1,2,4-thiadiazoles (including Hydrogenated) Patents (Class 548/128)
  • 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
  • Patent number: 8377574
    Abstract: An organic light-emitting device which has high emission efficiency and high durability even at low drive voltage is provided. An organic light-emitting device including an anode, a cathode, and an organic compound layer which is interposed between the anode and the cathode, wherein the organic compound layer include at least one dibenzo[c,g]fluorene compound represented by the following General Formula (1).
    Type: Grant
    Filed: May 14, 2009
    Date of Patent: February 19, 2013
    Assignee: Canon Kabushiki Kaisha
    Inventors: Shigemoto Abe, Jun Kamatani, Chiaki Nishiura
  • Patent number: 8372982
    Abstract: The present invention relates to a N-(Phenylcycloalkyl)carboxamide or N-(Benzylcycloalkyl)carboxamide or its thiocarboxamide derivative of formula (I) wherein A represents a carbo-linked, unsaturated or partially saturated, substituted or non-substituted 5-membered heterocyclyl group, T represents an oxygen or a sulphur atom, B represents a non aromatic carbocycle that can be substituted by one to four C1-C8-alkyl groups, and X, Z1, Z2 and Z3 represent various substituents; their process of preparation; the preparation of intermediate compounds; their use as fungicide active agents, particularly in the form of fungicide compositions and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions.
    Type: Grant
    Filed: February 16, 2010
    Date of Patent: February 12, 2013
    Assignee: Bayer Cropscience AG
    Inventors: Jurgen Benting, Peter Dahmen, Philippe Desbordes, Stephanie Gary, Marie-Claire Grosjean-Cournoyer, Philippe Rinolfi, Ulrike Wachendorff-Neumann
  • Publication number: 20130030180
    Abstract: Disclosed are compounds and methods for treating neurological and other disorders by administering to a subject in need thereof an effective amount of a compound having binding and/or modulation specificity for GFR? receptor molecules, which can be mimetics of glial-derived neurotrophic factor (GDNF) family ligands (GFLs), GFR?/RET signaling pathway agonists, and/or direct RET agonists (activators).
    Type: Application
    Filed: December 13, 2010
    Publication date: January 31, 2013
    Applicant: GeneCode AS
    Inventors: Mart Saarma, Mati Karelson, Maxim Bespalov, Mehis Pilv
  • Publication number: 20120329811
    Abstract: The present invention relates to novel compounds of Formula (I), wherein X1, X2, X3, X4, Y1, Y2, Y3, Y4, M1, M2, M3, Am and Bn 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: September 6, 2012
    Publication date: December 27, 2012
    Inventors: Christelle Boléa, Sylvain Celanire
  • Patent number: 8334235
    Abstract: The present invention relates to thiadiazolyloxyphenylamidines of the general formula (I), to a process for the preparation thereof, to the use of the amidines according to the invention in combating undesirable microorganisms and to a composition for this purpose comprising the thiadiazolyloxyphenylamidines according to the invention. The invention furthermore relates to a method for combating undesirable microorganisms by application of the compounds according to the invention to the microorganisms and/or to the habitat thereof.
    Type: Grant
    Filed: June 19, 2009
    Date of Patent: December 18, 2012
    Assignee: Bayer Cropscience AG
    Inventors: Pierre Cristau, Jörg Nico Greul, Ulrich Heinemann, Klaus Kunz, Oswald Ort, Thomas Seitz, Arnd Voerste, Peter Dahmen, Ulrike Wachendorff-Neumann, Klaus-Günther Tietjen, Hiroyuki Hadano
  • Patent number: 8324257
    Abstract: This invention relates to inhibitors of mitotic kinesins, particularly KSP, and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing the inhibitors and pharmaceutical compositions in the treatment of various disorders.
    Type: Grant
    Filed: October 3, 2007
    Date of Patent: December 4, 2012
    Assignee: Array Biopharma Inc.
