Two Of The Cyclos Share At Least Three Ring Members (e.g., Morphinans, Etc.) Patents (Class 546/74)
  • Patent number: 10464904
    Abstract: The invention relates to dextrorphan-derivatives, pharmaceutical compositions and pharmaceutical dosage forms containing such dextrorphan-derivatives as well as the use of those dextrorphan-derivatives and/or compositions for treating and preventing diseases and conditions in man and mammals.
    Type: Grant
    Filed: December 2, 2016
    Date of Patent: November 5, 2019
    Assignee: Heinrich-Heine-Universitat Dusseldorf
    Inventors: Eckhard Lammert, Alena Welters, Silke Otter, Jan Marquard, Thomas Meissner, Diran Herebian, Ertan Mayatepek
  • Patent number: 10287250
    Abstract: The present application relates to analogs of morphan and morphinan, compositions thereof, and methods for treating a disease or condition comprising administering an effective amount of the compounds or compositions to a subject in need thereof.
    Type: Grant
    Filed: May 15, 2017
    Date of Patent: May 14, 2019
    Assignee: ALKERMES PHARMA IRELAND LIMITED
    Inventors: Laura Cook Blumberg, Daniel R. Deaver, David J. Eyerman, Thomas Andrew Wynn
  • Patent number: 10081602
    Abstract: Provided are compounds, including those of Formula I; and pharmaceutically acceptable salts and solvates thereof. The compounds described herein relate to and/or have application(s) in (among others) the fields of drug discovery, pharmacotherapy, physiology, organic chemistry and polymer chemistry.
    Type: Grant
    Filed: May 24, 2017
    Date of Patent: September 25, 2018
    Assignee: Nektar Therapeutics
    Inventors: Franco J. Duarte, Neel K. Anand, Pankaj Sharma, Devendrapratap Singh
  • Patent number: 9868976
    Abstract: This disclosure relates to novel morphinan compounds and their derivatives, pharmaceutically acceptable salts, solvates, and hydrates thereof. This disclosure also provides compositions comprising a compound of this disclosure and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a ?1 receptor agonist that also has NMDA antagonist activity.
    Type: Grant
    Filed: March 11, 2016
    Date of Patent: January 16, 2018
    Assignee: Concert Pharmaceuticals, Inc.
    Inventor: Roger D. Tung
  • Patent number: 9688638
    Abstract: Provided are compounds, including those of Formula I; and pharmaceutically acceptable salts and solvates thereof. The compounds described herein relate to and/or have application(s) in (among others) the fields of drug discovery, pharmacotherapy, physiology, organic chemistry and polymer chemistry.
    Type: Grant
    Filed: November 27, 2014
    Date of Patent: June 27, 2017
    Assignee: Nektar Therapeutics
    Inventors: Franco J. Duarte, Neel K. Anand, Pankaj Sharma, Devendrapratap Singh
  • Patent number: 9656962
    Abstract: The application is directed to compounds of Formula (I) or (IA) and pharmaceutically acceptable salts and solvates thereof, wherein R1 R2, R3 and G are defined as set forth in the specification. The invention is also directed to use of compounds of Formula (I) or (IA), 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 19, 2014
    Date of Patent: May 23, 2017
    Assignee: Purdue Pharma L.P.
    Inventors: Jeffrey Lockman, Laykea Tafesse
  • Patent number: 9562014
    Abstract: The present invention provides (+)-morphinans comprising Toll-like receptor 9 (TLR9) antagonist activity, as well as methods for using the (+)-morphinans to treat pain. Also provided are pharmaceutical combination compositions comprising a (+)-morphinan and an opioid agonist/monoamine reuptake inhibitor, as well as methods for using the combination compositions to treat pain.
    Type: Grant
    Filed: December 22, 2010
    Date of Patent: February 7, 2017
    Assignee: Mallinckrodt LLC
    Inventors: Bobby N. Trawick, David W. Berberich, Christopher W. Grote
  • 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
  • Patent number: 9029543
    Abstract: The invention relates to a process for the synthesis of quaternized compounds of formula:
    Type: Grant
    Filed: April 5, 2012
    Date of Patent: May 12, 2015
    Assignee: Alkermes, Inc.
