Nitrogen Or Divalent Chalcogen Double Bonded Directly To Carbocyclic Ring Of The Pentacyclo Ring System (e.g., Morphinones, Etc.) Patents (Class 546/45)
  • Preparation of oxymorphone from oripavine
    Patent number: 8217175
    Abstract: 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.
    Type: Grant
    Filed: March 14, 2008
    Date of Patent: July 10, 2012
    Assignee: Mallinckrodt LLC
    Inventors: Peter X. Wang, Tao Jiang, Gary L. Cantrell, David Wayne Berberich
  • OPIOIDS FOR THE TREATMENT OF THE RESTLESS LEG SYNDROME
    Publication number: 20120172387
    Abstract: The present invention relates to an opioid controlled release oral dosage form comprising at least one opioid for the manufacture of a medicament to treat patients with restless leg syndrome (RLS).
    Type: Application
    Filed: December 21, 2011
    Publication date: July 5, 2012
    Applicant: Euro-Celtique S.A.
    Inventors: Wolfgang FLEISCHER, Karen REIMER, Karin GAWORA
  • FLUORINE CONTAINING COMPOUNDS AND METHODS OF USE THEREOF
    Publication number: 20120149900
    Abstract: Fluorinated compounds and methods of making fluorinated compounds are described herein.
    Type: Application
    Filed: January 8, 2010
    Publication date: June 14, 2012
    Inventors: Tobias Ritter, Laura Brass, Curtis Keith, Alan Watson, David J. Greenblatt
  • N-17-Alkylated Prodrugs of Opioids
    Publication number: 20120142718
    Abstract: Compounds of formula (II) R1R2R3N+—(C(R1a)(R2a))—Ar—Z—C(O)—Y—(C(R1)(R2))n—N—(R3)(R4)A?II, in which R1R2R3N+, R1a, R2a, Ar, Z, Y, R1, R2, n, R3, R4 and A? have the meanings given in the specification, are useful as prodrugs for opioids (Example 13).
    Type: Application
    Filed: February 15, 2008
    Publication date: June 7, 2012
    Inventors: Thomas E. Jenkins, Aleksandr Kolesnikov
  • Phenylethanoic Acid, Phenylpropanoic Acid and Phenylpropenoic Acid Conjugates and Prodrugs of Hydrocodone, Methods of Making and Use Thereof
    Publication number: 20120142720
    Abstract: The presently described technology provides phenylethanoic acid, phenylpropanoic acid, phenylpropenoic acid, a salt thereof, a derivative thereof or a combination thereof chemically conjugated to hydrocodone (morphinan-6-one, 4,5-alpha-epoxy-3-methoxy-17-methyl) to form novel prodrugs or compositions of hydrocodone which have a decreased potential for abuse of hydrocodone. The present technology also provides methods of treating patients, pharmaceutical kits and methods of synthesizing conjugates of the present technology.
    Type: Application
    Filed: July 1, 2010
    Publication date: June 7, 2012
    Applicant: KEMPHARM, INC.
    Inventors: Travis Mickle, Sven Guenther, Christal Mickle, Guochen Chi, Jaroslaw Kanski, Andrea K. Martin, Bindu Bera
  • PROCESS FOR THE DEMETHYLATION OF OXYCODONE AND RELATED COMPOUNDS
    Publication number: 20120142925
    Abstract: A process is provided for the N-demethylation of certain morphinans by reaction with ?-chloroethyl chloroformate followed by hydrolysis of the resulting intermediate.
    Type: Application
    Filed: May 25, 2007
    Publication date: June 7, 2012
    Applicant: ALPHARMA ApS
    Inventors: Ole Heine Kvernenes, Anne Mette Nygard, Audun Hegges, Harald Haivorsen
  • (S)-N-METHYLNALTREXONE
    Publication number: 20120136019
    Abstract: This invention relates to S-MNTX, methods of producing S-MNTX, pharmaceutical preparations comprising S-MNTX and methods for their use.
