Nitrogen Or Divalent Chalcogen Double Bonded Directly To Carbocyclic Ring Of The Pentacyclo Ring System (e.g., Morphinones, Etc.) Patents (Class 546/45)
  • Opioid-Ketamine and Norketamine Codrug Combinations for Pain Management
    Publication number: 20110112131
    Abstract: 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: Application
    Filed: March 27, 2009
    Publication date: May 12, 2011
    Applicant: University of Kentucky Research Foundation A144 ASTeCC Building
    Inventors: Joseph R. Holtman, Peter A. Crooks, Ujjwal Chakraborty
  • Opioid-Nornicotine Codrugs Combinations for Pain Management
    Publication number: 20110112130
    Abstract: 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: Application
    Filed: March 27, 2009
    Publication date: May 12, 2011
    Applicant: University of Kentucky Research Foundation
    Inventors: Joseph R. Holtman, Peter A. Crooks, Ujjwal Chakraborty
  • Method of reducing ?, ? unsaturated ketones in opioid compositions
    Patent number: 7939543
    Abstract: The present invention is directed to a process for reducing the level of ?, ?-unsaturated ketone in an opioid analgesic composition by hydrogenation the opioid analgesic composition with diimide or a diimide progenitor.
    Type: Grant
    Filed: February 27, 2006
    Date of Patent: May 10, 2011
    Assignee: Purdue Pharma L.P.
    Inventor: Robert J. Kupper
  • PREPARATION AND USE OF (R),(R)-2,2'-BIS-METHYLNALTREXONE
    Publication number: 20110100099
    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: February 6, 2008
    Publication date: May 5, 2011
    Applicant: Progenics Pharmaceuticals, Inc.
    Inventors: Alfred A. Avey, Julio Perez
  • Methods for -demethylation of morphine and tropane alkaloids
    Patent number: 7935820
    Abstract: The present invention provides a method for the N-demethylation of an N-methylated heterocycle, particularly a morphine or tropane alkaloid or derivative thereof. The method comprises reacting the heterocycle with a metal catalyst and a solvent in the presence of an oxidizing agent.
    Type: Grant
    Filed: June 29, 2007
    Date of Patent: May 3, 2011
    Assignee: Brock University
    Inventors: Robert James Carroll, Hannes Leisch, Tomas Hudlicky
  • Method for separation and purification of naltrexone by preparative chromatography
    Patent number: 7935821
    Abstract: A process for the purification of an impure preparation containing naltrexone by means of a reverse phase preparative chromatography process is provided. In an illustrative embodiment a chromatographic column is loaded with a stationary phase, typically a silica particle having an organic ligand bound thereto. With a loading ratio of from about 10 to about 1000 the impure preparation is acidified and passed through the column. The column is eluted with typically an aqueous solution with acetonitrile and the purified naltrexone is obtained in a specified fraction.
    Type: Grant
    Filed: June 7, 2006
    Date of Patent: May 3, 2011
    Assignee: Mallinckrodt Inc.
    Inventor: Enrico A. Antonini
  • Conversion of thebaine to morphine derivatives
    Patent number: 7928234
    Abstract: The present invention provides methods for the conversion of thebaine to a morphine derivative, such as hydrocodone. Novel ketal intermediates of the conversion are provided. A one-pot procedure for the conversion comprises treating thebaine with an acid in the presence of a metal catalyst.
    Type: Grant
    Filed: June 29, 2007
    Date of Patent: April 19, 2011
    Assignee: Brock University
    Inventors: Robert James Carroll, Hannes Leisch, Tomas Hudlicky
  • Process for the Preparation of Quaternary N-Alkyl Morphinan Alkaloid Salts
    Publication number: 20110082297
    Abstract: An improved process for the N-alkylation of tertiary morphinan alkaloid bases to form the corresponding quaternary morphinan alkaloid derivatives.
    Type: Application
    Filed: March 6, 2008
    Publication date: April 7, 2011
    Inventors: Peter X. Wang, Gary L. Cantrell, Robert E. Halvachs, Kevin R. Roesch, Henry J. Buehler, Joseph P. Haar, JR.
