Hetero Ring Is Six-membered Consisting Of Three Nitrogens And Three Carbon Atoms Patents (Class 514/241)
  • Patent number: 10323007
    Abstract: Described herein are quinazoline-based compounds and formulations thereof. In some embodiments, the compounds and/or formulations thereof can be effective to inhibit and/or kill A. baumannii. Also described herein are methods of treating a subject in need thereof by administering to the subject in need thereof a quinazoline-based compound and/or formulation thereof to the subject in need thereof.
    Type: Grant
    Filed: September 13, 2017
    Date of Patent: June 18, 2019
    Assignee: University of South Florida
    Inventors: Roman Manetsch, Kurt S. Van Horn, Whittney Burda, Lindsey N. Shaw, Renee Fleeman, Megan Barber, David Lawrence Flanigan
  • Patent number: 10316161
    Abstract: Materials and methods are described herein that include forming a porous polymer network with antimicrobial and antifouling properties. The antifouling portion may be a polymer, such as polyethylene glycol, and the antimicrobial portion may be a metal, or a different cationic species, such as a quaternary ammonium salt. The method generally includes forming a reaction mixture comprising a formaldehyde, a bridging group, and moieties with antifouling and antimicrobial properties.
    Type: Grant
    Filed: March 16, 2017
    Date of Patent: June 11, 2019
    Assignee: International Business Machines Corporation
    Inventors: Dylan J. Boday, Mareva B. Fevre, Jeannette M. Garcia, James L. Hedrick, Jason T. Wertz, Rudy J. Wojtecki
  • Patent number: 10159677
    Abstract: The present invention provides a method for treating a disease, disorder or condition associated with GPR139 using compounds of formula 1: which are agonists of GPR139, certain compounds encompassed by formula 1, pharmaceutical compositions thereof, processes for making the compounds, and intermediates thereof.
    Type: Grant
    Filed: August 22, 2017
    Date of Patent: December 25, 2018
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Stephen Hitchcock, Betty Lam, Holger Monenschein, Holly Reichard
  • Patent number: 10150737
    Abstract: The invention relates inter alia to compounds of the general formula (I) in which the A1-A4, T, n, W, Q, R1 and B1-B4 radicals are each as defined in the description. Also described are processes for preparing the compounds of the formula (I). The inventive compounds are especially suitable for controlling insects, arachnids and nematodes in agriculture, and ectoparasites in veterinary medicine.
    Type: Grant
    Filed: November 5, 2014
    Date of Patent: December 11, 2018
    Assignee: BAYER CROPSCIENCE AKTIENGESELLSCHAFT
    Inventors: Werner Hallenbach, Hans-Georg Schwarz, Kerstin Ilg, Ulrich Goergens, Johannes Koebberling, Andreas Turberg, Niels Boehnke, Michael Maue, Robert Velten, Tobias Harschneck, Julia Johanna Hahn, Sebastian Horstmann
  • Patent number: 9975878
    Abstract: Amine substituted triazine compounds and forms thereof that inhibit the function and reduce the level of B-cell specific Moloney murine leukemia virus integration site 1 (Bmi-1) protein and methods for their use to inhibit Bmi-1 function and reduce the level of Bmi-1 to treat a cancer mediated by Bmi-1 are described herein.
    Type: Grant
    Filed: November 21, 2013
    Date of Patent: May 22, 2018
    Assignee: PTC THERAPEUTICS, INC.
    Inventors: Hiroo Koyama, Ramil Baiazitov, Wu Du, Chang-sun Lee, Young-Choon Moon, Steven D. Paget, Hongyu Ren, Nadiya Sydorenko
  • Patent number: 9896668
    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: August 30, 2016
    Date of Patent: February 20, 2018
    Assignees: University of South Florida, Yale University
    Inventors: Said M. Sebti, Jin Q. Cheng, Andrew D. Hamilton, Katherine Kayser-Bricker
  • Patent number: 9839537
    Abstract: Methods of treating coronary and peripheral artery disease in diabetic patients with bioresorbable polymer stents are described. The stents may include everolimus.
    Type: Grant
    Filed: March 7, 2013
    Date of Patent: December 12, 2017
    Assignee: Abbott Cardiovascular Systems Inc.
