Nitrogen Attached Directly To The Piperidine Ring By Nonionic Bonding Patents (Class 514/329)
  • Publication number: 20120322828
    Abstract: This invention provides methods of controlling pain in an equine for an effective period of time 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: Application
    Filed: February 8, 2012
    Publication date: December 20, 2012
    Applicant: ELI LILLY AND COMPANY
    Inventors: Amy Louise Marr, Jane Granville Owens, Douglas Eugene Mouzin, Kari Lynette Riggs
  • Publication number: 20120315330
    Abstract: A pharmaceutical composition for the treatment of acute disorders is described. The composition comprises an essentially water-free, ordered mixture of at least one pharmaceutically active agent in the form of microparticles which are adhered to the surfaces of carrier particles which are substantially larger than the particles of the active agent or agents, and are essentially water-soluble, in combination with the bioadhesion and/or mucoadhesion promoting agent. The invention also relates to a method for preparing the composition and to the use of the composition for the treatment of acute disorders.
    Type: Application
    Filed: November 22, 2011
    Publication date: December 13, 2012
    Applicant: OREXO AB
    Inventors: ANDERS PETTERSSON, CHRISTER NYSTROM
  • Publication number: 20120316169
    Abstract: (R,S) 2-aryl-propionamide derivatives, or their single enantiomers (R) and (S) are disclosed useful in the treatment or prevention of symptoms and disorders such as pain and inflammation associated with the bradykinin B1 pathway.
    Type: Application
    Filed: October 28, 2010
    Publication date: December 13, 2012
    Applicant: DOMPÉ S.P.A.
    Inventors: Andrea Beccari, Andrea Aramini, Gianluca Bianchini, Alessio Moriconi
  • Publication number: 20120315283
    Abstract: Described herein are methods of using soluble epoxide hydrolase inhibitors to modulate the levels of epoxyeicosatrienoic acids (EETs) in order to increase angiogenesis and promote wound healing and tissue regeneration.
    Type: Application
    Filed: February 1, 2011
    Publication date: December 13, 2012
    Applicants: DANA-FARBER CANCER INSTITUTE, INC., CHILDREN'S MEDICAL CENTER CORPORATION
    Inventors: Dipak Panigraphy, Mark Kieran
  • Publication number: 20120302539
    Abstract: Certain compounds and pharmaceutically acceptable salts are provided herein. Also provided are pharmaceutical compositions comprising at least one compound or pharmaceutically acceptable salt therein and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain disease states responsive to the inhibition of transglutaminase TG2 activity are described. These disease states include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one compound or pharmaceutically acceptable salt thereof as a single active agent or administering at least one compound or pharmaceutically acceptable salt thereof in combination with one or more other therapeutic agents.
    Type: Application
    Filed: May 7, 2012
    Publication date: November 29, 2012
    Inventors: Michael Prime, Stephen Martin Courtney, Richard Marston, Celia Dominguez, Douglas Macdonald, John Wityak
  • Publication number: 20120295879
    Abstract: A compound having the general structure shown in Formula I: or pharmaceutically acceptable salts and/or solvates thereof are useful in treating diseases or conditions mediated by NK1 receptors, for example various physiological disorders, symptoms or diseases, including emesis, depression, anxiety and cough.
    Type: Application
    Filed: September 26, 2011
    Publication date: November 22, 2012
    Applicant: OPKO HEALTH, INC.
    Inventors: Anandan Palani, Xianhai Huang, Dong Xiao, Sapna S. Shah, Sunil Paliwal, Hon-Chung Tsui, Michelle Laci Wrobleski, Ashwin U. Rao, Cheng Wang, Neng-Yang Shih
  • Publication number: 20120295922
    Abstract: The present invention provides methods for treating and/or preventing mucostitis with one or more compounds, or pharmaceutically acceptable salts thereof, disclosed herein, or compositions comprising the same.
    Type: Application
    Filed: May 15, 2012
    Publication date: November 22, 2012
    Applicant: POLYMEDIX, INC.
    Inventors: Richard W. Scott, Bozena Korczak
  • Publication number: 20120295910
    Abstract: The present invention relates to new sulfonamide derivatives of formula (I), wherein R1-R8 and Z are as defined in the claims, and optical antipodes or racemates and/or salts and/or hydrates and/or solvates thereof, which are selective antagonists of bradykinin B1, to processes for producing these same compounds, pharmacological compositions containing them and to their use in therapy or prevention of painful and inflammatory conditions.
