Two Of The Cyclos Share At Least Three Ring Members (e.g., Morphinans, Etc.) Patents (Class 546/74)
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Patent number: 12146889Abstract: This disclosure relates to administration of a combination of: 1) about 100-110 mg, about 104-106 mg, or about 105 mg or less of bupropion hydrochloride, or a molar equivalent amount of the free base form or another salt form of bupropion; and 2) about 40-50 mg, about 44-46 mg, or about 45 mg or less of dextromethorphan hydrobromide, or a molar equivalent amount of the free base form or another salt form of dextromethorphan in certain patient populations, such as patients having moderate renal impairment, patients receiving a concomitant strong CYP2D6 inhibitor, patients who are known CYP2D6 poor metabolizers, those in need of an NMDA antagonist that does not cause dissociation, and those at risk of QT prolongation.Type: GrantFiled: October 25, 2023Date of Patent: November 19, 2024Assignee: ANTECIP BIOVENTURES II LLCInventor: Herriot Tabuteau
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Patent number: 12076316Abstract: The presently described technology provides compositions of one or more of oxoacids, amino acids, polyethylene glycols, and/or vitamin compounds chemically conjugated to levorphanol ((?)-17-methylmorphinan-3-ol) to form novel prodrugs and compositions of levorphanol.Type: GrantFiled: December 14, 2021Date of Patent: September 3, 2024Inventors: Travis Mickle, Sven Guenther, Sanjib Bera
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Patent number: 11376245Abstract: The present invention relates to compounds of formula (I) for use as peripheral NMDA receptor antagonists.Type: GrantFiled: June 13, 2017Date of Patent: July 5, 2022Assignees: INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE (INSERM), CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (CNRS), UNIVERSITE PARIS SUD, ASSISTANCE PUBLIQUE—HOPITAUX DE PARIS (APHP), HOPITAL MARIE LANNELONGUEInventors: Sylvia Cohen-Kaminsky, Marc Humbert, Sebastien Dumas, Gilles Bru-Mercier, Samir Messaoudi, Jean-Daniel Brion, Mouad Alami, Gilles Galvani
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Patent number: 11234975Abstract: The presently described technology provides compositions of one or more of oxoacids, amino acids, polyethylene glycols, and/or vitamin compounds chemically conjugated to levorphanol ((?)-17-methylmorphinan-3-ol) to form novel prodrugs and compositions of levorphanol.Type: GrantFiled: April 12, 2018Date of Patent: February 1, 2022Assignee: KEMPHARM, INC.Inventors: Travis Mickle, Sven Guenther, Sanjib Bera
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Patent number: 11214544Abstract: The presently described technology provides compositions of one or more of oxoacids, polyethylene glycols, and/or vitamin compounds chemically conjugated to dextrorphan, (+)-17-methylmorphinan-3-ol), to form novel prodrugs and compositions of dextrorphan.Type: GrantFiled: April 12, 2018Date of Patent: January 4, 2022Assignee: KEMPHARM, INC.Inventors: Travis Mickle, Sven Guenther, Sanjib Bera
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Patent number: 10865187Abstract: The application describes methods for making a deuterated dextromethorphan of Formula (I), deuterated dextromethorphan produced by these methods, and pharmaceutically acceptable salts thereof.Type: GrantFiled: June 24, 2020Date of Patent: December 15, 2020Assignee: Avanir Pharmaceuticals, Inc.Inventors: Matt Johnson, Cunxiang Zhao, Weihua Meng, Zhijun Lu, Yan Li
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Patent number: 10851063Abstract: A method for producing substantially pure levorphanol and related compounds, when compared to the conventional process, is provided. In particular, a method for producing substantially pure levorphanol tartrate dihydrate is described. Also described are compositions comprising levorphanol and related compounds, particularly compositions comprising levorphanol tartrate dihydrate, levomethorphan, and norlevorphanol in which the levomethorphan and norlevorphanol are present in the composition in reduced levels.Type: GrantFiled: October 4, 2018Date of Patent: December 1, 2020Assignee: AMPAC FINE CHEMICALS LLCInventors: William Dubay, Alex Nichols, Wei Chen, Alec Brozell, Ajay Ryerson
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Patent number: 10464904Abstract: 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: GrantFiled: December 2, 2016Date of Patent: November 5, 2019Assignee: Heinrich-Heine-Universitat DusseldorfInventors: Eckhard Lammert, Alena Welters, Silke Otter, Jan Marquard, Thomas Meissner, Diran Herebian, Ertan Mayatepek
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Patent number: 10287250Abstract: 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: GrantFiled: May 15, 2017Date of Patent: May 14, 2019Assignee: ALKERMES PHARMA IRELAND LIMITEDInventors: Laura Cook Blumberg, Daniel R. Deaver, David J. Eyerman, Thomas Andrew Wynn
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Patent number: 10081602Abstract: 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: GrantFiled: May 24, 2017Date of Patent: September 25, 2018Assignee: Nektar TherapeuticsInventors: Franco J. Duarte, Neel K. Anand, Pankaj Sharma, Devendrapratap Singh
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Patent number: 9868976Abstract: 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: March 11, 2016Date of Patent: January 16, 2018Assignee: Concert Pharmaceuticals, Inc.Inventor: Roger D. Tung
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Patent number: 9688638Abstract: 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: GrantFiled: November 27, 2014Date of Patent: June 27, 2017Assignee: Nektar TherapeuticsInventors: Franco J. Duarte, Neel K. Anand, Pankaj Sharma, Devendrapratap Singh
