Narcotic Patents (Class 514/812)
  • Patent number: 8846090
    Abstract: The invention concerns a storage stable pharmaceutical formulation comprising preferably two active compounds in a non-swellable diffusion matrix, whereby the compounds are released from the matrix in a sustained, invariant and, if several compounds are present, independent manner and the matrix is determined with respect to its substantial release characteristics by ethylcellulose and at least one fatty alcohol. The invention also concerns methods for producing such pharmaceutical formulations.
    Type: Grant
    Filed: January 11, 2012
    Date of Patent: September 30, 2014
    Assignee: Euro-Celtique S.A.
    Inventors: Bianca Brögmann, Silke Muhlau, Christof Spitzley
  • Patent number: 8846091
    Abstract: The invention concerns a storage stable pharmaceutical formulation comprising preferably two active compounds in a non-swellable diffusion matrix, whereby the compounds are released from the matrix in a sustained, invariant and, if several compounds are present, independent manner and the matrix is determined with respect to its substantial release characteristics by ethylcellulose and at least one fatty alcohol. The invention also concerns methods for producing such pharmaceutical formulations.
    Type: Grant
    Filed: October 18, 2013
    Date of Patent: September 30, 2014
    Assignee: Euro-Celtique S.A.
    Inventors: Bianca Brögmann, Silke Mühlah, Christof Spitzley
  • Patent number: 8822518
    Abstract: Novel compounds which are antagonists or inverse agonists at one or more of the opioid receptors, pharmaceutical compositions containing them, to processes for their preparation.
    Type: Grant
    Filed: December 12, 2013
    Date of Patent: September 2, 2014
    Assignee: GlaxoSmithKline LLC
    Inventors: David John Cowan, Andrew Lamont Larkin, Cunyu Zhang, David Lee Musso, Gary Martin Green, Rodolfo Cadilla, Paul Kenneth Spearing, Michael Joseph Bishop, Jason Daniel Speake
  • Patent number: 8822487
    Abstract: The invention is directed in part to oral dosage forms comprising a combination of an opioid agonist, acetaminophen 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).
    Type: Grant
    Filed: December 7, 2012
    Date of Patent: September 2, 2014
    Assignee: Purdue Pharma L.P.
    Inventors: Robert F. Kaiko, Robert D. Colucci
  • Patent number: 8377479
    Abstract: Described herein are compositions comprising particles of poorly soluble drugs encapsulated by stabilizers. Further described are pharmaceutical compositions comprising such encapsulated compositions. Also described are methods of making such encapsulated particle compositions, and methods of making the corresponding pharmaceutical compositions. The encapsulated particle compositions described herein allow poorly soluble drugs to be administered with good bioavailability by routes that are non-invasive to patients, such as by oral administration.
    Type: Grant
    Filed: September 2, 2008
    Date of Patent: February 19, 2013
    Assignee: Nanotherapeutics, Inc.
    Inventor: James D. Talton
  • Patent number: 7968604
    Abstract: Provided is a pharmaceutical composition for prevention and treatment of drug or alcohol addiction or bipolar disorder, comprising sodium phenylbutyrate (PBA). The pharmaceutical composition for prevention and treatment of drug or alcohol addiction or bipolar disorder in accordance with the present invention provides effects capable of inhibiting increases in locomotor activity which is a behavioral indicator of drug or alcohol addiction or bipolar disorder, by controlling a level of a neurotransmitter via regulation of expression of a neurotransmitter transporter.
    Type: Grant
    Filed: August 30, 2006
    Date of Patent: June 28, 2011
    Inventors: Jeong-Woo Cho, Sang-Rak Choi, Sun-Gwan Hwang
  • Patent number: 7943631
    Abstract: The present invention relates a method of treating drug addiction in an individual by administering to the addicted individual a therapeutically effective amount of dextro-morphine capable of activating an opioid receptor. It is disclosed here that dextro-morphine is suitable for treating addiction to natural opiates, semi-synthetic opiates, fully synthetic opioids, and endogenous opioid peptides, as well as nicotine.
    Type: Grant
    Filed: February 20, 2008
    Date of Patent: May 17, 2011
    Assignee: MCW Research Foundation, Inc.
