Two Of The Cyclos Share At Least Three Ring Members (e.g., Etheno Morphides, Etc.) Patents (Class 546/39)
  • Patent number: 11390628
    Abstract: Disclosed are methods for preparing buprenorphine from, for example, compounds such as nororipavine and northebaine.
    Type: Grant
    Filed: May 21, 2018
    Date of Patent: July 19, 2022
    Assignee: River Stone Biotech LLC
    Inventors: Patrick Roussel, Jimmy Van Wiltenburg, Marco Santella
  • Patent number: 11136331
    Abstract: There is provided a novel process for the preparation of a compound of formula I, wherein R1, R2, W, Z and are as described in the description, by demethylation of a corresponding O-methyl derivative with a borohydride-based reagent. This process may be used in the preparation of buprenorphine.
    Type: Grant
    Filed: October 12, 2018
    Date of Patent: October 5, 2021
    Assignee: CAMBREX CHARLES CITY, INC.
    Inventors: Par Holmberg, Lars Eklund, David Adams, Michael Letourneau, Margus Eek, Alo Soone
  • Patent number: 10745406
    Abstract: The present invention provides a process for the preparation of a compound of formula (VI), or a salt or derivative thereof, wherein R1 and R2 are independently C1-8 alkyl and * represents a stereocentre.
    Type: Grant
    Filed: October 28, 2016
    Date of Patent: August 18, 2020
    Assignee: EURO-CELTIQUE S.A.
    Inventors: Steve Whitelock, Deborah Phyllis Harding, Carl David Turner
  • Patent number: 10351830
    Abstract: Compositions, methods, and kits are disclosed directed at haptens, immunogens and immunoassays for oxycodone and metabolites thereof. The compounds are exemplified by compounds of the Formula I. The method comprises providing in combination in a medium (i) a sample suspected of containing oxycodone and/or oxycodone metabolites, a compound of the Formula I wherein R4 or R5 is a label, and an antibody for oxycodone or a metabolite thereof. The medium is examined for the presence of a complex comprising the labeled compound of Formula I where the presence of such as complex indicates the presence of oxycodone or oxycodone metabolite in the sample.
    Type: Grant
    Filed: December 11, 2015
    Date of Patent: July 16, 2019
    Assignee: Siemens Healthcare Diagnostics Inc.
    Inventors: Yi Feng Zheng, Yali Yang, Guoping Wang
  • Patent number: 10035807
    Abstract: The present invention relates to a method of preparing a compound of Formula II-a? or Formula II-b?, wherein RI represents hydrogen or a linear, branched and/or cyclic alkyl or alkenyl group having 1 to 10 carbon atoms; RII represents a linear, branched and/or cyclic alkyl or alkenyl group having 1 to 10 carbon atoms; RIII represents hydrogen or a linear, branched and/or cyclic alkyl or alkenyl group having 1 to 10 carbon atoms or a linear, branched and/or cyclic alkoxy group having 1 to 10 carbon atoms; RIV represents hydrogen or a linear, branched and/or cyclic alkyl group having 1 to 10 carbon atoms or an optionally substituted aryl or alkylaryl group having 6 to 40 carbon atom or acetyl or silyl or a protective group; and RV represents hydrogen or a methyl group; wherein RI and RII are different from each other.
    Type: Grant
    Filed: March 11, 2016
    Date of Patent: July 31, 2018
    Assignee: SIEGFRIED AG
    Inventors: Stefan Sahli, Beat Theodor Weber
  • Patent number: 10030031
    Abstract: The invention provides a method of treating drug and alcohol abuse, depression, anxiety, or a compulsive disorder in a subject comprising administering to the subject a compound having the formula: or a pharmaceutically acceptable salt or solvate thereof, wherein R, R1, R2, R3, R4, R5, and X are as defined in the specification.
    Type: Grant
    Filed: October 3, 2017
    Date of Patent: July 24, 2018
    Assignee: The University of Bath
    Inventors: John Lewis, Stephen Husbands
  • Patent number: 9988392
    Abstract: The application is directed to compounds of Formula (I) and pharmaceutically acceptable salts and solvates thereof, wherein R1, R1a, R1b, R1c, X, Y, Z, G, O, W1 and W2 are defined as set forth in the specification. The invention is also directed to use of compounds of Formula (I), and the pharmaceutically acceptable salts and solvates thereof, to treat disorders responsive to the modulation of one or more opioid receptors, or as synthetic intermediates. Certain compounds of the present invention are especially useful for treating pain.