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Patent number: 9656962Abstract: 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: GrantFiled: December 19, 2014Date of Patent: May 23, 2017Assignee: Purdue Pharma L.P.Inventors: Jeffrey Lockman, Laykea Tafesse
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Patent number: 9562014Abstract: 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: GrantFiled: December 22, 2010Date of Patent: February 7, 2017Assignee: Mallinckrodt LLCInventors: Bobby N. Trawick, David W. Berberich, Christopher W. Grote
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Patent number: 9040552Abstract: 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: GrantFiled: December 4, 2012Date of Patent: May 26, 2015Assignee: Alkermes, Inc.Inventors: Derrick Arnelle, Daniel Deaver, Reginald L. Dean, III, Mark Todtenkopf
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Patent number: 9029543Abstract: The invention relates to a process for the synthesis of quaternized compounds of formula:Type: GrantFiled: April 5, 2012Date of Patent: May 12, 2015Assignee: Alkermes, Inc.Inventor: Scott Duncan
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Publication number: 20150119416Abstract: 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: January 5, 2015Publication date: April 30, 2015Applicant: RENSSELAER POLYTECHNIC INSTITUTEInventor: Mark P. WENTLAND
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Publication number: 20150099776Abstract: 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: ApplicationFiled: May 9, 2013Publication date: April 9, 2015Applicants: PONTIFICIA UNIVERSIDAD CATÓLICA DE CHILE, UNIVERSITAT DE BARCELONAInventors: Diego Muñoz-Torrero López-Ibarra, Nibaldo Manuel Inestrosa CantÃn, Elisabet Viayna Gaza, Irene Sola Lao, Santiago Vázquez Cruz
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Publication number: 20150087670Abstract: 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: ApplicationFiled: February 24, 2013Publication date: March 26, 2015Inventor: Mahesh Kandula
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Patent number: 8987293Abstract: 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: GrantFiled: December 23, 2011Date of Patent: March 24, 2015Assignee: Phoenix Pharmalabs, Inc.Inventor: John Lawson
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Patent number: 8969562Abstract: 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: GrantFiled: March 11, 2014Date of Patent: March 3, 2015Assignee: AbbVie, Inc.Inventors: Albert Wayne Kruger, Shuang Chen, Steven Cramer Cullen, James Joseph Napier
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Patent number: 8962646Abstract: The invention relates to a compound of Formula I, II, III, IV or a pharmaceutically acceptable ester or prodrug thereof:Type: GrantFiled: June 29, 2012Date of Patent: February 24, 2015Assignee: Alkermes, Inc.Inventors: Laura Cook Blumberg, Derrick Arnelle
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Patent number: 8957085Abstract: 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 12, 2014Date of Patent: February 17, 2015Assignee: Rensselaer Polytechnic InstituteInventor: Mark P. Wentland
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Publication number: 20150045384Abstract: 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: ApplicationFiled: May 23, 2014Publication date: February 12, 2015Applicant: ALKERMES PHARMA IRELAND LIMITEDInventors: Laura Cook Blumberg, Dan Deaver, David Eyerman
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Patent number: 8946255Abstract: 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: GrantFiled: December 23, 2013Date of Patent: February 3, 2015Assignee: Purdue Pharma L.P.Inventors: Andrew Kassick, Jeffrey Lockman, Laykea Tafesse
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Publication number: 20150025067Abstract: Inhibitors of p67phox protein are provided herein, as well as pharmaceutical compositions and methods relating thereto.Type: ApplicationFiled: February 13, 2013Publication date: January 22, 2015Applicant: CHILDREN'S HOSPITAL MEDICAL CENTERInventors: Yi Zheng, Prakash Jagtap, Emily E. Bosco, Jaroslaw Meller, Marie-Dominique Filippi
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Publication number: 20150011768Abstract: 4-Hydroxybenzomorphans containing carboxamide or thiocarboxamide at the 3-position are useful as analgesics, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction medications.Type: ApplicationFiled: July 2, 2014Publication date: January 8, 2015Applicant: Rensselaer Polytechnic InstituteInventor: Mark P. WENTLAND
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Patent number: 8916582Abstract: 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: GrantFiled: March 13, 2014Date of Patent: December 23, 2014Assignee: Concert Pharmaceuticals, Inc.Inventors: Philip B. Graham, I. Robert Silverman
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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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Publication number: 20140315940Abstract: 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: March 13, 2014Publication date: October 23, 2014Applicant: Concert Pharmaceuticals, Inc.Inventors: Philip B. Graham, I. Robert Silverman
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Publication number: 20140275545Abstract: 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: ApplicationFiled: December 19, 2013Publication date: September 18, 2014Applicant: Rensselaer Polytechnic InstituteInventor: Mark P. WENTLAND