    Inventor: Leon F. Tseng
  • Patent number: 7402591
    Abstract: An analgesic composition in parenteral unit dosage form or in a unit dosage form suitable for delivery via the mucosa comprising an amount of buprenorphine which is less than the clinical dose required to achieve pain relief and an amount of naloxone such that the ratio by weight of buprenorphine to naloxone is in the range of from 12.5:1 to 27.5:1, or an amount of naltrexone or nalmefene such that the ratio by weight of buprenorphine to naltrexone or nalmefene is in the range of from 12.5:1 to 22.5:1. The analgesic action of the buprenorphine is potentiated by the low dose of naloxone, naltrexone or nalmefene.
    Type: Grant
    Filed: October 20, 2005
    Date of Patent: July 22, 2008
    Assignee: Reckitt Benckiser Healthcare (UK) Limited
    Inventors: Christopher Bourne Chapleo, Nicolas Calvert Varey, Keith McCormack
  • Patent number: 7255882
    Abstract: Benzodiazepine withdrawal induced anxiety is treated by administration of an enkephalinase inhibitor, and a gamma-aminobutyric acid (“GABA”) precursor, or an endorphin or enkephalin releaser. These components promote restoration of normal neurotransmitter function and are non-addictive. Use of the enkephalinase inhibitor D-phenylalanine, the GABA precursor glutamine, the serotonin precursor 5-HTP, glycine, and taurine, in combination with coenzymatic functionality of folic acid is preferred for activation of ligand-gated Cl? channel in the central nervous system. Food supplement embodiments provide the human body nutritional supplements to intake certain neurotransmitter precursor substrates, thereby enabling patients of all ages to self-regulate their ability to quell perturbations to equilibrium and simultaneously to adverse effects upon normal physiological and psychological functioning attributable to induced anxiety and panic associated with benzodiazepine withdrawal.
    Type: Grant
    Filed: October 29, 2004
    Date of Patent: August 14, 2007
    Inventors: Albert Howard Bieser, Terry Leo Neher
  • Patent number: 7074833
    Abstract: A method for treating or preventing a disorder or a condition by double inhibition of serotonin (5-HT) and noradrenaline (NA) reuptake in a subject in need thereof, while limiting the risks of cardiovascular disturbances and/or organ and/or tissue toxicity, comprising the step of administering to said subject a mixture of enantiomers of milnacipran enriched in the (1S,2R) enantiomer of milnacipran and/or of at least one of its metabolites, as well as their pharmaceutically-acceptable salts.
    Type: Grant
    Filed: March 22, 2004
    Date of Patent: July 11, 2006
    Assignee: Pierre Fabre Medicament
    Inventors: Jean Deregnaucourt, Richard Grosse
  • Patent number: 7026329
    Abstract: This invention relates to a method for selectively enhancing the analgesic potency of a bimodally-acting opioid agonist such as morphine and simultaneously attenuating anti-analgesia, hyperalgesia, hyperexcitability, physical dependence and/or tolerance effects associated with the administration of the bimodally-acting opioid agonist. The method of the present invention comprises administering to a subject an analgesic or sub-analgesic amount of a bimodally-acting opioid agonist such as morphine and an amount of an excitatory opioid receptor antagonist such as naltrexone or nalmefene effective to enhance the analgesic potency of the bimodally-acting opioid agonist and attenuate the anti-analgesia, hyperalgesia, hyperexcitability, physical dependence and/or tolerance effects of the bimodally-acting opioid agonist.
    Type: Grant
    Filed: December 13, 2002
    Date of Patent: April 11, 2006
    Assignee: Albert Einstein College of Medicine of Yeshiva University
    Inventors: Stanley M. Crain, Ke-fei Shen
  • Patent number: 7005452
    Abstract: The present invention concerns the use of a mixture of enantiomers enriched in the dextrogyral enantiomer of milnacipran and/or of at least one of its metabolites, as well as their pharmaceutically-acceptable salts, for the preparation of a drug intended to prevent or to treat disorders that can be managed by double inhibition of serotonin (5-HT) and norepinephrine (NE) reuptake, while limiting the risks of cardiovascular disturbances and/or organ and/or tissue toxicity.
