1,3,4-thiadiazoles (including Hydrogenated) Patents (Class 514/363)
  • Patent number: 10813916
    Abstract: The present invention relates to an immediate release solid oral pharmaceutical composition comprising an effective amount of Tizanidine or its pharmaceutically acceptable salts, esters, solvates, polymorphs, stereoisomers or mixtures thereof. The solid oral dosage form comprises one or more methacrylic acid copolymers or its derivatives and is bioequivalent to the commercially available counterpart (ZANAFLEX® capsule) after oral administration. The invention also relates to a process for preparation of a pharmaceutical capsule dosage form comprising an effective amount of Tizanidine Hydrochloride wherein, the dosage form comprises methacrylic acid copolymer or its derivatives.
    Type: Grant
    Filed: May 27, 2016
    Date of Patent: October 27, 2020
    Assignee: Jubilant Generics Limited
    Inventors: Pankaj Soni, Rashmi Ranjan Panda, Ganesh Vinayak Gat, Dinesh Kumar, Kamal S. Mehta, Ravikumar Nithiyanandam
  • Patent number: 10722498
    Abstract: The present invention provides a stable, ophthalmic aqueous composition for topical administration comprising acetazolamide and an aqueous liquid capable of forming a pharmaceutically acceptable gel in situ when applied topically to a patient, said composition has the pH of less than 4.5.
    Type: Grant
    Filed: January 22, 2018
    Date of Patent: July 28, 2020
    Assignee: SHILPA MEDICARE LIMITED
    Inventors: Andanayya Saraganachari, Abhilash Narayanaswamy, Sreenivasa Reddy, Shivakumar Pradeep
  • Patent number: 10532034
    Abstract: The present invention relates to a method of reducing the production of glutamate from glutamine by glutaminase C in a cell or tissue. The method involves inhibiting glutaminase C activity in the cell or tissue under conditions effective to reduce production of glutamate from glutamine. Compounds for carrying out this method are also disclosed and include those of formula (III): wherein B, R1c, R2c, m, and n are defined herein.
    Type: Grant
    Filed: March 25, 2010
    Date of Patent: January 14, 2020
    Assignee: Cornell University
    Inventors: Richard A. Cerione, Jon W. Erickson, Kristin Wilson Cerione, Jianbin Wang
  • Patent number: 10011574
    Abstract: Compounds and compositions comprising compounds that inhibit glutaminase are described herein. Also described herein are methods of using the compounds that inhibit glutaminase in the treatment of cancer.
    Type: Grant
    Filed: November 21, 2013
    Date of Patent: July 3, 2018
    Assignee: Agios Pharmaceuticals, Inc.
    Inventors: Rene M. Lemieux, Janeta Popovici-Muller, Francesco G. Salituro, Jeffrey O. Saunders, Jeremy Travins, Shunqi Yan
  • Patent number: 9801813
    Abstract: The present invention relates to a process for manufacturing an ophthalmic formulation of a carbonic anhydrase inhibitor, hydroxyl ethyl cellulose (HEC), and a beta-adrenergic antagonist for use in the treatment of ocular hypertension and glaucoma wherein the ophthalmic pharmaceutical formulation is devoid of benzalkonium chloride or any other preservatives. The present process for manufacturing is simpler, cost effective process to prepare the pharmaceutical ophthalmic formulation in a single tank, without the use of additional tanks that can be sterile filtered.
    Type: Grant
    Filed: October 13, 2014
    Date of Patent: October 31, 2017
    Assignee: Sentiss Pharma Private Limited
    Inventors: Mandar V. Shah, Deepak Bahri, Manish Kumar Singh
  • Patent number: 9505736
    Abstract: Provided are certain histone deacetylase (HDAC) inhibitors of Formula I, compositions thereof, and methods of their use.
    Type: Grant
    Filed: July 16, 2013
    Date of Patent: November 29, 2016
    Assignee: CHDI Foundation, Inc.
