One Of The Five Cyclos Is Five-membered And Includes Ring Chalcogen (e.g., Codeine, Morphine, Etc.) Patents (Class 546/44)
Nitrogen or divalent chalcogen double bonded directly to carbocyclic ring of the pentacyclo ring system (e.g., morphinones, etc.) (Class 546/45)
A single chalcogen is bonded directly to ring carbon of the pentacyclo ring system (e.g., desoxy morphine, etc.) (Class 546/46)
  • NALMEFENE PRODRUGS
    Publication number: 20110034502
    Abstract: The present invention relates to ester prodrugs of nalmefene of formula (I), pharmaceutical compositions comprising these compounds, chemical processes for preparing these compounds and their use in the treatment of substance abuse disorders such as alcohol abuse and alcohol dependence and impulse control disorders such as pathological gambling and addiction to shopping.
    Type: Application
    Filed: April 23, 2009
    Publication date: February 10, 2011
    Inventors: Michel Joseph, Maurice, Andre Guillaume, Tim Gaekens
  • 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
  • Preparation and utility of opioid analgesics
    Patent number: 7872013
    Abstract: The present disclosure is directed to modulators of opiate- and/or NMDA receptors and pharmaceutically acceptable salts and prodrugs thereof, the chemical synthesis thereof, and the use of such compounds for the treatment and/or management of pain, anxiety, neurodegeneration, drug dependence, coughing, muscular tension, and/or glaucoma and any other condition in which it is beneficial to modulate an opiate- and/or NMDA receptor.
    Type: Grant
    Filed: August 16, 2007
    Date of Patent: January 18, 2011
    Assignee: Auspex Pharmaceuticals, Inc.
    Inventors: Thomas G. Gant, Sepehr Sarshar
  • 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
  • Preparation of 6-Alpha-Amino N-Substituted Morphinans by Catalytic Hydrogen Transfer
    Publication number: 20100317683
    Abstract: The present invention provides processes for the stereoselective synthesis of 6-alpha-amino N-substituted morphinans. In particular, the invention provides processes for the reductive amination of 6-keto N-substituted morphinans by catalytic hydrogen transfer.
    Type: Application
    Filed: June 10, 2010
    Publication date: December 16, 2010
    Applicant: Mallinckrodt Inc.
    Inventors: Christopher W. Grote, Gary L. Cantrell, Joseph P. McClurg, Catherine E. Thomasson, Frank W. Moser
  • 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
  • Processes for preparing morphinans and intermediates thereof
    Patent number: 7838677
    Abstract: The present invention is directed to processes for the synthesis of morphinans. In particular, a process for cyclizing a ?,?-bicyclic ketone compound to form a nordihydrothebainone product using the Grewe cyclization reaction is improved by forming a reaction mixture comprising a ?,?-bicyclic ketone compound, a cyclizing acid and a water scavenging cyclization additive. In one embodiment, the Grewe transformation occurs in the presence of an acid anhydride as the cyclization additive. Further, the present invention is directed to processes for converting ?,?-bicyclic ketone compounds (e.g., by-products of the Grewe cyclization reaction) to ?,?-bicyclic ketone compounds, wherein the ?,?-bicyclic ketone compounds may be recovered to further undergo Grewe cyclization and form the nordihydrothebainone product.
    Type: Grant
    Filed: February 23, 2006
    Date of Patent: November 23, 2010
    Assignee: Mallinckrodt Inc
    Inventors: Peter Xianqi Wang, Frank W. Moser, Gary L. Cantrell, Jian Bao
  • NOVEL DICARBOXYLIC ACID LINKED AMINO ACID AND PEPTIDE PRODRUGS OF OPIOIDS AND USES THEREOF
    Publication number: 20100286186
    Abstract: The present invention concerns dicarboxylic acid linked amino acid and peptide prodrugs of opioid analgesics and pharmaceutical compositions containing such prodrugs. Methods for providing pain relief, decreasing the adverse GI side effects of the opioid analgesic and increasing the bioavailability of the opioid analgesic with the aforementioned prodrugs are also provided. In one embodiment, prodrugs having the amino acid side chains of valine, leucine, isoleucine and glycine; and mono-, di- and tripeptides thereof are provided.
