US Patent No: 7,749,542

Number of patents in Portfolio can not be more than 2000

Opioid agonist/antagonist combinations

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Abstract

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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).

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First Claim

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Patent Owner(s)

Patent OwnerAddressTotal Patents
PURDUE PHARMA L.P.STAMFORD, CT367

International Classification(s)

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Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Colucci, Robert D Newtown, US 20 1297
Kaiko, Robert F Weston, US 45 2123

Cited Art Landscape

Patent Info (Count) # Cites Year
 
Other [Check patent profile for assignment information] (5)
5,376,662 Method of attenuating nerve injury induced pain 67 1993
2004/0092,542 Tamper-resistant oral opioid agonist formulations 48 2003
2005/0095,291 Tamper-resistant oral opioid agonist formulations 59 2003
2005/0181,046 Tamper-resistant oral opioid agonist formulations 48 2003
2006/0039,970 Tamper-resistant oral opioid agonist formulations 35 2003
 
NOVA PHARMACEUTICAL CORPORATION (2)
4,760,069 Oximes of oxymorphone, naltrexone and naloxone as potent, selective opioid receptor agonists and antagonists 81 1985
4,889,860 Oximes of oxymorphone, naltrexone and naloxone as potent, selective opioid receptor agonists and antagonists 86 1987
 
The Lynx Project Limited (1)
6,310,072 Production of analgesic synergy by co-administration of sub-analgesic doses of a MU opioid agonist and a kappa-2 opioid agonist 64 1997
 
VIRGINIA COMMONWEALTH UNIVERSITY (4)
5,352,683 Method for the treatment of chronic pain 110 1993
5,321,012 Inhibiting the development of tolerance to and/or dependence on a narcotic addictive substance 165 1993
5,502,058 Method for the treatment of pain 145 1994
5,556,838 Inhibiting the development of tolerance to and/or dependence on an addictive substance 149 1994
 
NATIONAL INSTITUTES OF HEALTH (NIH), U.S. DEPT. OF HEALTH AND HUMAN SERVICES (DHHS), U.S. GOVERNMENT (1)
5,225,440 Attenuation of the opioid withdrawal syndrome by inhibitors of nitric oxide synthase 72 1991
 
Eli Lilly and Company (1)
5,998,434 Composition for treating pain 60 1998
 
SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCH (1)
4,803,208 Opiate agonists and antagonists 69 1985
 
ICN HUNGARY RT. (1)
5,317,022 Pharmaceutical composition and use 72 1992
 
G. D. Searle & Co. (1)
5,616,601 1,2-aryl and heteroaryl substituted imidazolyl compounds for the treatment of inflammation 144 1995
 
SCULLY SCOTT MURPHY & PRESSER, PC (1)
5,426,112 Growth regulation and related applications of opioid antagonists 118 1993
 
BAKER NORTON PHARMACEUTICALS, INC. (1)
4,873,076 Method of safely providing anesthesia or conscious sedation 80 1989
 
OMEROS CORPORATION (2)
5,858,017 Urologic irrigation solution and method for inhibition of pain, inflammation and spasm 123 1996
5,860,950 Arthroscopic irrigation solution and method for inhibition of pain and inflammation 111 1996
 
COLMAN PRODUCTS LIMITED (1)
4,935,428 Treating opiate dependence 94 1988
 
PEPTECH LIMITED (1)
5,534,492 Muramyl peptide for the treatment of toxicity 62 1995
 
The Rockefeller University (3)
4,987,136 Method for controlling gastrointestinal dysmotility 128 1986
4,769,372 Method of treating patients suffering from chronic pain or chronic cough 125 1986
4,785,000 Method of treating patients suffering from chronic pain or chronic cough 90 1987
 
ADIR ET COMPAGNIE (1)
5,130,311 Oxazolopyridine compounds, compositions and use 74 1991
 
Schaap; Robert J. (2)
5,316,759 Agonist-antagonist combination to reduce the use of nicotine and other drugs 90 1992
5,574,052 Agonist-antagonist combination to reduce the use of nicotine and other drugs 148 1994
 
E. I. DU PONT DE NEMOURS AND COMPANY (2)
4,451,470 Analgesic, antagonist, and/or anorectic 14-fluoromorphinans 81 1982
5,593,994 Prostaglandin synthase inhibitors 92 1994
 
BRISTOL-MYERS SQUIBB COMPANY (1)
4,457,933 Prevention of analgesic abuse 143 1981
 
