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One of the five cyclos is five-membered and includes ring chalcogen (e.g., codeine, morphine, etc.)

Subclass of:

514 - Drug, bio-affecting and body treating compositions

514001000 - DESIGNATED ORGANIC ACTIVE INGREDIENT CONTAINING (DOAI)

514183000 - Heterocyclic carbon compounds containing a hetero ring having chalcogen (i.e., O,S,Se or Te) or nitrogen as the only ring hetero atoms DOAI

514277000 - Hetero ring is six-membered consisting of one nitrogen and five carbon atoms

514279000 - Polycyclo ring system having the six-membered hetero ring as one of the cyclos

514280000 - Pentacyclo ring system having the six-membered hetero ring as one of the cyclos

514281000 - Two of the cyclos share at least three ring members (i.e., bridged)

Patent class list (only not empty are listed)

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Entries
DocumentTitleDate
20080280936Morphinan Compounds - 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 σ11-13-2008
20100144776USE OF SNPS FOR THE DIAGNOSIS OF A PAIN PROTECTIVE HAPLOTYPE IN THE GTP CYCLOHYDROLASE 1 GENE (GCH1) - The present invention relates to an in vitro method for diagnosing a genetic predisposition or susceptibility for pain in a mammal which comprises detecting of at least one particular single nucleotide polymorphism (SNP) in a sample obtained from said mammal in the genomic locus-derived nucleic acid or fragment thereof of the locus GCH1.06-10-2010
20090215808Oral pharmaceutical dosage forms - Abuse-resistant oral dosage forms suitable for administration of pharmacologically active agents are provided.08-27-2009
20100160364REMEDY OR PREVENTIVE FOR INTEGRATION DYSFUNCTION SYNDROME - A composition includes a therapeutic or prophylactic agent for schizophrenia, which therapeutic or prophylactic agent can treat especially positive symptoms of schizophrenia and does not cause impaired information processing related to cognitive deficiencies or the like which is a symptom of schizophrenia. The therapeutic or prophylactic agent for schizophrenia includes as an effective ingredient a compound having a specific morphinan skeleton or a pharmaceutically acceptable acid addition salt thereof.06-24-2010
20090082383DEUTERIUM-ENRICHED BUPRENORPHINE - The present application describes deuterium-enriched buprenorphine, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.03-26-2009
20090076053METHODS AND COMPOSITIONS FOR TREATING PAIN - Methods and compositions are described for the modulation of central nervous system and/or fetal effects of substances. Methods and compositions are described for the modulation of efflux transporter activity to increase the efflux of drugs and other compounds out of a physiological compartment and into an external environment. In particular, the methods and compositions disclosed herein provide for the increase of efflux transporter activity at blood-brain, blood-CSF and placental-maternal barriers to increase the efflux of drugs and other compounds from physiological compartments, including central nervous system and fetal compartments.03-19-2009
20090192183Oxymorphone Controlled Release Formulations - The invention pertains to a method of relieving pain by administering a controlled release pharmaceutical tablet containing oxymorphone which produces a mean minimum blood plasma level 12 to 24 hours after dosing, as well as the tablet producing the sustained pain relief.07-30-2009
20110195989Controlled Release Formulations of Opioids - Pharmaceutical formulations containing opioid components that each has a release profile. The components may provide immediate or controlled release of the opioid. The invention is also directed to methods of controlling release of one or more opioid compounds and methods of treating pain.08-11-2011
20110195988Pharmaceutical Composition - A liquid composition for administration to the buccal cavity of a patient comprising less than 10 mg/ml morphine and a pharmaceutically acceptable carrier08-11-2011
20130210854Compositions Comprising Enzyme-Cleavable Prodrugs of Active Agents and Inhibitors Thereof - The present disclosure provides pharmaceutical compositions, and their methods of use, where the pharmaceutical compositions comprise a prodrug that provides enzymatically-controlled release of a drug and an enzyme inhibitor that interacts with the enzyme(s) that mediates the enzymatically-controlled release of the drug from the prodrug so as to attenuate enzymatic cleavage of the prodrug. The disclosure provides pharmaceutical compositions which comprise an enzyme inhibitor and a prodrug that contains an enzyme-cleavable moiety that, when cleaved, facilitates release of the drug.08-15-2013
20130210853Injectable Flowable Composition Comprising Buprenorphine - 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.08-15-2013
20100113496PIPERIDINE MODULATORS OF VMAT2 - The present invention relates to new piperidine modulators of VMAT2, nicotinic acetylcholine receptors, and/or μ-opioid receptors, pharmaceutical compositions thereof, and methods of use thereof.05-06-2010
20100076007Polymorphs of 6-Beta-Naltrexol - The present invention provides polymorphs of 6-beta-naltrexol and process for their preparation. In particular, the present invention provides crystalline forms of the free base of 6-beta-naltrexol and processes for their preparation. The present invention also provides crystalline and amorphous forms of the hydrochloride salt of 6-beta-naltrexol and processes for their preparation.03-25-2010
20100076006Topiramate Plus Naltrexone for the Treatment of Addictive Disorders - The present invention provides for the use of combinations of drugs to treat addictive disorders.03-25-2010
20100035910Process for the Preparation of Quaternary N-Alkyl Morphinan Alkaloid Salts - An improved process for the N-alkylation of tertiary morphinan alkaloid bases to form the corresponding quaternary morphinan alkaloid derivatives.02-11-2010
20130079364Peripheral Opioid Agonists and Peripheral Opioid Antagonists - The present disclosure provides compositions, and their methods of use, where the compositions comprise a ketone-modified opioid drug, wherein the drug comprises a ketone-modified opioid and a substituent on the opioid that mediates retention of the drug in the peripheral nervous system as opposed to the central nervous system following ingestion by a subject.03-28-2013
20130035352GABA CONJUGATES AND METHODS OF USE THEREOF - 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.02-07-2013
20090181999USE OF COMPOSITIONS CONTAINING KAPPA-OPIOID RECEPTOR ANTAGONISTS FOR THE TREATMENT OF DISSOCIATIVE DISORDERS - The invention relates to the use of a composition comprising kappa opioid receptor antagonists for producing a drug for the treatment of dissociative disorders in humans.07-16-2009
20120264775Oligomer-Opioid Agonist Conjugates - 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.10-18-2012
20100041689Combined Effects of Topiramate and Ondansetron on Alcohol Consumption - The present invention provides for the use of combinations of drugs to treat addictive disorders. More specifically, the present invention relates the use of drugs in conjunction with behavioral intervention to treat alcohol-related diseases and disorders as well as treatment of obesity and regulating weight.02-18-2010
20100105715POLYMER CONJUGATES OF OPIOID ANTAGONISTS - The invention provides polymer conjugates of opioid antagonists comprising a polymer, such as poly(ethylene glycol), covalently attached to an opioid antagonist. The linkage between the polymer and the opioid antagonist is preferably hydrolytically stable. The invention also includes a method of treating one or more side effects associated with the use of opioid analgesics, such as constipation, nausea, or pruritus, by administering a polymer conjugate of the invention.04-29-2010
20090124650Method of Treating Pain Utilizing Controlled Release Oxymorphone Pharmaceutical Compositions and Instructions on Effects of Alcohol - The invention pertains to a method of using oxymorphone in the treatment of pain by providing a patient with an oxymorphone dosage form and informing the patient or prescribing physician of the effect of alcohol on the maximum concentration of oxymorphone.05-14-2009
20120165361DRUG COATING PROVIDING HIGH DRUG LOADING AND METHODS FOR PROVIDING THE SAME - The present invention is directed to aqueous drug coatings that include at least one insoluble drug, wherein the drug accounts for about 85 wt % to about 97 wt % of the drug coatings. A drug coating according to the present invention may include only one insoluble drug, two or more insoluble drugs, or one or more insoluble drugs in combination with one or more soluble drugs. The present invention also includes drug coating formulations suitable for providing drug coatings according to the present invention and dosage forms that include a drug coating according to the present invention.06-28-2012
20130090350Combination Analgesic Employing Opioid Agonist and Neutral Antagonist - In some embodiments, the invention provides a non-addictive analgesic co-formulation comprising an opioid agonist in an amount sufficient to confer analgesia in a mammalian subject (such as a human) and a neutral opioid antagonist in an amount sufficient to inhibit peripheral effects of the opioid agonist, and insufficient to block substantial central effects of the opioid agonist in the subject. The formulation may be formulated for oral administration to the subject. Such formulations, and methods of using the same, may also deter diversion, inhibit peripheral effects of the opioid agonist, and reduce addiction liability.04-11-2013
20130090349Tamper-resistant oral pharmaceutical dosage form comprising opioid agonist and opioid antagonist - A pharmaceutical dosage form for oral administration having a breaking strength of at least 300 N and comprising an opioid agonist, an opioid antagonist, and a polyalkylene oxide having an average molecular weight of at least 200,000 g/mol, wherein in accordance with Ph. Eur. the in vitro release profile of the opioid agonist essentially corresponds to the in vitro release profile of the opioid antagonist, and wherein the opioid agonist and the opioid antagonist are intimately mixed with one another and homogeneously dispersed in the polyalkylene oxide. The pharmaceutical dosage form is useful, for example, to treat pain in a patient in need of such treatment.04-11-2013
20090306119Non-Codeine Opioid Analgesic Process And Formulations - The invention is directed to the relief of pain using opioid analgesics other than codeine, preferably in combination with a non-steroidal anti-inflammatory agent. Treatment is by self-administration. Compositions for the treatments are provided. Compositions of opioid analgesics other than codeine adapted to avoid the problems of potential abuse are also provided. The compositions have potential use as both prescription and non-prescription medications.12-10-2009
20090312359USE OF METHYLNALTREXONE AND RELATED COMPOUNDS FOR TREATMENT OF GASTROINTESTINAL DYSFUNCTION INDUCED BY ENDOGENOUS OPIOIDS - A method of for preventing or treating gastrointestinal dysfunction and constipation caused by endogenous opioids in a patient who has been chronically taking opioids. The method comprises administering methylnaltrexone or another quaternary derivative of noroxymorphone most preferably by parenteral, intramuscular, intravenous or oral route.12-17-2009
20090093509Methods and Compositions for the Treatment of Pruritus - The present invention is based on the discovery that a nalmefene salt or a peripherally acting analogue of nalmefene is capable of providing long-acting activity against pruritus, when applied topically. In addition, treatment with a nalmefene salt or peripherally acting analogue of nalmefene, can provide disease-modifying effects against the chronic symptoms of atopic dermatitis, including reductions of inflammatory cell infiltrate into the skin, epidermal hyperplasia and trans-epidermal water loss. Compositions of the invention have an inhibitory effect on the itch-scratch-cycle, leading to both relief of pruritus and disease-modifying activity.04-09-2009
20130072514Sustained-Release Opioid Formulations and Methods of Use - The invention combines two different subunits with different release profiles in novel sustained-release oral dosage forms. In particular, the oral dosage forms include a subunit that comprises an opioid analgesic and a sustained-release material, wherein the dissolution rate in-vitro of the subunit, when measured by the standard USP Drug Release test of U.S. Pharmacopeia XXVI (2003) <724>, is less than about 10% within about 6 hours and at least about 60% within about 24 hours; less than about 10% within about 8 hours and at least about 60% within about 24 hours; or less than about 10% within about 12 hours and at least about 60% within about 24 hours; the dosage form providing a duration of therapeutic effect of about 24 hours.03-21-2013
20130072515CRYSTALLINE FORMS OF AN 8-AZABICYCLO[3.2.1]OCTANE COMPOUND - The invention provides a crystalline sulfate salt of 3-endo-(8-{2-[cyclohexylmethyl-((S)-2,3-dihydroxy-propionypamino]ethyl}-8-aza-bicyclo[3.2.1]oct-3-yl) benzamide or a solvate thereof. The invention also provides pharmaceutical compositions comprising such crystalline salt forms, methods of using such crystalline salt forms to treat diseases associated with mu opioid receptor activity, and processes useful for preparing such crystalline salt forms.03-21-2013
