Nitrogen Or Divalent Chalcogen Double Bonded Directly To Carbocyclic Ring Of The Pentacyclo Ring System (e.g., Morphinones, Etc.) Patents (Class 546/45)
  • Patent number: 10752592
    Abstract: The present application relates to analogues of morphan and morphinan, compositions thereof, and methods for treating a disease or condition comprising administering an effective amount of the compounds or compositions to a subject in need thereof.
    Type: Grant
    Filed: March 25, 2019
    Date of Patent: August 25, 2020
    Assignee: ALKERMES PHARMA IRELAND LIMITED
    Inventors: Laura Cook Blumberg, Daniel R. Deaver, David J. Eyerman, Thomas Andrew Wynn
  • Patent number: 10736890
    Abstract: The present application relates methods for treating a depressive symptom comprising administering an effective amount of a ? opioid receptor agonist or a pharmaceutically acceptable salt thereof to a subject in need thereof. Non-limiting examples of such agonist include the compounds of Formulas I, II, III, and IV, as well as the compounds of Table A.
    Type: Grant
    Filed: February 11, 2019
    Date of Patent: August 11, 2020
    Assignee: ALKERMES PHARMA IRELAND LIMITED
    Inventors: Laura Cook Blumberg, Daniel R. Deaver, David J. Eyerman, Thomas Andrew Wynn
  • Patent number: 10649669
    Abstract: Improved processes for making opioid products having low impurity levels including making 14-hydroxycodeinone and 14-hydroxymorphinone from thebaine and oripavine, respectively.
    Type: Grant
    Filed: June 17, 2019
    Date of Patent: May 12, 2020
    Assignee: Johson Matthey Public Limited Company
    Inventors: Saroop Matharu, Brian Heinrich, Ewart Grant, Hongzhi Zhang
  • Patent number: 10407434
    Abstract: In certain embodiments the invention is directed to a process for preparing an oxycodone hydrochloride composition having less than 25 ppm of 14-hydroxycodeinone.
    Type: Grant
    Filed: January 30, 2019
    Date of Patent: September 10, 2019
    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
  • Patent number: 10324632
    Abstract: Improved processes for making opioid products having low impurity levels including making 14-hydroxycodeinone and 14-hydroxymorphinone from thebaine and oripavine, respectively.
    Type: Grant
    Filed: December 19, 2017
    Date of Patent: June 18, 2019
    Assignee: Johnson Matthey Public Limited Company
    Inventors: Saroop Matharu, Brian Heinrich, Ewart Grant, Hongzhi Zhang
  • Patent number: 10316042
    Abstract: Compounds and compositions for use as starting materials or intermediate materials in the preparation of opioids including, e.g., oxymorphone base and/or an oxymorphone salt; processes for preparing these compounds and compositions; uses of these compounds and compositions in the preparation of APIs and pharmaceutical dosage forms; and uses of said APIs and pharmaceutical dosage forms in the treatment of medical conditions.
    Type: Grant
    Filed: July 15, 2013
    Date of Patent: June 11, 2019
    Assignee: RHODES TECHNOLOGIES
    Inventors: Stuart James Gebbie, Joshua R. Giguere, Keith McCarthy, Lonn S. Rider
  • Patent number: 10227354
    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: March 12, 2019
    Assignee: Cody Laboratories, Inc.
    Inventors: Zinovy Itov, Vladimir F. Kuznetsov, Iouri Voitsekhovski
  • Patent number: 10202396
    Abstract: Compounds and compositions for use as starting materials or intermediate materials in the preparation of opioids including, e.g., oxycodone base and/or an oxycodone salt; processes for preparing these compounds and compositions; uses of these compounds and compositions in the preparation of APIs and pharmaceutical dosage forms; and uses of said APIs and pharmaceutical dosage forms in the treatment of medical conditions.
    Type: Grant
    Filed: September 11, 2017
    Date of Patent: February 12, 2019
    Assignee: RHODES TECHNOLOGIES
    Inventors: Stuart James Gebbie, Joshua R. Giguere, Keith McCarthy, Lonn S. Rider
  • Patent number: 9981978
    Abstract: There is provided a novel process for the preparation of a compound of formula I, wherein R1, R2 and R3 are as described in the description, by conversion of a corresponding allylic alcohol.
