Nitrogen Or Divalent Chalcogen Double Bonded Directly To Carbocyclic Ring Of The Pentacyclo Ring System (e.g., Morphinones, Etc.) Patents (Class 546/45)
  • Sustained release solid formulations and methods of manufacturing the same
    Patent number: 8951557
    Abstract: Disclosed are a sustained release solid formulation comprising a drug, for example, oxycodone or its pharmaceutically acceptable salt, in a water-insoluble matrix, which comprises a wax type excipient and copovidone, and thus, has increased compressibility and fluidity and reduced adhesiveness, and a method of preparing the same.
    Type: Grant
    Filed: April 28, 2008
    Date of Patent: February 10, 2015
    Assignee: Hana Pharm. Co. Ltd.
    Inventors: Shajoung Chang, Oak Choi
  • PROCESS
    Publication number: 20150038715
    Abstract: The present invention provides a process for preparing an oxymorphone acid adduct, said process comprising hydrogenating an aqueous solution of 14-hydroxymorphinone and an acid to form a solution of the oxymorphone acid adduct, wherein the hydrogenation is carried out at one or more temperatures greater than 40° C. in the presence of a hydrogenation catalyst and hydrogen gas, wherein the level of 6?-oxymorphol produced is ?3.00 area % as determined by HPLC.
    Type: Application
    Filed: February 5, 2014
    Publication date: February 5, 2015
    Applicant: JOHNSON MATTHEY PUBLIC LIMITED COMPANY
    Inventors: EWART GRANT, BRIAN HEINRICH, SAROOP MATHARU, NICOLAS ARCHER
  • Abuse deterrent and anti-dose dumping pharmaceutical salts useful for the treatment of attention deficit/hyperactivity disorder
    Patent number: 8940729
    Abstract: A pharmaceutical composition comprising a drug substance consisting essentially of a pharmaceutically acceptable organic acid addition salt of an amine containing pharmaceutically active compound wherein the amine containing pharmaceutical active compound is selected from the group consisting of racemic or single isomer ritalinic acid or phenethylamine derivatives and the drug substance has a physical form selected from amorphous and polymorphic.
    Type: Grant
    Filed: April 11, 2012
    Date of Patent: January 27, 2015
    Assignee: Pisgah Laboratories, Inc.
    Inventors: Clifford Riley King, Stephen G. D'Ambrosio, David W. Bristol
  • Preparation of low impurity opiates in a continuous flow reactor
    Patent number: 8921557
    Abstract: The present invention relates to a novel process for preparing opiates or salts thereof. More particularly, the present invention relates to oxidizing the starting material in a continuous flow reactor, followed by either an isolation of the intermediate, or a direct reduction reaction.
    Type: Grant
    Filed: March 21, 2011
    Date of Patent: December 30, 2014
    Assignee: Siegfried AG
    Inventors: Beat Weber, Stefan Sahli
  • Preparation and use of (R),(R)-2,2?-bis-methylnaltrexone
    Patent number: 8916706
    Abstract: This invention relates to synthesis of (R),(R)-2,2?-bis-MNTX, as shown in Formula (I), and related methods and products.
    Type: Grant
    Filed: June 6, 2013
    Date of Patent: December 23, 2014
    Assignee: Progenics Pharmaceuticals, Inc.
    Inventors: Alfred A. Avey, Julio Perez
  • Process
    Patent number: 8916707
    Abstract: 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: Grant
    Filed: August 2, 2013
    Date of Patent: December 23, 2014
    Assignee: Johnson Matthey Public Limited Company
    Inventors: Nicolas Archer, Maureen Young, Timothy Davies, Amy Price, Michael Bease, Barbara Jamieson, Ewart Grant, Brian Heinrich, Saroop Matharu
  • (S)--methylnaltrexone
    Patent number: 8916581
    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: June 23, 2011
    Date of Patent: December 23, 2014
    Assignee: Progenics Pharmaceuticals, Inc.
