Benzene Ring Containing Patents (Class 514/741)
  • Patent number: 10081626
    Abstract: The invention provides novel 8-azabicyclo[3.2.1]octane compounds of formula (I): wherein R1, R2, R3, A, and G are defined in the specification, or a pharmaceutically-acceptable salt or solvate 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: Grant
    Filed: April 25, 2017
    Date of Patent: September 25, 2018
    Assignee: THERAVANCE BIOPHARMA R&D IP, LLC
    Inventors: Daniel D. Long, John R. Jacobsen, Lan Jiang
  • Patent number: 9663509
    Abstract: The invention provides novel 8-azabicyclo[3.2.1]octane compounds of formula (I): wherein R1, R2, R3, A, and G are defined in the specification, or a pharmaceutically-acceptable salt or solvate 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: Grant
    Filed: October 29, 2015
    Date of Patent: May 30, 2017
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventors: Daniel D. Long, John R. Jacobsen, Lan Jiang
  • Publication number: 20150110773
    Abstract: Methods and kits for GPP-targeting, e.g., for the treatment of oncogenic Kras-associated cancers, and methods for determining the efficacy of those methods are provided.
    Type: Application
    Filed: May 23, 2013
    Publication date: April 23, 2015
    Inventors: Alec C. Kimmelman, Jaekyoung Son, Lewis Cantley, Costas A. Lyssiotis
  • Patent number: 8969297
    Abstract: Provided herein are methods for the induction of hypothermia and the treatment of clinical insults in a subject through the administration of a regulated hypothermic multidrug combination. The compositions or multidrug combinations of the invention comprise a regulated hypothermic compound or a dopamine receptor agonist; a vasoactive compound; and an antiarrhythmic compound or a serotonin 5-HT3 receptor antagonist. Additional agents can be included in the composition including at least one of an antioxidant, a vitamin, N-acetylcysteine, and an antihyperglycemic compound. The invention further recognizes that a two phase delivery of multidrug combinations, a rapid infusion of the composition to induce hypothermia followed by a period of slow infusion to maintain the hypothermic state for a sustained period of time.
    Type: Grant
    Filed: June 9, 2010
    Date of Patent: March 3, 2015
    Assignee: The University of North Carolina at Chapel Hill
    Inventor: Laurence M. Katz
  • Publication number: 20150037377
    Abstract: The present invention relates to substituted cellulose acetates and methods of use thereof. One embodiment of the present invention provides a coating having a substituted cellulose acetate having a polar substituent that has an oxygen atom covalently bonded to a nonmetal selected from the group of sulfur, phosphorus, and boron; wherein the nonmetal is present in at least about 0.01% by weight of the substituted cellulose acetate.
    Type: Application
    Filed: October 16, 2014
    Publication date: February 5, 2015
    Applicant: Celanese Acetate LLC
    Inventors: Michael T. Combs, Thomas S. Garrett
  • Patent number: 8945603
    Abstract: A scleral lens is provided with a sodium channel blocker or a sodium channel modulator disposed in the pre-corneal tear film between the scleral lens and the cornea. This system can be used to deliver sodium channel blockers or a sodium channel modulators not currently used because of poor bioavailability. Methods of using this sodium channel blocker delivery system or a sodium channel modulator delivery system are also disclosed.
    Type: Grant
    Filed: January 29, 2014
    Date of Patent: February 3, 2015
    Assignee: Boston Foundation for Sight
    Inventor: Perry Rosenthal
  • Patent number: 8945606
    Abstract: A dissolving oral adhering disc (troche) with a dimple on at least one side to improve adhesion to hard convex surfaces in the mouth, including teeth, orthodontic braces, and gums (keratinized gingiva). The disc may be designed to prevent or treat a sore in the mouth opposite a tooth or brace and/or to release a medication into the mouth, to treat such as sore or to treat or prevent conditions elsewhere in the mouth or throat or stomach.
    Type: Grant
    Filed: October 10, 2008
    Date of Patent: February 3, 2015
    Assignee: OralHealth Corp.
    Inventor: Jeffrey T. Haley
  • Patent number: 8940798
    Abstract: The present invention concerns a method for treating and/or preventing a disease in a subject comprising the step of administrating an effective amount of a compound of formula I to a subject in need thereof.
    Type: Grant
    Filed: November 5, 2012
    Date of Patent: January 27, 2015
    Assignees: Centre National de la Recherche Scientifique (CNRS), Universite Montpellier 2 Sciences et Techniques
    Inventor: Anne Blangy
  • Patent number: 8940718
    Abstract: The disclosure is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.
