Nitrogen Or Divalent Chalcogen Double Bonded Directly To Carbocyclic Ring Of The Pentacyclo Ring System (e.g., Morphinones, Etc.) Patents (Class 546/45)
  • Polymorphs of 6-Beta-Naltrexol
    Publication number: 20100076007
    Abstract: The present invention provides polymorphs of 6-beta-naltrexol and process for their preparation. In particular, the present invention provides crystalline forms of the free base of 6-beta-naltrexol and processes for their preparation. The present invention also provides crystalline and amorphous forms of the hydrochloride salt of 6-beta-naltrexol and processes for their preparation.
    Type: Application
    Filed: September 21, 2009
    Publication date: March 25, 2010
    Applicant: Mallinckrodt Inc.
    Inventors: Jian Bao, Gary A. Nichols
  • Oxycodone hydrochloride having less than 25 ppm 14-hydroxycodeinone
    Patent number: 7683072
    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 16, 2007
    Date of Patent: March 23, 2010
    Assignee: Purdue Pharma L.P.
    Inventors: Robert Chapman, Lonn S. Rider, Qi Hong, Donald Kyle, Robert Kupper
  • Oxycodone hydrochloride having less than 25 ppm 14-hydroxycodeinone
    Patent number: 7674798
    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 16, 2007
    Date of Patent: March 9, 2010
    Assignee: Purdue Pharma L.P.
    Inventors: Robert Chapman, Lonn S. Rider, Qi Hong, Donald Kyle, Robert Kupper
  • Synthesis of R-N-methylnaltrexone
    Patent number: 7674904
    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: Grant
    Filed: May 25, 2006
    Date of Patent: March 9, 2010
    Assignee: Progenics Pharmaceuticals, Inc.
    Inventors: Harold D. Doshan, Julio Perez
  • Oxycodone hydrochloride having less than 25 PPM 14-hydroxycodeinone
    Patent number: 7674800
    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: March 29, 2007
    Date of Patent: March 9, 2010
    Assignee: Purdue Pharma L.P.
    Inventors: Robert Chapman, Lonn S. Rider, Qi Hong, Donald Kyle, Robert Kupper
  • Oxycodone hydrochloride having less than 25 ppm 14-hydroxycodeinone
    Patent number: 7674799
    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 16, 2007
    Date of Patent: March 9, 2010
    Assignee: Purdue Pharma L.P.
    Inventors: Robert Chapman, Lonn S. Rider, Qi Hong, Donald Kyle, Robert Kupper
  • Novel Opiate Reduction Utilizing Catalytic Hydrogen Transfer Reaction
    Publication number: 20100048905
    Abstract: An improved opiate synthesis scheme is provided. An improvement to the oxidation of oripavine and oripavine derivatives comprises the in-situ formation of the peroxacids required to oxidize the oripavine and oripavine derivatives to form an intermediate. An improvement to the reduction of the intermediate to form oxycodone and oxycodone derivatives comprises reduction utilizing a hydrogen transfer reagent. These improvements allow the production of oxycodone and oxycodone derivatives without isolation of the intermediate, providing a one-pot synthesis method.
    Type: Application
    Filed: April 15, 2008
    Publication date: February 25, 2010
    Inventors: Peter X. Wang, Tao Jiang, Gary L. Cantrell, David Wayne Berberich
  • Process for the Preparation of Quaternary N-Alkyl Morphinan Alkaloid Salts
    Publication number: 20100035910
    Abstract: An improved process for the N-alkylation of tertiary morphinan alkaloid bases to form the corresponding quaternary morphinan alkaloid derivatives.
    Type: Application
    Filed: September 3, 2009
    Publication date: February 11, 2010
    Applicant: Mallinckrodt Inc.
    Inventors: Peter X. Wang, Gary L. Cantrell, Robert E. Halvachs, Kevin R. Roesch, Henry J. Buehler, Joseph P. Haar
  • Morphinan derivatives, the quaternary ammonium salts thereof substituted in position 14, method for production and use thereof
    Patent number: 7655671
    Abstract: The present invention relates to a class of morphinan compounds and quaternary ammonium salts thereof, substituted in Position 14, which may be used as highly active analgesics or also as opioid antagonists. The present invention also relates to the pharmaceutically acceptable salts and easily produced derivatives thereof, a process for the production thereof and use thereof in the production of pharmaceutical specialities.
