Chalcogen Bonded Directly To Ring Carbon Of The Hetero Ring Patents (Class 514/445)
  • Patent number: 10858369
    Abstract: New pseudopolymorphic forms of (3R,3aS,6aR)-hexahydrofuro [2,3-b] furan-3-yl (1S,2R)-3-[[(4-aminophenyl) sulfonyl] isobutyl) amino]-1-benzyl-2-hydroxypropylcarbamate and processes for producing them are disclosed.
    Type: Grant
    Filed: May 16, 2018
    Date of Patent: December 8, 2020
    Assignee: Janssen Sciences Ireland Unlimited Company
    Inventors: Hans Wim Pieter Vermeersch, Daniel Joseph Christiaan Thone, Luc Donne Marie-Louise Janssens, Piet Tom Bert Paul Wigerinck
  • Patent number: 10702497
    Abstract: Uses of acyl-homoserine lactone compounds are described. In particular, uses of acyl-homoserine lactone compounds as anti-thrombotic agents, to inhibit platelets from becoming hypersensitive, and/or to prevent thrombosis, are described.
    Type: Grant
    Filed: December 12, 2018
    Date of Patent: July 7, 2020
    Assignee: The University of Toledo
    Inventors: Randall G. Worth, Glenn R. Westphal, Brenton R. Keeley, Leah M. Wuescher
  • Patent number: 10316004
    Abstract: A process for preparing clomazone is provided, the process comprising reacting 4,4-dimethyl-3-isoxazolidinone with 2-chlorobenzyl chloride in an aqueous medium in the presence of a base, in particular an alkali metal hydroxide. A method for preparing clomazone is also disclosed, the method comprising (a) crystallizing clomazone from solution in an organic solvent; and (b) isolating the resulting crystals. N-benzene is a particularly suitable solvent. Further, there is provided Form I crystalline 2-[(2-chlorophenyl)methyl]-4,4-dimethyl-3-isoxazolidinone (clomazone), wherein the polymorph Form I is characterized by at least one of the following properties: (i) an X-ray powder diffraction pattern having characteristic peaks expressed in degrees 2?(+/?0.20° ?) at one or more of the following positions: about 10.63, 16.07, 18.08, 19.11, 19.34, 21.20, 24.78 and 28.80; and (ii) an infrared (IR) spectrum having a characteristic peak: at about 2967 and 2870 cm?1.
    Type: Grant
    Filed: June 13, 2014
    Date of Patent: June 11, 2019
    Assignee: ROTAM AGROCHEM INTERNATIONAL COMPANY LIMITED
    Inventor: James Timothy Bristow
  • Patent number: 10195177
    Abstract: Uses of acyl-homoserine lactone compounds are described. In particular, uses of acyl-homoserine lactone compounds as anti-thrombotic agents, to inhibit platelets from becoming hypersensitive, and/or to prevent thrombosis, are described.
    Type: Grant
    Filed: September 27, 2016
    Date of Patent: February 5, 2019
    Assignee: The University of Toledo
    Inventors: Randall G. Worth, Glenn R. Westphal, Brenton R. Keeley, Leah M. Wuescher
  • Patent number: 9808527
    Abstract: Described herein are compounds and compositions that are useful in the treatment of HIV, AIDS, and AIDS-related diseases. In addition, compounds are described herein that are capable of inhibiting the dimerization of HIV proteases.
    Type: Grant
    Filed: November 20, 2007
    Date of Patent: November 7, 2017
    Assignee: Purdue Research Foundation
    Inventors: Arun K. Ghosh, Hiroaki Mitsuya, Yasuhiro Koh
  • Patent number: 9751851
    Abstract: Antivirulence strategies to combat Pseudomonas aeruginosa, are described. One strategy encompasses synthesis of a series of compounds that inhibit the production of pyocyanin, a redox-active virulence factor produced by this pathogen. A related strategy encompasses synthesis of compounds that inhibit the two P. aeruginosa quorum-sensing receptors, LasR and RhlR, inhibit production of pyocyanin, and inhibit biofilm formation.