    Type: Grant
    Filed: November 16, 2012
    Date of Patent: January 27, 2015
    Assignee: Gilead Pharmasset LLC
    Inventors: Elizabeth M. Bacon, Jeromy J. Cottell, Ashley Anne Katana, Darryl Kato, Evan S. Krygowski, John O. Link, James Taylor, Chinh Viet Tran, Teresa Alejandra Trejo Martin, Zheng-Yu Yang, Sheila Zipfel
  • Patent number: 8927579
    Abstract: A compound having formula I. R1, R2, R3 and R4 are independently H or lower alkyl. R5 is aryl, heteroaryl, cycloalkyl, heterocycloalkyl, aryloxy, heteroaryloxy, cycloalkyloxy, heterocycloalkyloxy, arylamino, heteroarylamino, cycloalkylamino, heterocycloalkyl amino, arylthio, heteroarylthio, cycloalkylthio, heterocycloalkylthio, or cyclic olefin, any of which may be substituted or non-substituted; or substituted alkyl, substituted alkyl oxy or substituted alkyl amino wherein the substituent is an aryl, a heteroaryl, a cycloalkyl, a heterocycloalkyl or a cyclic olefin, any of which may be substituted or non-substituted. X is C or N. n and p are independently whole numbers selected from 0, 1 and 2. (CH2)n and (CH2)p may be substituted or non-substituted. Ar1 and Ar2 are independently aryl or heteroaryl groups which may be substituted or non-substituted. Certain specific compounds are excluded.
    Type: Grant
    Filed: July 16, 2009
    Date of Patent: January 6, 2015
    Inventors: Nnae-Meka Ikechukwu Amobi, Christopher Smith
  • Patent number: 8921341
    Abstract: The disclosure is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.
    Type: Grant
    Filed: October 8, 2013
    Date of Patent: December 30, 2014
    Assignee: Gilead Pharmasset LLC
    Inventors: Elizabeth M. Bacon, Jeromy J. Cottell, Ashley Anne Katana, Darryl Kato, Evan S. Krygowski, John O. Link, James Taylor, Chinh Viet Tran, Teresa Alejandra Trejo Martin, Zheng-Yu Yang, Sheila Zipfel
  • Patent number: 8877806
    Abstract: This invention is directed to a method of treating Excessive daytime Sleepiness (EDS) in a subject, comprising the step of administering a therapeutically effective amount of a compound of Formula (I): Formula (I) or a pharmaceutically acceptable salt or ester thereof wherein Rx is a member selected from the group consisting of hydrogen, lower alkyl of 1 to 8 carbon atoms, halogen selected from F, Cl, Br and I, alkoxy containing 1 to 3 carbon atoms, nitro, hydroxy, trifluoromethyl, and thioalkoxy containing 1 to 3 carbon atoms; x is an integer of 1 to 3, with the proviso that R may be the same or different when x is 2 or 3; R1 and R2 can be the same or different from each other and are independently selected from the group consisting of hydrogen, lower alkyl of 1 to 8 carbon atoms, aryl, arylalkyl, cycloalkyl of 3 to 7 carbon atoms; R1 and R2 can be joined to form a 5 to 7-membered heterocycle substituted with a member selected from the group consisting of hydrogen, alkyl, and aryl groups, wherein the cyclic
    Type: Grant
    Filed: January 23, 2013
    Date of Patent: November 4, 2014
    Assignee: SK Biopharmaceuticals Co., Ltd.
    Inventors: Abdallah Ahnaou, Wilhelmus H. I. M. Drinkenburg, Joseph Palumbo, Jonathan Sporn
  • Patent number: 8822524
    Abstract: Disclosed herein is a species of peptide and non-peptide inhibitors of Akt, an oncogenic protein. Beginning with a residue of Akt target substrate GSK-3, the functional domains of the GSK-3 residue were characterized. Functionally homologous non-peptide groups were substituted for the amino acids of the GSK-3 creating a hybrid peptide-non-peptide and non-peptide compounds capable of binding to Akt. The non-peptide compounds show increased stability and rigidity compared to peptide counterparts and are less susceptible to degradation. The bound non-peptide compounds exhibit an inhibitory effect on Akt, similar to peptide-based Akt inhibitors.
