Imidazoles Patents (Class 514/396)
  • Patent number: 8513294
    Abstract: Disclosed are compounds of the general formula (I): compositions comprising an effective amount of said compounds either alone or in combination with other chemotherapeutic agents, and methods useful for treating or preventing cancer and for inhibiting tumor tissue growth. These compounds attenuate the oxidative damage associated with increased heme-oxygenase activity and can reduce cell proliferation in transformed cells. In addition, the described compounds and compositions are useful as neuroprotectants and for treating or preventing neurodegenerative disorders and other diseases of the central nervous system.
    Type: Grant
    Filed: January 13, 2011
    Date of Patent: August 20, 2013
    Assignees: Osta Biotechnologies, Queens University at Kingston, The Sir Mortimer B. Davis-Jewish General Hospital
    Inventors: Ajay Gupta, Hyman M. Schipper, Moulay Alaoui-Jamali, Walter A. Szarek, Kanji Nakatsu, Jason Z. Vlahakis
  • Patent number: 8507542
    Abstract: The presently disclosed subject matter relates to methods of administering an effective amount of dexmedetomidine to a pediatric patient in order to reduce the incidence of neurological damage. More particularly, the presently disclosed subject matter relates to methods of providing sedation or analgesia to a pediatric patient by administering a dexmedetomidine infusion and optionally a loading dose. The dexmedetomidine can be administered before, during, or after surgery.
    Type: Grant
    Filed: December 24, 2012
    Date of Patent: August 13, 2013
    Assignee: Hospira, Inc.
    Inventors: Marcelo Garcia da Rocha, Wayne Wisemandle, Dennis Stalker, Edward Koo
  • Publication number: 20130202657
    Abstract: The present invention generally relates to foams and, in particular, to foams for applications such as drug delivery, and particles that are made from such foams. One aspect relates to foams or particles containing pharmaceutically active agents. The foam may comprise a pharmaceutically acceptable polymeric carrier. In some cases, the foam or particle has an unexpectedly high specific surface area. A high specific surface area may, in some cases, facilitate delivery or release of the pharmaceutically active agent when the foam or particles made from the foam (e.g., by milling) are administered to a subject. The foam may also exhibit a relatively high loading of the pharmaceutically active agent. In some cases, the foam may be a microcellular foam. In one set of embodiments, the foam is created using a supercritical fluid, such as supercritical C02.
    Type: Application
    Filed: May 20, 2011
    Publication date: August 8, 2013
    Applicants: BASF SE, President and Fellows of Harvard College
    Inventors: Kosta Ladavac, Rodrigo E. Guerra, David Kaz, Vinothan Manoharan, Jens B. Rieger, Roland S. Koltzenburg, David A. Weitz
  • Patent number: 8501743
    Abstract: A personal care composition comprising a eutectic mixture, the eutectic mixture comprising a tertiary system, in which menthol may form part of the eutectic mixture or in the eutectic mixture comprises an antidandruff agent such as ketoconazole.
    Type: Grant
    Filed: November 4, 2008
    Date of Patent: August 6, 2013
    Assignee: Conopco, Inc.
    Inventors: Jason Shaun Burry, Richard Livesey Evans, Caroline Alexandra Hall, Ezat Khoshdel, Colina MacKay
  • Patent number: 8501798
    Abstract: The invention relates to compounds having the formula: wherein: Q, W, Y, Z, r, and Ar are as defined in the specification, and pharmaceutically acceptable salts thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
    Type: Grant
    Filed: June 19, 2012
    Date of Patent: August 6, 2013
    Assignee: Theravance, Inc.
    Inventors: Paul Allegretti, Seok-Ki Choi, Roland Gendron, Paul R. Fatheree, Robert Murray McKinnell
  • Patent number: 8501796
    Abstract: The present invention relates to method of lowering intraocular pressure in a subject in need of such treatment, which comprises administering a therapeutically effective amount of a composition comprising a ester pro-drugs of [3-(1-(1H-imidazol-4-yl)ethyl)-2-methylphenyl]methanol, of enantiomers thereof, of tautomers thereof, pharmaceutical compositions containing them and their use as pharmaceuticals.
