Nitrogen Double Bonded Directly At 2-position Of The Diazole Ring, Or Tautomeric Equivalent Patents (Class 514/388)
  • Patent number: 10583124
    Abstract: Compositions, methods of preparing compositions, and methods of treating parasitic nematode infections in wild birds include a fenbendazole premix and a grain formulation. The fenbendazole premix includes fenbendazole, a solvent, a solubilizing agent, and a premix grain carrier. The grain formulation includes a plurality of grains selected from the group consisting of ground corn, soybean meal, whole milo, wheat midds, and rice bran. The fenbendazole premix is integrated within the grain formulation thereby yielding a fenbendazole concentration in the composition of between 80 ppm and 120 ppm. Processes and methods of preparation include mixing the fenbendazole premix and grain formulation in an industrial ribbon mixer, fully integrating the fenbendazole within the grain formulation. Methods of treating include collecting and testing samples, determining a number and location of treatment systems, and charging a feeder with the claimed composition.
    Type: Grant
    Filed: February 25, 2016
    Date of Patent: March 10, 2020
    Inventor: Ronald J. Kendall
  • Patent number: 9616135
    Abstract: The disclosure relates to improving the aqueous solubility of 2-iminobiotin. In a particular aspect, the disclosure pertains to formulations suitable for administration of 2-iminobiotin to mammals suffering from disorders or conditions that benefit from that administration.
    Type: Grant
    Filed: April 1, 2015
    Date of Patent: April 11, 2017
    Assignee: Neurophyxia B.V.
    Inventor: Paul W. T. J. Leufkens
  • Patent number: 9023878
    Abstract: The disclosure relates to improving the aqueous solubility of 2-iminobiotin. In a particular aspect, the invention pertains to formulations suitable for administration of 2-iminobiotin to mammals suffering from disorders or conditions that benefit from said administration.
    Type: Grant
    Filed: May 26, 2011
    Date of Patent: May 5, 2015
    Assignee: Neurophyxia B.V.
    Inventor: Paul W. T. J. Leufkens
  • Patent number: 8981112
    Abstract: The present invention relates to spirocyclic acylguanidines and their use as inhibitors of the ?-secretase enzyme (BACE1) activity, pharmaceutical compositions containing the same, and methods of using the same as therapeutic agents in the treatment of neurodegenerative disorders, disorders characterized by cognitive decline, cognitive impairment, dementia and diseases characterized by production of ?-amyloid aggregates.
    Type: Grant
    Filed: March 4, 2013
    Date of Patent: March 17, 2015
    Assignees: Vitae Pharmaceuticals, Inc., Boehringer-Ingelheim International GmbH
    Inventors: Yuri Bukhtiyarov, Salvacion Cacatian, Lawrence Wayne Dillard, Cornelia Dorner-Ciossek, Klaus Fuchs, Lanqi Jia, Deepak S. Lala, Angel Morales-Ramos, Jonathan Reeves, Suresh B. Singh, Shankar Venkatraman, Zhenrong Xu, Jing Yuan, Yi Zhao, Yajun Zheng, Georg Rast
  • Patent number: 8889681
    Abstract: Pharmaceutical compositions comprising tricyclic 3,4-propinoperhydropurines and uses thereof for the treatment of facial wrinkling are provided.
    Type: Grant
    Filed: October 1, 2013
    Date of Patent: November 18, 2014
    Assignee: Korea Research Institute of Chemical Technology
    Inventor: Nestor Antonio Lagos Wilson
  • Patent number: 8871794
    Abstract: Methods and compositions for agonizing a type-2 orexin receptor (OX2R) in a cell determined to be in need thereof, including the general method of (a) administering to a subject a cyclic guanidinyl OX2R agonist and (b) detecting a resultant enhanced wakefulness or increased resistance to diet-induced accumulation of body fat, or abbreviated recovery from general anesthesia or jet lag.
    Type: Grant
    Filed: August 20, 2012
    Date of Patent: October 28, 2014
    Assignee: Board of Regents, The University of Texas System
    Inventor: Masashi Yanagisawa
  • Patent number: 8871763
    Abstract: Pharmaceutical compositions comprising tricyclic 3,4-propinoperhydropurines and uses thereof for the treatment of facial wrinkling are provided.
