A Single Chalcogen Is Bonded Directly To Ring Carbon Of The Pentacyclo Ring System (e.g., Desoxy Morphine, Etc.) Patents (Class 546/46)
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Publication number: 20110269964Abstract: The present invention provides an efficient process for preparing N-alkylated opiates. In particular, processes are provided for using a chloride-containing alkylating agent and a bromide or iodide salt to alkylate the corresponding nor-opiate.Type: ApplicationFiled: April 28, 2011Publication date: November 3, 2011Applicant: Mallinckrodt Inc.Inventors: Jian Bao, Catherine E. Thomasson, Esa T. Jarvi
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Publication number: 20110207763Abstract: 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: May 9, 2011Publication date: August 25, 2011Applicant: RENSSELAER POLYTECHNIC INSTITUTEInventor: Mark P. Wentland
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Publication number: 20110190331Abstract: The present invention provides a compound of formula I: wherein R1, R2, R2? and X? are as defined and described herein, methods of manufacture thereof and compositions thereof, useful for example as peripheral mu opioid receptor antagonists in treatment of side effects of opioid administration.Type: ApplicationFiled: March 28, 2008Publication date: August 4, 2011Inventors: Alfred A. Avey, Appavu Chandrasekaren, Harold D. Doshan, Julio Perez, Yakov Rotshteyn
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Patent number: 7985858Abstract: The present invention is directed to the conversion of a 6-keto morphinan to a 6-alpha-hydroxy morphinan in the presence of a ruthenium, rhodium, or iridium asymmetric catalyst and a hydrogen source.Type: GrantFiled: May 2, 2008Date of Patent: July 26, 2011Assignee: Mallinckrodt Inc.Inventors: Christopher W. Grote, Peter X. Wang, Tao Jiang, Gary L. Cantrell, Frank W. Moser, Catherine E. Thomasson
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Publication number: 20110177133Abstract: The invention pertains to the use of opioid antagonists for the treatment of urinary retention.Type: ApplicationFiled: July 7, 2009Publication date: July 21, 2011Inventors: Michael Hopp, Petra Leyendecker
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Publication number: 20110136845Abstract: 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: ApplicationFiled: December 22, 2010Publication date: June 9, 2011Applicant: Mallinckrodt Inc.Inventors: Bobby N. Trawick, David W. Berberich, Christopher W. Grote
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Patent number: 7935820Abstract: The present invention provides a method for the N-demethylation of an N-methylated heterocycle, particularly a morphine or tropane alkaloid or derivative thereof. The method comprises reacting the heterocycle with a metal catalyst and a solvent in the presence of an oxidizing agent.Type: GrantFiled: June 29, 2007Date of Patent: May 3, 2011Assignee: Brock UniversityInventors: Robert James Carroll, Hannes Leisch, Tomas Hudlicky
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Patent number: 7910599Abstract: A method for treating eating disorders by repeatedly administering naloxone in a dosage sufficient to block the effects of opiate agonists to a subject suffering from an eating disorder caused by one or more related problem responses; while the amount of naloxone in the subject's body is sufficient to block opiate effects, having the subject make one of the problem responses from which the subject suffers in the presence of stimuli similar to those to which it had been learned, after the amount of naloxone is no longer sufficient to block opiate effects, having the subject make healthy eating responses to food items that do not trigger the problem responses; and continuing the steps of administration of naloxone and having one after another of the problem responses made, followed by having a naloxone-free period in which healthy eating occurs, until the problem responses are extinguished.Type: GrantFiled: January 10, 2005Date of Patent: March 22, 2011Inventor: John David Sinclair