    Type: Grant
    Filed: September 15, 2011
    Date of Patent: August 6, 2013
    Assignee: Allergan, Inc.
    Inventors: Mohammad I. Dibas, Daniel W. Gil, John E. Donello, Ken Chow, Liming Wang, Michael E. Garst
  • Patent number: 8492553
    Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.
    Type: Grant
    Filed: September 7, 2012
    Date of Patent: July 23, 2013
    Assignee: Bristol-Myers Squibb Company
    Inventors: Carol Bachand, Makonen Belema, Daniel H. Deon, Andrew C. Good, Jason Goodrich, Clint A. James, Rico Lavoie, Omar D. Lopez, Alain Martel, Nicholas A. Meanwell, Van N. Nguyen, Jeffrey Lee Romine, Edward H. Ruediger, Lawrence B. Snyder, Denis R. St. Laurent, Fukang Yang, David R. Langley, Lawrence G. Hamann
  • Patent number: 8492568
    Abstract: The present invention provides chromane derivatives as transient receptor potential vanilloid (TRPV) modulators. In particular, the compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPV3. Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPV3.
    Type: Grant
    Filed: May 19, 2009
    Date of Patent: July 23, 2013
    Assignee: Glenmark Pharamceuticals S.A.
    Inventors: V. S. Prasada Rao Lingam, Abraham Thomas, Javed Yusuf Khatik, Neelima Khairatkar-Joshi, Vidya Ganapati Kattige
  • Patent number: 8486985
    Abstract: The invention provides methods for treating disorders associated with selective subtype modulation of alpha 2 adrenergic receptors. In particular, the invention provides methods employing well-defined N-[1-(2 and/or 3-substituted-phenyl)-alkyl]-(4,5-dihydro-1H-imidazol-2-yl)-amines and pharmaceutical compositions thereof to treat disorders associated with selective subtype alpha 2 adrenergic receptor modulation, such as ocular disorders, pain and central nervous system (CNS) motor disorders.
    Type: Grant
    Filed: May 11, 2009
    Date of Patent: July 16, 2013
    Assignee: Allergan, Inc.
    Inventors: Phong X. Nguyen, Ken Chow, Todd M. Heidelbaugh
  • Patent number: 8486980
    Abstract: Provided is a tricyclic compound having a PPAR ? agonist activity, which is represented by the general formula (I) wherein Z represents a single bond or the like, Y represents a hydrogen atom, lower alkyl optionally having substituent(s) or the like, X represents a hydrogen atom or the like, A represents aryl or the like, B and C are the same or different and each represents an aromatic carbocycle or the like, R4-R9 are the same or different and each represents hydrogen or the like, V represents a single bond or the like, R10 and R11 are the same or different and each represents hydrogen or the like, or a pharmaceutically acceptable salt thereof or the like:
    Type: Grant
    Filed: August 6, 2009
    Date of Patent: July 16, 2013
    Assignee: Kyowa Hakko Kirin Co., Ltd.
    Inventors: Arata Yanagisawa, Keiji Uehara, Masahiro Matsubara, Kimihisa Ueno, Michihiko Suzuki, Takeshi Kuboyama, Keisuke Yamamoto, Tomohiro Tamura
  • Publication number: 20130178465
    Abstract: The present invention provides intranasal formulations comprising dexmedetomidine, or a pharmaceutically acceptable salt thereof, and uses thereof.
    Type: Application
    Filed: December 11, 2012
    Publication date: July 11, 2013
    Applicant: RECRO PHARMA, INC.
    Inventor: Recro Pharma, Inc.
