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WO/2013/168011A1 |
The invention relates to the compounds of formula (I) and formula (II) or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising a...
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WO/2013/166271A1 |
The present disclosure is concerned with a process for the preparation of the above disclosed compounds, pharmaceutically acceptable salts thereof, deuterated forms thereof, isomers thereof, solvates thereof, or mixtures thereof which co...
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WO/2013/164383A1 |
The present invention relates to a new process for producing naltrexone [17-(cyclopropylmethyl)-4,5α-epoxy-3,14-dihydroxy-morphinan
-6-one] from noroxymorphone [4,5- α-epoxy-3,14-dihydroxy-morphinan-6-one] by alkylation with a cyclopro...
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WO/2013/163668A1 |
The present invention relates to genetically modified plants of the species Papaver bracteatum wherein the type or amount of one or more alkaloids produced by the plants has been modified. Specifically, the genetically modified plants ha...
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WO/2013/119886A1 |
The present invention provides processes for preparing nal-opiates without the isolation of intermediates. In general, the process provides for alkylation and reduction in the same pot to give the nal-opi- ate (I).
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WO/2013/113120A1 |
The oxazolidine derived from the reaction of oxymorphone with the Burgess reagent, temporariiy protected at 0-3 and C-6, reacts with Grignard or other suitable metallic or organometallic reagents to directly provide, for example, A/-ally...
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WO/2013/106528A1 |
Bivalent ligands that contain two pharmacophores linked through a spacer, one of which interacts with the μ-opioid receptor (MOR) and the other of which interacts with the co-receptor CC chemokine receptor 5 (CCR5), are used for the tre...
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WO/2013/095321A1 |
The present invention provides novel heroin hapten compounds and heroin immunoconjugates which can be used for in vivo production of antibodies that specifically bind to heroin and its psychoactive metabolites. The invention also provide...
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WO/2013/084060A1 |
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 a...
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WO/2013/083685A1 |
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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WO/2013/063204A1 |
The presently described technology provides compositions comprising aryl carboxylic acids chemically conjugated to hydromorphone (4,5-α-epoxy-3-hydroxy-17-methyl morphinan-6-one) to form novel prodrugs/compositions of hydromorphone. The...
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WO/2013/050748A2 |
An improved process for preparing buprenorphine and a method for increasing the yield of buprenorphine or a derivative thereof.
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WO/2013/036729A1 |
The invention relates to processes for the production of alkaloids without the isolation of intermediates.
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WO/2013/019825A1 |
The present Invention provides to an improved process for preparing alkaloid salts. In particular, the process comprises a stepwise addition of an acid to an alkaloid chosen from hydrocodone, codeine, and dihydrocodeine to form a flowabl...
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WO/2013/007986A1 |
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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WO/2012/163796A1 |
Crystalline, anhydrous hydrochloride salts of 4,5a-epoxy-3,14-dihydroxy-1 methylmorphinan-6-one (oxymorphone) are disclosed and three polymorphic form of these salts are reported. The invention further relates to a method for th producti...
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WO/2012/151669A1 |
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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WO/2012/149633A1 |
A high-yielding method for the N-demethylation of oxycodone- and oxymorphone-N-oxides by the reaction of these compounds with cyclodehydration reagents has been performed. This method has been utilized to improve the synthesis of various...
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WO/2012/096887A2 |
The embodiments provide Compound KC-8, N-1-[3-(oxycodone-6-enol-carbonyl-methyl-amino)-2,2-dimethyl
-propylamine]-arginine-glycine-malonic acid, or acceptable salts, solvates, and hydrates thereof. The present disclosure also provides co...
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WO/2012/063933A1 |
The present invention provides a compound represented by Formula (IA): an acid addition salt thereof, and/or stable crystals of solvates thereof. The crystals are extremely useful as an active ingredient for producing pharmaceutical prod...
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WO/2012/058714A1 |
The present invention relates to genetically modified plants of the species Papaver bracteatum wherein the type or amount of one or more alkaloids produced by the plants has been modified. Specifically, the genetically modified plants ha...
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WO/2012/059103A1 |
The present invention relates to an improved process for producing naltrexone [17- (cyclopropylmethyl)-4,5α-epoxy-3,14-dihydroxy-morphinan-6-o
ne] from noroxymorphone [4,5- α-epoxy-3,14-dihydroxy-morphinan-6-one] by alkylation with a c...
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WO/2012/054566A2 |
Compounds of formula: 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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WO/2012/038813A1 |
The present invention is directed to Buprenorphine Analog compounds of the Formula (I), Formula (IA) or Formula (IB) shown below, wherein R1, R2, R8, R 3a, R 3b, G, X, Z and Y are as defined herein. Compounds of the Invention are useful ...