  • Methods for Producing Hydrocodone, Hydromorphone or a Derivative Thereof
    Publication number: 20110071297
    Abstract: The present disclosure generally relates to methods for producing opioid derivatives. More particularly, the present disclosure relates to the preparation of hydromorphone, hydrocodone, or a derivative thereof, by means of a non-catalytic hydrogenation reaction of thebaine, oripavine or a derivative thereof, respectively, using a hydrazide reagent, followed by hydrolysis of the hydrogenated intermediate at a low temperature and for a short period of time. Additionally, the present disclosure relates to a composition comprising the desired hydromorphone, hydrocodone, or a derivative thereof, in combination with a 6-beta compound that is structurally related thereto.
    Type: Application
    Filed: September 20, 2010
    Publication date: March 24, 2011
    Applicant: Mallinckrodt inc.
    Inventors: Brian Orr, William E. Dummitt
  • Heterogeneous Ruthenium Metal Catalyst for the Production of Hydrocodone, Hydromorphone or a Derivative Thereof
    Publication number: 20110071016
    Abstract: The present disclosure generally relates to catalytic methods for producing opioid derivatives. More particularly, the present disclosure relates to the preparation of hydrocodone, hydromorphone, or a derivative thereof, by means of a conversion or an isomerization of codeine, morphine, or a derivative thereof, respectively, using a heterogeneous ruthenium metal catalyst.
    Type: Application
    Filed: September 21, 2010
    Publication date: March 24, 2011
    Applicant: Mallinckrodt Inc.
    Inventor: David E. GINDELBERGER
  • Preparation of 10-Keto Morphinans by Benzylic Oxidation
    Publication number: 20110071296
    Abstract: The present invention provides processes for the preparation of 10-keto and/or 10-hydroxy morphinans. In particular, the invention provides to processes for preparing a 10-keto morphinan by chromium-catalyzed benzylic oxidation of a morphinan with a periodic acid.
    Type: Application
    Filed: September 7, 2010
    Publication date: March 24, 2011
    Applicant: Mallinckrodt Inc.
    Inventors: Hang Sun, John E. Johnson, JR., Ricky L. Fenton, Sarah M. Dorn
  • Process for preparing oxycodone having reduced levels of 14-hydroxycodeinone
    Patent number: 7906647
    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: December 4, 2007
    Date of Patent: March 15, 2011
    Assignee: Noramco, Inc.
    Inventors: D. Phillip Cox, Yong Zhang, Wen-Chun Zhang, Karen E. James
  • Multi-Day Delivery Of Biologically Active Substances
    Publication number: 20110046599
    Abstract: Compositions and methods for modifying biologically active substances to achieve multi-day delivery of such substances, particularly through oral or parenteral administration, are disclosed. The compositions include the biologically active substance conjugated to a carrier having a suitably long half life, typically more than one day, wherein the conjugate optionally contains a spacer linking the carrier to the biologically active substance. Pharmaceutical formulations of the conjugates are also disclosed, as are methods of extending delivery of a single dose of a biologically active substance for more than one day.
    Type: Application
    Filed: June 26, 2008
    Publication date: February 24, 2011
    Inventor: Agis Kydonieus
  • Process for the synthesis of morphinane compounds and intermediates thereof
    Patent number: 7875718
    Abstract: This invention relates to intermediates useful in the preparation of opiate alkaloids, particularly morphinane compounds. The invention also relates to processes for preparing such intermediates and to processes which utilise such intermediates in the synthesis of morphinane compounds.
    Type: Grant
    Filed: March 19, 2007
    Date of Patent: January 25, 2011
    Assignees: Johnson Matthey Public Limited Company, GlaxoSmithKline Australia Pty. Ltd.