    Type: Grant
    Filed: December 23, 2014
    Date of Patent: June 5, 2018
    Assignee: PURDUE PHARMA L.P.
    Inventor: Laykea Tafesse
  • Patent number: 9834562
    Abstract: The application is directed to a process for increasing the proportion of 7?-epimer in an 7?/7?-epimer mixture of a 7-substituted 6?,14?-ethenomorphinan or a 7-substituted 6?,14?-ethanomorphinan, and specifically of compounds of Formula (I), wherein G, R2-R4, and are defined as set forth in the specification. The application is also directed to a process for purifying the 7?-epimer from an 7?/7?-epimer mixture of a 7-substituted 6?,14?-ethenomorphinan or a 7-substituted 6?,14?-ethanomorphinan. The application is also directed to a process for preparing 7?-substituted compounds of Formula Vb wherein G and R2-R5 are defined as set forth in the specification.
    Type: Grant
    Filed: December 23, 2013
    Date of Patent: December 5, 2017
    Assignee: RHODES TECHNOLOGIES
    Inventor: Helge Alfred Reisch
  • Patent number: 9732096
    Abstract: The present invention provides a buprenorphine dimer compound, wherein the two buprenorphine portions are linked via an ethylene spacer, wherein the spacer is bonded to the two opioid molecules via an ether bond. Pharmaceutical compositions comprising such a buprenorphine dimer drug are also disclosed, and the use of such compounds in the treatment of gastrointestinal hyperalgesia generally and in particular diarrhea-predominant irritable bowel syndrome.
    Type: Grant
    Filed: March 18, 2016
    Date of Patent: August 15, 2017
    Assignee: ORPHOMED, INC.
    Inventor: Nikhilesh Nihala Singh
  • Patent number: 9701688
    Abstract: The present invention is directed to a process for the preparation of opioid compounds such as buprenorphine, naltrexone, naloxone, nalbuphone, nalbuphine, and the like.
    Type: Grant
    Filed: April 17, 2015
    Date of Patent: July 11, 2017
    Assignee: NORAMCO, INC.
    Inventors: Matteo Conza, Vit Lellek, Hartmut Zinser
  • Patent number: 9701687
    Abstract: The present invention is directed to a process for the preparation of opioid compounds such as buprenorphine, naltrexone, naloxone, nalbuphone, nalbuphine, and the like.
    Type: Grant
    Filed: April 17, 2015
    Date of Patent: July 11, 2017
    Assignee: NORAMCO, INC.
    Inventors: Jessica Cardot, Wen-Chen Zhang
  • Patent number: 9624231
    Abstract: An improved process for preparing buprenorphine and a method for increasing the yield of buprenorphine or a derivative thereof.
    Type: Grant
    Filed: October 1, 2012
    Date of Patent: April 18, 2017
    Assignee: Johnson Matthey Public Limited Company
    Inventors: Nicolas Archer, David August, Michael Bease, Barbara Jamieson, Robert S. Marmor
  • Patent number: 9556156
    Abstract: The present invention discloses novel chemical compounds obtained by causing a covalent attachment of a modifying agent of the structure provided for formula 1, to a functional group or a heteroatom of a heterocyclic ring system in chemical compound with improved chemical and biological properties. Wherein: Y is DRUG-CO; DRUG-OCO; DRUG-NRCO, and X is selected from.
    Type: Grant
    Filed: October 7, 2013
    Date of Patent: January 31, 2017
    Assignee: SPHAERA PHARMA PTE LTD.
    Inventors: Sundeep Dugar, Frank Peter Hollinger, Dinesh Mahajan, Rhushikesh Chandrabhan Deokar
  • Patent number: 9309258
    Abstract: The present disclosure provides improved methods for N-dealkylation of tertiary amines, including methods for N-demethylation of alkaloids and opioids, in which the dealkylation reaction is carried out in a solvent comprising a tertiary alcohol. The present disclosure also provides improved processes for preparing semi-synthetic opioids that incorporate the disclosed methods for N-dealkylation of tertiary amines.
