Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To The Morpholine Ring Patents (Class 514/237.5)
  • Publication number: 20140288077
    Abstract: In one aspect, the invention relates to substituted 4-phenoxyphenol analogs, derivatives thereof, and related compounds, which are useful as inhibitors of proliferating cell nuclear antigen (PCNA); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating hyperproliferative disorders associated with PCNA using the compounds and compositions. 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: July 5, 2012
    Publication date: September 25, 2014
    Applicant: ST. JUDE CHILDREN'S RESEARCH HOSPITAL
    Inventors: Naoaki Fujii, Marcelo Actis, Chandanamali Punchihewa, Michele Connelly, Sean Wu
  • 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: 20140275037
    Abstract: Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain novel semicarbazides, sulfonyl carbazides, ureas and related compounds in therapeutically effective amounts are disclosed. Methods for preparing the compounds and methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by hemorrhagic fever viruses is disclosed, i.e., including but not limited to Arenaviridae (Junin, Machupo, Guanavito, Sabia and Lassa), Filoviridae (ebola and Marburg viruses), Flaviviridae (yellow fever, omsk hemorrhagic fever and Kyasanur Forest disease viruses), and Bunyaviridae (Rift Valley fever).
    Type: Application
    Filed: December 19, 2013
    Publication date: September 18, 2014
    Applicant: Siga Technologies, Inc.
    Inventors: Yijun Deng, Theodore J. Nitz, Thomas R. Bailey, Yanming Zhang, Sylvie Laquerre
  • Patent number: 8829199
    Abstract: A compound represented by formula (I) or a pharmacologically acceptable salt thereof, which can inhibit a fibroblast growth factor receptor (FGFR) family kinase in cancer tissues. (In the formula, A represents a 5- to 10-membered heteroaryl group, or a C6-10 aryl group; R1 and R2 independently represent H, OH, X, CN, NO2, a C1-4 haloalkyl group, a C1-6 alkyl group, or the like <R1 and R2 together form a (substituted) 3- to 10-membered heterocyclyl group or a (substituted) 5- to 10-membered heteroaryl group>; R3 represents H, a C1-5 alkyl group, a C6-10 aryl group, a C1-5 alkyl group, or a C1-4 haloalkyl group; and R4 represents H, X, a C1-3 alkyl group, a C1-4 haloalkyl group, OH, CN, NO2, or the like.
    Type: Grant
    Filed: August 5, 2010
    Date of Patent: September 9, 2014
    Assignees: Chugai Seiyaku Kabushiki Kaisha, F. Hoffmann-La Roche AG
    Inventors: Naoki Taka, Masayuki Ohmori, Kyoko Takami, Masayuki Matsushita, Tadakatsu Hayase, Ikumi Hyodo, Masami Kochi, Hiroki Nishii, Hirosato Ebiike, Yoshito Nakanishi, Toshiyuki Mio, Lisha Wang, Weili Zhao
  • Patent number: 8829200
    Abstract: The present invention relates to compounds of formula (IA) and (IB): and pharmaceutically acceptable salts thereof, wherein R1-R7 are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
    Type: Grant
    Filed: October 26, 2011
    Date of Patent: September 9, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Zhidong Chen, Stephane De Lombaert, Jonathon Alan Dines, Weimin Liu, Ho Yin Lo, Pui Leng Loke
  • Patent number: 8822467
    Abstract: The present invention provides biaryl oxyacetic acid compounds which may be useful for treating inflammatory disorders, including disorders affecting the respiratory system and skin.
    Type: Grant
    Filed: December 14, 2012
    Date of Patent: September 2, 2014
    Assignee: Ligand Pharmaceuticals Incorporated
    Inventors: Brian F. McGuinness, Koc-Kan Ho, Suresh Babu, Guizhen Dong, Jingqi Duo, Thuy X. H. Le, Kurt W. Saionz
  • Publication number: 20140235636
    Abstract: The invention provides certain N-acyloxysulfonamide and N-hydroxy-N-acylsulfonamide derivative compounds, pharmaceutical compositions and kits comprising such compounds, and methods of using such compounds or pharmaceutical compositions. In particular, the invention provides methods of using such compounds or pharmaceutical compositions for treating, preventing, or delaying the onset and/or develop of a disease or condition. In some embodiments, the disease or condition is selected from cardiovascular diseases, ischemia, reperfusion injury, cancerous disease, pulmonary hypertension and conditions responsive to nitroxyl therapy.
