The Five-membered Hetero Ring Consists Of Chalcogen, Plural Nitrogens, And Carbon Patents (Class 548/125)
  • Patent number: 11014895
    Abstract: A heterocyclic urea compound, and specifically discloses an indoleamine-2,3-dioxygenase inhibitor of a heterocyclic urea compound, which solves the problems of weak curative effect and larger toxic and side effects of existing immunological therapy drugs. The invention further provides a preparation method for an indoleamine-2,3-dioxygenase inhibitor of a heterocyclic urea compound, and an application of the indoleamine-2,3-dioxygenase inhibitor of a heterocyclic urea compound or a pharmaceutically acceptable salt thereof in preparing drugs for treating or preventing tumors.
    Type: Grant
    Filed: January 1, 2018
    Date of Patent: May 25, 2021
    Assignee: CHINA PHARMACEUTICAL UNIVERSITY
    Inventors: Sheng Jiang, Zhengchao Tu, Haiping Hao, Hequan Yao, Yatao Qiu, Yiwu Yao, Dong Chen
  • Patent number: 10006078
    Abstract: Use of phospho-Akt as a biomarker for predicting the response, such as resistance, to a compound, wherein phospho-Akt is Akt that has been phosphorylated on one or more residues, with the proviso that for Akt1, Akt2, and Akt3 the designation phospho-Akt is used to indicate phosphorylation at a site other than T308, T309 or T305 respectively, wherein the compound is a compound of general formula (I).
    Type: Grant
    Filed: March 28, 2012
    Date of Patent: June 26, 2018
    Assignee: BASILEA PHARMACEUTICA AG
    Inventors: Heidi Alexandra Lane, Felix Bachmann
  • Patent number: 9732055
    Abstract: The present invention relates to the composition and methods of use of Stat3 pathway inhibitors or cancer stem cell inhibitors in combination treatment of cancer.
    Type: Grant
    Filed: September 10, 2008
    Date of Patent: August 15, 2017
    Assignee: Boston Biomedical, Inc.
    Inventors: Chiang Jia Li, Keith Mikule, Youzhi Li
  • Patent number: 9366682
    Abstract: Use of stathmin as a biomarker for predicting the response, such as resistance, to a compound, wherein the compound is a furazanobenzimidazole compound of general formula (I).
    Type: Grant
    Filed: January 19, 2012
    Date of Patent: June 14, 2016
    Assignee: BASILEA PHARMACEUTICA AG
    Inventors: Heidi Alexandra Lane, Felix Bachmann
  • Patent number: 9061999
    Abstract: The present invention relates to compound (I) for use as an agent for preventing, inhibiting or treating AIDS, wherein X is CR0 or N; R0, R1, R2, R3, R4, R7 and R8 independently represent a hydrogen atom, a halogen atom or a group chosen among a (C1-C5)alkyl group, a (C3-C6)cycloalkyl group, a (C1-C5)fluoroalkyl group, a (C1-C5)alkoxy group, a (C1-C5)fluoroalkoxy group, a —CN group, a —COORa group, a —NO2 group, a —NRaRb group, a —NRa—SO2—NRaRb group, a —NRa—SO2—Ra group, a —NRa—C(?O)—Ra group, a —NRa—C(?O)—NRaRb group, a —SO2—NRaRb group, a —SO3H group, a —OH group, a —O—SO2—ORc group, a —O—P(?O)—(ORc)(ORd) group, a —O—CH2—COORc group and can further be a group chosen among: R5 represents a hydrogen atom, a (C1-C5)alkyl group or a (C3-C6)cycloalkyl group; R10 is a hydrogen atom or a chlorine atom, and R11 is a hydrogen atom or a (C1-C4)alkyl group or anyone of its pharmaceutically acceptable salts.
    Type: Grant
    Filed: December 13, 2011
    Date of Patent: June 23, 2015
    Assignees: ABIVAX, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE, INSTITUT CURIE, UNIVERSITE MONTPELLIER 2
    Inventors: Jamal Tazi, Florence Mahuteau, Romain Najman, Didier Scherrer, Noëlie Campos, Aude Garcel
  • Patent number: 9040498
    Abstract: The present invention relates to novel 1,2,3-triazolyl purine derivatives. The invention also relates to using the derivatives to treat cancer and various viral infections.
