One Of The Five Cyclos Is Five-membered And Includes Ring Chalcogen (e.g., Codeine, Morphine, Etc.) Patents (Class 546/44)
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Patent number: 8946254Abstract: Bivalent ligands that contain two pharmacophores linked through a spacer, one of which interacts with the ?-opioid receptor (MOR) and the other of which interacts with the co-receptor CC chemokine receptor 5 (CCR5), are used for the treatment of neurological disorders such as those associated with AIDS.Type: GrantFiled: January 10, 2013Date of Patent: February 3, 2015Assignee: Virginia Commonwealth UniversityInventors: Yan Zhang, Kurt F. Hauser, Dana E. Selley
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Patent number: 8921386Abstract: A drug substance with a pharmaceutically acceptable organic acid addition salt of an opioid wherein said organic acid is selected from Structure A: wherein R1-R4 are independently selected from H, alkyl or substituted alkyl of 1-6 carbons, adjacent groups may be taken together to form a cyclic alkyl, cyclic alkyl-aryl, or cyclic aryl moiety; R5 is selected from H, or an alkali earth cation; R6 and R7 are independently selected from H, alkyl of 1-6 carbons, an alkali earth cation, and aryl of 6 to 12 carbons, in a number sufficient to complete the valence bonding of X, and wherein X is selected from nitrogen, oxygen or sulfur; and wherein the drug substance has a morphology selected from amorphous and crystalline.Type: GrantFiled: May 31, 2012Date of Patent: December 30, 2014Assignee: Pisgah Laboratories, Inc.Inventors: Clifford Riley King, Stephen G. D'Ambrosio, David W. Bristol, Michael L. English
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Patent number: 8916707Abstract: The present invention provides a process for preparing an oxycodone acid adduct, said process comprising hydrogenating an aqueous solution of 14-hydroxycodeinone and an acid to form a solution of the oxycodone acid adduct, wherein the hydrogenation is carried out at one or more temperatures greater than ambient temperature in the presence of a hydrogenation catalyst and hydrogen gas, wherein the solution of oxycodone acid adduct comprises 6?-oxycodol in an amount ?about 0.800 area % as determined by HPLC.Type: GrantFiled: August 2, 2013Date of Patent: December 23, 2014Assignee: Johnson Matthey Public Limited CompanyInventors: Nicolas Archer, Maureen Young, Timothy Davies, Amy Price, Michael Bease, Barbara Jamieson, Ewart Grant, Brian Heinrich, Saroop Matharu
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Patent number: 8916706Abstract: This invention relates to synthesis of (R),(R)-2,2?-bis-MNTX, as shown in Formula (I), and related methods and products.Type: GrantFiled: June 6, 2013Date of Patent: December 23, 2014Assignee: Progenics Pharmaceuticals, Inc.Inventors: Alfred A. Avey, Julio Perez
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Publication number: 20140357656Abstract: Bivalent ligands that contain two pharmacophores linked through a spacer, one of which interacts with the ?-opioid receptor (MOR) and the other of which interacts with the co-receptor CC chemokine receptor 5 (CCR5), are used for the treatment of neurological disorders such as those associated with AIDS.Type: ApplicationFiled: January 10, 2013Publication date: December 4, 2014Applicant: Virginia Commonwealth UniversityInventors: Yan Zhang, Kurt F. Hauser, Dana E. Selley
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Patent number: 8901175Abstract: The use of opioids or opioid mimetics is suggested for the manufacture of a medicament for the treatment of resistant cancer patients.Type: GrantFiled: January 29, 2009Date of Patent: December 2, 2014Assignee: Universität UlmInventors: Erich Miltner, Claudia Friesen, Andreas Alt
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Patent number: 8901148Abstract: 8-Substituted-2,6-methano-3-benzazocines of general structure are useful as analgesics, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction medications.Type: GrantFiled: August 23, 2013Date of Patent: December 2, 2014Assignee: Rensselaer Polytechnic InstituteInventor: Mark P. Wentland
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Publication number: 20140330021Abstract: The presently described technology provides compositions comprising aryl carboxylic acids chemically conjugated to hydromorphone (4,5-?-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.Type: ApplicationFiled: July 21, 2014Publication date: November 6, 2014Inventors: Travis Mickle, Sven Guenther, Guochen Chi, Jaroslaw Kanski, Andrea K. Martin, Bindu Bera
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Patent number: 8877753Abstract: The invention relates to the use of a group of sigma receptor ligands of formula (I) for the potentiation of the analgesic effect of opioids and opiates and at the same time for decreasing the dependency induced by them.Type: GrantFiled: April 24, 2009Date of Patent: November 4, 2014Assignee: Laboratorios Del Dr. Esteve, S.A.Inventors: Helmut Heinrich Buschmann, Jose Miguel Vela Hernandez, Daniel Zamanillo-Castanedo