DYNAGEN, INC. (1)
5,486,362 Controlled, sustained release delivery system for treating drug dependency 124 1993
 
MERCK SHARP & DOHME LTD. (1)
5,880,132 Tachykinin antagonist and an opioid analgesic effective at treating pain or nociception 72 1997
 
Warner-Lambert Company (1)
5,149,538 Misuse-resistive transdermal opioid dosage form 193 1991
 
The University of Chicago (4)
4,719,215 Quaternary derivatives of noroxymorphone which relieve nausea and emesis 105 1986
4,861,781 Quaternary derivatives of noroxymorphone which relieve nausea and emesis 99 1987
5,102,887 Method for reducing emesis and nausea induced by the administration of an emesis causing agent 98 1990
5,972,954 Use of methylnaltrexone and related compounds 116 1997
 
UNITED BIOMEDICAL, INC. (1)
5,633,259 Method for identification of low/non-addictive opioid analgesics and the use of said analgesics for treatment of opioid addiction 66 1995
 
University of Oregon (1)
5,514,680 Glycine receptor antagonists and the use thereof 93 1993
 
MERCK FROSST COMPANY (1)
5,474,995 Phenyl heterocycles as cox-2 inhibitors 184 1994
 
CONTRAL CLINICS OY (3)
4,882,335 Method for treating alcohol-drinking response 92 1988
5,096,715 Method and means for treating alcoholism by extinguishing the alcohol-drinking response using a transdermally administered opiate antagonist 73 1989
5,086,058 Method for treating alcoholism with nalmefene 88 1990
 
ALZA CORPORATION (4)
4,573,995 Transdermal therapeutic systems for the administration of naloxone, naltrexone and nalbuphine 162 1984
5,236,714 Abusable substance dosage form having reduced abuse potential 125 1988
5,460,826 Morphine therapy 127 1994
5,866,164 Composition and dosage form comprising opioid antagonist 177 1997
 
YOUNG, JACQUELINE, MS. (1)
5,356,900 Method of treating chronic herpes virus infections using an opiate receptor antagonist 70 1993
 
SIMON, DAVID L. (1)
6,103,258 Salts and bases of the 17-(Cyclopropylmethyl)-4,5 alpha-epoxy-6-Methylenemorphinan-3,14 diol molecule for optimizing dopamine homeostasis during administration of opioid analgesics 59 1998
 
MERCK FROSST CANADA LTD. (10)
5,409,944 Alkanesulfonamido-1-indanone derivatives as inhibitors of cyclooxygenase 96 1993
5,604,260 5-methanesulfonamido-1-indanones as an inhibitor of cyclooxygenase-2 113 1993
5,436,265 1-aroyl-3-indolyl alkanoic acids and derivatives thereof useful as anti-inflammatory agents 114 1993
5,521,213 Diaryl bicyclic heterocycles as inhibitors of cyclooxygenase-2 123 1994
5,552,422 Aryl substituted 5,5 fused aromatic nitrogen compounds as anti-inflammatory agents 132 1995
5,536,752 Phenyl heterocycles as COX-2 inhibitors 109 1995
5,550,142 Phenyl heterocycles as cox-2 inhibitors 113 1995
5,510,368 N-benzyl-3-indoleacetic acids as antiinflammatory drugs 115 1995
5,604,253 N-benzylindol-3-yl propanoic acid derivatives as cyclooxygenase inhibitors 102 1995
5,639,780 N-benzyl indol-3-yl butanoic acid derivatives as cyclooxygenase inhibitors 101 1995
 