    Type: Grant
    Filed: September 6, 2007
    Date of Patent: February 2, 2010
    Assignee: Alcasynn Pharmaceuticals GmbH
    Inventors: Helmut Schmidhammer, Mariana Spetea, Johannes Schutz, Elisabeth Greiner, Falko Schüllner, Bettina Sailer, Kurt Stübegger
  • PROCESS USEFUL IN THE PREPARATION OF MORPHINAN ANTAGONISTS
    Publication number: 20100022774
    Abstract: A process for the preparation of morphinan antagonists of Formula (I) is described wherein R is a cyclopropyl, cyclobutyl or vinyl group and X is O, CH2 or diC1-4alkoxy group (optionally linked).
    Type: Application
    Filed: May 25, 2007
    Publication date: January 28, 2010
    Inventors: Ole Heine Kvernenes, Anne Mette Nygard, Audun Heggelund, Harald Halvorsen
  • Processs for preparing N-alkylnaltrexone halides
    Patent number: 7645880
    Abstract: The invention relates to a novel process for preparing N-methylnaltrexone bromide, comprising at least the steps consisting in: (i) reacting N-methylnaltrexone methyl sulfate in aqueous solution with an alkaline agent chosen from the group constituted by sodium carbonate, potassium carbonate, calcium carbonate, magnesium carbonate, cesium carbonate, strontium carbonate and mixtures thereof, for a pH of the aqueous reaction medium of between 7 and 10, and then in (ii) reacting the product thus obtained with hydrobromic acid, which is added for a pH of the aqueous reaction medium of between 0.5 and 5, in order thus to obtain the N-methylnaltrexone bromide.
    Type: Grant
    Filed: March 17, 2008
    Date of Patent: January 12, 2010
    Assignee: Sanofi-aventis
    Inventor: Alain Dlubala
  • Hydrocodone polymorphs
    Patent number: 7625918
    Abstract: Hydrocodone bitartrate forms are disclosed which are useful as analgesic agents either in combination with or as replacements for hydrocodone bitartrate.
    Type: Grant
    Filed: March 8, 2006
    Date of Patent: December 1, 2009
    Assignee: Noramco, Inc.
    Inventors: Eric J. Hagen, Aeri Park
  • Method of preparation of oxycodone
    Patent number: 7619087
    Abstract: A method of preparation of Oxycodone of formula I by reacting thebaine of formula II, or its analogue of formula III, wherein R represents a C2 to C5 alkyl, an alkylaryl, preferably benzyl, methoxybenzyl, or allyl, with hydrogen peroxide or peroxoacids in the presence of oxalic acid in admixture with acetic or formic acid. From the resulting crystalline precipitate of 14-hydroxycodeinone oxalate, by addition of a base, 14-hydroxycodeinone of formula IV is released, which is hydrogenated with hydrogen in the presence of a catalyst to yield Oxycodone (I): Oxycodone is transformed to hydrochloride, which is used as the active ingredient in analgesic formulations.
    Type: Grant
    Filed: August 16, 2005
    Date of Patent: November 17, 2009
    Assignee: Zentiva, a.s.
    Inventors: Vladislav Snuparek, Lubica Ratkovska, Bohumil Proksa
  • Demethylation of 14-hydroxy substituted alkaloid derivatives
    Patent number: 7619088
    Abstract: The present invention is directed to a method for demethylating 14-hydroxy substituted alkaloid derivatives, in particular of 14-hydroxy-17-methyl-4,5-epoxymorphinane-6-on-derivatives. This is achieved by reacting a starting compound with a compound of general formula R1OOC—N?N—COOR2 in a suitable solvent.
    Type: Grant
    Filed: October 29, 2008
    Date of Patent: November 17, 2009
    Assignee: Siegfried Ltd.
    Inventors: Erik Heinz Lauterbach, Thomas Dinkel, Sabrina Heller
  • STEREOSELECTIVE REDUCTION OF A MORPHINONE
    Publication number: 20090221766
    Abstract: A synthetic method is provided, wherein the method comprises stereoselectively reducing a ketone of a morphinone to form a reduced morphinone and optionally covalently attaching a water soluble polymer to the reduced morphinone.