    Type: Grant
    Filed: December 2, 2014
    Date of Patent: April 12, 2016
    Assignee: Rhodes Technologies
    Inventors: Joshua Robert Giguere, Helge Alfred Reisch, Sergio Sandoval, Jake Larry Stymiest
  • Patent number: 9175000
    Abstract: The present invention is directed to Buprenorphine Analog compounds of the Formula I, Formula II, Formula III, Formula IV, and Formula V, wherein R1, R2, R3a, R3b, R15a, R15b, X, Q, G, and Y are as defined herein. Compounds of the Invention are useful for treating pain and other conditions modulated by activity of opioid receptors.
    Type: Grant
    Filed: December 4, 2013
    Date of Patent: November 3, 2015
    Assignee: Purdue Pharma L.P.
    Inventor: Mark A. Youngman
  • Patent number: 9045497
    Abstract: A high-yielding method for the N-demethylation of oxycodone- and oxymorphone-N-oxides by the reaction of these compounds with cyclodehydration reagents has been performed. This method has been utilized to improve the synthesis of various morphine analogs, such as naltrexone, nalbuphone and naloxone.
    Type: Grant
    Filed: January 7, 2015
    Date of Patent: June 2, 2015
    Assignee: Brock University
    Inventors: Tomas Hudlicky, Lukas Werner, Ales Machara, Martina Wernerova, Mary Ann Endoma-Arias
  • Publication number: 20150133665
    Abstract: A high-yielding method for the N-demethylation of oxycodone- and oxymorphone-N-oxides by the reaction of these compounds with cyclodehydration reagents has been performed. This method has been utilized to improve the synthesis of various morphine analogs, such as naltrexone, nalbuphone and naloxone.
    Type: Application
    Filed: January 7, 2015
    Publication date: May 14, 2015
    Inventors: Tomas Hudlicky, Lukas Werner, Ales Machara, Martina Wernerova, Mary Ann Endoma-Arias
  • Publication number: 20150133664
    Abstract: The present invention relates to methods for the synthesis of morphine, codeine, intermediates, salts and derivatives thereof. In preferred embodiments, the invention relates to methods for improving the efficiency, steroselectivity, and overall yield of said codeine and morphine related derivatives and intermediates thereof. The present invention relates to new codeine and morphine related derivative compositions.
    Type: Application
    Filed: June 6, 2013
    Publication date: May 14, 2015
    Inventors: Philip Magnus, Bahman Ghavimi-Alagha
  • Publication number: 20150133483
    Abstract: The present invention provides a process for the preparation of a compound of formula (VI), or a salt or derivative thereof, wherein R1 and R2 are independently C1-8 alkyl and * represents a stereocentre.
    Type: Application
    Filed: August 29, 2014
    Publication date: May 14, 2015
    Inventors: Steve WHITELOCK, Deborah Phyllis HARDING, Carl David TURNER
  • Publication number: 20150087839
    Abstract: The present disclosure provides improved methods for N-dealkylation of tertiary amines, including methods for N-demethylation of alkaloids and opioids, in which the dealkylation reaction is carried out in a solvent comprising a tertiary alcohol. The present disclosure also provides improved processes for preparing semi-synthetic opioids that incorporate the disclosed methods for N-dealkylation of tertiary amines.
    Type: Application
    Filed: December 2, 2014
    Publication date: March 26, 2015
    Inventors: Joshua Robert GIGUERE, Helge Alfred REISCH, Sergio SANDOVAL, Jake Larry STYMIEST
  • Patent number: 8981098
    Abstract: The oxazolidine derived from the reaction of oxymorphone with the Burgess reagent, temporarily protected at O-3 and C-6, reacts with Grignard or other suitable metallic or organometallic reagents to directly provide, for example, A/-allyl, A/-methylcyclopropyl and /V-methylcyclobutyl derivatives that are further converted into naltrexone, naloxone, nalbuphone and nalbuphine in excellent yields. These morphine analogs can be prepared from the oxazolidine in a one-pot synthesis.
