1,4-thiazines Patents (Class 514/227.5)
  • Patent number: 10899746
    Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising a compound of the invention, a method for manufacturing compounds of the invention and therapeutic uses thereof.
    Type: Grant
    Filed: March 27, 2020
    Date of Patent: January 26, 2021
    Assignees: AMGEN INC., CYTOKINETICS, INC.
    Inventors: Luke Ashcraft, Alessandro Boezio, John Butler, Aroop Chandra, Chihyuan Chuang, Scott E. Collibee, Mikkel V. Debenedetto, Vincent DiMassa, Russell Graceffa, Justin Malinowski, David Moebius, Bradley Paul Morgan, Joshua Payette, Antonio Romero, David St. Jean, Jr., Richard Vargas, John Yeoman, Hanmo Zhang, Alan Cheng, Felix Gonzalez Lopez De Turiso, Michael Garrett Johnson
  • Patent number: 10876096
    Abstract: Cell culture compositions containing LFM-A13 or a structurally related compound can enhance global hepatic function. For example, LFM-A13 is shown to enhance levels of a broad variety of drug metabolism enzymes, including CYP enzymes, and other hepatic enzymes. LFM-A13 is also shown to promote differentiation of stem cells into hepatocytes. LFM-A13 and structurally related compounds can be used in cell culture to enhance global drug metabolism of liver cells for enhanced in vitro study the effects of drug metabolism on other candidate drug compounds.
    Type: Grant
    Filed: November 25, 2013
    Date of Patent: December 29, 2020
    Assignee: Corning Incorporated
    Inventors: Ronald Allen Faris, Yulong Hong, Joydeep Lahiri, Jin Liu, Olivia Grace Weeks
  • Patent number: 10835858
    Abstract: The embodiments provide an acidic gas absorbent, an acidic gas removal method, and an acidic gas removal apparatus. The absorbent absorbs an acidic gas in a large amount and hardly diffuses in air. The acidic gas absorbent according to the embodiment comprises an amine compound having a sulfonyl group and two or more amino groups.
    Type: Grant
    Filed: March 8, 2019
    Date of Patent: November 17, 2020
    Assignees: KABUSHIKI KAISHA TOSHIBA, TOSHIBA ENERGY SYSTEMS & SOLUTIONS CORPORATION
    Inventors: Yoshihiko Nakano, Akiko Suzuki, Takashi Kuboki, Toshihiro Imada, Shinji Murai, Reiko Yoshimura, Kenji Sano, Mitsuru Udatsu
  • Patent number: 10413535
    Abstract: The invention relates to antagonists of integrin ?4 and their use in pharmaceutical compositions, primarily topically administered ophthalmic compositions. The pharmaceutical compositions are useful for treating ocular inflammatory conditions, such as dry eye disease, non-infectious uveitis (e.g., anterior, intermediate, posterior, pan-uveitis), non-infectious conjunctivitis, iritis, or scleritis in animals, and particularly mammals, including humans.
    Type: Grant
    Filed: July 7, 2016
    Date of Patent: September 17, 2019
    Assignee: AXEROVISION, INC.
    Inventor: Achim H. Krauss
  • Patent number: 10351547
    Abstract: Described herein are compounds that are somatostatin modulators, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders that would benefit from modulation of somatostatin activity.
    Type: Grant
    Filed: December 20, 2017
    Date of Patent: July 16, 2019
    Assignee: CRINETICS PHARMACEUTICALS, INC.
    Inventors: Jian Zhao, Sangdon Han, Sun Hee Kim, Shimiao Wang, Yunfei Zhu
  • Patent number: 10233157
    Abstract: The present invention relates to the discovery that salt inducible kinases (SIKs) suppress the formation of anti-inflammatory molecules such as IL-10, which are important for the resolution of inflammation and identifies SIK inhibitors that may be used to treat disorders associated with undesirable inflammation, such as inflammatory bowel disease and/or autoimmune disorders.