20130072516METHOD OF ALCOHOL CESSATION AND TREATMENT - A method of alcohol cessation and treatment for a patient generally comprises the steps of administering a multi-vitamin to the patient, administering a medication group to the patient, and monitoring the patient. In various embodiments, the medication group may be administered to the patient via a first and second injection solution. The first injection solution generally comprises a therapeutically effective amount of an anti-addictive agent, such as naltrexone palmitate. The second injection solution generally comprises a therapeutically effective amount of an inhibitor of alcohol dehydrogenase, such as disulfiram. The method, which may also be referred to as procedure, may include various pre- and/or post-procedural steps as described herein.03-21-2013
20090197905QUATERNARY OPIOID CARBOXAMIDES - Compounds of formulas:08-06-2009
20130059876LIQUID NASAL SPRAY CONTAINING LOW-DOSE NALTREXONE - Liquid formulations for administration of naltrexone at low concentrations by the nasal route are described.03-07-2013
20130065916CRYSTALLINE FORMS OF A 3-CARBOXYPROPYL-AMINOTETRALIN COMPOUND - 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.03-14-2013
20110021551TREATMENT WITH OPIOID ANTAGONISTS AND mTOR INHIBITORS - Embodiments of the invention provide methods of treating a disorder or disease characterized by cellular proliferation and migration by co-administering a synergistically effective amount of an mTOR inhibitor and a μ-opioid receptor antagonist.01-27-2011
20090247562LARGE SUBSTITUENT, NON-PHENOLIC OPIOIDS AND METHODS OF USE THEREOF - 8-Substituted-2,6-methano-3-benzazocines of general structure10-01-2009
20130165467MANUFACTURING OF ACTIVE-FREE GRANULES AND TABLETS COMPRISING THE SAME - The present invention relates to prolonged release pharmaceutical dosage forms, the manufacture thereof as well as their use for administration to human beings.06-27-2013
20130165468TOPICAL PERIPHERAL NEURO-AFFECTIVE (TPNA) THERAPY - A method of treating peripheral neuropathic pain in humans resulting from a peripheral nerve injury and for treating muscle spasm in humans resulting from a peripheral nerve injury comprises applying a therapeutically effective amount of a drug selected from the group consisting of a dopamine agonist, a skeletal muscle relaxant, and a combination thereof topically to the site of the injury.06-27-2013
20130165466POLYMER CONJUGATES OF OPIOID ANTAGONISTS - The invention provides polymer conjugates of opioid antagonists comprising a polymer, such as poly(ethylene glycol), covalently attached to an opioid antagonist. The linkage between the polymer and the opioid antagonist is preferably hydrolytically stable. The invention also includes a method of treating one or more side effects associated with the use of opioid analgesics, such as constipation, nausea, or pruritus, by administering a polymer conjugate of the invention.06-27-2013
20100160363EXTENDED-RELEASE PHARMACEUTICAL FORMULATIONS - The present invention provides matrix-forming, sustained-release pharmaceutical formulations comprising four primary components: i) an effective amount of at least one drug substance; ii) at least one pharmaceutically acceptable, water-swellable, pH independent polymer; iii) at least one pharmaceutically-acceptable, anionic, pH dependent polymer; and (iv) a pharmaceutically-acceptable polymer selected from the group consisting of a) at least one pharmaceutically-acceptable cationic polymer; and b) at least one pharmaceutically acceptable hydrocolloid. The present formulations can be used with compounds having a wide range of solubilities as well as compounds characterized as having hydrophobic or hydrophilic characteristics.06-24-2010
20100197717COMBINATION OF A 5HT7 RECEPTOR LIGAND AND AN OPIOID RECEPTOR LIGAND - The present invention refers to a combination of a 5HT7 receptor ligand and an opioid receptor ligand, especially of a 5HT7 receptor agonist and an opioid receptor agonist, a medicament comprising this combination, or the use of this combination for the treatment of the symptoms of pain, the prevention or the prophylaxis of the symptoms of pain.08-05-2010
20090298862Methods useful for the treatment of pain, arthritic conditions or inflammation associated with a chronic condition - Methods, including those for administering novel pharmaceutical compositions, dosage forms containing an opioid active pharmaceutical ingredient, are useful for treating pain, arthritic conditions and/or inflammation associated with a chronic condition, including pain from arthritis and inflammation.12-03-2009
20080275074Anti-Itching Agent - A novel antipruritic useful for the treatment of pruritus accompanying various diseases is disclosed. The antipruritic comprises a specific morphinan derivative having a nitrogen-containing cyclic group or the pharmaceutically acceptable acid addition salt thereof such as N-(17-cyclopropylmethyl-4,5α-epoxy-3,14-dihydroxy-morphinan-6β-yl)-phthalimide hydrochloric acid salt11-06-2008
20110294843ADMINISTRATION SCHEME OF POLAR OPIOID METABOLITES FOR POST-OPERATIVE PAIN MANAGEMENT - Administration scheme of an analgesically active polar metabolite of an opioid or the salt thereof for the manufacture of a medicament for the treatment of pain after medical operation, whereas the medicament is administered at least once before the end of the medical operation.12-01-2011
20100048602Oligomer-Opioid Agonist Conjugates - 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.02-25-2010
20090291975DUAL OPIOID PAIN THERAPY - Provided are pharmaceutical compositions and methods for the alleviation of pain in a patient with optimal ratios of morphine and oxycodone that provide superior analgesic efficacy and lower incidence of adverse side effects compared to morphine and oxycodone alone. The pharmaceutical compositions comprise morphine and oxycodone, or pharmaceutically acceptable salts thereof, in ratios of about 3 to 2 to about 1 to 2, morphine to oxycodone by weight.11-26-2009
20100113495PHARMACEUTICAL COMPOSITIONS COMPRISING AN OPIOID RECEPTOR ANTAGONIST AND METHODS OF USING SAME - The present invention features compositions for intranasal administration comprising an opioid receptor antagonist. The invention also features methods of using such compositions in the treatment of various diseases and disorders, such as the treatment of alcoholism. In certain embodiments, the opioid receptor antagonist is naltrexone or a pharmaceutically acceptable salt thereof.05-06-2010
20100113497GABA CONJUGATES AND METHODS OF USE THEREOF - 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.05-06-2010
20110263630SYNTHESIS OF METABOLICALLY STABLE AGENTS FOR ALCOHOL AND DRUG ABUSE - Disclosed herein are compounds of formula (I); as defined herein, or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising the same, and methods of using these compounds for the treatment of substance addiction.10-27-2011
20100120811LONG-ACTING INJECTABLE ANALGESIC FORMULATIONS FOR ANIMALS - Long acting injectable analgesic formulations and methods for providing long lasting pain relief in animals are disclosed.05-13-2010
20100267758PHARMACEUTICAL FORMULATION - Stable pharmaceutical compositions useful for administering methylnaltrexone are described, as are methods for making the same. Kits, including these pharmaceutical compositions, also are provided.10-21-2010
20110263631COMBINATION OF A SEROTONIN AND NOREPINEPHRINE REUPTAKE INHIBITOR AND AN OPIOID AGONIST FOR THE TREATMENT OF PAIN - The invention provides a method of treating a pain condition in a mammal utilizing a specific serotonin and norepinephrine reuptake inhibitor (SNRI) and also the combination of the SNRI and an opioid agonist agent. The invention includes methods wherein the opioid agonist agent is administered at a dose that is lower than a dose administered for treating a pain condition when used alone.10-27-2011
20100120812Medicinal Compositions Comprising Buprenorphine And Naltrexone - An analgesic composition, in parenteral unit dosage form or in a unit dosage form suitable for delivery via the dermis or mucosa, comprises buprenorphine and an amount of naltrexone such that the ratio by weight of buprenorphine to naltrexone delivered to or reaching the plasma of a patient is in the range 100:1 to 5000:1. The analgesic action of the buprenorphine is potentiated by the low dose of naltrexone. Also provided are a method of treatment of pain and the use of buprenorphine and naltrexone for the manufacture of a medicament.05-13-2010
20100120813PERIPHERAL OPIOID RECEPTOR ANTAGONISTS AND USES THEREOF - The present invention provides a compound of formula I:05-13-2010
20120108622PHARMACEUTICAL FORMULATION CONTAINING GELLING AGENT - Disclosed in certain embodiments is a controlled release oral dosage form comprising a therapeutically effective amount of a drug susceptible to abuse together with one or more pharmaceutically acceptable excipients; the dosage form further including a gelling agent in an effective amount to impart a viscosity unsuitable for administration selected from the group consisting of parenteral and nasal administration to a solubilized mixture formed when the dosage form is crushed and mixed with from about 0.5 to about 10 ml of an aqueous liquid; the dosage form providing a therapeutic effect for at least about 12 hours when orally administered to a human patient.05-03-2012
20120108621PHARMACEUTICAL PREPARATION CONTAINING OXYCODONE AND NALOXONE - The invention concerns a storage stable pharmaceutical preparation comprising oxycodone and naloxone for use in pain therapy, with the active compounds being released from the preparation in a sustained, invariant and independent manner.05-03-2012
20100099696Tamper resistant oral dosage forms containing an embolizing agent - Oral dosage form containing a therapeutically effective amount of a drug susceptible to abuse and an effective amount of an embolizing agent which causes the production of a solid or semi-solid embolus or blockage after tampering.04-22-2010
20110172259DOSAGE FORM CONTAINING OXYCODONE AND NALOXONE - The present invention concerns a dosage form comprising oxycodone and naloxone which is characterized by specific in vivo parameters such as t07-14-2011
20090137618PRO-DRUGS FOR CONTROLLED RELEASE OF BIOLOGICALLY ACTIVE COMPOUNDS - Pro-drugs containing an electron withdrawing substituent, as defined in the specification, are useful in a method for providing a patient with post administration-activated, controlled release of a biologically active compound.05-28-2009
20110172260METHODS OF PROVIDING WEIGHT LOSS THERAPY IN PATIENTS WITH MAJOR DEPRESSION - Disclosed are methods of providing weight loss therapy, particularly for patients suffering from major depression.07-14-2011
20100311781SYNTHESIS OF R-N-METHYLNALTREXONE - 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.12-09-2010
20110207761Diversion- and/or abuse-resistant aompositions and methods for making the same - A composition formulated for diversion- and/or abuse-resistance, includes at least one active pharmaceutical ingredient (API), each present in an acidic form, a first compound capable of coupling to the acidic form of the API to form a complex, where the resulting complex is resistant to separation by conventional separation methods, and a second compound capable of preferentially coupling to the first compound to thereby release the API from the complex.08-25-2011
20090170888Antipruritic Agent for Pruritus Caused by Multiple Sclerosis - An antipruritic against pruritus caused by multiple sclerosis is disclosed. The antipruritic comprises as an effective ingredient an κ opioid receptor agonist compound having a 4,5-epoxymorphinan skeleton and having a specific chemical structure, such as Compound 1 having the following structure:07-02-2009
20120041014Methods of Converting a Patient's Treatment Regimen from Intravenous Administration of an Opioid to Oral Co-Administration of Morphine and Oxycodone Using a Dosing Algorithm to Provide Analgesia - A method of converting a treatment for pain comprising intravenous administration of opioids, to a treatment for pain comprising oral administration of a first dose of an immediate release morphine-oxycodone combination in patients in need of analgesia. The method may comprise (1) determining a four-hour average oral morphine equivalents, a one-hour average oral morphine equivalents, or determining a net average hourly intravenous dose, and (2) orally administering to the patient a first dose of a morphine-oxycodone combination in a 3:2 ratio by weight every four to six hours. Also, a method of treating pain in patients who had been administered opioids intravenously, comprising using a dosing algorithm to determine the first dose of the immediate release morphine-oxycodone combination.02-16-2012
20110207762OXYCODONE HYDROCHLORIDE HAVING LESS THAN 25 PPM 14-HYDROXYCODEINONE - In certain embodiments the invention is directed to a process for preparing an oxycodone hydrochloride composition having less than 25 ppm of 14-hydroxycodeinone.08-25-2011
20090181998OPIOID RECEPTOR SUBTYPE-SELECTIVE AGENTS - Opioid receptor compounds and pharmaceutical compositions thereof are presented. Also presented are methods for treating a condition mediated by an opioid receptor by administering an effective amount of the opioid receptor compound to a patient in need thereof.07-16-2009
