1,2,4-thiadiazoles (including Hydrogenated) Patents (Class 548/128)
  • Patent number: 9920039
    Abstract: The present invention relates to new oxazolidinone compounds of general formula (I) having antibiotic activity even against multiresistant bacterial strains (I).
    Type: Grant
    Filed: March 17, 2014
    Date of Patent: March 20, 2018
    Assignees: UNIVERSITÀ DEGLI STUDI DI MILANO—BICOCCA, ISTITUTO EURO MEDITERRANEO DI SCIENZA E TECNOLOGIA
    Inventors: Rosario Musumeci, Clementina Elvezia Anna Cocuzza, Cosimo Gianluca Fortuna, Andrea Pace, Antonio Palumbo Piccionello
  • Patent number: 9125410
    Abstract: Compositions and processes for controlling nematodes are described herein, e.g., nematodes that infest plants or animals. The compounds include oxazoles, oxadiazoles and thiadiazoles.
    Type: Grant
    Filed: April 3, 2013
    Date of Patent: September 8, 2015
    Assignee: Monsanto Technology LLC
    Inventors: Deryck J. Williams, Matt W. Dimmic, William P. Haakenson, Al Wideman, Barry J. Shortt, Tim Cheeseright, Michael J. Crawford
  • Patent number: 9044013
    Abstract: The present invention provides a glyoxime derivative displaying excellent pesticidal effect or a salt thereof and a pesticide containing the same as an active ingredient. This pesticide is characterized by containing as an active ingredient, a glyoxime derivative expressed by the general formula [I] (in which X represents a cyano group or a carbamoyl group, R1 represents a C1˜C8 alkyl group, a C3˜C6 cycloalkyl C1˜C6 alkyl group, etc, and R2 represents a hydrogen atom, a C1˜C8 alkyl group, a C3˜C6 cycloalkyl C1˜C6 alkyl group, etc.) or an agriculturally acceptable salt thereof.
    Type: Grant
    Filed: November 19, 2012
    Date of Patent: June 2, 2015
    Assignees: KUMIAI CHEMICAL INDUSTRY CO., LTD., IHARA CHEMICAL INDUSTRY CO., LTD.
    Inventors: Shunichirou Fukumoto, Daisuke Shikama, Toshihiro Nagata, Katsuya Kato, Kei Kawamoto, Masaaki Komatsu, Takeshi Matsuda, Seisuke Ito
  • Patent number: 9012443
    Abstract: The present invention provides compounds of Formula I, or pharmaceutically acceptable salts thereof, that are inhibitors of voltage-gated sodium channels, in particular Nav 1.7. The compounds are useful for the treatment of diseases treatable by inhibition of sodium channels such as pain disorders. Also provided are pharmaceutical compositions containing compounds of the present invention.
    Type: Grant
    Filed: December 6, 2012
    Date of Patent: April 21, 2015
    Assignee: Amgen Inc.
    Inventors: Christiane Boezio, Howard Bregman, James R. Coats, Erin F. Dimauro, Thomas Dineen, Bingfan Du, Russell Graceffa, Charles Kreiman, Daniel La, Isaac E. Marx, Nagasree Chakka, Hanh Nho Nguyen, Emily Anne Peterson, Matthew Weiss, Katrina W. Copeland, Holly L. Deak, Alessandro Boezio
  • Patent number: 8987265
    Abstract: Compounds of Formula I, including pharmaceutically acceptable salts thereof, as well as compositions containing these compounds, have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV:
    Type: Grant
    Filed: November 7, 2013
    Date of Patent: March 24, 2015
    Assignee: Bristol-Myers Squibb Company
    Inventors: Tao Wang, Zhiwei Yin, Paul Michael Scola
  • Publication number: 20150038483
    Abstract: The present invention is related to a compound represented by formula (I) wherein R1 is a hydrogen atom, substituted or unsubstituted alkyl, substituted or unsubstituted aromatic carbocyclyl, or the like; X is —N(R3)—, —O—, or —S—; Y is ?C(R4)—, or ?N—; Z is —N(R7)—, —O—, or —S—; R2 is substituted or unsubstituted alkyloxy, or the like, or a group represented by the following formula: —(CR2aR2b)n—R2c, wherein R2a is each independently a hydrogen atom, halogen, or the like; R2b is each independently a hydrogen atom, halogen, or the like; R2a and R2b which are attached to the same carbon atom may be taken together to form oxo, a substituted or unsubstituted non-aromatic carbocycle, or the like; two of R2a which are attached to the adjacent carbon atoms and/or two of R2b which are attached to the adjacent carbon atoms may be taken together to form a bond; R2c is substituted or unsubstituted aromatic carbocyclyl, or the like; n is an integer from 1 to 3; R3 and R7 are each independently a hydrogen atom, sub
    Type: Application
    Filed: March 26, 2013
    Publication date: February 5, 2015
    Inventors: Akira Yukimasa, Naotake Kobayashi, Kenji Takaya, Yoshio Hato
  • Publication number: 20150018551
    Abstract: Disclosed herein are therapeutic agents and/or preventive agents for pain or therapeutic agents and/or preventive agents for a sodium channel associated disease.