  • Publication number: 20130172357
    Abstract: The invention provides ?-2 adrenergic receptor agonist compositions and methods for treating glaucoma and other intraocular conditions. The preferred ?-2 agonist used in the inventive compositions and methods is dexmedetomidine.
    Type: Application
    Filed: February 5, 2013
    Publication date: July 4, 2013
    Applicant: EYE THERAPIES LLC
    Inventor: Eye Therapies LLC
  • Publication number: 20130165488
    Abstract: The present invention relates to novel TP receptor antagonists, which optionally cross the blood-brain barrier of a mammal. The invention also provides methods for treating a disorder related to activation of TP receptor utilizing the compounds of the invention.
    Type: Application
    Filed: February 28, 2013
    Publication date: June 27, 2013
    Applicant: The Trustees of the University of Pennsylvania
    Inventor: The Trustees of the University of Pennsylvania
  • Patent number: 8470862
    Abstract: A method for the prevention and treatment of hypotension and shock due to low peripheral resistance, comprising administering to a mammal in need thereof an effective amount of a certain imidazole derivative or pharmaceutically acceptable ester or salt thereof, and a method for the treatment of cardiopulmonary resuscitation, comprising administering to a mammal in need thereof an effective amount of a certain imidazole derivative or pharmaceutically acceptable ester or salt thereof.
    Type: Grant
    Filed: April 28, 2011
    Date of Patent: June 25, 2013
    Assignee: Recro Pharma, Inc.
    Inventors: Riitta Heino, Tiina Leino, Tarja Lehtimäki
  • Patent number: 8461192
    Abstract: PKCiota inhibitor 1H-imidazole-4-carboxamide, 5-amino-1-[2,3-dihydroxy-4-[(phosphonooxy)methyl]cyclopentyl]-,[1R-(1?,2?,3?,4?)], (ICA-1), targets a unique sequence (amino acid residues 469-475) in the catalytic domain of PKCiota and inhibits PKCiota activity. The data shows suprising and unexpected ability of ICA-1 to selectively inhibit the proliferation of cells that overexpress PKCiota.
    Type: Grant
    Filed: September 15, 2008
    Date of Patent: June 11, 2013
    Assignees: The University of South Florida, The United States of America Department of Veterans Affairs, The University of Florida Research Foundation, Inc.
    Inventors: Mildred Acevedo-Duncan, Shraddha R. Desai, Hla Yee Win, David A. Ostrov, Prajit P. Pillai, Diondra D. Hill
  • Publication number: 20130143938
    Abstract: Pharmaceutical compositions for the treatment of nasal congestion or migraine, wherein the pharmaceutical compositions comprise low concentrations of a super-selective subclass of selective ?-2 adrenergic receptor agonists.
    Type: Application
    Filed: February 1, 2013
    Publication date: June 6, 2013
    Applicant: Eye Therapies LLC
    Inventor: Eye Therapies LLC
  • Patent number: 8455527
    Abstract: The presently disclosed subject matter relates to pharmaceutical compositions comprising dexmedetomidine or a pharmaceutically acceptable salt thereof wherein the composition is formulated as a liquid for parenteral administration to a subject, and wherein the composition is disposed within a sealed container as a premixture. The pharmaceutical compositions can be used, for example, in perioperative care of a patient or for sedation.
    Type: Grant
    Filed: November 15, 2012
    Date of Patent: June 4, 2013
    Assignee: Hospira, Inc.
    Inventors: Priyanka Roychowdhury, Robert A. Cedergren
  • Publication number: 20130136784
    Abstract: A method utilizing a dissolvable device for the internal delivery of medication and more particularly to the use of fibers or non-woven fabrics made of a safe polymer material incorporating a medication that is released by dissolution of the fibers or non-woven fabrics over time, and more particularly a treatment method for controlling or regulating the pH in the vagina by stabilizing and adjusting the pH in the vagina by minimizing the impact of the vaginal flora.