201102077638-CARBOXAMIDO-2,6-METHANO-3-BENZAZOCINES - 8-Substituted-2,6-methano-3-benzazocines of general structure I in which A is —CH08-25-2011
20090005408PROCESS FOR THE PRODUCTION OF AN ABUSE-PROOFED DOSAGE FORM - The present invention relates to a process for the production of abuse-proofed, thermoformed dosage forms containing, apart from one or more active ingredients with potential for abuse and optionally physiologically acceptable auxiliary substances, at least one synthetic or natural polymer with a breaking strength of at least 500 N.01-01-2009
20090143417METHODS OF TREATING PAIN - The present invention is directed to methods and compositions for inducing, promoting or otherwise facilitating pain relief. More particularly the present invention discloses the combination of a nitric oxide donor and an opioid analgesic in the therapeutic management of vertebrate animals including humans, for the prevention or alleviation of pain, particularly moderate to severe pain. In particular, the nitric oxide donor is a slow-release nitric oxide donor or is formulated to provide a sustained release of a low dose of nitric oxide.06-04-2009
20080234306N-Oxides of 4,5-Epoxy-Morphinanium Analogs - Novel N-oxides of 4,5-epoxy-morphinanium analogs are disclosed. Pharmaceutical compositions containing the N-oxides of 4,5-epoxy-morphinanium analogs and methods of their pharmaceutical uses are also disclosed. The compounds disclosed are useful, inter alia, as modulators of opioid receptors.09-25-2008
20090325995Preparation of pharmaceutical formulations - A process for the production of a composition comprising a water-insoluble opioid which comprises the steps of: a) providing a mixture comprising: i) a water-insoluble opioid, ii) a water soluble carrier, and iii) a solvent for each of the opioid and the carrier, and b) spray-drying the mixture to remove the or each solvent and obtain a substantially solvent-free nano-dispersion of the opioid in the carrier12-31-2009
20130217716Pharmaceutical Formulation Containing Gelling Agent - Disclosed in certain embodiments is a controlled release oral dosage form comprising a therapeutically effective amount of a drug susceptible to abuse together with one or more pharmaceutically acceptable excipients; the dosage form further including a gelling agent in an effective amount to impart a viscosity unsuitable for administration selected from the group consisting of parenteral and nasal administration to a solubilized mixture formed when the dosage form is crushed and mixed with from about 0.5 to about 10 ml of an aqueous liquid; the dosage form providing a therapeutic effect for at least about 12 hours when orally administered to a human patient.08-22-2013
200902095706-Aminomorphinane Derivatives, Method for the Production and Use Thereof - This invention relates to compounds of the formula (I).08-20-2009
20090023765SUBSTITUTED PHENETHYLAMINES WITH SEROTONINERGIC AND/OR NOREPINEPHRINERGIC ACTIVITY - Chemical syntheses and medical uses of novel inhibitors of the uptake of monoamine neurotransmitters and pharmaceutically acceptable salts and prodrugs thereof, for the treatment and/or management of psychotropic disorders, anxiety disorder, generalized anxiety disorder, depression, post-traumatic stress disorder, obsessive-compulsive disorder, panic disorder, hot flashes, senile dementia, migraine, hepatopulmonary syndrome, chronic pain, nociceptive pain, neuropathic pain, painful diabetic retinopathy, bipolar depression, obstructive sleep apnea, psychiatric disorders, premenstrual dysphoric disorder, social phobia, social anxiety disorder, urinary incontinence, anorexia, bulimia nervosa, obesity, ischemia, head injury, calcium overload in brain cells, drug dependence, and/or premature ejaculation are described.01-22-2009
200902037236,7-unsaturated-7-carbamoyl substituted morphinan derivative - A novel compound which is useful as an agent for treating and/or preventing emesis, vomiting and/or constipation.08-13-2009
20090082382DEUTERIUM-ENRICHED NALTREXONE - The present application describes deuterium-enriched naltrexone, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.03-26-2009
20110230512Pharmaceutical Composition - A pharmaceutical composition comprising an analgesic or analgesic combination and a stool softener is disclosed. The analgesic is selected from morphine, meperidine, fentanyl, hydromorphone, oxymorphone, oxycodone, hydrocodone, methadone, propoxyphene, pentazocine, levorphanol, codeine, acetaminophen and combinations of these analgesics. The composition is formulated for oral administration as a liquid or solid dosage form for immediate, slow, delayed or sustained-release characteristics.09-22-2011
20110230511CARBOXAMIDE BIOISOSTERES OF OPIATES - A compound of formula I is disclosed.09-22-2011
20110230510PHARMACEUTICAL FORMULATIONS CONTAINING OPIOID AGONIST, OPIOID ANTAGONIST AND GELLING AGENT - Disclosed in certain embodiments is an oral dosage form comprising a therapeutically effective amount of an opioid analgesic, an opioid antagonist and one or more pharmaceutically acceptable excipients; the dosage form further including a gelling agent in an effective amount to impart a viscosity unsuitable for administration selected from the group consisting of parenteral and nasal administration to a solubilized mixture formed when the dosage form is crushed and mixed with from about 0.5 to about 10 ml of an aqueous liquid.09-22-2011
20080262013OXYMORPHONE CONTROLLED RELEASE FORMULATIONS - The invention pertains to a method of relieving pain by administering a controlled release pharmaceutical tablet containing oxymorphone which produces a mean minimum blood plasma level 12 to 24 hours after dosing, as well as the tablet producing the sustained pain relief.10-23-2008
20090221621Methods of Reducing Alcohol-Induced Dose Dumping for Opioid Sustained Release Oral Dosage Forms - Disclosed are methods of sustained release administration of opioids, including but not limited to hydromorphone and oxycodone, that exhibit improved properties with respect to co-ingestion with aqueous alcohol.09-03-2009
20110144145METHODS FOR TREATING VISCERAL FAT CONDITIONS - Disclosed are methods and compositions for treating visceral fat conditions and/or metabolic syndrome using combinations of naltrexone and bupropion.06-16-2011
20110144144IBUPROFEN AND NARCOTIC ANALGESIC COMPOSITIONS - Provided herein are compositions and methods of making compositions of ibuprofen in combination with a narcotic analgesic. Specifically provided is a pharmaceutical tablet composition comprising ibuprofen; a narcotic analgesic; colloidal silicon dioxide; a filler selected from the group consisting of microcrystalline cellulose and powdered cellulose; a disintegrant selected from the group consisting of croscarmellose sodium, crospovidone, and sodium starch glycolate; a binder consisting of an akylhydroxy methylcellulose; a starch; and a lubricant. Also provided herein is a method of preparing a pharmaceutical tablet composition comprising: (a) Granulating ibuprofen, a narcotic analgesic, a first glidant, a first disintegrant, a binder, and starch to form granules wherein said granulating step comprises a wet granulation process; (b) blending the granules with extra-granular material comprised of a second glidant, a second disintegrant, a filler and starch to form a blend of granules and extra-granular material; and (c) compressing the blend into a tablet.06-16-2011
20090253728Methods and Compositions for Treating Nociceptive Pain - The present invention provides methods and compositions useful for the treatment and prevention of pain.10-08-2009
20090253729Analgesic Agent - A pharmaceutical preparation useful for alleviating or treating a pain, e.g., a chronic pain (particularly, a neuropathic pain) is provided. The pharmaceutical preparation contains (a) a propionic acid-derived nonsteroidal anti-inflammatory agent (e.g., ibuprofen), (b) a non-pyrazolone antipyretic analgesic agent (e.g., acetaminophen), and (c) an opioid analgesic agent (e.g., codeine phosphate, dihydrocodeine phosphate). The pharmaceutical preparation may contain 5 to 100 parts by weight of the antipyretic analgesic agent (b) or 0.5 to 500 parts by weight of the analgesic agent (c) relative to 100 parts by weight of the anti-inflammatory agent (a). The pharmaceutical preparation may be substantially free from a nontoxic N-methyl-D-aspartate receptor antagonist and may contain 20 to 80 parts by weight of the antipyretic analgesic agent (b) and 1 to 100 parts by weight of the analgesic agent (c) relative to 100 parts by weight of the anti-inflammatory agent (a).10-08-2009
20100056554USE OF OPIOID FORMULATIONS IN NEEDLE-LESS DRUG DELIVERY DEVICES - The present invention concerns a needle-less drug delivery device being suitable for delivering drugs through a skin surface into a human or animal body comprising a pharmaceutical composition with at least one analgesic agent preferably being an opioid. The present invention also relates to the use of at least one analgesic agent, preferably being at least one opioid in a needle-less drug delivery device being suitable for injecting medication through a skin surface into the human or animal body. Further, the invention is concerned with a method of treating breakthrough pain by injecting at least one analgesic agent preferably being an opioid into the human or animal body using a needle-less drug delivery device.03-04-2010
20100273822Immediate release compositions and methods for delivering drug formulations using strong acid ion exchange resins - Solid oral dosage immediate release compositions comprising strong acid ion exchange resins and methods for delivering drug formulations.10-28-2010
20100168148Pharmaceutical formulation containing gelling agent - Disclosed in certain embodiments is a controlled release oral dosage form comprising a therapeutically effective amount of a drug susceptible to abuse together with one or more pharmaceutically acceptable excipients; the dosage form further including a gelling agent in an effective amount to impart a viscosity unsuitable for administration selected from the group consisting of parenteral and nasal administration to a solubilized mixture formed when the dosage form is crushed and mixed with from about 0.5 to about 10 ml of an aqueous liquid; the dosage form providing a therapeutic effect for at least about 12 hours when orally administered to a human patient.07-01-2010
20100261746PHARMACEUTICAL FORMULATION - Stable pharmaceutical compositions useful for administering methylnaltrexone are described, as are methods for making the same. Kits, including these pharmaceutical compositions, also are provided.10-14-2010
20100261747NOVEL PHARMACEUTICAL COMPOSITIONS AND METHODS OF PREPARATION AND USE - The present invention provides a standardized method for the detection of narcotic abuse. Narcotics are formulated with a test compound that is not completely metabolized by the body. Narcotic diversion is detected by urinalysis of the suspected abuser, wherein the test compound may be detected even if the diverted narcotic is completely metabolized by the body, or otherwise undetectable in the urine.10-14-2010
20130123293OPIOID-CONTAINING ORAL PHARMACEUTICAL COMPOSITIONS AND METHODS - The present invention provides sustained-release oral pharmaceutical compositions and methods of use. The sustained-release oral pharmaceutical compositions include an opioid (including salts thereof) and a salt of a non-steroidal anti-inflammatory drug (NSAID).05-16-2013
20130123294FORMULATIONS CONTAINING NALBUPHINE AND USES THEREOF - Immediate release, oral, pharmaceutical formulation including nalbuphine or a pharmaceutically acceptable salt thereof, and at least one hydrophilic granulation carrier, one hydrophilic binder and one lubricant.05-16-2013
20100152222Medicinal Compositions Comprising Buprenorphine And Nalmefene - An analgesic composition, in parenteral unit dosage form or in a unit dosage form suitable for delivery via the dermis or mucosa, comprises buprenorphine and an amount nalmefene such that the ratio by weight of buprenorphine to nalmefene delivered to or reaching the plasma of a patient is in the range 22.6:1 to 40:1. The analgesic action of the buprenorphine is potentiated by the low dose of nalmefene. Also provided are a method of treatment of pain and the use of nalmefene and buprenorphine for the manufacture of a medicament.06-17-2010
20100227876Methods of Reducing Side Effects of Analgesics - The invention provides for compositions and methods of reducing pain in a subject by administering a combination of mu-opioid receptor agonist, kappa1-opioid receptor agonist and a nonselective opioid receptor antagonist in amounts effective to reduce pain and ameliorate an adverse side effect of treatment combining opioid-receptor agonists. The invention also provides for methods of enhancing an analgesic effect of treatment with an opioid-receptor agonist in a subject suffering from pain while reducing an adverse side effect of the treatment. The invention also provides for methods of reducing the hyperalgesic effect of treatment with an opioid-receptor agonist in a subject suffering from pain while reducing an adverse side effect of the treatment. The invention further provides for methods of promoting the additive analgesia of pain treatment with an opioid-receptor agonist in a subject in need while reducing an adverse side effect of the treatment.09-09-2010
