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JP2015129167A |
To provide a phenolic opioid prodrug that provides enzymatically-controlled release of a phenolic opioid, and to provide an enzyme inhibitor that interacts with the enzyme that mediates the enzymatically-controlled release of the phenoli...
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JP2015129190A |
To provide stereoselective synthesis of R-MNTX and intermediates thereof, pharmaceutical preparations comprising R-MNTX and intermediates thereof and methods for their use.A composition comprises R-MNTX, and is free of HPLC detectable S-...
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JP5736040B2 |
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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JP2015515986A |
To provide a heterocyclic condensed morphinan, its use and a method for producing the same. The present disclosure is a method for producing the following disclosed compound, a pharmaceutically acceptable salt thereof, a dehydrohydride t...
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JP5728084B2 |
The present invention relates to a process for the synthesis of a compound of formula I:
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JP2015096554A |
To provide controlled release of phenolic opioids.Provided is a method of providing a patient with controlled release of a phenolic opioid using a prodrug capable, upon enzymatic activation, of releasing the phenolic opioid through intra...
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JP5697215B2 |
The present invention provides processes for the stereoselective synthesis of 6-alpha-amino N-substituted morphinans. In particular, the invention provides processes for the reductive amination of 6-keto N-substituted morphinans by catal...
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JP5695296B2 |
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 on...
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JP2015057448A |
To provide synthesis of 6-α-amino N-substituted morphinan by catalytic hydrogen transfer.There is provided a process for the stereoselective synthesis of 6-α-amino N-substituted morphinan. Particularly, there is provided a process for ...
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JP2015052019A |
To provide an improved method for producing a corresponding quaternary morphinan derivative by N-alkylation of a tertiary morphinan alkaloid base.There is provided a method for preparing a quaternary derivative of a tertiary N substitute...
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JP2015506952A |
Oxazolidine derived from the reaction of Burgess reagent with oxymorphone, temporarily protected by O-3 and C-6, reacts with Grignard reagent or other suitable metal or organometallic reagent, eg, N- Allyl, N-methylcyclopropyl, and N-met...
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JP5680069B2 |
The present invention provides processes for the stereoselective synthesis of 6-alpha-amino morphinans. In particular, the invention provides processes for the reductive amination of 6-keto normorphinans by catalytic transfer hydrogenation.
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JP5661062B2 |
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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JP2015500245A |
The present invention relates to an improved process for preparing lactam morphinan. This process generally proceeds with high yield and good selectivity by converting keto-morphinan to 7-membered ring lactam morphinan using a hydroxyami...
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JP2014240400A |
To provide compounds of new crystal forms of (R)-N-methylnaltrexone useful for reducing side effects associated with opioid therapy, and a pharmaceutical composition comprising the compound.This invention relates to compounds of B forms ...
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JP5627594B2 |
The present disclosure generally relates to a process for converting a fused, tricyclic compound to a fused, tetracyclic compound that includes a furan ring therein. More particularly, the present disclosure related to a process for prep...
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JP2014214156A |
To provide an X-form crystal of 17-cyclopropylmethyl-3,14β-dihydroxy-4,5α-epoxy-6β-[N-met
hyl-trans-3-(3-furyl) acrylamide]morphinan hydrochloride, a production method thereof, and a pharmaceutical composition.The X-form crystal of th...
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JP2014208640A |
To provide pain treatment agents and opioid and ORL1 receptor activity regulators.This invention relates to buprenorphine analog compounds represented by the following structure.
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JP2014526467A |
The invention relates to processes for the production of alkaloids without the isolation of intermediates.
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JP2014185180A |
To provide (+)-morphinanium quaternary salts and to provide processes for their production.The present invention provides (+)-morphinanium quaternary salts. The invention also provides processes for producing (+)-morphinanium quaternary ...
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JP2014169314A |
To provide a process for preparing hydrocodone.The present disclosure relates to a process for converting a fused, tricyclic compound to a fused, tetracyclic compound that includes a furan ring therein. More specifically, the present dis...
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JP5586223B2 |
A synthetic method is provided, wherein the method comprises stereoselectively reducing a ketone of a morphinone to form a reduced morphinone and optionally covalently attaching a water soluble polymer to the reduced morphinone.
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JP5587541B2 |
A process for purifying plant extracts which consist essentially of noroxymorphone compounds and which comprise, as impurities, α,β-unsaturated noroxymorphone compounds, by (a) converting the plant extract or the product of a subsequen...
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JP5587204B2 |
The invention generally provides processes and intermediate compounds useful for the production of (+) nal morphinan compounds. In particular, the process encompasses synthetic routes for the production of (+) nal morphinan compounds or ...
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JP5579076B2 |
The invention generally provides processes and intermediate compounds useful for the production of sinomenine derivatives. In particular, the process may encompass synthetic routes for the production of (+)-sinomenine derivatives and the...