    Inventors: Celia Dominguez, Perla Breccia, Christopher A. Luckhurst, Roland W. Bürli, Andrew J. Stott
  • Patent number: 9457016
    Abstract: Methods for treating autosomal dominant polycystic kidney disease (ADPKD) are described herein. More particularly, methods described herein relate generally to administering glutaminase1 inhibitors to subjects afflicted with ADPKD. Accordingly, the use and application of compounds or agents that inhibit glutaminase1 for treating ADPKD or for use in a medicament for treating ADPKD are encompassed herein.
    Type: Grant
    Filed: August 29, 2014
    Date of Patent: October 4, 2016
    Assignee: New York University
    Inventors: Edward Skolnik, Zhai Li
  • Patent number: 9320734
    Abstract: Pleckstrin homology domain binding compounds, pharmaceutical compositions including such compounds, and methods for their use are described herein.
    Type: Grant
    Filed: January 5, 2015
    Date of Patent: April 26, 2016
    Assignees: Board of Regents, The University of Texas System, Arizona Board of Regents on behalf of the University of Arizona
    Inventors: Daruka Mahadevan, Emmanuelle J. Meuillet, Eugene A. Mash, Jr., Vijay M. Gokhale, Garth Powis, Shuxing Zhang
  • Patent number: 9278962
    Abstract: Provided are compounds of Formula I: or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, R7, X, Z1, Z2, Z3, Z4 and m are as defined herein. Also provided is a pharmaceutically acceptable composition comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof. Also provided are methods of using a compound of Formula I, or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: May 6, 2014
    Date of Patent: March 8, 2016
    Assignee: Cytokinetics, Inc.
    Inventors: Luke W. Ashcraft, Gustave Bergnes, Chihyuan Chuang, Scott Collibee, Pu-Ping Lu, Bradley Morgan, Alex Muci, Xiangping Qian, Jeffrey Warrington, Zhe Yang
  • Patent number: 9221841
    Abstract: This invention relates to inhibitors of mitotic kinesins, particularly KSP, and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing the inhibitors and pharmaceutical compositions in the treatment and prevention of various disorders.
    Type: Grant
    Filed: March 19, 2015
    Date of Patent: December 29, 2015
    Assignee: Array BioPharma Inc.
    Inventors: Jeremy Hans, Eli M. Wallace, Qian Zhao, Shelley Allen, Ellen Laird, Joseph P. Lyssikatos, John E. Robinson, Christopher P. Corrette, Robert Kirk DeLisle, Walter C. Voegtli
  • Patent number: 9180118
    Abstract: The present invention relates to compounds of the formulae herein, their acceptable salts, solvates, hydrates and polymorphs thereof. The compounds of this invention are useful in treatment of disease, particularly leukemia. The invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating disease, disorders, or symptoms thereof in a subject.
    Type: Grant
    Filed: July 18, 2007
    Date of Patent: November 10, 2015
    Assignee: University of Rochester
    Inventors: Craig Jordan, Monica Guzman
  • Patent number: 9108960
    Abstract: The present invention provides nitrofurfuryl substituted phenyl linked piperidino-oxadiazolone compounds of general formula (A) as anti-tubercular agents; wherein G=formula (B); X?H, F; R?H, CH3, C2H5, Benzyl.
    Type: Grant
    Filed: December 18, 2012
    Date of Patent: August 18, 2015
    Assignee: Council of Scientific & Industrial Research
    Inventors: Ahmed Kamal, Arutla Viswanath, Jayanti Naga Srirama Chandra Murty, Farheen Sulthana, Gadupudi Ramakrishna, Inshad Ali Khan, Nitin Pal Kalia
  • Patent number: 9102639
    Abstract: This invention relates to inhibitors of mitotic kinesins, particularly KSP, and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing the inhibitors and pharmaceutical compositions in the treatment and prevention of various disorders.
    Type: Grant
    Filed: December 6, 2013
    Date of Patent: August 11, 2015
    Assignee: Array BioPharma Inc.
    Inventors: Jeremy Hans, Eli M. Wallace, Qian Zhao, Joseph P. Lyssikatos, Thomas D. Aicher, Ellen R. Laird, John Robinson, Shelley Allen
  • Publication number: 20150133446
    Abstract: The present invention provides imidazothiadiazole compounds of Formula (I) wherein A, B, D, Rx, R1, R2, R3, X1, X2 and s are as defined herein, or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein all of the variables are as defined herein. These compounds are inhibitors of platelet aggregation and thus can be used as medicaments.