    Type: Application
    Filed: August 1, 2012
    Publication date: November 22, 2012
    Inventors: Gyula Beke, Eva Bozo, Sandor Farkas, Katalin Hornok, Gyorgy Keseru, Eva Schmidt, Eva Szentirmay, Istvan Vago, Monika Vastag
  • Publication number: 20120289548
    Abstract: The invention provides compounds that are chemically modified by covalent attachment of a water-soluble oligomer. A compound of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different from those of the compound not attached to the water-soluble oligomer.
    Type: Application
    Filed: June 29, 2012
    Publication date: November 15, 2012
    Applicant: Nektar Therapeutics
    Inventors: Jennifer RIGGS-SAUTHIER, Bo-Liang Deng, Timothy A. Riley
  • Patent number: 8309119
    Abstract: The present invention aims at providing an adhesive preparation wherein a drug is sufficiently dissolved in an adhesive layer and is not easily separated from the adhesive layer even during preservation of the adhesive preparation. The present invention provides an adhesive preparation having an adhesive layer on at least one surface of a support, wherein the adhesive layer comprises a first synthetic rubber having a viscosity average molecular weight of 1,600,000-6,500,000, a drug, an organic liquid component and a tackifier. The present invention further provides the aforementioned adhesive preparation, wherein the organic liquid component is contained in the adhesive layer in a proportion of 20 wt % or above relative to the total weight of the adhesive layer.
    Type: Grant
    Filed: February 27, 2008
    Date of Patent: November 13, 2012
    Assignee: Nitto Denko Corporation
    Inventors: Masato Nishimura, Sachiko Terashi, Shiro Satoda, Keigo Inosaka, Kensuke Matsuoka
  • Patent number: 8304403
    Abstract: Compounds of formula Ia and Ib and wherein A, B, C and R1 are described herein.
    Type: Grant
    Filed: June 10, 2010
    Date of Patent: November 6, 2012
    Assignee: Bristol-Myers Squibb Company
    Inventors: Mark E. Salvati, Heather Finlay, Bang-Chi Chen, Lalgudi S. Harikrishnan, Ji Jiang, James A. Johnson, Muthoni G. Kamau, R. Michael Lawrence, Jianqing Li, John Lloyd, Michael M. Miller, Zulan Pi, Jennifer X. Qiao, Richard A. Rampulla, Jacques Y. Roberge, Tammy C. Wang, Yufeng Wang, Wu Yang
  • Publication number: 20120277250
    Abstract: The invention relates to compounds of formula I: or a pharmaceutically acceptable salt thereof, where R1-3, R5, R7, a, b, Q, X, X?, X?, Y, Z, and Ar are as defined in the specification. These compounds are muscarinic receptor antagonists. The invention also relates to pharmaceutical compositions containing such compounds, processes for preparing such compounds and methods of using such compounds to, for example, treat pulmonary disorders such as chronic obstructive pulmonary disease and asthma.
    Type: Application
    Filed: July 11, 2012
    Publication date: November 1, 2012
    Applicant: THERAVANCE, INC.
    Inventors: YuHua Ji, Craig HUSFELD, YongQi MU, Cameron Smith
  • Publication number: 20120277267
    Abstract: A composition for the intranasal delivery of fentanyl or a pharmaceutically acceptable salt thereof to an animal includes an aqueous solution of fentanyl or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable additive selected from (i) a pectin and (ii) a poloxamer and chitosan or a salt or derivative thereof; provided that when the composition comprises a pectin it is substantially free of divalent metal ions; and which, in comparison to a simple aqueous solution of fentanyl administered intranasally at the same dose, provides a peak plasma concentration of fentanyl (Cmax) that is from 10 to 80% of that achieved using a simple aqueous solution of fentanyl administered intranasally at an identical fentanyl dose. A method for treating or managing pain by intranasally administering the composition is also disclosed.
    Type: Application
    Filed: July 3, 2012
    Publication date: November 1, 2012
    Applicant: ARCHIMEDES DEVELOPMENT LIMITED
    Inventors: Peter James WATTS, Jonathan David CASTILE, William Columbus Ian LAFFERTY, Alan SMITH
  • Publication number: 20120277221
    Abstract: Behavioral pharmacological data with the compound of formula (I), a novel and selective 5HT2A/2C receptor inverse agonist, demonstrate in vivo efficacy in models of psychosis and dyskinesias. This includes activity in reversing MK-801 induced locomotor behaviors, suggesting that this compound may be an efficacious anti-psychotic, and activity in an MPTP primate model of dyskinesias, suggesting efficacy as an anti-dyskinesia agent. These data support the hypothesis that 5HT2A/2C receptor inverse agonism may confer antipsychotic and anti-dyskinetic efficacy in humans, and indicate a use of the compound of formula (I) and related agents as novel therapeutics for Parkinson's Disease, related human neurodegenerative diseases, and psychosis.
