One Of The Five Cyclos Is Five-membered And Includes Ring Chalcogen (e.g., Codeine, Morphine, Etc.) Patents (Class 546/44)
  • Patent number: 10799496
    Abstract: The present invention provides compounds useful for the treatment of opioid dependence, alcohol dependence, alcohol use disorder, or the prevention of relapse to opioid dependence in a subject in need thereof. Related pharmaceutical compositions and methods are also provided herein.
    Type: Grant
    Filed: July 11, 2019
    Date of Patent: October 13, 2020
    Assignee: Alkermes Pharma Ireland Limited
    Inventors: Brian M. Aquila, Hoan Huynh, Lewis D. Pennington, Ingo Mugge, Baudouin Gerard, Markus Haeberlein, Roman A. Valiulin, Julius F. Remenar, Demetri T. Moustakas, Thomas Andrew Wynn, Todd Bosanac
  • Patent number: 10512644
    Abstract: The invention provides compounds that are chemically modified by covalent attachment of a water-soluble oligomer. A compound of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different from those of the compound not attached to the water-soluble oligomer.
    Type: Grant
    Filed: October 19, 2018
    Date of Patent: December 24, 2019
    Assignee: Inheris Pharmaceuticals, Inc.
    Inventors: Jennifer Riggs-Sauthier, Bo-Liang Deng, Timothy A. Riley
  • Patent number: 10441661
    Abstract: The presently described technology provides compositions comprising aryl carboxylic acids chemically conjugated to hydromorphone (4,5-?-epoxy-3-hydroxy-17-methyl morphinan-6-one) to form novel prodrugs/compositions of hydromorphone. The hydromorphone prodrugs of the present technology have decreased side effects and decreased potential for abuse compared to unconjugated hydromorphone. The present technology also provides methods of treating patients, pharmaceutical kits and methods of synthesizing conjugates of the present technology.
    Type: Grant
    Filed: March 1, 2019
    Date of Patent: October 15, 2019
    Assignee: KemPharm, Inc.
    Inventors: Travis Mickle, Sven Guenther, Guochen Chi, Jaroslaw Kanski, Andrea K Martin, Bindu Bera
  • Patent number: 10428079
    Abstract: Processes for preparing oxycodone are provided. Said processes encompass a step which is a hydrogenation of an 14-hydroxycodeinone salt in the presence of trifluoroacetic acid and/or a glycol.
    Type: Grant
    Filed: March 30, 2018
    Date of Patent: October 1, 2019
    Assignee: RHODES TECHNOLOGIES
    Inventors: Joshua Robert Giguere, Keith Edward McCarthy, Marcel Schleusner
  • Patent number: 10391091
    Abstract: The invention relates to an improved method of preparing buprenorphine, a salt thereof, analogs of buprenorphine and their salts. In particular, the invention relates to a method of preparing buprenorphine and related products and salts in economic and ecologic ways having increased yields.
    Type: Grant
    Filed: October 13, 2015
    Date of Patent: August 27, 2019
    Assignee: Siegfried AG
    Inventors: Beat Theodor Weber, Lionel Roux
  • Patent number: 10363251
    Abstract: The present invention provides (+)-morphinans comprising Toll-like receptor 9 (TLR9) antagonist activity, as well as methods for using the (+)-morphinans to treat a variety of disorders.
    Type: Grant
    Filed: July 31, 2015
    Date of Patent: July 30, 2019
    Assignee: Mallinckrodt LLC
    Inventors: Bobby N. Trawick, David W. Berberich, Christopher W. Grote
  • Patent number: 10328070
    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: Grant
    Filed: November 27, 2018
    Date of Patent: June 25, 2019
    Assignee: Alkermes Pharma Ireland Limited
    Inventors: Harry G. Brittain, David A. Dickason, Joyce M. Hotz, Shawn L. Lyons, J. Michael Ramstack, Steven G. Wright
  • Patent number: 10287296
    Abstract: An invention includes a process for the preparation of (S)-2((4R,4aS,6R,7R,7aR,12bS)-7,9-dimethoxy-1,2,3,4,5,6,7,7a-octahydro-4a,7-ethano-4,12-methanobenzofuro[3,2-e]isoquinolin-6-yl)-3,3-dimethylbutan-2-ol.
