University of Illinois

Other

Boston Scientific Corporation

David M Knapp

Stephen J Davis

Brian J Brown

Martin D Burke

Eric P Gillis

Kaitlyn C Gray

Justin Robert Struble

Brice E Uno

Nagarjuna Palyam

Jenna A Klubnick

Jonathan Swift Stinson

Herbert R Radisch, Jr

Stephen Scott Davis

Ian Dailey

Pulin Wang

Graham R Dick

Timothy Samuel Girton

James F Johnson

Thomas A Trozera

Charles Horace Craig

Suk Joong Lee

A J Johnson

Jan Weber

Herbert R Radisch

Stephen Davis

Justin Struble

Brian T Berg

Provided are certain derivatives of amphotericin B (AmB) characterized by reduced toxicity and retained anti-fungal activity. Certain of the derivatives are C16 urea derivatives of AmB. Certain of the derivatives are C3, C5, C8, C9, C11, C13, or C15 deoxy derivatives of AmB. Certain of the derivatives include C3′ or C4′ modifications of the mycosamine appendage of AmB. Also provided are methods of making AmB derivatives of the invention, pharmaceutical compositions comprising AmB derivatives of the invention, and methods of use of AmB derivatives of the invention.

Amphotericin B derivatives with improved therapeutic index

Provided are certain derivatives of amphotericin B (AmB) characterized by reduced toxicity and retained anti-fungal activity. Certain of the derivatives are C16 urea derivatives of AmB. Certain of the derivatives are C3, C5, C8, C9, C11, C13, or C15 deoxy derivatives of AmB. Certain of the derivatives include C3' or C4&#x2032; modifications of the mycosamine appendage of AmB. Also provided are methods of making AmB derivatives of the invention, pharmaceutical compositions comprising AmB derivatives of the invention, and methods of use of AmB derivatives of the invention.

Described are methods of forming protected boronic acids that provide in a manner that is straightforward, scalable, and cost-effective a wide variety of building blocks, such as building blocks containing complex and/or pharmaceutically important structures, and/or provide simple or complex protected organoboronic acid building blocks. A first method includes reacting an imino-di-carboxylic acid and an organoboronate salt. A second method includes reacting a N-substituted morpholine dione and an organoboronic acid.

Methods for forming protected organoboronic acids

A method of performing a chemical reaction includes reacting a compound selected from the group consisting of an organohalide and an organo-pseudohalide, and a protected organoboronic acid represented by formula (I) in a reaction mixture:R&#x2014;B-T&#x2003;&#x2003;(I);where Rrepresents an organic group, T represents a conformationally rigid protecting group, and B represents boron having sphybridization. When unprotected, the corresponding organoboronic acid is unstable by the boronic acid neat stability test. The reaction mixture further includes a base having a pKof at least 1 and a palladium catalyst. The method further includes forming a cross-coupled product in the reaction mixture.

Slow release of organoboronic acids in cross-coupling reactions

A protected organoboronic acid includes a boron having an sphybridization, a conformationally rigid protecting group bonded to the boron, and an organic group bonded to the boron through a boron-carbon bond. A method of performing a chemical reaction includes contacting a protected organoboronic acid with a reagent, the protected organoboronic acid including a boron having an sphybridization, a conformationally rigid protecting group bonded to the boron, and an organic group bonded to the boron through a boron-carbon bond. The organic group is chemically transformed, and the boron is not chemically transformed.

System for controlling the reactivity of boronic acids

A control system is provided for a rolling mill that feeds sheet material from an unwind reel to a rewind reel, passing it between a pair of work rolls. The control system includes a speed sensor for sensing speed of the sheet material and a sensor for measuring material thickness. A force controller controls force exerted on the sheet material by the work rolls. A tension controller controls tension on the unwind reel. A programmed controller is operatively connected to the speed sensor, the force controller and the tension controller, and stores information representing cyclical deviations in thickness of the sheet material and controls the force controller and the tension controller using the stored information and the sensed speed.

Periodic gauge deviation compensation system

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Boonville, IN, United States of America

David M Knapp