    Type: Grant
    Filed: July 8, 2013
    Date of Patent: May 26, 2015
    Assignee: Research Foundation of the City University of New York
    Inventor: Mahesh K. Lakshman
  • Publication number: 20150133442
    Abstract: The invention features compositions and methods for inhibiting the Pin1 protein, and the treatment of disorders characterized by elevated Pin1 levels.
    Type: Application
    Filed: June 7, 2013
    Publication date: May 14, 2015
    Inventors: Kun Ping Lu, Matthew Brian Boxer, Mindy Irene Emily Davis, Rajan Pragani, Min Shen, Anton Momtchilov Simeonov, Shuo Wei, Xiao Zhen Zhou
  • Publication number: 20150133674
    Abstract: The present application is directed to processes and intermediates for making 4-({2-[(aminosulfonyl)amino]ethyl}amino)-N-(3-bromo-4-fluorophenyl)-N?-hydroxy-1,2,5-oxadiazole-3-carboximidamide, which is an inhibitor of indoleamine 2,3-dioxygenase, useful in the treatment of cancer and other disorders.
    Type: Application
    Filed: November 7, 2014
    Publication date: May 14, 2015
    Applicant: INCYTE CORPORATION
    Inventors: Ming Tao, William Frietze, David J. Meloni, Lingkai Weng, Jiacheng Zhou, Yongchun Pan
  • Patent number: 8993605
    Abstract: The present invention is directed to 1,2,5-oxadiazole derivatives, and compositions of the same, which are inhibitors of indoleamine 2,3-dioxygenase and are useful in the treatment of cancer and other disorders, and to the processes and intermediates for making such 1,2,5-oxadiazole derivatives.
    Type: Grant
    Filed: July 2, 2014
    Date of Patent: March 31, 2015
    Assignee: Incyte Corporation
    Inventors: Andrew P. Combs, Eddy W. Yue, Richard B. Sparks, Wenyu Zhu
  • Publication number: 20150076418
    Abstract: The invention relates to novel conjugated polymers comprising in their backbone one or more divalent donor units, like for example benzo[1,2-b:4,5-b?]dithiophene-2,6-diyl (BDT), that are linked on both sides to an acceptor unit, to methods of preparing the polymers and educts or intermediates used in such preparation, to polymer blends, mixtures and formulations containing the polymers, to the use of the polymers, polymer blends, mixtures and formulations as semiconductors organic electronic (OE) devices, especially in organic photovoltaic (OPV) devices and organic photodetectors (OPD), and to OE, OPV and OPD devices comprising these polymers, polymer blends, mixtures or formulations.
    Type: Application
    Filed: February 15, 2013
    Publication date: March 19, 2015
    Applicant: MERCK PATENT GMBH
    Inventors: Nicolas Blouin, Amy Phillips, Lana Nanson, Steven Tierney, Toby Cull, Priti Tiwana, Stephane Berney, Miguel Carrasco-Orozco, Frank Egon Meyer
  • Publication number: 20150051404
    Abstract: Compositions and methods are for inducing, promoting or otherwise facilitating pain relief. More particularly, sub-normovasodilatory doses of nitric oxide donors are used in the therapeutic management of vertebrate animals including humans, for the prevention or alleviation of pain, especially neuropathic pain. In some applications of the method, nitric oxide donors can be administered by any suitable route so as to provide concentrations of NO that are about ½ to 10?15 times those known to induce vasodilation in normal circulations.
    Type: Application
    Filed: August 22, 2014
    Publication date: February 19, 2015
    Inventor: MAREE THERESE SMITH
  • Patent number: 8957096
    Abstract: What is described are oxime ether-substituted benzoylamides of the general formula (I) as herbicides. In this formula (I), R, Y and Y are radicals such as hydrogen, organic radicals such as alkyl, and other radicals such as halogen. Q is a tetrazolyl, triazolyl or oxadiazolyl radical.