    Type: Application
    Filed: April 24, 2013
    Publication date: May 14, 2015
    Inventors: R. Michael Lawrence, Michael M. Miller, Dietmar Alfred Seiffert, Shoshana L. Posy, Pancras C. Wong, Jacques Banville, Edward H. Ruediger, Daniel H. Deon, Alain Martel, François Tremblay, Julia Guy, Jean-François Lavallée, Marc Gagnon
  • Patent number: 9028878
    Abstract: Compositions and methods, including novel homogeneous microparticulate suspensions, are described for treating natural surfaces that contain bacterial biofilm, including unexpected synergy or enhancing effects between bismuth-thiol (BT) compounds and certain antibiotics, to provide formulations including antiseptic formulations. Previously unpredicted antibacterial properties and anti-biofilm properties of disclosed BT compounds and BT compound-plus-antibiotic combinations are also described, including preferential efficacies of certain such compositions for treating certain gram-positive bacterial infections, and distinct preferential efficacies of certain such compositions for treating certain gram-negative bacterial infections.
    Type: Grant
    Filed: August 3, 2012
    Date of Patent: May 12, 2015
    Assignee: Microbion Corporation
    Inventor: Brett Hugh James Baker
  • Publication number: 20150126563
    Abstract: Pleckstrin homology domain binding compounds, pharmaceutical compositions including such compounds, and methods for their use are described herein.
    Type: Application
    Filed: January 5, 2015
    Publication date: May 7, 2015
    Applicants: BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM, Arizona Board of Regents on Behalf of the University of Arizona
    Inventors: Daruka MAHADEVAN, Emmanuelle J. MEUILLET, Eugene A. MASH, JR., Vijay M. GOKHALE, Garth POWIS, Shuxing ZHANG
  • 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: 20150119390
    Abstract: The present invention provides imidazothiadiazole compounds of Formula (I); Wherein W, Y, R0, R2, R4, Ra, Rb, X1, X2, X3 and X4 are as defined herein, or a stereoisomer, tautomer, pharmaceutically acceptable salt, prodrug ester or solvate form thereof, wherein all of the variables are as defined herein. These compounds are inhibitors of platelet aggregation and thus can be used as medicaments for treating or preventing thromboembolic disorders.
    Type: Application
    Filed: April 24, 2013
    Publication date: April 30, 2015
    Inventors: Alain Martel, François Tremblay, Anne Marinier, Eldon Scott Priestley, Shoshana L. Posy, R. Michael Lawrence, Michael M. Miller
  • Patent number: 9006454
    Abstract: The invention relates to compounds of formula (I) wherein R1, R2, X1, X2, Y, Ra, Rb, Q have the meanings given in claim 1. The compounds are useful e.g. in the treatment of autoimmune disorders, such as multiple sclerosis and also in the treatment of cancer disorders.
    Type: Grant
    Filed: March 26, 2010
    Date of Patent: April 14, 2015
    Assignee: Merck Serono S.A.
    Inventors: Siva Sanjeeva Rao Thunuguntla, Hosahalli Subramanya, Satish Reddy Kunnam, Sekhar Reddy Sanivaru Vijay, Chakrapani Bingi, Raviraj Kusanur, Matthias Schwarz, Michael Arlt
  • Publication number: 20150094297
    Abstract: The present invention provides thiazole compounds of Formula I wherein W, Y, R0, R2, R4, R5, R6, R7, X1, X2, X3 and X4 are as defined herein, or a stereoisomer, tautomer, pharmaceutically acceptable salt, prodrug ester or solvate form thereof, wherein all of the variables are as defined herein. These compounds are inhibitors of platelet aggregation and thus can be used as medicaments for treating or preventing thromboembolic disorders.