20090076052DEUTERIUM-ENRICHED NALMEFENE - The present application describes deuterium-enriched nalmefene, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.03-19-2009
20090076051DEUTERIUM-ENRICHED METHYLNALTREXONE - The present application describes deuterium-enriched methylnatrexone bromide, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.03-19-2009
20100240690COMPOSITIONS CONTAINING OPIOID ANTAGONISTS - Compositions containing opioid antagonists, particularly alvimopan and its active metabolite, with improved solubility and bioavailability for oral or parenteral administration, injectable dosage formulations, kits, and methods of making and using same are disclosed. In preferred embodiments, invention provides injectable formulations containing opioid antagonists, particularly alvimopan and its active metabolite, having low solubility that may be readily prepared, are stable during storage, and provide maximum levels of opioid antagonists when administered parenterally, particularly via injection. The results are achieved by a combination of processing techniques and component selection.09-23-2010
20110112130Opioid-Nornicotine Codrugs Combinations for Pain Management - The present invention relates to the field of pain management, and more particularly to synergistic codrugs comprising an opioid and nornicotine which have been combined to form a single chemical codrug entity. When the codrug is administered it produces a synergistic analgesic response to pain.05-12-2011
20110112131Opioid-Ketamine and Norketamine Codrug Combinations for Pain Management - The present invention relates to the field of pain management, and more particularly to synergistic codrugs comprising an opioid and ketamine or norketamine which have been combined to form a single chemical codrug entity. When the codrug is administered it produces a synergistic analgesic response to pain.05-12-2011
20100210675SOLVENT-FREE CRYSTALLINE FORM OF NALTREXONE - Solvent-free crystalline polymorphic form of naltrexone, characterized in that it has the XRD data listed in Table 1, and a method for the preparation of this polymorphic form; and a method for converting this polymorphic form of naltrexone into a known polymorphic form of naltrexone.08-19-2010
20100120815STABLE SOLID PREPARATION CONTAINING 4,5-EPOXYMORPHINAN DERIVATIVE - It is an object of the present invention to provide a stable solid preparation comprising a 4,5-epoxymorphinan derivative or a pharmacologically acceptable acid addition salt thereof as an effective ingredient.05-13-2010
20120142719Benzoic acid, benzoic acid derivatives and heteroaryl carboxylic acid conjugates of hydrocodone, prodrugs, methods of making and use thereof - 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.06-07-2012
20120142718N-17-Alkylated Prodrugs of Opioids - Compounds of formula (II) R06-07-2012
20120142720Phenylethanoic Acid, Phenylpropanoic Acid and Phenylpropenoic Acid Conjugates and Prodrugs of Hydrocodone, Methods of Making and Use Thereof - 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.06-07-2012
20120245193PERIPHERIALLY ACTING .mu. OPIOID ANTAGONISTS - The present invention relates to a novel functional peripherally-acting μ opioid receptor antagonist of Formula I:09-27-2012
20080287480Therapeutic Combination Comprising a Nmda Receptors Blocker and a Narcotic Analgesic Substance - The invention relates to a medicament comprising a combination of a substance that blocks both the ion channel associated to NMDA receptors and MAO enzymes and a narcotic analgesic substance, preferably a fixed combination, pharmaceutical compositions thereof, and to the use thereof for the treatment of subjects suffering of various types of pain and/or for inhibiting the development of tolerance, and/or physical dependence on a narcotic analgesic substance.11-20-2008
20090111844Combination analgesic employing opioid and neutral antagonist - A non-addictive analgesic co-formulation comprising an opioid agonist in an amount sufficient to confer analgesia in a mammalian subject and a neutral opioid antagonist in an amount sufficient to inhibit peripheral effects, and insufficient to block substantial central effects, of the opioid agonist in the subject. Such formulations, and methods of using same, may also deter diversion, inhibit peripheral effects, and reduce addiction liability.04-30-2009
20090111843Therapeutic or Prophylactic Agent for Functional Bowel Disorder - 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-4,5α-epoxy-3,14-dihydroxy-morphinan-6β-yl)-3,4,5,6-tetrahydrophthalimide tartaric acid salt (Compound 10).04-30-2009
20110046173COMBINATION ANALGESIC OPIOID PAIN THERAPY - Provided are pharmaceutical compositions and methods for the alleviation of pain in a patient with ratios of morphine and oxycodone that provide lower incidence of adverse side effects compared to equi-analgesic doses of morphine and oxycodone alone. The pharmaceutical compositions comprise an analgesic amount of morphine and an analgesic amount of oxycodone, or pharmaceutically acceptable salts thereof, in ratios of about 3 to 2 to about 1.25 to 1, morphine to oxycodone by weight.02-24-2011
20100311782SUBSTITUTED PIPERIDINYLPROPANOIC ACID COMPOUNDS AND METHODS OF THEIR USE - Novel 3,4-disubstituted-4-(3-carbamoylphenyl)-piperidinylpropanoic acid compounds and their salts, including pharmaceutically acceptable salts, pharmaceutical compositions and methods of their use are disclosed. The novel compounds are useful, inter alia, as antagonists of opioid receptors.12-09-2010
20110245287Hybrid Opioid Compounds and Compositions - Disclosed are hybrid opioid compounds, mixed opioid salts, compositions comprising the hybrid opioid compounds and mixed opioid salts, and methods of use thereof. More particularly, in one aspect the hybrid opioid compound includes at least two opioid compounds that are covalently bonded to a linker moiety. In another aspect, the hybrid opioid compound relates to mixed opioid salts comprising at least two different opioid compounds or an opioid compound and a different active agent. Also disclosed are pharmaceutical compositions, as well as to methods of treating pain in humans using the hybrid compounds and mixed opioid salts.10-06-2011
20100331354Intranasal Opioid Compositions - The present invention relates to pharmaceutical compositions for intranasal administration to a mammal that contain an effective amount of an opioid, a liquid nasal carrier for the opioid, and optionally a sweetener, flavoring agent or masking agent. In some embodiments of the present invention, the pharmaceutical compositions have improved bioavailability. In other embodiments of the present invention, the opioid compositions improve patient compliance.12-30-2010
20110034502NALMEFENE PRODRUGS - The present invention relates to ester 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.02-10-2011
20110118294Intranasal Opioid Compositions - The present invention relates to pharmaceutical compositions for intranasal administration to a mammal that contain an effective amount of an opioid, a liquid nasal carrier for the opioid, and optionally a sweetener, flavoring agent or masking agent. In some embodiments of the present invention, the pharmaceutical compositions have improved bioavailability. In other embodiments of the present invention, the opioid compositions improve patient compliance.05-19-2011
20110082167TOPICAL COMPOSITIONS OF OPIOID ANTAGONISTS AND METHODS FOR TREATING SKIN CONDITIONS THEREWITH - Provided are topical compositions comprising opioid antagonists, such as naltrexone or naloxone, or their pharmaceutically acceptable salts, and methods for treating skin conditions, such as those caused by human papillomavirus, therewith.04-07-2011
20090253730Method and composition for deterring abuse of opioid containing dosage forms - This invention relates to an abuse deterrent dosage form of opioid analgesics, wherein an analgesically effective amount of opioid analgesic is combined with a polymer to form a matrix.10-08-2009
20110136848MORPHINAN DERIVATIVES FOR THE TREATMENT OF DRUG OVERDOSE - The instant application relates to morphinan derivatives of Formula I with sustained effectiveness in treating drug toxicity and overdose:06-09-2011
20110245288TRANSDERMALLY DELIVERABLE OPIOID PRODRUGS, ABUSE-RESISTANT COMPOSITIONS AND METHODS OF USING OPIOID PRODRUGS - Described herein are opioid prodrugs, methods of making opioid agonist-antagonist prodrugs, compositions comprising opioid agonist-antagonist prodrugs, abuse-resistant formulations and dosage forms of opioid agonist-antagonist prodrugs, and methods of using opioid agonist-antagonist prodrugs.10-06-2011
20080312264Process for the production of an abuse-proofed solid dosage form - The present invention relates to a process for the production of an abuse-proofed solid dosage form containing at least one active ingredient with potential for abuse and a synthetic or natural polymer with a breaking strength of =500 N, characterised in that a corresponding mixture is processed by melt extrusion with the assistance of a planetary-gear extruder.12-18-2008
20090215809CRYSTALLINE FORM OF A (3S)-AMINOMETHYL-5-METHYL-HEXANOIC ACID PRODRUG AND METHODS OF USE - A crystalline form of a (3S)-aminomethyl-5-hexanoic acid prodrug and methods of preparing a crystalline form of a (3S)-aminomethyl-5-hexanoic acid prodrug, and methods of using a crystalline form of a (3S)-aminomethyl-5-hexanoic acid prodrug are provided.08-27-2009
20110251228NALMEFENE HYDROCHLORIDE DIHYDRATE - The present invention relates to the Nalmefene hydrochloride dihydrate, methods of manufacturing Nalmefene hydrochloride dihydrate, a pharmaceutical composition comprising Nalmefene hydrochloride dihydrate and a method of treatment comprising administering Nalmefene hydrochloride dehydrate.10-13-2011
20110251227ANALGESIC AGENTS - The invention provides a compound of formula (I) or a salt thereof, as well as compositions comprising such compounds. The compounds and compositions are useful as analgesics.10-13-2011
20100249169FORMULATIONS FOR PARENTERAL DELIVERY OF COMPOUNDS AND USES THEREOF - The present invention provides formulations that achieve effective delivery of methylnaltrexone compositions. The provided formulations are useful for preventing, treating delaying, diminishing or reducing the severity of side effects resulting from use of analgesic opioids.09-30-2010
20110071181EFFERVESCENT ORAL OPIATE DOSAGE FORMS AND METHODS OF ADMINISTERING OPIATES - Opiate containing dosage forms and methods using same are described. These dosage forms include substantially less opiates by weight than known oral formulations. These dosage forms are intended for oral administration across the oral mucosa.03-24-2011
20090264454COMBINED HYDROCODONE AND ANALGESIC FORMULATION AND METHOD - The present invention is directed to co-administration of hydrocodone and a second analgesic agent for the treatment of pain. A pharmaceutical composition suitable for the co-administration contains a therapeutically effective amount of hydrocodone or a pharmaceutically acceptable salt thereof, and a therapeutically effective amount of at least one second analgesic agent. A ratio of the hydrocodone or pharmaceutically acceptable salt thereof to the at least one second analgesic agent in the composition is within a range that provides greater pain relief than that obtainable by the administration of the hydrocodone or second analgesic agent alone. Examples of pharmaceutical compositions for co-administration of the agents are those containing hydrocodone and indomethacin (“Indocodone”), hydrocodone and naproxen (“Naprocodone”), hydrocodone and diclofenac (“Diclodone”) and hydrocodone and tramadol (“Tramacodone”).10-22-2009
20120202838DRUG FORMULATIONS - In one embodiment, the present invention relates to abuse-deterrent drug formulations comprise a plurality of discrete domains uniformly dispersed in a pharmaceutically acceptable matrix, wherein said domains have high fracture toughness and comprise at least one polymer and at least one abuse-relevant drug. In another embodiment, the present invention relates to a formulation comprising a plurality of discrete mechanically reinforcing particles uniformly dispersed in a pharmaceutically acceptable matrix, wherein said matrix has high fracture toughness and comprises at least one polymer and at least one active agent, at least one abuse-relevant drug or a combination of at least one active agent and at least one abuse-relevant drug.08-09-2012
20100120814Crystalline and Amorphous Forms of Naltrexone Hydrochloride - The present invention relates to novel crystalline forms of naltrexone hydrochloride including hydrated and solvated forms and a novel amorphous form. The invention also describes methods of preparing the various crystalline forms. The present invention also relates to pharmaceutical compositions containing crystalline and amorphous forms of naltrexone hydrochloride, as well as methods of treating addictive behavior by administering the pharmaceutical compositions.05-13-2010
20100261745PHARMACEUTICAL FORMULATION - Stable pharmaceutical compositions useful for administering methylnaltrexone are described, as are methods for making the same. Kits, including these pharmaceutical compositions, also are provided.10-14-2010