    Type: Grant
    Filed: May 26, 2017
    Date of Patent: March 19, 2019
    Assignees: Dana-Farber Cancer Institute, Inc., University Court of the University of Dundee
    Inventors: Philip Cohen, Kristopher Clark, Hwan Geun Choi, Nathanael S. Gray
  • Patent number: 10227314
    Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds which inhibit cystathionine-?-lyase (CSE). Also described herein are methods for using such CSE inhibitors, alone or in combination with other compounds, for treating diseases or conditions that would benefit from CSE inhibition.
    Type: Grant
    Filed: August 9, 2017
    Date of Patent: March 12, 2019
    Assignee: SOVA PHARMACEUTICALS, INC.
    Inventors: Sergio G. Durón, Justin Chapman, Simon G. Sydserff, Srinivas G. Rao, Gregory Stein
  • Patent number: 10065937
    Abstract: The invention pertains to novel FLT3 receptor antagonists of general formula (1). The compounds are useful for the treatment or the prevention of pain disorders, cancer and autoimmune diseases.
    Type: Grant
    Filed: July 30, 2015
    Date of Patent: September 4, 2018
    Assignees: INSERM (INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE), UNIVERSITE DE MONTPELLIER, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (CNRS), UNIVERSITE DE STRASBOURG
    Inventors: Jean Valmier, Jean-Philippe Leyris, Didier Rognan, Martine Schmitt
  • Patent number: 10017478
    Abstract: Described are cancer therapies and anti-cancer compounds. In particular, disclosed are inhibitors of Ack1 tyrosine kinase and their use in the treatment of cancer. Methods of screening for new Ack1 tyrosine kinase inhibitors are also disclosed. In specific example, compound having Formula I through IV are disclosed.
    Type: Grant
    Filed: November 9, 2017
    Date of Patent: July 10, 2018
    Assignee: H. Lee Moffitt Cancer Center and Research Institute, Inc.
    Inventors: Nupam P. Mahajan, Kiran N. Mahajan, Nicholas J. Lawrence, Harshani R. Lawrence
  • Patent number: 9932424
    Abstract: A copolymer of polyvinyl alcohol and trifluoro acetaldehyde derivatized to have a substituent that contains fluorine. Such compositions are useful in compatibilizing fluorinated molecules that are to be blended into liquid materials or systems, as well as materials and systems that may be aerosolizable or foamable liquids.
    Type: Grant
    Filed: November 16, 2015
    Date of Patent: April 3, 2018
    Assignee: Warner Babcock Institute for Green Chemistry, LLC
    Inventors: John Charles Warner, Jean R. Loebelenz, Peter N. Kariuki, David K. Bwambok
  • Patent number: 9907306
    Abstract: Compositions and processes for controlling nematodes are described herein, e.g., nematodes that infest plants or animals. The compounds include certain 2,5-substituted tetrazoles.
    Type: Grant
    Filed: April 14, 2016
    Date of Patent: March 6, 2018
    Assignee: Monsanto Technology LLC
    Inventors: Urszula Slomczynska, Matt W. Dimmic, William P. Haakenson, Jr., Al Wideman, Michael J. Crawford
  • Patent number: 9718803
    Abstract: Unsaturated nitrogen heterocyclic compounds of formula (I): as defined in the specification, compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, Huntington's Disease, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.
    Type: Grant
    Filed: December 17, 2015
    Date of Patent: August 1, 2017
    Assignee: Amgen Inc.
    Inventors: Jennifer R. Allen, Jian J. Chen, Michael J. Frohn, Essa Hu Harrington, Qingyian Liu, Alexander J. Pickrell, Shannon Rumfelt, Robert M. Rzasa, Wenge Zhong
  • Patent number: 9676745
    Abstract: The disclosures herein relate to novel compounds of formula wherein R1, R2, R3 and R4 and n are defined here, and their use in treating, preventing, ameliorating, controlling or reducing the risk of inflammation, neurological or psychiatric disorders associated with modulating mGlu5 receptor function.
    Type: Grant
    Filed: July 17, 2014
    Date of Patent: June 13, 2017
    Assignee: Heptares Therapeutics Limited
    Inventors: John Andrew Christopher, Miles Stuart Congreve, Sarah Joanne Aves, Benjamin Gerald Tehan
  • Patent number: 9670165
    Abstract: The present invention relates to the discovery that salt inducible kinases (SIKs) suppress the formation of anti-inflammatory molecules such as IL-10, which are important for the resolution of inflammation and identifies SIK inhibitors that may be used to treat disorders associated with undesirable inflammation, such as inflammatory bowel disease and/or autoimmune disorders.