    Type: Application
    Filed: September 30, 2014
    Publication date: January 15, 2015
    Inventors: Tsuyoshi Shinozuka, Hiroyuki Kobayashi, Sayaka Suzuki, Kyosuke Tanaka, Hiroko Kimoto, Yuki Domon
  • Patent number: 8901156
    Abstract: Disclosed are compounds having the formula: wherein X1, X2, X3, R1, R2, R3, R4, Y, A, Z, L and n are as defined herein, and methods of making and using the same.
    Type: Grant
    Filed: January 13, 2011
    Date of Patent: December 2, 2014
    Assignee: Tempero Pharmaceuticals, Inc.
    Inventors: Erkan Baloglu, Shomir Ghosh, Mercedes Lobera, Darby Schmidt
  • Patent number: 8889741
    Abstract: Disclosed herein are therapeutic agents and/or preventive agents for pain or therapeutic agents and/or preventive agents for a sodium channel associated disease.
    Type: Grant
    Filed: January 31, 2013
    Date of Patent: November 18, 2014
    Assignee: Daiichi Sankyo Company, Limited
    Inventors: Tsuyoshi Shinozuka, Hiroyuki Kobayashi, Sayaka Suzuki, Kyosuke Tanaka, Hiroko Kimoto, Yuki Domon
  • Publication number: 20140330011
    Abstract: Provided are compounds of Formula I: or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, R7, X, Z1, Z2, Z3, Z4 and m are as defined herein. Also provided is a pharmaceutically acceptable composition comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof. Also provided are methods of using a compound of Formula I, or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: May 6, 2014
    Publication date: November 6, 2014
    Applicant: 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
  • Publication number: 20140315933
    Abstract: The present invention relates to new sulfonamide URAT-1 inhibitor compounds of formula (I) or pharmaceutically acceptable salts thereof: to compositions containing them, to processes for their preparation and to intermediates used in such processes and to methods of treatment; wherein R1, R2, R3, R4, R5 and R6 are as defined in the description.
    Type: Application
    Filed: April 17, 2014
    Publication date: October 23, 2014
    Applicant: PFIZER LIMITED
    Inventors: Robert McKenzie Owen, Robert Ian Storer
  • Publication number: 20140303143
    Abstract: Disclosed are compounds of Formula (A) or a salt thereof, wherein “Het”, Ra, and Rb are defined herein, which have properties for blocking Nav 1.7 ion channels found in peripheral and sympathetic neurons. Also described are pharmaceutical formulations comprising the compounds of Formula (A) or their salts, and methods of treating neuropathic pain disorders using the same.
    Type: Application
    Filed: October 26, 2012
    Publication date: October 9, 2014
    Inventors: Mark E. Layton, Joseph E. Pero, Hannah Fiji, Michael J. Kelly, III, Pablo de Leon, Michael A. Rossi, Kevin F. Gilbert, Anthony J. Roecker, Zhijian Zhao, Swati I P. Mercer, Scott Wolkenberg, James Mulhearn, Lianyun Zhao, Dansu Li
  • Publication number: 20140296245
    Abstract: This invention is directed to benzensulfonamide compounds, as stereoisomers, enantiomers, tautomers thereof or mixtures thereof; or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the treatment of sodium channel-mediated diseases or conditions, such as pain.
