Entries |
Document | Title | Date |
20080207906 | 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. | 08-28-2008 |
20090156815 | N-demethylation of N-methyl morphinans - 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 employed as starting materials, for example, commonly available N-methyl opiates such as oripavine and thebaine, and C(3)-protected hydroxy derivatives of oripavine. | 06-18-2009 |
20090156816 | Sinomenine derivatives and processes for their synthesis - 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 their intermediates. | 06-18-2009 |
20090156817 | Process for the preparation of buprenorphine and derivatives for buprenorphine - 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 from norhydromorphone or derivatives of norhydromorphone. | 06-18-2009 |
20090312552 | Process for the Preparation of 6-Beta Hydroxy Morphinan Compounds - The invention provides processes for the conversion of a 6-keto morphinan to a 6-hydroxy morphinan. In particular, the invention provides a stereoselective process for the conversion of a 6-keto morphinan to a 6-beta-hydroxy morphinan. | 12-17-2009 |
20090318699 | Methods of synthesis of morphinans - 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 disclosure may also allow for the preparation of diastereomerically enriched morphinans using less time, and/or using fewer reaction steps, and/or providing better yield than previously used methods for preparing morphinans. The methods disclosed herein find utility in synthetic organic chemistry as well as medicinal chemistry. | 12-24-2009 |
20100036128 | PROCESS FOR MAKING MORPHINAN-6alpha-OLS - The present invention provides a process whereby morphinan-6-ones can be converted stereospecifically to the corresponding morphinan-6α-ols by catalytic hydrogenation under basic conditions. | 02-11-2010 |
20100069639 | Processes for the Synthesis of Five and Six Membered Heterocyclic Rings - The present invention provides processes for the synthesis of five and six membered rings. In particular, the present invention provides processes for the synthesis of five and six membered rings in alkaloids. | 03-18-2010 |
20100081817 | Processes for the selective amination of ketomorphinans - The present invention is generally directed to a process for the preparation of a ketomorphinan comprising maintaining a ketone group as unprotected and performing reductive amination using a hydrogen source and a catalyst. | 04-01-2010 |
20100081818 | Process for the Preparation of 6-Alpha-Hydroxy-N-Alkylated Opiates - The present invention is directed to the preparation of 6-hydroxy morphinans having formula (II) or N-alkylated 6-hydroxy morphinans having formula (III). | 04-01-2010 |
20100216995 | (+)-6-Hydroxy-Morphinan or (+)-6-Amino-Morphinan Derivatives - The present invention provides (+)-morphinanium compounds comprising substituted 6-hydroxy or 6-amine groups. The invention also provides methods for inhibiting microglial activation by administering the compounds of the invention. | 08-26-2010 |
20100234600 | PAPAVER SOMNIFERUM WITH HIGH CONCENTRATION OF CODEINE - The present invention is directed to an improved poppy straw, concentrate of poppy straw and opium of | 09-16-2010 |
20110118466 | PROCESS FOR PREPARING OXYMORPHONE, NALTREXONE, AND BUPRENORPHINE - Methods are provided which include converting oripavine to other opiates, including converting oripavine to naltrexone, buprenorphine, 14-hydroxymorphinone and/or converting 14-hydroxymorphinone to oxymorphone. Purification and salt formation are optionally included. | 05-19-2011 |
20120022259 | 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 R | 01-26-2012 |
20120035367 | Tandem Process for Preparing N-Alkyl Morphinans - 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-alkyl morphinans. | 02-09-2012 |
20120123123 | PREPARATION OF NALMEFENE HYDROCHLORIDE FROM NALTREXONE - 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 hydrochloride salt. | 05-17-2012 |
20120209002 | PROCESS FOR REDUCING THE 6-KETO GROUP OF A MORPHINAN ALKALOID TO THE 6-HYDROXY GROUP BY HYDROGENATION - 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 heterogenous catalyst and a solvent, to yield the 6-hydroxy morphinan alkaloid, wherein the reduction is carried out at a pH in the range of about 5 to about 7, and the 6-hydroxy morphinan alkaloid has an α:β ratio of >85:15. | 08-16-2012 |
20130018190 | 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. | 01-17-2013 |