    Type: Grant
    Filed: June 3, 2003
    Date of Patent: February 28, 2006
    Assignee: Pierre Fabre Medicament
    Inventors: Jean Deregnaucourt, Richard Grosse
  • Patent number: 6995169
    Abstract: An analgesic composition in parenteral unit dosage form or in a unit dosage form suitable for delivery via the mucosa comprising an amount of buprenorphine which is less than the clinical dose required to achieve pain relief and an amount of naloxone such that the ratio by weight of buprenorphine to naloxone is in the range of from 12.5:1 to 27.5:1, or an amount of naltrexone or nalmefene such that the ratio by weight of buprenorphine to naltrexone or nalmefene is in the range of from 12.5:1 to 22.5:1. The analgesic action of the buprenorphine is potentiated by the low dose of naloxone, naltrexone or nalmefene.
    Type: Grant
    Filed: May 14, 2002
    Date of Patent: February 7, 2006
    Assignee: Reckitt Benckiser Healthcare (UK) Limited
    Inventors: Christopher Bourne Chapleo, Nicolas Calvert Varey, Keith McCormack
  • Patent number: 6849253
    Abstract: Water-soluble borate-polyol complexes are useful as buffers and/or antimicrobials in aqueous ophthalmic compositions, including those containing polyvinyl alcohol. These compositions have greater antimicrobial activity than comparable compositions containing typical borate buffers and unexpectedly increase the antimicrobial efficacy of other antimicrobial agents when used in combination. In addition, use of the borate-polyol complexes avoids the incompatibility problem typically associated with the combination of borate buffer and polyvinyl alcohol; therefore, the compositions disclosed herein may also contain polyvinyl alcohol.
    Type: Grant
    Filed: November 22, 2002
    Date of Patent: February 1, 2005
    Assignee: Alcon Manufacturing, Ltd.
    Inventors: Masood Chowhan, Nissanke L. Dassanayake
  • Patent number: 6828349
    Abstract: The present invention provides a highly efficient method for treating substance addiction and for changing addiction-related behavior of a mammal suffering from substance addiction. The method includes administering to a mammal an effective amount of gamma vinylGABA or a pharmaceutically acceptable salt thereof. The present invention also provides a method of treatment of cocaine, morphine, heroin, nicotine, amphetamine, methamphetamine, or ethanol addiction by treating a mammal with an effective amount of gamma vinylGABA or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: November 9, 1998
    Date of Patent: December 7, 2004
    Assignee: Brookhaven Science Associates
    Inventors: Stephen L. Dewey, Jonathan D. Brodie, Charles R. Ashby, Jr.
  • Patent number: 6699474
    Abstract: Addictive drugs like cocaine, heroin or amphetamines are spreading in an epidemic manner in the western world and are an important factor in the spread of the acquired immune deficiency syndrome AIDS (multiple use of infected needles among drug addicts) the present invention describes a vaccine and immunoserum against drugs. The vaccine contains the drug bound to a carrier protein in order to produce antibodies against the drugs in the affected person. The use of the drug in the presence of the antibodies deactivates the drug. The desired drug effect is thus eliminated and the vicious circle between stimulation and application is broken.
    Type: Grant
    Filed: September 18, 1997
    Date of Patent: March 2, 2004
    Inventor: Erich Hugo Cerny
  • Patent number: 6696066
    Abstract: 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).
    Type: Grant
    Filed: September 16, 2002
    Date of Patent: February 24, 2004
    Assignee: Euro-Celtique S.A.
    Inventors: Robert F. Kaiko, Robert D. Colucci
  • Patent number: 6686370
    Abstract: Disclosed are compounds of the formula (I) wherein A, R1, R2, R3, R4 and X1 are as disclosed herein. The compounds have affinity for the ORL1 receptor and are useful in the treatment of chronic and acute pain.
    Type: Grant
    Filed: December 6, 2000
    Date of Patent: February 3, 2004
    Assignee: Euro-Celtique S.A.