    Type: Grant
    Filed: October 12, 2016
    Date of Patent: May 14, 2019
    Assignee: Noramco, Inc.
    Inventor: Wen-Chun Zhang
  • Patent number: 10258696
    Abstract: The presently described technology provides compositions comprising aryl carboxylic acids chemically conjugated to hydromorphone (4,5-?-epoxy-3-hydroxy-17-methyl morphinan-6-one) to form novel prodrugs/compositions of hydromorphone. The hydromorphone prodrugs of the present technology have decreased side effects and decreased potential for abuse compared to unconjugated hydromorphone. The present technology also provides methods of treating patients, pharmaceutical kits and methods of synthesizing conjugates of the present technology.
    Type: Grant
    Filed: August 3, 2018
    Date of Patent: April 16, 2019
    Assignee: KemPharm, Inc.
    Inventors: Travis Mickle, Sven Guenther, Guochen Chi, Jaroslaw Kanski, Andrea K. Martin, Bindu Bera
  • Patent number: 10166228
    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: Grant
    Filed: April 24, 2018
    Date of Patent: January 1, 2019
    Assignee: Alkermes Pharma Ireland Limited
    Inventors: Harry G. Brittain, David A. Dickason, Joyce M. Hotz, Shawn L. Lyons, J. Michael Ramstack, Steven G. Wright
  • Patent number: 10143690
    Abstract: The invention provides compounds that are chemically modified by covalent attachment of a water-soluble oligomer. A compound of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different from those of the compound not attached to the water-soluble oligomer.
    Type: Grant
    Filed: October 24, 2017
    Date of Patent: December 4, 2018
    Assignee: Nektar Therapeutics
    Inventors: Jennifer Riggs-Sauthier, Bo-Liang Deng, Timothy A. Riley
  • Patent number: 9980958
    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: Grant
    Filed: October 26, 2017
    Date of Patent: May 29, 2018
    Assignee: Alkermes Pharma Ireland Limited
    Inventors: Harry G. Brittain, David A. Dickason, Joyce M. Hotz, Shawn L. Lyons, J. Michael Ramstack, Steven G. Wright
  • Patent number: 9938286
    Abstract: The present invention relates to new nalmefene salts which salts fall within at least one of the two following categories: non-hydrate forming salts and non-solvate forming salts. In particular, the invention relates to the hydrogen adipate salt, the hydrogen malonate salt, the lactate salt, the hydrogen fumarate salt, the hydrogen succinate salt, the benzene sulfonate salt, the hydrogen maleate salt and the salicylate salt of nalmefene. The present invention also relates to such salts for use in therapy.
    Type: Grant
    Filed: June 12, 2017
    Date of Patent: April 10, 2018
    Assignee: H. LUNDBECK A/S
    Inventor: Heidi Lopez De Diego
  • Patent number: 9827240
    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: Grant
    Filed: December 16, 2016
    Date of Patent: November 28, 2017
    Assignee: Alkermes Pharma Ireland Limited
    Inventors: Harry G. Brittain, David A. Dickason, Joyce M. Hotz, Shawn L. Lyons, J. Michael Ramstack, Steven G. Wright
  • Patent number: 9725458
    Abstract: The present invention relates to new nalmefene salts which salts fall within at least one of the two following categories: non-hydrate forming salts and non-solvate forming salts. In particular, the invention relates to the hydrogen adipate salt, the hydrogen malonate salt, the lactate salt, the hydrogen fumarate salt, the hydrogen succinate salt, the benzene sulfonate salt, the hydrogen maleate salt and the salicylate salt of nalmefene. The present invention also relates to such salts for use in therapy.
    Type: Grant
    Filed: July 10, 2014
    Date of Patent: August 8, 2017
    Assignee: H. Lundbeck A/S
    Inventor: Heidi Lopez De Diego
  • Patent number: 9682076
    Abstract: The presently described technology provides compositions comprising aryl carboxylic acids and, for example NSAIDs, chemically conjugated to oxymorphone (4,5-?-epoxy-3,14-dihydroxy-17-methylmorphinan-6-one) to form novel prodrugs/compositions of oxymorphone, including benzoates, salicylates, propionates, fenamates, and acetates, which have a decreased potential for abuse of oxymorphone. The present technology also provides methods of treating patients, pharmaceutical kits and methods of synthesizing conjugates of the present technology.