    Inventor: Scott Duncan
  • Publication number: 20150119416
    Abstract: A compound of formula I is disclosed. Compounds of formula I are useful as analgesics, anti-inflammatory agents, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction medications.
    Type: Application
    Filed: January 5, 2015
    Publication date: April 30, 2015
    Applicant: RENSSELAER POLYTECHNIC INSTITUTE
    Inventor: Mark P. WENTLAND
  • Publication number: 20150099776
    Abstract: The compounds of formula (I), or its pharmaceutically acceptable salts, or any stereoisomer or mixture thereof, wherein: R1 is a (C1-C2) alkyl radical; R2 and R3 are radicals independently selected from the group consisting of F, Cl and methyl R4 is H or OH; A is a birradical selected from the group consisting of —(CH2)n— and —(CH2)-phenyl-(CH2)—; t is an integer from 0 to 1; and n is an integer from 8 to 15, are useful for the treatment of Alzheimer's disease.
    Type: Application
    Filed: May 9, 2013
    Publication date: April 9, 2015
    Applicants: PONTIFICIA UNIVERSIDAD CATÓLICA DE CHILE, UNIVERSITAT DE BARCELONA
    Inventors: Diego Muñoz-Torrero López-Ibarra, Nibaldo Manuel Inestrosa Cantín, Elisabet Viayna Gaza, Irene Sola Lao, Santiago Vázquez Cruz
  • Publication number: 20150087670
    Abstract: The invention relates to the compounds of formula I or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, and methods for the treatment of respiratory disorders may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of cough caused by minor throat and bronchial irritation (such as commonly accompanies the flu and common cold), as well as those resulting from inhaled particle irritants, upper respiratory infections, (pseudobulbar affect) in patients with amyotrophic lateral sclerosis and multiple sclerosis, neuropathic pain and pain associated with fibromyalgia.
    Type: Application
    Filed: February 24, 2013
    Publication date: March 26, 2015
    Inventor: Mahesh Kandula
  • Patent number: 8987293
    Abstract: Compounds of Formula (I) are disclosed. The variables R1-R11 are described herein. Certain compounds of Formula (I) are partial agonists of the mu, delta, and kappa opioid receptors, and are useful for treating pain and opioid addiction, with fewer side effects than conventional opioids. Methods for preparing the disclosed compounds, pharmaceutical compositions containing compounds of Formula (I), and methods of treating pain and opioid addiction in patients are also disclosed.
    Type: Grant
    Filed: December 23, 2011
    Date of Patent: March 24, 2015
    Assignee: Phoenix Pharmalabs, Inc.
    Inventor: John Lawson
  • Patent number: 8969562
    Abstract: A compound, (4s)-1-azaadamantane-4yl formate ester, is described. In addition, a process is described for preparing (4s)-1-azaadamantane-4yl formate ester, aminothiadiazole-phenyl phosphate salt, bromothiadizole-phenyl or (4s)-4-(5-phenyl-1,3,4-thiadiazol-2-yloxy)-1-azatricyclo[3.3.1.13,7]-decane dihydrogen citrate. Furthermore, a process is described, comprising step of hydrolyzing (4s)-1-azaadamantane-4yl formate ester to form (4s)-1-azaadamantan-4-ol HBr salt.
    Type: Grant
    Filed: March 11, 2014
    Date of Patent: March 3, 2015
    Assignee: AbbVie, Inc.
    Inventors: Albert Wayne Kruger, Shuang Chen, Steven Cramer Cullen, James Joseph Napier
  • 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
  • Patent number: 8957085
    Abstract: A compound of formula I is disclosed. Compounds of formula I are useful as analgesics, anti-inflammatory agents, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction medications.
    Type: Grant
    Filed: March 12, 2014
    Date of Patent: February 17, 2015
    Assignee: Rensselaer Polytechnic Institute
    Inventor: Mark P. Wentland
  • Publication number: 20150045384
    Abstract: The present application relates to analogues of morphan and morphinan, compositions thereof, and methods for treating a disease or condition comprising administering an effective amount of the compounds or compositions to a subject in need thereof.
