Two Of The Cyclos Share At Least Three Ring Members (e.g., Etheno Morphides, Etc.) Patents (Class 546/39)
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Patent number: 11390628Abstract: Disclosed are methods for preparing buprenorphine from, for example, compounds such as nororipavine and northebaine.Type: GrantFiled: May 21, 2018Date of Patent: July 19, 2022Assignee: River Stone Biotech LLCInventors: Patrick Roussel, Jimmy Van Wiltenburg, Marco Santella
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Patent number: 11136331Abstract: 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: GrantFiled: October 12, 2018Date of Patent: October 5, 2021Assignee: CAMBREX CHARLES CITY, INC.Inventors: Par Holmberg, Lars Eklund, David Adams, Michael Letourneau, Margus Eek, Alo Soone
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Patent number: 10745406Abstract: 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: GrantFiled: October 28, 2016Date of Patent: August 18, 2020Assignee: EURO-CELTIQUE S.A.Inventors: Steve Whitelock, Deborah Phyllis Harding, Carl David Turner
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Patent number: 10351830Abstract: 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: GrantFiled: December 11, 2015Date of Patent: July 16, 2019Assignee: Siemens Healthcare Diagnostics Inc.Inventors: Yi Feng Zheng, Yali Yang, Guoping Wang
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Patent number: 10035807Abstract: 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: GrantFiled: March 11, 2016Date of Patent: July 31, 2018Assignee: SIEGFRIED AGInventors: Stefan Sahli, Beat Theodor Weber
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Patent number: 10030031Abstract: 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: GrantFiled: October 3, 2017Date of Patent: July 24, 2018Assignee: The University of BathInventors: John Lewis, Stephen Husbands
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Patent number: 9988392Abstract: 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: GrantFiled: December 23, 2014Date of Patent: June 5, 2018Assignee: PURDUE PHARMA L.P.Inventor: Laykea Tafesse
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Patent number: 9834562Abstract: 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: GrantFiled: December 23, 2013Date of Patent: December 5, 2017Assignee: RHODES TECHNOLOGIESInventor: Helge Alfred Reisch
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Patent number: 9732096Abstract: 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: GrantFiled: March 18, 2016Date of Patent: August 15, 2017Assignee: ORPHOMED, INC.Inventor: Nikhilesh Nihala Singh
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Patent number: 9701688Abstract: 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: GrantFiled: April 17, 2015Date of Patent: July 11, 2017Assignee: NORAMCO, INC.Inventors: Matteo Conza, Vit Lellek, Hartmut Zinser
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Patent number: 9701687Abstract: 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: GrantFiled: April 17, 2015Date of Patent: July 11, 2017Assignee: NORAMCO, INC.Inventors: Jessica Cardot, Wen-Chen Zhang
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Patent number: 9624231Abstract: An improved process for preparing buprenorphine and a method for increasing the yield of buprenorphine or a derivative thereof.Type: GrantFiled: October 1, 2012Date of Patent: April 18, 2017Assignee: Johnson Matthey Public Limited CompanyInventors: Nicolas Archer, David August, Michael Bease, Barbara Jamieson, Robert S. Marmor
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Patent number: 9556156Abstract: 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: GrantFiled: October 7, 2013Date of Patent: January 31, 2017Assignee: SPHAERA PHARMA PTE LTD.Inventors: Sundeep Dugar, Frank Peter Hollinger, Dinesh Mahajan, Rhushikesh Chandrabhan Deokar
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Patent number: 9309258Abstract: 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: GrantFiled: December 2, 2014Date of Patent: April 12, 2016Assignee: Rhodes TechnologiesInventors: Joshua Robert Giguere, Helge Alfred Reisch, Sergio Sandoval, Jake Larry Stymiest
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Patent number: 9175000Abstract: 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: GrantFiled: December 4, 2013Date of Patent: November 3, 2015Assignee: Purdue Pharma L.P.Inventor: Mark A. Youngman
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Patent number: 9045497Abstract: 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: GrantFiled: January 7, 2015Date of Patent: June 2, 2015Assignee: Brock UniversityInventors: Tomas Hudlicky, Lukas Werner, Ales Machara, Martina Wernerova, Mary Ann Endoma-Arias
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Publication number: 20150133665Abstract: 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: ApplicationFiled: January 7, 2015Publication date: May 14, 2015Inventors: Tomas Hudlicky, Lukas Werner, Ales Machara, Martina Wernerova, Mary Ann Endoma-Arias