    Type: Grant
    Filed: December 2, 2015
    Date of Patent: June 20, 2017
    Assignee: KEMPHARM, INC.
    Inventors: Travis Mickle, Sven Guenther, Sanjib Bera, Jaroslaw Kanski, Andrea Martin
  • Patent number: 9657029
    Abstract: The invention relates to an improved method of preparing oxymorphone or a salt thereof from oripavine. In particular, the invention relates to a method of preparing oxymorphone with a content of alpha-beta-unsaturated ketones (ABUK)<10 ppm, wherein the content of 8,14-dihydroxydihydromorphinone in the prepared oxymorphone is >10 ppm.
    Type: Grant
    Filed: June 11, 2013
    Date of Patent: May 23, 2017
    Assignee: Siegfried Generics International AG
    Inventor: Jianguang Sun
  • Patent number: 9556189
    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: Grant
    Filed: June 7, 2016
    Date of Patent: January 31, 2017
    Assignee: Alkermes Pharma Ireland Limited
    Inventors: Harry G. Brittain, David A. Dickason, Joyce M. Hotz, Shawn L. Lyons, J. Michael Ramstack, Steven G. Wright
  • Patent number: 9546177
    Abstract: The present invention is directed to an improved process to convert morphine into noroxymorphone having economic and ecological advantages.
    Type: Grant
    Filed: July 22, 2014
    Date of Patent: January 17, 2017
    Assignee: SIEGRIED AG
    Inventors: Beat Theodor Weber, Lisa Hochstrasser
  • Patent number: 9512135
    Abstract: The invention provides compounds that are chemically modified by covalent attachment of a water-soluble oligomer. A compound of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different from those of the compound not attached to the water-soluble oligomer.
    Type: Grant
    Filed: December 4, 2015
    Date of Patent: December 6, 2016
    Assignee: Nektar Therapeutics
    Inventors: Jennifer Riggs-Sauthier, Bo-Liang Deng, Timothy A. Riley
  • Patent number: 9428516
    Abstract: The present disclosure is directed to crystalline forms of morphine sulfate and pharmaceutical compositions comprising any of the crystalline forms of morphine sulfate. Also provided are processes for the preparation of crystalline forms of morphine sulfate.
    Type: Grant
    Filed: September 29, 2015
    Date of Patent: August 30, 2016
    Assignee: Johnson Matthey Public Limited Company
    Inventors: Nicholas D. Paschalides, Mahmoud Mirmehrabi
  • Patent number: 9415044
    Abstract: An improved process for the N-alkylation of tertiary morphinan alkaloid bases to form the corresponding quaternary morphinan alkaloid derivatives.
    Type: Grant
    Filed: December 12, 2014
    Date of Patent: August 16, 2016
    Assignee: Mallinckrodt LLC
    Inventors: Peter X. Wang, Robert E. Halvachs, Kevin R. Roesch, Henry J. Buehler, Joseph P. Haar, Jr., Gary L. Cantrell
  • Patent number: 9365580
    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: Grant
    Filed: November 19, 2015
    Date of Patent: June 14, 2016
    Assignee: Alkermes Pharma Ireland Limited
    Inventors: Harry G. Brittain, David A. Dickason, Joyce M. Hotz, Shawn L. Lyons, J. Michael Ramstack, Steven G. Wright
  • Patent number: 9315514
    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: Grant
    Filed: August 26, 2013
    Date of Patent: April 19, 2016
    Assignee: Rhodes Technologies
    Inventor: Helge A. Reisch
  • Patent number: 9233168
    Abstract: The invention provides compounds that are chemically modified by covalent attachment of a water-soluble oligomer. A compound of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different from those of the compound not attached to the water-soluble oligomer.
    Type: Grant
    Filed: December 23, 2014
    Date of Patent: January 12, 2016
    Assignee: Nektar Therapeutics
    Inventors: Jennifer Riggs-Sauthier, Bo-Liang Deng, Timothy A. Riley
  • Patent number: 9149539
    Abstract: Naloxol-polyethylene glycol conjugates of the formula: are provided in oxalate or phosphate salt forms including crystalline forms. Methods of preparing the salt forms and pharmaceutical compositions comprising the salt forms are also provided.