    Type: Application
    Filed: June 23, 2011
    Publication date: May 31, 2012
    Applicant: Progenics Pharmaceuticals, Inc.
    Inventors: Thomas A. Boyd, Howard Wagoner, Suketu P. Sanghvi, Christopher Verbicky, Stephen Andruski
  • Compounds and Compositions for Use in Phototherapy and in Treatment of Ocular Neovascular Disease and Cancers
    Publication number: 20120129879
    Abstract: 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.
    Type: Application
    Filed: July 16, 2010
    Publication date: May 24, 2012
    Inventors: Gary L. Cantrell, Raghavan Rajagopalan, David W. Berberich, Amolkumar Karwa, Richard B. Dorshow
  • Stereoselective reduction of a morphinone
    Patent number: 8183376
    Abstract: 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.
    Type: Grant
    Filed: April 19, 2007
    Date of Patent: May 22, 2012
    Assignee: Nektar Therapeutics
    Inventors: Lin Cheng, Michael D. Bentley
  • Sinomenine Derivatives and Processes for their Synthesis
    Publication number: 20120116086
    Abstract: 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: Application
    Filed: January 18, 2012
    Publication date: May 10, 2012
    Applicant: Mallinckrodt LLC
    Inventors: Peter X. Wang, Tao Jiang, Gary L. Cantrell, David W. Berberich, Bobby N. Trawick, Subo Liao, John Brandt
  • METHOD FOR THE MANUFACTURING OF NALTREXONE
    Publication number: 20120116085
    Abstract: 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: Application
    Filed: November 2, 2011
    Publication date: May 10, 2012
    Applicant: H. Lundbeck A/S
    Inventors: Carla De Faveri, Florian Anton Martin Huber, Mariano Stivanello
  • OPIOID AND OPIOID-LIKE COMPOUNDS AND USES THEREOF
    Publication number: 20120114599
    Abstract: The present invention relates to opioid and opioid-like compounds, and pharmaceutical formulations thereof, and use thereof for prevention and treatment of disorders such as septic shock and organ damage.
    Type: Application
    Filed: September 9, 2011
    Publication date: May 10, 2012
    Inventors: Edwin S.C. WU, Mao-Hsiung Yen, Chin-Tsai Fan
  • Process for the preparation of 6-beta hydroxy morphinan compounds
    Patent number: 8168790
    Abstract: 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.
    Type: Grant
    Filed: June 16, 2009
    Date of Patent: May 1, 2012
    Assignee: Mallinckrodt LLC
    Inventors: Jian Bao, Tao Jiang, Gary L. Cantrell
  • Demethylation of 14-hydroxy substituted alkaloid derivatives
    Patent number: 8158793
    Abstract: 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 formula R1OOC—N?N—COOR2 in a suitable solvent.
    Type: Grant
    Filed: November 24, 2008
    Date of Patent: April 17, 2012
    Assignee: Siegfried Ltd.
    Inventors: Erik Heinz Lauterbach, Thomas Dinkel, Sabrina Heller, Andreas Bertogg
  • ORAL FORMULATIONS AND LIPOPHILIC SALTS OF METHYLNALTREXONE
    Publication number: 20120070495
    Abstract: The present invention provides compositions comprising methylnaltrexone or a salt thereof, and compositions and formulations thereof, for oral administration.
    Type: Application
    Filed: March 10, 2011
    Publication date: March 22, 2012
    Applicant: WYETH LLC
    Inventors: Syed M. SHAH, Christopher Richard DIORIO, Eric C. EHRNSPERGER, Xu MENG, Kadum A. AL SHAREFFI, Jonathan Marc COHEN
  • Process for preparing oxymorphone
    Patent number: 8134002
    Abstract: 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.
    Type: Grant
    Filed: May 2, 2007
    Date of Patent: March 13, 2012
    Assignee: Penick Corporation
    Inventor: Bao-Shan Huang
  • PROCESSES FOR PREPARING MORPHINAN-6-ONE PRODUCTS WITH LOW LEVELS OF ALPHA BETA-UNSATURATED COMPOUNDS
    Publication number: 20120059167
    Abstract: 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: Application
    Filed: November 11, 2011
    Publication date: March 8, 2012
    Applicant: Mallinckrodt Inc.