    Type: Application
    Filed: June 29, 2012
    Publication date: November 1, 2012
    Inventors: David M. WEINER, Robert E. Davis, Mark R. Brann, Carl-Magnus A. Anderson, Allan K. Uldam
  • Patent number: 8299258
    Abstract: The present invention relates to a process for the preparation of piperidine derivatives including sufentanil, and their pharmaceutically acceptable salts, such as the citrate salt in which a quaternary ammonium (nosylate) salt of an appropriate piperidine is reacted with a corresponding 4-NO2 sulfonate ester to produce the desired piperidine derivative at a high purity.
    Type: Grant
    Filed: November 4, 2009
    Date of Patent: October 30, 2012
    Assignee: Cambrex Charles City
    Inventors: Greg S. Buenger, Paul A. Jass, Kezia Peixoto Schutz
  • Publication number: 20120270903
    Abstract: An intranasnal spray device contains a composition for the intranasal delivery of fentanyl or a pharmaceutically acceptable salt thereof to an animal includes an aqueous solution of fentanyl or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable additive selected from (i) a pectin and (ii) a poloxamer and chitosan or a salt or derivative thereof; provided that when the composition comprises a pectin it is substantially free of divalent metal ions; and which, in comparison to a simple aqueous solution of fentanyl administered intranasally at the same dose, provides a peak plasma concentration of fentanyl (Cmax) that is from 10 to 80% of that achieved using a simple aqueous solution of fentanyl administered intranasally at an identical fentanyl dose. A method for treating or managing pain by intranasally administering the composition is also disclosed.
    Type: Application
    Filed: July 3, 2012
    Publication date: October 25, 2012
    Applicant: ARCHIMEDES DEVELOPMENT LIMITED
    Inventors: Peter James WATTS, Jonathan David CASTILE, William Columbus Ian LAFFERTY, Alan SMITH
  • Publication number: 20120269772
    Abstract: The present invention relates to pre-formulations comprising low viscosity, non-liquid crystalline, mixtures of: a) at least one neutral diacyl lipid and/or at least one tocopherol; b) at least one phospholipid; c) at least one biocompatible, oxygen containing, low viscosity organic solvent; wherein at least one bioactive agent is dissolved or dispersed in the low viscosity mixture and wherein the pre-formulation forms, or is capable of forming, at least one liquid crystalline phase structure upon contact with an aqueous fluid. The preformulations are suitable for generating parenteral, non-parenteral and topical depot compositions for sustained release of active agents. The invention additionally relates to a method of delivery of an active agent comprising administration of a preformulation of the invention, a method of treatment comprising administration of a preformulation of the invention and the use of a preformulation of the invention in a method for the manufacture of a medicament.
    Type: Application
    Filed: June 29, 2012
    Publication date: October 25, 2012
    Applicant: Camurus AB
    Inventors: Krister THURESSON, Fredrik TIBERG, Markus JOHANSSON, Ian HARWIGSSON, Fredrik JOABSSON, Markus JOHNSSON
  • Publication number: 20120270895
    Abstract: The present invention relates to pharmaceutical compositions for intranasal administration to a mammal that contain an effective amount of an opioid, a liquid nasal carrier for the opioid, and optionally a sweetener, flavoring agent or masking agent. In some embodiments of the present invention, the pharmaceutical compositions have improved bioavailability. In other embodiments of the present invention, the opioid compositions improve patient compliance.
    Type: Application
    Filed: June 12, 2012
    Publication date: October 25, 2012
    Inventor: Daniel P. Wermeling
  • Publication number: 20120270902
    Abstract: The invention provides N-substituted benzenesulfonamides for use in treating or preventing cognitive disorders, such as Alzheimer's Disease. Compounds of particular interest are defined by Formula (I), wherein R1, R2, R3, R4, and R3?, are as described in the specification. The invention also encompasses pharmaceutical compositions comprising compounds of Formula (I) as well as methods of treating cognitive disorders, including Alzheimer's disease using compounds of Formula (I).