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Publication number: 20150133664Abstract: 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: ApplicationFiled: June 6, 2013Publication date: May 14, 2015Inventors: Philip Magnus, Bahman Ghavimi-Alagha
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Publication number: 20150133483Abstract: 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: ApplicationFiled: August 29, 2014Publication date: May 14, 2015Inventors: Steve WHITELOCK, Deborah Phyllis HARDING, Carl David TURNER
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Publication number: 20150087839Abstract: 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: ApplicationFiled: December 2, 2014Publication date: March 26, 2015Inventors: Joshua Robert GIGUERE, Helge Alfred REISCH, Sergio SANDOVAL, Jake Larry STYMIEST
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Patent number: 8981098Abstract: 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: GrantFiled: January 30, 2013Date of Patent: March 17, 2015Assignee: Brock UniversityInventors: Tomas Hudlicky, Mary Ann Endoma-Arias
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Patent number: 8981097Abstract: 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: GrantFiled: June 11, 2014Date of Patent: March 17, 2015Assignee: Rusan Pharma LimitedInventors: Navin Satyapal Saxena, Kunal Saxena, Kaushik Babubhai Sata
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Patent number: 8969358Abstract: 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: GrantFiled: March 12, 2014Date of Patent: March 3, 2015Assignee: Purdue Pharma L.P.Inventors: Richard Goehring, Laykea Tafesse, Jiangchao Yao
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Patent number: 8921556Abstract: 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: GrantFiled: December 11, 2012Date of Patent: December 30, 2014Assignee: Rhodes TechnologiesInventors: Joshua Robert Giguere, Helge Alfred Reisch, Sergio Sandoval, Jake Larry Stymiest
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Publication number: 20140364612Abstract: 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: ApplicationFiled: June 11, 2014Publication date: December 11, 2014Inventors: Navin Satyapal SAXENA, Kunal SAXENA, Kaushik Babubhai SATA
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Publication number: 20140364448Abstract: 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: ApplicationFiled: December 7, 2012Publication date: December 11, 2014Applicant: PURDUE PHARMA L.P.Inventor: Donald J. Kyle
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Patent number: 8901148Abstract: 8-Substituted-2,6-methano-3-benzazocines of general structure are useful as analgesics, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction medications.Type: GrantFiled: August 23, 2013Date of Patent: December 2, 2014Assignee: Rensselaer Polytechnic InstituteInventor: Mark P. Wentland
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Patent number: 8901175Abstract: The use of opioids or opioid mimetics is suggested for the manufacture of a medicament for the treatment of resistant cancer patients.Type: GrantFiled: January 29, 2009Date of Patent: December 2, 2014Assignee: Universität UlmInventors: Erich Miltner, Claudia Friesen, Andreas Alt
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Patent number: 8853401Abstract: 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: GrantFiled: April 22, 2010Date of Patent: October 7, 2014Assignee: Brock UniversityInventors: Tomas Hudlicky, Robert Carroll, Hannes Leisch, Ales Machara, Lukas Werner, David R. Adams
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Publication number: 20140275117Abstract: 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: ApplicationFiled: March 12, 2014Publication date: September 18, 2014Applicant: PURDUE PHARMA L.P.Inventors: Richard Goehring, Laykea Tafesse, Jiangchao Yao
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Publication number: 20140235860Abstract: An improved process for preparing buprenorphine and a method for increasing the yield of buprenorphine or a derivative thereof.Type: ApplicationFiled: October 1, 2012Publication date: August 21, 2014Applicant: JOHNSON MATTEY PUBLIC LIMITED COMPANYInventors: Nicolas Archer, David August, Michael Bease, Barbara Jamieson, Robert S. Marmor
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Publication number: 20140213603Abstract: 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: ApplicationFiled: July 5, 2012Publication date: July 31, 2014Inventors: John Lewis, Stephen Husbands
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Publication number: 20140187571Abstract: 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: ApplicationFiled: December 23, 2013Publication date: July 3, 2014Applicant: Purdue Pharma L.P.Inventors: Donald J. KYLE, Laykea Tafesse, Xiaoming Zhou
