| Patent application number | Description | Published |
|---|
| 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 |
| 20080262231 | Processes for Preparing Morphinans and Intermediates Thereof - The present invention is directed to processes for the synthesis of morphinans. In particular, a process for cyclizing a β,γ-bicyclic ketone compound to form a nordihydrothebainone product using the Grewe cyclization reaction is improved by forming a reaction mixture comprising a β,γ-bicyclic ketone compound, a cyclizing acid and a water scavenging cyclization additive. In one embodiment, the Grewe transformation occurs in the presence of an acid anhydride as the cyclization additive. Further, the present invention is directed to processes for converting α,β-bicyclic ketone compounds (e.g., by-products of the Grewe cyclization reaction) to β,γ-bicyclic ketone compounds, wherein the β,γ-bicyclic ketone compounds may be recovered to further undergo Grewe cyclization and form the nordihydrothebainone product. | 10-23-2008 |
| 20080275017 | AROMATIC SULFENATES FOR TYPE I PHOTOTHERAPY - Novel sulfenate derivatives and their bioconjugates for phototherapy of tumors and other lesions. The sulfenates of the present invention are designed to absorb low-energy ultraviolet, visible, or near-infrared (NIR) region of the electromagnetic spectrum. The phototherapeutic effect is caused by direct interaction of free radicals, the reactive intermediate produced upon photofragmentation of the sulfenate moiety, with the tissue of interest. | 11-06-2008 |
| 20080293947 | Method of Preparation for Imidazolepyridines - The present invention relates to an improved process for preparing imidazo[1,2-a]pyridine-3-acetamides and more particularly, 6-methyl-2-p-tolylH-imidazo[1,2-a]pyridine. | 11-27-2008 |
| 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 |
| 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 |
| 20090156819 | 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 opioid substrates. | 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 |
| 20090247756 | Process for the Preparation of Hexahydroisoquinolines from 1,2,3,4-Tetrahydroisoquinolines - The present invention is directed to processes for the synthesis of morphinans. In particular, a process for the asymmetric reduction of an imine moiety in a 3,4-dihydroisoquinoline to produce a tetrahydroisoquinoline, followed by a Birch reduction to produce a hexahydroisoquinoline. In various embodiments, the 3,4-dihydroisoquinoline contains a phenol moiety protected with a labile protecting group. In other embodiments, the imine reduction reaction mixture contains silver tetrafluoroborate. | 10-01-2009 |
| 20090247760 | Preparation of Amides from an Acid and Amine for Intermediates in the Synthesis of Morphinans - The present invention is directed to processes for the synthesis of morphinans. In particular, a process for coupling a carboxylic acid compound with an amine compound to form an amide product that can then be isolated or the crude amide product can be cyclized to form a 3,4-dihydroisoquinoline. In one embodiment, the carboxylic acid contains a phenol moiety protected with a labile protecting group. The protected phenol reduces reaction times, simplifies work-up of the product, and reduces the amount of cyclizing agent, POCl | 10-01-2009 |
| 20090247761 | Preparation of 3,4-Dihydroisoquinolines in the Synthesis of Morphinans - The present invention is directed to processes for the synthesis of morphinans. In particular, a process for coupling a carboxylic acid compound with an amine compound to form an amide product that can then be isolated or the crude amide product can be cyclized to form a 3,4-dihydroisoquinoline. In one embodiment, the carboxylic acid contains a phenol moiety protected with a labile protecting group. The protected phenol reduces reaction times, simplifies work-up of the product, and reduces the amount of cyclizing agent, POCl | 10-01-2009 |
| 20090258843 | Compositions Containing Antiviral Compounds and Methods of Using the Same - The present invention is directed to compositions and methods for the treatment of various diseases, pathological disorders, and medical conditions such as viral infections and cancer. The compositions include (A) an antiviral compound or a pharmaceutically acceptable salt thereof; and (B) an agent selected from the group consisting of a substituted or unsubstituted imidazole or a pharmaceutically acceptable salt thereof; a non-steroidal anti-inflammatory agent or a pharmaceutically acceptable salt thereof; an amino acid or a pharmaceutically acceptable salt thereof; a carboxylic acid or a pharmaceutically acceptable salt thereof; a sulfonic acid or a pharmaceutically acceptable salt thereof; and a combination thereof. | 10-15-2009 |
