One Of The Five Cyclos Is Five-membered And Includes Ring Chalcogen (e.g., Codeine, Morphine, Etc.) Patents (Class 514/282)
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Publication number: 20150080424Abstract: A sustained-release oral dosage form of naltrexone or a pharmaceutically acceptable salt thereof is provided. The oral dosage form may be administered with another compound. Administration of the oral dosage form may reduce a side effect, which may be a side effect at least partially attributable to a weight-loss treatment. The oral dosage form may be administered to treat a weight-loss condition.Type: ApplicationFiled: November 26, 2014Publication date: March 19, 2015Inventors: Anthony A. McKinney, Gary D. Tollefson, Richard Soltero, Thea Elise Dunzo
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Publication number: 20150080422Abstract: Methods and compositions are provided for preventing or reversing loss of the therapeutic effect of a drug, where the loss is associated with the repeated administration of the drug to a patient. The method includes administering to the patient a dopamine receptor agonist or partial agonist or a drug that increases the extracellular level of dopamine by enhancing release of dopamine, decreasing the removal of dopamine from the extracellular space, enhancing the synthesis of dopamine within the brain, or decreasing metabolic degradation of dopamine; and also administering to the patient an opioid receptor antagonist in an ultra-low dose amount, wherein the ultra-low dose amount is effective to prevent or reverse loss of therapeutic effects associated with the repeated administration of the drug to the patient. The methods are useful for various treatments, including treating Parkinson's Disease, Restless Leg Syndrome, depression, schizophrenia, psychostimulant drug abuse, or attention deficit disorder.Type: ApplicationFiled: September 25, 2014Publication date: March 19, 2015Applicant: PharmoRx Therapeutics, Inc.Inventors: David M. Bear, Robert M. Kessler
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Publication number: 20150079150Abstract: A composition for controlled release of an opioid from a pharmaceutical composition, the method comprises controlling the release of at least one opioid into an aqueous medium by erosion of at least one surface of a pharmaceutical composition comprising I) a matrix composition comprising a) polymer or a mixture of polymers, b) an opioid and, optionally, c) one or more pharmaceutically acceptable excipients, and (i) a coating. The matrix composition has a conus-like shape so the surface area exposed to the aqueous medium increases at least during initial erosion of the matrix composition, and the dissolution of the opioid-when tested in a Dissolution Test as described herein with or without application of sinkers-results in a zero order release of at least 80% of the opioid contained in the composition. Such compositions are especially suitable for controlled release of an opioid to obtain a delayed pead concentration and a prolonged therapeutically effective plasma concentration upon oral administration.Type: ApplicationFiled: September 25, 2014Publication date: March 19, 2015Applicant: Egalet Ltd.Inventors: Gina Fischer, Daniel Bar-Shalom, Lillian Slot, Christine Andersen
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Publication number: 20150080384Abstract: Effective methods and compositions to deter abuse of pharmaceutical products (e.g., orally administered pharmaceutical products) including but not limited to immediate release, sustained or extended release and delayed release formulations for drugs subject to abuse comprising at least 10% by weight hydroxypropylcellulose; polyethylene oxide; and a disintegrant selected from the group consisting of crospovidone, sodium starch glycolate and croscarmellose sodium; wherein the ratio of hydroxypropylcellulose to polyethylene oxide on a weight basis is between about 10:1 and 1:10.Type: ApplicationFiled: November 24, 2014Publication date: March 19, 2015Applicant: ACURA PHARMACEUTICALS, INC.Inventors: Ronald L. LEECH, Rachelle L. HALL YUNG, Albert W. BRZECZKO
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Patent number: 8980291Abstract: A solid oral controlled-release oral dosage form of hydrocodone is disclosed. The dosage form comprising an analgesically effective amount of hydrocodone or a pharmaceutically acceptable salt thereof, and a sufficient amount of a controlled release material to render the dosage form suitable for twice-a-day administration to a human patient, the dosage form providing a C12/Cmax ratio of 0.55 to 0.85, said dosage form providing a therapeutic effect for at least about 12 hours.Type: GrantFiled: December 30, 2010Date of Patent: March 17, 2015Assignee: Purdue Pharma L.P.Inventors: Benjamin Oshlack, Hua-Pin Huang, John Masselink, Alfred P. Tonelli
