Two Of The Cyclos Share At Least Three Ring Members (e.g., Morphinans, Etc.) Patents (Class 546/74)
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Patent number: 8471023Abstract: 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: GrantFiled: June 10, 2010Date of Patent: June 25, 2013Assignee: Mallinckrodt LLCInventors: Christopher W. Grote, Gary L. Cantrell, Joseph P. McClurg, Catherine E. Thomasson, Frank W. Moser
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Patent number: 8461337Abstract: 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: GrantFiled: December 17, 2008Date of Patent: June 11, 2013Assignee: Mallinckrodt LLCInventors: Peter X. Wang, Tao Jiang, Gary L. Cantrell, David W. Berberich, Bobby N. Trawick, Subo Liao, John Brandt
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Patent number: 8455644Abstract: The present invention provides a compound of formula I: wherein X?, R1, and R2 are as defined herein, and compositions thereof.Type: GrantFiled: July 11, 2012Date of Patent: June 4, 2013Assignee: WyethInventors: 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
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Patent number: 8436175Abstract: 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: GrantFiled: March 22, 2011Date of Patent: May 7, 2013Assignee: Rensselaer Polytechnic InstituteInventor: Mark P. Wentland
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Patent number: 8431701Abstract: 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: GrantFiled: February 17, 2010Date of Patent: April 30, 2013Assignee: Mallinckrodt LLCInventors: Edmund C. Hudson, Sharon Woods
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Patent number: 8404706Abstract: The present invention relates to opioid and opioid-like compounds, and pharmaceutical formulations containing the same and methods of use thereof. Uses of the present invention include, but are not limited to, use for the prevention and treatment of septic shock and other disorders. The compounds described herein can be water soluble and can act through mechanisms mediated through pathways other than opiate receptors.Type: GrantFiled: April 6, 2011Date of Patent: March 26, 2013Assignee: Jenken Biosciences, Inc.Inventors: Edwin S. C. Wu, Mao-Hsiung Yen, Chin-Tsai Fan
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Patent number: 8367827Abstract: The present disclosure generally relates to a process for converting a fused, tricyclic compound to a fused, tetracyclic compound that includes a furan ring therein. More particularly, the present disclosure related to a process for preparing a hydrocodone compound, or a compound structurally related thereto, and in particular (+)-hydrocodone, by subjecting a structurally corresponding sinomenine starting compound to a super acid-assisted furan ring closure reaction.Type: GrantFiled: November 30, 2009Date of Patent: February 5, 2013Assignee: Mallinckrodt LLCInventors: Peter X. Wang, Tao Jiang, Subo Liao, Erin Moore
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Publication number: 20130029941Abstract: New highly functionalizable Huprine derivatives of formula I: and a method for preparing such compounds and their use for treating neurological diseases in which the level of acetylcholine is affected such as Alzheimer's disease.Type: ApplicationFiled: April 8, 2011Publication date: January 31, 2013Applicant: UNIVERSITE DE ROUENInventors: Cyril Ronco, Pierre Yves Renard, Ludovic Jean, Florian Nachon, Anthony Romieu
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Patent number: 8354534Abstract: The present invention relates to compounds of Formula I or II, or pharmaceutically acceptable salts, esters, or prodrugs thereof: which relates to morphinan 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: GrantFiled: February 13, 2009Date of Patent: January 15, 2013Assignee: Alkermes, Inc.Inventors: Derrick Arnelle, Daniel Deaver, Reginald L. Dean, III, Mark Todtenkopf
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Publication number: 20130011929Abstract: The present invention provides a compound of formula I: wherein X?, R1, and R2 are as defined herein, and compositions thereof.Type: ApplicationFiled: July 11, 2012Publication date: January 10, 2013Applicant: WyethInventors: 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
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Publication number: 20130005755Abstract: The invention relates to a compound of Formula I, II, III, IV or a pharmaceutically acceptable ester or prodrug thereof:Type: ApplicationFiled: June 29, 2012Publication date: January 3, 2013Inventors: Laura Cook Blumberg, Derrick Arnelle