| 20090299069 | Processes and Compounds for the Preparation of Normorphinans - The invention generally provides processes and intermediate compounds useful for the production of normorphinans and derivatives of normorphinans. | 12-03-2009 |
| 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 |
| 20100022776 | Preparation of Hexahydroisoquinolines from Dihydroisoquinolines - The present invention is directed to processes for the synthesis of morphinans. In particular, a process for the asymmetric reduction of an imine moiety in a 3,4-dihydroisoquinoline to produce a tetrahydroisoquinoline, followed by a Birch reduction to produce a hexahydroisoquinoline. In various embodiments, the 3,4-dihydroisoquinoline contains a phenol moiety protected with a labile protecting group. In other embodiments, the imine reduction reaction mixture contains silver tetrafluoroborate. | 01-28-2010 |
| 20100035910 | Process for the Preparation of Quaternary N-Alkyl Morphinan Alkaloid Salts - An improved process for the N-alkylation of tertiary morphinan alkaloid bases to form the corresponding quaternary morphinan alkaloid derivatives. | 02-11-2010 |
| 20100041826 | MULTICOMPONENT ASSEMBLIES HAVING ENHANCED BINDING PROPERTIES FOR DIAGNOSIS AND THERAPY - An organized mobile multicomponent conjugate (OMMC) and method of using to enhance binding of weakly binding compounds to a target. A lamellar structure containing at least two binding compounds is assembled under conditions in which the binding compounds self-regulate in or on the lamellar structure, forming a cooperative ensemble that is capable of binding with enhanced affinity to a complementary affinity site on a target. Each binding compound is bound to the lamellar surface, and may be connected by a linker. The OMMC may contain an effector molecule, such as a diagnostic or therapeutic agent, for administration to a patent who is then diagnosed or treated using the effector molecule. | 02-18-2010 |
| 20100041827 | MULTICOMPONENT ASSEMBLIES HAVING ENHANCED BINDING PROPERTIES FOR DIAGNOSIS AND THERAPY - An organized mobile multicomponent conjugate (OMMC) and method of using to enhance binding of weakly binding compounds to a target. A lamellar structure containing at least two binding compounds is assembled under conditions in which the binding compounds self-regulate in or on the lamellar structure, forming a cooperative ensemble that is capable of binding with enhanced affinity to a complementary affinity site on a target. Each binding compound is bound to the lamellar surface, and may be connected by a linker. The OMMC may contain an effector molecule, such as a diagnostic or therapeutic agent, for administration to a patent who is then diagnosed or treated using the effector molecule. | 02-18-2010 |
| 20100041888 | Process for the Preparation of 6-Alpha-Hydroxy-N-Alkylated Opiates - The present invention is directed to the conversion of a 6-keto morphinan to a 6-alpha-hydroxy morphinan in the presence of a ruthenium, rhodium, or iridium asymmetric catalyst and a hydrogen source. | 02-18-2010 |
| 20100048905 | Novel Opiate Reduction Utilizing Catalytic Hydrogen Transfer Reaction - 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 an intermediate. An improvement to the reduction of the intermediate to form oxycodone and oxycodone derivatives comprises reduction utilizing a hydrogen transfer reagent. These improvements allow the production of oxycodone and oxycodone derivatives without isolation of the intermediate, providing a one-pot synthesis method. | 02-25-2010 |
| 20100048906 | Preparation of Substituted Morphinan-6-Ones and Salts and Intermediates Thereof - The present invention is directed to processes for the synthesis of morphinan-6-ones and salts, intermediates, and analogs thereof. | 02-25-2010 |
| 20100056789 | Substituted Berbines and Processes for their Synthesis - The present invention provides processes for the synthesis of substituted berbine compounds. Also provided are intermediates used in the synthesis of substituted berbine compounds. | 03-04-2010 |
| 20100068242 | 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. | 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 |