    Type: Grant
    Filed: July 23, 2014
    Date of Patent: May 29, 2018
    Assignee: Cambrex Charles City, Inc.
    Inventors: Michael Tracey, Pär Holmberg, Belén Lindberg Martín Matute, Antonio Bermejo Gómez, Jan-Erling Bäckvall
  • Patent number: 9932349
    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: Grant
    Filed: September 9, 2016
    Date of Patent: April 3, 2018
    Assignee: Rensselaer Polytechnic Institute
    Inventor: Mark P. Wentland
  • Patent number: 9657030
    Abstract: The present disclosure provides processes for the N-dealkylation of tertiary amines and the use of transition metal catalysts to prepare tertiary N-allyl amine derivatives and secondary amine derivatives thereof. The tertiary amines can be alkaloids and, more particularly, the tertiary amines can be opioids. In specific embodiments, the present disclosure provides methods for use in processes for the synthesis of naloxone and naltrexone from oripavine.
    Type: Grant
    Filed: August 14, 2015
    Date of Patent: May 23, 2017
    Assignee: Rhodes Technologies
    Inventors: Joshua Robert Giguere, Keith Edward McCarthy, Helge Alfred Reisch, Sergio Sandoval, Jake Larry Stymiest
  • Patent number: 9624232
    Abstract: The present disclosure provides processes for the N-dealkylation of tertiary amines and the use of transition metal catalysts to prepare tertiary N-allyl amine derivatives and secondary amine derivatives thereof. The tertiary amines can be alkaloids and, more particularly, the tertiary amines can be opioids. In specific embodiments, the present disclosure provides methods for use in processes for the synthesis of naloxone and naltrexone from oripavine.
    Type: Grant
    Filed: August 14, 2015
    Date of Patent: April 18, 2017
    Assignee: Rhodes Technologies
    Inventors: Joshua Robert Giguere, Keith Edward McCarthy, Helge Alfred Reisch, Sergio Sandoval, Jake Larry Stymiest
  • Patent number: 9522919
    Abstract: In certain embodiments the invention is directed to a process for preparing an oxycodone hydrochloride composition having less than 25 ppm of 14-hydroxycodeinone.
    Type: Grant
    Filed: May 29, 2015
    Date of Patent: December 20, 2016
    Assignees: Purdue Pharma L.P., P.F. Laboratories, Inc., Purdue Pharmaceuticals L.P., Rhodes Technologies
    Inventors: Robert Chapman, Lonn S. Rider, Qi Hong, Donald Kyle, Robert Kupper
  • Patent number: 9475823
    Abstract: The present application relates to methods for the preparation of morphine derivatives. In particular, the present application relates to methods for the preparation of hydromorphone from oripavine and oripavine from thebaine.
    Type: Grant
    Filed: February 6, 2015
    Date of Patent: October 25, 2016
    Inventors: Tomas Hudlicky, Mary Ann Endoma-Arias, Brennan Augusta Murphy, Ivan Snajdr, Ales Machara
  • Patent number: 9309257
    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: August 21, 2014
    Date of Patent: April 12, 2016
    Assignee: Cody Laboratories, Inc.
    Inventors: Zinovy Itov, Vladimir F. Kuznetsov, Iouri Voitsekhovski
  • Patent number: 9233972
    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: August 14, 2014
    Date of Patent: January 12, 2016
    Assignee: Cody Laboratories, Inc.