    Type: Application
    Filed: April 25, 2014
    Publication date: August 21, 2014
    Applicants: Cardioxyl Pharmaceuticals, Inc., The Johns Hopkins University
    Inventors: John P. Toscano, Art Sutton, Vincent Jacob Kalish, Frederick Arthur Brookfield, Stephen Martin Courtney, Lisa Marie Frost
  • Publication number: 20140219989
    Abstract: The present invention provides a compound of Formula (I) as described herein, or a pharmaceutically acceptable salt thereof. The present invention also provides pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing a thromboses, embolisms, hypercoagulability or fibrotic changes.
    Type: Application
    Filed: July 3, 2012
    Publication date: August 7, 2014
    Inventors: Craig Boyle, William Greenlee, Samuel Chackalamannil, Claire Lankin
  • Publication number: 20140213589
    Abstract: The invention relates to hydroxyphenyl derivatives of formula (I); and uses thereof as anti-bacterial and/or anti-parasitic agents.
    Type: Application
    Filed: March 28, 2014
    Publication date: July 31, 2014
    Applicant: FAB PHARMA S.A.S.
    Inventors: Alexis DENIS, Vincent Gerusz, Yannick Bonvin
  • Publication number: 20140206537
    Abstract: This document discloses molecules having the following formula (“Formula One”): and processes associated therewith.
    Type: Application
    Filed: March 25, 2014
    Publication date: July 24, 2014
    Applicant: DOW AGROSCIENCES LLC
    Inventors: James E. Hunter, William C. Lo, Gerald B. Watson, Akshay Patny, Gary D. Gustafson, Dan Pernich, William K. Brewster, Debra L. Camper, Beth Lorsbach, Michael R. Loso, Thomas C. Sparks, Hemant Joshi, Adiraj Mandaleswaran, Ramadevi Sanam, Rambabu Gundla, Pravin S. Iyer
  • Patent number: 8785443
    Abstract: Prodrugs of methyl hydrogen fumarate, pharmaceutical compositions comprising prodrugs of methyl hydrogen fumarate, and methods of using prodrugs of methyl hydrogen fumarate and pharmaceutical compositions thereof for treating diseases such as psoriasis, asthma, multiple sclerosis, inflammatory bowel disease, and arthritis are disclosed.
    Type: Grant
    Filed: October 14, 2011
    Date of Patent: July 22, 2014
    Assignee: XenoPort, Inc.
    Inventors: Archana Gangakhedkar, Xuedong Dai, Noa Zerangue, Peter A. Virsik
  • Publication number: 20140200136
    Abstract: The present invention relates to pesticidal mixtures comprising as active compounds 1) at least one pesticidal active 3-arylquinazolin-4-one compound I of formula (I): wherein R1, R2, R3, R4, k and n are defined in the description; and 2) at least one fungicidal compounds II selected from azoles, strobilurins, carboxamides, carbamates, heterocyclic and various other compounds as defined in the description, in synergistically effective amounts. The invention relates further to methods and use of these mixtures for combating insects, arachnids or nematodes and harmful fungis in and on plants, and for protecting such plants being infested with pests, especially also for protecting seeds.