    Type: Application
    Filed: May 23, 2014
    Publication date: February 12, 2015
    Applicant: ALKERMES PHARMA IRELAND LIMITED
    Inventors: Laura Cook Blumberg, Dan Deaver, David Eyerman
  • Patent number: 8946255
    Abstract: The application is directed to compounds of Formula I: and pharmaceutically acceptable salts and solvates thereof, wherein R1, R2, R3, R4a, and R4b are defined as set forth in the specification. The invention is also directed to use of compounds of Formula I 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, 2013
    Date of Patent: February 3, 2015
    Assignee: Purdue Pharma L.P.
    Inventors: Andrew Kassick, Jeffrey Lockman, Laykea Tafesse
  • Publication number: 20150025067
    Abstract: Inhibitors of p67phox protein are provided herein, as well as pharmaceutical compositions and methods relating thereto.
    Type: Application
    Filed: February 13, 2013
    Publication date: January 22, 2015
    Applicant: CHILDREN'S HOSPITAL MEDICAL CENTER
    Inventors: Yi Zheng, Prakash Jagtap, Emily E. Bosco, Jaroslaw Meller, Marie-Dominique Filippi
  • Publication number: 20150011768
    Abstract: 4-Hydroxybenzomorphans containing carboxamide or thiocarboxamide at the 3-position are useful as analgesics, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction medications.
    Type: Application
    Filed: July 2, 2014
    Publication date: January 8, 2015
    Applicant: Rensselaer Polytechnic Institute
    Inventor: Mark P. WENTLAND
  • Patent number: 8916582
    Abstract: This invention relates to novel morphinan compounds and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a ?1 receptor agonist that also has NMDA antagonist activity.
    Type: Grant
    Filed: March 13, 2014
    Date of Patent: December 23, 2014
    Assignee: Concert Pharmaceuticals, Inc.
    Inventors: Philip B. Graham, I. Robert Silverman
  • 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
  • Publication number: 20140315940
    Abstract: This invention relates to novel morphinan compounds and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a ?1 receptor agonist that also has NMDA antagonist activity.
    Type: Application
    Filed: March 13, 2014
    Publication date: October 23, 2014
    Applicant: Concert Pharmaceuticals, Inc.
    Inventors: Philip B. Graham, I. Robert Silverman
  • Publication number: 20140275545
    Abstract: 8-Substituted-2,6-methano-3-benzazocines of general structure I in which A is —CH2—OH, —CH2NH2, —NHSO2CH3, and Y is O, S or NOH are useful as analgesics, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction medications. 8-Carboxamides, thiocarboxamides, hydroxyamidines and formamides are preferred.
    Type: Application
    Filed: December 19, 2013
    Publication date: September 18, 2014
    Applicant: Rensselaer Polytechnic Institute
    Inventor: Mark P. WENTLAND
  • Publication number: 20140275546
    Abstract: A compound, (4s)-1-azaadamantane-4yl formate ester, is described. In addition, a process is described for preparing (4s)-1-azaadamantane-4yl formate ester, aminothiadiazole-phenyl phosphate salt, bromothiadizole-phenyl or (4s)-4-(5-phenyl-1,3,4-thiadiazol-2-yloxy)-1-azatricyclo[3.3.1.13,7]-decane dihydrogen citrate. Furthermore, a process is described, comprising step of hydrolyzing (4s)-1-azaadamantane-4yl formate ester to form (4s)-1-azaadamantan-4-ol HBr salt.
    Type: Application
    Filed: March 11, 2014
    Publication date: September 18, 2014
    Applicant: AbbVie Inc.
    Inventors: Albert Wayne KRUGER, Shuang CHEN, Steven Cramer CULLEN, James Joseph NAPIER
  • Patent number: 8802655
    Abstract: 4-Hydroxybenzomorphans containing carboxamide or thiocarboxamide at the 3-position are useful as analgesics, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction medications. A compound of formula is disclosed, as are pharmaceutically acceptable acid addition salts, such as acetic, benzenesulfonic (besylate), benzoic, camphorsulfonic, citric, ethenesulfonic, fumaric, gluconic, glutamic, hydrobromic, hydrochloric, isethionic, lactic, maleic, malic, mandelic, methanesulfonic, mucic, nitric, pamoic, pantothenic, phosphoric, succinic, sulfuric, tartaric acid or p-toluenesulfonic acid salts. These compounds are useful for the treatment of pain.