    Inventors: Kateri Ahrendt, Robert Kirk Delisle, Jeremy Hans, Joseph P. Lyssikatos, John E. Robinson, Eli M. Wallace, Qian Zhao
  • Publication number: 20120295897
    Abstract: This invention is directed to spiro-oxindole compounds, as stereoisomers, enantiomers, tautomers thereof or mixtures thereof; 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: July 25, 2012
    Publication date: November 22, 2012
    Applicant: Xenon Pharmaceuticals Inc.
    Inventors: Mikhail Chafeev, Sultan Chowdhury, Lauren Fraser, Jianmin Fu, Jonathan Langille, Shifeng Liu, Jianyu Sun, Shaoyi Sun, Serguei Sviridov, Mark Wood, Alla Yurevna Zenova, Qi Jia, Jean-Jacques Cadieux, Simon J. Gauthier, Amy Frances Douglas, Tom Hsieh, Nagasree Chakka, Zoran Cikojevic
  • Patent number: 8314247
    Abstract: A hydrazone derivative of formula [I]: wherein Ring A is aryl or heteroaryl, Ring T is heteroaryl or heterocycle, R1 and R2 are independently hydrogen atom, halogen atom, cycloalkylsulfonyl, etc., R3 and R4 combine each other together with the adjacent nitrogen atom to form substituted or unsubstituted heterocycle, R5 is hydrogen atom, halogen atom, cyano, nitro, tetrazolyl, etc., and R6 is hydrogen atom, etc.; or a pharmaceutically acceptable salt thereof is useful as a glucokinase activation agent.
    Type: Grant
    Filed: January 9, 2008
    Date of Patent: November 20, 2012
    Assignee: Mitsubishi Tanabe Pharma Corporation
    Inventors: Iwao Takamuro, Kazutoshi Sugawara, Hiroshi Sugama
  • Publication number: 20120289698
    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: April 13, 2012
    Publication date: November 15, 2012
    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: 8309584
    Abstract: A novel sulfur containing heteroaryl-pyrazole compound of formula (I) or a pharmaceutically acceptable salt thereof is effective as a cannabinoid CB1 receptor inverse agonist or antagonist, which is useful for preventing or treating obesity and obesity-related metabolic disorders. The prevention also provide a method for preparing same, a pharmaceutical composition containing same, and a method for preventing or treating obesity and obesity-related metabolic disorders.
    Type: Grant
    Filed: September 25, 2008
    Date of Patent: November 13, 2012
    Assignee: Green Cross Corporation
    Inventors: Jinhwa Lee, Hee Jeong Seo, Min-Ah Kim, Jeongmin Kim, Sung-Han Lee, Myung Eun Jung, Mi-Soon Kim
  • Patent number: 8299103
    Abstract: Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse 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: June 1, 2010
    Date of Patent: October 30, 2012
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Alessandra Bartolozzi, Eugene Richard Hickey, Doris Riether
  • Patent number: 8293919
    Abstract: The present invention provides novel sulfone and sulfoxide substituted heterocyclic urea compounds having useful antibacterial activity. Use of these compounds as pharmaceutical compositions and methods of production are provided.
    Type: Grant
    Filed: July 23, 2008
    Date of Patent: October 23, 2012
    Assignee: Crestone, Inc.
    Inventors: Joseph Guiles, Thale Jarvis, Sarah Strong, Xicheng Sun, Jian Qiu, John C. Rohloff
  • Patent number: 8288403
    Abstract: The invention relates to methods for the treatment of Alzheimer's disease, cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica and Down syndrome which comprise administering a therapeutically effective amount of a compound of formula I wherein R1, R2, R3, V, W, Y, and Z are as defined herein or a pharmaceutically active acid addition salt of such compounds. The invention also relates to a subgenus of such compounds and pharmaceutical compositions containing them, as well as methods for their manufacture.