    Type: Grant
    Filed: October 29, 2012
    Date of Patent: February 17, 2015
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Andreas Van Almsick, Hartmut Ahrens, Hansjörg Dietrich, Isolde Häuser-Hahn, Ines Heinemann, Elmar Gatzweiler, Christopher Rosinger
  • Patent number: 8946271
    Abstract: Water soluble compounds having a furoxan structure which are capable of inhibiting metabolic pathways involved in the development of the tumours are provided. The use of such compounds as a medicament in the therapy of the tumours and as an adjuvant in the immunotherapy protocols against neoplasms is also described.
    Type: Grant
    Filed: February 23, 2011
    Date of Patent: February 3, 2015
    Assignees: Humanitas Mirasole S.p.A., Istituto Oncologico Veneto IRCCS
    Inventors: Antonella Viola, Enzo Bronte, Marco Crosetti, Loretta Lazzarato, Roberta Fruttero, Alberto Gasco
  • Publication number: 20150018209
    Abstract: The invention relates to sulfin- and sulfonimidoylbenzamides of general formula (S) used as herbicides. In said formula (I), R, R?, R?, X, W and Z represent radicals such as hydrogen, organic radicals such as alkyl, and other radicals such as halogens. Q represents a tetrazolyl-, triazolyl or oxadiazolyl radicals.
    Type: Application
    Filed: February 18, 2013
    Publication date: January 15, 2015
    Inventors: Hartmut Ahrens, Ralf Braun, Simon Doerner-Rieping, Arnim Koehn, Stefan Lehr, Hansjoerg Dietrich, Dirk Schmutzler, Elmar Gatzweiler, Christopher HUGH Rosinger
  • Publication number: 20150018210
    Abstract: Sulfinylaminobenzamides of the general formula (I) as herbicides are described. In this formula (I), R, R?, R?, X, W and Z are radicals such as hydrogen, organic radicals such as alkyl, and other radicals such as halogen. Q is a tetrazolyl, triazolyl or oxadiazolyl radical.
    Type: Application
    Filed: February 18, 2013
    Publication date: January 15, 2015
    Inventors: Hartmut Ahrens, Ralf Braun, Arnim Koehn, Stefan Lehr, Hansjoerg Dietrich, Dirk Schmutzler, Elmar Gatzweiler, Christopher Hugh Rosinger
  • Publication number: 20140377292
    Abstract: The present invention is directed to modulators of indoleamine 2,3-dioxygenase (IDO), as well as compositions and pharmaceutical methods thereof.
    Type: Application
    Filed: September 5, 2014
    Publication date: December 25, 2014
    Applicant: Incyte Corporation
    Inventors: Andrew P. Combs, Eddy W. Yue
  • Publication number: 20140371068
    Abstract: N-(1,2,5-Oxadiazol-3-yl)-, N-(1,3,4-oxadiazol-2-yl)-, N-(tetrazol-5-yl)- or N-(triazol-5-yl)arylcarboxamides of the general formula (I) are described as herbicides. In this formula (I), R, V, X, Y and Z are radicals such as hydrogen, organic radicals such as alkyl, and other radicals such as halogen. Q is a tetrazolyl, triazolyl or oxadiazolyl radical. W is CY or N.
    Type: Application
    Filed: December 10, 2012
    Publication date: December 18, 2014
    Inventors: Armin Koehn, Stefan Lehr, Ralf Braun, Simon Doerner-Rieping, Hartmut Ahrens, Hansjoerg Dietrich, Isolde Haeuser-Hahn, Christopher Hugh Rosinger, Elmar Gatzweiler
  • Publication number: 20140323306
    Abstract: The present invention relates to substituted 1,2,5-oxadiazole compounds of the formula I and the N-oxides and salts thereof and to compositions comprising the same. The invention also relates to the use of the 1,2,5-oxadiazole compounds or of the compositions comprising such compounds for controlling unwanted vegetation. Furthermore, the invention relates to methods of applying such compounds. In formula I, the variables have the following meanings R is e.g. hydrogen, cyano, nitro, halogen, C1-C6-alkyl, C3-C7-cycloalkyl, C3-C7-cycloalkyl-C1-C4-alkyl, C1-C6-haloalkyl, C2-C6-alkenyl, C2-C6-haloalkenyl, C2-C6-alkynyl, C2-C6haloalkynyl, C1-C4-alkoxy-C1-C4-alkyl, C1-C4-haloalkoxy-C1-C4-alkyl, O—Ra, Z—S(O)n—Rb, Z—C(?O)—Rc, Z—C(?O)—ORd, Z—C(?O)NReRf, Z—NRgRh, Z-phenyl and Z-heterocyclyl etc; R1 is e.g.