    Type: Application
    Filed: February 13, 2012
    Publication date: October 25, 2012
    Applicant: ELAN PHARMACEUTICALS, INC.
    Inventors: Martin Neitzel, Jennifer Marugg
  • Patent number: 8293767
    Abstract: The invention provides an acid addition salt of 4-(2,6-dichloro-benzoylamino)-1H-pyrazole-3-carboxylic acid piperidin-4-ylamide and crystals thereof, the salt being formed with an acid selected from methanesulphonic acid and acetic acid and mixtures thereof. Also provided are the novel uses of salts of 4-(2,6-dichloro-benzoylamino)-1H-pyrazole-3-carboxylic acid piperidin-4-ylamide, processes for the preparation of 4-(2,6-dichloro-benzoylamino)-1H-pyrazole-3-carboxylic acid piperidin-4-ylamide and its salts and novel chemical intermediates.
    Type: Grant
    Filed: July 22, 2011
    Date of Patent: October 23, 2012
    Assignee: Astex Therapeutics Limited
    Inventors: Paul Graham Wyatt, David Charles Rees, Mladen Vinkovic, Gary Trewartha
  • Publication number: 20120252845
    Abstract: The present invention relates to a sustained release medical composition comprising an active pharmaceutical ingredient and a geopolymeric binder. Preferably the active pharmaceutical ingredient is combined with the geopolymeric binder during the formation of that binder.
    Type: Application
    Filed: May 7, 2010
    Publication date: October 4, 2012
    Inventor: Hakan Engqvist
  • Publication number: 20120252846
    Abstract: Buccal aerosol sprays or capsules using polar and non-polar solvent have now been developed which provide biologically active compounds for rapid absorption through the oral mucosa, resulting in fast onset of effect. The buccal polar compositions of the invention comprise formulation I: aqueous polar solvent, active compound, and optional flavoring agent; formulation II: aqueous polar solvent, active compound, optionally flavoring agent, and propellant; formulation III: non-polar solvent, active compound, and optional flavoring agent; and formulation IV: non-polar solvent, active compound, optional flavoring agent, and propellant.
    Type: Application
    Filed: May 9, 2012
    Publication date: October 4, 2012
    Inventor: Harry A. Dugger, III
  • Patent number: 8268821
    Abstract: The present invention relates generally to the field of pain management, and in particular, the management of neuropathic or inflammatory pain including a neuropathic or inflammatory component of nociceptive pain. More particularly, the present invention provides methods and compositions which treat, alleviate, prevent, diminish or otherwise ameliorate the symptoms of neuropathic or inflammatory pain. The present invention further contemplates combination therapy involved in the treatment of pain in association with the treatment of a particular disease condition or pathology. The present invention further also provides sustained and slow release formulations, tamper-proof deliver systems and stents, catheters and other mechanical devices coated with formulations which permit sustained or slow release of active ingredients involved in pain management.
    Type: Grant
    Filed: December 1, 2010
    Date of Patent: September 18, 2012
    Assignee: Relevare Aust. Pty Ltd
    Inventors: Raymond Nadeson, Adam Paul Tucker, Colin Goodchild
  • Publication number: 20120232053
    Abstract: The invention provides compounds of the formula: in salt or zwitterionic form or a pharmaceutically acceptable salt thereof, wherein R1-6, a, Z and Q are as defined in the specification. These compounds are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes for preparing such compounds and methods of using such compounds to, for example, treat pulmonary disorders such as chronic obstructive pulmonary disease and asthma.
    Type: Application
    Filed: May 17, 2012
    Publication date: September 13, 2012
    Applicant: THERAVANCE, INC.
    Inventors: Craig Husfeld, YuHua Ji, Rick Lee, Li Li, YongQi Mu, Cameron Smith, Johnny Uy
  • Publication number: 20120220629
    Abstract: Disclosed are compounds, compositions and methods for the prevention and/or treatment of diseases which are pathophysiologically mediated by the ghrelin receptor.