    Inventors: Krishnankutty Sudhir, Wai-Fung Cheong, Lee Clark
  • Patent number: 9808464
    Abstract: The disclosure relates to compounds and compositions for forming bone and methods related thereto. In one embodiment, the disclosure relates to a composition comprising a compound disclosed herein, such as 2,4-diamino-1,3,5-triazine derivatives or salts thereof, for use in bone growth processes. In a typical embodiment, a bone graft composition is implanted in a subject at a site of desired bone growth or enhancement.
    Type: Grant
    Filed: October 25, 2016
    Date of Patent: November 7, 2017
    Assignees: Emory University, The United States of America as represented by the Department of Veterans Affairs
    Inventors: Scott D. Boden, Sreedhara Sangadala
  • Patent number: 9763866
    Abstract: The invention provides for methods for treating a hair loss disorder in a subject by administering a Janus Kinase/Signal Transducers and Activators of Transcription inhibitor.
    Type: Grant
    Filed: March 10, 2016
    Date of Patent: September 19, 2017
    Assignee: THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK
    Inventors: Angela M. Christiano, Raphael Clynes
  • Patent number: 9737552
    Abstract: Described herein are methods for the treatment of cognitive impairment in a subject with a neurological autoimmune disease and methods for determining whether a subject who has a central nervous system autoimmune disease is likely to acquire a cognitive impairment.
    Type: Grant
    Filed: December 14, 2011
    Date of Patent: August 22, 2017
    Assignee: The Johns Hopkins University
    Inventors: Adam Kaplin, Barbara S. Slusher, Kristen A. Rahn
  • Patent number: 9738624
    Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising the compounds of formula (I) or their pharmaceutically acceptable salts, and methods of using said compounds, salts and compositions in the treatment of various disorders associated with CRM1 activity.
    Type: Grant
    Filed: June 20, 2014
    Date of Patent: August 22, 2017
    Assignee: Karyopharm Therapeutics Inc.
    Inventors: Erkan Baloglu, Sharon Shacham, Dilara McCauley, Trinayan Kashyap, William Senapedis, Yosef Landesman, Gali Golan, Ori Kalid, Sharon Shechter
  • Patent number: 9718847
    Abstract: Heterocyclic compounds of formula (I), methods for their preparation, pharmaceutical compositions containing such a compound and their therapeutic uses.
    Type: Grant
    Filed: September 15, 2014
    Date of Patent: August 1, 2017
    Assignee: Plexxikon Inc.
    Inventors: Jiazhong Zhang, John Buell, Katrina Chan, Prabha N. Ibrahim, Jack Lin, Phuongly Pham, Songyuan Shi, Wayne Spevak, Guoxian Wu, Jeffrey Wu
  • Patent number: 9540332
    Abstract: The present invention is directed to a compound of Formula I or a pharmaceutically acceptable salt thereof; wherein R, R1, R2, R3, R4, m, and n are as defined herein, to pharmaceutical compositions comprising said compound, and to methods of treating diseases or conditions mediated by elevated persistent sodium current, such as an ocular disorder, multiple sclerosis, seizure disorder, and chronic pain.
    Type: Grant
    Filed: September 24, 2014
    Date of Patent: January 10, 2017
    Assignee: ALLERGAN, INC.
    Inventors: George R. Ehring, Ellen Chao, Herman Ng, Hau Ton, Jia Chian Li, Joseph S. Adorante, Michael E. Garst, Howard B. Rind, Mark R. Hansen, Alfred Arthur Avey, Jr., Lloyd Jay Dolby, Shervin Esfandiari, Vivian R. MacKenzie, Jeremiah Andrew Marsden, David Charles Muchmore
  • Patent number: 9475955
    Abstract: A film may be formed from film forming compositions which comprise at least one carboxamide based coalescing solvent. These coalescing solvents impart equivalent or improved wet-scrub resistance, block resistance, gloss, dirt pick-up resistance and leveling characteristics to the films on a substrate, without contributing to total VOC levels, when replacing conventional coalescing solvents. The present invention also includes a method for forming a film comprising applying a film forming composition comprising polyunsaturated reactive carboxamides to a substrate and curing the film under ambient conditions. The coalescing carboxamide solvents are suitable for paint, latex based caulk, adhesives and floor care applications.