    Type: Grant
    Filed: September 19, 2014
    Date of Patent: September 5, 2017
    Assignee: THE TRUSTEES OF PRINCETON UNIVERSITY
    Inventors: Bonnie L. Bassler, Martin F. Semmelhack, Knut Drescher, Albert Siryaporn, Laura C. Conrad-Miller, Colleen T. O'Loughlin
  • Patent number: 9468624
    Abstract: A novel small molecule antagonizes two types of acyl homoserine lactone receptors: membrane-bound and cytoplasmic. A focused library of analogs and derivatives of the original antagonist was synthesized. Analog and derivative molecules harbor a range of activities. The novel small molecule and most potent antagonist protects the eukaryote Caenorhabditis elegans from quorum-sensing-mediated killing by the bacterial pathogen Chromobacterium violaceum. The saving of C. elegans demonstrates the use of these molecules as small molecule antimicrobials.
    Type: Grant
    Filed: June 15, 2015
    Date of Patent: October 18, 2016
    Assignee: THE TRUSTEES OF PRINCETON UNIVERSITY
    Inventors: Bonnie L. Bassler, Lee R. Swem, Scott M. Ulrich, Colleen T. O'Loughlin
  • Patent number: 9427426
    Abstract: Indication of use of erdosteine as antidote in a large number of intoxications, especially in heavy metals like lead or mercury, and paracetamol. Indication of use of erdosteine as prophylaxis for intoxications. Erdosteine can be administered per os or intravenous, using a solution obtained with sodium hydrogen carbonate and bidistilled water.
    Type: Grant
    Filed: August 13, 2009
    Date of Patent: August 30, 2016
    Assignee: RAFIFARM S.R.L.
    Inventors: Marco Peretto, Cristina Sarbulescu, Victor Voicu
  • Patent number: 9415040
    Abstract: Methods are provided for identifying molecules that can be used to positively and negatively manipulate quorum-sensing-mediated communication to control bacterial behavior. Small-molecule antagonists that disrupt quorum-sensing-mediated activities are identified. Methods are provided for disrupting detection of acyl-homoserine lactone autoinducer in Gram-negative bacteria by contacting the bacteria with the antagonists. Methods of inhibiting quorum sensing-mediated activity in Gram-negative bacteria are provided wherein the activity is pathogenicity, bioluminescence, siderophore production, type III secretion, or metalloprotease production.
    Type: Grant
    Filed: May 8, 2015
    Date of Patent: August 16, 2016
    Assignee: The Trustees of Princeton University
    Inventors: Bonnie Bassler, Lee Swem
  • Patent number: 9175005
    Abstract: The present invention provides novel crystalline hydrochloride salt of darunavir, process for its preparation and to pharmaceutical composition comprising it. The present invention also provides novel process for preparation of darunavir amorphous form and pharmaceutical composition comprising it.
    Type: Grant
    Filed: July 8, 2014
    Date of Patent: November 3, 2015
    Assignee: HETERO RESEARCH FOUNDATION
    Inventors: Bandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Dasari Muralidhara Reddy, Rapolu Raji Reddy, Bandi Vamsi Krishna, Kesireddy Subash Chander Reddy
  • Patent number: 9084773
    Abstract: A novel small molecule antagonizes two types of acyl homoserine lactone receptors: membrane-bound and cytoplasmic. A focused library of analogs and derivatives of the original antagonist was synthesized. Analog and derivative molecules harbor a range of activities. The novel small molecule and most potent antagonist protects the eukaryote Caenorhabditis elegans from quorum-sensing-mediated killing by the bacterial pathogen Chromobacterium violaceum. The saving of C. elegans demonstrates the use of these molecules as small molecule antimicrobials.