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Patent number: 8338446Abstract: 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: GrantFiled: March 28, 2008Date of Patent: December 25, 2012Assignee: Wyeth LLCInventors: Charles K. Melucci, John Lokhnauth
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Publication number: 20120316343Abstract: The present invention provides compositions of 6-amino morphinan compounds and process for their synthesis. In particular, the processes provide for the reductive amination of 6-keto morphinans by catalytic transfer hydrogenation, to produce 6-amino morphinan compounds, which are epimerically and/or diastereomerically enriched.Type: ApplicationFiled: June 8, 2012Publication date: December 13, 2012Applicant: Mallinckrodt LLCInventors: Christopher W. Grote, Joseph P. McClurg, John E. Johnson, JR., Sarah M. Farris
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Publication number: 20120308589Abstract: 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: ApplicationFiled: February 9, 2011Publication date: December 6, 2012Applicants: Shanghai Institutes for Biological Sciences, Chinese Academy of Sciences, Shanghai Institute of Organic Chemistry, Chinese Academy of SciencesInventors: Zhujun Yao, Bing Sun, Yangtong Lou, Zhenyu Yang, Aizhong Chen, Zhao Ma
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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: 8293907Abstract: The present invention provides processes for the preparation of saturated ketone morphinan compounds by catalytic isomerization. In particular, the invention provides processes for the conversion of a morphinan comprising an allyl alcohol ring moiety into a morphinan comprising a saturated ketone ring moiety by an isomerization reaction catalyzed by an allyl-transition metal catalyst.Type: GrantFiled: April 9, 2010Date of Patent: October 23, 2012Assignee: Mallinckrodt Inc.Inventors: Peter X. Wang, Tao Jiang, David W. Berberich
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Publication number: 20120258981Abstract: The invention relates to a process for the synthesis of quaternized compounds of formula:Type: ApplicationFiled: April 5, 2012Publication date: October 11, 2012Applicant: Alkermes, Inc.Inventor: Scott Duncan
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Publication number: 20120245193Abstract: The present invention relates to a novel functional peripherally-acting ? opioid receptor antagonist of Formula I: The novel compounds of the present invention have reduced oral bioavailability without compromising opiate-induced analgesia in the CNS. The compounds of the present invention are further efficacious at low doses and are useful in treating gastrointestinal conditions associated with opioid analgesic therapy.Type: ApplicationFiled: February 14, 2012Publication date: September 27, 2012Inventors: Bernard Silverman, Mark Todtenkopf, Daniel Deaver, Lauren DiPetrillo
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Patent number: 8252808Abstract: The invention generally provides processes and intermediate compounds useful for the production of (+)-opiates. Non-limiting examples of (+) opiates that may be derived from one or more compounds of the invention include (+)-noroxymorphone, (+)-naltrexone, (+)-naloxone, (+)-N-cyclopropylmethylnorhydrocodone, (+)-N-cycloproylmethylnorhydromorphone, (+)-N-allylnorhydrocodone, (+)-N-allylnorhydromorphone, (+)-noroxycodone, (+)-naltrexol, (+)-naloxol, and (+)-3-O-methyl-naltrexone.Type: GrantFiled: December 17, 2008Date of Patent: August 28, 2012Assignee: Mallinckrodt LLCInventors: Peter X. Wang, Tao Jiang, Gary L. Cantrell, David W. Berberich, Bobby N. Trawick, Todd Osiek, Subo Liao, Frank W. Moser, Joseph P. McClurg
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Patent number: 8227609Abstract: A process for purifying plant extracts which consist essentially of noroxymorphone compounds and which comprise, as impurities, ?,?-unsaturated noroxymorphone compounds, by (a) converting the plant extract or the product of a subsequent stage in the synthesis of a selected noroxymorphone compound in a reaction which converts the hydroxyl groups present in the mixture to leaving groups of the formula —OR2 in which R2 is the introduced radical of the leaving group, (b) these leaving groups are optionally detached again, then (c) the resulting mixture is subjected to a selective hydrogenation, so that a saturated bond is formed in the ?,?-position of the unsaturated noroxymorphone compounds and any remaining leaving groups are each converted to a hydroxyl group and then optionally (d) the pure noroxymorphone compound is isolated; processing of the noroxymorphone purified in this way to naltrexone or naloxone or a salt of these compounds or a quaternary derivative of these compounds; pharmaceutical formulations cType: GrantFiled: February 9, 2006Date of Patent: July 24, 2012Assignee: CILAG AGInventors: Ulrich Weigl, Ulf Kötz, Ilia Freifeld