    Type: Application
    Filed: January 23, 2013
    Publication date: May 30, 2013
    Inventor: Robert J. Staab
  • Patent number: 8450318
    Abstract: Molecules having a spacer unit, linker and recognition unit(s) are used for the treatment of various diseases, disorders and conditions. The compounds are useful in treating infectious diseases and diseases, disorders or conditions related thereto. Further, the methods for treating diseases, disorders or conditions involve recognition and binding of carbohydrate structures.
    Type: Grant
    Filed: March 18, 2008
    Date of Patent: May 28, 2013
    Assignees: K.U. Leuven Research and Development
    Inventors: Monika Mazik, Jan Balzarini
  • Patent number: 8450353
    Abstract: Topical compositions and methods of use to treat symptoms of reduced skin elasticity are provided comprising desthiobiotin and certain desthiobiotin analogues. These compounds are effective in stimulating LOXL-1 activity and can thus increase elastin remodeling and improve appearance of fine lines, wrinkles, skin sagging and other symptoms of reduced elastin function.
    Type: Grant
    Filed: November 19, 2008
    Date of Patent: May 28, 2013
    Assignee: Avon Products, Inc.
    Inventors: Dmitri S. Ptchelintsev, Xiaochun Luo, Siming W. Chen
  • Patent number: 8450354
    Abstract: The present invention provides substituted imidazo[1,2-b]pyridazine derivatives, pharmaceutically acceptable salts thereof, and tautomers of any of the foregoing, where such compounds inhibit ?-site amyloid precursor protein-cleaving enzyme (BACE), which may be useful in the treatment of diseases in which BACE is involved, such as Alzheimer's disease. The invention also provides pharmaceutical compositions comprising any of these compounds and the use of any of these compounds and compositions in the treatment of diseases, disorders, or conditions in which BACE is involved.
    Type: Grant
    Filed: March 21, 2011
    Date of Patent: May 28, 2013
    Assignee: High Point Pharmaceuticals, LLC
    Inventors: Adnan M. M. Mjalli, Anitha Hari, Bapu Gaddam, Devi Reddy Gohimukkula, Dharma Rao Polisetti, Mohan Rao, Raju Bore Gowda, Robert Carl Andrews, Rongyuan Xie, Soumya P. Sahoo, Tan Ren, William Kenneth Banner
  • Publication number: 20130131133
    Abstract: The present invention relates to pharmaceutical compositions, containing 4-[1-(2,3-dimethylphenyl)ethyl]-1H-imidazole, (S) 4-[1-(2,3-dimethylphenyl)ethyl]-1H-imidazole or (S) [3-(1-(1H-imidazol-4-yl)ethyl)-2-methylphenyl]methanol, their use as pharmaceuticals for the treatment of retinal diseases, for retinal neuroprotection and vision enhancement.
    Type: Application
    Filed: November 19, 2012
    Publication date: May 23, 2013
    Applicant: Allergan, Inc.
    Inventor: Allergan, Inc.
  • Patent number: 8445526
    Abstract: The invention provides ?-2 adrenergic receptor agonist compositions and methods for treating glaucoma and other intraocular conditions. The preferred ?-2 agonist used in the inventive compositions and methods is dexmedetomidine.
    Type: Grant
    Filed: August 14, 2012
    Date of Patent: May 21, 2013
    Assignee: Glaucoma & Nasal Therapies LLC
    Inventor: Gerald Horn
  • Patent number: 8445525
    Abstract: The present invention relates to new substituted carboxylic acid amides of general formula wherein A, B and R1 to R5 are defined as in claim 1, the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties.