    Type: Grant
    Filed: November 4, 2009
    Date of Patent: October 16, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Karlheinz Baumann, Erwin Goetschi, Synese Jolidon, Anja Limberg, Thomas Luebbers
  • Publication number: 20120258990
    Abstract: The present invention relates to heterocyclic compounds of formula (I) which have microbiocidal activity, in particular fungicidal activity: formula (I) wherein G1 and G2 are independently O or S; T is —C(R9R10)—, —C(R11)?C(R12)—, —C?C—, NR13 or O; Y1 and Y2 are independently CR14 or N; Q is —C(?O)—N(R15)-z, —C(?S)—N(R16)-z, —C(?O)—O-z, —N(R17)—C(?O)-z, —N(R18)—C(?S)-z, —N(R19)—C(?O)—O-z or —N(R20)—C(?O)—N(R21)-z, in each case z indicates the bond that is connected to R8; n is 1, 2, 3 or 4 when T is —C(R9R10)—, NR13 or O; n is 1, 2, 3 when T is —C(R11)?C(R12)— or —C?C—; R1, R2, R3, R4, R11, R12 and R14 each independently are hydrogen, halogen, cyano, C1-C4alkyl, or C1-C4haloalkyl; R5, R13, R15, R16, R17, R18, R19, R20 and R21 each independently are hydrogen, C1-C4alkyl or C1-C4alkoxy; R6 and R7 each independently are hydrogen, halogen, cyano, hydroxy, C1-C4alkyl, C1-C4alkoxy, C1-C4alkylthio, C1-C4haloalkyl, C1-C4haloalkoxy, C1-C4haloalkylthio or together from a carbonyl group (?O); R9 and R10 each independent
    Type: Application
    Filed: November 25, 2010
    Publication date: October 11, 2012
    Applicant: SYNGENTA CROP PROTECTION, LLC
    Inventors: Sarah Sulzer, Clemens Lamberth
  • Publication number: 20120225879
    Abstract: The present invention is based on the use of a broad family of 5-imino-1,2,4-thiadiazoles as potential new drugs for the treatment of diseases in which PDE7 inhibition is important, specially inflammatory diseases, autoimmune and neurodegenerative disorders. On the other hand, compounds of the 5-imino-1,2,4-thiadiazole family are here described, as well as their synthetic procedures, and they may have great application as drug or drug candidates.
    Type: Application
    Filed: October 4, 2010
    Publication date: September 6, 2012
    Applicant: CONSEJO SUPERIOR DE INVESTIGACIONES CIENTIFACAS ( CSIC)
    Inventors: Ana Martínez Gil, Carmen Gil Ayuso-Gontan, Valle Palomo Ruiz, Daniel Perez Fernandez, Concepción Perez Martín, Ana María Perez Castillo, María Isabel Loza Garcia, María Isabe Cadavid Torres, José Brea Floriani
  • Patent number: 8252782
    Abstract: The invention relates to compounds of formula (I): wherein R1, R2, R3, R4, R5, and R6 as defined herein. The invention also relates to pharmaceutical compositions and methods of treating bacterial infections using compounds of formula (I).
    Type: Grant
    Filed: December 18, 2009
    Date of Patent: August 28, 2012
    Assignee: Pfizer Inc.
    Inventors: Steven Joseph Brickner, Mark Edward Flanagan, Manjinder Singh Lall
  • Publication number: 20120165339
    Abstract: A cyclopropane derivative represented by the following formula (I) or a pharmaceutically acceptable salt thereof has orexin receptor inhibitory action, and thus, is extremely useful as an agent for preventing or treating sleep disorder or dyssomnia caused by orexin, including insomnia as a typical example: wherein A1, A2 and A3 each independently represent an aryl group, a heterocyclyl group or the like, R1, R2 and R3 each independently represent a hydrogen atom, a C1-6 alkyl group or the like, X represents an oxygen atom or the like, and L represents a bond or the like.
    Type: Application
    Filed: December 20, 2011
    Publication date: June 28, 2012
    Applicant: EISAI R&D MANAGEMENT CO., LTD.
    Inventors: Taro Terauchi, Ayumi Takemura, Yuji Kazuta, Fumihiro Ozaki, Takashi Doko, Yu Yoshida, Toshiaki Tanaka, Keiichi Sorimachi, Yoshimitsu Naoe, Carsten Beuckmann
  • Publication number: 20120149679
    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: February 20, 2012
    Publication date: June 14, 2012
    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: 20120142666
    Abstract: Compounds of the formula (I), (II) and (III) 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.