    Inventors: Zinovy Itov, Vladimir F. Kuznetsov, Iouri Voitsekhovski
  • Patent number: 9221830
    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: February 3, 2015
    Date of Patent: December 29, 2015
    Assignee: Alkermes Pharma Ireland Limited
    Inventors: Harry G. Brittain, David A. Dickason, Joyce M. Hotz, Shawn L. Lyons, J. Michael Ramstack, Steven G. Wright
  • Patent number: 9193737
    Abstract: The present invention provides a process for preparing a saturated 6,14-dihydroxy morphinan. The process comprises contacting an unsaturated 6-O-hydrocarbyl morphinan with hydrogen peroxide and an organic acid to form an unsaturated 6-keto-14-hydroxy morphinan. The unsaturated 6-keto-14-hydroxy morphinan is contacted with a first reducing agent to form an unsaturated 6,14-dihydroxy morphinan, and the unsaturated 6,14-dihydroxy morphinan is contacted with a second reducing agent to form the saturated 6,14-dihydroxy morphinan.
    Type: Grant
    Filed: November 5, 2014
    Date of Patent: November 24, 2015
    Assignee: Mallinckrodt LLC
    Inventors: Peter X. Wang, Tao Jiang
  • Patent number: 9127014
    Abstract: The present disclosure provides processes for the N-dealkylation of tertiary amines and the use of transition metal catalysts to prepare tertiary N-allyl amine derivatives and secondary amine derivatives thereof. The tertiary amines can be alkaloids and, more particularly, the tertiary amines can be opioids. In specific embodiments, the present disclosure provides methods for use in processes for the synthesis of naloxone and naltrexone from oripavine.
    Type: Grant
    Filed: December 11, 2012
    Date of Patent: September 8, 2015
    Assignee: Rhodes Technologies
    Inventors: Joshua Robert Giguere, Keith Edward McCarthy, Helge Alfred Reisch, Sergio Sandoval, Jake Larry Stymiest
  • Patent number: 9120800
    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: Grant
    Filed: February 5, 2014
    Date of Patent: September 1, 2015
    Assignee: Johnson Matthey Public Limited Company
    Inventors: Ewart Grant, Brian Heinrich, Saroop Matharu, Nicolas Archer
  • Patent number: 9108976
    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: August 21, 2014
    Date of Patent: August 18, 2015
    Assignee: Cody Laboratories, Inc.
    Inventors: Zinovy Itov, Vladimir F. Kuznetsov, Iouri Voitsekhovski
  • Patent number: 9090620
    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: August 21, 2014
    Date of Patent: July 28, 2015
    Assignee: Cody Laboratories, Inc.
    Inventors: Zinovy Itov, Vladimir F. Kuznetsov, Iouri Voitsekhovski
  • Patent number: 9073934
    Abstract: The present invention provides methods of N-demethylating, N-methylated heterocycles and N-methyl, N-oxide heterocycles using a transition metal with an oxidation state of zero, ferrocene or substituted derivatives thereof, or Cr3+. N-demethylated heterocycles prepared by the methods of the present invention are also provided.
    Type: Grant
    Filed: September 16, 2010
    Date of Patent: July 7, 2015
    Assignee: MONASH UNIVERSITY
    Inventors: Peter John Scammells, Gaik Orbell
  • Publication number: 20150148365
    Abstract: The present invention generally relates to processes for preparing highly pure morphinan-6-one products. The processes involve reducing the concentration of alpha, beta 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: October 2, 2014
    Publication date: May 28, 2015
    Inventors: Henry J. Buehler, William E. Dummitt, Anthony Mannino, Dennis C. Aubuchon, Hong Gu
  • Publication number: 20150148284
    Abstract: A method of providing a patient with controlled release of a phenolic opioid using a prodrug capable, upon enzymatic activation, of releasing the phenolic opioid through intra-molecular cyclization leading to formation of a cyclic urea, carbamate or thiocarbamate.
    Type: Application
    Filed: November 24, 2014
    Publication date: May 28, 2015
    Inventors: Thomas E. Jenkins, Aleksandr Kolesnikov
  • Publication number: 20150148368
    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: February 4, 2015
    Publication date: May 28, 2015
    Applicant: GRÜNENTHAL GMBH
    Inventors: Andreas FISCHER, Dagmar Peters-Groth, Dagmar Lischke
  • Publication number: 20150148537
    Abstract: The present invention relates to processes for removal of Michael acceptors from certain compositions wherein the composition is treated with a thiol-containing compound under conditions sufficient to remove Michael acceptors and the resulting thiol-Michael adducts. Certain embodiments of the present invention enable quantification and/or removal of Michael acceptors and/or Michael acceptor precursors.