    Inventors: Donald Kyle, R. Richard Goehring
  • Patent number: 6653354
    Abstract: The present invention relates to the use of xenon as a neuroprotectant and/or as an inhibitor of synaptic plasticity. In a preferred aspect, the xenon acts as an NMDA antagonist. The present invention also provides a method of reducing the level of activation of the NMDA receptors in a mammal, the method comprising modulating the activity of the NMDA receptor by administering to the mammal a therapeutically effective amount of xenon, wherein said reduction achieves neuroprotection and/or an inhibition of synaptic plasticity. A further embodiment of the invention provides a pharmaceutical composition for providing neuroprotection and/or inhibition of synaptic plasticity, together with a process for the preparation thereof.
    Type: Grant
    Filed: June 14, 2001
    Date of Patent: November 25, 2003
    Assignee: Protexeon Limited
    Inventors: Nicholas Peter Franks, Mervyn Maze
  • Patent number: 6627635
    Abstract: The invention relates in part to a method of reducing the abuse potential of an oral dosage form of an opioid analgesic, wherein an analgesically effective amount of an orally active opioid agonist is combined with an opioid antagonist into an oral dosage form which would require at least a two-step extraction process to be separated from the opioid agonist, the amount of opioid antagonist including being sufficient to counteract opioid effects if extracted together with the opioid agonist and administered parenterally.
    Type: Grant
    Filed: March 22, 2001
    Date of Patent: September 30, 2003
    Assignee: Euro-Celtique S.A.
    Inventors: Philip J. Palermo, Robert F. Kaiko, Robert D. Colucci
  • Patent number: 6617361
    Abstract: A protocol for prevention of Alzheimer's disease onset is described. The protocol involves stimulating the implicit memory, followed by continuing such stimulation in conjunction with psychological treatments followed by continuing said stimulation of the implicit memory and, in addition, stimulating the explicit memory. Use of this protocol results in a permanent replacement of undesirable behaviors with desirable ones.
    Type: Grant
    Filed: November 13, 2001
    Date of Patent: September 9, 2003
    Assignee: Be Able, LLC
    Inventor: Mark H. Eig
  • Patent number: 6608064
    Abstract: The present invention is directed to the use of certain pyrido[1,2-a]-pyrazine derivatives, also described as bis-azabicyclic compounds and defined by the formula (I) herein, in the treatment of Parkinson's disease, attention deficit hyperactivity disorder and microadenomas in mammals, and to related compositions.
    Type: Grant
    Filed: May 3, 2001
    Date of Patent: August 19, 2003
    Assignee: Pfizer Inc
    Inventors: Stafford McLean, Stevin H. Zorn, Elisa R. Jackson
  • Patent number: 6593367
    Abstract: The present invention provides a method for changing addiction-related behavior of a mammal suffering from addiction to a combination of abused drugs. The method includes administering to the mammal an effective amount of gamma vinylGABA (GVG) or a pharmaceutically acceptable salt thereof, or an enantiomer or a racemic mixture thereof, wherein the effective amount is sufficient to diminish, inhibit or eliminate behavior associated with craving or use of the combination of abused drugs.
    Type: Grant
    Filed: July 28, 1999
    Date of Patent: July 15, 2003
    Assignee: Brookhaven Science Associates
    Inventors: Stephen L. Dewey, Jonathan D. Brodie, Charles R. Ashby, Jr.
  • Patent number: 6541520
    Abstract: The present invention provides a highly efficient method for treating substance addiction and for changing addiction-related behavior of a mammal suffering from substance addiction. The method includes administering to a mammal an effective amount of gamma vinylGABA or a pharmaceutically acceptable salt thereof. The present invention also provides a method of treatment of cocaine, morphine, heroin, nicotine, amphetamine, methamphetamine, or ethanol addiction by treating a mammal with an effective amount of gamma vinylGABA or a pharmaceutically acceptable salt thereof. In one embodiment, the method of the present invention includes administering to the mammal an effective amount of a composition which increases central nervous system GABA levels wherein the effective amount is sufficient to diminish, inhibit or eliminate behavior associated with craving or use of drugs of abuse.
    Type: Grant
    Filed: December 11, 1998
    Date of Patent: April 1, 2003
    Assignee: Brookhaven Science Associates
    Inventors: Stephen L. Dewey, Jonathan D. Brodie, Charles R. Ashby, Jr.
