1,3,4-thiadiazoles (including Hydrogenated) Patents (Class 514/363)
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Patent number: 12029728Abstract: The present disclosure describes a method of treating an infection, including a parasitic infection, using compounds of the invention. The compounds of the invention can selectively eradicate intracellular mammalian and human parasites.Type: GrantFiled: October 29, 2019Date of Patent: July 9, 2024Assignee: New Mexico Tech University Research Park CorporationInventors: Snezna Rogelj, Danielle Nicole Turner, Ivy Hurwitz, Alexander Aksenov
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Patent number: 12018029Abstract: The disclosure relates to compounds of Formula (I), or pharmaceutically acceptable salts thereof, wherein X1 and X5 is each selected from CR1 or N; X2, X3 and X4 is each selected from CR1, CR2 or N, provided at least one of X2, X3 and X4 is CR2 and provided only one of X1, X2, X3, X4 and X5 can be N. R1, R2, R3, R4, R5, L1, L2 and L3 are as defined herein. Compounds according to Formula (I) are pharmacologically effective as lysyl oxidase (LOX) inhibitors and are believed to be useful in the treatment of, for instance, cancer.Type: GrantFiled: June 5, 2019Date of Patent: June 25, 2024Assignee: The Institute of Cancer Research: Royal Cancer HospitalInventors: Leo Leung, Kiri North, Deborah Smithen, Mohammed Aljarah, Michael Brown, Ben Ayers, Dan Niculescu-Duvaz, Caroline Springer
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Patent number: 11911372Abstract: A compound of formula (I), or a pharmaceutically acceptable salt thereof.Type: GrantFiled: June 28, 2019Date of Patent: February 27, 2024Assignee: CTXT PTY LTDInventors: Paul Anthony Stupple, Helen Rachel Lagiakos, Richard Charles Foitzik, Michelle Ang Camerino, George Nikolakopoulos, Ylva Elisabet Bergman Bozikis, Wilhelmus Johannes Antonius Kersten, Scott Raymond Walker, Jonathan Grant Hubert
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Patent number: 11897849Abstract: A N?-(2-(5-phenyl-1,3,4-oxadiazol-2-ylthio)acetoxy)-1-naphthimidamide compound, its synthesis, and its use as an anti-microbial agent.Type: GrantFiled: October 9, 2023Date of Patent: February 13, 2024Assignee: KING FAISAL UNIVERSITYInventors: Hany Mohamed Abd El-Lateef Ahmed, Mai Mostafa Khalaf Ali, Antar Ahmed Abdelhamid Ahmed, Amer A. Amer
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Patent number: 11725004Abstract: This invention relates to novel (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: GrantFiled: August 10, 2021Date of Patent: August 15, 2023Assignee: Centrexion Therapeutics CorporationInventors: Doris Riether, Florian Paul Christian Binder, Henri Doods, Stephan Georg Mueller, Janet Rachel Nicholson, Achim Sauer
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Patent number: 11596600Abstract: The invention generally relates to compositions for inducing vasoconstriction. The compositions comprise highly selective alpha-2 adrenergic receptor agonists, at low concentrations, such as below 0.05% weight by volume. The compositions preferably comprise brimonidine. The compositions preferably have pH between about 5.5 and about 6.5.Type: GrantFiled: January 26, 2022Date of Patent: March 7, 2023Assignee: Eye Therapies, LLCInventor: Gerald Horn
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Patent number: 11286266Abstract: The present invention relates to 1-imidazothiadiazolo-2H-pyrrol-5-one derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.Type: GrantFiled: May 6, 2019Date of Patent: March 29, 2022Inventors: Hugues Chanteux, Yannick Quesnel, Claude Delatour, Laurent Provins
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Patent number: 11155565Abstract: The present invention relates to 2-oxo-1,3-oxazolidinyl imidazothiadiazole derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.Type: GrantFiled: July 5, 2018Date of Patent: October 26, 2021Inventors: Laurent Provins, Hugues Chanteux, Yannick Quesnel
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Patent number: 11155566Abstract: The present invention relates to 2-oxo-1-pyrrolidinyl imidazothiadiazole derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.Type: GrantFiled: December 4, 2018Date of Patent: October 26, 2021Inventors: Laurent Provins, Hugues Chanteux
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Patent number: 11155564Abstract: The present invention relates to 2-oxo-1-imidazolidinyl imidazothiadiazole derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.Type: GrantFiled: July 5, 2018Date of Patent: October 26, 2021Inventors: Laurent Provins, Hugues Chanteux
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Patent number: 10813916Abstract: 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: GrantFiled: May 27, 2016Date of Patent: October 27, 2020Assignee: Jubilant Generics LimitedInventors: Pankaj Soni, Rashmi Ranjan Panda, Ganesh Vinayak Gat, Dinesh Kumar, Kamal S. Mehta, Ravikumar Nithiyanandam
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Patent number: 10722498Abstract: 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: GrantFiled: January 22, 2018Date of Patent: July 28, 2020Assignee: SHILPA MEDICARE LIMITEDInventors: Andanayya Saraganachari, Abhilash Narayanaswamy, Sreenivasa Reddy, Shivakumar Pradeep
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Patent number: 10532034Abstract: 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: GrantFiled: March 25, 2010Date of Patent: January 14, 2020Assignee: Cornell UniversityInventors: Richard A. Cerione, Jon W. Erickson, Kristin Wilson Cerione, Jianbin Wang
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Patent number: 10011574Abstract: 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: GrantFiled: November 21, 2013Date of Patent: July 3, 2018Assignee: Agios Pharmaceuticals, Inc.Inventors: Rene M. Lemieux, Janeta Popovici-Muller, Francesco G. Salituro, Jeffrey O. Saunders, Jeremy Travins, Shunqi Yan
