Opioid Receptor Affecting Patents (Class 514/18.4)
  • Patent number: 10286146
    Abstract: A system for refilling the drug reservoir of an implanted drug pump device may facilitate wireless data exchange between the refill system and the implanted device, e.g., to verify proper drug selection prior to commencement of the refill process. Via the wireless link, the drug pump device and refill system can exchange data such as, for example, refill information (including, e.g., a type of drug), a drug pump device history, a drug dosage log, and/or a drug-delivery protocol. Further, the refill system can facilitate reprogramming the implanted device wirelessly.
    Type: Grant
    Filed: October 1, 2012
    Date of Patent: May 14, 2019
    Assignee: MINIPUMPS, LLC
    Inventors: Jason Shih, Sean Caffey
  • Patent number: 10017519
    Abstract: The invention describes pharmaceutical compounds and compositions comprised of a ligand attached to the opioid oxycodone, in a manner that substantially decreases or deters the potential for opioid abuse, addiction, illicit and illegal use, and overdose. When delivered at the proper dosage, the pharmaceutical composition provides therapeutic activity similar to that of the parent active agent.
    Type: Grant
    Filed: November 29, 2015
    Date of Patent: July 10, 2018
    Assignee: 3ST Research LLC
    Inventor: John K. Thottathil
  • Patent number: 9636379
    Abstract: The present invention encompasses methods and compositions for alleviating pruritus. The compositions may comprise an analgesic agent.
    Type: Grant
    Filed: December 22, 2014
    Date of Patent: May 2, 2017
    Assignee: WASHINGTON UNIVERSITY
    Inventors: Zhou-feng Chen, Yan-gang Sun
  • Patent number: 9493477
    Abstract: A method of providing a patient with controlled release of ketone-containing opioid using a prodrug capable, upon enzymatic activation and intramolecular cyclization, of releasing the ketone-containing opioid is disclosed. The disclosure also provides such prodrug compounds and pharmaceutical compositions comprising such compounds. Such pharmaceutical compositions can optionally include an enzyme inhibitor that interacts with the enzyme(s) to mediate the enzymatically-controlled release of the ketone-containing opioid from the prodrug so as to modify enzymatic cleavage of the prodrug. Also included are methods to use such compounds and pharmaceutical compositions.
    Type: Grant
    Filed: April 21, 2010
    Date of Patent: November 15, 2016
    Assignee: Signature Therapeutics, Inc.
    Inventors: Thomas E. Jenkins, Craig O. Husfeld, Julie D. Seroogy, Jonathan W. Wray
  • Patent number: 9375417
    Abstract: The present invention includes a transdermal composition which contains a pharmaceutically effective amount of a cannabinoid for delivery of the cannabinoid to the bloodstream of a user. The composition may comprise the following components: a surfactant-lecithin organogel; and a cannabinoid. The composition may also comprise an exogenous terpene. The cannabinoid is capable of diffusing from the composition into the bloodstream of the user, and may be used in methods for treating a patient suffering from a condition such as pain, nausea and emesis, convulsions, muscle spasm, inflammation, depression, and cachexia.
    Type: Grant
    Filed: December 4, 2014
    Date of Patent: June 28, 2016
    Assignee: MARY'S MEDICINALS LLC
    Inventors: Nicole Smith, Noel Erwin Palmer
  • Patent number: 9034377
    Abstract: The present invention relates to a plurality of dosage forms comprising a first dosage form and second dosage form each comprising a therapeutic agent, such as an opioid; wherein the dosage strength of the second dosage form is greater than that of the first dosage form; and wherein the steady state Cave and the steady state AUC of the first and second dosage forms are dose proportional and the single dose Cmax of the second dosage form is less than the minimum level for dose proportionality with respect to the first dosage form. The present invention also relates to methods of administering such dosage forms to a patient, as well as to kits comprising such dosage forms and instructions for administration of the dosage forms to a patient. The inventors believe that the dosage forms and methods of the present invention will lead to improved safety and patient acceptance.
    Type: Grant
    Filed: March 7, 2014
    Date of Patent: May 19, 2015
    Assignee: Purdue Pharma, L.P.
    Inventors: Curtis Wright, Robert Colucci, Ahmed El-Tahtawy
  • Publication number: 20150126455
    Abstract: The present invention pertains to novel uses of endomorphine-1 peptide, analogs, and salts thereof for therapy of children, patients currently suffering from drug addiction, patients prone to opioid addiction, and patients with chemo-induced pain.