    Type: Grant
    Filed: January 30, 2013
    Date of Patent: March 17, 2015
    Assignee: Brock University
    Inventors: Tomas Hudlicky, Mary Ann Endoma-Arias
  • Patent number: 8981097
    Abstract: There is provided an efficient industrial process for the preparation of 21-cyclopropyl-7?-(2-hydroxy-3,3-dimethyl-2-butyl)-6,14-endo-ethano-6,7,8,14-tetrahydro-oripavine, i.e. buprenorphine of Formula-I in high yield and purity, with enhanced safety and eco-friendly norms. The invention further relates to an improved process for preparation of intermediates thereof in high yield and purity.
    Type: Grant
    Filed: June 11, 2014
    Date of Patent: March 17, 2015
    Assignee: Rusan Pharma Limited
    Inventors: Navin Satyapal Saxena, Kunal Saxena, Kaushik Babubhai Sata
  • Patent number: 8969358
    Abstract: The present invention is directed to Buprenorphine Analog compounds of Formula I, II, III, IV or V and including various stereoisomers (such as Formula IA shown below), wherein R1, R3a, R3b, R16, R15, G, Q, X, A and Z are as defined herein. Compounds of the Invention may be useful for preparing medicaments useful for treating pain, constipation, and other conditions modulated by activity of opioid and ORL-1 receptors. Compounds of the Invention may be useful for treating Conditions such as pain, constipation, and others modulated by activity of opioid and ORL-1 receptors.
    Type: Grant
    Filed: March 12, 2014
    Date of Patent: March 3, 2015
    Assignee: Purdue Pharma L.P.
    Inventors: Richard Goehring, Laykea Tafesse, Jiangchao Yao
  • Patent number: 8921556
    Abstract: The present disclosure provides improved methods for N-dealkylation of tertiary amines, including methods for N-demethylation of alkaloids and opioids, in which the dealkylation reaction is carried out in a solvent comprising a tertiary alcohol. The present disclosure also provides improved processes for preparing semi-synthetic opioids that incorporate the disclosed methods for N-dealkylation of tertiary amines.
    Type: Grant
    Filed: December 11, 2012
    Date of Patent: December 30, 2014
    Assignee: Rhodes Technologies
    Inventors: Joshua Robert Giguere, Helge Alfred Reisch, Sergio Sandoval, Jake Larry Stymiest
  • Publication number: 20140364612
    Abstract: There is provided an efficient industrial process for the preparation of 21-cyclopropyl-7?-(2-hydroxy-3,3-dimethyl-2-butyl)-6,14-endo-ethano-6,7,8,14-tetrahydro-oripavine, i.e. buprenorphine of Formula-I in high yield and purity, with enhanced safety and eco-friendly norms. The invention further relates to an improved process for preparation of intermediates thereof in high yield and purity.
    Type: Application
    Filed: June 11, 2014
    Publication date: December 11, 2014
    Inventors: Navin Satyapal SAXENA, Kunal SAXENA, Kaushik Babubhai SATA
  • Publication number: 20140364448
    Abstract: The present invention is directed to Buprenorphine Analog compounds of the Formula (I), Formula (IA) or Formula (IB) shown below, wherein R1, R1a, R2, R8, R3a, R3b, G, X, Z, Y, and A® are as defined herein. Compounds of the Invention are useful for treating pain, constipation, and other conditions modulated by activity of opioid and ORL-1 receptors.
    Type: Application
    Filed: December 7, 2012
    Publication date: December 11, 2014
    Applicant: PURDUE PHARMA L.P.
    Inventor: Donald J. Kyle
  • Patent number: 8901148
    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: August 23, 2013
    Date of Patent: December 2, 2014
    Assignee: Rensselaer Polytechnic Institute
    Inventor: Mark P. Wentland
  • Patent number: 8901175
    Abstract: The use of opioids or opioid mimetics is suggested for the manufacture of a medicament for the treatment of resistant cancer patients.