    Type: Application
    Filed: August 31, 2012
    Publication date: July 17, 2014
    Applicant: BASF SE
    Inventors: Florian Kaiser, Steffen Gross, Egon Haden, Arun Narine
  • Publication number: 20140200197
    Abstract: The compounds encompassed by Formula I include compounds which are HIV protease inhibitors and other compounds which can be metabolized in vivo to HIV protease inhibitors. The compounds and their pharmaceutically acceptable salts are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
    Type: Application
    Filed: September 9, 2013
    Publication date: July 17, 2014
    Inventors: JOHN A. MCCAULEY, CHRISTIAN BEAULIEU, DAVID J. BENNETT, CHRISTOPHER J. BUNGARD, RONALD K. CHANG, SHELDON CRANE, THOMAS J. GRESHOCK, LI HAO, KATE HOLLOWAY, JESSE J. MANIKOWSKI, DANIEL MCKAY, CARMELA MOLINARO, OSCAR MIGUEL MORADEI, PHILIPPE G. NANTERMET, CHRISTIAN NADEAU, TUMMANAPALLI SATYANARAYANA, WILLIAM SHIPE, SANJAY KUMAR SINGH, VOUY LINH TRUONG, SIVALENKA VIJAYARADHI, PETER D. WILLIAMS, CATHERINE M. WISCOUNT
  • Publication number: 20140194416
    Abstract: The invention relates to N-hydroxylsulfonamide derivatives that donate nitroxyl (HNO) under physiological conditions and are useful in treating and/or preventing the onset and/or development of diseases or conditions that are responsive to nitroxyl therapy, including heart failure and ischemia/reperfusion injury. Novel N-hydroxylsulfonamide derivatives release NHO at a controlled rate under physiological conditions, and the rate of HNO release is modulated by varying the nature and location of functional groups on the N-hydroxylsulfonamide derivatives.
    Type: Application
    Filed: March 11, 2014
    Publication date: July 10, 2014
    Applicants: Cardioxyl Pharmaceuticals, Inc., The Johns Hopkins University
    Inventors: John P. Toscano, Frederick Arthur Brookfield, Andrew D. Cohen, Stephen Martin Courtney, Lisa Marie Frost, Vincent Jacob Kalish
  • Publication number: 20140194427
    Abstract: Provided is a compound of formula (I): or a pharmaceutically acceptable salt thereof. Also provided is a method of treating, prophylaxis, or amelioration of a disease, comprising administering to a subject in need of treatment for the disease an effective amount of a compound of formula (I) described herein. In one embodiment, the method is a neurodegenerative disease, such as multiple sclerosis, amyotrophic lateral sclerosis, Parkinson's disease, Huntington's disease, or Alzheimer's disease.
    Type: Application
    Filed: March 7, 2014
    Publication date: July 10, 2014
    Applicant: Biogen IDEC MA Inc.
    Inventor: Jianhua CHAO
  • Patent number: 8772336
    Abstract: This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.
    Type: Grant
    Filed: October 11, 2012
    Date of Patent: July 8, 2014
    Assignees: Merck Frosst Canada Ltd., Axys Pharmaceuticals, Inc.
    Inventors: Christopher I. Bayly, Cameron Black, Serge Leger, Chun Sing Li, Dan McKay, Christophe Mellon, Jacques Yves Gauthier, Vouy-Linh Truong, Cheuk Lau, Michel Therien, Michael J. Green, Bernard L. Hirschbein, James William Janc, James T. Palmer, Chitra I. Baskaran
  • Publication number: 20140179518
    Abstract: The present invention relates to pesticidal mixtures comprising as active components 1) at least one cyanosulfoximine compound I of the formula I wherein R1, R2 and G are defined as in the description; and 2) at least one fungicidal compounds II selected from azoles, strobilurins, carboxamides, carbamates, heterocyclic and various other compounds as defined in the description, in synergistically effective amounts. The invention relates further to methods and use of these mixtures for combating insects, arachnids or nematodes and harmful fungis in and on plants, and for protecting such plants being infested with pests, especially also for protecting seeds.
    Type: Application
    Filed: December 20, 2013
    Publication date: June 26, 2014
    Applicant: BASF SE
    Inventors: Delphine BREUNINGER, Henricus Maria Martinus BASTIAANS, Wolfgang VON DEYN, Matthias POHLMAN, Juergen LANGEWALD, Egon HADEN
  • Publication number: 20140171404
    Abstract: The present invention relates to novel compounds that are autotaxin inhibitors, processes for their preparation, pharmaceutical compositions and medicaments containing them and to their use in the treatment of an ATX-dependent or ATX-mediated disease or condition.
    Type: Application
    Filed: December 17, 2013
    Publication date: June 19, 2014
    Applicant: NOVARTIS AG
    Inventors: Vikki FURMINGER, Owen Rhys HUGHES, Darren Mark LEGRAND, Emily STANLEY, Christopher THOMSON
  • Publication number: 20140171313
    Abstract: This document discloses molecules having the following formula (“Formula One”): and processes associated therewith.