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Publication number: 20140163058Abstract: 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: ApplicationFiled: December 4, 2013Publication date: June 12, 2014Applicant: Purdue Pharma L.P.Inventor: Mark A. Youngman
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Patent number: 8710226Abstract: 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: GrantFiled: August 29, 2013Date of Patent: April 29, 2014Assignee: Sun Pharmaceutical Industries LimitedInventors: Nileshkumar Sureshbhai Patel, Srinivasu Kilaru, Rajamannar Thennati
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Patent number: 8709431Abstract: 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: GrantFiled: February 11, 2013Date of Patent: April 29, 2014Assignee: Bristol-Myers Squibb CompanyInventors: Naidu S. Chowdari, Sanjeev Gangwar, Bilal Sufi
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Publication number: 20140057931Abstract: 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: ApplicationFiled: September 20, 2011Publication date: February 27, 2014Applicant: PURDUE PHARMA L.P.Inventors: Donald J. Kyle, Laykea Tafesse
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Publication number: 20140057932Abstract: 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: ApplicationFiled: August 26, 2013Publication date: February 27, 2014Applicant: Rhodes TechnologiesInventor: Helge A. REISCH
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Publication number: 20140031550Abstract: 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: ApplicationFiled: August 29, 2013Publication date: January 30, 2014Applicant: Sun Pharmaceutical Industries Ltd.Inventors: Nileshkumar Sureshbhai PATEL, Srinivasu KILARU, Rajamannar THENNATI
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Patent number: 8530494Abstract: 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: GrantFiled: July 30, 2009Date of Patent: September 10, 2013Assignee: Purdue Pharma LPInventors: Donald J. Kyle, R. Richard Goehring, Marian E. Fundytus
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Patent number: 8530660Abstract: The present invention relates to carboxamide-substituted dyes, the production and use of such dyes as labeling groups in analytics.Type: GrantFiled: March 18, 2011Date of Patent: September 10, 2013Assignee: ATTO-TEC GmbHInventors: Jutta Arden-Jacob, Karl-Heinz Drexhage, Monika Hamers-Schneider, Norbert Kemnitzer, Alexander Zilles
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Publication number: 20130209494Abstract: 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: ApplicationFiled: February 11, 2013Publication date: August 15, 2013Applicant: Bristol-Myers Squibb CompanyInventor: Bristol-Myers Squibb Company
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Publication number: 20130197028Abstract: 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: ApplicationFiled: June 24, 2011Publication date: August 1, 2013Applicants: OKLAHOMA MEDICAL RESEARCH FOUNDATION, THE JOHNS HOPKINS UNIVERSITYInventors: Xuhang Li, Philip Alex, Michael B. Centola
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Patent number: 8492547Abstract: 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: GrantFiled: June 18, 2010Date of Patent: July 23, 2013Assignee: Mallinckrodt LLCInventor: Enrico A. Antonini
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Publication number: 20130123292Abstract: 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: ApplicationFiled: November 7, 2012Publication date: May 16, 2013Applicant: AllTranz Inc.Inventor: AllTranz Inc.
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Publication number: 20130102784Abstract: 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: ApplicationFiled: December 11, 2012Publication date: April 25, 2013Applicant: Rhodes TechnologiesInventor: Rhodes Technologies
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Patent number: 8318937Abstract: 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: GrantFiled: February 18, 2011Date of Patent: November 27, 2012Assignee: Johnson Matthey Public Limited CompanyInventors: Melville Mitchell, Neil Kenneth Thomson, George Scott Wilson, Neil John Goodwin, Maureen Joan Young
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Patent number: 8309568Abstract: 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: GrantFiled: February 19, 2009Date of Patent: November 13, 2012Assignee: Alltranz Inc.Inventors: Audra Lynn Stinchcomb, Miroslaw Jerzy Golinski, Dana Carmel Hammell, Jeffrey Lynn Howard
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Publication number: 20120283443Abstract: 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: ApplicationFiled: May 2, 2012Publication date: November 8, 2012Applicant: Brock UniversityInventors: Tomas Hudlicky, Lukas Werner, Ales Machara, Martina Wernerova, Mary Ann Endoma-Arias
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Patent number: 8293906Abstract: 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: GrantFiled: September 29, 2009Date of Patent: October 23, 2012Assignee: Mallinckrodt LLCInventors: Esa T. Jarvi, James R. Meyer