    Type: Grant
    Filed: March 13, 2013
    Date of Patent: June 6, 2017
    Assignees: Dana-Farber Cancer Institute, Inc., University Court of the University of Dundee
    Inventors: Philip Cohen, Kristopher Clark, Hwan Geun Choi, Nathanael Gray
  • Patent number: 9550797
    Abstract: The present invention relates to a process of preparing a Grignard reagent comprising reacting magnesium particulates in a fluid bed reactor. The present invention further relates to a continuous process comprising fluidizing magnesium particulates in a reactor, forming the Grignard reagent continuously, and reacting the Grignard reagent with a substrate.
    Type: Grant
    Filed: June 27, 2014
    Date of Patent: January 24, 2017
    Assignee: Patheon Holdings I B.V.
    Inventors: Mehul Thathagar, Peter Poechlauer, Rafael Wilhelmus Elisabeth Ghislain Reintjens, Michel Goldbach
  • Patent number: 9505743
    Abstract: The present invention relates generally to bis-amide containing MMP inhibiting compounds, and more particularly to selectively deuterated bis-amide MMP-13 inhibiting compounds that exhibit increased stability or potency in relation to currently known MMP-13 inhibitors. Additionally, the present invention relates to methods for treating pain and inflammation in a patient comprising administering to the patient a pain-reducing effective amount of a present compound.
    Type: Grant
    Filed: November 27, 2012
    Date of Patent: November 29, 2016
    Inventor: Irving Sucholeiki
  • Patent number: 9359314
    Abstract: The present invention relates to a thiazine amide derivative and a pharmaceutical use thereof, and particularly to a compound of formula I (in the formula, variables are as described in the specification), a pharmaceutically acceptable salt, solvate or hydrate thereof. The present invention further relates to a method for preparing the compound, a pharmaceutical composition containing the compound, and a method or use thereof for prevention or treatment of neurodegenerative diseases.
    Type: Grant
    Filed: August 24, 2012
    Date of Patent: June 7, 2016
    Assignee: Institute Of Pharmacology And Toxicology Academy Of Military Medical Sciences P.L.A. China
    Inventors: Song Li, Junhai Xiao, Dan Han, Wu Zhong, Lili Wang, Zhibing Zheng, Yunde Xie, Xinbo Zhou, Xingzhou Li, Xiaokui Wang, Dan Jiang, Wei Chen, Hongying Liu
  • Patent number: 9296878
    Abstract: The invention relates to stable compositions for providing PVC with fungicidal properties. Said stable compositions contain at least one thiabendazole as an active substance, at least one plasticizer for PVC, at least one thixotropic agent, and, optionally, other fungicidal agents. The invention also relates to methods for producing said formulations and the uses thereof for preventing PVC from being infested and destroyed by microorganisms. The invention further relates to mildew-resistant PVC materials provided with the compositions of the invention.
    Type: Grant
    Filed: March 26, 2013
    Date of Patent: March 29, 2016
    Assignee: LANXESS Deutschland GmbH
    Inventors: Hermann Uhr, Andreas Boettcher, Thomas Jaetsch
  • Patent number: 9221808
    Abstract: Compounds and compositions having activity as inhibitors of Rho-associated proteinkinases (ROCKs), and methods of making and using the subject compounds are disclosed.
    Type: Grant
    Filed: April 18, 2011
    Date of Patent: December 29, 2015
    Assignee: H. Lee Moffitt Cancer Center and Research Institute, Inc.
    Inventors: Nicholas J. Lawrence, Roberta Pireddu, Said M. Sebti
  • Patent number: 9212177
    Abstract: Compounds which exhibit antiviral activity, particularly against influenza virus, and methods of making and using thereof are described herein. In one embodiment, the compounds are heterocyclic amides containing piperazine and isozazole rings and optionally substituted with one or more substituents. The compounds can be formulated with one or more pharmaceutically acceptable excipients to form compositions suitable for enteral or parenteral administration. The compounds are preferably used to treat or prevent Influenza A infections, such as H1N1, H2N2, H3N2, H5N1, H7N7, H1N2, H9N2, H7N2, H7N3, and H10N7.