    Inventors: Craig Smith, Stuart Purcell, Lucy Waddell, Nicholas Hayes, Jarrod Ritchie, Scott Brian Halliday, Melville Mitchell, George Scott Wilson
  • Process for reducing contaminating Michael acceptor levels in oxycodone and other compositions
    Patent number: 7875623
    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: November 22, 2006
    Date of Patent: January 25, 2011
    Assignee: Controlled Chemicals, Inc.
    Inventors: Jules A. Shafer, Vladislav V. Telyatnikov, Hao Wang
  • Process for reducing impurities in oxycodone base
    Patent number: 7875719
    Abstract: The present invention is directed to a process for using n-butanol to prepare an oxycodone base compositions having reduced levels of impurities such as 14-hydroxycodeinone and DHDHC.
    Type: Grant
    Filed: December 4, 2007
    Date of Patent: January 25, 2011
    Inventors: D. Phillip Cox, Yong Zhang
  • 3-Oxy-Hydromorphone Derivatives
    Publication number: 20110015398
    Abstract: The present invention provides 3-oxy-hydromorphone derivatives, and in particular, 3-ester, 3-carbonate, and 3-sulfonate derivatives of hydromorphone.
    Type: Application
    Filed: July 9, 2010
    Publication date: January 20, 2011
    Applicant: Mallinckrodt Inc.
    Inventors: Gary L. Cantrell, Robert E. Halvachs, Frank W. Moser, David W. Berberich, Peter X. Wang
  • (+)-Morphinans as Antagonists of Toll-Like Receptor 9 and Therapeutic Uses Thereof
    Publication number: 20110015219
    Abstract: The present invention provides (+)-morphinans comprising Toll-like receptor 9 (TLR9) antagonist activity, as well as a method for identifying (+)-morphinans that may be therapeutically effective by determining whether the (+)-morphinan inhibits the activation of TLR9. Also provided are methods of using the (+)-morphinans comprising TLR9 antagonist activity to treat conditions such as traumatic pain, neuropathic pain, inflammatory disorders, acetaminophen toxicity, autoimmune disorders, neurodegenerative disorders, and cancer.
    Type: Application
    Filed: July 16, 2010
    Publication date: January 20, 2011
    Applicant: Mallinckrodt Inc.
    Inventors: Bobby N. Trawick, David W. Berberich
  • PROCESS FOR PREPARING OXYMORPHONE
    Publication number: 20110009634
    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: Application
    Filed: May 2, 2007
    Publication date: January 13, 2011
    Applicant: PENICK CORPORATION
    Inventor: Bao-Shan Huang
  • ABUSE RESISTANT DRUGS, METHOD OF USE AND METHOD OF MAKING
    Publication number: 20110002985
    Abstract: An abuse resistant oral pharmaceutical composition, comprising: a barrier layer, comprising a first polymer; a diffusion layer, comprising a second polymer, substantially covering the barrier layer, wherein the diffusion layer is bonded to the barrier layer and comprises a drug that is substantially homogeneously distributed within the second polymer and diffuses from the diffusion layer within the gastrointestinal (GI) tract; and optionally an expansion layer comprising an expandable polymer, wherein the expansion layer is substantially covered by the barrier layer. Methods of making the same and methods of using the same are also provided.
    Type: Application
    Filed: August 12, 2008
    Publication date: January 6, 2011
    Applicant: ABUSE DETERRENT PHARMACEUTICAL, LLC
    Inventors: Manish J. Shah, Ray J. Difalco
  • BENZOIC ACID, BENZOIC ACID DERIVATIVES AND HETEROARYL CARBOXYLIC ACID CONJUGATES OF HYDROCODONE, PRODRUGS, METHODS OF MAKING AND USE THEREOF
    Publication number: 20110002990
    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: July 1, 2010
    Publication date: January 6, 2011
    Inventors: Travis Mickle, Sven Guenther, Christal Mickle, Guochen Chi, Jaroslaw Kanski, Andrea K. Martin, Bindu Bera
  • PHENYLETHANOIC ACID, PHENYLPROPANOIC ACID AND PHENYLPROPENOIC ACID CONJUGATES AND PRODRUGS OF HYDROCODONE, METHOD OF MAKING AND USE THEREOF
    Publication number: 20110002991
    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: January 6, 2011
    Inventors: Travis Mickle, Sven Guenther, Christal Mickle, Guochen Chi, Jaroslaw Kanski, Andrea K. Martin, Bindu Bera
  • Crystalline Forms of Naltrexone Methobromide
    Publication number: 20100324078
    Abstract: The present invention relates to novel crystalline forms of naltrexone methobromide including hydrated and solvated forms. The invention also describes methods of preparing the various crystalline forms. The present invention also relates to pharmaceutical compositions containing crystalline forms of naltrexone methobromide, as well as methods of treating or preventing opioid induced side effects by administering the pharmaceutical compositions.