    Type: Application
    Filed: October 30, 2012
    Publication date: October 2, 2014
    Inventors: Shaoyi Sun, Alla Yurevna Zenova, Mikhail Chafeev, Qi Jia, Zaihui Zhang, Renata Marcella Oballa
  • Publication number: 20140274999
    Abstract: Provided herein is a method for the synthesis of cephalosporin antibiotic compounds comprising the conversion of a protected 7-amino group into a 7-carboxamide moiety in a single step.
    Type: Application
    Filed: March 14, 2014
    Publication date: September 18, 2014
    Inventors: Jan-Ji Lai, Pradip M. Pathare, Laxma Kolla, Adrien F. Soret
  • Publication number: 20140256736
    Abstract: This invention is directed to biaryl ether sulfonamides, or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain.
    Type: Application
    Filed: October 30, 2012
    Publication date: September 11, 2014
    Applicant: XENON PHARMACEUTICALS INC.
    Inventors: Shifeng Liu, Thilo Focken, Navjot Chahal, Zaihui Zhang, Renata Marcella Oballa, Julia Fonarev
  • Publication number: 20140256707
    Abstract: The present invention provides compounds of Formula I or II, or pharmaceutically acceptable salts thereof, that are inhibitors of voltage-gated sodium channels, in particular Nav 1.7. The compounds are useful for the treatment of diseases treatable by inhibition of channels such as pain disorders. Also provided are pharmaceutical compositions containing compounds of the present invention.
    Type: Application
    Filed: August 16, 2012
    Publication date: September 11, 2014
    Applicant: AMGEN INC.
    Inventors: Thomas Dineen, Isaac E. Marx, Hanh Nho Nguyen, Matthew Weiss
  • Patent number: 8815910
    Abstract: Compounds having activity as phosphate transport inhibitors, more specifically, inhibitors of intestinal apical membrane Na/phosphate co-transport, are disclosed. The compounds have the following structure (I): including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein X, Y and A are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
    Type: Grant
    Filed: January 4, 2013
    Date of Patent: August 26, 2014
    Assignee: Ardelyx, Inc.
    Inventors: Jason G. Lewis, Jeffrey W. Jacobs, Nicholas Reich, Michael R. Leadbetter, Noah Bell, Han-Ting Chang, Tao Chen, Marc Navre, Dominique Charmot, Christopher Carreras, Eric Labonte
  • Publication number: 20140199263
    Abstract: The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.
    Type: Application
    Filed: August 16, 2012
    Publication date: July 17, 2014
    Inventors: Casey Cameron McComas, Nigel J. Liverton, Joerg Habermann, Uwe Koch, Frank Narjes, Peng Li, Xuanjia Peng, Richard Soll, Hao Wu, Anandan Palani, Xing Dai, Hong Liu, Shuwen He, Zhong Lai, Qun Dang, Nicolas Zorn
  • Publication number: 20140155597
    Abstract: The purpose of the present invention is to provide a novel compound which has an anti-fungal activity on pathogenic fungi including fungi belonging to the genus Candida, the genus Aspergillus and the genus Trichophyton and is useful as a medicinal agent.
    Type: Application
    Filed: July 27, 2012
    Publication date: June 5, 2014
    Applicants: TOYAMA CHEMICAL CO., LTD., TAISHO PHARMACEUTICAL CO., LTD.
    Inventors: Tetsuya Tanikawa, Yasunobu Ushiki, Fumihito Ushiyama, Toru Yamaguchi, Naoya Ono, Keiko Yamamoto, Risa Tsuruta, Yasuhiro Tsutsui, Noritomo Fujino, Ayumu Mori
  • Publication number: 20140135332
    Abstract: The present invention provides compounds of Formula (I): and salts, racemates, isomers, diastereoisomers, enantiomers, hydrates, solvates, N-oxides, pharmaceutically acceptable derivatives or prodrugs thereof. Also provided the use of these compounds as antibacterials, compositions comprising them and processes for their manufacture.