| 20100113787 | Preparation of Oxymorphone from Oripavine - An improved method for the preparation of oxymorphone from oripavine is provided. Oripavine is oxidized to form 14-hydroxymorphinone after which the oxidation reaction is quenched to prevent the formation of 1-1′-dimer side products. The 14-hydroxymorphinone is then reduced, typically by catalytic hydrogenation to form oxymorphone. The inventive method disclosed is further applicable to the production of morphinan derivatives. | 05-06-2010 |
| 20100113788 | Process for the Preparation of 6-Alpha-Hydroxy-N-Alkylated Opiates - The present invention is directed to the preparation of 6-keto morphinans. | 05-06-2010 |
| 20100197921 | Preparation of N-Alkylated Opiates by Reductive Amination - The present invention is directed to the reduction of an N-imine moiety or a hemiaminal moiety of a morphinan in the presence of a ruthenium, rhodium, or iridium asymmetric catalyst and a hydrogen source. | 08-05-2010 |
| 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 |
| 20100280177 | MULTICOMPONENT ASSEMBLIES HAVING ENHANCED BINDING PROPERTIES FOR DIAGNOSIS AND THERAPY - An organized mobile multicomponent conjugate (OMMC) and method of using to enhance binding of weakly binding compounds to a target. A lamellar structure containing at least two binding compounds is assembled under conditions in which the binding compounds self-regulate in or on the lamellar structure, forming a cooperative ensemble that is capable of binding with enhanced affinity to a complementary affinity site on a target. Each binding compound is bound to the lamellar surface, and may be connected by a linker. The OMMC may contain an effector molecule, such as a diagnostic or therapeutic agent, for administration to a patent who is then diagnosed or treated using the effector molecule. | 11-04-2010 |
| 20100280232 | MULTICOMPONENT ASSEMBLIES HAVING ENHANCED BINDING PROPERTIES FOR DIAGNOSIS AND THERAPY - An organized mobile multicomponent conjugate (OMMC) and method of using to enhance binding of weakly binding compounds to a target. A lamellar structure containing at least two binding compounds is assembled under conditions in which the binding compounds self-regulate in or on the lamellar structure, forming a cooperative ensemble that is capable of binding with enhanced affinity to a complementary affinity site on a target. Each binding compound is bound to the lamellar surface, and may be connected by a linker. The OMMC may contain an effector molecule, such as a diagnostic or therapeutic agent, for administration to a patient who is then diagnosed or treated using the effector molecule. | 11-04-2010 |
| 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 |
| 20100317683 | Preparation of 6-Alpha-Amino N-Substituted Morphinans by Catalytic Hydrogen Transfer - 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 catalytic hydrogen transfer. | 12-16-2010 |
| 20100317861 | Remove Amination of 6-Keto Normorphinans by Catalytic Hydrogen Transfer - 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. | 12-16-2010 |
| 20100324078 | Crystalline Forms of Naltrexone Methobromide - The present invention relates to novel crystalline forms of naltrexone methobromide including hydrated and solvated forms. The invention also describes methods of preparing the various crystalline forms. The present invention also relates to pharmaceutical compositions containing crystalline forms of naltrexone methobromide, as well as methods of treating or preventing opioid induced side effects by administering the pharmaceutical compositions. | 12-23-2010 |
| 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 |
| 20110077222 | Sustained-Release Opiate and Opiate Derivative Compositions - The present invention provides sustained-release opiate compositions. In particular, the present invention provides sustained-release opiate compositions that include an opiate attached to a blood albumin binder. The present invention also relates to methods of administering an opiate with a sustained release pharmacokinetic profile. | 03-31-2011 |
| 20110082297 | Process for the Preparation of Quaternary N-Alkyl Morphinan Alkaloid Salts - An improved process for the N-alkylation of tertiary morphinan alkaloid bases to form the corresponding quaternary morphinan alkaloid derivatives. | 04-07-2011 |
| 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 |
| 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 |