    Type: Application
    Filed: April 19, 2007
    Publication date: September 3, 2009
    Applicant: Nektar Therapeutics AL, Corporation
    Inventors: Lin Cheng, Michael D. Bentley
  • QUATERNARY OPIOID CARBOXAMIDES
    Publication number: 20090197905
    Abstract: Compounds of formulas: are disclosed. The compounds are useful for ameliorating the side effects of therapeutic opiates.
    Type: Application
    Filed: August 8, 2008
    Publication date: August 6, 2009
    Applicant: RENSSELAER POLYTECHNIC INSTITUTE
    Inventor: Mark P. Wentland
  • AMINO ACID AND PEPTIDE PRODRUGS OF OPIOID ANALGESICS WITH REDUCED GI SIDE-EFFECTS
    Publication number: 20090192095
    Abstract: The present invention relates to methods for reducing gastrointestinal side effects in a subject, the gastrointestinal side effects being associated with the administration of an opioid analgesic. The methods comprise orally administering an opioid prodrug or pharmaceutically acceptable salt thereof to a subject, wherein the opioid prodrug is comprised of an opioid analgesic covalently bonded through a carbamate linkage to a peptide of 1-5 amino acids in length, and wherein upon oral administration, the prodrug or pharmaceutically acceptable salt minimizes at least one gastrointestinal side effect associated with oral administration of the opioid analgesic alone. Compositions for use with the method are also provided.
    Type: Application
    Filed: January 19, 2009
    Publication date: July 30, 2009
    Applicant: SHIRE LLC
    Inventors: Richard Franklin, Bernard T. Golding, Robert G. Tyson
  • AMINO ACID PEPTIDE PRO-DRUGS OF PHENOLIC ANALGESICS AND USES THEREOF
    Publication number: 20090186832
    Abstract: Prodrugs of meptazinol and other phenolic analgesics exhibiting low oral bioavailability with amino acids or lower peptides, pharmaceutical compositions containing such prodrugs and a method for providing pain relief with such prodrugs are provided. In addition, the present invention relates to methods for increasing the oral bioavailability of a phenolic analgesic. The method comprises orally administering a phenolic analgesic prodrug, wherein the phenolic analgesic is bound to an amino acid or peptide via a carbamate linkage, to a subject in need thereof. Prodrugs having side chains of valine, leucine, isoleucine and glycine amino acids and mono-, di- and tripeptides thereof are preferred.
    Type: Application
    Filed: January 19, 2009
    Publication date: July 23, 2009
    Applicant: SHIRE LLC
    Inventors: Richard Franklin, Bernard T. Golding, Robert G. Tyson
  • (S)--methylnaltrexone
    Patent number: 7563899
    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: May 25, 2006
    Date of Patent: July 21, 2009
    Assignee: Progenics Pharmaceuticals, Inc.
    Inventors: Thomas A. Boyd, Howard Wagoner, Suketu P. Sanghvi, Christopher Verbicky, Stephen Andruski
  • Antipruritic Agent for Pruritus Caused by Multiple Sclerosis
    Publication number: 20090170888
    Abstract: An antipruritic against pruritus caused by multiple sclerosis is disclosed.
    Type: Application
    Filed: March 9, 2006
    Publication date: July 2, 2009
    Applicant: TORAY INDUSTRIES, INC.
    Inventors: Hideo Umeuchi, Koki Ueno, Hiroshi Miyakawa
  • OPIOID AND OPIOID-LIKE COMPOUNDS AND USES THEREOF
    Publication number: 20090169508
    Abstract: The present invention relates to opioid and opioid-like compounds, and pharmaceutical formulations thereof, and use thereof for prevention and treatment of disorders such as septic shock and organ damage.
    Type: Application
    Filed: March 9, 2009
    Publication date: July 2, 2009
    Inventors: Edwin S.C. Wu, Mao-Hsiung Yen, Chin-Tsai Fan
  • Demethylation of 14-hydroxy substituted alkaloid derivatives
    Publication number: 20090163717
    Abstract: The present invention is directed to a method for demethylating 14-hydroxy substituted alkaloid derivatives, in particular of 14-hydroxy-17-methyl-4,5-epoxymorphinane-6-on-derivatives. This is achieved by reacting a starting compound with a compound of general formula R1OOC—N?N—COOR2 in a suitable solvent.