    Type: Application
    Filed: April 20, 2012
    Publication date: May 15, 2014
    Applicant: BIOTA SCIENTIFIC MANAGEMENT PTY LTD
    Inventors: David John Haydon, Lloyd George Czaplewski, Neil Robert Stokes, David Davies, Ian Collins, James T Palmer, Jeffrey Peter Mitchell, Gary Robert William Pitt, Daniel Offermann
  • Publication number: 20140100108
    Abstract: 3-Phenylisoxazoline-5-carboxamides and 3-phenylisoxazoline-5-thioamides of the formula (I) and their use as herbicides and fungicides are described. In this formula (I), X, X2 to X6, R1 to R4 are radicals such as hydrogen, halogen and organic radicals such as substituted alkyl. A is a bond or a divalent unit. Y is a chalcogen.
    Type: Application
    Filed: March 26, 2012
    Publication date: April 10, 2014
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Lothar Willms, Monika H. Schmitt, Thomas Frenzel, Klaus Bernhard Haaf, Isolde Haeuser-Hahn, Ines Heinemann, Elmar Gatzweiler, Christopher Hugh Rosinger, Jan Dittgen, Dieter Feucht, Jeffrey Martin Hills, Philippe Rinolfi, Heinz KEHNE
  • Patent number: 8680159
    Abstract: Substituted benzamide compounds corresponding to formula (I) in which R5, R6, R7, R8, a, b, c, d, t, D and X have defined meanings, a process for their preparation, pharmaceutical compositions comprising such compounds, and a method of using such compounds to treat pain and other conditions mediated at least in part via the bradykinin 1 receptor.
    Type: Grant
    Filed: September 22, 2011
    Date of Patent: March 25, 2014
    Assignee: Gruenenthal GmbH
    Inventors: Melanie Reich, Stefan Schunk, Ruth Jostock, Jean De Vry, Christa Kneip, Tieno Germann, Michael Engels
  • Publication number: 20140051862
    Abstract: This invention provides new compounds having NPY Y5 antagonistic activity. The present inventors found that a compound of the formula (I): wherein R1 is substituted or unsubstituted alkyl or the like; p, q and r are each independently 0 or 1; ring A is oxadiazole; and R2 is substituted or unsubstituted alkyl or the like, has NPY Y5 antagonistic activity.
    Type: Application
    Filed: April 25, 2012
    Publication date: February 20, 2014
    Applicant: Shionogi & Co., Ltd.
    Inventors: Kyohei Hayashi, Yuusuke Tamura, Naoki Omori
  • Publication number: 20140045862
    Abstract: Disclosed herein are therapeutic agents and/or preventive agents for pain or therapeutic agents and/or preventive agents for a sodium channel associated disease.
    Type: Application
    Filed: January 31, 2013
    Publication date: February 13, 2014
    Applicant: Daiichi Sankyo Company, Limited
    Inventor: Daiichi Sankyo Company, Limited
  • Patent number: 8629157
    Abstract: Compounds which modulate the CB2 receptor are disclosed. Compounds according to the invention bind to and are agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain (I).
    Type: Grant
    Filed: December 15, 2009
    Date of Patent: January 14, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Angela Berry, Rajashekhar Betageri, Eugene Richard Hickey, Someina Khor, Doris Riether, Lifen Wu, Renee M. Zindell
  • Publication number: 20130338111
    Abstract: The present invention relates to compounds of the formula and pharmaceutically acceptable salts, solvates or tautomers thereof, to processes for the preparation of, intermediates used in the preparation of, and compositions containing such compounds, and the uses of such compounds, in particular for the treatment of pain.
    Type: Application
    Filed: August 16, 2013
    Publication date: December 19, 2013
    Applicants: Icagen, Inc., Pfizer Limited
    Inventors: Serge Beaudoin, Michael Christopher Laufersweiler, Christopher John Markworth, Brian Edward Marron, David Simon Millan, David James Rawson, Steven Michael Reister, Kosuke Sasaki, Robert Ian Storer, Paul Anthony Stupple, Nigel Alan Swain, Christopher William West, Shulan Zhou
  • Publication number: 20130289057
    Abstract: The invention relates to N-arylaminomethylenebenzothiophenones of General Formula (I) for use as a drug for the treatment of cardiovascular diseases: wherein E is S, O, or CH2, D is CH or NH, and Ar is a phenyl or naphtyl moiety substituted by an electron-withdrawing group, an unsubstituted heteroaryl residue, or a heteroaryl residue substituted by alkyl or an electron-withdrawing group.