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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: 20110053971Abstract: The present invention relates to prodrugs of nalmefene of formula (I), pharmaceutical compositions comprising these compounds, chemical processes for preparing these compounds and their use in the treatment of substance abuse disorders such as alcohol abuse and alcohol dependence and impulse control disorders such as pathological gambling and addiction to shopping.Type: ApplicationFiled: April 23, 2009Publication date: March 3, 2011Applicant: JANSSEN PHARMACEUTICA NVInventors: Michel Joseph Maurice André Guillaume, Tim Gaekens
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Publication number: 20110054175Abstract: Described herein are fluorinated organic compounds and methods of making fluorinated organic compounds, for example, using palladium complexes. Also described herein are compositions and kits containing compounds and palladium complexes described herein.Type: ApplicationFiled: February 2, 2009Publication date: March 3, 2011Inventors: Tobias Ritter, Takeru Furuya, Hanns M. Kaiser
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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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Patent number: 7872013Abstract: The present disclosure is directed to modulators of opiate- and/or NMDA receptors and pharmaceutically acceptable salts and prodrugs thereof, the chemical synthesis thereof, and the use of such compounds for the treatment and/or management of pain, anxiety, neurodegeneration, drug dependence, coughing, muscular tension, and/or glaucoma and any other condition in which it is beneficial to modulate an opiate- and/or NMDA receptor.Type: GrantFiled: August 16, 2007Date of Patent: January 18, 2011Assignee: Auspex Pharmaceuticals, Inc.Inventors: Thomas G. Gant, Sepehr Sarshar
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Patent number: 7863427Abstract: Methods, compositions and kits are disclosed directed at haptens, immunogens and immnoassays for buprenorphine (BUP) and nor buprenorphine (norBUP). The method comprises providing in combination in a medium (i) a sample suspected of containing buprenorphine (BUP) or norbuprenorphine (norBUP) and (ii) an antibody raised against an immunogen of buprenorphine (BUP) or norbuprenorphine (norBUP). The medium is examined for the presence of a complex comprising a labeled hapten of buprenorphine (BUP) or norbuprenorphine (norBUP) where the presence of such as complex indicates the presence of the compound in the sample.Type: GrantFiled: April 12, 2007Date of Patent: January 4, 2011Assignee: Siemens Healthcare Diagnostics Inc.Inventors: Yi-Feng Zheng, Pratap Singh, Dorota Bolle, Hshiou-Ting Liu
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Publication number: 20100305147Abstract: The invention provides small molecule drugs that are chemically modified by covalent attachment of a water-soluble oligomer obtained from a monodisperse or bimodal water-soluble oligomer composition. A conjugate of the invention, when administered by any of a number of administration routes, exhibits a reduced biological membrane crossing rate as compared to the biological membrane crossing rate of the small molecule drug not attached to the water-soluble oligomer.Type: ApplicationFiled: June 24, 2010Publication date: December 2, 2010Inventors: Michael D. Bentley, Tracey X. Viegas, Richard R. Goodin, Lin Cheng, Xuan Zhao
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Publication number: 20100256176Abstract: The present invention relates to a method for the preparation of morphine compounds comprising a low content of ?,?-unsaturated compounds, which comprises the steps of: (i) bringing the crude morphine compound into contact with a base, at a pH of greater than 13, under conditions which make possible the Michael addition reaction on the ?,?-unsaturated compound(s) present; (ii) separating the morphine compound from the reaction mixture; and (iii) if appropriate, separating the addition product formed from the morphine compound. It also relates to a composition comprising at least 99% by dry weight of morphine compound or of a pharmaceutically acceptable salt thereof, and an ?,?-unsaturated compound in a content of less than 100 ppm.Type: ApplicationFiled: May 5, 2010Publication date: October 7, 2010Applicant: SANOFI-AVENTISInventor: Alain DLUBALA