    Type: Application
    Filed: February 24, 2012
    Publication date: August 30, 2012
    Inventors: Silvina GARCIA RUBIO, Claudio Pietra, Claudio Giuliano, Zhigang Li
  • Patent number: 8252319
    Abstract: Transdermal delivery systems for administering sufentanil through the skin are provided. The systems contain a sufficient amount of sufentanil to induce and maintain a constant state of analgesia when applied to a subject. The systems are characterized as having one or more features including a high degree of dosage form rate control over flux of sufentanil from the system, a high net flux of sufentanil from the system through the skin, lack of a permeation enhancer, an adhesive member demonstrating superior shear time, a low coefficient of variation in the net flux of sufentanil from the system, a high delivery efficiency, and a substantially constant steady state net flux of sufentanil from the system. Methods of using the transdermal delivery systems to administer a sufficient amount of sufentanil to induce and maintain analgesia for extended periods when applied to a subject are also provided.
    Type: Grant
    Filed: July 31, 2007
    Date of Patent: August 28, 2012
    Assignee: Durect Corporation
    Inventors: Su Il Yum, Felix Theeuwes
  • Patent number: 8252320
    Abstract: Transdermal delivery systems for administering sufentanil through the skin are provided. The systems contain a sufficient amount of sufentanil to induce and maintain a constant state of analgesia when applied to a subject. The systems are characterized as having one or more features including a high degree of dosage form rate control over flux of sufentanil from the system, a high net flux of sufentanil from the system through the skin, lack of a permeation enhancer, an adhesive member demonstrating superior shear time, a low coefficient of variation in the net flux of sufentanil from the system, a high delivery efficiency, and a substantially constant steady state net flux of sufentanil from the system. Methods of using the transdermal delivery systems to administer a sufficient amount of sufentanil to induce and maintain analgesia for extended periods when applied to a subject are also provided.
    Type: Grant
    Filed: July 31, 2007
    Date of Patent: August 28, 2012
    Assignee: Durect Corporation
    Inventors: Su Il Yum, Felix Theeuwes
  • Publication number: 20120214777
    Abstract: A stabilized bioadhesive composition containing an alkaline labile drug and a method for its preparation are provided. In one aspect, the composition is a hot-melt extruded (HME) composition comprising a preformed excipient mixture comprising an acidic component and an alkaline thermoplastic matrix-forming material, e.g. polymer. The excipient mixture is formed before blending with an alkaline labile drug. The blend is then hot-melt extruded to form the HME composition. By so doing, the acidic component is able to neutralize or render moderately acidic the excipient mixture. This particular process has been shown to substantially reduce the degradation of an alkaline labile drug during hot-melt extrusion. The excipient mixture softens or melts during hot-melt extrusion. It can dissolve or not dissolve drug-containing particles during extrusion.
    Type: Application
    Filed: May 3, 2012
    Publication date: August 23, 2012
    Applicant: Auxilium U.S. Holdings, LLC
    Inventors: Michael M. Crowley, Justin M. Keen, John J. Koleng, Feng Zhang
  • Patent number: 8246977
    Abstract: Transdermal delivery systems for administering sufentanil through the skin are provided. The systems contain a sufficient amount of sufentanil to induce and maintain a constant state of analgesia when applied to a subject. The systems are characterized as having one or more features including a high degree of dosage form rate control over flux of sufentanil from the system, a high net flux of sufentanil from the system through the skin, lack of a permeation enhancer, an adhesive member demonstrating superior shear time, a low coefficient of variation in the net flux of sufentanil from the system, a high delivery efficiency, and a substantially constant steady state net flux of sufentanil from the system. Methods of using the transdermal delivery systems to administer a sufficient amount of sufentanil to induce and maintain analgesia for extended periods when applied to a subject are also provided.
    Type: Grant
    Filed: October 21, 2005
    Date of Patent: August 21, 2012
    Assignee: Durect Corporation
    Inventors: Su Il Yum, Felix Theeuwes
  • Publication number: 20120208849
    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: Application
    Filed: February 8, 2012
    Publication date: August 16, 2012
    Applicant: ELI LILLY AND COMPANY
    Inventors: Garret Conrad Newbound, Terrence Patrick Clark
  • Publication number: 20120207798
    Abstract: The present invention relates to a method of attaching a handle to a solid oral dosage form by use of high frequency mechanical vibrations. The present invention also relates to a method of attaching a handle to a solid oral dosage form, the method comprising: (a) placing a handle in contact with a solid oral dosage form, wherein an area of contact between the handle and the solid oral dosage form forms a joint interface; (b) applying high frequency mechanical vibrations to the joint interface until the solid oral dosage form at the joint interface reaches a molten state; and (c) cooling the joint interface in a molten state to allow solidification, thereby attaching the handle to the solid oral dosage form.
    Type: Application
    Filed: April 26, 2012
    Publication date: August 16, 2012
    Applicant: Teva Women's Health, Inc.