    Type: Grant
    Filed: April 10, 2014
    Date of Patent: October 28, 2014
    Assignee: Phytotox, Ltd.
    Inventor: Nestor Antonio Lagos Wilson
  • Patent number: 8859562
    Abstract: The present invention relates to the use of an agent that inhibits the activity of an enzyme that mediates repair of a DNA strand break in the manufacture of a medicament for the treatment of diseases caused by a defect in a gene that mediates homologous recombination.
    Type: Grant
    Filed: July 23, 2004
    Date of Patent: October 14, 2014
    Assignee: The University of Sheffield
    Inventor: Thomas Helleday
  • Publication number: 20140296177
    Abstract: A new class of biotin protein ligase (BPL) inhibitors that have antibacterial activity against multiple Staphylococcus aureus isolates, including clinically important methicillin-resistant S. aureus (MRSA) are disclosed that are non-toxic.
    Type: Application
    Filed: September 21, 2012
    Publication date: October 2, 2014
    Inventors: Andrew Abel, Steven Polyak, Grant Booker, John Wallace, Tatiana Soares Da Costa, Angie Jarrad, William Tieu, Kelly Lee Keeling, Daniel Sejer Pederson, Nicole Pendini, Matthew Wilce, Min Yin Yap
  • Publication number: 20140242153
    Abstract: Disclosed are novel methods for making cochleates and cochleate compositions that include introducing a cargo moiety to a liposome in the presence of a solvent. Also disclosed are cochleates and cochleate compositions that include an aggregation inhibitor, and optionally, a cargo moiety. Additionally, anhydrous cochleates that include a protonized cargo moiety, a divalent metal cation and a negatively charge lipid are disclosed. Methods of using the cochleate compositions of the invention, including methods of administration, are also disclosed.
    Type: Application
    Filed: January 30, 2014
    Publication date: August 28, 2014
    Applicant: RUTGERS, THE STATE UNIVERSITY OF NEW JERSEY
    Inventors: Raphael J. Mannino, Susan Gould-Fogerite, Sara L. Krause-Elsmore, David Delmarre, Ruying Lu
  • Patent number: 8759537
    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, M, W, R1, R2, R6, R7, R8 have meanings given in the description.
    Type: Grant
    Filed: August 17, 2011
    Date of Patent: June 24, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Henning Priepke, Henri Doods, Raimund Kuelzer, Roland Pfau, Dirk Stenkamp, Benjamin Pelcman, Robert Roenn
  • Patent number: 8759535
    Abstract: Substituted fused imidazole derivatives, methods of their preparation, pharmaceutical compositions comprising a substituted fused imidazole derivative, and methods of use in treating inflammation are provided. The substituted fused imidazole derivatives may control the activity or the amount or both the activity and the amount of heme-oxygenase.
    Type: Grant
    Filed: February 16, 2011
    Date of Patent: June 24, 2014
    Assignee: High Point Pharmaceuticals, LLC
    Inventors: Adnan M. M. Mjalli, Dharma Rao Polisetti, Jareer Nabeel Kassis, Matthew J. Kostura, Mustafa Guzel, Otis Clinton Attucks, Robert Carl Andrews, Samuel Victory, Suparna Gupta
  • Patent number: 8686016
    Abstract: Disclosed is a method for preventing or treating an undesirable condition in a subject carrying cells homozygous null for the neurofibromatosis type 1 gene or subjects that are haploinsufficient for the neurofibromatosis type 1 gene, the method comprising administering to a subject in need thereof an effective amount of a schweinfurthin or schweinfurthin analog or derivative, or a pharmaceutically acceptable salt, prodrug, hydrate, or solvate thereof. Also disclosed is a new schweinfurthin compound of the formula.
    Type: Grant
    Filed: April 30, 2010
    Date of Patent: April 1, 2014
    Assignees: The United States of America, as represented by the Secretary, Department of Health and Human Services, University of Iowa Research Foundation
    Inventors: Karlyne Reilly, Thomas Turbyville, John A. Beutler, David Wiemer
  • Patent number: 8674113
    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, R9, Ra, Rb have meanings given in the description.