    Type: Application
    Filed: January 12, 2012
    Publication date: October 31, 2013
    Applicants: FORSCHUNGSVERBUND BERLIN E.V., MAX-DELBRUCK-CENTRUM FUR MOLEKULARE MEDIZIN
    Inventors: Enno Klussmann, Walter Rosenthal, Jelena Milic, Martin W. Bergmann
  • Patent number: 8546563
    Abstract: Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.
    Type: Grant
    Filed: October 30, 2008
    Date of Patent: October 1, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Angela Berry, Doris Riether, Renee M. Zindell, Nigel James Blumire
  • Publication number: 20130252944
    Abstract: The present invention relates to novel compounds of Formula (I), wherein M, A and Y are defined as in Formula (I); invention compounds are modulators of metabotropic glutamate receptors—subtype 4 (“mGluR4”) which are useful for the treatment or prevention of central nervous system disorders as well as other disorders modulated by mGluR4 receptors. The invention is also directed to pharmaceutical compositions and the use of such compounds in the manufacture of medicaments, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR4 is involved.
    Type: Application
    Filed: July 11, 2011
    Publication date: September 26, 2013
    Inventors: Christelle Bolea, Sylvain Celanire, Lam Tang, Philip Jones, Nigel J. Liverton, Richard Soll, Jingchao Dong, Zhiyu Lei, Fuqing Liu, Yanling Kong, Yi Ju, Haoyong Zhang, Jieping Wei, Qiaoxin Wei, Minxiang Zhang, Yunfu Luo
  • Patent number: 8536226
    Abstract: The present invention is directed to the use of a compound of formula (I) or pharmaceutically acceptable salt thereof, for the treatment of disorders mediated by the melanocortin-5 receptor, particularly dermatological disorders; and further directed to pharmaceutical compositions containing the compound of formula (I) or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: July 11, 2012
    Date of Patent: September 17, 2013
    Assignee: Janssen Pharmaceutica, NV
    Inventors: Magdalena Eisinger, Fa Zhang
  • Publication number: 20130225587
    Abstract: The compound of Formula (I), pharmaceutically acceptable salts thereof, solvates thereof, chelates thereof, non-covalent complexes thereof or produgs of compounds mentioned above or the mixture of any form above mentioned are provided. The use of the compounds in manufacturing a medicament for the treatment and/or prevention of diabetes, obesity and related disorders.
    Type: Application
    Filed: November 9, 2011
    Publication date: August 29, 2013
    Applicants: Zhejiang Beta Pharma Incorporation, Fujian Haixi Pharmaceuticals, Inc.
    Inventors: Xinshan Kang, Wei Long, Cunbo Ma, Yanping Wang, Xiaoyan Shen, Yunyan Hu, Fenlai Tan, Yinxiang Wang
  • Patent number: 8513289
    Abstract: Compounds described by the chemical formula (I) or pharmaceutically acceptable salts thereof: Formula (I); are inhibitors of p38 and are useful in the treatment of inflammation such as in the treatment of asthma, COPD, ARDS, rheumatoid arthritis, rheumatoid spondylitis, osteoarthritis, gouty arthritis and other arthritic conditions; inflamed joints, eczema, psoriasis or other inflammatory skin conditions such as sunburn; inflammatory eye conditions including conjunctivitis; pyresis, pain and other conditions associated with inflammation.