    Type: Application
    Filed: April 1, 2010
    Publication date: November 11, 2010
    Applicant: Shire LLC
    Inventors: Richard Franklin, Bernard T. Golding, Robert G. Tyson
  • 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
  • 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
  • PAPAVER SOMNIFERUM WITH HIGH CONCENTRATION OF CODEINE
    Publication number: 20100234600
    Abstract: The present invention is directed to an improved poppy straw, concentrate of poppy straw and opium of Papaver somniferum for the production of codeine containing little or no oripavine, morphine or thebaine. The present invention also provides plants, stands and seeds of Papaver somniferum and methods for the production of codeine.
    Type: Application
    Filed: May 22, 2009
    Publication date: September 16, 2010
    Inventors: Anthony J. Fist, James A.C. Miller, Davina Gregory
  • Chemically modified small molecules
    Patent number: 7786133
    Abstract: The invention provides small molecule drugs that are chemically modified by covalent attachment of a water-soluble oligomer obtained from a monodisperse or bimodal water-soluble oligomer composition. A conjugate of the invention, when administered by any of a number of administration routes, exhibits a reduced biological membrane crossing rate as compared to the biological membrane crossing rate of the small molecule drug not attached to the water-soluble oligomer.
    Type: Grant
    Filed: December 16, 2004
    Date of Patent: August 31, 2010
    Assignee: Nektar Therapeutics
    Inventors: Michael D. Bentley, Tacey X. Viegas, Richard R. Goodin, Lin Cheng, Xuan Zhao
  • (+)-6-Hydroxy-Morphinan or (+)-6-Amino-Morphinan Derivatives
    Publication number: 20100216995
    Abstract: The present invention provides (+)-morphinanium compounds comprising substituted 6-hydroxy or 6-amine groups. The invention also provides methods for inhibiting microglial activation by administering the compounds of the invention.
    Type: Application
    Filed: February 23, 2010
    Publication date: August 26, 2010
    Applicant: Mallinckrodt Inc.
    Inventors: Christopher W. Grote, Gary L. Cantrell, Peter X. Wang, Bobby N. Trawick, David W. Berberich
  • Regioselective metal catalyzed synthesis of annelated benzimidazoles and azabenzimidazoles
    Publication number: 20100216988
    Abstract: The present invention relates to a process for the regioselective synthesis of compounds of the formula I, wherein R1; R2; R3; R4; J1; J2; J3; J4 and G have the meanings indicated in the claims. The present invention provides a direct metal, e.g. palladium or copper, catalyzed, regioselective process to a wide variety of unsymmetrical, multifunctional N-substituted benzimidazoles or azabenzimidazoles of formula I starting from 2-halo-nitroarenes and N-substituted amides.
    Type: Application
    Filed: December 22, 2009
    Publication date: August 26, 2010
    Applicant: SANOFI-AVENTIS
    Inventors: Jorge ALONSO, Andreas LINDENSCHMIDT, Marc NAZARE, Omar RKYEK, Matthias URMANN, Nis HALLAND
  • Process for the Reductive Alkylation of Normorphinans
    Publication number: 20100210843
    Abstract: The invention provides a process for the N-alkylation of normorphinan compounds to produce N-alkylated morphinan compounds. In particular, the process relates to the alkylation of a normorphinan compound by a carboxaldehyde in the presence of a reducing agent to form an N-alkylated morphinan.
    Type: Application
    Filed: February 17, 2010
    Publication date: August 19, 2010
    Applicant: Mallinckrodt Inc.