    Type: Application
    Filed: May 17, 2013
    Publication date: May 7, 2015
    Inventor: Theodore E. Maione
  • Patent number: 8980300
    Abstract: A biocompatible plasticizer useful for forming a coating composition with a biocompatible polymer is provided. The coating composition may also include a biobeneficial polymer and/or a bioactive agent. The coating composition can form a coating on an implantable device. The implantable device can be used to treat or prevent a disorder such as atherosclerosis, thrombosis, restenosis, hemorrhage, vascular dissection or perforation, vascular aneurysm, vulnerable plaque, chronic total occlusion, claudication, anastomotic proliferation for vein and artificial grafts, bile duct obstruction, ureter obstruction, tumor obstruction, or combinations thereof.
    Type: Grant
    Filed: May 29, 2009
    Date of Patent: March 17, 2015
    Assignee: Advanced Cardiovascular Systems, Inc.
    Inventors: Stephen Dirk Pacetti, Yiwen Tang, Syed Faiyaz Ahmed Hossainy
  • Patent number: 8957025
    Abstract: The present invention relates to dipeptide enkephalin analogues of Formula (I) and their tautomers, ionic forms and pharmaceutically acceptable salts, and their use in medicine, in particular as opioid agonists.
    Type: Grant
    Filed: June 29, 2012
    Date of Patent: February 17, 2015
    Assignee: Pfizer Inc.
    Inventor: Dafydd Rhys Owen
  • Patent number: 8957030
    Abstract: The invention provides a method of reducing or preventing mitochondrial permeability transitioning. The method comprises administering an effective amount of an aromatic-cationic peptide having at least one net positive charge; a minimum of four amino acids; a maximum of about twenty amino acids; a relationship between the minimum number of net positive charges (pm) and the total number of amino acid residues (r) wherein 3pm is the largest number that is less than or equal to r+1; and a relationship between the minimum number of aromatic groups (a) and the total number of net positive charges (pt) wherein 2 a is the largest number that is less than or equal to pt+1, except that when a is 1, pt may also be 1.
    Type: Grant
    Filed: February 27, 2013
    Date of Patent: February 17, 2015
    Assignees: Cornell Research Foundation, Inc., Institute de Recherches Cliniques de Montreal
    Inventors: Hazel H. Szeto, Peter W. Schiller, Kesheng Zhao
  • Patent number: 8957024
    Abstract: The present invention encompasses methods and combinations for substantially inhibiting the opioid-induced internalization of gastrin-releasing peptide receptor (GRPR) in a pruritus specific neuron. Such methods and combinations provide a direct means of treating opioid-induce pruritus without compromising opioid analgesia.
    Type: Grant
    Filed: July 27, 2012
    Date of Patent: February 17, 2015
    Assignee: Washington University
    Inventors: Zhou-Feng Chen, Xianyu Liu
  • Patent number: 8951970
    Abstract: The invention relates to synthetic peptide amide ligands of the kappa opioid receptor and particularly to agonists of the kappa opioid receptor that exhibit low P450 CYP inhibition and low penetration into the brain. The synthetic peptide amides of the invention conform to the structure of formula I: Pharmaceutical compositions containing these compounds are useful in the prophylaxis and treatment of pain and inflammation associated with a variety of diseases and conditions. Such treatable pain includes visceral pain, neuropathic pain and hyperalgesia. Inflammation associated with conditions such as IBD and IBS, ocular and otic inflammation, other disorders and conditions such as pruritis, edema, hyponatremia, hypokalemia, ileus, tussis and glaucoma are treatable or preventable with the pharmaceutical compositions of the invention.
    Type: Grant
    Filed: July 6, 2012
    Date of Patent: February 10, 2015
    Assignee: Cara Therapeutics, Inc.
    Inventors: Claudio D. Schteingart, Frédérique Menzaghi, Guangcheng Jiang, Roberta Vezza Alexander, Javier Sueiras-Diaz, Robert H. Spencer, Derek T. Chalmers, Zhiyong Luo
  • Patent number: 8921305
    Abstract: Disclosed is a method for treating cancer and/or pain using an intra-patient dose escalation procedure to deliver dosages of crotoxin.
    Type: Grant
    Filed: January 22, 2013
    Date of Patent: December 30, 2014
    Assignee: Celtic Biotech Iowa, Inc.