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Patent number: 7803942Abstract: The present invention is directed to provide 17-cyclopropylmethyl-3,14?-dihydroxy-4,5?-epoxy-6?-[N-methyl-trans-3-(3-furyl)acrylamido]morphinan hydrochloride consistent in quality after production and having high purity. A crystal of 17-cyclopropylmethyl-3,14?-dihydroxy-4,5?-epoxy-6?-[N-methyl-trans-3-(3-furyl)acrylamido]morphinan hydrochloride including a A-form, B-form or C-form crystal thereof, and a process for producing the same are provided.Type: GrantFiled: April 6, 2006Date of Patent: September 28, 2010Assignee: Toray Industries, Inc.Inventors: Hisanori Wakita, Masahiro Akimoto, Takahiro Takeda
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Publication number: 20100190728Abstract: Disclosed are analgesic-related compositions and methods of using the compositions for modulation of analgesic receptor activity. The compositions and methods are useful for reducing pain, as well as for therapeutic intervention of addictions or other diseases or disorders amenable to treatment or prophylaxis by modulation of analgesic receptor signaling.Type: ApplicationFiled: May 31, 2005Publication date: July 29, 2010Applicant: Human Biomolecular Research InstituteInventors: John R. Cashman, James M. MacDougall
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Publication number: 20100160299Abstract: The present invention relates to novel therapeutic and diagnostic dendrimers. In particular, the present invention is directed to dendrimer-linker conjugates, methods of synthesizing the same, compositions comprising the conjugates, as well as systems and methods utilizing the conjugates (e.g., in diagnostic and/or therapeutic settings (e.g., for the delivery of therapeutics, imaging, and/or targeting agents (e.g., in disease (e.g., cancer) diagnosis and/or therapy, pain therapy, etc.)). Accordingly, dendrimer-linker conjugates of the present invention may further comprise one or more components for targeting, imaging, sensing, and/or providing a therapeutic or diagnostic material and/or monitoring response to therapy.Type: ApplicationFiled: September 30, 2009Publication date: June 24, 2010Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGANInventors: James R. Baker, JR., Xue-min Cheng, Abraham F.L. Van Der Spek, Baohua Mark Huang, Thommey P. Thomas
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Publication number: 20100113497Abstract: In one aspect, the present invention provides a composition of a covalent conjugate of a GABA analog with a drug. In another aspect, the present invention provides methods for treating pain and neurological disorders using the conjugates of GABA analogs.Type: ApplicationFiled: October 8, 2009Publication date: May 6, 2010Applicant: Kyphia Pharmaceuticals, Inc.Inventor: Feng Xu
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Publication number: 20100081820Abstract: The invention provides processes for the production of opiate alkaloids. In particular, the present invention provides processes for the formation of buprenorphine and derivatives of buprenorphine that minimizes the formation of impurities.Type: ApplicationFiled: September 29, 2009Publication date: April 1, 2010Applicant: Mallinckrodt Inc.Inventors: Esa T. Jarvi, James R. Meyer
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Patent number: 7671204Abstract: The present invention provides a synthetic process for the N-demethylation of N-methyl morphinans. In particular, the invention provides improved synthetic methods for the preparation of N-demethylated morphinan compounds that may be employed as starting materials, for example, commonly available N-methyl opiates such as oripavine and thebaine, and C(3)-protected hydroxy derivatives of oripavine.Type: GrantFiled: December 17, 2008Date of Patent: March 2, 2010Assignee: Mallinckrodt Inc.Inventors: Peter X. Wang, Tao Jiang, Gary L. Cantrell, David W. Berberich
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Publication number: 20100048602Abstract: 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: ApplicationFiled: September 11, 2009Publication date: February 25, 2010Applicant: Nektar TherapeuticsInventors: Jennifer Riggs-Sauthier, Bo-Liang Deng, Timothy A. Riley