EURO-CELTIQUE S.A. (36)
4,366,310 Controlled release compositions 77 1980
4,443,428 Extended action controlled release compositions 126 1982
4,940,587 Oral pharmaceutical composition through mucosa 122 1986
4,844,907 Pharmaceutical composition comprising analgesic and anti-inflammatory agent 145 1986
4,834,965 Controlled release pharmaceutical composition 104 1987
4,867,985 Spheroids 100 1988
5,071,646 Pharmaceutical ion exchange resin composition 138 1989
5,091,189 Controlled release dosage forms having a defined water content 56 1991
5,215,758 Controlled release matrix suppository for pharmaceuticals 111 1991
5,324,351 Aqueous dispersions of zein and preparation thereof 124 1992
5,356,467 Controlled release coatings derived from aqueous dispersions of zein 192 1993
5,500,227 Immediate release tablet cores of insoluble drugs having sustained-release coating 181 1993
5,622,722 Spheroid formulation 55 1994
5,508,043 Controlled release matrix for pharmaceuticals 69 1995
5,670,172 Pharmaceutical spheroid formulation 93 1995
6,024,982 Immediate release tablet cores of insoluble drugs having sustained-release coating 128 1995
5,811,126 Controlled release matrix for pharmaceuticals 108 1995
5,763,452 Pharmaceutical compositions and usages 54 1996
5,849,240 Method of preparing sustained release pharmaceutical compositions 153 1996
5,891,471 Pharmaceutical multiparticulates 138 1996
5,601,845 Pharmaceutical spheroid formulation 101 1996
5,843,480 Controlled release diamorphine formulation 111 1996
5,879,705 Sustained release compositions of morphine and a method of preparing pharmaceutical compositions 146 1997
5,908,848 Synergistic composition of codine and ibuprofen to treat arthritis 56 1997
5,942,241 Formulations and methods for providing prolonged local anesthesia 157 1997
6,068,855 Pharmaceutical composition containing a fusible carrier and method for producing the same 84 1997
5,965,163 Substained release compositions and a method of preparing pharmaceutical compositions 148 1997
6,077,532 Pharmaceutical ion exchange resin composition 63 1998
6,306,438 Stabilized sustained release tramadol formulations 83 1998
6,399,096 Pharmaceutical formulation 96 1998
6,143,328 Sustained release compositions and a method of preparing pharmaceutical compositions 73 1999
6,162,467 Sustained release compositions and a method of preparing pharmaceutical compositions 118 1999
6,210,714 Immediate release tablet cores of acetaminophen having sustained-release coating 93 2000
6,387,404 Immediate release tablet cores of insoluble drugs having sustained-release coating 108 2001
6,716,449 Controlled-release compositions containing opioid agonist and antagonist 106 2001
6,627,635 Method of preventing abuse of opioid dosage forms 122 2001
 
PURDUE PHARMA L.P. (39)
4,828,836 Controlled release pharmaceutical composition 210 1987
4,834,985 Controlled release pharmaceutical composition 224 1987
4,990,341 Controlled release hydromorphone composition 162 1989
5,266,331 Controlled release oxycodone compositions 217 1991
5,273,760 Stabilized controlled release substrate having a coating derived from an aqueous dispersion of hydrophobic polymer 233 1991
5,286,493 Stabilized controlled release formulations having acrylic polymer coating 230 1992
5,549,912 Controlled release oxycodone compositions 211 1993
5,472,712 Controlled-release formulations coated with aqueous dispersions of ethylcellulose 215 1993
5,478,577 Method of treating pain by administering 24 hour oral opioid formulations exhibiting rapid rate of initial rise of plasma drug level 222 1993
5,411,745 Powder-layered morphine sulfate formulations 141 1994
5,965,161 Extruded multi-particulates 169 1994
5,639,476 Controlled release formulations coated with aqueous dispersions of acrylic polymers 489 1995
5,508,042 Controlled release oxycodone compositions 229 1995
5,968,551 Orally administrable opioid formulations having extended duration of effect 230 1995
5,958,459 Opioid formulations having extended controlled released 144 1995
5,656,295 Controlled release oxycodone compositions 196 1996
5,681,585 Stabilized controlled release substrate having a coating derived from an aqueous dispersion of hydrophobic polymer 131 1996
5,672,360 Method of treating pain by administering 24 hour oral opioid formulations 212 1996
6,143,322 Method of treating humans with opioid formulations having extended controlled release 154 1997
5,958,452 Extruded orally administrable opioid formulations 197 1997
5,968,547 Method of providing sustained analgesia with buprenorphine 106 1997
6,077,533 Powder-layered oral dosage forms 80 1998
6,228,863 Method of preventing abuse of opioid dosage forms 187 1998
* 6,277,384 Opioid agonist/antagonist combinations 124 1998
6,103,261 Opioid formulations having extended controlled release 148 1999
6,335,033 Melt-extrusion multiparticulates 120 1999
6,261,599 Melt-extruded orally administrable opioid formulations 159 1999
6,294,195 Orally administrable opioid formulations having extended duration of effect 143 1999
6,375,957 Opioid agonist/opioid antagonist/acetaminophen combinations 183 2000
6,696,088 Tamper-resistant oral opioid agonist formulations 143 2001
* 6,475,494 Opioid agonist/antagonist combinations 108 2001
2003/0069,263 Pharmaceutical combinations of oxycodone and naloxone 69 2002
2003/0073,714 Opioid agonist formulations with releasable and sequestered antagonist 66 2002
* 6,696,066 Opioid agonist/antagonist combinations 143 2002
2003/0229,111 Naltrexone hydrochloride compositions 30 2003
2004/0186,121 Tamper-resistant oral opioid agonist formulations 55 2003
* 7,172,767 Opioid agonist / antagonist combinations 89 2003
2006/0182,801 Sequestered antagonist formulations 56 2006
* 7,419,686 Opioid agonist/antagonist combinations 55 2006
 