    Type: Application
    Filed: December 30, 2014
    Publication date: May 28, 2015
    Applicant: Controlled Chemicals, Inc.
    Inventors: Jules A. Shafer, Vladislav V. Telyatnikov, Hao Wang
  • Patent number: 9040705
    Abstract: The present invention provides processes for the preparation of saturated ketone morphinan compounds. In particular, the invention provides processes for the conversion of a morphinan comprising an allyl alcohol ring moiety into a morphinan comprising a saturated ketone ring moiety by an isomerization reaction catalyzed by an inorganic salt of a late transition metal.
    Type: Grant
    Filed: April 9, 2010
    Date of Patent: May 26, 2015
    Assignee: Mallinckrodt LLC
    Inventors: Peter X. Wang, Tao Jiang, Narayanasamy Gurusamy, Catherine K. Jung
  • Publication number: 20150141451
    Abstract: The invention relates to the compounds of formula I and formula II or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I or formula II, and methods for treating chronic pain in a disease may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection.
    Type: Application
    Filed: February 24, 2013
    Publication date: May 21, 2015
    Inventor: Mahesh Kandula
  • Patent number: 9034893
    Abstract: The present invention relates to processes for removal of Michael acceptors from certain compositions wherein the composition is treated with a thiol-containing compound under conditions sufficient to remove Michael acceptors and the resulting thiol-Michael adducts. Certain embodiments of the present invention enable quantification and/or removal of Michael acceptors and/or Michael acceptor precursors.
    Type: Grant
    Filed: December 6, 2010
    Date of Patent: May 19, 2015
    Assignee: Controlled Chemicals, Inc.
    Inventors: Jules A. Shafer, Vladislav V. Telyatnikov, Hao Wang
  • Publication number: 20150133484
    Abstract: The invention relates to an improved method of preparing oxymorphone or a salt thereof from oripavine. In particular, the invention relates to a method of preparing oxymorphone with a content of alpha-beta-unsaturated ketones (ABUK) <10 ppm, wherein the content of 8,14-dihydroxydihydromorphinone in the prepared oxymorphone is >10 ppm.
    Type: Application
    Filed: June 11, 2013
    Publication date: May 14, 2015
    Applicant: Siegfried Generics International AG
    Inventor: Jianguang Sun
  • Publication number: 20150126742
    Abstract: The present invention provides a process for preparing a saturated 6,14-dihydroxy morphinan. The process comprises contacting an unsaturated 6-O-hydrocarbyl morphinan with hydrogen peroxide and an organic acid to form an unsaturated 6-keto-14-hydroxy morphinan. The unsaturated 6-keto-14-hydroxy morphinan is contacted with a first reducing agent to form an unsaturated 6,14-dihydroxy morphinan, and the unsaturated 6,14-dihydroxy morphinan is contacted with a second reducing agent to form the saturated 6,14-dihydroxy morphinan.
    Type: Application
    Filed: November 5, 2014
    Publication date: May 7, 2015
    Inventors: Peter X. Wang, Tao Jiang
  • Patent number: 9023860
    Abstract: Pro-drugs containing an electron withdrawing substituent, as defined in the specification, are useful in a method for providing a patient with post administration-activated, controlled release of a biologically active compound.
    Type: Grant
    Filed: November 26, 2008
    Date of Patent: May 5, 2015
    Assignee: Signature Therapeutics, Inc.
    Inventor: Thomas E. Jenkins
  • Patent number: 9012468
    Abstract: The present invention provides processes for preparing nal-opiates without the isolation of intermediates. In general, the process provides for alkylation and reduction in the same pot to give the nal-opiate.
    Type: Grant
    Filed: February 8, 2013
    Date of Patent: April 21, 2015
    Assignee: Mallinckrodt LLC
    Inventors: Peter X. Wang, Tao Jiang
  • Publication number: 20150099773
    Abstract: An improved process for the N-alkylation of tertiary morphinan alkaloid bases to form the corresponding quaternary morphinan alkaloid derivatives.