    Type: Grant
    Filed: August 5, 2010
    Date of Patent: December 15, 2015
    Assignee: Versitech Limited
    Inventors: Yi Tsun Richard Kao, Dan Yang, Kwok-Yung Yuen
  • Patent number: 9199979
    Abstract: Thiazolylphenyl-benzenesulfonamido derivatives of formula (I) as defined in the specification, and pharmaceutically acceptable salts thereof, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.
    Type: Grant
    Filed: February 21, 2012
    Date of Patent: December 1, 2015
    Assignee: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Maurizio Pulici, Gabriella Traquandi, Chiara Marchionni, Alessandra Scolaro, Nicoletta Colombo
  • Publication number: 20150148318
    Abstract: A method of inhibiting the growth of cancer cells is disclosed in which cancer cells that contain an enhanced amount relative to non-cancerous cells of one or more of phosphorylated mTOR, Akt1, ERK2 and serine2152-phosphorylated filamin A are contacted with an FLNA-binding effective amount of a compound or a pharmaceutically acceptable salt thereof that binds to the pentapeptide of filamin A (FLNA) of SEQ ID NO: 1 and exhibits at least about 60 percent of the FITC-labeled naloxone binding amount when present at a 10 ?M concentration and using unlabeled naloxone as the control inhibitor at the same concentration. A compound that binds to the FLNA pentapeptide preferably also contains at least four of the six pharmacophores of FIGS. 19-24.
    Type: Application
    Filed: September 26, 2014
    Publication date: May 28, 2015
    Inventors: Hoau-Yan Wang, Lindsay Burns Barbier
  • Publication number: 20150133430
    Abstract: Provide herein are compounds and pharmaceutical compositions suitable as modulators of hemoglobin, methods and intermediates for their preparation, and methods for their use in treating disorders mediated by hemoglobin and disorders that would benefit from tissue and/or cellular oxygenation.
    Type: Application
    Filed: January 16, 2015
    Publication date: May 14, 2015
    Inventors: Qing XU, Zhe LI
  • Publication number: 20150080369
    Abstract: The present invention is directed to novel retinoid-related orphan receptor gamma (ROR?) modulators, processes for their preparation, pharmaceutical compositions containing these modulators, and their use in the treatment of inflammatory, metabolic and autoimmune diseases mediated by ROR?.
    Type: Application
    Filed: April 25, 2013
    Publication date: March 19, 2015
    Inventors: Veronique Birault, Amanda Jennifer Campbell, Stephen Harrison, Joelle Le, Lena Shukla
  • Publication number: 20150038499
    Abstract: Methods of improving patient safety and reducing undesirable side effects for patients considering therapeutic treatment using monomethyl fumarate and prodrugs of monomethyl fumarate are disclosed. In particular, a method of treating a disease in a patient in need of such treatment is provided. The method comprises testing the patient for a propensity for a deficiency in tissue glutathione S-transferase theta 1 enzyme (GSTT1) levels. Thereafter, a therapeutically effective amount of a compound selected from monomethyl fumarate (MMF), a prodrug of monomethyl fumarate, and combinations thereof is administered to the patient. During the treatment of the disease, blood lymphocyte concentration is periodically tested in the patient at a predetermined time interval length that is based on the enzyme level propensity testing result.
    Type: Application
    Filed: August 1, 2014
    Publication date: February 5, 2015
    Inventor: Peter A. Virsik
  • Publication number: 20150038493
    Abstract: The present invention relates to a series of molecules derived from 2,3-diaminopropionic acid (DAP), comprising or not comprising an 8-hydroxyquinoline (8-HQ) motif, and to the use of said molecules for trapping an alpha-oxoaldehyde resulting particularly from the degradation of the glucose or for trapping an alpha-beta-unsaturated aldehyde, resulting particularly from the oxidative degradation of fatty acids. These molecules can have a further application in the fields of cosmetics, food processing, and pharmaceuticals.