    Type: Grant
    Filed: January 31, 2014
    Date of Patent: August 12, 2014
    Assignee: Rensselaer Polytechnic Institute
    Inventor: Mark P. Wentland
  • Publication number: 20140194457
    Abstract: A compound of formula I is disclosed. Compounds of formula I are useful as analgesics, anti-inflammatory agents, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction medications.
    Type: Application
    Filed: March 12, 2014
    Publication date: July 10, 2014
    Applicant: Rensselaer Polytechnic Institute
    Inventor: Mark P. WENTLAND
  • Patent number: 8772310
    Abstract: The present invention provides a compound of formula I: wherein X?, R1, and R2 are as defined herein, and compositions thereof; useful as a peripheral mu opioid receptor antagonist.
    Type: Grant
    Filed: November 9, 2012
    Date of Patent: July 8, 2014
    Assignee: Wyeth LLC
    Inventors: Charles K. Melucci, John Lokhnauth
  • Publication number: 20140187573
    Abstract: The application is directed to compounds of Formula I: and pharmaceutically acceptable salts and solvates thereof, wherein R1, R2, R3, R4a, and R4b are defined as set forth in the specification. The invention is also directed to use of compounds of Formula I 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: Andrew KASSICK, Jeffrey LOCKMAN, Laykea TAFESSE
  • Patent number: 8748450
    Abstract: This disclosure relates to novel morphinan compounds and their derivatives, pharmaceutically acceptable salts, solvates, and hydrates thereof. This disclosure also provides compositions comprising a compound of this disclosure and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a ?1 receptor agonist that also has NMDA antagonist activity.
    Type: Grant
    Filed: July 24, 2013
    Date of Patent: June 10, 2014
    Assignee: Concert Pharmaceuticals, Inc.
    Inventor: Roger Tung
  • Publication number: 20140148475
    Abstract: 4-Hydroxybenzomorphans containing carboxamide or thiocarboxamide at the 3-position are useful as analgesics, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction medications. A compound of formula is disclosed, as are pharmaceutically acceptable acid addition salts, such as acetic, benzenesulfonic (besylate), benzoic, camphorsulfonic, citric, ethenesulfonic, fumaric, gluconic, glutamic, hydrobromic, hydrochloric, isethionic, lactic, maleic, malic, mandelic, methanesulfonic, mucic, nitric, pamoic, pantothenic, phosphoric, succinic, sulfuric, tartaric acid or p-toluenesulfonic acid salts. These compounds are useful for the treatment of pain.
    Type: Application
    Filed: January 31, 2014
    Publication date: May 29, 2014
    Applicant: Rensselaer Polytechnic Institute
    Inventor: Mark P. WENTLAND
  • Patent number: 8710072
    Abstract: This invention relates to novel morphinan compounds and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a ?1 receptor agonist that also has NMDA antagonist activity.
    Type: Grant
    Filed: September 18, 2009
    Date of Patent: April 29, 2014
    Assignee: Concert Pharmaceuticals, Inc.
    Inventors: Philip B. Graham, I. Robert Silverman
  • Patent number: 8703949
    Abstract: The present invention provides processes for the preparation of N-alkyl morphinans without the isolation of nor-morphinan intermediates. In particular, the invention provides tandem hydrolysis/alkylation reactions for the synthesis of N-alkyl morphinans.
    Type: Grant
    Filed: August 3, 2011
    Date of Patent: April 22, 2014
    Assignee: Mallinckrodt LLC
    Inventors: Subo Liao, Peter X. Wang, David W. Berberich, Douglas C. Miller
  • Publication number: 20140107143
    Abstract: Compounds of formulas: are disclosed. The compounds are useful for ameliorating the side effects of therapeutic opiates.