20110212985Naltrexone Long Acting Formulations and Methods of Use - The inventions described herein arose from unexpected discoveries made during clinical trials with a long acting formulation of naltrexone. As such, the invention includes a method for treating an individual in need of naltrexone comprising the step of parenterally administering a long acting formulation comprising naltrexone and to the use of naltrexone in the manufacture of medicaments for use in such methods.09-01-2011
20110160239ORAL ADMINISTRATION OF PERIPHERALLY-ACTING OPIOID ANTAGONISTS - Peripherally-acting opioid antagonists can be orally administered to treat the side effects of opioid administration in convenient dosing schedules.06-30-2011
20100004275AGENT FOR SUPPRESSING DEVELOPMENT OF TOLERANCE TO NARCOTIC ANALGESICS - A medicament for suppressing development of tolerance to analgesic effect induced by administration of a narcotic analgesic such as morphine, which comprises an antagonist of the vasopressin receptor 1b as an active ingredient.01-07-2010
20120202839METHODS AND COMPOSITIONS FOR DETERRING ABUSE OF ORALLY ADMINISTERED PHARMACEUTICAL PRODUCTS - This invention relates to an abuse deterrent formulation of an oral dosage form of a therapeutically effective amount of any active drug substance that can be subject to abuse combined with a gel forming polymer, a nasal mucosal irritating surfactant and a flushing agent. Such a dosage form is intended to deter abuse of the active drug substance via injection, nasal inhalation or consumption of quantities of the dosage unit exceeding the usual therapeutically effective dose.08-09-2012
20120277260USE OF METHYLNALTREXONE AND RELATED COMPOUNDS TO TREAT CONSTIPATION IN CHRONIC OPIOID USERS - A method of preventing or treating constipation in a patient who has been chronically taking opioids, the method comprising administering a quaternary derivative of noroxymorphone in an amount sufficient to prevent or treat the side effect in the patient, but which amount would be insufficient to treat a patient with the same opioid-induced side effect who had not chronically been administered opioids.11-01-2012
20100210676Chemically Modified Small Molecules - Methods of modifying the rate of systemic absorption of a drug administered to a subject by a pulmonary route, the method comprising covalently conjugating a hydrophilic polymer to a drug, wherein the drug has a half-life of elimination from the lung of less than about 180 minutes, to form a drug-polymer conjugate, wherein the drug-polymer conjugate has a net hydrophilic character and a weight average molecular weight of from about 50 to about 20,000 Daltons, and wherein the half-life of elimination from the lung of the drug-polymer conjugate is at least about 1.5-fold greater than the half-life of elimination from the lung of the drug, wherein the half-life of elimination from the lung is measured by bronchoalveolar lavage followed by assaying residual lung material.08-19-2010
20110053971NALMEFENE DI-ESTER PRODRUGS - 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.03-03-2011
20110028505COMPOSITIONS AND METHODS FOR REDUCING FOOD CRAVINGS - Disclosed are compositions for reducing food cravings, comprising a first compound and a second compound, where the first compound is an opioid antagonist and the second compound is an α-MSH agonist. Also disclosed are methods of reducing food cravings, comprising identifying an individual in need thereof and treating that individual to antagonize opioid receptor activity and to enhance α-MSH activity.02-03-2011
20100286186NOVEL DICARBOXYLIC ACID LINKED AMINO ACID AND PEPTIDE PRODRUGS OF OPIOIDS AND USES THEREOF - The present invention concerns dicarboxylic acid linked amino acid and peptide prodrugs of opioid analgesics and pharmaceutical compositions containing such prodrugs. Methods for providing pain relief, decreasing the adverse GI side effects of the opioid analgesic and increasing the bioavailability of the opioid analgesic with the aforementioned prodrugs are also provided. In one embodiment, prodrugs having the amino acid side chains of valine, leucine, isoleucine and glycine; and mono-, di- and tripeptides thereof are provided.11-11-2010
20120302592TOPIRAMATE PLUS NALTREXONE FOR THE TREATMENT OF ADDICTIVE DISORDERS - The present invention provides for the use of combinations of drugs to treat addictive disorders.11-29-2012
20120302590METHODS AND COMPOSITIONS TO PREVENT ADDICTION - Disclosed herein is a method of reducing or preventing the development of aversion to a CNS stimulant in a subject comprising, administering a therapeutic amount of the neurological stimulant and administering an antagonist of the kappa opioid receptor, to thereby reduce or prevent the development of aversion to the CNS stimulant in the subject. Also disclosed is a method of reducing or preventing the development of addiction to a CNS stimulant in a subject, comprising, administering the CNS stimulant and administering a mu opioid receptor antagonist to thereby reduce or prevent the development of addiction to the CNS stimulant in the subject. Also disclosed are pharmaceutical compositions comprising a central nervous system stimulant and an opioid receptor antagonist. Examples of central nervous system stimulants (such as methylphenidate) and opioid receptor antagonists (such as naltrexone) are provided.11-29-2012
20120302591METHODS OF USING 8-CARBOXAMIDO-2,6-METHANO-3-BENZAZOCINES - 8-Substituted-2,6-methano-3-benzazocines of general structure I in which A is —CH11-29-2012
20110136847High Concentration Formulations of Opioids and Opioid Derivatives - The present invention provides opioid formulations suitable for long-term delivery to a subject. The formulation of the invention comprises an opioid or opioid derivative (e.g., morphine, hydromorphone, fentanyl or a fentanyl congener), and an aqueous solvent comprising a low molecular weight carboxylic acid (e.g., C06-09-2011
20100324078Crystalline Forms of Naltrexone Methobromide - The present invention relates to novel crystalline forms of naltrexone methobromide including hydrated and solvated forms. The invention also describes methods of preparing the various crystalline forms. The present invention also relates to pharmaceutical compositions containing crystalline forms of naltrexone methobromide, as well as methods of treating or preventing opioid induced side effects by administering the pharmaceutical compositions.12-23-2010
20110086874Methods of Converting a Patient's Treatment Regimen from Intravenous Administration of an Opioid to Oral Co-Administration of Morphine and Oxycodone Using a Dosing Algorithm to Provide Analgesia - A method of converting a treatment for pain comprising intravenous administration of opioids, to a treatment for pain comprising oral administration of a first dose of an immediate release morphine-oxycodone combination in patients in need of analgesia. The method may comprise (1) determining a four-hour average oral morphine equivalents or determining a net average hourly intravenous dose, and (2) orally administering to the patient a first dose of a morphine-oxycodone combination in a 3:2 ratio by weight every four to six hours. Also, a method of treating pain in patients who had been administered opioids intravenously, comprising using a dosing algorithm to determine the first dose of the immediate release morphine-oxycodone combination.04-14-2011
20110178114TOPICAL REGIONAL NEURO-AFFECTIVE THERAPY - A method of treating a disease state or condition in humans via topical brainstem afferent stimulation therapy via the administration of a drug to the back of the neck of a human patient at the hairline in close proximity to and under or on the area of skin above the brain stem to provide regional neuro-affective therapy is disclosed.07-21-2011
20090203722Novel compositions and methods for enhancing potency or reducing adverse side effects of opiold agonists - The invention generally relates to novel compositions and methods with an opioid agonist and an opioid antagonist to differentially dose a human subject so as to either enhance analgesic potency without attenuating an adverse side effect of the agonist, or alternatively maintain the analgesic potency of the agonist while attenuating an adverse side effect of the agonist. The invention additionally relates to novel opioid compositions and methods for the gender-based dosing of men and women.08-13-2009
20110190331PERIPHERAL OPIOID RECEPTOR ANTAGONISTS AND USES THEREOF - The present invention provides a compound of formula I: wherein R08-04-2011
20100022574Methods to Treat Pain Using an Alpha-2 Adrenergic Agonist and an Endothelin Antagonist - The present invention relates, in general to treatment of pain comprising administering an alpha-2 adrenergic agonist and an endothelin antagonist, wherein administration of the agents acts as an analgesic and ameliorates pain in a subject.01-28-2010
20080214592METHODS OF TREATING ANXIETY DISORDERS - Disclosed are methods of treating an anxiety disorder, e.g., obsessive compulsive disorder, in an individual, comprising identifying an individual in need thereof and treating that individual to antagonize opioid receptor activity and to restore normal monoaminergic tone within the synapse.09-04-2008
20090030026Sustained release formulations of nalbuphine - Sustained release formulations of nalbuphine or pharmaceutically acceptable salts thereof; methods for making the sustained release formulations of nalbuphine or pharmaceutically acceptable salts thereof; and methods for using the sustained release formulations of nalbuphine or pharmaceutically acceptable salts thereof to treat patients suffering from pain are provided.01-29-2009
20090258891Macrocyclic Compounds As Antiviral Agents - The present invention relates to macrocyclic compounds of formula (I): wherein W, n, R10-15-2009
20110136849PROCESS FOR REDUCING CONTAMINATING MICHAEL ACCEPTOR LEVELS IN OXYCODONE AND OTHER COMPOSITIONS - The present invention relates to processes for removal of Michael acceptors from certain compositions wherein the composition is treated with a thiol-containing compound under conditions sufficient to remove Michael acceptors and the resulting thiol-Michael adducts. Certain embodiments of the present invention enable quantification and/or removal of Michael acceptors and/or Michael acceptor precursors.06-09-2011
20120178774TOLL-LIKE RECEPTOR MODULATORS AND USES THEREOF - The present invention provides a compound selected from the group consisting of:07-12-2012
20110065742Immediate release compositions and methods for delivering drug formulations using weak acid ion exchange resins in abnormally high PH environments - Immediate release compositions and methods for delivering drug formulations using weak acid ion exchange resins in abnormally high pH environments.03-17-2011
20110306627Morphinan Compounds - 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 σ12-15-2011
20110306628NON-PEPTIDYL, POTENT, AND SELECTIVE MU OPIOID RECEPTOR ANTAGONISTS - 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.12-15-2011
20090209569SELECTIVE OPIOID COMPOUNDS - The present invention relates to compounds of Formula I or II, or pharmaceutically acceptable salts, esters, or prodrugs thereof:08-20-2009
20100152221PHARMACEUTICAL COMPOSITION - Provided herein is a pharmaceutical composition comprising an antagonist, an agonist, a seal coat, and a sequestering polymer, wherein the antagonist, agonist, seal coat and at least one sequestering polymer are all components of a single unit, and wherein the seal coat forms a layer physically separating the antagonist from the agonist from one another. Methods for manufacturing such a pharmaceutical composition are also provided. Methods for treating pain using such compositions is also demonstrated.06-17-2010
20120010232COMPOSITIONS FOR AFFECTING WEIGHT LOSS - Disclosed are compositions for affecting weight loss comprising a first compound and a second compound, where the first compound is an opioid antagonist and the second compound causes increased agonism of a melanocortin 3 receptor (MC3-R) or a melanocortin 4 receptor (MC4-R) compared to normal physiological conditions. Also disclosed are methods of affecting weight loss, increasing energy expenditure, increasing satiety in an individual, or suppressing the appetite of an individual, comprising identifying an individual in need thereof and treating that individual to antagonize opioid receptor activity and to enhance α-MSH activity.01-12-2012
20090270438Novel compositions and formulations - There is provided according to the invention a non-pressurised pharmaceutical liquid solution spray composition comprising: (i) buprenorphine; and a solvent comprising ethanol which composition is substantially free of chloride. There is also provided according to the invention a non-pressurised pharmaceutical liquid solution spray formulation comprising: (i) buprenorphine; (ii) a solvent comprising ethanol; and (iii) one or more antioxidants each of a molar ratio of antioxidant:buprenorphine between 0.2:1 and 25:1.10-29-2009
20110166171SUSTAINED RELEASE MONOEXIMIC FORMULATIONS OF OPIOID AND NONOPIOID ANALGESICS - The present invention relates to monoeximic solid dosage forms for administering pharmaceutical agents, particularly Hydrocodone and acetaminophen, methods for preparing said dosage forms, and methods for providing therapeutic agents to patients in need of treatment.07-07-2011