    Type: Application
    Filed: December 18, 2013
    Publication date: June 19, 2014
    Applicant: DOW AGROSCIENCES LLC
    Inventors: William C. Lo, James E. Hunter, Gerald B. Watson, Akshay Patny, Pravin S. Iyer, Joshodeep Boruwa
  • Publication number: 20140171311
    Abstract: This document discloses molecules having the following formula (“Formula One”): and processes associated therewith.
    Type: Application
    Filed: December 18, 2013
    Publication date: June 19, 2014
    Applicant: DOW AGROSCIENCES LLC
    Inventors: William C. Lo, James E. Hunter, Gerald B. Watson, Akshay Patny, Pravin S. Iyer, Joshodeep Boruwa
  • Publication number: 20140171314
    Abstract: This document discloses molecules having the following formula (“Formula One”): and processes associated therewith.
    Type: Application
    Filed: December 18, 2013
    Publication date: June 19, 2014
    Applicant: Dow AgroSciences LLC
    Inventors: William C. Lo, James E. Hunter, Gerald B. Watson, Akshay Patny, Pravin S. Iyer, Joshodeep Boruwa
  • Publication number: 20140171312
    Abstract: This document discloses molecules having the following formula (“Formula One”): and processes associated therewith.
    Type: Application
    Filed: December 18, 2013
    Publication date: June 19, 2014
    Applicant: Dow AgroSciences LLC
    Inventors: William C. Lo, James E. Hunter, Gerald B. Watson, Akshay Patny, Pravin S. Iyer, Joshodeep Boruwa
  • Publication number: 20140171309
    Abstract: This document discloses molecules having the following formula (“Formula One”): and processes associated therewith.
    Type: Application
    Filed: December 18, 2013
    Publication date: June 19, 2014
    Applicant: DOW AGROSCIENCES LLC
    Inventors: William C. Lo, James E. Hunter, Gerald B. Watson, Akshay Patny, Pravin S. Iyer, Joshodeep Boruwa
  • Publication number: 20140171403
    Abstract: The present invention relates to novel compounds that are autotaxin inhibitors, processes for their preparation, pharmaceutical compositions and medicaments containing them and to their use in diseases and disorders mediated by autotaxin.
    Type: Application
    Filed: March 15, 2013
    Publication date: June 19, 2014
    Applicant: Novartis AG
    Inventors: Darren Mark Legrand, Vikki Furminger, Christopher Thomson, Owen Rhys Hughes, Emily Stanley
  • Publication number: 20140171308
    Abstract: This document discloses molecules having the following formula (“Formula One”): and processes associated therewith.
    Type: Application
    Filed: December 18, 2013
    Publication date: June 19, 2014
    Applicant: Dow AgroSciences LLC
    Inventors: William C. Lo, James E. Hunter, Gerald B. Watson, Akshay Patny, Pravin S. Iyer, Joshodeep Boruwa
  • Publication number: 20140171315
    Abstract: This document discloses molecules having the following formula (“Formula One”): and processes associated therewith.
    Type: Application
    Filed: December 18, 2013
    Publication date: June 19, 2014
    Applicant: Dow AgroSciences LLC
    Inventors: William C. Lo, James E. Hunter, Gerald B. Watson, Akshay Patny, Pravin S. Iyer, Joshodeep Boruwa
  • Publication number: 20140155263
    Abstract: Fungicidal mixtures comprising, as active components, 1) azolopyrimidinylamines of the formula I, in which the substituents are as defined in the description and 2) at least one active compound II selected from the following groups: azoles, strobilurins, carboxamides, heterocylic compounds, carbamates and other active compounds selected from the group consisting of guanidines, antibiotics, sulfur-containing heterocyclyl compounds, organophosphorus compounds, organochlorine compounds, inorganic active compounds, growth retardants and cyflufenamid, cymoxanil, dimethirimol, ethirimol, furalaxyl, metrafenone and spiroxamine; in a synergistically effective amount. Methods for controlling harmful fungi using mixtures of the compound I with active compounds II and the use of the compound I with active compounds II for preparing such mixtures, and also compositions comprising these mixtures.