    Type: Grant
    Filed: August 24, 2015
    Date of Patent: October 25, 2016
    Assignee: Stepan Company
    Inventors: Gary Luebke, Renee Luka, Andrew D Malec, Michael R Terry, Patrick Shane Wolfe
  • Patent number: 9453049
    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: August 29, 2014
    Date of Patent: September 27, 2016
    Assignees: University of South Florida, Yale University
    Inventors: Said M. Sebti, Jin Q. Cheng, Andrew D. Hamilton, Katherine Kayser-Bricker
  • Patent number: 9447084
    Abstract: The present invention relates to novel and inventive isoxazoline of formula (I) and salts thereof: wherein variables D1, D2, D3, D4, D5, R1, B1, B2, B3, R2, R3, R4, R5, R6, Y, Z, L, a and b are described herein are as defined in the description. The invention also relates to parasiticidal and pesticidal compositions comprising the isoxazoline compounds of formula (I), processes for their preparation and their uses to prevent or treat parasitic infections or infestations in animals and as pesticides.
    Type: Grant
    Filed: October 30, 2014
    Date of Patent: September 20, 2016
    Assignee: MERIAL, INC.
    Inventor: Charles Q Meng
  • Patent number: 9447030
    Abstract: The present invention relates to compounds of formula (I): or a pharmaceutically acceptable salt, hydrate, solvate, or prodrug thereof, wherein U, J, V, X, R2a, R2b, R2c, R5 and t are as described herein. The present invention relates generally to inhibitors of histone deacetylase and to methods of making and using them. These compounds are useful for promoting cognitive function and enhancing learning and memory formation. In addition, these compounds are useful for treating, alleviating, and/or preventing various conditions, including for example, neurological disorders, memory and cognitive function disorders/impairments, extinction learning disorders, fungal diseases and infections, inflammatory diseases, hematological diseases, and neoplastic diseases in humans and animals.
    Type: Grant
    Filed: October 28, 2013
    Date of Patent: September 20, 2016
    Assignees: Massachusetts Institute of Technology, The General Hospital Corporation, The Broad Institute, Inc.
    Inventors: Edward Holson, Florence Fevrier Wagner, Michel Weiwer, Li-Huei Tsai, Stephen Haggarty, Yan-Ling Zhang
  • Patent number: 9429579
    Abstract: The present invention relates to a blood analysis apparatus X for measuring concentrations of glucose and glycohemoglobin in blood. The blood analysis apparatus X is configured to perform the concentration measurement of the glucose and the glycohemoglobin by one sampling of blood 13. The blood analysis apparatus X is preferably configured to simultaneously carry out sample preparations for concentration measurement of the glucose and the glycohemoglobin by one sample preparation. The blood analysis apparatus X may be configured to perform dilution of a blood sample for measuring the glycohemoglobin and dilution of a blood sample for measuring the glucose using the same diluent.
    Type: Grant
    Filed: September 20, 2007
    Date of Patent: August 30, 2016
    Assignee: ARKRAY, INC.
    Inventors: Koji Sugiyama, Tatsuo Kamata, Takeshi Takagi
  • Patent number: 9345767
    Abstract: A method for predicting a therapeutic effect of chemotherapy with a combination drug containing tegafur, gimeracil, and oteracil potassium in a gastric cancer patient by: (1) measuring an expression level of epidermal growth factor receptor (EGFR) in a biological sample obtained from the patient; (2) comparing the expression level of EGFR obtained in step (1) with a corresponding predetermined cut-off point; and (3) predicting that the patient is likely to sufficiently respond to chemotherapy when a tegafur, gimeracil, and oteracil potassium combination drug is used with an EGFR inhibitor, when the step (2) comparison reveals that the expression level of EGFR is greater than the cut-off point, or predicting that the patient is likely to sufficiently respond to chemotherapy when a tegafur, gimeracil, and oteracil potassium combination drug is used alone, when the step (2) comparison reveals that the expression level of EGFR is not greater than the cut-off point.
    Type: Grant
    Filed: May 15, 2012
    Date of Patent: May 24, 2016
    Assignee: TAIHO PHARMACEUTICAL CO., LTD.
    Inventors: Takashi Kobunai, Hitoshi Saito, Teiji Takechi
  • Patent number: 9216981
    Abstract: A novel purinylpyridinylamino-2,4-difluorophenyl sulfonamide derivative, a pharmaceutically acceptable salt thereof, a preparation method thereof, and a pharmaceutical composition with an inhibitory activity against Raf kinase, containing the same as an active ingredient are provided. The purinylpyridinylamino-2,4-difluorophenyl sulfonamide derivative of the present invention effectively regulates the activity of B-Raf kinase, and thus may be useful for preventing or treating cancers induced by the over-activation of Raf kinase, especially various melanoma, colorectal cancer, prostate cancer, thyroid cancer, ovarian cancer and the like.