    Type: Application
    Filed: April 24, 2013
    Publication date: April 2, 2015
    Inventors: Jacques Banville, Roger Rèmillard, Edward H. Ruediger, Daniel H. Deon, Marc Gagnon, Laurence Dubé, Julia Guy, Eldon Scott Priestley, Shoshana L. Posy, Brad D. Maxwell, Pancras C. Wong, R. Michael Lawrence, Michael M. Miller
  • Patent number: 8993619
    Abstract: The invention relates to compounds of formula (I): useful for treating disorders mediated by acyl coA-diacylglycerol acyl transferase 1 (DGAT1), e.g. metabolic disorders. The invention also provides methods of treating such disorders, and compounds and compositions etc. for their treatment.
    Type: Grant
    Filed: April 26, 2013
    Date of Patent: March 31, 2015
    Assignee: Novartis AG
    Inventors: Sejal Patel, Justin Mao, Qian Liu, Rui Zheng, Tyler Harrison, Rohit Duvadie, Xin Chen, Frederic Zecri, Jay Larrow, Xuchun Zheng, Yizong Zhou, Jiong Ye, Yiping Ding, Yu Gai
  • Publication number: 20150087646
    Abstract: The present disclosure is directed to compounds of formula (I), and pharmaceutically acceptable salts thereof, as mPGES-1 inhibitors. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and are therefore useful in the treatment of pain and/or inflammation from a variety of diseases or conditions, such as asthma, osteoarthritis, rheumatoid arthritis, acute or chronic pain and neurodegenerative diseases.
    Type: Application
    Filed: June 10, 2013
    Publication date: March 26, 2015
    Applicant: GLENMARK PHARMACEUTICALS S.A.
    Inventors: Laxmikant Atmaram Gharat, Nagarajan Muthukaman, Neelima Khairatkar-Joshi, Vidya Ganapati Kattige
  • Patent number: 8980892
    Abstract: A compound of formula (I): wherein A1, A2, A3, A4, G1, R1, R2, R3, R4, R5a, R5b and R6 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising the compounds of formula (I) and to methods of using the compounds of formula (I) to control insect, acarine, nematode and mollusc pests.
    Type: Grant
    Filed: February 18, 2010
    Date of Patent: March 17, 2015
    Assignees: Syngenta Crop Protection LLC, Syngenta Limited
    Inventors: Peter Renold, Thomas Pitterna, Jerome Yves Cassayre, Myriem El Qacemi
  • Patent number: 8980920
    Abstract: The present invention relates to novel Linked Tricyclic Aryl Compounds, compositions comprising at least one Linked Tricyclic Compound, and methods of using Linked Tricyclic Aryl Compounds for treating or preventing HCV infection in a patient. in one aspect, the present invention provides Compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein: Non-limiting examples of the Compounds of Formula (II) include compound 56.
    Type: Grant
    Filed: May 28, 2010
    Date of Patent: March 17, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Qingbei Zeng, Kevin X. Chen, Anilkumar Gopinadhan Nair, Stuart B. Rosenblum, Joseph A. Kozlowski, F. George Njoroge
  • Publication number: 20150065486
    Abstract: Methods for treating autosomal dominant polycystic kidney disease (ADPKD) are described herein. More particularly, methods described herein relate generally to administering glutaminase1 inhibitors to subjects afflicted with ADPKD. Accordingly, the use and application of compounds or agents that inhibit glutaminase1 for treating ADPKD or for use in a medicament for treating ADPKD are encompassed herein.
    Type: Application
    Filed: August 29, 2014
    Publication date: March 5, 2015
    Inventors: Edward Skolnik, Zhai Li
  • Patent number: 8962663
    Abstract: Pleckstrin homology domain binding compounds, pharmaceutical compositions including such compounds, and methods for their use are described herein.
    Type: Grant
    Filed: March 7, 2013
    Date of Patent: February 24, 2015
    Assignees: Board of Regents, The University of Texas System, Arizona Board of Regents on Behalf of the University of Arizona
    Inventors: Daruka Mahadevan, Emmanuelle J. Meuillet, Eugene A. Mash, Jr., Vijay M. Gokhale, Garth Powis, Shuxing Zhang
  • Publication number: 20150051193
    Abstract: Compounds and methods are provided for the treatment of pathogen infections. In some embodiments, the anti-infective compounds have broad spectrum activity against a variety of infective diseases, where the diseases are caused by pathogens containing a basic amino acid PIP-2 pincer (BAAPP) domain that interacts with phosphatidylinositol 4,5-bisphosphate (PIP-2) to mediate pathogen replication. Also provided are methods of inhibiting a PI4-kinase and methods of inhibiting viral infection. In some embodiments, the compound is a PI4-kinase inhibiting compound that is a 5-aryl-thiazole. The subject compounds may be formulated or provided to a subject in combination with a second anti-infective agent, e.g. interferon, ribivarin, and the like.