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Publication number: 20100041888Abstract: The present invention is directed to the conversion of a 6-keto morphinan to a 6-alpha-hydroxy morphinan in the presence of a ruthenium, rhodium, or iridium asymmetric catalyst and a hydrogen source.Type: ApplicationFiled: May 2, 2008Publication date: February 18, 2010Inventors: Christopher W. Grote, Peter X. Wang, Tao Jiang, Gary L. Cantrell, Frank W. Moser, Catherine E. Thomasson
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Publication number: 20090299069Abstract: The invention generally provides processes and intermediate compounds useful for the production of normorphinans and derivatives of normorphinans.Type: ApplicationFiled: May 21, 2009Publication date: December 3, 2009Applicant: Mallinckrodt Inc.Inventors: Peter X. Wang, Frank W. Moser, Gary L. Cantrell, Tao Jiang, Robert E. Halvachs, Christopher W. Grote
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Publication number: 20090292124Abstract: A therapeutic and/or prophylactic agent for nausea and/or vomiting is provided. A therapeutic and/or prophylactic agent for nausea and/or vomiting, comprising a compound of the Formula (I) or a pharmaceutically acceptable salt or solvate thereof: R1 and R2 are each independently hydrogen or lower alkyl; R3 is hydrogen or lower alkoxycarbonyl; and R4 is hydrogen or lower alkyl; with the proviso that all of R1 to R3 are not simultaneously hydrogen; and R1 and R4 are not simultaneously hydrogen).Type: ApplicationFiled: October 10, 2006Publication date: November 26, 2009Applicant: TORAY INDUSTRIES, INC. a corporation of JapanInventors: Tsutomu Suzuki, Yasunobu Ishihara
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Publication number: 20090209569Abstract: 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: ApplicationFiled: February 13, 2009Publication date: August 20, 2009Applicant: Alkermes, Inc.Inventors: Derrick Arnelle, Daniel Deaver, Reginald L. Dean, III, Mark Todtenkopf
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Publication number: 20090203723Abstract: A novel compound which is useful as an agent for treating and/or preventing emesis, vomiting and/or constipation. A compound represented by the formula (I): wherein R1 and R2 are each independently hydrogen, optionally substituted lower alkyl, optionally substituted lower alkenyl, optionally substituted cycloalkyl, optionally substituted aryl etc., R3 is hydrogen, hydroxy, optionally substituted lower alkyl, optionally substituted lower alkenyl, optionally substituted lower alkynyl, optionally substituted lower alkoxy etc., R4 is hydrogen or lower alkyl, R5 is hydrogen, lower alkyl, cycloalkyl lower alkyl or lower alkenyl, or a pharmaceutically acceptably salt, or a solvate thereof is provided.Type: ApplicationFiled: May 25, 2006Publication date: August 13, 2009Inventors: Masanao Inagaki, Shin-ichiro Hara, Nobuhiro Haga, Yoshinori Tamura, Yoshihisa Goto, Tsuyoshi Hasegawa
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Patent number: 7538118Abstract: This invention relates to compounds of the formula (I).Type: GrantFiled: December 16, 2002Date of Patent: May 26, 2009Assignee: Alcasynn Pharmaceuticals GmbHInventors: Johannes Schütz, Helmut Schmidhammer
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Patent number: 7534888Abstract: Oxycodone.HCl polymorph forms are disclosed which are useful as analgesic agents either in combination with or as replacements for oxycodone.Type: GrantFiled: August 15, 2003Date of Patent: May 19, 2009Assignee: Noramco, Inc.Inventors: Abram Calderon, Douglas Phillip Cox, Patrick Thomas Cyr, Aeri Park
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Publication number: 20090111843Abstract: A therapeutic or prophylactic agent for functional bowel disorders comprising as an effective ingredient a morphinan derivative having a nitrogen-containing cyclic group or a pharmaceutically acceptable acid addition salt thereof is disclosed. The therapeutic or prophylactic agent for functional bowel disorders comprises as an effective ingredient a morphinan derivative or a pharmaceutically acceptable acid addition salt thereof, having a specific structure, such as N-(17-cyclopropylmethyl-4,5?-epoxy-3,14-dihydroxy-morphinan-6?-yl)-3,4,5,6-tetrahydrophthalimide tartaric acid salt (Compound 10).Type: ApplicationFiled: November 7, 2006Publication date: April 30, 2009Applicant: TORAY INDUSTRIES, INC.Inventors: Koji Kawai, Morihiro Fujimura, Sayoko Kanie, Yohei Noro