20130203999 | One Pot Process for Producing 6-Hydroxyl Nal-Opiate - 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-opiate. | 08-08-2013 |
20130281698 | Novel 6-Amino-Morphinan Derivatives, Method of Manufacturing Them and Their Application as Analgesics - This invention provides novel 6-amino-morphinan derivatives, methods of making same, and methods of using same for analgesic purposes. The derivatives of this invention are represented by the following formula: | 10-24-2013 |
20130338365 | NALMEFENE HYDROCHLORIDE DIHYDRATE - 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 comprising administering Nalmefene hydrochloride dehydrate. | 12-19-2013 |
20140206871 | LOW ABUK OXYCODONE, ITS SALTS AND METHODS OF MAKING SAME - 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 contaminant precursor, 8,14-dihydroxy-7,8-dihydrocodeinone, is reduced to a hydroxyl group thus forming a triol. This triol is substantially inert with respect to reforming 14-hydroxycodeinone and can be readily separated from oxycodone. | 07-24-2014 |
20140296525 | PROCESS FOR RECOVERY OF NALMEFENE HYDROCHLORIDE - 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 certain impurities. | 10-02-2014 |
20140330021 | Benzoic Acid, Benzoic Acid Derivatives and Heteroaryl Carboxylic Acid Conjugates of Hydromorphone, Prodrugs, Methods of Making and Use Thereof - 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 hydromorphone prodrugs of the present technology have decreased side effects and decreased potential for abuse compared to unconjugated hydromorphone. The present technology also provides methods of treating patients, pharmaceutical kits and methods of synthesizing conjugates of the present technology. | 11-06-2014 |
20150045555 | Conjugate of Polyethylene Gylcol and Naloxone and Pharmaceutical Composition and Use Thereof - Provided are a PEG-naloxone conjugate of general formula (II) and a pharmaceutical composition comprising the conjugate. In the conjugate, n is an integer in the range of 1-20. Also provided is a three-branched or four-branched conjugate of PEG and naloxone. Structural modification of naloxone with a hydrophilic polymer improves the pharmacokinetic properties of the drug, increase the water solubility of naloxone, improve the in vivo distribution of the drug, reduce the side effects of naloxone on central nervous system, and relieve bowel dysfunction and constipation caused by chronic administration of opioids. Also provided are a pharmaceutical composition comprising the conjugate of the invention and use of the conjugate. | 02-12-2015 |
20150126741 | CONVENIENT PREPARATION OF N-SUBSTITUTED MORPHINAN-6-OLS FROM MORPHINAN-6-ONES - Described herein are methods of preparing 6-hydroxy N-alkyl morphinan-6-ols from morphinan-6-ones, as illustrated below: | 05-07-2015 |
20150141649 | PREPARATION OF NORMORPHINANS - 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 carbamate, and then removing the carbamate functionality from the normorphinan carbamate to form the normorphinan. | 05-21-2015 |
20150361084 | Morphine Sulfate Methanolic Solvate, Processes for Making Same and Related Compositions and Methods for Treating Pain - Processes for reducing the amount of impurities, especially α,β-unsaturated ketones (ABUK), in materials containing morphine. Novel compounds, namely low ABUK morphine sulfate methanolic solvate, and a novel crystal form are also described. The method for making morphine sulfate methanolic solvate comprises mixing a morphine free base composition with methanol to form a solution and adding a liquid comprising sulfuric acid to the solution to form a morphine sulfate methanolic solvate precipitate. A method of making a morphine sulfate compound comprises drying the morphine sulfate methanolic solvate in the presence of water vapor, such that methanol molecules are removed and replaced with water vapor molecules. A composition for treating pain comprises the morphine sulfate compound and at least one pharmaceutically acceptable excipient. A method for treating pain comprises administering to a patient in need thereof the composition comprising the morphine sulfate compound and at least one pharmaceutically acceptable excipient. | 12-17-2015 |
20160024102 | CRYSTAL OF 6,7-UNSATURATED-7-CARBAMOYL MORPHINAN DERIVATIVE AND METHOD FOR PRODUCING THE SAME - Stable crystalline forms of a compound represented by the formula (IA): | 01-28-2016 |
20170233400 | METHODS FOR MAKING 3-O-PROTECTED MORPHINONES AND 3-O-PROTECTED MORPHINONE DIENOL CARBOXYLATES | 08-17-2017 |