    Type: Application
    Filed: June 25, 2008
    Publication date: December 23, 2010
    Inventors: Gary A. Nichols, Robert E. Halvachs, Gary L. Cantrell, Kevin R. Roesch, Joseph P. Haar, JR.
  • Method for making analgesics
    Patent number: 7851482
    Abstract: Improved analgesic oxymorphone hydrochloride contains less than 10 ppm of alpha, beta unsaturated ketones and pharmaceutical preparations comprising such oxymorphone hydrochloride. The oxymorphone hydrochloride is produced by reducing a starting material oxymorphone hydrochloride using gaseous hydrogen and under specified acidity, solvent system and temperature conditions. A specific polymorph of oxymorphone hydrochloride may be obtained by hydration.
    Type: Grant
    Filed: October 3, 2007
    Date of Patent: December 14, 2010
    Assignee: Johnson Matthey Public Limited Compnay
    Inventors: Jen-Sen Dung, Erno M. Keskeny, James J. Mencel
  • SYNTHESIS OF R-N-METHYLNALTREXONE
    Publication number: 20100311781
    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: January 22, 2010
    Publication date: December 9, 2010
    Inventors: Harold D. Doshan, Julio Perez
  • CRYSTAL FORMS OF (R)-N-METHYLNALTREXONE BROMIDE AND USES THEREOF
    Publication number: 20100305323
    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: March 28, 2008
    Publication date: December 2, 2010
    Inventors: Valeriya N. Smolenskaya, Kadum A. Al Shareffi, Julio Perez, Syed M. Shah, Thomas A. Boyd
  • Efficient Synthesis Of Morphine And Codeine
    Publication number: 20100292475
    Abstract: The present invention relates to methods for the synthesis of morphine, intermediates, salts and derivatives thereof. In preferred embodiments, the invention relates to methods for improving the efficiency and overall yield of said morphine, morphine related derivatives and intermediates thereof. In further embodiments, the invention relates to methods for improving the efficiency and overall yield of galanthamine and intermediates thereof.
    Type: Application
    Filed: May 12, 2010
    Publication date: November 18, 2010
    Inventors: Philip D. Magnus, Benjamin P. Fauber, Neeraj Sane
  • PROCESS FOR PREPARING OXYMORPHONE, NALTREXONE, AND BUPRENORPHINE
    Publication number: 20100274019
    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 16, 2007
    Publication date: October 28, 2010
    Applicant: PENICK CORPORATION
    Inventor: Bao-Shan Huang
  • Prodrugs of Peripheral Phenolic Opioid Antagonists
    Publication number: 20100267614
    Abstract: Compounds of formula (I), in which X, Y, R1, R2, n, R3 and R4 have the meanings given in the specification, are useful as pro-drugs of peripheral phenolic opioid antagonists.
    Type: Application
    Filed: February 15, 2008
    Publication date: October 21, 2010
    Inventor: Thomas E. Jenkins
  • Preparation of Saturated Ketone Morphinan Compounds by Catalytic Isomerization
    Publication number: 20100261904
    Abstract: The present invention provides processes for the preparation of saturated ketone morphinan compounds by catalytic isomerization. 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 allyl-transition metal catalyst.
    Type: Application
    Filed: April 9, 2010
    Publication date: October 14, 2010
    Applicant: Mallinckrodt Inc.