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Patent number: 8853401Abstract: 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 comprises quaternization of oripavine to provide a mixture of the R- and S-isomeric (at the nitrogen) quaternary salts. The R-isomer is readily isolated and converted to various N-(R)-morphinane and N-(S)-morphinone compounds. The R-isomer, S-isomer or a mixture of R- and S-isomers may be demethylated and converted to various morphinane and morphinone compounds.Type: GrantFiled: April 22, 2010Date of Patent: October 7, 2014Assignee: Brock UniversityInventors: Tomas Hudlicky, Robert Carroll, Hannes Leisch, Ales Machara, Lukas Werner, David R. Adams
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Patent number: 8853402Abstract: A process for the reduction of a 6-keto group in a morphinan alkaloid to the corresponding 6-hydroxy group includes hydrogenating the 6-keto group using gaseous hydrogen in the presence of a heterogeneous 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 ?:? ratio of >85:15.Type: GrantFiled: August 13, 2010Date of Patent: October 7, 2014Assignee: Johnson Matthey Public Limited CompanyInventors: George Scott Wilson, Maureen Joan Young
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Publication number: 20140296525Abstract: 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.Type: ApplicationFiled: December 6, 2012Publication date: October 2, 2014Inventors: Carla De Faveri, Mariano Stivanello
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Patent number: 8846903Abstract: Novel acyl-urea containing compounds, processes of preparing same, compositions containing same and uses thereof in the treatment of neurological diseases and disorders such as epilepsy, neuropathic pain, bipolar disorder, status epilepticus, chemically-induced convulsions and/or seizure disorders, febrile convulsions conditions, metabolic disturbances and a sustenance withdrawal conditions, are provided. Also provided are uses of these and other acyl-urea containing compounds in the treatment of neurological diseases and disorders.Type: GrantFiled: June 25, 2008Date of Patent: September 30, 2014Assignee: Yissum Research Development Company of the Hebrew University of Jerusalem Ltd.Inventors: Meir Bialer, Boris Yagen, Jakob Avi Shimshoni
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Patent number: 8841452Abstract: 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.Type: GrantFiled: December 6, 2012Date of Patent: September 23, 2014Assignee: H. Lundbeck A/SInventors: Carla De Faveri, Mariano Stivanello
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Publication number: 20140275149Abstract: Orally administrable pharmaceutical compositions, methods of administration, and methods of making the same are provided. The pharmaceutical compositions provide abuse deterrent properties.Type: ApplicationFiled: March 18, 2014Publication date: September 18, 2014Applicant: Inspirion Delivery Technologies, LLCInventors: Manish S. Shah, Ray J. DiFalco, Stefan Aigner
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Patent number: 8822687Abstract: 8?,14-Dihydroxy-7,8-dihydrocodeinone is described.Type: GrantFiled: February 24, 2010Date of Patent: September 2, 2014Assignees: Purdue Pharma L.P., The P.F. Laboratories, Inc., Purdue Pharmaceuticals L.P., Rhodes TechnologiesInventors: Robert Chapman, Lonn S. Rider, Qi Hong, Donald Kyle, Robert Kupper
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Patent number: 8816084Abstract: The present invention relates to a X-form crystal of 17-cyclopropylmethyl-3,14?-dihydroxy-4,5?-epoxy-6?-[N-methyl-trans-3-(3-furyl)acrylamido]morphinan hydrochloride and the manufacturing method thereof, wherein the X-form crystal of the compound has characteristic diffraction peaks at positions of 2? of 13.6°(±0.2°), 17.2°(±0.2°), 19.1°(±0.2°), 23.2°(±0.2°), and 23.8°(±0.2°) in a powder X-ray diffraction pattern thereof. The present invention also relates to a pharmaceutical composition comprising the above-mentioned X-form crystal of morphinan derivative hydrochloride.Type: GrantFiled: January 28, 2014Date of Patent: August 26, 2014Assignee: Everlight Chemical Industrial CorporationInventors: Yuan-Yi Wang, Yu-Kai Li, Yu-Ting Su, Chia-Chen Hung, Chi-Hsiang Yao
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Patent number: 8816083Abstract: The presently described technology provides compositions comprising aryl carboxylic acids chemically conjugated to hydromorphone (4,5-?-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.Type: GrantFiled: October 25, 2012Date of Patent: August 26, 2014Assignee: KemPharm, Inc.Inventors: Travis Mickle, Sven Guenther, Guochen Chi, Jaroslaw Kanski, Andrea K. Martin, Bindu Bera
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Publication number: 20140206871Abstract: 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.Type: ApplicationFiled: March 21, 2014Publication date: July 24, 2014Applicant: Johnson Matthey Public Limited CompanyInventors: Erno M Keskeny, James J. Mencel, Jen-Sen Dung