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Patent number: 7501434Abstract: The present invention relates to compounds of formula I, synthesis thereof, and methods of using the same.Type: GrantFiled: August 3, 2007Date of Patent: March 10, 2009Assignee: WyethInventors: Syed M. Shah, Kadum A. Ali, FangMing Kong, Tianmin Zhu, Charles T. Gombar
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Patent number: 7501433Abstract: The present invention relates to opioid and opioid-like compounds, and pharmaceutical formulations thereof, and use thereof for prevention and treatment of disorders such as septic shock and organ damage.Type: GrantFiled: April 12, 2005Date of Patent: March 10, 2009Assignee: Jenken Biosciences, Inc.Inventors: Edwin S. C. Wu, Mao-Hsiung Yen, Chin-Tsai Fan
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Publication number: 20090030025Abstract: Optionally substituted chromenoisoquinolines and analogs and derivatives thereof are described herein. In addition, syntheses of these compounds are described herein. In addition, uses of these compounds as dopamine receptor binding compounds are described herein.Type: ApplicationFiled: August 20, 2008Publication date: January 29, 2009Applicant: PURDUE RESEARCH FOUNDATIONInventors: David Nichols, Val J. Watts
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Publication number: 20090018154Abstract: An opioid derivative of oxymorphol, called 8-hydroxy-6-?-oxymorphol, has been discovered. This opioid is believed to bind at least to mu-opioid receptors and produce an analgesic or anti-tussive effect. Pharmaceutically acceptable salts of 8-hydroxy-6-?-oxymorphol, and pharmaceutical compositions comprising 8-hydroxy-6-?-oxymorphol or pharmaceutically acceptable salts thereof and pharmaceutically acceptable carrier, are also provided.Type: ApplicationFiled: May 13, 2008Publication date: January 15, 2009Applicant: Endo Pharmaceuticals, Inc., a corporation of DelawareInventors: Huai-Hung Danny Kao, Yadi Zeng, Debashis Das
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Publication number: 20090005565Abstract: The present invention provides a method for the N-demethylation and/or N-acylation of an N-methylated heterocycle such as morphine alkaloids or tropane alkaloids. The method comprises reacting the heterocycle with an acylating agent in the presence of a metal catalyst.Type: ApplicationFiled: June 29, 2007Publication date: January 1, 2009Inventors: Robert James Carroll, Hannes Leisch, Tomas Hudlicky, D. Phillip Cox
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Patent number: 7435817Abstract: The present invention relates to process for the preparation of a 14-hydroxynormorphinone derivative of formula IV comprising reacting the compound of formula III, with a cobalt (II) oxidant in the presence of a mild base and air or oxygen as the cooxidant; wherein R1 is (1C-7C)alkyl optionally substituted with one or more chlorines, butenyl, vinyl, benzyl, phenyl or naphthyl; and R2 is benzyl or benzyl substituted with one or more (1C-6C)alkoxy group or benzyl substituted with one or more halogen. The process is very suitable in the production of noroxymorphone.Type: GrantFiled: August 15, 2002Date of Patent: October 14, 2008Assignee: N.V. OrganonInventors: Joannes Theodorus Maria Linders, Pieter Vrijhof
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Publication number: 20080196123Abstract: The invention relates to a method for altering alkaloid biosynthesis in a plant, comprising: i) introducing into cells of a plant, an expressible exogenous nucleic acid comprising or consisting of an (S)-N-methylcoclaurine 3?-hydroxylase gene (cyp80b) or a derivative thereof, and ii) optionally propagating the plant, wherein expression of the exogenous nucleic acid in the plant or in its progeny results in altered levels of alkaloid biosynthesis.Type: ApplicationFiled: August 11, 2005Publication date: August 14, 2008Inventors: Toni M. Kutchan, Susanne Frick, Katja Kempe