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Publication number: 20120129879Abstract: The invention relates generally to anti-angiogenesis agents and related methods of using to anti-angiogenesis agents for biomedical applications including direct monotherapy and combination therapy for treatment of an angiogenesis related condition. In an embodiment, the invention provides a class of opioid compounds and structurally related opioid derivatives exhibiting anti-VEGF activity for use in therapeutic procedures, including phototherapy. Opioid compounds and structurally related opioid derivatives of the invention may be administered alone or in combination with administration of a phototherapy agent and/or other therapeutic agent.Type: ApplicationFiled: July 16, 2010Publication date: May 24, 2012Inventors: Gary L. Cantrell, Raghavan Rajagopalan, David W. Berberich, Amolkumar Karwa, Richard B. Dorshow
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Publication number: 20120122848Abstract: A novel (+)-3-hydroxymorphinan derivatives and a pharmaceutical composition comprising the same as an active ingredient, which are useful for preventing or treating a neurodegenerative disease, are provided.Type: ApplicationFiled: July 28, 2010Publication date: May 17, 2012Applicant: GREEN CROSS CORPORATIONInventors: Jinhwa Lee, Jong Yup Kim, Kwang-Seop Song, Jeongmin Kim, Kwang Woo Ahn, Yonggyu Kong
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Patent number: 8178551Abstract: The present invention is directed to a novel prodrug of (+)-3-hydroxymorphinan compound of formula (I) or a pharmaceutically acceptable salt thereof, a method for preparing the same, and its use for preventing or treating Parkinson's disease.Type: GrantFiled: March 7, 2008Date of Patent: May 15, 2012Assignee: Green Cross CorporationInventors: Jinhwa Lee, Jeongmin Kim, Myung Eun Jung, Jong Yup Kim, Kwang-Seop Song, Eun Jung Son, Suk Ho Lee, Ho Kyun Han, Min Ju Kim, MinWoo Lee
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Patent number: 8173678Abstract: Kappa opioid receptor antagonists are provided that yield significant improvements in functional binding assays to kappa opioid receptors, and the use of these antagonists in treatment of disease states that are ameliorated by binding of the kappa opioid receptor such as heroin or cocaine addictions.Type: GrantFiled: October 25, 2010Date of Patent: May 8, 2012Assignee: Research Triangle InstituteInventors: Frank Ivy Carroll, Hernan A. Navarro, Lawrence E. Brieaddy, Scott P. Runyon, James B. Thomas
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Patent number: 8136974Abstract: To provide a light-emitting device that is capable of red-light-emitting with high luminance and high efficiency and that is excellent in endurance; and a metal coordination compound metal coordination compound having a partial structure represented by formula (1) that can be used in the light-emitting device, and that can also be used in applications, such as organic electroluminescent device materials, electrochemiluminescence (ECL) device materials, emission sensors, photosensitizers, displays, photographic materials, laser dyes, color filter dyes, optical communications, color conversion filters, backlights, illuminations, photosensitizing dyes, various light sources, and the like.Type: GrantFiled: December 7, 2007Date of Patent: March 20, 2012Assignee: National Institute of Advanced Industrial Science and TechnologyInventor: Hideo Konno
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Patent number: 8115002Abstract: The present invention is directed to processes for the synthesis of morphinan-6-ones and salts, intermediates, and analogs thereof.Type: GrantFiled: September 6, 2007Date of Patent: February 14, 2012Assignee: Mallinckrodt LLCInventors: Peter X. Wang, Frank W. Moser, Gary L. Cantrell, Christopher W. Grote