    Type: Grant
    Filed: March 11, 2015
    Date of Patent: October 6, 2015
    Assignees: ASTRAZENECA AB, NEKTAR THERAPEUTICS
    Inventors: Bengt Aslund, Carl-Johan Aurell, Martin Hans Bohlin, Tesfai Sebhatu, Bo Ingvar Ymen, Eric Thomas Healy, David Richard Jensen, David Thomas Jonaitis, Stephan Parent
  • Patent number: 9108974
    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: Grant
    Filed: October 16, 2007
    Date of Patent: August 18, 2015
    Assignee: PENICK CORPORATION
    Inventor: Bao-Shan Huang
  • Patent number: 9040552
    Abstract: The present invention relates to compounds of Formula I or II, or pharmaceutically acceptable salts, esters, or prodrugs thereof: which relates to mophinan compounds useful as ?, ? and/or ? receptor opioid compounds and pharmaceuticals containing same that may be useful for mediating analgesia, combating drug addiction, alcohol addiction, drug overdose, mental illness, bladder dysfunctions, neurogenic bladder, interstitial cystitis, urinary incontinence, premature ejaculation, inflammatory pain, peripherally mediated and neuropathic pain, cough, lung edema, diarrhea, cardiac disorders, cardioprotection, depression, and cognitive, respiratory, diarrhea, irritable bowel syndrome and gastro-intestinal disorders, immunomodulation, and anti-tumor agents.
    Type: Grant
    Filed: December 4, 2012
    Date of Patent: May 26, 2015
    Assignee: Alkermes, Inc.
    Inventors: Derrick Arnelle, Daniel Deaver, Reginald L. Dean, III, Mark Todtenkopf
  • Publication number: 20150141649
    Abstract: The present invention provides processes for preparing normorphinans from N-substituted morphinans. In particular, the invention provides methods for removing the N-substituent from the N-substituted morphinan to from a normorphinan carbamate, and then removing the carbamate functionality from the normorphinan carbamate to form the normorphinan.
    Type: Application
    Filed: November 18, 2014
    Publication date: May 21, 2015
    Inventors: John Brandt, Subo Liao, Edmund C. Hudson, Esa T. Jarvi, Peter X. Wang, Michael Schaefer
  • 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: 20150126741
    Abstract: Described herein are methods of preparing 6-hydroxy N-alkyl morphinan-6-ols from morphinan-6-ones, as illustrated below: wherein the variables R1, R2, R3, R10, R11, R14, and are as defined herein and wherein the reactions occur in a one-pot procedure using a boron based reducing agent.
    Type: Application
    Filed: October 31, 2014
    Publication date: May 7, 2015
    Inventors: Peter X. Wang, Tao Jiang
  • Publication number: 20150112069
    Abstract: The invention provides compounds that are chemically modified by covalent attachment of a water-soluble oligomer. A compound of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different from those of the compound not attached to the water-soluble oligomer.
    Type: Application
    Filed: December 23, 2014
    Publication date: April 23, 2015
    Inventors: Jennifer Riggs-Sauthier, Bo-Liang Deng, Timothy A. Riley
  • Patent number: 9012468
    Abstract: The present invention provides processes for preparing nal-opiates without the isolation of intermediates. In general, the process provides for alkylation and reduction in the same pot to give the nal-opiate.
    Type: Grant
    Filed: February 8, 2013
    Date of Patent: April 21, 2015
    Assignee: Mallinckrodt LLC
    Inventors: Peter X. Wang, Tao Jiang
  • Patent number: 9012469
    Abstract: Naloxol-polyethlyene glycol conjugates of the formula: are provided in oxalate or phosphate salt forms including crystalline forms. Methods of preparing the salt forms and pharmaceutical compositions comprising the salt forms are also provided.