    Inventors: Thomas A. Boyd, Howard Wagoner, Suketu P. Sanghvi, Christopher Verbicky, Stephen Andruski
  • PROCESS FOR THE PREPARATION OF MORPHINE ANALOGS VIA THE REACTION OF ORGANOMETALLIC REAGENTS WITH AN OXAZOLIDINE DERIVED FROM MORPHINANS
    Publication number: 20140371458
    Abstract: The oxazolidine derived from the reaction of oxymorphone with the Burgess reagent, temporarily protected at 0-3 and C-6, reacts with Grignard or other suitable metallic or organometallic reagents to directly provide, for example, A/-allyl, A/-methylcyclopropyl and /V-methylcyclobutyl derivatives that are further converted into naltrexone, naloxone, nalbuphone and nalbuphine in excellent yields. These morphine analogs can be prepared from the oxazolidine in a one-pot synthesis.
    Type: Application
    Filed: January 30, 2013
    Publication date: December 18, 2014
    Applicant: Brock University
    Inventors: Tomas HUDLICKY, Mary Ann ENDOMA-ARIAS
  • 5-METHYLDIHYDROMORPHONE COMPOUNDS FOR TREATMENT OF PAIN
    Publication number: 20140323416
    Abstract: The aspects of the present disclosure are directed to novel compounds, formulations containing said compounds or pharmaceutically acceptable salts thereof which are suitable for administration to a patient. In particular, to 5-methyldihydromorphone prodrug compounds described in general Formula I and II and the use of the compounds for treating pain associated with a variety of chronic human disorders including for example neuropathic pain and pain associated with cancer, surgeries or injuries.
    Type: Application
    Filed: April 16, 2014
    Publication date: October 30, 2014
    Inventors: Anthony MARFAT, Peter CORNELIUS, Robert VOLKMANN, Panayiotis ZAGOURAS, Frederick Raymond NELSON, Anton Franz Joseph FLIRI
  • Process for preparing morphinan-6-one products with low levels of ?,?-unsaturated ketone compounds
    Patent number: 8871779
    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: Grant
    Filed: March 2, 2007
    Date of Patent: October 28, 2014
    Assignee: Mallinckrodt LLC
    Inventors: Henry J. Buehler, William E. Dummitt, Anthony Mannino, Dennis C. Aubuchon, Hong Gu
  • Polymorphic Forms of Naltrexone
    Publication number: 20140303200
    Abstract: This invention relates to the discovery of novel polymorphic forms of naltrexone, including solvates, hydrates, anhydrous and other crystalline forms and combinations thereof. These novel forms of naltrexone impart advantages in pharmaceutical formulations incorporating them, including sustained release, or long acting, formulations.
    Type: Application
    Filed: April 10, 2014
    Publication date: October 9, 2014
    Applicant: Alkermes, Inc.
    Inventors: Harry G. Brittain, David A. Dickason, Joyce M. Hotz, Shawn L. Lyons, J. Michael Ramstack, Steven G. Wright
  • Process for reducing the 6-keto group of a morphinan alkaloid to the 6-hydroxy group by hydrogenation
    Patent number: 8853402
    Abstract: 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: Grant
    Filed: August 13, 2010
    Date of Patent: October 7, 2014
    Assignee: Johnson Matthey Public Limited Company
    Inventors: George Scott Wilson, Maureen Joan Young
  • Peripheral opioid receptor antagonists and uses thereof
    Patent number: 8853232
    Abstract: 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: Grant
    Filed: September 4, 2013
    Date of Patent: October 7, 2014
    Assignees: Wyeth LLC, Progenics Pharmaceuticals., Inc.
    Inventors: Alfred A. Avey, Appavu Chandrasekaren, Harold D. Doshan, Julio Perez, Yakov Rotshteyn
  • Preparation of 14-hydroxycodeinone sulfate
    Patent number: 8846923
    Abstract: Synthetic methods are provided for preparation of oxycodone and salts thereof with an improved impurity profile. Thebaine is converted to 14-hydroxycodeinone sulfate intermediate to minimize a 7,8-dihydro-8,14-dihydroxycodeinone impurity. Efficient methods for conversion of oxycodone base to oxycodone hydrochloride are provided to minimize 14-hydroxycodeinone impurity in the final product.
    Type: Grant
    Filed: December 18, 2013
    Date of Patent: September 30, 2014
    Assignee: Cody Laboratories, Inc.