    Type: Application
    Filed: October 5, 2012
    Publication date: February 19, 2015
    Inventors: Jeffrey S. Glenn, Michael A. Gelman, Brandon Tavshanjian, Kevan Shokat, Ingrid Choong
  • Patent number: 8957060
    Abstract: Disclosed herein are solutions and kits for tumescent antibiotic delivery. Embodiments of the solution comprise an antibiotic component, an anesthetic component and a vasoconstrictor component. In addition, a method of use is disclosed comprising subcutaneous delivery of the solution. The disclosed solution, kit and method of subcutaneous delivery can be used for a variety of surgical procedures including liposuction, mastectomy and others. The tumescent antibiotic solution can be administered to a patient in situations where establishing IV access is difficult, impossible, or undesirable. A variety of delivery methods appropriate for surgical settings, as well as for use by first responders are likewise disclosed.
    Type: Grant
    Filed: May 30, 2012
    Date of Patent: February 17, 2015
    Inventor: Jeffrey Alan Klein
  • Publication number: 20150045399
    Abstract: Described herein are liver X receptor (LXR) modulators and methods of utilizing LXR modulators in the treatment of dermal diseases, disorders or conditions. Also described herein are pharmaceutical compositions containing such compounds.
    Type: Application
    Filed: September 2, 2014
    Publication date: February 12, 2015
    Applicant: Alexar Therapeutics, Inc.
    Inventor: Raju Mohan
  • Publication number: 20150038416
    Abstract: The invention relates to compounds that modulate the glucagon-like peptide 1 (GLP-1) receptor, methods of their synthesis, and methods of their therapeutic and/or prophylactic use. Such compounds are act as modulators or potentiators of GLP-1 receptor on their own, or with receptor ligands including GLP-1 peptides GLP-1(7-36) and GLP-1(9-36), or with peptide-based therapies, such as exenatide and liraglutide, and have the following general structure (where “” represents either or both the R and S form of the compound): where A, B, C, Y1, Y2, Z, R1, R2, R3, R4, R5, W1, n, p and q are as defined herein.
    Type: Application
    Filed: June 5, 2014
    Publication date: February 5, 2015
    Inventors: Marcus F. Boehm, Esther Martinborough, Manisha Moorjani, Junko Tamiya, Liming Huang, Adam R. Yeager, Enugurthi Brahmachary, Thomas Fowler, Andrew Novak, Premji Meghani, Michael Knaggs
  • Publication number: 20150025094
    Abstract: The present invention is directed to compounds such as: formula wherein linker is independently selected from the group consisting of —S—, —S—S—, —S—(CH2)n—, —NH—, —NH—(CH2)n—, —O—, —S02-, arylene, heteroarylene; R1 is selected from the group consisting of straight or branched C4-C20 alkyl, straight or branched C4-C20 alkenyl, straight or branched C4-C20 alkynyl, each optionally interrupted with at least one NH, C5-C7 saturated cycloalkyl or heteroalkyl ring, C5-C12 aromatic or heteroaromatic ring, each optionally substituted with at least one group selected from —COOH, —NH2, C1-C8 alkoxy, C1-C5 amidyle, C1-C5 carboxyl, halogen; and R2 is independently selected from the group consisting of H, OH, SH, NH2, NO2, halogen, CN, C1-C8 alkoxy, C1-C5 carboxylic acid, straight or branched C1-C8 alkyl, straight or branched C2-C10 alkenyl, straight or branched C2-C12 alkynyl each optionally substituted by at least one substituent selected from the group consisting of C1-C5 alkoxy, C1-C5 carboxylic acid, OH, SH, NH2, hal
    Type: Application
    Filed: August 1, 2012
    Publication date: January 22, 2015
    Applicants: YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEM LTD., DIAB R&d 1, BAR-IIan University
    Inventors: Shlomo Sasson, Erol Cerasi, Arie Lev Gruzman, Ella Meltzer-Mats
  • Publication number: 20150018330
    Abstract: The invention provides novel antimicrobial chemical entities based on a nitrothiazolide backbone that exhibit antibacterial and antiparasitic action against a wide range of human pathogens. The new classes of compounds show extended action against Gram positive bacteria including MRSA drug resistant pathogens. In the Gram-positive organisms, they specifically target and functionally inhibit microbial attachment to surfaces and biofilm formation. In Gram-negative bacteria, including enteroaggregative E. coli strains, these compounds function as pilicides by inhibiting the assembly of pilin subunits into adhesive filaments. Several of these compounds show potent antimicrobial action against Gram positive bacteria, perhaps involving novel targets. Many of the benzothiophene derivatives exhibit antimicrobial activity in the low micrograms per ml range and in blocking biofilm formation in the nanomolar range; ranges considered are well within the range of utility as therapeutics.