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Publication number: 20140200235Abstract: The invention provides compounds that are chemically modified by covalent attachment of a water-soluble oligomer. A compound of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different from those of the compound not attached to the water-soluble oligomer.Type: ApplicationFiled: September 20, 2013Publication date: July 17, 2014Applicant: NEKTAR THERAPEUTICSInventors: Jennifer RIGGS-SAUTHIER, Bo-Liang Deng, Timothy A. Riley
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Patent number: 8778958Abstract: The disclosed opioid-related compounds and pharmaceutical compositions thereof, are useful in a variety of applications relating to the modulation of receptors and receptor signaling within and outside the nervous system. For example, the compounds and compositions are useful in methods for the treatment of addictions and other CNS-related disorders. The disclosed compounds can be delivered or administered to a mammal including humans, alone in the form of a pharmaceutically acceptable salt or hydrolysable precursor thereof, or in the form of a pharmaceutical composition, wherein a therapeutically effective amount of a compound is mixed with suitable carriers or excipients.Type: GrantFiled: July 9, 2009Date of Patent: July 15, 2014Inventor: John R. Cashman
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Patent number: 8772308Abstract: Selective, non-peptide antagonists of the mu opioid receptor (MOR) and methods of their use are provided. The antagonists may be used, for example, to identify MOR agonists in competitive binding assays, and to treat conditions related to addiction in which MOR is involved, e.g. heroin, prescription drug and alcohol addiction.Type: GrantFiled: January 15, 2010Date of Patent: July 8, 2014Assignee: Virginia Commonwealth UniversityInventors: Yan Zhang, Dana E. Selley, William Dewey
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Patent number: 8754217Abstract: 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 dihydrate.Type: GrantFiled: June 25, 2013Date of Patent: June 17, 2014Assignee: H. Lundbeck A/SInventors: Heidi Lopez de Diego, Carla De Faveri, Florian Anton Martin Huber
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Processes for preparing morphinan-6-one products with low levels of alpha beta-unsaturated compounds
Patent number: 8748611Abstract: The present invention generally relates to processes for preparing highly pure morphinan-6-one products. The processes involve reducing the concentration of ?,?-unsaturated ketone compounds present as impurities in morphinan 6 one products or reaction mixtures including morphinan 6 one compounds by treatment with a sulfur-containing compound.Type: GrantFiled: November 11, 2011Date of Patent: June 10, 2014Assignee: Mallinckrodt LLCInventors: Henry J. Buehler, William E. Dummitt, Anthony Mannino, Dennis C. Aubuchon, Hong Gu -
Publication number: 20140155608Abstract: The present invention relates to a new process for producing naltrexone [17-(cyclopropylmethyl)-4,5?-epoxy-3,14-dihydroxy-morphinan-6-one] from noroxymorphone [4,5-?-epoxy-3,14-dihydroxy-morphinan-6-one] by alkylation with a cyclopropylmethyl halide.Type: ApplicationFiled: May 2, 2013Publication date: June 5, 2014Inventors: Carla De Faveri, Mariano Stivanello, Florian Anton Martin Huber
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Publication number: 20140142132Abstract: The present invention provides a compound of formula I: wherein R1, R2, R2? and X? are as defined and described herein, methods of manufacture thereof and compositions thereof, useful for example as peripheral mu opioid receptor antagonists in treatment of side effects of opioid administration.Type: ApplicationFiled: September 4, 2013Publication date: May 22, 2014Applicants: WYETH, LLC, PROGENICS PHARMACEUTICALS, INC.Inventors: Alfred A. Avey, Appavu Chandrasekaren, Harold D. Doshan, Julio Perez, Yakov Rotshteyn
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Patent number: 8729266Abstract: 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.Type: GrantFiled: June 16, 2008Date of Patent: May 20, 2014Assignee: Mallinckrodt LLCInventors: Christopher W. Grote, Brian Orr, Tao Jiang, Gary L. Cantrell
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Publication number: 20140121152Abstract: The embodiments provide prodrug compounds of Formulae I-XVII. The present disclosure also provides compositions, and their methods of use, where the compositions comprise a prodrug compound of Formulae I-XVII that provides controlled release of an active agent. Such compositions can optionally provide a trypsin inhibitor that interacts with the enzyme that mediates the controlled release of an active agent from the prodrug so as to attenuate enzymatic cleavage of the prodrug.Type: ApplicationFiled: March 8, 2012Publication date: May 1, 2014Applicant: Signature Therapeutics, Inc.Inventors: Thomas E. Jenkins, Craig O. Husfeld