    Type: Application
    Filed: November 13, 2012
    Publication date: October 30, 2014
    Applicant: BASF SE
    Inventors: Helmut Kraus, Matthias Witschel, Thomas Seitz, Trevor William Newton, Liliana Parra Rapado, Raphael Aponte, Klaus Kreuz, Klaus Grossmann, Jens Lerchl, Richard Roger Evans
  • Publication number: 20140315962
    Abstract: The present invention is directed to 1,2,5-oxadiazole derivatives, and compositions of the same, which are inhibitors of indoleamine 2,3-dioxygenase and are useful in the treatment of cancer and other disorders, and to the processes and intermediates for making such 1,2,5-oxadiazole derivatives.
    Type: Application
    Filed: July 2, 2014
    Publication date: October 23, 2014
    Applicant: INCYTE CORPORATION
    Inventors: Andrew P. Combs, Eddy W. Yue, Richard B. Sparks, Wenyu Zhu, Jiacheng Zhou, Qiyan Lin, Lingkai Weng, Tai-Yuen Yue, Pingli Liu
  • Publication number: 20140309116
    Abstract: The present invention relates to substituted 1,2,5-oxadiazole compounds of the formula (I) and the N-oxides and salts thereof and to compositions comprising the same. The invention also relates to the use of the 1,2,5-oxadiazole compounds or of the compositions comprising such compounds for controlling unwanted vegetation. Furthermore, the invention relates to methods of applying such compounds.
    Type: Application
    Filed: November 15, 2012
    Publication date: October 16, 2014
    Applicant: BASF SE
    Inventors: Helmut Kraus, Matthias Witschel, Thomas Seitz, Trevor William Newton, Liliana Parra Rapado, Raphael Aponte, Klaus Kreuz, Klaus Grossmann, Jens Lerchl, Richard Roger Evans
  • Publication number: 20140309112
    Abstract: What is described are oxime ether-substituted benzoylamides of the general formula (I) as herbicides. In this formula (I), R, Y and Y are radicals such as hydrogen, organic radicals such as alkyl, and other radicals such as halogen. Q is a tetrazolyl, triazolyl or oxadiazolyl radical.
    Type: Application
    Filed: October 29, 2012
    Publication date: October 16, 2014
    Inventors: Andreas Van Almsick, Hartmut Ahrens, Hansjörg Dietrich, Isolde Häuser-Hahn, Ines Heinemann, Elmar Gatzweiler, Christopher Rosinger
  • Patent number: 8859599
    Abstract: The present invention concerns compounds of general formula (I): Method of preparation and uses thereof.
    Type: Grant
    Filed: February 11, 2010
    Date of Patent: October 14, 2014
    Assignees: CNR—Consiglio Nazionale delle Ricerche, Istituto Scientifico Romagnolo per lo Studio e la Cura dei Tumori (I.R.S.T.) S.r.l.
    Inventors: Greta Varchi, Andrea Guerrini, Anna Tesei, Giovanni Brigliadori
  • Patent number: 8859596
    Abstract: Disclosed herein are cannabinoid receptor ligands of formula (I) wherein A1, A5, Rx, X4, and z are as defined in the specification. Compositions comprising such compounds, and methods for treating conditions and disorders using such compounds and compositions are also disclosed.
    Type: Grant
    Filed: September 16, 2009
    Date of Patent: October 14, 2014
    Assignee: AbbVie Inc.