    Type: Application
    Filed: July 30, 2014
    Publication date: January 15, 2015
    Applicant: UNIVERSITY OF VIRGINIA PATENT FOUNDATION
    Inventors: Paul S. Hoffman, Richard L. Guerrant, Timothy L. MacDonald, Thomas Eric Ballard, JR.
  • Patent number: 8933107
    Abstract: The present invention relates to aryloxy substituted phenylamidine derivatives of formula (I) wherein the substituents are as in the description, their process of preparation, their use as fungicide or insecticide active agents, particularly in the form of fungicide or insecticide compositions, and methods for the control of phytopathogenic fungi or damaging insects, notably of plants, using these compounds or compositions (I).
    Type: Grant
    Filed: September 12, 2006
    Date of Patent: January 13, 2015
    Assignee: Bayer Cropscience AG
    Inventors: Klaus Kunz, Jörg Greul, Oliver Guth, Benoît Hartmann, Kerstin Ilg, Wahed Ahmed Moradi, Thomas Seitz, Peter Dahmen, Arnd Voerste, Ulrike Wachendorff-Neumann, Ralf Dunkel, Ronald Ebbert, Eva-Maria Franken, Olga Malsam
  • Publication number: 20150004134
    Abstract: The invention relates to novel heterocyclic compounds and pharmaceutical preparations thereof. The invention further relates to methods of treating or preventing cancer using the novel heterocyclic compounds of the invention.
    Type: Application
    Filed: December 3, 2013
    Publication date: January 1, 2015
    Applicant: CALITHERA BIOSCIENCES, INC.
    Inventors: Mark K. Bennett, Matthew I. Gross, Susan D. Bromley, Jim Li, Lijing Chen, Bindu Goyal, Guy Laidig, Timothy Friend Stanton, Eric Brian Sjogren
  • Publication number: 20140378445
    Abstract: Disclosed are methods for treating Vascular Leak Syndrome. Further disclosed are methods for treating vascular leakage due to inflammatory diseases, inter alia, sepsis, lupus, inflammatory bowel disease. Yet further disclosed are methods for treating renal cell carcinoma and melanoma. Still further disclosed are methods for reducing metastasis of malignant cells and/or preventing the proliferation of carcinoma cells via spreading due to vascular leakage.
    Type: Application
    Filed: December 21, 2012
    Publication date: December 25, 2014
    Inventors: Robert Shalwitz, Kevin G. Peters
  • Publication number: 20140369961
    Abstract: The invention relates to novel heterocyclic compounds and pharmaceutical preparations thereof. The invention further relates to methods of treatment using the novel heterocyclic compounds of the invention.