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Patent number: 8710070Abstract: The present invention relates to the field of pain management, and more particularly to synergistic codrugs comprising an opioid and ketamine or norketamine which have been combined to form a single chemical codrug entity. When the codrug is administered it produces a synergistic analgesic response to pain.Type: GrantFiled: March 27, 2009Date of Patent: April 29, 2014Assignee: University of Kentucky Research FoundationInventors: Joseph R. Holtman, Peter A. Crooks, Ujjwal Chakraborty
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Patent number: 8710069Abstract: The present invention relates to the field of pain management, and more particularly to synergistic codrugs comprising an opioid and nornicotine which have been combined to form a single chemical codrug entity. When the codrug is administered it produces a synergistic analgesic response to pain.Type: GrantFiled: March 27, 2009Date of Patent: April 29, 2014Assignee: University of Kentucky Research FoundationInventors: Joseph R. Holtman, Peter A. Crooks, Ujjwal Chakraborty
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Patent number: 8710226Abstract: The present invention relates to an improved process for preparing morphinane analogues of formula 1 wherein the substituents R1, R2, R2a, R3, R4, R5 and Y have the meanings as defined in the specifications.Type: GrantFiled: August 29, 2013Date of Patent: April 29, 2014Assignee: Sun Pharmaceutical Industries LimitedInventors: Nileshkumar Sureshbhai Patel, Srinivasu Kilaru, Rajamannar Thennati
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Patent number: 8703950Abstract: 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.Type: GrantFiled: July 1, 2011Date of Patent: April 22, 2014Assignee: Johnson Matthey Public Limited Co.Inventors: Erno M. Keskeny, James J. Mencel, Jen-Sen Dung
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Patent number: 8703949Abstract: 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.Type: GrantFiled: August 3, 2011Date of Patent: April 22, 2014Assignee: Mallinckrodt LLCInventors: Subo Liao, Peter X. Wang, David W. Berberich, Douglas C. Miller
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Patent number: 8691989Abstract: 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.Type: GrantFiled: June 20, 2008Date of Patent: April 8, 2014Assignee: Phoenix Pharmalabs, Inc.Inventor: John A. Lawson
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Patent number: 8685996Abstract: 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 alcohol is a compound of formula (I): wherein R3 is a protecting group. Also disclosed are methods for making 3-O-protected morphine dienol carboxylates comprising allowing a compound of formula (I) to oxidize in the presence of a chlorine-containing compound and a compound of formula R1SR2; and allowing the product of the oxidation step to react with an acylating agent.Type: GrantFiled: May 15, 2012Date of Patent: April 1, 2014Assignee: Purdue Pharma L.P.Inventor: Andreas Stumpf
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Patent number: 8653271Abstract: The present invention is directed to novel codrugs comprising bupropion or hydroxybupropion and an opioid antagonist or an opioid agonist joined together by chemical bonding. The codrugs provide a significant increase in the transdermal flux across human skin, as compared to the basic opioid antagonist or opioid agonist.Type: GrantFiled: October 18, 2007Date of Patent: February 18, 2014Assignee: University of Kentucky Research FoundationInventors: Audra L. Stinchcomb, Peter A. Crooks, Mohamed O. Hamad, Paul K. Kiptoo
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Publication number: 20140013465Abstract: 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 have an increased expression of one or more of thebaine 6-O-demethylase, codeine O-demethylase and/or codeinone reductase relative to wild type P. bracteatum such that the genetically modified poppy plants produce an increased quantity of an alkaloid selected from codeine, oripavine and/or morphine relative to a wild type P. bracteatum. Also provided are progeny plants having the genetically modified poppy plants described above as a parent; mutant or derivative plants of the aforementioned plants; reproductive material derived from, straw produced from, straw concentrate produced from, latex derived from, or one or more isolated cells derived from, the aforementioned plants.Type: ApplicationFiled: March 15, 2013Publication date: January 9, 2014Applicant: TPI ENTERPRISES LTD.Inventors: Justin Taylor Coombs, Jarrod David Ritchie, Mark Alfred Tester, Damien Lightfoot, Deepa Jha
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Patent number: 8624030Abstract: 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.Type: GrantFiled: August 3, 2011Date of Patent: January 7, 2014Assignee: Mallinckrodt LLCInventors: Peter X. Wang, Tao Jiang, David W. Berberich, Subo Liao