    Type: Application
    Filed: November 24, 2008
    Publication date: June 25, 2009
    Inventors: Erik Heinz Lauterbach, Thomas Dinkel, Sabrina Heller, Andreas Bertogg
  • Hydromorphone polymorphs
    Patent number: 7550592
    Abstract: Hydromorphone hydrochloride forms are disclosed which are useful as analgesic agents either in combination with or as replacements for hydromorphone hydrochloride.
    Type: Grant
    Filed: April 17, 2006
    Date of Patent: June 23, 2009
    Assignee: Noramco, Inc.
    Inventors: Keith R. Lorimer, Alicia T. Ng
  • Processes for the preparation of normorphinan salts
    Publication number: 20090156819
    Abstract: The invention provides a process for the conversion of opioid derivatives into normorphinan compounds useful for making “nal” compound analgesics and antagonists. In particular, the process may be used for the production of pure normorphinan salts from crude opioid substrates.
    Type: Application
    Filed: December 17, 2008
    Publication date: June 18, 2009
    Inventors: Peter X. Wang, Tao Jiang, Gary L. Cantrell, David W. Berberich, Jian Bao, Bobby N. Trawick
  • Process and compounds for the production of (+)opiates
    Publication number: 20090156818
    Abstract: The invention generally provides processes and intermediate compounds useful for the production of (+)-opiates. Non-limiting examples of (+) opiates that may be derived from one or more compounds of the invention include (+)-noroxymorphone, (+)-naltrexone, (+)-naloxone, (+)-N-cyclopropylmethylnorhydrocodone, (+)-N-cycloproylmethylnorhydromorphone, (+)-N-allylnorhydrocodone, (+)-N-allylnorhydromorphone, (+)-noroxycodone, (+)-naltrexol, (+)-naloxol, and (+)-3-O-methyl-naltrexone.
    Type: Application
    Filed: December 17, 2008
    Publication date: June 18, 2009
    Inventors: Peter X. Wang, Tao Jiang, Gary L. Cantrell, David W. Berberich, Bobby N. Trawick, Todd Osiek, Subo Liao, Frank W. Moser, Joseph P. Mcclurg
  • Processes for the production of (+)- "NAL" morphinan compounds
    Publication number: 20090156820
    Abstract: The invention generally provides processes and intermediate compounds useful for the production of (+) nal morphinan compounds. In particular, the process encompasses synthetic routes for the production of (+) nal morphinan compounds or derivatives of (+) nal morphinan compounds from (+)-morphinan substrates such as (+)-hydrocodone, (+)-norhydrocodone or derivatives of either compound.
    Type: Application
    Filed: December 17, 2008
    Publication date: June 18, 2009
    Inventors: Peter X. Wang, Tao Jiang, Gary L. Cantrell, David W. Berberich, Bobby N. Trawick, Subo Liao
  • PRO-DRUGS FOR CONTROLLED RELEASE OF BIOLOGICALLY ACTIVE COMPOUNDS
    Publication number: 20090137618
    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: Application
    Filed: November 26, 2008
    Publication date: May 28, 2009
    Inventor: Thomas E. Jenkins
  • Demethylation of 14 hydroxy substituted alkaloid derivatives
    Publication number: 20090137809
    Abstract: The present invention is directed to a method for demethylating 14-hydroxy substituted alkaloid derivatives, in particular of 14-hydroxy-17-methyl-4,5-epoxymorphinane-6-on-derivatives. This is achieved by reacting a starting compound with a compound of general formula R1OOC—N?N—COOR2 in a suitable solvent.
    Type: Application
    Filed: October 29, 2008
    Publication date: May 28, 2009
    Applicant: SIEGFRIED Ltd
    Inventors: Erik Heinz Lauterbach, Thomas Dinkel, Sabrina Heller
  • Oxycodone polymorphs
    Patent number: 7534888
    Abstract: Oxycodone.HCl polymorph forms are disclosed which are useful as analgesic agents either in combination with or as replacements for oxycodone.
    Type: Grant
    Filed: August 15, 2003
    Date of Patent: May 19, 2009
    Assignee: Noramco, Inc.