    Type: Grant
    Filed: June 8, 2009
    Date of Patent: September 2, 2014
    Assignees: University of South Florida, Yale University
    Inventors: Said M. Sebti, Jin Q. Cheng, Andrew D. Hamilton, Katherine Kayser-Bricker
  • Patent number: 8809390
    Abstract: Disclosed is a compound having an acceleration effect on the secretion of human ?-defensin, LL-37, which is a human-derived anti-microbial peptide, a method for preparing same, and a composition for accelerating the secretion of anti-microbial peptide having same as an active ingredient, and the compound and the composition using same of the present invention enhance the anti-microbial effect and the immunity control effect that the anti-microbial peptide has in the body by accelerating the secretion of the anti-microbial peptide in the body.
    Type: Grant
    Filed: February 27, 2013
    Date of Patent: August 19, 2014
    Assignee: Neopharm Co., Ltd.
    Inventors: Byoeung-Deog Park, Jong-Hwan Bae, Se-Kyoo Jeong, Hyoung-Sub Gwak
  • Patent number: 8809401
    Abstract: Disclosed is a composition for transdermal administration containing tolterodine. The composition comprises lidocaine or a pharmaceutically acceptable salt thereof to achieve enhanced skin penetration. The composition enhances the skin penetration of tolterodine. Therefore, a successful commercial application of a tolterodine-containing transdermal preparation based on the composition can be expected.
    Type: Grant
    Filed: February 17, 2011
    Date of Patent: August 19, 2014
    Assignee: SK Chemicals Co., Ltd.
    Inventors: Yong Youn Hwang, Won-Jae Choi, Jae-Sun Kim, Yeo-Jin Park, Joon-Gyo Oh, Bong-Yong Lee, Hae-In Rhee, Jong-Seob Im
  • Patent number: 8778968
    Abstract: A compound having formula I. R1, R2, R3 and R4 are independently H or lower alkyl. R5 is aryl, heteroaryl, cycloalkyl, heterocycloalkyl, aryloxy, heteroaryloxy, cycloalkyloxy, heterocycloalkyloxy, arylamino, heteroarylamino, cycloalkylamino, heterocycloalkyl amino, arylthio, heteroarylthio, cycloalkylthio, heterocycloalkylthio, or cyclic olefin, any of which may be substituted or non-substituted; or substituted alkyl, substituted alkyl oxy or substituted alkyl amino wherein the substituent is an aryl, a heteroaryl, a cycloalkyl, a heterocycloalkyl or a cyclic olefin, any of which may be substituted or non-substituted. X is C or N. n and p are independently whole numbers selected from 0, 1 and 2. (CH2)n and (CH2)p may be substituted or non-substituted. Ar1 and Ar2 are independently aryl or heteroaryl groups which may be substituted or non-substituted. Certain specific compounds are excluded.
    Type: Grant
    Filed: July 16, 2009
    Date of Patent: July 15, 2014
    Inventors: Nnaemeka Ikechukwu Amobi, Ian Christopher Smith
  • Patent number: 8758788
    Abstract: Active compound mixtures comprising ipconazole and at least one further fungicidally active compound are highly suitable for protecting industrial materials against colonization and destruction by microorganisms.
    Type: Grant
    Filed: January 22, 2010
    Date of Patent: June 24, 2014
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Rainer Bruns, Martin Kugler, Thomas Jaetsch
  • Patent number: 8748468
    Abstract: Treatment of cancer and thromboembolic disorders using inhibitors of Factor VIIa are disclosed herein using a compound of Formula I:
    Type: Grant
    Filed: November 2, 2012
    Date of Patent: June 10, 2014
    Assignee: Pharmacyclics, Inc.
    Inventors: David Loury, Tarak Mody
  • Patent number: 8741950
    Abstract: The present invention relates to the use of compounds of the invention for treatment and/or prevention of fatigue, including fatigue associated with diseases or treatments.
    Type: Grant
    Filed: June 21, 2010
    Date of Patent: June 3, 2014
    Assignee: SK Biopharmaceuticals Co., Ltd.
    Inventors: Moise A. Khayrallah, Gary Bream, Stephen E. Butts, Susan Marie Melnick, Duncan Taylor
  • Patent number: 8709454
    Abstract: At least one phytosphingosine salicylate derivative and at least one lysate of at least one microorganism of the genus Bifidobacterium. Composition, combination. Use, including cosmetic use for reinforcing the repair and regeneration capacity of an epithelium, especially an epidermis, in particular an aged epidermis.
