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JP6181770B2 |
The application is directed to a process for increasing the proportion of 7β-epimer in an 7α/7β-epimer mixture of a 7-substituted 6α,14α-ethenomorphinan or a 7-substituted 6α,14α-ethanomorphinan, and specifically of compounds of F...
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JP2017137346A |
To provide stereoselective synthesis of R-MNTX and intermediates thereof, pharmaceutical preparations comprising R-MNTX or intermediates thereof and methods for their use.A composition comprises R-MNTX, wherein the composition is free of...
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JP2017137317A |
To provide processes for the N-dealkylation of tertiary amines and transition metal catalysts to prepare tertiary N-allyl amine derivatives and secondary amine derivatives thereof.The present invention provides a method for producing a c...
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JP6174662B2 |
A solid oral controlled-release dosage form of hydrocodone is disclosed, the dosage form comprising an analgesically effective amount of hydrocodone or a pharmaceutically acceptable salt thereof, and controlled release material.
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JP6165592B2 |
The present invention relates to opioid and opioid-like compounds, and pharmaceutical formulations containing the same and methods of use thereof. Uses of the present invention include, but are not limited to, use for the prevention and ...
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JP6161801B2 |
This invention relates to opioid ketal compounds of Formula (I), Formula (II), or Formula (III):or a pharmaceutically acceptable salts thereof, wherein R1 is H or CH3, R2 is H or OH, n is 0, 1, 2 or 3, R3 and R4 are independently H or op...
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JP6151307B2 |
The present invention provides a process for the preparation of a compound of formula (VI), or a salt or derivative thereof, wherein R 1 and R 2 are independently C 1-8 alkyl and * represents a stereocentre.
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JP6148182B2 |
The embodiments provide prodrug compounds of Formulae I-XVII. The present disclosure also provides compositions, and their methods of use, where the compositions comprise a prodrug compound of Formulae I-XVII that provides controlled rel...
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JP6149058B2 |
A solid oral controlled-release oral dosage form of hydrocodone is disclosed. The dosage form comprising an analgesically effective amount of hydrocodone or a pharmaceutically acceptable salt thereof, and a sufficient amount of a control...
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JP2017514845A |
The present invention relates to the process of preparing opioid compounds such as buprenorphine, naltrexone, naloxone, nalbuphine, nalbuphine and the like.
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JP6127040B2 |
The present disclosure provides processes for the N-dealkylation of tertiary amines and the use of transition metal catalysts to prepare tertiary N-allyl amine derivatives and secondary amine derivatives thereof. The tertiary amines can ...
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JP6121988B2 |
The present application is directed to an efficient conversion of C-14 hydroxylated morphine alkaloids to various morphine analogs, such as naltrexone, naloxone and nalbuphone. One feature of this process is an intramolecular functional ...
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JP6117780B2 |
The invention provides orvinol and thevinol compounds useful for the treatment of drug and alcohol abuse, the compounds being particularly useful for the prevention of relapse in recovering addicts.
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JP6086925B2 |
The present invention relates to an improved process for recovery of nalmefene hydrochloride [17-(cyclopropylmethyl)-4,5- alpha-epoxy-6-methylenemorphinan-3,14-diol hydrochloride] from an aqueous composition containing nalmefene and cert...
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JP2017502991A |
A method for preparing oxycodone is provided. The method comprises the step of hydrogenating the 14-hydroxycodeinone salt in the presence of trifluoroacetic acid and / or glycol.
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JP6055183B2 |
The present invention relates to the Nalmefene hydrochloride dihydrate, methods of manufacturing Nalmefene hydrochloride dihydrate, a pharmaceutical composition comprising Nalmefene hydrochloride dihydrate and a method of treatment compr...
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JP2016210815A |
To provide an improved method for forming a corresponding quaternary morphinan alkaloid derivative by carrying out N-alkylation of tertiary morphinan alkaloid base.The present invention is directed to a method for preparing a quaternary ...
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JP6042387B2 |
A solid oral controlled-release dosage form of hydrocodone is disclosed, the dosage form comprising an analgesically effective amount of hydrocodone or a pharmaceutically acceptable salt thereof, and controlled release material.
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JP6034789B2 |
Naloxol-polyethylene glycol conjugates of the formula: are provided in oxalate or phoshate salt forms including crystalline forms. To achieve a central analgesic effect, the conjugates will be administered an opioid agonist.
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JP2016196490A |
To provide new forms of (R)-N-methylnaltrexone, and compositions thereof, useful as a peripheral μ opioid receptor antagonist.The present invention provides a composition comprising a mixture of Forms A and C of a compound represented b...
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JP6027315B2 |
The invention generally provides processes and intermediate compounds useful for the production of normorphinans and derivatives of normorphinans.
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JP2016534991A |
The one pot method for preparing an N* Alkyl morphinane *6* oar from morphinane *6* ON is indicated on these specifications. It is characterized by the especially method comprising the following. It is a boron system reducing agent about...
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JP6013345B2 |
in which R4 is chosen from substituted phenyl, optionally substituted naphthylene, optionally substituted anthracene and optionally substituted aromatic heterocycle, are useful as analgesics.
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JP6009764B2 |
The present invention relates to ester prodrugs of nalmefene of formula (I), pharmaceutical compositions comprising these compounds, chemical processes for preparing these compounds and their use in the treatment of substance abuse disor...
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JP5988272B2 |
A method of preparing oxycodone includes forming 14-hydroxycodeine by reduction of 14-hydroxycodeinone and rearrangement of the 14-hydroxycodeine to form the oxycodone. During the reduction step, the ketone group of an undesirable contam...