    Type: Grant
    Filed: May 28, 2014
    Date of Patent: July 21, 2015
    Assignee: The Trustees of Princeton University
    Inventors: Bonnie L. Bassler, Lee R. Swem, Scott M. Ulrich, Colleen T. O'Loughlin
  • Patent number: 9056851
    Abstract: This invention provides a compound having the structure wherein R1 is H, wherein n and q are independently an integer from 0 to 8; A is absent or present and when present is wherein m is an integer from 0 to 8; R3 is an amino, alkyl, aryl, heteroaryl, diol, piperazine, morpholine, piperidine, triazole, azide or biphenyl, each with or without substitution, branched or unbranched, or and R4 is alkyl, aryl, or heteroaryl, each with or without substitution, branched or unbranched, R2 is H, CH3, or alkyl, aryl, heteroaryl, pyrrole, diazole, or triazole, each with or without substitution, branched or unbranched, or wherein n and q are independently an integer from 0 to 8; A is absent or present and when present is and R6 is azide, methoxy, trifluoromethyl, biphenyl, substituted phenyl, substituted triazole, or alkyl, aryl or heteroaryl, with or without substitution, branched or unbranched, when R1 is H then R2 is other than H or CH3, and
    Type: Grant
    Filed: March 23, 2012
    Date of Patent: June 16, 2015
    Assignee: The Research Foundation for The State University of New York
    Inventors: Peter Tonge, Carl Machutta, Gopal Reddy Bommineni, Kanishk Kapilashrami
  • Patent number: 9045476
    Abstract: Methods are provided for identifying molecules that can be used to positively and negatively manipulate quorum-sensing-mediated communication to control bacterial behavior. Small-molecule antagonists that disrupt quorum-sensing-mediated activities are identified. Methods are provided for disrupting detection of acyl-homoserine lactone autoinducer in Gram-negative bacteria by contacting the bacteria with the antagonists. Methods of inhibiting quorum sensing-mediated activity in Gram-negative bacteria are provided wherein the activity is pathogenicity, bioluminescence, siderophore production, type III secretion, or metalloprotease production.
    Type: Grant
    Filed: September 17, 2013
    Date of Patent: June 2, 2015
    Assignee: The Trustees of Princeton University
    Inventors: Bonnie Bassler, Lee Swem
  • Patent number: 9029413
    Abstract: Alterations of certain metabolite concentrations and fluxes that occur in response to viral infection are described. Host cell enzymes in the involved metabolic pathways are selected as targets for intervention; i.e., to restore metabolic flux to disadvantage viral replication, or to further derange metabolic flux resulting in “suicide” of viral-infected cells (but not uninfected cells) to limit viral propagation. While any of the enzymes in the relevant metabolic pathway can be selected, pivotal enzymes at key control points in these metabolic pathways are preferred as candidate antiviral drug targets. Inhibitors of these enzymes are used to reverse, or redirect, the effects of the viral infection. Drug candidates are tested for antiviral activity using screening assays in vitro and host cells, and in animal models. Animal models are then used to test efficacy of candidate compounds in preventing and treating viral infections. Antiviral activity of enzyme inhibitors is demonstrated.
    Type: Grant
    Filed: April 3, 2012
    Date of Patent: May 12, 2015
    Assignee: The Trustees of Princeton University
    Inventors: Josh Munger, Bryson Bennett, Thomas Shenk, Joshua Rabinowitz
  • Patent number: 8993617
    Abstract: The present invention directed to a method of treating multiple myeloma with the following compound: or a pharmaceutically acceptable salt thereof. The compound is a novel small molecule inhibitor of Ire1.
    Type: Grant
    Filed: November 8, 2011
    Date of Patent: March 31, 2015
    Assignee: The Board of Trustees of the Leland Stanford Junior University
    Inventors: Albert C. Koong, Ioanna Papandreou
  • Publication number: 20150051233
    Abstract: Embodiments of the invention include methods of treating, preventing, and/or reducing the risk of fibrosis in an individual in need thereof. In some embodiments, particular small molecules are employed for treatment, prevention, and/or reduction of the risk of fibrosis. In at least particular cases, the small molecules are inhibitors of STAT3.
    Type: Application
    Filed: July 18, 2014
    Publication date: February 19, 2015
    Inventors: David J. Tweardy, Moses M. Kasembeli, Marvin X. Xu, Sandeep K. Agarwal, Mesias Pedroza
  • Patent number: 8946286
    Abstract: A novel organic amine salt or salt with quaternary ammonium ion of 3-{[((2E)-2-{1-[5-(4-t-butylphenyl)-4-hydroxy-3-thienyl]ethylidene}hydrazino)carbonothioyl]amino}benzoic acid having useful properties as a drug is provided. A novel organic amine or salt with quaternary ammonium ion of 3-{[((2E)-2-{1-[5-(4-t-butylphenyl)-4-hydroxy-3-thienyl]ethylidene}hydrazino)carbonothioyl]amino}benzoic acid, a method for producing the organic amine salt or the salt with quaternary ammonium ion and a platelet increasing agent.
    Type: Grant
    Filed: November 1, 2011
    Date of Patent: February 3, 2015
    Assignee: Nissan Chemical Industries, Ltd.