    Inventors: Edumnd C. Hudson, Sharon Woods
  • Preparation and use of alkylating agents
    Patent number: 7776309
    Abstract: Methods of alkylating target compounds are disclosed. The alkylating agent can be radiolabelled. In some instances, the alkylating agent is synthesized and then reacted with a target compound without an intervening purification step. The method comprises a) synthesizing an alkylating agent having the formula: X—(CR1R2)aCR3R4-LG wherein, a is 0, 1, 2 or 3, R1, R2, R3 and R4 are independently H, X or alkyl, X is a halogen or a label, with the proviso that at least one X is a halogen, LG is a leaving group; and b) directly reacting said alkylating agent with a target compound comprising an alkylation reactive group under conditions suitable for the alkylation of said target compound.
    Type: Grant
    Filed: July 26, 2004
    Date of Patent: August 17, 2010
    Assignee: The Queen's Medical Center
    Inventor: John L. Lim
  • Preparation of N-Alkylated Opiates by Reductive Amination
    Publication number: 20100197921
    Abstract: The present invention is directed to the reduction of an N-imine moiety or a hemiaminal moiety of a morphinan in the presence of a ruthenium, rhodium, or iridium asymmetric catalyst and a hydrogen source.
    Type: Application
    Filed: June 16, 2008
    Publication date: August 5, 2010
    Inventors: Christopher W. Grote, Brian Orr, Tao Jiang, Gary L. Cantrell
  • LARGE SUBSTITUENT, NON-PHENOLIC AMINE OPIOIDS
    Publication number: 20100190817
    Abstract: 8-Substituted-2,6-methano-3-benzazocines of general structure are useful as analgesics, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction medications.
    Type: Application
    Filed: July 21, 2009
    Publication date: July 29, 2010
    Applicant: RENSSELAER POLYTECHNIC INSTITUTE
    Inventor: Mark P. Wentland
  • REMEDY OR PREVENTIVE FOR INTEGRATION DYSFUNCTION SYNDROME
    Publication number: 20100160364
    Abstract: A composition includes a therapeutic or prophylactic agent for schizophrenia, which therapeutic or prophylactic agent can treat especially positive symptoms of schizophrenia and does not cause impaired information processing related to cognitive deficiencies or the like which is a symptom of schizophrenia. The therapeutic or prophylactic agent for schizophrenia includes as an effective ingredient a compound having a specific morphinan skeleton or a pharmaceutically acceptable acid addition salt thereof.
    Type: Application
    Filed: June 20, 2008
    Publication date: June 24, 2010
    Applicant: TORAY INDUSTRIES, INC.
    Inventors: Satoru Yoshikawa, Hidenori Mochizuki
  • THERAPEUTIC OR PROPHYLACTIC AGENT FOR DYSKINESIA
    Publication number: 20100130524
    Abstract: An object of the present invention is to provide a drug with a high therapeutic or prophylactic effect on dyskinesia, without accompanying aggravation of symptoms of the primary disease, and with fewer side effects. Accordingly, the present invention provides a therapeutic or prophylactic agent for dyskinesia, comprising as an effective component a compound having a 4,5-epoxy morphinan skeleton, which compound is represented by the Formula (I) below, or a pharmaceutically acceptable acid addition salt thereof: [wherein the double line composed of a dashed line and a solid line represents a double bond or single bond, R1 is C4-C7 cycloalkylalkyl, R2 is C1-C5 straight or branched alkyl, and B is —CH?CH—.
    Type: Application
    Filed: April 24, 2008
    Publication date: May 27, 2010
    Inventors: Ken Ikeda, Hidenori Mochizuki
  • 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
  • Processes for the selective amination of ketomorphinans
    Publication number: 20100081817
    Abstract: The present invention is generally directed to a process for the preparation of a ketomorphinan comprising maintaining a ketone group as unprotected and performing reductive amination using a hydrogen source and a catalyst.
    Type: Application
    Filed: September 29, 2009
    Publication date: April 1, 2010
    Applicant: Mallinckrodt Inc.