    Type: Grant
    Filed: November 25, 2011
    Date of Patent: December 22, 2015
    Assignee: Medpacto, Inc.
    Inventors: Eun Kyong Shim, Nam Doo Kim, Tae Bo Shim, Seung Yong Kim
  • Patent number: 9150507
    Abstract: This invention provides a compound of the formula (I): a pharmaceutically acceptable salt or solvate thereof, wherein R1 is optionally substituted lower alkyl, Y is —S(O)n— wherein n is 1 or 2, or —CO—, R2 is hydrogen or lower alkyl, R7 is hydrogen or lower alkyl, X is lower alkylene, lower alkenylene, arylene, cycloalkylene or the like, and Z is lower alkyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl or the like.
    Type: Grant
    Filed: April 25, 2007
    Date of Patent: October 6, 2015
    Assignee: Shionogi & Co., Ltd.
    Inventors: Takayuki Okuno, Naoki Kouyama, Masahiro Sakagami
  • Patent number: 9120786
    Abstract: The present disclosure provides substituted triazine carboxamides of Formula I: and the pharmaceutically acceptable salts and solvates thereof, wherein A1, X, A2, E, and Z are defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula I to treat a disorder responsive to the blockade of sodium channels. Compounds of the present disclosure are especially useful for treating pain.
    Type: Grant
    Filed: February 26, 2014
    Date of Patent: September 1, 2015
    Assignee: Purdue Pharma, L.P.
    Inventors: Dawit Tadesse, Jianming Yu
  • Patent number: 9023849
    Abstract: The present application relates to novel substituted fused imidazoles and pyrazoles, to processes for preparation thereof, to the use thereof, alone or in combinations, for treatment and/or prophylaxis of diseases and to the use thereof producing medicaments for the treatment and/or prophylaxis of diseases, especially for treatment and/or prophylaxis of cardiovascular disorders.
    Type: Grant
    Filed: January 8, 2013
    Date of Patent: May 5, 2015
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Markus Follmann, Johannes-Peter Stasch, Gorden Redlich, Nils Griebenow, Dieter Lang, Frank Wunder, Holger Paulsen, Walter Hübsch, Alexandros Vakalopoulos, Adrian Tersteegen
  • Patent number: 9023874
    Abstract: The invention relates to alkylsulfide derivatives compounds of formula I as hereunder depicted or the enantiomers or veterinarily acceptable salts thereof which are useful for combating or controlling invertebrate pests, in particular arthropod pests and nematodes. The invention also relates to methods for controlling invertebrate pests by using these compounds and to plant propagation material and to agricultural and veterinary compositions comprising said compounds. wherein U, R1, R2, R3U, X, n and p are defined as in the description.
    Type: Grant
    Filed: November 11, 2010
    Date of Patent: May 5, 2015
    Assignee: Merial, Inc.
    Inventors: Sebastian Soergel, Ralph Paulini, Steffen Gross, Carsten Beyer, Matthias Pohlman, Henricus Maria Martinus Bastiaans, Michael Rack, Deborah L. Culbertson, Douglas D. Anspaugh, Sarah Thompson, Vincent Salgado
  • Publication number: 20150119362
    Abstract: The present invention relates to compounds and methods useful as inhibitors of phosphodiesterase 4 (PDE4) for the treatment or prevention of disease.
    Type: Application
    Filed: October 24, 2013
    Publication date: April 30, 2015
    Inventors: Mark E. Gurney, Timothy J. Hagen, Joel R. Walker, Xuesheng Mo, A. Samuel Vellekoop, Robert Campbell, Lei Zhu, Donna L. Romero
  • Publication number: 20150110864
    Abstract: A primary object of the present invention is to provide a novel combination therapy that exhibits a notable antitumor effect. As means for achieving the object, an antitumor agent comprising a combination of oxaliplatin, paclitaxel, and a combination drug containing tegafur, gimeracil, and oteracil potassium is provided.
    Type: Application
    Filed: March 15, 2013
    Publication date: April 23, 2015
    Applicant: Taiho Pharmaceutical Co., Ltd.