    Type: Application
    Filed: June 8, 2010
    Publication date: June 7, 2012
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Eugene Richard Hickey, Doris Riether, David Smith Thomson, Lifen Wu, Renee M. Zindell
  • Publication number: 20120142700
    Abstract: The present invention relates to heterocyclic compounds of formula (I) which have microbiocidal activity, in particular fungicidal activity, as well as methods of using the compounds of formula (I) to control microbes.
    Type: Application
    Filed: August 5, 2010
    Publication date: June 7, 2012
    Applicant: SYNGENTA CROP PROTECTION, LLC
    Inventors: Sarah Sulzer-Mosse, Clemens Lamberth, Mathias Stephan Respondex, Laura Quaranta
  • Patent number: 8168567
    Abstract: The present invention relates to thiadiazolyloxyphenylamidines of the general formula (I), to a process for the preparation thereof, to the use of the amidines according to the invention in combating undesirable microorganisms and to a composition for this purpose comprising the thiadiazolyloxyphenylamidines according to the invention. The invention furthermore relates to a method for combating undesirable microorganisms by application of the compounds according to the invention to the microorganisms and/or to the habitat thereof.
    Type: Grant
    Filed: April 8, 2008
    Date of Patent: May 1, 2012
    Assignee: Bayer Cropscience AG
    Inventors: Klaus Kunz, Ralf Dunkel, Jörg Nico Greul, Oliver Guth, Hartmann Benoit, Kerstin Ilg, Wahed Ahmed Moradi, Thomas Seitz, Ronald Ebbert, Peter Dahmen, Arnd Voerste, Ulrike Wachendorff-Neumann, Eva-Maria Franken, Olga Malsam, Klaus Tietjen
  • Publication number: 20120101136
    Abstract: 5-membered heteroaryl derivatives of formula (I) or salts thereof, processes for their preparation, pharmaceutical compositions containing them and their uses in the treatment of various disorders mediated by S1P1 receptors are disclosed.
    Type: Application
    Filed: June 24, 2010
    Publication date: April 26, 2012
    Inventors: Guanghui Deng, Xichen Lin, Feng Ren, Jia-Ning Xiang
  • Publication number: 20120101134
    Abstract: 5-membered heteroaryl derivatives of formula (I) or salts thereof, processes for their preparation, pharmaceutical compositions containing them and their uses in the treatment of various disorders mediated by S1P1 receptors are disclosed.
    Type: Application
    Filed: June 24, 2010
    Publication date: April 26, 2012
    Applicant: GLAXO GROUP LIMITED
    Inventors: Guanghui Deng, Xichen Lin, Qinghua Meng, Feng Ren, Jia-Ning Xiang, Heng Xu, Haibo Zhang, Baowei Zhao
  • Publication number: 20120101137
    Abstract: The object of the present invention is to provide a compound having a glucokinase-activating effect. A pharmaceutical composition comprising a compound represented by the general formula (I) or a pharmaceutically acceptable salt thereof as an active ingredient: wherein X means a nitrogen atom or CR6, wherein R6 means a hydrogen atom or a halogen atom; R1 means a hydrogen atom, a C1-C6 alkyl group, a C1-C6 alkoxy group or a C1-C6 alkylthio group; R2 means a hydrogen atom or a fluorine atom; R3 means a hydrogen atom or a C1-C6 alkyl group; and one of R4 and R5 means a hydrogen atom or a C1-C6 alkyl group, and the other means a C1-C6 alkylenecarboxylic acid, a C1-C6 alkylsulfonyl group, a C1-C6 alkylcarbonyl group, or CONH2.
    Type: Application
    Filed: June 26, 2010
    Publication date: April 26, 2012
    Applicant: SANWA KAGAKU KENKYUSHO CO., LTD.