    Type: Application
    Filed: October 5, 2012
    Publication date: February 5, 2015
    Inventors: Guy Potier, André Nobumichi Sasaki, Nicolas Audic
  • Publication number: 20150038498
    Abstract: Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: (I) or a pharmaceutically acceptable salt thereof, wherein Q is CH2, NR4, O, S, S(O) or S(O2), wherein R4 is H, C1-6 alkyl, aryl, or C3-8 cycloalkyl; R1 is a heterocycle or —(CR5R6)1-2NH2, wherein R5 and R6, each time in which they occur, are independently H, C1-6 alkyl, —CH2F, —CHF2, CF3 or —CH2OH; R2 is OH, NH2 or NHSO2CH3; and R3 is C1-6 alkyl.
    Type: Application
    Filed: March 22, 2013
    Publication date: February 5, 2015
    Inventors: Timothy Allen Blizzard, Tesfaye Biftu
  • Publication number: 20150031688
    Abstract: A dual thyrointegrin antagonist and a method for treating an angiogenesis-mediated disorder and/or a hyperthyroidism disorders by introducing the dual thyrointegrin antagonist into animals (e.g., mammals, human beings). The dual thyrointegrin antagonist includes a chemical structure having a thyroid hormone antagonist and ?v?3 integrin antagonist in the same molecule.
    Type: Application
    Filed: October 9, 2014
    Publication date: January 29, 2015
    Inventor: Shaker A. Mousa
  • Publication number: 20140343000
    Abstract: Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, C-17 and C-3 modified triterpenoids that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formulas I, II and III: These compounds are useful for the treatment of HIV and AIDS.
    Type: Application
    Filed: July 24, 2014
    Publication date: November 20, 2014
    Inventors: Alicia Regueiro-Ren, Zheng Liu, Jacob Swidorski, Ny Sin, Brian Lee Venables, Sing-Yuen Sit, Yan Chen, Jie Chen, Nicholas A. Meanwell
  • Publication number: 20140336185
    Abstract: Compounds that bind the glucagon-like peptide 1 (GLP-1) receptor, methods of their synthesis, methods of their therapeutic and/or prophylactic use, and methods of their use in stabilizing GLP-1 receptor in vitro for crystallization of the GLP-1 receptor are provided. Certain compounds may have activity as modulators or potentiators with respect to glucagon receptor, GIP receptor, GLP-1 and GLP-2 receptors, and PTH receptor on their own or in the presence of receptor ligands such as GIP (1-42), PTH (1-34), Glucagon (1-29), GLP-2 (1-33), GLP-1 (7-36), GLP-1 (9-36), oxyntomodulin and exendin variants.
    Type: Application
    Filed: May 31, 2012
    Publication date: November 13, 2014
    Inventors: Marcus F. Boehm, Esther Martinborough, Manisha Moorjani, Junko Tamiya, Liming Huang, Thomas Fowler, Andrew Novak, Premji Meghani, Enugurthi Brahmachary, Adam Richard Yeager
  • Patent number: 8877747
    Abstract: An indenone derivative of formula (1) is effective in enhancing the activity of osteoblastic cells and inhibiting bone resorption by osteoclastic cells, and a pharmaceutical composition comprising the indenone derivative or a pharmaceutically acceptable salt thereof is useful for preventing or treating bone diseases such as osteoporosis.
    Type: Grant
    Filed: October 21, 2009
    Date of Patent: November 4, 2014
    Assignee: Korea Research Institute of Chemical Technology
    Inventors: Jung Nyoung Heo, Myung Ae Bae, Nack Jeong Kim, Sung Youn Chang, Nam Sook Kang, Sung Eun Yoo, Eun Sook Hwang
  • Patent number: 8859539
    Abstract: A dual thyrointegrin antagonist and a method for treating an angiogenesis-mediated disorder and/or a hyperthyroidism disorders by introducing the dual thyrointegrin antagonist into animals (e.g., mammals, human beings). The dual thyrointegrin antagonist includes a chemical structure having a thyroid hormone antagonist and ?v?3 integrin antagonist in the same molecule.