    Inventors: William A. Carroll, Michael J. Dart, Jennifer M. Frost, Steven P. Latshaw, Teodozyj Kolasa, Tongmei Li, Sridhar Peddi, Bo Liu, Arturo Perez-Medrano, Meena Patel, Xueqing Wang, Derek W. Nelson
  • Publication number: 20140303171
    Abstract: Compounds of Formula I are disclosed: wherein A, R1, R2, R3, R4A, R4B, R5, R6 and R7 are defined herein. The compounds encompassed by Formula I include compounds which are 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: October 26, 2012
    Publication date: October 9, 2014
    Inventors: Michael John Boyd, Jean-Francois Chiasson, Sheldon Crane, André Giroux
  • Patent number: 8822511
    Abstract: The present invention is directed to 1,2,5-oxadiazole derivatives, and compositions of the same, which are inhibitors of indoleamine 2,3-dioxygenase and are useful in the treatment of cancer and other disorders, and to the processes and intermediates for making such 1,2,5-oxadiazole derivatives.
    Type: Grant
    Filed: September 20, 2013
    Date of Patent: September 2, 2014
    Assignee: Incyte Corporation
    Inventors: Andrew P. Combs, Eddy W. Yue, Richard B. Sparks, Wenyu Zhu
  • Patent number: 8822509
    Abstract: This invention discloses compositions and methods for inducing, promoting or otherwise facilitating pain relief. More particularly, the present invention discloses the use of sub-normovasodilatory doses of nitric oxide donors in the therapeutic management of vertebrate animals including humans, for the prevention or alleviation of pain, especially neuropathic pain. According to some embodiments of the present invention, nitric oxide donors are administered by any suitable route so as to provide concentrations of NO that are about ½ to 10?15 of those known to induce vasodilation in normal circulations.
    Type: Grant
    Filed: June 29, 2009
    Date of Patent: September 2, 2014
    Assignee: The University of Queensland
    Inventor: Maree Therese Smith
  • Publication number: 20140221316
    Abstract: This disclosure relates to novel compounds containing an H2S releasing moiety and a nitric oxide (NO) releasing moiety covalently linked with a core (e.g., a salicylic acid moiety) and the use of such compounds in treating inflammatory diseases, including cancers. Therapeutic potency of these compounds is significantly higher than NSAIDs containing a H2S-releasing moiety alone (HS-NSAIDs) and NSAID containing a NO-releasing moiety alone (NO-NSAIDs). The compounds, in addition, exhibit reduced side effect, e.g., reduced stomach ulcers, upon administration.
    Type: Application
    Filed: August 15, 2012
    Publication date: August 7, 2014
    Applicant: RESEARCH FOUNDATION OF THE CITY UNIVERSITY OF NEW YORK
    Inventors: Khosrow Kashfi, Ravinder Kodela
  • Patent number: 8796319
    Abstract: The present invention is directed to 1,2,5-oxadiazole derivatives, and compositions of the same, which are inhibitors of indoleamine 2,3-dioxygenase and are useful in the treatment of cancer and other disorders, and to the processes and intermediates for making such 1,2,5-oxadiazole derivatives.
    Type: Grant
    Filed: November 11, 2011
    Date of Patent: August 5, 2014
    Assignee: Incyte Corporation
    Inventors: Andrew P. Combs, Eddy W. Yue, Richard B. Sparks, Wenyu Zhu, Jiacheng Zhou, Qiyan Lin, Lingkai Weng, Tai-Yuen Yue, Pingli Liu
  • Patent number: 8772510
    Abstract: The present invention relates to compounds of formula (I) wherein R1, R2, R3, R5, W, X, X1, Y, Y1, Z and Z1 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit PDE10A and can be used in the treatment of CNS disorders such as schizophrenia, Alzheimer's disease, and Parkinson's disease.