    Type: Grant
    Filed: September 29, 2011
    Date of Patent: April 21, 2015
    Assignees: AstraZeneca AB, Nektar Therapeutics
    Inventors: Bengt Leonard Åslund, Carl-Johan Aurell, Martin Hans Bohlin, Eric Thomas Healy, David Richard Jensen, David Thomas Jonaitis, Stephan Parent, Tesfai Sebhatu, Bo Ingvar Ymén
  • Publication number: 20150094471
    Abstract: The present application is directed to an efficient conversion of C-14 hydroxylated morphine alkaloids to various morphine analogs, such as naltrexone, naloxone and nalbuphone. One feature of this process is an intramolecular functional group transfer from the C-14 hydroxyl to the N-17 nitrogen atom following a palladium-catalyzed N-demethylation.
    Type: Application
    Filed: December 16, 2014
    Publication date: April 2, 2015
    Inventors: Tomas Hudlicky, Ales Machara
  • Patent number: 8993764
    Abstract: There is provided a method for the synthesis of norbuprenorphine, and ultimately buprenorphine, utilizing oripavine as the starting material. Conventional methods of producing buprenorphine utilize thebaine as the starting material, requiring an O-demethylation step, typically a low to moderate yield transformation. The present use of oripavine as a starting material does not require an O-demethylation step, since the oripavine molecule lacks an O-3 methyl group.
    Type: Grant
    Filed: December 18, 2006
    Date of Patent: March 31, 2015
    Assignee: Mallinckrodt LLC
    Inventors: Anthony Mannino, Erik R. Hoefgin, Lloyd P. Hill, Henry J. Buehler
  • 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: 8980908
    Abstract: Selective, non-peptide antagonists of the mu opioid receptor (MOR) and methods of their use are provided. The antagonists may be used, for example, to identify MOR agonists in competitive binding assays, and to treat conditions related to addiction in which MOR is involved, e.g. heroin, prescription drug and alcohol addiction, as well as in the treatment of opioid induced constipation (OIC).
    Type: Grant
    Filed: May 27, 2014
    Date of Patent: March 17, 2015
    Assignee: Virginia Commonwealth University
    Inventors: Yan Zhang, Dana E. Selley, William Dewey
  • 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: 8962647
    Abstract: Provided are a PEG-naloxone conjugate of general formula (II) and a pharmaceutical composition comprising the conjugate. In the conjugate, n is an integer in the range of 1-20. Also provided is a three-branched or four-branched conjugate of PEG and naloxone. Structural modification of naloxone with a hydrophilic polymer improves the pharmacokinetic properties of the drug, increase the water solubility of naloxone, improve the in vivo distribution of the drug, reduce the side effects of naloxone on central nervous system, and relieve bowel dysfunction and constipation caused by chronic administration of opioids. Also provided are a pharmaceutical composition comprising the conjugate of the invention and use of the conjugate.
    Type: Grant
    Filed: February 21, 2013
    Date of Patent: February 24, 2015
    Assignee: Jenkem Technology Co., Ltd. (Tianjin)
    Inventors: Zhixiong Guo, Zewang Feng, Lihua Xu, Xuan Zhao
  • Patent number: 8962646
    Abstract: The invention relates to a compound of Formula I, II, III, IV or a pharmaceutically acceptable ester or prodrug thereof:
    Type: Grant
    Filed: June 29, 2012
    Date of Patent: February 24, 2015
    Assignee: Alkermes, Inc.
    Inventors: Laura Cook Blumberg, Derrick Arnelle
  • Publication number: 20150050339
    Abstract: The presently described technology provides phenylethanoic acid, phenylpropanoic acid, phenylpropenoic acid, a salt thereof, a derivative thereof or a combination thereof chemically conjugated to hydrocodone (morphinan-6-one, 4,5-alpha-epoxy-3-methoxy-17-methyl) to form novel prodrugs or compositions of hydrocodone which have a decreased potential for abuse of hydrocodone. The present technology also provides methods of treating patients, pharmaceutical kits and methods of synthesizing conjugates of the present technology.
    Type: Application
    Filed: September 23, 2014
    Publication date: February 19, 2015
    Inventors: Travis Mickle, Sven Guenther, Christal Mickle
  • Publication number: 20150045555
    Abstract: Provided are a PEG-naloxone conjugate of general formula (II) and a pharmaceutical composition comprising the conjugate. In the conjugate, n is an integer in the range of 1-20. Also provided is a three-branched or four-branched conjugate of PEG and naloxone. Structural modification of naloxone with a hydrophilic polymer improves the pharmacokinetic properties of the drug, increase the water solubility of naloxone, improve the in vivo distribution of the drug, reduce the side effects of naloxone on central nervous system, and relieve bowel dysfunction and constipation caused by chronic administration of opioids. Also provided are a pharmaceutical composition comprising the conjugate of the invention and use of the conjugate.