    Type: Application
    Filed: August 28, 2014
    Publication date: December 18, 2014
    Inventors: Jim Li, Lijing Chen, Bindu Goyal, Guy Laidig, Timothy F. Stanton, Eric B. Sjogren
  • Publication number: 20140350026
    Abstract: The present invention provides an anti-Coxsackie virus oxadiazole compound as represented by formula (I), or the pharmaceutically acceptable salt thereof, a preparation method, a pharmaceutical composition, and use thereof, wherein R is CH3 or CF3; R? and R? are respectively H, alkyl or halogen; A is O or S; n is a number from 1 to 6; X is O, S or NH; Y is alkyl, unsubstituted cycloalkyl, mono-substituted cycloalkyl, disubstituted cycloalkyl, poly-substituted cycloalkyl, unsubstituted aryl, mono-substituted aryl, disubstituted aryl, poly-substituted aryl, unsubstituted 5-6 membered heterocyclyl, mono-substituted 5-6 membered heterocyclyl, disubstituted 5-6 membered heterocyclyl, or poly-substituted 5-6 membered heterocyclyl. Compared to prior art, the oxadiazole compound of the present invention has excellent anti-Coxsackie virus activity, lower toxicity and high safety.
    Type: Application
    Filed: November 9, 2012
    Publication date: November 27, 2014
    Inventors: Xianjin Luo, Weidong Ye
  • Patent number: 8895535
    Abstract: Compounds of the formula I in which R1, R2, R3 and R4 have the meanings indicated in Claim 1, are inhibitors of methionine aminopeptidase and can be employed for the treatment of tumors.
    Type: Grant
    Filed: September 14, 2011
    Date of Patent: November 25, 2014
    Assignee: Merck Patent GmbH
    Inventors: Timo Heinrich, Frank Zenke, Michel Calderini, Djordje Musil
  • Publication number: 20140341850
    Abstract: A new class of haloalkyl heteroaryl benzamides is described. These compounds show strong activity against hepatitis viruses.
    Type: Application
    Filed: August 5, 2014
    Publication date: November 20, 2014
    Applicant: Romark Laboratories, L.C.
    Inventors: Jean-Francois Rossignol, J. Edward Semple
  • Publication number: 20140343077
    Abstract: A compound of formula (I) useful for the treatment or prevention of hepatitis C viral infection, (Formula (I)) wherein: X1 and X2 are each independently CRB or N; RB is H, (C1-6)alkyl, (C1-6)haloalkyl, halo.
    Type: Application
    Filed: August 22, 2012
    Publication date: November 20, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Christian Brochu, Chantal Grand-Maitre, Lee Fader, Cyrille Kuhn, Megan Bertrand-Laperle, Marc Pesant
  • Publication number: 20140329777
    Abstract: Methods to treat infectious diseases are disclosed herein. Some embodiments of the invention include administration of one or more COX inhibitors (e.g., COX-1 or COX-2 inhibitors) to treat infectious diseases. Other embodiments of the invention include administration of one or more COX inhibitors (e.g., COX-1 or COX-2 inhibitors) and administration of one or more antibiotics to treat infectious diseases.
    Type: Application
    Filed: April 22, 2014
    Publication date: November 6, 2014
    Inventors: Lisa Ann Morici, Saja Asakrah
  • Publication number: 20140315933
    Abstract: The present invention relates to new sulfonamide URAT-1 inhibitor compounds of formula (I) or pharmaceutically acceptable salts thereof: to compositions containing them, to processes for their preparation and to intermediates used in such processes and to methods of treatment; wherein R1, R2, R3, R4, R5 and R6 are as defined in the description.
    Type: Application
    Filed: April 17, 2014
    Publication date: October 23, 2014
    Applicant: PFIZER LIMITED
    Inventors: Robert McKenzie Owen, Robert Ian Storer
  • Patent number: 8865744
    Abstract: Disclosed are (cyano-dimethyl-methyl)-isoxazoles and -[1,3,4]thiadiazoles and their use as CB2 cannabinoid receptor agonists, pharmaceutical compositions containing the same, and their use for the treatment of CB2 receptor mediated disorders or conditions.
    Type: Grant
    Filed: May 15, 2014
    Date of Patent: October 21, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Doris Riether, Florian Paul Christian Binder, Henri Doods, Stephan Georg Mueller, Janet Rachel Nicholson, Achim Sauer
  • Patent number: 8865704
    Abstract: The present invention relates to known and novel compounds of formula (I) as herein described and pharmaceutical compositions thereof. The compounds of formula (I) have inhibitory effect on the Wnt pathway and are therefore useful in the preparation of a medicament, in particular for the treatment of cancer.