    Type: Grant
    Filed: November 1, 2010
    Date of Patent: October 14, 2014
    Assignee: Vascular Vision Pharmaceutical Company
    Inventor: Shaker A. Mousa
  • Publication number: 20140296227
    Abstract: The present invention relates to compounds of formula (I), wherein R1, R2, R3, R4 and R5 are independently selected from the group comprising, inter aliae, H, optionally substituted, branched or linear C1-C12 alkyl, halogen atom and C1-C12 haloalkyl, and wherein A represents a single bond or an optionally substituted C1-C6 alkylene radical, notably useful for the treatment of human neoplasms.
    Type: Application
    Filed: October 4, 2012
    Publication date: October 2, 2014
    Inventors: Marc Lopez, Yves Collette, Lynda Mezil, Jean-Michel Brunel, Sebastien Combes
  • Publication number: 20140275048
    Abstract: The present invention provides compounds of formula (I), and pharmaceutical compositions thereof.
    Type: Application
    Filed: March 14, 2014
    Publication date: September 18, 2014
    Applicant: Alkermes Pharma Ireland Limited
    Inventors: Tarek A. Zeidan, Scott Duncan, Christopher P. Hencken, Thomas Andrew Wynn, Carlos N. Sanrame
  • Publication number: 20140275008
    Abstract: Provide herein are compounds and pharmaceutical compositions suitable as modulators of hemoglobin, methods and intermediates for their preparation, and methods for their use in treating disorders mediated by hemoglobin and disorders that would benefit from tissue and/or cellular oxygenation.
    Type: Application
    Filed: March 15, 2013
    Publication date: September 18, 2014
    Inventors: Qing Xu, Zhe Li
  • Publication number: 20140228357
    Abstract: The present invention relates to novel compounds as HIF-1? inhibitors, manufacturing process thereof, and a pharmaceutical compositions. The compounds according to the present invention having inhibition activity against HIF-1?, can be used as a therapeutic prevention and/or treatment for various solid cancers such as colon cancer, liver cancer, stomach cancer and breast cancer. Also, the compounds according to the present invention are useful in the treatment of diabetic retinopathy and rheumatoid arthritis, which are aggravated by HIF-1?-mediated VEGFA expression.
    Type: Application
    Filed: September 27, 2012
    Publication date: August 14, 2014
    Inventors: Kyeong Lee, Mi-Sun Won, Hwan-Mook Kim, Song-Kyu Park, Ki-Ho Lee, Chang-Woo Lee, Bo-Kyung Kim, Hyun-Seung Ban, Kyung-Sook Chung, Naik Ravi
  • Patent number: 8802669
    Abstract: Disclosed are dihydropyrimidine compounds and preparation methods, pharmaceutical compositions and uses thereof. Specifically, the compounds described herein in general formula (I), or their isomers, pharmaceutically acceptable salts or hydrates are provided, wherein each variable has the meaning as defined in the description. Also provided are a process for preparing the compounds of the general formula (I), the use of the compounds, an isomer thereof, a pharmaceutically acceptable salt thereof or a hydrate thereof as a medicament, in particular as a medicament for the treatment and/or prevention of Hepatitis B.
    Type: Grant
    Filed: May 27, 2010
    Date of Patent: August 12, 2014
    Assignee: Institute of Pharmacology and Toxicology Academy of Military Medical Sciences, P.L.A. China
    Inventors: Song Li, Xiaoqian Xu, Guoming Zhao, Lili Wang, Hua Guan, Junhai Xiao, Wu Zhong, Zhibing Zheng, Yunde Xie, Xingzhou Li, Xiaokui Wang, Xinbo Zhou, Hongying Liu
  • Publication number: 20140221361
    Abstract: Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, C-19 modified triterpenoids that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formulas I and II: These compounds are useful for the treatment of HIV and AIDS.