    Type: Application
    Filed: February 10, 2014
    Publication date: June 5, 2014
    Applicant: BASF SE
    Inventors: Christine Beck, Matthias NIEDENBRÜCK, Maria Scherer, Reinhard Stierl, Siegfried Strathmann, Udo HÜNGER
  • Publication number: 20140127322
    Abstract: Disclosed are solid forms of 1-[4-[4-[5-(2,6-difluorophenyl)-4,5-dihydro-3-isoxazolyl]-2-thiazolyl]-1-piperidinyl]-2-[5-methyl-3-(trifluoromethyl)-1H-pyrazol-1-yl]ethanone (Compound 1). Methods for the preparation of solid forms of Compound 1 and for the conversion of one solid form of Compound 1 into another are disclosed. Disclosed are fungicidal compositions comprising a fungicidally effective amount of a solid form of Compound 1 and at least one additional component selected from the group consisting of surfactants, solid diluents and liquid carriers. Compositions comprising a mixture of a solid form of Compound 1 and at least one other fungicide or insecticide are also disclosed. Also disclosed are methods for controlling plant diseases caused by fungal plant pathogens comprising applying to a plant or portion thereof, or to a plant seed, a fungicidally effective amount of a solid form of Compound 1.
    Type: Application
    Filed: January 13, 2014
    Publication date: May 8, 2014
    Applicant: E I DU PONT DE NEMOURS AND COMPANY
    Inventors: MATTHEW RICHARD OBERHOLZER, ROBERT JAMES PASTERIS
  • Publication number: 20140128398
    Abstract: Compounds, compositions, and formulations, and accompanying methods useful for treating disorders arising from oxidative DNA damage, including oxidative DNA damage resulting from ionizing radiation or other therapy are described herein.
    Type: Application
    Filed: June 1, 2012
    Publication date: May 8, 2014
    Applicant: INDIANA UNIVERSITY RESEARCH AND TECHNOLOGY CORPORATION
    Inventors: Mark R. Kelley, Michael R. Vasko
  • Patent number: 8715709
    Abstract: Biocompatible intraocular implants include a beta adrenergic receptor antagonist and a polymer associated with the beta adrenergic receptor antagonist to facilitate release of the beta adrenergic receptor antagonist into an eye for an extended period of time. The beta adrenergic receptor antagonist may be associated with a biodegradable polymer matrix, such as a matrix of a two biodegradable polymers. The implants may be placed in an eye to treat one or more ocular conditions, such as an ocular neuropathies, for example, various forms of glaucoma.
    Type: Grant
    Filed: November 29, 2010
    Date of Patent: May 6, 2014
    Assignee: Allergan, Inc.
    Inventors: Glenn T. Huang, Thierry Nivaggioli
  • Patent number: 8710272
    Abstract: The present invention includes compounds, pharmaceuticals and cosmetics having at least one (substituted phenyl)-propenal moiety. The compounds and compositions of the present invention are useful in the treatment or prevention of medical conditions including androgen associated conditions, androgen associated inflammation, a wound (the compounds assist with wound healing), acne, rheumatoid arthritis, psoriasis, rosacea, and alopecia; Kennedy's disease (spinal and bulbar muscular atrophy, or SBMA), polyglutamine-mediated motor neuron degeneration; cancers such as prostate cancer, bladder cancer, breast cancer, ovarian cancer, hepatocellular (liver) cancer, and pancreatic cancer; and other medical conditions described herein. Treatment of such medical conditions includes administering to an individual suffering from a medical condition describe herein, a therapeutically effective amount of any of the disclosed compounds, their derivatives, or pharmaceutical compositions thereof.
    Type: Grant
    Filed: June 18, 2012
    Date of Patent: April 29, 2014
    Assignee: Androscience Corporation
    Inventors: Charles C. Y. Shih, Qian Shi, Hui-Kang Wang, Ching-Yuan Su
  • Publication number: 20140100227
    Abstract: Disclosed herein are novel C17-alkanediyl and alkenediyl derivatives of oleanolic acid, including those of the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds. Methods and intermediates useful for making the compounds, and methods of using the compounds, for example, as antioxidant inflammation modulators, and compositions thereof are also provided.
    Type: Application
    Filed: September 10, 2013
    Publication date: April 10, 2014
    Applicant: REATA PHARMACEUTICALS, INC.