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Patent number: 8980305Abstract: There is provided pharmaceutical compositions for the treatment of pain comprising a pharmacologically-effective amount of an opioid analgesic, or a pharmaceutically-acceptable salt thereof, presented in particulate form upon the surfaces of carrier particles comprising a pharmacologically-effective amount of an opioid antagonist, or a pharmaceutically-acceptable salt thereof, which carrier particles are larger in size than the particles of the opioid analgesic. The compositions are also useful in prevention of opioid abuse by addicts.Type: GrantFiled: March 13, 2013Date of Patent: March 17, 2015Assignee: Orexo ABInventor: Anders Pettersson
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Patent number: 8980908Abstract: Selective, non-peptide antagonists of the mu opioid receptor (MOR) and methods of their use are provided. The antagonists may be used, for example, to identify MOR agonists in competitive binding assays, and to treat conditions related to addiction in which MOR is involved, e.g. heroin, prescription drug and alcohol addiction, as well as in the treatment of opioid induced constipation (OIC).Type: GrantFiled: May 27, 2014Date of Patent: March 17, 2015Assignee: Virginia Commonwealth UniversityInventors: Yan Zhang, Dana E. Selley, William Dewey
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Patent number: 8980907Abstract: 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: GrantFiled: December 16, 2013Date of Patent: March 17, 2015Assignee: 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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Patent number: 8980319Abstract: Methods for producing stabilized solid dosage form pharmaceutical compositions are provided. In particular, methods for preparing protected granules containing morphinans, and solid dosage form pharmaceutical compositions produced using the morphinan-protected granules are provided.Type: GrantFiled: November 27, 2013Date of Patent: March 17, 2015Assignee: Mallinckrodt LLCInventors: Jae Han Park, Tiffani Eisenhauer, Anish Dhanarajan, Vishal Gupta, Stephen Overholt
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Patent number: 8980880Abstract: A pharmaceutical composition comprising a drug substance consisting essentially of a pharmaceutically acceptable organic acid addition salt of an amine containing pharmaceutically active compound wherein the amine containing pharmaceutical active compound is selected from the group consisting of racemic or single isomer ritalinic acid or phenethylamine derivatives and the drug substance has a physical form selected from amorphous and polymorphic.Type: GrantFiled: April 10, 2012Date of Patent: March 17, 2015Assignee: Pisgah Laboratories, Inc.Inventors: Clifford Riley King, Stephen G. D'Ambrosio, David W. Bristol
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Publication number: 20150072971Abstract: The present application relates methods for treating a depressive symptom comprising administering an effective amount of a ? opioid receptor agonist or a pharmaceutically acceptable salt thereof to a subject in need thereof. Non-limiting examples of such agonist include the compounds of Formulas I, II, III, and IV, as well as the compounds of Table A.Type: ApplicationFiled: May 23, 2014Publication date: March 12, 2015Applicant: Alkermes Pharma Ireland LimitedInventors: Laura Cook Blumberg, Dan Deaver, David Eyerman, Thomas Wynn
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Publication number: 20150071995Abstract: An abuse resistant oral pharmaceutical composition, comprising: a barrier layer, comprising a first polymer; a diffusion layer, comprising a second polymer, substantially covering the barrier layer, wherein the diffusion layer is bonded to the barrier layer and comprises a drug that is substantially homogeneously distributed within the second polymer and diffuses from the diffusion layer within the gastrointestinal (GI) tract; and optionally an expansion layer comprising an expandable polymer, wherein the expansion layer is substantially covered by the barrier layer. Methods of making the same and methods of using the same are also provided.Type: ApplicationFiled: November 7, 2014Publication date: March 12, 2015Inventors: Manish S. Shah, Ray J. DiFalco