    Inventors: Henry J. Buehler, William E. Dummitt, Anthony Mannino, Dennis C. Aubuchon, Hong Gu
  • PREPARATION OF OPIATE ANALGESICS BY REDUCTIVE ALKYLATION
    Publication number: 20120046466
    Abstract: 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 group or H; W is C(CH3)2OH, C(CH3)(C(CH3)3)OH or COCH3; Z is C2-C10 alkyl or C2-C10 arylalkyl; and is a single bond or a double bond, is disclosed. The process is a reductive alkylation in the presence of hydrogen and a reductive alkylation catalyst.
    Type: Application
    Filed: February 18, 2011
    Publication date: February 23, 2012
    Applicant: JOHNSON MATTHEY PUBLIC LIMITED COMPANY
    Inventors: Melville Mitchell, Neil Kenneth Thomson, George Scott Wilson, Neil John Goodwin, Maureen Joan Young
  • Processes for the Preparation of Morphinane and Morphinone Compounds
    Publication number: 20120046465
    Abstract: 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: Application
    Filed: April 22, 2010
    Publication date: February 23, 2012
    Inventors: Tomas Hudlicky, Robert Carroll, Hannes Leisch, Ales Machara, Lukas Werner, David R. Adams
  • Preparation of opiate analgesics by reductive alkylation
    Patent number: 8119803
    Abstract: 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 group or H; W is C(CH3)2OH, (CH3)(C(CH3)3)OH or COCH3; Z is C2-C10 alkyl or C2-C10 arylalkyl; and is a single bond or a double bond, is disclosed. The process includes reductive alkylation in the presence of hydrogen and a reductive alkylation catalyst.
    Type: Grant
    Filed: September 14, 2005
    Date of Patent: February 21, 2012
    Assignee: Johnson Matthey Public Limited Company
    Inventors: Melville Mitchell, Neil Kenneth Thomson, George Scott Wilson, Neil John Goodwin, Maureen Joan Young
  • N-Demethylation of 6-Keto Morphinans
    Publication number: 20120035366
    Abstract: 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: Application
    Filed: August 3, 2011
    Publication date: February 9, 2012
    Applicant: Mallinckrodt LLC
    Inventors: Peter X. Wang, Tao Jiang, David W. Berberich, Subo Liao
  • CRYSTALLINE FORMS OF OXYMORPHONE HYDROCHLORIDE
    Publication number: 20120022093
    Abstract: The present invention is directed to crystalline forms of oxymorphone hydrochloride.
    Type: Application
    Filed: July 21, 2011
    Publication date: January 26, 2012
    Inventors: Karen S. Gushurst, Leonard J. Chyall, Lien H. Koztecki, Brenton Skylar Wolfe
  • Process for the preparation of quaternary N-alkyl morphin or morphinan alkaloid derivatives
    Patent number: 8101756
    Abstract: 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.
    Type: Grant
    Filed: July 18, 2008
    Date of Patent: January 24, 2012
    Assignee: Siegfried Ltd.
    Inventors: Martin Eipert, Erik Heinz Lauterbach, Sabrina Heller, Thomas Dinkel, Stephanie Hake
  • Processes for the preparation of normorphinan salts
    Patent number: 8101757
    Abstract: 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.
    Type: Grant
    Filed: December 17, 2008
    Date of Patent: January 24, 2012
    Assignee: Mallinckrodt LLC
    Inventors: Peter X. Wang, Tao Jiang, Gary L. Cantrell, David W. Berberich, Jian Bao, Bobby N. Trawick
  • Process for the Synthesis of Substituted Morphinans
    Publication number: 20120010412
    Abstract: The present invention relates to a process for the synthesis of a compound of formula I:
    Type: Application
    Filed: April 28, 2011
    Publication date: January 12, 2012
    Applicant: Alkermes, Inc.