    Type: Grant
    Filed: October 6, 2010
    Date of Patent: October 21, 2014
    Assignee: Siena Biotech S.p.A.
    Inventors: Maurizio Varrone, Arianna Nencini, Joanna Margaret Quinn, Andrea Caricasole, Annette Cornelia Bakker, Giovanni Gaviraghi, Massimilano Salerno
  • Publication number: 20140309185
    Abstract: This document relates to inhibitors of G protein coupled receptor 6 kinase (GRK6) polypeptides as well as methods and materials for using such inhibitors to treat hematological malignancies, inflammation diseases, and autoimmune disorders.
    Type: Application
    Filed: October 26, 2012
    Publication date: October 16, 2014
    Inventors: Alexander Keith Stewart, Artem Plekhov, Robert Greenhouse
  • Patent number: 8859596
    Abstract: Disclosed herein are cannabinoid receptor ligands of formula (I) wherein A1, A5, Rx, X4, and z are as defined in the specification. Compositions comprising such compounds, and methods for treating conditions and disorders using such compounds and compositions are also disclosed.
    Type: Grant
    Filed: September 16, 2009
    Date of Patent: October 14, 2014
    Assignee: AbbVie Inc.
    Inventors: William A. Carroll, Michael J. Dart, Jennifer M. Frost, Steven P. Latshaw, Teodozyj Kolasa, Tongmei Li, Sridhar Peddi, Bo Liu, Arturo Perez-Medrano, Meena Patel, Xueqing Wang, Derek W. Nelson
  • Publication number: 20140301975
    Abstract: Methods of treating blood disorders are described.
    Type: Application
    Filed: June 20, 2014
    Publication date: October 9, 2014
    Inventor: Susan P. Perrine
  • Publication number: 20140296245
    Abstract: This invention is directed to benzensulfonamide compounds, as stereoisomers, enantiomers, tautomers thereof or mixtures thereof; or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the treatment of sodium channel-mediated diseases or conditions, such as pain.
    Type: Application
    Filed: October 30, 2012
    Publication date: October 2, 2014
    Inventors: Shaoyi Sun, Alla Yurevna Zenova, Mikhail Chafeev, Qi Jia, Zaihui Zhang, Renata Marcella Oballa
  • Patent number: 8846727
    Abstract: A new class of haloalkyl heteroaryl benzamides is described. These compounds show strong activity against hepatitis viruses.
    Type: Grant
    Filed: May 11, 2010
    Date of Patent: September 30, 2014
    Assignee: Romark Laboratories, L.C.
    Inventors: Jean-Francois Rossignol, J. Edward Semple
  • Publication number: 20140288133
    Abstract: A compound of Formula (I) or a pharmaceutically acceptable salt thereof: Wherein: Het is a 5 to 10-membered heteroaromatic ring; Either X is N and Y is CR5; or X is C and Y is S; Z is selected from N and CH; R1 is selected from H and C1-2alkyl; R2 is selected from H, C1-2alkyl, OH, —CH2OH and C1-2alkoxy; Each R3 is independently selected from OH, C1-3alkyl, F, Cl, Br, NH2, and C1-3alkoxy; R4 is selected from C1-3alkyl and haloC1-3 alkyl; R5 is selected from H, C1-3alkyl and haloC1-3alkyl; R6 and R7 are either i) each independently selected from H, C1-3alkyl and C1-3alkoxy; or ii) R6 and R7 together with the ring to which they are attached form a 9-membered bicylic ring; p is 0-3; and RA is selected from H and C1-3alkyl, compositions containing them, their use in therapy, for example in the treatment of tuberculosis, and methods for the preparation of such compounds, are provided.
    Type: Application
    Filed: June 4, 2014
    Publication date: September 25, 2014
    Applicant: GLAXO GROUP LIMITED
    Inventors: JULIA CASTRO PICHEL, RAQUEL FERNANDEZ MENENDEZ, ESTHER PILAR FERNANDEZ VELANDO, SILVIA GONZALEZ DEL VALLE, ARACELI MALLO-RUBIO