    Type: Grant
    Filed: December 8, 2011
    Date of Patent: March 18, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Henning Priepke, Henri Doods, Alexander Heim-Riether, Raimund Kuelzer, Roland Pfau, Klaus Rudolf, Dirk Stenkamp
  • Patent number: 8633324
    Abstract: MN-029 di-hydrochloride (MN-029.2HCl, Formula 2) is a potent vascular targeting agent. The present invention focuses on the synthesis and characterization of the di-hydrochloride salt MN-029 and the preparation of pharmaceutically acceptable formulations thereof. Methods are disclosed of using the compound and formulations thereof in the treatment of diseases that rely on the generation of neovasculature by angiogenesis for disease progression.
    Type: Grant
    Filed: July 27, 2012
    Date of Patent: January 21, 2014
    Assignee: Medicinova, Inc.
    Inventor: Kale Ruby
  • Patent number: 8623409
    Abstract: An oral clonidine dosage unit providing a twenty-four hour extended release profile following a single dose administration is provided. The dosage unit comprises a pharmaceutically effective amount of a coated complex comprising clonidine bound to a cationic exchange resin, which is characterized by a twenty-four hour release profile with a single peak, wherein said oral clonidine dosage unit provides a therapeutically effective plasma concentration for at least about 70%, or at least 85% of the twenty-four hour period following the single dose administration. Both liquid and solid formulations are provided, as are methods of treating a patient by a single administration of a formulation of the invention so as to achieve a therapeutic effect for 24-hours.
    Type: Grant
    Filed: October 20, 2010
    Date of Patent: January 7, 2014
    Assignee: Tris Pharma Inc.
    Inventors: Ketan Mehta, Yu-Hsing Tu
  • Publication number: 20130345273
    Abstract: Provided are methods for reversing the effects of agents used for muscular immobilization and/or loss of consciousness and/or loss of pain perception. The method comprises administering a composition comprising acyclic CB[n]-type compounds to an individual in need of reversal of the effects of neuromuscular blocking agents and/or anesthetic agents such that the effects of the agent(s) are partially fully reversed.
    Type: Application
    Filed: October 13, 2011
    Publication date: December 26, 2013
    Applicants: GENERAL HOSPITAL CORPORATION, UNIVERSITY OF MARYLAND, COLLEGE PARK
    Inventors: Lyle David Isaacs, Da Ma, Matthias Eikermann
  • Publication number: 20130245085
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein R0, R1, R2, R3, R4 and a are defined herein.
    Type: Application
    Filed: April 30, 2013
    Publication date: September 19, 2013
    Applicant: Janssen Pharmaceutica, NV
    Inventors: Mark J. Macielag, Mingde Xia, Xiaoqing Xu
  • Publication number: 20130224298
    Abstract: The invention relates to a novel two-phase preparation for use as a food supplement, dietary substance, and/or medicament. The medical use thereof for helping the immune system fight against viral diseases, especially herpes, is particularly preferred. Said preparation may have two different phases which may be used in a chronologically staggered manner, mutually blocking agents being in different phases and mutually boosting agents being in the same phase.
    Type: Application
    Filed: February 14, 2013
    Publication date: August 29, 2013
    Applicant: NUTRITEAM GMBH
    Inventor: NUTRITEAM GMBH
  • Publication number: 20130217668
    Abstract: Compounds of Formula (I) are useful inhibitors of anaplastic lymphoma kinase. Compounds of Formula (I) have the following structure: where the definitions of the variables are provided herein.
    Type: Application
    Filed: July 28, 2011
    Publication date: August 22, 2013
    Applicant: AMGEN INC.
    Inventors: Christiane M. Boezio, Alan C. Cheng, Deborah Choquette, Richard T. Lewis, Michele H. Potashman, Karina Romero, John C. Stellwagen, Douglas A. Whittington
  • Publication number: 20130190273
    Abstract: This technology relates generally to compounds and methods for stimulating neurogenesis (e.g., post-natal neurogenesis, including post-natal hippocampal and hypothalamic neurogenesis) and/or protecting neuronal cell from cell death. Various compounds are disclosed herein. In vivo activity tests suggest that these compounds may have therapeutic benefits in neuropsychiatric and/or neurodegenerative diseases such as schizophrenia, major depression, bipolar disorder, normal aging, epilepsy, traumatic brain injury, post-traumatic stress disorder, Parkinson's disease, Alzheimer's disease, Down syndrome, spinocerebellar ataxia, amyotrophic lateral sclerosis, Huntington's disease, stroke, radiation therapy, chronic stress, abuse of a neuro-active drug, retinal degeneration, spinal cord injury, peripheral nerve injury, physiological weight loss associated with various conditions, as well as cognitive decline associated with normal aging, chemotherapy, and the like.