    Type: Grant
    Filed: December 2, 2010
    Date of Patent: May 21, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Henning Priepke, Kai Gerlach, Roland Pfau, Norbert Hauel, Iris Kauffmann-Hefner, Georg Dahmann, Herbert Nar, Sandra Handschuh, Wolfgang Wienen, Annette Schuler-Metz
  • Patent number: 8436002
    Abstract: The present invention provides AKT inhibitors of the formula: Formula I The present invention also provides pharmaceutical compositions comprising compounds of Formula I, uses of compounds of Formula I and method of using compounds of Formula I.
    Type: Grant
    Filed: October 20, 2010
    Date of Patent: May 7, 2013
    Assignee: Eli Lilly and Company
    Inventors: Douglas Wade Beight, Timothy Paul Burkholder, Joshua Ryan Clayton, MariJean Eggen, Kenneth James Henry, Jr., Deidre Michelle Johns, Saravanan Parthasarathy, Huaxing Pei, Mark Edward Rempala, Jason Scott Sawyer
  • Patent number: 8435996
    Abstract: The invention relates to compounds that are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.
    Type: Grant
    Filed: July 31, 2008
    Date of Patent: May 7, 2013
    Assignee: Synta Pharmaceuticals Corp.
    Inventor: Shoujun Chen
  • Patent number: 8436033
    Abstract: The presently disclosed subject matter relates to pharmaceutical compositions comprising dexmedetomidine or a pharmaceutically acceptable salt thereof wherein the composition is formulated as a liquid for parenteral administration to a subject, and wherein the composition is disposed within a sealed container as a premixture. The pharmaceutical compositions can be used, for example, in perioperative care of a patient or for sedation.
    Type: Grant
    Filed: November 15, 2012
    Date of Patent: May 7, 2013
    Assignee: Hospira, Inc.
    Inventors: Priyanka Roychowdhury, Robert A. Cedergren
  • Patent number: 8436036
    Abstract: Compounds of the formula I: including any possible stereoisomers thereof, or a pharmaceutically acceptable salt and/or solvate thereof, as well as pharmaceutical formulations and the use of compounds of formula I as HCV inhibitors.
    Type: Grant
    Filed: April 23, 2010
    Date of Patent: May 7, 2013
    Assignee: Janssen R&D Ireland
    Inventors: Samuel Dominique Demin, David McGowan, Stefaan Julien Last, Pierre Jean-Marie Bernard Raboisson
  • Publication number: 20130096172
    Abstract: The presently disclosed subject matter relates to methods of administering an effective amount of dexmedetomidine to a pediatric patient in order to reduce the incidence of neurological damage. More particularly, the presently disclosed subject matter relates to methods of providing sedation or analgesia to a pediatric patient by administering a dexmedetomidine infusion and optionally a loading dose. The dexmedetomidine can be administered before, during, or after surgery.
    Type: Application
    Filed: December 24, 2012
    Publication date: April 18, 2013
    Applicant: HOSPIRA, INC.
    Inventor: HOSPIRA, INC.
  • Publication number: 20130096171
    Abstract: The presently disclosed subject matter relates to methods of administering an effective amount of dexmedetomidine to a pediatric patient in order to reduce the incidence of neurological damage. More particularly, the presently disclosed subject matter relates to methods of providing sedation or analgesia to a pediatric patient by administering a dexmedetomidine infusion and optionally a loading dose. The dexmedetomidine can be administered before, during, or after surgery.
    Type: Application
    Filed: December 24, 2012
    Publication date: April 18, 2013
    Applicant: HOSPIRA, INC.
    Inventor: HOSPIRA, INC.
  • Publication number: 20130096170
    Abstract: The presently disclosed subject matter relates to methods of administering an effective amount of dexmedetomidine to a pediatric patient in order to reduce the incidence of neurological damage. More particularly, the presently disclosed subject matter relates to methods of providing sedation or analgesia to a pediatric patient by administering a dexmedetomidine infusion and optionally a loading dose. The dexmedetomidine can be administered before, during, or after surgery.
    Type: Application
    Filed: January 4, 2012
    Publication date: April 18, 2013
    Applicant: HOSPIRA, INC.