20090069363Therapeutic Agent for Constipation - A therapeutic and/or prophylactic agent for constipation induced by a compound having an opioid μ receptor agonist activity, which agent comprises as an effective ingredient a compound having an opioid δ receptor antagonist activity, e.g., a compound of Formula (I):03-12-2009
20120022093CRYSTALLINE FORMS OF OXYMORPHONE HYDROCHLORIDE - The present invention is directed to crystalline forms of oxymorphone hydrochloride.01-26-2012
20120059025DRY POWDER COMPOUND FORMULATIONS AND USES THEREOF - The present invention provides lyophilized formulations comprising methylnaltrexone, and processes for preparation of provided formulations. Additionally provided are compositions and products containing the methylnaltrexone formulation, as well as methods for producing formulations, compositions and products. Provided formulations as well as compositions and products containing methylnaltrexone formulations are useful for preventing, treating delaying, diminishing or reducing the severity and/or incidence of side effects resulting from administration of analgesic opioids.03-08-2012
20120059024DRUG ABUSE DETERRENT, METHODS AND COMPOSITIONS - The present invention relates generally to the field of pain management. More particularly, the present invention relates to analgesic combinations of an opioid and flupirtine or retigabine which reduce the risk of substance abuse in pain management. Such combinations are referred to as abuse-deterrent fixed dose combinations (FDC).03-08-2012
20120065220Tamper Resistant Dosage Form Comprising An Anionic Polymer - A pharmaceutical dosage form and method of using same, the pharmaceutical dosage form exhibiting a breaking strength of at least 500 N, said dosage form containing 03-15-2012
20110046172 Medicinal Compositions - A composition, in parenteral unit dosage form or in a unit dosage form suitable for delivery via the dermis or mucosa, comprises buprenorphine and an amount of naloxone such that the ratio by weight of buprenorphine to naloxone delivered to or reaching the plasma of a patient is in the range of from 7.5:1 to 12.4:1. The analgesic action of the buprenorphine is potentiated by the low dose of naloxone, which also serves to reduce the likelihood of abuse of the composition by drug addicts. Also provided are a method of treatment of pain and the use of naloxone and buprenorphine for the manufacture of a medicament.02-24-2011
20110086873Methods of Converting a Patient's Treatment Regimen from Intravenous Administration of an Opioid to Oral Co-Administration of Morphine and Oxycodone Using a Dosing Algorithm to Provide Analgesia - A method of converting a treatment for pain comprising intravenous administration of opioids, to a treatment for pain comprising oral administration of a first dose of an immediate release morphine-oxycodone combination in patients in need of analgesia. The method may comprise (1) determining a four-hour average oral morphine equivalents or determining a net average hourly intravenous dose, and (2) orally administering to the patient a first dose of a morphine-oxycodone combination in a 3:2 ratio by weight every four to six hours. Also, a method of treating pain in patients who had been administered opioids intravenously, comprising using a dosing algorithm to determine the first dose of the immediate release morphine-oxycodone combination.04-14-2011
20120309779METHODS AND COMPOSITIONS COMPRISING SEQUENTIAL ADMINISTRATION OF OPIOID RECEPTOR AGONISTS - Methods and compositions for the alleviation of pain in a patient. The methods and compositions sequentially administer a therapeutically effective amount of first compound having opioid receptor agonist activity, followed by a therapeutic effective amount of a second or subsequent compound(s) having opioid receptor agonist activity, one or more non-opioid analgesic compounds or one or more hybrid opioid compounds, or mixtures thereof. The methods and compositions effectively alleviate pain with a lower incidence of opioid-induced side effects.12-06-2012
20110065743KAPPA OPIOID RECEPTOR LIGANDS - 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.03-17-2011
20120252832ABUSE-RESISTANT CONTROLLED-RELEASE OPIOID DOSAGE FORM - 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 an immediate release product as a single dose. The controlled release nature of the tablet 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.10-04-2012
20120316191Peripheral Opioid Receptor Antagonists and Uses Thereof - The present invention provides a compound of formula I:12-13-2012
20120316190Modulation of Cell Barrier Dysfunction - The invention provides prophylactic and therapeutic methods for administering a μ-opioid receptor antagonist, e.g., N-methylnaltrexone or a salt thereof, to treat cell barrier diseases and disorders, such as endothelial and epithelial cell barrier diseases and disorders, e.g., inflammatory bowel disease. Methods of reducing the symptoms of inflammatory bowel disease and the risk of developing inflammatory bowel disease are also provided.12-13-2012
20120316189METHODS AND COMPOSITIONS FOR REDUCING THE RISK ASSOCIATED WITH THE ADMINISTRATION OF OPIOID ANALGESICS IN PATIENTS DIAGNOSED OR UNDIAGNOSED RESPIRATORY ILLNESS - The present invention relates to methods for reducing the risk associated with the administration of opioid analgesics in patient diagnosed or undiagnosed with respiratory illness by administering an analgesic composition comprising a sub-analgesic dosage of a p-opioid agonist selected from the group consisting a morphine, fentanyl, sufentanil, alfentanil, oxymorphone and hydromorphone, or a pharmaceutically acceptable salt thereof, and a sub-analgesic dosage of oxycodone which is a κ2-opioid agonist or a pharmaceutically acceptable salt thereof.12-13-2012
20090131466Pharmaceutical Compositions - Provided herein is a pharmaceutical composition comprising an antagonist, an agonist, a seal coat, and a sequestering polymer, wherein the antagonist, agonist, seal coat and at least one sequestering polymer are all components of a single unit, and wherein the seal coat forms a layer physically separating the antagonist from the agonist from one another. Methods for manufacturing such a pharmaceutical composition are also provided.05-21-2009
20110184008CRYSTALLINE FORMS OF AN 8-AZABICYCLO[3.2.1]OCTANE COMPOUND - The invention provides a crystalline sulfate salt of 3-endo-(8-{2-[cyclohexylmethyl-((S)-2,3-dihydroxy-propionyl)amino]ethyl}-8-aza-bicyclo[3.2.1]oct-3-yl)benzamide or a solvate thereof. The invention also provides pharmaceutical compositions comprising such crystalline salt forms, methods of using such crystalline salt forms to treat diseases associated with mu opioid receptor activity, and processes useful for preparing such crystalline salt forms.07-28-2011
20110184007PHARMACEUTICAL COMPOSITIONS CONFIGURED TO DETER DOSAGE FORM SPLITTING - An oral pharmaceutical composition comprising a drug and one or more pharmaceutically acceptable excipients in a monolithic dosage form, wherein the dosage form is configured such that when the dosage form is divided into more than one piece and at least one of the pieces is administered to a subject the Cmax, AUC, and/or rate of drug released after administration is substantially the same or lower and the Tmax is higher than the Cmax, AUC, rate of drug released, and/or Tmax after administration of: (1) a comparable composition in intact dosage form of equal drug dosage of the administered at least one piece; (2) a bioequivalent drug composition in an intact dosage form of equal drug dosage to the administered at least one piece; and (3) a divided piece of a bioequivalent drug composition, wherein the divided piece comprises a drug dosage equal to the dosage of the administered piece of the oral composition. Methods of making the same and methods of using the same are also provided.07-28-2011
20090312358METHOD FOR MANAGEMENT OF DIARRHEA - The present invention is directed to methods of treatment and/or management of diarrhea, such as chronic diarrhea using sequential administration of opioid agonists to suppress gut mobility and opioid antagonists to reverse the effect to controllably allow bowel movements. The agonists and antagonists are administered with a time interval in between the administration or between the release of the drugs from a pharmaceutical composition. The invention is further directed to methods of controlling, treating or managing side effects caused by the opioid agonists, specifically the side effects resulting from mast cell activation and/or granulation.12-17-2009
20120165360AMINO- AND AMIDO-AMINOTETRALIN DERIVATIVES AND RELATED COMPOUNDS AS MU OPIOID RECEPTOR ANTAGONISTS - The invention provides amino- and amido-aminotetralin compounds of formula (I):06-28-2012
20120165359Opioid Agonist/Antagonist Combinations - The invention is directed in part to oral dosage forms comprising a combination of an orally analgesically effective amount of an opioid agonist and an orally active opioid antagonist, the opioid antagonist being included in a ratio to the opioid agonist to provide a combination product which is analgesically effective when the combination is administered orally, but which is aversive in a physically dependent subject. Preferably, the amount of opioid antagonist included in the combination product provides at least a mildly negative, “aversive” experience in physically dependent addicts (e.g., precipitated abstinence syndrome).06-28-2012
20120165358CONTROLLED RELEASE FORMULATIONS OF OPIOID AND NONOPIOID ANALGESICS - Sustained release dosage forms for twice daily oral dosing to a human patient for providing relief from pain are provided. The sustained release dosage form comprises an immediate release component and a sustained release component, wherein the immediate release component and the sustained release component collectively contain a therapeutically effective amount of an opioid analgesic and a therapeutically effective amount of nonopioid analgesic. In a preferred embodiment, the nonopioid analgesic is acetaminophen and the opioid analgesic is hydrocodone and pharmaceutically acceptable salts thereof, and in preferred embodiments, the pharmaceutically acceptable salt is bitartrate. The dosage forms produce plasma profiles in a patient characterized by a Cmax for hydrocodone of between about 0.6 ng/mL/mg to about 1.4 ng/mL/mg and an AUC for hydrocodone of between about 9.1 ng*hr/mL/mg to about 19.9 ng*hr/mL/mg (per mg hydrocodone bitartrate administered) and a Cmax for acetaminophen of between about 2.8 ng/mL/mg and 7.9 ng/mL/mg and an AUC for acetaminophen of between about 28.6 ng*hr/mL/mg and about 59.1 ng*hr/mL/mg (per mg acetaminophen administered) after a single dose.06-28-2012
20120129879Compounds and Compositions for Use in Phototherapy and in Treatment of Ocular Neovascular Disease and Cancers - The invention relates generally to anti-angiogenesis agents and related methods of using to anti-angiogenesis agents for biomedical applications including direct monotherapy and combination therapy for treatment of an angiogenesis related condition. In an embodiment, the invention provides a class of opioid compounds and structurally related opioid derivatives exhibiting anti-VEGF activity for use in therapeutic procedures, including phototherapy. Opioid compounds and structurally related opioid derivatives of the invention may be administered alone or in combination with administration of a phototherapy agent and/or other therapeutic agent.05-24-2012
20120214833SOLID DISPERSION OF RIFAXIMIN - A solid dispersion of rifaximin comprising rifaximin and pharmaceutically acceptable carrier. A pharmaceutical composition comprising the solid dispersion of rifaximin.08-23-2012
20100204259IMMEDIATE RELEASE COMPOSITION RESISTANT TO ABUSE BY INTAKE OF ALCOHOL - The present invention provides immediate release pharmaceutical compositions for oral administration that are resistant to abuse by intake of alcohol.08-12-2010
20130172381ORAL DOSAGE FORMS FOR OXYGEN-CONTAINING ACTIVE AGENTS AND OXYL-CONTAINING POLYMER - The disclosed invention is drawn to pharmaceutical tablets that provide delivery of active agents having at least three oxygen-containing groups, as well as a second active ingredient. Non-limiting examples of three oxygen-containing group active agents include guaifenesin, codeine, hydrocodone, and their pharmaceutically acceptable salts. In one embodiment, a pharmaceutical tablet for oral administration once every 12 hours is provided. The tablet includes a first active agent that is a tri-oxy active agent, a second active agent, and a release rate controlling non-ionic oxyl-containing hydrophilic polymer. The total oxyl content of the hydrophilic polymer in the tablet is about 4×1007-04-2013
20130172382ABUSE-RESISTANT CONTROLLED-RELEASE OPIOID DOSAGE FORM - 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 an immediate release product as a single dose. The controlled release nature of the tablet 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.07-04-2013
20120136020TREATMENT OF EFFECT OF CHEMICALS WITH THEIR ULTRADILUTE STEREOISOMERS - A method of treating an effect of a chemical agent, which agent is characterized by one or more chiral centres, by administering a dilution or an ultra-high dilution or potentised preparation of a stereoisomer of said chemical agent.05-31-2012
