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JP2022518461A |
Prodrugs of opioids such as levorphanol or morphine with enhanced physical and chemical stability to withstand tampering and to make long-acting sustained release formulations, and pharmaceutically acceptable thereof. Possible salts and ...
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JP2022017604A |
To provide a morphinan derivative that has an opioid κ receptor agonist effect.The morphinan derivative is represented by general formula (I) in the figure. (In the formula, R1 to R11 each represent a hydrogen atom, a C1-6 alkyl group t...
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JP2021104932A |
To provide a manufacturing method of a morphinan derivative having a buprenorphine skeleton.A manufacturing method of compounds represented by the following general formula, according to a dealkylation reaction using a boron trifluoride ...
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JP2021070635A |
To provide a method for producing morphinan derivatives having the buprenorphine skeleton.Compounds represented by the general formula in the figure are obtained using a Diels-Alder reaction.SELECTED DRAWING: None
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JP2021502963A |
The present invention is a process for preparing a compound of formula (2), wherein the compound of formula (1), a base, and an alkylating agent R4-X are reacted in a nitrile-containing polar aprotic solvent. Provides a process that invo...
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JP6814470B2 |
To provide morphinan derivatives having an opioid κ receptor agonist activity.The present invention provides: a morphinan derivative represented by the general formula (I) in the figure, where R is selected from hydrogen and Calkyl, and...
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JP2021000097A |
To provide methods for producing opium poppy having high levels of thebaine.A method of increasing accumulation of thebaine in an opium poppy plant or plant cells thereof comprises genetically modifying the genome of the plant or plant c...
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JP2020203872A |
To provide a process for the preparation of opioid compounds such as buprenorphine, naltrexone, naloxone, nalbuphone, nalbuphine, and the like.A process for the preparation of a compound of formula (I) includes reacting a compound of for...
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JP2020536974A |
Compound of formula I (in formula, R1, R2, W, Z, and II) are prepared by demethylating the corresponding O-methyl derivatives with a boron hydride-based reagent. To. The method can be used to prepare buprenorphine. [Chemical 1]
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JP6792745B2 |
The present invention is directed to a process for the preparation of opioid compounds such as buprenorphine, naltrexone, naloxone, nalbuphone, nalbuphine, and the like.
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JP6778234B2 |
A method of providing a patient with controlled release of ketone-containing opioid using a prodrug capable, upon enzymatic activation and intramolecular cyclization, of releasing the ketone-containing opioid is disclosed. The disclosure...
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JPWO2019045006A1 |
The following general formula (I)(In the formula, R1May have a hydrogen atom, a substituent C1-6Indicates an alkyl group, etc., R2And R3Indicates the same or different hydrogen atom, hydroxy group, etc., and R4Indicates a hydrogen atom, ...
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JP6744327B2 |
The present invention includes compounds having structural formula (I), or pharmaceutically acceptable salts, solvates, and/or esters thereof. These compounds are useful for treating itch or a pruritic condition. The present invention al...
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JP6726194B2 |
An improved method for the preparation of the low ABUK oxymorphone hydrochloride is provided. The oxymorphone hydrochloride is produced by hydrogenating a starting material comprising oxymorphone base and 14-hydroxymorphinone in a mixtur...
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JP6713523B2 |
The present invention relates to nalmefene for use in the treatment of anxiety disorders. The present invention further relates to nalmefene for use in the treatment of patients with alcohol dependence who have a co-morbid anxiety disord...
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JP2020079263A |
To provide new forms of (R)-N-methylnaltrexone, and compositions thereof, useful as a peripheral μ opioid receptor antagonist.There is provided a compound 1 in the B form represented by following formula, in which the compound has one o...
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JP2020073598A |
To provide a process for preparing an opioid compound such as buprenorphine, naltrexone, naloxone, nalbuphon, and nalbuphine.In a process for preparing a compound represented by formula (II), a compound represented by formula (IX) is rea...
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JP6660399B2 |
The present disclosure provides acetate salts of buprenorphine, and its anhydrates, solvates, hydrates, and crystalline forms thereof, where the acetate salts of buprenorphine are essentially free of impurities. The disclosure further pr...
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JP2020033359A |
To provide buprenorphine containing acceptable levels of impurities.The present disclosure provides acetate salts of buprenorphine, and its anhydrates, solvates, hydrates and crystalline forms thereof. The present disclosure further prov...
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JP2019199481A |
To provide constructs such that hydrolysis of the construct by a specified gastrointestinal enzyme directly or indirectly releases an opioid when taken orally as prescribed.The invention provides constructs such that hydrolysis of the co...
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JP6591759B2 |
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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JP6591944B2 |
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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JP6545785B2 |
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JP6503392B2 |
The present invention relates to a process for preparing 14-hydroxycodeinone from a thebaine composition.
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JP6491653B2 |
The present invention relates to new nalmefene salts which salts fall within at least one of the two following categories: non-hydrate forming salts and non-solvate forming salts. In particular, the invention relates to the hydrogen adip...
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JP6484618B2 |
The present invention provides a process for preparing a saturated 6,14-dihydroxy morphinan. The process comprises contacting an unsaturated 6-O-hydrocarbyl morphinan with hydrogen peroxide and an organic acid to form an unsaturated 6-ke...
