13 results about "Morphinan" patented technology

The present invention relates to a morphinan-type compound, a preparation method therefor, a composition thereof and the use thereof. Specifically disclosed is a compound I or a pharmaceutically acceptable salt thereof. The morphinan-type compound of the present invention has one or more of the following effect advantages: (1) a relatively high binding affinity for an opioid receptor; (2) a significant agonistic effect on KOR and MOR; (3) good selectivity for a κ receptor; and (4) a good therapeutic effect on inflammatory pain (for example, rapid onset of action or significant analgesic effect).

Disclosed herein are methods that may be used for the synthesis of benzylisoquinoline alkaloids (“BIAs”) such as alkaloid morphinan. The methods disclosed can be used to produce thebaine, oripavine, codeine, morphine, oxycodone, hydrocodone, oxymorphone, hydromorphone, naltrexone, naloxone, hydroxycodeinone, neopinone, and / or buprenorphine. Compositions and organisms useful for the synthesis of BIAs, including thebaine synthesis polypeptides, purine permeases, and polynucleotides encoding the same, are provided.

This disclosure relates to morphinan compounds and derivatives thereof, pharmaceutically acceptable salts, solvates and hydrates thereof, and compositions comprising the compounds, and use of such compounds and compositions in methods of treating diseases and conditions.

The present invention generally relates to processes for preparing highly pure morphinan-6-one products. The processes involve reducing the concentration of alpha, beta unsaturated ketone compounds present as impurities in morphinan 6 one products or reaction mixtures including morphinan 6 one compounds by treatment with a sulfur-containing compound.

A method of producing promorphinan, morphinan, nal-opioid, and nor-opioid alkaloid products through the increased conversion of a promorphinan alkaloid to a morphinan alkaloid. The method comprises contacting the promorphinan alkaloid with at least one enzyme. Contacting the promorphinan alkaloid with the at least one enzyme converts the promorphinan alkaloid to a morphinan alkaloid.

The invention provides a preparation method of a morphinan derivative and a salt thereof, and particularly relates to a preparation method of a compound A10 and an intermediate A09 thereof. The refining method of A09 provided by the invention is simple in post-treatment and relatively high in product purity and yield, the provided preparation method of the compound I adopts a continuous feeding reaction to convert the compound A08 into A09 and then directly performs a salt forming reaction, the method is simple to operate, the yield and the purity are simultaneously improved, the used solvent is high in safety, and the method is suitable for industrial application.

Disclosed herein are methods that may be used for the synthesis of benzylisoquinoline alkaloids (“BIAs”) such as alkaloid morphinan. The methods disclosed can be used to produce thebaine, oripavine, codeine, morphine, oxycodone, hydrocodone, oxymorphone, hydromorphone, naltrexone, naloxone, hydroxycodeinone, neopinone, and / or buprenorphine. Compositions and organisms useful for the synthesis of BIAs, including thebaine synthesis polypeptides, purine permeases, and polynucleotides encoding the same, are provided.

A method of producing promorphinan, morphinan, nal-opioid, and nor-opioid alkaloid products through the increased conversion of a promorphinan alkaloid to a morphinan alkaloid. The method comprises contacting the promorphinan alkaloid with at least one enzyme. Contacting the promorphinan alkaloid with the at least one enzyme converts the promorphinan alkaloid to a Morphinan alkaloid.

The invention relates to a morphinan type compound as well as a preparation method, a composition and application thereof. Specifically disclosed is a compound I or a pharmaceutically acceptable salt thereof. The morphinan type compound provided by the invention has one or more of the following effects and advantages: (1) the morphinan type compound is relatively high in binding affinity with an opioid receptor; (2) the compound has an obvious agonistic effect on KOR and MOR; (3) the selectivity to a kappa receptor is good; and (4) the ointment has a good treatment effect on inflammatory pain (for example, the ointment takes effect quickly or has an obvious pain effect).

The invention relates to a morphinan compound as well as a preparation method and application thereof, in particular to a morphinan compound as shown in a formula (I), and an isomer, a racemate, a pharmaceutically acceptable salt, a solvate or an isotope label of the morphinan compound. The invention also relates to a preparation method of the compound and a pharmaceutical composition containing the compound and application of the compound in preparation of drugs for preventing and / or treating central nervous system diseases. Compared with a compound disclosed in the prior art, the compound provided by the invention has the advantages of multi-target effect, lower drug dose, less toxic and side effects, better safety and tolerance and the like, is good in comprehensive druggability, and has a good clinical application prospect.

To provide a pharmaceutical product useful for the treatment or prevention of opioid δ receptor-related diseases. [Solution] The present invention relates to a pharmaceutical composition comprising a morphinan derivative that exerts opioid δ receptor agonist activity. By administering the pharmaceutical composition provided by the present invention, opioid δ receptor-related diseases (e.g., headaches) may be treated or prevented.

The present invention relates to morphinan compounds, a preparation method therefor, and the use thereof, and specifically relates to morphinan compounds represented by formula (I) and isomers, racemates, pharmaceutically acceptable salts, solvates or isotope-labelled substances thereof, a preparation method therefor, a pharmaceutical composition comprising same, and the use of same in preparing drugs for preventing and / or treating central nervous system diseases. Compared with compounds disclosed in the prior art, the compounds of the present invention have the advantages of acting on multiple targets, lower effective dose, fewer toxic and side effects, better safety and tolerance, etc., and have good overall druggability and thus possess good prospects in clinical application.

The invention provides a morphinan derivative in a crystal form and a preparation method thereof, and particularly relates to a crystal form I of a compound shown in a formula I and a preparation method thereof. The crystal form I provided by the invention has the advantages of good stability and low hygroscopicity, and is especially suitable for tablet preparation. On the other hand, the invention also provides a purification method of the compound, and the method has one or more advantages that the purification process is simple, the yield is high, the purity of the prepared crystal form is high, the safety of the used solvent is high, and the method is suitable for industrial application.