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Publication number: 20150071971Abstract: The invention provides sublingual formulations containing buprenorphine, a pharmaceutically acceptable salt thereof, or a derivative thereof. The invention further provides sublingual formulations containing buprenorphine and naloxone, pharmaceutically acceptable salts thereof or derivatives thereof. The invention further provides a method of treating pain or opioid dependence by administering sublingual formulations containing buprenorphine, a pharmaceutically acceptable salt thereof, or a derivative thereof to a patient in need thereof.Type: ApplicationFiled: August 26, 2014Publication date: March 12, 2015Inventors: Kiran P. Amancha, Chandeshwari S. Chilampalli, Venkat R. Goskonda
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Publication number: 20150072006Abstract: The invention relates to drug preparations with controlled active ingredient released in the form of microtablets which contain, as active ingredient, flupirtin or one of its physiologically compatible salts, and to processes for their production.Type: ApplicationFiled: March 1, 2013Publication date: March 12, 2015Inventors: Katrin Moschner, Torsten Hoffmann, Mario Weingart, Annegret Hildebrand-Cyrener
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Publication number: 20150071998Abstract: An abuse resistant oral pharmaceutical composition, comprising: a barrier layer, comprising a first polymer; a diffusion layer, comprising a second polymer, substantially covering the barrier layer, wherein the diffusion layer is bonded to the barrier layer and comprises a drug that is substantially homogeneously distributed within the second polymer and diffuses from the diffusion layer within the gastrointestinal (GI) tract; and optionally an expansion layer comprising an expandable polymer, wherein the expansion layer is substantially covered by the barrier layer. Methods of making the same and methods of using the same are also provided.Type: ApplicationFiled: November 7, 2014Publication date: March 12, 2015Inventors: Manish S. Shah, Ray J. DiFalco
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Patent number: 8975257Abstract: 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: GrantFiled: February 24, 2014Date of Patent: March 10, 2015Assignee: Purdue Pharma L.P.Inventor: Andreas Stumpf
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Patent number: 8975273Abstract: A solid oral controlled-release oral dosage form of hydrocodone is disclosed. The dosage form comprising an analgesically effective amount of hydrocodone or a pharmaceutically acceptable salt thereof, and a sufficient amount of a controlled release material to render the dosage form suitable for twice-a-day administration to a human patient, the dosage form providing a C12/Cmax ratio of 0.55 to 0.85, said dosage form providing a therapeutic effect for at least about 12 hours.Type: GrantFiled: September 11, 2014Date of Patent: March 10, 2015Assignee: Purdue Pharma L.P.Inventors: Benjamin Oshlack, Hua-Pin Huang, John Masselink, Alfred P. Tonelli
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Patent number: 8975271Abstract: A solid oral controlled-release oral dosage form of hydrocodone is disclosed. The dosage form comprising an analgesically effective amount of hydrocodone or a pharmaceutically acceptable salt thereof, and a sufficient amount of a controlled release material to render the dosage form suitable for twice-a-day administration to a human patient, the dosage form providing a C12/Cmax ratio of 0.55 to 0.85, said dosage form providing a therapeutic effect for at least about 12 hours.Type: GrantFiled: December 3, 2013Date of Patent: March 10, 2015Assignee: Purdue Pharma L.P.Inventors: Benjamin Oshlack, Hua-Pin Huang, John Masselink, Alfred P. Tonelli
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Patent number: 8975270Abstract: The present invention is directed to a buprenorphine sustained release delivery system capable of delivering buprenorphine, a metabolite, or a prodrug thereof for a duration of about 14 days to about 3 months. The buprenorphine sustained release delivery system includes a flowable composition and a solid implant for the sustained release of buprenorphine, a metabolite, or a prodrug thereof. The implant is produced from the flowable composition. The buprenorphine sustained release delivery system provides in situ 1-month and 3-month release profiles characterized by an exceptionally high bioavailability and minimal risk of permanent tissue damage and typically no risk of muscle necrosis.Type: GrantFiled: March 15, 2013Date of Patent: March 10, 2015Assignee: RB Pharmaceuticals LimitedInventors: Richard L. Norton, Andrew Watkins, Mingxing Zhou
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Patent number: 8975272Abstract: This invention relates to the discovery of novel polymorphic forms of naltrexone, including solvates, hydrates, anhydrous and other crystalline forms and combinations thereof. These novel forms of naltrexone impart advantages in pharmaceutical formulations incorporating them, including sustained release, or long acting, formulations.Type: GrantFiled: April 10, 2014Date of Patent: March 10, 2015Assignee: Alkermes, Inc.Inventors: Harry G. Brittain, David A. Dickason, Joyce M. Hotz, Shawn L. Lyons, J. Michael Ramstack, Steven G. Wright