    Inventors: Peter X. Wang, Tao Jiang, David W. Berberich
  • Ruthenium Catalysts for the Production of Hydrocodone, Hydromorphone or a Derivative Thereof
    Publication number: 20100261905
    Abstract: The present disclosure generally relates to catalytic methods for producing opioid derivatives. More particularly, the present disclosure relates to the preparation of hydrocodone, hydromorphone, or a derivative thereof, by means of an isomerization of codeine, morphine, or a derivative thereof, respectively, using a ruthenium catalyst.
    Type: Application
    Filed: April 9, 2010
    Publication date: October 14, 2010
    Applicant: Mallinckrodt Inc.
    Inventor: David J. Gindelberger
  • Preparation of Saturated Ketone Morphinan Compounds
    Publication number: 20100261907
    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: Application
    Filed: April 9, 2010
    Publication date: October 14, 2010
    Applicant: Mallinckrodt Inc.
    Inventors: Peter X. Wang, Tao Jiang, David W. Berberich, Narayanasamy Gurusamy, Catherine K. Jung
  • Preparation of 6-Keto, 3-Alkoxy Morphinans
    Publication number: 20100261906
    Abstract: The present invention provides processes for the preparation of saturated 6-keto, 3-alkoxy morphinans from unsaturated 6-hydroxy, 3-hydroxy morphinans, In particular, the invention provides processes that utilize catalytic isomerization and alkylation reactions for the preparation of saturated 6-keto, 3-alkoxy morphinans.
    Type: Application
    Filed: April 9, 2010
    Publication date: October 14, 2010
    Applicant: Mallinckrodt Inc.
    Inventors: Joseph P. Haar, JR., Kevin R. Roesch, David E. Gindelberger
  • Crystals of morphinan derivative and process for producing the same
    Patent number: 7803942
    Abstract: The present invention is directed to provide 17-cyclopropylmethyl-3,14?-dihydroxy-4,5?-epoxy-6?-[N-methyl-trans-3-(3-furyl)acrylamido]morphinan hydrochloride consistent in quality after production and having high purity. A crystal of 17-cyclopropylmethyl-3,14?-dihydroxy-4,5?-epoxy-6?-[N-methyl-trans-3-(3-furyl)acrylamido]morphinan hydrochloride including a A-form, B-form or C-form crystal thereof, and a process for producing the same are provided.
    Type: Grant
    Filed: April 6, 2006
    Date of Patent: September 28, 2010
    Assignee: Toray Industries, Inc.
    Inventors: Hisanori Wakita, Masahiro Akimoto, Takahiro Takeda
  • (+)-Morphinanium N-Oxides and Processes for their Production
    Publication number: 20100216997
    Abstract: The present invention provides (+)-morphinanium N-oxide compounds or pharmaceutically acceptable salts thereof. The invention also provides processes for producing (+)-morphinanium N-oxides or pharmaceutically acceptable salts thereof from the corresponding tertiary N-substituted (+)-morphinan compound or pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: February 23, 2010
    Publication date: August 26, 2010
    Applicant: Mallinckrodt Inc.
    Inventors: Gary L. Cantrell, Peter X. Wang, Bobby N. Trawick, Christopher W. Grote, David W. Berberich, Hang Sun, Subo Liao
  • (+)-Morphinanium Quaternary Salts and Processes for their Production
    Publication number: 20100216996
    Abstract: The present invention provides (+)-morphinanium quaternary salts. The invention also provides processes for producing (+)-morphinanium quaternary salts from tertiary N-substituted (+)-morphinan compounds.
    Type: Application
    Filed: February 23, 2010
    Publication date: August 26, 2010
    Applicant: Mallinckrodt Inc.
    Inventors: Gary L. Cantrell, Peter X. Wang, Bobby N. Trawick, Christopher W. Grote, David W. Berberich
  • SOLVENT-FREE CRYSTALLINE FORM OF NALTREXONE
    Publication number: 20100210675
    Abstract: Solvent-free crystalline polymorphic form of naltrexone, characterized in that it has the XRD data listed in Table 1, and a method for the preparation of this polymorphic form; and a method for converting this polymorphic form of naltrexone into a known polymorphic form of naltrexone.