    Type: Grant
    Filed: January 12, 2010
    Date of Patent: April 29, 2014
    Assignee: L'Oreal
    Inventors: David Amar, Bruno Bernard, Dominique Bernard, Isabelle Castiel
  • Patent number: 8673340
    Abstract: A scleral lens is provided with a sodium channel blocker or a sodium channel modulator disposed in the pre-corneal tear film between the scleral lens and the cornea. This system can be used to deliver sodium channel blockers or a sodium channel modulators not currently used because of poor bioavailability. Methods of using this sodium channel blocker delivery system or a sodium channel modulator delivery system are also disclosed.
    Type: Grant
    Filed: September 9, 2010
    Date of Patent: March 18, 2014
    Assignee: Boston Foundation for Sight
    Inventor: Perry Rosenthal
  • Patent number: 8664276
    Abstract: Stilbene analogs and pharmaceutical compositions that are useful for the treatment of various cancers, including without limitation, colorectal cancer (CRC) and breast cancer are disclosed. Such stilbene analogs include, for example, compounds of the following formula: wherein Ra, Rb, R4, R6, R7, R9 and R10 are all H; R2 and R3 are independently H, halo, amino, alkylamino, dialkylamino, N-oxides of dialkylamino, arylalkylamino, trialkylammonium, mercapto, alkylthio, alkanoyl, nitro, nitrosyl, cyano, alkoxy, alkenyloxy, aryl, heteroaryl, sulfonyl, sulfonamide, CONR11R12, NR11CO(R13), NR11COO(R13) or NR11CONR12R13; R11, R12 and R13, are independently, H, alkyl, aryl, heteroaryl or a fluorine; R8 is NRCRdZ wherein Rc is H, alkyl, alkoxy, aryl or heteroaryl, Rd is an alkyl group, Z is a an unshared pair of electrons, H, alkyl or oxygen; and R1 and R5 are halogen.
    Type: Grant
    Filed: January 27, 2012
    Date of Patent: March 4, 2014
    Assignee: University of Kentucky Research Foundation
    Inventors: David Watt, Chunming Liu, Vitaliy M. Sviripa, Wen Zhang
  • Patent number: 8637323
    Abstract: Nitric oxide probes including a compound represented by Formula, I, II, III, IV, V, VI or a combination thereof are provided. Methods of using these nitric oxide probes to detect nitric oxide are also provided.
    Type: Grant
    Filed: October 4, 2012
    Date of Patent: January 28, 2014
    Assignee: Board of Regents, The University of Texas System
    Inventors: Eric V. Anslyn, Youjun Yang, Michelle M. Adams
  • Patent number: 8637058
    Abstract: Composition for controlling phytopathogens comprising compound of the formula: wherein: R1 represents H, or a CO—R? acyl group; R2, the same or different when n is equal to 2, is a halogen, optionally selected from fluorine, chlorine, bromine or iodine; a C1-C9 alkyl group; a C1-C9 haloalkyl group; a C1-C9 alkoxyl group; a C1-C9 haloalkoxyl group; a C1-C9 thioalkyl group; a C1-C9 halothioalkyl group; a C3-C9 cycloalkyl group; a C2-C10 carboalkoxyl group; a cyano group; a hydroxyl group; R? represents a hydrogen; a C1-C9 alkyl group; a C1-C9 haloalkyl group; a C1-C9 alkoxyl group; a C1-C9 haloalkoxyl group; a C2-C10 carboalkoxyl group; a phenyl group; n is a number ranging from 0 to 2; X represents an oxygen atom, a nitrogen or sulfur atom in combination with a fungicide; method for controlling phytopathogens with compound of formula (1) with or without another fungicide.
    Type: Grant
    Filed: November 18, 2002
    Date of Patent: January 28, 2014
    Assignee: Isagro S.p.A.
    Inventors: Lucio Filippini, Marilena Gusmeroli, Alexia Elmini, Carlo Garavaglia, Luigi Mirenna
  • Patent number: 8575135
    Abstract: The disclosure is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.
    Type: Grant
    Filed: March 1, 2013
    Date of Patent: November 5, 2013
    Assignee: Gilead Sciences, Inc.
