Abstract: The embodiments provide prodrug compounds of Formulae I-XV. The present disclosure also provides compositions, and their methods of use, where the compositions comprise a prodrug compound of Formulae I-XV that provides controlled release of an opioid. Such compositions can optionally provide a trypsin inhibitor that interacts with the enzyme that mediates the controlled release of an opioid from the prodrug so as to attenuate enzymatic cleavage of the prodrug.
Abstract: The invention relates to a method or process for the chemical manufacture of depsipeptides of the formula I, wherein the symbols have the meaning defined in the description, to new intermediates and their manufacture, as well as related invention embodiments.
Type:
Grant
Filed:
April 18, 2012
Date of Patent:
December 24, 2013
Assignee:
Novartis AG
Inventors:
Murat Acemoglu, Heribert Hellstern, Felix Kollmer, John Lopez, Robert Schreiber, Christian Sprecher, Hans Stettler