    Inventors: Marcelo Garcia da Rocha, Wayne Wisemandle, Dennis James Stalker, Edward Koo
  • Patent number: 8414931
    Abstract: Disclosed is a wood preservative composition comprising micronized copper and copper-amine complex, wherein the copper component of the copper amine complex is from about 5% to about 50% by weight, based upon the total weight of copper in the composition. The copper amine complex serves to avoid wood surface “chalking” that is otherwise attributable to the presence of micronized copper in copper-based slurries used to treat wood products. In addition, the copper-amine complex enhances the antimicrobial efficacy of the composition when used in wood treatment applications by facilitating cell wall penetration of the treated wood.
    Type: Grant
    Filed: September 13, 2012
    Date of Patent: April 9, 2013
    Assignee: Arch Wood Protection, Inc.
    Inventor: Jayesh P. Patel
  • Patent number: 8410155
    Abstract: The present invention provides compounds of Formula (I) or (II): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L1, R3, R4, R8a, R11 and M are as defined herein. The compounds of Formula (I) or (II) are selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors or dual inhibitors of fXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.
    Type: Grant
    Filed: December 13, 2007
    Date of Patent: April 2, 2013
    Assignee: Bristol-Myers Squibb Company
    Inventor: Donald J. P. Pinto
  • Patent number: 8410150
    Abstract: A CPT inhibitor compound is represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof: or a pharmaceutically acceptable salt thereof. A pharmaceutical composition comprises a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. A method of treating a subject having cancer comprises administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: March 6, 2008
    Date of Patent: April 2, 2013
    Assignee: University Health Network
    Inventors: Heinz W. Pauls, Peter Brent Sampson, Bryan T. Forrest, Radoslaw Laufer, Yong Liu, Miklos Feher, Yi Yao, Guohua Pan
  • Patent number: 8409550
    Abstract: A skin care product comprising from about 0.001% to about 10% of a retinoid, in combination with 0.0001% to about 50% of at combination of retinoid boosters.
    Type: Grant
    Filed: June 21, 2012
    Date of Patent: April 2, 2013
    Assignee: Unilever Home & Personal Care, USA, Division of Conopco, Inc.
    Inventors: Stewart Paton Granger, Ian Richard Scott, Robert Mark Donovan, Susanne Teklits Iobst, Lisa Licameli
  • Publication number: 20130079344
    Abstract: Solutions for perioperative intraocular application by continuous irrigation during ophthalmologic procedures are provided. These solutions include multiple agents that act to inhibit inflammation, inhibit pain, effect mydriasis (dilation of the pupil), and/or decrease intraocular pressure, wherein the multiple agents are selected to target multiple molecular targets to achieve multiple differing physiologic functions, and are included in dilute concentrations in a balanced salt solution carrier.
    Type: Application
    Filed: March 14, 2012
    Publication date: March 28, 2013
    Applicant: OMEROS CORPORATION
    Inventors: Gregory A. Demopulos, Pamela Pierce Palmer, Jeffrey M. Herz
  • Patent number: 8404728
    Abstract: This disclosure relates to materials and methods for inhibiting Botulinum neurotoxin, and more particularly to materials and methods for inhibiting the zinc endopeptidase of Botulinum neurotoxin serotypes A, D and/or E (BoNTA, BoNTD and/or BoNTE).
    Type: Grant
    Filed: July 29, 2010
    Date of Patent: March 26, 2013
    Assignees: Mayo Foundation for Medical Education and Research, U.S. Army Medical Research and Material Command
    Inventors: Yuan-Ping Pang, Jewn Giew Park, Shaohua Wang, Anuradha Vummenthala, Rajesh K Mishra, Jon Davis, Charles B. Millard, James J. Schmidt
  • Patent number: 8404732
    Abstract: Methods of treating and managing ulcerative colitis, using imidazole-based compounds that inhibit S1P lyase, are disclosed.