    Type: Application
    Filed: September 27, 2013
    Publication date: April 17, 2014
    Applicant: Rensselaer Polytechnic Institute
    Inventor: Mark P. WENTLAND
  • Publication number: 20130345251
    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: August 23, 2013
    Publication date: December 26, 2013
    Applicant: Rensselaer Polytechnic Institute
    Inventor: Mark P. WENTLAND
  • Publication number: 20130338182
    Abstract: Compounds of Formula (I) are disclosed. The variables R1-R11 are described herein. Certain compounds of Formula (I) are partial agonists of the mu, delta, and kappa opioid receptors, and are useful for treating pain and opioid addiction, with fewer side effects than conventional opioids. Methods for preparing the disclosed compounds, pharmaceutical compositions containing compounds of Formula (I), and methods of treating pain and opioid addiction in patients are also disclosed.
    Type: Application
    Filed: December 23, 2011
    Publication date: December 19, 2013
    Applicant: PHEONIX PHARMALABS, INC.
    Inventor: John Lawson
  • Publication number: 20130281483
    Abstract: The present invention provides a compound of formula I: wherein X?, R1, and R2 are as defined herein, and compositions thereof; useful as a peripheral mu opioid receptor antagonist.
    Type: Application
    Filed: November 9, 2012
    Publication date: October 24, 2013
    Applicant: Wyeth LLC
    Inventor: Wyeth LLC
  • Patent number: 8563572
    Abstract: Compounds of formulas: are disclosed. The compounds are useful for ameliorating the side effects of therapeutic opiates.
    Type: Grant
    Filed: August 9, 2012
    Date of Patent: October 22, 2013
    Assignee: Rensselaer Polytechnic Institute
    Inventor: Mark P. Wentland
  • Publication number: 20130274280
    Abstract: This invention provides an oral pharmaceutical composition comprising a physiologically tolerable gelled oil-in-water emulsion containing a drug of abuse.
    Type: Application
    Filed: April 11, 2011
    Publication date: October 17, 2013
    Applicant: AYANDA GROUP AS
    Inventors: Kurt Ingar Draget, Ingvild Johanne Haug, Steinar Johan Engelsen, Tore Seternes, Magnus N. Hattrem
  • Patent number: 8557837
    Abstract: The invention relates to sinomenine derivatives, methods for their synthesis and their applications. The sinomenine derivatives include oxidation derivatives, and C-10 substituted sinomenine derivatives. Based on the readily oxidizable phenol group on sinomenine structure, using oxidation, oxidative dearomatization, or conjugated addition aromatization, one can introduce C-10 substitutions to synthesize the sinomenine derivatives. The sinomenine derivatives of the invention have the following structures: Using in vitro TNF-? inhibition assay, the activities of the synthetic compounds are assessed. Results from these assays shown that most compounds have anti-inflammatory effects, and some compounds have better activities than that of sinomenine. These compounds may be used in treating immune diseases such as rheumatoid arthritis (RA).
    Type: Grant
    Filed: February 9, 2011
    Date of Patent: October 15, 2013
    Assignees: Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, Shanghai Institutes for Biological Sciences, Chinese Academy of Sciences
    Inventors: Zhujun Yao, Bing Sun, Yangtong Lou, Zhenyu Yang, Aizhong Chen, Zhao Ma
  • Patent number: 8557784
    Abstract: The present invention provides a pharmaceutically acceptable compound, a pharmaceutical composition comprising the above-mentioned pharmaceutically acceptable compound. The pharmaceutically acceptable compound provided by the present invention is a salt of a basic group-containing morphinan derivative and a carboxyl group-containing glycyrrhizinic acid and has the ability to be used to manufacture medicaments for treating and/or preventing cough, ameliorating pains, treating respiratory system diseases, treating cardiovascular diseases and treating liver diseases.
    Type: Grant
    Filed: July 7, 2011
    Date of Patent: October 15, 2013
    Assignee: Standard Chem. & Pharm. Co., Ltd.
