Rhodes Technologies

Marinus Pharmaceuticals

Raymond C Glowaky

Robert J Kupper

Mingbao Zhang

David Czekai

Ping Chang

Michael David Rogers

This invention relates to novel opioid derivatives of Formula I: or a pharmaceutically acceptable salt or solvate thereof, wherein R, R, Rand Z are as defined herein in the disclosure. The invention also relates to the use of such compounds for the treatment or prevention of, for example, pain.

Opioid compounds and uses thereof

This invention relates to opioid ketal compounds of Formula (I), Formula (II), or Formula (III): or a pharmaceutically acceptable salts thereof, wherein Ris H or CH, Ris H or OH, n is 0, 1, 2 or 3, Rand Rare independently H or optionally substituted C-Calkyl, or when n is 0, then Rand Rand the carbon atoms to which they are attached together form six, or seven membered ring, which is optionally mono or disubstituted by C-Calkyl. The invention also relates to oxycodone ketal compounds of Formula (IV) or (V): or a pharmaceutically acceptable salts thereof. The invention also relates to the use of such compounds for the treatment, prevention, or amelioration of pain.

Opioid ketal compounds and uses thereof

This invention relates to opioid ketal compounds of Formula (I), Formula (II), or Formula (III): or a pharmaceutically acceptable salts thereof, wherein Ris H or CH, Ris H or OH, n is 0, 1, 2 or 3, Rand Rare independently H or optionally substituted C-Calkyl, or when n is 0, then Rand Rand the carbon atoms to which they are attached together form six, or seven membered ring, which is optionally mono or disubstituted by C-Calkyl. The invention also relates to oxycodone ketal compounds of Formula (IV) or (V): or a pharmaceutically acceptable salts thereof. The invention also relates to the use of such compounds for the treatment, prevention, or amelioration of pain. 

This invention relates to opioid ketal compounds of Formula (I), Formula (II), or Formula (III): or a pharmaceutically acceptable salts thereof, wherein Ris H or CH, Ris H or OH, n is 0, 1, 2 or 3, Rand Rare independently or optionally substituted C-Calkyl, or when n is 0, then Rand Rand the carbon atoms to which they are attached together form six, or seven membered ring, which is optionally mono or disubstituted by C-Calkyl. The invention also relates to oxycodone ketal compounds of Formula (IV) or (V): or a pharmaceutically acceptable salts thereof. The invention also relates to the use of such compounds for the treatment, prevention, or amelioration of pain. 

The disclosure provides an injectable neurosteroid nanoparticle formulation comprising nanoparticles having a D50 of less than 2000 nm the nanoparticles comprising a neurosteroid of Formula I, where the variables R-Rand X are defined herein and at least one surface stabilizer. The surface stabilizer can be a polymeric surface stabilizer such as hydroxyethyl starch, dextran, or povidone. The injectable neurosteroid nanoparticle formulation can be an intravenous formulation. The disclosure also provides a lyophilized powder of the injectable neurosteroid nanoparticle formulation that can be reconstituted in an aqueous solution prior to administration. The disclosure provides injectable neurosteroid nanoparticle formulations and dry powders of such formulations that have been sterilized by ebeam irradiation. The disclosure provides a method of treating a patient having a seizure disorder, stroke, or traumatic brain injury, comprising administering an effective amount of the injectable neurosteroid nanoparticle formulation. The disclosure also provides combination methods in which the injectable neurosteroid nanoparticle formulation is a first active agent that is administered in combination with at least one additional active agent.

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Killingworth, CT, United States of America

Raymond C Glowaky