    Type: Grant
    Filed: January 4, 2012
    Date of Patent: March 26, 2013
    Assignee: Lexicon Pharmaceuticals, Inc.
    Inventors: David J. Augeri, Jeffrey Bagdanoff, Lakmal W. Boteju, Kenneth G. Carson, Theodore C. Jessop, Spencer David Kimball
  • Publication number: 20130072532
    Abstract: Analgesic topical formulations of dexmedetomidine and methods of use thereof in the treatment and management of pain and other conditions.
    Type: Application
    Filed: January 7, 2011
    Publication date: March 21, 2013
    Applicant: Recro Pharma, Inc.
    Inventors: Geraldine A. Henwood, Randall J. Mack, Christopher T. Sharr, John J. Koleng, JR.
  • Patent number: 8399463
    Abstract: The invention relates to imidazole derivatives which have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1. The invention also relates to a pharmaceutically-suitable acid-addition salt of the above compound. The invention further relates to a composition comprising an imidazole derivative as described above, or a pharmaceutically-suitable acid-addition salt thereof, and to processes for preparing such compounds.
    Type: Grant
    Filed: September 19, 2011
    Date of Patent: March 19, 2013
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Guido Galley, Katrin Groebke Zbinden, Roger Norcross, Henri Stalder
  • Patent number: 8389570
    Abstract: The present invention is directed to certain hydroxamate derivatives that are useful in the treatment of hepatitis C. These compounds are also inhibitors of histone deacetylase and are therefore useful in the treatment of diseases associated with histone deacetylase activity. Pharmaceutical compositions and processes for preparing these compounds are also disclosed.
    Type: Grant
    Filed: August 12, 2011
    Date of Patent: March 5, 2013
    Assignee: Pharmacyclics, Inc.
    Inventors: Erik J. Verner, Martin Sendzik, Chitra Baskaran, Joseph J. Buggy, James Robinson
  • Publication number: 20130052248
    Abstract: An item of clothing (10) for daily pharmacological treatment of a fungal infection, comprising: a textile material (20) to manage moisture when the item of clothing (10) is worn; microcapsules (30) grafted on the textile material (20); and antifungal agents encapsulated within the microcapsules (30) to pharmacologically treat the fungal infection when released from the microcapsules (30).
    Type: Application
    Filed: August 26, 2011
    Publication date: February 28, 2013
    Inventors: Marcus Chun Wah YUEN, Joanne Yiu Wan YIP, Kevin CHEUK, Chi Wai KAN, Shuk Yan CHENG
  • Publication number: 20130045264
    Abstract: There is provided an antifouling coating composition capable of forming an antifouling coating film which has stable coating film consumption degree on ships, underwater structures and the like and which exhibits excellent antifouling property over a long term. The antifouling coating composition includes a hydrolyzable copolymer (A) and an antifouling agent (B), wherein the hydrolyzable copolymer (A) is, e.g., a metal salt bond-containing copolymer having a component unit derived from a monomer (a21) represented by the general formula (II): CH2?C(R2)—COO-M-O—CO—C(R2)?CH2??(II) [In the formula (II), M is zinc or copper, and R2 is a hydrogen atom or a methyl group], and a component unit derived from other unsaturated monomer (a22) copolymerizable with the monomer (a21), and wherein the antifouling agent (B) includes at least medetomidine.
    Type: Application
    Filed: March 18, 2011
    Publication date: February 21, 2013
    Applicant: CHUGOKU MARINE PAINTS, LTD.
    Inventors: Satoshi Masuda, Yusuke Hayashi, Yukio Kozono
  • Patent number: 8372871
    Abstract: Compounds of general formula (I) below: are characterized in that A represents in particular a C5-C10 heterocyclic group, Y represents in particular a single bond, and B represents in particular an aryl or heteroaryl group.