    Type: Grant
    Filed: April 26, 2010
    Date of Patent: August 20, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Hiroo Koyama, Soumya P. Sahoo, Ginger Xu-Qiang Yang, Daniel J. Miller
  • Publication number: 20130210807
    Abstract: The present invention describes and claims compounds of the Structural Formula I, Structural Formula II, or Structural Formula III: wherein R1, R2, R3 and R3? are —H or methyl, or R3 and R3 taken together form a double bond, or R3? is —H and R2 and R3 taken together form a spiro-cyclopropyl substituent, R4 is —H or —F, and R5 is —H, methyl, —CI or —Br, Formula II wherein R1 is —H, ethyl-, isopropyl-, cyclopropyl-, methyl- or methoxy-, R4 is —H or —F, and “Y” is: (a) —CH2—; (b) —CR6H-0-CR7R8—, wherein R6, R7, and R8 are independently —H or methyl; (c) —CR6H—N(R9)—CR7R8—, wherein R6, R7, and R8 are independently —H or methyl; (d) —CH2—C(R9)(R10)—C(R7)(R8)—, wherein R7, R8, R9 and R10 are independently —H or -methyl, or both R7 and R8 are —F, R9 and R10 are independently —H or -methyl, or both R9 and R10 are —F, or R9 and R10 taken together are (0=), which together with the carbon to which they are attached forms a carbonyl group.
    Type: Application
    Filed: July 9, 2011
    Publication date: August 15, 2013
    Inventors: Nigel J Liverton, Christelle Boléa, Sylvain Celanire, Yunfu Luo
  • Publication number: 20130210809
    Abstract: The present invention relates to novel compounds of Formula (1), wherein M, A and B are defined as in Formula (I); invention compounds are modulators of metabotropic glutamate receptors-subtype 4 (“mGluR4”) which are useful for the treatment or prevention of central nervous system disorders as well other disorders modulated by mGluR4 receptors. The invention is also directed to pharmaceutical compositions and the use of such compounds in the manufacture of medicaments, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR4 is involved.
    Type: Application
    Filed: July 12, 2011
    Publication date: August 15, 2013
    Inventors: Christelle Boléa, Sylvain Celanire, Cédric Boudou, Lam Tang, Jean-Philippe Rocher, Nigel John Liverton
  • Patent number: 8501791
    Abstract: The present invention is directed to novel 1,2,4-thiadiazol-2-ium derivatives useful as agonists or antagonists of the melanocortin receptor. More particularly, the compounds of the present invention are useful for the treatment of metabolic, CNS and dermatological disorders such as obesity, impaired oral glucose tolerance, elevated blood glucose levels, type II diabetes, Syndrome X, diabetic retinopathy, spinal cord injury, nerve injury, acute neurodegenerative disorders, chronic neurodegenerative disorders, plexopathies, male erectile dysfunction, dry eyes, acne, dry skin, aged skin, seborrheic dermatitis, rosacea, excessive ear wax, meibomian gland disorder, pseudofolliculitis, yeast infections, dandruff, hidradenitis suppurativa, ocular rosacea and eccrine gland disorder.
    Type: Grant
    Filed: July 13, 2010
    Date of Patent: August 6, 2013
    Assignee: Ortho-McNeil Pharamaceutical, Inc.
    Inventors: Magdalena Eisinger, Louis J. Fitzpatrick, Daniel H. Lee, Kevin Pan, Carlos Plata-Salaman, Allen B. Reitz, Virginia L. Smith-Swintosky, Boyu Zhao
  • Patent number: 8501946
    Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof: wherein A is hydrogen, C1-4alkyl, C3-6cycloalkyl, C1-3alkoxy, C1-3alkoxy C1-4alkyl, C1-2fluoroalkyl, halogen, NR6R7, optionally substituted heteroaryl (Het), or optionally substituted phenyl, and R1, R2, R3, R4, R5, R6 and R7 are as defined in the description. The compounds or salts are thought to modulate P2X7 receptor function and to be capable of antagonizing the effects of ATP at the P2X7 receptor. The invention also provides the use of the compound or salt in the treatment or prophylaxis of, for example, inflammatory pain, neuropathic pain, visceral pain, rheumatoid arthritis, osteoarthritis or neurodegenerative disorders.
    Type: Grant
    Filed: April 28, 2010
    Date of Patent: August 6, 2013
    Assignee: Glaxo Group Limited
    Inventors: David Kenneth Dean, Jorge Munoz-Muriedas, Mairi Sime, Jon Graham Anthony Steadman, Rachel Elizabeth Anne Thewlis, Giancarlo Trani, Daryl Simon Walter
  • Publication number: 20130172339
    Abstract: A compound of formula (I), wherein A is S, O or a double bond, and L is a substituted thiazolyl, phenyl or pyridyl. The compound is useful for the treatment of inflammation and cancer.
