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JP4903344B2 |
The present invention provides a method for preparing microparticles having a selected polymer molecular weight. The hold time and temperature of a solution containing a nucleophilic compound and a polymer having a starting molecular wei...
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JP4895220B2 |
The present invention relates to compounds that are useful for treating cellular proliferative diseases, for treating disorders mediated, at least in part, by KSP, and for inhibiting KSP. The invention also related to pharmaceutical comp...
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JP2012505843A |
Administration scheme of an analgesically active polar metabolite of an opioid or the salt thereof for the manufacture of a medicament for the treatment of pain after medical operation, whereas the medicament is administered at least onc...
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JP4890710B2 |
Compounds represented by the formulae: wherein each of Y, X and R individually is selected from the group consisting of hydrogen, hydroxy, halo, CF3, NO2, CN, NH2, COR1 and CO2R2 wherein R1 is selected from the group consisting of alkyl,...
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JP4886953B2 |
A method for the preparation of a ketone from a narcotic alkaloid having an allyl alcohol moiety is disclosed. The method includes mixing the narcotic alkaloid with an acid in the presence of a catalyst wherein the method is carried out ...
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JP4882744B2 |
A novel antipruritic useful for the treatment of pruritus accompanying various diseases is disclosed. The antipruritic comprises a specific morphinan derivative having a nitrogen-containing cyclic group or the pharmaceutically acceptable...
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JP4879740B2 |
This invention relates to intermediates useful in the preparation of opiate alkaloids, particularly morphinane compounds. The invention also relates to processes for preparing such intermediates and to processes which utilise such interm...
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JP4874523B2 |
This invention relates to a tamper-resistant transdermal-delivery device comprising an opioid, or a pharmaceutically acceptable salt thereof, and an acyl opioid antagonist, or a pharmaceutically acceptable salt thereof. The transdermal-d...
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JP4878732B2 |
The present invention provides methods for altering controlled substances in a manner that decreases their potential for abuse. The novel compounds may be combined in tablets with suitable excipients or formulated in solution for oral de...
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JP4867123B2 |
The present invention relates to a therapeutic agent for neuropathic pain containing, as an active ingredient, a compound represented by general formula (I) or a pharmacologically acceptable acid addition salt thereof: (wherein R<1>, R<2...
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JP4814486B2 |
A pharmaceutically active inventive compound comprises two independently active analgesic moieties covalently conjoined through a physiologically labile linker. A preferred embodiment comprises an opioid, such as morphine, covalently lin...
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JP4806190B2 |
This invention relates to N-substituted hydromorphones of Formula I or a pharmaceutically acceptable salt thereof. These compounds act as µ opioid receptor agonists. The invention is also directed to the use of compounds of Formula I fo...
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JP4806507B2 |
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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JP2011201906A |
To provide an improved analgesic oxymorphone hydrochloride.The invention relates to a pharmaceutical preparation which comprises oxymorphone hydrochloride containing less than 10 ppm of a 14-hydroxymorphinone. This oxymorphone hydrochlor...
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JP4786748B2 |
Improved analgesic oxymorphone hydrochloride contains less than 10 ppm of alpha, beta unsaturated ketones and pharmaceutical preparations comprising such oxymorphone hydrochloride. The oxymorphone hydrochloride is produced by reducing a ...
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JP2011524902A |
The disclosure describes morphinan compounds and methods for their synthesis. Preferred methods according to the disclosure allow for large-scale preparation of diastereomerically enriched morphinans. Preferred methods according to the d...
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JP2011524376A |
The present invention relates to a process for the preparation of an N-demethyl morphinane or a protected form thereof. In one form the preparation of the N-demethyl morphinane or a protected form thereof involves the N-demethylation of ...
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JP4763194B2 |
Compounds represented by the formula: wherein each of Y, X and R individually is H, OH, alkyl, alkoxy, aryl, halo, CF3 and NO2, provided that at least one of Y, X and R is other than H; and pharmaceutically acceptable salts thereof are p...
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JP4737583B2 |
The invention relates to pharmaceutical salts comprised of a pharmaceutical active substance, particularly N,N-dimethylaminopropylphenol compounds or tradamol, and of at least one sugar substitute such as saccharin, cyclamate or acesulfa...
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JP4706636B2 |
An analgesic which may be applied to wide variety of pain from various causes is disclosed. The analgesic comprises as an effective ingredient a specific morphinan derivative having a nitrogen containing heterocyclic group, such as comop...
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JP2011516464A |
The present invention relates to an improved process for preparing morphinane analogues of formula 1 wherein the substituents R1, R2, R2a, R3, R4, R5 and Y have the meanings as defined in the specifications.
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JP2011516464T |
The present invention relates to the preparing method with which the morphinane similar object of the formula (1) was improved, and is inside of a formula, and substitution machine R.1R2R2aR3R4R5And Y has the meaning defined in the speci...
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JP2011079843A |
To provide pharmaceutical salts containing a pharmaceutically-active compound and at least one sugar substitute, and a drug containing these salts.The present invention relates to the pharmaceutical salts of a (1RS, 3RS, 6RS)-6-dimethyla...
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JP2011512360A |
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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JP2011074018A |
To provide a fibromyalgia therapeutic agent or prophylactic agent which brings about a remarkable therapeutic effect or prophylactic effect.The fibromyalgia therapeutic agent or prophylactic agent has a compound having a specific morphin...
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JP4656081B2 |
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JP2011506605A |
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 emp...