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JP6462877B2 |
The presently described technology provides compositions comprising aryl carboxylic acids and, for example NSAIDs, chemically conjugated to oxymorphone (4,5-α-epoxy-3,14-dihydroxy-17-methylmorphinan-6-one) to form novel prodrugs/composi...
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JP6453380B2 |
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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JP2018184462A |
To provide a process for preparing an oxycodone hydrochloride composition having a reduced amount of 14-hydroxycodeinone.The process comprises the steps of hydrogenating an oxycodone hydrochloride composition having at least 100 ppm 14-h...
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JP2018534269A |
The present invention provides compositions and methods for treating or preventing pain. The present invention provides constructs that, when taken orally as prescribed, hydrolyze the constructs by designated gastrointestinal enzymes to ...
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JP6400848B2 |
The presently described technology provides compositions comprising aryl carboxylic acids and, for example NSAIDs, chemically conjugated to oxycodone (4,5-α-epoxy-14-hydroxy-17-methylmorphinan-6-one) to form novel prodrugs/compositions ...
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JP6389252B2 |
The present invention provides processes for preparing normorphinans from N-substituted morphinans. In particular, the invention provides methods for removing the N-substituent from the N-substituted morphinan to from a normorphinan carb...
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JP6384964B2 |
Solid forms of certain opioid agonists are provided herein. Methods of preparing the solid forms, methods of using the solid forms, and pharmaceutical compositions comprising the solid forms are also provided herein.
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JP2018123150A |
To provide solid forms of receptor antagonist (R)-N-methylnaltrexone useful as a peripheral μ opioid.The present invention provides a compound 1 in the B form, which is in the (R) configuration with respect to the nitrogen.SELECTED DRAW...
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JP2018111718A |
To provide a solid salt of α-6-mPEG-O- hydroxycodone as opioid agonists and uses thereof.Solid forms of certain opioid agonists are provided herein. Methods of preparing the solid forms, methods of using the solid forms, and pharmaceuti...
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JP6317755B2 |
The present invention is directed to Buprenorphine Analog compounds of the Formula I, Formula II, Formula III, Formula IV, and Formula V, wherein R1, R2, R3a, R3b, R15a, R15b, X, Q, G, and Y are as defined herein. Compounds of the Invent...
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JP2018048093A |
To provide a compound having peripheral, selective opioid κ receptor agonistic action.The present invention provides a morphinan derivative represented by the following formula (I) or formula (II), or a pharmacologically acceptable acid...
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JP2018039810A |
To provide a new treatment method for reducing alcohol consumption in alcohol dependence patients.Provided is a method for reducing alcohol consumption in alcohol dependent patients, including: (a) a step of identifying an alcohol depend...
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JPWO2016167318A1 |
A memory-improving agent and a memory-improving composition containing a compound that is an inverse agonist of an opioid δ receptor, a pharmaceutically acceptable salt thereof, or a solvate thereof as an active ingredient, represented ...
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JPWO2016152953A1 |
The present invention has peripheral-type selective opioid κ receptor operability and is based on side effects such as drug dependence and respiratory sedation based on opioid μ receptor operability, and central opioid κ receptor oper...
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JP6246589B2 |
The present invention relates to an improved process for producing naltrexone [17- (cyclopropylmethyl)-4,5a-epoxy-3,14-dihydroxy-morphinan-6-on
e] from noroxymorphone [4,5- a-epoxy-3,14-dihydroxy-morphinan-6-one] by alkylation with a cyc...
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JP6244035B2 |
Processes for preparing oxymorphone are provided. Said processes encompass a step which is a hydrogenation of an 14-hydroxymorphinone salt in the presence of trifluoroacetic acid and/or a glycol.
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JP6240279B2 |
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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JP6236446B2 |
Compounds and compositions for use as starting materials or intermediate materials in the preparation of opioids including, e.g., oxycodone base and/or an oxycodone salt; processes for preparing these compounds and compositions; uses of ...
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JP6236447B2 |
Compounds and compositions for use as starting materials or intermediate materials in the preparation of opioids including, e.g., oxymorphone base and/or an oxymorphone salt; processes for preparing these compounds and compositions; uses...
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JP2017193549A |
To provide 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.Provided is a process comprising: contacting a solution...
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JP2017193565A |
To provide an effective analgesic which reduces the potential for abuse or adverse side effects.The invention relates to opioid ketal compounds of Formula I, or pharmaceutically acceptable salts thereof, and the use of such compounds for...
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JP6215399B2 |
The present invention relates to an improved process for producing naltrexone [17- (cyclopropylmethyl)-4,5a-epoxy-3,14-dihydroxy-morphinan-6-on
e] from noroxymorphone [4,5- a-epoxy-3,14-dihydroxy-morphinan-6-one] by alkylation with a cyc...
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JP6203871B2 |
The present invention is directed to Buprenorphine Analog compounds of Formula I, II, III, IV or V and including various stereoisomers (such as Formula IA shown below), wherein R1, R3a, R3b, R16, R15, G, Q, X, A and Z are as defined here...
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JP6193298B2 |
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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