    Type: Application
    Filed: April 27, 2007
    Publication date: August 19, 2010
    Applicant: CILAG AG
    Inventors: Ulrich Weigl, Ulf Költz
  • Method for Separation and Purification of Naltrexone By Preparative Chromatography
    Publication number: 20100190986
    Abstract: A process for the purification of an impure preparation containing naltrexone by means of a reverse phase preparative chromatography process is provided. In an illustrative embodiment a chromatographic column is loaded with a stationary phase, typically a silica particle having an organic ligand bound thereto. With a loading ratio of from about 10 to about 1000 the impure preparation is acidified and passed through the column. The column is eluted with typically an aqueous solution with acetonitrile and the purified naltrexone is obtained in a specified fraction.
    Type: Application
    Filed: June 7, 2006
    Publication date: July 29, 2010
    Inventor: Enrico A. Antonini
  • Oral bioavailable prodrugs
    Patent number: 7759358
    Abstract: The invention is directed to forming duplex prodrugs that provide significant increase in the transdermal flux of drugs across human skin. The prodrugs are prepared by reacting a drug that can form an ester moiety with phosgene to form a carbonate. The drug can be an opiate or an opiate antagonist. When in contact with human skin, the duplex drug is biotransformed by enzymes or by hydrolysis into two drug molecules.
    Type: Grant
    Filed: July 23, 2004
    Date of Patent: July 20, 2010
    Inventors: Peter A. Crooks, Mohamed Omer Hamad, Audra Lynn Stinchcomb
  • CRYSTALLINE MICROPOWDER PARTICLES
    Publication number: 20100160634
    Abstract: Crystalline particles of N-(17-cyclopropylmethyl-4,5?-epoxy-3,14-dihydroxy-morphinan-6?-yl)-phthalimide or a pharmaceutically acceptable salt thereof are disclosed. The crystalline particles have a particle diameter distribution in which a particle diameter (D50) at the point where cumulative frequency of volume distribution cumulatively calculated from particles having a smaller diameter reaches 50% is within a range of 1 to 30 ?m, and a particle diameter (D90) at the point where cumulative frequency of volume distribution cumulatively calculated from particles having a smaller diameter reaches 90% is not more than 90 ?m, which crystalline particles have a degree of crystallinity of not less than 80%. By the crystalline particles, bioavailability of the active substance may be increased while ensuring storage stability of the compound.
    Type: Application
    Filed: May 20, 2008
    Publication date: June 24, 2010
    Inventors: Masahiro Akimoto, Toshikazu Komagata, Motohiro Shiraki, Akihiro Ando
  • 8a,14-DIHYDROXY-7,8-DIHYDROCODEINONE
    Publication number: 20100152449
    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: Application
    Filed: February 24, 2010
    Publication date: June 17, 2010
    Applicant: Purdue Pharma LP
    Inventors: Robert Chapman, Lonn S. Rider, Qi Hong, Donald Kyle, Robert Kupper
  • N-METHYLNALTREXONE ZWITTERION
    Publication number: 20100145051
    Abstract: The invention discloses and claims N-Methylnaltrexone zwitterion, of formula (I), substantially in the anhydrous form or a hydrate thereof:
    Type: Application
    Filed: November 25, 2009
    Publication date: June 10, 2010
    Applicant: SANOFI-AVENTIS
    Inventor: Alain DLUBALA
  • Process for Preparing Hydrocodone Using a Super Acid
    Publication number: 20100137598
    Abstract: The present disclosure generally relates to a process for converting a fused, tricyclic compound to a fused, tetracyclic compound that includes a furan ring therein. More particularly, the present disclosure related to a process for preparing a hydrocodone compound, or a compound structurally related thereto, and in particular (+)-hydrocodone, by subjecting a structurally corresponding sinomenine starting compound to a super acid-assisted furan ring closure reaction.