    Inventors: Tokuyuki Yamashita, Kaori Chikamatsu, Naoki Takahashi, Hisakazu Iwai, Masakazu Kogami, Masao Sakairi, Nobuhide Watanabe, Hiroki Fujieda, Daisuke Kataoka, Mitsuhiro Makino, Noriyasu Kato, Toshiyuki Miyazawa, Kazushige Nagai, Nobuyoshi Kasugai, Hiroyo Kataoka, Naoki Hiramatsu, Nobuaki Tsuruta, Yurie Yamada, Mika Miyoshi, Sei Murakami, Izumi Goto, Tohru Izuchi, Kimie Suzuki, Satoko Harada, Martin Lang, Markus Hans-Juergen Seifert, Kristina Kaarina Wolf
  • Patent number: 8148380
    Abstract: The present invention provides novel amide and sulfonamide substituted heterocyclic urea compounds having useful antibacterial activity. Use of these compounds as pharmaceutical compositions and method of their production are also provided.
    Type: Grant
    Filed: July 23, 2008
    Date of Patent: April 3, 2012
    Assignee: Crestone, Inc.
    Inventors: Joseph Guiles, Thale Jarvis, Sarah Strong, Xicheng Sun, Jian Qiu, John C. Rohloff
  • Publication number: 20120071663
    Abstract: The present invention relates to various processes for the preparation of N?-(4-{[3-(4-chloro-benzyl)-1,2,4-thiadiazol-5-yl]oxy}-2,5-dimethylphenyl)-N-ethyl-N-methylimidoformamide.
    Type: Application
    Filed: August 10, 2011
    Publication date: March 22, 2012
    Applicant: Bayer CropScience AG
    Inventors: Frank VOLZ, Thomas Himmler, Klaus Kunz, Jörg Greul, Ulrich Heinemann, Thomas Seitz, Pierre Cristau, Oswald Ort
  • Publication number: 20120064181
    Abstract: The subject invention relates to novel P2X3 receptor antagonists that play a critical role in treating disease states associated with pain, in particular peripheral pain, inflammatory pain, or tissue injury pain that can be treated using a P2X3 receptor subunit modulator.
    Type: Application
    Filed: March 15, 2010
    Publication date: March 15, 2012
    Inventors: Christopher S. Burgey, Zhengwu J. Deng, Diem Nguyen, Daniel V. Paone, Craig M. Potteiger, Shaun R. Stauffer, Carolyn Segerdell, Ashley Nomland, John J. Lim
  • Publication number: 20120046273
    Abstract: Muscarinic agonists, which are useful for stimulating muscarinic receptors and treating cognitive disorders, are provided. Methods of synthesizing such agonists also are provided. Also provided are compositions for enhancing cognitive function in subjects such as humans, the compositions comprising a muscarinic agonist or a pharmaceutically suitable form thereof. Also provided are methods of treating animals such as humans by administering such compositions.
    Type: Application
    Filed: March 5, 2010
    Publication date: February 23, 2012
    Applicant: MITHRIDION, INC.
    Inventors: Trevor M. Twose, Brent D. Abraham, Richard R. Copp, James G. Farnham, Seth A. Hanson, Michael L. Hendrickson, Jeffrey C. Ockuly, Melinda L. Verdone
  • Patent number: 8110577
    Abstract: The present invention provides histone deacetylase inhibitors of general formula (I), a process for the preparation of such compounds and uses of the compounds in medicine, especially in the treatment of cancers and the inhibition of histone deacetylase activity.
    Type: Grant
    Filed: October 19, 2007
    Date of Patent: February 7, 2012
    Assignee: Queen Mary & Westfield College
    Inventors: Simon Peter Joel, Charles Michael Marson
  • Publication number: 20120015988
    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.
    Type: Application
    Filed: May 4, 2009
    Publication date: January 19, 2012
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Eugene Richard Hickey, Doris Riether, David Smith Thomson, Renee M. Zindell, Patricia Amouzegh, Monika Ermann, Christopher Francis Palmer, Mark Whittaker
  • Publication number: 20120015941
    Abstract: The present invention provides novel amide and sulfonamide substituted heterocyclic urea compounds having useful antibacterial activity. Use of these compounds as pharmaceutical compositions and method of their production are also provided.