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WO/2012/018871A1 |
The present invention provides processes for the preparation of N-alkyl morphinans without the isolation of nor-morphinan intermediates. In particular, the invention provides tandem hydrolysis/alkylation reactions for the synthesis of N-...
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WO/2012/018872A1 |
The present invention provides processes for the demethylation of an N-methyl morphinan comprising a ketone functional group. In particular, the invention provides methods for the protection of the ketone functional group such that impur...
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WO/2012/013671A1 |
A process for the production of a 14-oxygenated morphinan-6-one of formula (I) wherein R1 is alkyl, alkenyl, alkynyl, cycloalkylalkyl, aralkyl, R3 is hydrogen, and R4 is hydrogen, wherein oripavine, 14-hydroxymorphinone or oxymorphone is...
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WO/2012/010106A1 |
Disclosed is a preparation method for a morphinan bromide quaternary ammonium salt as represented by Formula (I). The method comprises: transforming a compound as represented by Formula (II) in a compound as represented by Formula (I) by...
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WO/2012/008984A1 |
The present invention provides (+)-morphinans comprising Toll-like receptor 9 (TLR9) antagonist activity, as well as methods for using the (+)-morphinans to treat pain. Also provided are pharmaceutical combination compositions comprising...
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WO/2012/003468A1 |
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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WO/2011/154826A1 |
The present disclosure provides improved methods for N-dealkylation of tertiary amines, including methods for N-demethylation of alkaloids and opioids, in which the dealkylation reaction is carried out in a solvent comprising a tertiary ...
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WO/2011/137086A1 |
The present invention provides processes for the preparation of saturated ketone morphinan compounds from a morphinan comprising an allyl alcohol ring moiety, wherein the final product has a low metal content. In particular, the inventio...
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WO/2011/137331A2 |
4-Fluoro-4-phenylpiperidin-1-yl μ antagonists of general structure (I) are useful as treatments of conditions or diseases associated with binding opioid receptors.
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WO/2011/123863A1 |
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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WO/2011/117172A1 |
The present invention relates to a novel process for preparing opiates or salts thereof. More particularly, the present invention relates to oxidizing the starting material in a continuous flow reactor, followed by either an isolation of...
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WO/2011/093441A1 |
Disclosed is a novel medicinal agent which has an excellent therapeutic effect on biliary diseases and is therefore is useful for the treatment or prevention of biliary diseases. Specifically disclosed is a therapeutic or prophylactic ag...
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WO/2011/083304A1 |
The present invention concerns prodrugs of opioid analgesics and pharmaceutical compositions containing such prodrugs. Methods for providing more consistent pain relief by increasing the bioavailability of the opioid analgesic with the a...
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WO/2011/037854A2 |
The present disclosure generally relates to methods for producing opioid derivatives. More particularly, the present disclosure relates to the preparation of hydromorphone, hydrocodone, or a derivative thereof, by means of a non-catalyti...
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WO/2011/035276A2 |
The present disclosure generally relates to catalytic methods for producing opioid derivatives. More particularly, the present disclosure relates to the preparation of hydrocodone, hydromorphone, or a derivative thereof, by means of a co...
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WO/2011/034747A1 |
The present invention provides processes for the preparation of 10-keto and/or 10-hydroxy morphinans. In particular, the invention provides to processes for preparing a 10-keto morphinan by chromium-catalyzed benzylic oxidation of a morp...
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WO/2011/032214A1 |
The present invention provides methods of N-demethylating, N-methylated heterocycles and N-methyl, N-oxide heterocycles using a transition metal with an oxidation state of zero, ferrocene or substituted derivatives thereof, or Cr 3+ .N-d...
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WO/2011/031350A1 |
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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WO/2011/021029A1 |
The present invention relates to a process for the reduction of a 6-keto group in a morphinan alkaloid to the corresponding 6-hydroxy group, comprising hydrogenating the 6-keto group using gaseous hydrogen in the presence of a heterogene...
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WO/2011/009015A1 |
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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WO/2011/008636A1 |
The present invention provides 3-oxy-hydromorphone derivatives, and in particular, 3-ester, 3-carbonate, and 3-sulfonate derivatives of hydromorphone.
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WO/2011/005452A1 |
The present invention provides processes for the enrichment of buprenorphine in a product. In particular, the present invention provides processes for the enrichment of buprenorphine in a product using chromatographic techniques. Formula...
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WO/2010/144641A1 |
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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WO/2010/136039A1 |
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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WO/2010/132570A1 |
The present invention relates to methods for the synthesis of galanthamine, morphine, intermediates, salts and derivatives thereof, wherein the starting compound is biphenyl.
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WO/2010/121369A1 |
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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