    Type: Application
    Filed: February 19, 2013
    Publication date: July 25, 2013
    Applicant: BOARD OF REGENTS OF THE UNIVERSITY OF TEXAS SYSTEM
    Inventor: BOARD OF REGENTS OF THE UNIVERSITY OF TEXAS SYSTEM
  • Patent number: 8492314
    Abstract: The present invention provides a concentrate for dilution with water in the preparation of an agricultural composition for application to crops, soil or animals. The concentrate is recommended for use with agricultural chemicals whose agricultural activity varies with the pH of the water. It comprises an active ingredient and a combination of pH indicators for coloring the water, the pH indicators being selected so as to indicate different colors of spray water at different pH levels. The proportions of active ingredient and pH indicators are selected so that when the concentrate is added to water, the pH indicators indicate visually upper and lower pH limits for optimum activity of the agricultural chemical.
    Type: Grant
    Filed: May 11, 2007
    Date of Patent: July 23, 2013
    Assignee: AECI Limited
    Inventors: Hendrik Frederik Greyling, Hugo R Minnaar, Martin D Bloomberg
  • Publication number: 20130143936
    Abstract: The disclosure relates to improving the aqueous solubility of 2-iminobiotin. In a particular aspect, the invention pertains to formulations suitable for administration of 2-iminobiotin to mammals suffering from disorders or conditions that benefit from said administration.
    Type: Application
    Filed: May 26, 2011
    Publication date: June 6, 2013
    Inventor: Paul W. T. J. Leufkens
  • Patent number: 8426607
    Abstract: The present invention relates to substituted amino-benzimidazoles of general formula (1) wherein the groups R1 to R14 and A, are defined as in the specification and claims and the use thereof for the treatment of Alzheimer's disease (AD) and similar diseases.
    Type: Grant
    Filed: January 21, 2009
    Date of Patent: April 23, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Klaus Fuchs, Cornelia Dorner-Ciossek, Sandra Handschuh, Niklas Heine, Stefan Hoerer, Klaus Klinder
  • Publication number: 20130090342
    Abstract: The invention relates to new derivatives of formula (I), wherein the substituents are as defined in the specification; to processes for the preparation of such derivatives; pharmaceutical compositions comprising such derivatives; such derivatives as a medicament; such derivatives for the treatment of one or more IGF-1R mediated disorders or diseases.
    Type: Application
    Filed: June 16, 2011
    Publication date: April 11, 2013
    Applicant: NOVARTIS AG
    Inventors: Frederic Berst, Pascal Furet, Andreas Marzinzik
  • Patent number: 8394969
    Abstract: Novel compounds of the structural formula (I) are activators of AMP-protein kinase and are useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention are useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension.
    Type: Grant
    Filed: September 21, 2009
    Date of Patent: March 12, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Brett C. Bookser, Qun Dang, Tony S. Gibson, Hongjian Jiang, De Michael Chung, Jianming Bao, Jinlong Jiang, Andy Kassick, Ahmet Kekec, Ping Lan, Huagang Lu, Gergely M. Makara, F. Anthony Romero, Iyassu Sebhat, David Wilson, Dariusz Wodka
  • Publication number: 20130059852
    Abstract: Some embodiments of this invention include methods for treating disease and methods for administering a compound of Formula (I). In some aspects of the invention, diseases can be treated by administration of compositions comprising a compound of Formula (I). Pharmaceutical compositions of some embodiments of the present invention comprise a compound of Formula (I).
    Type: Application
    Filed: April 8, 2011
    Publication date: March 7, 2013
    Applicant: UNIVERSITY OF LOUISVILLE RESEARCH FOUNDATION, INC.