    Type: Application
    Filed: December 12, 2014
    Publication date: April 9, 2015
    Inventors: Peter X. Wang, Robert E. Halvachs, Kevin R. Roesch, Henry J. Buehler, Joseph P. Haar, Jr., Gary L. Cantrell
  • Publication number: 20150094471
    Abstract: The present application is directed to an efficient conversion of C-14 hydroxylated morphine alkaloids to various morphine analogs, such as naltrexone, naloxone and nalbuphone. One feature of this process is an intramolecular functional group transfer from the C-14 hydroxyl to the N-17 nitrogen atom following a palladium-catalyzed N-demethylation.
    Type: Application
    Filed: December 16, 2014
    Publication date: April 2, 2015
    Inventors: Tomas Hudlicky, Ales Machara
  • Publication number: 20150087839
    Abstract: The present disclosure provides improved methods for N-dealkylation of tertiary amines, including methods for N-demethylation of alkaloids and opioids, in which the dealkylation reaction is carried out in a solvent comprising a tertiary alcohol. The present disclosure also provides improved processes for preparing semi-synthetic opioids that incorporate the disclosed methods for N-dealkylation of tertiary amines.
    Type: Application
    Filed: December 2, 2014
    Publication date: March 26, 2015
    Inventors: Joshua Robert GIGUERE, Helge Alfred REISCH, Sergio SANDOVAL, Jake Larry STYMIEST
  • Patent number: 8980880
    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 10, 2012
    Date of Patent: March 17, 2015
    Assignee: Pisgah Laboratories, Inc.
    Inventors: Clifford Riley King, Stephen G. D'Ambrosio, David W. Bristol
  • Patent number: 8981098
    Abstract: The oxazolidine derived from the reaction of oxymorphone with the Burgess reagent, temporarily protected at O-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: Grant
    Filed: January 30, 2013
    Date of Patent: March 17, 2015
    Assignee: Brock University
    Inventors: Tomas Hudlicky, Mary Ann Endoma-Arias
  • Patent number: 8975272
    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: April 10, 2014
    Date of Patent: March 10, 2015
    Assignee: Alkermes, Inc.
    Inventors: Harry G. Brittain, David A. Dickason, Joyce M. Hotz, Shawn L. Lyons, J. Michael Ramstack, Steven G. Wright
  • Publication number: 20150065536
    Abstract: The presently described technology provides compositions comprising aryl carboxylic acids chemically conjugated to hydrocodone (morphinan-6-one, 4,5-alpha-epoxy-3-methoxy-17-methyl) to form novel prodrugs/compositions of hydrocodone, including benzoates and heteroaryl carboxylic acids, 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: November 6, 2014
    Publication date: March 5, 2015
    Inventors: Travis Mickle, Sven Guenther, Christal Mickle, Guochen Chi, Jaroslaw Kanski, Andrea K. Martin, Bindu Bera
  • Patent number: 8969368
    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: Grant
    Filed: November 27, 2013
    Date of Patent: March 3, 2015
    Assignee: Grünenthal GmbH
    Inventors: Andreas Fischer, Dagmar Peters-Groth, Dagmar Lischke
  • Patent number: 8962646
    Abstract: The invention relates to a compound of Formula I, II, III, IV or a pharmaceutically acceptable ester or prodrug thereof:
    Type: Grant
    Filed: June 29, 2012
    Date of Patent: February 24, 2015
    Assignee: Alkermes, Inc.
    Inventors: Laura Cook Blumberg, Derrick Arnelle
  • Patent number: 8962841
    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: Grant
    Filed: July 8, 2011
    Date of Patent: February 24, 2015
    Assignee: Brock University
    Inventors: Tomas Hudlicky, Robert James Carroll, Hannes Leisch, Ales Machara, Lukas Werner, Mary Ann Endoma-Arias
  • 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
  • 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
  • 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
  • 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
  • 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
  • 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