    Inventors: Shunsuke Iwamoto, Satoshi Nakano, Mariko Ishida, Masao Yamamoto, Kazuya Takeuchi
  • Publication number: 20150031714
    Abstract: Embodiments of the invention include methods of preventing and/or reducing the risk or severity of an allergic reaction in an individual. In some embodiments, particular small molecules are employed for prevention and/or reduction in the risk or severity of anaphylaxis. In at least particular cases, the small molecules are inhibitors of STAT3. In some cases, the small molecule comprises N-(1?,2-dihydroxy-1,2?-binaphthalen-4?-yl)-4-methoxybenzenesulfonamide.
    Type: Application
    Filed: July 18, 2014
    Publication date: January 29, 2015
    Inventors: David J. Tweardy, Moses M. Kasembeli, Marvin X. Xu, Josh Milner
  • Publication number: 20150023889
    Abstract: Disclosed are compounds, compositions, and methods relating to fluoride aptamers, fluoride-responsive riboswitches, fluoride-regulated expression constructs, fluoride transporters, nucleic acids encoding fluoride transporters, expression constructs encoding fluoride transporters, and cells containing or including any combination of these.
    Type: Application
    Filed: September 17, 2012
    Publication date: January 22, 2015
    Inventors: Ronald Breaker, Jenny Baker, Narasimhan Sudarsan, Zasha Weinberg, Adam Roth, Tyler Ames, James Nelson
  • Publication number: 20150025068
    Abstract: A compound of formula (I), useful for the treatment of cancer, inflammation and inflammatory disorders, and a pharmaceutical composition containing the compound.
    Type: Application
    Filed: December 21, 2012
    Publication date: January 22, 2015
    Inventors: Jessica Martinsson, Katarina Faernegardh, Mattias Joensson, Rune Ringom
  • Publication number: 20150024032
    Abstract: Embodiments of the invention include methods of treating, preventing, and/or reduce the risk or severity of a condition selected from the group consisting of muscle wasting, muscle weakness, cachexia, and a combination thereof in an individual in need thereof. In some embodiments, particular small molecules are employed for treatment, prevention, and/or reduction in the risk of muscle wasting. In at least particular cases, the small molecules are inhibitors of STAT3.
    Type: Application
    Filed: July 18, 2014
    Publication date: January 22, 2015
    Inventors: David J. Tweardy, Moses M. Kasembeli, Marvin X. Xu, Thomas Kristian Eckols
  • Publication number: 20150018411
    Abstract: The present invention concerns substances which act as selective ligands of nuclear receptors of the PPAR beta/delta subtype and which can be used for the treatment of PPAR beta/delta-mediated diseases. The substances of this invention act as inhibitors of PPAR beta/delta receptors.
    Type: Application
    Filed: June 6, 2012
    Publication date: January 15, 2015
    Applicant: PHILIPPS-UNIVERSITAT MARBURG
    Inventors: Wibke Diederich, Stefanie Dorr, Kerstin Kaddatz, Gerhard Klebe, Rolf Muller, Simone Naruhn, Veronika Pape, Josefine Stockert, Philipp Manuel Toth
  • Patent number: 8889732
    Abstract: Fused heterocyclic compounds useful for prevention, treatment or improvement of diseases against which activation of the thrombopoietin receptor is effective are provided. A compound represented by the formula (I) (wherein R1 is an aryl group fused to a saturated ring or the like, A, B, L1, R2, L2, L3, Y, L4, R3 and X are defined in the description), a tautomer, prodrug or a pharmaceutically acceptable salt of the compound or a solvate thereof.
    Type: Grant
    Filed: October 22, 2010
    Date of Patent: November 18, 2014
    Assignee: Nissan Chemical Industries, Ltd.
    Inventors: Yukihiro Shigeta, Shingo Umezawa, Shunsuke Iwamoto, Takanori Nakamura
  • Publication number: 20140336137
    Abstract: The invention relates to nitroso derivatives including carboxylic acid and phosphoric acid esters of hydroxy nitroso compounds that donate nitroxyl (HNO) under physiological conditions. The compounds and compositions of the invention are useful in treating and/or preventing the onset and/or development of diseases or conditions that are responsive to nitroxyl therapy, including heart failure, ischemia/reperfusion injury and cancer.