    Inventor: Scott Duncan
  • Methods for One-Pot N-Demethylation/N-Functionalization of Morphine and Tropane Alkaloids
    Publication number: 20110313163
    Abstract: The present invention provides a method for the N-demethylation and N-functionalization of an N-methylated heterocycle such as a morphine alkaloid or tropane alkaloid. The method comprises reacting the heterocycle with an functionalization agent in the presence of a transition metal catalyst in air or in the presence of an oxidant.
    Type: Application
    Filed: July 8, 2011
    Publication date: December 22, 2011
    Inventors: Tomas Hudlicky, Robert James Carroll, Hemes Lalush, Ales Machara, Lukas Werner, Mary Ann Endoma-Arias
  • LARGE SUBSTITUENT, NON-PHENOLIC OPIOIDS AND METHODS OF USE THEREOF
    Publication number: 20110306603
    Abstract: 8-Substituted-2,6-methano-3-benzazocines of general structure are useful as analgesics, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction medications.
    Type: Application
    Filed: August 23, 2011
    Publication date: December 15, 2011
    Applicant: RENSSELAER POLYTECHNIC INSTITUTE
    Inventor: Mark P. Wentland
  • Processes for the production of (+)- “Nal” morphinan compounds
    Patent number: 8067596
    Abstract: 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.
    Type: Grant
    Filed: December 17, 2008
    Date of Patent: November 29, 2011
    Assignee: Mallinckrodt LLC
    Inventors: Peter X. Wang, Tao Jiang, Gary L. Cantrell, David W. Berberich, Bobby N. Trawick, Subo Liao
  • Synthetic route to 14-hydroxyl opiates through 1-halo-thebaine or analogs
    Patent number: 8067597
    Abstract: Novel methods of synthesis of known and novel 14-hydroxyl opiates through 1-halothebaine and derivatives are described.
    Type: Grant
    Filed: May 22, 2006
    Date of Patent: November 29, 2011
    Assignee: Mallinckrodt LLC
    Inventors: Peter X. Wang, Frank W. Moser, Gary L. Cantrell, Daniel P. Magparangalan, Jian Bao
  • Process for preparing oxycodone having reduced levels of 14-hydroxycodeinone
    Patent number: 8058439
    Abstract: The present invention is directed to processes for preparing oxycodone base and oxycodone hydrochloride compositions having less than 10 ppm of 14-hydroxycodeinone.
    Type: Grant
    Filed: January 20, 2011
    Date of Patent: November 15, 2011
    Assignee: Noramco, Inc.
    Inventors: D. Phillip Cox, Yong Zhang, Wen-Chun Zhang, Karen E. James
  • Preparation of Saturated Ketone Morphinan Compounds Having Low Metal Content
    Publication number: 20110269963
    Abstract: 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: Application
    Filed: April 26, 2011
    Publication date: November 3, 2011
    Applicant: Mallinckrodt Inc.
    Inventors: Tao Jiang, Peter X. Wang, David W. Berberich
  • N-Alkylation of Opiates
    Publication number: 20110269964
    Abstract: The present invention provides an efficient process for preparing N-alkylated opiates. In particular, processes are provided for using a chloride-containing alkylating agent and a bromide or iodide salt to alkylate the corresponding nor-opiate.
    Type: Application
    Filed: April 28, 2011
    Publication date: November 3, 2011
    Applicant: Mallinckrodt Inc.
    Inventors: Jian Bao, Catherine E. Thomasson, Esa T. Jarvi
  • SYNTHESIS OF METABOLICALLY STABLE AGENTS FOR ALCOHOL AND DRUG ABUSE
    Publication number: 20110263630
    Abstract: Disclosed herein are compounds of formula (I); as defined herein, or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising the same, and methods of using these compounds for the treatment of substance addiction.