    Type: Grant
    Filed: August 30, 2012
    Date of Patent: July 8, 2014
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Stephan Bachmann, Alexander Flohr, Katrin Groebke Zbinden, Matthias Koerner, Bernd Kuhn, Jens-Uwe Peters, Markus Rudolph
  • Patent number: 8716489
    Abstract: An object is to provide a novel material having a bipolar property. Another object is to provide an oxadiazole derivative having a wide band gap. Another object is to reduce power consumption of a light-emitting element, a light-emitting device, and an electronic device. The present invention provides an oxadiazole derivative represented by General Formula (1). In the formula, Ar1 represents a substituted or unsubstituted aryl group having 6 to 10 carbon atoms in a ring, A represents a substituted or unsubstituted phenylene group, R11 to R15 and R21 to R25 are independently any of hydrogen, an alkyl group having 1 to 4 carbon atoms, an aryl group having 6 to 10 carbon atoms in a ring, and a substituted or unsubstituted 9H-carbazol-9-yl group.
    Type: Grant
    Filed: August 29, 2012
    Date of Patent: May 6, 2014
    Assignee: Semiconductor Energy Laboratory Co., Ltd.
    Inventors: Hiroko Nomura, Sachiko Kawakami, Nobuharu Ohsawa, Satoshi Seo
  • Publication number: 20140121206
    Abstract: The present invention relates to spirocarbamate compounds of Formula (I) in which R1, (R2)Y, R3, R4, X and A have the meanings given in the specification. The invention further provides pharmaceutical compositions containing the compounds or pharmaceutically acceptable salts thereof and relates to their use of these compounds as TRPV4 antagonists in treating or preventing conditions associated with TRPV4 imbalance.
    Type: Application
    Filed: June 15, 2012
    Publication date: May 1, 2014
    Applicant: GlaxoSmithKliine, LLC
    Inventors: Carl Brooks, Mui Cheung, Hilary Schenck Eidam, Krista B. Goodman, Marlys Hammond, Mark A. Hilfiker, Tram H. Hoang, Jaclyn R. Patterson, Patrick Stoy, Guosen Ye
  • Publication number: 20140106969
    Abstract: N-(1,2,5-Oxadiazol-3-yl)-, N-(tetrazol-5-yl)- and N-(triazol-5-yl)bicycloarylcarboxamides of the general formula (I) are described as herbicides. In this formula (I), R3, R4 and R5 are each radicals such as hydrogen, organic radicals such as alkyl, and other radicals such as halogen. Q is a heterocycle. X and Y are each oxygen and sulfur.
    Type: Application
    Filed: March 12, 2012
    Publication date: April 17, 2014
    Applicant: BAYER INTELLECTUAL PROPERTY GmbH
    Inventors: Andreas Almsick, Hartmut Ahrens, Arnim Köhn, Simon Dörner-Rieping, Ralf Braun, Isolde Häuser-Hahn, Christopher Hugh Rosinger, Ines Heinemann, Elmar Gatzweiler
  • Patent number: 8697911
    Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1 and R2 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: June 29, 2011
    Date of Patent: April 15, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Brian Nicholas Cook, Jennifer A. Kowalski, Xiang Li, Daniel Richard Marshall, Sabine Schlyer, Robert Sibley, Lana Louise Smith-Keenan, Fariba Soleymanzadeh, Ronald John Sorcek, Erick Richard Roush Young, Yunlong Zhang
  • Patent number: 8691853
    Abstract: Dopamine reuptake inhibitors, and their analogs, are disclosed for treating and delaying the progression of autoimmune diseases.
    Type: Grant
    Filed: October 5, 2011
    Date of Patent: April 8, 2014
    Assignee: Caliper Life Sciences, Inc.
    Inventors: Hao Chen, Alexel Miagkov, Lisa Leary, Ming Liu, Qi Su
  • Patent number: 8673948
    Abstract: This invention relates to non-steroidal compounds that are modulators of androgen receptor, and also to the methods for the making and use of such compounds.