    Type: Application
    Filed: February 21, 2013
    Publication date: February 12, 2015
    Inventors: Zhixiong Guo, Zewang Feng, Lihua Xu, Xuan Zhao
  • Patent number: 8952032
    Abstract: The invention provides compounds that are chemically modified by covalent attachment of a water-soluble oligomer. A compound of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different from those of the compound not attached to the water-soluble oligomer.
    Type: Grant
    Filed: September 20, 2013
    Date of Patent: February 10, 2015
    Assignee: Nektar Therapeutics
    Inventors: Jennifer Riggs-Sauthier, Bo-Liang Deng, Timothy A. Riley
  • Publication number: 20150038524
    Abstract: Naloxol-polyethylene glycol conjugates of the formula: are provided in oxalate or phosphate salt forms including crystalline forms. Methods of preparing the salt forms and pharmaceutical compositions comprising the salt forms are also provided.
    Type: Application
    Filed: September 29, 2011
    Publication date: February 5, 2015
    Applicant: ASTRAZENECA INTELLECTUAL PROPERTY
    Inventors: Bengt Leonard Aslund, Carl-Johan Aurell, Martin Hans Bohlin, David Richard Jensen, David Thomas Jonaitis, Eric Thomas Healy, Bo Ingvar Ymén, Stephan Parent, Tesfai Sebhatu
  • Patent number: 8946254
    Abstract: Bivalent ligands that contain two pharmacophores linked through a spacer, one of which interacts with the ?-opioid receptor (MOR) and the other of which interacts with the co-receptor CC chemokine receptor 5 (CCR5), are used for the treatment of neurological disorders such as those associated with AIDS.
    Type: Grant
    Filed: January 10, 2013
    Date of Patent: February 3, 2015
    Assignee: Virginia Commonwealth University
    Inventors: Yan Zhang, Kurt F. Hauser, Dana E. Selley
  • Patent number: 8946419
    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: Grant
    Filed: October 3, 2013
    Date of Patent: February 3, 2015
    Assignee: Mallinckrodt LLC
    Inventors: Christopher W. Grote, Amruta R. Poreddy
  • Patent number: 8921386
    Abstract: A drug substance with a pharmaceutically acceptable organic acid addition salt of an opioid wherein said organic acid is selected from Structure A: wherein R1-R4 are independently selected from H, alkyl or substituted alkyl of 1-6 carbons, adjacent groups may be taken together to form a cyclic alkyl, cyclic alkyl-aryl, or cyclic aryl moiety; R5 is selected from H, or an alkali earth cation; R6 and R7 are independently selected from H, alkyl of 1-6 carbons, an alkali earth cation, and aryl of 6 to 12 carbons, in a number sufficient to complete the valence bonding of X, and wherein X is selected from nitrogen, oxygen or sulfur; and wherein the drug substance has a morphology selected from amorphous and crystalline.
    Type: Grant
    Filed: May 31, 2012
    Date of Patent: December 30, 2014
    Assignee: Pisgah Laboratories, Inc.
    Inventors: Clifford Riley King, Stephen G. D'Ambrosio, David W. Bristol, Michael L. English
  • Patent number: 8916707
    Abstract: The present invention provides a process for preparing an oxycodone acid adduct, said process comprising hydrogenating an aqueous solution of 14-hydroxycodeinone and an acid to form a solution of the oxycodone acid adduct, wherein the hydrogenation is carried out at one or more temperatures greater than ambient temperature in the presence of a hydrogenation catalyst and hydrogen gas, wherein the solution of oxycodone acid adduct comprises 6?-oxycodol in an amount ?about 0.800 area % as determined by HPLC.
    Type: Grant
    Filed: August 2, 2013
    Date of Patent: December 23, 2014
    Assignee: Johnson Matthey Public Limited Company
    Inventors: Nicolas Archer, Maureen Young, Timothy Davies, Amy Price, Michael Bease, Barbara Jamieson, Ewart Grant, Brian Heinrich, Saroop Matharu