  • Patent number: 6495155
    Abstract: An injectable slow-release partial opioid agonist or opioid antagonist formulation is provided comprising a partial opioid agonist or opioid antagonist in a poly(D,L-lactide) excipient with a small amount of residual ethyl acetate. Upon intramuscular injection of the composition, a partial opioid agonist or opioid antagonist is released in a controlled manner over an extended period of time. The composition finds use in the treatment of heroin addicts and alcoholics to reduce consumption of the abused substances. Of particular interest are the drugs buprenorphine, methadone and naltrexone.
    Type: Grant
    Filed: August 25, 2000
    Date of Patent: December 17, 2002
    Assignee: Southern Research Institute
    Inventors: Thomas R. Tice, Jay K. Staas, Teresa M. Ferrell, Peter Markland
  • Patent number: 6492369
    Abstract: A method for preventing or treating drug dependence comprising administering to a human in need thereof a pharmaceutically effective amount of a 1,4-(diphenylalkyl)piperazine compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, wherein R1 is lower alkoxy; R2 is lower alkoxy; A is lower alkylene and B is lower alkylene;
    Type: Grant
    Filed: May 7, 2001
    Date of Patent: December 10, 2002
    Assignee: Santen Pharmaceutical Co., Ltd.
    Inventors: Tsutomu Suzuki, Shiro Mita, Kiyoshi Matsuno
  • Patent number: 6475494
    Abstract: 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).
    Type: Grant
    Filed: March 22, 2001
    Date of Patent: November 5, 2002
    Assignee: Euro-Celtique S.A.
    Inventors: Robert F. Kaiko, Robert D. Colucci
  • Patent number: 6468987
    Abstract: An enteral nutritional product for a person having ulcerative colitis contains in combination (a) an oil blend which contains eicosapentaenoic acid (20:5n3) and/or docosahexaenoic acid (22:6n3), and (b) a source of indigestible carbohydrate which is metabolized to short chain fatty acids by microorganisms present in the human colon. Preferably the nutritional product also contains one or more nutrients which act as antioxidants.
    Type: Grant
    Filed: September 14, 1999
    Date of Patent: October 22, 2002
    Assignee: Abbott Laboratories
    Inventors: Stephen Joseph Demichele, Keith Allen Garleb, John William McEwen, Martha Kay Fuller
  • Patent number: 6375957
    Abstract: The invention is directed in part to oral dosage forms comprising a combination of an opioid agonist, acetaminophen 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).
    Type: Grant
    Filed: February 11, 2000
    Date of Patent: April 23, 2002
    Assignee: Euro-Celtique, S.A.
    Inventors: Robert F. Kaiko, Robert D. Colucci
  • Patent number: 6365636
    Abstract: Water-soluble borate-polyol complexes are useful as buffers and/or antimicrobials in aqueous ophthalmic compositions, including those containing polyvinyl alcohol. These compositions have greater antimicrobial activity than comparable compositions containing typical borate buffers and unexpectedly increase the antimicrobial efficacy of other antimicrobial agents when used in combination. In addition, use of the borate-polyol complexes avoids the incompatibility problem typically associated with the combination of borate buffer and polyvinyl alcohol; therefore, the compositions disclosed herein may also contain polyvinyl alcohol.
    Type: Grant
    Filed: June 20, 2000
    Date of Patent: April 2, 2002
    Assignee: Alcon Manufacturing, Ltd.
    Inventors: Masood Chowhan, Nissanke L. Dassanayake
  • Patent number: 6352984
    Abstract: Methods and compositions are disclosed utilizing olanzapine-N-oxide for the treatment of psychosis in humans. Olanzapine-N-oxide exhibits a lessened liability toward drug-drug interactions than olanzapine and a more predictable dosing regimen than olanzapine. Olanzapine-N-oxide is also useful for the treatment of acute mania, mild anxiety states, anxiety disorders, schizophrenia, bipolar disorder, attention deficit hyperactivity disorder, autistic disorder, excessive aggression, substance abuse, depressive signs and symptoms, tic disorder, functional bowel disorder and fungal dermatitis.