    Type: Application
    Filed: February 4, 2014
    Publication date: August 7, 2014
    Inventors: Jacob Swidorski, Brian Lee Venables, Zheng Liu, Ny Sin, Nicholas A. Meanwell, Alicia Regueiro-Ren
  • Publication number: 20140163017
    Abstract: In one aspect, the invention relates to substituted (E)-N?-(1-phenylethylidene)benzohydrazide analogs, derivatives thereof, and related compounds, which are useful as inhibitors of lysine-specific histone demethylase, including LSD1; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds and compositions to treat disorders associated with dysfunction of the LSD1. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Application
    Filed: June 19, 2013
    Publication date: June 12, 2014
    Applicant: UNIVERSITY OF UTAH
    Inventors: Hariprasad Vankayalapati, Venkataswamy Sorna, Steven L. Warner, Bret Stephens, David J. Bearss, Sunil Sharma
  • Publication number: 20140135296
    Abstract: The invention provides methods of treating autophagy mediated diseases and disorders and related pharmaceutical compositions, diagnostics, screening techniques and kits. In one embodiment, the invention provides a method of determining whether a subject suffers from, or is at risk of developing, and autophagy mediated disease state and/or condition by evaluating LC3 levels.
    Type: Application
    Filed: May 10, 2012
    Publication date: May 15, 2014
    Inventors: Vojo Deretic, Eliseo Castillo, Steven Bradfute, Larry A. Sklar
  • Publication number: 20140128382
    Abstract: The present invention discloses certain iminothiazine compounds and mono- and dioxides thereof, including compounds Formula (I): and tautomers and stereoisomers thereof, and pharmaceutically acceptable salts of said compounds, said tautomers and said stereoisomers, wherein each of variables shown in the formula are as defined herein. The compounds of the invention may be useful as BACE inhibitors and/or for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and uses, including Alzheimer's disease, are also disclosed.
    Type: Application
    Filed: April 12, 2012
    Publication date: May 8, 2014
    Inventors: Wen-Lian Wu, Duane A. Burnett, Andrew W. Stamford, Jared N. Cumming, Chad E. Bennett, Eric J. Gilbert, Jack D. Scott, Younong Yu, Xuanjia Peng
  • Patent number: 8703828
    Abstract: In one aspect, compositions provide antimicrobial therapy as topical disinfectants. Particularly, one aspect relates to an alcohol containing antimicrobial composition that includes at least one paraben, a redox compound and an organic acid at a concentration of from about 1.5 percent to about 10 percent by weight, based on the total weight of the composition. In other aspects, antimicrobial compositions are used to topically sanitize wounds, skin areas and/or to disinfect surgical instruments or other surfaces. Still, in further aspects, methods, devices and kits relating to an antimicrobial composition are provided.
    Type: Grant
    Filed: March 4, 2013
    Date of Patent: April 22, 2014
    Assignee: Zurex Pharma, Inc.
    Inventors: Stephen R. Ash, Janusz Steczko
  • Publication number: 20140107109
    Abstract: The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables A4, A5, A6, A8, R1, R2, R3, R7 and n of Formula I, independently, are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and corresponding uses of the compounds and compositions for treatment of disorders and/or conditions related to A-beta plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, schizophrenia and other central nervous system conditions. The invention further provides compounds of Formula II and sub-formula embodiments thereof, intermediates and processes and methods useful for the preparation of compounds of Formulas I-II.
    Type: Application
    Filed: December 18, 2013
    Publication date: April 17, 2014
    Inventors: Richard T. LEWIS, Jennifer R. ALLEN, Yuan CHENG, Deborah CHOQUETTE, Oleg EPSTEIN, Angel GUZMAN-PEREZ, Paul E. HARRINGTON, Zihao HUA, Randall W. HUNGATE, Jason Brooks HUMAN, Ted JUDD, Qingyian LIU, Patricia LOPEZ, Ana Elena MINATTI, Philip OLIVIERI, Karina ROMERO, Shannon RUMFELT, Robert M. RZASA, Laurie SCHENKEL, John STELLWAGEN, Ryan WHITE, Qiufen XUE, Xiao ZHENG, Wenge ZHONG
  • Publication number: 20140094455
    Abstract: Compounds, including 3-carboxy aryl sulfonamide compounds, which agonize or antagonize aquaporin channels and methods of using them to treat disorders or diseases mediated by aquaporins.