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Patent number: 8974821Abstract: Dosage forms and drug delivery devices suitable for administration of pharmaceutical compounds and compositions, including the oral drug administration of compounds.Type: GrantFiled: March 5, 2013Date of Patent: March 10, 2015Assignee: Durect CorporationInventors: Su Il Yum, Grant Schoenhard, Arthur J. Tipton, John W. Gibson, John C. Middleton, Roger Fu, Michael S. Zamloot
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Publication number: 20150064246Abstract: An abuse resistant oral pharmaceutical composition, comprising: a barrier layer, comprising a first polymer; a diffusion layer, comprising a second polymer, substantially covering the barrier layer, wherein the diffusion layer is bonded to the barrier layer and comprises a drug that is substantially homogeneously distributed within the second polymer and diffuses from the diffusion layer within the gastrointestinal (GI) tract; and optionally an expansion layer comprising an expandable polymer, wherein the expansion layer is substantially covered by the barrier layer. Methods of making the same and methods of using the same are also provided.Type: ApplicationFiled: November 7, 2014Publication date: March 5, 2015Inventors: Manish S. Shah, Ray J. DiFalco
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Publication number: 20150064245Abstract: An abuse resistant oral pharmaceutical composition, comprising: a barrier layer, comprising a first polymer; a diffusion layer, comprising a second polymer, substantially covering the barrier layer, wherein the diffusion layer is bonded to the barrier layer and comprises a drug that is substantially homogeneously distributed within the second polymer and diffuses from the diffusion layer within the gastrointestinal (GI) tract; and optionally an expansion layer comprising an expandable polymer, wherein the expansion layer is substantially covered by the barrier layer. Methods of making the same and methods of using the same are also provided.Type: ApplicationFiled: November 7, 2014Publication date: March 5, 2015Inventors: Manish S. Shah, Ray J. DiFalco
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Publication number: 20150065536Abstract: The presently described technology provides compositions comprising aryl carboxylic acids chemically conjugated to hydrocodone (morphinan-6-one, 4,5-alpha-epoxy-3-methoxy-17-methyl) to form novel prodrugs/compositions of hydrocodone, including benzoates and heteroaryl carboxylic acids, which have a decreased potential for abuse of hydrocodone. The present technology also provides methods of treating patients, pharmaceutical kits and methods of synthesizing conjugates of the present technology.Type: ApplicationFiled: November 6, 2014Publication date: March 5, 2015Inventors: Travis Mickle, Sven Guenther, Christal Mickle, Guochen Chi, Jaroslaw Kanski, Andrea K. Martin, Bindu Bera
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Publication number: 20150064247Abstract: An abuse resistant oral pharmaceutical composition, comprising: a barrier layer, comprising a first polymer; a diffusion layer, comprising a second polymer, substantially covering the barrier layer, wherein the diffusion layer is bonded to the barrier layer and comprises a drug that is substantially homogeneously distributed within the second polymer and diffuses from the diffusion layer within the gastrointestinal (GI) tract; and optionally an expansion layer comprising an expandable polymer, wherein the expansion layer is substantially covered by the barrier layer. Methods of making the same and methods of using the same are also provided.Type: ApplicationFiled: November 7, 2014Publication date: March 5, 2015Inventors: Manish S. Shah, Ray J. DiFalco
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Publication number: 20150064223Abstract: Provided herein are methods for treating certain conditions, including diabetes, obesity, and other metabolic diseases, disorders or conditions by administrating a composition comprising a biguanide or related heterocyclic compound, e.g., metformin. Also provided herein are biguanide or related heterocyclic compound compositions, and methods for the preparation thereof for use in the methods of the present invention. Also provided herein are compositions comprising metformin and salts thereof and methods of use.Type: ApplicationFiled: July 11, 2012Publication date: March 5, 2015Applicant: Elcelyx Therapeutics, Inc.Inventors: Alain D. Baron, Mark S. Fineman, Nigel R.A. Beeley