    Inventors: Zinovy Itov, Vladimir F. Kuznetsov, Iouri Voitsekhovski
  • Process for recovery of nalmefene hydrochloride
    Patent number: 8841452
    Abstract: 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: Grant
    Filed: December 6, 2012
    Date of Patent: September 23, 2014
    Assignee: H. Lundbeck A/S
    Inventors: Carla De Faveri, Mariano Stivanello
  • ABUSE DETERRENT COMPOSITIONS AND METHODS OF USE
    Publication number: 20140275149
    Abstract: Orally administrable pharmaceutical compositions, methods of administration, and methods of making the same are provided. The pharmaceutical compositions provide abuse deterrent properties.
    Type: Application
    Filed: March 18, 2014
    Publication date: September 18, 2014
    Applicant: Inspirion Delivery Technologies, LLC
    Inventors: Manish S. Shah, Ray J. DiFalco, Stefan Aigner
  • MACROCYCLIC COMPOUNDS AS PROTEIN KINASE INHIBITORS
    Publication number: 20140256717
    Abstract: There is provided compounds of formula I, wherein R1, R2a, R2b, R2c, X, Y, Z, R3 and ring A/B have meanings given in the description, and pharmaceutically-acceptable esters, amides, solvates or salts thereof, which compounds are useful in the treatment of diseases in which inhibition of a protein or lipid kinase (e.g. PI3-K, particularly class I PI3K, PIM family kinase and/or mTOR) is desired and/or required, and particularly in the treatment of cancer. The invention also relates to combinations containing such compounds.
    Type: Application
    Filed: May 18, 2012
    Publication date: September 11, 2014
    Applicant: Centro Nacional de Investigaciones Oncológicas (CNIO)
    Inventors: Joaquín Pastor Fernández, Rosa Maria Álvarez Escobar, Rosario Concepción Riesco Fagundo, Ana Belén García García, Antonio Rodríguez Hergueta, Jose Ignacio Martin Hernando, Carmen Blanco Aparicio, David Álvaro Cebrián Muñoz
  • 6-AMIDO DERIVATIVES OF 4, 5-a EPOXYMORPHINANS FOR THE TREATMENT OF PAIN
    Publication number: 20140255308
    Abstract: 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: Application
    Filed: May 19, 2014
    Publication date: September 11, 2014
    Applicant: MEMORIAL SLOAN-KETTERING CANCER CENTER
    Inventors: Gavril Pasternak, Susruta Majumdar
  • 8a,14-dihydroxy-7,8-dihydrocodeinone
    Patent number: 8822687
    Abstract: 8?,14-Dihydroxy-7,8-dihydrocodeinone is described.
    Type: Grant
    Filed: February 24, 2010
    Date of Patent: September 2, 2014
    Assignees: Purdue Pharma L.P., The P.F. Laboratories, Inc., Purdue Pharmaceuticals L.P., Rhodes Technologies
    Inventors: Robert Chapman, Lonn S. Rider, Qi Hong, Donald Kyle, Robert Kupper
  • Crystals of morphinan derivative, manufacturing method thereof, and pharmaceutical composition using the same
    Patent number: 8816084
    Abstract: 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: Grant
    Filed: January 28, 2014
    Date of Patent: August 26, 2014
    Assignee: Everlight Chemical Industrial Corporation
    Inventors: Yuan-Yi Wang, Yu-Kai Li, Yu-Ting Su, Chia-Chen Hung, Chi-Hsiang Yao
  • METHOD OF PREPARING BUPRENORPHINE
    Publication number: 20140235860
    Abstract: An improved process for preparing buprenorphine and a method for increasing the yield of buprenorphine or a derivative thereof.
    Type: Application
    Filed: October 1, 2012
    Publication date: August 21, 2014
    Applicant: JOHNSON MATTEY PUBLIC LIMITED COMPANY
    Inventors: Nicolas Archer, David August, Michael Bease, Barbara Jamieson, Robert S. Marmor
  • USE OF OPIOID ANTAGONISTS FOR TREATING URINARY RETENTION
    Publication number: 20140220146
    Abstract: The invention pertains to the use of opiod antagonists for the treatment of urinary retention.
    Type: Application
    Filed: April 10, 2014
    Publication date: August 7, 2014
    Applicant: Euro-Celtique S.A.