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JP5581211B2 |
are disclosed. The compounds are useful for ameliorating the side effects of therapeutic opiates.
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JP2014148548A |
To provide sinomenine derivatives and a process for synthesizing the same.Sinomenine (alkaloid isolated from a root of Sinomenium acutum) was reported to have an antiinflammatory activity, an analgesic activity, a hypotensive activity an...
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JP5564943B2 |
Crystalline particles of N-(17-cyclopropylmethyl-4,5±-epoxy-3,14-dihydroxy-morphinan
-6²-yl)-phthalimide or a pharmaceutically acceptable salt thereof are disclosed. The crystalline particles have a particle diameter distribution in wh...
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JP2014139205A |
To provide a method of reducing the amount of 14-hydroxy codeinone in manufacturing oxycodone hydrochloride.There is provided a method for preparing oxycodone hydrochloride composition having less than 25 ppm of 14-hydroxy codeinone incl...
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JP5543991B2 |
The present invention relates to a process for preparing 14-hydroxycodeinone from a thebaine composition.
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JP5536730B2 |
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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JP5525524B2 |
The present invention is directed to Buprenorphine Analog compounds of the Formula I, Formula II or Formula III shown below, wherein R 1 , R 2 , R 8 , R 3 , R 3a , R 3b , X, Z and Y are as defined herein. Compounds of the Invention are u...
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JP2014077007A |
To provide a process for producing a pure normorphinan salt from a crude opioid substrate.Provided is a method for producing a pure normorphinan salt from a crude opioid substrate (wherein, each of Rs represents a hydrogen atom or a hydr...
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JP2014073964A |
To provide morphinan derivatives having opioid δ receptor agonist action.Provided are morphinan derivatives represented by the specified general formula (I) or pharmacologically acceptable acid addition salts thereof. The morphinan deri...
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JP5478506B2 |
The invention provides a process for the conversion of opioid derivatives into normorphinan compounds useful for making “nal” compound analgesics and antagonists. In particular, the process may be used for the production of pure norm...
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JP2014065719A |
To provide compounds useful for treatment, prevention, amelioration, delay or reduction of severity and/or incidence of side effects associated with opioid administration.Compounds of the formula I-a or I-b are useful as peripheral μ op...
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JP2014062069A |
To provide a method of producing a naltrexamine derivative which retains high yield and high stereoselectivity without the need to use sodium cyanoborohydride or a borane-pyridine complex as a reducing agent nor the need to use an alcoho...
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JP5462156B2 |
The present invention provides a method for the N-demethylation and/or N-acylation of an N-methylated heterocycle such as morphine alkaloids or tropane alkaloids. The method comprises reacting the heterocycle with an acylating agent in t...
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JP5461386B2 |
The present invention provides a compound of formula I: wherein R 1 , R 2 , R 2' and X - are as defined and described herein, and compositions thereof, useful as peripheral mu opioid receptor antagonists.
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JP5460771B2 |
Novel methods for the treatment and/or prevention of ileus. The methods may comprise administering to a patient an effective amount of a peripheral mu opioid antagonist compound. Preferred compounds for use in the methods include piperid...
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JP2014055179A |
To provide processes and intermediate compounds useful for production of (+)-opiates.The invention generally provides processes and intermediate compounds useful for production of (+) nal morphinan compounds. In particular, the process e...
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JP5453151B2 |
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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JP5438250B2 |
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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JP5442862B2 |
The presently described technology provides compositions comprising aryl carboxylic acids chemically conjugated to hydrocodone (morphinan-6-one, 4,5-alpha-epoxy-3-methoxy-17-methyl) to form novel prodrugs/compositions of hydrocodone, inc...
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JP5420427B2 |
The invention provides opioid agonists that are chemically modified by covalent attachment of a water-soluble oligomer (PEG). A compound of the invention, when administered by any of a number of administration routes, exhibits characteri...
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JP5415075B2 |
The present invention relates to processes for removal of Michael acceptors from certain compositions wherein the composition is treated with a thiol-containing compound under conditions sufficient to remove Michael acceptors and the res...
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JP5406288B2 |
The invention pertains to the use of opiod antagonists for the treatment of urinary retention.
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JP5378486B2 |
The present invention relates to a process for preparing 14-hydroxycodeinone from a thebaine composition.
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JP5373764B2 |
An improved opiate synthesis scheme is provided. An improvement to the oxidation of oripavine and oripavine derivatives comprises the in-situ formation of the peroxacids required to oxidize the oripavine and oripavine derivatives to form...
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JP5371746B2 |
The present invention relates to a method of providing a patient with controlled release of a phenolic opioid using a prodrug capable, upon enzymatic activation, of releasing the phenolic opioid through intra-molecular cyclization leadin...
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