Florida Atlantic University

Eli Lilly and Company

Salvatore Donato Lepore

Michael Robert Wiley

Gerald Floyd Smith

John Joseph Masters

David Kent Herron

Ying Kwong Yee

Theodore Goodson, Jr

David Mendel

Sajan Joseph

Leander Merritt

Anne Louise Tebbe

Andrew Michael Ratz

Angela Lynn Marquart

Kenneth Dawson-Scully

Wesley L Bollinger

Nadia K Sial

Elijah J St Germain

Ankush Baburao Argade

Samantha L Maki

Theodore Junior Goodson

Ankush B Rigel Pharmaceuticals Inc Argade

Neuroprotective compounds for reducing neurological damage due to cellular stress in an individual are of Formula 1: or an enantiomer, diastereomer, racemic mixture or a pharmaceutically acceptable salt thereof, wherein: Ar=aryl; Y=aryl substituent (ortho, meta, or para) selected from the group consisting of: alkyl, alkyloxy, alkylamino, RRN, and halo; X&#x2550;O, N, or S; R&#x2550;H, alkyl, aryl, OH, alkyloxy, aryloxy, NH, alkylamino, RRN, or arylamino; Rand R=alkylcarbonyl, arylcarbonyl, alkyl, or H, individually; R=arylCH&#x2550;CH, alkylCH&#x2550;CH, alkyl; R&#x2550;H, alkyl, or aryl; and Rand R=alkyl, individually. Methods of reducing neurological damage due to cellular stress in an individual include administering to the individual during or after the cellular stress a neuroprotective compound of Formula I in a therapeutically effective amount to restore synaptic function during or after the cellular stress.

Bridged bicyclic compounds and their derivatives as neuroprotective agents and methods of use thereof

Sulfonate leaving groups include a cation chelating moiety, e.g. a polyether or crown ether. The chelating moiety stabilizes the sulfonate leaving group by forming a complex with a cation of a cation-nucleophile combination. The stabilized leaving group is more easily displaced under many conditions than are standard arylsulfonate leaving groups such as the toxyl group. The chelating moiety also favors certain cations depending on the identity of the moiety thereby enhancing the reaction rate with nucleophilic salts containing the preferred cation. Use of the inventive leaving groups results in improved yields, decreased reaction times and improved product purity.

Nucleophile assisting leaving groups

This application relates to a compound of formula (I) (or a pharmaceutically acceptable salt of the compound or prodrug thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa and/or thrombin, as well as a process for its preparation and intermediates therefor. An example of a compound of formula (I) is (a). 

Aromatic ether derivatives useful as thrombin inhibitors

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Delray Beach, FL, United States of America

Salvatore Donato Lepore