    Inventors: Abram Calderon, Douglas Phillip Cox, Patrick Thomas Cyr, Aeri Park
  • DEUTERIUM-ENRICHED NALTREXONE
    Publication number: 20090082382
    Abstract: The present application describes deuterium-enriched naltrexone, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
    Type: Application
    Filed: August 22, 2008
    Publication date: March 26, 2009
    Applicant: PROTIA, LLC
    Inventor: Anthony W. Czarnik
  • DEUTERIUM-ENRICHED METHYLNALTREXONE
    Publication number: 20090076051
    Abstract: The present application describes deuterium-enriched methylnatrexone bromide, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
    Type: Application
    Filed: August 22, 2008
    Publication date: March 19, 2009
    Applicant: PROTIA, LLC
    Inventor: Anthony W. Czarnik
  • Opioid and opioid-like compounds and uses thereof
    Patent number: 7501433
    Abstract: The present invention relates to opioid and opioid-like compounds, and pharmaceutical formulations thereof, and use thereof for prevention and treatment of disorders such as septic shock and organ damage.
    Type: Grant
    Filed: April 12, 2005
    Date of Patent: March 10, 2009
    Assignee: Jenken Biosciences, Inc.
    Inventors: Edwin S. C. Wu, Mao-Hsiung Yen, Chin-Tsai Fan
  • Crystals of Morphinan Derivative and Process for Producing the Same
    Publication number: 20090062544
    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: Application
    Filed: April 6, 2006
    Publication date: March 5, 2009
    Inventors: Hisanori Wakita, Masahiro Akimoto, Takahiro Takeda
  • Process for the preparation of quaternary N-alkyl morphin or morphinan alkaloid derivatives
    Publication number: 20090054651
    Abstract: The present invention relates to a process for the preparation of quaternary N-alkyl morphin or morphinan alkaloid derivatives. This is achieved by using a nucleophilic nitrogen, phosphor or sulfur containing base in the reaction mixture.
    Type: Application
    Filed: July 18, 2008
    Publication date: February 26, 2009
    Inventors: Martin Eipert, Erik Heinz Lauterbach, Sabrina Heller, Thomas Dinkel, Stephanie Hake
  • (R)-N-Stereoisomers of 7,8-Saturated-4,5-Epoxy-Morphinanium Analogs
    Publication number: 20090047279
    Abstract: Novel (R)—N-stereoisomers of 7,8-saturated-4,5-epoxy-morphinanium analogs are disclosed. Pharmaceutical compositions containing the (R)—N-stereoisomers of 7,8-saturated-4,5-epoxy-morphinanium analogs and methods for their pharmaceutical uses are also disclosed. Such analogs are disclosed as being useful in treating, among varying conditions, opioid-induced constipation.
    Type: Application
    Filed: November 21, 2007
    Publication date: February 19, 2009
    Applicant: Progenics Pharmaceuticals, Inc.
    Inventors: Julio Perez, Amy Qi Han, Yakov Rotshteyn
  • METHODS FOR N-DEMETHYLATION OF MORPHINE AND TROPANE ALKALOIDS
    Publication number: 20090005564
    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: Application
    Filed: June 29, 2007
    Publication date: January 1, 2009
    Inventors: Robert James Carroll, Hannes Leisch, Tomas Hudlicky
  • PREPARATION OF OXYCODONE
    Publication number: 20080312443
    Abstract: A process for preparing oxycodone or an oxycodone salt, wherein the oxycodone or oxycodone salt has low levels of impurities (especially 14-hydroxycodeinone) is disclosed. The process comprises the steps of: a) preparing a mixture comprising oxycodone and a solvent and adjusting the pH of the mixture to less than 6; and subsequently b) exposing the mixture to hydrogenation reagents for a period of at least 1 hour.
    Type: Application
    Filed: August 18, 2008
    Publication date: December 18, 2008
    Applicant: Johnson Matthey Public Limited Company
    Inventors: Michael Lawrence Casner, Jen-Sen Dung, Emo M. Keskeny, Jin Luo
  • Process for Preparing Morphinan-6-One Products with Low Levels of Alpha, Beta-Unsaturated Ketone Compounds
    Publication number: 20080312442
    Abstract: The present invention generally relates to processes for preparing highly pure morphinan-6-one products. The processes involve reducing the concentration of ?,?-unsaturated ketone compounds present as impurities in morphinan 6 one products or reaction mixtures including morphinan 6 one compounds by treatment with a sulfur-containing compound.