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Publication number: 20150064231Abstract: A control release and abuse-resistant opiate drug delivery oral wafer or edible oral film dosage to treat pain and substance abuse is provided. The drug delivery oral wafer or edible oral film dosage includes a controlled release layer containing enteric-release beads dispersed in a polymer matrix. The enteric-release beads are formed from a therapeutic amount of an opioid agonist and/or pharmaceutically acceptable salt thereof and a sub-therapeutic amount of opioid antagonist and/or pharmaceutically acceptable salt thereof coated or encapsulated in an enteric-release polymer. The controlled release polymer matrix dissolves or disintegrates following administration or consumption of the oral wafer or edible oral film, releasing the enteric-release beads to be swallowed, with subsequent absorption of the active ingredients within the patient's intestines.Type: ApplicationFiled: April 11, 2013Publication date: March 5, 2015Applicant: LTS Lohmann Therapie-Systeme AGInventor: Michael Li
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Publication number: 20150064248Abstract: An abuse resistant oral pharmaceutical composition, comprising: a barrier layer, comprising a first polymer; a diffusion layer, comprising a second polymer, substantially covering the barrier layer, wherein the diffusion layer is bonded to the barrier layer and comprises a drug that is substantially homogeneously distributed within the second polymer and diffuses from the diffusion layer within the gastrointestinal (GI) tract; and optionally an expansion layer comprising an expandable polymer, wherein the expansion layer is substantially covered by the barrier layer. Methods of making the same and methods of using the same are also provided.Type: ApplicationFiled: November 7, 2014Publication date: March 5, 2015Inventors: Manish S. Shah, Ray J. DiFalco
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Patent number: 8969370Abstract: The invention provides 3-carboxypropyl-aminotetralin compounds of formula (I): wherein R1, R2, R3, R4, R5, and R6 are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.Type: GrantFiled: March 4, 2014Date of Patent: March 3, 2015Assignee: Theravance Biopharma R&D IP, LLCInventors: Sean G. Trapp, Michael R. Leadbetter, Daniel D. Long, Pierre-Jean Colson, Miroslav Rapta, Ying Yu
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Patent number: 8969368Abstract: Crystalline, anhydrous hydrochloride salts of 4,5?-epoxy-3,14-dihydroxy-17-methylmorphinan-6-one (oxymorphone) are disclosed and three polymorphic forms of these salts are reported. The invention further relates to a method for the production of such salts, a pharmaceutical composition comprising an effective amount of such a salt and such a salt as a medicament and for the treatment and/or prevention of pain.Type: GrantFiled: November 27, 2013Date of Patent: March 3, 2015Assignee: Grünenthal GmbHInventors: Andreas Fischer, Dagmar Peters-Groth, Dagmar Lischke
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Patent number: 8969371Abstract: The present disclosure relates to compositions, kits, uses, systems and methods related to naltrexone plus bupropion for treating an overweight or obese subject at increased risk of adverse cardiovascular outcomes. Preferably, the subject has had type-two diabetes for a period of less than 6 years or is a current smoker, optionally that does not have type-two diabetes.Type: GrantFiled: July 2, 2014Date of Patent: March 3, 2015Assignee: Orexigen Therapeutics, Inc.Inventors: Preston Klassen, Kristin Taylor
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Patent number: 8969367Abstract: The invention provides crystalline solid forms of (S)-4-((2S,3S)-7-carbamoyl-1,1-diethyl-3-methoxy-1,2,3,4-tetrahydronaphthalen-2-ylamino)-2-cyclohexylmethyl-butyric acid. The invention also provides pharmaceutical compositions comprising such crystalline solid forms, methods of using such crystalline solid forms to treat diseases associated with mu opioid receptor activity, and processes useful for preparing such crystalline solid forms.Type: GrantFiled: June 17, 2013Date of Patent: March 3, 2015Assignee: Theravance Biopharma R&D IP, LLCInventors: Sean M. Dalziel, Miroslav Rapta
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Patent number: 8969369Abstract: Abuse-resistant, controlled release opioid tablets are a combination containing an opioid antagonist such as naloxone at a level above that needed to suppress the euphoric effect of the opioid, if the combination were crushed to break the controlled release properties causing the opioid and opioid antagonist to be released as a immediate release product as a single dose. The controlled release nature of the table prevents the accumulation of orally effective amounts of opioid antagonist when taken normally. The opioid antagonist is contained in a controlled-release matrix and released, over time, with the opioid.Type: GrantFiled: December 20, 2013Date of Patent: March 3, 2015Assignee: Purdue Pharma L.P.Inventors: Frank S. Caruso, Huai-Hung Kao