    Inventors: Edumnd C. Hudson, Douglas Teramura, Christopher W. Grote, Catherine E. Thomasson, Gary L. Cantrell
  • Process for the Preparation of 6-Alpha-Hydroxy-N-Alkylated Opiates
    Publication number: 20100081818
    Abstract: The present invention is directed to the preparation of 6-hydroxy morphinans having formula (II) or N-alkylated 6-hydroxy morphinans having formula (III).
    Type: Application
    Filed: December 3, 2009
    Publication date: April 1, 2010
    Applicant: Mallinckrodt Inc.
    Inventors: Christopher W. Grote, Peter X. Wang, Tao Jiang, Gary L. Cantrell, Frank W. Moser, Catherine E. Thomasson
  • Processes for the Synthesis of Five and Six Membered Heterocyclic Rings
    Publication number: 20100069639
    Abstract: The present invention provides processes for the synthesis of five and six membered rings. In particular, the present invention provides processes for the synthesis of five and six membered rings in alkaloids.
    Type: Application
    Filed: September 14, 2009
    Publication date: March 18, 2010
    Applicant: Mallinckrodt Inc.
    Inventors: Peter X. Wang, Tao Jiang, David W. Berberich
  • 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
  • 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
  • Method and system for separation and purification of at least one narcotic alkaloid using reverse phase preparative chromatography
    Patent number: 7671203
    Abstract: An apparatus and method for separating at least one narcotic alkaloid that includes loading a stationary phase media into a high performance preparative liquid chromatography column, feeding a crude narcotic alkaloid solution into the chromatographic column, applying a mobile phase to the chromatographic column, and recovering a narcotic alkaloid eluate from the chromatographic column. The narcotic eluates arc collected and treated separately from each other. Each separated alkaloid, however, has sufficient recovery and purity.
    Type: Grant
    Filed: February 18, 2003
    Date of Patent: March 2, 2010
    Assignee: Mallinckrodt Inc.
    Inventor: Enrico Anthony Antonini
  • N-demethylation of N-methyl morphinans
    Patent number: 7671204
    Abstract: The present invention provides a synthetic process for the N-demethylation of N-methyl morphinans. In particular, the invention provides improved synthetic methods for the preparation of N-demethylated morphinan compounds that may be employed as starting materials, for example, commonly available N-methyl opiates such as oripavine and thebaine, and C(3)-protected hydroxy derivatives of oripavine.
    Type: Grant
    Filed: December 17, 2008
    Date of Patent: March 2, 2010
    Assignee: Mallinckrodt Inc.
    Inventors: Peter X. Wang, Tao Jiang, Gary L. Cantrell, David W. Berberich
  • Buprenorphine formulations for intranasal delivery
    Patent number: 7666876
    Abstract: Aqueous formulations suitable for intranasal administration comprise buprenorphine or a physiologically acceptable salt or ester thereof and (a) a pectin having a degree of esterification of less than 50%, (b) chitosan and a polyoxyethylene-polyoxypropylene copolymer (poloxamer) or (c) chitosan and hydroxypropylmethylcellulose. Such formulations can induce rapid and prolonged analgesia when delivered intranasally to a patient. The buprenorphine or buprenorphine salt or ester may be delivered to the bloodstream to produce within 30 minutes a therapeutic plasma concentration of buprenorphine, Cther, of 0.2 ng/ml or greater which is maintained for a duration Tmaint of at least 2 hours.
    Type: Grant
    Filed: March 19, 2002
    Date of Patent: February 23, 2010
    Assignees: Vernalis (R&D) Limited, Archimedes Development Limited
    Inventors: Phillip John Birch, Ann Gail Hayes, Peter James Watts, Jonathan David Castile
  • PROCESS FOR MAKING MORPHINAN-6alpha-OLS
    Publication number: 20100036128
    Abstract: The present invention provides a process whereby morphinan-6-ones can be converted stereospecifically to the corresponding morphinan-6?-ols by catalytic hydrogenation under basic conditions.