    Inventors: John O. Trent, Jason B. Meier, Kelby B. Napier
  • Publication number: 20130041002
    Abstract: MN-029 di-hydrochloride (MN-029.2HCl, Formula 2) is a potent vascular targeting agent. The present invention focuses on the synthesis and characterization of the di-hydrochloride salt MN-029 and the preparation of pharmaceutically acceptable formulations thereof. Methods are disclosed of using the compound and formulations thereof in the treatment of diseases that rely on the generation of neovasculature by angiogenesis for disease progression.
    Type: Application
    Filed: July 27, 2012
    Publication date: February 14, 2013
    Inventor: Kale RUBY
  • Publication number: 20130030004
    Abstract: The present invention relates to compounds of formula I: or a pharmaceutically acceptable salt thereof, that inhibit bacterial gyrase and/or TopoIV and pharmaceutically acceptable compositions comprising said compounds. These compounds, and compositions thereof, are useful in treating bacterial infection. Accordingly, the present invention also relates to methods for treating bacterial infections in mammals.
    Type: Application
    Filed: November 6, 2006
    Publication date: January 31, 2013
    Inventors: Paul Charifson, David Deininger, Joseph Drumm, Anne-Laure Grillot, Arnaud LeTiran, Yusheng Liao, Emanuele Perola, Steven Ronkin, Dean Stamos, Tiansheng Wang
  • Publication number: 20130005666
    Abstract: The NF-E2-related factor 2 (Nrf2) is a key transcriptional regulator of antioxidant defense and detoxification. To directly monitor stabilization of Nrf2 we fused its Neh2 domain, responsible for the interaction with its nucleocytoplasmic regulator, Keap1, to firefly luciferase (Neh2-luciferase). It is shown herein that Neh2 domain is sufficient for recognition, ubiquitination and proteasomal degradation of Neh2-luciferase fusion protein. The novel Neh2-luc reporter system allows direct monitoring of the adaptive response to redox stress and classification of drugs based on the time-course of reporter activation. The novel reporter was used to screen a library of compounds to identify activators of Nrf2. The most robust and yet non toxic Nrf2 activators found—nordihydroguaiaretic acid, fisetin, and gedunin-induced astrocyte-dependent neuroprotection from oxidative stress via an Nrf2-dependent mechanism.
    Type: Application
    Filed: June 29, 2012
    Publication date: January 3, 2013
    Applicant: CORNELL UNIVERSITY
    Inventors: Rajiv RATAN, Irina GAZARYAN, Natalya A. SMIRNOVA
  • Publication number: 20120315298
    Abstract: A method for treating a neurofibroma, e.g. dermal neurofibroma, a subdermal neurofibroma, or a superficial plexiform neurofibroma, in a subject in need of such treatment is disclosed. The method comprises locally applying a composition to a neurofibroma either topically or intralesionally. This method does not encompass systemic administration of the composition to the subject to have an effect on the neurofibromas. Compositions useful for such treatments and methods of preparing the compositions are disclosed.
    Type: Application
    Filed: June 15, 2012
    Publication date: December 13, 2012
    Applicant: NEXGENIX PHARMACEUTICALS, INC
    Inventors: Ruihong CHEN, Allan E. Rubenstein, Xiaodong Shen, Scott Stewart, Jin-Chen Yu
  • Patent number: 8329914
    Abstract: Novel compounds of the structural formula (I) are activators of AMP-protein kinase and are useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention are useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension.
    Type: Grant
    Filed: October 22, 2009
    Date of Patent: December 11, 2012
    Assignees: Merck Sharp & Dohme Corp, Metabasas Therapeutics, Inc.
    Inventors: Jianming Bao, Ping Lan, Huagang Lu, Gergely M. Makara, F. Anthony Romero, Iyassu Sebhat, Dariusz Wodka, Qun Dang, De Michael Chung, Tony S. Gibson, Hongjian Jiang, Daniel K. Cashion
  • Publication number: 20120295895
    Abstract: A method of treating an ocular disorder in a subject associated with aberrant all-trans-retinal clearance in the retina, the method comprising administering to the subject a therapeutically effective amount of a primary amine compound of formula: wherein R1 is an aliphatic and/or aromatic compound.