    Inventors: Tahseen A. CHOWDHURY, Edward J. GABRIELSKI, Christopher H. BAKER
  • Publication number: 20120209223
    Abstract: Disclosed is a transdermal therapeutic system for administering an active ingredient through the skin comprising: a) a back layer, b) a reservoir on the back layer comprising b1) a first layer containing active ingredient, at least one gel former, at least one plasticizer, and a first polyisobutylene; and b2) a second layer containing active ingredient, at least one gel former, at least one plasticizer, and a second polyisobutylene, wherein the first polyisobutylene is different from the second polyisobutylene, wherein at least the first layer contains undissolved active ingredient in the form of active ingredient particles; and wherein the active ingredient is fentanyl or an analogue of the fentanyl.
    Type: Application
    Filed: September 14, 2010
    Publication date: August 16, 2012
    Applicant: ACINO AG
    Inventors: Nouha Salman, Bjoern Schurad, Ingo Teutsch
  • Patent number: 8242175
    Abstract: New histone deacetylase inhibitors according to the general formula (I) wherein: Q is a bond, CH2, CH—NR3R4, NR5 or oxygen, X is CH or nitrogen, Y is a bond, CH2, oxygen or NR6, Z is CH or nitrogen, R1, R2 are, independently, hydrogen, halogen, C1-C6 alkyl or C1-C6 haloalkyl, R11, R12 are, independently, hydrogen or C1-C6 alkyl, and R3, R4, R5 and R6 are as further defined in the specification.
    Type: Grant
    Filed: December 7, 2010
    Date of Patent: August 14, 2012
    Assignee: DAC S.R.L.
    Inventors: Antonello Mai, Saverio Minucci, Florian Thaler, Gilles Pain, Andrea Colombo, Stefania Gagliardi, Pier Giuseppe Pelicci, Marco Ballarini, Gaetano Gargiulo, Silvio Massa
  • Publication number: 20120184581
    Abstract: The invention provides compounds that are chemically modified by covalent attachment of a water-soluble oligomer. A compound of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different from those of the compound not attached to the water-soluble oligomer.
    Type: Application
    Filed: July 21, 2010
    Publication date: July 19, 2012
    Applicant: Nektar Therapeutics
    Inventors: Jennifer Riggs-Sauthier, Bo-Liang Deng, Timothy A. Riley
  • Publication number: 20120178741
    Abstract: This invention comprises the novel compounds of formula (I) wherein n, m, t, R1, R2, R3, R4, R5, L, Q, X, Y, Z and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.
    Type: Application
    Filed: March 21, 2012
    Publication date: July 12, 2012
    Applicant: JANSSEN PHARMACEUTICA N.V.
    Inventors: Kristof Van Emelen, Leo Jacobus Jozel Backx, Sven Franciscus Anna Van Brandt, Patrick René Angibaud, Isabelle Noélle Constance Pilatte, Marc Gustaaf Celine Verdonck, Hans Louis Jos De Winter, Jimmy Arnold Viviane Van heusden
  • Publication number: 20120165360
    Abstract: The invention provides amino- and amido-aminotetralin compounds of formula (I): wherein R1, R2, R3, R4, R5, R6, R7, and n are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.
    Type: Application
    Filed: March 5, 2012
    Publication date: June 28, 2012
    Applicant: THERAVANCE, INC.
    Inventors: Sean G. Trapp, Michael R. Leadbetter, Daniel D. Long, Lan Jiang, Sabine Axt
  • Patent number: 8198262
    Abstract: Methods of treating, preventing and/or managing cancer as well as and diseases and disorders associated with, or characterized by, undesired angiogenesis are disclosed. Specific methods encompass the administration of an immunomodulatory compound alone or in combination with a second active ingredient. The invention further relates to methods of reducing or avoiding adverse side effects associated with chemotherapy, radiation therapy, hormonal therapy, biological therapy or immunotherapy which comprise the administration of an immunomodulatory compound. Pharmaceutical compositions, single unit dosage forms, and kits suitable for use in methods of the invention are also disclosed.
    Type: Grant
    Filed: August 19, 2008
    Date of Patent: June 12, 2012
    Assignee: Celgene Corporation
    Inventor: Jerome B. Zeldis
  • Publication number: 20120141471
    Abstract: The present invention includes compositions that are useful in preventing or treating metastasis in a subject diagnosed with cancer. The present invention also includes methods of preventing or treating metastasis in a subject diagnosed with cancer, wherein the method comprises administering to the subject in need thereof an effective amount of a pharmaceutical formulation comprising at least one pharmaceutically acceptable carrier and at least one CX3CR1 or fractalkine antagonist.