    Inventors: Michael HOPP, Petra LEYENDECKER
  • METHODS FOR MAKING 3-O-PROTECTED MORPHINONES AND 3-O-PROTECTED MORPHINONE DIENOL CARBOXYLATES
    Publication number: 20140171643
    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: Application
    Filed: February 24, 2014
    Publication date: June 19, 2014
    Applicant: Purdue Pharma L.P.
    Inventor: Andreas STUMPF
  • Processes for preparing morphinan-6-one products with low levels of alpha beta-unsaturated compounds
    Patent number: 8748611
    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: Grant
    Filed: November 11, 2011
    Date of Patent: June 10, 2014
    Assignee: Mallinckrodt LLC
    Inventors: Henry J. Buehler, William E. Dummitt, Anthony Mannino, Dennis C. Aubuchon, Hong Gu
  • METHOD FOR THE MANUFACTURING OF NALTREXONE
    Publication number: 20140155608
    Abstract: 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: Application
    Filed: May 2, 2013
    Publication date: June 5, 2014
    Inventors: Carla De Faveri, Mariano Stivanello, Florian Anton Martin Huber
  • Polymorphic forms of naltrexone
    Patent number: 8735420
    Abstract: This invention relates to the discovery of novel polymorphic forms of naltrexone, including solvates, hydrates, anhydrous and other crystalline forms and combinations thereof. These novel forms of naltrexone impart advantages in pharmaceutical formulations incorporating them, including sustained release, or long acting, formulations.
    Type: Grant
    Filed: November 30, 2012
    Date of Patent: May 27, 2014
    Assignee: Alkermes, Inc.
    Inventors: Harry G. Brittain, David A. Dickason, Joyce M. Hotz, Shawn L. Lyons, J. Michael Ramstack, Steven G. Wright
  • PERIPHERAL OPIOID RECEPTOR ANTAGONISTS AND USES THEREOF
    Publication number: 20140142132
    Abstract: 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: Application
    Filed: September 4, 2013
    Publication date: May 22, 2014
    Applicants: WYETH, LLC, PROGENICS PHARMACEUTICALS, INC.
    Inventors: Alfred A. Avey, Appavu Chandrasekaren, Harold D. Doshan, Julio Perez, Yakov Rotshteyn
  • Abuse deterrent and anti-dose dumping pharmaceutical salts useful for the treatment of attention deficit/hyperactivity disorder
    Patent number: 8716278
    Abstract: A pharmaceutical composition comprising a drug substance consisting essentially of a pharmaceutically acceptable organic acid addition salt of an amine containing pharmaceutically active compound wherein the amine containing pharmaceutical active compound is selected from the group consisting of racemic or single isomer ritalinic acid or phenethylamine derivatives and the drug substance has a physical form selected from amorphous and polymorphic.
    Type: Grant
    Filed: April 11, 2012
    Date of Patent: May 6, 2014
    Assignee: Pisgah Laboratories, Inc.
    Inventors: Clifford Riley King, Stephen G. D'Ambrosio, David W. Bristol
  • Tandem process for preparing N-alkyl morphinans
    Patent number: 8703949
    Abstract: 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: Grant
    Filed: August 3, 2011
    Date of Patent: April 22, 2014
    Assignee: Mallinckrodt LLC
    Inventors: Subo Liao, Peter X. Wang, David W. Berberich, Douglas C. Miller
  • Low ABUK oxycodone, its salts and methods of making same
    Patent number: 8703950
    Abstract: 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: Grant
    Filed: July 1, 2011
    Date of Patent: April 22, 2014
    Assignee: Johnson Matthey Public Limited Co.
    Inventors: Erno M. Keskeny, James J. Mencel, Jen-Sen Dung
  • QUATERNARY OPIOID CARBOXAMIDES
    Publication number: 20140107143
    Abstract: Compounds of formulas: are disclosed. The compounds are useful for ameliorating the side effects of therapeutic opiates.
    Type: Application
    Filed: September 27, 2013
    Publication date: April 17, 2014
    Applicant: Rensselaer Polytechnic Institute
    Inventor: Mark P. WENTLAND
  • Treatment with opioid antagonists and mTOR inhibitors
    Patent number: 8685995
    Abstract: Embodiments of the invention provide methods of treating a disorder or disease characterized by cellular proliferation and migration by co-administering a synergistically effective amount of an mTOR inhibitor and a ?-opioid receptor antagonist.