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Patent number: 9801813Abstract: 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: GrantFiled: October 13, 2014Date of Patent: October 31, 2017Assignee: Sentiss Pharma Private LimitedInventors: Mandar V. Shah, Deepak Bahri, Manish Kumar Singh
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Patent number: 9505736Abstract: Provided are certain histone deacetylase (HDAC) inhibitors of Formula I, compositions thereof, and methods of their use.Type: GrantFiled: July 16, 2013Date of Patent: November 29, 2016Assignee: CHDI Foundation, Inc.Inventors: Celia Dominguez, Perla Breccia, Christopher A. Luckhurst, Roland W. Bürli, Andrew J. Stott
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Patent number: 9457016Abstract: 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: GrantFiled: August 29, 2014Date of Patent: October 4, 2016Assignee: New York UniversityInventors: Edward Skolnik, Zhai Li
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Patent number: 9320734Abstract: Pleckstrin homology domain binding compounds, pharmaceutical compositions including such compounds, and methods for their use are described herein.Type: GrantFiled: January 5, 2015Date of Patent: April 26, 2016Assignees: Board of Regents, The University of Texas System, Arizona Board of Regents on behalf of the University of ArizonaInventors: Daruka Mahadevan, Emmanuelle J. Meuillet, Eugene A. Mash, Jr., Vijay M. Gokhale, Garth Powis, Shuxing Zhang
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Patent number: 9278962Abstract: 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: GrantFiled: May 6, 2014Date of Patent: March 8, 2016Assignee: 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
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Patent number: 9221841Abstract: 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: GrantFiled: March 19, 2015Date of Patent: December 29, 2015Assignee: 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
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Patent number: 9180118Abstract: 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: GrantFiled: July 18, 2007Date of Patent: November 10, 2015Assignee: University of RochesterInventors: Craig Jordan, Monica Guzman
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Patent number: 9108960Abstract: 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: GrantFiled: December 18, 2012Date of Patent: August 18, 2015Assignee: Council of Scientific & Industrial ResearchInventors: Ahmed Kamal, Arutla Viswanath, Jayanti Naga Srirama Chandra Murty, Farheen Sulthana, Gadupudi Ramakrishna, Inshad Ali Khan, Nitin Pal Kalia
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Patent number: 9102639Abstract: 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: GrantFiled: December 6, 2013Date of Patent: August 11, 2015Assignee: Array BioPharma Inc.Inventors: Jeremy Hans, Eli M. Wallace, Qian Zhao, Joseph P. Lyssikatos, Thomas D. Aicher, Ellen R. Laird, John Robinson, Shelley Allen
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Publication number: 20150133446Abstract: 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: ApplicationFiled: April 24, 2013Publication date: May 14, 2015Inventors: 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
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Patent number: 9028878Abstract: 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: GrantFiled: August 3, 2012Date of Patent: May 12, 2015Assignee: Microbion CorporationInventor: Brett Hugh James Baker
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Publication number: 20150126563Abstract: Pleckstrin homology domain binding compounds, pharmaceutical compositions including such compounds, and methods for their use are described herein.Type: ApplicationFiled: January 5, 2015Publication date: May 7, 2015Applicants: BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM, Arizona Board of Regents on Behalf of the University of ArizonaInventors: Daruka MAHADEVAN, Emmanuelle J. MEUILLET, Eugene A. MASH, JR., Vijay M. GOKHALE, Garth POWIS, Shuxing ZHANG
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Patent number: 9023874Abstract: 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: GrantFiled: November 11, 2010Date of Patent: May 5, 2015Assignee: 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
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Publication number: 20150119390Abstract: 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: ApplicationFiled: April 24, 2013Publication date: April 30, 2015Inventors: Alain Martel, François Tremblay, Anne Marinier, Eldon Scott Priestley, Shoshana L. Posy, R. Michael Lawrence, Michael M. Miller
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Patent number: 9006454Abstract: 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: GrantFiled: March 26, 2010Date of Patent: April 14, 2015Assignee: 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
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Publication number: 20150094297Abstract: 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: ApplicationFiled: April 24, 2013Publication date: April 2, 2015Inventors: 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
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Patent number: 8993619Abstract: 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: GrantFiled: April 26, 2013Date of Patent: March 31, 2015Assignee: Novartis AGInventors: 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
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Publication number: 20150087646Abstract: 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: ApplicationFiled: June 10, 2013Publication date: March 26, 2015Applicant: GLENMARK PHARMACEUTICALS S.A.Inventors: Laxmikant Atmaram Gharat, Nagarajan Muthukaman, Neelima Khairatkar-Joshi, Vidya Ganapati Kattige
