Patent application number | Description | Published |
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 |
20090156818 | Process and compounds for the production of (+)opiates - The invention generally provides processes and intermediate compounds useful for the production of (+)-opiates. Non-limiting examples of (+) opiates that may be derived from one or more compounds of the invention include (+)-noroxymorphone, (+)-naltrexone, (+)-naloxone, (+)-N-cyclopropylmethylnorhydrocodone, (+)-N-cycloproylmethylnorhydromorphone, (+)-N-allylnorhydrocodone, (+)-N-allylnorhydromorphone, (+)-noroxycodone, (+)-naltrexol, (+)-naloxol, and (+)-3-O-methyl-naltrexone. | 06-18-2009 |
20090156820 | Processes for the production of (+)- "NAL" morphinan compounds - 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 derivatives of (+) nal morphinan compounds from (+)-morphinan substrates such as (+)-hydrocodone, (+)-norhydrocodone or derivatives of either compound. | 06-18-2009 |
20090221825 | 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. | 09-03-2009 |
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 |
20100081819 | Processes for the synthesis of tertiary amines - The invention provides processes for the preparation of morphinans having a tertiary amine. In particular, the present invention provides processes for the formation of tertiary amine alkaloids by direct N-alkylation of secondary amine alkaloids, the processes co-mediated by an alkylating agent and a protic solvent or a mixture of a protic solvent and an aprotic solvent. | 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 |
20100216996 | (+)-Morphinanium Quaternary Salts and Processes for their Production - The present invention provides (+)-morphinanium quaternary salts. The invention also provides processes for producing (+)-morphinanium quaternary salts from tertiary N-substituted (+)-morphinan compounds. | 08-26-2010 |
20100216997 | (+)-Morphinanium N-Oxides and Processes for their Production - The present invention provides (+)-morphinanium N-oxide compounds or pharmaceutically acceptable salts thereof. The invention also provides processes for producing (+)-morphinanium N-oxides or pharmaceutically acceptable salts thereof from the corresponding tertiary N-substituted (+)-morphinan compound or pharmaceutically acceptable salt thereof. | 08-26-2010 |
20100261904 | Preparation of Saturated Ketone Morphinan Compounds by Catalytic Isomerization - The present invention provides processes for the preparation of saturated ketone morphinan compounds by catalytic isomerization. In particular, the invention provides processes for the conversion of a morphinan comprising an allyl alcohol ring moiety into a morphinan comprising a saturated ketone ring moiety by an isomerization reaction catalyzed by an allyl-transition metal catalyst. | 10-14-2010 |
20100261907 | Preparation of Saturated Ketone Morphinan Compounds - The present invention provides processes for the preparation of saturated ketone morphinan compounds. In particular, the invention provides processes for the conversion of a morphinan comprising an allyl alcohol ring moiety into a morphinan comprising a saturated ketone ring moiety by an isomerization reaction catalyzed by an inorganic salt of a late transition metal. | 10-14-2010 |
20100303882 | Medical Devices for Localized Drug Delivery - In certain embodiments, the invention relates to an implantable medical device that includes a body having an internal cavity. Receptor sites in the internal cavity may be adapted to repeatedly bind to, temporarily hold, and release an active agent. An opening may extend through the body and into the internal cavity to allow the active agent into and out of the internal cavity. This opening may be sized and shaped to prevent blood cells from entering the internal cavity through the opening while allowing the active agent to enter and/or exit the cavity via the opening. A polymeric structure may be located in the internal cavity. This polymeric structure may include artificial receptor site mimics for the active agent. | 12-02-2010 |
20100305688 | Medical Devices for Localized Drug Delivery - In certain embodiments, the invention relates to an implantable medical device that includes a body having an internal cavity. Receptor sites in the internal cavity may be adapted to repeatedly bind to, temporarily hold, and release an active agent. An opening may extend through the body and into the internal cavity to allow the active agent into and out of the internal cavity. This opening may be sized and shaped to prevent blood cells from entering the internal cavity through the opening while allowing the active agent to enter and/or exit the cavity via the opening. A polymeric structure may be located in the internal cavity. This polymeric structure may include artificial receptor site mimics for the active agent. | 12-02-2010 |
20110015219 | (+)-Morphinans as Antagonists of Toll-Like Receptor 9 and Therapeutic Uses Thereof - 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 inhibits the activation of TLR9. Also provided are methods of using the (+)-morphinans comprising TLR9 antagonist activity to treat conditions such as traumatic pain, neuropathic pain, inflammatory disorders, acetaminophen toxicity, autoimmune disorders, neurodegenerative disorders, and cancer. | 01-20-2011 |
20110015398 | 3-Oxy-Hydromorphone Derivatives - The present invention provides 3-oxy-hydromorphone derivatives, and in particular, 3-ester, 3-carbonate, and 3-sulfonate derivatives of hydromorphone. | 01-20-2011 |
20110071299 | One-Pot Preparation of Hexahydroisoquinolines from Amides - The present invention provides an efficient process for the preparation of hexahydroisoquinolines from amides. In particular, the invention provides a good yielding, one-pot process for the synthesis of hexahydroisoquinolines. | 03-24-2011 |
20110071300 | One-Pot Preparation of Hexahydroisoquinolines from Dihydroisoquinolines - The present invention provides an efficient process for the preparation of hexahydroisoquinolines from dihydroisoquinolines. In particular, the invention provides a good yielding, one-pot process for the synthesis of hexahydroisoquinolines. | 03-24-2011 |
20110136845 | (+)-Morphinans as Antagonists of Toll-Like Receptor 9 and Therapeutic Uses Thereof - 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 a (+)-morphinan and an opioid agonist/monoamine reuptake inhibitor, as well as methods for using the combination compositions to treat pain. | 06-09-2011 |
20110269963 | Preparation of Saturated Ketone Morphinan Compounds Having Low Metal Content - 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 invention provides processes that utilize isomerization reactions catalyzed by transition metal catalysts and the subsequent removal of the transition metal using metal scavengers. | 11-03-2011 |
20120035366 | N-Demethylation of 6-Keto Morphinans - 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 impurities are not generated during the demethylation of the N-methyl morphinan. | 02-09-2012 |
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 |
20120116086 | 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. | 05-10-2012 |
20120129879 | Compounds and Compositions for Use in Phototherapy and in Treatment of Ocular Neovascular Disease and Cancers - The invention relates generally to anti-angiogenesis agents and related methods of using to anti-angiogenesis agents for biomedical applications including direct monotherapy and combination therapy for treatment of an angiogenesis related condition. In an embodiment, the invention provides a class of opioid compounds and structurally related opioid derivatives exhibiting anti-VEGF activity for use in therapeutic procedures, including phototherapy. Opioid compounds and structurally related opioid derivatives of the invention may be administered alone or in combination with administration of a phototherapy agent and/or other therapeutic agent. | 05-24-2012 |
20130066080 | Production of Alkaloids without the Isolation of Intermediates - The invention relates to processes for the production of alkaloids without the isolation of intermediates. | 03-14-2013 |
20130137874 | One-Pot Preparation of Hexahydroisoquinolines from Amides - The present invention provides an efficient process for the preparation of hexahydroisoquinolines from amides. In particular, the invention provides a good yielding, one-pot process for the synthesis of hexahydroisoquinolines. | 05-30-2013 |
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 |