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Publication number: 20120029007Abstract: 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: ApplicationFiled: June 8, 2011Publication date: February 2, 2012Inventors: Philip B. Graham, I. Robert Silverman
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Patent number: 8106065Abstract: An antitussive, which can be used for therapy or prophylaxis of coughing, is disclosed. The antitussive comprises as an effective ingredient a morphinan derivative having a nitrogen-containing cyclic substituent or a pharmaceutically acceptable acid addition salt thereof, having a specific structure, such as the compound below [N-(17-cyclopeopylmethyl-4,5?-epoxy-3,14-dihydroxy-morphinan-6?-yl)-3,4,5,6-tetrahydrophthalimide]. The antitussive has an excellent therapeutic or prophylactic effect against coughing and the side effects thereof are small.Type: GrantFiled: December 15, 2006Date of Patent: January 31, 2012Assignee: Toray Industries, Inc.Inventors: Naoki Izumimoto, Koji Kawai
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Patent number: 8080661Abstract: The invention provides processes for the preparation of morphinans having a tertiary amine. In particular, the present invention provides processes for the formation of tertiary amine alkaloids by direct N-alkylation of secondary amine alkaloids, the processes co-mediated by an alkylating agent and a protic solvent or a mixture of a protic solvent and an aprotic solvent.Type: GrantFiled: September 29, 2009Date of Patent: December 20, 2011Assignee: Mallinckrodt LLCInventors: Peter X. Wang, Tao Jiang, David W. Berberich
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Publication number: 20110306603Abstract: 8-Substituted-2,6-methano-3-benzazocines of general structure are useful as analgesics, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction medications.Type: ApplicationFiled: August 23, 2011Publication date: December 15, 2011Applicant: RENSSELAER POLYTECHNIC INSTITUTEInventor: Mark P. Wentland
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Publication number: 20110257214Abstract: 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: ApplicationFiled: September 18, 2009Publication date: October 20, 2011Inventors: Philip B. Graham, I. Robert Silverman
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Publication number: 20110243889Abstract: The present invention relates to opioid and opioid-like compounds, and pharmaceutical formulations containing the same and methods of use thereof. Uses of the present invention include, but are not limited to, use for the prevention and treatment of septic shock and other disorders. The compounds described herein can be water soluble and can act through mechanisms mediated through pathways other than opiate receptors.Type: ApplicationFiled: April 6, 2011Publication date: October 6, 2011Inventors: Edwin S.C. WU, Mao-Hsiung Yen, Chin-Tsai Fan
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Patent number: 8026252Abstract: 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: June 3, 2009Date of Patent: September 27, 2011Assignee: Rensselaer Polytechnic InstituteInventor: Mark P. Wentland
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Publication number: 20110230511Abstract: 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: ApplicationFiled: March 22, 2011Publication date: September 22, 2011Applicant: RENSSELAER POLYTECHNIC INSTITUTEInventor: Mark P. Wentland
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Publication number: 20110212173Abstract: There is described a pharmaceutical composition for controlled release of an active compound wherein the active compound is selected from the group comprising tramadol, resveratrol, acetaminophen, xorphanol, cinfenoac, furcloprofen, bismuth subsalicylate, enofelast, triflusal, ketorfanol, indriline, furofenac, cizolirtine, dacemazine, demelverine, and fenethazine, and derivatives and/or combinations thereof for the treatment or alleviation of depression. More particularly, there is described an abuse resistant pharmaceutical composition for the treatment of inter alia, depression and controlled release pharmaceutical compositions of related thereto.Type: ApplicationFiled: June 17, 2009Publication date: September 1, 2011Applicant: e-Therapeutics PleInventors: Malcolm Philip Young, Olusola Clement Idowu, Philip McKeown