    Type: Application
    Filed: July 28, 2014
    Publication date: November 13, 2014
    Inventors: Lisa Marie Frost, Stephen Martin Courtney, Frederick Arthur Brookfield, Vincent Jacob Kalish
  • Publication number: 20140323510
    Abstract: Disclosed herein is a compound of the formula Therapeutic methods, compositions, and medicaments, related thereto are also disclosed.
    Type: Application
    Filed: May 8, 2014
    Publication date: October 30, 2014
    Applicant: Allergan, Inc.
    Inventors: Yariv Donde, Jeremiah H. Nguyen
  • Publication number: 20140275232
    Abstract: A novel small molecule antagonizes two types of acyl homoserine lactone receptors: membrane-bound and cytoplasmic. A focused library of analogs and derivatives of the original antagonist was synthesized. Analog and derivative molecules harbor a range of activities. The novel small molecule and most potent antagonist protects the eukaryote Caenorhabditis elegans from quorum-sensing-mediated killing by the bacterial pathogen Chromobacterium violaceum. The saving of C. elegans demonstrates the use of these molecules as small molecule antimicrobials.
    Type: Application
    Filed: May 28, 2014
    Publication date: September 18, 2014
    Applicant: THE TRUSTEES OF PRINCETON UNIVERSITY
    Inventors: Bonnie L. Bassler, Lee R. Swem, Scott M. Ulrich, Colleen T. O'Loughlin
  • Patent number: 8835488
    Abstract: This application describes compounds that can act as opioid receptor ligands, which compounds can be used in the treatment of, for example, pain and pain related disorders.
    Type: Grant
    Filed: March 23, 2012
    Date of Patent: September 16, 2014
    Assignee: Trevena, Inc.
    Inventors: Dennis Yamashita, Dimitar Gotchev, Philip Pitis, Xiao-Tao Chen, Guodong Liu, Catherine C. K. Yuan
  • Publication number: 20140249163
    Abstract: The present disclosure describes new inhibitors or antagonists of Ras useful for the treatment of conditions resulting from Ras-induced or mediated cellular processes, including cellular proliferation, differentiation, apoptosis, senescence, and survival. These cellular processes may be associated with a non-malignant or malignant disease, disorder, or pathological condition. The present disclosure also describes a method for inhibiting such Ras-induced or mediated cellular processes. The method entails administering a Ras antagonist in an amount effective to inhibit such cellular processes.
    Type: Application
    Filed: October 5, 2012
    Publication date: September 4, 2014
    Applicant: PICES THERAPEUTICS LLC
    Inventors: James H. Wikel, Michael J. Brownstein
  • Patent number: 8822467
    Abstract: The present invention provides biaryl oxyacetic acid compounds which may be useful for treating inflammatory disorders, including disorders affecting the respiratory system and skin.
    Type: Grant
    Filed: December 14, 2012
    Date of Patent: September 2, 2014
    Assignee: Ligand Pharmaceuticals Incorporated
    Inventors: Brian F. McGuinness, Koc-Kan Ho, Suresh Babu, Guizhen Dong, Jingqi Duo, Thuy X. H. Le, Kurt W. Saionz
  • Publication number: 20140243401
    Abstract: The invention relates to methods of screening to find compounds that are cytotoxic to tumor cells and methods of treating tumor cells using these compounds. In particular, the invention relates to methods of screening for compounds that inhibit mammalian mitochondrial fatty acid synthase (mmFAS) and methods of treating tumor cells using mmFAS inhibitors. This invention also provides methods for inhibiting or preventing cancer cell survival by the administration of mitochondrial fatty acid synthase (FAS) inhibitors. Specifically, this invention describes a method for prohibiting or delaying the development of cancer, the growth of cancer or invasion of cancer from pre-malignant (noninvasive) lesions, or metastasis of cancer based upon the findings that this method compromises energy balance in cancer cells, in turn compromising their basic functions and causing their cell death.
    Type: Application
    Filed: November 23, 2011
    Publication date: August 28, 2014
    Applicant: The Johns Hopkins University
    Inventor: Gabrielle Ronnett
  • Publication number: 20140243366
    Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.
    Type: Application
    Filed: May 1, 2014
    Publication date: August 28, 2014
    Applicant: CalciMedica, Inc.
    Inventors: Jeffrey P. WHITTEN, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey
  • Publication number: 20140235702
    Abstract: This invention is in the field of medicinal chemistry. In particular, the invention relates to a new class of small-molecules having sulfonamido-1-hydroxynaphthalene structure which function as inhibitors of Mcl-1 protein, and their use as therapeutics for the treatment of cancer and other diseases.