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Publication number: 20150057303Abstract: This invention relates to stereoselective synthesis of R-MNTX and intermediates thereof, pharmaceutical preparations comprising R-MNTX or intermediates thereof and methods for their use.Type: ApplicationFiled: March 18, 2014Publication date: February 26, 2015Applicant: PROGENICS PHARMACEUTICALS, INC.Inventors: Harold D. Doshan, Julio Perez
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Publication number: 20150057304Abstract: The present disclosure relates to an oral, immediate release, abuse deterrent pill containing at least one active pharmaceutical ingredient susceptible to abuse which is homogenously spread throughout a carrier matrix used to deter abuse. The pill is prepared using hot melt extrusion and a forming unit through a continuous process. The formed pill is abuse deterrent to parenteral administration due at least to particle size, viscosity, or purity limitations.Type: ApplicationFiled: August 12, 2014Publication date: February 26, 2015Applicant: Pharmaceutical Manufacturing Research Service, Inc.Inventors: Edwin R. Thompson, Eric R. Thompson, Nicholas R. Myslinski, Steven F. Kemeny
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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: 8962841Abstract: The present invention provides a method for the N-demethylation and N-functionalization of an N-methylated heterocycle such as a morphine alkaloid or tropane alkaloid. The method comprises reacting the heterocycle with an functionalization agent in the presence of a transition metal catalyst in air or in the presence of an oxidant.Type: GrantFiled: July 8, 2011Date of Patent: February 24, 2015Assignee: Brock UniversityInventors: Tomas Hudlicky, Robert James Carroll, Hannes Leisch, Ales Machara, Lukas Werner, Mary Ann Endoma-Arias
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Patent number: 8962647Abstract: Provided are a PEG-naloxone conjugate of general formula (II) and a pharmaceutical composition comprising the conjugate. In the conjugate, n is an integer in the range of 1-20. Also provided is a three-branched or four-branched conjugate of PEG and naloxone. Structural modification of naloxone with a hydrophilic polymer improves the pharmacokinetic properties of the drug, increase the water solubility of naloxone, improve the in vivo distribution of the drug, reduce the side effects of naloxone on central nervous system, and relieve bowel dysfunction and constipation caused by chronic administration of opioids. Also provided are a pharmaceutical composition comprising the conjugate of the invention and use of the conjugate.Type: GrantFiled: February 21, 2013Date of Patent: February 24, 2015Assignee: Jenkem Technology Co., Ltd. (Tianjin)Inventors: Zhixiong Guo, Zewang Feng, Lihua Xu, Xuan Zhao
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Publication number: 20150050339Abstract: The presently described technology provides phenylethanoic acid, phenylpropanoic acid, phenylpropenoic acid, a salt thereof, a derivative thereof or a combination thereof chemically conjugated to hydrocodone (morphinan-6-one, 4,5-alpha-epoxy-3-methoxy-17-methyl) to form novel prodrugs or compositions of hydrocodone which have a decreased potential for abuse of hydrocodone. The present technology also provides methods of treating patients, pharmaceutical kits and methods of synthesizing conjugates of the present technology.Type: ApplicationFiled: September 23, 2014Publication date: February 19, 2015Inventors: Travis Mickle, Sven Guenther, Christal Mickle
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Publication number: 20150051191Abstract: Alcoholism, and symptoms and negative effects thereof may be treated using ibudilast or a pharmaceutically acceptable salt thereof. Abstinence from alcohol consumption may be maintained using ibudilast or a pharmaceutically acceptable salt thereof. Withdrawal from alcohol may be facilitated and negative effects thereof reduced by using ibudilast or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: August 14, 2014Publication date: February 19, 2015Applicant: MEDICINOVA, INC.Inventors: Yuichi IWAKI, Kirk JOHNSON
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Patent number: 8956651Abstract: The present invention provides compositions comprising methylnaltrexone or a salt thereof, and compositions and formulations thereof, for oral administration.Type: GrantFiled: August 14, 2013Date of Patent: February 17, 2015Assignee: Wyeth, LLCInventors: Syed M. Shah, Christopher Richard Diorio, Eric C. Ehrnsperger, Xu Meng, Kadum A. Al Shareffi, Jonathan Marc Cohen