    Inventors: Christopher F. BENDER, Xin JIANG, Eric ANDERSON, Melean VISNICK
  • Publication number: 20140100224
    Abstract: The present application is related to compounds which are novel neurotrophin mimetics. The application also discloses the treatment of disorders associated with p75 expression, such as degradation or dysfunction of cells expressing p75 in a mammal by administering an effective amount of such compounds.
    Type: Application
    Filed: June 26, 2013
    Publication date: April 10, 2014
    Applicants: The University of North Carolina at Chapel Hill, U.S. Government represented by the Department of Veterans Affairs, The Regents of the University of California
    Inventors: Frank M. Longo, Stephen M. Massa
  • Patent number: 8691977
    Abstract: Chemical entities which are triterpenoid derivatives, pharmaceutical compositions and methods of treatment of inflammatory, neurodegenerative, neoplastic and autoimmune diseases are described.
    Type: Grant
    Filed: August 22, 2011
    Date of Patent: April 8, 2014
    Assignee: Neupharma, Inc.
    Inventors: Xiangping Qian, Yong-Liang Zhu
  • 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: 20140094464
    Abstract: The invention described herein pertains to compounds and compositions for treating Ape1 mediated diseases. In particular, the invention described herein pertains to quinone compounds and pharmaceutical compositions containing them for treating Ape1 mediated diseases.
    Type: Application
    Filed: May 25, 2012
    Publication date: April 3, 2014
    Applicant: INDIANA UNIVERSITY RESEARCH AND TECHNOLOGY CORPORATION
    Inventors: Mark R. Kelley, James H. Wikel
  • Publication number: 20140088074
    Abstract: Fluorinated arylalkylaminocarboxamide derivatives of formula (I) are described wherein W, J, n, R1, R2, R3, R4, R5 and R6 have the meanings as defined in the specification and pharmaceutically salts thereof, pharmaceutical compositions containing them as active ingredients and their use as sodium and/or calcium channel modulators useful in preventing, alleviating and curing a wide range of pathologies, including neurological, psychiatric, cardiovascular, inflammatory, ophthalmic, urological, and gastrointestinal diseases, where the above mechanisms have been described as playing a pathological role.
    Type: Application
    Filed: May 29, 2012
    Publication date: March 27, 2014
    Applicant: NEWRON PHARMACEUTICALS S.P.A.
    Inventor: Paolo Pevarello
  • Patent number: 8680100
    Abstract: The present invention is directed to compounds represented by structural formula (I), or a pharmaceutically acceptable salt or a transition metal chelate, coordinate or complex thereof or a transition metal chelate, coordinate or complex of a deprotonated form of the compound. Pharmaceutical composition and method of use for these compounds are also included.
    Type: Grant
    Filed: December 1, 2009
    Date of Patent: March 25, 2014
    Assignee: Synta Pharmaceuticals Corp.
    Inventors: Jun Jiang, Teresa Kowalczyk-Przewloka, Stefan M. Schweizer, Zhi-Qiang Xia, Shoujun Chen, Christopher Borella, Lijun Sun
  • Publication number: 20140080832
    Abstract: Compounds which directly inhibit IRE-1? activity in vitro, prodrugs, and pharmaceutically acceptable salts thereof. Such compounds and prodrugs are useful for treating diseases associated with the unfolded protein response and can be used as single agents or in combination therapies.
    Type: Application
    Filed: November 13, 2013
    Publication date: March 20, 2014
    Applicant: MANNKIND CORPORATION
    Inventors: John Bruce PATTERSON, David Gregory LONERGAN, Gary A. FLYNN, Qingping ZENG, Peter V. PALLAI
  • Patent number: 8642596
    Abstract: Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain novel semicarbazides, sulfonyl carbazides, ureas and related compounds in therapeutically effective amounts are disclosed. Methods for preparing the compounds and methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by hemorrhagic fever viruses is disclosed, i.e., including but not limited to Arenaviridae (Junin, Machupo, Guanavito, Sabia and Lassa), Filoviridae (ebola and Marburg viruses), Flaviviridae (yellow fever, omsk hemorrhagic fever and Kyasanur Forest disease viruses), and Bunyaviridae (Rift Valley fever).
    Type: Grant
    Filed: December 6, 2005
    Date of Patent: February 4, 2014
    Assignee: Siga Technologies, Inc.