    Inventor: Junji Uchida
  • Patent number: 8980828
    Abstract: The invention relates to a composition for use as a medicament comprising insulin in combination with at least one compound of formula (I) wherein the radicals R1 to R6 have the meaning according to claim 1, and/or physiologically acceptable salts thereof. Another object of the invention concerns a pharmaceutical composition comprising as active ingredients effective amounts of insulin and at least one compound of formula (I), together with pharmaceutically tolerable adjuvants, for the prophylactic or therapeutic treatment and/or monitoring of physiological and/or pathological conditions that are associated with insulin resistance. The invention also relates to a pharmaceutical package comprising insulin in a first dosage unit and at least one compound of formula (I) in a second dosage unit.
    Type: Grant
    Filed: July 15, 2013
    Date of Patent: March 17, 2015
    Assignee: Poxel S.A.S.
    Inventors: Didier Mesangeau, Daniel Cravo, Annick Audet
  • Patent number: 8975257
    Abstract: Disclosed are methods for making aldehydes and ketones comprising allowing the corresponding primary or secondary alcohol to react in the presence of trichoroisocyanuric acid, a compound of formula R1SR2 and a base. In one embodiment, the alcohol is a compound of formula (I): wherein R3 is a protecting group. Also disclosed are methods for making 3-O-protected morphine dienol carboxylates comprising allowing a compound of formula (I) to oxidize in the presence of a chlorine-containing compound and a compound of formula R1SR2; and allowing the product of the oxidation step to react with an acylating agent.
    Type: Grant
    Filed: February 24, 2014
    Date of Patent: March 10, 2015
    Assignee: Purdue Pharma L.P.
    Inventor: Andreas Stumpf
  • Patent number: 8962013
    Abstract: The UV-stable solid transdermal therapeutic system (TTS) with UV absorber for photosensitive active pharmaceutical ingredients has a backing layer (1), at least one active ingredient-containing matrix (2), and a detachable protective film (3). Optionally an adhesive layer (4) and a separating layer (5) are introduced between the backing layer (1) and the at least one active ingredient-containing matrix (2). At least one hydroxyphenyltriazine compound acting as UV absorber is embedded in the backing layer (1), in the active ingredient-containing matrix (2), or in the adhesive layer (4). The TTS according to the invention achieves high stability at low concentrations of UV absorber, preferably 0.5 to 3% (m/m), so as to reduce or avoid skin irritation.
    Type: Grant
    Filed: May 2, 2006
    Date of Patent: February 24, 2015
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Thomas Langguth, Stefan Bracht
  • Publication number: 20150051209
    Abstract: The present invention relates to compounds of formula I: in which n, R1, R2, R3a, R4 and R5 are defined in the Summary of the Invention; capable of inhibiting the activity of MEK. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of hyperproliferative diseases like cancer.
    Type: Application
    Filed: August 5, 2014
    Publication date: February 19, 2015
    Applicant: NOVARTIS AG
    Inventors: Mark Gary BOCK, Henrik MOEBITZ, Sunil Kumar PANIGRAHI, Ramulu PODDUTOORI, Susanta SAMAJDAR
  • Patent number: 8940774
    Abstract: Provided are tris-quaternary ammonium compounds which are modulators of nicotinic acetylcholine receptors. Also provided are methods of using the compounds for modulating the function of a nicotinic acetylcholine receptor, and for the prevention and/or treatment of central nervous system disorders, substance use and/or abuse and/or gastrointestinal tract disorders.
    Type: Grant
    Filed: November 26, 2013
    Date of Patent: January 27, 2015
    Inventors: Peter Crooks, Linda Dwoskin, Roger Papke, Guangrong Zheng, Sangeetha Sumithran
  • Publication number: 20150025078
    Abstract: Provided are biocidal compositions comprising glutaraldehyde and a compound selected from the group consisting of 1-(3-chloroallyl)-3,5,7-triaza-1-azoniaadamantane; tris(hydroxymethyl)-nitromethane; and a hexahydrotriazine compound. The compositions are useful for controlling microorganisms in aqueous or water-containing systems.