    Inventors: Elizabeth M. Bacon, Jeromy J. Cottell, Ashley Anne Katana, Darryl Kato, Evan S. Krygowski, John O. Link, James Taylor, Chinh Viet Tran, Teresa Alejandra Trejo Martin, Zheng-Yu Yang, Sheila Zipfel
  • Patent number: 8569384
    Abstract: Antimicrobial compositions are provided that include a hydroalcoholic solvent system comprising a lower C2-C5 alcohol and water; a cationic antimicrobial agent such as chlorhexidine gluconate; a fatty component containing at least one free hydroxyl group, such as a C12-C21 fatty alcohol, a C12-C21 fatty ester, a C12-C21 fatty ether, a C12-C21 fatty amide, and combinations thereof; and optionally an emollient ester such as diesters of bibasic acids and trimesters of citric acid. The compositions described herein display improved antimicrobial efficacy and improved cosmetic elegance. Methods of using the antimicrobial compositions are provided.
    Type: Grant
    Filed: November 13, 2012
    Date of Patent: October 29, 2013
    Assignee: 3M Innovative Properties Company
    Inventors: Robert A. Asmus, Terry R. Hobbs
  • Patent number: 8569536
    Abstract: Active compounds of Formula I are described: wherein: R1 and R2 are each independently C1-C4 alkyl; or R1 and R2 together form a C2-C7 alkylene chain; and Z is a non-steroidal anti-inflammatory drug (NSAID); along with pharmaceutically acceptable salts and prodrug thereof, and methods of using the same.
    Type: Grant
    Filed: August 20, 2012
    Date of Patent: October 29, 2013
    Assignee: Wake Forest University Health Sciences
    Inventor: S. Bruce King
  • Patent number: 8563590
    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: Grant
    Filed: January 12, 2012
    Date of Patent: October 22, 2013
    Assignee: ProteoTech, Inc.
    Inventors: Thomas Lake, Alan D. Snow
  • Patent number: 8552046
    Abstract: Treatment of cancer and thromboembolic disorders using inhibitors of Factor VIIa are disclosed herein using a compound of Formula I.
    Type: Grant
    Filed: October 16, 2008
    Date of Patent: October 8, 2013
    Assignee: Pharmacyclics, Inc.
    Inventors: David Loury, Norbert Purro
  • Patent number: 8529928
    Abstract: Biodegradable polymers incorporating biomolecules and methods of their use are provided. Certain aspects provide biomolecules crosslinked with diglycidyl esters. The disclosed compositions have numerous applications including cellular regeneration, wound healing, and cellular differentiation.
    Type: Grant
    Filed: July 6, 2007
    Date of Patent: September 10, 2013
    Assignee: Georgia Tech Research Corporation
    Inventors: Yadong Wang, Blaine Zern, Christiane Gumera
  • Publication number: 20130225694
    Abstract: Nitrone-based compositions are disclosed that may be utilized for the prevention and treatment of a variety of ophthalmic diseases or conditions where RPE65 protein isomerohydrolase is implicated. Methods of production and use of said nitrone-based compositions, as well as pharmaceutical and ophthalmic compositions containing same, are disclosed.
    Type: Application
    Filed: February 25, 2013
    Publication date: August 29, 2013
    Applicants: Oklahoma Medical Research Foundation, The Board of Regents of the University of Oklahoma
    Inventors: Robert E. Anderson, Nawajes A. Mandal, Jian-Xing Ma, Gennadiy Moiseyev, Robert A. Floyd
  • Patent number: 8518990
    Abstract: A method for treating, preventing or ameliorating a hyperliferative disease and/or disorder in a mammal, comprises administering a therapeutically effective amount of one or more compounds selected from the group consisting of a compound of Formula (III), a compound of Formula (IV), and a pharmaceutically acceptable salt of Formula (III) or Formula (IV): wherein R2 is selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, vinyl and allyl.
    Type: Grant
    Filed: September 28, 2011
    Date of Patent: August 27, 2013
    Assignee: Oncophor, LLC
    Inventors: Gilles Klopman, Suman K. Chakravarti
  • Patent number: 8486968
    Abstract: This invention relates to compounds of formula I their use as inhibitors of the microsomal prostaglandin E2 synthase-1 (mPGES-1), pharmaceutical compositions containing them, and their use as medicaments for the treatment and/or prevention of inflammatory diseases and associated conditions. A, L, M, W, R1, R2, R3, R4, R6, R7, Ra, Rb have meanings given in the description.
    Type: Grant
    Filed: December 8, 2011
    Date of Patent: July 16, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Henning Priepke, Henri Doods, Raimund Kuelzer, Roland Pfau, Dirk Stenkamp, Benjamin Pelcman, Robert Roenn, Dimitrijs Lubriks, Edgars Suna
  • Patent number: 8466186
    Abstract: This invention relates to compounds of formula I their use as inhibitors of the microsomal prostaglandin E2 synthase-1 (mPGES-1), to pharmaceutical compositions containing them, and their use as medicaments for the treatment and/or prevention of inflammatory diseases and associated conditions. A, M, W, R1, R2, R3, R4, R6, R2, R7, R8, R9, Ra, Rb have meanings given in the description.