EUROCELTIQUE S.A., 122, BOULEVARD DE LA PETRUSSE, LUXEMBOURG (2)
4,844,909 Controlled release hydromorphone composition 155 1987
4,844,910 Spheroids 65 1987
 
McGinnis; Carolyn (1)
4,608,376 Opiate agonists and antagonists 65 1982
 
Aminotek Sciences, Inc. (1)
5,256,669 Methods and compositions for treating acute or chronic pain and drug addiction 73 1992
 
University of Kentucky Research Foundation (1)
4,464,378 Method of administering narcotic antagonists and analgesics and novel dosage forms containing same 198 1981
 
The United States of America as represented by the Secretary of the Army (1)
5,834,477 Opiate analgesic formulation with improved safety 57 1994
 
GENERAL ELECTRIC COMPANY (1)
5,226,331 Apparatus and method for measuring the particle number rate and the velocity distribution of a sprayed stream 47 1991
 
RUTGERS, STATE UNIVERSITY OF NEW JERSEY, THE, OLD QUEEN BUILDING, SOMERSET AND GEORGE STREETS, NEW BRUNSWICK, NJ 08903 (1)
4,806,341 Transdermal absorption dosage unit for narcotic analgesics and antagonists and process for administration 154 1986
 
ALBERT EINSTEIN COLLEGE OF MEDICINE OF YESHIVA UNIVERSITY (12)
5,472,943 Method of simultaneously enhancing analgesic potency and attenuating dependence liability caused by morphine and other opioid agonists 118 1993
5,585,348 Use of excitatory opioid receptor antagonists to prevent growth factor-induced hyperalgesia 90 1993
* 5,512,578 Method of simultaneously enhancing analgesic potency and attenuating dependence liability caused by exogenous and endogenous opiod agonists 113 1994
5,624,932 Method for identification of low/non-addictive opioid analgesics and the use of said analgesics for treatment of opioid addiction 64 1995
* 5,580,876 Method of simultaneously enhancing analgesic potency and attenuating dependence liability caused by morphine and other bimodally-acting opioid agonists 102 1995
5,767,125 Method of simultaneously enhancing analgesic potency and attenuating dependence liability caused by morphine and other bimodally-acting opioid agonists 98 1996
6,096,756 Method of simultaneously enhancing analgesic potency and attenuating dependence liability caused by morphine and other bimodally-acting opioid agonists 105 1998
6,194,382 Method and composition for treating irritable bowel syndrome using low doses of opioid receptor antagonists 63 1999
2001/0006,967 METHOD OF SIMULTANEOUSLY ENHANCING ANALGESIC POTENCY AND ATTENUATING ADVERSE SIDE EFFECTS CAUSED BY TRAMADOL AND OTHER BIMODALLY-ACTING OPIOID AGONISTS 44 1999
6,362,194 Method and simultaneously enhancing analgesic potency and attenuating dependence liability caused by morphine and other bimodally-acting opioid agonists 55 2000
6,395,705 Method and composition for treating irritable bowel syndrome using low doses of opioid receptor antagonists 59 2001
6,765,010 Compositions and methods for enhancing analgesic potency of tramadol and attenuating its adverse side effects 53 2002
 
RECKITT BENCKISER HEALTHCARE (UK) LIMITED (2)
4,582,835 Analgesic compositions 137 1984
4,661,492 Analgesic compositions 104 1985
 
THE BOARD OF TRUSTEES OF THE LELAND STANFORD JUNIOR UNIVERSITY (1)
4,806,543 Method and compositions for reducing neurotoxic injury 91 1986
 
REGENTS OF THE UNIVERSITY OF MINNESOTA (6)
4,401,672 Non-addictive narcotic antitussive preparation 77 1981
4,730,048 Gut-selective opiates 100 1985
5,352,680 Delta opioid receptor antagonists to block opioid agonist tolerance and dependence 120 1992
5,457,208 Kappa opioid receptor antagonists 87 1993
5,578,725 Delta opioid receptor antagonists 70 1995
5,780,479 Use of opioid antagonists to treat impulse-control disorders 66 1997
 