    Type: Grant
    Filed: March 20, 2009
    Date of Patent: April 1, 2014
    Assignee: The University of Chicago
    Inventors: Jonathan Moss, Patrick A. Singleton
  • CRYSTALLINE, ANHYDROUS FORMS OF OXYMORPHONE HYDROCHLORIDE
    Publication number: 20140088132
    Abstract: Crystalline, anhydrous hydrochloride salts of 4,5?-epoxy-3,14-dihydroxy-17-methylmorphinan-6-one (oxymorphone) are disclosed and three polymorphic forms of these salts are reported. The invention further relates to a method for the production of such salts, a pharmaceutical composition comprising an effective amount of such a salt and such a salt as a medicament and for the treatment and/or prevention of pain.
    Type: Application
    Filed: November 27, 2013
    Publication date: March 27, 2014
    Applicant: GRÜNENTHAL GMBH
    Inventors: Andreas FISCHER, Dagmar PETERS-GROTH, Dagmar LISCHKE
  • Process for the preparation of quaternary N-alkyl morphinan alkaloid salts
    Patent number: 8669366
    Abstract: An improved process for the N-alkylation of tertiary morphinan alkaloid bases to form the corresponding quaternary morphinan alkaloid derivatives.
    Type: Grant
    Filed: March 6, 2008
    Date of Patent: March 11, 2014
    Assignee: Mallinckrodt LLC
    Inventors: Peter X. Wang, Gary L. Cantrell, Robert E. Halvachs, Kevin R. Roesch, Henry J. Buehler, Joseph P. Haar, Jr.
  • PROCESS FOR PREPARING OXYMORPHONE, NALTREXONE, AND BUPRENORPHINE
    Publication number: 20140051861
    Abstract: Methods are provided which include converting oripavine to other opiates, including converting oripavine to naltrexone, buprenorphine, 14-hydroxymorphinone and/or converting 14-hydroxymorphinone to oxymorphone. Purification and salt formation are optionally included.
    Type: Application
    Filed: October 23, 2013
    Publication date: February 20, 2014
    Applicant: PENICK CORPORATION
    Inventor: Bao-Shan HUANG
  • Enhancing transdermal delivery of opioid antagonists and agonists using codrugs linked to bupropion or hydroxybupropion
    Patent number: 8653271
    Abstract: 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: Grant
    Filed: October 18, 2007
    Date of Patent: February 18, 2014
    Assignee: University of Kentucky Research Foundation
    Inventors: Audra L. Stinchcomb, Peter A. Crooks, Mohamed O. Hamad, Paul K. Kiptoo
  • Abuse deterrent and anti-dose dumping pharmaceutical salts useful for the treatment of attention deficit/hyperactivity disorder
    Patent number: 8653065
    Abstract: A pharmaceutical composition comprising a drug substance consisting essentially of a pharmaceutically acceptable organic acid addition salt of an amine containing pharmaceutically active compound wherein the amine containing pharmaceutical active compound is selected from the group consisting of racemic or single isomer ritalinic acid or phenethylamine derivatives and the drug substance has a physical form selected from amorphous and polymorphic.
    Type: Grant
    Filed: April 11, 2012
    Date of Patent: February 18, 2014
    Assignee: Pisgah Laboratories, Inc.
    Inventors: Clifford Riley King, Stephen G. D'Ambrosio, David W. Bristol
  • PROCESS
    Publication number: 20140045876
    Abstract: 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: Application
    Filed: August 2, 2013
    Publication date: February 13, 2014
    Applicant: JOHNSON MATTHEY PUBLIC LIMITED COMPANY
    Inventors: NICOLAS ARCHER, MAUREEN YOUNG, TIMOTHY DAVIES, AMY PRICE, MICHAEL BEASE, BARBARA JAMIESON, EWART GRANT, BRIAN HEINRICH, SAROOP MATHARU
  • (+)-6-Hydroxy-Morphinan or (+)-6-Amino-Morphinan Derivatives
    Publication number: 20140031543
    Abstract: 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: Application
    Filed: October 3, 2013
    Publication date: January 30, 2014
    Applicant: Mallinckrodt LLC
    Inventors: Christopher W. Grote, Amruta R. Poreddy
  • Production of alkaloids without the isolation of intermediates
    Patent number: 8624031
    Abstract: The invention relates to processes for the production of alkaloids without the isolation of intermediates.