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Publication number: 20110206780Abstract: The present invention relates to new morphinan modulators of NMDA receptors, ?1 receptors, ?2 receptors, and/or ?3?4 nicotinic receptors, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: January 5, 2011Publication date: August 25, 2011Applicant: Auspex Pharmaceuticals, Inc.Inventors: Thomas G. Gant, Sepehr Sarshar, Chengzhi Zhang
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Patent number: 7999105Abstract: Processes are described for the synthesis of 3-hydroxymorphinan derivatives by hydrolysis of side products from the O-demethylation of 3-methoxymorphinan derivatives.Type: GrantFiled: February 18, 2009Date of Patent: August 16, 2011Assignee: Mallinckrodt Inc.Inventors: Peter X. Wang, Tao Jiang, Gary L. Cantrell, David W. Berberich, Frank W. Moser, Jian Bao
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Publication number: 20110190267Abstract: The present invention concerns prodrugs of opioid analgesics and pharmaceutical compositions containing such prodrugs. Methods for providing more consistent pain relief by increasing the bioavailability of the opioid analgesic with the aforementioned prodrugs are provided. The invention also provides for decreasing the adverse GI side effects of opioid analgesics.Type: ApplicationFiled: December 23, 2010Publication date: August 4, 2011Applicant: Shire Pharmaceuticals, Inc.Inventors: Richard Franklin, Karl Swift, Bernard T. Golding, Robert G. Tyson
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Patent number: 7973049Abstract: 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: GrantFiled: April 30, 2008Date of Patent: July 5, 2011Assignee: Concert Pharmaceuticals Inc.Inventor: Roger Tung
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Patent number: 7943633Abstract: Anti-malarial alkyloid compounds have the formula: wherein R1-R11 have various disclosed values or their pharmaceutically acceptable salts, and pharmaceutical compositions containing the same.Type: GrantFiled: October 20, 2006Date of Patent: May 17, 2011Assignees: Universite Pierre et Marie Curie (Paris VI), Centre National de la Recherche Scientifique, Museum National d'Histoire Naturelle, Institut Malgache de Recherche AppliqueeInventors: François Frappier, Marie-Pierre Frappier, legal representative, Jérôme Frappier, legal representative, Dominique Mazier, Maëlle Carraz, Jean-François Franetich, Akino Jossang, Roger Joyeau, Phillippe Rasoanaivo
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Publication number: 20110112131Abstract: The present invention relates to the field of pain management, and more particularly to synergistic codrugs comprising an opioid and ketamine or norketamine which have been combined to form a single chemical codrug entity. When the codrug is administered it produces a synergistic analgesic response to pain.Type: ApplicationFiled: March 27, 2009Publication date: May 12, 2011Applicant: University of Kentucky Research Foundation A144 ASTeCC BuildingInventors: Joseph R. Holtman, Peter A. Crooks, Ujjwal Chakraborty
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Publication number: 20110112130Abstract: The present invention relates to the field of pain management, and more particularly to synergistic codrugs comprising an opioid and nornicotine which have been combined to form a single chemical codrug entity. When the codrug is administered it produces a synergistic analgesic response to pain.Type: ApplicationFiled: March 27, 2009Publication date: May 12, 2011Applicant: University of Kentucky Research FoundationInventors: Joseph R. Holtman, Peter A. Crooks, Ujjwal Chakraborty
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Patent number: 7932264Abstract: The present invention relates to the preparation and pharmacological use of sinomenine derivatives of formula I. The approach disclosed herein is the modification of D ring by-substituting for R. Additional substitutions in the other rings are also provided herein. Several of the sinomenine derivatives have significantly greater anti-inflammation activity when compared with the parent compound.Type: GrantFiled: December 15, 2006Date of Patent: April 26, 2011Assignee: Naturemed Group CorporationInventors: Jie Wang, Yi Pan
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Patent number: 7923454Abstract: The present invention relates to opioid and opioid-like compounds, and pharmaceutical formulations containing the same and methods of use thereof. Uses of the present invention include, but are not limited to, use for the prevention and treatment of septic shock and other disorders. The compounds described herein can be water soluble and can act through mechanisms mediated through pathways other than opiate receptors.Type: GrantFiled: September 8, 2004Date of Patent: April 12, 2011Assignee: Jenken Biosciences, Inc.Inventors: Edwin S. C. Wu, Mao-Hsiung Yen, Chin-Tsai Fan