    Inventors: Chin-Tsai Fan, Cheng-Shun Lai, Wen-Yen Yeh, Yu-Ying Liu
  • Patent number: 8541436
    Abstract: This disclosure relates to novel morphinan compounds and their derivatives, pharmaceutically acceptable salts, solvates, and hydrates thereof. This disclosure also provides compositions comprising a compound of this disclosure and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a ?1 receptor agonist that also has NMDA antagonist activity.
    Type: Grant
    Filed: May 31, 2011
    Date of Patent: September 24, 2013
    Assignee: Concert Pharmaceuticals Inc.
    Inventor: Roger Tung
  • Publication number: 20130231361
    Abstract: 4-Hydroxybenzomorphans containing carboxamide or thiocarboxamide at the 3-position are useful as analgesics, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction medications. A compound of formula is disclosed, as are pharmaceutically acceptable acid addition salts, such as acetic, benzenesulfonic (besylate), benzoic, camphorsulfonic, citric, ethenesulfonic, fumaric, gluconic, glutamic, hydrobromic, hydrochloric, isethionic, lactic, maleic, malic, mandelic, methanesulfonic, mucic, nitric, pamoic, pantothenic, phosphoric, succinic, sulfuric, tartaric acid or p-toluenesulfonic acid salts. These compounds are useful for the treatment of pain.
    Type: Application
    Filed: April 15, 2013
    Publication date: September 5, 2013
    Applicant: Rensselaer Polytechnic Institue
    Inventor: Mark P. WENTLAND
  • Patent number: 8519133
    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: Grant
    Filed: June 10, 2010
    Date of Patent: August 27, 2013
    Assignee: Mallinckrodt LLC
    Inventors: Christopher W. Grote, Gary L. Cantrell, Joseph P. McClurg, Catherine E. Thomasson, Frank W. Moser
  • Publication number: 20130210835
    Abstract: A composition of an antitussive, a decongestant, or an antihistamine to treat respiratory and oral pharyngeal congestion and related symptoms in a patient.
    Type: Application
    Filed: June 13, 2011
    Publication date: August 15, 2013
    Applicant: GM PHARMACEUTICAL, INC
    Inventor: Odes W. Mitchell
  • Patent number: 8471023
    Abstract: The present invention provides processes for the stereoselective synthesis of 6-alpha-amino morphinans. In particular, the invention provides processes for the reductive amination of 6-keto normorphinans by catalytic transfer hydrogenation.
    Type: Grant
    Filed: June 10, 2010
    Date of Patent: June 25, 2013
    Assignee: Mallinckrodt LLC
    Inventors: Christopher W. Grote, Gary L. Cantrell, Joseph P. McClurg, Catherine E. Thomasson, Frank W. Moser
  • Patent number: 8461337
    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: Grant
    Filed: December 17, 2008
    Date of Patent: June 11, 2013
    Assignee: Mallinckrodt LLC
    Inventors: Peter X. Wang, Tao Jiang, Gary L. Cantrell, David W. Berberich, Bobby N. Trawick, Subo Liao, John Brandt
  • Patent number: 8455644
    Abstract: The present invention provides a compound of formula I: wherein X?, R1, and R2 are as defined herein, and compositions thereof.
    Type: Grant
    Filed: July 11, 2012
    Date of Patent: June 4, 2013
    Assignee: Wyeth
    Inventors: Nataliya Bazhina, George Joseph Donato, III, Steven R. Fabian, John Lokhnauth, Sreenivasulu Megati, Charles Melucci, Christian Ofslager, Niketa Patel, Galen Radebaugh, Syed M. Shah, Jan Szeliga, Huyi Zhang, Tianmin Zhu
  • Patent number: 8436175
    Abstract: A compound of formula I is disclosed. Compounds of formula I are useful as analgesics, anti-inflammatory agents, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction medications.
    Type: Grant
    Filed: March 22, 2011
    Date of Patent: May 7, 2013
    Assignee: Rensselaer Polytechnic Institute
    Inventor: Mark P. Wentland
  • Patent number: 8431701
    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: Grant
    Filed: February 17, 2010
    Date of Patent: April 30, 2013
    Assignee: Mallinckrodt LLC
    Inventors: Edmund C. Hudson, Sharon Woods