    Type: Grant
    Filed: September 7, 2012
    Date of Patent: January 7, 2014
    Assignee: Mallinckrodt LLC
    Inventors: Peter X. Wang, Tao Jiang, David W. Berberich
  • 3-oxy-hydromorphone derivatives
    Patent number: 8623888
    Abstract: The present invention provides 3-oxy-hydromorphone derivatives, and in particular, 3-ester, 3-carbonate, and 3-sulfonate derivatives of hydromorphone.
    Type: Grant
    Filed: July 9, 2010
    Date of Patent: January 7, 2014
    Assignee: Mallinckrodt LLC
    Inventors: Gary L. Cantrell, Robert E. Halvachs, Frank W. Moser, David W. Berberich, Peter X. Wang
  • N-demethylation of 6-keto morphinans
    Patent number: 8624030
    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: Grant
    Filed: August 3, 2011
    Date of Patent: January 7, 2014
    Assignee: Mallinckrodt LLC
    Inventors: Peter X. Wang, Tao Jiang, David W. Berberich, Subo Liao
  • CRYSTAL FORMS OF (R)-N-METHYLNALTREXONE BROMIDE AND USES THEREOF
    Publication number: 20140004188
    Abstract: The present invention provides a new forms of (R)—N-methylnaltrexone, and compositions thereof, useful as a peripheral mu opioid receptor antagonist.
    Type: Application
    Filed: November 21, 2012
    Publication date: January 2, 2014
    Inventors: Progenics Pharmaceuticals, Inc., Wyeth, LLC
  • LARGE SUBSTITUENT, NON-PHENOLIC OPIOIDS AND METHODS OF USE THEREOF
    Publication number: 20130345251
    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, 2013
    Publication date: December 26, 2013
    Applicant: Rensselaer Polytechnic Institute
    Inventor: Mark P. WENTLAND
  • SYNTHESIS OF R-N-METHYLNALTREXONE
    Publication number: 20130323286
    Abstract: This invention relates to stereoselective synthesis of R-MNTX and intermediates thereof, pharmaceutical preparations comprising R-MNTX or intermediates thereof and methods for their use.
    Type: Application
    Filed: November 7, 2012
    Publication date: December 5, 2013
    Applicant: PROGENICS PHARMACEUTICALS, INC.
    Inventor: Progenics Pharmaceuticals, Inc.
  • Preparation of nalmefene hydrochloride from naltrexone
    Patent number: 8598352
    Abstract: 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: Grant
    Filed: May 21, 2010
    Date of Patent: December 3, 2013
    Assignee: H. Lundbeck A/S
    Inventors: Carla De Faveri, Mauro Casarin, Michele Brusegan
  • Method for the manufacturing of naltrexone
    Patent number: 8580963
    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: Grant
    Filed: November 2, 2011
    Date of Patent: November 12, 2013
    Assignee: H. Lundbeck A/S
    Inventors: Carla De Faveri, Florian Anton Martin Huber, Mariano Stivanello
  • PREPARATION AND USE OF (R),(R)-2,2'-BIS-METHYLNALTREXONE
    Publication number: 20130296570
    Abstract: This invention relates to synthesis of (R),(R)-2,2?-bis-MNTX, as shown in Formula (I), and related methods and products.
    Type: Application
    Filed: June 6, 2013
    Publication date: November 7, 2013
    Inventors: Alfred A. Avey, Julio Perez
  • Morphinan derivatives and preparation methods thereof
    Patent number: 8563721
    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: Grant
    Filed: June 19, 2009
    Date of Patent: October 22, 2013
    Assignee: Chongqing Pharmaceutical Research Institute Co., Ltd.
    Inventors: Huafu Sun, Jie Luo, Wenrun Ye, Jie Deng, Bo Lin, Chunyan Dan, Bin Fan
  • Crystalline forms of oxymorphone hydrochloride
    Patent number: 8563571
    Abstract: The present invention is directed to crystalline forms of oxymorphone hydrochloride.
    Type: Grant
    Filed: July 21, 2011
    Date of Patent: October 22, 2013
    Assignee: Noramco, Inc.
    Inventors: Karen S. Gushurst, Leonard J. Chyall, Lien H. Koztecki, Brenton Skylar Wolfe