    Type: Application
    Filed: October 8, 2012
    Publication date: August 21, 2014
    Inventors: Zaneta Nikolovska-Coleska, Hollis D. Showalter, Chenzhong Liao, Ramzi Mohammad, Fardokht Abulwerdi
  • Publication number: 20140227173
    Abstract: Provided are methods for treating cancer in a patient, comprising administering to a patient in need thereof a therapeutically effective regimen, the regimen comprising administering a gamma-secretase inhibitor, wherein the regimen results in a reduction in the cancer cell population in the patient. In some embodiments of the methods, the therapeutically effective regimen stabilizes, reduces or eliminates the cancer stem cell population. Also provided are compounds of the formula I or a pharmaceutically acceptable salt thereof, wherein R1, R2, and X are as herein described.
    Type: Application
    Filed: February 6, 2014
    Publication date: August 14, 2014
    Applicant: The Johns Hopkins University
    Inventors: Charles Eberhart, Xing Fan, Anirban Maitra
  • Publication number: 20140221351
    Abstract: The present invention relates to novel bis-sulfonamide derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.
    Type: Application
    Filed: April 8, 2014
    Publication date: August 7, 2014
    Applicant: ALLERGAN, INC.
    Inventors: HAIQING YUAN, RICHARD L. BEARD, XIAOXIA LIU, JOHN E. DONELLO, VEENA VISWANATH, MICHAEL E. GARST
  • Patent number: 8791049
    Abstract: Provided are improved agricultural processes for the improved cultivation of rice wherein the crops are treated to control undesired vegetative growth using a plant treatment composition comprising both halosulfuron and thifensulfuron to provide improved herbicidal efficacy against Heteranthera limosa, commonly referred to as “duck salad”. Also provided are compositions useful in the improved agricultural processes, as well as herbicidal treatment regimens. Unexpectedly high rates of efficacy against Heteranthera limosa, amongst rice plant in rice crops are disclosed.
    Type: Grant
    Filed: December 13, 2010
    Date of Patent: July 29, 2014
    Assignee: Gowan Co.
    Inventors: Eric Paige Webster, Dominic Frank Alonso, Sergio Comparini, Wallace Keith Majure, Sandra Alcaraz, Charles Paul Grasso, Eric James McEwen, Tak Wai Cheung
  • Patent number: 8772331
    Abstract: A novel small molecule antagonizes two types of acyl homoserine lactone receptors: membrane-bound and cytoplasmic. A focused library of analogs and derivatives of the original antagonist was synthesized. Analog and derivative molecules harbor a range of activities. The novel small molecule and most potent antagonist protects the eukaryote Caenorhabditis elegans from quorum-sensing-mediated killing by the bacterial pathogen Chromobacterium violaceum. The saving of C. elegans demonstrates the use of these molecules as small molecule antimicrobials.
    Type: Grant
    Filed: July 17, 2012
    Date of Patent: July 8, 2014
    Assignee: The Trustees of Princeton University
    Inventors: Bonnie L. Bassler, Lee R. Swem, Scott M. Ulrich, Colleen T. O'Loughlin
  • Patent number: 8765797
    Abstract: Methods and compounds for treating cancer, dmg resistance and/or metastasis are described herein. These methods and compounds can inhibit the expression of aberrant TG2 expression and/or inhibit the binding of GTP to TG2, and thereby prevent the induction of epithelial to mesenchymal transition of cancer cells, and a stem cell-like phenotype.
    Type: Grant
    Filed: June 21, 2011
    Date of Patent: July 1, 2014
    Assignee: Board of Regents, The University of Texas System
    Inventors: Kapil Mehta, Anupam Kumar, Jansina Fok, Shuxing Zhang
  • Publication number: 20140142156
    Abstract: Compounds which modulate quorum sensing in quorum sensing bacteria. Compounds of the invention inhibit quorum sensing and/or activate quorum sensing in various bacteria. Compounds that inhibit quorum sensing are particularly useful for inhibition of detrimental bacterial biofilm formation. Compounds that activate quorum sensing are particularly useful for promoting growth and biofilm formation of beneficial bacterial.