    Inventors: Yijun Deng, Theodore J. Nitz, Thomas R. Bailey, Yuanming Zhang, Sylvie Laquerre
  • Publication number: 20140011807
    Abstract: The present invention provides a nitrogen-containing saturated heterocyclic compound of the formula [I]: wherein R1 is a cycloalkyl group and the like, R22 is an optionally substituted aryl and the like, R is a lower alkyl and the like, T is a carbonyl group, Z is —O— and the like, and R3 to R6 are the same or different and a hydrogen atom and the like; or a pharmaceutically acceptable salt, that is useful as a renin inhibitor.
    Type: Application
    Filed: March 15, 2012
    Publication date: January 9, 2014
    Applicants: SHANGHAI PHARMACEUTICALS HOLDING CO., LTD., MITSUBISHI TANABE PHARMA CORPORATION
    Inventors: Toru Iijima, Hiroshi Sugama, Takayuki Kawaguchi, Jingkang Shen, Guangxin Xia, Jianshu Xie
  • Publication number: 20140005175
    Abstract: Compounds of formula II are described: wherein D, n, Ra, Rb, and Rc are as herein defined, along with pharmaceutical compositions and methods of using compounds of formula II for treating or reducing the risk of peritoneal carcinomatosis in a patient.
    Type: Application
    Filed: August 26, 2013
    Publication date: January 2, 2014
    Applicants: Cephalon, Inc., University of Utah Research Foundation, University of Hawaii
    Inventors: Bruce D. Dorsey, Scott K. Kuwada, Jay P. Theroff, Craig A. Zificsak
  • Publication number: 20130345213
    Abstract: Compounds of Formula (I) along with processes for their preparation that are useful for treating, managing and/or lessening the diseases, disorders, syndromes or conditions associated with the modulation of calcium sensing (CaSR) receptors. Methods of treating, managing and/or lessening the diseases, disorders, syndromes or conditions associated with the modulation of calcium sensing (CaSR) receptors of Formula (I).
    Type: Application
    Filed: March 9, 2012
    Publication date: December 26, 2013
    Applicant: LUPIN LIMITED
    Inventors: Manojkumar Ramprasad Shukla, Vinod Dinkar Chaudhari, Majid Bashir Sayyed, Ramesh Dattatraya Phadtare, Navnath Bajirao Walke, Sanjeev Anant Kulkarni, Venkata P. Palle, Rajender Kumar Kamboj
  • Publication number: 20130338160
    Abstract: The present invention includes compounds, pharmaceuticals and cosmetics having at least one (substituted phenyl)-propenal moiety. The compounds and compositions of the present invention are useful in the treatment or prevention of medical conditions including androgen associated conditions, androgen associated inflammation, a wound (the compounds assist with wound healing), acne, rheumatoid arthritis, psoriasis, rosacea, and alopecia; Kennedy's disease (spinal and bulbar muscular atrophy, or SBMA), polyglutamine-mediated motor neuron degeneration; cancers such as prostate cancer, bladder cancer, breast cancer, ovarian cancer, hepatocellular (liver) cancer, and pancreatic cancer; and other medical conditions described herein. Treatment of such medical conditions includes administering to an individual suffering from a medical condition describe herein, a therapeutically effective amount of any of the disclosed compounds, their derivatives, or pharmaceutical compositions thereof.
    Type: Application
    Filed: June 18, 2013
    Publication date: December 19, 2013
    Inventors: Charles SHIH, Qian Shi, Hui-kang Wang
  • Publication number: 20130324539
    Abstract: Improved methods of treating multiple sclerosis and/or psoriasis using prodrugs of methyl hydrogen fumarate are disclosed. The methods comprise administering certain prodrugs of methyl hydrogen fumarate. The methods are able to achieve high blood plasma concentrations of the active metabolite, methyl hydrogen fumarate, without causing significant gastrointestinal irritation. New prodrugs of methyl hydrogen fumarate are also disclosed.