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Patent number: 8980920Abstract: 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: GrantFiled: May 28, 2010Date of Patent: March 17, 2015Assignee: Merck Sharp & Dohme Corp.Inventors: Qingbei Zeng, Kevin X. Chen, Anilkumar Gopinadhan Nair, Stuart B. Rosenblum, Joseph A. Kozlowski, F. George Njoroge
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Patent number: 8980892Abstract: 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: GrantFiled: February 18, 2010Date of Patent: March 17, 2015Assignees: Syngenta Crop Protection LLC, Syngenta LimitedInventors: Peter Renold, Thomas Pitterna, Jerome Yves Cassayre, Myriem El Qacemi
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Publication number: 20150065486Abstract: 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: ApplicationFiled: August 29, 2014Publication date: March 5, 2015Inventors: Edward Skolnik, Zhai Li
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Patent number: 8962663Abstract: Pleckstrin homology domain binding compounds, pharmaceutical compositions including such compounds, and methods for their use are described herein.Type: GrantFiled: March 7, 2013Date of Patent: February 24, 2015Assignees: Board of Regents, The University of Texas System, Arizona Board of Regents on Behalf of the University of ArizonaInventors: Daruka Mahadevan, Emmanuelle J. Meuillet, Eugene A. Mash, Jr., Vijay M. Gokhale, Garth Powis, Shuxing Zhang
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Publication number: 20150051193Abstract: 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: ApplicationFiled: October 5, 2012Publication date: February 19, 2015Inventors: Jeffrey S. Glenn, Michael A. Gelman, Brandon Tavshanjian, Kevan Shokat, Ingrid Choong
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Patent number: 8957060Abstract: 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: GrantFiled: May 30, 2012Date of Patent: February 17, 2015Inventor: Jeffrey Alan Klein
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Publication number: 20150045399Abstract: 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: ApplicationFiled: September 2, 2014Publication date: February 12, 2015Applicant: Alexar Therapeutics, Inc.Inventor: Raju Mohan
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Publication number: 20150038416Abstract: 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: ApplicationFiled: June 5, 2014Publication date: February 5, 2015Inventors: Marcus F. Boehm, Esther Martinborough, Manisha Moorjani, Junko Tamiya, Liming Huang, Adam R. Yeager, Enugurthi Brahmachary, Thomas Fowler, Andrew Novak, Premji Meghani, Michael Knaggs
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Publication number: 20150025094Abstract: 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, halType: ApplicationFiled: August 1, 2012Publication date: January 22, 2015Applicants: YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEM LTD., DIAB R&d 1, BAR-IIan UniversityInventors: Shlomo Sasson, Erol Cerasi, Arie Lev Gruzman, Ella Meltzer-Mats
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Publication number: 20150018330Abstract: 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: ApplicationFiled: July 30, 2014Publication date: January 15, 2015Applicant: UNIVERSITY OF VIRGINIA PATENT FOUNDATIONInventors: Paul S. Hoffman, Richard L. Guerrant, Timothy L. MacDonald, Thomas Eric Ballard, JR.
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Patent number: 8933107Abstract: 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: GrantFiled: September 12, 2006Date of Patent: January 13, 2015Assignee: Bayer Cropscience AGInventors: 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
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Publication number: 20150004134Abstract: 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: ApplicationFiled: December 3, 2013Publication date: January 1, 2015Applicant: 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
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Publication number: 20140378445Abstract: 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: ApplicationFiled: December 21, 2012Publication date: December 25, 2014Inventors: Robert Shalwitz, Kevin G. Peters
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Publication number: 20140369961Abstract: 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: ApplicationFiled: August 28, 2014Publication date: December 18, 2014Inventors: Jim Li, Lijing Chen, Bindu Goyal, Guy Laidig, Timothy F. Stanton, Eric B. Sjogren
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Publication number: 20140350026Abstract: 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: ApplicationFiled: November 9, 2012Publication date: November 27, 2014Inventors: Xianjin Luo, Weidong Ye
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Patent number: 8895535Abstract: 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: GrantFiled: September 14, 2011Date of Patent: November 25, 2014Assignee: Merck Patent GmbHInventors: Timo Heinrich, Frank Zenke, Michel Calderini, Djordje Musil
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Publication number: 20140341850Abstract: A new class of haloalkyl heteroaryl benzamides is described. These compounds show strong activity against hepatitis viruses.Type: ApplicationFiled: August 5, 2014Publication date: November 20, 2014Applicant: Romark Laboratories, L.C.Inventors: Jean-Francois Rossignol, J. Edward Semple
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Publication number: 20140343077Abstract: 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: ApplicationFiled: August 22, 2012Publication date: November 20, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Christian Brochu, Chantal Grand-Maitre, Lee Fader, Cyrille Kuhn, Megan Bertrand-Laperle, Marc Pesant