    Type: Grant
    Filed: January 29, 2009
    Date of Patent: December 2, 2014
    Assignee: Universität Ulm
    Inventors: Erich Miltner, Claudia Friesen, Andreas Alt
  • Patent number: 8853401
    Abstract: The present application describes processes for the synthesis of morphinane and morphinone compounds, useful as pharmaceutical agents. Also included are novel intermediates useful in the preparation of these compounds. The process comprises quaternization of oripavine to provide a mixture of the R- and S-isomeric (at the nitrogen) quaternary salts. The R-isomer is readily isolated and converted to various N-(R)-morphinane and N-(S)-morphinone compounds. The R-isomer, S-isomer or a mixture of R- and S-isomers may be demethylated and converted to various morphinane and morphinone compounds.
    Type: Grant
    Filed: April 22, 2010
    Date of Patent: October 7, 2014
    Assignee: Brock University
    Inventors: Tomas Hudlicky, Robert Carroll, Hannes Leisch, Ales Machara, Lukas Werner, David R. Adams
  • Publication number: 20140275117
    Abstract: The present invention is directed to Buprenorphine Analog compounds of Formula I, II, III, IV or V and including various stereoisomers (such as Formula IA shown below), wherein R1, R3a, R3b, R16, R15, G, Q, X, A and Z are as defined herein. Compounds of the Invention may be useful for preparing medicaments useful for treating pain, constipation, and other conditions modulated by activity of opioid and ORL-1 receptors. Compounds of the Invention may be useful for treating Conditions such as pain, constipation, and others modulated by activity of opioid and ORL-1 receptors.
    Type: Application
    Filed: March 12, 2014
    Publication date: September 18, 2014
    Applicant: PURDUE PHARMA L.P.
    Inventors: Richard Goehring, Laykea Tafesse, Jiangchao Yao
  • Publication number: 20140235860
    Abstract: An improved process for preparing buprenorphine and a method for increasing the yield of buprenorphine or a derivative thereof.
    Type: Application
    Filed: October 1, 2012
    Publication date: August 21, 2014
    Applicant: JOHNSON MATTEY PUBLIC LIMITED COMPANY
    Inventors: Nicolas Archer, David August, Michael Bease, Barbara Jamieson, Robert S. Marmor
  • Publication number: 20140213603
    Abstract: The invention provides orvinol and thevinol compounds useful for the treatment of drug and alcohol abuse, the compounds being particularly useful for the prevention of relapse in recovering addicts.
    Type: Application
    Filed: July 5, 2012
    Publication date: July 31, 2014
    Inventors: John Lewis, Stephen Husbands
  • Publication number: 20140187571
    Abstract: The application is directed to compounds of Formula I-A and pharmaceutically acceptable salts and solvates thereof, wherein Cy, R1a-R3a, R4a, and R4b are defined as set forth in the specification. The invention is also directed to use of compounds of Formula I-A to treat disorders responsive to the modulation of one or more opioid receptors, or as synthetic intermediates. Certain compounds of the present invention are especially useful for treating pain.
    Type: Application
    Filed: December 23, 2013
    Publication date: July 3, 2014
    Applicant: Purdue Pharma L.P.
    Inventors: Donald J. KYLE, Laykea Tafesse, Xiaoming Zhou
  • Publication number: 20140163058
    Abstract: The present invention is directed to Buprenorphine Analog compounds of the Formula I, Formula II, Formula III, Formula IV, and Formula V, wherein R1, R2, R3a, R3b, R15a, R15b, X, Q, G, and Y are as defined herein. Compounds of the Invention are useful for treating pain and other conditions modulated by activity of opioid receptors.
    Type: Application
    Filed: December 4, 2013
    Publication date: June 12, 2014
    Applicant: Purdue Pharma L.P.
    Inventor: Mark A. Youngman
  • Patent number: 8710226
    Abstract: The present invention relates to an improved process for preparing morphinane analogues of formula 1 wherein the substituents R1, R2, R2a, R3, R4, R5 and Y have the meanings as defined in the specifications.
    Type: Grant
    Filed: August 29, 2013
    Date of Patent: April 29, 2014
    Assignee: Sun Pharmaceutical Industries Limited
    Inventors: Nileshkumar Sureshbhai Patel, Srinivasu Kilaru, Rajamannar Thennati
  • Patent number: 8709431
    Abstract: Enediyne compounds having a structure according to formula (I), where R0, R2, R3, R4, R5, R6, and R7 are defined herein, can be used in chemotherapeutic drugs, especially in conjugates, for the treatment of diseases such as cancer.