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Patent number: 8614224Abstract: 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.Type: GrantFiled: January 18, 2012Date of Patent: December 24, 2013Assignee: Mallinckrodt LLCInventors: Peter X. Wang, Tao Jiang, Gary L. Cantrell, David W. Berberich, Bobby N. Trawick, Subo Liao, John Brandt
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Publication number: 20130338365Abstract: 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.Type: ApplicationFiled: June 25, 2013Publication date: December 19, 2013Inventors: Heidi Lopez de DIEGO, Carla de FAVERI, Florian Anton Martin HUBER
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Patent number: 8609682Abstract: The invention provides a compound of formula (I) or a salt thereof, as well as compositions comprising such compounds. The compounds and compositions are useful as analgesics.Type: GrantFiled: July 10, 2009Date of Patent: December 17, 2013Assignee: Regents of The University of MinnesotaInventors: Philip S. Portoghese, Ajay S. Yekkirala
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Patent number: 8598352Abstract: 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.Type: GrantFiled: May 21, 2010Date of Patent: December 3, 2013Assignee: H. Lundbeck A/SInventors: Carla De Faveri, Mauro Casarin, Michele Brusegan
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Publication number: 20130310414Abstract: A therapeutic or prophylactic agent for cachexia includes as an effective ingredient a compound having a specified morphinan skeleton represented by a compound of the following structure: or a pharmacologically acceptable acid addition salt thereof.Type: ApplicationFiled: January 30, 2012Publication date: November 21, 2013Applicant: Toray Industries, Inc.Inventors: Tomohiko Suzuki, Yoshitaka Yoshizawa, Mikito Hirakata
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Patent number: 8580963Abstract: The present invention relates to an improved process for producing naltrexone[17-(cyclopropylmethyl)-4,5?-epoxy-3,14-dihydroxy-morphinan-6-one] from noroxymorphone[4,5-?-epoxy-3,14-dihydroxy-morphinan-6-one] by alkylation with a cyclopropylmethyl halide.Type: GrantFiled: November 2, 2011Date of Patent: November 12, 2013Assignee: H. Lundbeck A/SInventors: Carla De Faveri, Florian Anton Martin Huber, Mariano Stivanello
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Publication number: 20130289060Abstract: 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.Type: ApplicationFiled: October 19, 2011Publication date: October 31, 2013Applicant: MEMORIAL SLOAN-KETTERING CANCER CENTERInventors: Gavril Pasternak, Susruta Majumdar
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Patent number: 8569228Abstract: 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 compositions, and their methods of use, where the compositions comprise a prodrug, Compound KC-8, that provides controlled release of oxycodone. Such compositions can optionally provide a trypsin inhibitor that interacts with the enzyme that mediates the controlled release of oxycodone from the prodrug so as to attenuate enzymatic cleavage of the prodrug.Type: GrantFiled: January 9, 2012Date of Patent: October 29, 2013Assignee: Signature Therapeutics, Inc.Inventors: Thomas E. Jenkins, Craig O. Husfeld
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Publication number: 20130281698Abstract: This invention provides novel 6-amino-morphinan derivatives, methods of making same, and methods of using same for analgesic purposes.Type: ApplicationFiled: October 9, 2012Publication date: October 24, 2013Applicant: AlcaSynn Pharmaceuticals GmbHInventor: AlcaSynn Pharmaceuticals GmbH
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Patent number: 8563721Abstract: The present invention relates to morphinan derivatives and preparation methods thereof, especially to ketal hydroxyl protected compounds of morphinan derivatives and preparation method thereof, and to a method for preparing corresponding alkylated morphinan derivatives by using the ketal hydroxyl protected compounds as intermediates, and more especially to a ketal hydroxyl protected compound of methylnaltrexone as intermediate for preparing methylnaltrexone and a method for preparing methylnaltrexone through said intermediate.Type: GrantFiled: June 19, 2009Date of Patent: October 22, 2013Assignee: Chongqing Pharmaceutical Research Institute Co., Ltd.Inventors: Huafu Sun, Jie Luo, Wenrun Ye, Jie Deng, Bo Lin, Chunyan Dan, Bin Fan
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Patent number: 8563724Abstract: 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.Type: GrantFiled: February 23, 2010Date of Patent: October 22, 2013Assignee: Mallinckrodt LLCInventors: Christopher W. Grote, Gary L. Cantrell, Peter X. Wang, Bobby N. Trawick, David W. Berberich
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Patent number: 8563725Abstract: 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.Type: GrantFiled: April 26, 2011Date of Patent: October 22, 2013Assignee: Mallinckrodt LLCInventors: Tao Jiang, Peter X. Wang, David W. Berberich