    Type: Application
    Filed: August 10, 2009
    Publication date: February 11, 2010
    Inventors: Robert Rezaie, Timothy S. Bailey
  • 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 FOR THE COVALENT COUPLING OF TWO MOLECULES BY MEANS OF A DIELS-ALDER REACTION WITH INVERSE ELECTRON REQUIREMENT
    Publication number: 20100016545
    Abstract: The present invention relates to a process for linking two molecules by means of a Diels Alder reaction with inverse electron requirement (DARinv), comprising the following steps: reaction of a (a) triazine or tetrazine with one or more electron-attracting substituents on the ring as a diene component, the electron-attracting substituents being selected from: COOR C(O)NR2 CX3 (X=halogen) halogen CN SO2—R or SO3—R PR2 wherein R?H, alkyl, aryl, heterocycle, which in turn may be substituted, where appropriate, with alkyl, OH, SH, halogen, aryl, heterocycle, nitro, carboxyamido or amine group.
    Type: Application
    Filed: June 18, 2007
    Publication date: January 21, 2010
    Applicant: DEUTSCHES KREBSFORSCHUNGSZENTRUM STIFTUNG DES OFFENTLICHEN RECHTS
    Inventors: Manfred Wiessler, Eduard Müller, Peter Lorenz, Christian Kliem, Heinz Fleischhacker
  • Methods of synthesis of morphinans
    Publication number: 20090318699
    Abstract: The disclosure describes morphinan compounds and methods for their synthesis. Preferred methods according to the disclosure allow for large-scale preparation of diastereomerically enriched morphinans. Preferred methods according to the disclosure may also allow for the preparation of diastereomerically enriched morphinans using less time, and/or using fewer reaction steps, and/or providing better yield than previously used methods for preparing morphinans. The methods disclosed herein find utility in synthetic organic chemistry as well as medicinal chemistry.
    Type: Application
    Filed: June 20, 2008
    Publication date: December 24, 2009
    Inventor: John A. Lawson
  • Process for the Preparation of 6-Beta Hydroxy Morphinan Compounds
    Publication number: 20090312552
    Abstract: The invention provides processes for the conversion of a 6-keto morphinan to a 6-hydroxy morphinan. In particular, the invention provides a stereoselective process for the conversion of a 6-keto morphinan to a 6-beta-hydroxy morphinan.
    Type: Application
    Filed: June 16, 2009
    Publication date: December 17, 2009
    Applicant: Mallinckrodt inc.
    Inventors: Jian Bao, Tao Jiang, Gary L. Cantrell
  • 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
  • LARGE SUBSTITUENT, NON-PHENOLIC OPIOIDS AND METHODS OF USE THEREOF
    Publication number: 20090247562
    Abstract: 8-Substituted-2,6-methano-3-benzazocines of general structure are useful as analgesics, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction medications.
    Type: Application
    Filed: June 3, 2009
    Publication date: October 1, 2009
    Applicant: RENSSELAER POLYTECHNIC INSTITUTE
    Inventor: Mark P. Wentland
  • Papaver Somniferum Strain With High Concentration Of Thebaine
    Publication number: 20090227796
    Abstract: The present invention is directed to an improved poppy straw, concentrate of poppy straw and opium of Papaver somniferum for the production of thebaine containing little or no oripavine, codeine or morphine. The present invention also provides plants, stands and seeds of Papaver somniferum and methods for the production of thebaine.
    Type: Application
    Filed: March 5, 2009
    Publication date: September 10, 2009
    Inventor: Anthony J. Fist
  • 6-Aminomorphinane Derivatives, Method for the Production and Use Thereof
    Publication number: 20090209570
    Abstract: This invention relates to compounds of the formula (I).