    Type: Application
    Filed: December 12, 2013
    Publication date: May 22, 2014
    Applicant: WISCONSIN ALUMNI RESEARCH FOUNDATION
    Inventors: Helen E. BLACKWELL, Christine E. McINNIS
  • Publication number: 20140113941
    Abstract: This invention provides a compound having the structure wherein R1 is H, wherein n and q are independently an integer from 0 to 8; A is absent or present and when present is wherein m is an integer from 0 to 8; R3 is an amino, alkyl, aryl, heteroaryl, diol, piperazine, morpholine, piperidine, triazole, azide or biphenyl, each with or without substitution, branched or unbranched, or and R4 is alkyl, aryl, or heteroaryl, each with or without substitution, branched or unbranched, R2 is H, CH3, or alkyl, aryl, heteroaryl, pyrrole, diazole, or triazole, each with or without substitution, branched or unbranched, or wherein n and q are independently an integer from 0 to 8; A is absent or present and when present is and R6 is azide, methoxy, trifluoromethyl, biphenyl, substituted phenyl, substituted triazole, or alkyl, aryl or heteroaryl, with or without substitution, branched or unbranched, when R1 is H then R2 is other than H or CH3, and
    Type: Application
    Filed: March 23, 2012
    Publication date: April 24, 2014
    Applicant: The Research Foundation for The State University of New York
    Inventors: Peter Tonge, Carl Machutta, Gopal Reddy Bommineni, Kanishk Kapilashrami
  • Patent number: 8703970
    Abstract: Disclosed herein are compounds having photoremovable protecting groups which are removed after the compounds absorbs light of a given wavelength and undergo an electrocyclic reaction between a chromophore in the compound attached via an anilide to a benzothiophene ring.
    Type: Grant
    Filed: February 27, 2013
    Date of Patent: April 22, 2014
    Assignee: Marquette University
    Inventors: Mark G. Steinmetz, Majher I. Sarker, Tasnuva Shahrin
  • Publication number: 20140107123
    Abstract: The invention relates to the treatment and prevention of type I diabetes. More specifically, the invention relates to compounds that treat or prevent the body's immune system from destroying ?-cells (i.e., insulin-producing cells in the pancreatic islets of Langerhans) by inhibition of JNK2, selective inhibition of JNK2, or inhibition of the expression of the MAPK9 gene or gene product. In one embodiment, the present invention contemplates the diagnosis, identification, production, and use of compounds which modulate MAPK9 gene expression or the activity of the MAPK9 gene product including but not limited to, JNK2, the nucleic acid encoding MAPK9 and homologues, analogues, and deletions thereof, as well as antisense, ribozyme, triple helix, antibody, and polypeptide molecules as well as small inorganic molecules. The present invention contemplates a variety of pharmaceutical formulations and routes of administration for such compounds.
    Type: Application
    Filed: August 5, 2013
    Publication date: April 17, 2014
    Applicant: University of Massachusetts
    Inventors: Roger J. Davis, Anja Jaeschke
  • Publication number: 20140107160
    Abstract: The invention relates to compounds represented by Structural Formula I, which can bind to CCR9 receptors and block the binding of a ligand (e.g., TECK) to the receptors. The invention also relates to a method of inhibiting a function of CCR9, and to the use compounds represented by Structural Formula I in research, therapeutic, prophylactic and diagnostic methods.
    Type: Application
    Filed: October 9, 2013
    Publication date: April 17, 2014
    Applicant: Millennium Pharmaceuticals, Inc.
    Inventors: Paul E. Fleming, Geraldine C.B. Harriman, Zhan Shi, B. Shaowu Chen
  • Publication number: 20140088158
    Abstract: The present invention relates to compounds of the formula I, wherein A, Y, Z, R20 to R22 and R50 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. Specifically, they are inhibitors of the endothelial differentiation gene receptor 2 (Edg-2, EDG2), which is activated by lysophosphatidic acid (LPA) and is also termed as LPA1 receptor, and are useful for the treatment of diseases such as atherosclerosis, myocardial infarction and heart failure, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.
    Type: Application
    Filed: November 27, 2013
    Publication date: March 27, 2014
    Applicant: SANOFI
    Inventors: Josef PERNERSTORFER, Heinz-Werner KLEEMANN, Matthias SCHAEFER, Alena SAFAROVA, Marcel PATEK
  • Patent number: 8680139
    Abstract: Disclosed are novel compounds which are useful as therapeutics, especially in anti-neoplastic therapy and in other therapeutic regimes where cysteine protease inhibition is implicated.