    Type: Application
    Filed: September 19, 2011
    Publication date: July 4, 2013
    Applicant: KANCERA AB
    Inventors: Styrbjorn Bystrom, Charles Hedgecock, Evert Homan, Thomas Lundback, Jessica Martinsson, Meral Sari, Katarina Farnegardh, Mattias Jonsson
  • Patent number: 8466182
    Abstract: The present invention relates to compounds of Formula I below and their tautomers or pharmaceutically acceptable salts, compositions and methods of uses thereof.
    Type: Grant
    Filed: November 2, 2011
    Date of Patent: June 18, 2013
    Assignees: The J. David Gladstone Institutes, A Testamentary Trust Established Under The Will Of J. David Gladstone, University of Maryland, Baltimore
    Inventors: Paul J. Muchowski, Joseph M. Muchowski, Robert Schwarcz, Paolo Guidetti
  • Publication number: 20130150339
    Abstract: The present invention provides compounds of Formula I, or pharmaceutically acceptable salts thereof, that are inhibitors of voltage-gated sodium channels, in particular Nav 1.7. The compounds are useful for the treatment of diseases treatable by inhibition of sodium channels such as pain disorders. Also provided are pharmaceutical compositions containing compounds of the present invention.
    Type: Application
    Filed: December 6, 2012
    Publication date: June 13, 2013
    Applicant: Amgen Inc.
    Inventor: Amgen Inc.
  • Patent number: 8445499
    Abstract: Bipiperidinyl compounds of the formula: are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. Pharmaceutically acceptable salts and solvates are included as well. The compounds are useful as agonists of the g-protein coupled receptor GPR-119.
    Type: Grant
    Filed: March 21, 2012
    Date of Patent: May 21, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Harold B. Wood, Alan D. Adams, Stanley Freeman, Jason W. Szewczyk, Conrad Santini, Yong Huang
  • Patent number: 8445476
    Abstract: Carbacephem ?-lactam antibiotics having the following chemical structures (I) and (II) are disclosed: including stereoisomers, pharmaceutically acceptable salts, esters and prodrugs thereof, wherein Ar2, R1, R2 and R3 are as defined herein. The compounds are useful for the treatment of bacterial infections, in particular those caused by methicillin-resistant Staphylococcus spp.
    Type: Grant
    Filed: April 21, 2010
    Date of Patent: May 21, 2013
    Assignee: Achaogen, Inc.
    Inventors: Allan S. Wagman, Heinz E. Moser
  • Publication number: 20130109696
    Abstract: The invention relates to sulfonamide derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to new sulfonamide Nav1.7 inhibitors of formula (I) or pharmaceutically acceptable salts thereof, wherein X, Y1, Y2, Z, R1, R2 and R3 are as defined in the description. Nav 1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain.
    Type: Application
    Filed: July 1, 2011
    Publication date: May 2, 2013
    Applicant: Pfizer Limited
    Inventors: Benjamin Scott Greener, Brian Edward Marron, David Simon Millan, David James Rawson, Robert Ian Storer, Nigel Alan Swain
  • Patent number: 8431249
    Abstract: An organic light-emitting device is provided which efficiently emits light with high brightness and has durability. The organic light-emitting device includes a dibenzo[c,g]fluorene compound having two dibenzo[c,g]fluorene skeletons, and has an organic compound layer containing the dibenzo[c,g]fluorene compound.
    Type: Grant
    Filed: October 29, 2009
    Date of Patent: April 30, 2013
    Assignee: Canon Kabushiki Kaisha
    Inventors: Chiaki Nishiura, Jun Kamatani, Shigemoto Abe
  • Patent number: 8410023
    Abstract: Compositions and processes for controlling nematodes are described herein, e.g., nematodes that infest plants or animals. The compounds include oxazoles, oxadiazoles and thiadiazoles.