    Type: Application
    Filed: July 23, 2008
    Publication date: January 19, 2012
    Applicant: CRESTONE, INC.
    Inventors: Joseph Guiles, Thale Jarvis, Sarah Strong, Xicheng Sun, Jian Qiu, John C. Rohloff
  • Publication number: 20110319379
    Abstract: The present invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof wherein R1, R4, R6, X, Y and Z are as defined herein. The compounds of Formula (I) have been found to act as glucokinase activators. Consequently, the compounds of Formula (I) and the pharmaceutical compositions thereof are useful for the treatment of diseases, disorders, or conditions mediated by glucokinase.
    Type: Application
    Filed: March 4, 2010
    Publication date: December 29, 2011
    Inventors: Jeffrey W. Corbett, Angel Guzman-Perez, Jeffrey A. Pfefferkorn, Meihua Tu
  • Publication number: 20110301150
    Abstract: Provided are a substituted azole derivative and pharmaceutically acceptable salts thereof, a pharmaceutical composition including an effective amount of the derivative, and a method for treating Parkinson's disease in a mammal including administering an effective amount of the compound to the mammal. The azole derivative of the following Formula (I) and pharmaceutically useful salts thereof have an efficacy against Parkinson's disease from inhibitory effects of the activity of MAO-B.
    Type: Application
    Filed: February 25, 2010
    Publication date: December 8, 2011
    Inventors: Cheol-Hyoung Park, Hye-Kyung Min, Mi-Jung Lim, Ji-Won Lee, Jin-Yong Chung, Choon-Ho Ryu, Yeo-Jin Yoon, Mi-Kyung Ji, Joo-Young Park
  • Patent number: 8071631
    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: August 16, 2007
    Date of Patent: December 6, 2011
    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: 20110269738
    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: Application
    Filed: April 28, 2011
    Publication date: November 3, 2011
    Applicant: Glaxo Group Limited
    Inventors: Guanghui Deng, Xichen Lin, Feng Ren, Baowei Zhao
  • Publication number: 20110237589
    Abstract: The present invention relates to guanidine compounds of the general formula I corresponding enantiomeric, diastereomeric and/or tautomeric forms thereof as well as pharmaceutically acceptable salts thereof. The present compound further relates to the use of guanidine compounds as binding partners for 5-HT5 receptors for the treatment of diseases which are modulated by a 5-HT5 receptor activity, in particular for the treatment of neurodegenerative and neuropsychiatric disorders as well as the associated signs, symptoms and dysfunctions.
    Type: Application
    Filed: February 4, 2011
    Publication date: September 29, 2011
    Inventors: Astrid Netz, Wilhelm Amberg, Udo Lange, Michael Ochse, Charles W. Hutchins, Francisco-Xavier Garcia-Ladona, Wolfgang Wernet, Andreas Kling, Andrea Hager-Wernet
  • Publication number: 20110230477
    Abstract: The present invention is directed to novel compounds of formula (I) and their use in treating metabolic diseases.
    Type: Application
    Filed: December 7, 2009
    Publication date: September 22, 2011
    Applicant: Euroscreen S.A.
    Inventors: Hamid Hoveyda, Cyrille Evangelos Brantis, Guillaume Dutheuil, Ludivine Zoute, Didier Schils, Jerome Bernard
  • Publication number: 20110224259
    Abstract: The invention relates to novel heterocyclic derivatives as inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5). QC catalyzes the intramolecular cyclization of N-terminal glutamine residues into pyroglutamic acid (5-oxo-prolyl, pGlu*) under liberation of ammonia and the intramolecular cyclization of N-terminal glutamate residues into pyroglutamic acid under liberation of water.