    Type: Grant
    Filed: March 31, 2010
    Date of Patent: March 25, 2014
    Assignee: Progenra
    Inventors: Ping Cao, Joseph Weinstock, William D. Kingsbury, Craig A. Leach, Suresh Kumar Kizhakkethil-George, Benjamin Nicholson
  • Patent number: 8680137
    Abstract: This invention relates to methods of screening for modulators of mammalian cell injury cause by TRPM7 gene and protein activity, compounds that modulate TRPM7 gene and protein activity and methods of treatment of mammalian cell injury using modulators of TRPM7 gene and protein activity.
    Type: Grant
    Filed: December 13, 2010
    Date of Patent: March 25, 2014
    Assignee: Nono Inc.
    Inventors: Xiujun Sun, Michael Tymianski, Jonathan David Garman
  • Patent number: 8680135
    Abstract: The present invention relates generally to substituted benzofurans, benzothiophenes, and indoles and their use as tubulin polymerization inhibitors.
    Type: Grant
    Filed: October 22, 2012
    Date of Patent: March 25, 2014
    Assignee: Bionomics Limited
    Inventors: Jason Hugh Chaplin, Gurmit Singh Gill, Damian Wojciech Grobelny, Bernard Luke Flynn, Gabriel Kremmidiotis
  • Patent number: 8673910
    Abstract: The subject invention concerns compounds having activity as inhibitors of proteasomes and methods of using the subject compounds. In one embodiment, a compound of the invention has the chemical structure shown in formula I: or a pharmaceutically acceptable salt or hydrate thereof. In another embodiment, a compound of the invention has the chemical structure shown in formula II: or a pharmaceutically acceptable salt or hydrate thereof.
    Type: Grant
    Filed: June 30, 2009
    Date of Patent: March 18, 2014
    Assignees: H. Lee Moffitt Cancer Center and Research Institute, University of South Florida
    Inventors: Harshani Lawrence, Yiyu Ge, Said M. Sebti, Wayne Guida
  • Publication number: 20140073611
    Abstract: The disclosure relates to a platform of using zebrafish in screening candidates for treating and/or preventing myopia and keratoconus disease. The disclosure is mainly based on that Lumican, one of several SLRPs, plays an important role in the regulation of fibrillogenesis or the genes affecting the size of eyeballs in zebrafish, in addition to playing an important role in clinical myopia. Therefore, the disclosure uses the established zebrafish model to further identify the drugs affecting the expression of lumican and collagen fibrillogenesis, and/or the regulation of eyeball size. These drugs are potential candidates for treating myopia and/or keratoconus disease.
    Type: Application
    Filed: May 21, 2013
    Publication date: March 13, 2014
    Applicant: National Taiwan University
    Inventors: I-Jong Wang, Wei-Ting Ho, Ting-Hsuan Chiang, I-Tsen Lin
  • Publication number: 20140057953
    Abstract: The invention relates to selective, non-steroidal 17beta-hydroxysteroid dehydrogenase type 2 (l7beta-HSD2) inhibitors of formula (I), their production and use, notably for the treatment and prophylaxis of sex steroid deficient diseases like osteoporosis in men and women.
    Type: Application
    Filed: March 2, 2012
    Publication date: February 27, 2014
    Inventors: Rolf Hartmann, Sandrine Marchais-Oberwinkler, Kuiying Xu, Ruth Werth
  • Patent number: RE45314
    Abstract: The invention relates to N-hydroxysulfonamide derivatives that donate nitroxyl (HNO) under physiological conditions and are useful in treating and/or preventing the onset and/or development of diseases or conditions that are responsive to nitroxyl therapy, including heart failure and ischemia/reperfusion injury. Novel N-hydroxysulfonamide derivatives release NHO at a controlled rate under physiological conditions, and the rate of HNO release is modulated by varying the nature and location of functional groups on the N-hydroxysulfonamide derivatives.
    Type: Grant
    Filed: October 3, 2013
    Date of Patent: December 30, 2014
    Assignees: The Johns Hopkins University, Cardioxyl Pharmaceuticals, Inc.
    Inventors: John P. Toscano, Frederick Arthur Brookfield, Andrew D. Cohen, Stephen Martin Courtney, Lisa Marie Frost, Vincent Jacob Kalish