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JP2011042681A |
To provide N-substituted hydromorphones or pharmaceutically acceptable salts thereof.The N-substituted hydromorphones represented by formula I or pharmaceutically acceptable salts thereof are provided (wherein, R indicates a 1C-6C alkyl ...
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JP2011506601A |
The invention generally provides processes for the production of buprenophine and derivatives of buprenorphine. In particular, the process may encompass synthetic routes for the production of buprenorphine or derivatives of buprenorphine...
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JP4624497B2 |
PCT No. PCT/EP97/00711 Sec. 371 Date Oct. 28, 1999 Sec. 102(e) Date Oct. 28, 1999 PCT Filed Feb. 15, 1997 PCT Pub. No. WO97/31918 PCT Pub. Date Sep. 4, 1997The present invention relates to morphine and diamorphine salts of anionic non-na...
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JP2011503040A |
Preparation of morphine compounds with low content of ~a-~b unsaturated compounds, comprises: contacting crude morphine compound with a base in conditions allowing Michael addition reaction on the ~a-~b unsaturated compounds; separating ...
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JP2010533719A |
The present invention is directed to the reduction of an N-imine moiety or a hemiaminal moiety of a morphinan in the presence of a ruthenium, rhodium, or iridium asymmetric catalyst and a hydrogen source.
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JP4559730B2 |
The present invention relates to process for the preparation of a 14-hydroxynormorphinone derivative of formula IV comprising reacting the compound of formula III, with a cobalt (II) oxidant in the presence of a mild base and air or oxyg...
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JP2010531813A |
The present invention provides methods for the conversion of thebaine to a morphine derivative, such as hydrocodone. Novel ketal intermediates of the conversion are provided. A one-pot procedure for the conversion comprises treating theb...
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JP4532109B2 |
The present invention relates to oripavine derivatives of formula (I), wherein R<1> is hydrogen or methyl, R<2> is methyl, cyclopropyl methyl, cyclobutyl methyl or allyl, R<3> is thiophenyl ethyl or cycloalkyl methyl where the cycloalkyl...
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JP2010155869A |
To provide a compound and composition stable before exposing to a biological fluid such as plasma, etc., relatively insoluble in the biological fluid such as plasma, etc., and returning to at least one kind of analgesic compounds or comp...
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JP2010522756A |
The present invention provides a new form of (R)-N-methylnaltrexone bromide, and compositions thereof, useful as a peripheral mu opiod receptor antagonist.
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JP2010522189A |
An improved method for the preparation of oxymorphone from oripavine is provided. Oripavine is oxidized to form 14-hydroxymorphinone after which the oxidation reaction is quenched to prevent the formation of 1-1′-dimer side products. T...
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JP2010520185A |
There is provided a composition for the treatment of pain in human patients wherein said composition comprises buprenorphine to naloxone in a ratio by weight of from 2.1:1 to 8:1, the amount of buprenorphine and naloxone being suitable t...
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JP2010111656A |
To provide a method for efficiently producing a thebaine derivative which is important compound as an intermediate for synthesizing pharmaceuticals.The method for producing the thebaine derivative (I) is provided, including the following...
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JP4453254B2 |
A therapeutic drug for psychoneurotic disorders, which is useful for therapies of psychoneurotic disorders, especially restless legs syndrome is disclosed. The therapeutic drug for psychoneurotic disorders according to the present invent...
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JP2010511725A |
The present invention is directed to a process for using n-butanol to prepare an oxycodone base compositions having reduced levels of impurities such as 14-hydroxycodeinone and DHDHC.
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JP2010511726A |
The present invention is directed to processes for preparing oxycodone base and oxycodone hydrochloride compositions having less than 10 ppm of 14-hydroxycodeinone.
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JP2010510318A |
Methods for the synthesis of 4,5-epoxy-morphinaniums using dimethyl formamide and resolution of the diastereomeric products by means of HPLC.
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JP2010510326A |
Novel N-oxides of 4,5-epoxy-morphinanium analogs are disclosed. Pharmaceutical compositions containing the N-oxides of 4,5-epoxy-morphinanium analogs and methods of their pharmaceutical uses are also disclosed. The compounds disclosed ar...
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JP2010510328A |
Novel (R)-N-stereoisomers of 7,8-saturated-4,5-epoxy-morphinanium analogs are disclosed. Pharmaceutical compositions containing the (R)-N-stereoisomers of 7,8-saturated-4,5-epoxy-morphinanium analogs and methods for their pharmaceutical ...
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JP2010510325A |
Novel (S)-N-stereoisomers of 7,8-saturated-4,5-epoxy-morphinanium analogs are disclosed. Pharmaceutical compositions containing the (S)-N-stereoisomers of 7,8-saturated-4,5-epoxy-morphinanium analogs and methods for their pharmaceutical ...
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JP2010510329A |
Novel (R)-N-stereoisomers of 7,8-saturated-4,5-epoxy-morphinanium analogs are disclosed. Pharmaceutical compositions containing the (R)-N-stereoisomers of 7,8-saturated-4,5-epoxy-morphinanium analogs and methods for their pharmaceutical ...
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JP2010024141A |
To provide a useful compound for the efficient production method of morphine.This compound is expressed by general formula (I), (II), or (III) [wherein R1 is a 1-6C alkyl; R2 is an amino-protecting group without substantially being elimi...
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JP2010501011A |
The present disclosure is directed to modulators of opiate- and/or NMDA receptors and pharmaceutically acceptable salts and prodrugs thereof, the chemical synthesis thereof, and the use of such compounds for the treatment and/or manageme...
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