    Type: Grant
    Filed: November 10, 2009
    Date of Patent: February 12, 2013
    Assignee: Centre National de la Recherche Scientifique
    Inventors: Jean-Yves Winum, Jean-Louis Montero, Stephan Köhler
  • Publication number: 20130023490
    Abstract: The present invention provides for, inter alia, novel topical formulations comprising at least one 1-N-arypyrazole derivative and amitraz and to methods for treating, controlling, or preventing parasite infestations on mammals or birds The inventive formulations include spot-on, pour-on or spray formulations and may include a further ectoparasiticide, such as an IGR compound, an avermectin or milbemycin derivative, or a pyrethroid insecticides, and anthelmintics, such as benzimidazoles and imidazothiazoles. The inventive formulation provides a larger duration of parasite control at a faster rate of control. The inventive formula remains effective up to three months from the first application. Moreover, the inventive formulations prevent tick attachment to the animal, thereby providing protection against tick borne diseases. The ectoparasites which may be controlled, treated or prevented by the present invention includes ticks, fleas, mites, mange, lice, mosquitoes, flies and cattle grubs.
    Type: Application
    Filed: July 23, 2012
    Publication date: January 24, 2013
    Inventors: Albert BOECKH, Luiz Gustavo CRAMER, Mark D. SOLL
  • Patent number: 8357714
    Abstract: Provided are pharmaceutical compositions, and methods of use of the compositions, for the non-surgical treatment of ptosis (eyelid droop). In one embodiment the composition includes oxymetazoline 0.1% formulated for topical administration to an eye. In one embodiment the composition includes a synergistic combination of oxymetazoline and phenylephrine, formulated for topical administration to an eye. Oxymetazoline alone causes no pupillary dilation (mydriasis), and a synergistic combination of oxymetazoline and phenylephrine induces no clinically significant mydriasis. In addition to providing desirable cosmetic effects, the compositions and methods of the invention can improve visual fields otherwise compromised by ptosis.
    Type: Grant
    Filed: October 11, 2011
    Date of Patent: January 22, 2013
    Assignee: Voom, LLC
    Inventor: Mark Silverberg
  • Patent number: 8357715
    Abstract: Hetero-substituted acetanilide derivatives are disclosed as analgesic agents. The compounds of the invention are useful in methods for treating a disease or condition in a mammal characterized by pain and/or fever.
    Type: Grant
    Filed: March 31, 2010
    Date of Patent: January 22, 2013
    Assignee: Janssen Pharmaceutica, NV
    Inventors: John R. Carson, James J. McNally
  • Publication number: 20130012555
    Abstract: Dihydroxyaryl compounds and pharmaceutically acceptable esters, their synthesis, pharmaceutical compositions containing them, and their use in the treatment of IAPP or amylin fibril diseases, and the manufacture of medicaments for such treatment.
    Type: Application
    Filed: January 12, 2012
    Publication date: January 10, 2013
    Inventors: Thomas Lake, Alan D. Snow
  • Patent number: 8344011
    Abstract: The present invention is directed to novel opioid receptor modulators of Formula (I). The invention further relates to methods for preparing such compounds, pharmaceutical compositions containing them, and their use in the treatment of disorders that may be ameliorated or treated by the modulation of opioid receptors.
    Type: Grant
    Filed: July 19, 2010
    Date of Patent: January 1, 2013
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Henry J. Breslin, Chaozhong Cai, Wei He, Robert W. Kavash
  • Patent number: 8344012
    Abstract: Described herein are compounds useful in the modulation of blood uric acid levels, formulations containing them and methods of making and using them. In some embodiments, the compounds described herein are used in the treatment or prevention of disorders related to aberrant levels of uric acid.
    Type: Grant
    Filed: September 4, 2009
    Date of Patent: January 1, 2013
    Assignee: Ardea Biosciences, Inc.
    Inventors: Esmir Gunic, Jean-Luc Girardet, David A. Paisner