    Type: Grant
    Filed: December 8, 2011
    Date of Patent: June 18, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Henning Priepke, Raimund Kuelzer, Juergen Mack, Roland Pfau, Dirk Stenkamp, Benjamin Pelcman, Robert Roenn, Dimitrijs Lubriks, Edgars Suna
  • Patent number: 8461081
    Abstract: The invention relates to biocide compositions, comprising (a) at least one dialkylamide based on oleic and/or linoleic acid, and (b) at least one biocide. The compositions exhibit an improved stability even if stored at temperatures between 5° and 40° C. for an extended period.
    Type: Grant
    Filed: February 14, 2008
    Date of Patent: June 11, 2013
    Assignee: Cognis IP Management GmbH
    Inventors: Joaquin Bigorra Llosas, Javier Raya, Bernd Fabry, Rainer Höfer, Benoit Abribat
  • Patent number: 8440715
    Abstract: This invention is directed to a method of treating Excessive daytime Sleepiness (EDS) in a subject, comprising the step of administering a therapeutically effective amount of a compound of Formula (I): Formula (I) or a pharmaceutically acceptable salt or ester thereof wherein Rx is a member selected from the group consisting of hydrogen, lower alkyl of 1 to 8 carbon atoms, halogen selected from F, Cl, Br and I, alkoxy containing 1 to 3 carbon atoms, nitro, hydroxy, trifluoromethyl, and thioalkoxy containing 1 to 3 carbon atoms; x is an integer of 1 to 3, with the proviso that R may be the same or different when x is 2 or 3; R1 and R2 can be the same or different from each other and are independently selected from the group consisting of hydrogen, lower alkyl of 1 to 8 carbon atoms, aryl, arylalkyl, cycloalkyl of 3 to 7 carbon atoms; R1 and R2 can be joined to form a 5 to 7-membered heterocycle substituted with a member selected from the group consisting of hydrogen, alkyl, and aryl groups, wherein the cyclic
    Type: Grant
    Filed: June 7, 2006
    Date of Patent: May 14, 2013
    Assignee: SK Biopharmaceuticals Co., Ltd.
    Inventors: Abdallah Ahnaou, Wilhelmus H. L. M. Drinkenburg, Joseph Palumbo, Jonathan Sporn
  • Patent number: 8435548
    Abstract: Disclosed are peptide derivatives, wherein glutathione-like peptides are connected to benzoic acid derivatives, and a cosmetic composition comprising the same. The peptide derivatives have excellent tyrosinase inhibition and anti-oxidative activities to show excellent skin whitening effect, biocompatibility without skin stimulation, and stability during long-term storage. Therefore, they can be effectively used for a cosmetic composition for skin whitening.
    Type: Grant
    Filed: December 23, 2009
    Date of Patent: May 7, 2013
    Assignee: Bio-FD&C Co., Ltd
    Inventors: Dai Hyun Jung, Sang Hyun Moh, Jung Hun Lee, Su Jung Kim, Hyung Sik Kim, Hyo Hyun Seo, Yeon Ja Bae
  • Patent number: 8420637
    Abstract: The present invention provides a method of treating glaucoma or ocular hypertension which comprises applying to the eye of a person in need thereof an amount sufficient to treat glaucoma or ocular hypertension of a compound of formula I wherein Y, Q, Z, R, R1 and R2 are as defined in the specification. The present invention further comprises pharmaceutical compositions, e.g. ophthalmic compositions, including said compound of formula I.
    Type: Grant
    Filed: September 22, 2009
    Date of Patent: April 16, 2013
    Assignee: Allergan, Inc.
    Inventors: June Chen, Simon Pettit, Hans Fliri
  • Patent number: 8415393
    Abstract: The present invention provides methods for the design and identification of novel antimicrobial compounds, and provides antimicrobial compounds identified using these methods. These antimicrobial compounds inhibit the binding of a prokaryotic single-stranded DNA binding protein to a polypeptide that binds to the prokaryotic single-stranded DNA binding protein. In some examples, the prokaryotic single-stranded DNA binding protein is prokaryotic Exonuclease I. In one embodiment, the antimicrobial compound has the structure wherein Y is selected from the group consisting of CH2, O, and NH, R1 is selected from the group consisting of H, F, Cl, Br, and I, R2 is selected from the group consisting of H and CF3, R3 is selected from the group consisting of H and CO2H, R4 is selected from the group consisting of H and OH, and R5 is selected from the group consisting of H, alkoxy, and NO2.