    Type: Application
    Filed: July 9, 2009
    Publication date: October 27, 2011
    Applicant: HUMAN BIOMOLECULAR RESEARCH INSTITUTE
    Inventor: John R. Cashman
  • ANALGESIC AGENTS
    Publication number: 20110251227
    Abstract: 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: Application
    Filed: July 10, 2009
    Publication date: October 13, 2011
    Applicant: REGENTS OF THE UNIVERSITY OF MINNESOTA
    Inventor: Philip S. Portoghese
  • Hybrid Opioid Compounds and Compositions
    Publication number: 20110245287
    Abstract: Disclosed are hybrid opioid compounds, mixed opioid salts, compositions comprising the hybrid opioid compounds and mixed opioid salts, and methods of use thereof. More particularly, in one aspect the hybrid opioid compound includes at least two opioid compounds that are covalently bonded to a linker moiety. In another aspect, the hybrid opioid compound relates to mixed opioid salts comprising at least two different opioid compounds or an opioid compound and a different active agent. Also disclosed are pharmaceutical compositions, as well as to methods of treating pain in humans using the hybrid compounds and mixed opioid salts.
    Type: Application
    Filed: February 9, 2011
    Publication date: October 6, 2011
    Inventors: John W. Holaday, Philip Magistro
  • Large substituent, non-phenolic opioids and methods of use thereof
    Patent number: 8026252
    Abstract: 8-Substituted-2,6-methano-3-benzazocines of general structure are useful as analgesics, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction medications.
    Type: Grant
    Filed: June 3, 2009
    Date of Patent: September 27, 2011
    Assignee: Rensselaer Polytechnic Institute
    Inventor: Mark P. Wentland
  • CARBOXAMIDE BIOISOSTERES OF OPIATES
    Publication number: 20110230511
    Abstract: A compound of formula I is disclosed. Compounds of formula I are useful as analgesics, anti-inflammatory agents, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction medications.
    Type: Application
    Filed: March 22, 2011
    Publication date: September 22, 2011
    Applicant: RENSSELAER POLYTECHNIC INSTITUTE
    Inventor: Mark P. Wentland
  • Process for the preparation of buprenorphine and derivatives for buprenorphine
    Patent number: 8017777
    Abstract: 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.
    Type: Grant
    Filed: December 17, 2008
    Date of Patent: September 13, 2011
    Assignee: Mallinckrodt LLC
    Inventors: Peter X. Wang, Tao Jiang, Gary L. Cantrell, David W. Berberich, Bobby N. Trawick, Subo Liao
  • 8-CARBOXAMIDO-2,6-METHANO-3-BENZAZOCINES
    Publication number: 20110207763
    Abstract: 8-Substituted-2,6-methano-3-benzazocines of general structure I in which A is —CH2—OH, —CH2NH2, —NHSO2CH3, and Y is O, S or NOH are useful as analgesics, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction medications. 8-Carboxamides, thiocarboxamides, hydroxyamidines and formamides are preferred.
    Type: Application
    Filed: May 9, 2011
    Publication date: August 25, 2011
    Applicant: RENSSELAER POLYTECHNIC INSTITUTE
    Inventor: Mark P. Wentland
  • ()--methylnaltrexone
    Patent number: 8003794
    Abstract: This invention relates to S-MNTX, methods of producing S-MNTX, pharmaceutical preparations comprising S-MNTX and methods for their use.
    Type: Grant
    Filed: July 20, 2009
    Date of Patent: August 23, 2011
    Assignee: Progenics Pharmaceuticals, Inc.
    Inventors: Thomas A. Boyd, Howard Wagoner, Suketu P. Sanghvi, Christopher Verbicky, Stephen Andruski
  • Methods for making 3-O-protected morphinones and 3-O-protected morphinone dienol carboxylates
    Patent number: 8003793
    Abstract: 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: Grant
    Filed: February 4, 2005
    Date of Patent: August 23, 2011
    Assignee: Purdue Pharma L.P.
    Inventor: Andreas Stumpf
  • Process for the preparation of 3-hydroxymorphinan derivatives
    Patent number: 7999105
    Abstract: Processes are described for the synthesis of 3-hydroxymorphinan derivatives by hydrolysis of side products from the O-demethylation of 3-methoxymorphinan derivatives.