    Type: Grant
    Filed: October 14, 2010
    Date of Patent: April 2, 2013
    Assignee: Monsanto Technology LLC
    Inventors: Urszula Slomczynska, Matt W. Dimmic, William P. Haakenson, Jr., Al Wideman
  • Patent number: 8410282
    Abstract: This compounds correspond to the formula (I), where: R1 represents and aryl or heteroaryl group optionally substituted by one or more substituents selected from the group consisting of halogen atoms, straight or branched optionally substituted lower alkyl, cycloalkyl, hydroxy, straight or branched, optionally substituted lower alkoxy, cyano, or —CO2R?, wherein R? represents a hydrogen atom or a straight or branched, optionally substituted lower alkyl group; R2 represents a group selected from: a) a straight or branched lower alkyl group substituted by one or more carboxylic groups (—COOH) and optionally substituted by one or more halogen atoms; b) a cycloalkyl group substituted by one or more carboxylic groups (—COOH) and optionally substituted by one or more halogen atoms; c) a straight or branched alkylcycloalkyl or cycloalkylalkyl group substituted by one or more carboxylic groups (—COOH) and optionally substituted by one or more halogen atoms. Formula (I).
    Type: Grant
    Filed: September 30, 2008
    Date of Patent: April 2, 2013
    Assignee: Palobiofarma, S.L.
    Inventors: Lyhen Gonzalez Lio, Juan Alberto Camacho Gomez
  • Patent number: 8410150
    Abstract: A CPT inhibitor compound is represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof: or a pharmaceutically acceptable salt thereof. A pharmaceutical composition comprises a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. A method of treating a subject having cancer comprises administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: March 6, 2008
    Date of Patent: April 2, 2013
    Assignee: University Health Network
    Inventors: Heinz W. Pauls, Peter Brent Sampson, Bryan T. Forrest, Radoslaw Laufer, Yong Liu, Miklos Feher, Yi Yao, Guohua Pan
  • Publication number: 20130072471
    Abstract: Compounds, compositions and methods are provided which are useful in the treatment of diseases through the inhibition of sodium ion flux through voltage-gated sodium channels. More particularly, the invention provides substituted aryl sulfonamides, compositions comprising these compounds, as well as methods of using these compounds or compositions in the treatment of central or peripheral nervous system disorders, particularly pain and chronic pain by blocking sodium channels associated with the onset or recurrence of the indicated conditions. The compounds, compositions and methods of the present invention are of particular use for treating neuropathic or inflammatory pain by the inhibition of ion flux through a voltage-gated sodium channel.
    Type: Application
    Filed: November 15, 2012
    Publication date: March 21, 2013
    Inventors: Brian Edward Marron, Paul Christopher Fritch, Christopher John Markworth, Andrew Thomas Maynard, Nigel Alan Swain
  • Patent number: 8399485
    Abstract: Bipiperidyl compounds of the formula: (I) are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. Pharmaceutically acceptable salts and solvates are included as well. The compounds are useful as agonists of the g-protein coupled receptor GPR-119.
    Type: Grant
    Filed: December 10, 2007
    Date of Patent: March 19, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Harold B. Wood, Alan D. Adams, Stanley Freeman, Jason W. Szewczyk, Conrad Santini, Yong Huang, Ralph T. Mosley
  • Publication number: 20130060025
    Abstract: Provided are compounds of Formula I: or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, R7, X, Z1, Z2, Z3, Z4 and m are as defined herein. Also provided is a pharmaceutically acceptable composition comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof. Also provided are methods of using a compound of Formula I, or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: September 12, 2012
    Publication date: March 7, 2013
    Inventors: Luke W. Ashcraft, Gustave Bergnes, Chihyuan Chuang, Scott Collibee, Pu-Ping Lu, Bradley Morgan, Alex Muci, Xiangping Qian, Jeffrey Warrington, Zhe Yang
  • Patent number: 8389508
    Abstract: The present invention relates to novel compounds having pharmacological activity, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders.
    Type: Grant
    Filed: April 28, 2011
    Date of Patent: March 5, 2013
    Assignee: Glaxo Group Limited
    Inventors: Guanghui Deng, Xichen Lin, Feng Ren, Baowei Zhao