    Type: Application
    Filed: October 3, 2014
    Publication date: January 22, 2015
    Inventor: Bei Yin
  • Publication number: 20150001066
    Abstract: A wipe for anti-microbial disinfecting includes a flexible substrate and an anti-microbial ion source integrated on the substrate. The flexible substrate is made entirely or in part of woven fiber cloth, non-woven fiber cloth, woven synthetic cloth, non-woven synthetic cloth, or natural fiber cloth. The anti-microbial ion source is configured to dissolve in an aqueous solution to form an anti-microbial solution. The flexible substrate is configured to absorb the anti-microbial solution for use in cleaning.
    Type: Application
    Filed: June 25, 2014
    Publication date: January 1, 2015
    Inventor: Ashok V. Joshi
  • Patent number: 8921547
    Abstract: The present invention provides compounds which are modulators of TNF-? signaling and methods of use thereof for treating a patient having a TNF-? mediated condition.
    Type: Grant
    Filed: July 19, 2013
    Date of Patent: December 30, 2014
    Assignee: Genzyme Corporation
    Inventors: Scott F. Sneddon, John L. Kane, Bradford H. Hirth, Frederic Vinick, Shuang Qiao, Sharon R. Nahill, John M. Williams, Hans-Peter Biemann
  • Patent number: 8912323
    Abstract: The present invention relates to dendrimer synthesis. Specifically, the present invention relates to triazine scaffolds capable of click chemistry for one-step synthesis of functionalized dendrimers, and methods of making and using the same.
    Type: Grant
    Filed: September 30, 2010
    Date of Patent: December 16, 2014
    Assignee: The Regents of the University of Michigan
    Inventors: James R. Baker, Jr., Hong Zong, Thommey P. Thomas
  • Patent number: 8906918
    Abstract: Embodiments of the present disclosure, in one aspect, relate to a 2,4-diaminoquinazoline compound, pharmaceutical compositions including a 2,4-diaminoquinazoline compound, methods of treatment of a condition (e.g., infection) or disease, methods of treatment using compositions or pharmaceutical compositions, and the like.
    Type: Grant
    Filed: March 22, 2013
    Date of Patent: December 9, 2014
    Assignee: University of South Florida (A Florida Non-Profit Corporation)
    Inventors: Roman Manetsch, Lindsey Neil Shaw, Kurt Steven Van Horn, Whittney Nicole Burda
  • Patent number: 8901313
    Abstract: The invention relates to novel compounds of Formula I: wherein A, Y, R1, R2 and the subscript b each has the meaning as described herein and compounds of Formula I, and stereoisomers, geometric isomers, tautomers, solvates, metabolites, isotopes, pharmaceutically acceptable salts, or prodrugs thereof. Compounds of Formula I and pharmaceutical compositions thereof are useful in the treatment of disease and disorders in which undesired or over-activation of NF-kB signaling is observed.
    Type: Grant
    Filed: March 15, 2012
    Date of Patent: December 2, 2014
    Assignee: Genentech, Inc.
    Inventors: Steven Staben, Jianwen Feng, Pui Leng Loke, Christian A. G. N. Montalbetti
  • Patent number: 8895730
    Abstract: A method of synthesizing a two-photon active tris(diarylamino-9,9-di(R)fluorenyl)-1,3,5-triazine compound having the structure: where Y is hydrogen, a thermally self-polymerizable acrylic, or a methacrylic group; R is an alkyl group of the formula —CmH2m+1, wherein the subscript m ranges from 1 to 6, or an alkylether group of the formula —(CH2CH2O)pMe, wherein the subscript p ranges from 1 to 5; R? is an alkyl group; and the R?—(OY)x groups are attached to the phenyl rings of the triarylamine moiety either in a para position or a meta position and the subscript x ranges from 1 to 3. The compound may be synthesized by (a) synthesizing a diarylamine intermediate, (b) synthesizing a brominated 1,3,5-triazine intermediate as a three-arm core structure, and (c) forming the two-photon active tris(diarylamino-9,9-di(R)fluorenyl)-1,3,5-triazine compound by covalently joining the diarylamine and each arm of the three-arm core structure and removing the acetone protecting groups.
    Type: Grant
    Filed: October 7, 2013
    Date of Patent: November 25, 2014
    Assignee: The United States of America as represented by the Secretary of the Air Force
    Inventors: Loon-Seng Tan, Ramamurthi Kannan, Matthew Dalton
  • Patent number: 8889679
    Abstract: Provided are biocidal compositions comprising glutaraldehyde and a compound selected from the group consisting of 1-(3-chloroallyl)-3,5,7-triaza-1-azoniaadamantane; tris(hydroxymethyl)-nitromethane; and a hexahydrotriazine compound. The compositions are useful for controlling microorganisms in aqueous or water-containing systems.