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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: 20150045383Abstract: An extended release composition for an analgesic active pharmaceutical ingredient which may be an opioid, preferably hydrocodone as the only active ingredient. The extended release composition preferably comprises a extended release composition which may be in the form of beads contained in an oral dosage form such as gelatin capsules. The composition is designed to release hydrocodone in a way such that the increase in hydrocodone exposure in hepatically impaired patients is not clinically significant. The oral dosage units are supplied as part of a kit, which also includes a primary package and a package insert all sold as a commercially marketed product.Type: ApplicationFiled: October 24, 2014Publication date: February 12, 2015Inventors: ANDREW HARTMAN, CHRISTOPHER M. RUBINO, CYNTHIA Y. ROBINSON
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Publication number: 20150044282Abstract: An abuse resistant oral pharmaceutical composition, comprising: a barrier layer, comprising a first polymer; a diffusion layer, comprising a second polymer, substantially covering the barrier layer, wherein the diffusion layer is bonded to the barrier layer and comprises a drug that is substantially homogeneously distributed within the second polymer and diffuses from the diffusion layer within the gastrointestinal (GI) tract; and optionally an expansion layer comprising an expandable polymer, wherein the expansion layer is substantially covered by the barrier layer. Methods of making the same and methods of using the same are also provided.Type: ApplicationFiled: September 23, 2014Publication date: February 12, 2015Inventors: Manish S. SHAH, Ray J. DiFalco
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Patent number: 8951556Abstract: Dosage forms and drug delivery devices suitable for administration of pharmaceutical compounds and compositions, including the oral drug administration of compounds.Type: GrantFiled: March 5, 2013Date of Patent: February 10, 2015Assignee: Durect CorporationInventors: Su Il Yum, Grant Schoenhard, Arthur J. Tipton, John W. Gibson, John C. Middleton, Roger Fu, Michael S. Zamloot
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Patent number: 8952032Abstract: 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: GrantFiled: September 20, 2013Date of Patent: February 10, 2015Assignee: Nektar TherapeuticsInventors: Jennifer Riggs-Sauthier, Bo-Liang Deng, Timothy A. Riley
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Patent number: 8952031Abstract: The invention provides amino- and amido-aminotetralin compounds of formula (I): wherein R1, R2, R3, R4, R5, R6, R7, and n are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.Type: GrantFiled: March 5, 2012Date of Patent: February 10, 2015Assignee: Theravance Biopharma R&D IP, LLCInventors: Sean G. Trapp, Michael R. Leadbetter, Daniel D. Long, Lan Jiang, Sabine Axt
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Patent number: 8951557Abstract: Disclosed are a sustained release solid formulation comprising a drug, for example, oxycodone or its pharmaceutically acceptable salt, in a water-insoluble matrix, which comprises a wax type excipient and copovidone, and thus, has increased compressibility and fluidity and reduced adhesiveness, and a method of preparing the same.Type: GrantFiled: April 28, 2008Date of Patent: February 10, 2015Assignee: Hana Pharm. Co. Ltd.Inventors: Shajoung Chang, Oak Choi
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Publication number: 20150037409Abstract: A solid oral controlled-release dosage form of hydrocodone is disclosed, the dosage form comprising an analgesically effective amount of hydrocodone or a pharmaceutically acceptable salt thereof, and controlled release material.Type: ApplicationFiled: October 21, 2014Publication date: February 5, 2015Inventors: Benjamin Oshlack, Hua-Pin HUANG, John K. Masselink, Alfred Tonelli
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Publication number: 20150037377Abstract: The present invention relates to substituted cellulose acetates and methods of use thereof. One embodiment of the present invention provides a coating having a substituted cellulose acetate having a polar substituent that has an oxygen atom covalently bonded to a nonmetal selected from the group of sulfur, phosphorus, and boron; wherein the nonmetal is present in at least about 0.01% by weight of the substituted cellulose acetate.Type: ApplicationFiled: October 16, 2014Publication date: February 5, 2015Applicant: Celanese Acetate LLCInventors: Michael T. Combs, Thomas S. Garrett