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| Number | Title | Issue Date |
| 8183376 | Stereoselective reduction of a morphinone 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. ... | 05/22/2012 |
| 8158793 | Demethylation of 14-hydroxy substituted alkaloid derivatives The present invention is directed to a method for demethylating 14-hydroxy substituted alkaloid derivatives, in particular of 14-hydroxy-17-methyl-4,5-epoxymorphinane-6-on-derivatives. This is achieved by reacting a starting compound with a compound of general formu... | 04/17/2012 |
| 8134002 | Process for preparing oxymorphone Methods are provided which include converting oripavine to other opiates, including converting oripavine to 14-hydroxymorphinone and/or converting 14-hydroxymorphinone to oxymorphone. Purification and salt formation are optionally included. ... | 03/13/2012 |
| 8119803 | Preparation of opiate analgesics by reductive alkylation A process for preparing a compound of formula (A), (B) or (C): wherein P is H, CH3 or a hydroxyl protecting group; X is O, a protected ketone, OH, a protected hydroxyl group or H; Y is OH, a protected hydroxyl gr... | 02/21/2012 |
| 8101756 | Process for the preparation of quaternary N-alkyl morphin or morphinan alkaloid derivatives The present invention relates to a process for the preparation of quaternary N-alkyl morphin or morphinan alkaloid derivatives. This is achieved by using a nucleophilic nitrogen, phosphor or sulfur containing base in the reaction mixture. ... | 01/24/2012 |
| 8101757 | Processes for the preparation of normorphinan salts 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 normorphinan salts from crude opi... | 01/24/2012 |
| 8067597 | Synthetic route to 14-hydroxyl opiates through 1-halo-thebaine or analogs Novel methods of synthesis of known and novel 14-hydroxyl opiates through 1-halothebaine and derivatives are described. ... | 11/29/2011 |
| 8058439 | Process for preparing oxycodone having reduced levels of 14-hydroxycodeinone The present invention is directed to processes for preparing oxycodone base and oxycodone hydrochloride compositions having less than 10 ppm of 14-hydroxycodeinone. ... | 11/15/2011 |
| 8003794 | ()--methylnaltrexone This invention relates to S-MNTX, methods of producing S-MNTX, pharmaceutical preparations comprising S-MNTX and methods for their use. ... | 08/23/2011 |
| 8003793 | Methods for making 3-O-protected morphinones and 3-O-protected morphinone dienol carboxylates Disclosed are methods for making aldehydes and ketones comprising allowing the corresponding primary or secondary alcohol to react in the presence of trichoroisocyanuric acid, a compound of formula R1SR2 and a base. In one embodiment, the alcoh... | 08/23/2011 |
| 7999105 | Process for the preparation of 3-hydroxymorphinan derivatives Processes are described for the synthesis of 3-hydroxymorphinan derivatives by hydrolysis of side products from the O-demethylation of 3-methoxymorphinan derivatives. ... | 08/16/2011 |
| 7999104 | Methods for one-pot -demethylation/-acylation of morphine and tropane alkaloids 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 the presence of a metal cataly... | 08/16/2011 |
| 7935820 | Methods for -demethylation of morphine and tropane alkaloids The present invention provides a method for the N-demethylation of an N-methylated heterocycle, particularly a morphine or tropane alkaloid or derivative thereof. The method comprises reacting the heterocycle with a metal catalyst and a solvent in the presence of an... | 05/03/2011 |
| 7935821 | Method for separation and purification of naltrexone by preparative chromatography A process for the purification of an impure preparation containing naltrexone by means of a reverse phase preparative chromatography process is provided. In an illustrative embodiment a chromatographic column is loaded with a stationary phase, typically a silica par... | 05/03/2011 |
| 7928234 | Conversion of thebaine to morphine derivatives 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 thebaine with an acid in the pres... | 04/19/2011 |
| 7906647 | Process for preparing oxycodone having reduced levels of 14-hydroxycodeinone The present invention is directed to processes for preparing oxycodone base and oxycodone hydrochloride compositions having less than 10 ppm of 14-hydroxycodeinone. ... | 03/15/2011 |
| 7875719 | Process for reducing impurities in oxycodone base 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. ... | 01/25/2011 |
| 7875718 | Process for the synthesis of morphinane compounds and intermediates thereof 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 intermediates in the synthesis of m... | 01/25/2011 |
| 7692013 | Method for separation and purification of hydrocodone by preparative chromatography A process for the purification of an impure preparation containing hydrocodone by means of a reverse phase preparative chromatography process is provided. In an illustrative embodiment a chromatographic column is loaded with a stationary phase, typically a silica pa... | 04/06/2010 |
| 7674904 | Synthesis of R-N-methylnaltrexone This invention relates to stereoselective synthesis of R-MNTX and intermediates thereof, pharmaceutical preparations comprising R-MNTX or intermediates thereof and methods for their use. ... | 03/09/2010 |
| 7645880 | Processs for preparing N-alkylnaltrexone halides The invention relates to a novel process for preparing N-methylnaltrexone bromide, comprising at least the steps consisting in: (i) reacting N-methylnaltrexone methyl sulfate in aqueous solution with an alkaline agent chosen from t... | 01/12/2010 |