    Type: Grant
    Filed: August 7, 2000
    Date of Patent: March 5, 2002
    Assignee: Sepracor Inc.
    Inventor: William E. Yelle
  • Patent number: 6333357
    Abstract: A protocol for permanent modification of behavior and elimination of undesired habits is described. The protocol involves stimulating the implicit memory, followed by continuing such stimulation in conjunction with psychological treatments followed by continuing said stimulation of the implicit memory and, in addition, stimulating the explicit memory. Use of this protocol results in a permanent replacement of undesirable behaviors with desirable ones.
    Type: Grant
    Filed: November 5, 1999
    Date of Patent: December 25, 2001
    Assignee: Be Able, LLC
    Inventor: Mark H. Eig
  • Patent number: 6306425
    Abstract: An injectable slow-release naltrexone formulation is provided comprising naltrexone in a poly(D,L-lactide) matrix with a small amount of residual ethyl acetate. Upon intramuscular injection of the composition, naltrexone is released in a controlled manner over an extended period of time. The composition finds use in the treatment of heroin addicts and alcoholics to reduce consumption of the abused substances.
    Type: Grant
    Filed: April 7, 2000
    Date of Patent: October 23, 2001
    Assignee: Southern Research Institute
    Inventors: Thomas R. Tice, Jay K. Staas, Teresa M. Ferrell
  • Patent number: 6288047
    Abstract: A method of treating an individual with an immune system with decreased activity by administering an effective amount of a lipid preparation derived from a natural source and enriched to contain at least 10% (w/w) phosphatidic acid (PA) is disclosed.
    Type: Grant
    Filed: March 23, 2000
    Date of Patent: September 11, 2001
    Assignee: Modus Biological Membranes Ltd.
    Inventors: Meir Shinitzky, Avner Shenfeld
  • Patent number: 6277384
    Abstract: 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).
    Type: Grant
    Filed: December 22, 1998
    Date of Patent: August 21, 2001
    Assignee: Euro-Celtique S.A.
    Inventors: Robert F. Kaiko, Robert D. Colucci
  • Patent number: 6274633
    Abstract: The present invention relates to the use of xenon as an NMDA antagonist. In particular, the invention relates to a method of treatment comprising modulating the activity of an NMDA receptor in a mammal, the method comprising modulating the activity of the NMDA receptor by administering to the mammal a therapeutically effective amount of xenon. In a further aspect, the invention provides a process for the preparation of a pharmaceutical composition suitable for modulating the activity of an NMDA receptor.
    Type: Grant
    Filed: August 23, 1999
    Date of Patent: August 14, 2001
    Assignee: Imperial College of Science, Technology, and Medicine
    Inventors: Nicholas Peter Franks, Mervyn Maze
  • Patent number: 6228863
    Abstract: The invention relates in part to a method of reducing the abuse potential of an oral dosage form of an opioid analgesic, wherein an analgesically effective amount of an orally active opioid agonist is combined with an opioid antagonist into an oral dosage form which would require at least a two-step extraction process to be separated from the opioid agonist, the amount of opioid antagonist including being sufficient to counteract opioid effects if extracted together with the opioid agonist and administered parenterally.
    Type: Grant
    Filed: December 22, 1998
    Date of Patent: May 8, 2001
    Assignee: Euro-Celtique S.A.
    Inventors: Philip J. Palermo, Robert D. Colucci, Robert F. Kaiko
  • Patent number: 6204284
    Abstract: The invention is a method of treatment for the relief of an addictive, compulsive disorder which comprises the administration to a human or animal suffering from such a disorder an effective amount of the compound of the formula: wherein R is hydrogen, alkyl (C1-C6); R1 is hydrogen, mono or disubstituted halogen, alkoxy (C1-C3), CF3, alkyl (C1-C6); and R2 is hydrogen, methyl or ethyl, or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: March 31, 1995
    Date of Patent: March 20, 2001
    Assignee: American Cyanamid Company
    Inventors: Bernard Beer, Joseph William Epstein
  • Patent number: 6203813
    Abstract: The present invention provides an opiate antagonist implant which is an admixture of an opiate antagonist, in either acid or base form, and a pharmaceutically acceptable carrier. The admixture is uniformly compressed into a subcutaneously implantable pellet which is effective to release levels of the opiate antagonist over desired amounts of time when subcutaneously implanted in a patient to effectively inhibit the effects of a number of addictive drugs.