    Type: Application
    Filed: March 2, 2007
    Publication date: December 18, 2008
    Inventors: Henry J. Buehler, William E. Dummitt, Anthony Mannino, Dennis C. Aubuchon, Hong Gu
  • PREPARATION OF OXYCODONE
    Publication number: 20080306265
    Abstract: A method of purifying oxycodone or a salt thereof includes the steps of: a) preparing a solution including the oxycodone or salt thereof in a solvent, the solution having a pH less than 6, and; b) maintaining the solution at a temperature of at least 55° C. for a period of at least 1 hour; wherein the step of maintaining is performed in the absence of hydrogenation reagents.
    Type: Application
    Filed: August 15, 2008
    Publication date: December 11, 2008
    Applicant: Johnson Matthey Public Limited Company
    Inventors: Michael Lawrence Casner, Jen-Sen Dung, Erno M. Keskeny, Jin Luo
  • C-14 oxidation of morphine derivatives
    Patent number: 7435817
    Abstract: The present invention relates to process for the preparation of a 14-hydroxynormorphinone derivative of formula IV comprising reacting the compound of formula III, with a cobalt (II) oxidant in the presence of a mild base and air or oxygen as the cooxidant; wherein R1 is (1C-7C)alkyl optionally substituted with one or more chlorines, butenyl, vinyl, benzyl, phenyl or naphthyl; and R2 is benzyl or benzyl substituted with one or more (1C-6C)alkoxy group or benzyl substituted with one or more halogen. The process is very suitable in the production of noroxymorphone.
    Type: Grant
    Filed: August 15, 2002
    Date of Patent: October 14, 2008
    Assignee: N.V. Organon
    Inventors: Joannes Theodorus Maria Linders, Pieter Vrijhof
  • Novel 6-Amino-Morphinan Derivatives, Method of Manufacturing Them and Their Application as Analgesics
    Publication number: 20080234307
    Abstract: This invention relates to a class of 6-amino-morphinan compounds of formula (I) which can be used as highly active analgesics. This invention also relates to their pharmaceutically acceptable salts and easily accessible derivatives (e.g. esters or amides of the amino acid derivatives), to a process for their manufacture and their application in the manufacture of pharmaceutical specialties.
    Type: Application
    Filed: September 12, 2006
    Publication date: September 25, 2008
    Applicant: AlcaSynn Pharmaceuticals GmbH
    Inventors: Johannes Schuetz, Peter Kayatz
  • Polymorphic Forms of Naltrexone
    Publication number: 20080227804
    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: September 25, 2007
    Publication date: September 18, 2008
    Applicant: ALKERMES, INC.
    Inventors: Harry G. Brittain, David A. Dickason, Joyce Hotz, Shawn L. Lyons, J. Michael Ramstack, Steven G. Wright
  • PROCESS FOR PREPARING N-ALKYLNALTREXONE HALIDES
    Publication number: 20080214817
    Abstract: The invention relates to a novel process for preparing N-methylnaltrexone bromide, comprising at least the steps consisting in: (i) reacting N-methylnaltrexone methyl sulfate in aqueous solution with an alkaline agent chosen from the group constituted by sodium carbonate, potassium carbonate, calcium carbonate, magnesium carbonate, cesium carbonate, strontium carbonate and mixtures thereof, for a pH of the aqueous reaction medium of between 7 and 10, and then in (ii) reacting the product thus obtained with hydrobromic acid, which is added for a pH of the aqueous reaction medium of between 0.5 and 5, in order thus to obtain the N-methylnaltrexone bromide.
    Type: Application
    Filed: March 17, 2008
    Publication date: September 4, 2008
    Applicant: SANOFI-AVENTIS
    Inventor: Alain Dlubala
  • PHARMACEUTICAL COMPOSITIONS OF HYDROMORPHONE FOR PREVENTION OF OVERDOSE OR ABUSE
    Publication number: 20080207668
    Abstract: The invention relates to compounds, compositions and methods comprised of a chemical moiety attached to hydromorphone. The invention provides embodiments that provide a decrease in the potential of hydromorphone to cause overdose or to be abused while still delivering therapeutic activity similar to that of the parent hydromorphone.
    Type: Application
    Filed: October 5, 2007
    Publication date: August 28, 2008
    Applicant: New River Pharmaceuticals Inc.