    Type: Grant
    Filed: May 21, 2008
    Date of Patent: April 9, 2013
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: James L. Keck, Douglas A. Bernstein
  • Patent number: 8394357
    Abstract: The present invention concerns an improved optical method and optical sensing device for determining the levels of polyhydroxyl-substituted organic molecules in vitro and/or in vivo in aqueous media. The range of detection is between about 400 and 800 nm. In particular, a sensory devise is implemented in a mammal to determine sugar levels. Specifically, a dye is combined with a conjugated nitrogen-containing heterocyclic aromatic boronic acid-substituted bis-onium compound in the presence of a sugar, such as fructose or glucose. The viologens are preferred as the aromatic conjugated nitrogen-containing boronic acid substituted compounds. The method is useful to determine sugar levels in a human being.
    Type: Grant
    Filed: August 8, 2008
    Date of Patent: March 12, 2013
    Assignee: The Regents of the University of California
    Inventors: Bakthan Singaram, Ritchie A. Wessling
  • Patent number: 8377475
    Abstract: In one aspect, the present invention features a tablet including: (i) a first drug layer including naproxen; (ii) a second drug layer including a decongestant (e.g., pseudoephedrine) wherein said second drug layer is a sustained release layer adapted to deliver a therapeutically effective amount of pseudoephedrine for a period of at least twelve hours; and (iii) a barrier layer that does not include naproxen, wherein the barrier layer is in contact with the first drug layer; and (iv) a third drug layer including cetirizine, wherein the third drug layer is in contact with the barrier layer and is not in contact with the first drug layer.
    Type: Grant
    Filed: January 4, 2010
    Date of Patent: February 19, 2013
    Assignee: McNeil-PPC, Inc.
    Inventors: Satish Kamath, Indukumar G. Shah, Michael Nichols, Dinesh Patel
  • Patent number: 8362051
    Abstract: Wallboard and facing paper that provides increased mold resistance at lower biocide loadings. The biocide is: (a) an n-alkyl isothiazolinone such as octylisothiazolinone (OIT), a monohalo and dihalo substituted n-alkylisothiazolinone such as chloromethylisothiazolinone (CMIT) or dichlorooctylisothiazolinone (DCOIT), 3-iodo-2-propynyl-butylcarbamate (IPBC), chlorothalonil, methylene-bis-thiocyanate, or mixtures of two or more thereof; or (b) carbendazim and a second biocide selected from 3-iodo-2-propynyl-butylcarbamate (IPBC), diiodomethyltolylsulfone (DIMTS), sodium pyrithione, octylisothiazolinone (OIT), dichlorooctylisothiazolinone (DCOIT), and chlorothalonil.
    Type: Grant
    Filed: January 18, 2008
    Date of Patent: January 29, 2013
    Assignee: Rohm and Haas Company
    Inventors: Sheila M. Tinetti, Paul Foley, Li Wang, Michael V. Enzien, Sanjay B. Bishnoi
  • Patent number: 8362087
    Abstract: This invention relates to pharmaceutical compositions for veterinary use in form of aqueous injectable suspensions comprising Florfenicol or Florfenicol in form of a substantially water-insoluble complex, co-crystal or salt, sterile and micronised, in a concentration up to 500 mg/ml. The suspensions enable parenteral antimicrobial therapies in animals, with limited numbers of injections and showing good general- and local tolerances. They also possess a limited sedimentation on standing as well as after shipping, are easily resuspendable and have good syringablity.
    Type: Grant
    Filed: July 30, 2004
    Date of Patent: January 29, 2013
    Assignee: Calluna Pharma BVBA
    Inventors: Erwin Embrechts, Jan Embrechts
  • Patent number: 8344029
    Abstract: It is an object of the present invention to provide a substituted propanamide derivative or a pharmacologically acceptable salt thereof that is useful as a prophylactic or therapeutic agent for a bone metabolic disease. The present invention relates to a pharmaceutical composition comprising a compound having General Formula (I) or a pharmacologically acceptable salt thereof as an active ingredient: [wherein, R1 represents a C6-C10 aryl group that may be substituted by a group selected from Substituent Group ?, for example; R2 represents a C6-C10 aryl group that may be substituted by a group selected from Substituent Group ?, for example; and X represents a hydroxyl group or a C1-C6 alkoxy group, for example].