20120136021OXIDATION-STABILIZED TAMPER-RESISTANT DOSAGE FORM - A thermoformed pharmaceutical dosage form having a breaking strength of at least 300 N, 05-31-2012
20120136019(S)-N-METHYLNALTREXONE - This invention relates to S-MNTX, methods of producing S-MNTX, pharmaceutical preparations comprising S-MNTX and methods for their use.05-31-2012
20120136022GASTRIC RETENTIVE EXTENDED-RELEASE DOSAGE FORMS COMPRISING COMBINATIONS OF A NON-OPIOID ANALGESIC AND AN OPIOID ANALGESIC - Compositions and methods for the treatment of pain in a mammal are described. More specifically, a dosage form designed for release of acetaminophen and an opioid is described, wherein the dosage form provides delivery of the drugs to the upper gastrointestinal tract (“GI”) of a mammal for an extended period of time.05-31-2012
20100261744PHARMACEUTICAL FORMULATION - Stable pharmaceutical compositions useful for administering methylnaltrexone are described, as are methods for making the same. Kits, including these pharmaceutical compositions, also are provided.10-14-2010
20120252831COMPOSITIONS OF OPIOID ANTAGONISTS AND METHODS FOR TREATING SCLERODERMA THEREWITH - Provided are compositions comprising opioid antagonists, such as naltrexone naloxone, or nalmefene, or their pharmaceutically acceptable salts, and methods for treating scleroderma, including systemic sclerosis, therewith.10-04-2012
20120172387OPIOIDS FOR THE TREATMENT OF THE RESTLESS LEG SYNDROME - The present invention relates to an opioid controlled release oral dosage form comprising at least one opioid for the manufacture of a medicament to treat patients with restless leg syndrome (RLS).07-05-2012
20100273821METHODS AND COMPOSITIONS FOR TREATING DRY EYE - This invention relates to treatment of dry eye. In particular, the invention relates to methods and formulations for treating dry eye based on topical application of opioid antagonists such as naltrexone.10-28-2010
20100280059COMPOSITIONS COMPRISING AN ANTIHISTAMINE, ANTITUSSIVE AND DECONGESTANT IN EXTENDED RELEASE FORMULATIONS - The invention provides oral formulations for the treatment of cold and allergy symptoms. Each formulation combines an antihistamine, an antitussive, and/or a decongestant into one extended release composition. The invention further provides for methods of making and using such formulations, as well as for methods for preventing abuse or extraction of a single drug present in an oral extended release composition comprising two or more of an antihistamine, antitussive, and/or decongestant.11-04-2010
20120178773Compositions Comprising Enzyme-Cleavable Oxycodone Prodrug - The embodiments provide Compound KC-7, N-1-[(S)-2-(oxycodone-6-enol-carbonyl-methyl-amino)-2-carbonyl-sarcosine-ethyl amine]-arginine-glycine-acetate, or acceptable salts, solvates, and hydrates thereof. The present disclosure also provides compositions, and their methods of use, where the \compositions comprise a prodrug, Compound KC-7, that provides controlled release of oxycodone. Such compositions can optionally provide a trypsin inhibitor that interacts with the enzyme that mediates the controlled release of oxycodone from the prodrug so as to attenuate enzymatic cleavage of the prodrug.07-12-2012
20120178772Compositions Comprising Enzyme-Cleavable Oxycodone Prodrug - The embodiments provide Compound KC-8, N-1-[3-(oxycodone-6-enol-carbonyl-methyl-amino)-2,2-dimethyl-propylamine]-arginine-glycine-malonic acid, or acceptable salts, solvates, and hydrates thereof. The present disclosure also provides compositions, and their methods of use, where the compositions comprise a prodrug, Compound KC-8, that provides controlled release of oxycodone. Such compositions can optionally provide a trypsin inhibitor that interacts with the enzyme that mediates the controlled release of oxycodone from the prodrug so as to attenuate enzymatic cleavage of the prodrug.07-12-2012
20120178771Oral Pharmaceutical Compositions of Buprenorphine and Method of Use - The present invention is directed to oral, therapeutically effective pharmaceutical compositions of buprenorphine and it pharmaceutically acceptable salts and the use thereof, including delayed onset and controlled release dosage forms. The present invention is also directed delayed onset, rapid release dosage forms and delayed onset, extended release dosage forms of oral buprenorphine which provide robust efficacy and reduced potential for abuse and misuse.07-12-2012
20100010031TRANSORAL DOSAGE FORMS COMPRISING SUFENTANIL AND NALOXONE - The invention pertains to methods that include administering to a subject a transoral dosage form comprising a pharmaceutical carrier and sufentanil, and maintaining a mean pH ranging from about 3.5 to about 5.5 during a dosing period after administration of the transoral dosage form as determined using an in vitro donor media test. Related dosage forms are also disclosed. Also disclosed are transoral dosage forms and related methods, wherein a transoral dosage form may comprise: (1) about 5 to about 1000 micrograms of sufentanil; (2) about 50 micrograms to about 100 milligrams of naloxone; and (3) acidifying material in an amount sufficient to provide a mean pH ranging from about 3.5 to about 5.5 during a dosing period after administration of the transoral dosage form as determined using an in vitro donor media test; wherein the dosing period begins no earlier than about 1 minute after administration of the transoral dosage form, and ends no later than about 120 minutes after administration of the transoral dosage form.01-14-2010
20100010030EXTENDED RELEASE HYDROCODONE ACETAMINOPHEN AND RELATED METHODS AND USES THEREOF - The present invention generally provides a method of treatment and improvement of quality of life for patients adversely affected by various pain conditions. One preferred embodiment provides a method of treatment of acute pain, moderate to moderately severe pain, chronic pain, non-cancer pain, osteoarthritic pain, bunionectomy pain or lower back pain in a patient in need thereof, comprising providing at least one or two dosage form having about 15 mg of hydrocodone and its salt and about 500 mg of acetaminophen, once, twice or thrice daily. Preferably, the dosage form is about 30 mg of hydrocodone and about 1000 mg of acetaminophen taken twice daily. Alternatively, the dosage form is about 15 mg of hydrocodone and about 500 mg of acetaminophen taken twice daily.01-14-2010
20100010029Acute Pain Medications Based on Fast Acting Diclofenac-Opioid Combinations - Provided are combined oral dosage forms for the treatment of pain, particularly combined dosage forms that are specially formulated for rapid bioavailability, and that contain diclofenac potassium and an opioid selected from hydrocodone, oxycodone, fentanyl and tramadol.01-14-2010
20120083506REDUCTION OF OPIOID BLOOD FLUCTUATIONS - The present invention relates to the use of a sustained release matrix containing at least one opioid for producing a solid oral formulation in table form suitable for reducing blood concentration fluctuations of said opioid.04-05-2012
20120083505Use of opioid receptor antagonists for acute treatment of paraphilic arousal states - The present invention is directed to an opioid receptor antagonist or a pharmaceutically acceptable salt thereof for use in a method of acute treatment of paraphilic sexual arousal states in patients suffering from paraphilia.04-05-2012
20120225902METHODS FOR MAKING 3-O-PROTECTED MORPHINONES AND 3-O-PROTECTED MORPHINONE DIENOL CARBOXYLATES - 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 R09-06-2012
20120225901DOSAGE FORM CONTAINING OXYCODONE AND NALOXONE - The present invention concerns a dosage form comprising oxycodone and naloxone which is characterized by specific in vivo parameters such as t09-06-2012
20120190702USE OF METHYLNALTREXONE AND RELATED COMPOUNDS TO TREAT CONSTIPATION IN CHRONIC OPIOID USERS - A method of preventing or treating constipation in a patient who has been chronically taking opioids, the method comprising administering a quaternary derivative of noroxymorphone in an amount sufficient to prevent or treat the side effect in the patient, but which amount would be insufficient to treat a patient with the same opioid-induced side effect who had not chronically been administered opioids.07-26-2012
20090018154OPIOID AND METHODS OF MAKING AND USING THE SAME - An opioid derivative of oxymorphol, called 8-hydroxy-6-α-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-α-oxymorphol, and pharmaceutical compositions comprising 8-hydroxy-6-α-oxymorphol or pharmaceutically acceptable salts thereof and pharmaceutically acceptable carrier, are also provided.01-15-2009
20090012110MORPHINE COMPOUNDS FOR PHARMACEUTICAL COMPOSITIONS - The invention relates to new morphine compounds of the formula:01-08-2009
20120270895Intranasal Opioid Compositions - The present invention relates to pharmaceutical compositions for intranasal administration to a mammal that contain an effective amount of an opioid, a liquid nasal carrier for the opioid, and optionally a sweetener, flavoring agent or masking agent. In some embodiments of the present invention, the pharmaceutical compositions have improved bioavailability. In other embodiments of the present invention, the opioid compositions improve patient compliance.10-25-2012
20120270894Controlled Release of Phenolic Opioids - A method of providing a patient with controlled release of a phenolic opioid using a prodrug capable, upon enzymatic activation, of releasing the phenolic opioid through intra-molecular cyclization leading to formation of a cyclic urea, carbamate or thiocarbamate.10-25-2012
20100234413COMPOSITIONS AND METHODS FOR PROPHYLAXIS AND TREATMENT OF ADDICTIONS - The present invention relates to methods of treating or preventing addiction and relapse use of addictive agents, and treating or preventing addictive or compulsive behaviour and relapse practice of an addictive behaviour or compulsion, by administering a peroxisome proliferator-activated receptor gamma (PPARγ) agonist, alone or in combination with another therapeutic agent, such as, for example, an opioid receptor antagonist or an antidepressant, or an addictive agent, such as, for example, an opioid agonist. The present invention also includes pharmaceutical compositions for treating or preventing addiction or relapse that include a PPARγ agonist and one or more other therapeutic or addictive agents, as well as unit dosage forms of such pharmaceutical compositions, which contain a dosage effective in treating or preventing addiction or relapse. The methods and compositions of the invention are useful in the treatment or prevention of addiction to any agent, including alcohol, nicotine, marijuana, cocaine, and amphetamines, as well as compulsive and addictive behaviours, including pathological gambling and pathological overeating.09-16-2010
20120101118TAMPER RESISTANT DOSAGE FORMS - Tamper resistant controlled release formulations.04-26-2012
20120289534PACKAGE FOR IMPROVED TREATMENT OF CONDITIONS - The present invention provides an improved package from the administration of active ingredients. The present invention provides a package comprising: a standard portion comprising one or more active ingredients in a plurality of different potencies, and a rescue portion comprising one or more same or different active ingredients. The package may be optionally be used with a patient assessment module. The present invention also provides a kit comprising: a package comprising a standard portion comprising one or more active ingredients in a plurality of different potencies, and a patient assessment module comprising instructions for administration of the standard portion. The package may optionally further comprise a rescue portion.11-15-2012
20100168147Medicinal Compositions Comprising Buprenorphine And Naloxone - There is provided a composition for the treatment of pain in human patients wherein said composition comprises buprenorphine to naloxone in a ratio by weight of from 2.1:1 to 8:1, the amount of buprenorphine and naloxone being suitable to provide analgesia, the composition being in a transdermal or transmucosal dosage form. Also provided are an associated method and use.07-01-2010
20130012533CONTROLLED RELEASE OXYCODONE COMPOSITIONS - A method for preparing a solid oral dosage form comprising up to about 160 mg of oxycodone or a salt thereof to control pain in substantially all patients is disclosed. The method comprises wet granulating at least one hydrophilic or hydrophobic polymer, preferably a hydroxyalkyl cellulose or an alkyl cellulose, with oxycodone or a salt thereof to form a controlled-release matrix. Repeated “q12h” (i.e., every 12 hour) administration of the dosage form through steady-state conditions results in a mean maximum plasma concentration of oxycodone up to about 240 ng/ml from a mean of about 2 to about 4.5 hours after administration, and a mean minimum plasma concentration up to about 120 ng/ml from about 10 to about 14 hours after administration.01-10-2013
20100130524THERAPEUTIC OR PROPHYLACTIC AGENT FOR DYSKINESIA - An object of the present invention is to provide a drug with a high therapeutic or prophylactic effect on dyskinesia, without accompanying aggravation of symptoms of the primary disease, and with fewer side effects.05-27-2010