    Type: Application
    Filed: June 8, 2012
    Publication date: November 22, 2012
    Inventors: Krzysztof Palczewski, Akiko Maeda, Marcin Golczak
  • Patent number: 8299108
    Abstract: New substituted benz-azole compounds, compositions and methods of inhibition of Raf kinase activity in a human or animal subject are provided. The new compounds compositions may be used either alone or in combination with at least one additional agent for the treatment of a Raf kinase mediated disorder, such as cancer.
    Type: Grant
    Filed: September 29, 2003
    Date of Patent: October 30, 2012
    Assignee: Novartis AG
    Inventors: Payman Amiri, Wendy Fantl, Barry Haskell Levine, Daniel J. Poon, Savithri Ramurthy, Paul A. Renhowe, Sharadha Subramanian, Leonard Sung
  • Patent number: 8258163
    Abstract: Methods and compositions for agonizing a type-2 orexin receptor (OX2R) in a cell determined to be in need thereof, including the general method of (a) administering to a subject a cyclic guanidinyl OX2R agonist and (b) detecting a resultant enhanced wakefulness or increased resistance to diet-induced accumulation of body fat, or abbreviated recovery from general anesthesia or jet lag.
    Type: Grant
    Filed: June 4, 2009
    Date of Patent: September 4, 2012
    Assignee: Board of Regents, The University of Texas System
    Inventor: Masashi Yanagisawa
  • Patent number: 8236965
    Abstract: A subject of the present application is new benzimidazole derivatives of formula in which A, Y, R1, R2, R3 and R4 represent different variable groups. These products have an antagonist activity of GnRH (Gonadotropin-Releasing Hormone). The invention also relates to pharmaceutical compositions containing said products and their use for the preparation of a medicament.
    Type: Grant
    Filed: December 23, 2008
    Date of Patent: August 7, 2012
    Assignee: IPSEN Pharma S.A.S.
    Inventors: Lydie Poitout, Valérie Brault, Eric Ferrandis, Christophe Thurieau
  • Patent number: 8232410
    Abstract: The present invention relates to novel benzimidazole derivatives and pharmaceutically acceptable salts thereof. Another aspect of the invention relates to methods of treating a patient infected by Mycobacterium tuberculosis or Francisella tulerensis by administering to the patient a benzimidazole derivative or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: April 21, 2008
    Date of Patent: July 31, 2012
    Assignee: The Research Foundation of State University of New York
    Inventors: Iwao Ojima, Seung-yub Lee
  • Patent number: 8178694
    Abstract: Heterocyclylaminoalkyl Substituted Benzimidazoles Inhibitors of RSV replication of formula (I): The salts and stereochemically isomeric forms thereof, wherein Q is hydrogen, C1-6alkyl optionally substituted with a heterocycle or Q is C1-6alkyl substituted with both —OR4 and a heterocycle; wherein said heterocycle is oxazolidine, thiazolidine, 1-oxo-thiazolidine, 1,1-dioxothiazolidine, morpholinyl, thiomorpholinyl, 1-oxo-thiomorpholinyl, 1,1-dioxothiomorpholinyl, hexahydrooxazepine, hexahydrothiazepine, 1-oxo-hexahydrothiazepine, 1,1-dioxo-hexahydrothiazepine, pyrrolidine, piperidine, homopiperidine, piperazine; which heterocyle may be substituted with 1-2 substituents; each Alk is C1-6alkanediyl; R1 is Ar or optionally substituted piperidinyl, piperazinyl, morpholinyl, thiomorpholinyl, pyridyl, pyrazinyl, pyridazinyl, pyrimidinyl, furanyl, tetrahydrofuranyl, thienyl, pyrrolyl, thiazolyl, oxazolyl, imidazolyl, isothiazolyl, pyrazolyl, isoxazo lyl, oxadiazolyl, quinolinyl, quinoxalinyl, benzofuranyl, benzothien
    Type: Grant
    Filed: June 20, 2006
    Date of Patent: May 15, 2012
    Assignee: Tibotec Pharmaceuticals Ltd.