    Type: Grant
    Filed: May 21, 2010
    Date of Patent: November 18, 2014
    Assignee: Dow Global Technologies LLC
    Inventor: Bei Yin
  • Patent number: 8889677
    Abstract: This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, Ar, R1, R2, R3 have meanings given in the description.
    Type: Grant
    Filed: January 11, 2013
    Date of Patent: November 18, 2014
    Assignee: Boehringer Ingellheim International GmbH
    Inventors: Matthias Grauert, Daniel Bischoff, Georg Dahmann, Raimund Kuelzer, Klaus Rudolf
  • Publication number: 20140335174
    Abstract: The present invention provides a dry-coated tablet comprising: an inner core containing, as active ingredients, (a) tegafur, (b) gimeracil, and (c) oteracil potassium; and an outer shell.
    Type: Application
    Filed: May 24, 2012
    Publication date: November 13, 2014
    Applicant: TAIHO PHARMACEUTICAL CO., LTD.
    Inventors: Takumi Okamoto, Takashi Yoshizawa, Yoshito Ohnishi
  • Publication number: 20140329884
    Abstract: The present invention provides novel 1,3,5-triazinane-2,4,6-trione derivatives, such as compounds of any one of Formulae (I) and (II), and salts thereof, and methods of preparing the compounds. Also provided are compositions including a compound of the invention and an agent (e.g., an siRNA, mRNA, or plasmid DNA). The present invention also provides methods and kits using the compositions for delivering an agent to a subject (e.g., to the liver, spleen, or lung of the subject) or cell and for treating and/or preventing a range of diseases, such as genetic diseases, proliferative diseases, hematological diseases, neurological diseases, liver diseases, and lung diseases.
    Type: Application
    Filed: May 1, 2014
    Publication date: November 6, 2014
    Inventors: Yizhou Dong, Akinleye C. Alabi, Hao Yin, Joseph R. Dorkin, Delai Chen, Robert S. Langer, Daniel Griffith Anderson, Ahmed A. Eltoukhy
  • Publication number: 20140329674
    Abstract: The present specification discloses honeybee repellents exhibiting repellent properties similar to 2-heptanone, compositions comprising such repellents, uses to repel a honeybee from a mammal, location, plant, structure treated of such repellents, and methods of treating a mammal, location, plant, structure by applying such repellents.
    Type: Application
    Filed: May 3, 2014
    Publication date: November 6, 2014
    Applicant: INSCENT, INC.
    Inventors: Daniel F. Woods, Spiros Dimitratos, Robin W. Justice
  • Publication number: 20140315839
    Abstract: Provided is a pest control composition containing a novel iminopyridine derivative and other pest control agents. Provided is a pest control composition containing an iminopyridine derivative represented by the following Formula (I) and at least one of other pest control agents: [in the formula (I), Ar represents a 5- to 6-membered heterocycle which may be substituted, A represents a heterocycle having a 5- to 10-membered unsaturated bond including one or more nitrogen atoms, and has an imino group substituted with an R group at a position adjacent to the nitrogen atom present on the cycle, Y represents hydrogen, halogen and the like, and R represents any one of groups represented by the following Formulae (a) to (e), (y) or (z)].
    Type: Application
    Filed: July 1, 2014
    Publication date: October 23, 2014
    Applicant: MEIJI SEIKA PHARMA CO., LTD.
    Inventors: Ryo HORIKOSHI, Yasumichi ONOZAKI, Satoshi NAKAMURA, Masahiro NOMURA, Makoto MATSUMURA, Masaaki MITOMI
  • Patent number: 8864853
    Abstract: An additive mixture for fuels including a) at least one N-formal, b) at least one antioxidant and c) at least one corrosion inhibitor. The additive mixture ensures that the additized fuels and lubricants have biocidal and corrosion-inhibiting additization, especially when they include proportions of renewable raw materials, such as biodiesel, and when they are in contact with copper-containing surfaces.