    Inventor: Paul F. Reid
  • Patent number: 8921306
    Abstract: The present invention relates to nociceptin peptide mimetics that have ?-helical structures and bind to and modulate the opioid receptor-like-1 (ORL-1) receptor. The peptide mimetics are constrained cyclic nociceptin analogs which have either agonist or antagonist activity. Pharmaceutical compositions comprising the nociceptin peptide mimetics and methods of treating or preventing a disease or condition ameliorated by modulating the ORL-1 receptor are also described.
    Type: Grant
    Filed: June 7, 2011
    Date of Patent: December 30, 2014
    Assignee: The University of Queensland
    Inventors: David Fairlie, Rosemary Sharon Harrison, Nicholas Evan Shepherd
  • Patent number: 8906859
    Abstract: The invention relates to methods of use of synthetic peptide amides that are ligands of the kappa opioid receptor in the treatment and prevention of kappa opioid receptor-associated diseases and conditions; and particularly to uses of these agonists in the prophylaxis, inhibition and treatment of pain, inflammation and pruritis associated with a variety of diseases, disorders and conditions. Inflammatory conditions preventable or treatable by the methods of the invention include diseases and conditions associated with elevated levels of a proinflammatory cytokines, such as TNF-?, IL-?, IL-6, MMP-1 and MMP-3.
    Type: Grant
    Filed: August 26, 2010
    Date of Patent: December 9, 2014
    Assignee: Cera Therapeutics, Inc.
    Inventors: Claudio D. Schteingart, Frederique Menzaghi, Guangcheng Jiang, Roberta Vezza Alexander, Javier Sueiras-Diaz, Robert H. Spencer, Derek T. Chalmers, Robert Zhiyong Luo
  • Patent number: 8877891
    Abstract: The use of opioid peptides of a novel structure is claimed which, in addition to a pharmacophore, additionally contain structural elements reactive with tachykinin receptors. Due to the synergistic reactivity of the opioid with an additional element, an increased analgesic activity is obtained facilitating protracted effective use due to decreased drug tolerance effects. The drugs may particularly be of use in the treatment of chronic pain as effective analgesics during inflammation caused by rheumatism, gout, neurodegenerative states, post-surgical and post-traumatic inflammations or ones induced by tumors.
    Type: Grant
    Filed: June 30, 2011
    Date of Patent: November 4, 2014
    Inventor: Andrej Lipkowski
  • Publication number: 20140302151
    Abstract: Methods and compositions for treating pain are disclosed. The compositions are based on dry powders comprising microparticles of diketopiperazines and an analgesic active agent. The analgesic in the compositions comprises one or more peptide analgesics or derivatives thereof, which are administered to a subject using a pulmonary inhalation drug delivery system comprising a dry powder inhaler and the analgesic composition. The present compositions produce fewer side effects associated with current opioid therapy.
    Type: Application
    Filed: October 24, 2012
    Publication date: October 9, 2014
    Inventors: Andrea Leone-Bay, Richard A. Houghten, Joseph J. Guarneri, Grayson W. Stowell
  • Publication number: 20140249091
    Abstract: Methods and materials are provided for the production of glycosylated peptides that exhibit high affinity and specificity for delta opioid receptors. The methods and materials of the present invention may be used for treatment of conditions involving pain, such as acute pain and nociceptic pain, neuralgia and myalgia.
    Type: Application
    Filed: October 8, 2013
    Publication date: September 4, 2014
    Applicant: BIOUSIAN BIOSYSTEMS, INC.
    Inventors: Robin Polt, Edward J. Bilsky
  • Publication number: 20140154272
    Abstract: The invention provides a compound of formula (I), wherein R1 is H, C(NH)NH2, an amino acid, or a peptide; X is OH, NH2, NHR2, NR2R3, an amino acid, or a peptide; R2 and R3 are selected from alkyl, alkylenearyl, or alkyleneheteroaryl; each R4 and R5 is independently H or CH3; Z is 2-amino-2,3-dihydro-1H-indene-2-carboxylic acid; 2-amino-1,2,3,4-tetrahydronaphthalene-2-carboxylic acid; 6-amino-6,7,8,9-tetrahydro-5H-benzo[7]annulene 6-carboxylic acid; cyclohexylalanine; cyclohexylglycine; homophenylalanine; 1-naphthylalanine; 2-naphthylalanine; 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid; or octahydro-1H-indole-2-carboxylic acid; n is 0, 1, 2, 3, or 4; with the proviso that X is not NH2 when R1 is H, R4 is H, R5 is CH3, Z is Aci, and n is 2; or a pharmaceutically acceptable salt, ester or solvate thereof. A method of treating pain and a method for treating a mu-opioid receptor mediated disorder and/or a delta-opioid receptor mediated disorder also are provided.