    Type: Grant
    Filed: October 9, 1998
    Date of Patent: March 20, 2001
    Inventor: Lance L. Gooberman
  • Patent number: 6197827
    Abstract: The present invention encompasses methods of treating patients for tobacco addiction and nicotine addiction, for palliating the effects of nicotine withdrawal, for providing or facilitating the effects of smoking cessation therapies and as long-term smoking cessation maintenance therapy. The invention also includes related pharmaceutical compositions comprising nicotine receptor antagonists and either an anti-depressant or an anti-anxiety drug. Specific combinations of drugs (mecamylamine HCl and bupropion HCl) as well as mecamylamine in combination with certain drug classes (e.g., anti-anxiety drugs and anti-depressants) comprise the pharmaceutical compositions disclosed. These compositions are also contemplated for use in the treatment of cocaine addiction and the treatment of alcohol dependence.
    Type: Grant
    Filed: November 16, 1999
    Date of Patent: March 6, 2001
    Assignee: Cary Medical Corporation
    Inventor: Douglas D. Cary
  • Patent number: 6159963
    Abstract: The invention provides a method for treating substance abuse comprising administering an effective amount of olanzapine or pharmaceutically acceptable salt thereof to a patient in need thereof.
    Type: Grant
    Filed: November 25, 1997
    Date of Patent: December 12, 2000
    Assignee: Eli Lilly and Company
    Inventors: Charles M Beasley, Kurt Rasmussen, Gary D Tollefson
  • Patent number: 6143278
    Abstract: The invention is directed to methods and pharmaceutical compositions for the topical administration of opioid analgesic drugs such as morphine. In particular, the invention relates to topical administration of an opioid analgesic agent, e.g., morphine sulfate, in admixture with a skin- or mucosal-specific penetration enhancer, to produce a localized analgesic effect in inflamed or non-inflamed skin or mucosal tissue, and without a transdermal or transmucosal migration of opioid agent, e.g., into the systemic circulation.
    Type: Grant
    Filed: February 23, 1998
    Date of Patent: November 7, 2000
    Inventor: George F. Elkhoury
  • Patent number: 6121259
    Abstract: Methods and compositions are disclosed utilizing olanzapine-N-oxide for the treatment of psychosis in humans. Olanzapine-N-oxide exhibits a lessened liability toward drug-drug interactions than olanzapine and a more predictable dosing regimen than olanzapine. Olanzapine-N-oxide is also useful for the treatment of acute mania, mild anxiety states, anxiety disorders, schizophrenia, bipolar disorder, attention deficit hyperactivity disorder, autistic disorder, excessive aggression, substance abuse, depressive signs and symptoms, tic disorder, functional bowel disorder and fungal dermatitis.
    Type: Grant
    Filed: November 22, 1999
    Date of Patent: September 19, 2000
    Assignee: Sepracor Inc.
    Inventor: William E. Yelle
  • Patent number: 6103766
    Abstract: Compounds of Formula I and their pharmaceutically acceptable salts having selective dopamine D3 receptor activity suitable for treating central nervous system disorders. Formula I: ##STR1## R.sub.1 is independently H or a C.sub.1 -C.sub.8 alkyl including isomeric forms thereof;R.sub.2 is H, C.sub.1 -C.sub.3 alkyl, a halogen, OCH.sub.3 , OCF.sub.3, CF.sub.3, CN, SCH.sub.3 or NHCOCH.sub.3 ; andR.sub.3 is H, C.sub.1 -C.sub.3 alkyl, a halogen, OCH.sub.3 , OCF.sub.3, CF.sub.3, CN, SCH.sub.3 or NHCOCH.sub.3.
    Type: Grant
    Filed: May 7, 1999
    Date of Patent: August 15, 2000
    Assignee: Pharmacia & Upjohn Company
    Inventors: Arthur Glenn Romero, Jeffrey A. Leiby
  • Patent number: 6103703
    Abstract: Disclosed herein is a method for reducing stimulant dependencies in mammals that involves administration of a therapeutically-effective amount of a cytosine-containing or cytidine-containing compound, such as CDP-choline.