20120149724MODULATING ENDOGENOUS BETA-ENDORPHIN LEVELS - Systemic beta-endorphin can be elevated in response to cutaneous irradiation, including ultraviolet and ionizing radiation. Increases in systemic beta-endorphin levels associated with cutaneous irradiation can be modulated with opiate receptor antagonists, particularly compounds that antagonize opioid receptor binding by beta endorphin.06-14-2012
20130023553PEGYLATED OPIOIDS WITH LOW POTENTIAL FOR ABUSE AND SIDE EFFECTS - Provided are methods for reducing the addiction potential and/or reducing one or more CNS-side effects related to the administration of an opioid analgesic drug by administering the opioid analgesic drug in the form of an oligomeric polyethylene glycol conjugate compound. The compounds provided demonstrate notably reduced potential for substance abuse, and possess altered pharmacokinetic profiles relative to the opioid agonists alone, but are not subject to the risk of physical tampering that allows for the recovery and abuse of the opioid agonist associated with certain alternative delivery formulations.01-24-2013
20100087472USE OF METHYLNALTREXONE AND RELATED COMPOUND TO TREAT CONSTIPATION IN CHRONIC OPIOID USERS - A method of preventing or treating constipation in a patient who has been chronically taking opioids, the method comprising administering a quaternary derivative of noroxymorphone in an amount sufficient to prevent or treat the side effect in the patient, but which amount would be insufficient to treat a patient with the same opioid-induced side effect who had not chronically been administered opioids.04-08-2010
20080234307Novel 6-Amino-Morphinan Derivatives, Method of Manufacturing Them and Their Application as Analgesics - This invention relates to a class of 6-amino-morphinan compounds of formula (I) which can be used as highly active analgesics. This invention also relates to their pharmaceutically acceptable salts and easily accessible derivatives (e.g. esters or amides of the amino acid derivatives), to a process for their manufacture and their application in the manufacture of pharmaceutical specialties.09-25-2008
20080227805SUSTAINED RELEASE PARENTERAL FORMULATIONS OF BUPRENORPHINE - An oil-in-water buprenorphine formulation including buprenorphine and a surfactant that emulsifies the buprenorphine in oil, wherein the drug release is controlled by varying the oil concentration and/or pH. A buprenorphine aqueous suspension formulation including a free base buprenorphine and a suspension stabilizer. A buprenorphine oil formulation including a buprenorphine salt suspended in a pharmaceutically acceptable oil. Methods of providing sustained release of buprenorphine over a period of time.09-18-2008
20080227804Polymorphic Forms of Naltrexone - 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.09-18-2008
20080227803Indolomorphinan Derivative Having Carboxy in 6'-Position - A compound represented by the formula (I):09-18-2008
20080227802Agent For Suppressing Development of Tolerance to Narcotic Analgesics - A medicament for suppressing development of tolerance to analgesic effect induced by administration of a narcotic analgesic such as morphine, which comprises an antagonist of the vasopressin receptor 09-18-2008
20080221144Controlled Release Formulations - The present invention relates to controlled release transmucosal formulations which mediate absorption and methods of use comprising a pharmaceutically active agent, preferably morphine, and a water soluble polymer, chitosan, and preferably one more antioxidants, one or more antimicrobial agents, and water.09-11-2008
20080221143Morphine and Morphine Precursors - Methods and materials related to the use of morphine, morphine precursors (e.g., reticuline), and inhibitors of morphine synthesis or activity to treat diseases, to reduce inflammation, or to restore normal function are provided.09-11-2008
20130178492PHARMACEUTICAL COMPOSITIONS COMPRISING HYDROMORPHONE AND NALOXONE - The present invention relates to prolonged release pharmaceutical dosage forms, the manufacture thereof as well as their use for administration to human beings.07-11-2013
20130123292TRANSDERMALLY DELIVERABLE OPIOID PRODRUGS, ABUSE-RESISTANT COMPOSITIONS AND METHODS OF USING OPIOID PRODRUGS - 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.05-16-2013
20080207669(S)-N-Stereoisomers of 7,8-Saturated-4,5-Epoxy-Morphinanium Analogs - Novel (S)-N-stereoisomers of 7,8-saturated-4,5-epoxy-morphinanium analogs are disclosed. Pharmaceutical compositions containing the (S)-N-stereoisomers of 7,8-saturated-4,5-epoxy-morphinanium analogs and methods for their pharmaceutical uses are also disclosed. Such analogs are disclosed as being useful in treating, among varying conditions, hypermotility of the gastrointestinal tract.08-28-2008
20080207668PHARMACEUTICAL COMPOSITIONS OF HYDROMORPHONE FOR PREVENTION OF OVERDOSE OR ABUSE - The invention relates to compounds, compositions and methods comprised of a chemical moiety attached to hydromorphone. The invention provides embodiments that provide a decrease in the potential of hydromorphone to cause overdose or to be abused while still delivering therapeutic activity similar to that of the parent hydromorphone.08-28-2008
20080207667Use of nalbuphine and related compounds to treat symptoms of respiratory problems - The present invention relates to treatment of respiratory diseases. More specifically, the present invention relates to treatment of respiratory diseases in humans and lower animals with nalbuphine.08-28-2008
20130158061CONTROLLED RELEASE HYDROCODONE - 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.06-20-2013
201301580608-AZABICYCLO[3.2.1]OCTANE COMPOUNDS AS MU OPIOID RECEPTOR ANTAGONISTS - The invention provides novel 8-azabicyclo[3.2.1]octane compounds of formula (I):06-20-2013
20080200493Use of Oxycodone for Treating Visceral Pain - It is possible to effectively treat moderate to severe visceral pain by administering analgesic medications comprising the opioid oxycodone or pharmaceutically acceptable salts thereof. Visceral pain and especially acute (i.e. non-chronic) visceral pain can be effectively treated by administering oxycodone at a dosage which is lower than the corresponding dosage of other opioids like morphine.08-21-2008
20110275658OPIOID-CONTAINING ORAL PHARMACEUTICAL COMPOSITIONS AND METHODS - The present invention provides sustained-release oral pharmaceutical compositions and methods of use. The sustained-release oral pharmaceutical compositions include an opioid (including salts thereof) and a salt of a non-steroidal anti-inflammatory drug (NSAID).11-10-2011
20110237615Narcotic Drug Formulations with Decreased Abuse Potential - The present application relates to novel narcotic formulations having a decreased injection abuse potential In a representative embodiment, the formulation comprises methadone hydrochloride (09-29-2011
20110237614Pegylated Opioids with Low Potential for Abuse - The invention provides opioid agonists covalently bound to a water-soluble oligomer having reduced potential for substance abuse and uses thereof. The compounds of the invention possess altered pharmacokinetic profiles relative to the opioid agonists alone, but are not subject to the risk of physical tampering that allows for the recovery and abuse of the opioid agonist associated with certain alternative delivery formulations.09-29-2011
20130150395BENZOIC ACID, BENZOIC ACID DERIVATIVES AND HETEROARYL CARBOXYLIC ACID CONJUGATES OF HYDROMORPHONE, PRODRUGS, METHODS OF MAKING AND USE THEREOF - The presently described technology provides compositions comprising aryl carboxylic acids chemically conjugated to hydromorphone (4,5-α-epoxy-3-hydroxy-17-methyl morphinan-6-one) to form novel prodrugs/compositions of hydromorphone. The hydromorphone prodrugs of the present technology have decreased side effects and decreased potential for abuse compared to unconjugated hydromorphone. The present technology also provides methods of treating patients, pharmaceutical kits and methods of synthesizing conjugates of the present technology.06-13-2013
20100305147CHEMICALLY MODIFIED SMALL MOLECULES - 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.12-02-2010
20100317683Preparation of 6-Alpha-Amino N-Substituted Morphinans by Catalytic Hydrogen Transfer - The present invention provides processes for the stereoselective synthesis of 6-alpha-amino N-substituted morphinans. In particular, the invention provides processes for the reductive amination of 6-keto N-substituted morphinans by catalytic hydrogen transfer.12-16-2010
20100317682Single Dosage Unit Including Opioid and Methylnaltrexone or Methylnaltrexone Salt - The use of methylnaltrexone bromide in combination and in one dosage unit, with any opioid drug in order to prevent the constipation which can be associated with opioids.12-16-2010
20120283283METHODS FOR DETECTING ENHANCED RISK OF OPIOID-INDUCED HYPOXIA IN A PATIENT - Methods for detecting enhanced risk of opioid-induced respiratory dysfunction in patients with normal levels of oxygen saturation. The method may comprise: (1) assaying blood of the patient for a normal level of oxygen saturation; (2) measuring the patient's respiration rate at rest for a normal rate; and (3) correlating the normal level of oxygen saturation and the normal rate of respiration with enhanced risk of opioid-induced respiratory dysfunction if: (a) the patient is at an altitude of about 1000 feet above sea level or greater; or (b) the patient's oxygen saturation level is normal but no greater than about 95%; or (c) the patient received prior dosing with intravenous opioid and is converted to dosing with an oral opioid. The method may further comprise administering opioids to a patient after detecting whether there is an enhanced risk of opioid-induced respiratory dysfunction.11-08-2012
20110288113METHOD TO REDUCE OR ELMINATE THE USE BY A PATIENT OF A TOLERANCE-INDUCING PHARAMACOLOGICAL AGENT - A multiple total daily dose regimen is developed in order to decrease the use by a patient of a tolerance-inducing pharmacological agent. In one example, the method reduces or phases out altogether a patient's chronic use of opioid drugs by use of a successive reduction of the total daily dose of an opioid drug in sub-therapeutic decrements over the course of 3-7 days per therapeutic dose.11-24-2011
20110288112Method of Providing Sustained Analgesia With Buprenorphine - A method of effectively treating pain in humans is achieved by administering buprenorphine in accordance with first order kinetics over an initial three-day dosing interval, such that a maximum plasma concentration from about 20 pg/ml to about 1052 pg/ml is attained, and thereafter maintaining the administration of buprenorphine for at least an additional two-day dosing interval in accordance with substantially zero order kinetics, such that the patients experience analgesia throughout the at least two-day additional dosing interval.11-24-2011
20130190343COMPOSITIONS AND METHODS FOR MINIMIZING OR REVERSING AGONIST-INDUCED DESENSITIZATION - 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.07-25-2013
20130190342COMPOSITIONS OF BUPRENORPHINE AND ANTAGONISTS - The invention relates to a composition comprising buprenorphine and a μ opioid receptor antagonist, wherein the composition is characterized by an Agonist Antagonist Activity Index (AAnAI) of between about 0.7 and about 2.2; wherein;07-25-2013
20120029008CRYSTALLINE AND AMORPHOUS FORMS OF NALBUPHINE HYDROCHLORIDE - The present invention is directed to novel crystalline and amorphous forms of nalbuphine hydrochloride.02-02-2012
20120029007MORPHINAN COMPOUNDS - 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 σ02-02-2012
20130197020Method of Providing Sustained Analgesia With Buprenorphine - A method of effectively treating pain in humans is achieved by administering buprenorphine in accordance with first order kinetics over an initial three-day dosing interval, such that a maximum plasma concentration from about 20 pg/ml to about 1052 pg/ml is attained, and thereafter maintaining the administration of buprenorphine for at least an additional two-day dosing interval in accordance with substantially zero order kinetics, such that the patients experience analgesia throughout the at least two-day additional dosing interval.08-01-2013
20130197021COMBINATION OF ACTIVE LOADED GRANULES WITH ADDITIONAL ACTIVES - The present invention relates to prolonged release pharmaceutical dosage forms, the manufacture thereof as well as their use for administration to human being08-01-2013
20130203797THERAPEUTIC OR PROPHYLACTIC AGENT FOR BILIARY DISEASES - A therapeutic or prophylactic agent for biliary tract diseases includes as an effective component a specific compound having a morphinan skeleton represented by Compound 1, or a pharmaceutically acceptable acid addition salt thereof:08-08-2013
201200887873-CARBOXYPROPYL-AMINOTETRALIN DERIVATIVES AND RELATED COMPOUNDS AS MU OPIOID RECEPTOR ANTAGONISTS - The invention provides 3-carboxypropyl-aminotetralin compounds of formula (I):04-12-2012
20120088786IMMEDIATE RELEASE PHARMACEUTICAL COMPOSITIONS COMPRISING OXYCODONE AND NALOXONE - The present invention pertains to oral immediate release pharmaceutical compositions suitable for treating patients suffering from pain comprising oxycodone and naloxone or their pharmaceutically acceptable salts.04-12-2012

Patent applications in class One of the five cyclos is five-membered and includes ring chalcogen (e.g., codeine, morphine, etc.)