    Type: Application
    Filed: March 3, 2011
    Publication date: September 15, 2011
    Applicant: PROBIODRUG AG
    Inventors: Ulrich HEISER, Daniel RAMSBECK, Torsten HOFFMANN, Livia BOEHME, Hans-Ulrich DEMUTH
  • Publication number: 20110224202
    Abstract: Compounds that inhibit PDE10 are disclosed that have utility in the treatment of a variety of conditions, including (but not limited to) psychotic, anxiety, movement disorders and/or neurological disorders such as Parkinson's disease, Huntington's disease, Alzheimer's disease, encephalitis, phobias, epilepsy, aphasia, Bell's palsy, cerebral palsy, sleep disorders, pain, Tourette's syndrome, schizophrenia, delusional disorders, drug-induced psychosis and panic and obsessive-compulsive disorders. Pharmaceutically acceptable salts, stereoisomers, solvates and prodrugs of the compounds are also provided. Also disclosed are compositions containing a compound in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for inhibiting PDE10 in a warm-blooded animal in need of the same.
    Type: Application
    Filed: March 10, 2011
    Publication date: September 15, 2011
    Applicant: Omeros Corporation
    Inventors: Neil S. Cutshall, Jennifer Lynn Gage, Thomas Neil Wheeler, Thomas L. Little
  • Publication number: 20110207935
    Abstract: The present invention provides compounds useful as agents for the prevention or treatment of a disease associated with abnormal plasma uric acid level and the like. The present invention relates to fused ring derivatives represented by the following formula (I) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of plasma uric acid level, prodrugs thereof, salts thereof or the like. In the formula (I), X1 and X2 represent CH or N; ring U represents aryl or heteroaryl; m represents integral number from 0 to 2; n represents integral number from 0 to 3; R1 represents a hydroxy group, amino or C1-6 alkyl; R2 represents C1-6 alkyl, C1-6 alkoxy C1-6 alkyl or the like.
    Type: Application
    Filed: October 14, 2009
    Publication date: August 25, 2011
    Applicant: KISSEI PHARMACEUTICAL CO., LTD.
    Inventors: Kazuo Shimizu, Masato Iizuka, Hideki Fujikura, Yasushi Takigawa, Masahiro Hiratochi
  • Patent number: 8003675
    Abstract: A 3,4-dihalogenoisothiazole derivative represented by the general formula [I] (wherein R1 is a halogen atom; A is an oxygen atom or a sulfur atom; and R is a C1-C6 alkyl group, a C2-C5 alkenyl group, a C2-C5 alkynyl group, a C3-C6 cycloalkyl group, a phenyl group or a 5- to 10-membered heterocyclic group containing at least one of oxygen atom, sulfur atom and nitrogen atom), or a salt thereof.
    Type: Grant
    Filed: July 6, 2007
    Date of Patent: August 23, 2011
    Assignees: Kumiai Chemical Industry Co., Ltd., Ihara Chemical Industry Co., Ltd.
    Inventors: Toshihiro Nagata, Atsushi Kogure, Isao Kaneko, Norihisa Yonekura, Ryo Hanai
  • Publication number: 20110200557
    Abstract: The present disclosure relates to 2-amidothiadiazole derivatives of formula (I) as well as pharmaceutical compositions comprising them, and their use in therapy as agonists of the S1P1 receptors.
    Type: Application
    Filed: October 13, 2009
    Publication date: August 18, 2011
    Inventors: Pedro Manuel Grima Poveda, Nuria Aguilar Izquierdo, Marta Mir Cepeda, Manuel Lopez Martinez
  • Publication number: 20110178140
    Abstract: A novel sulfur containing heteroaryl-pyrazole compound of formula (I) or a pharmaceutically acceptable salt thereof is effective as a cannabinoid CB1 receptor inverse agonist or antagonist, which is useful for preventing or treating obesity and obesity-related metabolic disorders. The prevention also provide a method for preparing same, a pharmaceutical composition containing same, and a method for preventing or treating obesity and obesity-related metabolic disorders.