    Type: Grant
    Filed: July 18, 2006
    Date of Patent: January 1, 2013
    Assignee: Daiichi Sankyo Company, Limited
    Inventors: Kazumasa Aoki, Koji Suda, Kentoku Gotanda, Tomio Kimura
  • Patent number: 8338491
    Abstract: Antimicrobial compositions are provided that include a hydroalcoholic solvent system comprising a lower C2-C5 alcohol and water; a cationic antimicrobial agent such as chlorhexidine gluconate; a fatty component containing at least one free hydroxyl group, such as a C12-C21 fatty alcohol, a C12-C21 fatty ester, a C12-C21 fatty ether, a C12-C21 fatty amide, and combinations thereof; and optionally an emollient ester such as diesters of bibasic acids and triesters of citric acid. The compositions described herein display improved antimicrobial efficacy and improved cosmetic elegance.
    Type: Grant
    Filed: October 25, 2007
    Date of Patent: December 25, 2012
    Assignee: 3M Innovative Properties Company
    Inventors: Robert A. Asmus, Terry R. Hobbs
  • Patent number: 8338392
    Abstract: The present invention is a method for identifying agents which modulate microRNA activity. The invention involves contacting a cell harboring a microRNA and a microRNA binding sequence, which is operably linked to a nucleic acid molecule encoding a reporter protein, with a test agent increases or decreases the expression of the reporter protein thereby identifying a microRNA modulator. Antagonists identified by this screening assay are provided, as are methods for using the same to inhibit microRNA activity and prevent or treat disease.
    Type: Grant
    Filed: February 20, 2009
    Date of Patent: December 25, 2012
    Assignees: The Wistar Institute, North Carolina State University
    Inventors: Qihong Huang, Alexander Deiters, Kiranmai Gumireddy
  • Patent number: 8334322
    Abstract: Drug substances comprising a pharmaceutically acceptable organic acid addition salt of amine containing pharmaceutically active compounds useful for the treatment of a therapeutic ailment administration and exhibiting prophylactic properties when employed in non-therapeutic administration.
    Type: Grant
    Filed: December 22, 2011
    Date of Patent: December 18, 2012
    Assignee: Pisgah Laboratories, LLC
    Inventors: David William Bristol, Clifford Riley King, Joseph Pike Mitchener, Jr., Vicki Haynes Audia
  • Publication number: 20120316211
    Abstract: Provided herein are methods of detecting evidence of Chagas disease in a biological sample, comprising the step of measuring the presence of at least one protein selected from the group consisting of gelsolin, myosin light chain 2, vimentin, myosin heavy chain 11, vinculin, and plasminogen in said sample, wherein significantly elevated levels of the protein is a biomarker for the presence or severity of Chagas disease.
    Type: Application
    Filed: May 11, 2012
    Publication date: December 13, 2012
    Applicant: The Board or Regents of the University of Texas System
    Inventor: Nisha Jain Garg
  • Patent number: 8318798
    Abstract: [Problems] To provide a neuronal cell death inhibitor and a therapeutic agent for a neurodegenerative disease, particularly Parkinson's disease. [Means for Solving Problems] It is known that DJ-1 protein is involved in Parkinson's disease and is capable of inhibiting neuronal cell death caused by oxidative stress. Based on this knowledge, screening is made for a low molecular weight molecule capable of binding to an active site of DJ-1 protein (i.e., a region around a cysteine residue at position-106) using an analysis softwear FastDock (Fujitsu Ltd.). When various tests are made using candidate low molecular weight compounds each having a binding energy of ?60 kcal/mol or lower, these compounds show a therapeutic effect on a neurodegenerative disease.
    Type: Grant
    Filed: November 17, 2006
    Date of Patent: November 27, 2012
    Assignee: National University Corporation Hokkaldo University
    Inventor: Hiroyoshi Ariga
  • Patent number: 8303991
    Abstract: The invention relates to a method for making composite active particles for use in a pharmaceutical composition for pulmonary administration, the method comprising a milling step in which particles of active material are milled in the presence of particles of an additive material which is suitable for the promotion of the dispersal of the composite active particles upon actuation of an inhaler. The invention also relates to compositions for inhalation prepared by the method.
    Type: Grant
    Filed: April 26, 2010
    Date of Patent: November 6, 2012
    Assignee: Vectura Limited
    Inventors: John Staniforth, Matthew Michael James Green, David Alexander Vodden Morton