    Type: Grant
    Filed: June 21, 2010
    Date of Patent: October 21, 2014
    Assignee: l'Air Liquide Societe Anonyme pour l'etude et L'exploitation des Procedes Georges Claude
    Inventors: Wolfgang Beilfuss, Ralf Gradtke, Jennifer Knopf, Ingo Krull
  • Publication number: 20140296068
    Abstract: This document discloses molecules having the following formula (Formula One) and processes related thereto.
    Type: Application
    Filed: October 24, 2012
    Publication date: October 2, 2014
    Applicant: DOW AGROSCIENCES LLC
    Inventors: Negar Garizi, Tony K. Trullinger, Ricky Hunter, Yu Zhang, Noormohamed M. Niyaz, Daniel Knueppel, Christian T. Lowe, Ann M. Buysse
  • Patent number: 8846910
    Abstract: The present invention relates to ?-hydroxy and amino-substituted carboxylic acids, which act as matrix metalloproteinase inhibitors, particularly diastereomerically pure ?-hydroxy carboxylic acids, corresponding processes for their synthesis, and pharmaceutical compositions containing the compounds of the present invention. Compounds of the present invention are useful in the treatment of various inflammatory, autoimmune, and allergic diseases, such as methods of treating asthma, rheumatoid arthritis, COPD, rhinitis, osteoarthritis, psoriatic arthritis, psoriasis, pulmonary fibrosis, wound healing disorders, pulmonary inflammation, acute respiratory distress syndrome, perodontitis, multiple sclerosis, gingivitis, atherosclerosis, neointimal proliferation, which leads to restenosis and ischemic heart failure, stroke, renal diseases, tumor metastasis, and other inflammatory disorders characterized by the over-expression and over-activation of a matrix metalloproteinase.
    Type: Grant
    Filed: July 8, 2013
    Date of Patent: September 30, 2014
    Assignee: Ranbaxy Laboratories Limited
    Inventors: Viswajanani J. Sattigeri, Venkata P. Palle, Manoj Kumar Khera, Ranadheer Reddy, Manoj Kumar Tiwari, Ajay Soni, Abdul Rehman Abdul Rauf, Sony Joseph, Arpita Musib, Sunanda G. Dastidar, Punit Kumar Srivastava
  • Patent number: 8841294
    Abstract: The invention relates to insecticidal and acaricidal mixtures comprising certain cyclic ketoenols and agonists or antagonists of nicotinic acetylcholine receptors for protecting plants against attack by pests.
    Type: Grant
    Filed: January 6, 2005
    Date of Patent: September 23, 2014
    Assignee: Bayer Cropscience AG
    Inventors: Reiner Fischer, Christoph Erdelen
  • Patent number: 8828908
    Abstract: Bicyclic dione compounds of formula (I), and derivatives thereof, which are suitable for use as herbicides.
    Type: Grant
    Filed: May 27, 2008
    Date of Patent: September 9, 2014
    Assignee: Syngenta Limited
    Inventors: Christopher John Mathews, Matthew Brian Hotson, Alan John Dowling, James Nicholas Scutt, Mangala Govenkar, Lee Challinor
  • Patent number: 8816073
    Abstract: The present invention relates to ?-hydroxy and amino-substituted carboxylic acids, which act as matrix metalloproteinase inhibitors, particularly diastereomerically pure ?-hydroxy carboxylic acids, corresponding processes for their synthesis, and pharmaceutical compositions containing the compounds of the present invention. Compounds of the present invention are useful in the treatment of various inflammatory, autoimmune, and allergic diseases, such as methods of treating asthma, rheumatoid arthritis, COPD, rhinitis, osteoarthritis, psoriatic arthritis, psoriasis, pulmonary fibrosis, wound healing disorders, pulmonary inflammation, acute respiratory distress syndrome, perodontitis, multiple sclerosis, gingivitis, atherosclerosis, neointimal proliferation, which leads to restenosis and ischemic heart failure, stroke, renal diseases, tumor metastasis, and other inflammatory disorders characterized by the over-expression and over-activation of a matrix metalloproteinase.
    Type: Grant
    Filed: July 8, 2013
    Date of Patent: August 26, 2014
    Assignee: Ranbaxy Laboratories Limited
    Inventors: Viswajanani J. Sattigeri, Venkata P. Palle, Manoj Kumar Khera, Ranadheer Reddy, Manoj Kumar Tiwari, Ajay Soni, Abdul Rehman Abdul Rauf, Sony Joseph, Arpita Musib, Sunanda G. Dastidar, Punit Kumar Sricastava