    Type: Grant
    Filed: August 19, 2011
    Date of Patent: March 18, 2014
    Assignee: GlaxoSmithKline, LLC
    Inventors: Philip Stewart Turnbull, Rodolfo Cadilla, Andrew Larkin, Huiquiang Zhou, Eugene L. Stewart, Katherine Stetson, Darryl Lynn McDougald, Amarjit Sab Randhawa, John A. Ray
  • Publication number: 20140066307
    Abstract: Use of N-(1,2,5-Oxadiazol-3-yl)benzamides of formula (I) or salts thereof for controlling unwanted plants in areas of transgenic crop plants being tolerant to HPPD inhibitor herbicides by containing one or more chimeric gene(s) comprising (I) a DNA sequence encoding hydroxyphenylpyruvate dioxygenase (HPPD) derived from a member of a group of organisms consisting of (a) Avena, (b) Pseudomonas, (c) Synechococcoideae, (d) Blepharismidae, (e) Rhodococcus, (f) Picrophilaceae, (g) Kordia, or (II) comprising one or more mutated DNA sequences of HPPD encoding genes of the before defined organisms.
    Type: Application
    Filed: March 21, 2012
    Publication date: March 6, 2014
    Applicant: Bayer Intellectual Property GmbH
    Inventors: Fabien Poree, Andreas Van Almsick, Arnim Köhn, Bernd Laber, Ruediger Hain
  • Patent number: 8618144
    Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of ?3-adrenoceptor.
    Type: Grant
    Filed: April 28, 2010
    Date of Patent: December 31, 2013
    Assignee: Merck Sharp & Dohme Corp
    Inventors: Peter Lin, Lehua Chang, Scott D. Edmondson
  • Patent number: 8604034
    Abstract: The present invention relates to compounds of formula (I) its salts, isomers or prodrugs thereof useful in the treatment of viral infections, in particular respiratory syncytial virus (RSV) infections. The present invention also relates to processes for preparing the compounds and intermediates used in their preparation.
    Type: Grant
    Filed: February 8, 2011
    Date of Patent: December 10, 2013
    Assignee: Biota Scientific Management Pty Ltd.
    Inventors: Jeffrey Peter Mitchell, Gary Pitt, Alistair George Draffan, Penelope Anne Mayes, Laura Andrau, Kelly Anderson
  • Publication number: 20130323271
    Abstract: In one aspect, the invention relates to compounds having the formula: where R1, R2, R3, R7, R8, Z, X, b, and c are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds are nitric oxide donors and have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.
    Type: Application
    Filed: May 30, 2013
    Publication date: December 5, 2013
    Inventors: Mathai Mammen, Adam D. Hughes
  • Patent number: 8592464
    Abstract: The present invention relates to nitric oxide furoxan derivative compounds which showed to be active in the treatment of tumors. In addition, they may be used as adjuvants in cancer immunotherapy.
    Type: Grant
    Filed: January 15, 2010
    Date of Patent: November 26, 2013
    Assignees: Humanitas Mirasole S.p.A., Istituto Oncologico Veneto IRCCS
    Inventors: Antonella Viola, Enzo Bronte, Marco Crosetti, Loretta Lazzarato, Roberta Fruttero, Alberto Gasco
  • Patent number: 8580799
    Abstract: The present invention relates to hydroximoyl-heterocycle derivatives of formula (I) wherein T represents a substituted or non-substituted heterocyclyl group, Q represents a carbo or heterocyclic group, A represent a carbo or heterocyclic group or a carbo or hetero-polycylic group, and L1 represents various linking groups, their process of preparation, intermediate compounds for their preparation, 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: December 8, 2009
    Date of Patent: November 12, 2013
    Assignee: Bayer Cropscience AG
    Inventors: Christian Beier, Jurgen Benting, David Bernier, Pierre-Yves Coqueron, Philippe Desbordes, Christophe Dubost, Stephanie Gary, Pierre Genix, Daniela Portz, Ulrike Wachendorff-Neumann
  • Patent number: 8563714
    Abstract: The present invention relates to bridged spiro[2.4]heptane derivatives of formula (I), wherein W, Y, Z, R1 and R2 are as defined in the description, their preparation and their use as pharmaceutically active compounds as ALX receptor and/or FPRL2 agonists for the treatment of inflammatory and obstructive airways diseases.
    Type: Grant
    Filed: May 17, 2010
    Date of Patent: October 22, 2013
    Assignee: Actelion Pharmaceuticals Ltd.