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Patent number: 7405301Abstract: This invention relates to a method for N-demethylating an N-methyl morphinane comprising the steps of: (i) treating said N-methyl morphinane with an oxidizing agent to form the N-oxide morphinane; and (ii) treating said N-oxide morphinane with a reducing agent. This invention also relates to a method for oxidizing a ?7-morphinane compound to a ?6, ?8-morphinane compound, comprising the steps of treating said ?7-morphinane with ?-MnO2 for a time and under conditions sufficient to oxidize said ?7-morphinane, and treating the ?-MnO2 with glycol or a derivative thereof, and/or an inorganic salt.Type: GrantFiled: August 24, 2001Date of Patent: July 29, 2008Assignee: GlaxoWellcome Australia Ltd.Inventors: Peter Scammells, Nicholas Gathergood, Justin Ripper
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Patent number: 7399859Abstract: The present invention generally relates to catalysts of formula (III) [M(P(Ra)(Rb)N(Rc)(Rd))2Xn]mYp that selectively convert morphine/codeine to hydromorphone/hydrocodone, and methods of use thereof.Type: GrantFiled: February 6, 2007Date of Patent: July 15, 2008Assignee: Cody Laboratories Inc.Inventor: Vladimir Kouznetsov
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Patent number: 7399858Abstract: A method for the catalytic production of hydrocodone derivatives and hydromorphone derivatives, respectively, utilizing a transition metal catalyst of the formula [M(PR4R5R6)nXm]p; wherein M is a Group VIII transition metal; R4, R5 and R6 are selected from the group consisting of alkyl, aryl, alkoxyl, phenoxy and combinations thereof; X is a halide or an anion; n is 1, 2, 3 or 4; m is 1 or 2; and p is at least 1.Type: GrantFiled: March 7, 2006Date of Patent: July 15, 2008Assignee: Mallinckrodt Inc.Inventors: Peter X. Wang, Frank W. Moser, Gary L. Cantrell, Daniel P. Magparangalan, Jian Bao
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Publication number: 20080161570Abstract: Methods for the synthesis of 4,5-epoxy-morphinaniums using dimethyl formamide and resolution of the diastereomeric products by means of HPLC.Type: ApplicationFiled: November 19, 2007Publication date: July 3, 2008Applicant: Progenerics Pharmaceuticals, Inc.Inventors: Julio Perez, Amy Qi Han, Alfred A. Avey
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Publication number: 20080146804Abstract: Disclosed are methods for making aldehydes and ketones comprising allowing the corresponding primary or secondary alcohol to react in the presence of trichoroisocyanuric acid, a compound of formula R1SR2 and a base. In one embodiment, the alcohol is a compound of formula (I): wherein R3 is a protecting group. Also disclosed are methods for making 3-O-protected morphine dienol carboxylates comprising allowing a compound of formula (I) to oxidize in the presence of a chlorine-containing compound and a compound of formula R1SR2; and allowing the product of the oxidation step to react with an acylating agent.Type: ApplicationFiled: February 4, 2005Publication date: June 19, 2008Applicant: EURO-CELTIQUE S.A.Inventor: Andreas Stumpf
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Publication number: 20080076789Abstract: Described herein are opioid prodrugs, methods of making opioid prodrugs, formulations comprising opioid prodrugs, and methods of using opioid prodrugs. One embodiment described herein relates to the transdermal administration of a buprenorphine prodrug in an abuse-resistant formulation for treating and preventing diseases and/or disorders.Type: ApplicationFiled: September 24, 2007Publication date: March 27, 2008Applicant: AllTranz Inc.Inventors: Audra Lynn Stinchcomb, Miroslaw Jerzy Golinski, Dana Carmel Hammell, Jeffrey Lynn Howard
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Patent number: 7323565Abstract: A method for the catalytic conversion of codeine, morphine or analogs thereof into hydrocodone, hydromorphone or analogs thereof utilizing a transition metal complex of a tertiary phosphine halide as catalyst.Type: GrantFiled: November 5, 2003Date of Patent: January 29, 2008Assignee: Mallinckrodt Inc.Inventors: Peter Xianqi Wang, Carl Ray White