    Type: Application
    Filed: June 22, 2012
    Publication date: June 5, 2014
    Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN
    Inventor: Henry I. Mosberg
  • Patent number: 8716436
    Abstract: The invention relates to cyclic peptide agonists that bind to the mu (morphine) opioid receptor and their use in the treatment of acute and/or chronic pain. Embodiments of the invention are directed to cyclic pentapeptide and hexapeptide analogs of endomorphin that have (i) a carboxy-terminal extension with an amidated hydrophilic amino acid and (ii) a substitution in amino acid position 2. These peptide analogs exhibit decreased tolerance relative to morphine, increased solubility compared to similar tetrapeptide analogs, while maintaining favorable or improved therapeutic ratios of analgesia to side effects.
    Type: Grant
    Filed: May 22, 2012
    Date of Patent: May 6, 2014
    Assignees: The Administrators of the Tulane Educational Fund, U.S. Department of Veterans Affairs
    Inventors: James E. Zadina, Laszlo Hackler
  • Patent number: 8691768
    Abstract: The present invention provides methods of treating or preventing a substance-related disorder using selective delta opioid receptor-1 (DOP-R1) agonists, delta opioid receptor-2 (DOP-R2) antagonists, and/or mu opioid receptor (MOP-R) antagonists, or a pharmaceutically acceptable salt, solvate, hydrate, or prodrug thereof. The methods provided herein further comprise administering a therapeutically effective amount of a combination of a DOP-R1 agonist and a DOP-R2 antagonist. The methods also comprise administering a therapeutically effective amount of a combination of a DOP-R1 agonist and an MOP-R antagonist. The methods provided herein further comprise administering a therapeutically effective amount of a combination of a DOP-R1 agonist and a DOP-R2 antagonist and a MOP-R antagonist. The invention also relates to compositions containing the same. The invention also relates to methods of determining delta opioid receptor specificity of candidate agents.
    Type: Grant
    Filed: May 1, 2009
    Date of Patent: April 8, 2014
    Assignee: The Regents of the University of California
    Inventors: Howard L. Fields, Jennifer M. Mitchell, Elyssa B. Margolis
  • Patent number: 8637031
    Abstract: Methods are disclosed for treating osteoarthritis in a human subject in need thereof, comprising administering to the subject a therapeutically effective amount of an anti-human NGF antibody, or antigen-binding fragment thereof, wherein at least one symptom associated with osteoarthritis is prevented, ameliorated or improved.
    Type: Grant
    Filed: October 10, 2012
    Date of Patent: January 28, 2014
    Assignee: Regeneron Pharmaceuticals, Inc.
    Inventors: Lynn MacDonald, Richard Torres, Marc R. Morra, Joel H. Martin, Joel C. Reinhardt, Paul Tiseo
  • Patent number: 8603984
    Abstract: This invention provides methods of controlling pain in a canine comprising transdermally administering a composition comprising fentanyl, a penetration enhancer, and a volatile liquid, wherein the composition is a solution. The invention also provides a single unit dose of the composition.
    Type: Grant
    Filed: February 8, 2012
    Date of Patent: December 10, 2013
    Assignee: Eli Lilly and Company
    Inventors: Garret Conrad Newbound, Terrence Patrick Clark
  • Patent number: 8603525
    Abstract: An orally disintegrating multilayer tablet comprising at least two discrete layers, one of which comprises at least one active agent that promotes the oxidation of opioids, preferably acetaminophen, and the other of which contains granules including an inert core which is coated with at least one opioid and at least one binder, wherein said opioid coating is coated with a subcoat comprising a compound soluble in gastric fluids, said subcoat being coated with a taste-masking coating comprising a polymer or copolymer comprising dialkylaminoalkyl(meth)acrylate units and a pore-forming agent.
    Type: Grant
    Filed: July 31, 2007
    Date of Patent: December 10, 2013
    Assignee: Ethypharm
    Inventors: Pascal Oury, Catherine Herry, Didier Hoarau
  • Patent number: 8598123
    Abstract: The present invention relates to compounds of Formula (I) and their pharmaceutically acceptable salts, wherein the substituents are as described herein, and their use in medicine, in particular as opioid agonists.