    Type: Application
    Filed: November 30, 2009
    Publication date: June 3, 2010
    Applicant: Mallinckrodt Inc.
    Inventors: Peter X. Wang, Tao Jiang, Subo Liao, Erin Moore
  • Crystalline and Amorphous Forms of Naltrexone Hydrochloride
    Publication number: 20100120814
    Abstract: The present invention relates to novel crystalline forms of naltrexone hydrochloride including hydrated and solvated forms and a novel amorphous form. The invention also describes methods of preparing the various crystalline forms. The present invention also relates to pharmaceutical compositions containing crystalline and amorphous forms of naltrexone hydrochloride, as well as methods of treating addictive behavior by administering the pharmaceutical compositions.
    Type: Application
    Filed: April 10, 2008
    Publication date: May 13, 2010
    Inventors: Gary A. Nichols, Michelle R. Menze, Anthony Mannino
  • PERIPHERAL OPIOID RECEPTOR ANTAGONISTS AND USES THEREOF
    Publication number: 20100120813
    Abstract: The present invention provides a compound of formula I: wherein X?, R1, and R2 are as defined herein, and compositions thereof.
    Type: Application
    Filed: September 30, 2009
    Publication date: May 13, 2010
    Applicant: Wyeth
    Inventors: Nataliya Bazhina, George Joseph Donato, III, Steven R. Fabian, John Lokhnauth, Sreenivasulu Megati, Charles Melucci, Christian Ofslager, Niketa Patel, Galen Radebaugh, Syed M. Shah, Jan Szeliga, Huyi Zhang, Tianmin Zhu
  • Preparation of Oxymorphone from Oripavine
    Publication number: 20100113787
    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: Application
    Filed: March 14, 2008
    Publication date: May 6, 2010
    Inventors: Peter X. Wang, Tao Jiang, Gary l. Cantrell, David Wayne Berberich
  • Process for the Preparation of 6-Alpha-Hydroxy-N-Alkylated Opiates
    Publication number: 20100113788
    Abstract: The present invention is directed to the preparation of 6-keto morphinans.
    Type: Application
    Filed: December 3, 2009
    Publication date: May 6, 2010
    Applicant: Mallinckrodt Inc.
    Inventors: Christopher W. Grote, Peter X. Wang, Tao Jiang, Gary L. Cantrell, Frank W. Moser, Catherine E. Thomasson
  • (S)-N-methylnal trexone
    Publication number: 20100105911
    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: July 20, 2009
    Publication date: April 29, 2010
    Inventors: Thomas A. Boyd, Howard Wagoner, Suketu P. Sanghvi, Christopher Verbicky, Stephen Andruski
  • Method for separation and purification of hydrocodone by preparative chromatography
    Patent number: 7692013
    Abstract: A process for the purification of an impure preparation containing hydrocodone by means of a reverse phase preparative chromatography process is provided. In an illustrative embodiment a chromatographic column is loaded with a stationary phase, typically a silica particle having an organic ligand bound thereto. The impure preparation is acidified and passed through the column with a loading ratio of from about 10 to about 1000. The column is eluted, typically with an aqueous solution of acetonitrile, and the purified hydrocodone is obtained in a specified fraction.
    Type: Grant
    Filed: October 26, 2005
    Date of Patent: April 6, 2010
    Assignee: Mallinkrodt Inc.
    Inventor: Enrico A. Antonini
  • Processes for the synthesis of tertiary amines
    Publication number: 20100081819
    Abstract: The invention provides processes for the preparation of morphinans having a tertiary amine. In particular, the present invention provides processes for the formation of tertiary amine alkaloids by direct N-alkylation of secondary amine alkaloids, the processes co-mediated by an alkylating agent and a protic solvent or a mixture of a protic solvent and an aprotic solvent.
    Type: Application
    Filed: September 29, 2009
    Publication date: April 1, 2010
    Applicant: Mallinckrodt Inc.
    Inventors: Peter X. Wang, Tao Jiang, David W. Berberich