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Publication number: 20110071296Abstract: The present invention provides processes for the preparation of 10-keto and/or 10-hydroxy morphinans. In particular, the invention provides to processes for preparing a 10-keto morphinan by chromium-catalyzed benzylic oxidation of a morphinan with a periodic acid.Type: ApplicationFiled: September 7, 2010Publication date: March 24, 2011Applicant: Mallinckrodt Inc.Inventors: Hang Sun, John E. Johnson, JR., Ricky L. Fenton, Sarah M. Dorn
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Publication number: 20110065743Abstract: Kappa opioid receptor antagonists are provided that yield significant improvements in functional binding assays to kappa opioid receptors, and the use of these antagonists in treatment of disease states that are ameliorated by binding of the kappa opioid receptor such as heroin or cocaine addictions.Type: ApplicationFiled: October 25, 2010Publication date: March 17, 2011Applicant: Research Triangle InstituteInventors: Frank Ivy CARROLL, Hernan A. Navarro, Lawrence E. Brieaddy, Scott P. Runyon, James B. Thomas
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Publication number: 20110015219Abstract: The present invention provides (+)-morphinans comprising Toll-like receptor 9 (TLR9) antagonist activity, as well as a method for identifying (+)-morphinans that may be therapeutically effective by determining whether the (+)-morphinan inhibits the activation of TLR9. Also provided are methods of using the (+)-morphinans comprising TLR9 antagonist activity to treat conditions such as traumatic pain, neuropathic pain, inflammatory disorders, acetaminophen toxicity, autoimmune disorders, neurodegenerative disorders, and cancer.Type: ApplicationFiled: July 16, 2010Publication date: January 20, 2011Applicant: Mallinckrodt Inc.Inventors: Bobby N. Trawick, David W. Berberich
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Publication number: 20100317858Abstract: To provide a light-emitting device that is capable of red-light-emitting with high luminance and high efficiency and that is excellent in endurance; and a metal coordination compound metal coordination compound having a partial structure represented by formula (1) that can be used in the light-emitting device, and that can also be used in applications, such as organic electroluminescent device materials, electrochemiluminescence (ECL) device materials, emission sensors, photosensitizers, displays, photographic materials, laser dyes, color filter dyes, optical communications, color conversion filters, backlights, illuminations, photosensitizing dyes, various light sources, and the like.Type: ApplicationFiled: December 7, 2007Publication date: December 16, 2010Applicant: NATIONAL INSTITUTE OF ADVANCE INDUSTRIAL SCIENCE AND TECHNOLOGYInventor: Hideo Konno
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Publication number: 20100317861Abstract: 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: ApplicationFiled: June 10, 2010Publication date: December 16, 2010Applicant: Mallinckrodt Inc.Inventors: Christopher W. Grote, Gary L. Cantrell, Joseph P. McClurg, Catherine E. Thomasson, Frank W. Moser
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Patent number: 7838677Abstract: The present invention is directed to processes for the synthesis of morphinans. In particular, a process for cyclizing a ?,?-bicyclic ketone compound to form a nordihydrothebainone product using the Grewe cyclization reaction is improved by forming a reaction mixture comprising a ?,?-bicyclic ketone compound, a cyclizing acid and a water scavenging cyclization additive. In one embodiment, the Grewe transformation occurs in the presence of an acid anhydride as the cyclization additive. Further, the present invention is directed to processes for converting ?,?-bicyclic ketone compounds (e.g., by-products of the Grewe cyclization reaction) to ?,?-bicyclic ketone compounds, wherein the ?,?-bicyclic ketone compounds may be recovered to further undergo Grewe cyclization and form the nordihydrothebainone product.Type: GrantFiled: February 23, 2006Date of Patent: November 23, 2010Assignee: Mallinckrodt IncInventors: Peter Xianqi Wang, Frank W. Moser, Gary L. Cantrell, Jian Bao