    Inventors: Jean-François Bonfanti, Philippe Muller, Jérôme Michel Claude Fortin, Frédéric Marc Maurice Doublet
  • Publication number: 20120108562
    Abstract: PAD4 inhibitory compositions and methods for their use in treatment of cancer and autoimmune disease are provided according to embodiments of the present invention.
    Type: Application
    Filed: November 1, 2011
    Publication date: May 3, 2012
    Applicant: The Penn State Research Foundation
    Inventors: Gong Chen, Yanming Wang, Pingxin Li, Jing Hu, Shu Wang, Yuji Wang
  • Publication number: 20110312969
    Abstract: Compounds of general formula (I): wherein R1, R2, R3, R4, R5, R6, X and Y are as defined herein are inhibitors of Bcl-2 and are useful for treating diseases characterised by abnormal cell growth and/or dysregulated apoptosis.
    Type: Application
    Filed: December 8, 2009
    Publication date: December 22, 2011
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Stephen Peter East, Mark Whittaker, Osamu Ichihara, Adrian Kotei Kotei, Smantha Jayne Bamford
  • Publication number: 20110293558
    Abstract: The invention in some aspects relates to methods, devices and compositions for evaluating material properties, such as mechanical and rheological properties of substances, particularly biological substances, such as cells, tissues, and biological fluids. In some aspects, the invention relates to methods, devices and compositions for evaluating material properties of deformable objects, such as cells. In further aspects, the invention relates to methods, devices and compositions for diagnosing and/or characterizing disease based on material properties of biological cells.
    Type: Application
    Filed: March 21, 2011
    Publication date: December 1, 2011
    Applicant: Massachusetts Institute of Technology
    Inventors: Subra Suresh, Jianzhu Chen, Irene Yin-Ting Chang
  • Patent number: 7960561
    Abstract: This invention relates to novel 2-(phenylamino)benzimidazole derivatives useful as modulators of small-conductance calcium-activated potassium channels (SK channels). In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.
    Type: Grant
    Filed: June 21, 2006
    Date of Patent: June 14, 2011
    Assignee: Neurosearch A/S
    Inventors: Ulrik Svane Sørensen, Lene Teuber, Dan Peters, Dorte Strøbæk, Tina Holm Johansen, Karin Sandager Nielsen, Palle Christophersen
  • Patent number: 7956196
    Abstract: Novel 1,3-dihydro-benzimidazol-2-ylidene amine derivatives of formula the addition salts and stereochemically isomeric forms wherein each Alk is C1-6alkanediyl; Q is hydrogen; C1-6alkyl substituted with one or two Ar2 radicals; C1-6alkyl substituted with quinolinyl, oxazolidinyl, thiazolidinyl, morpholinyl, thiomorpholinyl, or with pyrrolidinonyl; —CO—Ar2; or Q is a radical of formula wherein t is 1, 2 or 3; R4 is amino, mono-or di(C1-6alkyl)amino; R1 is Ar2, —CO—Ar2 or a monocyclic or bicyclic heterocycle which may optionally be substituted; R2 is as R1 and additionally can be hydrogen; where Q is other than hydrogen, R3 is hydrogen; and where Q is other than hydrogen, R3 is a radical: wherein R6 is hydrogen, C1-6alkyl, substituted C1-6alkyl; R7, R8, R9 are halo, cyano, C1-6alkyl, substituted C1-6alkyl, C2-6alkenyl, cyanoC2-6alkenyl, C2-6alkynyl, cyanoC2 6alkynyl, Ar1, R10a—0—, R10a—S—, —N(R5aR5b), R10a—O—C(?O)—, N(R5aR5b)—C(?O)—, R10a—C(?O)—NR5b—, R10b—C(?O)—O—; and R8 and/or R9 may also be
    Type: Grant
    Filed: March 17, 2006
    Date of Patent: June 7, 2011
    Assignee: Tibotec Pharmaceuticals Ltd.
    Inventors: Jean-François Bonfanti, Jérôme Michel Claude Fortin, Ismet Dorange
  • Patent number: 7947709
    Abstract: Compounds of formula I, wherein R1, R2, R3, X and Ar, are as defined herein or pharmaceutically acceptable salts thereof, inhibit HIV-1 reverse transcriptase and afford a method for prevention and treatment of HIV-1 infections and the treatment of AIDS and/or ARC. The present invention also relates to compositions containing compounds of formula I useful for the prevention and treatment of HIV-1 infections and the treatment of AIDS and/or ARC.