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JP5982063B2 |
The application is directed to compounds of Formula I and pharmaceutically acceptable salts, prodrugs, and solvates thereof, wherein G, R2-R5, and are defined as set forth in the specification. The invention is also directed to use of co...
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JP5977240B2 |
The present invention is directed to Buprenorphine Analog compounds of the Formula (I), Formula (IA) or Formula (IB) shown below, wherein R1, R2, R8, R3a, R 3b, G, X, Z and Y are as defined herein. Compounds of the Invention are useful f...
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JP5957180B2 |
An improved process for the N-alkylation of tertiary morphinan alkaloid bases to form the corresponding quaternary morphinan alkaloid derivatives.
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JP5946921B2 |
The present invention is directed to Buprenorphine Analog compounds of the Formula (I), Formula (IA) or Formula (IB) shown below, wherein R1, R1a, R2, R8, R3a, R3b, G, X, Z, Y, and A® are as defined herein. Compounds of the Invention ar...
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JP2016519161A |
It is related with the method of treating the illness or state including that this application medicates Mol Juan, the similar object of morphinane, its constituent, and a necessity medical treatment subject with the effective amount of ...
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JP5941038B2 |
Described herein are opioid prodrugs, methods of making opioid agonist-antagonist prodrugs, compositions comprising opioid agonist-antagonist prodrugs, abuse-resistant formulations and dosage forms of opioid agonist-antagonist prodrugs, ...
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JP2016102115A |
To provide buprenorphine analogs having activity as opioid receptor agonists and/or antagonists.This invention relates to compositions represented by formula (I). The compounds of the Invention are useful for treating pain, constipation,...
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JP2016084364A |
To provide processes and intermediate compounds useful for the production of normorphinans and derivatives of normorphinans.The invention generally provides processes and intermediate compounds useful for the production of normorphinans ...
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JP2016041698A |
To provide a novel pain therapeutic prodrug for preventing misuse, abuse or overdose of ketone-containing opioid.The present invention relates to a prodrug of oxycodone being ketone-containing opioid, represented by a compound of the fol...
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JP5875748B2 |
An improved process for the N-alkylation of tertiary morphinan alkaloid bases to form the corresponding quaternary morphinan alkaloid derivatives.
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JP5864417B2 |
The present invention provides (+)-morphinans comprising Toll-like receptor 9 (TLR9) antagonist activity, as well as a method for identifying (+)-morphinans that may be therapeutically effective by determining whether the (+)-morphinan i...
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JP5834052B2 |
A solid oral controlled-release oral dosage form of hydrocodone is disclosed. The dosage form comprising an analgesically effective amount of hydrocodone or a pharmaceutically acceptable salt thereof, and a sufficient amount of a control...
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JP5827123B2 |
The invention provides opioid agonists, in particular morphine and codeine, covalently bound to a water-soluble oligomer, namely a polyethylene glycol (PEG) oligomer having reduced potential for substance abuse and uses thereof. The comp...
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JP5824448B2 |
The present application describes processes for the synthesis of morphinane and morphinone compounds, useful as pharmaceutical agents. Also included are novel intermediates useful in the preparation of these compounds. The process compri...
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JP5818219B2 |
The solid preparation which improved the dissolution profile and the stability of the 6,7-unsaturation-7-carbamoyl morphinan derivative is provided. When 6,7-unsaturation-7-carbamoyl morphinan derivative, croscarmellose sodium and ferric...
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JP5818851B2 |
The present invention relates to compounds of Formula I or II, or pharmaceutically acceptable salts, esters, or prodrugs thereof: which relates to morphinan compounds useful as μ, δ, and/or κ receptor opioid compounds and pharmaceutic...
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JP2015193658A |
To provide processes for the demethylation of an N-methyl morphinan comprising a ketone functional group.The present invention provides processes for the demethylation of an N-methyl morphinan comprising a ketone functional group. In par...
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JP2015187134A |
To provide an oxycodone hydrochloride composition that contains a reduced amount of 14-hydroxycodeinone compared to compositions known in the art.An oral pharmaceutical preparation contains oxycodone of 5-320 mg and 14-hydroxycodeinone o...
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JP2015180698A |
To provide chemically modified opioid agonists that possess advantages over opioid agonists lacking the chemical modification.Provided is a conjugate comprising an opioid agonist, hydroxycodone (oxycodone), and hydrocodone (dihydrocodein...
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JP2015180661A |
To provide a process for reductive alkylation of normorphinans.There is provided a process for a process of alkylation of a normorphinan compound by a carboxaldehyde in the presence of a reducing agent to form an N-alkylated morphinan re...
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JP5794980B2 |
Method for producing nalmefene hydrochloride from naltrexone, which method is particular well adapted for large-scale industrial application, and has been found to be efficient, to give a high yield and to afford highly pure nalmefene hy...
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JP5787764B2 |
The present invention provides a process for the preparation of a compound of formula (VI), or a salt or derivative thereof, wherein R 1 and R 2 are independently C 1-8 alkyl and * represents a stereocentre.
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JP2015166331A |
To provide crystals of nalfurafine whose purity is increased to such a level that there is no problem in using the same as a raw material of nalfurafine hydrochloride.Provided are: crystals of 17-cyclopropylmethyl-3,14β-dihydroxy-4,5α-...
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JP5784507B2 |
The present invention provides (+)-morphinanium quaternary salts. The invention also provides processes for producing (+)-morphinanium quaternary salts from tertiary N-substituted (+)-morphinan compounds.
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JP5778042B2 |
The invention provides a process for the N-alkylation of normorphinan compounds to produce N-alkylated morphinan compounds. In particular, the process relates to the alkylation of a normorphinan compound by a carboxaldehyde in the presen...
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