    Inventors: Daniel Bur, Olivier Corminboeuf, Sylvaine Cren, Corinna Grisostomi, Xavier Leroy, Sylvia Richard-Bildstein
  • Patent number: 8551426
    Abstract: Provided are an RNase activity inhibitory compound to effectively control the activity of the RNase promoting degradation of extracted RNAs and, in addition, a sample storage container including the same. The RNase activity inhibitory compound and the sample storage container according to the present invention may be effectively used to store RNAs during RNA extraction or the extracted RNAs.
    Type: Grant
    Filed: June 12, 2009
    Date of Patent: October 8, 2013
    Assignee: Bioneer Corporation
    Inventors: Jong Hoon Kim, Hwangseo Park, Han Oh Park
  • Patent number: 8546389
    Abstract: The present invention relates to viral polymerase inhibitors of formula (I), salts, N-oxides, solvates, hydrates, racemates, enantiomers or isomers thereof, processes for their preparation and their use in the treatment of Flaviviridae viral infections such as Hepatitis C virus (HCV) infections:
    Type: Grant
    Filed: October 20, 2011
    Date of Patent: October 1, 2013
    Assignee: Biota Scientific Management Pty Ltd.
    Inventors: Rosliana Halim, Michael Harding, Richard Hufton, Craig James Morton, Saba Jahangiri, Brett Raymond Pool, Tyrone Pieter Jeynes, Alistair George Draffan, Barbara Frey, Michael John Lilly
  • 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
  • Patent number: 8513290
    Abstract: Analogs of largazole are described herein. Methods of treating cancer and blood disorders using largazole and largazole analogs and pharmaceutical compositions comprising the same are additionally described herein. Methods for preparing largazole analogs are likewise described.
    Type: Grant
    Filed: June 7, 2012
    Date of Patent: August 20, 2013
    Assignees: Colorado State University Research Foundation, Dana-Farber Cancer Institute, Inc., University of Notre Dame du Lac
    Inventors: Robert M. Williams, James E. Bradner, Albert Bowers, Tenaya Newkirk, Olaf G. Wiest
  • 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
  • Publication number: 20130190340
    Abstract: Certain aspects of the invention relate to compounds, compositions and methods that are useful for treating or preventing a disease in a subject by enhancing the degradation of a protein. In other aspects, said compounds can be useful research tools for investigating protein degradation. In other aspects, said compounds are useful research tools for investigating protein function. In certain embodiments, the degraded protein is implicated in a disease or disorder whose pathology is related at least in part to the excessive expression of the protein or the expression of a mutant form of the protein.
    Type: Application
    Filed: June 30, 2011
    Publication date: July 25, 2013
    Applicant: Brandeis University
    Inventors: Lizbeth K. Hedstrom, Marcus Long, Deviprasad R. Gollapalli
  • Patent number: 8455657
    Abstract: A process is described for the preparation of 3-alkylsulfinylbenzoyl derivatives of the formula (IIIa) by reaction of 3-alkylsulfinylbenzoic acids of the formula (Ib) with compounds of the formula (II) in the presence of a chlorinating agent and a base. In the formulae specified above, Y is a radical such as pyrazolyl and cyclohexanedionyl. R1, R2 and R3 are radicals such as halogen, nitro, cyano and alkyl.
    Type: Grant
    Filed: December 22, 2011
    Date of Patent: June 4, 2013
    Assignee: Bayer Cropscience AG
    Inventors: Mark James Ford, Jan Peter Schmidt, Helmut Kohlhepp
  • Patent number: 8450351
    Abstract: The present invention is directed to N-hydroxyamidino compounds which are modulators of indoleamine 2,3-dioxygenase (IDO), as well as pharmaceutical compositions thereof and methods of use thereof relating to the treatment of cancer and other diseases.
    Type: Grant
    Filed: December 19, 2006
    Date of Patent: May 28, 2013
    Assignee: Incyte Corporation
    Inventors: Andrew P. Combs, Amy Takvorian, Wenyu Zhu, Richard B. Sparks