    Type: Grant
    Filed: February 11, 2013
    Date of Patent: April 29, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Naidu S. Chowdari, Sanjeev Gangwar, Bilal Sufi
  • Publication number: 20140057931
    Abstract: The present invention is directed to Buprenorphine Analog compounds of the Formula (I), Formula (IA) or Formula (IB) shown below, wherein R1, R2, R8, R3a, R 3b, G, X, Z and Y are as defined herein. Compounds of the Invention are useful for treating pain, constipation, and other conditions modulated by activity of opioid and ORL-1 receptors.
    Type: Application
    Filed: September 20, 2011
    Publication date: February 27, 2014
    Applicant: PURDUE PHARMA L.P.
    Inventors: Donald J. Kyle, Laykea Tafesse
  • Publication number: 20140057932
    Abstract: The application is directed to compounds of Formula I and pharmaceutically acceptable salts, prodrugs, and solvates thereof, wherein G, R2-R5, and are defined as set forth in the specification. The invention is also directed to use of compounds of Formula I as synthetic intermediates or to treat disorders responsive to the modulation of one or more opiopid receptors. Certain compounds of the present invention are especially useful for treating pain.
    Type: Application
    Filed: August 26, 2013
    Publication date: February 27, 2014
    Applicant: Rhodes Technologies
    Inventor: Helge A. REISCH
  • Publication number: 20140031550
    Abstract: The present invention relates to an improved process for preparing morphinane analogues of formula 1 wherein the substituents R1, R2, R2a, R3, R4, R5 and Y have the meanings as defined in the specifications.
    Type: Application
    Filed: August 29, 2013
    Publication date: January 30, 2014
    Applicant: Sun Pharmaceutical Industries Ltd.
    Inventors: Nileshkumar Sureshbhai PATEL, Srinivasu KILARU, Rajamannar THENNATI
  • Patent number: 8530494
    Abstract: The present invention is directed to Buprenorphine Analog compounds of the Formula I, Formula II or Formula III shown below, wherein R1, R2, R8, R3, R3a, R3b, X, Z and Y are as defined herein. Compounds of the Invention are useful for treating pain and other conditions modulated by activity of opioid and ORL1 receptors.
    Type: Grant
    Filed: July 30, 2009
    Date of Patent: September 10, 2013
    Assignee: Purdue Pharma LP
    Inventors: Donald J. Kyle, R. Richard Goehring, Marian E. Fundytus
  • Patent number: 8530660
    Abstract: The present invention relates to carboxamide-substituted dyes, the production and use of such dyes as labeling groups in analytics.
    Type: Grant
    Filed: March 18, 2011
    Date of Patent: September 10, 2013
    Assignee: ATTO-TEC GmbH
    Inventors: Jutta Arden-Jacob, Karl-Heinz Drexhage, Monika Hamers-Schneider, Norbert Kemnitzer, Alexander Zilles
  • Publication number: 20130209494
    Abstract: Enediyne compounds having a structure according to formula (I), where R0, R2, R3, R4, R5, R6, and R7 are defined herein, can be used in chemotherapeutic drugs, especially in conjugates, for the treatment of diseases such as cancer.
    Type: Application
    Filed: February 11, 2013
    Publication date: August 15, 2013
    Applicant: Bristol-Myers Squibb Company
    Inventor: Bristol-Myers Squibb Company
  • Publication number: 20130197028
    Abstract: Agonists and antagonists of nAChR?7 and their use as therapeutic agents for treating and managing inflammatory bowel diseases (IBD), such as Crohn's disease (CD) and ulcerative colitis (UC), are disclosed. Agonists and antagonists of nAChR?7 and their use as therapeutic agents for treating and managing inflammatory bowel diseases (IBD), such as Crohn's disease (CD) and ulcerative colitis (UC), are disclosed.