    Type: Grant
    Filed: September 7, 2012
    Date of Patent: December 3, 2013
    Assignee: Pfizer Inc.
    Inventors: Christopher Gordon Barber, Dafydd Rhys Owen, Lisa Rosemary Thompson
  • Patent number: 8536131
    Abstract: The invention relates to synthetic peptide amide ligands of the kappa opioid receptor and particularly to agonists of the kappa opioid receptor that exhibit low P450 CYP inhibition and low penetration into the brain. The synthetic peptide amides of the invention conform to the structure: The compounds are useful in the prophylaxis and treatment of pain and inflammation associated with a variety of diseases and conditions.
    Type: Grant
    Filed: October 27, 2010
    Date of Patent: September 17, 2013
    Assignee: Cara Therapeutics, Inc.
    Inventors: Claudio D. Schteingart, Frédérique Menzaghi, Guangcheng Jiang, Roberta Vezza Alexander, Javier Sueiras-Diaz, Robert H. Spencer, Derek T. Chalmers, Zhiyong Luo
  • Publication number: 20130196908
    Abstract: The invention provides for methods and compositions for treatment of pain via craniofacial mucosal administration of an analgesic compound (e.g. a non-opioid analgesic peptide, an NOP agonist or N/OFQ). Intranasal administration of certain analgesic peptides such as N/OFQ results in global analgesic effects.
    Type: Application
    Filed: March 13, 2013
    Publication date: August 1, 2013
    Applicant: TRIGEMINA, INC.
    Inventor: TRIGEMINA, INC.
  • Patent number: 8497237
    Abstract: 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.
    Type: Grant
    Filed: January 9, 2012
    Date of Patent: July 30, 2013
    Assignee: Signature Therapeutics, Inc.
    Inventors: Thomas E. Jenkins, Craig O. Husfeld
  • Patent number: 8486894
    Abstract: The invention relates to synthetic peptide amides that are ligands of the kappa opioid receptor and particularly to agonists of the kappa opioid receptor that exhibit low P450 CYP inhibition and low penetration into the brain. The synthetic peptide amides of the invention conform to the structure: wherein Xaa is a D-amino acid and G is selected from the following three groups: The compounds are useful in the prophylaxis and treatment of pain, pruritis and inflammation associated with a variety of diseases and conditions.
    Type: Grant
    Filed: May 5, 2010
    Date of Patent: July 16, 2013
    Assignee: Cara Therapeutics, Inc.
    Inventors: Claudio D. Schteingart, Frédérique Menzaghi, Guangcheng Jiang, Roberta Vezza Alexander, Javier Sueiras-Diaz, Robert H. Spencer, Derek T. Chalmers, Zhiyong Luo
  • Publication number: 20130178427
    Abstract: The invention relates to cyclic peptide agonists that bind to the mu (morphine) opioid receptor and their use in the treatment of acute and/or chronic pain. Embodiments of the invention are directed to cyclic pentapeptide and hexapeptide analogs of endomorphin that have (i) a carboxy-terminal extension with an amidated hydrophilic amino acid and (ii) a substitution in amino acid position 2, and a 2?,6?-dimethyltyrosine (Dmt) residue in place of the N-terminal tyrosine residue a position 1. These peptide analogs exhibit increased solubility compared to similar tetrapeptide analogs while maintaining favorable or improved therapeutic ratios of analgesia to side effects.
    Type: Application
    Filed: March 8, 2013
    Publication date: July 11, 2013
    Applicant: THE ADMINISTRATORS OF THE TULANE EDUCATIONAL FUND
    Inventor: The Administrators of the Tulane Education Fund
  • Publication number: 20130157928
    Abstract: The present invention relates to nociceptin peptide mimetics that have ?-helical structures and bind to and modulate the opioid receptor-like-1 (ORL-1) receptor. The peptide mimetics are constrained cyclic nociceptin analogues which have either agonist or antagonist activity. Pharmaceutical compositions comprising the nociceptin peptide mimetics and methods of treating or preventing a disease or condition ameliorated by modulating the ORL-1 receptor are also described.