    Type: Application
    Filed: December 6, 2011
    Publication date: June 7, 2012
    Inventors: Joseph M. Salvino, Olimpia Meucci, Alessandro Fatatsis, Whitney L. Jamieson
  • Publication number: 20120142668
    Abstract: Disclosed are 4-amino-2-butenamides of Formula (I) having pharmacological activity, pharmaceutical compositions containing them, and methods for the treatment of diseases mediated by the cathepsin C enzyme such as chronic obstructive pulmonary disease.
    Type: Application
    Filed: August 11, 2010
    Publication date: June 7, 2012
    Inventors: Niall Anderson, Ann M. Bullion, Neysa Nevins, Michael R. Palovich, Steven L. Sollis, Michael D. Wall, Jakob Busch-Petersen, Brian Evans, Huijie Li
  • Publication number: 20120129816
    Abstract: The present invention relates to novel aryl sulfonamide amine compounds of the formula (I), their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates described herein and pharmaceutically acceptable compositions containing them.
    Type: Application
    Filed: March 3, 2009
    Publication date: May 24, 2012
    Applicant: Suven Life Sciences Limited
    Inventors: Ramakrishna Nirogi, Anil Karbhari Shinde, Rama Sastri Kambhampati, Pradeep Jayarajan, Gopinadh Bhyrapuneni, Venkateswarlu Jasti
  • Publication number: 20120122870
    Abstract: Ischemia-reperfusion injury remains a primary cause of morbidity and mortality in individuals who experience disruption of normal blood flow to one or more major organs. For example, there are no clinically proven strategies that prevent acute renal failure following cardiac surgery. The present invention provides a variety of methods for the treatment or prevention of ischemia-reperfusion injury. In one aspect of the invention, a method for treating or preventing ischemia-reperfusion injury includes administering to a subject an effective amount of a sphingosine kinase inhibitor. Sphingosine kinase inhibitors are very effective in the protection against IR-induced acute renal failure and liver failure. Moreover, the effects occur very early after administration, requiring only a very short time of treatment. Toxicology studies with sphingosine kinase inhibitors demonstrate that they have low toxicity, even in long-term treatment.
    Type: Application
    Filed: May 10, 2010
    Publication date: May 17, 2012
    Applicants: MUSC FOUNDATION FOR RESEARCH DEVELOPMENT, APOGEE BIOTECHNOLOGY CORPORATION
    Inventors: Charles D. Smith, Zhi Zhong, Lynn W. Maines
  • Publication number: 20120122792
    Abstract: S-t-butyl protected cysteine di-peptide analogs and related compounds and methods of using these compounds for the treatment of diseases and/or conditions, including but not limited to diseases and/or conditions of Central Nervous System (CNS).
    Type: Application
    Filed: November 11, 2011
    Publication date: May 17, 2012
    Applicant: PROMENTIS PHARMACEUTICALS, INC.
    Inventors: Edward M. Johnson, II, Daniel G. Lawton
  • Publication number: 20120115907
    Abstract: The present invention relates to novel renin inhibitors of general formula (1), novel intermediates involved in their synthesis, their pharmaceutically acceptable salts and pharmaceutical compositions containing them. The present invention also relates to a process of preparing compounds of general formula (1), their tautomeric forms, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, and novel intermediates involved in their synthesis.
    Type: Application
    Filed: April 22, 2010
    Publication date: May 10, 2012
    Applicant: CADILA HEALTHCARE LIMITED
    Inventors: Pravain Thombare, Jigar Desai, Mukul R. Jain
  • Publication number: 20120115850
    Abstract: The invention relates to 5-HT6 receptor antagonists. Novel arylamine compounds and use of these compounds and their pharmaceutical compositions, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with serotonin action, such as in treating obesity, and obesity-related disorders, e.g., cardiovascular disease, digestive disease, respiratory disease, cancer and type II diabetes; and psychological disorders such as schizophrenia, are disclosed.