    Type: Application
    Filed: June 24, 2011
    Publication date: August 1, 2013
    Applicants: OKLAHOMA MEDICAL RESEARCH FOUNDATION, THE JOHNS HOPKINS UNIVERSITY
    Inventors: Xuhang Li, Philip Alex, Michael B. Centola
  • Patent number: 8492547
    Abstract: The present invention provides processes for the enrichment of buprenorphine in a product. In particular, the present invention provides processes for the enrichment of buprenorphine in a product using chromatographic techniques.
    Type: Grant
    Filed: June 18, 2010
    Date of Patent: July 23, 2013
    Assignee: Mallinckrodt LLC
    Inventor: Enrico A. Antonini
  • Publication number: 20130123292
    Abstract: Described herein are opioid prodrugs, methods of making opioid prodrugs, formulations comprising opioid prodrugs, and methods of using opioid prodrugs. One embodiment described herein relates to the transdermal administration of a buprenorphine prodrug in an abuse-resistant formulation for treating and preventing diseases and/or disorders.
    Type: Application
    Filed: November 7, 2012
    Publication date: May 16, 2013
    Applicant: AllTranz Inc.
    Inventor: AllTranz Inc.
  • Publication number: 20130102784
    Abstract: The present disclosure provides improved methods for N-dealkylation of tertiary amines, including methods for N-demethylation of alkaloids and opioids, in which the dealkylation reaction is carried out in a solvent comprising a tertiary alcohol. The present disclosure also provides improved processes for preparing semi-synthetic opioids that incorporate the disclosed methods for N-dealkylation of tertiary amines.
    Type: Application
    Filed: December 11, 2012
    Publication date: April 25, 2013
    Applicant: Rhodes Technologies
    Inventor: Rhodes Technologies
  • Patent number: 8318937
    Abstract: A process for preparing a compound of formula (A), (B) or (C): wherein P is H, CH3 or a hydroxyl protecting group; X is O, a protected ketone, OH, a protected hydroxyl group or H; Y is OH, a protected hydroxyl group or H; W is C(CH3)2OH, C(CH3)(C(CH3)3)OH or COCH3; Z is C2-C10 alkyl or C2-C10 arylalkyl; and is a single bond or a double bond, is disclosed. The process is a reductive alkylation in the presence of hydrogen and a reductive alkylation catalyst.
    Type: Grant
    Filed: February 18, 2011
    Date of Patent: November 27, 2012
    Assignee: Johnson Matthey Public Limited Company
    Inventors: Melville Mitchell, Neil Kenneth Thomson, George Scott Wilson, Neil John Goodwin, Maureen Joan Young
  • Patent number: 8309568
    Abstract: Described herein are opioid prodrugs, methods of making opioid prodrugs, formulations comprising opioid prodrugs, and methods of using opioid prodrugs. One embodiment described herein relates to the transdermal administration of a buprenorphine prodrug in an abuse-resistant formulation for treating and preventing diseases and/or disorders.
    Type: Grant
    Filed: February 19, 2009
    Date of Patent: November 13, 2012
    Assignee: Alltranz Inc.
    Inventors: Audra Lynn Stinchcomb, Miroslaw Jerzy Golinski, Dana Carmel Hammell, Jeffrey Lynn Howard
  • Publication number: 20120283443
    Abstract: A high-yielding method for the N-demethylation of oxycodone- and oxymorphone-N-oxides by the reaction of these compounds with cyclodehydration reagents has been performed. This method has been utilized to improve the synthesis of various morphine analogs, such as naltrexone, nalbuphone and naloxone.
    Type: Application
    Filed: May 2, 2012
    Publication date: November 8, 2012
    Applicant: Brock University
    Inventors: Tomas Hudlicky, Lukas Werner, Ales Machara, Martina Wernerova, Mary Ann Endoma-Arias
  • Patent number: 8293906
    Abstract: The invention provides processes for the production of opiate alkaloids. In particular, the present invention provides processes for the formation of buprenorphine and derivatives of buprenorphine that minimizes the formation of impurities.
    Type: Grant
    Filed: September 29, 2009
    Date of Patent: October 23, 2012
    Assignee: Mallinckrodt LLC
    Inventors: Esa T. Jarvi, James R. Meyer