    Type: Grant
    Filed: February 18, 2009
    Date of Patent: August 16, 2011
    Assignee: Mallinckrodt Inc.
    Inventors: Peter X. Wang, Tao Jiang, Gary L. Cantrell, David W. Berberich, Frank W. Moser, Jian Bao
  • Methods for one-pot -demethylation/-acylation of morphine and tropane alkaloids
    Patent number: 7999104
    Abstract: 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 catalyst.
    Type: Grant
    Filed: June 29, 2007
    Date of Patent: August 16, 2011
    Assignee: Brock University
    Inventors: Robert James Carroll, Hannes Leisch, Tomas Hudlicky, D. Phillip Cox
  • Process for the preparation of 6-alpha-hydroxy-N-alkylated opiates
    Patent number: 7985858
    Abstract: 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.
    Type: Grant
    Filed: May 2, 2008
    Date of Patent: July 26, 2011
    Assignee: Mallinckrodt Inc.
    Inventors: Christopher W. Grote, Peter X. Wang, Tao Jiang, Gary L. Cantrell, Frank W. Moser, Catherine E. Thomasson
  • USE OF OPIOID ANTAGONISTS FOR TREATING URINARY RETENTION
    Publication number: 20110177133
    Abstract: The invention pertains to the use of opioid antagonists for the treatment of urinary retention.
    Type: Application
    Filed: July 7, 2009
    Publication date: July 21, 2011
    Inventors: Michael Hopp, Petra Leyendecker
  • PROCESS FOR THE PREPARATION OF MORPHINE ANALOGUES
    Publication number: 20110152527
    Abstract: 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: Application
    Filed: March 23, 2009
    Publication date: June 23, 2011
    Inventors: Nileshkumar Sureshbhai Patel, Srinivasu Kilaru, Rajamannar Thennati
  • PROCESS FOR PREPARING OXYCODONE HAVING REDUCED LEVELS OF 14- HYDROXYCODEINONE
    Publication number: 20110144340
    Abstract: The present invention is directed to processes for preparing oxycodone base and oxycodone hydrochloride compositions having less than 10 ppm of 14-hydroxycodeinone.
    Type: Application
    Filed: January 20, 2011
    Publication date: June 16, 2011
    Inventors: D. Phillip Cox, Yong Zhang, Wen-Chun Zhang, Karen E. James
  • PREPARATION OF OPIATE ANALGESICS BY REDUCTIVE ALKYLATION
    Publication number: 20110144341
    Abstract: 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 group or H; W is C(CH3)2OH, C(CH3)(C(CH3)3)OH or COCH3; Z is C2-C10 alkyl or C2-C10 arylalkyl; and is a single bond or a double bond, is disclosed. The process is a reductive alkylation in the presence of hydrogen and a reductive alkylation catalyst.
    Type: Application
    Filed: February 18, 2011
    Publication date: June 16, 2011
    Applicant: JOHNSON MATTHEY PUBLIC LIMITED COMPANY
    Inventors: Melville Mitchell, Neil Kenneth Thomson, George Scott Wilson, Neil John Goodwin, Maureen Joan Young
  • (+)-Morphinans as Antagonists of Toll-Like Receptor 9 and Therapeutic Uses Thereof
    Publication number: 20110136845
    Abstract: 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.
    Type: Application
    Filed: December 22, 2010
    Publication date: June 9, 2011
    Applicant: Mallinckrodt Inc.
    Inventors: Bobby N. Trawick, David W. Berberich, Christopher W. Grote
  • MORPHINAN DERIVATIVES AND PREPARATION METHODS THEREOF
    Publication number: 20110112297
    Abstract: 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: Application
    Filed: June 19, 2009
    Publication date: May 12, 2011
    Applicant: Chongqing Pharmaceutical Research Institute Co., Ltd.
    Inventors: Huafu Sun, Jie Luo, Wenrun Ye, Jie Deng, Bo Lin, Chunyan Dan, Bin Fan