    Type: Grant
    Filed: April 27, 1999
    Date of Patent: August 15, 2000
    Assignee: The McLean Hospital Corporation
    Inventors: Perry F. Renshaw, Scott Lukas
  • Patent number: 6087356
    Abstract: Methods for rapid detoxification of patients addicted to opioid narcotics are provided. The methods include administering nalmefene to induce acute withdrawal, and administering dextromethorphan with nalmefene or other opioid antagonists to reduce the patient's subjective feelings of residual withdrawal symptoms following detoxification. In one method of rapid detoxification, unconsciousness is induced by anesthetizing the patient with desflurane.
    Type: Grant
    Filed: May 25, 1999
    Date of Patent: July 11, 2000
    Inventor: David Lew Simon
  • Patent number: 6083962
    Abstract: A method of treating and reducing a drug dependency such as a nicotine dependency is provided. The method comprises initially administering to a subject a drug, such as nicotine or another agonist of the drug in an amount which would normally provide the desired pharmacologic effects and at least partially satiate the needs for the drug by a user. The method also comprises administering to the subject an antagonist to the drug or its other agonist in an amount sufficient to at least partially block the pharmacologic defects of the drug or its other agonist while there is a substantial amount of the drug or other agonist present in the system of the user. In one embodiment of the invention, the drug and the antagonist are administered substantially simultaneously so as to occupy a substantial portion of the receptors of the user for that drug thereby blocking or attenuating the effects of any further intake of the drug or other agonist.
    Type: Grant
    Filed: April 10, 1997
    Date of Patent: July 4, 2000
    Assignee: Robert J. Schaap
    Inventors: Jed E. Rose, Edward D. Levin
  • Patent number: 6068981
    Abstract: A method of monitoring a therapeutic regimen in an animal, the method involving a) providing to the animal a therapeutic compound and a detectable compound that passes into the bloodstream, excretory system, or other tissue or body fluid in detectable form; b) after a period of time, following step (a), sufficient for passage of a detectable amount of the detectable compound into the body fluid or tissue, collecting a sample of the fluid or tissue from the animal; and c) measuring or detecting the detectable compound, or a detectable metabolite thereof, in the sample, wherein the detectable compound involves one member of a specific binding pair, and detection is carried out using the second member of the specific binding pair.
    Type: Grant
    Filed: October 3, 1997
    Date of Patent: May 30, 2000
    Assignee: Biocode, Inc.
    Inventors: James H. Rittenburg, Frank G. Angella, Michael G. Pappas
  • Patent number: RE39300
    Abstract: Nontoxic substances that block the N-methyl-D-aspartate (NMDA) receptor, e.g., a morphinan such as dextromethorphan or dextrorphan, or that block a major intracellular consequence of NMDA-receptor activation, e.g., a ganglioside such as GM1 or GT1b, a phenothiazine such as trifluoperazine or a naphthalenesulfonamide such as N-(6-aminohexyl)-5-chloro-1-naphthalenesulfonamide, inhibit the development of tolerance to and/or dependence on addictive drugs, e.g., narcotic analgesics such as morphine, codeine, etc.
    Type: Grant
    Filed: June 15, 2001
    Date of Patent: September 19, 2006
    Assignee: Virginia Commonwealth University Medical College of Virginia
    Inventors: David J. Mayer, Jianren Mao
  • Patent number: RE43879
    Abstract: The present invention concerns the use of a mixture of enantiomers enriched in the dextrogyral enantiomer of milnacipran and/or of at least one of its metabolites, as well as their pharmaceutically-acceptable salts, for the preparation of a drug intended to prevent or to treat disorders that can be managed by double inhibition of serotonin (5-HT) and norepinephrine (NE) reuptake, while limiting the risks of cardiovascular disturbances and/or organ and/or tissue toxicity.
    Type: Grant
    Filed: February 27, 2012
    Date of Patent: December 25, 2012
    Assignee: Pierre Fabre Medicament
    Inventors: Jean Deregnaucourt, Richard Grosse