    Type: Application
    Filed: September 25, 2008
    Publication date: July 21, 2011
    Applicant: GREEN CROSS CORPORATION
    Inventors: Jinhwa Lee, Hee Jeong Seo, Min-Ah Kim, Jeongmin Kim, Sung-Han Lee, Myung Eun Jung, Mi-Soon Kim
  • Publication number: 20110172236
    Abstract: A series of substituted aryl sulfone derivatives represented by Formula I, or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, calcium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, urinary incontinence, itchiness, allergic dermatitis, epilepsy, diabetic neuropathy, irritable bowel syndrome, depression, anxiety, multiple sclerosis, sleep disorder, bipolar disorder and stroke, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds.
    Type: Application
    Filed: September 21, 2009
    Publication date: July 14, 2011
    Inventors: Prasun K. Chakravarty, Joseph L. Duffy, Pengcheng Patric Shao
  • Publication number: 20110160211
    Abstract: A compound having a hypoglycemic effect is provided. The compound and a pharmaceutically acceptable salt thereof are useful for the treatment or prevention of diabetes, obesity, and the like. The compound is represented by the general formula (1): (wherein R1 and R2 are each independently a hydrogen atom, a halogen atom, an amino group, a hydroxyl group, a hydroxyamino group, a nitro group, a cyano group, a sulfamoyl group, a C1 to C6 alkyl group, a C1 to C6 alkoxy group, a C1 to C6 alkylsulfanyl group, a C1 to C6 alkylsulfinyl group, a C1 to C6 alkylsulfonyl group, or a C1 to C6 alkoxy-C1 to C6 alkylsulfonyl group, and A is a substituted or unsubstituted heteroaryl group).
    Type: Application
    Filed: April 27, 2009
    Publication date: June 30, 2011
    Inventors: Yasumichi Fukuda, Yoshikazu Asahina, Masanori Takadoi, Masanori Yamamoto
  • Patent number: 7968157
    Abstract: A discotic nematic material comprising a compound of R1—H1—Ar—H2—R wherein Ar represents a substituted or unsubstituted aromatic hydrocarbon ring; H1 and H2 represent an aromatic hetero ring; and R1 and R2 represent a substituent having from 1 to 30 carbon atoms. The discotic nematic material contains a discotic liquid-crystal compound having a smaller number of side branches and capable of expressing an ND phase.
    Type: Grant
    Filed: February 6, 2007
    Date of Patent: June 28, 2011
    Assignee: Fujifilm Corporation
    Inventor: Makoto Takahashi
  • Publication number: 20110152080
    Abstract: The present invention relates to thiadiazolyloxyphenylamidines of the general formula (I), to a process for the preparation thereof, to the use of the amidines according to the invention in combating undesirable microorganisms and to a composition for this purpose comprising the thiadiazolyloxyphenylamidines according to the invention. The invention furthermore relates to a method for combating undesirable microorganisms by application of the compounds according to the invention to the microorganisms and/or to the habitat thereof.
    Type: Application
    Filed: June 19, 2009
    Publication date: June 23, 2011
    Applicant: Bayer Cropscience AG
    Inventors: Pierre Cristau, Joerg Nico Greul, Ulrich Heinemann, Klaus Kunz, Oswald Ort, Thomas Seitz, Arnd Voerste, Peter Dahmen, Ulrike Wachendorff-Neumann, Klaus-Guenther Tietjen, Hiroyuki Hadano
  • Patent number: 7960556
    Abstract: The invention provides novel 1,2,4-thiadiazole derivatives useful for preventing or treating an ?-synucleopathy such as Parkinson's disease, as well as pharmaceutical compositions including them as biologically active ingredients, and methods for manufacturing them.
    Type: Grant
    Filed: November 22, 2007
    Date of Patent: June 14, 2011
    Assignee: NV reMYND
    Inventors: Gerard Griffioen, Stefaan Wera, Hein Roger Duhamel, Ellen Gommé, Nele Van Damme
  • Publication number: 20110136869
    Abstract: Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.
    Type: Application
    Filed: June 1, 2010
    Publication date: June 9, 2011
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Alessandra Bartolozzi, Eugene Richard Hickey, Doris Riether, Lifen Wu, Renee M. Zindell, Nigel James Blumire, Monika Ermann, Edward Thomas Glenn, Someina Khor, Przemyslaw Zawadzki