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Patent number: 7320984Abstract: The invention provides a morphinan derivative of the Formula (I): wherein R1 is methyl, cyclopropylmethyl or the like; R2 and R3 are hydroxy, methoxy, acetoxy or the like; both Y and Z are valence bonds, —C(?O)— or the like; X is C2-C5 carbon chain (one of the carbon atoms may be substituted by oxygen, sulfur or nitrogen) constituting a part of the ring structure, or the like; (R4)k is substituted or non-substituted benzene fused ring, carbonyl group or the like; R9 is hydrogen or the like; R10 and R11 are bound to represent —O—, or the like, and R6 is hydrogen or the like or a pharmaceutically acceptable acid addition salt thereof. The invention also provides a therapeutic or prophylactic agent for urinary frequency or urinary incontinence, comprising as an effective ingredient the morphinan derivative or the pharmaceutically acceptable acid addition salt thereof; a method for therapy or prophylaxis of the diseases.Type: GrantFiled: October 8, 2003Date of Patent: January 22, 2008Assignee: Toray Industries, Inc.Inventors: Naoki Izumimoto, Koji Kawai, Kuniaki Kawamura, Morihiro Fujimura, Toshikazu Komagata
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Patent number: 7321038Abstract: A method for the catalytic conversion of codeine, morphine or analogs thereof into hydrocodone, hydromorphone or analogs thereof utilizing a transition metal catalyst of the formula [M(PR3R4R5)nXm]p; wherein R1 is H, alkyl, aryl or acyl; M is a Group VIII transition metal; R3, R4 and R5 are selected from the group consisting of alkyl, aryl, alkoxyl, phenoxyl and combinations thereof; X is a halide or an anion; n is 1, 2, 3 or 4; m is 1 or 2; and p is at least 1.Type: GrantFiled: October 25, 2004Date of Patent: January 22, 2008Assignee: Mallinckrodt Inc.Inventors: Peter Xianqi Wang, Carl Ray White
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Patent number: 7285665Abstract: A process for the preparation of a quaternary derivative of the morphinan alkaloid, the process comprising contacting a tertiary N-substituted morphinan alkaloid with an alkyl halide in an anhydrous solvent system, wherein the solvent system comprises an aprotic dipolar solvent with the aprotic dipolar solvent constituting at least 25 wt. % of the solvent system.Type: GrantFiled: November 5, 2003Date of Patent: October 23, 2007Assignee: Mallinckrodt Inc.Inventors: Gary L. Cantrell, Robert E. Halvachs
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Patent number: 7230005Abstract: The abuse potential of a bioavailable drug such as an opiate analgesic agent is reduced and its duration of action is extended by converting it to a poorly absorbed ester prodrug or other prodrug derivative prior to formulation. Unlike many existing sustained release formulations of active pharmaceutical agents wherein an active pharmaceutical agent can be released by chewing, crushing, or otherwise breaking tablets or capsule beads containing the active pharmaceutical agent, such mechanical processing of tablets or capsule beads containing a prodrug of this invention neither releases the active drug nor compromises the controlled conversion of prodrug to drug. Moreover, tablets and capsule beads containing prodrugs of this invention or other drugs can be formulated with a sufficient amount of a thickening agent such as hydroxypropylmethylcellulose or carboxymethylcellulose to impede inappropriate intravenous and nasal administration of formulations that are not indicated for these modes of administration.Type: GrantFiled: March 15, 2004Date of Patent: June 12, 2007Assignee: Controlled Chemicals, Inc.Inventors: Jules A. Shafer, Vladislav V. Telyatnikov, Zhiwei Guo
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Patent number: 7220842Abstract: Methods, compositions and kits are disclosed directed at haptens, immunogens and immunoassays for buprenorphine (BUP) and nor buprenorphine (norBUP). The method comprises providing in combination in a medium (i) a sample suspected of containing buprenorphine (BUP) or norbuprenorphine (norBUP) and (ii) an antibody raised against an immunogen of buprenorphine (BUP) or norbuprenorphine (norBUP). The medium is examined for the presence of a complex comprising a labeled hapten of buprenorphine (BUP) or norbuprenorphine (norBUP) where the presence of such as complex indicates the presence of the compound in the sample.Type: GrantFiled: April 5, 2004Date of Patent: May 22, 2007Assignee: Dade Behring Inc.Inventors: Yi-Feng Zheng, Pratap Singh, Dorota Bolle, Hshiou-Ting Liu