    Type: Grant
    Filed: June 20, 2008
    Date of Patent: May 24, 2011
    Assignee: Roche Palo Alto LLC
    Inventors: Todd Richard Elworthy, Joan Heather Hogg, Joshua Kennedy-Smith, Counde O'Yang, Mark Smith, Zachary Kevin Sweeney, Jeffrey Wu
  • Publication number: 20110082143
    Abstract: Bicyclic heteroaryl compounds of formula (I) shown below are disclosed. Each variable in formula (I) is defined in the specification. Also disclosed is treatment of cancer with these compounds.
    Type: Application
    Filed: October 1, 2010
    Publication date: April 7, 2011
    Applicant: National Taiwan University
    Inventors: Chung-Ming Sun, Min-Liang Kuo
  • Patent number: 7842817
    Abstract: This invention relates to novel 2-amino benzimidazole derivatives useful as modulators of small-conductance calcium-activated potassium channels (SK channels). In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.
    Type: Grant
    Filed: January 10, 2006
    Date of Patent: November 30, 2010
    Assignee: Neurosearch A/S
    Inventors: Ulrik Svane Sørensen, Lene Teuber, Dan Peters, Dorte Strøbæk, Tina Holm Johansen, Karin Sandager Nielsen, Palle Christophersen
  • Patent number: 7829698
    Abstract: Provided are nanoparticles prepared by the aggregation of cucurbituril derivatives and having a particle size of 1 to 1,000 nm, a pharmaceutical composition in which a pharmaceutically active substance is loaded into the nanoparticles, and preparation methods thereof.
    Type: Grant
    Filed: July 18, 2008
    Date of Patent: November 9, 2010
    Assignee: Postech Foundation
    Inventors: Kimoon Kim, Sang Yong Jon, Young Jin Jeon, Dong Hyun Oh, Narayanan Selvapalam
  • Publication number: 20100280087
    Abstract: This invention relates to novel 2-amino benzimidazole derivatives useful as modulators of small-conductance calcium-activated potassium channels (SK channels). In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.
    Type: Application
    Filed: July 8, 2010
    Publication date: November 4, 2010
    Inventors: Ulrik Svane Sørensen, Lene Teuber, Dan Peters, Dorte Strøbæk, Tina Holm Johansen, Karin Sandager Nielsen, Palle Christophersen
  • Patent number: 7763643
    Abstract: The present invention comprises compounds and compositions comprising substituted thiophene derivatives with the following backbone structure: The compounds of this type are of useful in the treatment of various disorders, such as, respiratory disorders and snoring, acute and chronic disorders, disorders induced by ischemic and/or reperfusion events and by proliferative or fibrotic events, disorders of the central nervous system and lipid metabolism, diabetes, blood coagulation and infection by parasites.
    Type: Grant
    Filed: January 30, 2009
    Date of Patent: July 27, 2010
    Assignee: Sanofi-Aventis Deutschland GmbH
    Inventors: Hans-Jochen Lang, Uwe Heinelt, Armin Hofmeister, Klaus Wirth, Michael Gekle, Markus Bleich
  • Patent number: 7741493
    Abstract: The present invention relates to a novel series of 4,5-diphenyl-2-amino-4,5-dihydro-imidazole derivatives of the formula II: wherein R, R1, R2, R3, R4, R5, X and Y are as defined herein. This invention also relates to methods of making these compounds. The compounds of this invention are P2X7 ion channel blockers and are therefore useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases having an inflammatory component, including inflammatory bowel disease, rheumatoid arthritis and disease conditions associated with the central nervous system, such as stroke, Alzheimer's disease, etc.
    Type: Grant
    Filed: November 29, 2007
    Date of Patent: June 22, 2010
    Assignee: Aventis Pharmaceuticals Inc.
    Inventors: Patrick Shum, Alexandre Gross, Liang Ma, Daniel G. McGarry, Gregory H. Merriman, David Rampe, Garth Ringheim, Jeffrey Stephen Sabol, Francis A. Volz