    Type: Application
    Filed: May 10, 2011
    Publication date: May 10, 2012
    Inventors: Oren Becker, Rosa Melendez, Yael Marantz, Anurag Sharadendu, Merav Fichman, Mercedes Lobera, Hanoch Senderowitz, Srinivasa Rao Cheruku, Sharon Shacham, Laurence Wu, Ashis Saha, Pini Orbach, Dale S. Dhanoa
  • Publication number: 20120095386
    Abstract: Device structure 100 for iontophoresis provides electrode 101 and electrically conductive layer 102. Electrically conductive layer 102 contains active ingredient D and basic water swelling methacrylate copolymer P1 and/or acidic water swelling methacrylate copolymer P2. Electrode 101 and electrically conductive layer 102 are placed into a hollow of backing 103 and electrode terminal 104 is connected to electrode 101 through backing 103. Adhesive layer 105 is set around backing 103, and liner 106 to be removed when using the device, is placed so as to cover the hollow of backing 103.
    Type: Application
    Filed: October 1, 2010
    Publication date: April 19, 2012
    Applicant: HISAMITSU PHARMACEUTICAL CO., INC.
    Inventors: Hirotoshi Adachi, Noriyuki Kuzumaki, Tetsuya Arimoto, Naruhito Higo
  • Publication number: 20120094989
    Abstract: The present invention relates to compounds having 5-hydroxytryptamine receptor modulating activity, in particular compounds having an acidic moiety held distant from the 5-HT pharmacophore by a rigid linker group, to compositions containing such compounds and methods of treatment using them. Such compounds have an increased affinity for the 5-HT receptor and a reduced hERG effect. Certain compounds of the invention further exhibit an angiotensin II receptor modulating activity. Claimed are compounds of formula (I): HT-L-A. HT is a 5-HT receptor modulating moiety containing a basic nitrogen atom; A is an acid moiety; L is a linker moiety.
    Type: Application
    Filed: April 1, 2010
    Publication date: April 19, 2012
    Applicant: SERODUS AS
    Inventors: Jo Klaveness, Bjame Brudeli, Finn Olav Levy, Lise Roman Moltzau, Trygve Gulbrandsen
  • Patent number: 8158651
    Abstract: The treatment of acute pain with a sufficient dosage by intranasal administration of fentanyl results in a time to onset of action comparable to intravenous administration and a significantly faster onset of action than nasal titration of fentanyl. The nasal administration of a sufficient amount of fentanyl to obtain pain relief has lower maximum plasma concentrations comparable to intravenous administration and results in lower rates of adverse events like respiratory depression, nausea and vomiting. Compositions fur use in the method are also disclosed.
    Type: Grant
    Filed: January 24, 2007
    Date of Patent: April 17, 2012
    Assignee: Nycomed Danmark Aps
    Inventors: Jesper Grarup, Hanne Wulf Nielsen
  • Publication number: 20120088787
    Abstract: The invention provides 3-carboxypropyl-aminotetralin compounds of formula (I): wherein R1, R2, R3, R4, R5, and R6 are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.
    Type: Application
    Filed: December 19, 2011
    Publication date: April 12, 2012
    Applicant: THERAVANCE, INC.
    Inventors: Sean G. Trapp, Michael R. Leadbetter, Daniel D. Long, John R. Jacobsen, Priscilla Van Dyke, Pierre-Jean Colson, Miroslav Rapta, Ying Yu
  • Patent number: 8148405
    Abstract: The invention provides N-{2-[((2S)-3-{[1-(4-chlorobenzyl)piperidin-4-yl]amino}-2-hydroxy-2-methylpropyl)oxy]-4-hydroxyphenyl}acetamide benzoate or a solvate thereof, pharmaceutical compositions containing the salt or solvate and use of the salt or solvate in therapy.
    Type: Grant
    Filed: July 31, 2006
    Date of Patent: April 3, 2012
    Assignee: AstraZeneca AB
    Inventors: Julien Giovannini, Bo-Goran Josefsson
  • Publication number: 20120071511
    Abstract: Disclosed is a fentanyl-containing adhesive preparation for external use, wherein an adhesive layer is laminated on a supporting body. The adhesive layer contains SIS, a tackifier resin that is composed of a rosin resin and terpene resin, and a softener that is composed of a plybutene and a liquid paraffin. The adhesive layer also contains fentanyl as an active ingredient. The fentanyl-containing adhesive preparation for external use has excellent skin permeation of fentanyl and high preparation stability, without suffering from crystallization of fentanyl during storage.
    Type: Application
    Filed: July 21, 2010
    Publication date: March 22, 2012
    Inventors: Mamoru Naruse, Kenichi Hattori, Kunihiko Matsushita