    Type: Application
    Filed: June 7, 2011
    Publication date: June 20, 2013
    Inventors: David Fairlie, Rosemary Sharon Harrison, Nicholas Evan Shepherd
  • Patent number: 8420602
    Abstract: A compound provided by the present invention includes an endocannabinoid, endocannabinoid derivative, or endocannabinoid analog moiety covalently bonded to a biologically active peptide. One example of an inventive compound described is a conjugate of an endocannabinoid, endocannabinoid derivative, or endocannabinoid analog moiety covalently coupled to an opioid peptide, such as an endorphin, enkephalin, dynorphin or endomorphin. Also detailed are processes for making the described conjugates and pharmaceutical compositions including such compounds.
    Type: Grant
    Filed: May 13, 2005
    Date of Patent: April 16, 2013
    Inventor: Landon C. G. Miller
  • Patent number: 8420600
    Abstract: The present invention is directed to compositions and methods for relieving pain at a site in a human or animal by administering at a discrete site in a human or animal a dose of capsaicin in an amount effective to denervate the discrete site without eliciting an effect outside the discrete location.
    Type: Grant
    Filed: August 7, 2006
    Date of Patent: April 16, 2013
    Assignee: Vallinex, Inc.
    Inventors: Ronald Burch, Richard B. Carter, Jeff Lazar
  • Publication number: 20130072438
    Abstract: Disclosed herein are opioid peptide conjugates (for example, opioid peptide esters). In some embodiments, the disclosed conjugates include an opioid peptide consisting of two to six amino acids and a moiety conjugated to the opioid peptide by an ester bond. In some examples, the moiety is an alcohol, a sugar, a lipid, or dehydroascorbic acid. Also disclosed are methods of altering nociception including administering an effective amount of one or more disclosed opioid peptide conjugates to a subject (such as a human subject).
    Type: Application
    Filed: September 13, 2012
    Publication date: March 21, 2013
    Inventor: Joel S. Goldberg
  • Patent number: 8399414
    Abstract: The object of this invention is to provide a novel pharmaceutical composition for getting rid of pains and anxiety in patients. This invention relates to a pharmaceutical composition containing lactoferrin as an active ingredient. The composition of this invention is useful for treatment of at least one disease or condition selected from the group consisting of pains, including the phase 1 pain and the phase 2 pain, anxiety and stress. The composition is particularly beneficial to alleviating or getting rid of the pain and anxiety which significantly lower quality of life of patients with end-stage cancer. The composition of this invention is also useful for treatment of pains, including the phase 1 pain and the phase 2 pain, and inflammation which accompany arthritis or diseases in the junctions of bones (e.g. rheumatoid arthritis, osteoarthritis, frozen shoulder, sports injuries such as tennis elbow and baseball shoulder, and low back pain).
    Type: Grant
    Filed: January 17, 2003
    Date of Patent: March 19, 2013
    Assignee: NRL Pharma, Inc.
    Inventors: Etsumori Harada, Takashi Takeuchi, Kenichiro Hayashida, Kunio Ando, Hirohiko Shimizu
  • Patent number: 8399415
    Abstract: Oligopeptides according to formula (I) and/or (II), R1-Tyr-Pro-Trp-Phe-NH2 (I, SEQ ID NO:1); R1-Tyr-Pro-PhePhe-NH2 (II, SEQ ID NO:2), wherein R1 is linked to the NH2-group of the amino-terminal part of Tyr and is selected from the group consisting of —H; a linear saturated or unsaturated or branched saturated or unsaturated acyl group having 1 to 24 carbon atoms, which may be functionalized by a —OH, —SH, —COOH or —CONH+ group; a sterol or a sphingolipid group which is linked to the amino terminal part of Tyr via a bifunctional linker are disclosed. Cosmetic compositions containing the oligopeptides are also disclosed.
    Type: Grant
    Filed: December 16, 2011
    Date of Patent: March 19, 2013
    Assignee: Cognis IP Management GmbH
    Inventors: Véronique Gillon, Philippe Moussou, Jean-Luc Contet-Audonneau, Olga Freis
  • Publication number: 20130053326
    Abstract: Compositions and methods for treatment of sexual dysfunctions by administering to a subject a pharmaceutical composition comprising a delta opioid receptor agonist in an amount effective to delay the onset of ejaculation in the subject during sexual stimulation.
    Type: Application
    Filed: January 2, 2003
    Publication date: February 28, 2013
    Inventors: Kwen-Jen Chang, Klim King, Kestutis P. Biciunas, Robert W. McNutt, JR., William Pendergast, Shyi-Tai Jan
  • 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: 8367610
    Abstract: A method for administering nerve growth factor to treat cravings is provided. Pharmaceutical compositions for the treatment of cravings comprising nerve growth factor are also provided.