    Inventor: James Scott Moncrief
  • (S)-N-Stereoisomers of 7,8-Saturated-4,5-Epoxy-Morphinanium Analogs
    Publication number: 20080207669
    Abstract: Novel (S)-N-stereoisomers of 7,8-saturated-4,5-epoxy-morphinanium analogs are disclosed. Pharmaceutical compositions containing the (S)-N-stereoisomers of 7,8-saturated-4,5-epoxy-morphinanium analogs and methods for their pharmaceutical uses are also disclosed. Such analogs are disclosed as being useful in treating, among varying conditions, hypermotility of the gastrointestinal tract.
    Type: Application
    Filed: November 21, 2007
    Publication date: August 28, 2008
    Applicant: Progenics Pharmaceuticals, Inc.
    Inventors: Julio Perez, Amy Qi Han, Yakov Rotshteyn
  • Modulation of Alkaloid Siosynthesis in Plants and Plants Having Altered Alkaloid Biosynthesis
    Publication number: 20080196123
    Abstract: The invention relates to a method for altering alkaloid biosynthesis in a plant, comprising: i) introducing into cells of a plant, an expressible exogenous nucleic acid comprising or consisting of an (S)-N-methylcoclaurine 3?-hydroxylase gene (cyp80b) or a derivative thereof, and ii) optionally propagating the plant, wherein expression of the exogenous nucleic acid in the plant or in its progeny results in altered levels of alkaloid biosynthesis.
    Type: Application
    Filed: August 11, 2005
    Publication date: August 14, 2008
    Inventors: Toni M. Kutchan, Susanne Frick, Katja Kempe
  • Chemical methods
    Patent number: 7405301
    Abstract: This invention relates to a method for N-demethylating an N-methyl morphinane comprising the steps of: (i) treating said N-methyl morphinane with an oxidizing agent to form the N-oxide morphinane; and (ii) treating said N-oxide morphinane with a reducing agent. This invention also relates to a method for oxidizing a ?7-morphinane compound to a ?6, ?8-morphinane compound, comprising the steps of treating said ?7-morphinane with ?-MnO2 for a time and under conditions sufficient to oxidize said ?7-morphinane, and treating the ?-MnO2 with glycol or a derivative thereof, and/or an inorganic salt.
    Type: Grant
    Filed: August 24, 2001
    Date of Patent: July 29, 2008
    Assignee: GlaxoWellcome Australia Ltd.
    Inventors: Peter Scammells, Nicholas Gathergood, Justin Ripper
  • 7,8-Saturated-4,5-Epoxy-Morphinanium Analogs
    Publication number: 20080176884
    Abstract: Novel 7,8-saturated-4,5-epoxy-morphinanium analogs are disclosed. Pharmaceutical compositions containing the 7,8-saturated-4,5-epoxy-morphinanium analogs and methods of their pharmaceutical uses are also disclosed. The compounds disclosed are useful, inter alia, as modulators of opioid receptors.
    Type: Application
    Filed: November 21, 2007
    Publication date: July 24, 2008
    Applicant: Progenics Pharmaceuticals, Inc.
    Inventors: Julio Perez, Amy Qi Han, Yakov Rotshteyn
  • Method for the catalytic production of hydrocodone, hydromorphone, and derivatives thereof
    Patent number: 7399858
    Abstract: A method for the catalytic production of hydrocodone derivatives and hydromorphone derivatives, respectively, utilizing a transition metal catalyst of the formula [M(PR4R5R6)nXm]p; wherein M is a Group VIII transition metal; R4, R5 and R6 are selected from the group consisting of alkyl, aryl, alkoxyl, phenoxy and combinations thereof; X is a halide or an anion; n is 1, 2, 3 or 4; m is 1 or 2; and p is at least 1.
    Type: Grant
    Filed: March 7, 2006
    Date of Patent: July 15, 2008
    Assignee: Mallinckrodt Inc.
    Inventors: Peter X. Wang, Frank W. Moser, Gary L. Cantrell, Daniel P. Magparangalan, Jian Bao
  • Method for catalytic preparation of hydromorphone and hydrocodone
    Patent number: 7399859
    Abstract: The present invention generally relates to catalysts of formula (III) [M(P(Ra)(Rb)N(Rc)(Rd))2Xn]mYp that selectively convert morphine/codeine to hydromorphone/hydrocodone, and methods of use thereof.
    Type: Grant
    Filed: February 6, 2007
    Date of Patent: July 15, 2008
    Assignee: Cody Laboratories Inc.
    Inventor: Vladimir Kouznetsov