| 7619087 | Method of preparation of oxycodone A method of preparation of Oxycodone of formula I by reacting thebaine of formula II, or its analogue of formula III, wherein R represents a C2 to C5 alkyl, an alkylaryl, preferably benzyl, methoxybenzyl, or allyl, with hydrogen peroxide or per... | 11/17/2009 |
| 7619088 | Demethylation of 14-hydroxy substituted alkaloid derivatives The present invention is directed to a method for demethylating 14-hydroxy substituted alkaloid derivatives, in particular of 14-hydroxy-17-methyl-4,5-epoxymorphinane-6-on-derivatives. This is achieved by reacting a starting compound with a compound of general formu... | 11/17/2009 |
| 7563899 | (S)--methylnaltrexone This invention relates to S-MNTX, methods of producing S-MNTX, pharmaceutical preparations comprising S-MNTX and methods for their use. ... | 07/21/2009 |
| 7550592 | Hydromorphone polymorphs Hydromorphone hydrochloride forms are disclosed which are useful as analgesic agents either in combination with or as replacements for hydromorphone hydrochloride. ... | 06/23/2009 |
| 7534888 | Oxycodone polymorphs Oxycodone.HCl polymorph forms are disclosed which are useful as analgesic agents either in combination with or as replacements for oxycodone. ... | 05/19/2009 |
| 7435817 | C-14 oxidation of morphine derivatives 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 (... | 10/14/2008 |
| 7405301 | Chemical methods This invention relates to a method for N-demethylating an N-methyl morphinane comprising the steps of: (i) treating said N-methyl morphinane with an oxidizing agent to form the N-oxide morphinane; and (ii) treating said N-oxide morphinane with a reducing agent. This... | 07/29/2008 |
| 7399858 | Method for the catalytic production of hydrocodone, hydromorphone, and derivatives thereof A method for the catalytic production of hydrocodone derivatives and hydromorphone derivatives, respectively, utilizing a transition metal catalyst of the formula [M(PR4R5R6)nXm]p; wherein M is a Grou... | 07/15/2008 |
| 7399859 | Method for catalytic preparation of hydromorphone and hydrocodone The present invention generally relates to catalysts of formula (III) [M(P(Ra)(Rb)N(Rc)(Rd))2Xn]mYp that selectively convert morphin... | 07/15/2008 |
| 7348430 | Production of opioid analgesics The present invention includes a process for the manufacture of dihydrothebaine, dihydrocodeinone enol acetate, hydrocodone, and analogs thereof by reacting dihydrocodeine or analogs thereof with benzophenone in the presence of potassium tert-alkylate in a hydrocarb... | 03/25/2008 |
| 7323565 | Method for the catalytic production of hydrocodone and hydromorphone A method for the catalytic conversion of codeine, morphine or analogs thereof into hydrocodone, hydromorphone or analogs thereof utilizing a transition metal complex of a tertiary phosphine halide as catalyst. ... | 01/29/2008 |
| 7321038 | Method for the catalytic production of hydrocodone and hydromorphone A method for the catalytic conversion of codeine, morphine or analogs thereof into hydrocodone, hydromorphone or analogs thereof utilizing a transition metal catalyst of the formula [M(PR3R4R5)nXm]p; ... | 01/22/2008 |
| 7285665 | Process for the preparation of quaternary N-alkyl morphinan alkaloid salts A process for the preparation of a quaternary derivative of the morphinan alkaloid, the process comprising contacting a tertiary N-substituted morphinan alkaloid with an alkyl halide in an anhydrous solvent system, wherein the solvent system comprises an aprotic dip... | 10/23/2007 |
| 7199129 | Derivatives of morphine-like opioid compounds The present disclosure concerns compounds of formula (I) and pharmaceutically acceptable salts, hydrates, solvates, pharmaceutically acceptable derivatives, pro-drugs, tautomers and/or isomers thereof. The disclosure also relates to processes for the preparation of ... | 04/03/2007 |
| 7172767 | Opioid agonist / antagonist combinations The invention is directed in part to oral dosage forms comprising a combination of an orally analgesically effective amount of an opioid agonist and an orally active opioid antagonist, the opioid antagonist being included in a ratio to the opioid agonist to provide ... | 02/06/2007 |
| 7164021 | Opiate analogs selective for the δ-opioid receptor Novel compounds which selectively bind to the δ-opioid receptor have been designed. These compounds have greater selectivity, improved water (blood) solubility, and enhanced therapeutic value as analgesics. Because agonists with selectivity for the δ-opioid recept... | 01/16/2007 |
| 7153966 | Preparation of oxycodone A process for preparing oxycodone or an oxycodone salt, wherein the oxycodone or oxycodone salt has low levels of impurities (especially 14-hydroxycodeinone) is disclosed. The process comprises the steps of: a) preparing a mixture ... | 12/26/2006 |
| 7129248 | Process for preparing oxycodone hydrochloride having less than 25 ppm 14-hydroxycodeinone In certain embodiments the invention is directed to a process for preparing an oxycodone hydrochloride composition having less than 25 ppm of 14-hydroxycodeinone. ... | 10/31/2006 |
| 7071336 | Process for manufacturing opioid analgesics Oxycodone is manufactured in high yields and with a high purity using a composition including a thebaine component into 14-hydroxycodeinone and then reduction of 14-hydroxycodeinone to oxycodone. ... | 07/04/2006 |
