Mallinckrodt, Inc.

Galera Therapeutics, LLC

Galera Labs, LLC

Specgx LLC

Bobby N Trawick

David W Berberich

Gary Lee Cantrell

Peter Xianqi Wang

Subo Liao

Tao Jiang

Christopher W Grote

Dennis Patrick Riley

Urszula Slomczynska

Arati Naik

Joseph P McClurg

John Brandt

Frank William Moser

Jian Bao

Hang Sun

Todd Osiek

Joseph P Mcclurg

Mark H Owens

Joseph Mcclurg

Urszula J Slomczynska

Denis P Riley

The present invention provides (+)-morphinans comprising Toll-like receptor 9 (TLR9) antagonist activity, as well as methods for using the (+)-morphinans to treat pain. Also provided are pharmaceutical combination compositions comprising a (+)-morphinan and an opioid agonist/monoamine reuptake inhibitor, as well as methods for using the combination compositions to treat pain.

(+)-morphinans as antagonists of Toll-like receptor 9 and therapeutic uses thereof

(+)-morphinans as antagonists of toll-like receptor 9 and therapeutic uses thereof

The present invention provides (+)-morphinans comprising Toll-like receptor 9 (TLR9) antagonist activity, as well as methods for using the (+)-morphinans to treat a variety of disorders.

The invention provides methods for preparing substituted phenylalkanes. In particular, the processes comprise reacting a phenyl boronic compound with an &#x3b1;-&#x3b2; unsaturated carbonyl-containing compound via an asymmetric 1,4-addition reaction. The processes may be useful in the synthesis of tapentadol.

Process for preparing substituted phenylalkanes

A high performance liquid chromatography method to routinely and reproducibly detect and quantitate metal complexes is provided. The metal complexes used in the method of the invention can be different metal complexes, or they can be stereoisomers of the same metal complexes. The high performance liquid chromatography method of the present invention is suitable for the separation of diastereomers of the same metal complexes. Also provided is a chiral high performance liquid chromatography method to separate enantiomers of metal complexes. Superoxide dismutase mimetic compounds are also provided.

Chromatography of metal complexes

The invention generally provides processes and intermediate compounds useful for the production of sinomenine derivatives. In particular, the process may encompass synthetic routes for the production of (+)-sinomenine derivatives and their intermediates.

Sinomenine derivatives and processes for their synthesis

The present invention provides (+)-morphinanium compounds comprising substituted 6-hydroxy or 6-amine groups. The invention also provides methods for inhibiting microglial activation by administering the compounds of the invention.

(+)-6-hydroxy-morphinan or (+)-6-amino-morphinan derivatives

The present invention provides (+)-morphinanium N-oxide compounds or pharmaceutically acceptable salts thereof. The invention also provides processes for producing (+)-morphinanium N-oxides or pharmaceutically acceptable salts thereof from the corresponding tertiary N-substituted (+)-morphinan compound or pharmaceutically acceptable salt thereof.

(+)-morphinanium N-oxides and processes for their production

The present invention provides (+)-morphinanium quaternary salts. The invention also provides processes for producing (+)-morphinanium quaternary salts from tertiary N-substituted (+)-morphinan compounds.

(+)-morphinanium quaternary salts and processes for their production

The invention generally provides processes and intermediate compounds useful for the production of (+)-opiates. Non-limiting examples of (+) opiates that may be derived from one or more compounds of the invention include (+)-noroxymorphone, (+)-naltrexone, (+)-naloxone, (+)-N-cyclopropylmethylnorhydrocodone, (+)-N-cycloproylmethylnorhydromorphone, (+)-N-allylnorhydrocodone, (+)-N-allylnorhydromorphone, (+)-noroxycodone, (+)-naltrexol, (+)-naloxol, and (+)-3-O-methyl-naltrexone.

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Florissant, MO, United States of America

Bobby N Trawick