    Type: Application
    Filed: May 30, 2013
    Publication date: December 5, 2013
    Inventors: Peter A. Virsik, David J. Wustrow, Thamil Annamalai
  • Publication number: 20130316906
    Abstract: The invention relates to novel compounds of the formula (I) in which R1, R2, R3, R4, R5, Y, Q and G have the meanings given above, to a plurality of processes and intermediates for their preparation and to their use as herbicides and/or pesticides. Moreover, the invention relates to selective herbicidal compositions comprising, firstly, the phenyl-substituted bicyclooctane-1,3-dione derivates and, secondly, a crop plant compatibility-improving compound. The present invention furthermore relates to increasing the activity of crop protection compositions comprising in particular phenyl-substituted bicyclooctane-1,3-dione derivates by adding ammonium salts or phosphonium salts and, if appropriate, penetrants, to the corresponding compositions, to processes for their preparation and to their use in crop protection as pesticides and/or for preventing unwanted plant growth.
    Type: Application
    Filed: October 28, 2011
    Publication date: November 28, 2013
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Alfred Angermann, Stefan Lehr, Guido Bojack, Reiner Fischer, Isolde Häuser-hahn, Ines Heinemann, Elmar Gatzweiler, Christopher Hugh Rosinger, Arnd Voerste, Dieter Feucht
  • Patent number: 8592486
    Abstract: The invention relates to compounds of structural formulas (I), (VII) and (XI): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, wherein X1, X2, X3, Y, Z, L, R1, R2, R3, R18 and n are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.
    Type: Grant
    Filed: May 14, 2012
    Date of Patent: November 26, 2013
    Assignee: Synta Pharmaceuticals Corp.
    Inventors: Lijun Sun, Shoujun Chen, Zhi-Qiang Xia, Jun Jiang, Yu Xie, Junyi Zhang
  • Publication number: 20130274240
    Abstract: The present invention provides an agent for the prophylactic or treatment of diabetes, diabetic complications, insulin resistance syndrome, metabolic syndrome, hyperglycemia, dyslipidemia, atherosclerosis, cardiac failure, cardiomyopathy, myocardial ischemia, brain ischemia, cerebral apoplexy, pulmonary hypertension, hyperlactacidemia, mitochondrial disease, mitochondrial encephalomyopathy or cancer, namely, a PDHK inhibitor and the like. A compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, or a solvate thereof: wherein each symbol is as defined in the specification.
    Type: Application
    Filed: November 5, 2012
    Publication date: October 17, 2013
    Inventor: JAPAN TOBACCO INC.
  • Publication number: 20130261121
    Abstract: The present invention includes compounds, pharmaceuticals and cosmetics having at least one (substituted phenyl)-propenal moiety. The compounds and compositions of the present invention are useful in the treatment or prevention of medical conditions including androgen associated conditions, androgen associated inflammation, a wound (the compounds assist with wound healing), acne, rheumatoid arthritis, psoriasis, rosacea, and alopecia; Kennedy's disease (spinal and bulbar muscular atrophy, or SBMA), polyglutamine-mediated motor neuron degeneration; cancers such as prostate cancer, bladder cancer, breast cancer, ovarian cancer, hepatocellular (liver) cancer, and pancreatic cancer; and other medical conditions described herein. Treatment of such medical conditions includes administering to an individual suffering from a medical condition describe herein, a therapeutically effective amount of any of the disclosed compounds, their derivatives, or pharmaceutical compositions thereof.
    Type: Application
    Filed: June 18, 2012
    Publication date: October 3, 2013
    Inventors: Charles C.Y. SHIH, Qian Shi, Hui-Kang Wang, Ching-Yuan Su
  • Publication number: 20130244962
    Abstract: Several parasites responsible for mammalian diseases are dependent on cysteine protease for various life-cycle functions. Inhibition or decreasing function of these proteases can be useful in the treatment and/or prevention of these parasitic diseases including; toxoplasmosis, malaria, African trypanosomiasis, Chagas disease, leishmaniasis, schistosomiasis, amebiasis, giardiasis, clonorchiasis, opisthorchiasis, paragonimiasis, fasciolopsiasis, lymphatic filariasis, onchocerciasis, dracunculiasis, ascariasis, trichuriasis, stronglyoidiasis, trichostrongyliasis, trichomoniasis or cestodiasis.
    Type: Application
    Filed: April 11, 2013
    Publication date: September 19, 2013
    Applicant: Merck Frosst Canada Ltd.
    Inventors: Elise ISABEL, Christopher MELLON, Christian BEAULIEU