    Type: Grant
    Filed: October 5, 2009
    Date of Patent: February 5, 2013
    Assignee: Beech Tree Labs, Inc.
    Inventor: John McMichael
  • Publication number: 20130012448
    Abstract: The invention relates to synthetic peptide amide ligands of the kappa opioid receptor and particularly to agonists of the kappa opioid receptor that exhibit low P450 CYP inhibition and low penetration into the brain. The synthetic peptide amides of the invention conform to the structure of formula I: Pharmaceutical compositions containing these compounds are useful in the prophylaxis and treatment of pain and inflammation associated with a variety of diseases and conditions. Such treatable pain includes visceral pain, neuropathic pain and hyperalgesia. Inflammation associated with conditions such as IBD and IBS, ocular and otic inflammation, other disorders and conditions such as pruritis, edema, hyponatremia, hypokalemia, ileus, tussis and glaucoma are treatable or preventable with the pharmaceutical compositions of the invention.
    Type: Application
    Filed: July 6, 2012
    Publication date: January 10, 2013
    Applicant: CARA THERAPEUTICS, INC.
    Inventors: Claudio D. Schteingart, Frédérique Menzaghi, Guangcheng Jiang, Roberta Vezza Alexander, Javier Sueiras-Diaz, Robert H. Spencer, Derek T. Chalmers, Zhiyong Luo
  • Publication number: 20120329724
    Abstract: The present invention relates to compounds of Formula (I) and their pharmaceutically acceptable salts, wherein the substituents are as described herein, and their use in medicine, in particular as opioid agonists.
    Type: Application
    Filed: September 7, 2012
    Publication date: December 27, 2012
    Inventors: Christopher Gordon Barber, Dafydd Rhys Owen, Lisa Rosemary Thompson
  • Publication number: 20120322740
    Abstract: The invention relates to cyclic peptide agonists that bind to the mu (morphine) opioid receptor and their use in the treatment of acute and/or chronic pain. Embodiments of the invention are directed to cyclic pentapeptide and hexapeptide analogs of endomorphin that have (i) a carboxy-terminal extension with an amidated hydrophilic amino acid and (ii) a substitution in amino acid position 2. These peptide analogs exhibit decreased tolerance relative to morphine, increased solubility compared to similar tetrapeptide analogs, while maintaining favorable or improved therapeutic ratios of analgesia to side effects.
    Type: Application
    Filed: May 22, 2012
    Publication date: December 20, 2012
    Applicants: UNITED STATES DEPARTMENT OF VETERANS AFFAIRS, THE ADMINISTRATORS OF THE TULANE EDUCATIONAL FUND
    Inventors: James E. ZADINA, Laszlo HACKLER
  • Patent number: 8309088
    Abstract: Methods are disclosed for treating osteoarthritis in a human subject in need thereof, comprising administering to the subject a therapeutically effective amount of an anti-human NGF antibody, or antigen-binding fragment thereof, wherein at least one symptom associated with osteoarthritis is prevented, ameliorated or improved.
    Type: Grant
    Filed: September 23, 2010
    Date of Patent: November 13, 2012
    Assignee: Regeneron Pharmaceuticals, Inc.
    Inventors: Lynn MacDonald, Richard Torres, Marc R. Morra, Joel H. Martin, Joel C. Reinhardt, Paul Tiseo
  • Patent number: 8236766
    Abstract: The invention relates to synthetic peptide amides that are ligands of the kappa opioid receptor and particularly to agonists of the kappa opioid receptor that exhibit low P450 CYP inhibition and low penetration into the brain. The synthetic peptide amides of the invention conform to the structure: wherein Xaa is a D-amino acid and G is selected from the following three groups: The compounds are useful in the prophylaxis and treatment of pain, pruritus and inflammation associated with a variety of diseases and conditions.
    Type: Grant
    Filed: June 8, 2009
    Date of Patent: August 7, 2012
    Assignee: Cara Therapeutics, Inc.
