78 results about "Morphinans" patented technology

Methods for producing stabilized solid dosage form pharmaceutical compositions are provided. In particular, methods for preparing protected granules containing morphinans, and solid dosage form pharmaceutical compositions produced using the morphinan-protected granules are provided.

Methods for producing stabilized solid dosage form pharmaceutical compositions are provided. In particular, methods for preparing protected granules containing morphinans, and solid dosage form pharmaceutical compositions produced using the morphinan-protected granules are provided.

The invention provides processes for the preparation of morphinans having a tertiary amine. In particular, the present invention provides processes for the formation of tertiary amine alkaloids by direct N-alkylation of secondary amine alkaloids, the processes co-mediated by an alkylating agent and a protic solvent or a mixture of a protic solvent and an aprotic solvent.

The present invention provides a synthetic process for the N-demethylation of N-methyl morphinans. In particular, the invention provides improved synthetic methods for the preparation of N-demethylated morphinan compounds that may be employed as starting materials, for example, commonly available N-methyl opiates such as oripavine and thebaine, and C(3)-protected hydroxy derivatives of oripavine.

The application is directed to compounds of Formula (I) and pharmaceutically acceptable salts and solvates thereof, wherein R¹, R², Y, Z, and G are defined as set forth in the specification. The invention is also directed to use of compounds of Formula (I), and pharmaceutically acceptable salts and solvates thereof, to treat disorders responsive to the modulation of one or more opioid receptors, or as synthetic intermediates. Certain compounds of the present invention are especially useful for treating pain.

The application is directed to compounds of Formula I′-A

especially to compounds of Formula I-A

and pharmaceutically acceptable salts and solvates thereof, wherein R^1a-R^5a, Y, Z are defined as set forth in the specification. The invention is also directed to use of compounds of Formula I′-A, and especially compounds of Formula I-A, to treat disorders responsive to the modulation of one or more opioid receptors, or as synthetic intermediates. Certain compounds of the present invention are especially useful for treating pain.

The present invention is directed to processes for the synthesis of morphinans. In particular, a process for cyclizing a β,γ-bicyclic ketone compound to form a nordihydrothebainone product using the Grewe cyclization reaction is improved by forming a reaction mixture comprising a β,γ-bicyclic ketone compound, a cyclizing acid and a water scavenging cyclization additive. In one embodiment, the Grewe transformation occurs in the presence of an acid anhydride as the cyclization additive. Further, the present invention is directed to processes for converting α,β-bicyclic ketone compounds (e.g., by-products of the Grewe cyclization reaction) to β,γ-bicyclic ketone compounds, wherein the β,γ-bicyclic ketone compounds may be recovered to further undergo Grewe cyclization and form the nordihydrothebainone product.

The present invention provides processes for the preparation of saturated 6-keto, 3-alkoxy morphinans from unsaturated 6-hydroxy, 3-hydroxy morphinans, In particular, the invention provides processes that utilize catalytic isomerization and alkylation reactions for the preparation of saturated 6-keto, 3-alkoxy morphinans.

The application is directed to compounds of Formula (I) or (IA) and pharmaceutically acceptable salts and solvates thereof, wherein R¹ R², ^R3 and G are defined as set forth in the specification. The invention is also directed to use of compounds of Formula (I) or(IA), and the pharmaceutically acceptable salts and solvates thereof, to treat disorders responsive to the modulation of one or more opioid receptors, or as synthetic intermediates. Certain compounds of the present invention are especially useful for treating pain.