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Publication number: 20140275546Abstract: 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: ApplicationFiled: March 11, 2014Publication date: September 18, 2014Applicant: AbbVie Inc.Inventors: Albert Wayne KRUGER, Shuang CHEN, Steven Cramer CULLEN, James Joseph NAPIER
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Patent number: 8802655Abstract: 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: GrantFiled: January 31, 2014Date of Patent: August 12, 2014Assignee: Rensselaer Polytechnic InstituteInventor: Mark P. Wentland
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Publication number: 20140194457Abstract: 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 12, 2014Publication date: July 10, 2014Applicant: Rensselaer Polytechnic InstituteInventor: Mark P. WENTLAND
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Patent number: 8772310Abstract: 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: November 9, 2012Date of Patent: July 8, 2014Assignee: Wyeth LLCInventors: Charles K. Melucci, John Lokhnauth
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Publication number: 20140187573Abstract: 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: ApplicationFiled: December 23, 2013Publication date: July 3, 2014Applicant: Purdue Pharma L.P.Inventors: Andrew KASSICK, Jeffrey LOCKMAN, Laykea TAFESSE
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Patent number: 8748450Abstract: 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: July 24, 2013Date of Patent: June 10, 2014Assignee: Concert Pharmaceuticals, Inc.Inventor: Roger Tung
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Publication number: 20140148475Abstract: 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: ApplicationFiled: January 31, 2014Publication date: May 29, 2014Applicant: Rensselaer Polytechnic InstituteInventor: Mark P. WENTLAND
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Patent number: 8710072Abstract: 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: GrantFiled: September 18, 2009Date of Patent: April 29, 2014Assignee: Concert Pharmaceuticals, Inc.Inventors: Philip B. Graham, I. Robert Silverman
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Patent number: 8703949Abstract: 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: GrantFiled: August 3, 2011Date of Patent: April 22, 2014Assignee: Mallinckrodt LLCInventors: Subo Liao, Peter X. Wang, David W. Berberich, Douglas C. Miller
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Publication number: 20140107143Abstract: Compounds of formulas: are disclosed. The compounds are useful for ameliorating the side effects of therapeutic opiates.Type: ApplicationFiled: September 27, 2013Publication date: April 17, 2014Applicant: Rensselaer Polytechnic InstituteInventor: Mark P. WENTLAND
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Publication number: 20130345251Abstract: 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, 2013Publication date: December 26, 2013Applicant: Rensselaer Polytechnic InstituteInventor: Mark P. WENTLAND
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Publication number: 20130338182Abstract: 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: ApplicationFiled: December 23, 2011Publication date: December 19, 2013Applicant: PHEONIX PHARMALABS, INC.Inventor: John Lawson
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Publication number: 20130281483Abstract: 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: ApplicationFiled: November 9, 2012Publication date: October 24, 2013Applicant: Wyeth LLCInventor: Wyeth LLC
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Patent number: 8563572Abstract: Compounds of formulas: are disclosed. The compounds are useful for ameliorating the side effects of therapeutic opiates.Type: GrantFiled: August 9, 2012Date of Patent: October 22, 2013Assignee: Rensselaer Polytechnic InstituteInventor: Mark P. Wentland
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Publication number: 20130274280Abstract: This invention provides an oral pharmaceutical composition comprising a physiologically tolerable gelled oil-in-water emulsion containing a drug of abuse.Type: ApplicationFiled: April 11, 2011Publication date: October 17, 2013Applicant: AYANDA GROUP ASInventors: Kurt Ingar Draget, Ingvild Johanne Haug, Steinar Johan Engelsen, Tore Seternes, Magnus N. Hattrem
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Patent number: 8557837Abstract: 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: GrantFiled: February 9, 2011Date of Patent: October 15, 2013Assignees: Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, Shanghai Institutes for Biological Sciences, Chinese Academy of SciencesInventors: Zhujun Yao, Bing Sun, Yangtong Lou, Zhenyu Yang, Aizhong Chen, Zhao Ma
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Patent number: 8557784Abstract: 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: GrantFiled: July 7, 2011Date of Patent: October 15, 2013Assignee: Standard Chem. & Pharm. Co., Ltd.Inventors: Chin-Tsai Fan, Cheng-Shun Lai, Wen-Yen Yeh, Yu-Ying Liu
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Patent number: 8541436Abstract: 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: May 31, 2011Date of Patent: September 24, 2013Assignee: Concert Pharmaceuticals Inc.Inventor: Roger Tung
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Publication number: 20130231361Abstract: 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: ApplicationFiled: April 15, 2013Publication date: September 5, 2013Applicant: Rensselaer Polytechnic InstitueInventor: Mark P. WENTLAND