality of chemical reactions utilizing the solid support template
Abstract: Multifunctionalized support resin for the solid phase synthesis of combinatorial libraries is disclosed. The support resin comprises a resin backbone to which is attached a template containing at least two more attachment points which carry mutiple functionalized benzyl-type linkers. Each linker displays differing chemical stability under cleavage conditions so that products can be selectively and sequentially cleaved and separated from the reaction vessel. The linkers are independently different benzyl-type moieties, and each product synthesized on the linkers may have a different chemical structure. The support resin may further comprise an additional linker which is directly attached to the resin backbone. This linker can benzyl-type linkers or other traditional cleavable-linkers. The invention is further directed to a method for the production of mutiple combinatorial libraries in a simultaneous fashion utilizing the above described support resin.
Abstract: A method of synthesizing &agr;-sulfonamido amide, carboxylic acid or hydroxamic acid derivatives comprising providing a set of polymer-bound reactant(s) (sulfonamide, aldehyde or ketone, isocyanide or acid) to react with three sets of the other three reactants to form an array of polymer-bound &agr;-sulfonamido amide-type intermediates and use of such intermediates for the preparation of combinatorial libraries.
Type:
Grant
Filed:
May 15, 2002
Date of Patent:
June 24, 2003
Assignee:
Advanced Syntech, LLC
Inventors:
Eugene Campian, Boliang Lou, Adnan M. M. Mjalli
Abstract: Compounds having the structure
are peroxisome proliferator-activated receptor-gamma (PPAR-gamma) selective agonists and as such are useful in the modulation of blood glucose and the increase of insulin sensitivity in mammals. This activity of the piperazine derivatives of the invention make them particularly useful in the treatment of those conditions selected from the group consisting of diabetes, atherosclerosis, hyperglycemia, hyperlipidemia, obesity, syndrome X, insulin resistance, hypertension, heart failure and cardiovascular disease in mammals.
Abstract: Novel compositions comprising heterocyclic hydroxamic acid derivatives of the general formula:
These compounds are useful in the treatment of diseases and conditions in which matrix metalloproteinases are involved, such as cancer, arthritis, tumor metastasis and multiple sclerosis (MS).