The McLean Hospital Corporation (1)
5,075,341 Treatment for cocaine abuse 150 1989
 
Ortho-McNeil Pharmaceutical, Inc. (1)
5,336,691 Composition comprising a tramadol material and acetaminophen and its use 94 1992
 
NAPP PHARMACEUTICAL GROUP LIMITED (3)
5,591,452 Controlled release formulation 102 1994
6,326,027 Controlled release formulation 95 1995
6,254,887 Controlled release tramadol 98 1996
 
ENCINAL PHARMACEUTICAL INVESTMENTS, LLC (1)
5,869,097 Method of therapy comprising an osmotic caplet 86 1992
 
PURDUE PHARMA COMPANY, THE (2)
4,861,598 Controlled release bases for pharmaceuticals 202 1986
4,970,075 Controlled release bases for pharmaceuticals 170 1989
 
DUPONT MERCK PHARMACEUTICAL COMPANY, THE (1)
4,722,928 N-oxide prodrug derivatives of 3-hydroxy morphinans and partial morphinans having improved oral bioavailability, pharmaceutical compositions, and processes 35 1985
 
PUREUE PHARMA L.P. (1)
4,834,984 Controlled release dihydrocodeine composition 148 1987
 
LIFESHIELD SCIENCES LLC (1)
2004/0158,312 Braided endoluminal device having tapered filaments 21 2003
 
BASF AKTIENGESELLSCHAFT (2)
4,806,558 Diarylacetylenes and their use in treating acne 67 1985
4,957,681 Preparation of pharmaceutical mixtures 124 1989
* Cited By Examiner

Patent Citation Ranking

Forward Cite Landscape

Patent Info (Count) # Cites Year
 
RECRO GAINESVILLE LLC (1)
9,132,096 Abuse resistant pharmaceutical compositions 0 2014
 
PURDUE PHARMA L.P. (23)
8,518,925 Opioids for the treatment of the chronic obstructive pulmonary disease (COPD) 6 2005
9,101,625 Buprenorphine-wafer for drug substitution therapy 0 2007
8,987,290 Use of opioid formulations in needle-less drug delivery devices 0 2007
* 2010/0056,554 USE OF OPIOID FORMULATIONS IN NEEDLE-LESS DRUG DELIVERY DEVICES 0 2007
9,271,940 Immediate release pharmaceutical compositions comprising oxycodone and naloxone 0 2010
* 8,105,631 Opioid agonist/antagonist combinations 30 2010
8,673,355 Opioid agonist/antagonist combinations 9 2011
8,846,090 Matrix for sustained, invariant and independent release of active compounds 9 2012
8,822,487 Opioid agonist/opioid antagonist/acetaminophen combinations 9 2012
8,846,091 Matrix for sustained, invariant and independent release of active compounds 9 2013
9,084,729 Abuse-resistant controlled-release opioid dosage form 2 2013
8,969,369 Abuse-resistant controlled-release opioid dosage form 11 2013
9,056,051 Abuse-resistant controlled-release opioid dosage form 4 2014
9,205,082 Opioid agonist/antagonist combinations 0 2014
8,936,808 Opioid agonist/opioid antagonist/acetaminophen combinations 2 2014
8,932,630 Opioid agonist/antagonist combinations 2 2014
9,168,252 Abuse-resistant controlled-release opioid dosage form 2 2015
9,161,937 Abuse-resistant controlled-release opioid dosage form 2 2015
9,370,512 Buprenorphine-wafer for drug substitution therapy 0 2015
9,283,216 Abuse-resistant controlled-release opioid dosage form 0 2015
9,283,221 Abuse-resistant controlled-release opioid dosage form 0 2015
9,358,230 Abuse-resistant controlled-release opioid dosage form 0 2016
9,345,701 Abuse-resistant controlled-release opioid dosage form 0 2016
 
QRxPharma Ltd. (1)
* 8,933,092 Methods and compositions comprising sequential administration opioid receptor agonists 1 2012
 
EGALET LTD. (7)
8,877,241 Morphine controlled release system 2 2004
9,005,660 Immediate release composition resistant to abuse by intake of alcohol 2 2010
9,023,394 Formulations and methods for the controlled release of active drug substances 1 2013
8,808,745 Morphine polymer release system 5 2013
9,044,402 Abuse-deterrent pharmaceutical compositions for controlled release 1 2014
9,375,428 Morphine controlled release system 0 2014
9,358,295 Immediate release composition resistant to abuse by intake of alcohol 0 2015
* Cited By Examiner

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