    Type: Application
    Filed: April 27, 2009
    Publication date: August 20, 2009
    Inventors: Johannes SCHUTZ, Helmut SCHMIDHAMMER
  • Registry Method and Control System for Dea Schedule II-V Medicines
    Publication number: 20090208413
    Abstract: The present invention provides compositions and methods for synthesizing labeled drugs. The present invention further provides methods for preventing or stopping prescription drug abuse for all agents registered as a Drug Enforcement Agency (DEA) schedule II through schedule V medications. According to the present invention, methods are provided for monitoring patient compliance with prescribed drug treatment. The present invention also provides methods for facilitating a replacement prescription when a patient is left without access to their prescribed drug. Furthermore, the present invention provides a method to improve employee compliance with an employer's drug policies via either a voluntary or compulsory system for enhanced drug testing.
    Type: Application
    Filed: February 23, 2006
    Publication date: August 20, 2009
    Inventors: Alan J Reis, Christian Schafmeister
  • Large substituent, non-phenolic opioids
    Patent number: 7557119
    Abstract: 8-Substituted-2,6-methano-3-benzazocines of general structure are useful as analgesics, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction medications.
    Type: Grant
    Filed: July 21, 2006
    Date of Patent: July 7, 2009
    Assignee: Rensselaer Polytechnic Institute
    Inventor: Mark P. Wentland
  • 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
  • Sinomenine derivatives and processes for their synthesis
    Publication number: 20090156816
    Abstract: The invention generally provides processes and intermediate compounds useful for the production of sinomenine derivatives. In particular, the process may encompass synthetic routes for the production of (+)-sinomenine derivatives and their intermediates.
    Type: Application
    Filed: 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, John Brandt
  • Process for the preparation of buprenorphine and derivatives for buprenorphine
    Publication number: 20090156817
    Abstract: The invention generally provides processes for the production of buprenophine and derivatives of buprenorphine. In particular, the process may encompass synthetic routes for the production of buprenorphine or derivatives of buprenorphine from norhydromorphone or derivatives of norhydromorphone.
    Type: 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
  • N-demethylation of N-methyl morphinans
    Publication number: 20090156815
    Abstract: The present invention provides a synthetic process for the N-demethylation of N-methyl morphinans. In particular, the invention provides improved synthetic methods for the preparation of N-demethylated morphinan compounds that may be employed as starting materials, for example, commonly available N-methyl opiates such as oripavine and thebaine, and C(3)-protected hydroxy derivatives of oripavine.
    Type: Application
    Filed: December 17, 2008
    Publication date: June 18, 2009
    Inventors: Peter X. Wang, Tao Jiang, Gary L. Cantrell, David W. Berberich
  • 6-aminomorphinane derivatives, method for production and use thereof
    Patent number: 7538118
    Abstract: This invention relates to compounds of the formula (I).
    Type: Grant
    Filed: December 16, 2002
    Date of Patent: May 26, 2009
    Assignee: Alcasynn Pharmaceuticals GmbH
    Inventors: Johannes Schütz, Helmut Schmidhammer
  • DEUTERIUM-ENRICHED BUPRENORPHINE
    Publication number: 20090082383
    Abstract: The present application describes deuterium-enriched buprenorphine, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
    Type: Application
    Filed: September 19, 2008
    Publication date: March 26, 2009
    Applicant: Protia, LLC
    Inventor: Anthony W. Czarnik
  • Method of Altering the Alkaloid Composition in Poppy Plants
    Publication number: 20090075822
    Abstract: The method of altering the alkaloid composition of a poppy plant comprising the step of applying an effective amount of acylcyclohexanedione compound or agriculturally acceptable salt thereof to said poppy plant or locus thereof. Further, the present invention also provides the method of altering the alkaloid composition of a poppy plant comprising the step of applying an effective amount of methyl jasmonate or agriculturally acceptable salt thereof to said poppy plant or locus thereof.
    Type: Application
    Filed: May 6, 2005
    Publication date: March 19, 2009
    Applicant: GLAXOSMITHKLINE AUSTRALIA PTY LTD
    Inventor: Paul Cotterill
  • DEUTERIUM-ENRICHED NALMEFENE
    Publication number: 20090076052
    Abstract: The present application describes deuterium-enriched nalmefene, 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