    Inventors: Claudio D. Schteingart, Frederique Menzaghi, Guangcheng Jiang, Roberta Vezza Alexander, Javier Sueiras-Diaz, Robert H. Spencer, Derek T. Chalmers, Zhiyong Luo
  • Patent number: 8217007
    Abstract: The invention relates to synthetic peptide amide ligands of the kappa opioid receptor and particularly to agonists of the kappa opioid receptor that exhibit low P450 CYP inhibition and low penetration into the brain. The synthetic peptide amides of the invention conform to the structure of formula I: Pharmaceutical compositions containing these compounds are useful in the prophylaxis and treatment of pain and inflammation associated with a variety of diseases and conditions. Such treatable pain includes visceral pain, neuropathic pain and hyperalgesia. Inflammation associated with conditions such as IBD and IBS, ocular and otic inflammation, other disorders and conditions such as pruritis, edema, hyponatremia, hypokalemia, ileus, tussis and glaucoma are treatable or preventable with the pharmaceutical compositions of the invention.
    Type: Grant
    Filed: May 25, 2010
    Date of Patent: July 10, 2012
    Assignee: Cara Therapeutics, Inc.
    Inventors: Claudio D. Schteingart, Frédérique Menzaghi, Guangcheng Jiang, Roberta Vezza Alexander, Javier Sueiras-Diaz, Robert H. Spencer, Derek T. Chalmers, Robert Zhiyong Luo
  • Patent number: 8163701
    Abstract: Disclosed herein are prodrugs of active agents which contain at least one amine, phenol, carboxylic acid, or thiol functionality. Also disclosed herein are methods of making prodrugs of active agents, pharmaceutical compositions of prodrugs of active agents and methods of using prodrugs of active agents and pharmaceutical compositions.
    Type: Grant
    Filed: August 21, 2006
    Date of Patent: April 24, 2012
    Assignee: Signature Therapeutics, Inc.
    Inventor: Thomas E. Jenkins
  • Publication number: 20120093929
    Abstract: The present invention relates to a composition, comprising (i) a matrix made of polymeric nanofibers, and (ii) an opioid agonist within the matrix.
    Type: Application
    Filed: May 5, 2009
    Publication date: April 19, 2012
    Applicant: Euro-Celtique S.A.
    Inventors: Alexander Oksche, Kevin J. Smith, Derek Prater, Malcolm Walden, Will Heath, Bernard Kennedy, Vanessa Addison, Hassan Mohammad
  • Patent number: 8106016
    Abstract: The invention relates to pharmaceutical compounds and compositions comprised of a chemical moiety attached to an opioid such as oxycodone in a manner that substantially decreases the potential of the opioid to cause overdose. When delivered at the proper dosage the pharmaceutical composition provides therapeutic activity similar to that of the parent active agent. Further the compounds and compositions of the invention are useful in preventing addiction and susceptibility to addiction.
    Type: Grant
    Filed: December 8, 2006
    Date of Patent: January 31, 2012
    Assignee: Shire LLC
    Inventors: James Scott Moncrief, Suma Krishnan, Travis Mickle, Christopher Lauderback, Sanjib Bera, Sven Guenther, Wendy Hirschelman
  • Patent number: 8101574
    Abstract: Oligopeptides according to formula (I) and/or (II), R1-Tyr-Pro-Trp-Phe-NH2 (I); R1-Tyr-Pro-Phe-Phe-NH2 (II), wherein R1 is linked to the NH2-group of the amino-terminal part of Tyr and is selected from the group consisting of —H; a linear saturated or unsaturated or branched saturated or unsaturated acyl group having 1 to 24 carbon atoms, which may be functionalized by a —OH, —SH, —COOH or —CONH2 group; a sterol or a sphingolipid group which is linked to the amino terminal part of Tyr via a bifunctional linker are disclosed. Cosmetic compositions containing the oligopeptides are also disclosed.
    Type: Grant
    Filed: October 25, 2006
    Date of Patent: January 24, 2012
    Assignee: Cognis IP Management GmbH
    Inventors: Véronique Gillon, Philippe Moussou, Jean-Luc Contet-Audonneau, Olga Freis
  • Patent number: 8084429
    Abstract: Provided are compounds represented by: wherein R1 is a D-alanine, D-serine, D-threonine, D-methionine, D-leucine, D-asparagine or D-glutamine side chain and R2 is a phenylalanine or tryptophan side-chain, and compositions containing such compounds.
    Type: Grant
    Filed: August 7, 2003
    Date of Patent: December 27, 2011
    Inventors: Andrzej Lipkowski, Daniel Carr, Iwona Bonney, Dariusz Kosson, Aleksandra Misjecka-Kesik