    Type: Application
    Filed: August 19, 2013
    Publication date: April 3, 2014
    Applicant: ARIZONA BOARD OF REAGENTS ON BEHALF OF THE UNIVERSITY OF ARIZONA
    Inventors: Gary A. Flynn, Andrea J. Yool, Elton Rodrigues Migliati, Leslie S. Ritter
  • Publication number: 20140018341
    Abstract: A method of inhibiting phosphorylation of the tau protein and/or a TLR4-mediated immune response is disclosed. The method contemplates administering to cells in recognized need thereof such as cells of the central nervous system an effective amount of a of a compound or a pharmaceutically acceptable salt thereof that binds to a pentapeptide of filamin A (FLNA) of SEQ ID NO: 1, and contains at least four of the six pharmacophores of FIGS. 35-40.
    Type: Application
    Filed: July 11, 2013
    Publication date: January 16, 2014
    Inventors: Hoau-Yan Wang, Lindsay Burns Barbier
  • Patent number: 8604025
    Abstract: Certain substituted sulfonamide derivatives selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure.
    Type: Grant
    Filed: February 5, 2013
    Date of Patent: December 10, 2013
    Assignee: Cytokinetics, Inc.
    Inventors: Bradley Paul Morgan, Fady Malik, Erica Anne Kraynack, Alexander Ramon Muci, Xiangping Qian, David J. Morgans, Jr.
  • Patent number: 8575155
    Abstract: A composition and method is provided for modifying sperm fertility in mammals for the purpose of biasing the gender in favor of male offspring. The composition includes an amount of a class of compounds of phenoxazine or phenothiazine, having the structure (FIG. 1) and ionic derivatives thereof, wherein R1 is H, a lower alkyl group or N(R3)2, R2 is N, S, O, and R3 is H or a lower alkyl group. A second component of the composition is an amount of a hexose sugar or the phosphorylated hexose esters of such. When mixed with living sperm prior to or at the time of insemination, the composition results in modified rates of conception and an alteration of the birth sex ratio.
    Type: Grant
    Filed: November 26, 2008
    Date of Patent: November 5, 2013
    Inventor: Timothy James Williams
  • Patent number: 8563544
    Abstract: Provided herein are 2,5-disubstituted arylsulfonamide CCR3 antagonists, e.g., compounds of Formula I, and pharmaceutical compositions thereof: Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a CCR3-mediated disorder, disease, or condition.
    Type: Grant
    Filed: October 26, 2012
    Date of Patent: October 22, 2013
    Assignee: Axikin Pharmaceuticals, Inc.
    Inventors: Tai Wei Ly, Garrett Thomas Potter
  • Patent number: 8546583
    Abstract: The present invention relates to compounds of formula (I), or pharmaceutical salts, prodrugs, salts of prodrugs, or combinations thereof, wherein R1, R2, R3, R4, and L1 are defined in the specification, compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions. The present invention also relates to compounds of formula (II), or pharmaceutical salts, prodrugs, salts of prodrugs, or combinations thereof, wherein R1a, R2a and (Rx)n are as defined in the specification, compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.
    Type: Grant
    Filed: May 30, 2007
    Date of Patent: October 1, 2013
    Assignee: AbbVie Inc.
    Inventors: Alan S. Florjancic, Michael J. Dart, Keith B. Ryther, Arturo Perez-Medrano, William A. Carroll, Meena V. Patel, Karin Rosemarie Tietje, Tongmei Li, Teodozyj Kolasa, Megan E. Gallagher, Sridhar Peddi, Jennifer M. Frost, Derek W. Nelson
  • Patent number: RE48334
    Abstract: The present invention relates to a compound represented by the formula wherein ring A is a nitrogen-containing heterocycle; ring B is an aromatic ring optionally having substituent(s); ring D is an aromatic ring optionally having substituent(s); L is a group represented by the formula R2, R3, R4a and R4b are each independently a hydrogen atom, an optionally halogenated C1-6 alkyl group or an optionally halogenated C3-6 cycloalkyl group, or R2 and R3 are optionally bonded via an alkylene chain or an alkenylene chain, or R4a and R4b are optionally bonded via an alkylene chain or an alkenylene chain; R1 is a hydrogen atom or a substituent; m and n are each independently an integer of 0 to 5; m+n is an integer of 2 to 5; and is a single bond or double bond, or a salt thereof; and the like.
    Type: Grant
    Filed: February 28, 2017
    Date of Patent: December 1, 2020
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Junya Shirai, Hideyuki Sugiyama, Taku Kamei, Hironobu Maezaki